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Pharmaceutics

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  1. Pharmaceutics General

  2. Abbreviations • Cata  Downward. • Dis  Apart. • Infra  Below. • Ultra  Above. • Meso  Middle. • Retro  Backward. • Cephal  Head (cephalgia = headache) • Celi  Abdominal (celiotomy). • Colo  Large intestine (coloprotitis) colon + rectum. • Chole  Gall bladder (cholecystectomy = removal). • Card - Cor  Heart (pericardium = over the heart). • Cost  Ribs (intercostals) • Intra-articular  Parentral administration in the joint. • Intra-synovial  Parentral administration in the synovial fluid. • Intra-thecal  Parentral administration in the spinal cord. • a. c.  Before meals • p. c.  After meals • i. c.  Between meals • c. c.  With meals • H. S.  At bed time • M a n  In the morning • No Oct  At night • P.R.N  When necessary • S.O.S  When needed • B.I.D (or bd)  Twice daily • T.I.D (or tds)  Thrice daily • Q.I.D (or qds)  Four-times daily • Q.D (QA, OD, or qd)  Every day (once daily) • Q.O.D  Every other day • Q.H  Every hour • O. U  Both eyes • O. S  Left eye • O. D  Right eye • A. U  Both ears • A. S  Left ear • A. D  Right ear • BNF  Caustic solution / irritating vapor

  3. Abbreviations • ad or add  Add. • div  Divide. • d.t.d.  Give of such doses. • ft. or Fiat  Make. • M  Mix. • Solv.  Dissolve. • Q.S.  A sufficient quantity. • a.a. or aa  Of each. • s.s.  A half. • e. t.  and • Cum or c  With. • S.  Without. • Rep  Repeat. • Non-rep  Do not repeat. • Sat  Immediately. • Ut dict.(ud or emp)  Use as directed. • Cong. Or c  Gallon. • Octarious or o  Pint. • Sig.  Write, let it be marked. • Caps  Capsules • ung.  Ointment. • gtt.  Drops. • P.O  Per oral / by mouth Roman numbers: • X = 10 • L = 50 • C = 100

  4. Some Common Names of Disease • St. Vitus Disease  Chorea • Down’s Syndrome  Mongolism • Honsen’s Disease  Leprosy (caused by Mycobacterium lepra) • Shingles Disease  Herpes Zoster • Cooley’s Disease  Familial erythroplastic anemia • Grave’s Disease ‘Goiter’  Enlargement of thyroid gland  hyperthyroidism  exophthalmoses • Myxodema ‘Gull’s Disease’  Caused by $ secretion of the thyroid gland (hypothyroidism) • Paget’s Disease  Hyperparathyroidism • Hodgkin’s Disease  Enlargement of the lymph nodes • Acromegaly (after puberty)  #in pituitary gland secretions, ttt  bromocriptine • Klinefelter’s Syndrome  $ development of seminiferous tubules of testis. • Stein Leventhal Syndrome  Increased levels of androgens in ovaries • Cushing Syndrome  # cortisol levels secreted from adrenal cortex  moon face, buffalo hump & HT. • Addison’s Disease  Hypofunction of adrenal cortex. • Adam’s Stokes Disease  Affects the heart & causes sudden heart block • Bright’s Disease  Affects the kidney (glomerulonephritis). • Albright’s Disease  Fibrous dysplasia of bone & cartilages. • Mysthenia Gravis  Weakness of the muscles due to lack of acetylcholine (# cholinesterase). • Reynold's Disease  Cyanosis of fingers & toes. • Crohn’s Disease  Inflammation of layers of the intestinal tract  regional enteritis or ileitis & ulcerative colitis (due to infection/irritating food) • Menier’s Disease  Tinnitus, dizziness & deafness. • Herpes Simplex  Watery blisters on skin & mucous memb. (lips) • STY  Staphylococcal infection of one or more of the glands of Zeis or moll (p 263)

  5. Some Common Disease Terms • Blepharitis  Inflammation of the eye lid. • Gastritis  Inflammation of the stomach wall. • Glossitis  Inflammation of the tongue. • Stomatitis  Inflammation of the oral mucosa. • Cholecystitis  Inflammation of the gall bladder (usually due to stones) • Cholestasis  obstruction of bile flow due to ppt of bile pigment  calculi. There is # plasma bile acids (serum bilirubin). • Polyphagia  Excessive carving for food. • Dysphagia  Difficulty in swallowing. • Alopecia  Baldness. • Hirsutism  Abnormal hairiness (hair distribution). • Hives  Common name for urticaria. • Nystagmus  Rapid movement of the eye ball which may be: horizontal, vertical, rotatory or mixed. • Hypertrophy  Enlargement or over growth of an organ. • Atrophy  Diminishing of an organ. • Hyperhydrosis  Excessive sweating. • Hyperkinesia  Increased motor activity. • Hyperthesia  Excessive sensitivity to stimulation. • Anesthesia  Diminished sensitivity to stimulation. • Myalgia  Muscle pain. • Myositis  Inflammation of the voluntary (skeletal) muscles. • Spondylitis  Inflammation of the vertebrae. • Amyloidosis  Deposition of amyloid (complex protein) in various organs • Phlebitis  Inflammation of the vein. • Embolism  An obstruction in the vessel. • Stenosis  A constriction or narrowing of the blood vessel. • Tricuspid stenosis  Narrowing of veins. • Aneurism  A weakened, bulging portion of artery (circumscribed dilatation of artery due to BP  blood-containing sac) • Epistaxis  Bleeding from the nose. • Ascitis  Accumulation of serous fluids peritoneal cavity (treated by spironolactone in absence of renal insufficiency). • Oedema  Excessive accumulation of interstitial fluids. • Nephritis  Non-suprative inflammatory or degenerative kidney disease characterized by proteinuria & hematuria.

  6. Pyelonephritis  Inflammation of the kidney. • Emphysema  Airflow obstruction disease with distention of all air spaces distal to terminal bronchioles with alveolar destruction • Necrosis  Localized death of a part of the tissue surrounded by healthy tissue (death in mass) • Necrobiosis  Gradual degeneration in the depth of tissues. • Necrosin  A substance obtained from inflamed tissue, it induces inflammatory changes in normal tissue Side Effects of Certain Drugs • Methyl dopa / Ascorbic acid  Positive Coomb’s test. • Penicillins / Cephalosporins  Positive Coomb’s test. • Diazoxide (vasodilator)  Na+ retention. • Guanethidine  Inhibits ejaculation • Guanethidine & Hydralazine  Orthostatic hypotension. • Hydralazine in large doses  Systemic Lupus Erythmatosis (SLE). • Procainamide  Systemic Lupus Erythmatosis (SLE). • Prazocin (Minipress) (a blocker)  Postural hypotension (syncope) & Tachycardia • Sulfa-isoxazole / Succinamides  Steven’s Johnson’s Syndrome. • Isoniazide (INH)  Peripheral neuritis. • Chlorpromazine (phenothiazine)  extra-pyramidal side effects + occulo- cutaneous pigmentation • Xss Bromides (as hypnotics)  Acne-type rash on excessive use. • Morphine, Atropine, Al(OH)3  Constipation • Digitalis, Oral contracep., Mg(OH)2  Diarrhea • Phenylbutazone (NSAID)  Blood dyscrasis on excessive use. • Acetaminophen  Hepatic necrosis. • Agranulocytosis (Type II hypersensitivity mechanism): is a condition characterized by marked leucopenia & neutopenia. It occurs as a hypersensitivity reaction to many drugs: • Phenyl butazone – Thiouracil derivatives • Chloramphenicol – Sulfonamides • Trimethadione (petit mal) – Gold preparations • Chloropromazine (major tranquilizer) – Thiazide diuretics Some Tests • Cod liver oil  Rats. – Insulin  Rabbits. • Heparin & Protamine  Sheep. – Oxytocin  Chicken.

  7. What is chilblains: • It is a frost-bite due to extreme exposure to cold  freezing of the skin & superficial tissue which looks as if burnt (congestion/swelling)  may lead to gangrene • Bed sores are due to: a. Pressure atrophy • 1 T q.i.d. , P.C & HS means • One tablet four times daily after meals and at bed time. • How to minimize parallex when measuring liquids: • By looking straight directly through. • By looking at an angle of 45. • Long-term treatment with corticosteroids causes: • Cushing syndrome # cortisone • Addison’s syndrome $ cortisone • What is IDA: • It is the reference book for formulations • SLE is a side effect of: • Procainamide c. Hydralazine • Digitalis d. Methyl dopa • Emphesima is: • Permanent alveolar space destruction in the lungs.

  8. Poisoning • In accidental drug poisoning use: • Ipeca syrup to induce vomiting first. • Hence, activated charcoal to adsorb the remaining poison. • Do not give them together as the charcoal may adsorb the alkaloid of ipeca. • Cyanide, DDT, boric acid & FeSO4: are not adsorbed on activated charcoal. • Ipeca: is used as an emetic (15-30 mg/day in one dose) & expectorant (0.25-0.5 mg TID). It is used only in adults & is not recommended in children under 6 years. • Universal Antidote: is a mixture of: d Activated charcoal. d MgO d Tannic acid • Overdose treatment: • Amphetamines: these are bases. d Urine acidification to enhance excretion. d Barbiturates or chlorpromazine to control CNS stimulation. d Beta-blockers to control hypertension. • Barbiturates: these are acids. d Urine alkalanization to enhance excretion. d Forced diuresis & artificial kidney (hemodialysis). d IV dextran to control hypotension. d Artificial respiration. • Benzodiazepines (non-barbiturate hypnotics): are safe up to 50-100 X therapeutic dose. Antidote for benzodiazepines is flumezanil. Activated charcoal is used to $ absorption. • Narcotics: d 0.4 mg Naloxone IV. • Acetaminophen (paracetamol): N-acetyl p-aminophenol. d Treated with N-acetyl cystine given IV within the first 12 hours. d Charcoal reduces absorption. • Acetyl salicylic acid toxicity is characterized by: d Bleeding d Headache d Dimness of vision d Hyper-ventilation d Tinnitus d Mental confusion d Sweating d Thirst • Salicylates: are acids, thus treatment of toxicity involves: d Urine alkalanization to enhance excretion. d Gastric lavage with NaHCO3. d Haemodialysis in severe cases.

  9. Organo-phosphorus compounds poisoning: these are commonly found in insecticides / pesticides (e.g. diazians, dichlorons, parathion). They act as cholinesterase inhibitors (form very stable compound with acetylcholine esterase enzyme). Symptoms of poisoning include: d Salivation d Hypotension d Muscle twitches. d Diarrhea & vomiting d Abdominal spasm d Miosis d Increased sweating d Bronchospasms It is treated with: d Atropine injection to antagonize the muscarinic effects. d Pralidoxime (PAM) which forms a complex with phosphorus, preventing it from reaching the enzyme d Barbiturates to treat convulsions. d Blood transfusion. • Organic solvents toxicity: • Inhalation of # conc. of gasoline vapors in confined quarters  sudden death. • The CNS effects experienced by those engaging in drug abuse phenomenon of glue sniffing are related to the action of tolune. d Gasoline vapors, like other hydrocarbons, may sensitize the myocardium to catechol-amines leading to ventricular fibrillations, rapid CNS deprivation & respiratory failure. d Inhalation of kerosene vapors is less hazardous than is the ingestion of kerosene. • Methanol poisoning: methanol is converted by alcohol dehydrogenase to formaldehyde then formic acid demyelination of optic nerve  blindness.It is treated by giving ethanol. Also for ethylene glycol toxicity  ethanol • Treatment of hyperkalemia: there are 3 methods: • If there are ECG changes, Ca++ is given to counteract the effect of excess K+ on heart. • HCO3 or “glucose + insulin” can be used to rapidly shift K+ from the extracellular to the intracellular compartment. • If there are no ECG changes: Exchange resin (e.g. kayexolate) or dialysis can be used to remove excess K+ from the body. The most appropriate option is the administration of kayexolate enema (rectally) containing 50 gm in sorbitol solution. • Cyanide poisoning: is one of the most rapidly acting poisons. • It has very # affinity for the Fe3+ state, reacting directly with iron of cytochrome oxidase in the mitochondria, cellular respiration is thus inhibited & cytotoxic hypoxia results. • Diagnosis of cyanide poisoning may be facilitated by the characteristic odour of bitter almonds with which the physician should be familiar. • Cyanide poisoning is treated by Na dicobalt ededate, amyl nitrite inhalation (or Na nitrite IV injection), Na thiosulfate. This converts Hb to methemoglobin, which has greater affinity for cyanide thus releasing cytochrome oxidase.

  10. CO toxicity: CO has much higher affinity for Hb than O2 carboxy Hb (responsible for the cherry red cyanosis seen in CO toxicity); carboxy Hb is incapable of carrying O2 to tissues. • The toxic reactions resulting from exposure to CO are primarily the result of tissue hypoxia produced by the inability of blood to transport sufficient oxygen. • Anemic persons are more susceptible to CO poisoning than normal individuals. • Although the formation of carboxy Hb decreases the oxygen carrying capacity of blood it does not decrease the PO2 of arterial blood & as a result there is no stimulation of chemoreceptors. • Carboxy Hb is a compound that dissociates most rapidly in presence of O2 which displaces CO in the Hb molecule & converts carboxy Hb to Oxy Hb. Thus, CO toxicity can be treated through maintenance of respiration, removal from exposure source, blood transfusion, administration of 100% oxygen, or hyperbaric O2 when applicable. • Lead Poisoning: may be acute or chronic, yet acute poisoning is relatively infrequent. • Organic lead compounds are more likely to produce CNS symptoms, while aberrations in Hb synthesis are more apt to be associated with inorganic lead poisoning. • Exposure to lead produces unmistakable, progressive mental deterioration in children. • Pb toxicity can be treated with chelating agents: EDTA, penicillamine, or dimercaprol (BAL); of which penicillamine only is effective by the oral route. • Mercury Poisoning: 3 major forms of Hg must be distinguished: Hg vapor (elemental Hg), salts of Hg & organic mercurials. • Hg has special affinity for the S atom in thiol gps of enzymes to inactivate them, which is ultimately responsible for its toxicity. • Hg may be absorbed through the GIT, respiratory system or the skin. • The upper limit for Hg conc. in blood is 0.01-0.03 mg/ml. • The kidney is the target organ for inorganic Hg while the CNS is the target for elemental Hg & organic Hg compounds. • Arsenic Toxicity: both organic & inorganic forms of As are readily available in industrial & medicinal products. Pathways & byproducts of As biotransformation are not yet identified. • As produces dilatation of capillaries & increases the permeability of capillary walls. • It does not cross the BBB. • Symptoms include: blood, casts & protein in urine, vesicoes under intestinal mucosa, peripheral neuropathy & facial edema (it does not produce polycythemia). • BAL is the 1ry agent used for As toxicity. • Pepto-Bismol (Bismuth subsalicylate) is toxic if absorbed  colors stools black. • BAL & penicillamine are antidotes for heavy metals (Hg, Cu, Gold, As & antimony). • EDTA: is used as a chelating agent in heavy divalent metal poisoning. (e.g. Pb, Zn, Ca). • Deferoxamine is the antidote for Fe poisoning.

  11. Vomiting is contra-indicated in poisoning with: (as it might cause aspiration pneumonitis) • Bleaching liquid. – Organic acids – INH • Gasoline. – Liquid petroleum. • What is the antidote for phenylephrine poisoning? • Phentolamine c) Isoprotrenol • Atropine d) Histamine • What is the pharmacology of CO poisoning? • Interaction with Hb • Interaction with cytochrome oxidase. • What is the max time after which we can give N-acetyl cystine for acetaminophen toxicity : • 3 – 12 hrs. c. 24 hrs • 2 – 6 hrs d. 48 hrs • Grayish mouth & loss of teeth are symptoms of : • Lead poisoning c. Iron poisoning • Copper poisoning • EDTA can chelate Ca2+ & Fe3+ in the following proportions: • One mole of Ca 2+ + one mole of Fe 3+. • 2 moles of Ca 2+ + 2 moles of Fe 3+. • 2 moles of Ca 2+ + 3 mole of Fe 3+. • 3 moles of Ca 2+ + 3 moles of Fe 3+. • None of the above. • Which CNS poison is selectively toxic to the retina: • Methanol c. Disulfuram e. Warfarin • Arsenic d. CCl4 • Methanol toxicity is due to its conversion in the body to: • Ethanolc. Acetaldehyde • Carbonic d. Formic acid / formaldehyde • Methanol toxicity may cause: • Blindness b. Deafness • Overuse of digitalis may result in: • Habituationc. Addiction • Tolerance d. Cumulative poisoning • The first toxic symptoms of digitalis toxicity are: • GIT irritation c. AV block e. Flushing • Cerebral excitement d. Undue depression of heart EDTA is the antidote, also for As & Zn

  12. Which of the following symptoms is not associated with digitalis poisoning? • AV block c) Vomiting e) Constipation • Ventricular tachycardia d) Vagal arrest of the heart • Because the action of warfarin (dicumarol) persists for several days, its continued use may lead to cumulative poisoning which can be counteracted with? • Vitamin K c) Protamine sulfate • Prothrombin. d) Heparin • Organic pesticides (malathion) may be effectively counteracted with? • PAM (an emergency antidote) c) Charcoal • Pentaoline d) Dopamine • The greatest threat for morphine poisoning is: • Respiratory depression c. Renal shut down • Paralysis of spinal chord d. CV collapse • Among the signs of barbiturate poisoning are: • Hypotension. b. Diuresis. • Decreased respiratory volume. e. Alkalosis. • Which of the following could be used as antidote for curarae poisoning: • Neostegmine c. Atropine • Homatropine d. Hexamethonium. • What is the disadvantage of fluorinated drinking water: • It may cause mottling of teeth. • Poison ivy is treated by: • Calamine lotion c. Hydrocortisone (0.5% systemic) • Burrow’s solution d. Silver nitrate • Mechanism of action of dimercaprol & penicillamine in heavy metal poisoning: • Formation of a chelate (stable complex) that is non toxic & easily excreted (more water soluble) • Atropine poisoning causes all except: • Diarrhea. • Ca EDTA is used as an antidote for: • Pb poisoning (any divalent metal poisoning) • BAL (dimercaprol) is used as an antidote for: • Hg poisoning • A chelating agent used in Ca toxicity & in rheumatoid arthritis: • Penicillamine b. EDETA

  13. Solutions, Syrups, Elixirs & Tinctures • Preparations containing sugar are syrups & elixirs. • Preparations containing alcohol are tinctures, spirits & elixirs. • Essential oils: are used in perfume industry. • Methyl- & Propyl-paraben (preservatives) are used in combination to $ amount needed of each (achieve solubility, no ppt). The combination has strong antiseptic action (synergistic effect); also effective over a wide pH range. Their activity is $ in presence of non-ionic SAA. • Benzyl alcohol: in a conc. of < 1% is used as a preservative. • Benzyl alcohol: In a conc. of > 1% (3-5%) is used as a co-solvent. • Aluminium subacetate & Aluminium subgalate are used as astringents (in hemorrhoids). • Burrow’s solution: is an Al acetate solution. This is a topical solution with antiseptic & astringent properties, used as a mouth wash. • Flexible Collodion: is prepared by dissolving 2% camphor & 3% castor oil in collodion. • Salicylic acid Collodion: is prepared by dissolving salicylic acid in flexible collodion; it is used for removal of callous (warts). • Coal Tar solution: also called LCD (Liquor Carbonis detergent). It contains: d Coal tar d alcohol d Polysorbate 80. Polysorbate 80 is included to disperse the water insoluble coal tar which may ppt if mixed with water. • Sand is used during manufacturing of coal tar, to # its surface area & dissolution in alcohol. • Acidulin: releases HCl in vitro. • Rubitussin: contains glyceryl guaiacoate – an antitussive substance. • Coricidin: contains an anti-histaminic – chlorpheniramine maleate. • Formula 44 syrup: contains the active ingredient cetamlum. • Panalba: contains albamycin combined with tetracycline. • Organic solvents for internal use include: • Glycerol / Ethanol  for oral preparations • Vegetable oils (linseed, peanut & cotton seed oil)  as vehicles for parentrals. • Reading of a solution: the measure should be held at the level of the eye, to prevent paralox. • Controlled room temperature: temp between 15oC - 30oC (59oF - 86oF) • Cool place: temp between 8oC - 15oC (46oF - 59oF) • Cold place: temp between 2oC - 8oC (36oF - 46oF) e.g. refrigerator.

  14. Emulsifying Agents • Any compound that $ the interfacial tension & forms a film at the interface can function as an emulsifying agent. (Also known as wetting agents or surfactants). • The effectiveness of a compound depends on its: d Chemical structure d Conc. d Solubility d Physical properties d pH d Electrostatic effects. • Emulsifying agents can be classified as: • True emulsifiers: 1ry agents, capable of forming / stabilizing emulsions by themselves. • Stabilizers: auxiliary agents, do not form acceptable emulsions when used alone, but do assist 1ry agents in stabilizing the product by # viscosity. • Emulsifying agents can also be classified as: • Natural: Acacia, tragacanth, agar, pectin, gelatin, methyl-, carboxy-methyl-cellulose. • Synthetic EAs: dNon-ionic SA: (the molecule has no tendency to migrate to either pole) are resistant to the addition of acids & electrolytes; e.g. A Sorbitan esters (Spans): hydrophobic (HLB < 9)  w/o emulsions. A Polysorbates (Tweens): hydrophilic (HLB 11 – 20)  o/w emulsions. Spans & tweens can be used in combination to produce EA with total conc. 2% w/v. dAnaionic SA: A Sulphuric acid esters: e.g. Na lauryl sulfate (HLB < 9) (7-9) A Sulphonic acid derivatives: e.g. dioctyl sodium sulfo-succinate. A Soaps: these are for external use only, have high pH & are sensitive to theaddition of electrolytes & acids. . Alkali soaps: hydrophilic  o/w emulsions. . Metallic soaps: water insoluble  w/o emulsions. . Monovalent soaps:  o/w emulsions. . Polyvalent soaps:  w/o emulsions. dCataionic SA: e.g. A Benzalkonium chloride: used in conc. of 1% & is incompatible with soaps. A Cetyl pyredinium chloride. • The Critical Micellar Conc.: of a surfactant is the conc. above which the surface tension remains constant (does not decrease). Triethanolamine is an anionic surfactant

  15. ]W / O • Hydrophilic – Lipophilic Balance System: is used to classify thousands of non-ionic surfactants. These are given numerical designations between 1-20 depending on the relative hydrophilic – lipophilic portions of the molecule. • Emulsifiers with HLB < 9 are more lipophilic  w/o emulsions • Emulsifiers with HLB > 11 are more hydrophilic  o/w emulsions • Emulsifiers with HLB 9-11 can give both types of emulsions. • HLB: • 0 – 3  Anti-foaming • 3 – 6  W / O emulsion • 7 – 9  Wetting agent (SAA) • 9 – 18  O / W emulsion • 9 – 15  Detergent • 15 – 18  Solubilizing Agent • < 10, a compound is said to have a low HLB, >10 the compound is said to have a high HLB • Egg yolk (phospholipid): may be used in some pharmaceuticals as an emulsifying agent. • Lecithin (phospholipid): is a natural emulsifying agent. • Creaming: is the concentration of an emulsion resulting in accumulation of the concentrate at the top of the emulsion. Reagitation reconstitutes the emulsion again. • It is a reversible process, & is increased by the # in droplet size. Surfactants $ creaming. Suspensions • A suspension is a 2 phase system: in which the internal (or dispersed) phase is a solid & the external (or continuous) phase is a liquid. • Aggregation of the suspending agent: is called micelles (also one of the ultra-microscopic structure of the protoplasm – a colloidal structure). • Surface active agents (e.g. Na lauryl sulfate) promote wetting of solids. • If the contact angle is less than 90  the substance can be wetted. • If the contact angle is equal to zero  the substance is wetted. • In a suspension, settling of particles can be overcome by: • Adding non-ionic SAA. – Reducing particle size. • Increasing viscosity (by adding shear thinning agents). • Calamine: consists of 98% ZnO + 2% ferric oxide (Fe2O3). • Acetyl sulfa-isoxazole: is insoluble & tasteless, thus is ideal for flavored oral suspensions. • Propoxyphen napsylate: a narcotic analgesic, is a water insoluble powder which forms stable suspension. Propoxyphen HCl is soluble but unstable for commercial use. ]O / W

  16. Ointments • Yellow ointment: consists of 5% yellow wax (bees wax) in white petrolatum. • White ointment: consists of 5% white wax in petrolatum. It is hydrophobic (has a low water number). Thus aqueous solutions cannot be incorporated as a w/o phase in white ointment. • Hydrophilic petrolatum contains cholesterol which acts as an emulsifier, thus can be used to make a w/o emulsion. • Vaginal preparations: • Most commercial vaginal suppositories use a base of polyethylene glycol (PEG) (O/W). • An excellent choice of a diluent for compressed vaginal tablets would be lactose. • Coal tar ointment: Coal tar is mixed with polysorbate (as base), then added to ZnO paste. • Sulphur ointment: is used in the treatment of mild cases of scabies. • Calamine ointment: contains ZnO to protect the skin from further infections (protection). • Ziradyl: contains zirconium salt and is used as a protectant. • Compound undecylenic acid ointment consists of: - 20% Zn undecylenate • 5% free undecylenic acid - Poly ethylene glycol as a base. • Desenex: contains Zn undecylenate and is used as antifungal in athlete’s foot. • Seborrhea is a disease of the scalp, face & other areas of the body causing scaly scalp. It is treated with 0.01% cortisone e.g. betamethazone valerate (Betnovate). • Ointment bases: • Oleaginous bases: are good bases for oil insoluble ingredients (e.g. white ointment, petrolatum, lanoline derivatives, glyceryl monostearate & isopropyl palmitate). • W/O emulsion bases: e.g. cold cream, lanoline, eucerine. • O/W emulsion bases: e.g. vanishing cream, Lubriderm & hydrophilic ointment. • Water soluble bases: polyethylene glycol, propylene glycol & cetaphil. • Absorption bases: Aquaphor, hydrophilic petrolatum, wool fat (anhydrous lanoline). • Trituration: is the process of grinding a substance to a very fine powder. • Pulverization by intervention is the process of reducing the particle size of a substance to fine powder by utilizing a solvent which can be removed easily, e.g. camphor + alcohol. • Levigation: A process of reducing a powdered drug to a smooth paste using a levigating agent which should be compatible with the powdered drug. It is a process of wetting & smoothing. E.g. the incorporation of powder into ointment base by adding a wetting agent (oleaginous vehicles e.g. mineral oil; hydrophilic vehicle e.g. glycerol). • Precipitated sulphur: is used in preparing ointments as it has finer particle size & greater surface area than other forms of sulphur. It produces a smooth ointment. • A gel structure can be formed by Bentonite, Agar, or Accacia.

  17. Other Formulations • Percolation: is an extraction process of the desired constituent of a powdered drug by the descend of a suitable solvent at a controlled rate through a column of the drug. • Maceration: is an extraction process of the desired constituent of a powdered drug by soaking in a suitable solvent. • Lyophalization (freeze drying): loss of moisture under low temp. It involves rapidly freezing a substance (below eutectic point) & dehydration under low pressure (# vacuum). • Micrometrics: it is the study of all aspects of small particles e.g. particle size, separation of particles, etc. • Impalpable: refers to a substance that is imperceptible to the touch. • In order to apply powder to the skin, a particle size of < 50m is desirable. • Particle size for aerosols  2 – 6 m. • Particle size for inhalation  0.1 m. • The powder surface area: can be determined by the adsorption of a gas. • In a crystallization process: Addition of a reactant with vigorous stirring will lead to the formation of crystals with solvent embedded in it or very fine filterable powder. • Freon II: a fluorinated hydrocarbon used as a propellant in aerosols; as it has harmful effects on environment, is currently replaced by flouro-hydrocarbons. It is used only in deodorants. • Nicorette: marketed as a chewing gum, each piece containing 2 mg of nicotine-resin complex. It is used to help physically dependant cigarette smokers to quit smoking. It does not eliminate the desire to smoke. It is contraindicated in pregnancy & cardiac problems. Tablets • The Wurster Process: can be used to coat tablets. • Tablets are coated: to mask bad taste & / or unpleasant odor. • Picking: is said to occur when poorly manufactured tablets have small particles on the surface (due to tablet powder sticking to the punch face). • Mottling: is uneven color distribution of tablets due to poor mixing of tablet granulations. • Shellac is sometimes included as a sealing subcoat in the production of sugar coated tablets. It prevents the tablet from absorbing water from subsequent coating solutions. • Methyl stearate is used as a lubricant, while talc is used as a glidant in tableting. • Fillers in tablet manufacturing: Mannitol, Lactose, Cellulose & Ca3 (PO4) 2. • Disintegrants in tablet manufacturing: Mannitol, Lactose, Cellulose & Ca3 (PO4) 2. • Mannitol (in manufacturing) has 2 functions: • It possesses characteristics that make it almost a sweetener for chewable tablets. • It is included in many lyophilized (freeze dried) products as a bulking agent as the cake.

  18. Liquid droplets dispersed in another liquid is called: • Emulsion b. Suspension c. Gel • Which of the following vehicles is suitable for internal use: • Ethylene glycol c. Butanol e. Methanol • Ethanol d. Isopropanol f. Propylene glycol • Addition of mineral oil to sulphur is: • Trituration (powder with powder) c. Levigation e. Attrition • Milling d. Pulverization • Menthioglycerol in a parentral procaine penicillin suspension is: • Wetting agent. c. Antioxidant. e.Solubilizer. • Suspending agent. d.Buffer. • Polyoxyethylene sorbitan monooleate is used in a mouth wash as: • Flavoring agent c. Preservative e. Antioxidant. • Oil solubilizer d. Buffer. • Which of the following agents is used as anti-oxidant in aqueous solutions: • Na bisulphite (Na thiosulfate) b. Vitamin C c. EDTA • Na lauryl sulfate is a surfactant: • Anaionic b. Non-ionic c. Cataionic • What is the use of cellulose in tablet formulation: • As a diluent b. As a lubricant c. As a glidant • What is the use of talc in a formulation: • As a diluent b. As a lubricant c. As a glidant • Methyl cellulose is a(n) surfactant: • Anaionic b. Non-ionic c.Cationic • Which of the following has a phospholipid structure: • Lecithin c. bile acid c. Cardiolipin • Aquaphor is: • Anhydrous ointment base ??? • Hydrophilic petrolatum ??? • Lanoline 900 gm + Fatty acid (oil) + Cetyl alcohol + Water 500 ml, the resulting formula is: • O/W emulsion

  19. A sustained release formulation has no value in: • Drugs having long half-life. b.Drugs having short half-life. • Which of these suppository bases can be used for both oil- & water-soluble drugs: • PEG (carbowax) c. Cocoa butter • Glycerin d. Glycerinated gelatin • The sedimentation rate of a poorly soluble drug in a suspension can be decreased by adding: • Non-ionic surfactantd. Thyxotropic gel • Shear thickening gel e. Dilatant colloidal clay • An agent that increases the viscosity. • Levigation depends upon: • Ointment base b. Particle size c. Both • Which of the following is true about enteric coated tablets: • Protected from moisture b.Protected from gastric juice • What is bentonite magma: • A preservative b. A suspending agent • A substance has an HLB of 10 – 18 forms: • Good W/O c. Is good for solubilization • Good O/W d. None of the above • Which of the following can be used as an emulsifying agent for O/W parentral emulsions: • Lecithin • Burrow’s solution is used as : • Astringent b. Keratolytic • Fereon, which is used as a propellant in aerosols,: • has a harmful effect on the environment (Ozone) • In tablet manufacturing, Mg stearate is used as: • Lubricant b. Glidant c. Diluent. • Which is not a suitable suspending agent in clear gel preparations: • Bentonite. • Which compound is used as a preservative & antibacterial: • Benzalconium chloride b. Propylene glycol. c. Benzoyl alcohol. • Hydrophilic petrolatum employs wool alcohol to: • Render petrolatum emulsifyable. • Arrangement of surfactant molecules in a sphere is called: • Micelle

  20. Which drugs are used in smoking cesation: • Nicoderm d. Nicorette g. Nicotrol • Regitine e. Bupropione (Zyban) h. Clonidil • Rivia f. Normatol • On the label of Nicorette gum resin it should be indicated: • Do not take more than 20 mg per day • Not used for patients under 18, pregnant nor lactating women • Do not throw into the garbage (toxic to animals) • Chew, park against the cheek then chew again • What advice do you give to a patient taking Nicorette gum resin: • The number of chewing gums should not exceed 10 per day • Changing the site of chewing. • Park against the cheek every 15 min. • Which is not considered a tablet processing problem: • Peeling c. Sticking e. Mottling • Capping d. Picking. • Which is true about surfactants: • Have hydrophylic, lipophylic properties • Are either anaionic, cataionic or non-ionic • Are amphiphobic • React as acids & bases (Amphoteric) • The physical stability of a solution can be determined by: • Precipitationb.Odor c. Viscosity • A flocculated sediment has: • Has a large volume of sediment c. Easily re-dispersed by shaking • Has a clear supernatant • Diazepam, ethanol & phenol, phenol is: • Cosolvent • Cimetidine HCl, water & phenol, phenol is: • Preservative • The process by which a substance accumulates on the surface of a body is: • Adsorption b. Absorption • Which is not in suspension: • Adsorption c. Aggregation • Flocculation d. Crystal growth

  21. Fluorinated hydrocarbons (Fereon) are replaced by: • Hydrocarbons c. Chlorofluorocarbons (CFCs) • Inert gas d. Hydrofluoroalkanes (Hydrofluorocarbons) • Which of the following happens when a tablet reaches the stomach: • Absorbs water c. Swells • Undergoes hydrolysis • Which is true about sedimentation: • Larger particles have higher sedimentation rates • Decreasing particle density decreases sedimentation rate • Sedimentation increases with the decrease in viscosity • Which increases wetting of powders: • Polysorbate 80 b. Benzyl alcohol. • Which is used to prepare O/W emulsion: • Accacia c. PEG • Methyl cellulose d. Polysorbate • Which is used as a base for vaginal suppositories: • Propylene glycol b. Cocoa butter • The removal of tablet surface material by a punch is called: • Picking b. Mottling • Which is not included as an emulsion problem: • Cracking • Creaming in an emulsion is due to: • Increasing droplet size • Diazipam + Alcohol + Propylene glycol (or ethylene glycol) 45% in a Rx is: • Co-solvent c. Preservative • Antioxidant d. Solvent • Gel preparations can include all except: • Carageenan c. Accacia • PEG d. Agar • Elixirs are: • Sweetened hydro-alcoholic formulations • Tri-ethanolamine is used as: • Emulsifying agent • Which is used as a humectant: • Glycerol

  22. Ophthalmic Preparations • The cornea of the eye: consists of 3 layers: • Outermost layer  the corneal epithelium. • Substantia propria  the stroma. • Inner layer  the corneal endothelium. • Stroma is the deepest & most hydrophilic & least lipophilic layer. • The capacity of the precorneal area: for instilling eye drops is ~ 0.01 – 0.02 ml. (the normal tears volume is ~ 0.007 ml). • A wetting agent is used for contact lenses: to prevent dryness (e.g. Na lauryl sulfate). • On using soft lenses: An antimicrobial preservative for ophthalmics is considered adequately effective if it re-sterilizes the solution within 1 hr. • A combination of benzalkonium chloride & EDTA (0.01% of each) is effective against most common micro-organisms including strains of P. aeruginosa that are resistant to benzalkonium chloride alone. • Benzalkonium chloride, in addition to its use as a preservative is also used to adjust the pH of nasal drops to reduce irritation. • Thiomersal: is used as a preservative in contact lenses’ solution. • Pabin is a proteolytic enzyme used in contact lens solutions as a protein remover to dissolve proteinaceous residues that slowly build up on lenses. It is present in protein removal tablets. • Collyrium means an eye wash (may contain boric acid). • Liquifilm is an ophthalmic vehicle containing polyvinyl alcohol to increase the viscosity & thus increase contact time with the corneal surface. • Methyl cellulose, carboxymethyl cellulose & hydroxypropyl methylcellulose are used to increase viscosity of eye drops. • A red dispensing cap or top in eye drops identifies mydriatic drugs (as atropine, mydriacil). • A green dispensing cap or top in eye drops identifies miotic drugs (as pilocarpine). • Nasal & ophthalmic solutions: should have low or mild buffer capacity so that the natural buffer system can overcome any pH difference otherwise it will cause irritation. • They should have an acidic pH (5.5 – 7.5)  use phosphate buffer. • They should be isotonic. • They should have an antimicrobial preservative.

  23. Difference Mode of action Onset of action Duration of action Vision Pilocarpine Contraction of sphincter muscle of the pupil leads to drainage of aqueous humor & $ IOP 2 – 4 hrs 4 – 8 hrs Accommodation of near vision due to miosis. Timoptic Decrease the production of aqueous humor  $ IOP 1 – 2 hrs 24 hrs No effect on vision because there is no miosis. • Difference between pilocarpine & beta-blockers (Timoptic) in treatment of glaucoma • Narrow angle glaucoma: is treated by pilocarpine, timolol, phospholine iodine, pheostegmine ( anticholine esterase) or carbacol 0.5 - 1% (which is similar to acetylcholine). • Advantages of timolol maleate (Timoptic) over pilocarpine • Reduces the elevated IOP through $ production of aqueous humor. • Exerts its maximal effect within 1 – 2 hours. • Maintains significant effect for 24 hrs after one single dose. • Little or no effect on visual accuracy or accommodation. • Little or no effect on pupil size. • Pilocarpine: the miotic effect of pilocarpine is observed 5-30 min after installation in the eye & the intraocular pressure is reduced within 2 – 4 hours. • Phospholine Iodine: is an anti-cholinesterase drug (# acetylcholine) & used to treat glaucoma. Prolonged use of this drug, reduces the activity of pseudo-cholinesterase. • Epinephrine (adrenaline) is contraindicated for narrow angle glaucoma: since dilatation of the pupil may lead to blindness. It may be used in open angle glaucoma as it increases the drainage, & reduces the production of aqueous humor. • Similarly, phenylephrine, guanithidine, antazoline & hematropineare contraindicated for narrow angle glaucoma: as they cause mydriasis. • 90% of glaucomas are open (wide) angle glaucoma. • Filters used in ophthalmics have pose size = 0.2m.

  24. Phospholine is an irreversible cholinesterase inhibitor. • Methyl cellulose is used in ophthalmic solutions to: • Increase contact time of solution in the eye. c. Increase infiltration • Increase drop size • Drugs of choice for the treatment of narrow angle glaucoma include: • Physostigmine (eserine), pilocarpine, phospholine, iodine myosis. • Carbachol (0.5 – 1% eye drops). • Demecarium (reversible cholinesterase inhibitor). • Hematropine (atropine derivative) • The Rx shown is: Rx Atropine sulphate Carboxymethyl cellulose (# viscosity) Benzalkonium chloride (Preservative) Na3PO4 / Na2HPO4 (Buffer) Aqua • Suspension c. Cream • Ophthalmic solution • The English name of collyrium is: • Eye wash. c. Clear solution. • Ointment. • What is the effect of beta-blockers (Timolol) on the intra-ocular pressure : • Increase the intra-ocular pressure • Decrease the intra-ocular pressure • 90% of the cases of glaucoma are: • Narrow angle glaucoma • Wide (open) angle glaucoma • To increase the bioavailability of ophthalmic solutions: • Increase conc. of drug c. Add mono-ploymer • Increase the retention time (by increasing viscosity). • Hydroxy methyl cellulose in atropine eye drops is used to: • Inhibit bacterial growth • Increase corneal contact time. • Which agent is used in otic solutions to increase bioavailability: • Ethyl alcohol c. Methyl alcohol • Glycerol. • A sympathomemetic drug will $ IOP by: • Decreasing synthesis of aqueous humor. • Increasing drainage of aqueous humor.

  25. Which is the most lipophilic barrier of the eye: • Cornea. c. Conjunctiva • Eye lids d. Aqueous humor. • All of the following are used in eye allergy except: • Xalatan (eye pressure) • Side effects of Xalatan (Catamaprost) include: • Pigmentation (eyes are more black) • Increased thickness of eye lashes • In ophthalmic preparations, the absolute bioavailability is: • Zero % c. 50%. • 75%. • The rate limiting step in an ophthalmic preparation is: • Corneal penetration • A solution of phenyl ephrine & boric acid is: • Hypertonic b.Isotonic • Which is correct about ophthalmic solutions: • Methyl & propyl parabens (preservatives) are not used in ophthalmic preparations • Polyvinyl alcohol increases viscosity in ophthalmic preparations. • Surface active agents are used in lens solutions to increase wetting. • Percentage bioavailability is zero. • Best way of application of eye drops is to: • Make an occular sac in which to insert drops. • Insert drops in the cap. • Close the eye & apply pressure on the internal corner. • Which agent is used in otic solutions to increase bioavailability: • Ethyl alcohol c. Methyl alcohol • Glycerol. • A sympathomemetic drug will $ IOP by: • Decreasing synthesis of aqueous humor. • Increasing drainage of aqueous humor.

  26. Parentrals • The gauge number of needles (G): this number refers to the external diameter of the cannula. The larger the gauge number the smaller the diameter of the cannula. • Hypodermic Needle: is a small needle used to inject a drug under the skin. It consists of: • Hub: the extension of the needle that fits onto the syringe. • Bevel: Portion of the needle that is ground for sharpness. • Heel: the back portion of the bevel • Cannula: the shaft portion of the needle (made of steel) • Lumen: the cavity in the needle through which drug is injected. • A short bevel needle: is preferred for IV injection as it reduces the possibility of perforating the back wall of the vein. • A very short bevel needle: is preferred for ID injections. • Insulin preparations: have low viscosity & small volumes to inject. Thus small pore (25G – 26G) & short (1/2 or 5/8``) needles are adequate for SC injection. (Insulin is given SC because of good absorption from this site, ease of self-administration & to $ tissue damage). • Winged needle (Butterfly): consists of a stainless steel needle with 2 flexible plastic wing-like projections that serve 2 purposes during IV injection: • They ease manipulation of the needle during insertion in the vein. • Allow the needle to be anchored to the skin with a tape. • A Busher Automatic Injector: is a metal device in which the patient places a filled hypodermic syringe & needle. It automatically administers the injection. • Becton-Dickinson (B-D): supplies insulin syringes with 0.5 ml volume. • Autoclaving: sterilization under steam & pressure (15 min at 121oC). • Propylene syringes are autoclavable while other plastic syringes must be gas sterilized (using ethylene oxide). Vials are also sterilized using ethylene oxide. • Venoclysis is the IV administration of large volume parentrals by infusion. (= IV infusion). • Hypodermoclysis: is the intentional administration of IV fluids in the SC tissue (e.g. in infants & obese women). • LVPs: means large volume parentral solutions. • Piggy pack: saves the patient from multiple injections (as intermittent therapy of antibiotics). • IV infusion: maximum volume / day is 4 L otherwise it might cause fluid overload. • Diazepam should not be added to IV infusions as it will precipitate. • IV admixture must be used within 24 hrs (when refrigerated 2-8oC to limit microbial growth)

  27. Needle Gauge:13 – 27  largest number: S.C.  24 – 25 Comp. Parentrals  18 – 20 I.M.  12 – 19 Needle length: ¼ - 6 inches I.D.  ¼ - 5/8 inches S.C.  ½ - 5/8 inches Compound Parentrals  1.5 inches I.V.  1.25 – 1.5 inches Intra-cardiac  3.5 inches Filters: Depth Filters: Fritted glass or unglazed porcelain. Serum Filters: Cellulose ester or ….. or ……

  28. Parentral Solvents & Solutions • Purified water USP: The method of preparationmust be indicated on the label (i.e. distillation, ion-exchange, …etc.). • Water for injection (WFI): is a pyrogen-free water, freshly prepared by careful treatment of distilled water. It must be used within 24 hrs as it may get contaminated with microorganisms. During manufacturing of parentrals, WFI is most commonly used, & is sterilized near the end of the manufacturing process. • Test for pyrogen-free water: is made by measuring the temp. of tested animals. If the water is pyrogenic a increase in body temp. of tested animals. • The Limulus test: is an in vitro test for pyrogen. It is more rapid, sensitive & simple than the rabbit (in vivo) test. • Sterile water for injection: is used to reconstitute penicillin, ampicillin, erythromycin,…etc. • Oily injections have vegetable oil (e.g. linseed, cotton seed, sesame, peanut or corn oil but never olive, castor, mineral or theobroma oil) as solvent. • Parentral stability: for parentral admixture (e.g. ampicillin) normal saline is more stable (8 hrs at room temp) than 5% dextrose (4 hrs at room temp). Thus normal saline is preferred. • Erythromycin precipitates if reconstituted with normal saline. • Garamycin (Gentamycin sulfate): is one of the soluble antibiotics & is stable in aqueous solution for 2 years; thus it is available as a solution ready for injection. • Dextran is a plasma expander (# extracellular fluid volume). • The acetonide salt: is used to improve the solubility characteristics of some drugs; e.g. triamcinolone acetonide (Kenacort) & fluocinolone acetonide (Synalar). • SC injections must particularly be isotonic as these come in contact with nerve endings & stay for a long time; otherwise they will be painful. • IV injections must not be in suspension form otherwise it might block the blood vessel. • IM injections are sometimes preferred over IV injections to avoid capillary damage. • Parental formulations should be: d Pyrogen free d Sterile (preserved) d Particle free d Isotonic (to prevent irritation / hemolysis) • Inert gases sometimes replace oxygen to improve stability of the injection. Unless otherwise specified, they are not indicated on the label. • Quantities of all ingredients in parentral solution should be specified on the label including: d Antimicrobials, d Antioxidants d Chelating agents d Isotonic adjustors N.B: pH adjustors (HCl / NaOH) are not specified as the amount needed varies between batches.

  29. Parental Electrolytes • IV fluid system (Glass bottles): can be divided into 2 types based on the presence or absence of an airway tube. • Baxter: utilize a plastic airway tube through the stopper to above the fluid surface when inverted for administration. • Abbott: utilized a filtered airway in the administration set. • The isotonicity of blood is equal to 0.9% NaCl solution or 5% dextrose solution w/v. • Parentral electrolytes: their conc. is usually expressed in mEq. • Sodium Cation: is the most prevalent cation in the extracellular fluid of humans, present as Cl-. (135 – 145 mEq / L). • Potassium Cation: is the most prevalent cation in the intracellular fluid of humans, present as PO4. (3.5 – 5.5 mEq / L). • Potassium PO4is used as a source of PO4 & if only K is needed use KCl or K acetate. • Calcium PO4 & CO3 have limited solubility & thus may precipitate in parentral admixtures. • To reduce the possibility of pptn in a mixture of K3 PO4 & Ca gluconate we must: • Lower the conc. to 20 mEq / L for each. • Dissolve K3 PO4 first then add Ca gluconate slowly while stirring. • Since K3 PO4 is available as a mixture of monobasic (KH2PO4) & dibasic (K2HPO4) it is more suitable to express the conc. in mmoles/L (rather than mEq/L) based on K average. • Adults need 10 – 15 mM of phosphorous / day. • Ringer’s injection: is an isotonic electrolyte solution of Na+, K+, Ca++ & Cl-, in a balanced physiologic preparation. • Lactated Ringer’s injection (Hartmann’s solution) is considered to be the most closely related to the extracellular fluid of the human body. • Heparin Na: should not be given IM as it is painful & may cause localized haematoma. • Ascorbic acid injection: is highly acidic, thus alkali as NaOH, NaHCO3, Na2CO3 are used to adjust the pH between 5.5 & 7. • Liposyn & Intralipid: are parentral emulsions intended to provide fatty acids. These should be administered separately & should not be admixed with other drugs / solutions. • Narrow safety margin drugs: given by slow IV infusion to maintain constant therap. conc. • Extravascular blood (blood donation): blood is prevented from clotting by removing the Ca++ cation by adding a mixture of citrate salts (Na, K, NH4) which will react with the Ca in blood to form Ca citrate. Upon administration to a recipient, citrate is rapidly metabolized in the liver releasing free Ca & blood is capable of clotting normally.

  30. Albumin & Globulin • Inradermal test with gamma-globulin: will cause localized inflammation (incorrectly interpreted as +ve reaction) & treated with epinephrine which should be available. • Serum globulin contains 17% gamma-globulin. (serum hepatitis is seldom reported). • Normal Human Serum-albumin USP 5% or 25%: is a sterile preparation of serum albumin used to treat shock or hemorrhage. It is stable to heat & is stored at room temp. • Serum albumin: is a protein in plasma which controls blood volume through its water containing capacity. • The label of biologicals: should specify the storage temp (2 - 8oC with few exceptions). Types of Glass • The water resistance of glass containers: is measured by testing the amount of alkali released into water (which # the pH & may $ stability). • Type I glass: is made of barosilicate. It is the best material; more resistant towater attack. • Type II glass: is specially treated with SO2 & is called treated soda-lime glass. • Type III glass: is typical soda-lime glass & is for non-parentral use (not for injections). • Leaching: means the release of a container’s ingredient into the product; e.g. Zn is released (or leached) from a rubber closure of a vial into the drug. • Adsorption: When 2 substances are taken up and one is attached superficially to the other, it is said to be adsorbed (this is a reversible process). The term is used to refer to binding of a substance on the surface of the container. • Diffusion: is the passage of a substance through a 2nd substance (e.g. volatile oil or a dye through the walls of the container). • Porosity: indicates small holes through which a substance can pass. Sustained Release Formulations • Advantages: • Less frequent dosing is more convenient for patients & nurses. • Maintains therapeutic effect for longer period of time (vs. conventional dosage forms) • Eliminates the fall of serum levels below the minimum effective level (MEL)  the patient is receiving therapeutically adequate amount of the drug at all times. • The maxima (peaks) in drug conc. (seen with multiple dose administration of conventional dosage) are eliminated  more economic use of the drug & $ side effects (since higher blood levels  higher side effects). • Elimination of maxima decreases the total amount of drug needed to achieve MEL.

  31. Parentrals should be: • Sterile b. Particle free c. Pyrogen free • In an IM injection, which is least required : • Plastic c. Pseudo-plastic • Dilatant (# shear stress  # viscosity  # resistance to flow) • Which of the following organic solvents is used to prepare internal use injections: • Glycerol c. Alcohol d. Acetone • Vegetable oil (peanut, sesame or cotton seed oil but neither olive nor theobroma oil) • At the site of injection, the rate of absorption is decreased by: • Friction. c. Heating. d. Cooling. • Injection of adrenaline. ( vasoconstriction  $ absorption  prolonged effect) • In a parentral Rx of hormone, adrenaline is used as: • Vasoconstrictor. • Blood substitution after injury or surgery is with: • Plasma. b.0.9% NaCl. c. 5% dextrose. • Which of the following statements concerning immune serum globulin is true: • immune serum globulin contains ~ 50% gamma globulin. • Serum hepatitis is one of the most common reported adverse effects. • Skin test should not be performed before injection. • Virus infections attenuated by gamma globulin are non-infecting. • Where is Limulus amebecytes used: • Test for pyrogen • The major contaminant in parentrals is from: • Raw materials c. Personnel • Equipments d. Atmosphere • Intra-articular injection means: • In the synovial fluid b. In the joint or the synovial space • For the preparation of LVPs we use: • Purified water for injection USP b. Sterile water for injection USP ??? • Testosterone is sterilized by: • Dry heat sterilization b. Gas sterilization • To improve the stability of parentrals we use: • Inert gas instead of oxygen.

  32. Type II glass: • Is best for parentrals • Prepared by de-alkalizing Type III glass by SO2 more resistant to water • Specially treated soda-lime glass • Castor oil has : • Very low I2 value (almost zero) • Dry heat sterilization is used for: • Mineral oil b. Testosterone • In ethylene oxide sterilization,: • You must first aireate the substance to be sterilized. • In parentrals, phenol is used as: • Preservative (0.5%). • Extravasation is a problem with IV injections, it describes: • Escape of blood to the surrounding tissue. • Escape of injected fluid to the surrounding tissue. • A clot at the end of the needle. • Ethylene oxide sterilization: • Has high penetration power for sealed plastic containers • Is used for the sterilization of chemical waste products • Where is Limulus amebecytes used: • Test for pyrogen • The major contaminant in parentrals is from: • Raw materials c. Personnel • Equipments d. Atmosphere • Intra-articular injection means: • In the synovial fluid b. In the joint or the synovial space • For the preparation of LVPs we use: • Purified water for injection USP b. Sterile water for injection USP ??? • Testosterone is sterilized by: • Dry heat sterilization b. Gas sterilization • To improve the stability of parentrals we use: • Inert gas instead of oxygen.

  33. Acids & Alcohol • Glacial acetic acid: 100% w/w. It is the highest conc. & the strongest acid. • Acetic acid USP: 36 – 37% w/w. • Diluted acetic acid: 6% w/v. • Phosphoric acid BNF: 85 – 88% w/w. • Diluted phosphoric acid: 10% w/v. • HCl USP: 35% w/w. • Absolute alcohol USP: 100% v/v ethanol. • Alcohol USP (grain alcohol): contains 95% ethanol (94.9% v/v = 92.3% w/w). • Proof alcohol: 50% v/v. • Dilute alcohol is 49% v/v ethanol. • Rubbing alcohol is 70% v/v ethanol. • The volume of alcohol: is determined at a temp of 15.6oC (60oF). • A cough syrup is labeled as containing 20% alcohol by volume, this is equivalent to 20 ml absolute alcohol in every 100 ml of syrup. • Its proof strength is calculated by doubling the % v/v, thus it will be 40%. • Shrinkage: It occurs when alcohol is mixed with purified water & is primarily due to hydrogen bonding (attraction forces between H atoms & electro –ve atoms as O / N /F). • Mineral oil is immiscible with alcohol & with castor oil. • Acetic acid: is used as a bladder irrigator. • Boric acid: is a mild antiseptic used in eye washes or in topical / vaginal preparations. • Tannic acid: is an astringent used in burns & wounds. • Undecylenic acid (Desenex): is a fungistatic agent used in treating ring worm (athlete's foot). • Trans-retinoic acid (Acutane) (iso-retinol): is used topically for the treatment of acne. • Para-amino benzoic acid (PABA): is used as a sun screen & in Enrlish test.

  34. Antiseptics • Iodine solution USP: contains I2 & NaI. They react to form Na I3, a water soluble complex (hydrotrophy) without loss of antibacterial activity. • Iodine Tincture & Solution: both contain 2% I2 & 2.4% NaI, but differ in the vehicle: • The solution is prepared using purified water USP. • The tincture is prepared using diluted alcohol USP (49% alcohol). • In the Tincture: NaI is not added to help solubilize I2 in alcohol (I2 is readily soluble in alcohol) but to prevent pptn. if water is added. • Official hydrogen peroxide solution: is 3% solution of H2O2; this is also called 10 volume solution meaning that 1 ml of solution liberates 10 volumes of O2. • 20 volume (6%) H2O2 solution: is considered too strong for medicinal use. It is used to bleach hair & fabrics. • The antiseptic properties of H2O2 solution: is dependent on the catalaze enzyme which breaks 2 H2O2 2 H2O + 2 O. The nascent oxygen oxidizes the bacterial cell. • Hydrogen peroxide is used in cleansing wounds & diluted 1:1 with water & used as a mouth wash, to treat Vincent angina (Trench mouth). • Sodium hypochlorite solution (NaOCl): Known as Dakin’s solution (Clorox). It is a disinfectant & not an antiseptic, because of its high alkalinity which is too strong to be applied to living tissue. • Benisone Gel: contains beta-methazone benzoate (steroid) & is used as an anti-inflammatory in dermatitis. It does not contain benzoyl peroxide. (Betnovate is beta-methazone valerate) • Benzoyl peroxide is used topically to treat acne. The Law of Pharmacy Practice • Patients have the right to know the effects of the drug from the pharmacist. • When filling a Rx: to get maximum patient satisfaction, the patient should receive both oral & written counseling (instructions). • Vicarious Liabilities of the pharmacist: An innocent master may be held responsible for the harm caused to a 3rd person by the torsion acts of his servants while they are acting within the cope of their employment, HE WHO ACTS THROUGH OTHERS, ACTS HIMSELF. i.e. the pharmacist has responsibility of all subordinates working in the pharmacy. • Authorization: It is the responsibility of the pharmacist who handles this authorization. • Negligence: is less than average pharmacy care. • The main reason for keeping a low inventory is to decrease the cost of inventory. • The % turn over for a good business is 5%.

  35. Anti-emetics • Metoclopramide (Primperan): is a dopamine antagonist that stimulates the motility of the stomach & is used in: • Diabetic gastro-paresis (delayed gastric emptying) in diabetics • Gastro-esophageal reflux disorder (GERD) • Antiemetic in cancer chemotherapy where it acts through 2 mechanisms: • Centrally: central antiemetic effect (being a dopamine antagonist) • Peripheral: cholinomimetic effect • Chlorpromazine: a phenothiazine (major tranquilizer) is used as anti-emetic. • Emetrol is also used as anti-emetic. • Nabilone: a cannabinol used as anti-emetic for nausea & vomiting in cancer chemotherapy. • Anti-cancer drugs induce nausea & vomiting by stimulation of the chemoreceptor trigger zone (CTZ) & vomiting center. Antacids • Antacids relief pain. They are more effective if given 2-3 hours after meals. If given hourly their dose must be reduced. • NaHCO3 (baking soda): has alkaline pH when dissolved in water, thus used as antacid. It has poor alcohol solubility. When heated, it produces a more alkaline carbonate solution. • Antacids hinder the absorption of penicillin, tetracyclines, INH & iron preparations. • Aluminium hydroxide & magnesium hydroxide (milk of magnesia) are antacids that hinder the absorption of penicillin & must be given 4 hrs before or after penicillin dosing. Also hinder the absorption of tetracyclines & INH. • The most common side effect of Al(OH)3 is constipation. • Antacids should be taken 1-3 hour PC & HS: as they neutralize HCl secreted in response to eating. They should be repeated 3-4 times daily. (PC = after meals HS = at bed time) • Sucralfate (Sulcrate): is used in treating duodenal ulcers, it forms a complex with ulcerated area protecting it from gastric acids & enzymes  healing of ulcer; given before meals. • H2 receptor antagonists (Cimetidine): are used to treat peptic ulcers. • The ideal antacid is that which raises the pH of the stomach contents to ~ 3.5 - 5. This will neutralize 90% of the acid & greatly reduce the proteolytic activity of pepsin. • Buffering to higher pH serves unuseful purposes. • At pH 4 pepsin will be completely inhibited.

  36. Anti-diarrheals • Kaopectate: contains Kaolin + pectin  treats diarrhea. • Polycarbophil: is the safest anti-diarrheal drug. It absorbs large amounts of water leading to stool formation. It has no effect on the digestive enzymes & nutrients. It is not absorbed. • Bismuth subsalicylate (Pepto-Bismol): used in chronic diarrhea, & traveler’s diarrhea; its mechanism of action is: • Inhibit protein by local action • Has adsorbent properties • Salicylate portion has anti-diarrheal action due to inhibition of prostaglandin synthesis which may be a mediator of intestinal secretions. • Blacken the stool due to inhibition of bisulphite. • GIT hemorrhage. • In diarrhea: • Activated charcoal is a good adsorbent, but is not used as it has a laxative effect. • Kaolin & attapulgite (adsorbent clays – Mg & Al silicate) adsorb alkaloids, toxins, bacteria; but as they also adsorb enzymes/nutrients, are only used in mild diarrhea. • Diphenoxylate (Lomotil) • It is a Meperidine analogue. • CNS depressant (poteniates barbiturates, alcohol & neuroleptics). • Should not be used for > 5 days in adults & is not recommended for children. • Decrease GIT propulsion. • No analgesic activity. • Short duration of action, given QID. • Lomotil contains diphenoxylate + atropine to prevent its abuse as a narcotic, thus it does not cause addiction. • Loperamide (Imodium) • Related to diphenoxylate & haloperidol but is not a Meperidine analogue. • No CNS depression (does not stimulate opiate receptors). • No tolerance, no dependence • Decrease GIT propulsion. • No analgesic activity. • More potent, rapid onset & prolonged duration of action, given BID - TID. • No withdrawal symptoms.

  37. Laxatives • MgSO4, Mg citrate, Na2HPO4, Na3PO4: laxatives with a purgative, non-systemic cathartic effect, used to # peristalsis of intestine by # bulk of stools (laxation by osmosis, like enemas). • Paraffin oil is used as a lubricant cathartic (soften the stool by lubrication). • Sodium docusate (stool softener) is the best laxative in old age. • Poloxamer 188: is a surfactant, it softens the stool by reducing surface tension. • Bisacodyl (Dulcolax): stimulates the intestinal wall. It is manufactured as enteric coated tablets (to avoid gastric irritation). It should not be taken within 1 hr of ingestion of milk or antacids (as these may cause premature dissolution  gastric irritation). • Psyllium & Carbophils: produces bulky stool. • Lactulose: is a synthetic disaccharide used in the treatment of chronic constipation. Additionally it is used to decrease NH3 from blood. • Senokot: is a laxative containing senna powder. • Some Laxatives Include: • Neolid: 76% castor oil in aqueous emulsion. • Agoval: Mineral oil + phenolphthalein. • Kondremul: Mineral oil + cliondrus. • Petrogolar: Mineral oil in aqueous emulsion. • Neo cultol: chocolate flavored mineral oil jelly. • For elderly patients suffering from constipation: advise a stool softener, if found ineffective you can advise: Moderate exercise, Warm water & Fibrous diet. Urinary Tract • Cunning ham clamp: is a device used to stop urine flow in an incontinent male to prevent nocturnal enuresis (involuntary discharge of urine during sleep). • Pyridium: is a red dye (azodye) used as a urinary analgesic. It causes discoloration of urine. • Acidification of urine can be done with NH4Cl, which, when ingested, the NH4+ dissociates to NH3 and H+. NH3 is converted into urea which has osmotic properties. H+ is buffered & Cl- is filtered along with Na+, thus maintaining electrical neutrality to the extent that urinary Na+ is not replaced by H+ in renal tubules. Na+ & water are lost in urine. • Alkalanization of urine can be done with NaHCO3 to # excretion of phenobarbitone & salicylates.

  38. Which of the following agents is used to acidify urine (or to # excretion of an alkaline drug): • NH4Cl c. Vitamin C • Sodium citrate d. NaHCO3 • Mineral oil is not used as a laxative because: • It interferes with the absorption of fat soluble vitamins. • It can cause lipid pneumonia if it gains access to the lungs. • It is indigestible. • Which agent is used in non-infective diarrhea: • Loperamid (Imodium). • Peptobismol (Bisthmus subsalicylate) ( used in traveler's diarrhea). • Atropine (is incorporated with diphenoxylate in Lomotil to discourage abuse). • Which of the following agents block or decrease the action of penicillin: • Probenecid • Salicylate • Aluminium hydroxide • A 50 year old patient makes bowl movement 3 times / week. What do you advise him to take: • Stimulant laxative. • Advise to exercise. • Advise to take more fiber diet. • Stool softener • Drink warm water T.I.D. • Which of the following is a non-systemic laxative antacid: • Al(OH)3. c. Mg(OH)2. • NaHCO3 d. CaCO3. • A person comes to the pharmacist complaining of hard stool after every 2 – 3 days, what should be advised: • Stool softener c. Warm water • Fiber diet d. Dulcolax • Gastric antacids inhibit (delay) the absorption of iron : a. Fe 2+ Fe 3+ thus $ absorption. • For a patient with gastric ulcer, antacids should be given : • 1 hr before meals & 3-4 hrs afterwards & at bed time. • Maximum 7 times a day

  39. Which f the following antacids causes rebound acidity: • CaCO3b. Na2CO3 c. NaHCO3 • Hexyl resorsinol (an antiseptic) is better adsorbed (more powerful) than resorsinol because: • It has larger molecular size. • It has a higher O/W partition coefficient. • All of the following can increase gastric secretions except: • Stomastatin ($ gastric secretions). b. Protein. • All of the following drugs can be given with or without food except: • Sucralfate (must be given on empty stomach with plenty of water). • Which drugs must be given with plenty of water: • Allopurinol b. Fosimax c. Cotrimoxazole. • The antacid used in hyperphosphatemia is: • Al(OH)3. c. Mg(OH)2. • Excessive antacid use will lead to: • Rebound hyperacidity (Xss antacid  # pH of stomach  # release of gastrin  # HCl release  # acidity) • Chronic use of Al(OH)3 will lead to: a. Hypophosphatemia. b. Hyperphosphatemia • Mg trisilicate is used as: • A laxative (similar to MgSO4 & Mg(OH)2 • What is true about mineral oil: • Chronic use  $ absorption of fat soluble vitamins. • Used as a laxative. c. Sterilized by dry heat • Has slow absorption from the GIT. • Acne is treated by: • Benizone Gel. c. Persagel • Benzagel d. Desquan ??? • Which of the following agents is bacteriostatic not bactericidal: • Boric acid c. Iodine • Trichloro-ethanol d. Benzalkonium chloride • Emetrol is: • Phosphate / carbohydrate solution containing levulose & dextrose & ortho phosphoric acid with controlled pH. • Used to treat motion sikness • Given 15 – 30 ml q 15 min not more than 7 doses.

  40. Disorders of the Thyroid Gland • Hyperparathyroidism (Paget’s disease): leads to decreased Ca metabolism  increased decalcification of bone, hypercalcemia & hypophosphatemia, thus: • Stimulation of osteoblasts, osteocytes, chromocytes  bone dystrophy It is treated with Calcitonin to decrease Ca++ in blood • Hypoparathyroidism: is a metabolic disorder of Ca metabolism in which serum Ca levels of patient $ (hypocalcemia), & serum phosphate levels # in an inversely proportional manner. • Grave’s Disease: (hyperthyroidism) characterized by exophthalmoses & enlargement of thyroid; treated by antithyroid drugs (thiouracil, propyl thiouracil, methimazole, carbimazole) • Mechanism of action of anti-thyroid drugs: • Inhibit organ function – Inhibit oxidation of I2. • Inhibit coupling of iodo-tyrosine to free tyrosine • Inhibit periferal deiodination of T4 T3 • Conditions leading to hyperthyroidism include: • Graves Disease (Diffuse toxic goiter) • Plummer’s disease (Nodular toxic goiter) • Multi-nodular toxic goiter • Tri-iodo-thyronine toxicosis (T3 toxicosis) • Elderly patients with chronic disease should be screened for thyroid disease. • Myxodema (Gull’s Disease): is a disease due to hypothyroidism & is treated by L-thyroxin (Eltroxin, Synthroid) or desicated thyroid preparation (less common). • Hashimato’s thyroiditis is a cause of hypothyroidism. • The dose of L-thyroxin is determined by: • Age, weight, height. – Duration of hypothyroidism • Pretreatment TSH levels. – Presence of other chronic disease • Myxodema is characterized by: • Skin dryness c. Slow pulse e. Impaired mental function • Loss of hair d. Low body temp • Myoxedema coma: is a life threatening condition of hypothyroidism, treated by a loading dose of L-throxin (400 mg IV bolus) followed by oral iodo-thyronine 25mg OD till the patient improves, hence shift to oral L-thyroxin. • Lugol’s I2: a strong I2 solution taken orally as a preoperative preparation for thyroidoctomy. It inhibits the synthesis of iodotyrosine, iodothyroxin & antagonizes the effect of thyrotropine on endocytosis, proteolysis & thyroid hormone secretion. • Euthyroid: refers to a person with normal thyroid function.

  41. Which of the following disorders is related to hypothyroidism: • Cushing syndrome. (Increased secretion of cortisone) • Addison disease. (decreased secretion of cortisone) • Grave disease (Increased thyroxin secretion  exophthalmoses) • Myasthenia gravis (decreased secretion of acetylcholine) • Myxodema or Gull’s disease(decreased thyroxin secretion) • Mechanism of action of methimizole: • Inhibits iodination of tyrosine & mono-iodotyrosine • Inhibits coupling of iodotyrosines • Hypothyroidism is due to: • Treatment with I 131 c. Grave’s disease • Hashimato’s goiter • Calcitonin: • Decreases Ca in blood b. Increases Ca in blood • Hyperparathyroidism (Paget’s disease) leads to: • Decreased Ca & increased P in blood • Increased Ca & decreased P in blood (treated with calcitonin) • Thiouracil is used to treat: • Graves’ disease b. Jodbasedow’s disease ??? • Plummer’s disease • Mechanism of action of propyl thiouracil: • Inhibits organification of iodine • Inhibits conversion of T4 T3 • Inhibits encoupling of iodotyrosine to free thyroxin

  42. Bronchial Asthma • Selective b2 Stimulants (also known as adrenergic anti-histaminics): • Salbutamol (Ventoline) – Terbutaline (Bricanyl) – Albuterol • These, being selective are better agents than isoprotrenol in treating bronchial asthma. • Isoprotrenol (Isoprenaline), a non-selective b-agonist, stimulates the heart  cardiac arrest / cardiac shock. It has no a-agonist effect. • Cromolyn disodiumor cromoglycate sodium (Intal inhaler): • Stabilizes the sensitized mast cells  $ histamine release. • Not effective in acute asthmatic attacks • Is used as a prophylactic agent in asthma • Is used in chronic asthma as adjuvant to cortisone • Is used as a prophylactic agent in allergic rhinitis. • Choledyl: is a partially enteric coated theophylline. • H1 receptor antagonists (antihistaminics): are used to treat asthma & nausea. • In acute asthma (status asthmaticus) & anaphylactic shock adrenaline is used. • Epinephrine is vasoconstrictor if used locally, it is a bronchodilator if injected SC  it is the drug of choice for allergy-induced bronchospasm. • What is the drug of choice in allergy-induced bronchospasms? a. Adrenaline b. Sodium cromoglycate • What is the drug of choice in acute asthma? a. Adrenaline b. Salbutamol (or albuterol) • Episodic cough & wheezing that improves on treatment is: a. Asthma b. Chronic bronchitis • All the following factors affect asthma except: a. Food additives c. Staying away from dust c. Taking inhalation regularly • Asthma is triggered by: a. Smoke c. Stress c. Fresh painting d. Cold weather • Cromylene disodium is used as: a. A prophylactic agent in allergic rhinitis • Shake well before use is a direction for: a. Flovent c. Pulmicort (Pulmihaler) c. Ibrotonium (Atrovent)

  43. A patient on fluticasone (Flexonaze) & salmetrol has worsened asthma, advise him to: a. Take oral cortecosteroids c. Take inhaled corticosteroids b. Take ibratonium • Antiasthmatics (adrenergic antihistaminics) are mainly: a. B2 agonists b. B2 antagonists • Episodic cough & wheezing that improves on treatment is: a. Asthma b. Chronic bronchitis • All the following factors affect asthma except: a. Food additives c. Staying away from dust c. Taking inhalation regularly • Asthma is triggered by: a. Smoke c. Stress c. Fresh painting d. Cold weather • Cromylene disodium is used as: a. A prophylactic agent in allergic rhinitis • Shake well before use is a direction for: a. Flovent c. Pulmicort (Pulmihaler) c. Ibrotonium (Atrovent)

  44. Vitamins & Minerals • Vitamin B complex: Consists of vitamin B1 (thiamine) + B2 (Riboflavin) + B6 (Pyridoxine) + B12 ( cyanocobolamine). • Macrocytic Megaloplastic Anemia is treated by: vitamin B12 & folic acid. • Perinaceous anemia: failure of vitamin B12 absorption due to lack of gastric intrinsic (Castle) factor (secreted by parietal cells of stomach & essential for absorption of B12 – the extrinsic factor). Castle’s factor binds with ingested B12, preventing its destruction in the upper GIT. • Parietal cells of the stomach secrete HCl & intrinsic factor. • Perinaceous (Addisonian) anemia is treated by vitamin B12 (IV, IM or deep SC injection). • Folic acid is never given alone to treat perinaceous anemia (as it will mask the symptoms). • Vitamin C, EDTA & Na bisulfite are used as antioxidants in aqueous solutions (EDTA is a chelating agent for heavy metals). • Vitamin E (or alternatively butylated hydroxy toluene) is used as antioxidant in oily solutions. (Anti-oxidant = reducing agent). • Chronic use of mineral oil decreases absorption of fat sol. vitamins a hypovitaminosis. • Vitamin K occurs in 2 forms: • Vitamin K1 = phytonadione  natural from plant origin. • Vitamin K2 = Menaquinione  natural (synthesized by G +ve bacteria). • Vitamin K3 = Menadione  synthetic, water soluble. • Warfarin inhibits vitamin K synthesis. • Carotene: is the precursor of vitamin A (Retinol). • Vitamin A (retinol): is useful in the treatment of acne vulgaris. • 13 trans-retinoic acid is used topically in the treatment of acne vulgaris. • 13 cis-retinoic acid is used orally in the treatment of acne vulgaris. • Vitamin D is important for the regulation of Ca++ & P metabolism (# Ca, $ P) similar to the parathyroid hormone. This action is opposed by calcitonin, which is used to treat hyperparathyroidism.

  45. Iron • Iron deficiency (& lead toxicity) leads to: • Microcytic anemia (small RBCs). • Hypochromic anemia (low hemoglobin content). • Imferon: is an iron-dextran injection (ferric hydroxide) for the treatment of iron deficiency anemia resistant to oral iron administration. • Iron deficiency anemia: is more prevalent in females. • The best dose for iron deficiency is: 300 mg / day IM (imferon) for 6-12 months • Continue oral therapy after remission for 6 – 12 months. • Iron will cause black discoloration of the stool. • Iron: after oral administration is absorbed from the duodenum by an active transport process. • Vitamin C is added to iron preparations to enhance its absorption & also as a reducing agent to maintain iron in the soluble ferrous state & to form a soluble absorbable chelate with iron in the ferric state. • Antacids $ GIT absorption of iron, thus it is advisable to take the iron preparation 1 hr before the antacid. Lower pH (acidity) of the intestine favors iron absorption. • Hemochromatosis: is the excessive storage of iron in parenchymal tissue  tissue damage, bronzy skin, cirrhosis, diabetes mellitus. Potassium • KCl is an obvious substitute for NaCl since: d It has the same salty taste. d It is crystalline. d It is an electrolyte that already exists in the body. • KCl is contraindicated in severe kidney disease & oligurea. It is not given by IV bolus (IV injection of high conc. of KCl may cause cardiac arrest). • Symptoms of Na depletion include weakness, nausea & muscle cramps. • Slow K: is a potassium source. It is composed of KCl embedded in wax matrix. • Koachlor, Kaon & Kayciel are potassium sources too. • Isochlor: is not a K source. It contains 2 mg chlorpheniramine maleate + 12.5 mg pseudo-ephedrine HCl / teaspoonful. It is used in URTIs & bronchial congestion.

  46. Which of the following agents is keratolytic (in acne treatment): • Retinoic acid. c. Retinol. • Vitamin C. • Symptoms of perinaceous anemia are treated by: • Folic acid b. Iron preparation. • Vitamin B12 IM / IV or SC • Acne is treated by : • Retinoic acid • Retinol • Tocopherol acetate (Vitamin E) • In iron deficiency anemia which is not true: • More prevalent in females. • Over dose can cause liver damage. • Causes microcytic, hypochromic anemia. • Oral iron preparations are better than parentral ones. • Oral iron preparations are similar parentral ones. • Which vitamin is occasionally used as an anti-oxidant: • Vitamin D d. Vitamin E • Vitamin K e. Vitamin B3 • Vitamin B1 • Which vitamin is necessary for collagen synthesis: • Vitamin D c. Vitamin C • Vitamin K d. Vitamin A • Vitamin A deficiency results in: • Keratinizationb. Night blindness • Vitamin D important for: • Regulation of Ca & phosphorus levels in the body (it acts as a hormone) • The intrinsic factor (glycoprotein) that helps in vitamin B12 absorption is secreted from: • Pareital cells b. Globet cells • What is the effect of antacids on iron absorption: • Decreases absorption b. Increases absorption. • What is the effect of Vitamin C on iron absorption: • Decreases absorption b. Increases absorption.

  47. Which vitamin acts as a para-hormone: • Vitamin D3. b. Vitamin A. c. Vitamin C. • Which vitamin contains a quinone structure: • Vitamin D b. Vitamin E c. Vitamin K. • The Structure of nicotinic acid is: • Pyridine ring b. Purine ring c. Pyrimidine ring • Which form of vitamin E is the most active as an anti-oxidant: • Alpha. b. Beta c.Delta. • Smokers suffer from deficiency of: • Vitamin D b. Vitamin C c. Vitamin E • Which is not true about vitamin D3: • Hydroxylation at C25 occurs in the liver. • Hypercalcemia occurs due to all except: • Granulomatous disease b. #ed exposure to sun light (# vitamin D) • Vitamin E deficiency results in: • Anemia in neonates. • Large doses of iron leads to: • Liver collapse • Thiamine (Vitamin B1) deficiency leads to: • Beriberi b. Nerve degeneration. • Breast fed children need which vitamin as a supplement: • Vitamin Drops. • Which is true about vitamin K: • Is deficient in new born • Is essential for synthesis of clotting factors II, VII, IX, X • Is essential for protein synthesis & transformation • Which is true about vitamins: • Inorganic nutrients • Organic nutrients that act as co-enzymes in metabolic processes • Which mineral (metal) is present in the body in largest amount: • Mg c. Zn • Fe d. Cu

  48. Obstetrics & Gynecology • Terratogenisity is critical at week 3-8, 1st trimester (fetus resists terratogenisity  day 1-20). • Terratogenic drugs  damage to embryo: CNS, eyes, axial skeleton, lower limbs & heart. • The placenta is fully functioning in 2nd week, umbilical cord is formed at the 2nd – 3rd week. • There is no direct communication between mother’s blood & fetus. • Blood supply to the fetus is through the umbilical artery  providing nutrients. • Micronor is a contraceptive containing progestin only. It is administered daily & continuously so long as contraception is required. • Ovral is a combination of estrogen + progestin & is administered on a cyclical regimen for 21 days starting from the 5th day of the menstrual cycle. • Progesta-sert system: is an intra-uterine device (IUD) inserted in the uterus as a contraceptive. It undergoes zero-order release of progesterone for a 1 year period. • Estrogens in contraceptive pills: may cause embolism (thrombus formation). • Smoking with oral contraception may aggravate embolism. • Benefits with contraceptive pills use outweigh the risks: Benefits: Protection from the risk of pregnancy. Protection against iron deficiency anemia. Alleviation of dysmenorrhea. $ incidence of ectopic pregnancy. Alleviation of premenstrual tension. $ incidence of benign breast disease. Alleviation of heavy & irregular menses. $ incidence of ovarian & endometrial cancer. Protection from pelvic inflammatory disease due to thickening of cervical mucous secretion. Stronger uterine contraction prevent ascend of bacteria in uterus & fallopian tube. Risks: CV complications (venous thrombosis, IHD, cerebral stoke) • Diethyl Stelbesterol (estrogen): is used in treating senile vaginitis. • Premature labor: may be prevented by using terbutaline (Bricanyl), a sympathomemetic b2 selective agonist. • PGE2 + tamoxifen (Nolvadex) (anti-estrogen) are used to terminate pregnancy. • Pregnant women with deep venous thrombosis (DVT): can be treated only with heparin (also used in prophylaxis of thrombosis & arterial embolism); warfarin is contraindicated. • Factors affecting drug excretion in breast milk: • PKa – Partition coefficient. – Nursing schedule. • Lipid solubility. – Conc. of the drug.

  49. Obstetrics & Gynecology • The main source of newborn eye infections is from the vagina (Chlamydia)  ttt AgNO3. • Corpus albican: is a mass of fibrous tissue that replaces the regressing corpus luteum following rapture of the graffian follicle. It forms a white sac which gradually decreases in size & finally disappears. • Corpus albican: is present in non-pregnant women of child bearing age. • Corpus luteum: is present in pregnant women. Geriatric Patients • In elderly patients there is a decrease in: • Cardiac output & Creatinin clearance & GFR. • Total body fluids. • Blood flow to various organs. • Plasma albumin conc. (although total plasma protein conc. does not change significantly). • Muscle mass & brain weight. • Kidney, spleen, pancreas, lungs & liver become smaller. • Blood vessels lose elasticity. Dehydration • Lytren: is an orally administered electrolyte solution containing dextrose (or glucose), K, Na, Ca, Mg & Cl. It is used to supply glucose & electrolytes in balanced proportions in order to avoid serious deficits from occurring in patients suffering from mild-to-moderate fluid loss.

  50. Anti-estrogens include: • Clopiphene b. Tamoxifen (also anti-cancer) • In post-menoposal therapy, : • Conjugated estrogen carries the risk of endometrial cancer. • Progesterone combined with estrogen reduces the chance of cancer. • Progesterone alone is effective but does not help vaginal itching & dryness. • When corpus albicans is found in the uterus, it can be said that • Woman is of child bearing age (Non-pregnant). • Woman is at puberty. • Woman is experiencing menopause. • Woman is pregnant. • What is Gravida: • It is the number of times a woman became pregnant. • What is the role of estrogen & progestins in managing post-menopausal symptoms esp. with respect to bleeding: • Estrogen reduces bleeding. b. Progestins reduce side effects. • In menopause, The management therapy includes: • Conjugated estrogen 0.3 – 1.25 mg/day. • During ovulation the secreted hormones include (reach maximum level): • FSH. b. LH. • During Fertilization which of the following hormones has maximum effect: • # levels of progesterone & estrogens (stimulate human chorionic gonadotropine). • Oral contraception is contra-indicated in all except: • Breast cancer d. Pregnancyg.Hypertension • Deep venothrombosis e.Depression h. Diabetes • Liver cirrhosis f. Seizures / Epilepsy • Conjugated estrogens carry the risk of: • Endometrial cancer • Progestrone reduces the risk of estrogen • Progestrone affects blood vessels but is not effective in vaginal hypertrophy • All of the following parameters may decrease in elderly patients except: • Serum Creatinine c. BUN e. Skin hydration • Albumin d. GFR f. Lean body mass