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Cholinergics / anticholinergics and drugs affecting the endocrine system. By Linda Self. Cholinergics. PNS Receptors Acetylcholine Direct and indirect acting cholinergic drugs. Direct acting cholinergics. Urecholine Actions— indications. Indirect acting agents. Affect cholinesterase

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cholinergics
Cholinergics
  • PNS
  • Receptors
  • Acetylcholine
  • Direct and indirect acting cholinergic drugs
direct acting cholinergics
Direct acting cholinergics
  • Urecholine
  • Actions—
  • indications
indirect acting agents
Indirect acting agents
  • Affect cholinesterase
  • Neostigmine ( prostigmine) is prototype
  • Mestinon (pyridostigmine) is drug of choice for MG
  • Tensilon(edrophonium)diagnostic agent
  • Antilirium (physostigmine)only agent that crosses blood brain barrier
  • Aricept (donepazil)—use in AD
cholinergic and myasthenic crises
Cholinergic and Myasthenic crises
  • Difficult to distinguish
  • Treatments differ
  • Myasthenic crisis requires more medication, cholinergic crisis requires less
  • Distinguished by the timing of s/s—within one hour of anticholinesterases, likely cholinergic excess. If within three hours, myasthenic problem.
  • Cholinergic crisis-Tx supportively, atropine, decrease anticholinesterase med
  • Myasthenic-Supportive treatment and increase of anticholinesterase med
  • (testing may require intubation and ventilator assist)
organophosphate poisoning
Organophosphate poisoning
  • Tabin, Sarin—nerve gases
  • Insecticides—malathion, parathion
  • Decontaminate—clothing, flushing with water, activated charcoal and lavage
  • Atropine for muscarinic effects—hypersalivation, urination, defecation, laryngospasm)
  • Protopam (pralidoxime) for nicotinic effects –causes poison to release enzyme cholinesterase
slide7
AD
  • Use reversible indirect acting cholinergics
  • Aricept (donepezil)does not cause liver toxicity. Can cause n/v, bradycardia, PUD, exac. of asthma
  • Razadye (galantamine)-long acting
  • Exelon (rivastigmine)
  • Cognex (tacrine)– more hepatototoxicity
anticholinergics
Anticholinergics
  • Most affect muscarinic receptors in brain, secretory glands, heart and smooth muscle
  • Few affect nicotinic receptors, e.g., Robinul (glycopyrolate)
  • Effects of anticholinergics are diffuse
  • Indications—GI (gastritis, UC, irritable bowel; GU antispasmotic in overactive bladder; ophthalmology for exams, glaucoma; respiratory for bronchodilation; cardiology to increase heart rate
  • Antilirium for overdose of anticholinergics
anticholinergics9
Anticholinergics
  • Atropine
  • Atrovent
  • Scopolamine—antiemetic, motion sickness
  • Spiriva (tiotropium)
  • Bentyl (antiscretory/antispasmotic)
  • Cogentin
  • Trihexy (Parkinson’s)
corticosteroids hematopoietic immunizing immunosuppressive agents and drugs used in oncology
Corticosteroids; Hematopoietic, Immunizing, immunosuppressive agents and drugs used in oncology
immunity
Immunity
  • Defense
  • Specificity, memory and inducibility
  • Normal immunity –ability to recognize self and non-self
  • Recognition of epitopes (distinctive molecules on non-self antigens)
  • Underactive=immunodeficiency
  • Overactive=autoimmune diseases
immunity12
Immunity
  • Natural
  • Acquired immunity—active or passive (antibodies are transferred)
  • Cellular—involving activated T cells
  • Humoral—involves B cells and antibodies
  • All antigens elicit both types
immunizations
Immunizations
  • Administration of antigen to induce antibody formation (active) or serum from immune people (passive)
  • Regulated by US FDA
active immunity
Active Immunity
  • Vaccines and toxoids
  • Vaccines are suspensions of microorganisms or antigenic products
  • Toxoids are bacterial toxins that have been modified to retain antigenic properties, not permanent
indications for active immunity
Indications for active immunity
  • Give before exposure to actual illness
  • Diphtheria,tetanus, pertussis, hemophilus influenza (Hib) , inactivated polio vaccine, pneumococcal (PCV), hepatitis A and B, varicella, MMR, PPV, MC4, influenza
  • Some combinations
contraindications to use of agents for active immunity
Contraindications to use of agents for active immunity
  • Febrile illnesses
  • Immunosuppressed
  • Immunodeficiency states
  • Leukemia
  • Lymphoma
  • In pregnancy
  • If generalized malignancy
passive immunity
Passive Immunity
  • Immune serums are biologic products used for passive immunity
  • Temporary
  • Agents: cytomegalovirus immune globulin, hepatitis B immune globulin, rabies immune globulin, rubella, tetanus immune globuline, varicella zoster, RSV immune globulin, tetanus immune globulin
key points in immunizations
Key Points in Immunizations
  • Women of childbearing age should not get pregnant for three months after receiving Rubella immunization
  • Influenza-may start at 6 months; annually in those over 65
  • Tetanus toxoid—after initial immunization, give every ten years
  • Children with HIV—should not receive live vaccines
  • Pneumococcal at 65; may repeat in five years if with chronic conditions
  • After Varicella, avoid close contact with newborns, pregnant women and immunocompromised persons
  • After immunizations, stay in area 30 minutes
hematopoietic and immunostimulant drugs
Hematopoietic and Immunostimulant Drugs
  • Cytokines or biologic response modifiers given to restore normal function or increase ability of the immune system
  • Examples: certain interferons and interleukins, colony stimulating factors
definitions
Definitions
  • Cytokines—substances produced by bone marrow cells, regulate cellular activities; are the key components in producing hematopoietic and immunostimulant drugs
  • Interferons—glycoproteins w/antiviral activity
  • Interleukins—cytokines that enable communication between leukocytes and other cells involved in inflammation or cell-mediated response. Result—maximized response to a given pathogen or foreign antigen.
hematopoietic and immunostimulant drugs21
Hematopoietic and immunostimulant drugs
  • Very powerful
  • Difficult to maintain therapeutic dosing for prolonged time
  • Can have untoward and unanticipated side effects
  • Can act as antiproliferative and immunoregulatory agents; can augment natural killer cells
  • Parenteral
  • Significant side effects decreasing compliance
hematopoietic agents
Hematopoietic Agents
  • Epogen (epoetin alfa)=erythropoietin
  • Use for anemia
  • Hct 2x weekly, adjust as Hct increases to 36%
colony stimulating factors
Colony stimulating factors
  • Neupogen (filgrastim) stimulate blood cell production by marrow in patients with bone marrow transplantation or chemotherapy induced neutropenia
  • Leukine—angiogenetic, used in ischemic heart disease
interleukins
Interleukins
  • Proleukin (aldesleukin)—recombinant version if IL-2
  • Activates cellular immunity, produces TNF and inhibits tumor growth
  • For metastatic renal cell CA
  • Toxicity can cause GI bleed, dysrhythmias, resp. embarrassment
  • Contraindicated in recent organ transplantation
interferons
Interferons
  • Alfa -2a and 2b for hairy cell leukemia and Kaposi’s sarcoma
  • alfa n1 approved for chronic hepatitis C
  • Beta for multiple sclerosis
corticosteroids
Corticosteroids
  • Decrease inappropriate or undesirable immune response. Examples include: RA, SLE, asthma or suppression of transplant rejection
  • Glucocorticoids
  • Effects—catabolism, decrease immune response, decrease utilization and increase production of glucose, stabilize mast cells, affect gastric mucosa, muscle atrophy and adrenal cortex suppression
corticosteroids27
Corticosteroids
  • Prednisone is prototype
  • Celestone (betamethasone)
  • Decadron (dexamethasone)
  • Solucortef (methylprednisolone)
  • Kenalog (triamcinolone)
immunosuppressant drugs
Immunosuppressant Drugs
  • Use in concert with steroids
  • Used in autoimmune disorders
  • Newer agents modify specific components of immune response, fewer SE
  • Imuran-bone marrow depression is SE
  • Sandimmune (cyclosporine)—monitor renal and hepatic toxicity, CNS toxicity
  • Methotrexate—bone marrow suppression
  • Remicade—infusion reactions, GI upset, others
cytotoxic antiproliferative agents
Cytotoxic, Antiproliferative Agents
  • Used primarily in cancer
  • Imuran (azathioprine) antimetabolite that targets rapidly proliferating cells including T and B lymphocytes
  • Rheumatrex (methotrexate) folate antagonist. Used for cancer and for autoimmune or inflammatory disorders.
antirejection agents
Antirejection Agents
  • Sandimmune (cyclosporine)—inhibits synthesis of IL- 2 necessary for activation of T cells and B cells.
  • Rapamune (sirolimus) affects T cell activation and proliferation secondary to several interleukins
  • Prograf (tacrolimus)—prevents rejection of transplanted organs by inhibiting T lymphocytes
monoclonal antibodies
Monoclonal Antibodies
  • Remicade (infliximab). Inhibits TNF from binding to receptors. Used in RA and Crohn’s.
  • Enbrel (etanercept) TNF receptor binder. RA.
  • Arava (Leflunomide) antiproliferative and anti-inflammatory activities. Inhibits pyrimidines needed for RNA and DNA synthesis. RA.
drugs affecting the endocrine system
Drugs affecting the Endocrine System

Review of Endocrine system

  • Hypothalamus—releasing hormones that affect both anterior and posterior pituitary
  • Ant. Pituitary---GH, ACTH, TSH, FSH, LH, Prolactin, melanocyte stimulating hormone
  • Post. Pituitary—ADH, oxytocin
  • Adrenals
  • Thyroid
  • pancreas
hypothalamic hormones
Hypothalamic hormones
  • Generally parenteral or intranasally, broken down in GI system
  • Equivalent to gonadotropin releasing hormones
  • Factrel (gonadorelin)—used for diagnostic testing of gonadotropin function
  • Zoladex (goserelin)—reduces hormonal levels so useful in metastatic breast cancer, prostate cancer and in endometriosis
  • Lupron (leuprolide)-advanced prostate cancer, central precocious puberty, endometriosis, uterine fibroids
hypothalamic hormones34
Hypothalamic hormones
  • None of the GnRH equivalents can be given orally
  • Factrel (gonaderelin) diagnostic testing
  • Lupron( leuprolide)decreases estrogen and testosterone levels
  • Zoladex (goserelin) decreases estrogen and testosterone levels
  • Sandostatin (octreotide)—somatostatin. Decreases GH, decreases GI secretions and motility. Given in severe diarrhea as well as with acromegaly.
anterior pituitary hormones
Anterior Pituitary Hormones
  • Cosyntropin (corticotropin)-diagnostic test of adrenal function
  • Protropin (somatrem)—synthesized growth hormone. Promotes growth in those deficient in GH or in renal failure. Tissue wasting with AIDS.
  • Chorex (HCG)—synthetic LH. Diagnostic test of testosterone production, cryptorchidism
  • Pergonal (menotropins)—preparation containing both LH and FSH. Usually combined with HCG to induce ovulation.
anterior pituitary hormones36
Anterior Pituitary Hormones
  • Thytropar (thyrotropin)—used as diagnostic agent to distinguish between primary and secondary hypothyroidism
  • Humatrope (somatropin) for children with GH deficiency. Not effective in epiphyseal closure. Tissue wasting of AIDs
posterior pituitary hormones
Posterior Pituitary Hormones
  • DDAVP (desmopressin) and Pitressin (vasopressin) are synthetic equivalents of ADH. Useful in diabetes insipidus.
  • Parenteral desmopressin used as hemostatic agent in hemophilia and Von Willebrand’s Disease. Tx of bleeding esophageal varices.
  • Pitocin (oxytocin) promotes uterine contractility. Used in induction of labor and to control postpartum bleeding.
drugs used for calcium and bone disorders
Drugs used for Calcium and Bone Disorders
  • Bisphosphanates—Fosamax (alendronate), Actonel (risedronate) and Zometa (zoledronic acid)
  • Bind to bone, inhibit calcium resorption
  • Take on empty stomach, with water, 30 minutes before other intake
  • Calcimar, Miacalcin (calcitonin-salmon) for hypercalcemia, Paget’s Disease, and osteoporosis. Slows bone resorption, may be helpful with bone pain.
drugs used for calcium and bone disorders39
Drugs used for calcium and bone disorders
  • Symptomatic hypocalcemia, calcium gluconate
  • Oral calcium preparations for osteopenia or nutritional deficiency
  • Corticosteroids—inhibit cytokine release by cytolytic effects of some bone tumors, inhibit calcium absorption from intestine and by increasing calcium excretion in urine. Used in hypercalcemia due to malignancies or Vitamin D intoxication
drugs used for calcium and bone disorders40
Drugs used for calcium and bone disorders
  • Estrogens most beneficial immediately after menopause. Decrease bone breakdown, increase calcium absorption from gut and increase calcitriol.
  • Evista (raloxifene) and Nolvadex (tamoxifen) act like estrogen in some tissues and prevent the action of estrogen in other body tissues
  • Evista is classified as a selective estrogen receptor modulator and is approved for postmenopausal osteoporosis.
calcium and bone disorders
Calcium and bone disorders
  • Nolvadex (tamoxifen) is classified as an antiestrogen. Used to prevent and treat breast cancer. Also has estrogenic effects so can be used to prevent osteoporosis
  • Forteo (teriparatide)—recombinant DNA version of parathormone. Increases bone formatin by increasing osteoblasts. Increases serum levels of calcium and calcitriol. Not known to cause deposition of calcium in soft tissues
  • Vit D 400 IU for 6months to 24 years; 200IU/day 25 years and older
  • Lasixcauses increased excretion of calcium
adrenal agents
Adrenal Agents
  • Adrenal cortex produces glucocorticoids, mineralocorticoids and adrenal sex hormones
  • Hydrocortisone is prototype
  • Florinef (fludrocortisone)—only mineralocorticoiddescribed in text
pearls
Pearls
  • Thiazide diuretics contraindicated in hypercalcemia as decrease urinary excretion of calcium
  • Look at albumin levels when examining calcium levels
  • Children on growth hormone, ht. and wt. chart weekly, follow epiphyseal closure
  • Dietary calcium is superior to supplemental
  • Menopausal women should have 1000 mg of calcium daily
pearls44
Pearls
  • Vasopressin-watch for water intoxication, chest pain, MI
  • Oxytocin can result in uterine rupture
  • Octreotide can cause arrhythmias, bradycardia, hyperglycemia, injection site pain and symptoms of gallstones
acute hypercalcemia
Acute hypercalcemia
  • Medical emergency
  • For severe s/s or level >12mg/dL. Rehydrate
  • IV saline
  • Lasix
  • Fosamax or Zometa
  • Monitor serum calcium levels
  • Calcium channel not so effective
thyroid and antithyroid drugs
Thyroid and antithyroid drugs
  • Thyroid produces thyroxine, triidothyronine and calcitonin
  • Thyroxine is called T4 (has 4 atoms of iodine)
  • Triidothyronine has 3 atoms of iodine so is called T3
thyroid
Thyroid
  • Essential for normal G&D
  • Critical for brain development and maturation
  • Increases rate of cellular metabolism and oxygen consumption
  • Increases heart rate, force of contraction and cardiac output
  • Increases fat metabolism including cholesterol
  • Inhibition of pituitary secretion of TSH
thyroid disorders
Thyroid Disorders
  • Goiter—enlargement of thyroid due to lack of iodine in diet; thyroiditis, tumors, hyper or hypo function of the thyroid
  • Compensate for iodine deficiency, pituitary secretes more TSH; thyroid enlarges producing more hormone, possibly effecting a normal hormone level
  • Correction of goiter involves replacing iodine; replacement of thyroid hormone. May have regression or may need excision
hypothyroidism
Hypothyroidism
  • Occurs secondary to disease or destruction of the thyroid
  • Causes: Hashimoto’s thyroiditis, previous exposure to radiation, treatment with amiodarone, lithium or iodine
hypothyroidism50
Hypothyroidism
  • Congenital=Cretinism; may occur with lack of iodine in mother’s diet. S/S in infancy, can result in severe mental retardation
  • Hypothyroidism may be subclinical but may progress.
  • S/S initially vague but become more pronounced: cold intolerance, fatigue, aches and pains, puffy appearance, mental sluggishness, anemia, bradycardia
  • Tx-exogenous thyroxine
  • Replacement indicated if TSH is >10 microunits/L
hypothyroidism51
Hypothyroidism
  • Myxedema coma
  • Characterized by hypothermia, cardiovascular collapse, coma, hyponatremia, hypoglycemia, and lactic acidosis
  • Predisposing factors include: cold, infection, CNS depressants
  • Tx—synthetic levothyroxine is drug of choice.
  • In myxedema coma, Tx will be given IV.
hyperthyroidism
Hyperthyroidism
  • Characterized by excessive secretion of thyroid hormone
  • May be associated with overtreatment with thyroid drugs, nodular goiter, thyroiditis, functioning thyroid cancer, pituitary adenoma resulting in excess TSH secretion
  • Subclinical hyperthyroidism is defined as reduced TSH (below 0.1 microunit/L) and normal T3 and T4 levels
  • Greatly increases the risk for atrial fibrillation
hyperthyroidism53
Hyperthyroidism
  • Thyroid storm or thyrotoxic crisis is a severe complication. Will result in: severe tachycardia, fever, dehydration, heart failure and coma
  • Tx depends on cause. May need surgery or radioactive iodine therapy
  • Antithyroid drugs include Propylthioruracil (PTU)and Tapazole (methimazole), and iodine preparations
drugs used in hypothyroidism
Drugs used in hypothyroidism
  • Synthroid, Levothyroid (levothyroxine)—synthetic T4. Offers uniform dosing and potency.
  • Euthroid and Thyrolar (Liotrix) contains both levothyroxine and triiodothyronine in a 4:1 ratio approximating natural thyroid hormone
drugs used in hyperthyroidism
Drugs used in hyperthyroidism
  • PTU is prototype of thioamide antithyroid drugs
  • Can be used alone or in combination with thyroidectomy and in Tx of thyrotoxic crises
  • Acts by inhibiting conversion of T4 to more active T3. Does not affect thyroid stores. Short acting requiring TID dosing.
drugs used in hyperthyroidism56
Drugs used in hyperthyroidism
  • Tapazole (methimazole)---similar to PTU
  • Lugol’s (strong iodine solution) and saturated solution of potassium iodide (SSKI)—these drugs inhibit release of thyroid hormone, causing them to accumulate in the gland
  • Lugol’s decreases the size and vascularity of the thyroid before thyroidectomy
  • Iodine preparations should not be followed by PTU, Tapazole or radioactive iodine. The latter drugs cause release of stored thyroid and can precipitate crisis.
sodium iodide 131
Sodium Iodide 131
  • Radioactive isotope of iodine. Thyroid picks up the isotope from circulating blood. Act by emitting beta and gamma rays. Rays destroy thyroid tissue and decrease production of thyroid hormones. Also used for diagnosis and in the treatment of cancer.
  • Usually given in a single dose as outpatient. No special precautions. May be months before therapeutic effect. During this time, on maintenance medications.
  • Iodine preparations and thioamideantithyroid drugs are contraindicated during pregnancy. Can result in goiter and hypothyroidism in fetus or newborn.