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Cholinergics / anticholinergics and drugs affecting the endocrine system

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 / anticholinergics and drugs affecting the endocrine system

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  1. Cholinergics/anticholinergics and drugs affecting the endocrine system By Linda Self

  2. Cholinergics • PNS • Receptors • Acetylcholine • Direct and indirect acting cholinergic drugs

  3. Direct acting cholinergics • Urecholine • Actions— • indications

  4. 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

  5. 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)

  6. 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

  7. 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

  8. 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

  9. Anticholinergics • Atropine • Atrovent • Scopolamine—antiemetic, motion sickness • Spiriva (tiotropium) • Bentyl (antiscretory/antispasmotic) • Cogentin • Trihexy (Parkinson’s)

  10. Corticosteroids; Hematopoietic, Immunizing, immunosuppressive agents and drugs used in oncology

  11. 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

  12. 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

  13. Immunizations • Administration of antigen to induce antibody formation (active) or serum from immune people (passive) • Regulated by US FDA

  14. 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

  15. 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

  16. Contraindications to use of agents for active immunity • Febrile illnesses • Immunosuppressed • Immunodeficiency states • Leukemia • Lymphoma • In pregnancy • If generalized malignancy

  17. 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

  18. 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

  19. 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

  20. 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.

  21. 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

  22. Hematopoietic Agents • Epogen (epoetin alfa)=erythropoietin • Use for anemia • Hct 2x weekly, adjust as Hct increases to 36%

  23. 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

  24. 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

  25. Interferons • Alfa -2a and 2b for hairy cell leukemia and Kaposi’s sarcoma • alfa n1 approved for chronic hepatitis C • Beta for multiple sclerosis

  26. 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

  27. Corticosteroids • Prednisone is prototype • Celestone (betamethasone) • Decadron (dexamethasone) • Solucortef (methylprednisolone) • Kenalog (triamcinolone)

  28. 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

  29. 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.

  30. 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

  31. 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.

  32. 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

  33. 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

  34. 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.

  35. 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.

  36. 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

  37. 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.

  38. 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.

  39. 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

  40. 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.

  41. 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

  42. Adrenal Agents • Adrenal cortex produces glucocorticoids, mineralocorticoids and adrenal sex hormones • Hydrocortisone is prototype • Florinef (fludrocortisone)—only mineralocorticoiddescribed in text

  43. 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

  44. 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

  45. 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

  46. 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

  47. 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

  48. 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

  49. Hypothyroidism • Occurs secondary to disease or destruction of the thyroid • Causes: Hashimoto’s thyroiditis, previous exposure to radiation, treatment with amiodarone, lithium or iodine

  50. 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

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