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149 Cards in this Set
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gonadorelin (Lutrepulse)
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Gonadorelin (Lutrepulse)
Class: GnRH MOA: regulate FSH/LH pulsatile secretion Use: Central Amenorrhea (Replacement Therapy IV), Idiopathic hypogonadotropic hypogonadism AE: ovarian hyperstim, anaphylaxis Contra: Interaction: Admin: parental |
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Leuprolide (Lupron)
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Leuprolide (Lupron)
Class: GnRH analog MOA: long acting, downregulate GnRH ^decrease LH/FSH Use: ovulation supression, prostate/breast cancer, endometriosis, idiopathic precocius puberty AE: Androgen-like effects Contra: pregnancy, lactation, osteoporosis Interaction: Admin: SQ/IM |
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Goserelin (Lupron)
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Goserelin (Lupron)
Class: GnRH analog MOA: long acting, downregulate GnRH ^decrease LH/FSH Use: ovulation supression, prostate/breast cancer, endometriosis, idiopathic precocius puberty AE: Androgen-like effects Contra: pregnancy, lactation, osteoporosis Interaction: Admin: SQ/IM |
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Naferelin (Synarel)
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Nafarelin (Synarel)
Class: GnRH analog MOA: long acting, downregulate GnRH ^decrease LH/FSH Use: ovulation supression, prostate/breast cancer, endometriosis, idiopathic precocius puberty AE: Androgen-like effects Contra: pregnancy, lactation, osteoporosis Interaction: Admin: SQ/IM |
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Ganirelix (Antagon)
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Ganirelix (Antagon)
Class: GnRH antag MOA: rapid reversibile suppressor LH/FSH Use: prevent premature LH surge (control ovarian hyperstimulation) AE: ab pain, headache, ovarian hyperstimulation syndrome Contra: pregnancy, lactation Interaction: Admin: SQ |
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Sermorelin (Geref)
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Sermorelin (Geref)
Class: GHRH analog MOA: pulsatile release, stim IGF, indirect anabolic/growth promotion Use: GH def, GH def diag AE: facial flushing, N/V Contra: Interaction: drugs affect secretion GH - insulin, glucocorticoids, NSAIDS.... increase GH level - Clonidine, levodopa... decrease response GHRH - antimuscarinic drugs Admin: |
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Octreotide (Sandostatin)
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Octreotide (Sandostatin)
Class: somatostatin analog MOA: inhibit secretion GI/pit horm (more selective) Use: acromegaly, hyperfxn endocrine tumors (GI secreting, VIP secreting tumors & carcinoid tumor) AE: supress insulin release, gallstone, abd pain, diarrhea, N/V Contra: Interaction: decreased bioavailability cyclosporine.. additive beta and Ca channel blockers Admin: |
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Bromocriptine (Parlodel)
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Bromocriptine (Parlodel)
Class: D2 receptor antag MOA: inhib prolactin release - ant pit Use: hyperprolactinemia, acromegaly, parkinson's AE: N/V, dizzy, ORTHO HTN, seizures, arrhythmias, stroke Contra: sev ischemic disease, HTN, toxemia of pregnancy Interaction: drugs that increase prolactin - phenothiazine (chlorpromazine) - antag + butyrophenone (haloperidol) - antag + MAOI.... AntiHTN agent - additive hypotensive effect Admin: |
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Human chorionic gonadotropin (Pregnyl)
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Human chorionic gonadotropin (Pregnyl)
Class: Gonadotropin prep MOA: produced by placenta, isolated in urine from pregnant... contain LH Use: Infertility - Induce ovulation, hypogonadism AE: ovarian enlargement - hyperstim, thromboembolism Contra: Interaction: Admin: IM |
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Menotropin (Pergonal, Repronex)
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Menotropin (Pergonal -IM, Repronex -SQ)
Class: Gonadotropin prep isolated in urine from menopausal women (contain FSH/LH) MOA: Use: infertility - induce ovulation, hypogonadism AE: ovarian enlargment - hyperstim, thromboembolism Contra: Interaction: Admin: IM/SQ |
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Urofollitropin (Metrodin)
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Urofollitropin (Metrodin)
Class: pure FSH MOA: Use: induce ovulation in women with PCO AE: ovarian enlargment - hyperstimulation, thromboembolism Contra: Interaction: Admin: |
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Somatropin (Humatrope)
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Somatropin (Humatrope)
Class: recomb GH MOA: IGF effect longer than drug 1/2 life, slow induction/clearance IGF Use: replacement therapy 4 GH def, Turner's syndrome for girls, AIDS wasting or cachexia AE: headache, intracranial HTN, muscle pain, mild hyperglycemia, ab production to GH, leukemia Contra: when epiphyses closed Interaction: corticosteroid, sex steroid Admin: IM/SQ |
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Somatrem (Protropin)
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Somatrem (Protropin)
Class: recomb GH analog MOA: IGF effect longer than drug 1/2 life, slow induction/clearance IGF Use: replacement therapy 4 GH def, Turner's syndrome in girls, AIDS wasting or cachexia AE: headache, intracranial HTN, muscle pain, mild hyperglycemia, ab production to GH, leukemia Contra: when epiphyses closed Interaction: corticosteroid, sex steroid Admin: IM/SQ |
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Arginine Vasopressin (Pitressin)
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Arginine Vasopressin (Pitressin)
Class: made hypo, post pit horm MOA: antidiuretic, increase resorption H2O renal collecting ducts (increase bv), stim contraction vasc sm (increase bp) USE: diabetes insipidus, hemophilia A, vonWillebrands, enuresis AE: H2O INTOX, vasoconstriction Contra: chronic nephritis Interaction: (+) carbamazepine, chlorpropamide, tricyclic (increase bp HTN crisis) ...(-) Li, heparin, epi, etoh Admin: IM/SQ |
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Desmopressin (DDAVP)
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Desmopressin (DDAVP)
Class: vasopressin synthetic analog (minimal vasoconst effect than AVP) MOA: antidiuretic, increase resorption H2O renal CD (increase bv), stim contraction vasc sm (increase bp) USE: diabetes insipidus, hemophilia A,vonWillebrands, enuresis AE: H2O INTOX, vasoconstrict Contra: Interaction: (+ - inappropriate ADH - directly stimulate ADH secretion centrally by carbamazepine, chlorpropamide, tricyclic (increase bp HTN crisis) ...(- interfere with cellular axn of ADH in collecting ducts) Li, heparin, epi, etoh Admin: IM/SQ/oral/nasal *nasal drug of choice for CAD* |
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Oxytocin (Pitocin)
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Oxytocin (Pitocin)
Class: post pit MOA: released by reflex - dilation uterus/sucking USE: IV - induce/enhance uterine contract... IM - prevent postpartum hemorrhage... Nasal - stim milk letdown AE: arrhythmias, CNS stim, excessive uterine contraction, hyponatremia Contra: abn fetal presentation, premature, cephalopelvic disproportion Interaction: Admin: |
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Thyrotropin (TSH, Thyropar)
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Thyrotropin (TSH, Thyropar)
CLASS: TSH from bovine ant pit MOA: stim synthesis/release T3/T4 and I- transport USE: hypothyroid diag - diff btw primary and secondary.... thyroid carcinoma - enhance uptake of 131I by thyroid AE: N/V, headahce, fever, sinus tachy, a fib CONTRA: CAD, adrenal insuff INTERACTION: sympthomimetics - additive effect... hepatic enzyme inducers - barbs, rifampin, carbamazepine... estrogens increase levels of TBG ADMIN: IM/SQ |
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Recombinant TSH (Thyrogen)
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Recombinant TSH (Thyrogen)
CLASS: recombinant TSH MOA: stim synthesis/release T3/T4 and I- transport USE: hypothyroid diag - diff btw primary and secondary.... thyroid carcinoma - enhance uptake of 131I by thyroid AE: N/V, headahce, fever, sinus tachy, a fib CONTRA: INTERACTION: sympthomimetics - additive effect... hepatic enzyme inducers - barbs, rifampin, carbamazepine... estrogens increase levels of TBG ADMIN: IM/SQ |
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Levothyroxine Na (T4, Synthroid)
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Levothyroxine Na (T4, Synthroid)
CLASS: Thyroid hormone MOA: USE: hypothyroid, TSH suprression, nodular thyroid disease AE: headache, insomnia, diarrhea, tachy, arrythmia, wt loss, amenorrhea, fever, tremors CONTRA: heart disease, adrenal insufficiency INTERACTION: increase anticoag activity of warfarin... Increase TBG binding - estrogen, tamoxifen... Decrease TBG binding - aspirin, phenytoin, furosemide, androgens, carbamazepine... Hepatic enzyme inducers - barbs, rifampin, carbamazepine... bound by cholestyramine in GI ADMIN: |
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Liothyronine (T3 Cytomel)
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Liothyronine (T3 Cytomel)
CLASS: Thyroid hormone MOA: t1/2=1 day, faster onset, more express, need freq dosing USE: hypothyroidism, TSH suppress AE: diarrhea, wt loss, tachy, headache, tremor, arrythmias, fever, amenorrhea, insomnia INTERACTION: increase anticoag activity warfarin... increase TBG binding - estrogens, tamoxifen... decrease TBG binding - carbamazepine, aspirin, pheny, furosemide, androgens... Hepatic enzyme inducer - barb, rifampin, carbamazepine... bound by cholestyramine in GI tract |
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Liotrix (T3/T4 Thyrolar)
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Liotrix (T3/T4 Thyrolar)
CLASS: Combo thyroid horm MOA: USE: hypothyroidism, TSH suppression AE: headache, tremors, fever, tachy, arrythmias, insomnia, amenorrhea, weight loss, diarrhea CONTRA: INTERACTION: increase activity of warfarin... increase binding TBG - estrogens, tamoxifen... decrease binding TBG - aspirin, phenytoin, carbamazepine, furosemide, androgens... hepatic enzyme inducers - rifampin, carbamazepine, barb ADMIN: |
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Propylthiouracil (PTU, Propylthyracil)
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Propylthiouracil (PTU, Propylthyracil)
CLASS: Thioureylene (anti-thyroid) MOA: inhibit periph conversion T4/T3, inhibit MIT/DIT coupling, inactivate oxidized thyroid peroxidase USE: hyperthyroid, graves, hyperfxn thyroid nodules, thyroid storm (DOC) AE: headache, vertigo, edema, N/V, Rash: urticaria, puritus, alopecia CONTRA: INTERACTION: reduces response to oral anticoag, shorter life, plasma bound protein ADMIN: oral |
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Methimazole (Tapazole)
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Methimazole (Tapazole)
CLASS: thioureylene (anti-thyroid) MOA: inactivate oxidation thyroid peroxiase, inhib MIT/DIT coupling USE: hyperthyroidism, graves, hyperfxning thyroid nodules, thyroid storm AE: headache, vertigo, edema, N/V, rash: urticaria, puritus, alopecia; AGRANULOCYTOSIS, APLASTIC ANEMIA CONTRA: INTERACTION: reduces response to oral anticoag ADMIN: oral, once a day |
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Lugol's solution (Strong I-)
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Lugol's Solution (Strong I-)
CLASS: iodide solution MOA: inhib synth further secretion, [] dependent, high dose prevent incorporation I into thyroid hormone USE: hyperthyroidism, preop period in prep for surgery, thyroid storm AE: N/V, diarrhea, acneiform rash, hypersensitivity (III), angioedema, hemorrhage, induction of goiter and myxedema CONTRA: INTERACTION: alters free Li [] ADMIN: oral |
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Ipodate (Oragrafin Sodium); Iopanoic Acid (Telepaque)
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Ipodate (Oragrafin Sodium); Iopanoic Acid (Telepaque)
CLASS: Contrast agent MOA: inhib T4-->T3 in periphery, euthyroid in 3 days, suppress T4, inhib release of horm USE: hyperthyroidism and thyroid storm AE: Few - well tolerated.. resemble iodides CONTRA: toxicity in preg INTERACTION: none ADMIN: oral |
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Diatrizoate (Hypaque)
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Diatrizoate (Hypaque)
CLASS: Contrast Agent MOA: inhibit T4--> T3 periphery, euthyroid 3 days, suppress T4, inhib release of horm USE: hyperthyroidism, thyroid storm AE: few - well tolerated - sim to I CONTRA: toxicity in preg INTERACTION: ADMIN: IV |
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Potassium Iodide (Thyro-Block)
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Potassium Iodide (Thyro-Block)
CLASS: Iodide solution MOA: rapid inhib release thyroid horm, limit transport I --> thyroid, inhib MIT/DIT synth USE: hyperthyroidism, preop period for surgery, thyroid storm AE: N/V, diarrhea, acneiform rash, hypersensitivity (III), angioedema, hemorrhage, induction goiter and myxedema CONTRA: INTERACTION: alter free Li [] ADMIN: oral |
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131 I (Iodotope)
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131 I (Iodotope)
CLASS: Radioactive iodide MOA: USE: hyperthyroidism in poor surgical subjects, additional rx when subtotal thyroidectomy ineffective, toxic nodular goiter AE: high incidence delayed hypothyroidism, long rx period CONTRA: preg INTERACTION: ADMIN: |
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adjunctive therapy for thyroid? (3)
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Beta Adrenergic Antag - propanolol/atenolol antagonizes sympathomimetic effects
CCB - Diltiazem controls tachy (decrease incidence) Corticosteroids - Dexamethazone inhib periph conversion T4-->T3; antipyretic |
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ACTH regulates?
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glucocorticoids
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hypothal --(__)-- ant pit --(__)-- adrenal cortex --(__)-- negative feedback to (x3) --_____ positive feedback to (x2)
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hypothal --(_CRH_)-- ant pit --(_ACTH_)-- adrenal cortex --(_CORTISOL_)-- negative feedback to (HYPOTHAL, ANT PIT, IMMUNE SYS) --___IL-1, 2, 6, TNFa__ positive feedback to (HYPOTHAL, ANT PIT)
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__-> Glucocorticoid --(__)--> ___
how released? when released most? |
_CH_-> Glucocorticoid --(11-B OH IN MITOCH)--> CORTISOL
pulsatile release highest levels in morning |
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metabolic axns of glucocorticoids
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increase glycogenolysis, gluconeogenesis, protein catabolism... decrease protein synth, osteoclast formation & activity, Ca absorption in GI tract, TSH secretion
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physical axn of glucocorticoids
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anti-inflamm (decrease production PG, cytokine, IL)
decrease prolif and migration of lymphocyte and macrophages *inhibit accumulation neutrophils and monocytes at infection site and suppress activity |
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Cortisol, Hydrocortisone (Cortef)
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Cortisol, Hydrocortisone (Cortef)
CLASS: short acting glucocort MOA: USE: *REPLACEMENT THERAPY* replace cortisol hyperfxn (cushing, congenital adrenal hyperplasia); hypofxn (addisons)... anti-inflamm (allergic rxn, infection, transplants... adjuvant... diagnostic dexamethasone suppression, fetal lung maturation AE: suppress HPA; increased physiological response CONTRA: INTERACTION: many ADMIN: IM/IV/ORAL |
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Prednisone (Deltasone); Prednisolone (Delta-Cortef)
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Prednisone (Deltasone)
CLASS: intermed acting glucocort MOA: USE: *INFLAMMATION* replacement, anti-infl... collagen dz, vasculitis, GI inflammatory dz, renal autoimmune dz, bronchial asthma, COPD AE: suppress HPA, increase physiological response CONTRA: liver dysfxn INTERACTION: many ADMIN: oral; IV/IM **1st choice chronic use** |
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Methyl Prednisone (A-Methapred)
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Methyl Prednisone (A-Methapred)
CLASS: long acting gluco MOA: USE: replacement, anti-inflamm... collagen dz, vasculitis, GI inflamm, renal autoimmune dz, bronchial asthma, copd AE: suppress HPA, increase physiological response CONTRA: INTERACTION: many ADMIN: |
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Dexamethasone (Decadron); Betamethasone (Celestone)
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Dexamethasone (Decadron); Betamethasone (Celestone)
CLASS: long acting gluco MOA: USE: septic shock, brain edema *max anti-inflamm* AE: b/c long 1/2 life, pronounced growth/bone suppression CONTRA: INTERACTION: many ADMIN: IM/ORAL/TOPICAL/IV; ORAL TOPICAL INHALE **BEST USED ACUTELY** |
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Mifepristone (RU-486)
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Mifepristone (RU-486)
CLASS: glucocorticoid antag @ higher doses MOA: block receptor, interfere with regulation HPA axis, increase ACTH & cortisol USE: hypercorticism AE: precipitate acute adrenal insufficiency CONTRA: INTERACTION: ADMIN: |
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LONG TERM GLUCOCORTICOID RX SIDE EFFECT/TOXICITY?
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BONE: children/women high risk... decrease osteoblast activity, increase Vit D --> 1, 25 OH but block ability to reabsorb (hypocalcemia, increase PTH release, bone absorption
Glucose - hyperglycemia GUT - increased peptic ulcer CNS - increased arousal/euphoria but prolonged=depression/sleep disturbances/psychosis |
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WAT IS THE DOC FOR HYPOPARATHYROIDISM?
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dihydrotachysterol
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what is a fatal side effect of Vit D?
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hypercalcemia
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what drug interaction can increase the risk of Vit D side effect?
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Thiazides decrease Ca excretion and increase serum Ca levels
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mech axn Vit D?
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INCREASES SERUM Ca
1) increase bone resorption by increase osteoclast activity 2) increase GI absorption of Ca and P 3) decrease renal excretion Ca and P 4) inhibit PTH secretion (by increasing serum Ca) |
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mech axn parathyroid horm?
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INCREASES serum Ca
1) increase GI absorption Ca but decreases absorption P 2) stimulate Vit D formation 3) stim bone resorption |
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mech axn calcitonin?
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DECREASES SERUM Ca
1) inhibits bone resorption 2) decreases GI absorption Ca 3) increases renal excretion of Ca and P |
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mech axn bisphosphonates??
what drug is in this class? |
alendronate
1) inhibit bone resorption -inhibit osteoclast activity 2) inhibit formation, aggregation, dissolution hydroxyapetite |
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AE associated with first generation bisphosphonates?
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inhibit mineralization - cause osteomalacia
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pharmacokinetics of bisphosphonates?
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poor intestinal absorption
cannot take with food excreted unchanged in urine |
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AE of Vit D?
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hypercalcemia, hyperphosphatemia
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AE calcitonin
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hypersensitivity rxn
hypocalcemia GI disturbances |
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AE etidronate
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osteomalacia
GI disturbances |
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AE alendronate
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GI disturbances, rash, musculoskeletal pain
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what non-hormonal drug is used to rx osteoporosis?
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alendronate
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mech Sulfonylureas?
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glipizide, glyburide
STIM insulin release |
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mech Biguanides?
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metformin
increase insulin BINDING to receptor |
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mech ThiazolidinedioneS?
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"TRPS"
risoglitazone, pioglitazone increase SENSITIVITY of TARGET TISSUE to insulin |
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mech Alpha glucosidase Inhibitors?
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arabose
prevent ABSORPTION of glucose, starch, dextrin, disaccharides in intestine |
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what is a short acting insulin
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SHILis NIL LU
humalog, insulin, lisipro |
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what are intermediate acting insulins?
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SHILis NIL LU
NPH, lente |
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what are long acting insulins?
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SHILis NIL LU
ultralente |
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what are insulin's axns?
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Carb metab: increase glycogen synthesis, pentose shunt, glucose oxidation, facilitates glucose transport via GLUT 4... decrease gluconeogenesis
Lipid metab: increases FA transport and TG synthesis... decrease lipolysis Protein metab: increases aa transport, protein synthesis... decreases protein degredation |
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why lispro and not insulin?
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liSpRo
more RAPID onset SHORTER duration axn prevents SPIKING + rebound hypoglycemia therefore better pt compliance + tighter regulation of plasma glucose concentrations |
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what drugs/hormones stimulate insulin release normally?
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Nutrients - glucose, aa, FA, ketone bodies
Hormones - secretin, gastrin, VIP, GIP Drugs - beta 2 agonist, muscarinic cholinergic agonist, sulfonylureas |
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what hormones/drugs inhibit insulin release?
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*all work DIRECTLY on beta cells in pancreas*
hormones - somatostatin, glucagon drugs - alpha 2 agonists |
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complications from insulin therapy?
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ALLERGIC RXN - IgE mediated... Rx by switching to human insulin or desensitization
RESISTANCE - IgG mediated... resensitizing with thiazolidinedione |
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1st generation sulfonylureas vs 2nd generation sulfonylureas
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1st gen sulfonylureas -
variable t1/2 (2-48hrs) 2nd gen sulfonylureas - 10-100x greater potency t1/2 = 24 hrs binds tighter to plasma binding proteins BOTH - bind plasma binding proteins |
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AE of oral antidiabetic agents?
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hypoglycemia
acarbose causes flatulence |
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contraindications of sulfonylureas?
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no insulin, pregnancy/lactation, hepatic renal insuffiency
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drug interactions of sulfonylureas?
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SALICYLATES displace sulfonylureas from binding proteins
SALICYLATES, PROBENECID, SULFONAMIDES decrease urinary excretion of sulfonylureas MAOI, CHLORAMPHENICOL, PHENYLBUTAZONE reduce hepatic metab of sulfonylureas |
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contra of biguanides?
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hepatic/renal disorder - increases risk for lactic acidosis
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contra of thiazolidinedione
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none
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contra of alpha glucosidase inhibitors?
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none
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human GnRh vs long-acting GnRH analog?
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gonadorelin (human GnRH) - short t1/2, used for replacement therapy (amenorrhea, hypogonadism
leuprolide, goserelin, nafarelin - longer t1/2, down regulates receptor, used to suppress hormone production (breast/prostate cancer, endometriosis, precocius puberty, ovulation suppression |
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native somatostatin vs somatostatin analog
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native - limited by short t1/2, also rebound hypersecretion GH
analog (octreotide) - resistant to enzymatic degradation, longer t1/2, oral, more selective for inhibiting GH |
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ganirelix mech?
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GnRH antag
rapid reversible suppression LH/FSH |
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ganirelix clinical use?
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controlled ovarian hyperstimulation - prevent premature LH surge
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ganirelix AE?
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ovarian hyperstimulation syndrome
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bromocriptine AE during initiation of rx?
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orthostatic hypotension, N/V, dizziness
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what drugs potentiate bromocriptine effect?
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antihypertensive agents
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what drugs inhibit bromocriptine effect
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drugs that increase prolactin - phenothiazines, butyrophenones, MAO
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why do the effects of somatropin (GH) outlast drug's t1/2?
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IGF effect is longer than t 1/2 b/c it has
IGF has slow induction and clearance |
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what is the DOC in CAD
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desmopressin
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desmopressin AE?
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water intoxification
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what potentiates desmopressin?
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siADH drugs - directly stimulate ADH secretion centrally
carbamazepine, chlorpropamide, tricyclics |
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what inhibits desmopressin?
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drugs that interefere with ADH axns in Collecting duct
Li, heparin, epi, etoh |
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what is the DOC for thyroid preparations?
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levothyroxine
takes 4-6 weeks to reach steady state plasma [ ] must be converted to T3 |
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how do you dose T4 for pregnant pt?
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increase dosage
high estrogen levels during pregnancy stimulate increased production TBG less T4 available |
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thyrotropin use?
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hypothyroidism diagnosis (differentiates btw primary/secondary , thyroid carcinoma
enhances iodine uptake into thyroid gland use in conjuction with 131 I |
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propylthiouracil vs methimazole mech?
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THIOUREYLENE
propylthiouracil - inhibits peripheral conversion T4 -> T3 both 1)inhibit thyroid perixidase mediated iodination (irreversibly inactivates oxidized form of thyroid peroxidase) 2) inhibit MIT/DIT coupling |
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propylthiouracil vs methimazole AE?
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both:
rash, GI upset, headache methimazole: agranulocytosis, aplastic anemia |
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how do you rx thyroid storm?
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1) iodide w/in 24 hrs (inhibits release of hormones)
2) propylthiouracil (longer t1/2, longer time to get effect) - used b/c inhibits peripheral conversion 3) for symptom - also give propanolol |
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what is thyroid storm?
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life threatening thyrotoxicosis
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AE associated with hyperthyroidism rx with radioactive iodine?
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high incidence of delayed hypothyroidism
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what are short acting glucocorticoids?
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8-12 hrs
hydrocortisone, cortisol |
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what are intermediate acting glucocorticoids?
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18-36
prednisolone, prednisone |
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what are long acting glucocorticoids?
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1-3 days
betamethasone, dexamethasone |
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what is cortisol and hydrocortisone used for?
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rx allergic rxn
suppress immune sys anti-inflamm |
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what is prednisone and prednisolone used for?
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anti-inflamm to rx
asthma, COPD, renal autoimmune disease, GI inflamm disease, vasculitis, collagen diseases |
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what is the clinical use of dexamethasone and betamethasone?
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dexamethasone suppression test
septic shock edema lymphatic cancer (lymphotoxic nature) |
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chronic vs alternate day glucocorticoid therapy
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chronic - some pt don't respond
alternate day - adv prolonged anti-inflammatory effects minimize HPA suppression facilitate HPA recovery minimizes reduction in bone growth minimizes risk 4 hypercortisolism (Cushing-like syndrome) abrupt switching can lead to hypocortisolism (tired, N/V, hypotension) |
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AE to glucocorticoid therapy?
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bone - increased bone loss
decreased bone growth glucose - hyperglycemia due to blockade of insulin effects increased synthesis of glucose gut - increased ulcers increased HCl secretion reduced formation of mucus lining CNS - first: arousal/euphoria later: depression/psychosis HPA: Suppression of your own HPA axis inability to synthesize your own cortisol immune system - suppression increased risk 4 infection |
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which drug is a glucocorticoid antag?
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mifepristone
anti-progestin @ higher doses blocks glucocortisol receptor rx hypercortisolism |
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MOA and uses for mitotane
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MOA: similar to DDT, unknown mech
use: adenocortical carcinoma |
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MOA and uses for aminoglutethimide
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moa: inhib P450-scc (P450-11 beta @ high doses)
use: cushing's ACTH hypersecretion breast cancer (aromatase inhibition) |
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MOA and uses for ketoconazole
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MOA: inhib P450-17 alpha
(P450-scc @ high doses) use: cushings *MOST EFFECTIVE* |
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MOA and uses for trilostane
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MOA: inhib 3 beta hydroxysteroid dehydrogenase
use: cushings |
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physiological mech of mineralocorticoids
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salt retention - increase Na reabsorption, excrete K
aldosterone binds to response element on DNA induces formation AIP, which increase cycling and change permeability activates and inserts Na channels/pumps into 1) basolateral membrane(increase Na pump axn) 2) lumenal membrane (increase Na conduct activity, make (-), drive H & K to lumen) in DCT and CD |
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AE of mineralocorticoid agonist?
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Na retention
hypertension @ high doses elicit symptoms resembling adrenal hypersecretion |
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AE Mitotane?
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anorexia,
N, lethargy |
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AE Aminoglutethimide
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GI,
neurological, signs of adrenal insufficiency |
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AE Ketoconazole
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hepatic dysfxn
decrease metab of antihistamines -> prolong QT interval |
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AE Trilostane
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adrenal insufficiency
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why are natural estrogens given only parentally?
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extensive first pass effect
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what forms of estrogen can be given orally?
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conjugated and synthetic estrogens
conjugated estrogens are hydrolyzed in intestine to estrogen and have less first pass effect C17 substitution decrease hepatic metabolism of synthetic estrogen |
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what forms of estrogen are commonly used in postmenopausal therapy?
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conjugated estrogens
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where are conjugated estrogens derived from?
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premarin - female horse urine
Cenestin - yam and soy |
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benefits of estrogen therapy in postmenopausal women
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inhibit bone resorption in osteoporosis
decrease vasomotor symptoms prevent cardiovascular dz (increase HDL/LDL ratio) |
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AE of estrogen replacement therapy in postmenopausal women
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N
migrane mood lability thromboembolism gallbladder dz HTN |
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oral vs transdermal estrogens for postmenopausal hormone replacement therapy
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oral
increase SSBG levels, increase secretion of CH to bile, increase exposure of liver to high [] of estrogens, relieves vasomotor symptoms, protects against blood loss, CV benefits transdermal decreased beneficial changes in plasma lipoproteins, skin rxn to patches, relieves vasomotor symptoms and protects against bone loss, consistent blood levels |
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raloxifine MOA?
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Selective estrogen receptor modulator
decreases bone resorption and remodeling |
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where does raloxifine have estrogen vs anti-estrogen effects?
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estrogen effects:
bone + lipid metabolism anti-estrogen effects: breast + uterus |
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why are progestins included in postmenopausal hormone replacement therapy?
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addition of progestins limits endometrial hyperplasia and risk of endometrial cancer
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MOA of antiestrogens?
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antag @ estrogen receptor
blocks binding of estrogen to its receptor |
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what confirmation of antiestrogens are responsible for antiestrogenic activity
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trans
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clinical uses of antiestrogens
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clomiphene - induce ovulation
tamoxifen + toremifine - breast cancer anastrozole and exemestane - advanced breast cancer in postmenopausal women GnRH analog + Ganirelix - suppress preovulatory surges - controlled ovarian hyperstimulation |
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clomiphene vs tamoxifen pharmacokinetics
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both -
extensive plasma protein binding enterohepatic recirc accumulation in fatty tissues tamoxifen has an active metabolite that is more potent than itself |
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AE of toremifene vs tamoxifen
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both:
N/V hot flashes menstral irregularities PE increased risk of endometrial cancer tamoxifen only - hyperlipidemia TOREMIFINE PREFERRED IN PT WITH CV OR HIGH CH |
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current clinical uses for mifepristone in Great Britain
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medical abortion in first trimester
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MOA and use of aromatase inhibitors
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anastrozole - nonsteroidal, competitive aromatase inhib
exemestane - steroidal, irreversible aromatase inhib *BOTH RX ADVANCED BREAST CANCER IN POSTMENOPAUSAL WOMEN* |
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how to administer testosterone so give good absorption and CONSISTENT blood levels?
what do you do this to rx? |
scrotal patches - mimics circadial rhythm
rx hypogonadism |
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how does methyl sub @ C17 of testosterone alter pharm axns and administration
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decreases hepatic metabolism
longer t1/2 allow oral administration |
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why should testosterone derivatives (fluoxymesterone NOT be used to rx hypogonadism?
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associated with hepatotoxicity and liver cancer with prolonged use
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MOA nilutamide
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irreversible androgen receptor antag
used in combo with orchiectomy |
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MOA flutamide vs bicalutamide
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both competitive antag
use in combo with GnRH agonist or radiation rx for metastatic prostate cancer |
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DOC 4 endometriosis?
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Danazol
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what Danazol use?
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*ENDOMETRIOSIS*, hereditary angioneurotic edema
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AE Danazol
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masculinization,
acne, hirsutism, menstrual irregularities |
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what drugs used to rx prostatic cancer & MOA?
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GnRH analog - suppress HPT axis, downregulate system
ketoconazole - block CP-450 enzymes involved in steroid biosynthesis flutamide and bicalutamide - nonsteroidal, competitive receptor antag Nilutamide - nonsteroidal irreversible androgen receptor antag |
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what drug commonly used to rx benign prostatic hyperplasia
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finasteride
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use finasteride?
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male pattern baldness
*NO USE IN WOMEN B/C TERATOGEN* |
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finesteride MOA?
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inhib 5-alpha reductase
competitive inhibitor test -> DHT |
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Fludrocortisone (Florinef)
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Fludrocortisone (Florinef
CLASS: Mineralocort agonist MOA: USE: hypoaldosteronism AE: salt retention, HTN CONTRA: INTERACTION: high doses resemble glucocorticoids (adrenal hypersecretion) ADMIN: |
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Spironolactone (Aldactone)
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Spironolactone (Aldactone)
CLASS: Mineralocort antag MOA: no bind DNA so no AIP USE: hyperaldosteronism, refractory edema AE: Hyperkalemia CONTRA: INTERACTION: sailcylates - block secretion of active metabolite ADMIN: poor bioavailability |
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Aminoglutethimide (Cytadren)
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Aminoglutethimide (Cytadren)
CLASS: Corticosteroid synthesis inhib MOA: inhib P450 scc (rate limiting enzymes for all steroid) USE: Cushings, breast cancer, hypersecretion ectopic production ACTH AE: GI distress, neurological, adrenal insufficiency, shut down body cortisol CONTRA: INTERACTION: many - induces P450 CYP3A ADMIN: |
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Ketoconazole (Nizoral)
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Ketoconazole (Nizoral)
CLASS: Corticosteroid synthesis inhib MOA: inhib P450 17 alpha, 11 beta, scc USE: *MOST EFFECTIVE FOR CUSHINGS* AE: hepatic dysfxn, PVC CONTRA: INTERACTION: second generation antihistamine - increase QT interval ADMIN: |
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Trilostane (Modrastane)
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Trilostane (Modrastane)
CLASS: Corticosteroid synthesis inhib MOA: inhib 3 beta OH steroid dehydrogenase (block pregnenolone to progest) USE: Cushings AE: Adrenal insufficiency CONTRA: INTERACTION: ? ADMIN: |
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Metyrapone (Metopirone)
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Metyrapone (Metopirone)
CLASS: corticosteroid synthesis inhib MOA: USE: HPA testing AE: HTN, hirsutism CONTRA: INTERACTION: ADMIN: no longer available in US |
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Mitotane (Lysodren)
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Mitotane (Lysodren)
CLASS: Corticosteroid Synthesis inhib MOA: USE: adrenocortical carcinoma (hypersecretion cortisol) AE: anorexia, lethargy, nausea CONTRA: INTERACTION: unknown ADMIN: |
