Desmopressin
-V2 selective
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-DOC central diabetes insipidus
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8-arginine vasopressin
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-More specific for subtype of vasopressin receptor
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-Hemophilia
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Antithyroid drugs
-PTU
-Methimazole
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-Block coupling reactions
-Block some peripheral conversion
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-Slow onset
-Uncomplicated hyperthyroid condition
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-PTU safer in pregnancy
-maculopapular rash is common
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Antithyroid drugs
-Iodine
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-Short term use, possible use in thyrotoxicosis. Decreases gland side, fragility, vascularity.
-No long term use
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Adrenal steroid antagonists
-Spironolactone
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-Blocks aldosterone and androgen receptors
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Adrenal steroid antagonist
-Mifepristone
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-Blocks glucocorticoid and progestin receptors
-RU-486
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Estrogen drugs
-Conjugated equine estrogens
-Ethnyl estradiol
-Diethylstilbesterol
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-Increase feedback inhibition of FSH and LH
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-Contraception
-Hormone replacement
-Female hypogonadism
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-Nausea, breast tenderness, gall bladder disease, endometrial hyperplasia
-Blood coagulation
-Increased risk of endometrial cancer unless progestins are added
-DES in pregnancy increases risk of vaginal adenocarcinoma
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Danazol |
-Inhibition of ovarian steroid synthesis
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-Useful in endometriosis and fibrocystic breast disease
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Clomipherene
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-Decreases feedback inhibition
-Increases FSH/LH
-Increases ovulation
-Partial estrogen agonist via blockade of negative feedback to pituitary
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-Increase fertility
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-Adverse effects include multiple births
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SERMs
-Tamoxifen
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-E receptor agonist at bone
-E receptor antagonist at breast
-E receptor partial agonist at endometrium
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-Useful for breast CA (estrogen sensitive)
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-Risk of endometrial CA
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SERMs
-Raloxifene
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-E receptor agonist at bone
-Antagonist at breast and uterus
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-Used for osteoporosis
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-No increased CA risk
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Progestin |
-Major natural progestin
-Increase feedback inhibition of gonadotropins
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-Depot contraception
-HRT
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-Decrease HDL
-Increased LDL
-Glucose intolerance
-Breakthrough bleeding
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OCPs
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-Combination of estrogens and progestins in varied dose.
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-contraception
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-Nausea/bloating
-Headache
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Androgen antagonists
-Leuprolide
-Finasteride
-Ketoconazole
***Recall that alpha antagonists are used for BPH***
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-Leuprolide is a GnRH analogue that is used for prostate CA
-Finasteride is a 5a reductase inhibitor used for BPH and male pattern baldness
-Ketoconazole is a synthesis inhibitor used in androgen receptor positive cancer
-Finasteride stops conversion of testosterone to DHT
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Insulin
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-Lispro and regular insulin are usually used at meal time
-Lente and ultralente are more “basal” types of insulin
-Lente and ultralente usually given sometime during the day to mimic insulin secretion from the pancreas
-Ultralente is the longest acting insulin
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-Antihypoglycemia
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-Hypoglycemia
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Sulfonyureas
FIRST GENERATION:
-Acetohexamide
-Chlorpropramide
SECOND GENERATION:
-Tolbutamide
-Glipizide
-Glyburide
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-Glucose acts asan insulonogen by increasing intracellular Atp. Closure of K channels leads to Ca influx leading to insulin release
-Sulfonyureas block K channels causes membrane depolarization, influx of calcium.
-Sulfonyureas are insulin secreteagogues.
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-Antihypoglycemic
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-Hypoglycemia is biggest problem; more of an issue with first generation drugs
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