Drug



Pituitary | | |

|Somatropin |Recombinant GH |GH deficiency (kids + adults) |HA, emesis, (ICP, edema, | |

| | | |arthralgia, myalgia, | |

| | | |carpal tunnel syndrome | |

|Sermorelin acetate |Synthetic GHRH |GH deficiency (kids ONLY) |Same as above |LESS effective than Somatropin;|

| |(SubQ) | | |cheaper |

|Octreotide |Somatostatin analog |GH excess |GI upset, gallstones |(GH & tumor size (depends on |

| |(SubQ, IM) | | |binding affinity) |

|Pegvisomant |GH antagonist |GH excess |Abnormal liver fxn tests |Binds receptor w/o inducing |

| | | |(reversible) |dimerization |

|Bromocriptine |DAR agonists |Hyperprolactinemia |N/V, insomnia, CNS effects |(PRL & tumor size |

|Pergolide |DAR agonists |Hyperprolactinemia |Same as above |(PRL & tumor size |

|Gonadotropins |Pure FSH, rFSH |Hypogonadism, infertility |Multiple births, ovarian | |

|Menotropins | | |hyperstimulation syndrome, pain, | |

| | | |N/V/D, respiratory distress | |

|Gonadorelin acetate |Synthetic GnRH |Hypogonadism, infertility |Phlebitis, multiple births (LESS | |

| |(IV) | |than w/ Gonadotropins) | |

|Ganirelix |GnRH antagonist |Hypergonadism | | |

|Desmopressin acetate |ADH analog |DI (ADH deficiency) |Cutaneous hyperstimulation, | |

| |(oral or nasal spray) | |vasoconstriction, (HR, | |

| | | |H2O retention, GI cramping | |

| | | |CI—CAD, renal failure | |

|Ameloride |Thiazide diuretics |Nephrogenic DI | |Paradoxical (urine output |

|Triamterene | | | | |

|Demeclocycline |ADH antagonist |SIADH | |Inhibits ADH action in |

| | | | |collecting ducts |

|Oxytocin (Pitocin) |(IV) |Induce labor & lactation |Uterine rupture, fetal hypoxia, | |

| | | |vasodilation, hypotension, (HR | |

| | | | | |

|Thyroid | | | | |

|Levothyroxine sodium | |Hypothyroidism (long duration), |Arrhythmias, anxiety |Lower doses in elderly |

|(Synthroid) | |Nodular thyroid, thyroid CA |CI—AlOH, Ca, Fe ((absorption), |(nodule size & TSH levels |

| | | |pre-existing heart dz | |

|Liothyronine sodium |(pill or IV) |Myxedema coma (quick onset) | | |

|Liotrix |T3/T4 mixture |Hypothyroidism |LESS SE than Synthroid | |

|131I |(oral) |Hyperthyroidism, thyroid CA |Radiation effects (2° cancer) |Destroys thyroid parenchyma |

| | | |CI—pregnancy, kids | |

|Propylthiouracil |Thioureylenes |Hyperthyroidism (pre-surgery) |Agranulocytosis, bone marrow |Inactivates thyroid peroxidase,|

|Methimazole | | |suppression, rash, joint pain, N, |Propylthiouracil also inhibits |

| | | |gingival bleeding, liver damage, |D1 deiodinase |

| | | |poor healing | |

|Thiocyanate |Anions |Hyperthyroidism |Fatal aplastic anemia |Induced by cabbage & smoking |

|Perchlorate | | |(Perchlorate)—NO longer used | |

|Iodide (KI) |(large doses) |Severe thyrotoxicosis |Mouth burning, HA, cough, |Benefits disappear w/ time |

| | |(rapid onset) |GI irritation, pulmonary edema, |(thyroid vascularity |

| | | |cutaneous bleeding | |

| | | | | |

|Estrogens & Progestins | | | |

|17(-estradiol |Natural estrogens | | | |

|Estrone |Natural estrogens | | |1/10th potent as estradiol |

|Estriol |(estradiol metabolites) | | |Placental estrogen |

|Equilin sulfate |Conjugated estrogens |HRT | |Modified to prevent liver |

|Estrone sulfate | | | |inactivation |

|Ethinyl estradiol (EE) |Synthetic estrogens |OCs (longest duration) | |MOST potent |

|Mestranol |(inactive EE precursor) | | |Lipid soluble (stored in fat) |

|Diethylstilbestrol |Non-steroidal estrogen |Prevent miscarriage |Infertile daughters |NO longer used |

|Tamoxifen |Anti-estrogen (SERMs) |Estrogen-sensitive breast CA |hot flashes, venous thrombosis | |

|Raloxifen | |Osteoporosis | | |

|Clomiphene |Anti-estrogen |Induces ovulation | | |

|Hydroxyprogesterone |Synthetic progestins |Depot contraceptives |Poor lipid profile, glucose | |

|Medroxyprogesterone |(IM) |MOST common HRT |intolerance | |

|(Provera) | | | | |

|Norethindrone |Synthetic progestins |COCs, POP (lactating women, |Androgenic, higher failure rate, |LESS potent |

| | |thrombotic dz, smokers) |menstrual disturbances | |

|Levonorgestrel |Synthetic progestins |COCs |MOST androgenic |MOST potent |

|(Norplant) |(sub-dermal) | | | |

|Desogestrel |Synthetic progestins |COCs |NOT androgenic |LEAST potent |

|Norgestimate | | | | |

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|Contraceptives | | | | |

|RU-486 (Mifepristone) |GR antagonist |Abortion (first 7w), | |Rx during Dx OR for inoperable |

| | |Cushing’s dz | |tumors |

|Ortho-Tri-Cyclen |EE + Norgestimate |COC | |#1 prescription OC |

|Triphasil (Tri-Levlen) |EE + Norgestrel |COC | |#2 prescription OC |

|Ortho-Novum 7/7/7 |EE + Norethindrone |COC | |#3 prescription OC |

|Mircette |Lower dose EE + Desogestrel |Novel COC (esp. for PMS) | |E constant |

|Yasmin |EE + Drospirenone |Novel COC (NO Na+/H2O retention) |Hyperkalemia |Resembles diuretic |

| | | |CI—liver, renal, adrenal dz |Spironolactone |

|Ortho-Evra | |Birth control patch |LESS effective in obese pts |7d patch for 3w |

|Preven Kit |High dose OCs |Emergency contraceptive | |1st dose 72h, then 12h later |

| | | | | |

|Hormone Replacement Therapy | | | |

|Premarin |(pills or vaginal cream) | | | |

|Prempro |CE + Medroxyprogesterone |MOST common HRT |(CHD, breast cancer, stroke, PE | |

| | | |(colon CA, hip fractures, | |

| | | |endometrial CA | |

|Premphase |CE + higher dose MP | | | |

|Estrace |Micronized estradiol (oral) | | |Lower estrogen |

|Estraderm |Transdermal estradiol | | |NO 1st-pass metabolism |

|Prometrium |Micronized progesterone | |LESS (HDL | |

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|Androgens | | | | |

|Leuprolide |GnRH agonist |Prostatic CA, precocious puberty, | |Disrupts hypothalamic pulsing (|

| | |uterine leiomyoma, PMS | |(LH/FSH secretion ( |

| | |endometriosis, BPH, breast CA | |(testosterone production |

|Ketoconazole |Imidazole anti-fungals |Prostatic CA | |Inhibits P450; (synthesis of |

| | |(NOT FDA approved) | |aldosterone, cortisol, & T |

|Finasteride |Testosterone analog |Prostatic CA, BPH, alopecia | |Specific Type II |

| | | | |5(-reductase inhibitor |

|Flutamide |Non-steroidal testosterone |Metastatic prostatic CA (combo w/ | |Beneficial effects disappear as|

| |antagonist |Leuprolide) | |blocks (-) feedback |

|Androgel |Testosterone |Hypogonadism, breast CA, anemia of| | |

|Testim |(topical) |chronic dz, | | |

| | |AIDS wasting syndrome, | | |

| | |female-to-male gender change | | |

| | | | | |

|Glucocorticoids & Mineralocorticoids | | | |

|Cortisone |Cortisols |Glucocorticoid deficiency | |LESS potent |

|Hydrocortisone | |Eczema, psoriasis (face, groin) | | |

|Prednisone |(oral) |Acute eczematous rxn |Poor wound healing, susceptibility|MORE potent |

|Prednisolone | |Graft rejection (combo w/ other |to infections |Tapered over 21d |

|Methylprednisone |(IV) |immunosuppressants), | | |

| | |alleviate MS Sx, lymphoid CA | | |

| | |rheumatic dz (combo w/ NSAIDs) | | |

|Triamcinolone acetonide |(injection) |Asthma, skin lesions, joint pain | |MORE potent |

|Budesonide |(oral) |Crohn’s dz (refractory) | |Dissolves in pH of ileum & |

| | | | |ascending colon |

|Beclomethasone | |Asthma | |MOST potent |

|Betamethasone | |Eczema, psoriasis (thicker skin) | |MOST potent |

|Dexamethasone | |Lymphoid cancers | |MOST potent |

|ZK216348 |Selective GR agonist |Anti-inflammatory |LESS SE, | |

| | | |BUT suppresses ACTH | |

|Ketoconazole |Imidazole anti-fungals |Glucocorticoid excess, | |Inhibits synthesis of |

| | |Adrenal CA, hirsutism, | |pregnenolone, cortisol, & |

| | |breast CA | |androstenedione |

|Aminoglutethimide | |Glucocorticoid excess, | |Inhibits synthesis of |

| | |adrenal CA | |pregnenolone, cortisol, & |

| | | | |androstenedione |

|Metyrapone | |Glucocorticoid excess | |Inhibits ONLY synthesis of |

| | |Dx test for adrenal fxn | |cortisol (11(-hydroxylase) |

|Fludrocortisone | |Mineralocorticoid deficiency |HTN, hypokalemia |10X affinity for MR than GR |

|Spironolactone |MR antagonist |Mineralocorticoid excess |Hyperkalemia, hyperchloremia |High doses inhibit AR |

| | | | | |

|Calcium homeostasis | | | |

|Calcitriol |1,25-(OH)2-vit.D |Vit.D-dependent rickets |Hypercalcemic spikes |(Ca2+ & PO4 GI absorption |

| | |Renal osteodystrophy | |(bone resorption, inhibits PTH |

| | |Psoriasis, leukemia | | |

| | |Osteoporosis? | | |

|Dihydrotachysterol (DHT) |Vit.D2 analog |Hypoparathyroidism | |Faster onset, shorter duration |

| | |Pseudo-hypoparathyroidism | |than vit.D |

|Calcitonin |Produced in thyroid C-cells |Osteoporosis, Paget’s dz | |Inhibits bone resportion |

|Estrogen |17( |Osteoporosis | |(osteoblast production of IL-6 |

| | | | |(osteoclast chemoattractant) |

|Raloxifene |SERM |Osteoporosis |NOT SEs as w/ estrogen | |

| | | |(endometrial & breast CA) | |

|Etidronate |Bisphosphonates |Osteoporosis |May induce osteomalacia |Inhibits bone resorption (binds|

| | |Paget’s dz (6m/3m cycles) | |& prevents hydroxyapatite |

| | | | |crystallization) |

|Toxicology | | | | |

|Dimercaprol |Chelation Rx |Arsenic & mercury |(HR, HTN, N/V, (prothrombin time, |NOT Rx neurologic Sx |

| |British anti-lewisite (BAL) | |painful injections | |

| |(repeat parenteral injections) | |CI—cadmium & Fe (nephrotoxic) | |

|Succimer |Chelation Rx |Lead, arsenic, mercury |LESS toxic; GI upset, |MORE H2O-soluble |

|DMPS | | |skin rash, (liver enzymes |(well-absorbed GI) |

|Calcium disodium edentate |Chelation Rx |Pb, Fe, Zn |Renal tubular necrosis |Minimize SE w/ hydration & |

|(EDTA) |(IV) |(higher affinity than Ca2+) | |limit to (5d Rx |

|Penicillamine |Chelation Rx |Cu |Allergies, nephrotoxic, autoimmune|Well-absorbed GI |

| | |Adjunct for Ag, arsenic, Pb |(hemolytic anemia) | |

|Deferoxamine |Chelation Rx |Acute Fe |Urticaria, neurotoxic, hepatic & |Poor GI absorption |

| |(parenteral) | |renal dysfxn, histamine release | |

|Fomepizole |Alcohol dehydrogenase inhibitor |MtOH, ethylene glycol |LESS monitoring than EtOH | |

| | | | | |

|Diabetes | | | | |

|Insulin Lispro (Humalog) |Ultra-short acting insulin |Type I w/ hypoglycemic risk |Hypoglycemia (ANS ( |15min before meal |

|Aspart insulin |Recombinant human insulin |Active persons, recent onset Type |neuroglycopenic), allergies, |LESS hypoglycemia b/w meals & |

| | |I (residual (-cell fxn) |lipoatropy or -hypertrophy, edema |during night |

|Regular insulin |Short-acting insulin |Ketoacidosis, pre-surgery, | |30-45min before meal |

| |(ONLY insulin dosed IV) |childbirth (IV dosing) | |Better control w/ IV infusion |

|NPH |Intermediate-acting insulin |Basal insulin levels | |Varying amounts of Zn2+ |

|Lente | | | | |

|Ultralente |Long-acting insulin |Basal insulin levels | |Peaks rapidly w/ constant |

|Insulin Glargine (Lantus) | |(24h duration, QD at bedtime) | |levels for duration |

|70/30 |Mixtures of short & long-acting |Large breakfasts & lunches | | |

|50/50 | |Large dinners | | |

|Chlorpropamide |1st-generation sulfonylureas |Type II DM |Hypoglycemia (worse w/ |LONGEST duration, 24-72h |

|Tolbutamide |(“-amides”) | |longer-acting), GI upset, |SHORTEST duration, 6-8h |

| |(insulin secretors) | |pruritis, anemia |CHEAPEST |

| | | |CI—renal or hepatic dz, |Bound to plasma proteins |

| | | |gestational DM (cross placenta) | |

|Glipizide |2nd-generation sulfonylureas |Type II DM | |MORE potent |

| |(“Gl-“) | | | |

|Metformin (Glucophage) |Biguanides |DOC Type II DM |N/D, metallic taste, anorexia, B12|NOT hypoglycemic |

| |(insulin sensitizers) | |& folate deficiency |NOT alter weight |

| | | |CI—Hx of lactic acidosis, CHF, |Positive lipid profile |

| | | |hypoxic lung dz, radio dyes, |NOT plasma protein bound |

| | | |Cr >1.5 males & 1.4 females | |

|Acarbose |(-glucosidase inhibitors |BOTH Types I & II DM |GI upset (LESS w/ Miglitol) |Blocks CHO absorption in brush |

|Miglitol | | | |border |

|Troglitazone (Rezulin) |1st-generation thiazolinediones |(#glucose transporters |Hepatotoxic |REMOVED from market |

|Rosiglitazone (Avandia) |2nd-generation thiazolinediones | |URIs, HAs, weight gain |Positive lipid profile |

|Pioglitazone (Actos) |(QD dosing) | |NOT GI upset |Delayed onset (weeks) |

| | | |CI—liver dz (MUST monitor fxn) | |

|Repaglinide (Prandin) |Meglitinides |Moderately elevated glucose | |Oral form of Insulin Lispro |

|Nateglinide (Starlix) |(insulin secretors) |(rapid onset, short duration) | | |

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