Drug - University of Kentucky
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 | |
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|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 | |
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|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 |
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|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 | | |
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|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 |
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|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 | |
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|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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