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Endocrine Drugs
One Liners
| Question | Answer |
|---|---|
| Somatostatin (SRIF) analog used for acromegaly, carcinoid, glucagonoma and other GH producing pituitary tumors | Octreotide |
| Somatotropin (GH) analog used in GH deficiency (dwarfism) | Somatrem |
| GHRH analog used as diagnostic agent | Sermorelin |
| GnRH agonist used for infertility or different types of CA depending on pulsatile or steady usage respectively | Leuprolide |
| GnRH antagonist with more immediate effects, used for infertility | Ganirelix |
| Dopamine (DA) agonist (for Parkinson's disease), used also for hyperprolactinemia | Bromocriptine |
| Hormone inhibiting prolactin release | Dopamine |
| ACTH analog used for diagnosis of patients with corticosteroid abnormality | Cosyntropin |
| Synthetic analog of ADH hormone used for diabetes * insipidus and nocturnal enuresis | Desmopressin (DDAVP) |
| SE of OCs | Increased thromboembolic events |
| Most widely used thyroid drugs such as Synthroid and Levoxyl contain | L-thyroxine (T4) |
| T3 compound less widely used | Cytomel |
| Anti-thyroid drugs | Thioamides, iodides, radioactive iodine, and ipodate |
| Thioamide agents used in hyperthyroidism | Methimazole and propylthiouracil (PTU) |
| Thioamide less likely to cross placenta, inhibits peripheral conversion of T4 to T3 in high doses, and should be used with extreme caution in pregnancy | PTU |
| PTU (propylthiouracil) MOA | Inhibits thyroid hormone synthesis by blocking iodination of the tyrosine residues of thyroglobulin |
| Can be effective for short term therapy of thyroid storm, but after several weeks of therapy causes an exacerbation of hyperthyroidism | Iodide salts |
| Dose may need to be increased during pregnancy or with Ocs due to increased TBG in plasma | Thyroxine |
| Permanently cures thyrotoxicosis , patients will need thyroid replacement therapy thereafter. Contraindicated in pregnancy | Radioactive iodine |
| Radio contrast media that inhibits the conversion of T4 to T3 | Ipodate |
| Block cardiac adverse effects of thyrotoxicosis such as tachycardia, inhibits the conversion of T4 to T3 | Beta-blockers such as propranolol |
| Vitamins containing iron should NOT be taken simultaneously with levothyroxine because | Iron deiodinates thyroxine |
| Thyroxine dose may need to be increased in hypothyroid patient during pregnancy because | Estogens increase maternal TBG |
| Used for Addison's disease , Congenital Adrenal Hyperplasia (CAH) , inflammation, allergies, and asthma (as a local inhalation) | Glucocorticoids |
| Short acting glucocorticoids | Cortisone and hydrocortisone (equivalent to cortisol) |
| Intermediate acting glucocorticoids | Prednisone, methylprednisolone, prednisolone, and triamcinolone |
| Long acting glucocorticoids | Betamethasone and dexamethasone |
| Mineralocorticoids | Fludrocortisone and deoxycorticosterone |
| Some side effects of corticosteroids | Osteopenia, impaired wound healing, inc. risk of infection, inc. appetite, HTN, edema, PUD, euphoria, psychosis, stria, thinning of skin |
| Period of time of therapy after which GC therapy will need to be tapered | 5-7 days |
| Used for Cushing's syndrome (increased corticosteroid) | Dexamethasone suppression test |
| Inhibits conversion of cholesterol to pregnenolone therefore inhibiting corticosteroid synthesis | Aminoglutethimide |
| Antifungal agent used for inhibition of all gonadal and adrenal steroids | Ketoconazole |
| Antiprogestin used as potent antagonist of GC receptor | Mifepristone |
| Diuretic used to antagonize aldosterone receptors | Spironolactone |
| Common SE of spironolactone | Gynecomastia and hyperkalemia |
| Slightly increased risk of breast cancer, endometrial cancer, heart disease (questionable), has beneficial effects on bone loss | Estrogen |
| Antiestrogen drugs used for fertility and breast cancer respectively | Clomiphene and tamoxifen |
| Common SE of tamoxifen and raloxifene | Hot flashes |
| Selective estrogen receptor modulator (SERM) used for prevention of osteoporosis and prophylaxis in women with risk factors for breast cancer | Raloxifene |
| Non-steroidal estrogen agonist causes clear cell adenocarcinoma of the vagina in daughters of women who used it during pregnancy | Diethylstilbestrol (DES) |
| Estrogen mostly used in oral contraceptives (OC) | Ethinyl estradiol and mestranol |
| Anti-progesterone used as abortifacient | Mifepristone (RU-486) |
| Constant low dose of estrogen and increasing dose of progestin for 21 days (last 5 days are sugar pills or iron prep) | Combination oral contraceptives (OC) |
| Oral contraceptive available in a transdermal patch | Ortho-Evra |
| Converted to more active form DHT by 5 alpha- reductase | Testosterone |
| 5 alpha-reductase inhibitor used for benign prostatic hyperplasia (BPH) and male pattern baldness | Finasteride (Proscar and Propecia respectively) |
| Anabolic steroid that has potential for abuse | Nandrolone, oxymetholone, and oxandrolone |
| Anti-androgen used for hirsutism in females | Cyproterone acetate |
| Drug is used with testosterone for male fertility | Leuprolide |
| What do alpha cells in the pancreas produce? | Glucagon |
| What do delta cells in the pancreas produce? | Somatostatin |
| Product of proinsulin cleavage used to assess insulin abuse | C-peptide |
| Exogenous insulin contains | Little C-peptide |
| Endogenous insulin contains | Normal C-peptide |
| Very rapid acting insulin, having fastest onset and shortest duration of action | Lispro (Humalog), aspart, glulisine |
| Rapid acting, crystalline zinc insulin used to reverse acute hyperglycemia | Regular (Humulin R) |
| Long acting insulin | Ultralente (humulin U) |
| Ultra long acting insulin, has over a day duration of action | Glargine (Lantus), detemir |
| Major SE of insulin | Hypoglycemia |
| Important in synthesis of glucose to glycogen in the liver | GLUT 2 |
| Important in muscle and adipose tissue for glucose transport across muscles and TG storage by lipoprotein lipase activation | GLUT 4 |
| Examples of alpha-glucosidase inhibitors (AGI) | Acarbose, miglitol |
| MOA of alpha-glucosidase inhibitors | Act on intestine, delay digestion and absorption of glucose formed from digestion of starch and disacchrides |
| Alpha-glucosidase inhibitor associated with elevation of LFT's | Acarbose |
| SE of alpha-glucosidase inhibitors | Flatulence (do not use beano to tx), diarrhea, abdominal cramps |
| Amino acid derivative, active as an insulin secretagogue | Nateglinide |
| MOA of nateglinide | Insulin secretagogue - closes ATP- sensitive K+ channel |
| Biguanide | Metformin |
| Drugs available in combination with metformin | Glyburide, glipizide, and rosiglitazone |
| MOA of metformin | Decreases hepatic glucose production and intestinal glucose absorption; increase insulin sensitivity |
| Vascular effects of metformin | Decreased micro and macro vascular disease |
| Most important potential SE of metformin | Lactic acidosis |
| Incidence of hyoglycemia with metformin | None |
| Meglitinide class of drugs | Repaglinide |
| MOA of repaglinide | Insulin release from pancreas; faster and shorter acting than sulfonylurea |
| First generation sulfonylurea | Chlorpropamide, tolbutamide, tolazamide, etc. |
| Second generation sulfonylurea | Glyburide, glipizide, glimepiride, etc. |
| sulfonylurea MOA | Insulin release from pancreas by modifying K+ channels |
| Common SE of sulfonylureas, repaglinide, and nateglinide | Hypoglycemia |
| Sulfonylurea NOT recommended for elderly because of very long half life | Chlorpropamide |
| Reason troglitazone was withdrawn from market | Hepatic toxicity |
| MOA of thiazolindinediones | Stimulate PPAR-gamma receptor to regulate CHO and lipid metabolism |
| SE of Thiazolindinediones | Edema, mild anemia; interaction with drugs that undergo CytP450 3A4 metabolism |
| Hyperglycemic agent that increases cAMP and results in glycogenolysis, gluconeogenesis, reverses hypoglycemia, also used to reverse severe beta- blocker overdose and smooth muscle relaxation | Glucagon |
| Rapid acting insulins that do not self-aggregate | lispro insulin, aspart insulin, glulisine insulin |
| Peakless ling acting insulin | Insulin glargine |
Created by:
tessah10
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