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Endocrine Drugs

One Liners

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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