One-Liners-Pharm-Endocrine

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Somatostatin (SRIF) analog used for acromegaly, carcinoid, glucagonoma and other GH producing pituitary tumors

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Octreotide

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Somatotropin (GH) analog used in GH deficiency (dwarfism)

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Somatrem

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GHRH analog used as diagnostic agent

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Sermorelin

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GnRH agonist used for infertility or different types of CA depending on pulsatile or steady usage respectively

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Leuprolide

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GnRH antagonist with more immediate effects, used for infertility

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Ganirelix

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Dopamine (DA) agonist (for Parkinson's disease), used also for hyperprolactinemia

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Bromocriptine

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Hormone inhibiting prolactin release

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Dopamine

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ACTH analog used for diagnosis of patients with corticosteroid abnormality

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Cosyntropin

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Synthetic analog of ADH hormone used for diabetes insipidus and nocturnal enuresis

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Desmopressin (DDAVP)

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Most widely used thyroid drugs such as Synthroid and Levoxyl contain

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L-thyroxine (T4)

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T3 compound less widely used

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Cytomel

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Anti-thyroid drugs

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Thioamides, iodides, radioactive iodine, and ipodate

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Thioamide agents used in hyperthyroidism

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Methimazole and propylthiouracil (PTU)

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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

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PTU

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PTU (propylthiouracil) MOA

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Inhibits thyroid hormone synthesis by blocking iodination of the tyrosine residues of thyroglobulin

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Can be effective for short term therapy of thyroid storm, but after several weeks of therapy causes an exacerbation of hyperthyroidism

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Iodide salts

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Permanently cures thyrotoxicosis, patients will need thyroid replacement therapy thereafter. Contraindicated in pregnancy

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Radioactive iodine

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Radio contrast media that inhibits the conversion of T4 to T3

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Ipodate

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Block cardiac adverse effects of thyrotoxicosis such as tachycardia, inhibits the conversion of T4 to T3

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Beta-blockers such as propranolol

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Pneumonic for 3 zones of adrenal cortex

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GFR

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Used for Addison's disease, Congenital Adrenal Hyperplasia (CAH), inflammation, allergies, and asthma (as a local inhalation)

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Glucocorticoids

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Short acting GC's

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Cortisone and hydrocortisone (equivalent to cortisol)

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Intermediate acting GC's

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Prednisone, methylprednisolone, prednisolone, and triamcinolone

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Long acting GC's

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Betamethasone, dexamethasone, and paramethasone

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Mineralocorticoids

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Fludrocortisone and deoxycorticosterone

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Some side effects of corticosteroids

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Osteopenia, impaired wound healing, inc. risk of infection, inc. appetite, HTN, edema, PUD, euphoria, psychosis

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Period of time of therapy after which GC therapy will need to be tapered

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5-7 days

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Used for Cushing's syndrome (increased corticosteroid) and sometimes for adrenal function test

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Metyrapone

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Inhibits conversion of cholesterol to pregnenolone therefore inhibiting corticosteroid synthesis

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Aminoglutethimide

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Antifungal agent used for inhibition of all gonadal and adrenal steroids

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Ketoconazole

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Antiprogestin used as potent antagonist of GC receptor

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Mifepristone

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Diuretic used to antagonize aldosterone receptors

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Spironolactone

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Common SE of spironolactone

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Gynecomastia and hyperkalemia

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Slightly increased risk of breast cancer, endometrial cancer, heart disease (questionable), has beneficial effects on bone loss

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Estrogen

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Antiestrogen drugs used for fertility and breast cancer respectively

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Clomiphene and tamoxifen

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Common SE of tamoxifen and raloxifene

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Hot flashes

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Selective estrogen receptor modulator (SERM) used for prevention of osteoporosis and currently being tested for treatment of breast cancer (Stars study)

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Raloxifene

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Non-steroidal estrogen agonist causes clear cell adenocarcinoma of the vagina in daughters of women who used it during pregnancy

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Diethylstilbestrol (DES)

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Estrogen mostly used in oral contraceptives (OC)

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Ethinyl estradiol and mestranol

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Anti-progesterone used as abortifacient

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Mifepristone (RU-486)

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Constant low dose of estrogen and increasing dose of progestin for 21 days (last 5 days are sugar pills or iron prep)

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Combination oral contraceptives (OC)

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Oral contraceptive available in a transdermal patch

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Ortho-Evra

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Converted to more active form DHT by 5 alpha-reductase

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Testosterone

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5 alpha-reductase inhibitor used for benign prostatic hyperplasia (BPH) and male pattern baldness

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Finasteride (Proscar and Propecia respectively)

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Anabolic steroid that has potential for abuse

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Nandrolone and stanozolol

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Anti-androgen used for hirsutism in females

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Cyproterone acetate

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Drug is used with testosterone for male fertility

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Leuprolide

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Alpha cells in the pancreas

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Produce glucagon

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Beta cells in the pancreas

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Produce insulin

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Beta cells are found

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Islets of Langerhans

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Delta cells in the pancreas

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Produce Somatostatin

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Product of proinsulin cleavage used to assess insulin abuse

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C-peptide

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Exogenous insulin

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Little C-peptide

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Endogenous insulin

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Normal C-peptide

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Very rapid acting insulin, having fastest onset and shortest duration of action

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Lispro (Humalog)

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Rapid acting, crystalline zinc insulin used to reverse acute hyperglycemia

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Regular (Humulin R)

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Long acting insulin

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Ultralente (humulin U)

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Ultra long acting insulin, has over a day duration of action

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Glargine (Lantus)

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Major SE of insulin

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Hypoglycemia

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Important in synthesis of glucose to glycogen in the liver

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GLUT 2

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Important in muscle and adipose tissue for glucose transport across muscles and TG storage by lipoprotein lipase activation

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GLUT 4

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Examples of alpha-glucosidase inhibitors (AGI)

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Acarbose, miglitol

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MOA of AGI's

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Act on intestine, delay absorption of glucose

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SE of AGI's

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Flatulence (do not use beano to tx), diarrhea, abdominal cramps

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Alpha-glucosidase inhibitor associated with elevation of LFT's

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Acarbose

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Amino acid derivative

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Nateglinide

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MOA of nateglinide

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Insulin secretagogue

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Biguanide

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Metformin

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Drugs available in combination with metformin

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Glyburide, glipizide, and rosiglitazone

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MOA of metformin

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Decreases hepatic glucose production and intestinal glucose absorption; increase insulin sensitivity

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Most important potential SE of metformin

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Lactic acidosis

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Meglitinide

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Repaglinide

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MOA of repaglinide

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Insulin release from pancreas; faster and shorter acting than sulfonylurea

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First generation sulfonylurea

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Chlorpropamide, tolbutamide, tolazamide, etc.

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Second generation sulfonylurea

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Glyburide, glipizide, glimepiride, etc.

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MOA of both generations

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Insulin release from pancreas by modifying K+ channels

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Common SE of sulfonylureas, repaglinide, and nateglinide

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Hypoglycemia

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Sulfonylurea NOT recommended for elderly because of very long half life

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Chlorpropamide

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Thiazolidinediones

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Pioglitazone, Rosiglitazone, Troglitazone (withdrawn/d from market)

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Reason troglitazone was withdrawn from market

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Hepatic toxicity

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MOA of thiazolindinediones

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Stimulate PPAR-gamma receptor to regulate CHO and lipid metabolism

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SE of Thiazolindinediones

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Edema, mild anemia; interaction with drugs that undergo CytP450 3A4 metabolism

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Hyperglycemic agent that increases cAMP and results in glycogenolysis, gluconeogenesis, reverses hypoglycemia, also used to reverse severe beta-blocker overdose and smooth muscle relaxation

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Glucagon

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Available bisphosphonates

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Alendronate, etidronate, risedronate, pamidronate, tiludronate, and zoledronic acid

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MOA of Bisphosphonates

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Inhibits osteoclast bone resorption

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Only bisphosphonates available IV

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Etidronate

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Uses of bisphosphonates

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Osteoporosis, Paget's disease, and osteolytic bone lesions, and hypercalcemia from malignancy

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Major SE of bisphosphonates

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Chemical esophagitis

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Bisphosphonates that cannot be used on continuous basis because it caused osteomalacia

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Etidronate

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Used for prevention of postmenopausal osteoporosis in women

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Estrogen (HRT-Hormone replacement therapy)

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Increase bone density, also being tested for breast CA tx.

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Raloxifene (SERM-selective estrogen receptor modulator)

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Used intranasally and decreases bone resorption

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Calcitonin (salmon prep)

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Used especially in postmenopausal women, dosage should be 1500 mg

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Calcium

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Vitamin given with calcium to ensure proper absorption

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Vitamin D

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3 zones of adrenal cortex and their products

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Glomerulosa (mineralocorticoids), fasciculata (glucocorticoid=GC), and reticularis (adrenal androgens)