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153 Cards in this Set
- Front
- Back
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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 |
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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SE of OCs
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Increased thromboembolic events
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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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Dose may need to be increased during pregnancy or with Ocs due to increased TBG in plasma
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Thyroxine
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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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Vitamins containing iron should NOT be taken simultaneously with levothyroxine because
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Iron deiodinates thyroxine
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Thyroxine dose may need to be increased in hypothyroid patient during pregnancy because
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Estogens increase maternal TBG
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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)
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Mnemonic 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-medium acting glucocorticoids
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Cortisone, Hydrocortisone, Prednisone, Prednisolone, Methylprednisolone
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Intermediate acting glucocorticoids
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Triamcinolone, Fluprednisolone
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Long acting glucocorticoids
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Betamethasone and dexamethasone
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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, stria, thinning of skin
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Used for Cushing's syndrome (increased corticosteroid)
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Dexamethasone suppression test
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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 prophylaxis in women with risk factors for breast cancer
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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, oxymetholone, and oxandrolone
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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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What do alpha cells in the pancreas produce?
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Glucagon
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What do beta cells in the pancreas produce?
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Insulin
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Where are beta cells found in the pancreas?
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Islets of Langerhans
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What do delta cells in the pancreas produce?
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Somatostatin
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Product of proinsulin cleavage used to assess insulin production
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C-peptide
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Exogenous insulin contains
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No C-peptide
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Endogenous insulin contains
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Normal C-peptide
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Very rapid acting insulin, having fastest onset and
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Lispro (Humalog), aspart (Novolog),
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shortest duration of action
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glulisine (Apidra)
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Short acting, crystalline zinc insulin used to reverse acute hyperglycemia
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Regular (Humulin/Novolin R)
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Long acting insulins
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Glargine, detemir
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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 digestion and absorption of glucose formed from digestion of starch and disacchrides
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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, active as an insulin secretagogue
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Nateglinide
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MOA of nateglinide
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Insulin secretagogue - closes ATP- sensitive K+ channel
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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, sitagliptin, saxagliptin, pioglitazone
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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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Vascular effects of metformin
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Decreased micro and macro vascular disease
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Most important potential SE of metformin
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Lactic acidosis
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Incidence of hyoglycemia with metformin
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None
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Meglitinide class of drugs
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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, weight gain
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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 thiazolidinediones
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Decrease insulin resistance, stimulate PPAR-gamma receptors
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SE of Thiazolindinediones
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Edema, mild anemia; interaction with drugs that undergo CytP450 3A4 metabolism, risk for angina/MI
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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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Names of three bisphosphonates available IV
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Pamidronate, zoledronate, ibandronate
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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 prophlaxis
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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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Disease caused by excess ergot alkaloids
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St. Anthony's Fire
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Endogenous substances commonly interpreted as histamine, serotonin, prostaglandins, and vasoactive peptides
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Autocoids
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Syndrome of hypersecretion of gastric acid and pepsin usually caused by gastrinoma; it is associated with severe peptic ulceration and diarrhea
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Zollinger-Ellison Syndrome
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Drug that causes contraction of the uterus
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Oxytocin
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Distribution of histamine receptors H1, H2, and H3
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Smooth muscle; stomach, heart, and mast cells; nerve endings, CNS respectively
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Prototype antagonist of H1 and H2 receptors
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Diphenhydramine and cimetidine, respectively
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1st generation antihistamine that is highly sedating
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Diphendydramine
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1st generation antihistamine that is least sedating
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Chlorpheniramine or cyclizine
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2nd generation antihistamines
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Fexofenadine, loratadine, and cetirizine
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Generation of antihistamine that has the most CNS effects
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First generation due to being more lipid-soluble
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Major indication for H1 receptor antagonist
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Use in IgE mediated allergic reaction
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Antihistamine that can be used for anxiety and insomnia and is not addictive
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hydroxyzine (Atarax)
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H1 antagonist used in motion sickness
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Dimenhydrinate, meclizine, and other 1st generation
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Most common side effect of 1st generation antihistamines
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Sedation
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Lethal arrhythmias resulting from concurrent therapy with azole fungals (metabolized by CYP 3A4) and these antihistamines which inhibit the 3A4 iso- enzyme.
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Terfenadine and astemizole (have been removed from the market)
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H2 blocker that causes the most interactions with other drugs
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Cimetidine
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Clinical use for H2 blockers
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Acid reflux disease, duodenal ulcer and peptic ulcer disease
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Receptors for serotonin (5HT-1) are located
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Mostly in the brain, and they mediate synaptic inhibition via increased K+ conductance
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5HT-1d agonist used for migraine headaches
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Sumatriptan, naratriptan, and rizatriptan
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Triptan available in parenteral and nasal formulation
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Sumatriptan
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H1 blocker that is also a serotonin antagonist
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Cyproheptadine
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Agents for reduction of postpartum bleeding
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Oxytocin, ergonovine and ergotamine
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Agents used in treatment of carcinoid tumor
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Ketanserin cyproheptadine, and phenoxybenzamine
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5HT-3 antagonist used in chemotherapeutic induced emesis
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Ondansetron, granisetron, dolasetron and alosetron
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5HT-3 antagonist that has been associated with QRS and QTc prolongation and should not be used in patients with heart disease
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Dolasetron
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DOC to treat chemo-induced nausea and vomiting
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Odansetron
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Drug used in ergot alkaloids overdose, ischemia and gangrene
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Nitroprusside
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Reason ergot alkaloids are contraindicated in pregnancy
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Uterine contractions
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SE of ergot alkaloids
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Hallucinations resembling psychosis
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Ergot alkaloid used as an illicit drug
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LSD
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Dopamine agonist used in hyperprolactinemia
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Bromocriptine
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Peptide causing increased capillary permeability and edema
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Bradykinin and histamine
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Mediator of tissue pain, edema, inactivated by ACE, and may be a contributing factor to the development of angioedema
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Bradykinin
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Drug causing depletion of substance P (vasodilator)
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Capsaicin
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Prostaglandins that cause abortions
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Prostaglandin E1 (misoprostol) PGE2, and PGF2alpha
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Difference between COX 1 and COX 2
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COX 1 is found throughout the body and COX 2 is only in inflammatory tissue
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Drug that selectively inhibits COX 2
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Celecoxib and rofecoxib
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Inhibitor of lipoxygenase
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Zileuton
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Major SE of zileuton
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Liver toxicity
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Inhibitor of leukotrienes (LTD4) receptors and used in asthma
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Zafirlukast and montelukast
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Used in pediatrics to maintain patency of ductus arteriosis
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PGE1
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Approved for use in severe pulmonary HTN
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PGI2 (epoprostenol)
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Prostaglandin used in the treatment of impotence
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Alprostadil
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Irreversible, nonselective COX inhibitor
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Aspirin
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Class of drugs that reversibly inhibit COX
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NSAIDS
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Primary endogenous substrate for Nitric Oxidase Synthase
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Arginine
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MOA and effect of nitric oxide
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Stimulates cGMP which leads to vascular smooth muscle relaxation
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Long acting beta 2 agonist used in asthma
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Salmeterol, formoterol
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Muscarinic antagonist used in asthma
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Ipratropium
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MOA action of cromolyn
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Mast cell stabilizer
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Methylxanthine derivative used as a remedy for intermittent claudication
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Pentoxifylline
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MOA of corticosteroids
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inhibit phospholipase A2
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SE of long term corticosteroid therapy and remedy
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Adrenal suppression and weaning slowly, respectively |
