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106 Cards in this Set

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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
Thyroid and anti-thyroid drugs

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
Adrenocorticosteroid and adrenocortical antagonists

3 zones of adrenal cortex and their products
Glomerulosa (mineralocorticoids), fasciculata (glucocorticoid=GC), and reticularis (adrenal androgens)
Mnemonic for 3 zones of adrenal cortex
GFR
Used for Addison's disease , Congenital Adrenal Hyperplasia (CAH) , inflammation, allergies, and asthma (as a local inhalation)
Glucocorticoids
Short-medium acting glucocorticoids
Cortisone, Hydrocortisone, Prednisone, Prednisolone, Methylprednisolone
Intermediate acting glucocorticoids
Triamcinolone, Fluprednisolone
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
Inhibitors of corticosteroids biosynthesis

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
Gonadal hormones and inhibitors

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
Pancreatic hormones, antidiabetics, and hyperglycemics

What do alpha cells in the pancreas produce?
Glucagon
What do beta cells in the pancreas produce?
Insulin
Where are beta cells found in the pancreas?
Islets of Langerhans
What do delta cells in the pancreas produce?
Somatostatin
Product of proinsulin cleavage used to assess insulin production
C-peptide
Exogenous insulin contains
No C-peptide
Endogenous insulin contains
Normal C-peptide
Very rapid acting insulin, having fastest onset and
Lispro (Humalog), aspart (Novolog),
shortest duration of action
glulisine (Apidra)
Short acting, crystalline zinc insulin used to reverse acute hyperglycemia
Regular (Humulin/Novolin R)
Long acting insulins
Glargine, 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 AGI's
Act on intestine, delay digestion and absorption of glucose formed from digestion of starch and disacchrides
SE of AGI's
Flatulence (do not use beano to tx), diarrhea, abdominal cramps
Alpha-glucosidase inhibitor associated with elevation of LFT's
Acarbose
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, sitagliptin, saxagliptin, pioglitazone
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.
MOA of both generations
Insulin release from pancreas by modifying K+ channels
Common SE of sulfonylureas, repaglinide, and nateglinide
Hypoglycemia, weight gain
Sulfonylurea NOT recommended for elderly because of very long half life
Chlorpropamide
Thiazolidinediones
Pioglitazone, Rosiglitazone, Troglitazone (withdrawn/d from market)
Reason troglitazone was withdrawn from market
Hepatic toxicity
MOA of thiazolidinediones
Decrease insulin resistance, stimulate PPAR-gamma receptors
SE of Thiazolindinediones
Edema, mild anemia; interaction with drugs that undergo CytP450 3A4 metabolism, risk for angina/MI
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
Drugs used in bone homeostasis

Available bisphosphonates
Alendronate, etidronate, risedronate, pamidronate, tiludronate, and zoledronic acid
MOA of Bisphosphonates
Inhibits osteoclast bone resorption
Names of three bisphosphonates available IV
Pamidronate, zoledronate, ibandronate
Uses of bisphosphonates
Osteoporosis, Paget's disease, and osteolytic bone lesions, and hypercalcemia from malignancy
Major SE of bisphosphonates
Chemical esophagitis
Bisphosphonates that cannot be used on continuous basis because it caused osteomalacia
Etidronate
Used for prevention of postmenopausal osteoporosis in women
Estrogen (HRT-Hormone replacement therapy)
Increase bone density, also being tested for breast CA prophlaxis
Raloxifene (SERM-selective estrogen receptor modulator)
Used intranasally and decreases bone resorption
Calcitonin (salmon prep)
Used especially in postmenopausal women, dosage should be 1500 mg
Calcium
Vitamin given with calcium to ensure proper absorption
Vitamin D