Insulin (forms)

Lispro, Regular (IV only, meal time insulin)

Lente, Ultralente (basal insulin)

Glargine (insulin analog w/ no onset or peak, used to supply a constant background level)

Glipizide and Glyburide

2nd generation sulfonylureas (1st gen. chlorpropamide) 

MOA: block K+ channels that keep beta cells hyperpolarized so that they are then depolarized and release insulin (over time get decreased release of glucagon from alpha cells)

SE: hypoglycemia, weight gain, hypersensitivity

Glipizide (dec. dose in hepatic dysfunction)

Glyburide (dec. dose in renal dysfunction)

Hypoglycemia (sxs and tx)

Sxs: lip/tongue tingling, lethargy, confusion, sweats, tremors, tachycardia, coma, seizures

Tx: oral glucose, IV dextrose if unconscious, or glucagon

Metformin

MOA: Increased tissue sensitivity to insulin and/or dec. hepatic gluconeogenesis

Uses: monotherapy or combo (synergistic w/ sulfonylureas), euglycemic b/c doesn't cause hypoglycemia

SE: possible lactic acidosis, GI distress

Acarbose

MOA: inhibits alpha-glucosidase in brush border of SI --> dec. formation of absorbable carbohydrates --> dec. postprandial glucose and demand for insulin

NO hypoglycemia

SE: GI discomfort, flatulence, diarrhea, may increase LFTs?

Pioglitazone and Rosiglitazone

Thiazolidinediones 

MOA: binds to peroxisome proliferator-activating receptors (PPARs) involved in transcription of insulin-responsive genes --> inc sensitization of tissues to insulin and receptor number & dec. in hepatic gluconeogenesis

SE: less hypoglycemia, but weight gain and edema

Exenatide

glucagon-like peptide-1

MOA: GLP-1 is an incretin released from SI and augments glucose-dependent insulin secretion

Uses: adjunct used in type 2 diabetes (have to be able to still make insulin)

SE: nausea, hypoglycemia when used w/ oral sulfonureas 

Repaglinide

MOA: stimulates insulin release from pancreatic beta cells

Use: similar to oral sulfonylureas, used as an adjunct in type-2 right before meals 

Endocrine uses for glucocorticoids

prednisone, dexamethasone, and mineralocorticoid fludrocortisone

 Uses:

Addison dz (replacement therapy)

Adrenal insufficiency states (infxn, shock, trauma)

Premature delivery to prevent respiratory distress

Adrenal hyperplasia - feedback inhibition of ACTH

Spironolactone (endocrine)

Adrenal steroid antagonist

MOA: blocks aldosterone and androgen receptors

Uses: CHF, hyperaldosteronism, female hirsutism

Mifepristone

MOA: blocks glucocorticoid and progestin receptors

Uses: abortifacient

Ketoconazole (endocrine)

Estrogens

Conjugated equine estrogens, ethinyl estradiol and mestranol, diethylstilbestrol

Uses:

female hypogonadism

hormone replacement therapy: dec. bone resorption

contraception (feedback inhibition of FSH,LH)

dysmenorrhea

uterine bleeding

acne

prostate cancer

SE: nausea, breast tenderness, endometrial hyperplasia, inc. gallbladder dz/cholestasis, inc. in blood coagulation (via dec. in antithrombin III)

Cancer risk: endometrial (unless give progestins w/) breast cancer, DES given during breast feeding can lead to vaginal adenocarcinoma in offspring

Anastrozole

MOA: aromatase inhibitor --> dec. estrogen synthesis

Use: estrogen-dependent, postmenopausal breast cancer

Clomiphene

MOA: dec. feedback inhibition --> inc. FSH/LH --> ovulation --> pregnancy

Use: fertility drug

Adverse effect: multiple births

Tamoxifen

Selective estrogen-receptor modulators

MOA: estrogen receptor agonist (bone), antagonist (breast), partial agonist (endometrium)

Uses: estrogen-dependent breast cancer and for prophylaxis in high-risk pts

SE: increased risk of endometrial cancer

Raloxifene

Selective estrogen-receptor modulators

MOA: estrogen receptor agonist (bone), antagonist (breast and uterus)

Uses: prophylaxis of postmenopausal osteoporosis

When used in menopause there is no inc. cancer risk

Medroxyprogesterone and Norethindrone

Progestins, used to increase oral bioavailability and increase feedback inhibition of LH

Uses: contraception w/ estrogens and hormone replacement therapy w/ estrogens to dec. endometrial cancer

SE: dec. HDL/inc. LDL, glucose intolerance, breakthrough bleeding, androgenic (hisutism and acne)

Oral contraceptives

combo of estrogens (ethinyl estradiol, mestranol) w/ progestins (norgestrel, norethindrone) in varied doses (suppress gonadotropins esp. LH surge)

SE: (estrogens) nausea, bloating, HA, mastalgia, (progestins) weight gain, hirsutism, acne, tiredness, depression, dec. HDL

DI: dec. effectiveness w/ antimicrobials and enzyme inducers (P450)

Benefits: dec. risk of endometrial/ovarian cancer, dec. dysmenorrhea/endometriosis/PID/osteoporosis

Methyltestosterone & Oxandrolone, Nandrolone

Oxandrolone/Nandrolone (increased anabolic action)

Uses: male hypogonadism and for anabolic actions (inc muscle mass, inc. RBCs, dec. nitrogen excretion)

SE: excessive masculinization, premature closure of epiphysis, cholestatic jaundice, aggression, dependence

Flutamide

MOA: androgen receptor blocker

Uses: androgen-receptor positive prostate cancer

Leuprolide

GnRH analong, androgen antagonist

Uses: androgen receptor positive prostate cancer

Finasteride

5-alpha reductase inhibitor

MOA: prevents conversion of testosterone to dihydrotestosterone

Uses: BPH, male pattern baldness

Propylthiouracil and Methimazole

MOA: inhibits oxidation of iodide to iodine by peroxidase, inhibits iodination of tyrosyl residues on thyroglobulin to form MIT/DIT, inhibits coupling of MIT/DIT, and high doses of PTU inhibits conversion of T4 to T3 via 5 prime deiodinase

Uses: uncomplicated hyperthyroidism

SE: maculopapular rash, both drugs X placental barrier but PTU safer b/c more protein bound

Radioactive iodine

I131, destroys thyroid

Uses: inhibits active accumulation of iodide into gland

Lugol's solution (KI + iodine)

Uses: thyrotoxicosis, preoperatively to decrease gland size, fragility and vascularity

Somatrem or Somatropin

MOA: GH

Uses: pituitary dwarfism, osteoporosis

Octreotide

MOA: somatostatin

Uses: acromegaly, carcinoid, secretory GI-tumors

Cosyntropin

MOA: ACTH

Uses: infantile spasms

Leuprolide, nafarelin

MOA: GnRH

Uses: endometriosis, prostate carcinoma (repository form) 

Urofollitropin, Placental HCG, menotropins

MOA: FSH, LH, and FSH & LH

Uses: hypogonadal states

Bromocriptine & Pergolide

Pergolide (currently off market)

MOA: prolactin inhibitory hormone

Uses: hyperprolactinemia

Desmopressin

MOA: ADH

MOA: Neurogenic (pituitary) diabetes insipidus, hemophilia A (increases VIII from liver), von Willebrand dz (increases vWF factor from endothelium), primary noturnal enuresis

Drugs used for carcinoid

Bisphosphonates

-dronate (eg: etidronate, pamidronate, alendronate) 

MOA: stabilize hydroxyapatite bone structure and induce osteoblasts to secrete inhibitors of -clasts (dec. resorption of bone)

Uses: Paget's dz, postmenopausal osteoporosis, alendronate is DOC for glucocorticoid-induced osteoporosis

SE: etidronate & pamidronate (bone mineralization defects), GI distress including esophageal ulcers in alendronate)

Teriparatide

MOA: recombinant DNA, PTH analog

Use: stimulate osteoblasts and new bone formation

SE: used for less than 2 yrs b/c increased risk of osteosarcoma