Endocrine Drugs Flashcards
Mecasermin
MOA: IGF-1 analog
Use: children w/ IGF-1 deficiency
SE: hypoglycemia, intracranial HTN, asymptomatic elevation of liver enzymes
Pegvisomant
MOA: GH receptor antagonist
Octreotide
MOA: somatostatin analog
Effect: inhibits release of GH, TSH, glucagon, insulin and gastrin
Use: reduces sx’s caused by hormone-secreting tumors, helps localize neuroendocrine tumors, acute control of bleeding from esophageal varices
SE: N/V/steatorrhea/constipation, gallstones, cardio conduction disturbances, B12 deficiency (long-term use)
Bromocriptine and Cabergoline
MOA: dopamine agonists
Use: hyperprolactinemia, acromegaly
SE: nausea, HA, orthostatic hypotension, psych sx’s, cold-induced vasospasm, pulmonary infiltrates w/ chronic high-dose therapy
Follitropin and Urofollitropin
MOA: purified FSH
Menotropins
MOA: purified extract of FSH and LH
Gonadorelin
MOA: gonadotropin-releasing hormone
Goserelin, Leuprolide, Na\farelin
MOA: gonadotropin-releasing hormone analogs
Leuprolide and Nafarelin
Use: central precocious puberty
Cetrorelix and Ganirelix
MOA: competitive antagonist of GnRH receptors
Effect: prevent LH surge during controlled ovarian hyper stimulation
Use: suppression of gonadotropin production
Corticotropin and Cosyntropin
MOA: ACTH analogs
Effect: increased production of hormones from adrenal cortex
Use: differentiate between primary and secondary adrenal insufficiency, tx infantile spasm (West Syndrome)
SE: similar to glucocorticoids (Cushingoid?)
Oxytocin
.
Somatotropin
MOA: growth hormone
Effect: mediated by IGF-1 via the JAK/STAT pathway
Ethinyl Estradiol and Mestranol
MOA: synthetic estrogens
Effect: secondary female sex traits, endometrial proliferation, decreased bone resorption, increased HDL and decreased LDL, increased production of clotting factors 2, 7, 9, 10; increased production of NO and prostacyclin in vasculature
Use: post-menopausal hormone therapy, primary hypogonadism, oral contraceptives, menstrual abnormalities, tx of androgen-dependent prostate ca
Selective Estrogen Receptor Modulators (SERMS) names
Tamoxifen / Raloxifene / Clomiphene
Tamoxifen
MOA: binds to estrogen receptor and act as antagonist in breast tissue, and agonist in non-breast tissue (endometrium, liver, bone)
Use: prevention and tx of hormone-responsive breast ca (can lower risk of osteoporosis in breast ca pt undergoing tx)
SE: hot flashes, nausea, endometrial hyperplasia, thromboembolism
Raloxifene
MOA: bind estrogen receptors and act as antogonist in uterus and breast tissue, and as agonist in bone (inhibit resorption)
Use: prevention of hormone-responsive breast ca, prevent and tx osteoporosis in post-menopausal women
SE: hot flashes, nausea, leg cramps, thromboembolism, but NO RISK of endometrial hyperplasia
Clomiphene
MOA: acts as antagonist in hypothalamus
Effect: prevents normal feedback inhibition
Use: tx of infertility associated w/ anovulatory cycles (e.g. PCOS)
SE: hot flashes, N/V, wt gain, breast tenderness, ovarian hyper-stimulation, multiple simultaneous pregnancies, visual disturbances
Fluvestrant
Selective Estrogen Receptor Downregulator (SERD)
MOA: bind estrogen receptors and cause the receptor to be degraded and downregulated in all tissues
Use: adjuvant tx of hormone-receptor positive metastatic breast ca that is resistant to first-line antiestrogen (Tamoxifen) therapy
PK: given IM
SE: hot flashes, arthralgias, myalgias
Anastrozole and Letrozole
Non-steroidal aromatase inhibitor
MOA: competitive reversible inhibitor of aromatase
Effect: less peripheral conversion of androgens to estrogen
Use: adjuvant in chemo tx in ER+ breast ca
SE: hot flashes, nausea, fatigue, alopecia, dermatitis
Exemestrane
Steroidal aromatase inhibitor
MOA: irreversible inhibitor of aromatase
Effect: less peripheral conversion of androgens to estrogen
Use: adjuvant in chemo tx in ER+ breast ca
SE: hot flashes, nausea, fatigue, alopecia, dermatitis
Synthetic Progestins
Medroxyprogesterone / Norgestrol / Norethindrone / Norgestimate / Desogestreol / Drospirenone
Progestins
MOA: bind progesterone receptor and activate gene expression
Effect: decrease growth and increases vascularization of endometrium, thickening of cervical mucus, assoc w/ increased body temp, maintenance of pregnancy
Use: contraceptives, endometrial ca, abnml uterine bleeding, HRT, infertility
Mifepristone
Antiprogestin
MOA: competitive inhibitor at progesterone receptor
Use: combo w/ Misoprostol as abortifacient
SE: N/V/D/abd pn, uterine bleeding
Androgens
.
Testosterone / Methyltestosterone
Use: tx primary or secondary hypogonadism, chronic wasting assoc w/ HIV or cancer, stimulate anabolism to promote recovery s/p burns, increase lean body mass in athletes
Donazol
Use: endometriosis, fibrocystic breast dz
*has anti-estrogen activity as well
Flutamide
MOA: non-steroidal competitive inhibitor at androgen receptors
Use: prostate carcinoma
SE: mild gynecomastia, hot flashes, reversible hepatotoxicity
Spironolactone
MOA: mineralocorticoid receptor and androgen receptor antagonist
Use: reduction of androgenic sx’s d/t PCOS (hirsutism), aldosteronism, diuretic
SE: gynecomastia, amenorrhea, hyperkalemia
Finasteride
MOA: 5α-reductase inhibitor
Effect: decreases conversion of testosterone to DHT
Use: BPH and male-pattern baldness
SE: rarely impotence and gynecomastia
Ketoconazole
MOA: potent non-selective inhibitor of adrenal and gonadal steroid synthesis
Use: Cushing’s syndrome (non-operable), prostate cancer (resistant to other drugs)
SE: gynecomastia, amenorrhea, CYP450 inhibitor
Absolute CIs for Contraceptives
Pregnancy Thrombophlebitis or thromboembolic disorders Stroke or CAD Breast cancer Abnormal vaginal bleeding Estrogen-dependent cancer Tumor of the liver Uncontrolled HTN DM w/ vascular dz Age > 35 and smoking > 15 cigarettes/day Thrombophlebitis Migraine WITH aura Active hepatitis Surgery/injury w/ prolonged immobilization
Relative CIs for Contraceptives
Migraine w/o aura HTN Cardiac or renal dz DM gallbladder dz Cholestasis during pregnancy Sickle cell dz Lactation
Dinoprostone
MOA: synthetic PGE2
Effect: ripen cervix, stimulate uterine contractions
Use: cervical ripening to induce labor
PK: vaginal insert or cervical gel
Misoprostol
MOA: PGE1 analog
Effect: ripen cervix, stimulate uterine contractions
Use: cervical ripening to induce labor
PK: intravaginal, PO, sublingual administration
Oxytocin
MOA: activates Gq, activation of phospholipase C and increases release of Ca2+ from SR, also activates voltage-gated Ca2+ channels which activates MLCK = contractions
Use: labor induction, postpartum hemorrhage
SE: fetal distress, placental abruption or uterine rupture, at high concentrations can activate vasopressin receptors causing fluid retention, hyponatremia, heart failure, sz and death
Methylergonovine
MOA: partial α1 agonist and some serotonin agonism
Use: postpartum hemorrhage
SE: HTN, HA, n/v, CP
CI: angina pectoris, MI, pregnancy, CVA, TIA, HTN
Carboprost Tromethamine
PGF2α analog
PK: given IM
Magnesium Sulfate
MOA: uncoupled excitation-contraction in myometrial cells through inhibition of cellular APs
Use: primary tocolytic agent to tx preterm labor
SE: respiratory distress or cardiac arrest in mother, respiratory and motor depression of neonate
Indomethacin
MOA: NSAID to block prostaglandins affect on the uterus
Use: delay preterm labor
SE: can cause oligohydramnios, premature closure of ductus arteriosus
CI: don’t use after 32 wks gestation
Nifedipine
MOA: blocks entry of Ca2+ into myometrial cells, inhibiting contractility
Use: delay preterm labor
SE: maternal tachycardia, palpitations, flushing, HA, dizziness, nausea
Atosiban
MOA: competitive antagonist at oxytocin receptors
NOT AVAILABLE IN THE US (so why TF they teach us this shit)
Mifepristone + Misoprostol
MOA: antiprogestin + PGE1
Use: early abortion (< 8 wks)
SE: cramping and diarrhea
Methotrexate
MOA: inhibition of dihydrofolate reductase
Effect: buildup of DHF polyglutamate and MTX polyglutamate
Use: off-label for early abortion (< 8 wks)
PK: given injection of MTX and pregnancy will abort w/in days-wks
SE: nausea and cramping
Terbutaline
MOA: β2 agonist leads to activation of Gs protein causing increase in cAMP, activation of PKA which phosphorylates MLCK
Effect: relaxation of myometrial smooth muscle
Use: delaying preterm labor
SE: n/v, CP, dyspnea, hyperglycemia, hypokalemia, hypotension
Serious complications: pulmonary edema, cardiac insufficiency, arrhythmias, MI, maternal death
Fludrocortisone
Mineralocorticoid w/ mainly salt-retaining effect and some anti-inflammatory effect
Use: adrenal insufficiency (low plasma Na+)
short-acting glucocorticoids
Hydrocortisone and Cortisone
Intermediate-acting Glucocorticoids
(12-36h)
Prednisone / Prednisolone / Methylprednisolone / Triamcinolone
Long-acting Glucocorticoids
Betamethasone and Dexamethasone
*NO mineralocorticoid activity
Steroid drugs used for premature fetal lung development
Betamethasone, Dexamethasone and Hydrocortisone
Metformin
MOA: increases tissue sensitivity to insulin
Effect: increased up take of glucose via GLUT-4, decreased gluconeogenesis in liver by decreasing PEP CK activity
Use: first-line tx in DM2
SE: lactic acidosis and GI upset, can cause decreased absorption of folate and B12
Sulfonylureas
MOA: block ATP-dependent K+ channels in β cells of pancreas causing depolarization which allows Ca2+ influx
Effect: increased insulin release d/t influx of Ca2+
Use: DM2
SE: HS rxn, rash, hypoglycemia and weight gain
PK: high plasma protein binding, metabolized by P450
Chlorpromazine
Class: Sulfonamide
SE: Disulfiram-like effect and SIADE
Thiazolidinediones
MOA: stimulate PPAR-γ, altering expression of insulin-responsive genes
Effect: sensitize tissues to insulin via adiponectin, decrease gluconeogenesis, decrease serum TGs
SE: edema, CHF exacerbation (so CI in these pt’s)
Rosiglitazone
Class: Thiazolidinedione
SE: increased risk of angina/MI
Pioglitazone
Class: Thiazolidinediones
SE: increase risk of bladder ca
GLP-1 Agonists
Exenatide / Liraglutide
MOA: stimulate release of GLP-1 (glucagon like peptide 1)
SE: pancreatitis, increased risk of medullary carcinoma of thyroid
CI: MEN2 pt bc of thyroid ca risk
DDP-4 Inhibitors
“-gliptins”
MOA: prolong the action of endogenous GLP-1
SE: pancreatitis, NASH (non-alcoholic steatohepatitis d/t fat buildup in liver)
Miglitol / Acarbose
MOA: α-glycosides inhibitors
Effect: decrease absorption of glucose by decreasing starch metabolism, decrease insulin demand
SE: flatulence, GI sx’s
Pramlintide
MOA: synthetic analog of amylin
Effect: delays gastric emptying, decreases appetite
Cangliflozin
MOA: SGLT-2 inhibitor
Effect: decreased renal PCT reabsorption of glucose
SE: increased risk of UTIs bc of the glucosuria
Propylthiouracin (PTU)
MOA: thyroid peroxidase inhibitor, peripheral 5’-deiodinase inhibitor
Effect: block formation of thyroid hormone in thyroid
Use: hyperthyroidism, safe in pregnancy
SE: agranulocytosis, maculopapular rash
Methimazole
MOA: thyroid peroxidase inhibitor
Effect: block formation of thyroid hormone in thyroid
SE: agranulocytosis, maculopapular rash
CI: pregnancy
Propranolol (thyroid)
MOA: blocks β1 and β2 adrenergic receptors and inhibits 5’-deiodinase
DOC: initial drug used in thyroid storm
Use: symptomatic relief in Grave’s
Radioactive Iodine
MOA: destroys thyroid gland
CI: Grave’s ophthalmology bc it worsens the condition, harmful to fetus/children
Bisphosphonates
“-dronate”
MOA: analogs of pyrophosphate, stabilize hdyroxyapatite
Effect: inhibit bone resorption
Use: first line tx of Paget dz, osteoporosis, malignancy assoc. w/ hypercalcemia (small cell lung ca)
SE: erosion of esophagus/stomach, osteonecrosis of jaw, increased risk of esophageal adenocarcinoma
Calcitonin
MOA: inhibits osteoclasts bone resorption
Use: postmenopausal osteoporosis, hypercalcemia of malignancy (small cell lung ca), second-line for Paget’s if Bisphosphonates fail
Teriparatide
MOA: PTH analog that stimulates osteoblasts
PK: given once daily (pulsatile)
SE: increased risk of osteosarcoma (only recommended for 2 year course)
Denosumab
MOA: monoclonal ab against RANKL
Effect: prevents RANK/RANKL binding and inhibits activation of osteoclasts
Use: osteoporosis
Vitamin D
Ergocalciferol and Cholecalciferol are provitamins
Calcitriol is active metabolite (assoc w/ higher rates of hypercalcemia)
Plicamycin
Antineoplastic abx
MOA: inhibition of DNA-dependent RNA synthesis
Effect: osteoclasts unable to respond to PTH
Use: indicated when Bisphosphonates and Calcitonin fail
SE: thrombocytopenia, hemorrhage, death
(Monitor platelets, LFTs, creatinine, Ca2+)
Sevelamer
MOA: chelate phosphate trapping in the gut w/o affecting Ca2+ absorption
Use: dialysis pt
SE: Sevalemer Hydrochloride assoc w/ metabolic acidosis where Sevalemer Carbonate isn’t
Cinacalcet
MOA: enhances sensitivity of PTH Ca2+ sensing receptor to extracellular Ca2+
Use: dialysis pt w/ 2° hyperparathyroidism refractory to phosphate binders and Vit D supplementation
Fluoride
MOA: enhances osteoblasts activity
Effect: increases bone density but reduces microstructure quality which increases risk of fx
Thiazides (Ca2+)
MOA: inhibit Na+/Cl- symporter in DCT
Effect: increase proximal reabsorption of Ca2+ d/t volume depletion, increased Ca2+ reabsorption in DCT
SE: hypokalemia, hypomagnesemia, hyperglycemia, hypercalcemia
Gallium Nitrate
MOA: inhibits bone resorption
Use: hypercalcemia of malignancy
SE: nephrotoxicity
Calcipotriol
Synthetic Vid D3 analog
MOA: inhibits keratinocytes proliferation and enhances keratinocyte differentiation in pt w/ Psoriasis
Use: topical tx for psoriasis
SE: burning/dermatitis @ site
