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Endocrine Drugs Flashcards

1
Q

Mecasermin

A

MOA: IGF-1 analog
Use: children w/ IGF-1 deficiency
SE: hypoglycemia, intracranial HTN, asymptomatic elevation of liver enzymes

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2
Q

Pegvisomant

A

MOA: GH receptor antagonist

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3
Q

Octreotide

A

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)

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4
Q

Bromocriptine and Cabergoline

A

MOA: dopamine agonists
Use: hyperprolactinemia, acromegaly
SE: nausea, HA, orthostatic hypotension, psych sx’s, cold-induced vasospasm, pulmonary infiltrates w/ chronic high-dose therapy

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5
Q

Follitropin and Urofollitropin

A

MOA: purified FSH

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6
Q

Menotropins

A

MOA: purified extract of FSH and LH

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7
Q

Gonadorelin

A

MOA: gonadotropin-releasing hormone

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8
Q

Goserelin, Leuprolide, Na\farelin

A

MOA: gonadotropin-releasing hormone analogs

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9
Q

Leuprolide and Nafarelin

A

Use: central precocious puberty

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10
Q

Cetrorelix and Ganirelix

A

MOA: competitive antagonist of GnRH receptors
Effect: prevent LH surge during controlled ovarian hyper stimulation
Use: suppression of gonadotropin production

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11
Q

Corticotropin and Cosyntropin

A

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?)

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12
Q

Oxytocin

A

.

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13
Q

Somatotropin

A

MOA: growth hormone
Effect: mediated by IGF-1 via the JAK/STAT pathway

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14
Q

Ethinyl Estradiol and Mestranol

A

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

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15
Q

Selective Estrogen Receptor Modulators (SERMS) names

A

Tamoxifen / Raloxifene / Clomiphene

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16
Q

Tamoxifen

A

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

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17
Q

Raloxifene

A

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

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18
Q

Clomiphene

A

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

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19
Q

Fluvestrant

A

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

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20
Q

Anastrozole and Letrozole

A

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

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21
Q

Exemestrane

A

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

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22
Q

Synthetic Progestins

A

Medroxyprogesterone / Norgestrol / Norethindrone / Norgestimate / Desogestreol / Drospirenone

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23
Q

Progestins

A

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

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24
Q

Mifepristone

A

Antiprogestin
MOA: competitive inhibitor at progesterone receptor
Use: combo w/ Misoprostol as abortifacient
SE: N/V/D/abd pn, uterine bleeding

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25
Androgens
.
26
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
27
Donazol
Use: endometriosis, fibrocystic breast dz | *has anti-estrogen activity as well
28
Flutamide
MOA: non-steroidal competitive inhibitor at androgen receptors Use: prostate carcinoma SE: mild gynecomastia, hot flashes, reversible hepatotoxicity
29
Spironolactone
MOA: mineralocorticoid receptor and androgen receptor antagonist Use: reduction of androgenic sx’s d/t PCOS (hirsutism), aldosteronism, diuretic SE: gynecomastia, amenorrhea, hyperkalemia
30
Finasteride
MOA: 5α-reductase inhibitor Effect: decreases conversion of testosterone to DHT Use: BPH and male-pattern baldness SE: rarely impotence and gynecomastia
31
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
32
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 ```
33
Relative CIs for Contraceptives
``` Migraine w/o aura HTN Cardiac or renal dz DM gallbladder dz Cholestasis during pregnancy Sickle cell dz Lactation ```
34
Dinoprostone
MOA: synthetic PGE2 Effect: ripen cervix, stimulate uterine contractions Use: cervical ripening to induce labor PK: vaginal insert or cervical gel
35
Misoprostol
MOA: PGE1 analog Effect: ripen cervix, stimulate uterine contractions Use: cervical ripening to induce labor PK: intravaginal, PO, sublingual administration
36
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
37
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
38
Carboprost Tromethamine
PGF2α analog | PK: given IM
39
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
40
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
41
Nifedipine
MOA: blocks entry of Ca2+ into myometrial cells, inhibiting contractility Use: delay preterm labor SE: maternal tachycardia, palpitations, flushing, HA, dizziness, nausea
42
Atosiban
MOA: competitive antagonist at oxytocin receptors | NOT AVAILABLE IN THE US (so why TF they teach us this shit)
43
Mifepristone + Misoprostol
MOA: antiprogestin + PGE1 Use: early abortion (< 8 wks) SE: cramping and diarrhea
44
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
45
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
46
Fludrocortisone
Mineralocorticoid w/ mainly salt-retaining effect and some anti-inflammatory effect Use: adrenal insufficiency (low plasma Na+)
47
short-acting glucocorticoids
Hydrocortisone and Cortisone
48
Intermediate-acting Glucocorticoids
(12-36h) | Prednisone / Prednisolone / Methylprednisolone / Triamcinolone
49
Long-acting Glucocorticoids
Betamethasone and Dexamethasone | *NO mineralocorticoid activity
50
Steroid drugs used for premature fetal lung development
Betamethasone, Dexamethasone and Hydrocortisone
51
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
52
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
53
Chlorpromazine
Class: Sulfonamide SE: Disulfiram-like effect and SIADE
54
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)
55
Rosiglitazone
Class: Thiazolidinedione SE: increased risk of angina/MI
56
Pioglitazone
Class: Thiazolidinediones SE: increase risk of bladder ca
57
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
58
DDP-4 Inhibitors
“-gliptins” MOA: prolong the action of endogenous GLP-1 SE: pancreatitis, NASH (non-alcoholic steatohepatitis d/t fat buildup in liver)
59
Miglitol / Acarbose
MOA: α-glycosides inhibitors Effect: decrease absorption of glucose by decreasing starch metabolism, decrease insulin demand SE: flatulence, GI sx’s
60
Pramlintide
MOA: synthetic analog of amylin Effect: delays gastric emptying, decreases appetite
61
Cangliflozin
MOA: SGLT-2 inhibitor Effect: decreased renal PCT reabsorption of glucose SE: increased risk of UTIs bc of the glucosuria
62
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
63
Methimazole
MOA: thyroid peroxidase inhibitor Effect: block formation of thyroid hormone in thyroid SE: agranulocytosis, maculopapular rash CI: pregnancy
64
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
65
Radioactive Iodine
MOA: destroys thyroid gland CI: Grave’s ophthalmology bc it worsens the condition, harmful to fetus/children
66
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
67
Calcitonin
MOA: inhibits osteoclasts bone resorption Use: postmenopausal osteoporosis, hypercalcemia of malignancy (small cell lung ca), second-line for Paget’s if Bisphosphonates fail
68
Teriparatide
MOA: PTH analog that stimulates osteoblasts PK: given once daily (pulsatile) SE: increased risk of osteosarcoma (only recommended for 2 year course)
69
Denosumab
MOA: monoclonal ab against RANKL Effect: prevents RANK/RANKL binding and inhibits activation of osteoclasts Use: osteoporosis
70
Vitamin D
Ergocalciferol and Cholecalciferol are provitamins Calcitriol is active metabolite (assoc w/ higher rates of hypercalcemia)
71
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+)
72
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
73
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
74
Fluoride
MOA: enhances osteoblasts activity Effect: increases bone density but reduces microstructure quality which increases risk of fx
75
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
76
Gallium Nitrate
MOA: inhibits bone resorption Use: hypercalcemia of malignancy SE: nephrotoxicity
77
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

Pharmacology (27 decks)

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