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Pharmacology > Endocrine Drugs > Flashcards

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
Q

Androgens

A

.

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26
Q

Testosterone / Methyltestosterone

A

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

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27
Q

Donazol

A

Use: endometriosis, fibrocystic breast dz

*has anti-estrogen activity as well

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28
Q

Flutamide

A

MOA: non-steroidal competitive inhibitor at androgen receptors
Use: prostate carcinoma
SE: mild gynecomastia, hot flashes, reversible hepatotoxicity

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29
Q

Spironolactone

A

MOA: mineralocorticoid receptor and androgen receptor antagonist
Use: reduction of androgenic sx’s d/t PCOS (hirsutism), aldosteronism, diuretic
SE: gynecomastia, amenorrhea, hyperkalemia

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30
Q

Finasteride

A

MOA: 5α-reductase inhibitor
Effect: decreases conversion of testosterone to DHT
Use: BPH and male-pattern baldness
SE: rarely impotence and gynecomastia

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31
Q

Ketoconazole

A

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
Q

Absolute CIs for Contraceptives

A 
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
Q

Relative CIs for Contraceptives

A 
Migraine w/o aura
HTN
Cardiac or renal dz
DM
gallbladder dz
Cholestasis during pregnancy
Sickle cell dz
Lactation
34
Q

Dinoprostone

A

MOA: synthetic PGE2
Effect: ripen cervix, stimulate uterine contractions
Use: cervical ripening to induce labor
PK: vaginal insert or cervical gel

35
Q

Misoprostol

A

MOA: PGE1 analog
Effect: ripen cervix, stimulate uterine contractions
Use: cervical ripening to induce labor
PK: intravaginal, PO, sublingual administration

36
Q

Oxytocin

A

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
Q

Methylergonovine

A

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
Q

Carboprost Tromethamine

A

PGF2α analog

PK: given IM

39
Q

Magnesium Sulfate

A

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
Q

Indomethacin

A

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
Q

Nifedipine

A

MOA: blocks entry of Ca2+ into myometrial cells, inhibiting contractility
Use: delay preterm labor
SE: maternal tachycardia, palpitations, flushing, HA, dizziness, nausea

42
Q

Atosiban

A

MOA: competitive antagonist at oxytocin receptors

NOT AVAILABLE IN THE US (so why TF they teach us this shit)

43
Q

Mifepristone + Misoprostol

A

MOA: antiprogestin + PGE1
Use: early abortion (< 8 wks)
SE: cramping and diarrhea

44
Q

Methotrexate

A

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
Q

Terbutaline

A

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
Q

Fludrocortisone

A

Mineralocorticoid w/ mainly salt-retaining effect and some anti-inflammatory effect
Use: adrenal insufficiency (low plasma Na+)

47
Q

short-acting glucocorticoids

A

Hydrocortisone and Cortisone

48
Q

Intermediate-acting Glucocorticoids

A

(12-36h)

Prednisone / Prednisolone / Methylprednisolone / Triamcinolone

49
Q

Long-acting Glucocorticoids

A

Betamethasone and Dexamethasone

*NO mineralocorticoid activity

50
Q

Steroid drugs used for premature fetal lung development

A

Betamethasone, Dexamethasone and Hydrocortisone

51
Q

Metformin

A

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
Q

Sulfonylureas

A

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
Q

Chlorpromazine

A

Class: Sulfonamide
SE: Disulfiram-like effect and SIADE

54
Q

Thiazolidinediones

A

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
Q

Rosiglitazone

A

Class: Thiazolidinedione
SE: increased risk of angina/MI

56
Q

Pioglitazone

A

Class: Thiazolidinediones
SE: increase risk of bladder ca

57
Q

GLP-1 Agonists

A

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
Q

DDP-4 Inhibitors

A

“-gliptins”
MOA: prolong the action of endogenous GLP-1
SE: pancreatitis, NASH (non-alcoholic steatohepatitis d/t fat buildup in liver)

59
Q

Miglitol / Acarbose

A

MOA: α-glycosides inhibitors
Effect: decrease absorption of glucose by decreasing starch metabolism, decrease insulin demand
SE: flatulence, GI sx’s

60
Q

Pramlintide

A

MOA: synthetic analog of amylin
Effect: delays gastric emptying, decreases appetite

61
Q

Cangliflozin

A

MOA: SGLT-2 inhibitor
Effect: decreased renal PCT reabsorption of glucose
SE: increased risk of UTIs bc of the glucosuria

62
Q

Propylthiouracin (PTU)

A

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
Q

Methimazole

A

MOA: thyroid peroxidase inhibitor
Effect: block formation of thyroid hormone in thyroid
SE: agranulocytosis, maculopapular rash
CI: pregnancy

64
Q

Propranolol (thyroid)

A

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
Q

Radioactive Iodine

A

MOA: destroys thyroid gland
CI: Grave’s ophthalmology bc it worsens the condition, harmful to fetus/children

66
Q

Bisphosphonates

A

“-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
Q

Calcitonin

A

MOA: inhibits osteoclasts bone resorption
Use: postmenopausal osteoporosis, hypercalcemia of malignancy (small cell lung ca), second-line for Paget’s if Bisphosphonates fail

68
Q

Teriparatide

A

MOA: PTH analog that stimulates osteoblasts
PK: given once daily (pulsatile)
SE: increased risk of osteosarcoma (only recommended for 2 year course)

69
Q

Denosumab

A

MOA: monoclonal ab against RANKL
Effect: prevents RANK/RANKL binding and inhibits activation of osteoclasts
Use: osteoporosis

70
Q

Vitamin D

A

Ergocalciferol and Cholecalciferol are provitamins

Calcitriol is active metabolite (assoc w/ higher rates of hypercalcemia)

71
Q

Plicamycin

A

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
Q

Sevelamer

A

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
Q

Cinacalcet

A

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
Q

Fluoride

A

MOA: enhances osteoblasts activity
Effect: increases bone density but reduces microstructure quality which increases risk of fx

75
Q

Thiazides (Ca2+)

A

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
Q

Gallium Nitrate

A

MOA: inhibits bone resorption
Use: hypercalcemia of malignancy
SE: nephrotoxicity

77
Q

Calcipotriol

A

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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