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Human Disease Systems > GI+Repro Pharm > Flashcards

GI+Repro Pharm Flashcards

1
Q

androgens

A

testosterone, methyltestosterone

HRT in hypogonadism, secondary sex characteristics in trans men, reverse protein loss (+anabolic steroids)

MOA: testosterone converted to dihydrotestosterone by 5-alpha-reductase; testosterone and dihydrotestosterone bind to cell receptors and regulate protein expression

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2
Q

androgen AEs

A

in females: masculinization (hirsutism, clitoral enlargement, deepening voice); amenorrhea

in males: azoospermia, decreased testicular size, gynecomastia

both: acne, sleep apnea, erythrocytosis, decreased HDL, increased LDL, aggressiveness, psychosis, premature closing of epiphyseal plate (short stature), hepatic dysfunction

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3
Q

antiandrogens (drugs and MOAs)

A

abiraterone: 17-alpha-hydroxylase/17,20-lyase inhibitor => decreased steroid synthesis

finasteride: type II 5-alpha-reductase inhibitor => blocks testosterone action in prostate

flutamide, bicalutamide: non-steroidal antiandrogen

spironolactone: aldosterone antagonist that also antagonizes testosterone receptor (may also inhibit synthesis)

ketoconazole: antifungal that also inhibits 17-alpha-hydroxylase/17,20-lyase

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4
Q

antiandrogen indications

A

abiraterone: metastatic prostate cancer, hypertension, hypokalemia

finasteride: benign prostatic hyperplasia, male pattern baldness

flutamide, bicalutamide: prostate cancer; to treat flare response when GnRH analogues are used; hirsutism

spironolactone: PCOS, hirsutism (off-label)

ketoconazole: prostate cancer (not first line)

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5
Q

selective estrogen receptor modulators (SERMs)

A

tamoxifen: antagonist in breast, partial agonist in endometrium

raloxifene: antagonist in breast and endometrium, agonist at bone

clomiphene: antagonist in hypothalamus and pituitary, agonist in ovary => induces ovulation

tamoxifen, raloxifene for osteoporosis; clomiphene to stimulate ovulation

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6
Q

selective estrogen receptor modulators (SERMs): AEs

A

tamoxifen: venous thrombosis, hot flashes, weight gain due to fluid retention, mild nausea, endometrial carcinoma

raloxifene: same as tamoxifen but WITHOUT endometrial carcinoma

clomiphene: ovarian enlargement, hot flashes

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7
Q

aromatase inhibitors

A

anastrozole, letrozole

MOA: block synthesis of estrogen

indication: ER+ breast cancer in post-menopausal women; ovulation induction (letrozole)

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8
Q

danazole

A

MOA: weak partial agonist activity at progestin, androgen, and glucocorticoid receptors; also inhibits steroid synthesis

indication: endometriosis, fibrocystic disease of breast

AE: weight gain, edema, decreased breast size, acne, oily skin, increased hair growth

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9
Q

fulvestrant

A

MOA: selective estrogen receptor downregulator (SERD) and potent antiestrogen; immobilizes ERa in nuclear matrix => polyubiquitination and degradation via 26S proteosome

indication: ER+ breast cancer when other treatments have failed

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10
Q

mifepristone

A

MOA: competitive progesterone antagonist => causes blastocyst to die => eliminates source of hCG required to maintain corpus luteum

indication: induces abortion; administered with misoprostol (stimulates uterine contractions)

AE: excessive vaginal bleeding

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11
Q

estrogen preparations

A

premarin, prempro (conjugated equine estrogens)

ethinyl estradiol, mestranol (synthetic estrogen)

transdermal estradiol

estradiol cypionate, estradiol valerate (slowly absorbed IM injections)

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12
Q

progestin preparations

A

medroxyprogesterone acetate (progesterone esters)

norgestrel, levonorgestrel (earlier synthetic analogues that have some androgenic activity)

northindrone (intermediate androgenic activity)

drospirenone (spironolactone derivative with anti-aldosterone and anti-androgenic effects)

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13
Q

combination oral contraceptives

A

yasmin (ethinyl estradiol + drospirenone); ethinyl estradiol + levonorgestrel

MOA: prevent midcycle LH surge at hypothalamus and pituitary; also cause glandular atrophy of uterine endometrium and formation of thick cervical mucus

AE (estrogen): nausea, breast tenderness, edema, skin hyperpigmentation, migraine, headache, hypertension, small increased risk of gallstones or gallbladder disease, endometrial hyperplasia/ cancer, increased blood coagulation, DVT, MI, strike

AE (progesterone): hirsutism, acne, weight gain, glucose intolerance, increased LDL, decreased HDL, breakthrough bleeding, depression, vaginitis, UTI

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14
Q

progestin-only contraception

A

norethindrone

MOA: prevents ovulation in 70-80% of cycles by slowing frequency of GnRH pulse generation and blunting LH surge; thickens cervical mucus; endometrial atrophy

indication: breastfeeding women and those with estrogen contraindications

AE: more irregular spotting

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15
Q

morning-after contraception

A

levonorgestrel (Plan B): may prevent ovulation, transport of fertilized egg, or implantation

ulipristal: progesterone receptor modulator

AE: cramping, nausea

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16
Q

drugs used in HRT for osteoporosis

A

raloxifene (SERM), allendronate (bisphosphae derivative)

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17
Q

drugs to treat gonorrhea (name, MOA, AE)

A

ceftriaxone
-MOA: third generation cephalosporin; inhibits cell wall synthesis by binding to transpeptidase
-AE: hypersensitivity reactions, seizures

doxycycline
-MOA: tetracycline; inhibits protein synthesis by binding to 30S subunit and blocking amino acid-linked tRNA from binding
-AE: esophageal irritation, discoloration of teeth (contraindicated in pregnancy and children)

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18
Q

drugs to treat syphilis (drug, MOA, AE)

A

penicillin G

MOA: inhibits biosynthesis of cell wall peptidoglycan => makes organism osmotically unstable

AE: Jarisch-Herxheimer reaction (acute febrile reaction with headache and myalgia that occurs within 24 hours of syphilis treatment - not a penicillin AE)

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19
Q

drugs to treat trichomoniasis (drugs, MOA, AE)

A

metronidazole (preferred), tinidazole

MOA: nitroimidazole family; nitro group is reduced in anaerobic bacteria and sensitive protozoans, reactive products are responsible for antimicrobial activity

AE: nausea, headache, anorexia, metallic taste; patients should abstain from alcohol for 24 hours

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20
Q

drugs to treat pelvic inflammatory disease (regimens, MOA, AE)

A

1) ceftriaxone + doxycycline + metronidazole

2) cefotetan OR cefoxitin + doxycycline

cefoxitin/cefotetan:
-MOA: second generation cephalosporins
-AE: thrombophlebitis, disulfiram-like reaction with ethanol, inhibit vitamin K production (prolong bleeding time)

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21
Q

drugs to treat herpes (drugs, MOA, AE)

A

acyclovir, famciclovir, valacyclovir

MOA: nucleoside analogues; phosphorylated by viral thymidine kinase => compound acts as a substrate and inhibitor of viral DNA polymerase and is incorporated into DNA (terminates chain elongation)

AE: crystalluria if not well-hydrated

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22
Q

[?] has a lower degree of placental metabolism, so it crosses the placenta; it is used to promote fetal lung maturation

A

betamethasone (a corticosteroid)

23
Q

[?] overdose is the most common poisoning in pregnancy

A

acetaminophen

fetal hepatocytes cannot conjugate the highly reactive metabolic intermediate

24
Q

[?] have been associated with fetal renal failure, and are contraindicated in pregnancy

A

angiotensin-converting enzyme (ACE) inhibitors

25
Q

[?] may produce fetal hypothyroidism when exposure occurs beyond 12-14 weeks

A

propylthiouracil, methimazole

26
Q

[?] chelate calcium ions that are deposited in developing teeth, producing discoloration

A

tetracyclines (doxycycline)

27
Q

fetal exposure to [?] causes vaginal carcinoma in young women

A

diethylstilbestrol

28
Q

injectable drugs for ED

A

aprostadil (PGE1 analogue => increases cAMP)

trimix (phentolamine [blocks a-adrenergic receptor vasoconstriction] + papaverine [vasorelaxation] + PGE1 [increases cAMP])

AE: pain at injection site

29
Q

phosphodiesterase-5 inhibitors for ED

A

sildenafil, vardenafil, tadalafil

MOA: inhibition of PDE-5 prevents the degradation of cGMP => potentiates relaxation of corporeal arterial and sinusoidal smooth muscle

AE: headache, flushing, dyspepsia, nasal congestion, altered vision (blue aura), diarrhea

30
Q

centrally acting agent for ED

A

apomorphine

MOA: dopamine D1/D2 agonist; works at level of hypothalamus

AE: nausea, headache, yawning, dizziness

31
Q

proton pump inhibitors

A

lansoprazole, omeprazole, esomeprazole, pantoprazole, dexlansoprazole

use: peptic ulcer disease, NSAID-associated ulcers, GERD, laryngopharyngeal reflux, Zollinger-Ellison syndrome, stress-related gastritis

MOA: forms covalent disulfide link with cysteinyl residue in proton pump on luminal side of parietal cells => irreversible inhibition of acid secretion

AE: increased hip fractures, B12 deficiency, increased C. difficile, possible pneumonia link, chronic use can => fundic gland polyposis of stomach and chronic kidney disease

32
Q

omeprazole/ esomeprazole drug interactions

A

inhibits metabolism of warfarin, diazepam, phenytoin, carbamazepine

inhibits conversion of clopidogrel to active form

33
Q

gastric antacids

A

aluminum and magnesium hydroxides, calcium carbonate, sodium bicarbonate

use: acid indigestion, peptic ulcer disease

MOA: neutralizes acid

AE: constipation (aluminum alone), diarrhea (magnesium alone), calcium carbonate and sodium bicarbonate => flatulence

34
Q

mucosal protective agents

A

sucralfate: adheres to ulcer craters and epithelial cells, allows ulcer to heal
-use: peptic ulcer disease
-DDI: inhibits absorption of digoxin

bismuth subsalicylate: antisecretory, anti-inflammatory, antimicrobial effects
-use: nausea, abdominal cramps
-AE: dark stool, black staining of tongue

35
Q

antihistamines for nausea/vomiting

A

dimenhydrinate, meclizine, diphenhydramine: motion sickness

promethazine: nausea/vomiting induced by medications, anesthetics, etc.

doxylamine, pyridoxine (B6): nausea/vomiting related to pregnancy

MOA: block H1 receptors, significant antimuscarinic activity

AE: sedation, confusion, dizziness, tinnitus, incoordination, tremors, antimuscarinic effects

36
Q

anticholinergics for nausea/vomiting

A

scopolamine

uses: motion sickness, postoperative nausea/vomiting

AE: dry mouth, urinary retention, blurred vision, exacerbation of narrow angle glaucoma

37
Q

dopamine receptor antagonists for nausea/vomiting

A

prochlorperazine: post-chemotherapy/radiation nausea/vomiting, pre/postoperative

metoclopramide: nausea/vomiting in GI dysmotility syndromes, GERD, intractable hiccups

MOA: blocks D2 (both) and 5HT3 (metoclopramide) receptors in chemo trigger zone

AE: sedation, dystonia, EPS, impaired thermoregulation, tardive dyskinesia

38
Q

serotonin receptor antagonists for nausea/vomiting

A

ondansetron, granisetron, palonosetron

use: chemotherapy/ irradiation-induced nausea/vomiting, postoperative

MOA: 5HT3 antagonist that acts at solitary tract nucleus and area postrema

39
Q

substance P antagonists for nausea/vomiting

A

aprepitant, fosaprepitant

MOA: substance P is present in vagal afferents innervating solitary tract nucleus

uses: combined with other treatments, delayed nausea

40
Q

agents to treat chronic hepatitis B

A

entecavir: nucleoside analogue that inhibits all 3 functions of BHV polymerase

tenofovir: nucleotide analogue

INF-alpha/pegylated interferon: binds to cell surface receptors => suppression of cell proliferation, increased phagocytosis, augmentation of lymphocytic cytotoxicity, inhibits viral replication

41
Q

INF-alpha/pegylated interferon AE

A

severe flare of disease (prelude to HBeAg clearance, can lead to liver failure in patients with cirrhosis)

headache, fever, chills, myalgia, malaise in 30% during first week of therapy

42
Q

agents to treat chronic hepatitis C

A

glecaprevir: NS3/4A protease inhibitor

velpatasvir, ledipasavir, pibrentasvir: NS5A inhibitor

sofosbuvir: NS5B polymerase inhibitor

43
Q

agents to treat IBD

A

dicyclomine: antimuscarinic; blocks muscarinic receptors on enteric plexus and smooth muscle

sulfasalazine/ mesalamine: 5-aminosalicylic acid may inhibit prostaglandin synthesis, block neutrophil migration, or act as free radical scavengers

azathioprine, 6-mercaptopurine, methotrexate: immunosppressants

infliximab, adalimumab: anti-TNF

vedolizumab: integrin receptor antagonist (prevent T cell migration)

44
Q

agents to treat non-infectious diarrhea

A

diphenoxylate, loperamide: opioid agonists => sustained segmental contraction of smooth muscle, which prevents rhythmic waves of smooth muscle

bismuth subsalicylate: inhibits intestinal secretions

45
Q

bulk-forming laxatives

A

bran, psyllium, methylcellulose

MOA: indigestable hydrophilic substances that swell upon contact with water, forming a bulky gel that distends colon and promotes peristalsis

AE: abdominal pain; flatulence and bloating (bran)

46
Q

stool softeners

A

docusate sodium

MOA: emulsify stool by permitting water and lipids to penetrate; may also cause water secretion into intestine and colon

short-term setting only

47
Q

lubricants

A

mineral oil, glycerin suppositories

MOA: coat the bowel and decrease colonic absorption of water => easier passage of stool

AE: long-term use can impair absorption of fat-soluble vitamins

48
Q

stimulant laxatives

A

senna, bisacodyl

MOA: thought to stimulate intestinal motility

AE: abdominal cramps, diarrhea

short-term treatments only; bowel prep for colonoscopy (biscodyl)

49
Q

osmotic laxatives

A

magnesium hydroxide, lactulose, low dose polyethylene glycol

MOA: poorly absorbed in intestine and colon => net water movement into GI tract => distends bowel, increasing intestinal motility

magnesium hydroxide can cause hypermagnesium in patients with renal insufficiency

50
Q

purgatives

A

balanced polyethylene glycol, magnesium citrate, sodium phosphate

MOA: rapid movement of water into distal small bowel => high volume liquid stool

AE: magnesium citrate and sodium phosphate can cause electrolyte disorders

51
Q

chloride channel activators (laxatives)

A

lubiprostone: directly stimulates chloride channel in small intestine => chloride-rich secretion in intestine => stimulates intestinal motility

linaclatode: stimulates guanylate cyclase on luminal side of epithelium => increase chloride and bicarb secretion => increased fluid retention and motility

52
Q

anti-nematodes

A

albendazole, mebendazole: binds B-tubulin => inhibits production of tubulin dimers and formation of cytoplasmic tubules => decrease glucose uptake, depletes, glycogen/ATP

pyrantel pamoate: activate cholinergic receptors => depolarization blockade

ivermectin: may activate glutamate-gated chloride channel => hyperpolarize cell membrane

moxidectin: binds chloride channels and GABA receptors to increase permeability => paralysis of pharyngeal muscles

53
Q

anti-trematodes/ cestodes

A

praziquantel

MOA: increased permeability of outer segment (tegument) of schistosomes to Ca++ => depolarization; also causes tegument breakdown

54
Q

anti-ectoparasides

A

permethrin: blocks sodium channels => paralysis

malathion: inhibits acetylcholinesterase => increase ACh => activate and desensitize nicotinic receptors

spinosad: activates nicotinic receptors => paralysis

Human Disease Systems (11 decks)

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