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GI pharm Flashcards

1
Q

cimetidine
ranitidine
famotidine
nizatidine

A

H2 receptor antagonists:

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2
Q

omeprazole and the –prazoles

A

MOA: Irreversible inhibition of gastric-parietal cell proton pump -prodrugs that require activation in acid environment

**PK: **take before or w/ meal; metabolized in liver by P450 enzymes

Use:

  • short term treatment of gastric and duodenal ulcers (esp NSAID induced)
  • GERD
  • tx of choice for ZE syndrome, MEN, systemic mastocytosis
  • combo therapy for H. pylori

AE: inhib P450 leads to dec. clearance warfarin, benzo’s, phenytoin; elevated Gastrin levels

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3
Q

octreotide

A

Somatostatin analog (inhibits gastric and pancreatic secretion)

Used in ZE syndrome and
Portal hypertensive bleeding

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4
Q

Antacids
MgOH2
AlOH2
CaCO3

A

MOA: Neutralize gastric acid

**Use: **

  • treatment dyspeptic Sx
  • may hasten ulcer healing

AE:

MgOH2: diarrhea
AlOH2: constipation
CaCO3: stimulate gastrin release and acid secretion “Acid rebound”
*don’t use in renal failure

OTC

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5
Q

Sucralfate

A

MOA: Adheres to ulcer craters and forms a protective barrier

Use: Duodenal ulcer

AE: No systemic toxicity; May bind concomitant meds

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6
Q

reasons for non-healing ulcers

A
  • -non-compliance
  • -H. pylori infection
  • -NSAID use
  • -tobacco use
  • -inadequate duration therapy
  • -Hypersecretory state (ZE syndrome)
  • -non-peptic ulcer related disease (malignancy)
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7
Q

Carbechol
Bethanechol

A

cholinergic receptor agonists

Muscarinic receptors which when activated lead increase in intracellular Ca

enhance GI motility

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8
Q

Metaclopromide

A

MOA: Dopamine receptor antagonist, 5-HT3 antagonist, 5-HT4 agonist

Use: Symptomatic relief to pts with gastric motor failure (diabetic gastroparesis), decreases hearburn in GERD, anti-emetic (cancer),

AE:

  • Somnolence, nervousness, dystonia
  • -parkinsonism/tardive dyskinesia
  • -galctorrhea and menstrual d/o (inc. prolactin)
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9
Q

Tegerserod maleate

A

5-HT4 partial agonist; increase GI motility

constipation predominant IBS in women

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10
Q

erythromycin

A

MOA: Motilin agonist (Motilin receptors found on smooth muscle cells, when stimulated induce and amplify MMC; potent contractile element of upper GI tract)

Use:

Diabetic gastroparesis
Intestinal pseudoobstruction

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11
Q

Treatment of irritable bowel syndrome

A

Constipation predominant: bulking agent
Diarrhea predominant: antispasmodics/anticholinergics
Constipation: prokinetics
Constipation predom in women: tegerserod maleate

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12
Q

treatment of gastroparesis

A

Metoclopramide
Erythromycin
Cisparide
Botulinum toxin (intrapyloric injection)

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13
Q

Treatment of pancreatic insufficienc

A

Treatment of pancreatic insufficiency: steatorrhea when lipase output <10% normal

1) pancreatin: alcoholic extract hog pancreas
2) pancrelipase: enriched hog pancreas prep

Dosing
–With meals
–Titrated to therapeutic effect
–Higher gastric pH enhances activity

Toxicity:

  • uric acid renal stones
  • lactose in pills poorly tolerated in lactose intolerant pts
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14
Q

Bile salt therapy

A

1) Chenodiol: oral therapy to dissolve gallstones but limited by diarrhea
2) Ursodiol: epimer of chenodiol w/ fewer toxicities; used to dissolve gallstones and in primary biliary cirrhosis

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15
Q

Metronidazole, ciprofloxacin treatment in Crohn’s diseae

A
  • Useful in mild to moderate Crohn’s disease
  • induce remission
  • Adjunct treatment
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16
Q

Sulfasalazine

A

MOA: Multiple sits in inflammation cascase; inhibition leukotrienes is most imp!

Use: -mild to moderate UC (maintaining remission)

AE: Due to sulfa component…
–Dose related malaise, nausea, abdominal pain
–Impaired folic acid absorption (supplements needed)
–Reversible decrease in sperm count
–Severe skin reactions, rarely (Stevens-Johnson syndrome)
–Bone marrow suppression

Sulfasalazine: 5-ASA linked with sulfapyridine which is digested in colon

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17
Q

Melsalamine

A

coated 5-ASA which slows release

Use: Mild to moderate UC
–Asacol (works distal colon)
–Pentasa (works jejunum thru colon)
–Enemas (local delivery distal colitis and rectal disease)

AE: lacks sulfa component and assoc. toxicities

18
Q

Glucocorticoids

A

Treatment of choice for severe IBD (Abdominal pain, fever, leukocytosis, rectal bleeding)
-used short-term to achieve remission

Budesonide (maintenance use in crohns disease)

19
Q

Azathioprine, 6-mercaptopurine

A

MOA–Suppress lymphocyte proliferation

Use: 2nd line therapy for severe or steroid resistant IBD
-useful for maintaining remission (slow onset action)

AE: Bone marrow suppression, pancreatitis, drug induced malignancy

*TPMT testing for slow metabolizers

20
Q

Cyclosporine

A

MOA: Calcineurin inhibitor, suppresses pro-inflammatory transcription factors

Use: –For severe UC not responding to steroids

AE–Use limited by toxicity
•Renal insufficiency
•Hypertension

21
Q

TNF-alpha inhib

A

Binds TNFa which is known to be increased in mucosa of crohn’s pts

-used for inducing and maintaining remission in Crohns disease

23
Q

Bulk forming agents
-pysillium
carboxymethylcellulose
-methylcellulose

A

MOA: hydrophilic colloids form gel in large intestine, distending and stimulating peristalsis

Use: Chronic constipation, chronic diarrhea, diarrhea w/ incontinence, diarrhea in IBS

Contraind: : GI obstruction or perforation, gastric retention, undiagnosed abd. Pain, vomiting, appendicitis, toxic colitis, ileus, megacolon; avoid in pts with swallowing difficulities, severely swollen colon, watch Na, K, aspartame

AE: Bloating, flatulence, abdominal cramps (diminish with time)

Other: Adsorb other oral meds, separate by 1 hr

24
Q
  • *Osmotic/Saline/Hyperosmotic**
  • magnesium citrate/hydroxide
  • polyethylene glycol/Electrolyte solutions
  • lactulose
  • sorbitol
A

MOA: Non-adsorbable/non-digestable salts or sugars hold water in intestine by osmotic force; distends intestine and stimulates peristalsis

Use: constipation (chronic), evacuation of colon prior to radiologic/endoscopic procedures, sugars—hepatic encephalopathy, prompt evacuation in 1-3hrs,

Contraind: GI obstruction or perforation, gastric retention, undiagnosed abd. Pain, vomiting, appendicitis, toxic colitis, ileus, megacolon, ulcerative colitis, diverticulitis, colostomy/ileostomy, Severe renal insufficiency, heart block, rectal bleeding

AE:

  • magnesium salts: hypermagnesia if renal insuff, cramping/pain
  • sodium salts: hyperphosphatemia, hypocalcemia if reanl insuff
  • PEG/ES: nausea, vomiting, cramps, bloating, abd. Fullness
  • sugars: gas, bloating, distension

Interactions:

  • Mg(OH): may dec. absorption of antibiotics and cause premature release of enteric coated meds
  • PEG/ES: oral meds given 1 hr before start may be not be absorbed

-watch hydration

25
* *Surfactants (stool softeners)** - anioninc surfactants - detergents: docusate, dioctyl sodium sulfosucinate
MOA: Anionic surfactants become emulsified w/ stool, softening it and making passage easier Use: Stool softener, Adjunct therapy for hemorrhoids ContraInd: GI obstruction or perforation, gastric retention, undiagnosed abd. Pain, vomiting, appendicitis, toxic colitis, ileus, megacolon, fecal impaction/intestinal obstruction, acute abdominal pain, don’t use with mineral oil Mild AE: abdominal cramping Interactions: May inc. mineral oil absorption and toxicity (don’t give together) Other: take with a full glass of water, no laxative action, do not use for \>1wk, does not work after constipation occurs
26
* *Lubricants** - mineral oil ## Footnote
MOA: Penetrates and lubricates feces for easier passage, prevents water reabsorption Use: Fecal impaction, post-MI/surgery/partum to avoid straining ContraInd: GI obstruction or perforation, gastric retention, undiagnosed abd. Pain, vomiting, appendicitis, toxic colitis, ileus, megacolon, diverticulitis, UC, colostomy, ileostomy AE: Risk aspiration in debilitated pts, incontinence/anal leakage, malabsorption fat soluble vitamins, chronic intestinal hypomotility Interactions: Docusate, may decrease fat soluble vitamin absorption Other: Some absorption when given orally, no absorption as enema
27
* *Irritant/Stimulant/Contact** - anthraquinones—cascara sagrada (bark) - senna/sennosides: Cassia plant leaves - aloe: lily family leaf - castor oil/ricinoleic acid - diphenylmethane: bisacodyl (ducolax)
MOA: Contact irritant effects on enterocytes, enteric neurons, and muscle,accumulation water and electrolytes and stimulate intestinal motility Use: Constipation, preparation for surgery, delivery, GI exam ContraInd: Rectal bleeding, N/V, acute abdomen or bowel obstruction, appendicitis, or gastroenteritis \*not for chronic use AE: Anthraquinones: cathartic colon, cramps, severe diarrhea, dependency, tachyphylaxis - castor oil: damage microvilli and inc. intestinal permeability, AVOID, cramping - diphenylmethane: mucosal damage, cramping, inflammation w/ suppositories Interacionts:-antacids/milk (GI upset) Other: Anthraquinones: digested by colonic bacteria to active form, onset 6-12hrs - Castor oil: hydrolyzed to ricinoleic acid, stim fluid secretion and speeds GI transit, quick onset - diphenylmethanes: require hydrolysis to active form, stimulates enteric nerves, contact effects
28
Methylnaltrexone
MOA: Peripheral opiod receptor antagonist,does not cross BBB Use: Opioid induced constipation ContraInd: mechanical GI obstruction AE: Diarrhea, abdominal pain, dizziness, could inc. pain Other: Subcutaneous injection, Pregnancy category B
29
30
Alvimopan
MOA: Competitive antagonist at peripheral mu opioid rectpor, slow dissociation (does not reverse analgesia of central opioid agonists) Use: Post-operative ileus, in hospital use only ContraIndications Therapeutic doses or opioids used more than 7 consecutive days AE: Dyspepsia, hypokalemia, urinary retention Interactions: Drugs that inhibit p-glycoprotein (amiodarone, diltiazem, cyclosporine, itraconazole, quinidine, spironolactone, verpamil) Other: - not P450 substrate - is a substrate for p-glycoprotein - pregnancy category B
31
Lubiprostone
MOA: Agonist at GI CLC-2 Cl- channels, inc. production of chloride rich intestinal fluids w/o affecting Na/K levels Use: Chronic idiopathic constipation in adults, IBS w/ constipation (F\>18), no restriction in length of use ContraInd: Chronic diarrhea, diarrhea predominant IBS, mechanical GI obstruction AE: Nausea, diarrhea, abdominal pain Other: Poor systemic absorption
32
linaclotide
MOA: Guanylate cyclase C agonist→inc. cGMP Use: Chronic idiopathic constiation in adults, IBS w/ constipation ContraInd: Mechanical GI obstruction, not for use in pediatric pts (\<17yo) AE: Severe diarrhea, abd pain, flatulence, abd distension Other: * Not metabolized by P450 or p-glycoprotein * minimal systemic exposure * pregnancy category C
33
* *Narcotic analog** - phenylpiperidine - loperamide (Imodium) - diphenoxylate - atropine - diphenoxin - paregoric
MOA: Stimulate opiate receptors in myenteric plexus→ delayed intestinal transit and reduced secretion Use: Acute, nonspecific diarrhea; loperamide for chronic diarrhea ContraInd: * -“septic” pts * -toxic megacolon * -ulcerative colitis * -pseudomembranous colitis * -diarrhea d/t organisms that penetrate wall (toxigenic E. coli, salmonella, shigella) AE: Constipation, distension, bloating, nausea, vomiting, CNS depression, drowsiness, dizziness, fatigue, toxic megacolon Interactions: **Diphenoxylate/Atropine: ** * inc CNS depression w/ alcohol, barbituates, CNS depressants * w/ MOAI hypertensive crisis -avoid atropine in pediatric pts and pts w/ hepatic impairment
34
Bismuth subsalicylate (pepto bismol)
MOA: Bind bacterial toxins, absorb fluid in gut, anti-secretory effects in infectious diarrhea, anti-inflammatory Use: diarhhea, traveler’s diarrhea ContraInd: Hypersensitivity to salicylates, children \<16 w/ viral infection, chronic use in pts w/ renal failure, AE: Temporary black tongue stools, high doses w/ enteritis→bismuth or salicylate toxicity Interactions: Bind other drugs, take oral meds 1 hr before or 4hrs after
35
Octreotide
MOA: Somatostain analog, hyperpolarizes gut neurons, dec. Ach release and slows peristalsis; prevents release of secretion inducing NT (VIP, serotonin) Use: \*severe refractory diarrhea (Eg. AIDS, endocrine tumor related—carcinoid, VIPoma) ContraInd: Hypersensitivity to drugs or components AE: Gallbladder stasis, inhibition of pancreatic secretions, injection site irritation, nausea, diarrhea, abd. pain Interactions: Dec. plasma levels of cyclosporine
36
* *Anticholinergics** - atropine - belladonna alkaloids
Cholinergic receptors, dec intestinal muscle tone and peristalsis, slowed movement fecal matter thru GI tract
37
Sucralfate (carafate)
MOA: Topical mucosal protective agents, Forms ulcer-adherent complex at ulcer site and acts as protective barrier, stimulate mucosal PG and bicarb secretion, bind EGFR and FRGR Use: Treatment of duodenal and gastric ulcers Aluminum may accumulate w/ dec. renal function Interactions: \*requires acidic pH for activation so don’t co-administer w/ antacids, H2 receptor antagonists, PPI, can inhibit absorption of other meds
38
39
Misoprostol
MOA: Systemic mucosal protective agents, Misoprostol Inhibits gastric acid secretion and stimulates secretion of mucin and bicarb and improving mucosal blood flow Use: Prevention of NSAID induced gastric ulcers or mucosal injury ContraInd: Pregnancy category X (miscarriage due to uterine contraction stimulation), hx of allergy to prostaglandins, IBS AE: Dose dependent diarrhea, cramping, nausea, headache (resolve in 1-2wks) Interactions: Reduced availability when taken w/ antacids, does not affect P450 No dose adjustment for elderly or impaired renal function
40
Anatacids
MOA: Anatacids Neutralize gastric acid Use: Relief GI Sx ContraInd: Caution in pts w/ renal failure AE: Constipation, diarrhea Interactions: LOTS! Dec. absorption * Imp: theophyline, fluoroquinolone, antibiotics, tetracycline, isoniazid, ketoconazole, iron

Endo (7 decks)

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