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Pharm > Gastrointestinal > Flashcards

Gastrointestinal Flashcards

1
Q

Antacids, AE, and drug interactions?

A
  • Aluminum Hydroxide - constipation
  • Magnesisum Hydroxide - osmotic diarrhea
  • Calcium Carbonate - CO2 causes bleching and can lead to metabolic alkalosis (milk alkali syndrome)

Drug Interactions:

  • binding/chelation of many drugs
  • incrased gastric pH alters dissolution of weakly charged drugs
  • Decreased absorption of co-adminisitered tetracyclines, fluoroquinolones, itraconazole, and iron
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2
Q

H2 Receptor Antagonist, AE, uses

A
  • Cimetidine - Gynecomastia, galactorrhea, male improtence, confusion, dizziness, HA, increased gastric pH > B12 deficiency, inhibitor of CYP 450
  • Ranitidine
  • Famotidine
  • Nizatidine

Uses: GERD, PUD, nonucler dyspepsia, prophylaxis against stress-related gastritis

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3
Q

PPI AE, uses

A
  • Omperazole - inhibit CYP450 and CYP2C19 (Clopidogrel)
  • Esomeprazole - inhibit CYP2C19
  • Lansoprazole - inhibit CYP2C19
  • Rabeprazole
  • Pantoprazole

AE: diarrhea, abdominal pain, HA in less than 5%; vitamin B12 deficiency, increase risk of community PNA and C. difficile colitis, hypomagnesemia, osteopenia,

Uses: pts who fail BID H2RA therapy, severe GERD, PUD, gastrinoma, nonulcer dyspepsia, prophylaxis against stress-related gastritis

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4
Q

H. pylori eradication

A

Triple therapy for 10-14 days:

  • Clarithromycin + Amoxicillin + PPI
  • Clarithromycin + Metronidazole + PPI

Quadruple therapy for 14 days

  • Bismuth subsalicylate + Metronidazole + Tetracycline + PPI
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5
Q

What are the Mucosal Protective Agents?

A
  1. Misoprostol
  2. Sucralfate
  3. Bismuth Subsalicylate
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6
Q

Misoprostol MOA, uses, AE, and contraindications?

A

MOA: analog of PGE1 > binds EP3 receptors > Gi pathway > decrease gastric acid secretion, stimulate mucus/bicarbonate secretion, enchance mucosal blood flow

Uses: prevention of NSAID-induced ulcers in high risk pts

AE: diarrhea, abdominal pain/cramps in 30% of pts

CI: pregnancy due to abortifacient effects

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7
Q

Sucralfate MOA, uses

A

MOA: salt of sucrose + sulfated aluminum hydroxide > paste that binds selectivly to ulcers > barrier preventing further damage and stimulates mucosal prostaglandin and bicarbonate secretion

Uses: management of GERD in pregnancy

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8
Q

Bismuth Subsalicylate MOA uses, AE, contraindications

A

MOA: suppresses H. pylori and has no neutralizing action on gastric acid

Uses: quadruple therapy of H. pylori, pepto-bismol for dyspepsia, acute diarrhea, traveler’s diarrhea (decrease fluid secretions in the enteric tract)

AE: metabolite of bismuth sulfide causes harmless blackening of stool, salicylate toxicity when combinded with other salicylate

CI: pts with renal failure

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9
Q

Name the Prokinetic Agents

A
  • Bethanechol - muscarinic agonist not preferred
  • Neostigmine - ACh esterase inhibitor not preferred
  • Erythromycin
  • Cisapride - no longer avialable in US
  • Metoclopramide
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10
Q

Erythromycin MOA, uses

A

MOA: agonist effects at motilin receptor but rapid down regulation of receptors leads to early tolerance

Uses: diabetic gastroparesis

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11
Q

Cisapride MOA, uses, AE

A

MOA: 5-HT4 receptor agonist, 5-HT3 antagonist, direct smooth muscle stimulant

Uses: GERD and gastroparesis

AE: occasionally fatal cardiac ventricular arrhythmias

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12
Q

Metoclopramide MOA, Uses, AE

A

MOA: 5-HT4 agonist, 5-HT3 antagonist (vagal and central), D2 antagonist > increase lower esophageal sphincter tone, stimulates antral and SI contraction

Uses: gastroparesis, anti-emetic, previously GERD until more effective therapies

AE: extrapyramidal effcts because of DA antagonism and galactorrhea by inhibitory effect of dopamine on prolactine realse

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13
Q

What are the types of antiemetics?

A
  • Antimuscarinics - Scopolamine
  • H1 Antagonists - Diphenhydramine, Meclizine, Cyclizine
  • 5-HT3 Antagonist - Onsansetron, Granisetron
  • NK1 Antagonist - Aprepitant
  • D2 Antagonist - Promethazine, Droperidol
  • Corticosteroids - Dexamethasone, Methylprenisolone
  • Benzodiazepines - Lorazepam, Alprazolam, Diazepam
  • Cannabinoids - Dronabinol
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14
Q

Scopolamine MOA, uses

A

MOA: antimuscarinic

Uses: prevention/Tx of motion sickness, postoperative N/V, second line for CINV

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15
Q

H1 Antagonists MOA, Uses

A
  • Diphenhydramine
  • Meclizine
  • Cyclizine

MOA: antagonist of H1 on vestibular afferents and brainstem

Uses: motion sickness, and postoperative emesis

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16
Q

5-HT3 Antagonists MOA, uses

A
  • Ondansetron
  • Granisetron

MOA: receptor antagonist on vagal afferents, STN, STX, and AP

Uses: DOC for prophylaxis imediate CINV, hyperemesis gravidarum

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17
Q

NK1 Antagonist MOA, uses, contraindication

A
  • Aprepitant (fosaprepitant for parenteral formulation)

MOA: antagonsit of NK1 receptors for substance P

Uses: prophylaxis against delayed CINV; given orally with dexamethasone and 5-HT3 antagonist

CI: CYP3A4 metabolism may affect metabolism of warafarin and oral contraceptives

18
Q

D2 Antagonist MOA, uses, AE

A
  • Promethazine
  • Droperidol

MOA: receptor antagonism at the CTZ

Uses: motion sickness

AE: extrapyramidal effects

19
Q

Corticosteroids MOA, uses

A
  • Dexamethasone
  • Methylprednisolone

MOA: supression of peritumoral inflammation and prostaglandin production

Uses: adjuvant in Tx of nausea with pts with metastatic CA

20
Q

Benzodiazepines MOA, Uses, AE

A
  • Lorazepam
  • Alprazolam
  • Diazepam

MOA: facilitate GABAA action in the CNS by increasing frequency of chloride channel opening

Uses: sedative, amnesic, anti-anxiety effects reduce anticipatory component of N/V

AE: CNS depression and dependence

21
Q

Cannabinoids

A
  • Dronabinol (delta-9-detrahydrocannabinol)

MOA: stimulates CB1 receptors in brainstem

Uses: prophylatic agents for chemotherapy pts when other anti-emetic medications are not effetive

AE: marijuana-like “highs”, central sympathomimetic activity (palpitations, tachycardia, vasodilation, hypotension, conjunctival injection), paranoid; withdrawal has irritability, insomnia, restlessness

22
Q

What are the types of Laxatives?

A
  • Bulk-forming laxatives - Methylcellulose, Psyllium, Bran
  • Cathartics (stimulant laxatives) - Castor oil, Bisocodyl, Senna
  • Stool Softeners - Docusate, Glycerin
  • Lubricant Laxatives - Mineral oil
  • Osmotic laxatives - Lactulose, Magnesium Salts, PEG
  • Lubiprostone
  • Selective Mu-Opiod Receptor antagonist - Alvimopan, Methylnaltrexone
23
Q

Bulk forming laxatives MOA and contraindications?

A
  • Methylcellulose
  • Psyllium
  • Bran

MOA: nondigestible colloids which absorb water to form bulky soft jelly that distends colon to promote peristalsis

CI: immobile pts and pts on long term opiod therapy because of risk of intestinal obstruction

24
Q

Cathartics (stimulant laxatives) MOA, AE, contraindications?

A
  • Castor oil - CI in pregnanacy bc can cause uterine contractions
  • Bisacodyl - minimal systemic absorption
  • Senna - chornic use lead to melanosis coli (brown pigmentation of colonic mucosa)

MOA: direct stimulation of enteric nervous system > increase motility

25
Stool Softeners MOA
* **Docusate** * **Glycerin** MOA: surfactants which allow water to penetrate and thereby soften stool in bowel
26
Lubricant Laxatives MOA, contraindications
* **Mineral oil** MOA: coats fecal material preventing water reabsorption CI: should not be given with docusate as the mineral oil will be absorbed into stool negating its laxative effect
27
Osmotic Laxatives MOA, AE, CI
* **Lactulose** - metabolzied by colonic bacteria \> severe flatus and cramping * **Magnesium Salts** - CI in renal insufficiency \> hypermagnesemia * **Polyethylene Glycol (PEG)** - high osmostic pressure used for complete bowel preparation and preferred management of chornic constipation MOA: nonabsorbable sugars or salts which exert osmotic pull to retain water in intestinal lumen
28
Lubiprostone MOA, uses, AE, CI
MOA: stimulates type 2 chloride channels of small intestines \> increase secretion of chloride \> intestinal motility Uses: chornic constipation including IBS with predominant constipation AE: diarrhea CI: children
29
Selective Mu-opioid Receptors Antagonist MOA,
* **Alvimopan** * **Methylnaltrexone** MOA: antagonist of Mu-opioid receptor of the gut and do not cross BBB Uses: acute and chronic opioid use
30
What are the types of antidiarrheal drugs?
* Opioid Agonists * Somatostatin Analogs * Bismuth Compounds
31
Opioid Agonists AE, CI
* **Loperamide** - low potential for addiction because * **Dioxyphenolate** - higher dose has CNS effect and prolonged use \> opioid dependence CI: children and pts with severe colitis
32
Somatostatin Analogs
* **Octreotide** Uses: secretory diarrhea due to neuroendocrine tumors (carcinoid, VIPoma), diarrhea caused by vagotomy/dumping syndrome/short bowel syndrome/AIDS AE: decrease pancreatic exocrine function, steatorrhea \> deficiency of fat-soluble vitamins, inhibition of gallbladder contractility lead to biliary sludge \> gallstones
33
What is the first line strategy for IBS?
* No medication, pts keep food diary and try sequential: 1. Exclusion of gas-producing foods 2. Low fermentable oligo-, di-, and monosaccharides and polyols (FODMAPs) 3. Lactose and/or gluten omission
34
How is IBS treated with medication?
Constipation predominant IBS: * **Lubiprostone** Diarrrhea predominant IBS: * **Loperamide** (_opioid agonist_) * **Alosetron** (_5-HT3 antagonist_) \> reduce nocious visceral sensations of bloating, nausea, and pain * **Hyoscyamine, Dicyclomine, Glycopyrrolate, Methscopolamine** (_anticholinergic_) \> antispasmodic GIT
35
What are the types of drugs used to treat IBD?
* Aminosalicylates * Glucocorticoids * Immunosupressants * Anti-TNF-alpha * Anti-Integrins
36
Aminosalicylates (5-aminosalicylic acid) MOA, uses,
* **Sulfasalazine** - 5-ASA + sulfapyridine (reduces absorption in jejunum) by azo bond * **Balsalazide** - 5-ASA linked to an inert unabsorbed carrrier * **Mesalamine** - 5-ASA physically packaged for time release or pH sensitive _MOA:_ modulation fo cyclooxygenase and lipoxygenase pathways, inhibition of nuclear factor-KB (proinflammatory transcription factor), inhibiton of cellular immunity mechanisms, and scavenges reactive oxygen species \>\>\> gross reduction of inflammatory mediators _Uses:_ IDB _AE:_ nausea, GI upset, HA, arthralgia, myalgia, bone marrow supression, hypersensitivity reactions; up to 40% unable to tolerate sulfazine
37
Glucocorticoids MOA, uses
* **Prednisone** * **Prednisolone** * **Budesonide** - topical effects on luminal surface with repaid first pass metabolism so low systemic bioavailability compared to prednisone/prednisolone * **Hydrocortisone** - enema for signmoid and rectal IBD flares MOA: immunosupresive and anti-inflammatory by interaction with intracellular glucocorticoid response elements, inhibiton of phospholipase A2/cyclooxygenase, inhibition of nuclear factor-KB Uses: induce remission of acute exacerbation IBD
38
Immunosupressants Purine Metabolites MOA, uses, AE, CI
* **Mercaptopurine (6-MP)** * **Azathioprine** MOA: purine metabolites Uses: induction and maintenance of IBD remission AE: N/V, hepatotoxicity, and bone marrow depression CI: Allopurinol becuase it reduces xanthine oxidase activity which breaks down 6-MP
39
Methotrexate MOA, AE
MOA: inhibits dihydrofolate reductase \> decrease production of thymidine and purines and reduces inflammatory action of IL-1 AE; bone marrow depression, megablostic anemia, and mucositis
40
Anti-TNF-alpha MOA, uses
* **Infliximab** * **Adalimumab** _MOA:_ bind and inactivate TNF which releases proinflammatory cytokines, stimulation of hepatic acute phase reactants, upregulation of endothelial adhesion molecules promoting leukocyte migration _Uses:_ Tx acute and chronic IBD; infliximab for moderate/severe colitis that is nonresponsive to mesalamine/corticosteroids
41
Natalizumab MOA, uses, AE
_MOA:_ humanized monoclonal antibody targeting several integrins on circulating inflammatory cells _Uses:_ moderate/severe, unresponsive Crohn's disease _AE:_ infusion reactions, opportunistic infections, reactivation of human polyomavirus (JC virus) \> progressive multifocal leukoencephalopathy
42
Pancrelipase
_MOA:_ combination of amylase, lipase, and protease which can be enteric coated or noncoated _Uses:_ exocrine pancreatic insufficiency (enzymes \<10% normal) _AE:_ diarrhea, abdominal pain; rarely hyperuricosuria, renal stones, and colonic strictures

Pharm (14 decks)

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