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Pharmacology > Gastrointestinal Drugs > Flashcards

Gastrointestinal Drugs Flashcards

1
Q

Sodium bicarbonate (NaHCO3)

A

Antacid
Duration: 1-2 hrs
Rate of reactivity: fast
Common adverse effects: reduced drug bioavailability, enteric infection
Specific adverse effects: metabolic alkalosis, excessive NaCl absorption, gas/bloating
Clinical use: GERD, peptic ulcers, dyspepsia
Equally efficacious to H2-receptor antagonists
Adjunctive therapy

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2
Q

Calcium carbonate (CaCO3)

A

Antacid
Duration: 1-2 hrs
Rate of reactivity: moderate
Common adverse effects: reduced drug bioavailability, enteric infection
Specific adverse effects: acid rebound, gas/bloating, hypercalcemia (large doses), hypophosphatemia (rare)
Clinical use: GERD, peptic ulcers, dyspepsia
Equally efficacious to H2-receptor antagonists
Adjunctive therapy

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3
Q

Magnesium hydroxide (Mg(OH)2)

A

Antacid
Duration: 1-2 hrs
Rate of reactivity: slow
Common adverse effects: reduced drug bioavailability, enteric infection
Specific adverse effects: osmotic diarrhea, hypermagnesemia (large doses over extended periods of time)
Clinical use: GERD, peptic ulcers, dyspepsia
Equally efficacious to H2-receptor antagonists
Adjunctive therapy

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4
Q

Aluminium hydroxide (Al(OH)2)

A

Antacid
Duration: 1-2 hrs
Rate of reactivity: slow
Common adverse effects: reduced drug bioavailability, enteric infection
Specific adverse effects: constipation, aluminum toxicity (impaired renal function), hypophosphatemia, bone resorption, hypercalcemia
Clinical use: GERD, peptic ulcers, dyspepsia
Equally efficacious to H2-receptor antagonists
Adjunctive therapy

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5
Q

cimetidine (Tagemet)
ranitidine (Zantac)
nizatidine (Axid)
famotidine (Pepcid)

A

H2-receptor antagonist: competitive inhibition of histamine, partial block of muscarinic-induced HCl secretion
Duration: 10hrs or 6 hrs OTC
Common adverse effects: headache, diarrhea, fatigue, constipation, infection, drug kinetics, bradycardia (IV), hypotension (IV)
Cimetidine specific considerations: CNS effects( confusion, hallucinations, agitation), endocrine effects (inhibits androgen receptors and estradiol metabolism—>gynecomastia, increases prolactin levels), inhibits hepatic CYP metabolism
Clinical use: GERD, peptic ulcers, dyspepsia, gastritis
Equally efficacious to anacids

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6
Q 
Omeprazole (Prilosec)
Lansoprazole (Prevacid)
Rabeprazole (Aciphex)
Esomeprazole (Nexium)
Pantoprazole (Protonix)
A

Proton pump inhibitors (PPIs): low pH activated, irreversibly binds and inhibits proton bump
Duration of action: 24 hrs, takes 3-4 days of dosing to reach max effect
Common adverse effects: extremely safe, decreased drug bioavailability, diarrhea, headache, abdominal pain
Adverse effects: decreased nutritional absorption (Vitamin B12, iron, calcium, zinc), enteric & respiratory infection
Clinical use: GERD, peptic ulcers, dyspepsia, gastritis, hypersecretory diseases, NSAID-associated ulcers, H. pylori associated ulcers
Most efficacious inhibitors of acid secretion

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7
Q

Sucralfate (Carafate)

A

Mucosal protective agent
Mechanism: adheres to ulcer and creates physical barrier; stimulates mucus secretion (PGEs?)
Duration of action: 6 hrs
Common adverse effects: constipation, impaired drug absorption
Adverse effects: caution w/ renal insufficient patients
Clinical use: prevent stress-related bleeding when you do not want to prevent acid secretion (hospitalized patient–>infection)

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8
Q

Bismuth subsalicylate (Pepto-Bismol)

A

Mucosal protective agent
Mucosal protective agent
Mechanism: adheres to ulcer and creates physical barrier; stimulates mucus secretion (PGEs?)
Mucosal protective agent
Mechanism: adheres to ulcer and creates physical barrier; stimulates mucus secretion (PGEs?)
Duration of action: 6 hrs
Common adverse effects: constipation, impaired drug absorption
Adverse effects: caution w/ renal insufficient patients
Clinical use: H. pylori associated ulcers, travelers diarrhea, dyspepsia

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9
Q

Misoprostol (Cytotec)

A

Mucosal protective agent
Mechanism: PGE analogue stimulating mucus and bicarb secretion
Duration of action: 6 hrs
Common adverse effects: cramping, diarrhea
Adverse effects: abortificient (stimulates uterus contractions)
Clinical use: NSAID associated ulcers

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10
Q

H. pylori & gastric ulcer Tx

A

“new triple therapy”: PPI, clarithromycin, amoxicillin or metronidazole
“old triple therapy”: bismuth subsalicylate, tetracycline, metronidazole
“quadruple therapy”: bismuth subsalicylate, PPI, clarithromycin, amoxicillin or metronidazole

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11
Q

Metoclopramide (Reglan)

A

Prokinetic agent
Mechanism of action: D2 antagonist
Clinical use: GERD, impaired gastric emptying, dyspepsia, antiemetic
Adverse effects: CNS (restlessness, drowsiness, insomnia, anxiety); altered motor function (Parkinsonian symptoms)

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12
Q

Bethanechol (Urecholine

A

Prokinetic agent
Mechanism of action: M3 agonist
Clinical use: GERD, gastroparesis
Adverse effects: cholinergic side effects

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13
Q

Neostigmine (Prostigmin)

A

Prokinetic agent
Mechanism of action: AChE inhibitor
Clinical use: non-obstructive (urinary retention, abdominal distension)
Adverse effects: cholinergic side effects

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14
Q

Erythromycin (Erythrocin)

A

Prokinetic agent
Mechanism of action: Motilin receptor agonist
Clinical use: gastroparesis
Adverse effects: acute cholestatic hepatitis, jaundice

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15
Q

Methylcellulose (Citrucel)

A

Laxative: bulk-forming
Mechanism of action: fiber adds bulk and retains water
Absorption: poor
Clinical use: constipation, minimize straining, prior to surgical and endoscopic procedures
Adverse effect: gas/bloating

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16
Q

Glycerin (Colace)

A

Laxative: surfactant
Mechanism of action: coats and penetrates fecal material
Absorption: poor
Clinical use: constipation, minimize straining, prior to surgical and endoscopic procedures
Adverse effect: nutrient malabsorption

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17
Q

Lactulose (Enulose)

A

Laxative: osmotic
Mechanism of action: changes osmotic pressure
Absorption: poor
Clinical use: constipation, minimize straining, prior to surgical and endoscopic procedures
Adverse effect: gas, electrolyte flux

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18
Q

Senna (Ex-Lax

A 
Laxative: stimulant
Mechanism of action: stimulate ENS 
Absorption: poor
Clinical use: constipation, minimize straining, prior to surgical and endoscopic procedures
Adverse effect: GI irritation
19
Q

Tegaserod (Zelnorm)

A

Laxative: serotonin agonist
Mechanism of action: 5-HT4 partial agonist
Absorption: 10%
Clinical use: chronic idopathic constipation
Adverse effect: GI, CV, NOT available for general use

20
Q

Lubiprostone (Amitize)

A

Laxative: chloride channel activator
Mechanism of action: prostaglandin derivative
Absorption: poor
Clinical use: chronic constipation
Adverse effect: nausea/vomiting, diarrhea

21
Q

Methylnaltrexone (Relistor)

A

Laxative: Mu-opioid receptor
Mechanism of action: block peripheral mu-opioid receptors
Absorption: poor CNS penetration
Clinical use: opioid-induced constipation during palliative care
Adverse effect: abdominal pain, flatulence, nausea, diarrhea

22
Q

Alvimopan (Entereg)

A

Laxative: Mu-opioid receptor
Mechanism of action: block peripheral mu-opioid receptors
Absorption: poor CNS penetration
Clinical use: postoperative ileus in hospitalized pts w/ bowel resection
Adverse effect: abdominal pain, flatulence, nausea, diarrhea, MI (so use for only 7 days)

23
Q

Loperamide (Imodium)

A

Antidiarrheal agents
Mechanism of action: opioid agonist
Clinical use: diarrhea (IBS)
Adverse effects: constipation (very safe)

24
Q

Diphenoxylate (Lomotil)

A

Antidiarrheal agents
Mechanism of action: opioid agonist
Clinical use: diarrhea
Adverse effects: CNS effects, atropine effects

25
Q

Bismuth subsalicylate (Pepto-Bismol)

A

Antidiarrheal agents
Mechanism of action: inhibit PG synthesis (intestinal), absorb toxins
Clinical use: non-specific diarrhea, travelers diarrhea
Adverse effects: salicylate toxicity

26
Q

Cholestyramine (Prevalite)

A

Antidiarrheal agents
Mechanism of action: bind bile acids and salts
Clinical use: impaired bile-salt absorption mediated diarrhea
Adverse effects: bloating, flatus, constipation, fecal impaction, impaired fat absorption

27
Q

Octreotide (Sandostatin)

A

Antidiarrheal agents
Mechanism of action: Somatostatin receptor agonist
Clinical use: secretory diarrhea (severe cases)
Adverse effects: impaired pancreatic secretion, decreased GI motility (nausea, pain), decreased gall bladder contraction, glucose homeostasis

28
Q

Ondansetron (Zofran)

A 
Antiemetic agents (direct regulator)
Mechanism: 5-HT3 antagonist
Clinical use: chemotherapy, postoperative, postradiation
Adverse effects: headache, dizziness, constipation, prolonged QT interval
29
Q

Scopolamine (Transderm Scop)

A

Antiemetic agents (direct regulator)
Mechanism: M1 antagonist
Clinical use: motion sickness
Adverse effects: antimuscarinic effects

30
Q

Metoclopramide (Octamide)

A

Antiemetic agents (direct regulator)
Mechanism: D2 antagonist
Clinical use: chemo & radiation therapy induced nausea and vomiting
Adverse effects: extrapyramidal (Parkinsonian symptoms)

31
Q

Dimenhydrinate (Dramamine)

A

Antiemetic agents (direct regulator)
Mechanism: H1 antagonist
Clinical use: motion sickness
Adverse effects: drowsiness

32
Q

Aprepitant (Emend)

A 
Antiemetic agents (direct regulator)
Mechanism: NK1 antagonist
Clinical use: chemotherapy
Adverse effects: fatigue, dizziness, diarrhea, CYP3A4 interactions
33
Q

Prochlorperazine (Compro)

A

Antiemetic agents (direct regulator)
Mechanism: M1 D2 H1 antagonist
Clinical use: severe nausea/vomiting
Adverse effects: extrapyramidal, drowsiness, anticholinergic

34
Q

Lorazepam (Ativan)

A

Antiemetic agents (indirect regulator)
Mechanism: GABA agonist
Clinical use: anxiety/chemotherapy
Adverse effects: drowsiness

35
Q

Nabilone (Cesamet)

A

Antiemetic agents (indirect regulator)
Mechanism: Cannabinoid agonist
Clinical use: chemotherapy
Adverse effects: dysphoria, sedation, increased appetite

36
Q

Dexamethasone

A

Antiemetic agents (indirect regulator)
Mechanism: Glucocorticoid agonist
Clinical use: chemotherapy, postoperative (increase effectiveness of 5-HT antagonists)
Adverse effects: weight gain, water retention, other corticosteroid effects

37
Q

Alosetron (Lotrenex)

A

Tx for IBS
Mechanism of action:5HT3 antagonist–>block visceral pain, motility, and secretions
Clinical use: IBS diarrhea (women)
Adverse effect: constipation, ischemic colitis (fatal)
Last resort drug

38
Q

Azathioprine (Azoson)

6-mercaptopurine

A

Antimetabolite
Mechanism: inhibits purine synthesis resulting in decreased DNA synthesis and repair–> decreased cell proliferation (inhibit immune system)
Administration: IM, SC, oral
Clinical use: maintenance of remission of IBD (onset 17 wks)
Adverse effects: nausea, vomiting, bone marrow suppression

39
Q

Infliximab (Remicade)

A

Anti-TNFalpha therapy
Mechanism: TNF-alpha monoclonal antibody–>bind/sequester TNF-alpha–>inhibit immune response
Clinical use: moderate to severe IBD
Adverse effects: infection

40
Q

Mesalamine (Pentosa)

A

Aminosalicyclates: 5-aminosalicylic acid (5-ASA)
Mechanism: inhibit COX production of PGs, interfere with inflammatory cytokine production, inhibit NF-kappaB signaling
Administration: oral
Target: throughout intestine
Modification: time release microgranules, pH sensitive resin
Clinical use: 1st line agent for mild to moderate ulcerative colitis
Must reach lesion sight, does NOT work if absorbed systemically
Adverse effects: headache, dizziness, abdominal pain

41
Q

Methotrexate (Rheumatrex)

A

Antimetabolite
Mechanism: inhibits DHFR resulting in impaired cellular proliferation
Administration: IM, SC, oral
Clinical use: maintenance of remission of Crohn’s (onset 8-12 wks)
Adverse effects: low dose side effects uncommon, but include bone marrow depression and megaloblastic anemia

42
Q

Prednisone (Predone)
Prednisolone
Hydrocortisone
Budesonide

A

Glucocorticoids
Mechanism: suppression of inflammatory cytokines (TNF-alpha, IL-1); suppresion of chemokines (IL-8); suppression of adhesion molecules; suppression of signal transduction molecules that mediate cytokine and chemokine activities (NOS, PLA2, COX2, NF-kappaB)
Administration: IV, oral, suppository
Clinical use: moderate to severe active IBD
Adverse effect: glucocorticoid adverse effects

43
Q

Sulfasalazine (Azulfidine)
Balsalazide
Olsalazine

A

Aminosalicyclates: 5-aminosalicylic acid (5-ASA)
Mechanism: inhibit COX production of PGs, interfere with inflammatory cytokine production, inhibit NF-kappaB signaling
Administration: oral
Target: colon
Modification: Azo bond linked
Clinical use: 1st line agent for mild to moderate ulcerative colitis
Must reach lesion sight, does NOT work if absorbed systemically
Adverse effects: nausea, GI upset, headache, arthralgia, myalgia, bone marrow suppression, malaise (40% pts can’t tolerate)

44
Q

Tegaserod

A

Tx for IBS
Mechanism of action: 5HT4 partial agonist–> increase motility, decrease firing to CNS (block pain)
Clinical use: IBS constipation
Adverse effect: GI pain, dyspepsia, flatulence, nausea/vomiting, diarrhea, CV (MI & stroke)
NOT fro general use

Pharmacology (34 decks)

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