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Gastrointestinal Drugs Flashcards

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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

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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)

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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)

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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)

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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)

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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)

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A

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

24
Q

Diphenoxylate (Lomotil)

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A

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

25
Bismuth subsalicylate (Pepto-Bismol)
Antidiarrheal agents Mechanism of action: inhibit PG synthesis (intestinal), absorb toxins Clinical use: non-specific diarrhea, travelers diarrhea Adverse effects: salicylate toxicity
26
Cholestyramine (Prevalite)
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
Octreotide (Sandostatin)
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
Ondansetron (Zofran)
``` Antiemetic agents (direct regulator) Mechanism: 5-HT3 antagonist Clinical use: chemotherapy, postoperative, postradiation Adverse effects: headache, dizziness, constipation, prolonged QT interval ```
29
Scopolamine (Transderm Scop)
Antiemetic agents (direct regulator) Mechanism: M1 antagonist Clinical use: motion sickness Adverse effects: antimuscarinic effects
30
Metoclopramide (Octamide)
Antiemetic agents (direct regulator) Mechanism: D2 antagonist Clinical use: chemo & radiation therapy induced nausea and vomiting Adverse effects: extrapyramidal (Parkinsonian symptoms)
31
Dimenhydrinate (Dramamine)
Antiemetic agents (direct regulator) Mechanism: H1 antagonist Clinical use: motion sickness Adverse effects: drowsiness
32
Aprepitant (Emend)
``` Antiemetic agents (direct regulator) Mechanism: NK1 antagonist Clinical use: chemotherapy Adverse effects: fatigue, dizziness, diarrhea, CYP3A4 interactions ```
33
Prochlorperazine (Compro)
Antiemetic agents (direct regulator) Mechanism: M1 D2 H1 antagonist Clinical use: severe nausea/vomiting Adverse effects: extrapyramidal, drowsiness, anticholinergic
34
Lorazepam (Ativan)
Antiemetic agents (indirect regulator) Mechanism: GABA agonist Clinical use: anxiety/chemotherapy Adverse effects: drowsiness
35
Nabilone (Cesamet)
Antiemetic agents (indirect regulator) Mechanism: Cannabinoid agonist Clinical use: chemotherapy Adverse effects: dysphoria, sedation, increased appetite
36
Dexamethasone
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
Alosetron (Lotrenex)
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
Azathioprine (Azoson) | 6-mercaptopurine
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
Infliximab (Remicade)
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
Mesalamine (Pentosa)
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
Methotrexate (Rheumatrex)
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
Prednisone (Predone) Prednisolone Hydrocortisone Budesonide
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
Sulfasalazine (Azulfidine) Balsalazide Olsalazine
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
Tegaserod
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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