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Pharmacology > GI Drugs > Flashcards

GI Drugs Flashcards

1
Q

Aluminum Hydroxde

A

Antacid
MOA: neutralization of low gastric pH protects esophageal mucosa from reflux corrosion
SE: constipation

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2
Q

Magnesium Hydroxide

A

Antacid
MOA: neutralization of low gastric pH protects esophageal mucosa from reflux corrosion
SE: osmotic diarrhea (can become life threatening if someone abuses the drug)

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3
Q

Calcium Carbonate

A

Antacid
MOA: neutralization of low gastric pH protects esophageal mucosa from reflux corrosion
SE: CO2 causes belching and can lead to metabolic alkalosis (milk alkali syndrome)

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4
Q

Antacid Drug Interactions

A

Decreased absorption of coadministgered tetracyclines, fluoroquinolones, itraconazole and iron

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5
Q

H2 Receptor Antagonist (names)

A

Prototype: Cimetidine

2nd generation: Ranitidine, Famotidine, Nizatidine (no anti-adrogenic or CNS adverse effects)

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6
Q

H2 Antagonists

A

MOA: selective competitive inhibition at the parietal H2 Gs receptor
Effect: suppress basal gastric acid secretion w/ modest effect on meal stimulated secretion
Use: GERD, PUD, nonulcer dyspepsia, prophylaxis against stress-related gastritis

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7
Q

Cimetidine SEs

A

Sx’s: gynecomastia, galactorrhea, male impotence (acts as nonsteroidal anti-androgen and prolactin stimulant); confusion, dizziness and HAs; B12 deficiency and myelosuppression in long term use
Interactions: CYP450 inhibition causing increased serum concentration of Warfarin, Diazepam and Phenytoin

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8
Q

Proton Pump inhibitors

A

MOA: irreversibly bind and inhibit H-K ATPase in gastric parietal cells
Effect: suppress basal and meal stimulated gastric acid production
Use: pts that fail 2x daily H2RA therapy, severe GERD, PUD (H. pylori, NSAID ulcers), gastrinoma, nonulcer dyspepsia,
SEs: diarrhea, abd pn, HA

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9
Q

Proton Pump Inhibitors (names)

A

“-prazole” drugs

Omeprazole / Esomeprazole / Lansoprazole / Rabeprazole / Pantoprazole

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10
Q

Omeprazole SEs

A

CYP450 inhibition, will inhibit metabolism of Warfarin, Diazepam and Phenytoin

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11
Q

CYP2C19 inhibitors

A

Omeprazole / Esomeprazole / lansoprazole

*Clopidogrel requires CYP2C19 to convert it to active form so these drugs are CI in a pt taking Clopidogrel

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12
Q

H. pylori Eradication

A

Triple therapy (10-14d): Clarithromycin + Amoxicillin + PPI orrrr Clarithromycin + Metronidazole + PPI

Quadruple therapy (14d):
Bismuth Subsalicylate + Metronidazole + Tetracycline + PPI
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13
Q

Misoprostol

A

PGE1 analog
MOA: binds EP3 receptor stimulating Gi pathway
Effect: decreased gastric acid secretion, stimulates mucus and bicarbonate secretion, enhances mucosal blood flow
Use: prevention of NSAID-induced ulcers; diarrhea, abd pn
*CI in pregnancy

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14
Q

Sucralfate

A

Salt of sucrose + sulfate aluminum hydroxide
MOA: forms viscous paste that binds selectively to ulcers forming a physical barrier
Effect: stimulates mucosal prostaglandin and HCO3- secretion
Use: initial management of GERD in pregnancy

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15
Q

Bismuth Subsalicylate

A

Use: suppresses H. pylori
SE: dark stools, salicylate toxicity in combo w/ other salicylate products
CI: pts w/ ESRD

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16
Q

Prokinetic Agents

A

M1 agonists
Effect: enhance contractions in relatively uncooradinated fashion that produces little or no net propulsive activity
(Bethanechol / Neostigmine - not currently indicated for tx GI motility disorders)

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17
Q

Erythromycin

A

Motility receptor agonist
Effect: downregulation of motility receptors leading to early tolerance so its use is limited to short courses
Use: DM gastroparesis

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18
Q

Cisapride

A

MOA: 5-HT4 agonist, 5-HT3 antagonist, direct smooth muscle stimulant
Use: was used for GERD and gastroparesis (no longer used in US bc it has potential to cause ventricular arrhythmias)

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19
Q

Metoclopramide

A

MOA: 5-HT4 agonist, vagal and central 5-HT3 antagonist, DA antagonist
Effect: increases LES tone, stimulates natural and small intestinal contractions
Use: gastroparesis, anti-emetic, previously used for GERD sx relief
SE: extrapyramidal effects d/t DA antagonism (more common in young ppl @ high doses), galactorrhea by blocking inhibitory effect of DA on prolactin release

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20
Q

Scopolamine

A

Antimuscarinic

Use: prevention and tx of motion sickness, post-op N/V

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21
Q

H1 Antagonists

A

Diphenhydramine / Meclizine / Cyclizine
MOA: act on vestibular afferents as well as brainstem
Use: motion sickness and post-op emesis

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22
Q

5-HT3 Antagonists

A

Ondansetron / Granisetron
MOA: antagonize receptors in vagal afferents, STN, CTZ and AP
Use: DOC for prophylaxis against chemo induced N/V, hyperemesis gravidarum, post-op N
SE: constipation, diarrhea, HA< lightheadedness

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23
Q

Arepitant

A

NK1 antagonist
MOA: antagonist of NK1 receptors for substance P
Use: prophylaxis against delayed cancer induced N/V
Administration: PO incombo w/ dexamethasone and 5-HT3 receptor antagonist
Metabolism: CYP3A4 metabolism and may affect metabolism of Warfarin and oral contraceptives

24
Q

Promethazine / Droperidol

A

D2 antagonists
MOA: D2 antagonism at CTZ
Use: motion sickness
SE: extrapyramidal effects

25
Q

Dexamethasone / Methylprednisone

A

Corticosteroids
Effect: suppression of peritumoral inflammatoin and prostaglandin production
Use: adjuvants in tx of nause in
pt’s w/ metastatic ca

26
Q

Dronabinol

A

Cannabinoid
MOA: stimulates CB1 subtype of cannabinoid receptors on neurons in/around vomiting center in brainstem
Use: prophylactic in pt’s receiving chemo when other meds arent effective
SEs: palpitations, tachycardia, vasodilation, hypotension, conjunctival injection, paranoid rxns

27
Q

Lorazepam / Alprazolam / Diazepam

A

Effect: facilitate GABAa action in CNS by increasing frequency of Cl- channel opening
Use: adjuncts d/t sedative, amnesiac, anti-anxiety effects
SE: CNS depression and dependence

28
Q

Methylcellulose / Psyllium / Bran

A

Bulk-forming laxatives
MOA: nondigestible colloids absorb water to form bulky soft jelly that distended the colon to promote peristalsis
CI: immobile pt’s and those in long-term opioids therapy

29
Q

Castor Oil

A

MOA: directly stimulate enteric nervous system to increase motility
Metabolism: broken down to ricinoleic acid in small intestine
CI: pregnancy (bc it may cause uterine contractions)

30
Q

Senna

A

Stimulant laxative

SE: chronic use may lead to melanosis coli (brown pigment of colonic mucosa)

31
Q

Docusate / Glycerine

A

Stool softener

MOA: surfactants which allow water to penetrate and soften formed stool in the bowel

32
Q

Mineral Oil

A

Lubricant laxative

CI: not given with Ducosate as mineral oil will be absorbed into stool thereby negating its laxative effect

33
Q

Osmotic Laxatives

A

Lactulose / Magnesium Hydroxide / Magnesium Sulfate

MOA: nonabsorbable sugars or slots exert osmotic pull to retain water

34
Q

Lactulose

A

Metabolized by colonic bacteria and can lead to severe flats w/ cramping

35
Q

Magnesium Salts

A

Shouldn’t be used fro prolonged periods in persons w/ renal insufficiency bc they may cause hypermagnesemia

36
Q

Polyethylene Glycol (PEG)

A

Osmotic laxative
MOA: water soluble polymer that generates high osmotic pressure in gut lumen
Use: complete bowel prep before GI endoscopy, preferred for management of chronic constipation

37
Q

Lubiprostone

A

MOA: stimulates type 2 Cl- channels of small intestine
Effect: increases secretion of Cl- resulting in 👆🏽intestinal mobility
Use: chronic constipation and IBS w/ predominant constipation
SE: diarrhea
CI: children

38
Q

Alvimopan / Methylnaltrexone

A

Selective mu-opioid receptor antagonists
MOA: dont cross BBB so act at level of the gut to maintain normal motility in pt’s w/ acute or chronic use of opioid analgesics

39
Q

Loperamide

A 
Opioid agonist
MOA: activates present-tic mu-opioid receptors in entered nervous system to inhibit ACh release and decreases gut peristalsis
Use: IBS w/ diarrhea predominance
*low potential for addiction
CI: children and pt's w/ severe colitis
40
Q

Dioxyphenolate

A

Opioid agonist
MOA: activates present-tic mu-opioid receptors in entered nervous system to inhibit ACh release and decreases gut peristalsis
*can cross CNS at higher doses
CI: children and pt’s w/ severe colitis

41
Q

Octreotide

A

Somatostatin analog
Effect: decrease pancreatic exocrine fxn
Use: secretory diarrhea d/t neuroendocrine tumors, diarrhea 2° to vagotomy, dumping syndrome, short bowel syndrome, AIDS
SE: steatorrhea (can lead to fat-soluble vitamin deficiency), gallstones (d/t decreased gallbladder contractility)

42
Q

Bismuth Subsalicylate

A

MOA: coating and salicylate component
Effect: decreases fluid secretion in the enteric trace
Use: traveler’s diarrhea

43
Q

Aminosalicylates

A

Sulfasalazine / Balsalazide / Mesalamine
MOA: 5-aminosalicylates acid (5-ASA) at high concentrations at target sites given PO or suppository/enema depending on the site of dz
Use: long term maintenance of IBD remission

44
Q

Sulfasalazine

A

5-ASA linked to sulfapyridine by an ago bond
(Only partially absorbed in jejunum after PO administration)
SE: HA, arthralgia, myalgia, BM suppression, HS rxns

45
Q

Balsalazide

A

5-ASA linked to inert unabsorbed carrier molecule

*delivers max amts to colon

46
Q

Mesalamine

A

5-ASA packaged in microgranules taht release the active drug into desired portion of gut

47
Q

Glucocorticoids

A

Prednisone / Prednisolone / Budesonide
Effects: interaction w/ intracellular glucocorticoid response elements, inhibition of phospholipase A2 and COX, inhibition of NF-κB

48
Q

Prednisone / Predisonolone

A

Intermediate duration of action which allows for once daily dosing

49
Q

Hydrocortisone

A

Administered via enema for sigmoid and rectal iBD flares

50
Q

Budesonide

A

High rate of first pass metabolism when given PO which decreases the rate of systemic SEs compared to other systemic corticosteroids

51
Q

Mercaptopurine / Azathioprine

A

Immunosuppressive purines
MOA: steroid sparing effect
Use: IBD remission
SE (toxicity): N/V, hepatotoxicity and BM suppression
CI: administered w/ allopurinol bc it reduces xanthine oxide activity which can increase serum concentrations of these purines

52
Q

Methotrexate

A

MOA: inhibits dihydrofolate reductase to decrease thymidine and purine production
Effect: reduces IL-1 effects
SE: BM suppression, megaloblastic anemia, mucositis (folate supplementation is recommended)

53
Q

Anti-TNF-α Drugs

A

Infliximab / Adalimumab
MOA: bind and inactivate TNF
Effect: suppress pro-inflammatory response
Use: acute and chronic IBD

54
Q

Infliximab

A

Use: moderate-severe colitis that isn’t responsive to Mesalamine or steroids

55
Q

Natalizumab

A

Anti-integrin
MOA: monoclonal Ab targeting integrity on circulating inflammatory cells
Effect: disruption of leukocyte vascular wall adhesion and subsequent tissue migration
Use: moderate-severe unresponsive Crohn’s dz
SE: infusion rxns, opportunistic infections, reactivation of JC virus resulting in PML

56
Q

Pancrelipase

A

MOA: combination of amylase, lipase and proteases given PO with each meal
Use: exocrine pancreas insufficiency (CF, chronic pancreatitis)
SE: diarrhea, abd pn, hyperuricosuria, renal stones, colic strictures

57
Q

Alosetron

A

5-HT3 antagonist

Use: diarrhea IBS

Pharmacology (27 decks)

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