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Pharm III > Exam 2 GI drugs > Flashcards

Exam 2 GI drugs Flashcards

1
Q

Misoprostol (Cytotec): Class, use, SE

A

PGE1 analogue
Prevents/reduces NSAID induced damage
Nausea, diarrhea, HA dizzy
- do not use in preg (induce abortion)

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2
Q

MOA, PK, use of PPI “prazole”

A

Pro drugs activated in parietal cell to sulfenamide
1x/d dosing on empty stomach, eat 30 min later
irreversible block of acid formation (takes 2-5 d)
long lasting effect (1-2 d to replace pump)

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3
Q

SE of PPI “prazoles”

A

Nausea, diarrhea, colic
OP (decrease Ca abs), Decrease Mg abs (cramps)
HA, dizzy, sleepiness, increased LFT uncommon
Skin rash, bacterial overgrowth possible
Omeprazole may inhibit CYP2C19 (phenytoin, warfarin, diazepam, clopidogrel)

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4
Q

PPI: Use

A 
Ulcers unresponsive to H2 blockers
4 wk to heal duodenal ulcer, 8 wk gastric
DOC GERD
Pt on NSAIDS
ZES
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5
Q

Sodium Bicarb: Class, use

A

Acid Neutralizing agent (GI)
Inorganic base neutralizes acid by binding to HCl
Temporary fix for heartburn, gastritis; adjunct to other drugs bc rapid acting

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6
Q

Calcium Carbonate (tums): Class, use

A

Acid Neutralizing (GI)
Inorganic base neutralizes acid by binding to HCl
Temporary fix for heartburn, gastritis; adjunct to other drugs bc rapid acting

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7
Q

MgOH/AlOH (Maalox, Gaviscon): Class, use

A

Acid Neutralizing (GI)
Inorganic base neutralizes acid by binding to HCl
Temporary fix for hearburn, gastritis; adjunct to other drugs bc rapid acting

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8
Q

PK H2 blockers “tidines”

A

Oral, half life 12 hr
Liver metab, kidney excretion
Most effective at night

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9
Q

SE of H2 blockers “tidines”

A

Few (worse in elderly)
HA, dizziness, nausea, rash itch
Cimetidine: anti testosterone (gynecomastia, loss libido, impotence); also inhibits metab of drugs meta by CYP3A4 (warfarin, phenytoin, theophylline, digoxin

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10
Q

What drugs are metab by CYP3A4

A

Warfarin, phenytoin, theophylline, digoxin

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11
Q

“tidines”: Class, use

A

H2 blockers
Decrease GI acid formation through H2 receptor blockade (now OTC)
Used to treat/prevent ulcers (stress/NSAID induced), pre anesthesia, GERD adjunts, with H1 antagonists for severe allergic rxn

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12
Q

What is Sucralfate (Carafate)

A

Cytoprotective Agent,
Take on empty stomach
Polymerizes to provide protective barrier cells in ulcer base; rarely used
Has aluminum – constipation; upset stomach and drug interactions

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13
Q

Tx of H pylori and Ulcers

A

Block acid and kill bactera: Pepto Bismol, Metro, Clarithromycin, tetracycline, amoxicillin, H2 blocker

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14
Q

What are the prokinetic agents

A

Metoclopramide (D2 antagonist that increases ACh release, antiemetic – SE cramping, diarrhea, tardive dyskinesia, infant methemoglobinemia, don’t use if pregnant)
Bethanechol (M agonist – diarrhea, cramps)
Erythromycin (used in diabetic gastroparesis)

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15
Q

Sx and tx of IBS

A

Abd pain, bloating, gas, constipation/diarrhea
Visceral hyperalgesia
Tx: diet, drugs, reduced stress
Glycopyrrolate, dicyclomine, TCAs (M antagonists, antispasmodic, TCA for chronic pain)

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16
Q

Drugs for treating IBS

A

Glycopyrrolate, dicyclomine (both antispasmodics aka antiM drugs), TCAs (good for chronic pain)

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17
Q

Pathophysiology of IBS

A

Stimulation of 5-HT4 receptors on nerve terminal increases ACh release, increases peristalsis
Release of 5-HT from Enterochromaffin cells stimulates 5HT3 receptors
Sends pain signal to CNS

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18
Q

Alosetron (Lotronex) class, MOA and use

A

Serotonin 5HT3 receptor antagonist
IBS with severe diarrhea in women
Constipation most common SE
SE can be severe – GI obstruction, perforation
Many contraindications, risk benefit statement req

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19
Q

Tegaserod (zelnorm) class, MOA, details

A

5-HT4 partial agonist, off market bc cardiac risk

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20
Q

Targets for vestibular system

A

H1 and M1 receptor

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21
Q

Targets for CTZ

A

Chemoreceptors, D2 receptor, NK receptor, 5 HT3 receptor

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22
Q

Targets for GI tract and heart

A

Mechanoreceptors, chemoreceptors, 5 HT3 receptors

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23
Q

“setrons” class MOA, use

A

Serotonin 5HT3 antagonists
Tx N/V induced by chemo, radiation, gastric dz
NOT for motion sickness
SE: HA, constipation, dizziness

24
Q

Prochlorperazine (Compazine), Promethazine (Phenergan): Class, MOA, Use, SE

A

Antinausea/antiemetics
Block DA, M and Histamine recpetors
Use: post op, gastroeneteritis, chemo, motion sickness (DOC motion sickness is dimenhydrinate and scopolamine)
SE: sedation

25
Q

Dranbinol (Marinol) /Medical marijuana/Nabilone: Class, MOA, use, SE

A

THC cannabinoid used for chemo induced N/V

Stimulates appetite

26
Q

DOC motion sickness

A

Scopolamine, dimenhydrinate (Dramamine)

27
Q

What influences bowel function: peristalsis/motility

A

Increased by PNS, decreased somewhat by SNS

Decreased by opioids (CNS and PNS effects)

28
Q

Describe function of the bowel

A

8-9 L H2O/d enters, most reabs - only 100 mL in feces
Abs of water, electrolyes
Secretion water &electrolyes
Abs of CHO, PRO, minerals and nutrients (via transporters)

29
Q

Define normal bowel freq vs constipation

A

Normal is >3x/wk
25% people think they are constipated (due to decreased freq, difficulty initiating, feces too firm, incomplete emptying) but 1/3 who use laxatives are not actually constipated
Chronic use of laxatives causes problems

30
Q

How do Laxatives work

A

Increase GI motility, prevent reab of water/electrolyte
Enhance secretion of water/electrolytes
Dissolve or lubricate feces

31
Q

What are the types of laxatives and their intensity

A 
Bulk forming: mild
Osmotic: INTENSE, cathartic
Mucosal agents: irritant
Lubricating
Stool softeners
32
Q

What are the bulk forming laxatives and SE/recommendations

A 
Fiber: dietary, methylcellulose (Citrucel), Psyllium (Metamucil), Polycarbophil
*High fiber diet best
SE: bloating, flatulence common
Rec: plenty of water
*Some may later abs of drugs
33
Q

What are the Osmotic Laxatives

A

MgOH (milk of magnesia) (also stimulates GI tract, increases peristalsis)
Sodium salts: oral or enema (fleet)
Sorbitol, mannitol, sucralose (also used as sweeteners)
Lactulose (chronolac): used in cirrhossis and liver dz to decrease NH4, causes gas
Polyethelene glycol (Colyte, miralax): prep colonoscopy, miralax OTC for constipation
Drink lots of water!!!!

34
Q

How do mucosal agents work? Class?

A 
Laxatives
Stimulate peristalsis
Enhance secretion/inhibit absorption H2O
Mild: Bisacodyl, Senna (Senokot)
Intense: Castor oil (requires bile, stimulates uterus so do not use if preg; used for surery, dx)
35
Q

Bisacodyl, Senna (senokot) class, MOA

A

Mild mucosal agent/laxative

Stimulate peristalsis, enhance secretion/inhibit abs H2O

36
Q

Bisacodyl: class, MOA, use

A 
Mucosal agent (laxative)
Stimulates peristalsis, enhances secretion, inhibits absorption of H2O
37
Q

Castor oil: class, MOA, use

A

Mucosal agent (intense)
Requires bile, stimulates uterus (CI in preg)
Used for surgery, diagnostic (colonoscopy)
Don’t use if pt has gallbladder or bile problem

38
Q

Lubricants/softeners: MOA, use, effectiveness

A

Increase bulk
Soften and lubricate stool
Not very effective
Mineral oil, Docusate (emulsifies), Glycerin (lubricate)

39
Q

Mineral Oil: class, MOA, use, SE

A

Lubricant/softener
Increases bulk, softens and lubricates stool
Can decrease abs of Fat soluble vitamins (A, D, E, K)
If inhaled into lungs, can cause lipoid pneumonia
Can cause leaking – stains clothing and furniture

40
Q

Docusate sodium (Colace, Doxinate): class, MOA, use, SE

A 
Most effective of the lubricant/softener class
Emulsifies, softens colonic contents and may increase water abs
41
Q

Glycerin: class, MOA, use

A

Lubricant/softener (laxative)

Suppositories that help lubricate distal end of bowel

42
Q

How effective are lubricants/softeners

A

Not very effective

43
Q

Lubiprostone (amitiza): MOA, use, SE

A

Laxative
PGE1 analogue, activates ClC2Cl channels in luminal cells to increase fluid secretion
Softer stool, better motility, less constipation
NO effect on electrolytes, no laxative dependence, not absorbed systemically
SE: N, D, HA

44
Q

Uses of Laxatives?

A

Reduce straining, maintain soft stools
Empty bowel for dx or surgical procedures
Decrease Bowel tone
Geriatrics, pregnancy
Get rid of pathogens/toxins
Constipation (cause may include opioids) – manage with diet, water consumption, exercise

45
Q

Contraindications for laxative use

A

N/V, cramps
Undx abdominal pain
Appendicitis
Obstruction

46
Q

Overuse of laxatives…

A 
Occasional = ok
Chronic = adverse effects incl dependence, electrolyte/fluid imbalance, spastic colitis, Ulcerative colitis (UC)
47
Q

Pathophysiology and risks of Diarrhea. Causes?

A

Fluid > capacity to absorb
Frequent, loose watery stools
Dehydration/electrolye imbalance
Causes: Pathogens, IBS, inflammation, Malabs, laxatives, thyroid dz, drugs

48
Q

How do antidiarrheal drugs work

A

Absorb excess water (fiber, Aluminum salts)
Inhibit secretion
Decrease motility (opioids, anticholinergics)
*note: fiber good for both constipation and diarrhea
*note: opioids very effective

49
Q

Adsorbents: MOA, use, effectiveness

A

Absorb water, form gel like mass
Bulk forming agents (man are also laxatives)
May benefit watery diarrhea by increasing bulk
Dietary approach: bananas, applesauce, rice
NOT very effective

50
Q

Loperamide (Imodium): class, MOA

A

Anti diarrheal opioid
Does not enter CNS, low abuse potential
May cause abdominal pain, constipation

51
Q

Diphenoxylate/atropine (Lomotil): class, MOA, SE

A

Antidiarrheal
Opioid with atropine reduces abuse potential, increases effectiveness (OD = sx atropine poisoning)
Anticholinergic SE: red as a beet, blind as a bad, dry as a bone, mad as a hatter

52
Q

When should you not use opioids to treat Diarrhea

A

Infections (will decrease expulsion of pathogens)
UC (toxic megacolon risk)
Recovering drug addicts (some abuse potential – diphenoxylate)

53
Q

Bismuth subsalicylate (pepto bismol): class, MOA, use, SE

A 
Anti-diarrheal for “Travellers diarrhea”
Absorbs water and pathogens
Salicylate = anti inflam
SE: black tongue, mouth and stool
CI: ASA allergy, kids (Reyes), asthmatics (asa asthma)
54
Q

Simethicone (Gas-X): class, MOA, use

A

Antiflatulent that coats and dissipates gas to make it pass less noticeably; decreases bloating

55
Q

Sulfasalazine (azulfidine): MOA, use, SE

A

Anti inflam 5 aminosalicylic acid + sulfapyridine
Activated by bacteria in GI tract
Tx: IBD (UC and crohns)
SE: allergic rxn possible (salicylate)
Avoid in children bc risk of Reyes syndrome

Pharm III (9 decks)

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