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Mandie's Pharm test I > GI Drugs > Flashcards

GI Drugs Flashcards

1
Q

omeprazole/esomeprazole/lansoprazole

A
  • proton pump inhibitors (H+K+ATPase)
  • 1st line rx
  • 80-95% reduction of H+ production
  • prodrugs that require acid activation to react with and irreversibly inhibit the proton pump
  • enter parietal cells from systemic circulation, activated within the acidic environment around the PP
  • all are acid labile and must be abs into blooat at higher pH
  • admin as gelatin capsules, EC, mixed with bicarb
  • can give lansoprazole IV
  • only active for about 2 hours
    rx: GERD, erosive esophagitis, peptic ulcers, Zollinger-Ellison syndrome, NSAID ulcers, H.Pylori
  • Cleared via liver
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2
Q

PPI adverse reactions

A

Main SE: Drug interactions through altered CYP activity

  • increase serum warfarin concentration
  • decrease activation of clopidigerl
  • hepatic failure reduces clearance, sep of esomeprazole/lansoprazole
  • Nausea, abd pain, constipation, flatulance, diarrhea
  • myopathy, arthralgias, h/a, skin rashes
  • rebound hypergastrinemia and gastritis can occur with sudden w/d
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3
Q

cimetidine, ranitidine, famotidine

A
  • H2 receptor antagonists (more inhibit basal acid level maintained by ECL cells)
  • used for nocturnal acid secretion, duodenal ulcers, Zollinger-Ellison syndrom
  • not as effective as PPI but still decrease acid seccretion 70%
  • renal excretion via OCT
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4
Q

H2 antagonists Se

A

diarrhea, h/a, drowsiness, fatigue, muscle pain
-CNS effects in parenteral admin and elderly: hallucinations, delirium, confusion, slurred speech, h/a
LT use of cimetidine: decreases testosterone binding to the adrogen receptor and hydroxylation of estradiol causing galactorrhea in women and dec sperm count in men
-decrease pepsin/IF output
-Tolerance in 3 days
-rebound

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5
Q

misoprostol MOA

A
  • synthetic analogue of PGE1, induces Bicarb prod in epithelial cells and blocks cAMP prod in parietal cells
  • reduces 80-90% of basal or food induced acid prod
  • short acting (3 hr)
  • generally only used to prevent NSAID induced injury (PPI and H2 more commonly used)
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6
Q

misoprostol SE

A
  • diarrhea (30%)
  • exacerbate IBD
  • increase uterine contractions
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7
Q

sucralfate

A

-octasulfate of sucrose with aluminum hydroxide
-forms a sticky neutral pH polymer coating that swells and covers the epithelium
-used for stress ulcers (sticks better to duodenum than gastric area)
-acid acivated, take before food and avoid antacids and PPI
SE: constipation (no use with obstructions); can block absorption of other drugs through stomach

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8
Q

aluminum hydroxide, magnesium hydroxide, calcium carbonate

A

-antacids
-neutralize pH of gastric contents
-fast acting (15 mins), w food can last (2-3 hours)
-largely supplanted by PPI, but common OTC drug
-Mag Hydrox is fast and stimulates gastric emptying; Aluminum is slower and delays emptying.
SE: rebound acid secretion
AL: constipation, nausea, may contribute to osteoporosis and encephalopathy with renal insufficiency
Ca: hypercalcemia (transient normally)
Mag: contraindicated in renal disease
all: may interfere with GI abs of other drugs

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9
Q

pirenzepine

A
  • muscarinic antagonist, selective for M1 receptors
  • blocks neurotransmission in the intramural ganglia, resulting in less vagal stimulation of parietal and ECL cells
  • reduces acid 40-50%
  • sig anticholinergic side effects, rarely used
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10
Q

H. Pyroli infection

A

1/3 of infections are pathogenic

  • Vacuolating endotoxin A, associated with PUD, gastritis, GERD
  • bacteria need acid, which activates the toxin as well. They bind to apical membranes and kill epithelial and immunce cells
  • rx with acid neutralization, cytoprotection, antibacterial agents
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11
Q

tegaserod

A

serotonin partial agonist in the gut used for females with IBS. can improve lower bowel motility in cases of chronic constipation and bloating. only mildly effective.
-SE include fatal cardiac arrythmias

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12
Q

cisapride

A

5HT4 receptor agonst and adenylate cyclase stimulate. Used for GERD and gastroparesis.
SE include fatal cardiac arrythmias

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13
Q

bethanechol

A

-cholinergic derivate used to selectively activate M2 & M3 receptors, stimulates constriction of SM for GI motility. SE: bradycardia, flushing, diarrhea, cramps, salivation, blurry vision

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14
Q

Neostigmine methylsulfate

A

AChE inhibitor can be used acutely to counter an ileus. Idea is to stimulate constriction of SM for GI motility

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15
Q

metoclopramide

A

a general dopamine receptor antagonist (enhances normal ACh response, dopa at d2 receptors decreases Ach release). increases lower esophageal sphincter tone and upper GI motility, can relieve GERD but does not promote healing. Now used for N/V in dysmotility syndromes and as an antiemetic (antagonizes 5HT3, strongly affects CTZ, increases motility/defecation). Also as a laxative.
SE: extrapyramidal SE, dystonias, Parkinsonism, Tardive dyskinesia with chronic use

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16
Q

erythromycin, oleandomycin, azithromycin, and clarithromycin

A

all imitate motilin (22 AA peptide hormone that amplifies motor activity through efects on enteric neurons and SM, secreted by enterochromaffin cells); typically cause gastric dumping which can move bezoars and improve gastric emptying with ileus, scleroderma, pseudo obstructions
-fast dumps can be painful, not recommended for chronic use

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17
Q

laxation vs catharsis

A

laxation: evacuation of formed fecal material from the rectum
catharsis: uniform evacuation of material from the entire colon

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18
Q

magnesium citrate

A

osmotic laxative: non-absorbable agent, increase osmotic pressure and cause H20 retention

  • these are really cathartics causing bowel emptying with watery stool, but act as laxatives at lower dosage
  • Magnesium may stimulate CCK receptors and increase motility as well
  • should be avoided by indiv w renal insuff, cardiac disease, electrolyte abnormalities, diuretic use
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19
Q

mag hydroxide

A

osmotic laxative: non-absorbable agent, increase osmotic pressure and cause H20 retention

  • these are really cathartics causing bowel emptying with watery stool, but act as laxatives at lower dosage
  • Magnesium may stimulate CCK receptors and increase motility as well
  • should be avoided by indiv w renal insuff, cardiac disease, electrolyte abnormalities, diuretic use
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20
Q

mag sulfate

A

osmotic laxative: non-absorbable agent, increase osmotic pressure and cause H20 retention

  • these are really cathartics causing bowel emptying with watery stool, but act as laxatives at lower dosage
  • Magnesium may stimulate CCK receptors and increase motility as well
  • should be avoided by indiv w renal insuff, cardiac disease, electrolyte abnormalities, diuretic use
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21
Q

polyethylene glycol

A

osmotic laxative: non-absorbable agent, increase osmotic pressure and cause H20 retention
-these are really cathartics causing bowel emptying with watery stool, but act as laxatives at lower dosage

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22
Q

lactulose

A

osmotic laxative: non-absorbable agent, increase osmotic pressure and cause H20 retention
-used for constipation associated with opioid use and vincristine

23
Q

mannitol

A

osmotic laxative: non-absorbable agent, increase osmotic pressure and cause H20 retention
-used for constipation associated with opioid use and vincristine

24
Q

sorbitol

A

osmotic laxative: non-absorbable agent, increase osmotic pressure and cause H20 retention
-used for constipation associated with opioid use and vincristine

25
Q

glycerin

A
  • a suppository that acts as a hydroscopic agent and lubricant
  • increased water retention stim peristalsis and prod an evacuation reflex
  • can produce movement within an hour
26
Q

docusate

A
  • stool wetting agent
  • surfactant that allows mixing of fatty substances and water in stool, as effective as stool softeners. Do not increase frequency
27
Q

bisacodyl

A

oral or rectal irritant laxative

  • thought to induce moderate inflammation leading to reduced water absorption and increased motility
  • generally safe, but OD causes catharsis
  • warn pt not to chew tabs, mix with milk or antacids to ensure tab reaches the site of ax in small intesting and avoid gastric irritation
28
Q

castor oil

A
  • smooth muscle stimulant, used as a laxative, cathartic, and to induce labor
  • speeds motility in the small bowel. 4 ml will prod laxative in 4 hours.
29
Q

methylcellulose

A

bulk forming laxatives, generally fiber based

  • material not broken down or absorbed, bulk material stim peristalsis/mass ax
  • great for regular soft stools
  • may exacerbate obstructions
  • may absorb other drugs
30
Q

psyllium

A

bulk forming laxatives, generally fiber based

  • material not broken down or absorbed, bulk material stim peristalsis/mass ax
  • great for regular soft stools
  • may exacerbate obstructions
  • may absorb other drugs
31
Q

polycarbophil

A

bulk forming laxatives, generally fiber based

  • material not broken down or absorbed, bulk material stim peristalsis/mass ax
  • great for regular soft stools
  • may exacerbate obstructions
  • may absorb other drugs
32
Q

carbooxymethylcelluose (polycarbophil derivatives)

A
  • bulk forming agent, based on colloids or polymers
  • absorb water in the GI tract to decrease stool fluidity
  • only symptomatic relief
33
Q

diphenoxylate/difenoxin

A
  • difenoxin is the active metabolite of diphenoxylate
  • piperidine derivates, antidiarrheal opioid
  • can have CNS effects, packaged with atropine to discourage abuse
34
Q

loperamide

A

-mu opioid receptor agonists that stops bowel motility

40 to 50x more potent than morphine, but does not enter CNS

35
Q

octreotide

A

parenteral octapeptide derivative of somatostatin (decreases pancreatic secretions)
-used to combat secretory diarrhea of homorone secreting tumors
-used for post op gastric dumping syndrome and diarrhea r/t chemo
-used to rest pancreas in pancreatitis
-reduces secretion of many GI hormones, including erotonin, gastrin, insulin, and secretin
-SE: Nausea, bloating, injection site pain
LT therapy may result in gallstones

36
Q

bismuth subsalicylate

A

Bismuth: 99% unabsorbed and eliminated in feces, has anti secretory, anti inflammatory and anti microbial activity; commonly included in H. Pylori Rx
Salicylate released in acidic environment, NSAD activity that is absorbed systemically
Mag aluminum silicate (clay)
-may have bulk forming effects

37
Q

alosetron

A

5HT3 antagonist used for diarrhea predominant IBS; generally produces effects opposite of 5HT4 agonists, but also may reduce visceral sensitivity by reducing sensory and vagal nerve signaling
-can produce serious constipation and potentially fatal ischemic colitis

38
Q

emesis control

A

CTZ: area postrema at the bottomof the 4th ventricle, traverses BBB and so senses both spinal fluid and blood for toxins
-solitary tract nucleus (STN) of vagus nerve

39
Q

ondansteron

A

5HT3 antagonist (4 hours); acts centrally on CTZ and STN
-acts peripherally in small intestine
(serotonin promotes gut motility)
-liver excretion

40
Q

graniesteron

A

5HT3 antagonist (9-12 hours); acts centrally on CTZ and STN
-acts peripherally in small intestine
(serotonin promotes gut motility)
liver excretion

41
Q

dolasteron

A

5HT3 antagonist (7-9 hours); acts centrally on CTZ and STN
-acts peripherally in small intestine
(serotonin promotes gut motility)
liver excretion

42
Q

palonosteron

A 
IV only
5HT3 antagonist, highest affinity in the class (40 hours); acts centrally on CTZ and STN
-acts peripherally in small intestine
(serotonin promotes gut motility)
liver/renal excretion
43
Q

5HT3 antagoinists SE

A

constipation, diarrhea, h/a, lightheadedness

44
Q

prochlorperazine

A

dopamine receptor antagonists, originally used as antipsychotics
-targets D2 receptors in CTZ and H1 receptors, can be good for motion sickness
-not as effective as reglan or 5HT3 antagonists against chemo induced N/V
SE: parkinsonism, extrapyramidal SE with LT use, dissociative dysphoria

45
Q

chlorpromazine

A

dopamine receptor antagonists, originally used as antipsychotics
-targets D2 receptors in CTZ and H1 receptors, can be good for motion sickness
-not as effective as reglan or 5HT3 antagonists against chemo induced N/V
SE: parkinsonism, extrapyramidal SE with LT use, dissociative dysphoria

46
Q

cyclizine

A

h1 receptor antagonists, widely used for motion sickness and post op emesis

  • act primarily on brainstem and vestibular apparatus
  • also has anticholinergic effects used in pt with abdominal ca
47
Q

promethazine

A

h1 receptor antagonists, widely used for motion sickness and post op emesis
-act primarily on brainstem and vestibular apparatus

48
Q

hydroxyzine

A

h1 receptor antagonists, widely used for motion sickness and post op emesis
-act primarily on brainstem and vestibular apparatus

49
Q

diphenhydramine

A

h1 receptor antagonists, widely used for motion sickness and post op emesis
-act primarily on brainstem and vestibular apparatus

50
Q

scopalomine

A

-muscarinic ACh receptor antagonist
-v effective for ST or LT prevention of motion sickness
-primarily acts on vestibular apparatus, not effective for chemi induced nausea. minimal CTZ effects
SE: dry mouth, blurred vision, may induce outburst of uncontrolled behavior when used in the presence of pain or anxiety

51
Q

glucocorticoids for IBD

A

-targets immune and inflammatory response in general, indicated for acute exacerbations and severe disease
-3 groups: 40% respond; 40% bcm dependent; 20% no response
-budesonide is 200x more potent than hydrocortisone, but only 10% bioavailable and most of that is removed in hepatic 1st pass. works like a topical rx in bowel
SE: immunosuppression, endocrine disruption, steroid psychoses and other effects typical of steroid rx

52
Q

thiopurines for IBD

A

6 mercaptopurine/azathioprine
-derivatives of cancer chemo with immunosuppressive effects
-all are prodrugs, inhibit DNA synthesis
-rapidly proliferating immune cells are targeted, used to maintain remission in UC and Chron’s, may help with fistulas in Chron’s
-effective in 2/3 patients, but req weeks/months for clinical response
SE: pancreatitis, fever, rash, arthralgia, N/V, BM suppression

53
Q

infliximab

A

monoclonal AB to TNF-alpha. interferes with the inflammatory response in IBD
-used to maintain remission, may gain use in acute UC, must be given parenterally
SE: increased URI, lack of effective response to TB

54
Q

adalimumab

A

human AB to TNF-alpha. somewhat less effective
-used to maintain remission, may gain use in acute UC, must be given parenterally
SE: increased URI, lack of effective response to TB

Mandie's Pharm test I (10 decks)

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