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Therapeutics - Exam 6 > Lectures 61/62 > Flashcards

Lectures 61/62 Flashcards

GI Protectant (Hockerman)

1
Q

sodium bicarbonate - NaHCO3

A

systemically absorbed
neutralizing capacity - High
AE - systemic alkalosis, fluid retention, excess CO2 gas
commercially - in alka-seltzer with ASA

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2
Q

calcium carbonate - CaCO3

A

systemically absorbed
neutralizing capacity - moderate
AE - hypercalcemia, nephrolithiasis, milk-alkali syndrome CO2
commercially - tums and in rolaids with magnesium hydroxide

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3
Q

aluminum hydroxide - Al(OH)3

A

minimally absorbed
neutralizing capacity - high
AE - constipation, hypophosphatemia, if absorbed encephalopathy
commercially - AlternaGEL, in Maalox/Mylanta with magnesium hydroxide

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4
Q

Magnesium hydroxide - Mg(OH)2

A

minimally absorbed
neutralizing capacity - high
AE - diarrhea, if absorbed CNS toxicity
commercially - in Maalox/Mylanta with alumnium hydroxide and in Rolaids with calcium carbonate

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5
Q

PPI mechanism

A

irreversibly inhibit the proton pump to prevent H+ from leaving the parietal and combing with Cl- to form acidic HCl
prodrugs

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6
Q

PPI DRUGS

A

esomeprazole (nexium)
omeprazole (prilosec)
lansoprazole (prevacid)
rabeprazole (aciphex)
pantoprazole (protonix)
dexlansoprazole (dexilant)

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7
Q

vonoprazan

A

not a prodrug
potassium-competitive acid blocker (P-CAB)
recently approved in the US

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8
Q

sucralfate mechanism

A

polymerizes and forms protective barrier at ulcer site
acidic pH activates complex

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9
Q

misoprostol (cytotec) mechanism

A

reduced acid secretion of the parietal cells
has cytoprotective effects of enhanced mucus and bicarbonate secretion
semi-synthetic PGE1 derivative
used in combo with chronic NSAIDs

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10
Q

BSS mechanism

A

converted to bismuth salts and salicylic acid in the GI tract with antibacterial, antiviral, and antisecretory activity

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11
Q

rationale for antibiotic treatment of ulcers

A

many peptic ulcers are associated with infection of gastric mucosa by the gram negative bacili, H Pylori

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12
Q

combination therapy for antibiotic treatment of ulcers

A
  1. BSS
  2. some antibiotic - metronidazole, tetracycline, amoxicillin, clarithromycin
  3. H2RA or PPI
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13
Q

laxative classes

A

bulk and osmotic laxatives
stool softeners
secretory/stimulant laxatives

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14
Q

bulk and osmotic laxatives

A

psyllium (metamucil), methylcellulose (citrucel), calcium polycarbophil (FiberCon), PEG 3350 (Miralax), or Macrogol/Movicol
mechanism - increase water in the intestinal lumen via non-absorable sugars by osmotic force leading to distention and an increase in peristalsis

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15
Q

stool softeners

A

examples - docusate sodium (colace), mineral oil, glycerin, surfactants, and lubricants
mechanism - incorporate into stool to make passage easier and decrease water absorption; lubricate lower bowel to reduce fecal impaction; can decrease absorption of fat soluble vitamins

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16
Q

secretory/stimulant laxatives

A

examples - castor oil, bisacodyl, duloclax, cascara, senna, and aloes
mechanism - poorly known; irritation of the mucosa affects fluid secretion/absorption balance and induces peristalsis

17
Q

5HT4 receptor agonists

A

Prucalopride (Motegrity) and Tegaserod (Zelnorm)
serotonin receptor, GPCR, GaS coupled, activation leads to increased cAMP, PKA activation, and release of ACh

18
Q

Prucalopride (Motegrity) uses

A

chronic idiopathic constipation in adults

19
Q

Tegaserod (Zelnorm) uses

A

IBS with constipation in women under 65yo

20
Q

Tenapanor

A

sodium hydrogen exchanger (NHE3) inhibition to prevent the absorption of sodium from the luminal contents

21
Q

prokinetic drugs

A

prucalopride
tegaserod
tenapanor
bethanechol
erythromycin
metoclopramide
neostigmine
Cl channel activators
Opioid receptor antagonists

22
Q

metoclopramide (reglan)

A

D2 dopamine receptor antagonist
blockade of D2 receptors in the myenteric plexus leads to increase ACh release and produces anti-emetic effects
USES - promotes gastric emptying to facilitate small bowel intubation, post op and diabetic gastroparesis, and GERD

23
Q

chloride channel activator drugs

A

lubiprostone (amitiza)
plecanatide (trulance)
linaclotide (linzess)

24
Q

lubiprostone (amitiza)

A

stimulation of type 2 chloride channel (CIC-2)
increases chloride rich fluid secretion into the intestine
USES - IBS with constipation

25
Q

plecanatide (trulance) and Linaclotide (Linzess)

A

peptide activator of guanylate cyclase C (GC-C)
increases chloride-rich fluid secretion into intestine
USES - IBS with constipation

26
Q

centrally acting opioid receptor antagonists

A

naloxone (narcan)
naltrexone
nalmefene
anti-addictive agents

27
Q

peripherally acting opioid receptor antagonists

A

naloxgeol (movantik)
alvimopan (entereg)
naldemedine (symproic)
cannot cross BBB

28
Q

antidiarrheals

A

slow peristalsis to increase water and electrolyte absorption
opiates and 5HT receptor antagonist

29
Q

opiates

A

mechanism - inhibition of presynaptic cholinergic nerves
diphenoxylate (combined with atropine for lomotil; active in the CNS) and loperamide (poorly traverse the BBB, acts locally)

30
Q

Alosetron (Lotronex)

A

mechanism - blocks visceral afferent spin sensation and decreases colon motility
USES - women with severe IBS-D
5HT receptor antagonist

31
Q

anti-emetics

A

5HT receptor antagonists
NK1 antagonists
antihistamines/anticholinergics
D2 dopamine receptor antagonists

32
Q

anti-emetic 5HT receptor antagonists

A

ondansetron (zofran), granisetron, dolasetron, palonosetron
mechanism - blocks activity of afferent nerves from stoamch adn small intestine which activate the trigger center in the CNS
USES - CINV

33
Q

NK1 antagonists

A

drugs - aprepitant, netupitant, rolapitant
can be combined with 5HT3 antagonists

34
Q

antihistamines/anticholinergics

A

drugs - dimehydrinate (dramamine), meclizine (antivert), promethazine, scopolamine
USES - prevent motion sickness

35
Q

anti-emetic D2 dopamine receptor antagonists

A

drugs - metoclopramide (reglan), prochlorperazine (compazine), droperidol (inapsine)

Therapeutics - Exam 6 (11 decks)

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