GI System from Pharm Perspective Flashcards

1
Q

What are the receptors for SNS on GI

A
  1. wall - relaxed by acting on Alpha 2 and beta 2

2. spincters - contract by alpha 1

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2
Q

What are the receptors for PNS on GI

A
  1. contracts walls via M3
  2. relaxes sphincters via M3
  3. increases secretions via M3
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3
Q

What will happen w/ ganglionic blockade of PNS

A

reduced tone and motility; constipation; decreased gastric and pancreatic secretions

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4
Q

What are symptoms of excess cholinergic effects

A

DUMBELLS

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5
Q

What are the symptoms of cholinergic deficit

A

Constipation, urinary retention, mydriasis/blurred vision, bronchodilation, tachycardia, antiemesis, decreased glandular secretions, restlessness, confusion, delirium, hallucinations

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6
Q

What is the role of Ach in ENS

A

primary excitiatory transmitter to SM and secretory cells. Major neuron-neuron transmitter in ENS

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7
Q

What is the role of Dopamine in ENS

A

modulatoary transmitter in ENS

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8
Q

What is the role of enkephalin and related opioids

A

present in some secretomotor and interneurons in ENS. inhibits Ach release and peristalsis. May stimulate secretion

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9
Q

What is the role of serotonin

A

important transmitter or cotransmitter at excitatory neuron-neuron junctions in the ENS

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10
Q

What is being considered for treatment of some IBS cases

A

Might be related to serotonin disequilibrium. there is excess 5HT in D-IBS. Insufficient release of 5HT for C-IBS.
-giving partial agonists so that you can treat the spectrum of diseases

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11
Q

MOA of Tegarserod

A

partial 5HT-4 agonists. Withdrawn from market b/c of many heart problems

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12
Q

MOA of citalopram

A

SSRI

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13
Q

What has been IDed as playing a pivotal role in inflammation of IBD

A

TNF-alpha. Now using mabs that soak up the TNF-alpha w/ infliximab. This therapy is only started after steroid therapy is unsuccessful

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14
Q

What are the effects of opioid receptors and GI phys

A

Receptors are found in the ENS. they relieve pain but have a delayed transit effect in the GI causing constipation

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15
Q

What is the MOA of Naloxone and methylnaltrexone

A

opioid receptors. micro-receptors w/ Beta-endorphin being the ligand. Location of receptors are in both myenteric and submucosal plexus

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16
Q

What is the GI effects of naloxone and methylnaltrexone

A

delayed transit, visceral antinociception

17
Q

What are the different forms of drug-induced diarrhea

A
  1. osmotic
  2. secretory
  3. disordered motility
  4. inflammatory - due to disruption of colonic flora, disruption of acid-base environment or epithelial homeostasis
18
Q

Who is an increased risk for pill-induced esophagitis

A
  1. old age
  2. institutionalization
  3. preexisting esophageal or swallowing disorders
  4. recumbent position
    * gelatin capsules, extended/sustained release products increase risk of this
19
Q

What are common side effects of pill-induced esophagitis

A
  1. constipation
  2. bleeding, erosions – dont’ forget NSAIDS can do this
  3. pill esophagitis
20
Q

What is drug absorption based on

A
  1. depends on drug formulation and physiochemical properties.
  2. absorption can occur throughout the GI tract depending on formulation and local pH
  3. Pgp interactions - if there is decreased Pgp activity there will be a dramatically increased drug concentration
  4. CYP3A4 - overlapping role w/ Pgp and cyp metabolism can even be controlled by Pgp
21
Q

What are some drug interactions of antacids

A
  1. chelations especially for antimicrobials such as Doxy, tetra, and most fluoroquinolones.
  2. can cause constipation or diarrhea and can alkalinze the urine
22
Q

Drug interactions of H2 blockers

A
  1. increase pH - affects many drugs
  2. Cimetidine - inhibits lots of CYPs affecting many drugs
  3. Famotidine - decreased theophylline clearance
23
Q

Drug interactions of PPIs

A
  1. all substrates for CYP2C19, all exert some degree of 2C19 inhibition
  2. decreased effectiveness of clopidogrel (needs 2C19 activation)
  3. decrease bioavailability of antiretrovirals