Constipation, Diarrhea, Nausea/Vomiting Flashcards
methyl cellulose / psyllium MOA
dietary fiber and bulk forming laxative - hydrophilic muciloid that forms gelatinous mass when mixed with water
methyl cellulose / psyllium AE
allergic reactions, flatulence, borborygmi, intestinal obstruction
DDI of metamucil
inhibit coumarin absorption
DDI of citrucel (cellulose)
bind & impede drug absorption
uses for dietary fibers
both for constipation as a stool former and to treat IBS diarrhea by forming bulkier stool
AE for laxatives
- abuse
2. lag time leads to overdose and the following shit storm
lactulose MOA
not absorbed and produces osmotic laxative effect, fecal acidifier and TRAPS ammonia in ammonium form for excretion
stimulant laxatives (3)
bisacodyl (dulcolax)
senna
cascara sagrade extract
MOA of stimulant laxatives
mostly on LARGE bowel
- increase permeability of mucosa
- increas back diffusion of H20 & electrolytes
- propulsive contractility of colon
- stimulate prostaglandin synthesis
AE for bisacodyl (dulcolax)
excessive fluid loss, electrolyte loss, intestinal enterocyte damage
PK for bisacodyl (dulcolax)
prodrug - bacteria activated, is administered in enteric coated tab
AE for senna
abdominal pain, nephritis, melanotic pigmentation of colonic mucosa, abnormal urine coloration
PK for senna
natural derivative of senna/cascara - more gentle than the synthetics
castor oil MOA
rapid-acting and effective anionic surfactant - produces catharsis
castor oil AE
colic, dehydration, electrolyte imbalance - can induce uterine contraction in pregnancy
2 surfactant laxatives
castor oil & docusate sodium (colace)
docusate sodium (colace) MOA
anionic surfactant, weakly active, primarily used as stool softener, no effect on intestinal peristalsis
AE for docusate sodium (colace)
irritate mucosa and increase other drug absorption
CI for docusate sodium (colace)
not for use during abdominal pain, n/v
long term or short term use for docusate sodium (colace)
short term
lubiprostone MOA
activates intestinal Cl channels in a protein kinase-A independent fashion - increases intestinal fluid secretion & motility & alleviates symptoms of idiopathic constipation
Tegaserod MOA
activation of 5-HT4 recetpors in GI tract - effective motility stimulant (also 5-HT2b antagonist)
Tegaserod AE
5-HT2b antagonist activity has shown CV adverse effects
opiate (1)
loperamide
loperamide effects
- dec salivary, gastric, intestinal secretions
- dec motility of stomach & intestines
- inc muscle tone but dec cramps
- inc tone of sphincters
- inc contact time and reabsorption
loperamide MOA
interacts with intestinal opioid receptors and binds to and inhibits calcium binding protein calmodulin
anticholinergic for motion sickness
scopolamine
MOA of scopolamine
blocks activation of muscarinic receptors and dec cochlear sensation of motion
AE of scopolamine
sedation, extrapyramidal (drowsiness, dry mouth)
scopolamine PK
patch placed behind ear before trip
use for scopolamine
MS prophylaxis
H1 antihistamines - antiemetics
cyclizine, meclizine, chlorpheniramine
which are piperazine derivative H1 antihistamines
cyclizine and meclizine
pharm effects of cyclizine and meclizine
significant anti-cholinergic effects
AE for H1 antihistamines
sedation, anticholinergic
which H1 antihistamine has the least sedative & GI AE
chlorpheniramine
clinical use for cyclizine
OTC to counter MS
clinical use for meclizine
vertigo and menier’s disease
antidopaminergics (3) - antiemetics
chlorpromazine, droperidol, metoclopramide
chlorpromazine MOA
blocks DA receptors in CTZ and centrally acting anticholinergic
clinical utility for chlorpromazine
n/v, intractable hiccough
droperidol MOA
blocks DA receptors in CTZ
droperidol clinical utility
poor antipsychotic but highly useful antiemetic
metoclopramide MOA
DA receptor antagonist that blocks chemotherapeutic induced activation of D2 receptors in CTZ - also stimulates gastric emptying
metoclopramide clinical utility
prophylaxis prior to cancer chemo & prevention of post-op n/v
serotonin antagonists
granisetron, dolasetron
MOA of serotonin antagonists
5-HT antagonist blocks receptors in stomach/SI
- block signal to CTZ and to VC
- block 5-HT3 receptor in CTZ
which serotonin antagonist has longest half life
dolasetron
clinical utility for methylprednisolone
anti-emetic effect through prevention of prostaglandins - given with aforementioned entiemetics to increase their potency and reduce side effect profile
aprepitant MOA
substance P/neurokinin 1 (NK1) antagonist - crosses BBB and inhibits central emesis
PK of aprepitant
half life 9-13 hours, given orally
metabolism by CYP3A4
lorazepam utility
effective for anticipatory vomiting because causes somnolence and amnesia