GI medications Flashcards
Where is the vomiting/emesis center in the brain
medulla oblongata
What does the vomiting/emesis center in the brain do
coordinates contractions of the pharyngeal, GI, and abdominal wall to expel gastric contents
What activates the vomiting center
Afferent fibers in the gut
CTZ
Cerebral cortex
vestibular apparatus
What is CTZ
chemoreceptor trigger zone
What are the chemoreceptors that effect the vomiting center of the brain
Seretonin 5-HT3
Dopamine D2
Muscarinic M1
How does the vestibular apparatus activate the vomiting center of the brain
There are afferent fibers that go into the cerebellum and triggers the release of acetylcholine / histamine
How does the Gut activate the committing center of the brain
There is a vagal afferent pathway to the solitary tract nucleus and then to the vomiting center
There is nerve stimulation of CTZ
D2, 5-HT3 and NK1 receptors
What groups of drugs are used for N/V
Cholinergic/muscarinic antagonist
Dopamine antagonist
seretonin antagonist
Cannabinoids
Histamine antagonists
What drugs for N/V are cholinergic antagonists
Scopolamine (Patch/IV)
What is the MOA of Scopolamine
Blocks acetylcholine at parasympathetic sites and reduces histamine and serotonin activity
What is the PK of scopolamine
Onset 6-8hours
lasts 72 hours
hepatic metabolism
What are the side effects of scopolamine
bradycardia, tachycardia, flushing, orthostatic hypotension, cognitive impairment, psychosis & hallucinations
Which patients cannot use scopolamine
Contraindicated in narrow-angle glaucoma
*or any agents containing belladonna
Which N/V medications are dopamine receptor antagonists
Phenothiazines
Butyrophenones
Benzamides
Which drugs are phenothiazines
Prochlorperazine
Which drugs are Butyrophenones
Haloperidol
Droperidol
Which drugs are benzamides
Metoclopramide
Trimethobenzamide
What is the MOA of dopamine receptor antagonists
Acts on CTZ and afferent pathways primarily in the gut
Does have M1 and Hq blocking effects
*metoclopramide has weak 5-HT3 blockage at higher doses
What are the side effects of dopamine receptor antagonists
Extrapyramidal rxns, QT prolongations, CNS effects, Hyperprolactinemia, tar dive dyskinesia
What major interactions do dopamine agonists have
TCA, SSRI, alcohol, anticholinergics, potassium
Which drugs are serotonin receptor antagonists
Ondansetron
Granisteron
What is the MOA of ondansetron
Blocks seretonin centrally
What are the side effects of Ondansetron
QT prolongation, dizziness, confusion, SOB, constipation
What are things to monitor with ondansetron
EKG monitoring
K+Mg levels
seretonin syndrome
Which drugs does ondansetron interact with
amioderone
QT prolongation drugs
CYP3A4 inducers
Which drugs are QT prolongators
SSRI
Antiarrhythmic agents
tramadol
St. Johns wart
What drugs are cannabinoids
Dronabinol
What are the side effects of cannabinoids
Euphoria, abdominal pain, vomiting, flushing, palpitations, xerostoma, vertigo
What major interactions do cannabinoids have
alcohol, anticholinergics, CNS depressants, CYP3A4 effectors, metronidazole, disulfiram, warfarin
What drugs are histamine antagonists
Promethazine
Meclizine
Dimenhydrinate
What is the MOA of Promethazine
Blocks the mesolimbic dopaminergic receptors in postsynaptic sites
blocks the release of hormones from the hypothalamus
blocks H1 in brainstem
What serious issue is associated with injectible promethazine
Tissue injury with extrav
What is the MOA of meclizine
Block H1 and prevents vasodilation, bronchoconstriction, and spasmodic contraction of GI smooth muscle
*may effect CTZ
What are the side effects of meclizine
Sedation
headaches
vomiting
blurred vision
Which patients should not receive meclizine
glaucoma
asthma
urinary retention
pyloric/duodenal obstruction
What does meclizine have major interactions with
alcohol
amphetamines
anticholinergics
nitro
K
What is the MOA of Dimenhydrinate
Binds the H1 receptor sites in peripheral sites including GI tract, respiratory tract, and blood vessels. Blocks CTZ and has central anticholinergic activity
What are the side effects of Dimenhydrinate
Tachycardia, sedation, dizziness, xerostoma, anorexia, blurred vision, thickened bronchial secretions, SJS
Which patients should you avoid using dimenhydrinate in
CVD, Thyroid dysfunction, respiratory disease, urinary obstruction, glaucoma, seizures
*dont use with ototoxic abx
What drug classes are used for Diarrhea and IBS-D
Opiod agonist
seretonin modulators
Bile Acid sequestrants
anti-spasmodics
antimicrobials
What is the MOA of opioid agonists
activates opioid receptor in the GI tract and alters peristalsis by preventing smooth muscle contraction
reduces stool volume and can prevent electrolyte depletion
Which patients should not use an opioid agonist
Those with infectious diarrhea or toxic megacolon
Which drugs are opioid agonists
Loperamide
Octreotide
Eluxadoline
Diphenoxylate/atropine
What are the side effects of loperamide
Constipation, dizziness, abdominal pain/cramping
What is the BBW with loperamide
cardiac arrest with large doses
Which opioid agonist contains atropine to prevent abuse
Diphenoxylate/atropine
What are the side effects of diphenoxylate/atropine
Flushing, tachycardia, xeroderma, toxic megacolon, urinary retention
What major interactions do diphenoxylate/atropine have
Azelistine, glucagon, pro kinetic agents, opioids, kava kava, nitro, zolpidem
What is the MOA of octreotide
Inhibits serotonin release and inhibits the secretion of gastrin, VIP, insulin, secretin, motion, and pancreatic polypeptide
What are the side effects of octreotide
bradycardia, fatigue, headache, dizziness, pruritic, hyperglycemia, cholelithiasis, biliary obstruction, URI, cardiac arrhythmias
Which drugs cannot be taken with octreotide
anti diabetic agents, cyclosporin, midodrine, MAOIs, quinolones, salicylates, SSRI
What is the MOA of Eluxadoline
Binds to mu, kappa, and delta opioid receptors in the intestinal lumen. Decreases intestinal motility without causing constipation
What are the side effects of Eluxadoline
Dizziness, drowsiness, constipation, N/V, elevated LFTs, URI, pancreatitis
Which patients cannot take Eluxadoline
those with ETOH abuse
hx of obstruction
Which drugs cannot be taken with Eluxadoline
alcohol, CNS depressants, aldosterone, opioid agonist, rosuvastatin, rifampin
When is Alosetron used
chronic, severe IBS-D
Which serotonin receptor modulator is used in emergencies only and why
Tegaserod d/t risk of cardiac arrest
Which drugs are serotonin modulators
Alosteron
Tegaserod
What is the MOA of Alosteron
Selective 5-HT3 agonist. Acts on the enteric neurons both centrally and peripherally. Affects visceral pain, colonic transit, and alters secretions in the GI tract
What are the side effects of Alosteron
Constipation, fatigue, headaches, abdominal pain, nausea, ischemic colitis
What is the MOA of bile acid sequestrants
Binds to bile salts in the intestine. Inhibits reuptake of bile salts, increases fecal loss of bile salts bound to LDL cholesterol as well.
*50% have bile acid malabsorption
What are the side effects of bile acid sequestrants
Bloating, biliary colic, gallbladder calcification, melena, dental erosion, tinnitus
*dont admin within 4-6 hours of other meds… can interfere with absorption
Which IBS-D drugs are antimicrobials
Rifamixin
Metronidazole
ciprofloxacin
amoxicilin
Neomycin
What is the MOA of Rifamixin
Binds to bacterial DNA dependent RNA polymerase thus inhibiting RNA synthesis
What are the side effects of Rifamixin
Peripheral edema
dizziness
ascites
headache
What may happen is rifamixin is used chronically
pseudomembranous colitis
Which drugs should rifamixin NOT be used with
cyclosporin
lactobacillus
sodium picosulfate
Which drugs are anti-spasmodics
Hyoscyamine
Dicyclomine
What is the MOA of anti-spasmodics
blocks acetylcholine at parasympathetic receptors. Antagonizes histamine and serotonin
What are the side effects of anti-spasmodics
tachycardia
mental status changes
impotence
urinary retention
increased IOP
Which groups of medications can be used for constipation
stool softeners
bulking laxative
osmotic laxatives
stimulant laxatives
selective opioid antagonists
guanylate cyclase- C agonists
What drugs are stool softeners
Docusate sodium
What is the MOA for decussate sodium
lowers the surface tension at the oil-water interface of the feces, allowing for water and lipids to penetrate the stool to help hydrate and soften the fecal material
What is a side effect of decussate sodium
throat irritation
Which drugs are bulking laxatives
methylcellulose
psyllium husk powder
wheat dextrin
calcium polycarbophil
What is the MOA of bulking laxatives
absorb and retain water in the intestine thus increasing the mass of stool which promotes peristalsis through distention of intestinal lumen
What are the side effects of bulking laxatives
bloating, flatulence, GI distress
Which drugs are osmotic laxatives
Saline
Lactulose
polyethylene glycol
glycerin
What is the MOA with saline laxatives
retain water in the intestine thus increasing the intraluminal pressure and promotion of peristalsis
What are some side effects of saline laxatives
Bloating, abd pain, phosphate nephropathy, hypokalemia
*caution with myasthenia gravis
What is the MOA of lactulose
disaccharide that promotes fluid retention in the intestine to increase intraluminal pressure and promote peristalsis
What are the side effects of lactulose
electrolyte imbalance, hypernatremia, hypokalemia, diarrhea
What are the side effects of Glycerin suppository
rectal burning, abdominal cramping, tenesmus, irritation
What drugs are stimulant laxatives
Dulcolax
Senna
What is the MOA of stimulant laxatives
alter the fluid excretion by acting directly on the cells of the intestinal mucosa and increase motility by acting on cells
Which drugs are opioid antagonists
naloxegol
methylnaltrexone
What is the MOA of naloxegol
Mu receptor antagonist by binding to polyethylene glycol to prevent crossing BBB
What are the side effects of Naloxegol
abdominal pain, headaches, diarrhea, nausea, GI perforations
What meds are IBS-C
Lubiprostone
Linaclotide
What is the MOA of Lubiprostone
Activates chord channels and increases fluid secretion by the cells in the intestinal membrane
also counteracts the anti secretory effects of opioids
What is the MOA of Linaclotide
Acts on guanylate cyclase on the epithelium of the intestine, increasing cyclic guanosine monophosphate. Stimulates chloride and bicarbonate secretion and intraluminal pressure promoting peristalsis