GI Drugs
Quiz yourself by thinking what should be in
each of the black spaces below before clicking
on it to display the answer.
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| emesis | N/V, protective to expel toxins from GIT, involve central chemoreceptor trigger zone in the mid-brainstem, serotonin, dopamine, muscarinic receptor
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| antiemetics | used for chemotherapy, post radiation therapy, motion sickness, opioids use, postop, CINV (chemo induced N/V) inject 30min prior to chemo and combo w/corticosteroids and NK1 receptor antagonists, well tolerated
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| Serotonin 5HT3 receptor antagonists, CYP metabolized, prolong QT interval | Ondansetron (Zofran), Dolasetron, Granisetron, Palonosetron
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| Ondansetron (Zofran), Dolasetron, Granisetron | Serotonin 5HT3 receptor antagonists, antiemetics, PO/IV, 4-9 hr. half life
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| Palonosetron | antiemetic, serotonin 5HT3 antagonists, potent, longer half life 40 hr, high affinity
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| Antiemetics SE | HA, dizziness, contipation (GI 5HT)
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| Dolasetron | more pronounced QT elongation
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| avoid with other drugs that can alter cardiac conduction? | Class 1C, Class 3
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| Corticosteriods Dexamethasone (Decadron) | antiemetic properties, enhance efficacy of 5HT3 receptor antagonists for CINV
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| Phenothiazines Prochlorperazine, Chlorpromazine | antiemetic, antihistamine, anticholinergic, good for motion sickeness, antagonize/block dopamine, histamine, cholingeric receptors at trigger zone, lots of SE
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| Phenothiazines SE Prochlorperazine, Chlorpromazine | sedative, anticholinergic effects
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| Antihistamines | diphenhydramine (benedryl)
meclizine (bonine)
scopolamine
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| diphenhydramine Benedryl | anticholinergic, antihistamine properties
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| Meclizine Bonine | antihistamine, minimal anticholinergic actions = less sadtion
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| scopolamine | antihistamine, potent muscarinic actions = very sedating, best tolerated as transdermal patch (sustained release) for motion sickness
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| What group of drugs have the suffix -setron? | antiemetics
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| Aprepitant (Emend) | highly selective PO substance P neurokinin 1 (NK1) receptor antagonist, used in combo w/antiemetics regimens (5HT3 antagonist+corticosteriod) to prevent CINV, CYP substrate, SE: fatigue, dizziness, diarrhea
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| What does substance P signify? | pain
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| Fosaprepitant | IV, converts to aprepitant within 30 min
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| What is Fos-? | prodrug with an esterase for activation
(aprepitant)
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| Triple therapy for emesis? | 5HT3 antagonist
dexamethasone
NK1 receptor antagonist
for 94% prevention
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| Double therapy for emesis? | 5HT3 antagonist
dexamethasone
for 67% prevention
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| Cannabinoid agonists (Cannabis) Dronabinol | used for nausea, appetite stimulant, pain, emesis, natural-occurring cannabinoid CB1 receptors in brain, SE: high, paranoia, withdrawal, abuse potential
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