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Antiemetics

GI Drugs

QuestionAnswer
emesis N/V, protective to expel toxins from GIT, involve central chemoreceptor trigger zone in the mid-brainstem, serotonin, dopamine, muscarinic receptor
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
Serotonin 5HT3 receptor antagonists, CYP metabolized, prolong QT interval Ondansetron (Zofran), Dolasetron, Granisetron, Palonosetron
Ondansetron (Zofran), Dolasetron, Granisetron Serotonin 5HT3 receptor antagonists, antiemetics, PO/IV, 4-9 hr. half life
Palonosetron antiemetic, serotonin 5HT3 antagonists, potent, longer half life 40 hr, high affinity
Antiemetics SE HA, dizziness, contipation (GI 5HT)
Dolasetron more pronounced QT elongation
avoid with other drugs that can alter cardiac conduction? Class 1C, Class 3
Corticosteriods Dexamethasone (Decadron) antiemetic properties, enhance efficacy of 5HT3 receptor antagonists for CINV
Phenothiazines Prochlorperazine, Chlorpromazine antiemetic, antihistamine, anticholinergic, good for motion sickeness, antagonize/block dopamine, histamine, cholingeric receptors at trigger zone, lots of SE
Phenothiazines SE Prochlorperazine, Chlorpromazine sedative, anticholinergic effects
Antihistamines diphenhydramine (benedryl) meclizine (bonine) scopolamine
diphenhydramine Benedryl anticholinergic, antihistamine properties
Meclizine Bonine antihistamine, minimal anticholinergic actions = less sadtion
scopolamine antihistamine, potent muscarinic actions = very sedating, best tolerated as transdermal patch (sustained release) for motion sickness
What group of drugs have the suffix -setron? antiemetics
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
What does substance P signify? pain
Fosaprepitant IV, converts to aprepitant within 30 min
What is Fos-? prodrug with an esterase for activation (aprepitant)
Triple therapy for emesis? 5HT3 antagonist dexamethasone NK1 receptor antagonist for 94% prevention
Double therapy for emesis? 5HT3 antagonist dexamethasone for 67% prevention
Cannabinoid agonists (Cannabis) Dronabinol used for nausea, appetite stimulant, pain, emesis, natural-occurring cannabinoid CB1 receptors in brain, SE: high, paranoia, withdrawal, abuse potential
Created by: cburrows