GI motility drugs Flashcards
Location of emesis center
Medulla
Afferents of the emesis center
CTZ in area postrema
Vestibular apparatus
Vagal afferents via solitary tract nucleus
Activating receptors on the CTZ
Serotonin
5-HT3
Dopamine D2
Muscarinic M1
Substances released by vestibular apparatus to activate vomiting center
Ach
Histamine
Drug class of Hyoscine
Anticholinergic antiemetic
Drug class of scopolamine
Anticholinergic antiemetic
Drug class of dicyclomine
Anticholinergic antiemetic
Most effective drug for motion sickness
Hyoscine
Side effects of anticholinergic antiemetics
Sedation and dry mouth
Use of anticholinergic antiemetics
Motion sickness
H1 antihistamine with significant antimuscarinic acitivity
Promethazine
Drug class of promethazine
H1 antihistamine and D2 blocker
Drug class of Doxylamine
H1 antihistamine
Drug class of meclizine
H1 antihistamine
H1 antihistamine that is less sedative and has a longer duration of action
Meclizine
Duration of action of meclizine
24 hrs
Antiemetic available in a slow-release patch that lasts 72 hrs
Scopolamine
Drug class of cinnarizine
H1 antihistamine
Use of meclizine
Sea sickness
Uses of cinnarizine
Vertigo
Motion sickness
General uses of H1 antihistamine antiemetics
Motion sickness
General side effects of H1 antihistamine antiemetics
Sedation and dry mouth –> anticholinergic action
Drug class of chlorpromazine
D2 blocker (neuroleptic) antiemetic
Drug class of domperidone
D2 blocker (neuroleptic) antiemetic
Mechanism of D2 blocker antiemetics
D2 receptor antagonist that primarily acts on CTZ, as it does not cross the BBB
Drug class of ondansetron
First generation 5-HT3 antagonist
Drug class of Granisetron
First generation of 5-HT3 antagonist
Drug class of dolasetron
First generation 5-HT3 antagonist
Use and administration of first generation 5-HT3 antagonists
Given 3-5 days after chemotherapy for N/V
Also used for postoperative nausea
Drug class of palonosetron
Second generation 5-HT3 antagonist
5-HT3 antagonist with a longer duration of action
Palonosetron
Antiemetic that may prevent N/V for up to 7 days after chemotherapy, approved for treating both acute and delayed N/V
Palonosetron
Antiemetic drug class that prevents both peripheral and central stimulation of the vomiting center
5-HT3 antagonists
Drug class of aprepitant
NK1 receptor antagonist
Drug that blocks the emetic action of substance P at NK1 receptor
Aprepitant