Anti-Emetics Flashcards
SCOPOLAMINE (Transderm Scop) Class
Anticholinergic; anti-emetic and anti-vertigo (dermal patch)
SCOPOLAMINE (Transderm Scop) MOA
blocks activity of acetylcholine at PSNS sites in smooth muscle, secretory glands, and CNS
SCOPOLAMINE (Transderm Scop) Indications
nausea, vertigo
SCOPOLAMINE (Transderm Scop) S/E
sedation, dry mouth, pupillary dilatation, constipation; confusion, urinary retention
MECLIZINE (Antivert) Class
antiemetic, H1 antagonist
MECLIZINE (Antivert) Indication
prevention and treatment of motion sickness
MECLIZINE (Antivert) MOA
central anticholinergic blockage in chemoreceptor trigger zone and decreases excitability of vestibular-cerebellar pathways which reduces motion sickness
MECLIZINE (Antivert) S/E
sedation, fatigue, vomiting, blurred vision
PROMETHAZINE (Phenergen) Class
Phenothiazine
PROMETHAZINE (Phenergen) Indication
Antiemetic, motion sickness, sedative
PROMETHAZINE (Phenergen) MOA
blocks CNS dopamine receptors (D2); competes for H1 receptors
PROMETHAZINE (Phenergen) S/E
VERY SEDATIN, confusion, delirium, extrapyramidal symptoms; cardiac arrhythmias, orthostatic hypotension, urinary retention
HALOPERIDOL (Haldol) Class
Butyrophenones; typical antipsychotic
HALOPERIDOL (Haldol) Indication
antiemetic; schizophrenia, Tourette’s disorder; emergency sedation of agitated-aggressive patients (off label)
HALOPERIDOL (Haldol) MOA
blocks postsynaptic mesolimbic D1 and D2 receptors; also suppresses the reticular activating system (RAS) thereby reducing emesis
HALOPERIDOL (Haldol) S/E
agitation, akithesia, alteration of temp regulation, confusion; QT prolongation, EPS (tardive dyskinesia), NMS, anticholinergic effects
METOCLOPROMIDE (Reglan) Class
Benzamide; anti-emetic; prokinetic
METOCLOPROMIDE (Reglan) Indication
anti-emetic; diabetic gastroparesis, GERD
METOCLOPROMIDE (Reglan) MOA
blocks D and 5-HT receptors in CRTZ
METOCLOPROMIDE (Reglan) S/E
AV block, drowsiness, fatigue, diarrhea; Tardive dyskinesia, EPS (esp acute dystonic reactions initial 24-48h); pseudoparkinsonism; rarely NMS
DEXAMETHASONE (Maxidex) Class
corticosteroid
DEXAMETHASONE (Maxidex) Indication
anti-emetic; immune modulation
DEXAMETHASONE (Maxidex) MOA
enhance effect of 5-HT3-receptor antagonists CRTZ
DEXAMETHASONE (Maxidex) S/E
single dose regimen so minimal
DRONABINOL (Marinol) class
Tetrahydrocannabinol (THC)
DRONABINOL (Marinol) Indication
appetite stimulant; anti-emetic (chemo related)
DRONABINOL (Marinol) MOA
unknown
DRONABINOL (Marinol) S/E
euphoria, dysphoria, sedation, dry mouth; tachycardia, orthostatic hypotension
Contra: hx schizophrenia, seizure disorders, hepatic disease
ONDANESTRON (Zofran) Class
serotonin antagonist
ONDANESTRON (Zofran) Indication
post-op, radiation and chemotherapy induced N/V
ONDANESTRON (Zofran) MOA
peripheral and CRTZ 5-HT3 receptor blockade
ONDANESTRON (Zofran) S/E
headache, dizziness, constipation, malaise, fatigue; QT prolongation, hypoxia
Contra: hypersensitivity; cardiac arrhythmias
If we blockade central and peripheral 5-HT3 receptors, where are they located?
Intestinal vagal & spinal afferent nerves
When is Odanestron most effective?
When pretreated, and on a scheduled bases.
APREPITANT (Emend) Class
neurokinin-1 antagonist
APREPITANT (Emend) Indicaiton
prevention chemo induced N/V; post-op N/V
APREPITANT (Emend) MOA
blocks central NK1 receptors; augments anti-emetic effect of 5-HT3 receptor antagonism and corticosteroids
APREPITANT (Emend) S/E
fatigue, nausea, constipation, muscle weakness, diarrhea
Can we combine Aprepitant with anything else to prevent chemo induced N/V?
5-HT3 & corticosteroids
LORCASERIN (Belviq) Class
peripherally-acting opioid antagonist
LORCASERIN (Belviq) Indicaiton
opioid-induced constipation
LORCASERIN (Belviq) MOA
Mu-opioid receptor antagonist (conjugated with PEG reducing its ability to cross BBB) so acts peripherally in GI tract
LORCASERIN (Belviq) S/E
abdominal pain, headache, N/V/D
