Anti-Nausea And Anti-Emetic Drugs - Dr. Segars Flashcards
what do anti N/V medication do
block either 5-HT, H1, M1,D2, or Neurokinin1 (substance P) receptors
6 classes of medication MOA
- Serotonin receptor antagonist
- Neurokinin receptor antagonist
- Histamine Receptor antagonist
- Dopamine receptor antagonist
- Muscarinic receptor antagonist
- Cannabinoid receptor AGONIST
2 extra classes on their own for N/V
Glucocorticosteroids (Dexamethasone*)
Benzodiazepines (alprazolam, lorazepam)
5 5-HT receptor antagonists
- Dolasetron
- Granisetron
- Ondansetron
- Palonosetron
- Alosetron (only for IBS-D)
5-HT receptor antagonists work how
block receptor activation when seratonin is released from intestinal enterochromaffin cells to the vagal nerve terminals
5-HT receptor antagonists
used for what
any use (first one to go to) - post-operative, radiation, chemo, preg, infections, vertigo motion sickness
5-HT receptor antagonists
adverse effects you should think about
- serotonin syndrome : pt taking other serotonin drugs (psychiatry) can get this and feel very bad like the flu
- Dose-dependent QT prolongations : pt with arrhythmia or MI or heart conditions on QT prolonging drugs, or pt with electrolyte imbalance like hypo-K or Mg, need to be monitored with EKG and can still take this drug (except for Dolesetron)
5-HT receptor antagonists half lives
short except Palonosetron and Granisetron have long half-life and = for delayed chemo N/V 1 dose only
5-HT receptor antagonists D-D interactions
antiarrhythmics, QT prolonging agents
3 NK1 Receptor Antagonists
- Aprepitant, Foraorepitant (fos = given as IV and then cleaved to active form)
- Netupitant, fosnetupitant
- Rolapitant
NK1 Receptor Antagonist used for what
Chemotherapy induced N/V only
usually used with other anti-emetic drugs
NK1 Receptor Antagonist adverse effects and in body interactions
- GI,CNS mild like all other emetic drugs
2. Netupitant and Rolapitant = active metabolites still working as anti-emetic so long halflife drug
6 H1 receptor Antagonists
- Diphenhydramine, Dimenhydrinate = in Benadryl
- Hydroxyzine
- Promethazine
- Meclizine
- Cyclizine
- Doxylamine
H1 receptor Antagonist used when
- Doxylamine + Pyridoxine (VitB6) = for pregnancy
- Meclizine + Cyclizine = motion sickness and vertigo
- all other reasons
H1 receptor Antagonist adverse effects
- Drowsiness
- dry mouth
- constipation
- urinary retention
- blurred vision
- Decreased BP
* *** Anti cholinergic effects
4 D2 receptor Antagonists
- Prochlorperazine
- Olanzapine
- Metoclopramide
- Amisulpride
D2 receptor Antagonist Metoclopramide does what and is used for
stimulated ACh in GI = enhance GI motility AND increase LES tone ** common needed in DM pts
= help dymotility, gastroparesis
D2 receptor Antagonist Amisulpride used for
prevention and tx os Post-operative N/V by IV = only when all other therapies fail