Nausea/Vomiting drugs Flashcards
What are the receptors targeted by anti emetic drugs
- 5-HT3 . . serotonin type-3
- H1
- M1
- D2
- NK1
Which of the classes of drugs for vomiting is the only AGONIST
Cannabinoid Receptor Agonist
What do Serotonin receptor antagonists end with
Setron
Tell me about serotonin receptor antagonists
- Very strong and effective
- Indicated for chemo induced N/V (CINV)
- also Radiation induced, Post-operative, and Pregnancy
Most worrisome adverse effect of Serotonin antagonists
- Dose-dependent QT prolongation and Torsade’s
- Use extreme caution when other QT-prolonging agents (anti-arrhythmics)
Most 5-HT3 receptors have short half-lives . . which is the one that has long half life that lasts 24-40 hours
Palonsetron
What do NK1 antagonists end with
Pitant
Indications for NK1 antagonists
-moderate antiemetic agents so only used for Chemo and with another agent
What are the NK1 antagonists that are used for prophylaxis of post-operative N/V
- only aprepitant and fosaprepitant
- up to 3 hours prior to anesthesia induction
Which of the NK1 antagonists have moderate-major active metabolites and longer half lives
Netupitant/Rolapitant
What are the H1 receptor antagonists
- Diphenhydramine
- Dimenhydrinate
- Hydroxyzine
- Promethazine
- Meclizine
- Cyclizine
Describe the H1 receptor antagonists
- weak antiemetics
- Never used by themselves for chemo
- usually just used for normal run of the mill N/V
What are the adverse effects of H1 antagonists
Classic anticholinergic effects
- Dry mouth
- Urinary retention
- Blurred vision
- Sedation
H1 antagonists for motion sickness
- Meclizine
- Cyclizine
What are the antiemetic D2 antagonists?
- Chlorpromazine
- Perphenazine
- Prochlorperazine
- Metoclopramide