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
what is the D2 antagonist used to stimulate ACh actions in GI, enhanding GI motility and increasing LES tone
Metoclopramide
Adverse effects of dopamine receptor antagonists
Classic anticholinergic effects
M1 receptor antagonist
Scopolamine
Weak antiemetic transdermal patch for motion sickness
Scopolamine
Cannabinoid receptor Agonists
- Dronabinol
- Nabilone
Strength of Cannabinoid receptor agonists
Strong Antiemetic agents
Use for cannabinoids
commonly reserved for TREATMENT RESISTANT clinical scenarios
Cannabinoids can be used for appetite stimulation in what patients
-Anorexic patients due to severe disease (Cancer or AIDS)
Drug interactions for Cannabinoids
- CNS depressants
- Cardiovascular and sympathomimetics
