Agents for Nausea & Vomiting Flashcards
Name a major chemosensory area for emesis.
Chemoreceptor Trigger Zone (CTZ)
Where is the CTZ found?
Area postrema of the fourth ventricle of the brain
Name drug classes with examples of specific drugs that are effective in the treatment of nausea & vomiting.
- Antihistamine-anticholinergics
- Benzodiazepines
- Butyrophenones
- Cannabinoids
- Corticosteroids
- Phenothiazines
- Substituted Benzamides-Metoclopramide
- 5-HT3 receptor blockers
- Neurokinin receptor blockers
How does metoclopramide work as an antiemetic?
Blocks D2 receptors centrally in the CTZ
- Prokinetic
- Increases resting tone, contactility, LES tone, & motility
Does NOT influence colon transport time
What are the DOC for treating emesis during pregnancy?
(Antihistamine-Anticholinergics Meclizine Cyclizine Promethazine
What antihistamine is often used to treat motion sickness?
Meclizine
What anticholinergic is often used to treat motion sickness? How is it normally administered?
Scopolamine Transdermal patch to prevent systemic anticholinergic effects
What medication is often used in combo regimens to enhance antiemetic activity?
Dexamethasone
What are the s/e of phenothiazine antiemetics?
Extrapyramidal symptoms Sedation Hypotension
Why doesn’t ondansetron cause extrapyramidal s/e?
Blocks 5-HT3 instead of dopamine receptors in the CTZ
What chemotherapy agent has one of the highest emetogenic potentials?
Cisplatin
What antibiotic has prokinetic properties for the GI tract?
Erythromycin, though tolerance to this effect develops rapidly, it’s usefulness is limited by its nausea & vomitting s/e
Give examples of Antihistamine-Anticholinergics used to treat nausea & vomiting
- Diphenhydramine
- Hydoxyzine
- Meclizine
- Cyclizine
- Promethazine
- Pyrilamine
- Scopolamine
- Trimethobenzamide
Give examples of Benzodiazepines used in the treatment of nausea & vomiting
- Alprozolam
- Diazepam
- Lorazepam
Give examples of Butyrophenones used in the treatment of nausea & vomiting
- Haloperidol
- Droperidol
- Domperidone
Give examples of cannabinoids used for the treatment of nausea & vomiting
- Dronabinol
- Nabilone
What are the corticosteroids used to treat nausea & vomiting?
- Dexamethasone
- Methylprednisolone
What phenothiazines are used to treat nausea & vomiting?
- Prochlorperazine
- Chlorpromazine
- Perphenazine
What substituted Benzamides are used for the treatment of nausea & vomiting?
- Metoclopramide
What 5-HT3 Receptor Blockers are POWERFUL CENTRAL-ACTING antiemetics?
What are some of their clinical uses?
”-setron”
-
Ondansetron
- At a party but feeling queasy? Keep ON DANCing with ONDANSetron!
- Dolasetron
- Granisetron
Clinical Use:
- Control N&V postoperatively
- pts undergoing chemotherapy
What Neurokinin Receptor Blockers are used for the treament of nausea & vomiting?
- Aprepitant (oral)
- Fosaprepitant (IV formulation converted to aprepitant)
Do synthetic cannabinoids have psychotropic activity?
No
What is intractable emesis leading to dehydration & hypotension during pregnancy called?
Hyperemesis Gravidarum
What are the s/e of cannabinoids?
- Anxiety
- Memory Loss
- Confusion
- Motor incoordination
- Hallucinations
- Euphoria
- Relaxation
- Hunger
- Gynecomastia
