A Review of the History and Pharmacology of Anti- Nausea Medications
Alex Rosen1, Noah Rosen2
1Schreiber High School, 2Neurology, Zucker SOM at Northwell Health
Objective:
To review the history of medications used for nausea, describe their origins, pharmacology and current usage.
Background:
The earliest anti nausea medications came from plant extracts including muscarinic receptor antagonists and opium.  Throughout the 20th century, a range of different therapeutic classes developed, both by derivation from native treatments as well as through focused drug discovery.  This has led to at least 6 clear major classes of medications used for anti-emetic effect.
Design/Methods:
A comprehensive review of literature in both PubMed and Google Scholar was conducted.  Relevant primary source and secondary review articles were reviewed for relevance and consistency and summary details obtained for each drug class.
Results:

Most current anti-nausea medications fall into 6 different pharmacologic classes:

1.  Muscarinic receptor antagonists including atropine and hyoscine derived from nightshades and may affect the area post rami directly

2.  Histamine Receptor Antagonists such as dimenhydrinate and diphenhydramine tested on US Troops in 1948 and which often contain stimulating medication to offset sedating effect.

3.  Dopamine Receptor Antagonists including Phenothiazines such as Promethazine in 1947 and chlorpromazine in 1950.  

4.  Benzodiazepines such as lorazepam which does not directly affect the area post rami but enhances GABA which reduces anxiety, produce sedative effect with potential for anterograde amnesia.

5.  Selective 5-hydroxytryptamine, (5HT3) receptor antagonists such as metoclopramide originally developed to offset emetic effect from cisplatin at those receptors and leading to selective agents such as granisetron.

6.  Neurokinin Receptor Antagonists which offset the effect of substance P but have been found to reduce chemotherapy induced emesis.

 

Conclusions:
The 20th century had seen great advances in the management of nausea.  Prior to World War 2, options were limited to natural plant derivatives and untested remedies.  By the end of the century, 6 distinct classes existed with a range of different pharmacologic targets. 
10.1212/WNL.0000000000217539
Disclaimer: Abstracts were not reviewed by Neurology® and do not reflect the views of Neurology® editors or staff.