Emetics
Emetics
Antiemetics and emetics are two groups of drugs with opposing actions.
Antiemetic drugs decrease nausea, reducing the urge to vomit. Emetic
drugs triggers vomiting.
Nausea and vomiting are also the most frequently listed adverse effects
of oral medications. Nurses should remember that because the vomiting
center lies in the brain, nausea and vomiting may occur with parenteral
formulations as well as with oral drugs. The most extreme example of
this occurs with antineoplastic drugs, most of which cause intense
nausea and vomiting regardless of the route they are administered. The
capacity of a chemotherapeutic drug to cause vomiting is called its
emetogenic potential. Nausea and vomiting are a common reason for
patients’ lack of adherence to the therapeutic regimen and
discontinuation of drug therapy.
Emetics
Emetics are used to induce vomiting in a person who has ingested toxic
substances. Examples include: Ipecac syrup (orally), apomorphine
(subcutaneously), levodopa (orally) etc.
Antiemetics
1) Anticholinergics:
This is one of the oldest classes of antiemetics, of which many members
are potent inhibitors of muscarinic receptor (M1) activity both peripherally
and centrally. Anticholinergic drugs such as atropine, scopolamine and
glycopyrrolate have been used preoperatively to inhibit salivation and
excessive respiratory secretions during anesthesia. Anticholinergics act
by inhibiting cholinergic transmission from the vestibular nuclei to higher
centers within the cerebral cortex, thereby explaining their predominant
use in the treatment of motion sickness.
Drug interactions:
● Coadministration of anticholinergic drugs and glucagon increases
risk of gastrointestinal adverse reactions due to additive effects on
inhibition of gastrointestinal motility.
● Anticholinergics decrease levels of promethazine by inhibition of
GI absorption.
● Anticholinergics decrease levels of haloperidol by inhibition of GI
absorption. Applies only to the oral form of both agents.
2) Antihistamines
They are specifically used for nausea and vomiting caused by inner ear
stimulation. As a consequence, these drugs prevent or treat motion
sickness. They usually prove most effective when given before activities
that produce motion sickness and are much less effective when nausea
or vomiting has already begun. Antihistamines, including buclizine,
cyclizine, dimenhydrinate,
diphenhydramine, promethazine, meclizine.
Adverse effects:
Sedation, Dry mouth, Urinary retention, Hallucinations etc.
Drug interactions:
● Antihistamines can cause CNS depression and sedation when
taken with CNS depressants, such as barbiturates, tranquilizers,
antidepressants, alcohol, and opioids.
● Atropine decreases levels of promethazine by inhibition of GI
absorption.
3) Antidopaminergics
The major indication for phenothiazines relates to treating psychoses,
but they are also very effective antiemetics.
Phenothiazines and butyrophenones are the two classes here.
Phenothiazines (e.g. prochlorperazine, perphenazine, and
trifluoperazine) and butyrophenones (e.g. haloperidol and droperidol) act
as antagonists at dopamine (D2) receptors in the CTZ,
They produce their antiemetic effect by blocking the dopaminergic
receptors in the chemoreceptor trigger zone in the
brain. Phenothiazines are sometimes used for drug-associated emesis,
including chemotherapy-induced nausea and vomiting (CINV).
Butyrophenones that have high antiemetic activity include haloperidol
(Haldol) and droperidol (Inapsine). Prochlorperazine is less sedating and
available as a buccal tablet and suppository for use when vomiting
precludes oral administration.
Domperidone
Although domperidone does not readily cross the BBB, it is a selective
antagonist of D2 receptors at the CTZ, which lies outside the BBB in the
area postrema. It is used in drug-associated vomiting, including CINV,
and is relatively non-sedating.
Drug interactions:
● Anticholinergic/sedative combos decrease levels of
prochlorperazine.
● Artemether/lumefantrine will increase the level or effect of
prochlorperazine by affecting hepatic enzyme CYP2D6
metabolism.
● Antidopaminergics decrease the effects of methyldopa.
Drug interactions:
● Metoclopramide decreases levels of apomorphine
● Metoclopramide increases levels of cyclosporine by enhancing GI
absorption.
6) Corticosteroids
Corticosteroids are known to have antiemetic effects. Their mechanism
of action is unclear but steroid receptors are thought to exist in the area
postrema. Glucocorticoids may act via the following mechanisms:
● Anti-inflammatory effect.
● Interaction with the neurotransmitter serotonin, and receptor
proteins tachykinin NK1 and NK2, alpha-adrenaline, etc.
Dexamethasone (Decadron) and methylprednisolone (Solu-Medrol) are
used to prevent chemotherapy-induced and postsurgical nausea and
vomiting. They are reserved for the short-term therapy of acute cases
because of the potential for serious long-term adverse effects.
8) Cannabinoids
The antiemetic activity of cannabinoids is likely related to stimulation of
central and peripheral cannabinoid (CB1) receptors.
MOA: Cannabinoid CB1 receptors are found in several areas of the CNS
and the action of nabilone at these receptors may inhibit neuronal
serotonin release in the dorsal vagal nucleus which triggers the CTZ.
Tronabinol (Marinol) and nabilone (Cesamet) are given orally to produce
antiemetic effects and relaxation without the euphoria produced by
marijuana. Nabilone is indicated for nausea and vomiting caused by
cytotoxic chemotherapy unresponsive to conventional antiemetics.
NOTE:
Pregnancy-associated nausea and/or vomiting occurs in about 70% of
women during the first trimester. Risk factors for vomiting include
● a personal history of previous pregnancy-associated
nausea/vomiting or
● motion sickness or
● migraine-associated nausea/vomiting,
In first-trimester nausea and vomiting, simple measures such as small
frequent carbohydrate-rich meals and reassurance are sufficient to
control symptoms. Ginger and P6 acupressure have also been
advocated, although the evidence base is equivocal in early pregnancy
(Jewell and Young, 2003). It is important to avoid antiemetic drugs when
possible, but promethazine has been recommended in severe vomiting,
with prochlorperazine or metoclopramide as second-line agents. A
combination of pyridoxine (vitamin B6) and an antihistamine
(doxylamine) is approved for the treatment of nausea in pregnancy but
this combination treatment appears to be less effective for controlling
vomiting.