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Emetics

Antiemetics and emetics are drugs that either reduce nausea and vomiting or induce vomiting, respectively. Nausea and vomiting can be triggered by various factors, including gastrointestinal issues, emotional stress, and certain medications, with antiemetics being crucial in managing these symptoms. Different classes of antiemetics, such as anticholinergics, antihistamines, and serotonin antagonists, have specific mechanisms and indications for use, including chemotherapy-induced nausea and vomiting.
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0% found this document useful (0 votes)
7 views8 pages

Emetics

Antiemetics and emetics are drugs that either reduce nausea and vomiting or induce vomiting, respectively. Nausea and vomiting can be triggered by various factors, including gastrointestinal issues, emotional stress, and certain medications, with antiemetics being crucial in managing these symptoms. Different classes of antiemetics, such as anticholinergics, antihistamines, and serotonin antagonists, have specific mechanisms and indications for use, including chemotherapy-induced nausea and vomiting.
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ANTIEMETICS AND 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.

Pathophysiology of nausea and vomiting


Vomiting is a defense mechanism used by the body to rid itself of toxic
substances. Vomiting is a reflex primarily controlled by the vomiting
center of the medulla of the brainstem, which receives sensory signals
from the digestive tract, the inner ear, and the chemoreceptor trigger
zone (CTZ) in the cerebral cortex. Interestingly, the CTZ is not protected
by the blood-brain barrier, as is most of the brain; thus, these neurons
can directly sense the presence of toxic substances in the blood. Once
the vomiting reflex is triggered, wavelike contractions of the stomach
quickly propel its contents upward and out of the body.

Nausea and vomiting are common symptoms associated with a wide


variety of conditions such as
●​ GI infections,
●​ food poisoning
●​ Nervousness (emotional imbalances
●​ Motion sickness
●​ Extreme pain
●​ General anesthetics
●​ Migraine headaches
●​ Trauma to the head or abdominal organs
●​ Inner ear disorders
●​ Diabetes.

Psychological factors play a significant role, as patients often become


nauseated during periods of extreme stress or when confronted with
unpleasant sights, smells, or sounds.

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.

Ipecac syrup is used to induce vomiting in the early management of oral


poisoning or drug overdose. Ipecac syrup induces vomiting by
stimulating the vomiting center located in the brain’s medulla. Currently
the use of ipeca syrup has been replaced with activated charcoal.

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.

Adverse effects: Delirium, Hallucinations, Hypotension, Tachycardia etc.


Contraindications: myasthenia gravis, obstructive uropathy, paralytic
ileus, severe ulcerative colitis ,etc

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.

Contraindications: Children aged <2 years,


Use with caution in asthma, hepatic impairment, peptic ulcer disease.

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.

Adverse effects: Drowsiness, Tachycardia, Pruritus. They also cause


acute dystonia (especially in children), and tardive dyskinesias or
parkinsonism when used for prolonged periods.

Contraindications: Postoperative management of nausea/vomiting


following pediatric surgery, children <2 years, severe cardiovascular
disease( use with caution)

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.

4)​ Selective 5HT3-receptor antagonists


Serotonin ,or 5-hydroxytryptamine (5HT) ,plays an important role in
nausea and vomiting. Some available agents include granisetron,
dolasetron, ondansetron ,and palonosetron. They are all more expensive
than antihistamines, phenothiazines, anticholinergics ,or dopamine
antagonists. The serotonin 5-HT3 receptor antagonists block serotonin
stimulation centrally in the chemoreceptor trigger zone and peripherally
in the vagal nerve terminals, both of which stimulate vomiting. Selective
5HT3-receptor antagonists that act centrally and peripherally are now
commonly used to treat or prevent CINV (with drugs of moderate to high
emetogenic potential) and PONV. They are also effective in
radiotherapy-induced nausea and vomiting.

Adverse effects: constipation, headache, diarrhea, and dizziness.

Contraindications/caution: Reduce dose with severe hepatic impairment.

5)​ Prokinetic agents


Metoclopramide
At lower doses, metoclopramide acts as a selective dopamine receptor
antagonist at the CTZ. However, it also exerts peripheral dopamine
antagonism at these doses, and stimulates cholinergic receptors in
gastric smooth muscle, thus stimulating gastric emptying. It may,
therefore, be more effective than phenothiazines and butyrophenones
when nausea is related to gastrointestinal or biliary disease.
At higher doses, it may exert some 5HT3-receptor antagonism but at
these doses, the incidence of acute dystonic reactions, particularly in
young women and the elderly, may limit its usefulness in CINV.

Adverse effects: Dizziness, Sedation, Fatigue, Extrapyramidal


symptoms.
Contraindications: History of tardive dyskinesia (TD), Patients with
history of epilepsy, pheochromocytoma (A neuroendocrine tumour of the
medulla of the adrenal glands).

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.

7)​ Neurokinin-1 (NK1) receptor antagonists


Substance P is a bioactive peptide that shares a common amino acid
sequence with other bioactive peptides known as
tachykinins.
Selective NK1 receptor antagonists, aprepitant and fosaprepitant (a
prodrug of aprepitant),are now available for use as an adjunct to
dexamethasone and a 5HT3 antagonist in preventing, but not treating
nausea and vomiting associated with moderately and highly emetogenic
chemotherapy.

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.

9)​ Complementary and alternative medicines


A systematic review of randomized trials has also demonstrated the
efficacy of ginger (at least 1 g preoperatively) in PONV. Ginger has also
been claimed to be beneficial in motion sickness and
pregnancy-associated nausea, but the
evidence for each is limited to single randomized trials (Ernst and Pittler,
2000).

Systematic reviews support the use of stimulating wrist acupuncture


point P6 for preventing PONV in combination with or as an alternative to,
conventional antiemetics. Pressure point P-6 is also called Neiguan
(nay-gwann). It is found on your inner arm near your wrist. Doing
acupressure on this point can help with nausea and prevent vomiting.

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.

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