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Summary of this article: commonly used clinical antiemetic drugs and precautions for their use

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Author: Gao Lili

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Nausea and vomiting are common clinical symptoms, and according to the pathogenesis, vomiting can be divided into reflex vomiting, central vomiting, and vestibular disorder vomiting
.
Antiemetic drugs are a class of drugs that play an antiemetic effect by affecting different links of the gag reflex, including 5-HT3 receptor antagonists, gastrointestinal motility drugs, antacids, NK-1 receptor antagonists, glucocorticoids, and anticholinergics
.

5-HT3 receptor antagonist 5-HT3 receptor antagonist plays a role by antagonizing 5-HT3 receptor related to nausea and vomiting, and can be used clinically for nausea and vomiting (CINV) caused by radiotherapy and chemotherapy, nausea and vomiting (PONV) after surgery, nausea and vomiting caused by opioids, nausea and vomiting caused by gastrointestinal dysfunction, etc
.
Such drugs include ondansetron, granisetron, azasetron, dolasetron, tropisetron, ramosetron, palonosetron, etc.
, of which palonosetron has the longest half-life of 40 hours
.

Notes

1.
Ondansetron

Common adverse reactions of ondansetron are headache, head and epigastric fever, akathisia, diarrhea, rash, acute dystonic reactions, constipation, etc.
, which can occasionally cause transient aminotransferase elevation
.

Bronchospasm, tachycardia, chest pain, hypokalemia, ECG changes, and large seizures are rare
.
Contraindicated in patients with
gastrointestinal obstruction.

2.
Grasetron

Adverse reactions of granisetron include headache, rarely constipation, drowsiness, diarrhea, which can temporarily increase AST/ALT and change blood pressure
.

Because it can slow down the movement of the digestive tract, patients with digestive tract dyskinesia are closely observed when using it; If granisetron is combined with rifampicin or other liver enzyme inducers, it will cause a decrease
in the plasma concentration of granisetron.

3.
Azasetron

Common adverse reactions of azasetron include rash, general itching, fever, fatigue, leg spasm, facial flushing, vascular pain, and sometimes headache, heavy head, anxiety, irritability, pallor, cold or palpitations, and may appear thirst, elevated ALT/AST/total bilirubin
.

It is easy to decompose when exposed to light, and should be used quickly and protected from light
after opening.

4.
Tropasetron

Common adverse reactions of tosetron include headache, constipation, dizziness, fatigue and gastrointestinal disorders, and occasionally rash, itching, urticaria, etc
.

Transient elevation of aminotransferases has been reported; May have an effect on blood pressure, and the daily dose of uncontrolled hypertension does not exceed 10 mg; Patients with liver and kidney dysfunction should be used with caution; In combination with rifampicin or other liver enzyme inducers, the metabolism of toxietron can be accelerated and the blood concentration can be reduced
.

5.
Remosetron

The adverse reactions of ramosetron are mainly body heat, headache, heavy head, etc.
, and can also cause diarrhea, constipation, head fever, tongue numbness, hiccups, increased blood creatinine, abnormal liver function, etc.
; It can have a compatibility reaction with mannitol injection, bumetanide injection, furosemide injection, etc.
, and should be avoided
.
In addition, patients with congenital long QT syndrome, underlying heart diseases such as congestive heart failure and bradycardia and electrolyte abnormalities (eg, hypokalemia, hypomagnesemia) are at higher risk of arrhythmias, and 5-HT3 receptor antagonists
should be used with caution when other drugs that may prolong the QT interval (eg, olanzapine, haloperidol) have been or may develop into the cardiac conduction interval, especially when the QT interval is prolonged.
The main class of gastrointestinal motility drugs are dopamine D2 receptor antagonists (metoclopramide, domperidone, itopride ride), 5-HT4 receptor agonists (cisapride ride, mosapride, cinipride and prucapride ), which can be used clinically for nausea and vomiting (CINV), postoperative nausea and vomiting (PONV), gastrointestinal dysfunction nausea and vomiting, etc
.

Notes

1.
Metoclopramide

Metoclopramide easily penetrates the blood-brain barrier and can block central dopamine receptors and cause extrapyramidal reactions, and elderly patients should pay more attention
.

After blocking the pituitary dopamine receptor, it can cause hyperprolactinemia, causing breast tenderness, lactation and menstrual irregularities; Injection administration may cause orthostatic hypotension and interact more
with other drugs.

2.
Domperidone

Domperidone is not easy to penetrate the blood-brain barrier, almost no antagonism to dopamine D2 receptors in the brain, but can still be in some central parts lacking blood-brain barrier protection such as CTZ (blockade of its receptors can produce antiemetic effect), anterior pituitary (release of prolactin) effect, the effect of the latter can cause excessive secretion of prolactin, resulting in hyperprolactinemia, elderly men long-term use can appear breast tenderness or milk leakage phenomenon
.

Domperidone has a serious effect on the heart, can cause Q-T interval prolongation and arrhythmia, and has been reported
to cause sudden cardiac death.

Because it rarely penetrates the blood-brain barrier, extrapyramidal adverse effects are rare, but can still be seen in infants and Alzheimer's patients with imperfect blood-brain barrier development
.
Drugs that significantly inhibit CYP3A4 enzyme and may cause Q-T interval prolongation such as ketoconazole, fluconazole, voriconazole, erythromycin, clarithromycin, amiodarone, combined with domperidone, increase the risk of torsades de pointes, and their combination is contraindicated; It is combined with lithium and diazepam to cause extrapyramidal symptoms
.

3.
Cisapride

Cisapride may cause prolongation of the Q-T interval, fainting, and severe arrhythmias, which can cause convulsive epilepsy, extrapyramidal reactions, and urinary frequency
.
In combination with CYP3A4 enzyme inhibitors such as triazole antifungal drugs such as itraconazole, fluconazole, macrolides such as erythromycin, clarithromycin, HIV protease inhibitors and nafazolidone, it can cause cisapride concentration to increase, increase the risk of arrhythmias in the Q-T interval, such as ventricular tachycardia, ventricular fibrillation and torsades de pointes, and try to avoid taking the same dose
.
Avoid taking drugs that cause Q-T interval prolongation, such as antiarrhythmic drugs (quinidine, disopyramide, procainamide, amiodarone, sotalol, etc.
), tricyclic/tetracyclic antidepressants (such as amitriptyline, maprotiline), antipsychotics, antihistamines, etc
.

4.
Mosapride

If mosapride is combined with anticholinergic drugs such as atropine, scopolamine, etc.
, its effect will be weakened; In addition, mosapride may have an effect on the Q-T interval of the heart, and avoid combination with
drugs that can prolong the Q-T interval, such as flecainide, amiodarone, etc.
Antacids include proton pump inhibitors (PPIs) and H2 receptor antagonists, and can be used clinically in patients with chemotherapy-induced nausea and vomiting (CINV) and gastric disorders
.

Precautions The adverse reactions of PPI are nausea, gastrointestinal flatulence, diarrhea, abdominal pain, constipation, headache, dizziness, etc.
, and occasionally anaphylactic shock, pancytopenia, vasculitis, lupus erythematosus, interstitial nephritis, bronchial asthma, skeletal muscle pain and even rhabdomyolysis and other serious adverse reactions
.
H2 receptor antagonist adverse reactions include dizziness, drowsiness, disorientation, male breast swelling and feminization, female lactation, etc.
, long-term medication can cause gastric bacteria to multiply, induce infection
.
NK-1 receptor antagonists NK-1 receptor antagonists
(including aprepitant, fosapitant, netupitant, rolapitant) through highly selective binding to NK-1 (P substance neurokinin 1) receptors in the brain, antagonistic P substance and antiemetic, clinically can be used for chemotherapy-induced nausea and vomiting, postoperative nausea and vomiting, opioid-induced nausea and vomiting
.
In addition, the combination netupitant/palonosetron has the dual effects of NK-1 receptor antagonist and 5-HT3 receptor antagonist, and can be used for chemotherapy-induced nausea and vomiting
.

Precautions Adverse reactions of aprepitant include indigestion, belching, loss of appetite, diarrhea, abdominal pain, constipation, fatigue, weakness, mild headache, dizziness, weakness, hypotension, bone marrow suppression, cough, dehydration, etc.
, severe Stevens-Johnson syndrome
.
Aprepitant is a substrate of CYP3A4 and has a mild to moderate inhibitory effect (dose-dependent) on CYP3A4 and may be a delayed inducer of the CYP3A4 isoenzyme and an inducer
of CYP2C9.
It is contraindicated to be used
in combination with pimozide, terfenadine, asimizole, cisapride .

Aprepitant is combined with ifosfamide, and ifosfamide-induced neurotoxicity has been reported
.
The glucocorticoid dexamethasone, prednisone and methylprednisolone are representative drugs of glucocorticoids, which can be used clinically for chemotherapy-induced nausea and vomiting (CINV), postoperative nausea and vomiting (PONV), and opioid-induced nausea and vomiting
.

Precautions The adverse reactions of glucocorticoids are obviously related to the type, dose, course of treatment, dosage form and usage of drugs, and the adverse reactions that can lead to include metabolic disorders, inducing and aggravating infections, abnormal blood pressure, bleeding tendency, weight gain, osteoporosis, spontaneous fractures, osteonecrosis of the femoral head, etc.
, can not be stopped suddenly, arbitrarily increase or decrease the dose or change the number of medications
。

It is contraindicated in patients with active ulcers, duodenal ulcers, recent gastrointestinal anastomosis, severe psychiatric history, severe osteoporosis, and virus, bacterial, and fungal infections that cannot be controlled by antimicrobial therapy
.

With caution for gastric ulcer, gastritis or esophagitis, hypertension, congestive heart failure, myasthenia gravis, diabetes, hypothyroidism, osteoporosis, hyperlipoproteinemia, epilepsy, emotional instability and psychotic tendency, liver function damage, renal function damage or stones
.

➤ In combination with digitalis drugs, it may increase the risk of arrhythmias caused by hypokalemia;

➤When combined with potassium-excreting drugs such as amphotericin B and diuretics, it can cause excessive potassium loss, and there are reports of heart enlargement and congestive heart failure;

➤Oral contraceptives, ritonavir can increase the blood concentration of glucocorticoids;

➤ When combined with nonsteroidal anti-inflammatory drugs (NSAIDs), the incidence of gastrointestinal bleeding and ulceration increases;
➤ Glucocorticoids may raise blood sugar and weaken the effect of hypoglycemic drugs;

➤ Recent use of barbiturates, carbamazepine, phenytoin, primidone, rifampicin may reduce the effect of systemic glucocorticoids;

➤ In combination with protein anabolic androgenic steroids, it can increase the incidence of edema and aggravate acne;

➤ In combination with immunosuppressants, it can increase the risk of infection and may induce lymphoma or other lymphoproliferative diseases;

➤Long-term combination with anticholinergic drugs such as atropine can cause increased intraocular pressure;

➤ In combination with anticholinesterase drugs, it can cause myasthenia gravis and severe weakness, if possible, stop anticholinesterase drugs
at least 24 hours before the start of glucocorticoid therapy.
Anticholinergic drugs such drugs include diphenhydramine, hydroxyzine, doxylamine, scopolamine, diphenidol, etc.
, which can be used clinically for motion sickness vomiting, postoperative nausea and vomiting (PONV), and nausea and vomiting caused by opioids
.

Precautions Peripheral anticholinergic effects can cause dry mouth, dry eyes, viscous respiratory secretions, constipation, arrhythmias, increased intraocular pressure, blurred vision, mydriasis, erectile dysfunction, urinary retention and dysuria, etc.
It can also affect the conduction of neurons or neuro-muscle junctions, resulting in transient disturbances of nerve function and lack of concentration
.
Patients with angle-closure glaucoma, urinary retention, prostatic hyperplasia, prostatic hypertrophy, and pyloroduodenal obstruction should be used
with caution.
Antihistamines can cause central inhibition, such as sedation, lethargy, drowsiness, fatigue, hallucinations, decreased alertness, irritability, nervousness, anxiety, insomnia, headache, dizziness, lack of coordination and tremors, etc.
, and can reduce rapid eye movement sleep, which may lead to decreased learning ability, especially first-generation antihistamines
.
Avoid using drugs that have inhibitory effects on the center such as sedative hypnotic drugs such as diazepam, antipsychotic drugs such as chlorpromazine, barbiturates, opioids, anti-epileptic drugs, etc.
, otherwise it will cause dizziness, malaise, movement disorders, blurred vision, diplopia and other central nervous system excessive inhibitory symptoms, especially children, the elderly, and the weak.

Aerial workers, drivers, and machine operators are prohibited or used
with caution.

It should also be noted that first-generation antihistamines have anticholinergic effects that delay gastric emptying
.

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