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    Home > Active Ingredient News > Digestive System Information > Clinical essentials: six types of commonly used antiemetic drugs and precautions for their use

    Clinical essentials: six types of commonly used antiemetic drugs and precautions for their use

    • Last Update: 2022-04-29
    • Source: Internet
    • Author: User
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    Author: Gao Lili This article is published by the author authorized by the author, please do not reprint without authorization
    .

    Nausea and vomiting are common clinical symptoms.
    According to different pathogenesis, vomiting can be divided into reflex vomiting, central vomiting and vestibular disorder vomiting
    .

    Antiemetic drugs are a class of drugs that exert antiemetic effects by affecting different aspects of the gag reflex, including 5-HT3 receptor antagonists, gastrointestinal motility drugs, acid suppressants, NK-1 receptor antagonists, glucocorticoids , Anticholinergic drugs
    .

    5-HT3 receptor antagonists 5-HT3 receptor antagonists work by antagonizing 5-HT3 receptors related to nausea and vomiting, and can be clinically used for chemotherapy-induced nausea and vomiting (CINV), postoperative nausea and vomiting (PONV) , opioid-induced nausea and vomiting, gastrointestinal dysfunction, nausea and vomiting,
    etc.

     Such drugs include ondansetron, granisetron, azasetron, dolasetron, tropisetron, ramosetron, palonosetron, etc.
    Among them, palonosetron has the longest half-life, for 40h
    .

     Matters needing attention 1.
    The common adverse reactions of ondansetron are headache, fever in the head and upper abdomen, akathisia, diarrhea, rash, acute dystonic reaction, constipation, etc.
    high
    .

    Bronchospasm, tachycardia, chest pain, hypokalemia, ECG changes, grand mal seizures are rare
    .

     Contraindicated in patients with gastrointestinal obstruction
    .

     2.
    Granisetron The adverse reactions of granisetron include headache, rare constipation, lethargy and diarrhea, which can temporarily increase AST/ALT and change blood pressure
    .

    Because it can slow down the movement of the digestive tract, patients with dyskinesia should be closely observed; if granisetron is combined with rifampicin or other liver enzyme inducers, the plasma concentration of granisetron will decrease
    .

     3.
    Azasetron The common adverse reactions of Azasetron include rash, body itching, fever, fatigue, leg cramps, facial flushing, vascular pain, sometimes headache, heavy head, anxiety, irritability, pale face, Cold or palpitations, thirst, ALT/AST/total bilirubin elevation may occur
    .

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

     4.
    Tropisetron Tropisetron Common adverse reactions include headache, constipation, dizziness, fatigue and gastrointestinal dysfunction, and occasionally rash, itching, urticaria,
    etc.

    There are reports of transient elevation of aminotransferase; it may have an effect on blood pressure, and the daily dose for uncontrolled hypertension should not exceed 10 mg; use with caution in patients with liver and renal insufficiency; in combination with rifampicin or other liver enzyme inducers, It can accelerate the metabolism of tropisetron and reduce the blood concentration
    .

     5.
    Ramosetron The adverse reactions of ramosetron are mainly body heat, headache, heavy head, etc.
    , and can also cause diarrhea, constipation, head fever, numbness of the tongue, hiccups, increased serum creatinine, abnormal liver function, etc.
    ; and Mannitol injection, bumetanide injection, furosemide injection, etc.
    may cause incompatibility reactions, and mixed use should be avoided
    .

     In addition, patients with congenital long QT syndrome, underlying cardiac diseases such as congestive heart failure and bradycardia and electrolyte abnormalities (eg, hypokalemia, hypomagnesemia) are at higher risk for arrhythmias, and other possible When drugs that prolong the QT interval (such as olanzapine, haloperidol) have or may develop cardiac conduction interval, especially when the QT interval is prolonged, 5-HT3 receptor antagonists should be used with caution
    .

    Gastrointestinal motility drugs are mainly dopamine D2 receptor antagonists (metoclopramide, domperidone, itopride), 5-HT4 receptor agonists (cisapride, mosapride, ciclopride) Pride and prucalopride), which can be used clinically for chemotherapy-induced nausea and vomiting (CINV), postoperative nausea and vomiting (PONV), and gastrointestinal dysfunction, such as nausea and vomiting
    .

     Matters needing attention 1.
    Metoclopramide Metoclopramide easily penetrates the blood-brain barrier and can block central dopamine receptors and cause extrapyramidal reactions.
    Elderly patients should pay more attention
    .

    After blocking the pituitary dopamine receptors, it can cause hyperprolactinemia, causing breast tenderness, lactation and irregular menstruation, etc.
    ; injection may cause orthostatic hypotension, and there are many interactions with other drugs
    .

     2.
    Domperidone Domperidone is not easy to pass through the blood-brain barrier, and has almost no antagonistic effect on dopamine D2 receptors in the brain, but it can still be used in some central sites that lack the protection of the blood-brain barrier, such as CTZ (blocking of its receptors can produce antiemetics.
    effect), the anterior pituitary gland (releasing prolactin) has an effect, and the effect of the latter can cause excessive secretion of prolactin, resulting in hyperlactinaemia, and long-term use of elderly men may cause breast tenderness or galactorrhea
    .

    Domperidone has serious effects on the heart, can cause QT interval prolongation and arrhythmia, and has been reported to cause sudden cardiac death
    .

    Because it rarely crosses the blood-brain barrier, extrapyramidal adverse reactions are rare, but can still be seen in infants and Alzheimer's patients with underdeveloped blood-brain barrier
    .

     Drugs that significantly inhibit the enzyme CYP3A4 and may cause QT prolongation, such as ketoconazole, fluconazole, voriconazole, erythromycin, clarithromycin, and amiodarone, when combined with domperidone, will increase the incidence of torsades de pointes It is contraindicated in combination with lithium and diazepam, which can cause extrapyramidal symptoms
    .

     3.
    Cisapride Cisapride may cause QT interval prolongation, fainting and severe arrhythmia, convulsive epilepsy, extrapyramidal reactions and frequent urination
    .

     Combination with CYP3A4 enzyme inhibitors such as triazole antifungal drugs such as itraconazole, fluconazole, macrolides such as erythromycin, clarithromycin, HIV protease inhibitors and nefazodone can cause The increased concentration of cisapride increases the risk of arrhythmias in the QT interval, such as ventricular tachycardia, ventricular fibrillation and torsades de pointes, so try to avoid taking it together
    .

     Avoid taking drugs that cause QT interval prolongation, such as antiarrhythmic drugs (quinidine, disopyramide, procainamide, amiodarone, sotalol, etc.
    ), tricyclic/tetracyclic antidepressants Drugs (such as amitriptyline, maprotiline), antipsychotics, antihistamines,
    etc.

     4.
    Mosapride If mosapride is used in combination with anticholinergic drugs such as atropine, scopolamine, etc.
    , its effect will be weakened; in addition, mosapride may have an impact on the cardiac QT interval, so avoid and prolong the QT interval.
    Combination of drugs such as flecainide and amiodarone
    .

     Acid suppressants, including proton pump inhibitors (PPIs) and H2 receptor antagonists, can be used clinically for chemotherapy-induced nausea and vomiting (CINV) and in patients with gastric diseases
    .

     Matters needing attention The adverse reactions of PPI are nausea, flatulence, diarrhea, abdominal pain, constipation, headache, dizziness, etc.
    , occasionally anaphylactic shock, pancytopenia, vasculitis, lupus erythematosus, interstitial nephritis, bronchial asthma, Serious adverse reactions such as musculoskeletal pain and even rhabdomyolysis
    .

     Adverse reactions of H2 receptor antagonists include dizziness, drowsiness, disorientation, male breast swelling and feminization, female lactation, etc.
    Long-term use can cause bacterial growth in the stomach and induce infection
    .

     NK-1 receptor antagonists NK-1 receptor antagonists (including aprepitant, fosaprepitant, netupitant, lorapitant) interact with NK-1 (substance P neurokinin 1) in the brain.
    ) The highly selective binding of receptors, antagonizing substance P and antiemetic, can be used for nausea and vomiting caused by chemotherapy, nausea and vomiting after surgery, nausea and vomiting caused by opioids,
    etc.

     In addition, the compound netupitant/palonosetron has the dual effects of NK-1 receptor antagonist and 5-HT3 receptor antagonist, and can be used for nausea and vomiting caused by chemotherapy
    .

    Matters needing attention The 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 mild to moderate inhibitory effects on CYP3A4 (dose-dependently), and may be a delayed inducer of CYP3A4 isoenzymes, as well as an inducer of CYP2C9
    .

     It is forbidden to use in combination with pimozide, terfenadine, asimidazole, and cisapride
    .

    Ifosfamide-induced neurotoxicity has been reported when aprepitant is co-administered with ifosfamide
    .

    Glucocorticoids dexamethasone, prednisone, methylprednisolone are the representative drugs of glucocorticoids, which can be used clinically for chemotherapy-induced nausea and vomiting (CINV), postoperative nausea and vomiting (PONV), opioid-induced nausea and vomiting, etc.

    .

    Matters needing attention The adverse reactions of glucocorticoids are obviously related to the type, dose, course of treatment, dosage form and usage of the drug.
    The adverse reactions that can be caused include metabolic disorders, induced and aggravated infections, abnormal blood pressure, bleeding tendency, weight gain, osteoporosis, Spontaneous fractures, necrosis of the femoral head, etc.
    , cannot be stopped suddenly, the dose can be increased or decreased at will, or the number of times of medication cannot be changed
    .

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

     Use with caution in gastric ulcer, gastritis or esophagitis, hypertension, congestive heart failure, myasthenia gravis, diabetes, hypothyroidism, osteoporosis, hyperlipoproteinemia, epilepsy, emotional instability and psychotic tendencies, liver function damage, renal impairment, or stones
    .

     ➤Combination with digitalis drugs may increase the risk of arrhythmia caused by hypokalemia; ➤When combined with drugs with potassium excretion such as amphotericin B and diuretics, it can cause excessive potassium loss, which may cause cardiac hypertrophy.
    Reports of Yamato congestive heart failure; ➤ Oral contraceptives, ritonavir can increase the blood concentration of glucocorticoids; ➤ When combined with non-steroidal anti-inflammatory drugs (NSAIDs), the incidence of gastrointestinal bleeding and ulcers Increased; ➤Glucocorticoids may increase blood sugar and weaken the effect of hypoglycemic drugs; ➤Recent use of barbiturates, carbamazepine, phenytoin, primidone, rifampin and other drugs may reduce the effect of systemic glucocorticoids.
    Effect; ➤ Combination with anabolic hormones can increase the incidence of edema and aggravate acne; ➤ Combination with immunosuppressive agents can increase the risk of infection and may induce lymphoma or other lymphoproliferative diseases; ➤ Combination with anticholinergic drugs Long-term combined use of drugs such as atropine can cause increased intraocular pressure; ➤ Combination with anticholinesterase drugs can cause severe weakness in myasthenia gravis.
    If possible, stop anticholinesterase at least 24 hours before the start of glucocorticoid therapy drug
    .

     Anticholinergic drugs include diphenhydramine, hydroxyzine, doxylamine, scopolamine, diphenidol, etc.
    , which can be clinically used for motion sickness and vomiting, postoperative nausea and vomiting (PONV), and opioid-induced nausea vomiting,
    etc.

     Precautions Peripheral anticholinergic effects can cause dry mouth, dry eyes, thick respiratory secretions, constipation, arrhythmia, increased intraocular pressure, blurred vision, mydriasis, erectile dysfunction, urinary retention and dysuria, etc.
    Transient disturbance of nerve function and inattention caused by conduction of neurons or nerve-muscle junctions
    .

     Use with caution in patients with angle-closure glaucoma, urinary retention, benign prostatic hyperplasia, prostatic hypertrophy, and pyloric duodenal obstruction
    .

     Antihistamines can cause central depression, such as sedation, drowsiness, drowsiness, fatigue, hallucinations, decreased vigilance, restlessness, nervousness, anxiety, insomnia, headache, dizziness, lack of coordination and tremor, etc.
    , and can reduce the rapid eye movement period Sleep, may lead to decreased learning ability, especially first-generation antihistamines
    .

     Avoid use with drugs that have inhibitory effects on the central nervous system such as sedative and hypnotic drugs such as diazepam, antipsychotic drugs such as chlorpromazine, barbiturates, opioids, antiepileptic drugs, otherwise it will cause dizziness, systemic Fatigue, ataxia, blurred vision, diplopia and other symptoms of excessive central nervous system inhibition, especially in children, the elderly, and the infirm
    .

    High-altitude workers, drivers, machinery operators are prohibited or used with caution
    .

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

     References: 10 Wan Xuehong et al.
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    Chinese Journal of Cancer, 2018 , 28(11):946-9553 Chinese Expert Consensus on the Prevention and Treatment of Nausea and Vomiting Associated with Tumor Drug Therapy (2019 Edition) [J].
    Frontiers in Chinese Medicine, 2019, 11(11):16-244 Guidelines for the Prevention and Treatment of Nausea and Vomiting Associated with Tumor Therapy (2014 Edition) [J].
    Journal of Clinical Oncology, 2014, 19(3): 263-2725 Expert opinion on the prevention and treatment of postoperative nausea and vomiting (2012) [J].
    Journal of Clinical Anesthesiology, 2012, 28(4): 413-4166 2014 Chinese Anesthesiology Guidelines and Expert Consensus [M].
    Beijing: People's Health Publishing House, 2014: 305-3107 Pharmacy Professional Knowledge (2) [M].
    Beijing: China Medical Science and Technology Press, 2015: 064-074, 082-0858 Zhu Yizhu et al.
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    Chinese Journal of Geriatrics,2015,34(7 ): 698-70112 Consensus of medical experts on the management of perioperative drug therapy in enhanced recovery after surgery (Guangdong Pharmaceutical Association, December 31, 2019) 13 Chen Xinqian et al.
    Chen Xinqian New Pharmacology [M].
    Beijing: People's Health Publishing House, 2018 :281,381,468-469,565-573,798-811,81414 Chinese expert consensus on chronic gastritis in the elderly[J].
    Chinese Journal of Gerontology,2018,37(5):485-48815Li Xiaowen et al.
    Research status of the safety of gastrointestinal motility drugs[J] ].
    China Journal of New Drugs and Clinical Medicine, 2015, 34(9): 657-66016 Wang Baoxi et al.
    Research status and prospect of gastrointestinal motility drugs [J].
    Chinese Journal of Practical Pediatrics, 2014, 27(9): 483-48517 Zhao Zhigang, et al.
    Treatment Guidelines · Gastrointestinal Diseases [M].
    Beijing: Chemical Industry Press, 2018: 518 Zhang Yubei.
    Research progress and clinical application evaluation of gastrointestinal motility drugs[J].
    Drug Evaluation and Analysis in Chinese Hospitals, 2006,6(6):336-33819 Ma Rui.
    Prevention and treatment of adverse reactions of commonly used drugs in digestive system[J].
    Chinese Clinical Doctor's Journal, 2008, 36(2): 1220 Guidelines for the Clinical Application of Glucocorticoids[J].
    Chinese Journal of Endocrinology and Metabolism, 2012, 28: Added 2a-1-3221 Expert Consensus on Emergency Application of Glucocorticoids[J] .
    Chinese Journal of Emergency Medicine, 2020,19(6):765-76922 Guidelines for drug treatment and pharmaceutical care of novel coronavirus pneumonia and common comorbidities[J].
    202023 Expert consensus on the application of antihistamines in dermatology[J].
    Zhonghua Journal of Dermatology, 2017, 50(6): 393-39524 Guangzhou Consensus 2018 for the treatment of allergic rhinitis with oral H1 antihistamines [J].
    Chinese Journal of Ophthalmology and Otolaryngology, 2018, 18(3): 149-156
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