Drug class and drug | Mechanism of action | Indications | Side effects |
Antihistamines | Minimal antiemetic activity | ||
Diphenhydramine | Vestibular suppression, anti-ACh effect, and H1 antagonist | Motion sickness. | Sedation, anti-ACh effects* |
Hydroxyzine | |||
Dimenhydrinate | |||
Meclizine | |||
Antipsychotics | Mild to moderate antiemetic activity | ||
Promethazine | D2 antagonist at CTZ and H1 antagonist | Chemotherapy-induced vomiting. | Anti-ACh effects*, extrapyramidal reactions, QTc prolongation |
Prochlorperazine | D2 antagonist at CTZ | ||
Chlorpromazine | |||
Olanzapine | D2 antagonist at CTZ, 5-HT6 antagonist | ||
Substituted benzamides | Moderate antiemetic activity | ||
Metoclopramide | D2 antagonist at CTZ and 5-HT4 agonist in gut | GERD; gastroparesis; chemotherapy-induced vomiting. | Irritability and extrapyramidal reactions |
Trimethobenzamide | D2 antagonist at CTZ | ||
Cisapride | 5-HT4 agonist, ACh release in gut | GERD; gastroparesis. | Diarrhea, abdominal pain, headache, QT prolongation |
Benzimidazole derivatives | Moderate antiemetic activity | ||
Domperidone | D2 antagonist in gut | Gastroparesis; chemotherapy-induced vomiting. | Headaches; not available in the United States |
Motilin agonist | |||
Erythromycin | Motilin agonist and ACh release | Gastroparesis (eg, postinfectious). | Nausea, diarrhea |
5-HT3 receptor antagonists | High antiemetic activity | ||
Ondansetron | 5-HT3 antagonist at CTZ and decreases vagal afferents from gut | Chemotherapy- and postoperative-induced vomiting; cyclic vomiting syndrome. Ondansetron has also been used in the treatment of acute gastroenteritis. Ondansetron comes in PO, IM, and IV formulations. All others are IV formulations only. Palonosetron has a longer half-life (40 hours). | Headache, constipation |
Granisetron | |||
Tropisetron | |||
Dolasetron | |||
Palonosetron | |||
Tachykinin receptor antagonists | High antiemetic activity | ||
Aprepitant | NK1 antagonist, acts on emetic program | Chemotherapy-induced vomiting (effect is on delayed phase, >24 hours); cyclic vomiting syndrome. | Fatigue, dizziness, diarrhea |
Anticholinergics | Minimal to mild antiemetic activity | ||
Scopolamine | Vestibular suppression, anti-ACh | Motion sickness. | Sedation, anti-ACh effects* |
Butyrophenones | Moderate antiemetic activity | ||
Droperidol | D2 antagonist at CTZ; anxiolytic action and sedation | Chemotherapy- and postoperative-induced vomiting. | Hypotension, sedation, extrapyramidal effects |
Benzodiazepines | Minimal antiemetic activity | ||
Lorazepam | Enhanced central GABA-ergic signaling; induces anxiolysis, sedation, and amnesia | Adjunctive therapy (sedation) for chemotherapy-induced vomiting and cyclic vomiting syndrome¶. Diazepam may be given rectally. | Sedation, respiratory depression |
Diazepam | |||
Antimigraine-abortive triptans | |||
Sumatriptan | 5-HT1B1D agonist; induces cerebral vasoconstriction, relaxes gastric fundus | Abortive approach for migraine, abdominal migraine, cyclic vomiting syndrome¶. Subcutaneous, PO, nasal and rectal formulations. | Transient burning sensation in chest and neck |
Zolmitriptan | PO, ODT, and nasal formulations. | ||
Frovatriptan | PO formulation; longer half-life (26 hours). | ||
Rizatriptan | ODT formulation. | ||
Other – NSAIDs | |||
Ketorolac | Cyclooxygenase inhibitor of prostaglandin synthesis | Abortive approach for migraine, cyclic vomiting syndrome¶. | Gastrointestinal bleeding |
Antimigraine – prophylactic medication | |||
Cyproheptadine | H1 antagonist and 5-HT2 antagonist | Prevention of migraine, abdominal migraine, cyclic vomiting syndrome. | Sedation, anti-ACh effects*, weight gain due to appetite stimulation |
Pizotifen, pizotyline | 5-HT2 antagonist | Not available in the United States | |
Propranolol | β1, β2 adrenergic antagonist | Prevention of abdominal migraine, cyclic vomiting syndrome. | Hypotension, bradycardia, fatigability; monitor pulse |
Amitriptyline, nortriptyline | 5-HT2 antagonist, increases synaptic norepinephrine | Prevention of migraine, abdominal migraine, cyclic vomiting syndrome¶. | Sedation, anti-ACh effects*, QTc prolongation |
Corticosteroids | |||
Dexamethasone | Unknown | Adjunctive therapy for chemotherapy- and postoperative-induced vomiting. | Adrenal suppression |
Cannabinoids | |||
Dronabinol | Acts on CB1R receptors on vagus | Chemotherapy-induced vomiting. | Disorientation, vertigo, hallucinations |
Nabilone |
ACh: acetylcholine; H: histamine; D: dopamine; CTZ: chemoreceptor trigger zone; 5-HT: 5-hydroxytryptamine (serotonin); GERD: gastroesophageal reflux disease; PO: orally; IM: intramuscularly; IV: intravenously; NK: neurokinin; GABA: gamma aminobutyric acid; ODT: orally dissolving tablet; NSAID: nonsteroidal antiinflammatory drug; CB1R: cannabinoid receptor 1.
* Anticholinergic effects include blurred vision, dry mouth, hypotension, palpitations, and urinary retention.
¶ Pharmacotherapy for cyclic vomiting syndrome may be preventive, supportive, or abortive, depending on the patient's characteristics. For detailed guidance, refer to UpToDate content and tables on cyclic vomiting syndrome.آیا می خواهید مدیلیب را به صفحه اصلی خود اضافه کنید؟