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Dolasetron
Dolasetron is a selective serotonin 5-HT3 receptor antagonist used to prevent and treat nausea and vomiting caused by chemotherapy, radiotherapy, and surgery. It is particularly effective in managing chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV). This article synthesizes information from the British National Formulary (BNF), Lippincott Textbook of Pharmacology, and Lange Basic & Clinical Pharmacology to provide a detailed overview of dolasetron, including its mechanism, uses, dosing, side effects, precautions, and drug interactions.
Dolasetron works by selectively blocking 5-HT3 receptors in the chemoreceptor trigger zone (CTZ) and the gastrointestinal (GI) tract. By inhibiting these receptors, dolasetron:
- Prevents the stimulation of the vomiting center in the brain, reducing nausea and vomiting.
- Blocks serotonin release from enterochromaffin cells in the GI tract, which is often triggered by chemotherapy or radiation (Lippincott, Lange).
Dolasetron is metabolized to its active form, hydrodolasetron, which is responsible for its therapeutic effects (BNF).
- Chemotherapy-Induced Nausea and Vomiting (CINV):
- Used to prevent acute nausea and vomiting associated with moderately emetogenic chemotherapy (BNF).
- Postoperative Nausea and Vomiting (PONV):
- Effective in preventing and treating nausea and vomiting after surgery (Lippincott).
- Chemotherapy-Induced Nausea and Vomiting:
- 100 mg orally 1 hour before chemotherapy, or 1.8 mg/kg intravenously 30 minutes before chemotherapy (BNF).
- Postoperative Nausea and Vomiting:
- 12.5 mg intravenously 15 minutes before the end of surgery, or 100 mg orally 2 hours before surgery (Lippincott).
Administration:
- Oral tablets can be taken with or without food.
- Intravenous administration should be done slowly over 30 seconds to minimize side effects (Lange).
- Common: Headache, dizziness, and constipation (Lippincott).
- Serious:
- QT Prolongation: Risk of arrhythmias, particularly with high doses or in patients with underlying heart conditions (Lange).
- Hypersensitivity Reactions: Rare cases of anaphylaxis or rash (BNF).
- QT Prolongation: Avoid in patients with congenital long QT syndrome or those taking other QT-prolonging drugs (BNF).
- Pregnancy: Generally considered safe but should be used under medical supervision (Lippincott).
- Liver Impairment: Dose reduction may be necessary in patients with severe hepatic impairment (Lange).
- QT-Prolonging Drugs (e.g., amiodarone, sotalol): Increased risk of arrhythmias (BNF).
- Apomorphine: Contraindicated due to risk of profound hypotension and loss of consciousness (Lippincott).
- Tramadol: Dolasetron may reduce the analgesic effect of tramadol (Lange).
Dolasetron is the generic name for this medication. It is marketed under the brand name Anzemet®. Generic versions are also available, making it more accessible for patients
