Dolasetron (Mesylate)
Also known as: Octohydro-3-oxo-2, 6-methano-2H-quinolizin-8-Y<ester, 1H-indole-3-carboxylic acid
Dolasetron (Mesylate) is a specific 5HT-3 antagonist, similar to ondensetron. It block 5HT-3 receptors in the gastrointestinal tract and in the CNS. Dolasetron (Mesylate) is used chiefly in the management of nausea and vomiting induced by cytotoxic drugs during chemotherapy or in post-operative nausea and vomiting.
Primary Characteristics
Dolasetron (Mesylate) is also known as Octohydro-3-oxo-2, 6-methano-2H-quinolizin-8-Y<ester, 1H-indole-3-carboxylic acid.
It is of Synthetic origin and belongs to Methanesulfonate.
Molecular Weight: 428.5 · pKa: 6.4 · Solubility in Water: > 1 in 10 · Solubility in Alcohol: 1 in 140 · Non-proprietary name: Dolasetron (Mesylate).
Pharmacokinetics
Absorption: Dolasetron (Mesylate) has an oral bioavailability is 77% (±5%).
Distribution: Dolasetron (Mesylate) has a volume of distribution is 5.0 - 7.9 l/kg. plasma protein binding is ~ 70%.
Elimination: it is metabolised via hepatic, plasma half-life is ~ 7hr, renal excretion is 1% (unchanged).
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Indications
Dolasetron (Mesylate) is primarily indicated in conditions like Nausea and vomiting (chemotherapy induced), Nausea and vomiting (prevention), Nausea and vomiting (radiothrapy induced).
Contraindications
Dolasetron (Mesylate) is contraindicated in conditions like Heart disease, Hypersensitivity.
Dosage
Dolasetron (Mesylate)'s dosage details are as follows:
| Dose | Single Dose | Frequency | Route | Instructions |
|---|---|---|---|---|
| Adult Dosage | ||||
| 200 mg | 200 mg | — | PO | For Prevention of Cancer Chemotherapy-Induced Nausea and Vomiting: Should be given within one hour before chemotherapy. |
| Paediatric Dosage (20kg) | ||||
| 1.8 – 100 mg/kh | — | — | IV | Over 2 years of age , with in 1 hour before chemotherapy, for prevention of chemotherapy induce nuas |
| Neonatal Dosage (3kg) | ||||
| No data. | ||||
Drug Interactions
Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Side Effects
The signs and symptoms that are produced after acute overdosage of Dolasetron (Mesylate) are Hypotension, Dizziness, Metastatic Melenoma.
Dolasetron (Mesylate) is known to cause more or less tolerable side effects which are usually transient. These include Abdominal pain, Abnormal LFT, Constipation , Diarrhea, Dizziness, Drowsiness, Fatigue, Headache, Hot flushes, Hypertension , QT prolongation, Symptomatic cardiovascular events, Weakness.
Warnings / Precautions
Interference in Pathology
Dolasetron (Mesylate) may interfere in the diagnosis of No well documented.
Available Brands
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Single Ingredient
Storage Conditions
Drug Classification
- 1.17.2 — Antiemetics & antinauseants
Manufacturers
Manufacturers of Dolasetron (Mesylate) in Pakistan: