Tropisetron (Tropisetron). {(1a H, 5a H) -8-methyl-8-azabicyclo- [3,2,1] oct-3a-yl ester} 1H-indole-3-carboxylic acid. Available in the form of hydrochloride.
| Tropisetron | |
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| Chemical compound | |
| Gross formula | C 17 H 20 N 2 O 2 |
| Cas | |
| PubChem | |
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Synonyms: Navoban, Navoban, Tropindol .
Content
- 1 General information
- 2 Contraindications
- 3 release form
- 4 Storage
General Information
An antiemetic effective against vomiting due to chemotherapy with anticancer drugs. The mechanism of action is associated with the selective blocking of peripheral and central serotonin receptors (C- or 5-HT 3 receptors; see Serotonin ).
The drug is rapidly absorbed from the gastrointestinal tract. After ingestion, the maximum concentration of the drug in blood plasma is reached within 3 hours. It is slowly excreted from the body; the duration of action is about 24 hours, which allows the use of the drug once a day. There are differences in the metabolic rate of the drug in different patients. In individuals with a high metabolic rate, about 8% of tropisetron is excreted in the urine in unchanged form and about 70% in the form of metabolites (pharmacologically inactive). In patients with a low metabolic rate, a higher percentage of the drug excreted in the urine unchanged.
Tropisetron is used to prevent nausea and vomiting during chemotherapy of tumors.
Assign to adults in the form of six-day courses in a daily dose of 0.005 g (5 mg). On the 1st day, administered intravenously shortly before the start of chemotherapy. From the 2nd to the 6th day, the drug is taken orally.
For intravenous infusions, dilute the contents of one ampoule (5 ml containing 5 mg of tropisetron equal to 5.64 mg of tropisetron hydrochloride) in 100 ml of isotonic sodium chloride solution or 5% glucose solution; administered slowly. Inside appoint in the form of capsules containing 5 mg of tropisetron.
Capsules are taken on an empty stomach (1 hour before breakfast), washed down with water.
The drug is usually well tolerated. Possible side effects: headache, dizziness, feeling tired, constipation or diarrhea; in patients with arterial hypertension, blood pressure may increase; in rare cases, visual hallucinations are possible.
It is not recommended to prescribe the drug to children (lack of a sufficient number of observations).
It should be borne in mind that rifampicin , phenobarbital and other drugs that induce the activity of liver enzymes reduce the concentration of tropisetron in blood plasma.
Contraindications
Contraindications: pregnancy, breast-feeding.
Release form
Method of release: 0.1% solution in ampoules of 5 ml (5 mg of the drug in an ampoule) in a package of 5 ampoules; capsules containing 5 mg of tropisetron.
Storage
Storage: List B.