Dolasetron

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Contents

[edit] BRAND NAMES

[edit] STRUCTURE

Dolasetron.jpg

[edit] MECHANISM OF ACTION

Dolasetron and its active metabolite, hydrodolasetron, are selective serotonin 5-HT3 receptor antagonists not shown to have activity at other known serotonin receptors and with low affinity for dopamine receptors. The serotonin 5-HT3 receptors are located on the nerve terminals of the vagus in the periphery and centrally in the chemoreceptor trigger zone of the area postrema. It is thought that chemotherapeutic agents produce nausea and vomiting by releasing serotonin from the enterochromaffin cells of the small intestine, and that the released serotonin then activates 5-HT3 receptors located on vagal efferents to initiate the vomiting reflex.

[edit] INDICATIONS

Prevention of nausea and vomiting associated with moderately emetogenic cancer chemotherapy, including initial and repeat courses in adults and children 2 years and older.

[edit] DOSAGE

Tablets:

Adults

The recommended oral dosage is 100 mg given within one hour before chemotherapy.


Pediatric Patients

The recommended oral dosage in pediatric patients 2 to 16 years of age is 1.8 mg/kg given within one hour before chemotherapy, up to a maximum of 100 mg. Safety and effectiveness in pediatric patients under 2 years of age have not been established.

[edit] CONTRAINDICATIONS

  • Known hypersensitivity to the drug.

[edit] PRECAUTIONS

Dolasetron should be administered with caution in patients who have or may develop prolongation of cardiac conduction intervals, particularly QTc. These include patients with hypokalemia or hypomagnesemia, patients taking diuretics with potential for inducing electrolyte abnormalities, patients with congenital QT syndrome, patients taking anti­-arrhythmic drugs or other drugs which lead to QT prolongation, and cumulative high dose anthracycline therapy.

[edit] INTERACTIONS

[edit] PREGNANCY AND LACTATION

  • Nursing Mothers: It is not known whether dolasetron mesylate is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when dolasetron is administered

to a nursing woman.

[edit] SIDE EFFECTS

[edit] RELATED LINKS

[edit] BIBLIOGRAPHY

[edit] REFERENCES

Antiemetics
5-HT3 receptor antagonists Dolasetron   Granisetron   Ondansetron   Palonosetron   Tropisetron
Dopamine antagonists Alizapride   Bromopride   Clebopride   Domperidone   Metoclopramide   Prochlorperazine   Thiethylperazine
H1 antagonists Dimenhydrinate   Meclizine
NK1 receptor antagonists‎ Aprepitant   Fosaprepitant   Maropitant
Motion sickness‎ Cinnarizine   Dimenhydrinate   Meclizine   Meclizine/Pyridoxine   Scopolamine (Patch)
Pregnancy Meclizine/Pyridoxine   Ondansetron
Veterinary Maropitant