Dolasetron

Dolasetron
Clinical data
AHFS/Drugs.com Monograph
MedlinePlus a601001
Pregnancy
category
  • B (US)
Routes of
administration		 Intravenous, oral
ATC code A04AA04 (WHO)
Legal status
Legal status
  • ℞ (Prescription only)
Pharmacokinetic data
Protein binding 69 to 77%
Biological half-life 8.1 hours
Identifiers
CAS Number 115956-12-2 YesY
PubChem (CID) 60654
DrugBank DB00757 YesY
ChemSpider 16736416 YesY
UNII 82WI2L7Q6E YesY
KEGG D07867 YesY
ChEMBL CHEMBL1201240 N
ECHA InfoCard 100.130.141
Chemical and physical data
Formula C19H20N2O3
Molar mass 324.374 g/mol
3D model (Jmol) Interactive image
 NYesY (what is this?)  (verify)

Dolasetron (trade name Anzemet) is a serotonin 5-HT3 receptor antagonist used to treat nausea and vomiting following chemotherapy. Its main effect is to reduce the activity of the vagus nerve, which is a nerve that activates the vomiting center in the medulla oblongata. It does not have much antiemetic effect when symptoms are due to motion sickness. This drug does not have any effect on dopamine receptors or muscarinic receptors.

Dolasetron breaks down slowly, staying in the body for a long time. One dose usually lasts 4 to 9 hours and is usually administered once or twice daily. This drug is removed from the body by the liver and kidneys.

Clinical uses

Adverse effects

Dolasetron is a well-tolerated drug with few side effects. Headache, dizziness, and constipation are the most commonly reported side effects associated with its use. There is a potential for prolonging of the QT interval to occur as well. There have been no significant drug interactions reported with this drug's use. It is broken down by the liver's cytochrome P450 system and it has little effect on the metabolism of other drugs broken down by this system. Intravenous dolasetron is contraindicated in Chemotherapy-induced nausea and vomiting (CINV). Doxorubicin and cyclophosphamide are as emetogenic as cisplatin, and preventive drugs should always be considered. The 5HT3 agonists are the mainstays of prevention and are frequently used in combination with other drugs such as corticosteroids and the NK1 receptor antagonist aprepitant. However, the FDA recently issued a drug communication stating that the injection form of dolasetron, a 5HT3 agonist, should no longer be used in adult or pediatric patients with CINV. Dolasetron injection can increase the risk of developing torsade de pointes, a potentially fatal abnormal heart rhythm. Patients with underlying heart conditions or existing heart rate or rhythm problems are at increased risk. Although the oral form of this agent can still be used, careful monitoring and correction of potassium and magnesium levels should be initiated prior to and during treatment. In addition, in older patients and in patients with heart failure, a slow heart rate, underlying cardiac disease, and those with renal impairment, monitoring with electrocardiography is indicated when this drug is used. Congenital long-QT syndrome and drugs that prolong the PR or QRS interval are contraindications to dolasetron therapy. Dolasetron injection may still be used for the prevention and treatment of postoperative nausea and vomiting. As per Food and Drug Administration.

See also

References

This article is issued from Wikipedia - version of the 4/2/2016. The text is available under the Creative Commons Attribution/Share Alike but additional terms may apply for the media files.