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US Brand Name
Mechanism of Action
Selective 5-HT3 receptor antagonist; dolasetron binds to 5-HT3 receptors located on vagal neurons in GI tract, blocking signal to vomiting center in the brain, thus preventing N/V
Half-life: parent compound <10 min, hydrodolasetron (active) 4-9 hr
Peak plasma time: IV: 0.6 hr, PO: 1-1.5 hr
Bioavailability: 59-80% (PO)
Vd: 5.8-10 L/kg
Protein binding: 69-77%
Metabolism: dolasetron is metabolized to hydrodolasetron (active) by carbonyl reductase; hydrodolasetron is subsequently metabolized by CYP2D6 and CYP3A
Metabolites: hydrodolasetron (active)
Total body clearance: 9.4-13.4 mL/min/kg
Renal clearance: 2.6-3.4 mg/kg
Excretion: urine (53-61%); feces (25-33%)
Uses of Anzemet
Anzemet is a prescription medicine used to prevent nausea and vomiting caused by chemotherapy. Anzemet is also used to prevent or treat nausea and vomiting after surgery.
This medication may be prescribed for other uses. Ask your doctor or pharmacist for more information.
Sanofi-Aventis U.S. LLC
Anzemet Drug Class
Anzemet is part of the drug class:
Serotonin 5HT3 antagonists
- Store Anzemet tablets at room temperature in the container it came in, tightly closed.
- Keep this and all medications out of the reach of children.
What should I discuss with my health care provider before taking dolasetron?
You should not take dolasetron if you are allergic to it.
To make sure you can safely take dolasetron, tell your doctor if you have any of these other conditions:
a serious heart condition such as "sick sinus syndrome";
a heart rhythm disorder such as slow heartbeats, or atrial fibrillation (fast, irregular heart rhythm);
personal or family history of long QT syndrome;
congestive heart failure; or
an electrolyte imbalance (such as low levels of potassium or magnesium in your blood).
It is not known whether this medicine will harm an unborn baby. Tell your doctor if you are pregnant.
It is not known whether dolasetron passes into breast milk or if it could harm a nursing baby. Tell your doctor if you are breast-feeding a baby.
Dolasetron should not be given to a child younger than 2 years old.
Uses for Anzemet
Cancer Chemotherapy-induced Nausea and Vomiting
Prevention of nausea and vomiting associated with emetogenic cancer chemotherapy;2 3 4 5 6 7 8 may use orally with initial and repeat courses of moderately emetogenic chemotherapy.2 3
In December 2010, FDA informed healthcare professionals that IV dolasetron should no longer be used to prevent nausea and vomiting associated with cancer chemotherapy in pediatric patients and adults because of the risk of prolongation of cardiac conduction intervals and development of abnormal heart rhythms.17 (See Cardiovascular Effects under Cautions.)
For prevention of nausea and vomiting associated with highly emetogenic chemotherapy regimens (including an anthracycline plus cyclophosphamide), ASCO recommends a 3-drug antiemetic regimen consisting of an NK1 receptor antagonist (e.g., either oral aprepitant or IV fosaprepitant), a 5-HT3 receptor antagonist (e.g., dolasetron, granisetron, ondansetron, palonosetron), and dexamethasone.20 21 ASCO states that fixed-combination netupitant and palonosetron plus dexamethasone is an additional treatment option.21
For moderately emetogenic chemotherapy regimens, ASCO recommends a 2-drug antiemetic regimen preferably consisting of palonosetron and dexamethasone.20 21 If palonosetron is not available, a first-generation 5-HT3 receptor antagonist (preferably granisetron or ondansetron) may be substituted.20 Limited evidence suggests that aprepitant may be added to this regimen; in such cases, use of any 5-HT3 receptor antagonist is appropriate.20
For chemotherapy regimens with a low emetogenic risk, ASCO recommends administration of a single dose of dexamethasone prior to chemotherapy.20
For chemotherapy regimens with minimal emetogenic risk, ASCO states that routine antiemetic administration is not necessary.20
Postoperative Nausea and Vomiting
Oral or IV use for prevention and treatment of postoperative nausea and vomiting.1 2 3
Routine prophylaxis not recommended in patients in whom there is little expectation that nausea and/or vomiting will occur postoperatively.1
Recommended for patients who, in the clinician’s judgement, must avoid nausea and/or vomiting postoperatively, even when anticipated incidence is low.1 8
Indications and Usage for Anzemet
Anzemet Tablets are indicated for the prevention of nausea and vomiting associated with moderately emetogenic cancer chemotherapy, including initial and repeat courses in adults and children 2 years and older.
Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.
There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.
Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.
How should I take Anzemet?
Take Anzemet exactly as prescribed by your doctor. Follow all directions on your prescription label. Do not take this medicine in larger or smaller amounts or for longer than recommended.
Anzemet is usually taken 1 hour before chemotherapy. Follow your doctor's instructions.
Store at room temperature away from moisture, heat, and light.
Anzemet side effects
Get emergency medical help if you have signs of an allergic reaction to Anzemet: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.
Call your doctor at once if you have:
headache with chest pain and severe dizziness, fainting, fast or pounding heartbeats;
a light-headed feeling, like you might pass out;
slow heart rate, weak pulse, slow breathing;
swelling in your hands or feet;
little or no urinating; or
high levels of serotonin in the body - agitation, hallucinations, fever, fast heart rate, overactive reflexes, nausea, vomiting, diarrhea, loss of coordination, fainting.
Common Anzemet side effects may include:
This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
Dolasetron Breastfeeding Warnings
AU: Use is not recommended. US: Caution is recommended. Excreted into human milk: Unknown Excreted into animal milk: Unknown Comments: The effects in the nursing infant are unknown.
When animal models were given the oral formulation of this drug, survival, growth, and development of pups were not affected.