dolasetron

Therapeutic Classification: antiemetics

Pharmacologic Classification: five ht3 antagonists

Indications ⬆ ⬇

REMS

PO: Prevention of nausea and vomiting associated with emetogenic chemotherapy.

Action ⬆ ⬇

Blocks the effects of serotonin at receptor sites (selective antagonist) located in vagal nerve terminals and in the chemoreceptor trigger zone in the CNS.

Therapeutic effects:

Decreased incidence and severity of nausea/vomiting associated with emetogenic chemotherapy or surgery.

Pharmacokinetics ⬆ ⬇

Absorption: Well absorbed but rapidly metabolized to hydrodolasetron, the active metabolite.

Distribution: Unknown.

Metabolism/Excretion: 61% of hydrodolasetron is excreted unchanged by the kidneys.

Half-Life: Hydrodolasetron: 8.1 hr (shorter in children).

Time/Action Profile ⬆ ⬇

(antiemetic effect)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	1–2 hr	up to 24 hr

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity;
Congenital long QT syndrome;
Complete heart block (unless pacemaker present).

Use Cautiously in:

Patients with risk factors for cardiac conduction abnormalities (underlying structural heart disease, sick sinus syndrome, AF and slow ventricular rate, myocardial ischemia, concurrent beta blocker, verapamil, diltiazem, or antiarrhythmic therapy);
Hypokalemia, hypomagnesemia, concurrent therapy with diuretics, or history of cumulative high-dose anthracycline therapy;
OB: Safety not established in pregnancy;
Lactation: Safety not established in breastfeeding;
Pedi: Children 2 yr (safety and effectiveness not established);
Geri: risk of cardiac conduction abnormalities in older adults.

Adv. Reactions/Side Effects ⬆ ⬇

CV: bradycardia, CARDIAC ARREST, heart block, hypertension, hypotension, PR interval prolongation, QRS interval prolongation, QT interval prolongation, tachycardia, TORSADES DE POINTES, VENTRICULAR ARRHYTHMIAS

Derm: pruritus

GI: diarrhea, dyspepsia

GU: oliguria

MS: pain

Neuro: headache (↑ in patients with cancer), dizziness, fatigue, syncope

Misc: chills, fever, SEROTONIN SYNDROME

Interactions ⬆ ⬇

Drug-drug:

Concurrent diuretic or antiarrhythmic therapy or cumulative high-dose anthracycline therapy may ↑ risk of conduction abnormalities.
Atenolol and cimetidine may ↑ hydrodolasetron levels and risk of toxicity.
Rifampin may ↓ hydrodolasetron levels and effectiveness.
↑risk of QT interval prolongation with other QT interval prolonging agents.
Drugs that affect serotonergic neurotransmitter systems, including SSRIs, SNRIs, tricyclic antidepressants, MAO inhibitors, fentanyl, lithium, buspirone, tramadol, methylene blue, and triptans, ↑ risk of serotonin syndrome

Route/Dosage ⬆ ⬇

PO (Adults ): 100 mg given within 1 hr before chemotherapy.
PO (Children 2–16 yr): 1.8 mg/kg given within 1 hr before chemotherapy (not to exceed 100 mg).

Availability ⬆ ⬇

Assessment ⬆ ⬇

Assess patient for nausea, vomiting, abdominal distention, and bowel sounds before and after administration.
Monitor ECG in patients with HF, bradycardia, underlying heart disease, renal impairment, and older adults.

Lab Test Considerations:

Monitor serum potassium and magnesium prior to and periodically during therapy.

Implementation ⬆ ⬇

PO: Administer within 1 hr before chemotherapy.

Patient/Family Teaching ⬆ ⬇

Explain purpose of dolasetron to patient.
Advise patient to notify health care professional if nausea or vomiting occurs.
Advise patient to notify health care professional if symptoms of abnormal heart rate or rhythm (racing heart beat, shortness of breath, dizziness, fainting) occur.
Rep: Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding.

Evaluation/Desired Outcomes ⬆ ⬇

Prevention of nausea and vomiting associated with emetogenic cancer chemotherapy.

US Brand Names ⬆ ⬇

Code ⬆

NDC Code

30698- Validus Pharmaceuticals LLC
- 30698-120- ANZEMET
  - 30698-120-05- 5 TABLET, FILM COATED in 1 BOTTLE (30698-120-05)

30698- Validus Pharmaceuticals LLC
- 30698-121- ANZEMET
  - 30698-121-05- 5 TABLET, FILM COATED in 1 BOTTLE (30698-121-05)

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Pronunciation ⬇

Classifications ⬆ ⬇