Dolasetron mesylate


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Dolasetron mesylate
Dolasetron mesylate (Anzemet)
Dolasetron mesylate
(dohl- AH-seh-tron)
Pregnancy Category: B Anzemet (Rx)

Classification: Antinauseant/antiemetic, serotonin 5-HT 3 antagonist

Action/Kinetics: Selective serotonin 5-HT 3 antagonist that prevents N&V by inhibiting released serotonin from combining with receptors on vagal efferents that initiate vomiting reflex. May also cause acute, usually reversible, PR and QT c prolongation and QRS widening, perhaps due to blockade of sodium channels by active metabolite of dolasetron. Well absorbed from GI tract. Metabolized to active hydrodolasetron: peak plasma levels: 1 hr; t 1/2: 8.1 hr. Food does not affect bioavailability. Hydrodolasetron is excreted through urine and feces. Is eliminated more quickly in children than in adults.

Uses: Prevention of N&V associated with moderately-emetogenic cancer chemotherapy (initially and repeat courses). Prevention of postoperative N&V.

Special Concerns: Use with caution during lactation and in those who have or may develop prolongation of cardiac conduction intervals, including QT c. These include clients with hypokalemia or hypomagnesemia, those taking diuretics with potential for electrolyte abnormalities, in congenital QT syndrome, those taking anti-arrhythmic drugs or other drugs which lead to QT prolongation, and cumulative high dose anthracycline therapy. Safety and efficacy in children less than 2 years of age have not been determined.

Side Effects: Chemotherapy clients. Headache, fatigue, diarrhea, bradycardia, dizziness, pain, tachycardia, dyspepsia, chills, shivering. Postoperative clients. Headache, hypotension, dizziness, fever, pruritus, oliguria, hypertension, tachycardia. Chemotherapy or postoperative clients. C V: Hypotension, edema, peripheral edema, peripheral ischemia, thrombophlebitis, phlebitis. GI: Constipation, dyspepsia, abdominal pain, anorexia, pancreatitis, taste perversion. CNS: Flushing, vertigo, paresthesia, tremor, ataxia, twitching, agitation, sleep disorder, depersonalization, confusion, anxiety, abnormal dreaming. Dermatologic: Rash, increased sweating. Hematologic: Hematuria, epistaxis, anemia, purpura, hematoma, thrombocytopenia. Hypersensitivity: Rarely, anaphylaxis facial edema, urticaria. Musculoskeletal: Myalgia, arthralgia. Respiratory: Dyspnea, bronchospasm. GU: Dysuria, polyuria, acute renal failure. Ophthalmic: Abnormal vision, photophobia. Miscellaneous: Tinnitus.

Laboratory Test Alterations: PTT, AST, ALT, alkaline phosphatase. Prolonged prothrombin time.

Drug Interactions: Possible interaction with drugs that the prolong QT c interval.

How Supplied: Injection: 20 mg/mL; Tablet: 50 mg, 100 mg

Dosage
?Tablets Prevention of N&V during chemotherapy.
Adults: 100 mg within 1 hr before chemotherapy. Children, 2 to 16 years: 1.8 mg/kg within 1 hr before chemotherapy, up to a maximum of 100 mg.
Prevention of postoperative N&V.
Adults: 100 mg within 2 hr before surgery. Children, 2 to 16 years: 1.2 mg/kg within 2 hr before surgery, up to a maximum of 100 mg.
?IV Prevention of N&V during chemotherapy.
Adults: 1.8 mg/kg as a single dose about 30 min before chemotherapy. Alternatively, a fixed dose of 100 mg can be given over 30 seconds. Children, 2 to 16 years: 1.8 mg/kg as a single dose about 30 min before chemotherapy, up to a maximum of 100 mg.
Prevention of postoperative N&V.
Adults: 12.5 mg given as a single dose. Children, 2 to 16 years: 0.35 mg/kg, up to a maximum of 12.5 mg. For adults and children, give about 15 min before cessation of anesthesia or as soon as nausea and vomiting presents.

Note: For children, injection may be mixed with apple or apple-grape juice and used for oral dosing. When injection is used PO, recommended dose for prevention of cancer chemotherapy N&V is 1.8 mg/kg (up to a maximum of 100 mg) and dose for prevention of postoperative N&V is 1.2 mg/kg (up to a maximum of 100 mg). Diluted injection may be kept up to 2 hr at room temperature before use.

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