Trade Names:Anagrelide- Capsules 1 mg
Trade Names:Agrylin- Capsules 0.5 mgGen-Anagrelide (Canada)PMS-Anagrelide (Canada)Sandoz Anagrelide (Canada)
Studies support a hypothesis of dose-related reduction in platelet production resulting from a decrease in megakaryocyte hypermaturation.
Food decreased C max 14% but increased AUC 20%.
Two major metabolites (RL603 and 3-hydroxyanagrelide).
More than 70% of dose recovered in urine. Plasma t ½ is 1.3 h.
AUC increased 8-fold with moderate hepatic function impairment.
Thrombocythemia (caused by myeloproliferative disorders) to reduce elevated platelet count and risk of thrombosis events; to relieve associated symptoms, including thrombohemorrhagic events.
Severe hepatic function impairment.
PO 0.5 mg 4 times daily or 1 mg twice daily for at least 7 days. Titrate to minimum effective dose to reduce and maintain platelet count less than 600,000/mcL. Avoid dosage increases more than 0.5 mg/day in any 1 wk period (max, 10 mg/day or 2.5 mg/dose).Children (initial dose)
PO 0.5 mg/day for at least 7 days. Titrate to minimum effective dose to reduce and maintain platelet count less than 600,000/mcL. Avoid dosage increases more than 0.5 mg/day in any 1 wk period (max, 10 mg/day or 2.5 mg/dose).Hepatic Function ImpairmentAdults and children (initial dose)
PO 0.5 mg/day for at least 7 days. Avoid dosage increases more than 0.5 mg/day in any 1-wk period.
Store at controlled room temperature (59° to 86°F).
Anagrelide plasma concentrations, theoretically, may be elevated, increasing the pharmacologic effects and adverse reactions.CYP1A2 substrates (eg, theophylline)
Plasma levels of drugs metabolized by CYP1A2 may be elevated, theoretically increasing the pharmacologic effects and adverse reactions.Cyclic AMP PDE III substrates (eg, cilostazol, milrinone)
Because anagrelide inhibits cyclic AMP PDE III, the effects of drugs that are substrates for cyclic AMP PDE III theoretically may be exacerbated.Sucralfate
May reduce the oral absorption of anagrelide.
None well documented.
Palpitations (26%); chest pain, tachycardia (8%); angina pectoris, arrhythmia, CV disease, heart failure, hemorrhage, hypertension, postural hypotension, syncope, thrombosis, vasodilation (1% to less than 5%).
Headache (44%); asthenia (23%); dizziness (15%); paresthesia (6%); amnesia, confusion, depression, insomnia, nervousness, somnolence (1% to less than 5%).
Rash (including urticaria [8%]); pruritus (6%); alopecia, skin disease (1% to less than 5%).
Pharyngitis (7%); abnormal vision, amblyopia, diplopia, epistaxis, rhinitis, tinnitus, visual field abnormality (1% to less than 5%).
Diarrhea (26%); nausea (17%); abdominal pain (16%); flatulence, vomiting (10%); anorexia (8%); dyspepsia (5%); aphthous stomatitis, constipation, eructation, gastritis, GI distress or hemorrhage, melena (1% to less than 5%).
Dysuria, hematuria (1% to less than 5%).
Anemia, ecchymosis, lymphadenopathy, thrombocytopenia (1% to less than 5%).
Elevated liver enzymes (1% to less than 5%).
Edema (21%); peripheral edema (9%); dehydration (1% to less than 5%).
Back pain (6%); arthralgia, leg cramps, myalgia (1% to less than 5%).
Dyspnea (12%); cough (6%); asthma, bronchitis, pneumonia, respiratory disease, sinusitis (1% to less than 5%).
Pain (15%); fever (9%); malaise (6%); chills, flu-like symptoms, photosensitivity (1% to less than 5%).
Evaluate platelet counts every 2 days during first week of treatment and then at least weekly thereafter until maintenance dosage is reached. Frequently monitor blood counts (WBC, hemoglobin), liver function (liver enzymes), and renal function (serum creatinine, BUN) while platelet count is being lowered (usually during first 2 wk of treatment). Closely monitor patients with known or suspected heart disease, renal insufficiency, or hepatic function impairment.
Category C .
Safety and efficacy not established for patients younger than 6 yr of age.
Use with caution; closely monitor patients.
Contraindicated in patients with severe hepatic function impairment. Assess potential benefits vs risk of therapy in patients with mild to moderate hepatic function impairment; dose reduction required in patients with moderate hepatic function impairment; carefully monitor patients for CV effects.
Use with caution in patients with known or suspected heart disease. May cause vasodilation, tachycardia, palpitations, and heart failure. Evaluate CV status before starting therapy and carefully monitor patients during treatment.
May occur but promptly recovers upon discontinuation of therapy.
Thrombocytopenia, which potentially can cause bleeding, and cardiac and CNS toxicity.
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