Anagrelide: Indication, Dosage, Side Effect, Precaution

Generic Medicine Info Patient Medicine Information

This information is not country-specific. Please refer to the Indonesia prescribing information.

Generic Medicine Info

Indications and Dosage

Oral
Essential thrombocythemia

Adult: Initially, 1 mg daily in 2 divided doses, increase dose after at least 1 wk by not more than 0.5 mg at wkly intervals until platelet count is in normal range. Maintenance: 1-3 mg daily. Max: 10 mg daily (max single dose: 2.5 mg).
Child: ≥7 yr Initially, 0.5 mg daily for 1 wk, adjust by increments of 0.5 mg at wkly intervals until platelet count is in normal range. Maintenance: 1-3 mg daily. Max: 10 mg daily (max single dose: 2.5 mg).

Renal Impairment

Moderate to severe (CrCl <50 mL/min): Contraindicated.

Hepatic Impairment

Moderate to severe: Contraindicated.

Administration

May be taken with or without food.

Contraindications

Moderate to severe hepatic and renal (CrCl <50 mL/min) impairment.

Special Precautions

Patient w/ CV disease (e.g. those w/ risk factors for prolongation of QT interval). Childn. Pregnancy and lactation.

Adverse Reactions

GI disturbances, tachycardia, palpitations, anaemia, dizziness, headache, fatigue, fluid retention, rash, GI haemorrhage, pancreatitis, chest pain, anorexia, CHF, arrhythmias, HTN, syncope, blood disorders, haemorrhage, dyspnoea, ecchymosis, pneumonia, pleural effusion, sleep disturbances, epistaxis, paraesthesia, hypoaesthesia, nervousness, depression, amnesia, confusion, dry mouth, wt changes, impotence, oedema, myalgia, arthralgia, back pain, alopecia, skin discolouration, fever, pruritus, malaise; Torsade de pointes, interstitial lung disease, tubulointerstitial nephritis, hepatitis. Rarely, colitis, gingival bleeding, gastritis, postural hypotension, MI, angina, vasodilatation, cardiomyopathy, cardiomegaly, pericardial effusion, pulmonary HTN and infiltrates, somnolence, migraine, impaired coordination, dysarthria, asthenia, renal failure, nocturia, visual disturbances, dry skin, tinnitus.

Pregnancy Category (US FDA)

PO: C

Patient Counseling Information

This drug may cause dizziness, if affected, do not drive or operate machinery.

Monitoring Parameters

Assess and monitor cardiac function before and during treatment. Closely monitor platelet counts esp at the start of the treatment. Monitor Hb, WBC, renal and hepatic function.

Overdosage

Symptoms: Hypotension, sinus tachycardia, vomiting. Management: Supportive treatment.

Drug Interactions

May exacerbate effects of PDE III inhibitors (e.g. cilostazol, amrinone). May potentiate effects of other drugs that modify platelet function (e.g. acetylsalicylic acid). Enhanced QTc-prolonging effect w/ drugs that prolong QT interval (e.g. amiodarone, pimozide).

Food Interaction

Grapefruit juice may decrease clearance of anagrelide.

Action

Description:
Mechanism of Action: Anagrelide is a cyclic adenosine monophosphate (cAMP) phosphodiesterase (PDE) III inhibitor which reduces platelet production and inhibits platelet aggregation at high concentrations.
Pharmacokinetics:
Absorption: Well absorbed from the GI tract. Time to peak plasma concentration: Approx 1 hr.
Distribution: Extensively distributed into large peripheral compartment. Crosses the placenta.
Metabolism: Extensively metabolised by CYP1A2 isoenzyme to form 3-hydroxyanagrelide.
Excretion: Via urine (<1% as unchanged drug, >70% as metabolites); faeces (approx 10%). Plasma half-life: Approx 1.3 hr.

Chemical Structure

Storage

Store at 25°C. Protect from light.

MIMS Class

Anticoagulants, Antiplatelets & Fibrinolytics (Thrombolytics)

ATC Classification

L01XX35 - anagrelide ; Belongs to the class of other antineoplastic agents. Used in the treatment of cancer.

References

Anagrelide Hydrochloride Capsule (IVAX Pharmaceuticals, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 27/10/2015.

Anon. Anagrelide. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 27/10/2015.

Buckingham R (ed). Anagrelide Hydrochloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 27/10/2015.

Joint Formulary Committee. Anagrelide. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 27/10/2015.

McEvoy GK, Snow EK, Miller J et al (eds). Anagrelide Hydrochloride. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 27/10/2015.

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