Anagrelide


Concise Prescribing Info
Indications/Uses
Essential thrombocythemia.
Dosage/Direction for Use
Adult : PO Initial: 1 mg/day in 2 divided doses, increase dose after at least 1 wk by not more than 0.5 mg at wkly intervals. Maintenance: 1-3 mg/day. Max: 10 mg/day (max single dose: 2.5 mg).
Dosage Details
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.
Patient Counseling Information
This drug may cause dizziness, if affected, do not drive or operate machinery.
MonitoringParameters
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: 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

Chemical Structure Image
Anagrelide

Source: National Center for Biotechnology Information. PubChem Database. Anagrelide, CID=135409400, https://pubchem.ncbi.nlm.nih.gov/compound/Anagrelide (accessed on Jan. 20, 2020)

Storage
Store at 25°C. Protect from light.
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.

Disclaimer: This information is independently developed by MIMS based on Anagrelide from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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