Systemic Therapy Program
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Cancer Type

Document Type

Drug Monographs
Treatment Regimens
Scientific Name:
ANAGRELIDE
Brand Name(s):
Agrylin®

Drug Monograph

Pharmacology

Mechanism of Action

Reduces platelet counts by inhibiting the postmitotic phase of megakaryocyte development . Ploidy and size are reduced and platelet maturation is inhibited. These effects occur at concentrations considerably lower than those required for inhibition of platelet aggregation. The latter is not generally observed when anagrelide is used to treat thrombocythemia.

Pharmacokinetics

Oral Absorption:
~75%; Bioavailability is reduced by food
Distribution:
Does not accumulate in plasma after repeated administration.  Excretion in breast-milk unknown
Cross blood brain barrier? No information
Vd: 12 L/kg
PPB: no information
Metabolism:
Extensive, at least 4 metabolites have been identified: Activity of metabolites is not reported.
Excretion:
Renal; 72% to75% as metabolites, <1% unchanged ; 3% to 18% fecally
Urine >70%;  <1% unchanged
Cl  no information
t½ a 1.3 hours   t½ b: 76 hours

Side Effects

IMMEDIATE ONSET (hours to days)

• headache (45%)
• dizziness (15%), weakness (22%)
• nausea (15%)
• tachycardia

EARLY ONSET (days to weeks)

• diarrhea (25%), abdominal discomfort (17%)
• thrombocytopenia
• palpitations (26%)
• edema (20%)

DELAYED/LATE ONSET

• congestive heart disease (rare)

Therapeutics

Approved Indications

Thrombocythemia secondary to myeloproliferative disorders.

Routes

Oral

Dosing

Oral:
• Initial dose- 0.5mg po qid or 1mg po bid for 1 week
• Dose adjustment- Titrate dose to lowest level to maintain platelet count <600 (or within normal range); increase in increments no greater than 0.5mg/day each week
• Dosage should not exceed 10mg/day or 2.5mg/dose

Contraindications

• Hypersensitivity to Anagrelide • Heart disease

Monitoring

Clinical Monitoring

RECOMMENDED CRITERIA
• Baseline and periodic liver function tests [serum alkaline phosphatase, GGT, ALT, AST & Bilirubin levels (serum proteins may be added if indicated)]
• Baseline renal function tests [serum creatinine, electrolytes & BUN]
• Routine monitoring of platelet levels

SUGGESTED CRITERIA
• If patient has known or suspected heart disease: baseline & periodic cardiovascular examination and monitoring

Significant Interactions

Platelet aggregation affecting drugs (eg, aspirin, NSAID’s, clopidogrel, ticlopidine), anticoagulants, sucralfate, thrombolytic agents.

Product Information

Commercial Product Description

White capsules with 0.5mg Anagrelide.

Pharmaceutical Considerations

Tablet
0.5 mg; inactive ingredient includes lactose. Store at room temperature.  Protect from light.

Handling Risk Level

Pregnancy CPOSSIBLE HAZARDOUS DRUG
FDA Pregnancy Risk Factor C

  • Consider handling this drug using precuations outlined in CCNS Policies for Occupational Safety, Preparing Cancer Chemotherapy and Administering Cancer Chemotherapy

Note

HANDLING RISK LEVEL:
HAZARD RISK LEVEL 3
FDA Pregnancy Risk Factor C
• Consider handling this drug using precuations outlined in CCNS Policies for Preparing Cancer Chemotherapy and Administering Cancer Chemotherapy and the CCNS Standard for Oral Systemic Therapy for Cancer
Go to "Additional Information" tab (above) for links to CCNS Policies

Availability & Funding

Administrative Information (Nova Scotia)

• CCNS Provincial Formulary Status- Community Level • Take Home Prescription • CDHA Formulary Status: Non-Formulary • Pharmacare Formulary Status: Non-Formulary • Go to "Additional Information" tab (above) for links to Provincial Formulary of Cancer Drugs