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anagrelide (Agrylin)
Tradename: Agrylin.
Indications:
1) myeloproliferative disorder [5]
a) chronic myelogenous leukemia
b) polycythemia vera
2) essential thrombocythemia
Dosage:
1) start 0.5 mg PO QID,
2) after 1 week, adjust to lowest effective dose
3) maximum: 10 mg/day
Tabs: 0.5 & 1 mg.
Pharmacokinetics:
1) bioavailability modestly reduced by food (13%)
2) metabolized extensively in liver
3) metabolites excreted in the urine
4) elimination 1/2 life 1.3-1.8 hours
Monitor:
- serum AST & serum ALT [4]
a) while the platelet count is being lowered (usually during the 1st 2 weeks of therapy)
b) at least monthly in patients with hepatic insufficiency
Adverse effects:
1) headache 44%
2) palpitations 26%
3) diarrhea 26%
4) asthenia 23%
5) edema 21%
6) nausea 17%
7) abdominal pain 16%
8) dizziness 15%
9) other pain 15%
10) dyspnea 12%
11) flatulence 10%
12) vomiting 10%
13) fever 9%
14) peripheral edema 8%
15) rash, including urticaria 8%
16) chest pain 8%
17) anorexia 8%
18) tachycardia 8%
19) pharyngitis 7%
20) malaise 6%
21) cough 6%
22) paresthesias 6%
23) back pain 6%
24) pruritus 6%
25) dyspepsia 5%
26) mulitiple other adverse effects (< 5%)
Mechanism of action:
1) still under investigation
2) inhibits maturation of megakaryocytes
3) inhibits ADP & collagen induced platelet aggregation
-> platelet aggregation inhibited at doses higher than those requires to reduce platelet count
4) inhibits cAMP phosphodiesterase
Interactions
drug interactions
drug adverse effects (more general classes)
General
antiplatelet agent
thrombocytosis agent
Properties
MISC-INFO: elimination route LIVER
KIDNEY
1/2life 1.3-1.8 HOURS
pregnancy-category C
safety in lactation ?
Database Correlations
PUBCHEM correlations
References
- The Pharmacological Basis of Therapeutics, 9th ed.
Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- Medical Knowledge Self Assessment Program (MKSAP) 11, American
College of Physicians, Philadelphia 1998
- Physician's Desk Reference (PDR) 52nd edition, Medical
Economics, 1998
- Prescriber's Letter 17(7): 2010
Recommended Lab Monitoring for Common Medications
Liver Function Test Scheduling
Detail-Document#: 260704
(subscription needed) http://www.prescribersletter.com
- Deprecated Reference