anagrelide (Agrylin)
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Introduction
Tradename: Agrylin.
Indications
Dosage
Tabs: 0.5 & 1 mg.
Pharmacokinetics
- bioavailability modestly reduced by food (13%)
- metabolized extensively in liver
- metabolites excreted in the urine
- elimination 1/2 life 1.3-1.8 hours
elimination via liver
elimination via kidney
1/2life = 1.3-1.8 hours
Monitor
- serum AST & serum ALT[4]
- while the platelet count is being lowered (usually during the 1st 2 weeks of therapy)
- at least monthly in patients with hepatic insufficiency
Adverse effects
- headache 44%
- palpitations 26%
- diarrhea 26%
- asthenia 23%
- edema 21%
- nausea 17%
- abdominal pain 16%
- dizziness 15%
- other pain 15%
- dyspnea 12%
- flatulence 10%
- vomiting 10%
- fever 9%
- peripheral edema 8%
- rash, including urticaria 8%
- chest pain 8%
- anorexia 8%
- tachycardia 8%
- pharyngitis 7%
- malaise 6%
- cough 6%
- paresthesias 6%
- back pain 6%
- pruritus 6%
- dyspepsia 5%
- mulitiple other adverse effects (< 5%)
Mechanism of action
- still under investigation
- inhibits maturation of megakaryocytes
- inhibits ADP & collagen induced platelet aggregation
- platelet aggregation inhibited at doses higher than those requires to reduce platelet count
- inhibits cAMP phosphodiesterase
More general terms
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
- ↑ 4.0 4.1 Prescriber's Letter 17(7): 2010 Recommended Lab Monitoring for Common Medications Liver Function Test Scheduling Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=260704&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 5.0 5.1 Deprecated Reference