Anagrelide

Anagrelide

drugbox
IUPAC_name = 6,7-dichloro-1,5-dihydroimidazo
(2,1-b)quinazolin-2(3"H")-one



CAS_number = 68475-42-3
ATC_prefix = L01
ATC_suffix = XX35
PubChem = 2182
ChemSpiderID = 2097
DrugBank = APRD00798
C = 10 | H = 7 | Cl = 2 | N = 3 | O = 1
molecular_weight = 256.088 g/mol
bioavailability =
protein_bound =
metabolism =
elimination_half-life = 1.3 hours
excretion =
pregnancy_category =
legal_status = Rx-only
routes_of_administration = Oral

Anagrelide (Agrylin/Xagrid, Shire) is a drug used for the treatment of essential thrombocytosis (ET; essential thrombocythemia). It also has been used in the treatment of chronic myeloid leukemia. cite journal |author=Voglová J, Maisnar V, Beránek M, Chrobák L |title= [Combination of imatinib and anagrelide in treatment of chronic myeloid leukemia in blastic phase] |language=Czech |journal=Vnitr̆ní lékar̆ství |volume=52 |issue=9 |pages=819–22 |year=2006 |pmid=17091608 |doi=]

Mechanism

It works by inhibiting the maturation of megakaryocytes into platelets.cite journal |author=Petrides PE |title=Anagrelide: what was new in 2004 and 2005? |journal=Semin. Thromb. Hemost. |volume=32 |issue=4 Pt 2 |pages=399–408 |year=2006 |pmid=16810615 |doi=10.1055/s-2006-942760] The exact mechanism of action is unclear, although it is known to be a potent (IC50 = 36nM) inhibitor of phosphodiesterase-III.

Uses

According to a 2005 Medical Research Council randomized trial, the combination of hydroxyurea with aspirin is superior to the combination of anagrelide and aspirin for the initial management of ET. The hydroxyurea arm had a lower likelihood of myelofibrosis, arterial thrombosis, and bleeding, but it had a slightly higher rate of venous thrombosis. [Harrison CN, Campbell PJ, Buck G, Wheatley K, East CL, Bareford D, Wilkins BS, van der Walt JD, Reilly JT, Grigg AP, Revell P, Woodcock BE, Green AR; United Kingdom Medical Research Council Primary Thrombocythemia 1 Study. Hydroxyurea compared with anagrelide in high-risk essential thrombocythemia. "N Engl J Med" 2005;353:33-45. PMID 16000354.]

ide-effects

Common side effects are headache, diarrhea, unusual weakness/fatigue, hair loss, nausea and dizziness.

Less common side effects include: congestive heart failure, myocardial infarction, cardiomyopathy, cardiomegaly, complete heart block, atrial fibrillation, cerebrovascular accident, pericarditis, pulmonary infiltrates, pulmonary fibrosis, pulmonary hypertension, pancreatitis, gastric/duodenal ulceration, renal impairment/failure and seizure.

References


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Look at other dictionaries:

  • anagrelide — noun A drug that inhibits the maturation of platelets from megakaryocytes, used in the treatment of thrombocytosis and leukaemia …   Wiktionary

  • anagrelide — anag·re·lide ə nag rə .līd n a phosphodiesterase inhibitor administered esp. in the form of its hydrochloride C10H7Cl2N3O·HCl to treat thrombocytosis because of its antiplatelet activity see agrylin …   Medical dictionary

  • anagrelide — A drug that is used to decrease the number of platelets in the blood in order to prevent blood clotting …   English dictionary of cancer terms

  • anagrelide hydrochloride — an·ag·re·lide hy·dro·chlo·ride (an agґrə līd) an agent used to reduce elevated platelet counts and the risk of thrombosis in the treatment of hemorrhagic thrombocythemia; administered orally …   Medical dictionary

  • ANG — anagrelide; angiogenin; angiogram, angiography; angiotensin …   Medical dictionary

  • ANG — • anagrelide; • angiogenin; • angiogram, angiography; • angiotensin …   Dictionary of medical acronyms & abbreviations

  • Essential thrombocytosis — DiseaseDisorder infobox Name = Essential thrombocytosis ICD10 = ICD10|D|75|2|d|70, ICD10|D|47|3|d|37 ICD9 = ICD9|238.71 ICDO = 9962/3 Caption = OMIM = 187950 DiseasesDB = 4522 MedlinePlus = 000543 eMedicineSubj = med eMedicineTopic = 2266 MeshID …   Wikipedia

  • Phosphodiesterase inhibitor — A phosphodiesterase inhibitor is a drug that blocks one or more of the five subtypes of the enzyme phosphodiesterase (PDE), therefore preventing the inactivation of the intracellular second messengers cyclic adenosine monophosphate (cAMP) and… …   Wikipedia

  • Thrombocytosis — Infobox Disease Name = PAGENAME Caption = DiseasesDB = 27591 ICD10 = ICD9 = ICD9|289.9 ICDO = OMIM = MedlinePlus = eMedicineSubj = med eMedicineTopic = 2267 eMedicine mult = eMedicine2|ped|2238 MeshID = Thrombocytosis is the presence of high… …   Wikipedia

  • Анагрелид — В этой статье не хватает ссылок на источники информации. Информация должна быть проверяема, иначе она может быть поставлена под сомнение и удалена. Вы можете …   Википедия

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