Anagrelide

Structural formula
General
Non-proprietary name	Anagrelide
other names	6,7-dichloro-1,5-dihydroimidazo [2,1- b ] quinazolin-2-one
Molecular formula	C 10 H 7 Cl 2 N 3 O
External identifiers / databases
CAS number 68475-42-3 58579-51-4 ( hydrochloride ) PubChem 2182 ChemSpider 2097 DrugBank DB00261 Wikidata Q408163
Drug information
ATC code	L01 XX35
Drug class	Cytostatic
properties
Molar mass	256.09 g · mol -1
Melting point	> 280 ° C (as hydrochloride)
safety instructions
Please note the exemption from the labeling requirement for drugs, medical devices, cosmetics, food and animal feed GHS hazard labeling no classification available
As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Anagrelide is a drug from the group of imidazolidine compounds. Anagrelide reduces the number of platelets produced in the bone marrow, thereby reducing the number of platelets in the blood to a normal level. It is used in the therapy of thrombocytoses that occur in patients with myeloproliferative diseases such as essential thrombocythemia (ET), polycythemia vera (PV), chronic myeloid leukemia (CML) or osteomyelofibrosis (OMF).

Mechanism of action

After the drug was originally ascribed an inhibitory effect on the clumping of blood platelets ( platelet aggregation inhibition ), clinical studies have shown that the substance has no effect on platelet function, but nevertheless leads to a rapid decrease in the platelet count in the blood. The exact mechanism by which it works is still unclear. It is known, however, that anagrelide the cAMP - phosphodiesterase inhibits type third Based on studies in cell cultures, it is discussed that the substance works in the precursor cells of platelets ( megakaryocytes ) by slowing their maturation and reducing their size and ploidy .

Side effects

• common: headache, dizziness, tiredness, heavy heartbeat, nausea, diarrhea, anemia

Therapy requires clinical monitoring of the patient for blood count , kidney and liver function. In the post-marketing setting, serious cardiovascular side effects have been observed in patients with no suspected heart disease who had normal findings on pre-treatment cardiovascular exams. Anagrelide should be used with caution in patients of all ages with known or suspected heart disease and is intended as a second-line therapy in high-risk patients .

Comparison of anagrelide versus hydroxycarbamide

A study published in the "New England Journal of Medicine" in 2005 suggests that anagrelide is inferior to the reference substance hydroxycarbamide : Over 800 people with essential thrombocythemia who are at high risk due to a high platelet count (over 1 million / µl) and other criteria for vascular complications, they received low-dose acetylsalicylic acid (ASA) from 75 to 100 mg either anagrelide or hydroxycarbamide.

After an observation period of more than 3 years - with a comparable reduction in platelet count - 14% of the anagrelide group and only 9% of the hydroxycarbamide group had suffered arterial or venous thrombosis or serious bleeding. The dropout rate in the anagrelide group was also higher. Transformation into osteomyelofibrosis was also significantly more common with anagrelide . However, the study mentioned has come under fire due to methodological inaccuracies and the results of further ongoing studies should be awaited.

Trade names

Monopreparations

Agrylin (USA, CDN), Thromboreductin (AT, PL, HU, CH, RO, CZ, SK, LT, LV), Xagrid (D, CH)

Web links

• Public Assessment Report (EPAR) of the European Medicines Agency (EMA) for: Anagrelide

literature

• MN Silverstein et al. In: N. Eng. J. Med. , 1988, 318, p. 1292.
• RM Petitt et al. In: Semin. Hematol. , 1997, 34, p. 51.
• New England Journal of Medicine , July 7, 2005; 353, pp. 33-45

Individual evidence

1. ↑ Entry on anagrelide. In: Römpp Online . Georg Thieme Verlag, accessed on May 30, 2014.
2. ↑ This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.
3. ↑ Xagrid. Summary of Product Characteristics. (PDF; 133 kB) European Medicines Agency, November 2009; Retrieved March 13, 2010.
4. ^ MD Oertel: Anagrelide, a selective thrombocytopenic agent. In: American Journal of Health-System Pharmacy , Volume 55, Number 19, October 1998, pp. 1979-1986, PMID 9784784
5. ↑ Red Hand Letter from Shire in February 2013. (PDF; 517 kB) Retrieved February 6, 2013 . 
6. ↑ Red List , 08/2009.
7. ↑ Type of application. (PDF) Pharmazie.com
8. ↑ AGES-PharmMed (08/2009).

This article is about a health issue. It is not used for self-diagnosis and does not replace a diagnosis by a doctor. Please note the information on health issues !