Anagrelide
Gale Encyclopedia of Cancer:
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Anagrelide
Key Terms: Platelets.
Definition
Anagrelide, also known by the brand name Agrylin, is used to treat patients with thrombocytosis, a condition in which patients have too many platelet cells in their blood. Platelets are a cell type formed in the bone marrow that are involved in the blood clotting process.
Purpose and Description
Anagrelide reduces the platelet count in patients with blood disorders.
Recommended Dosage
Adult patients taking anagrelide should receive 0.5 mg of the drug four times daily or one mg twice daily. Based on the response to therapy, the dose of anagrelide can be increased by 0.5 mg per day every seven to 14 days if necessary. The goal is to maintain platelets at a count of less than 600,000 at the lowest dose of the drug possible to keep side effects at a minimum.
Precautions
Patients with heart disease should be given anagrelide with caution. Anagrelide should be given with caution, if at all, in patients taking drugs that affect platelet aggregations such as aspirin, clopidrogel, ticlopodine, or non-steroidal agents.
Pregnant mothers should be warned that anagrelide administration may cause fetal abnormalities. Pregnant patients should consult their physician about the current state of knowledge regarding risks and alternatives before beginning administration of anagrelide. Female patients of childbearing age should attempt to avoid pregnancy while taking this drug. Mothers who are nursing should discontinue nursing while taking this drug.
Side Effects
The most common side effects of anagrelide are palpitations, fluid gain resulting in swelling, headaches, dizziness, diarrhea, stomach discomfort, mild to moderate nausea, passing gas, weakness, shortness of breath, and decreased platelets. Less common side effects of anagrelide include increased heart rate and chest pain, malaise, rash, vomiting, and decreased appetite. As with all medications, patients should contact their physician or nurse if any of these side effects occur.
Interactions
There are no proven interactions between anagrelide and other drugs. The drug sucralfate may interfere with the absorption of anagrelide. Prior to starting any over-the-counter medications, herbal medications, or new medications, patients should consult their physician, nurse, or pharmacist to prevent drug interactions.
—Michael Zuck, Ph.D.
Drug Info:
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Anagrelide
Brand names: Agrylin®
Chemical formula:
Anagrelide Hydrochloride Oral capsule
What is this medicine?
ANAGRELIDE (an AG re lide) is used to lower platelet counts. This helps to prevent blood clots from forming. It also reduces the risk of problems like intestinal bleeding, stroke, and heart attack caused by having too many platelets.
This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.
What should I tell my health care provider before I take this medicine?
They need to know if you have any of these conditions:
•heart disease
•kidney disease
•liver disease
•an unusual or allergic reaction to anagrelide, other medicines, foods, dyes, or preservatives
•pregnant or trying to get pregnant
•breast-feeding
How should I use this medicine?
Take this medicine by mouth with a glass of water. Follow the directions on the prescription label. Take your medicine at regular intervals. Do not take your medicine more often than directed. Do not stop taking except on the advice of your doctor or health care professional.
Talk to your pediatrician regarding the use of this medicine in children. While this medicine may be prescribed for children as young as 7 years of age for selected conditions, precautions do apply.
Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.
What may interact with this medicine?
•aspirin and aspirin-like drugs
•cilostazol
•fluvoxamine
•medicines called inotropes like milrinone, enoximone, amrinone, and olprinone
•medicines that treat or prevent blood clots like warfarin
•sucralfate
•theophylline
This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.
What should I watch for while using this medicine?
Visit your doctor or health care professional for regular checks on your progress.
This medicine can make you more sensitive to the sun. Keep out of the sun. If you cannot avoid being in the sun, wear protective clothing and use sunscreen. Do not use sun lamps or tanning beds/booths.
What side effects may I notice from receiving this medicine?
Side effects that you should report to your doctor or health care professional as soon as possible:
•allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
•blood in urine
•breathing problems
•chest pain or tightness
•irregular heartbeat
•seizures
•trouble passing urine or change in the amount of urine
•unusual bleeding or bruising
•unusual swelling
•unusually weak or tired
Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
•abdominal pain
•back pain
•diarrhea
•gas
•headache
•loss of appetite
•nausea, vomiting
This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
Where should I keep my medicine?
Keep out of the reach of children.
Store at room temperature between 15 and 30 degrees C (59 and 86 degrees F). Protect from light. Throw away any unused medicine after the expiration date.
Last updated: 7/1/2002
Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.
Oxford A-Z of Medicinal Drugs:
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anagrelide
A drug used in the treatment of thrombocythaemia, a disorder marked by excess proliferation of platelet-forming cells resulting in abnormalities in blood clotting. It works by inhibiting the formation of platelets. Anagrelide is available as capsules on prescription only.
Side effects:
include headache, diarrhoea, unusual weakness or fatigue, hair loss, nausea, and dizziness.
Precautions:
anagrelide should not be taken by women who are pregnant or breastfeeding. It should be used with caution in people with cardiovascular disease or impaired liver or kidney function.
Interactions with other drugs:
Cilostazol should not be taken with anagrelide.
Phosphodiesterase inhibitors enoximone and milrinone should not be taken with anagrelide.
Proprietary preparation:
Xagrid.
| anaemia, anabolic steroids, amylmetacresol | |
| anakinra, analgesics, analogue |
Wikipedia on Answers.com:
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Anagrelide
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| Systematic (IUPAC) name | |
| 6,7-dichloro-1,5-dihydroimidazo (2,1-b)quinazolin-2(3H)-one |
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| Clinical data | |
| Trade names | Agrylin |
| AHFS/Drugs.com | monograph |
| MedlinePlus | a601020 |
| Pregnancy cat. | ? |
| Legal status | ℞ Prescription only |
| Routes | Oral |
| Pharmacokinetic data | |
| Half-life | 1.3 hours |
| Identifiers | |
| CAS number | 68475-42-3  |
| ATC code | L01XX35 |
| PubChem | CID 2182 |
| DrugBank | DB00261 |
| ChemSpider | 2097 |
| UNII | K9X45X0051 |
| KEGG | D07455 |
| ChEBI | CHEBI:142290 |
| ChEMBL | CHEMBL760 |
| Chemical data | |
| Formula | C10H7Cl2N3O |
| Mol. mass | 256.088 g/mol |
| SMILES | eMolecules & PubChem |
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 (what is this?) (verify) |
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Anagrelide (Agrylin/Xagrid, Shire) is a drug used for the treatment of essential thrombocytosis (ET; essential thrombocythemia), or overproduction of blood platelets. It also has been used in the treatment of chronic myeloid leukemia. [1]
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Contents
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Mechanism
Anagrelide works by inhibiting the maturation of platelets from megakaryocytes.[2] The exact mechanism of action is unclear, although it is known to be a phosphodiesterase inhibitor.[3] It is a potent (IC50 = 36nM) inhibitor of phosphodiesterase-II.[citation needed] It inhibits PDE-3 and phospholipase A2. [4]
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.[5] Anagrelide can be useful in times when hydroxyurea proves ineffective.
Side-effects
Common side effects are headache, diarrhea, unusual weakness/fatigue, hair loss, nausea and dizziness.
The same MRC trial mentioned above also analyzed the effects of anagrelide on bone marrow fibrosis, a common feature in patients with myelofibrosis. The use of anagrelide was associated with a rapid increase in the degree of reticulin deposition (the mechanism by which fibrosis occurs), when compared to those in whom hydroxyurea was used. Patients with myeloproliferative conditions are known to have a very slow and somewhat variable course of marrow fibrosis increase. This trend may be accelerated by anagrelide. Interestingly, this increase in fibrosis appeared to be linked to a drop in hemoglobin as it progressed. Fortunately, stopping the drug (and switching patients to hydroxyurea) appeared to reverse the degree of marrow fibrosis. Thus, patients on anagrelide may need to be monitored on a periodic basis for marrow reticulin scores, especially if anemia develops, or becomes more pronounced if present initially. [6]
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.
Due to these issues, anagrelide should not generally be considered for first line therapy in ET.
References
- ^ Voglová J, Maisnar V, Beránek M, Chrobák L (2006). "[Combination of imatinib and anagrelide in treatment of chronic myeloid leukemia in blastic phase]" (in Czech). Vnitr̆ní lékar̆ství 52 (9): 819–22. PMID 17091608.
- ^ Petrides PE (2006). "Anagrelide: what was new in 2004 and 2005?". Semin. Thromb. Hemost. 32 (4 Pt 2): 399–408. doi:10.1055/s-2006-942760. PMID 16810615.
- ^ Jones GH, Venuti MC, Alvarez R, Bruno JJ, Berks AH, Prince A (February 1987). "Inhibitors of cyclic AMP phosphodiesterase. 1. Analogues of cilostamide and anagrelide". J. Med. Chem. 30 (2): 295–303. PMID 3027338.
- ^ Harrison CN, Bareford D, Butt N, et al. (May 2010). "Guideline for investigation and management of adults and children presenting with a thrombocytosis". Br. J. Haematol. 149 (3): 352–75. doi:10.1111/j.1365-2141.2010.08122.x. PMID 20331456.
- ^ Harrison CN, Campbell PJ, Buck G, et al. (July 2005). "Hydroxyurea compared with anagrelide in high-risk essential thrombocythemia". N. Engl. J. Med. 353 (1): 33–45. doi:10.1056/NEJMoa043800. PMID 16000354.
- ^ Campbell PJ, Bareford D, Erber WN, et al. (June 2009). "Reticulin accumulation in essential thrombocythemia: prognostic significance and relationship to therapy". J. Clin. Oncol. 27 (18): 2991–9. doi:10.1200/JCO.2008.20.3174. PMID 19364963. http://www.jco.org/cgi/pmidlookup?view=long&pmid=19364963.
External links
- Shire Pharmaceuticals Agrylin/Xagrid website for international visitors
- Shire Pharmaceuticals Xagrid website for UK visitors
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Gale Encyclopedia of Cancer
Gale Encyclopedia of Cancer. Copyright © 2006 by The Gale Group, Inc. All rights reserved.
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Oxford A-Z of Medicinal Drugs
Market University Press. © 2000, 2003, 2010 An A-Z of Medicinal Drugs. All rights reserved.
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