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Anagrelide

 
Oncology Encyclopedia: Anagrelide
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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.

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Drug Info: Anagrelide
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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.

Wikipedia: Anagrelide
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Anagrelide
Systematic (IUPAC) name
6,7-dichloro-1,5-dihydroimidazo
(2,1-b)quinazolin-2(3H)-one
Identifiers
CAS number 68475-42-3
ATC code L01XX35
PubChem 2182
DrugBank APRD00798
ChemSpider 2097
Chemical data
Formula C10H7Cl2N3O 
Mol. mass 256.088 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life 1.3 hours
Excretion  ?
Therapeutic considerations
Pregnancy cat.

?
Legal status

℞ Prescription only
Routes Oral
 Yes check.svgY(what is this?)  (verify)

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. [1]

Contents

Mechanism

It 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]

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.[4]

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. [5]

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, anegralide should be not generally be considered for first line therapy in ET.

References

  1. ^ 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. 
  2. ^ 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. 
  3. ^ PMID 3027338
  4. ^ 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.
  5. ^ http://www.ncbi.nlm.nih.gov/pubmed/19364963?itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsPanel.Pubmed_RVDocSum&ordinalpos=1, J Clin Oncol. 2009 Jun 20;27(18):2991-9. Reticulin accumulation in essential thrombocythemia: prognostic significance and relationship to therapy. Campbell PJ, Bareford D, Erber WN, Wilkins BS, Wright P, Buck G, Wheatley K, Harrison CN, Green AR.

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This entry is from Wikipedia, the leading user-contributed encyclopedia. It may not have been reviewed by professional editors (see full disclaimer)

 
 
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Oncology Encyclopedia. Gale Encyclopedia of Cancer. Copyright © 2006 by The Gale Group, Inc. All rights reserved.  Read more
Drug Info. Gold Standard. Copyright © 2008 by Gold Standard. All rights reserved.  Read more
Wikipedia. This article is licensed under the Creative Commons Attribution/Share-Alike License. It uses material from the Wikipedia article "Anagrelide".  Read more