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Bosentan

 
Drug Info: Bosentan

Brand names: Tracleer™

Chemical formula:



Bosentan Oral tablet

What is this medicine?

BOSENTAN (boe SEN tan) is used to treat a serious heart and lung disorder called primary pulmonary hypertension. This medicine may help to increase your ability to exercise and improve your breathing.
 
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:
•liver disease
•an unusual or allergic reaction to bosentan, 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. You can take this medicine with or without food. Take your doses at regular intervals. Do not take more often than directed. Do not stop taking except on your doctor's advice.

A special MedGuide will be given to you by the pharmacist with each prescription and refill. Be sure to read this information carefully each time.

Talk to your pediatrician regarding the use of this medicine in children. Special care may be needed.

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?

Do not take this medicine with any of the following medications:
•cyclosporine
•female hormones, like estrogens or progestins and birth control pills, patches, rings, or injections
•glyburide
•ritonavir
 
This medicine may also interact with the following medications:
•amiodarone
•amprenavir
•certain medicines for fungal infections like fluconazole, itraconazole or ketoconazole
•certain medicines for high cholesterol like atorvastatin, cerivastatin, lovastatin, simvastatin
•diltiazem
•erythromycin
•rifampicin
•sildenafil
•tacrolimus
 
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 checks on your progress. Despite receiving this medicine, your condition may worsen and you may need your dose adjusted. Call your doctor or health care professional if your conditions gets worse.
 
Pregnancy must be avoided while taking this medicine due to the potential for serious side effects to an unborn child. If you are female of child-bearing potential, you will have to have pregnancy tests regularly (at least monthly) while you are taking this medicine. Discuss options to prevent pregnancy with your physician. This medicine may reduce the effectiveness of hormonal birth control methods, including birth control pills, patches, implanted hormonal products, or injections.
 
This medicine has caused reduced sperm counts in some men. This may interfere with the ability to father a child. You should talk to your doctor or health care professional if you are concerned about your fertility.
 
Your health care professional will have to check blood tests regularly (at least monthly) to check the effect of this medicine on your liver.

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
•cool, pale skin
•dark urine
•fast, irregular heartbeat
•feeling faint or lightheaded, falls
•fever
•swelling of the ankles or legs
•stomach pain, nausea, vomiting
unusual bleeding or bruising
•unusually weak or tired
•yellowing of eyes or skin

Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
•flushing of the skin
•headache
•itching of the skin
•runny nose or sore throat
•stomach upset

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). 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.

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Wikipedia: Bosentan
Top
Bosentan
Systematic (IUPAC) name
4-tert-butyl-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-(pyrimidin-2-yl)pyrimidin-4-yl]benzene-1-sulfonamide
Identifiers
CAS number 147536-97-8
ATC code C02KX01
PubChem 104865
DrugBank APRD00829
ChemSpider 94651
Chemical data
Formula C27H29N5O6S 
Mol. mass 551.614 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability 50%
Protein binding >98%
Metabolism Hepatic
Half life 5 hours
Excretion  ?
Therapeutic considerations
Pregnancy cat.

X

Legal status

Prescription only

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

Bosentan (BOZENTAN) is a dual endothelin receptor antagonist important in the treatment of pulmonary artery hypertension (PAH). It is licensed in the United States, the European Union and other countries by Actelion Pharmaceuticals for the management of PAH under the trade name Tracleer.

Contents

Mechanism of action

Bosentan is a competitive antagonist of endothelin-1 at the endothelin-A (ET-A) and endothelin-B (ET-B) receptors. Under normal conditions, endothelin-1 binding of ET-A or ET-B receptors causes pulmonary vasoconstriction. By blocking this interaction, bosentan decreases pulmonary vascular resistance. Bosentan has a slightly higher affinity for ET-A than ET-B.

Clinical uses

Bosentan is indicated mainly for the treatment of pulmonary hypertension. In 2007, Tracleer (bosentan) was approved in the European Union also for reducing the number of new digital ulcers in patients with systemic sclerosis and ongoing digital ulcer disease.

In the United States, Tracleer® is indicated for the treatment of pulmonary arterial hypertension (WHO Group I) in patients with WHO Class II-IV symptoms, to improve exercise capacity and decrease the rate of clinical worsening.[1]

External links

See also

References

  1. ^ http://www.tracleer.com/pdf/09%20276%2001%2000%200809_Tra%20PI_4%20Pg_081409pdf.pdf
  • Tracleer Prescribing Information [1] available in PDF format.

Cipla ltd also markets bosentan as bosenta & bozena in 62.5mg and 125mg


 
 
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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 "Bosentan" Read more