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Tracleer
Overview
What is Tracleer?
Tracleer is the proprietary name for bosentan, an endothelin receptor antagonist that belongs to a class of highly substituted pyrimidine derivatives, with no chiral centers. It is designated chemically as 4-tert-butyl-N-[6-(2-hydroxy-ethoxy)-5-(2-methoxy-phenoxy)-[2,2´]-bipyrimidin-4-yl]- benzenesulfonamide monohydrate and has the following structural formula:
Bosentan has a molecular weight of 569.64 and a molecular formula of CHNOS∙HO. Bosentan is a white to yellowish powder. It is poorly soluble in water (1.0 mg/100 mL) and in aqueous solutions at low pH (0.1 mg/100 mL at pH 1.1 and 4.0; 0.2 mg/100 mL at pH 5.0). Solubility increases at higher pH values (43 mg/100 mL at pH 7.5). In the solid state, bosentan is very stable, is not hygroscopic and is not light sensitive.
Tracleer is available as 62.5 mg and 125 mg film-coated tablets for oral administration, and contains the following excipients: corn starch, pregelatinized starch, sodium starch glycolate, povidone, glyceryl behenate, magnesium stearate, hydroxypropylmethylcellulose, triacetin, talc, titanium dioxide, iron oxide yellow, iron oxide red, and ethylcellulose. Each Tracleer 62.5 mg tablet contains 64.54 mg of bosentan monohydrate, equivalent to 62.5 mg of anhydrous bosentan. Each Tracleer 125 mg tablet contains 129.08 mg of bosentan monohydrate, equivalent to 125 mg of anhydrous bosentan.
Tracleer is also available as a 32 mg tablet for oral suspension and contains the following excipients: cellulose microcrystalline, calcium hydrogen phosphate anhydrous, croscarmellose sodium, silica colloidal anhydrous, tartaric acid, tutti frutti flavor, aspartame (E951) acesulfame potassium, and magnesium stearate. Each dispersible tablet contains 1.87 mg of phenylalanine. Each dispersible tablet contains 33.045 mg of bosentan monohydrate, equivalent to 32 mg anhydrous bosentan.
What does Tracleer look like?
What are the available doses of Tracleer?
62.5 mg tablets: round, biconvex, orange-white tablets, debossed with identification marking "62,5"
125 mg tablets: oval, biconvex, orange-white tablets, debossed with identification marking "125"
32 mg tablets for oral suspension: clover-shaped, quadrisected, pale yellow to off-white tablets, debossed with identification marking "32" on the side opposite the quadrisection lines
What should I talk to my health care provider before I take Tracleer?
How should I use Tracleer?
Tracleer® is indicated for the treatment of pulmonary arterial hypertension (PAH) (WHO Group 1):
Healthcare professionals who prescribe Tracleer must enroll in the Tracleer REMS Program and must comply with the required monitoring to minimize the risks associated with Tracleer
Obtain a pregnancy test in females of reproductive potential prior to Tracleer treatment, monthly during treatment and one month after stopping Tracleer. Initiate treatment with Tracleer in females of reproductive potential only after a negative pregnancy test , , .
Measure liver aminotransferase levels prior to initiation of treatment and then monthly .
What interacts with Tracleer?
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What are the warnings of Tracleer?
Sorry No Records found
What are the precautions of Tracleer?
Sorry No Records found
What are the side effects of Tracleer?
Sorry No records found
What should I look out for while using Tracleer?
Pregnancy ()
Use with Cyclosporine A ()
Use with Glyburide ()
Hypersensitivity ()
Because of the risks of hepatotoxicity and birth defects, Tracleer is available only through a restricted program called the Tracleer REMS Program. The Tracleer REMS Program is a component of the Tracleer Risk Evaluation and Mitigation Strategy (REMS). Under the Tracleer REMS, prescribers, patients, and pharmacies must enroll in the program
What might happen if I take too much Tracleer?
Bosentan has been given as a single dose of up to 2400 mg in normal volunteers, or up to 2000 mg/day for 2 months in patients, without any major clinical consequences. The most common side effect was headache of mild to moderate intensity. In the cyclosporine A interaction study, in which doses of 500 and 1000 mg twice daily of bosentan were given concomitantly with cyclosporine A, trough plasma concentrations of bosentan increased 30-fold, resulting in severe headache, nausea, and vomiting, but no serious adverse events. Mild decreases in blood pressure and increases in heart rate were observed.
In the postmarketing period, there was one reported overdose of 10,000 mg of Tracleer taken by an adolescent male patient. He had symptoms of nausea, vomiting, hypotension, dizziness, sweating, and blurred vision. He recovered within 24 hours with blood pressure support.
Bosentan is unlikely to be effectively removed by dialysis due to the high molecular weight and extensive plasma protein binding.
How should I store and handle Tracleer?
62.5 mg film-coated, round, biconvex, orange-white tablets, debossed with identification marking "62,5", packaged in a white high-density polyethylene bottle and a white polypropylene child-resistant cap or in foil blister-strips for hospital unit-dosing. NDC 66215-101-06: Bottle containing 60 tablets.NDC 66215-101-03: Carton of 30 tablets in 10 blister strips of 3 tablets.125 mg film-coated, oval, biconvex, orange-white tablets, debossed with identification marking "125", packaged in a white high-density polyethylene bottle and a white polypropylene child-resistant cap or in foil blister-strips for hospital unit-dosing. NDC 66215-102-06: Bottle containing 60 tablets. NDC 66215-102-03: Carton of 30 tablets in 10 blister strips of 3 tablets.32 mg tablets for oral suspension, pale yellow to off-white, clover-shaped, quadrisected on one side and debossed with "32" on the other side, packaged in child resistant Aluminum/Aluminum peel-push blisters.NDC 66215-103-56: Carton of 56 tablets for oral suspension in 4 blister-strips of 14 tablets.NDC 66215-103-14: Blister strip of 14 tablets for oral suspension.62.5 mg film-coated, round, biconvex, orange-white tablets, debossed with identification marking "62,5", packaged in a white high-density polyethylene bottle and a white polypropylene child-resistant cap or in foil blister-strips for hospital unit-dosing. NDC 66215-101-06: Bottle containing 60 tablets.NDC 66215-101-03: Carton of 30 tablets in 10 blister strips of 3 tablets.125 mg film-coated, oval, biconvex, orange-white tablets, debossed with identification marking "125", packaged in a white high-density polyethylene bottle and a white polypropylene child-resistant cap or in foil blister-strips for hospital unit-dosing. NDC 66215-102-06: Bottle containing 60 tablets. NDC 66215-102-03: Carton of 30 tablets in 10 blister strips of 3 tablets.32 mg tablets for oral suspension, pale yellow to off-white, clover-shaped, quadrisected on one side and debossed with "32" on the other side, packaged in child resistant Aluminum/Aluminum peel-push blisters.NDC 66215-103-56: Carton of 56 tablets for oral suspension in 4 blister-strips of 14 tablets.NDC 66215-103-14: Blister strip of 14 tablets for oral suspension.62.5 mg film-coated, round, biconvex, orange-white tablets, debossed with identification marking "62,5", packaged in a white high-density polyethylene bottle and a white polypropylene child-resistant cap or in foil blister-strips for hospital unit-dosing. NDC 66215-101-06: Bottle containing 60 tablets.NDC 66215-101-03: Carton of 30 tablets in 10 blister strips of 3 tablets.125 mg film-coated, oval, biconvex, orange-white tablets, debossed with identification marking "125", packaged in a white high-density polyethylene bottle and a white polypropylene child-resistant cap or in foil blister-strips for hospital unit-dosing. NDC 66215-102-06: Bottle containing 60 tablets. NDC 66215-102-03: Carton of 30 tablets in 10 blister strips of 3 tablets.32 mg tablets for oral suspension, pale yellow to off-white, clover-shaped, quadrisected on one side and debossed with "32" on the other side, packaged in child resistant Aluminum/Aluminum peel-push blisters.NDC 66215-103-56: Carton of 56 tablets for oral suspension in 4 blister-strips of 14 tablets.NDC 66215-103-14: Blister strip of 14 tablets for oral suspension.62.5 mg film-coated, round, biconvex, orange-white tablets, debossed with identification marking "62,5", packaged in a white high-density polyethylene bottle and a white polypropylene child-resistant cap or in foil blister-strips for hospital unit-dosing. NDC 66215-101-06: Bottle containing 60 tablets.NDC 66215-101-03: Carton of 30 tablets in 10 blister strips of 3 tablets.125 mg film-coated, oval, biconvex, orange-white tablets, debossed with identification marking "125", packaged in a white high-density polyethylene bottle and a white polypropylene child-resistant cap or in foil blister-strips for hospital unit-dosing. NDC 66215-102-06: Bottle containing 60 tablets. NDC 66215-102-03: Carton of 30 tablets in 10 blister strips of 3 tablets.32 mg tablets for oral suspension, pale yellow to off-white, clover-shaped, quadrisected on one side and debossed with "32" on the other side, packaged in child resistant Aluminum/Aluminum peel-push blisters.NDC 66215-103-56: Carton of 56 tablets for oral suspension in 4 blister-strips of 14 tablets.NDC 66215-103-14: Blister strip of 14 tablets for oral suspension.62.5 mg film-coated, round, biconvex, orange-white tablets, debossed with identification marking "62,5", packaged in a white high-density polyethylene bottle and a white polypropylene child-resistant cap or in foil blister-strips for hospital unit-dosing. NDC 66215-101-06: Bottle containing 60 tablets.NDC 66215-101-03: Carton of 30 tablets in 10 blister strips of 3 tablets.125 mg film-coated, oval, biconvex, orange-white tablets, debossed with identification marking "125", packaged in a white high-density polyethylene bottle and a white polypropylene child-resistant cap or in foil blister-strips for hospital unit-dosing. NDC 66215-102-06: Bottle containing 60 tablets. NDC 66215-102-03: Carton of 30 tablets in 10 blister strips of 3 tablets.32 mg tablets for oral suspension, pale yellow to off-white, clover-shaped, quadrisected on one side and debossed with "32" on the other side, packaged in child resistant Aluminum/Aluminum peel-push blisters.NDC 66215-103-56: Carton of 56 tablets for oral suspension in 4 blister-strips of 14 tablets.NDC 66215-103-14: Blister strip of 14 tablets for oral suspension.62.5 mg film-coated, round, biconvex, orange-white tablets, debossed with identification marking "62,5", packaged in a white high-density polyethylene bottle and a white polypropylene child-resistant cap or in foil blister-strips for hospital unit-dosing. NDC 66215-101-06: Bottle containing 60 tablets.NDC 66215-101-03: Carton of 30 tablets in 10 blister strips of 3 tablets.125 mg film-coated, oval, biconvex, orange-white tablets, debossed with identification marking "125", packaged in a white high-density polyethylene bottle and a white polypropylene child-resistant cap or in foil blister-strips for hospital unit-dosing. NDC 66215-102-06: Bottle containing 60 tablets. NDC 66215-102-03: Carton of 30 tablets in 10 blister strips of 3 tablets.32 mg tablets for oral suspension, pale yellow to off-white, clover-shaped, quadrisected on one side and debossed with "32" on the other side, packaged in child resistant Aluminum/Aluminum peel-push blisters.NDC 66215-103-56: Carton of 56 tablets for oral suspension in 4 blister-strips of 14 tablets.NDC 66215-103-14: Blister strip of 14 tablets for oral suspension.62.5 mg film-coated, round, biconvex, orange-white tablets, debossed with identification marking "62,5", packaged in a white high-density polyethylene bottle and a white polypropylene child-resistant cap or in foil blister-strips for hospital unit-dosing. NDC 66215-101-06: Bottle containing 60 tablets.NDC 66215-101-03: Carton of 30 tablets in 10 blister strips of 3 tablets.125 mg film-coated, oval, biconvex, orange-white tablets, debossed with identification marking "125", packaged in a white high-density polyethylene bottle and a white polypropylene child-resistant cap or in foil blister-strips for hospital unit-dosing. NDC 66215-102-06: Bottle containing 60 tablets. NDC 66215-102-03: Carton of 30 tablets in 10 blister strips of 3 tablets.32 mg tablets for oral suspension, pale yellow to off-white, clover-shaped, quadrisected on one side and debossed with "32" on the other side, packaged in child resistant Aluminum/Aluminum peel-push blisters.NDC 66215-103-56: Carton of 56 tablets for oral suspension in 4 blister-strips of 14 tablets.NDC 66215-103-14: Blister strip of 14 tablets for oral suspension.62.5 mg film-coated, round, biconvex, orange-white tablets, debossed with identification marking "62,5", packaged in a white high-density polyethylene bottle and a white polypropylene child-resistant cap or in foil blister-strips for hospital unit-dosing. NDC 66215-101-06: Bottle containing 60 tablets.NDC 66215-101-03: Carton of 30 tablets in 10 blister strips of 3 tablets.125 mg film-coated, oval, biconvex, orange-white tablets, debossed with identification marking "125", packaged in a white high-density polyethylene bottle and a white polypropylene child-resistant cap or in foil blister-strips for hospital unit-dosing. NDC 66215-102-06: Bottle containing 60 tablets. NDC 66215-102-03: Carton of 30 tablets in 10 blister strips of 3 tablets.32 mg tablets for oral suspension, pale yellow to off-white, clover-shaped, quadrisected on one side and debossed with "32" on the other side, packaged in child resistant Aluminum/Aluminum peel-push blisters.NDC 66215-103-56: Carton of 56 tablets for oral suspension in 4 blister-strips of 14 tablets.NDC 66215-103-14: Blister strip of 14 tablets for oral suspension.62.5 mg film-coated, round, biconvex, orange-white tablets, debossed with identification marking "62,5", packaged in a white high-density polyethylene bottle and a white polypropylene child-resistant cap or in foil blister-strips for hospital unit-dosing. NDC 66215-101-06: Bottle containing 60 tablets.NDC 66215-101-03: Carton of 30 tablets in 10 blister strips of 3 tablets.125 mg film-coated, oval, biconvex, orange-white tablets, debossed with identification marking "125", packaged in a white high-density polyethylene bottle and a white polypropylene child-resistant cap or in foil blister-strips for hospital unit-dosing. NDC 66215-102-06: Bottle containing 60 tablets. NDC 66215-102-03: Carton of 30 tablets in 10 blister strips of 3 tablets.32 mg tablets for oral suspension, pale yellow to off-white, clover-shaped, quadrisected on one side and debossed with "32" on the other side, packaged in child resistant Aluminum/Aluminum peel-push blisters.NDC 66215-103-56: Carton of 56 tablets for oral suspension in 4 blister-strips of 14 tablets.NDC 66215-103-14: Blister strip of 14 tablets for oral suspension.
Clinical Information
Chemical Structure
No Image foundClinical Pharmacology
Bosentan is a specific and competitive antagonist at endothelin receptor types ET and ET. Bosentan has a slightly higher affinity for ET receptors than for ET receptors. The clinical impact of dual endothelin blockage is unknown.
Endothelin-1 (ET-1) is a neurohormone, the effects of which are mediated by binding to ET and ET receptors in the endothelium and vascular smooth muscle. ET-1 concentrations are elevated in plasma and lung tissue of patients with PAH, suggesting a pathogenic role for ET-1 in this disease.
Non-Clinical Toxicology
Pregnancy ()Use with Cyclosporine A ()
Use with Glyburide ()
Hypersensitivity ()
Because of the risks of hepatotoxicity and birth defects, Tracleer is available only through a restricted program called the Tracleer REMS Program. The Tracleer REMS Program is a component of the Tracleer Risk Evaluation and Mitigation Strategy (REMS). Under the Tracleer REMS, prescribers, patients, and pharmacies must enroll in the program
Because tetracyclines have been shown to depress plasma prothrombin activity, patients who are on anticoagulant therapy may require downward adjustment of their anticoagulant dosage.
Since bacteriostatic drugs may interfere with the bactericidal action of penicillin, it is advisable to avoid giving tetracycline-class drugs in conjunction with penicillin.
Absorption of tetracyclines is impaired by antacids containing aluminum, calcium, or magnesium, and iron-containing preparations.
The concurrent use of tetracycline and methoxyflurane has been reported to result in fatal renal toxicity.
Concurrent use of tetracyclines with oral contraceptives may render oral contraceptives less effective.
Administration of isotretinoin should be avoided shortly before, during, and shortly after minocycline therapy. Each drug alone has been associated with pseudotumor cerebri (see ).
Increased risk of ergotism when ergot alkaloids or their derivatives are given with tetracyclines.
ALT or AST > 3 × ULN were observed in 11% of Tracleer-treated patients (n = 658) compared to 2% of placebo-treated patients (n = 280). Three-fold increases were seen in 12% of 95 pulmonary arterial hypertension (PAH) patients on 125 mg twice daily and 14% of 70 PAH patients on 250 mg twice daily. Eight-fold increases were seen in 2% of PAH patients on 125 mg twice daily and 7% of PAH patients on 250 mg twice daily. Bilirubin increases to ≥ 3 × ULN were associated with aminotransferase increases in 2 of 658 (0.3%) of patients treated with Tracleer. In a pooled analysis of four pediatric studies conducted in PAH (n =100), elevations in liver aminotransferases ≥ 3 × ULN were observed in 2% of patients. The combination of hepatocellular injury (increases in aminotransferases of > 3 × ULN) and increases in total bilirubin (≥ 2 × ULN) is a marker for potential serious hepatotoxicity.
Elevations of AST or ALT associated with Tracleer are dose-dependent, occur both early and late in treatment, usually progress slowly, are typically asymptomatic, and usually have been reversible after treatment interruption or cessation. Aminotransferase elevations also may reverse spontaneously while continuing treatment with Tracleer.
Liver aminotransferase levels must be measured prior to initiation of treatment and then monthly and therapy adjusted accordingly . Discontinue Tracleer if liver aminotransferase elevations are accompanied by clinical symptoms of hepatotoxicity (such as nausea, vomiting, fever, abdominal pain, jaundice, or unusual lethargy or fatigue) or increases in bilirubin ≥ 2 × ULN.
Avoid initiation of Tracleer in patients with elevated aminotransferases (> 3 × ULN) prior to drug initiation because monitoring hepatotoxicity in these patients may be more difficult .
In WHO Functional Class II patients, consider whether the benefits of Tracleer are sufficient to offset the risk of hepatotoxicity, which may preclude future use as their disease progresses.
The following important adverse reactions are described elsewhere in the labeling:
Reference
This information is obtained from the National Institute of Health's Standard Packaging Label drug database.
"https://dailymed.nlm.nih.gov/dailymed/"
While we update our database periodically, we cannot guarantee it is always updated to the latest version.
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