Bosentan Brand Name– Tracleer
What is Bosentan
Bosentan is a cardiovascular agent that belongs to a group of compounds known as endothelin-receptor antagonists and is indicated for use in pulmonary arterial hypertension in patients with WHO Class II to IV symptoms. It is a specific and competitive antagonist at both type A and B endothelin-1 receptors.
Bosentan is associated with a high frequency of elevated hepatic enzymes, a potential for teratogenic effects, and many drug interactions. Bosentan is extensively metabolized by, and a significant inducer of, CYP2C9 and CYP3A4 isoenzymes.
Due to the risk for fetal harm and the potential hepatotoxicity of the drug, registration in the Bosentan REMS program is required for prescribers, pharmacies, and patients. Information may be obtained by visiting www.BosentanREMSProgram.com.
Indications
- persistent pulmonary hypertension of the newborn
- pulmonary hypertension
For the treatment of pulmonary hypertension (pulmonary arterial hypertension WHO Group 1)
NOTE: Studies establishing effectiveness in adult patients were comprised predominately of patients with NYHA Functional Class II to IV symptoms and etiologies of idiopathic or heritable pulmonary arterial hypertension (PAH) (60%), PAH associated with connective tissue diseases (21%) and PAH associated with congenital heart disease with left-to-right shunts (18%).
Side Effects
- anaphylactoid reactions
- anemia
- angioedema
- arthralgia
- blurred vision
- chest pain (unspecified)
- cirrhosis
- diaphoresis
- dizziness
- Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS)
- edema
- elevated hepatic enzymes
- fluid retention
- flushing
- headache
- hepatic failure
- hepatotoxicity
- hyperbilirubinemia
- hypotension
- infection
- jaundice
- leukopenia
- nasal congestion
- nausea
- neutropenia
- oligospermia
- palpitations
- peripheral edema
- pharyngitis
- rash
- sinusitis
- syncope
- teratogenesis
- thrombocytopenia
- vomiting
- weight gain
Monitoring Parameters
- hemoglobin/hematocrit
- LFTs
- pregnancy testing
- serum bilirubin (total and direct)
Contraindications
- anemia
- breast-feeding
- contraception requirements
- edema
- geriatric
- heart failure
- hepatic disease
- hepatitis
- hepatotoxicity
- infertility
- jaundice
- peripheral edema
- phenylketonuria
- pregnancy
- pregnancy testing
- pulmonary edema
- reproductive risk
- veno-occlusive disease (VOD)
- ventricular dysfunction
Interactions
- Abacavir; Dolutegravir; Lamivudine
- Abemaciclib
- Acetaminophen; Butalbital; Caffeine; Codeine
- Acetaminophen; Caffeine; Dihydrocodeine
- Acetaminophen; Chlorpheniramine; Dextromethorphan; Phenylephrine
- Acetaminophen; Chlorpheniramine; Dextromethorphan; Pseudoephedrine
- Acetaminophen; Chlorpheniramine; Phenylephrine; Phenyltoloxamine
- Acetaminophen; Codeine
- Acetaminophen; Dextromethorphan; Guaifenesin; Phenylephrine
- Acetaminophen; Dextromethorphan; Phenylephrine
- Acetaminophen; Dextromethorphan; Pseudoephedrine
- Acetaminophen; Dichloralphenazone; Isometheptene
- Acetaminophen; Guaifenesin; Phenylephrine
- Acetaminophen; Hydrocodone
- Acetaminophen; Oxycodone
- Acetaminophen; Pseudoephedrine
- Acrivastine; Pseudoephedrine
- Alfentanil
- Aliskiren; Amlodipine
- Aliskiren; Amlodipine; Hydrochlorothiazide, HCTZ
- Aliskiren; Hydrochlorothiazide, HCTZ
- Aliskiren; Valsartan
- Alpha-blockers
- Alprazolam
- Ambrisentan
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- Amiodarone
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- Amlodipine
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- Amlodipine; Benazepril
- Amlodipine; Celecoxib
- Amlodipine; Hydrochlorothiazide, HCTZ; Olmesartan
- Amlodipine; Hydrochlorothiazide, HCTZ; Valsartan
- Amlodipine; Olmesartan
- Amlodipine; Telmisartan
- Amlodipine; Valsartan
- Amobarbital
- Amoxicillin; Clarithromycin; Lansoprazole
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