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bosentan
generic
Black Box Warnings .
Appropriate Use
available only through Bosentan Risk Evaluation and Mitigation Strategy (REMS) Program to minimize hepatic injury and fetal exposure; prescribers, pharmacies, and pts must enroll at 1-866-359-2612 or www.bosentanremsprogram.com
Hepatotoxicity
AST/ALT elev. >3x ULN reported in 11% of pts, incl. small number of cases assoc. w/ elev. bilirubin; measure AST/ALT at baseline and qmo; rare unexplained hepatic cirrhosis cases reported w/ tx >12mo in pts w/ multiple comorbidities, drug tx; rare reports of hepatic failure; one case of pronounced AST/ALT elev. w/ non-specific sx after >20mo tx, which resolved slowly after tx D/C, reinforces importance of strict adherence to qmo monitoring and tx algorithm, incl. tx D/C if elev. AST/ALT w/ hepatotoxicity s/sx; avoid use if baseline AST/ALT >3x ULN since more difficult to monitor hepatotoxicity; D/C tx if elev. AST/ALT w/ clinical sx of hepatotoxicity (e.g. nausea, vomiting, fever, abdominal pain, jaundice, unusual lethargy/fatigue) or bilirubin >2x ULN, or if AST/ALT >8x ULN; no experience w/ tx reintroduction
Embryo-Fetal Toxicity
major birth defect risk if used in pregnancy; exclude pregnancy prior to tx start, then obtain pregnancy test qmo; must use 2 reliable forms of contraception during tx and x1mo after D/C in women of childbearing potential; no additional contraception needed if tubal sterilization hx or current IUD use; hormonal contraceptives, incl. oral, injectable, transdermal, or implantable, should not be sole method as they may not be effective in combo w/ bosentan
Adult Dosing .
Dosage forms: TAB: 62.5 mg, 125 mg
Restricted Distribution in US
- [1-866-359-2612 or www.bosentanremsprogram.com for more info]
pulmonary arterial HTN
- [<40 kg]
- Dose: 62.5 mg PO bid; Max: 125 mg/day; Info: D/C and monitor at least q2wk if AST/ALT >3x up to 8x ULN; may resume prior dose if AST/ALT return to baseline; D/C w/o reintroduction if elev. AST/ALT w/ clinical sx of hepatotoxicity or serum bilirubin >2x ULN, or if AST/ALT >8x ULN
- [>40 kg]
- Dose: 125 mg PO bid; Start: 62.5 mg PO bid x4wk; Max: 250 mg/day; Info: decr. dose to 62.5 mg bid or interrupt tx and monitor at least q2wk if AST/ALT >3x up to 5x ULN; D/C and monitor at least q2wk if AST/ALT >5x up to 8x ULN; may restart tx if AST/ALT return to baseline; D/C w/o reintroduction if elev. AST/ALT w/ clinical sx of hepatotoxicity or serum bilirubin >2x ULN, or if AST/ALT >8x ULN
renal dosing
- [see below]
- renal impairment: no adjustment
- HD/PD: not defined
hepatic dosing
- [see below]
- Child-Pugh Class B or C or baseline AST/ALT >3x ULN: avoid use
Peds Dosing .
- Dosage forms: TAB: 62.5 mg, 125 mg; DISPERSE TAB: 32 mg
Restricted Distribution in US
- [1-866-228-3546 or www.tracleerrems.com for more info]
pulmonary arterial HTN
- [3-12 yo, 4-8 kg]
- Dose: 16 mg PO bid; Max: 32 mg/day; Info: D/C and monitor at least q2wk if AST/ALT >3x up to 8x ULN; may resume prior dose if AST/ALT return to baseline; D/C w/o reintroduction if elev. AST/ALT w/ clinical sx of hepatotoxicity or serum bilirubin >2x ULN, or if AST/ALT >8x ULN
- [3-12 yo, 9-16 kg]
- Dose: 32 mg PO bid; Max: 64 mg/day; Info: D/C and monitor at least q2wk if AST/ALT >3x up to 8x ULN; may resume prior dose if AST/ALT return to baseline; D/C w/o reintroduction if elev. AST/ALT w/ clinical sx of hepatotoxicity or serum bilirubin >2x ULN, or if AST/ALT >8x ULN
- [3-12 yo, 17-24 kg]
- Dose: 48 mg PO bid; Max: 96 mg/day; Info: D/C and monitor at least q2wk if AST/ALT >3x up to 8x ULN; may resume prior dose if AST/ALT return to baseline; D/C w/o reintroduction if elev. AST/ALT w/ clinical sx of hepatotoxicity or serum bilirubin >2x ULN, or if AST/ALT >8x ULN
- [3-12 yo, 25-40 kg]
- Dose: 64 mg PO bid; Max: 128 mg/day; Info: D/C and monitor at least q2wk if AST/ALT >3x up to 8x ULN; may resume prior dose if AST/ALT return to baseline; D/C w/o reintroduction if elev. AST/ALT w/ clinical sx of hepatotoxicity or serum bilirubin >2x ULN, or if AST/ALT >8x ULN
- [13 yo and older, <40 kg]
- Dose: 62.5 mg PO bid; Max: 125 mg/day; Info: D/C and monitor at least q2wk if AST/ALT >3x up to 8x ULN; may resume prior dose if AST/ALT return to baseline; D/C w/o reintroduction if elev. AST/ALT w/ clinical sx of hepatotoxicity or serum bilirubin >2x ULN, or if AST/ALT >8x ULN
- [13 yo and older, >40 kg]
- Dose: 125 mg PO bid; Start: 62.5 mg PO bid x4wk; Max: 250 mg/day; Info: decr. dose to 62.5 mg bid or interrupt tx and monitor at least q2wk if AST/ALT >3x up to 5x ULN; D/C and monitor at least q2wk if AST/ALT >5x up to 8x ULN; may restart tx if AST/ALT return to baseline; D/C w/o reintroduction if elev. AST/ALT w/ clinical sx of hepatotoxicity or serum bilirubin >2x ULN, or if AST/ALT >8x ULN
renal dosing
- [see below]
- renal impairment: no adjustment
- HD/PD: not defined
hepatic dosing
- [see below]
- Child-Pugh Class B or C or baseline AST/ALT >3x ULN: avoid use