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Pharmakokinetics of Ambrisentan 5mg.
The pharmacokinetics of Ambrisentan in healthy volunteers are characterized by linear dose dependence. After oral administration, Ambrisentan is absorbed, Cmax is reached after approximately 2 hours. AUC in the plasma of the metabolite 4-hydroxymethyl ambrisentan is approximately 4% of the AUC of the starting material. Eating does not affect bioavailability.
The binding with plasma proteins is high – 99%. CSS on average is 15% of Cmax. The cumulating factor is about 1.2 after long-term use.
In vitro studies have shown that ambrisentan is a substrate of P-glycoprotein. In vivo, the inversion of S-ambrisentan into R-ambrisentan is negative.
T1 / 2 of ambrisentan is 15 hours. Effective T1 / 2 of ambrisentan is about 9 hours. The average clearance value for oral intake is 38 ml / min and 19 ml / min in healthy volunteers and in patients with pulmonary arterial hypertension, respectively. It is mainly excreted out of the kidney, but the relative role of metabolism and biliary elimination is insufficiently characterized.
Indications of Ambrisentan 5mg.
Treatment of pulmonary arterial hypertension to improve the tolerance of physical activity to slowing the progression of clinical symptoms. In studies, efficacy was established primarily in patients with symptoms that corresponded to functional class II-III and idiopathic etiology or hereditary etiology (64%) or pulmonary arterial hypertension associated with connective tissue diseases (32%).
Dosage mode of Ambrisentan 5mg.
The dose is 5 mg 1 time / day, with good tolerability, it is possible to increase the dose to 10 mg 1 time / day.
Application in a dose of more than 10 mg in patients with pulmonary arterial hypertension has not been studied.
Side effects of Ambrisentan 5mg.
On the part of the respiratory system: nasal congestion (swelling of the nasal mucosa), sinusitis.
On the part of the digestive system: there may be an increase alanine aminotransferase and aspartate aminotransferase activity (in most such cases, patients had other causes that could cause a violation of liver function, including heart failure, liver enlargement, hepatitis, alcoholism, hepatotoxic remedies).
Common reactions: peripheral edema, hot flashes.
Contraindications of Ambrisentan 5mg.
Idiopathic pulmonary fibrosis with or without secondary pulmonary hypertension, severe renal failure (10 or more Child-Pugh scores), increased hepatic transaminase activity more than 3 times higher than congenital adrenal hyperplasia; pregnancy (onset or planned); children and adolescents under 18; increased sensitivity to Ambrisentan.