Indications & Uses
Ambris 10 is indicated for:
Pharmacology
Endothelin-1 (ET-1) is a powerful peptide that acts on the cells that make it and on the cells next to them. It works through two receptor types, ETA and ETB, found in vascular smooth muscle and the endothelium. ETA mainly causes vasoconstriction and cell proliferation, whereas ETB mainly causes vasodilation, slows cell proliferation, and clears ET-1 from the body.
Ambrisentan blocks the ETA receptor with high affinity. It is far more selective for ETA than for ETB (more than 4000-fold). What this high selectivity means in clinical practice is not yet known.
In healthy people, the pharmacokinetics of Ambrisentan (S-Ambrisentan) are dose proportional. Its absolute bioavailability is not known. After an oral dose, Ambrisentan is absorbed and reaches peak concentration in about 2 hours, in both healthy subjects and PAH patients. Food does not change how much of the medicine is absorbed. Laboratory studies show that Ambrisentan is a substrate of P-gp. About 99% of it binds to plasma proteins.
Ambrisentan is removed from the body mainly through non-renal routes. How much is broken down by metabolism compared with eliminated through bile has not been well studied. In plasma, the AUC of 4-hydroxymethyl Ambrisentan is about 4% of the AUC of the parent Ambrisentan. In the body, S-Ambrisentan converts to R-Ambrisentan only to a negligible extent.
The mean oral clearance of Ambrisentan is 38 mL/min in healthy subjects and 19 mL/min in PAH patients. Its terminal half-life is 15 hours. Even so, at steady state the mean trough concentration is about 15% of the mean peak concentration, and after long-term daily dosing the accumulation factor is about 1.2. This means the effective half-life of Ambrisentan is about 9 hours.
Dosage Reference
Reference Information Only
Dosages shown are general references from official sources. Always consult your doctor or pharmacist for personalized dosing.
Adults:
Adult dose: Treatment usually starts at 5 mg once daily. If this dose is well tolerated, it may be increased to 10 mg once daily. Ambrisentan can be taken with or without food.
Pediatric patients: Safety and effectiveness in children have not been established.
Side Effects
Decreases in hemoglobin concentration and hematocrit have been seen with other endothelin receptor antagonists, and this effect was also observed in clinical studies with Ambrisan.
Cautions & Contraindications
Warnings & Precautions
Fluid Retention: Peripheral edema is a recognised class effect of endothelin receptor antagonists, and can also occur as a clinical consequence of PAH itself and of worsening PAH. Pulmonary Veno-occlusive Disease: If a patient develops acute pulmonary edema after starting a vasodilating agent such as Ambrisan, pulmonary veno-occlusive disease should be considered as a possible cause. If this is confirmed, Ambrisan should be discontinued. Haematological Changes: Endothelin receptor antagonists, including Ambrisan, have been associated with decreases in haemoglobin concentration and haematocrit; such decreases were observed in clinical studies with Ambrisan. Hepatic Impairment: Ambrisan is not recommended for patients with moderate or severe hepatic impairment.
Contraindications
Ambrisentan can harm an unborn baby if taken during pregnancy, so it must not be used by women who are or could become pregnant. Anyone who takes this medicine while pregnant, or who becomes pregnant while on it, should be made fully aware of the risk this poses to the baby. Before starting Ambrisentan, pregnancy must be ruled out, and effective measures should be taken to avoid pregnancy both during treatment and for one month after stopping it. This medicine is also not suitable for patients with Idiopathic Pulmonary Fibrosis (IPF), including those with IPF accompanied by pulmonary hypertension (WHO Group 3).
Pregnancy & Breastfeeding
Pregnancy Category X. It is not known whether Ambrisentan passes into breast milk, so breastfeeding is not recommended for mothers taking this medicine.
⚠️ Talk to your doctor before taking any medicine during pregnancy or while breastfeeding.
Storage
Keep Ambrisentan in a cool, dry place, below 30°C. Protect it from light and moisture.
Drug Interactions
Common questions about Ambris 10 10 mg
What is Ambris 10 10 mg Tablet?
Ambris 10 10 mg Tablet is a medicine that contains Ambrisentan. It is made by Opsonin Pharma Limited. It belongs to the Anti-hypertensive group of medicines.
What is Ambris 10 used for?
Ambris 10 is used for: Hypertension.
What are the side effects of Ambris 10?
Decreases in hemoglobin concentration and hematocrit have been seen with other endothelin receptor antagonists, and this effect was also observed in clinical studies with Ambrisan.
Can I take Ambris 10 during pregnancy or while breastfeeding?
Pregnancy Category X. It is not known whether Ambrisentan passes into breast milk, so breastfeeding is not recommended for mothers taking this medicine. Talk to your doctor before taking any medicine during pregnancy or while breastfeeding.
How should I store Ambris 10?
Keep Ambrisentan in a cool, dry place, below 30°C. Protect it from light and moisture.
Can I take other medicines with Ambris 10?
Some medicines can interact with Ambrisentan, for example: Cyclosporine. Tell your doctor or pharmacist about every medicine you take.
Do I need a prescription for Ambris 10?
Ambris 10 is a prescription (Rx) medicine. Take it as your doctor advises.