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Embelin 5mg Tablet 1 Strip
Embelin is used for the treatment of Pulmonary Arterial Hypertension (PAH) (WHO Group 1) to improve exercise capacity and delay clinical deterioration.
- Use as per the guidance of a registered healthcare professional.
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✅ Description:
Endothelin-1 (ET-1) is a powerful peptide involved in various vascular actions. It exerts its effects through two receptor subtypes: ETA and ETB. ETA primarily causes vasoconstriction and cell proliferation, while ETB induces vasodilation, antiproliferation, and ET-1 clearance. Ambrisentan is a potent ETA receptor antagonist, with over 4000 times greater selectivity for ETA over ETB. The exact clinical significance of this high selectivity is not well understood.
Ambrisentan is absorbed with peak levels appearing about 2 hours after oral administration, and food does not affect its absorption. It is highly bound to plasma proteins (99%) and eliminated through non-renal pathways. Although its terminal half-life is around 15 hours, the accumulation factor after long-term dosing indicates an effective half-life of about 9 hours.
✔️ Dosage & Administration
- Adults: Start with 5 mg once daily, which can be increased to 10 mg once daily if well tolerated. It can be taken with or without food.
- Pediatric patients: The safety and effectiveness of Ambrisentan in children have not been established.
- Use as per the guidance of a registered healthcare professional.
✔️ Side Effects
Decreased hemoglobin levels and hematocrit have been observed in clinical trials with Embelin, similar to other endothelin receptor antagonists.
✔️ Interaction
Co-administration with Cyclosporine can increase Embelin exposure by about 2-fold, so the dosage of Embelin should be limited to 5 mg once daily when taken with Cyclosporine.
✔️ Contraindications
Ambrisentan is contraindicated in pregnant women as it may cause fetal harm. Pregnancy must be excluded before starting treatment and prevented during treatment and for one month after stopping. It is also contraindicated in patients with Idiopathic Pulmonary Fibrosis (IPF), including those with pulmonary hypertension (WHO Group 3).
✔️ Pregnancy & Lactation
- Pregnancy Category X: Ambrisentan may harm the fetus and should not be used during pregnancy.
- It is unknown whether Ambrisentan is excreted in human milk, so breastfeeding is not recommended during treatment.
✔️ Precautions & Warnings
- Fluid Retention: Peripheral edema is a common side effect of endothelin receptor antagonists and can also result from worsening PAH.
- Pulmonary Veno-occlusive Disease: If acute pulmonary edema occurs during the start of therapy, consider pulmonary veno-occlusive disease and discontinue Embelin if confirmed.
- Hematological Changes: Hemoglobin and hematocrit reductions have been seen with Embelin, similar to other drugs in its class.
- Hepatic Impairment: Embelin is not recommended for use in patients with moderate or severe liver impairment.
✔️ Storage Conditions
Store in a cool, dry place below 30°C, away from light and moisture.
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here information is for informational purposes only.
The information contained herein should NOT be used as a substitute
for the advice of a qualified physician. This may not cover
everything about particular health conditions,
lab tests, medicines, all possible side effects, drug interactions,
warnings, alerts, etc. Please consult your healthcare professional
and discuss all your queries related to any disease or medicine. We
intend to support, not replace, the doctor-patient relationship.
