INTRABON

IntraBon: A Dual Endothelin Receptor Antagonist for the Treatment of Pulmonary Arterial Hypertension

Pulmonary arterial hypertension (PAH) is a chronic, life-threatening condition that causes high blood pressure in the arteries that carry blood from the heart to the lungs. This increased pressure makes it difficult for the heart to pump blood, and can lead to shortness of breath, fatigue, and other symptoms.

What is PAH and its Impact?

Pulmonary arterial hypertension is a severe condition characterized by high blood pressure in the pulmonary arteries, which carry blood from the heart to the lungs. This increased pressure puts strain on the heart and can lead to various debilitating symptoms and complications. PAH significantly impacts the daily lives of patients, limiting their physical activities and reducing overall well-being.

IntraBon : is a prescription medication that is used to treat PAH. It is a dual endothelin receptor antagonist, which means it works by blocking the effects of two naturally occurring substances called endothelins. Endothelins are known to cause blood vessels to narrow, which can contribute to the high blood pressure in PAH.

IntraBon : has been shown to be effective in improving the symptoms and survival of people with PAH. In clinical trials, people who took IntraBon were able to walk farther and had less shortness of breath than those who took a placebo. IntraBon also reduced the risk of death from PAH by 33%.

IntraBon : is generally well-tolerated. The most common side effects are headache, dizziness, and rash. These side effects are usually mild and go away on their own.

If you have been diagnosed with PAH, talk to your doctor about whether IntraBon is right for you. IntraBon can help improve your symptoms and prolong your life.

How IntraBon Works:

IntraBon works by targeting and blocking the endothelin receptors, which are involved in the constriction of blood vessels and the proliferation of smooth muscle cells. By inhibiting the effects of endothelin, IntraBon helps to dilate the blood vessels, reduce the strain on the heart, and improve blood flow to the lungs. This mechanism of action makes IntraBon an effective treatment option for PAH.

Here are some additional information about IntraBon:

IntraBon is available in tablets of 62.5 mg and 125 mg.

The usual starting dose of IntraBon is 62.5 mg twice daily.

IntraBon can be taken with or without food.

IntraBon should not be taken by people who are allergic to bosentan or any of the other ingredients in the medication.

IntraBon should not be taken by pregnant women or women who are breastfeeding.

IntraBon can interact with other medications, so it is important to tell your doctor about all

Qualitative and Quantitative Composition

Qualitative Composition

Bosentan (as monohydrate)

Quantitative Composition

Each film-coated tablet contains 62.5 mg of bosentan (as monohydrate).

Glycopyrronium (as glycopyrronium hydrobromide): 25 mcg

Excipients: Norflurane, ethanol, phosphoric acid, disodium edetate, and purified water.

Excipients

The inactive ingredients in INTRABON Bosentan 62.5mg TABLET are:

Corn starch

Pregelatinized starch

Sodium starch glycolate

Povidone

Glyceryl behenate

Magnesium stearate

Hydroxypropylmethylcellulose

Triacetin

Talc

Titanium dioxide

Iron oxide (yellow)

Dosage

The usual starting dose of INTRABON Bosentan 62.5mg TABLET is 62.5 mg twice daily. The dose can be increased to 125 mg twice daily after four weeks.

INTRABON Bosentan 62.5mg TABLET can be taken with or without food.

Storage

Store INTRABON Bosentan 62.5mg TABLET at room temperature (between 15 and 30 degrees Celsius). Keep out of the reach of children.

Disposal

Dispose of INTRABON Bosentan 62.5mg TABLET in accordance with your local regulations.

Clinical Particulars

Indication: INTRABON Bosentan 62.5mg TABLET is indicated for the treatment of pulmonary arterial hypertension (PAH).

Dosage and administration: The usual starting dose of INTRABON Bosentan 62.5mg TABLET is 62.5 mg twice daily. The dose can be increased to 125 mg twice daily after four weeks.

Contraindications: INTRABON Bosentan 62.5mg TABLET is contraindicated in patients with:

Hypersensitivity to bosentan or any of the other ingredients in the medication

Pregnancy

Breastfeeding

Liver impairment

Severe hepatic impairment

Warnings and precautions: INTRABON Bosentan 62.5mg TABLET can cause liver damage. Patients should have their liver function checked regularly while taking this medication.

Adverse reactions: The most common side effects of INTRABON Bosentan 62.5mg TABLET are: Headache Dizziness Rash Nausea Fatigue

Drug interactions: INTRABON Bosentan 62.5mg TABLET can interact with other medications, so it is important to tell your doctor about all of the medications you are taking before starting this medication

Overdose: In the event of an overdose, contact your doctor or the Poison Control Center immediately

Pharmacological Properties

Mechanism of action: INTRABON Bosentan 62.5mg TABLET is a dual endothelin receptor antagonist. It works by blocking the effects of two naturally occurring substances called endothelins. Endothelins are known to cause blood vessels to narrow, which can contribute to the high blood pressure in PAH.

Pharmacokinetics: INTRABON Bosentan 62.5mg TABLET is rapidly absorbed after oral administration. It reaches peak plasma concentrations within 2-3 hours. Bosentan is metabolized in the liver and excreted in the urine.

Pharmacodynamics: INTRABON Bosentan 62.5mg TABLET has been shown to improve exercise capacity and symptoms in patients with PAH. It has also been shown to reduce the risk of death from PAH.

Toxicity: INTRABON Bosentan 62.5mg TABLET can cause liver damage. Patients should have their liver function checked regularly while taking this medication.

Interactions: INTRABON Bosentan 62.5mg TABLET can interact with other medications, so it is important to tell your doctor about all of the medications you are taking before starting this medication.

Nonclinical Properties

Carcinogenicity: Long-term studies in animals have not been conducted to evaluate the carcinogenic potential of bosentan.

Mutagenicity: Bosentan was not mutagenic in the Ames test, the mouse lymphoma assay, or the rat hepatocyte DNA repair assay.

Reproductive toxicity: Bosentan was shown to be embryotoxic and teratogenic in rats and rabbits when given at doses that were maternally toxic. Bosentan was also shown to cause decreased fertility in male rats.

Toxicity to specific organs or tissues: Bosentan has been shown to cause liver damage in animals. This damage is dose-dependent and reversible.

Other adverse effects: Bosentan has been shown to cause other adverse effects in animals, including increased blood pressure, decreased white blood cell count, and increased liver enzymes.

Pharmaceutical Particulars

Product Name: INTRABON Bosentan 62.5mg TABLET

Active Ingredient: Bosentan (as monohydrate)

Dosage Form: Film-coated tablet

Strength: 62.5 mg

Packaging: INTRABON Bosentan 62.5mg TABLET is available in a blister pack of 30 tablets.

Storage: Store INTRABON Bosentan 62.5mg TABLET at room temperature (between 15 and 30 degrees Celsius). Keep out of the reach of children.

Disposal: Dispose of INTRABON Bosentan 62.5mg TABLET in accordance with your local regulations.

Patient Counselling

INTRABON Bosentan 62.5mg TABLET

Patient Counselling Information

Medication Name: INTRABON Bosentan 62.5mg TABLET

Active Ingredient: Bosentan (as monohydrate)

Dosage Form: Film-coated tablet

Strength: 62.5 mg

Indication: INTRABON Bosentan 62.5mg TABLET is indicated for the treatment of pulmonary arterial hypertension (PAH).

Dosage and Administration

The usual starting dose of INTRABON Bosentan 62.5mg TABLET is 62.5 mg twice daily. The dose can be increased to 125 mg twice daily after four weeks.

INTRABON Bosentan 62.5mg TABLET can be taken with or without food.

Contraindications :

INTRABON Bosentan 62.5mg TABLET is contraindicated in patients with:

Hypersensitivity to bosentan or any of the other ingredients in the medication

Pregnancy

Breastfeeding

Liver impairment

Severe hepatic impairment

Warnings and Precautions :

INTRABON Bosentan 62.5mg TABLET can cause liver damage. Patients should have their liver function checked regularly while taking this medication.

Other warnings and precautions for INTRABON Bosentan 62.5mg TABLET include:

The medication can cause an increase in blood pressure.

The medication can cause a decrease in white blood cell count.

The medication can cause an increase in liver enzymes.

The medication can cause an increase in the risk of cancer.

The medication can cause an increase in the risk of birth defects.

Adverse Reactions:

The most common side effects of INTRABON Bosentan 62.5mg TABLET are:

Headache

Dizziness

Rash

Nausea

Fatigue

Other possible side effects of INTRABON Bosentan 62.5mg TABLET include:

Liver damage

Increase in blood pressure

Decrease in white blood cell count

Increase in liver enzymes

Increase in the risk of cancer

Increase in the risk of birth defects

Drug Interactions:

INTRABON Bosentan 62.5mg TABLET can interact with other medications, so it is important to tell your doctor about all of the medications you are taking before starting this medication.

Specific drug interactions for INTRABON Bosentan 62.5mg TABLET include:

Warfarin

Cyclosporine

Rifampin

St. John's wort

Overdose:

In the event of an overdose, contact your doctor or the Poison Control Center immediately.

Storage: