PULMOTEN 62.5mg Tab.

Pulmoten 62.5 is a prescription medicine used to treat pulmonary arterial hypertension (high pressure in the blood vessels that carry blood from the heart to the lungs). It even helps to improve your quality of life, exercising ability and delay in disease progression. Pulmoten 62.5 should be taken with or without food. This medicine should be used regularly to get the most benefit from it. The dose and how often you take it depends on what you are taking it for. Your doctor will decide how much you need to improve your symptoms. You should take this medicine for as long as it is prescribed for you. The most common side effects of this medicine include headache, swelling of the legs and ankles, and diarrhea. If these bother you or appear serious, let your doctor know. There may be ways of reducing or preventing them. Some serious side effects which mean your doctor should know immediately include Anemia (low number of red blood cells) and abnormal liver function such as nausea, vomiting, dark urine, fever, and dark urine. Your doctor might check you for blood tests to check for anemia and liver function. Before taking this medicine, let your doctor know if you have liver dysfunctioning. Inform your doctor if you are pregnant or breastfeeding. Women are suggested to use reliable contraceptive pills to avoid pregnancy and should continue even after one month of stopping the treatment. Your doctor should also know about all other medicines you are taking as many of these may make this medicine less effective or change the way it works.

Uses of Pulmoten 62.5

• Pulmonary arterial hypertension (PAH)

Side effects of Pulmoten 62.5

• Headache
• Ankle swelling
• Edema (swelling)
• Diarrhea
• Anemia (low number of red blood cells)
• Respiratory tract infection

How to use Pulmoten 62.5

Take this medicine in the dose and duration as advised by your doctor. Swallow it as a whole. Do not chew, crush or break it. Pulmoten 62.5 may be taken with or without food, but it is better to take it at a fixed time.

How Pulmoten 62.5 works

Pulmoten 62.5 is an endothelin receptor blocker. It blocks the action of endothelin (a natural substance) that causes blood vessels to narrow (constrict). This narrowing increases the pressure in the blood vessels of the lungs. Pulmoten 62.5 helps relax these blood vessels and increases the supply of blood to the lungs.

What if you forget to take Pulmoten 62.5?

If you miss a dose of Pulmoten 62.5, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular schedule. Do not double the dose.

Indication

Pulmonary Arterial Hypertension (PAH)

Administration

Bosentan should be administered in the morning and evening with or without food.

Adult Dose

Oral Pulmonary hypertension Adult: >12 yr <40 kg: Initial and maintenance dose is 62.5 mg bid; >40 kg: Initially, 62.5 mg bid for 4 wk, then increased to a maintenance dose of 125 mg bid. Elderly: No dosage adjustment needed. Hepatic impairment: Mild: No dosage adjustment needed. Moderate and severe: Contraindicated.

Renal Dose

Renal impairment: No dosage adjustment needed in renal impairment or dialysis patients.

Contraindication

Patients with WHO Class II symptoms showed reduction in the rate of clinical deterioration and a trend for improvement in walk distance. Physicians should consider whether these benefits are sufficient to offset the risk of hepatotoxicity in WHO Class II patients, which may preclude future use as their disease progresses.

Mode of Action

Competitive antagonist of endothelin-1; blocks endothelin receptors on vascular endothelium and smooth muscle resulting in inhibition of vasoconstriction

Precaution

Hepatotoxicity and teratogenicity. Elevations of AST or ALT associated with Bosentan are dose-dependent, occur both early and late in treatment, usually progress slowly, are typically asymptomatic, and usually have been reversible after treatment interruption or cessation. Aminotransferase elevations also may reverse spontaneously while continuing treatment with Tracleer. Liver aminotransferase levels must be measured prior to initiation of treatment and then monthly and therapy adjusted accordingly .Discontinue Bosentan if liver aminotransferase elevations are accompanied by clinical symptoms of hepatotoxicity (such as nausea, vomiting, fever, abdominal pain, jaundice, or unusual lethargy or fatigue) or increases in bilirubin > 2 Lactation: Not known if excreted in breast milk; not recommended

Side Effect

>10% Hgb decreased; >1 g/dL (57%),Inhibition of spermatogenesis (25%),Headache (16-22%),Nasopharyngitis (11%),Transaminses increased (12%),Respiratory tract infection (22%),Increased transaminases (12%) 1-10% Edema, lower limb (5-8%),Flushing (7-9%),Hypotension (7%),Hepatic abnormalities (4%),Palpitations (4%),Anemia (3%),Dyspepsia (4%),Edema, general (4%),Fatigue (2%),Pruritus (4%) <1% Hyperbilirubinemia,Vasculitis,Jaundice,Leukopenia,Thrombocytopenia,Leukocytoplastic

Pregnancy Category Note

Pregnancy Based on animal data, bosentan may cause fetal harm, including birth defects and fetal death, when administered to a pregnant female and is contraindicated during pregnancy; see Contraindications and Black Box Warnings In animal reproduction studies, oral administration of bosentan to pregnant rats at 2 times the maximum recommended human dose (MRHD) on a mg/m2 basis caused teratogenic effects in rats (eg, malformations of the head, mouth, face, and large blood vessels) Advise pregnant women of the potential risk to a fetus Patient should contact her physician immediately for pregnancy testing if onset of menses is delayed or pregnancy is suspected If the pregnancy test is positive, the physician and patient must discuss the risks to her, the pregnancy, and the fetus Based on findings in animals, bosentan may impair fertility in males of reproductive potential; It is unknown whether effects on fertility would be reversible Lactation There are no data on the presence of bosentan in human milk, the effects on the breastfed infant, or the effect on milk production Because of the potential for serious adverse reactions, such as fluid retention and hepatotoxicity, in breastfed infants from bosentan, advise women not to breastfeed during treatment with bosentan

Interaction

Increased bosentan levels w/ CYP3A4 inhibitors (e.g. ketoconazole, ritonavir, diltiazem), CYP2C9 inhibitors (e.g. amiodarone, fluconazole), tacrolimus. Rifampicin initially increases but subsequently decreases bosentan concentration. May decrease plasma levels of warfarin, statins (e.g. simvastatin, lovastatin), hormonal contraceptives, sildenafil, tadalafil. Potentially Fatal: Increased risk of hepatotoxicity may occur w/ glibenclamide. Ciclosporin markedly increases bosentan concentration.