Bosentan is available only under a special program from a certified pharmacy. You must be registered in the program and understand the risks and benefits of taking this medication.
Bosentan APOTEX is a drug made in Australia. You need a doctor's prescription to buy it. But its analogues can be bought online anywhere in the world without going to a specialist.
Bosentan is a complete analogue of Bosentan APOTEX. It has the same composition, dosage and methods of use. Also Bosentan has a lower cost compared to Bosentan APOTEX.
To buy Bosentan APOTEX, click on the "buy now" button and then in our online store select the medicine and the desired dosage. Follow the instructions below.
Free delivery is valid for purchases from $200. We deliver medicines around the world and provide the best prices.
You can also use a coupon giving a 5% discount.
Side effects
Use the medicine exactly as directed. low blood pressure, fainting; irregular heartbeats; or swelling of the feet/ankles/legs, or upset stomach, swelling in your legs or ankles, with or without weight gain; flushing, headache, joint pain; dizziness,
Warnings
Some medicines can cause unwanted or dangerous effects when used with bosentan. Your doctor may change your treatment plan if you also use:
- cyclosporine; or
- glyburide.
Bosentan can decrease sperm count and may affect fertility in men (your ability to have children).
If you are the parent or caregiver of a female child taking this medicine, talk to the child's doctor once you notice any signs of puberty (breast development or pubic hair), even if menstrual periods have not yet begun.
Interactions
Elbasvir: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Elbasvir. Avoid combination
Indinavir: May increase the serum concentration of Bosentan. Bosentan may decrease the serum concentration of Indinavir. Management: Initiate bosentan at, or adjust bosentan to, 62.5 mg once daily or every other day (based on tolerability) in indinavir-treated patients (see ritonavir for dosing if that agent is used). Additionally, monitor for possible reduced response to indinavir. Consider therapy modification
Neratinib: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Neratinib. Avoid combination
Food interaction
Take without regard to meals.
Pregnancy
- The estimated background risk of major birth defects and miscarriage of the indicated population is unknown.
- Pregnant women should be extra careful while using this drug.
Overview
Impact on the ability to drive vehicles and moving machinery
The effect of bosentan on the ability to drive a car and engage in other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions has not been studied, but given that bosentan can cause dizziness, caution should be exercised when performing such activities.
Storage conditions
Trade Names
Traklir: coated tablets 125 mg, 62.5 mg; Actelion Pharmaceuticals (Switzerland)
Synonyms
Composition and form of release
Bozentan (in the form of a monohydrate). Orange-white coated tablets (62.5 mg, 125 mg).
pharmachologic effect
Non-selective antagonist of endothelin receptors such as ETA and ETB. Vasodilator. The neurohormone endothelin-1 (ET-1) is one of the most powerful vasoconstrictors. It induces fibrosis, cell proliferation, hypertrophy and myocardial remodeling, and exhibits pro-inflammatory activity. These effects are caused by ET-1 when it is bound to ETD and ETB receptors located in the endothelium and vascular smooth muscle cells.
The concentration of ET-1 increases with cardiovascular diseases, which suggests the pathogenic role of ET-1 in the development of these diseases. Bozentan competitively blocks ET receptors and does not bind to other receptors, reduces the resistance of systemic and pulmonary vessels.
Pharmacokinetics
Bioavailability - 50%, does not depend on food intake. Binding to plasma proteins - 98%. It is metabolized in the liver with the participation of isoenzymes CYP2C9 and CYP3A4 with the formation of 3 metabolites, including one active. Bosentan is an inducer of the isoenzymes CYP2C9 and CYP3A4, as well as, possibly, the isoenzyme CYP2C19 and P-glycoprotein. Excreted in the bile and slightly in the urine.
Indications
Application
Tablets should be taken orally in the morning and evening, regardless of the time of meal. At the initial stage, therapy and observation should be carried out only by a doctor who has experience in the treatment of pulmonary arterial hypertension. The initial dose is 62.5 mg 2 r / day for 4 weeks, then the dose is increased to a maintenance dose of 125 mg 2 r / day.
In the case of clinical deterioration (for example, when walking distance is reduced by at least 10% during the 6-minute test compared with the initial values ​​determined before the start of therapy), despite the use of bosentan for at least 8 weeks (of which the Bosentan dose of at least 4 weeks), alternative treatment methods should be considered.
Drug withdrawal is carried out gradually along with the use of alternative therapy. If you need to increase the dose of bosentan, APOTEX should carefully weigh the risk / benefit ratio for the patient, taking into account the fact that the hepatotoxicity of the drug depends on the dose. Side effect. Side effects included headache, hot flashes, feeling hot, impaired liver function, dyspepsia, dry mouth, swelling of the lower extremities, palpitations, arterial hypotension, anemia, fatigue, and pruritus. All of these phenomena were dose dependent.
Contraindications
Impaired liver APOTEX of moderate and severe severity, an initial excess of liver enzyme activity by more than 3 times, concomitant use of cyclosporin A, pregnancy, age up to 12 Bosentan, hypersensitivity to bosentan or to any of the components of the drug.
Overdose
When prescribing bosentan to healthy volunteers once in a dose of 2400 mg and patients with other diseases, in addition to pulmonary hypertension at a dose of 2000 mg / day for 2 months, the most common adverse event was headache in mild or moderate form. There is no specific experience with taking an excessive dose of bosentan in excess of the indicated doses. Overdose can lead to severe arterial hypotension, requiring active support of cardiovascular function.
Interaction with other medicines
The simultaneous use of inhibitors of isoenzymes CYP3A4 and CYP2C9 should be avoided. Bozentan is an inducer of the isoenzymes CYP2C9 and CYP3A4, presumably also induces the isoenzyme CYP2C19. Thus, plasma concentrations of substances metabolized by these isoenzymes will decrease while taking bosentan.
The possibility of changes in the effectiveness of drugs that are metabolized by these isoenzymes should be considered. Bozentan is metabolized by isoenzymes CYP2C9 and CYP3A4. Suppression of the activity of these isoenzymes can lead to an increase in the concentration of bosentan in blood plasma. Caution should be exercised when using a combination of bosentan with inhibitors of the isoenzyme CYP2C9, CYP3A4 (fluconazole, voriconazole, ketoconazole, itraconazole, ritonavir, etc.).
Since estrogens and progestogens are partially metabolized by isoenzymes of the cytochrome P450 system, there is a risk of a lack of contraceptive effect while taking bosentan. For this reason, women of childbearing age should use additional or alternative methods of contraception while taking bosentan. The simultaneous use of bosentan with cyclosporine A is contraindicated. This is due to the fact that with their simultaneous use, the concentrations of bosentan in the blood plasma were approximately 30 times higher than the levels observed with the introduction of only one bosentan. In the stable phase, the concentration of bosentan in blood plasma was 3-4 times higher than when using only one bosentan. The mechanism of this interaction has not yet been clarified. Blood cyclosporin A concentrations (CYP3A4 isoenzyme substrate) decreased by about 50%.
