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 GH 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 GH. It has the same composition, dosage and methods of use. Also Bosentan has a lower cost compared to Bosentan GH.
To buy Bosentan GH, 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
Your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. flushing, tiredness, fatigue, dizziness, headache, low blood pressure, fainting; swelling in your legs or ankles, with or without weight gain; irregular heartbeats; or
Warnings
Do not use bosentan if you are pregnant or think you might be pregnant. This medicine can cause serious birth defects. Tell your doctor right away if you miss a menstrual period or think you may have become pregnant during treatment.
Bosentan can decrease sperm count and may affect fertility in men (your ability to have children).
You should not use bosentan if you are allergic to it, or if you are pregnant or might become pregnant during treatment.
Interactions
CycloSPORINE (Systemic): May increase the serum concentration of Bosentan. Bosentan may decrease the serum concentration of CycloSPORINE (Systemic). Avoid combination
Clarithromycin: Bosentan may increase serum concentrations of the active metabolite(s) of Clarithromycin. Specifically, bosentan may increase concentrations of 14-hydroxyclarithromycin. Bosentan may decrease the serum concentration of Clarithromycin. Clarithromycin may increase the serum concentration of Bosentan. Management: Consider alternative antimicrobial if possible. The clinical activity of clarithromycin may be altered, and increased bosentan toxicity may be expected. Consider therapy modification
Olaparib: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Olaparib. Avoid combination
Food interaction
Take without regard to meals.
Pregnancy
- If progestins were given to the mother in that same dosage, serious birth defects could occur.
- Talk to your healthcare provider if you have questions about this risk during pregnancy.
Overview
The simultaneous use of Traklir in a dose of 125 mg 2 times / day. within 5 days, it reduced the levels of simvastatin concentration in blood plasma (substrate of the isoenzyme CYP3A4) and the active metabolite of β-hydroxy acid by 34% and 46%, respectively. Concomitant use of simvastatin did not affect plasma concentrations of bosentan. It is recommended to monitor cholesterol levels with subsequent dose adjustment.
The simultaneous use of Traklir in a dose of 62.5 mg 2 times / day. for 6 days and ketoconazole (a potent inhibitor of CYP3A4) led to about a 2-fold increase in the concentrations of bosentan. No dose adjustment for Traklir is required. Similar increases in plasma concentrations of bosentan can be expected while taking other potent inhibitors of CYP3A4 (such as itraconazole and ritonavir), although this can used not been demonstrated during in vivo studies. However, when using combination therapy in combination with a CYP3A4 inhibitor in patients with impaired CYP2C9 metabolism, the risk of increasing the concentration of bosentan in the blood plasma by a significant level increases, which can lead to the development of potentially serious side effects.
The simultaneous use of Traklir at a dose of 500 mg 2 times / day. within 7 days led to a decrease in AUC, Cmax and Cmin of digoxin by 12%, 9% and 23%, respectively. The mechanism of this interaction may be the induction of P-glycoprotein. The clinical relevance of this interaction does not Bosentan serious.
The limited results of the study (AC-052-356, BREATHE-3), in which 10 children received Traclir in combination with epoprostenol, indicate that after single and multiple doses of Cmax and AUC bosentan were approximately the same in patients receiving and not treated with a long course of epoprostenol in the form of infusions.
Dosage and administration
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 times / day. for 4 weeks, then the dose is increased to a maintenance dose of 125 mg 2 times / day. In the case of clinical deterioration (for example, when the walking distance is reduced by at least 10% during the 6-minute test compared to the initial values determined before the start of therapy) despite the use of Traklir for at least using weeks (of which the recommended dose at least 4 weeks), alternative treatment methods should be considered. However, some patients who did not have a therapeutic response after 8 weeks of taking Traklir may experience a positive effect after an additional 4-8 weeks of therapy. If a decision is made to cancel Traklir, this should be done gradually simultaneously with the use of alternative therapy.
In the event of a clinical deterioration several months after the start of therapy, despite the use of Traklir, the appropriateness of its continuation should be reviewed. In some patients who do not have a positive effect when taking a dose of 125 mg 2 times / day, exercise tolerance can improve with an increase in dose to 250 mg 2 treatment for / day. The risk / benefit ratio for the patient complete be carefully weighed taking into account the fact that the hepatotoxicity of the drug is dose-dependent.
For children, the drug is prescribed taking into account body weight
Body Weight (kg) Initial Dose (4 weeks) Maintenance Dose
≥10, but ≤20 31.25 mg 1 time / day. 31.25 mg 2 times / day.
> 20, but ≤40 31.25 mg 2 times / day. 62.5 mg 2 times / day.
> 40 62.5 mg 2 times / day. 125 mg 2 times / day.
Insufficiently documented data regarding the effectiveness and safety of therapy in children under 12 years of age.
There is only limited experience with observations after abruptly discontinuing Traklir therapy. There is no evidence of a serious exacerbation of the disease as a result of such cancellation. Nevertheless, in order to avoid the threat of worsening of the clinical condition due to the possible effect of withdrawal, it is recommended to gradually reduce the dose Bosentan it by half within 3-7 days). During treatment withdrawal, Bosentan is recommended to conduct intensive monitoring of the patient's condition.
No dose adjustment is required for patients with mild hepatic impairment. Traklir is contraindicated in patients with impaired liver function of moderate and severe severity.
For patients with impaired Bosentan function, dose adjustment is not required. No change in dose required during dialysis.
No dose adjustment required for patients over 65.
There is only limited experience in therapy in patients weighing less than 40 kg.
Storage conditions: The drug should be here out of the reach of children at a temperature not exceeding 30 ° C.
Shelf life: 3 years.
Conditions of dispensing from pharmacies: Prescription drug.
Structure
In 1 tablet bosentan monohydrate 62.5 mg or 125 mg. Corn starch, pregelatinized starch, sodium carboxymethyl starch, glyceryl tribhenate, povidone, hypromellose, magnesium stearate, triacetin, titanium dioxide, talc, iron oxide, as auxiliary substances.
Release form
Film-coated tablets 62.5 mg and 125 mg.
pharmachologic effect
Pharmacodynamics and pharmacokinetics
Pharmacodynamics
Traklir (Bosentan) is an antagonist (non-selective) endothelin receptors. Neurohormone endothelin-1 - the most powerful vasoconstrictor, playing a role in the genesis hypertension. He induces fibrosis, cell proliferation and myocardial hypertrophy. These effects appear upon binding. endothelin with receptors in vascular endothelium.
The concentration of this neurohormone increases with cardiovascular disease, pulmonary hypertension, CHF, myocardial https://zentherapycenter.com/let-c/coplavix.php, atherosclerosis and hypertension. Active substance by blocking ET receptors, reduces vascular resistance, which leads to a decrease in pressure when pulmonary hypertension, increased cardiac output, while Heart rate does not change.
Pharmacokinetics
Pharmacokinetics depend on the dose and time. Bioavailability is 50%, it is not affected by food intake. Cmax in plasma is determined after 3-5 hours. 98% bound to proteins. Metabolized in the liver to three metabolites, one of them is pharmacologically active. Bosentan -inductor CYP2C9 and CYP3A4. Excreted in bile and only 3% in urine.
With unexpressed impaired liver function, the pharmacokinetics do not change. With severe renal impairment, the concentration of the active substance decreases. The concentration of metabolites increases 2 times. No dose adjustment required.
Indications for use
As part of complex therapy, it is used for:
- primary Lacto-Free arterial hypertension;
- secondary pulmonary arterial hypertension (at scleroderma, if there is no severe lung damage);
- pulmonary hypertension against the background of congenital heart defects;
- prevention of ulcerative lesions in systemic scleroderma.
Contraindications
- hypersensitivity;
- age up to 3 years;
- pregnancy;
- breast-feeding;
- arterial hypotension;
- level up liver transaminase;
- impaired liver function (moderate and severe);
- reception at the same time cyclosporin A;
- reproductive age in women (in the absence of contraception).
Caution is prescribed with unexpressed impaired liver function.
Side effects
