Misenbo 62.5 Hasan tablets treat pulmonary hypertension (3 blisters x 10 tablets)

Dosage form Bosentan
Specifications High blood pressure

Ingredient

Composition information	Content
Bosentan	62.5mg

Uses

Indications

Treatment of pulmonary hypertension (Group I in the World Health Organization) in patients with symptoms of group III or IV of the World Health Organization, to improve training capacity and reduce the proportion of clinical cases.

Pharmacokology

endothelin - 1 (et - 1) is a neurological hormone acting by the cohesion with ETA and ETB receptors in endothelial and smooth muscle. ET -1 concentration increases in plasma and lung tissue of patients with pulmonary hypertension, suggesting the role of ET -1. Bosentan is a specific and competitive antagonist in the receptors of ETA and ETB endothelin. Bosentan has a slightly higher affinity for ETA receptor compared to the ETB receptor.

Pharmacokinetics

absorption

In healthy people, after taking the drug, the maximum plasma concentration of Bosentan is achieved within 3-5 hours and the sale time is about 5 hours. Less data on patients shows that Bosentan's accumulation in patients with pulmonary hypertension is about 2 times larger than healthy adults.

Bosentan's absolute bioavailability is about 50% and is not affected by food.

Distribution

The distribution volume is about 18 liters. Bosentan is highly connected (> 98%) with plasma prelhisin, mainly with albumin. Bosentan does not penetrate red blood cells.

Metabolism

The drug is metabolized in the liver. Bosentan has 3 metabolites, a pharmacological activity and can contribute 10-20% to the effect of Bosentan. Bosentan is an enzyme induction CYP2C9, CYP3A4 and maybe CYP2C19.

Elimination

Total clearance after 1 dose of intravenous injection is about 4 liters/hour in patients with pulmonary hypertension. When taking multiple doses, plasma concentrations in healthy adults gradually decrease by 50 - 65% of the concentration noticeable after using a single dose, possibly due to the induction effect of the metabolic enzymes in the liver. Stable state is achieved within 3-5 days. Bosentan is eliminated by the excretion of bile after being metabolized in the liver. Under 3% of an oral dose is excreted in urine. Disease time is about 5 hours.

Before taking Misenbo 62.5 Hasan tablets treat pulmonary hypertension (3 blisters x 10 tablets)

How to use

must take pills in the morning and afternoon, or not with food.

Dosage

Patients over 12 years old

Start treatment with Misenbo 62.5 mg/time x 2 times/day for 4 weeks. Then increase the dose up to the maintenance dose of 125 mg/time x 2 times/day. The person may be low (

Children

recommended dose for children 1 month old - 12 years old:

10 - 20 kg: Starting 31.25 mg/time/day, after 4 weeks to the maintenance dose of 31.25 mg/time x 2 times/day.

20 - 40 kg: Starting 31.25 mg/time x 2 times/day, after 4 weeks increase to maintenance dose 62.5 mg/time x 2 times/day.

Over 40 kg: Start 62.5 mg/time x 2 times/day, after 4 weeks increase to maintenance dose 125 mg/time x 2 times/day.

Patients with renal failure

No dose adjustment.

Note: The above dose is for reference only. Specific dosage depends on the condition and level of progression of the disease. For a suitable dose, you need to consult a doctor or medical specialist.What to do when overdose? Overdose can lead to obvious hypotension requires positive cardiovascular support.

There is no separate experience of overdose bosentan.

What to do when you forget a dose? However, if close to the next dose, skip the forgotten dose and take the next dose at the time as planned. Note that it should not be used double the prescribed dose.

Side Effects

Common, ADR> 1/100

No report.

Uncommon, 1/1000

No report.

Rare, ADR

The immune system: anaphylactic shock, angioedema.

Not determined frequency

Nervous system: headache, blushing, dizziness.

Respiratory system, chest and mediastinum: rhinitis.

General disorder: edema, fatigue.

blood vessels: Hypotenem pressure.

Cardiovascular system: Brushing chest drums.

Digestive system: digestive disorders.

Skin and subcutaneous tissue: itching, rash.

Blood and lymphatic system: Anemia.

Muscle system: cramps.

Liver system: Increased liver enzyme depends on the dose, abnormalities of liver function, cirrhosis, liver failure.

Instructions on how to handle ADR

When experiencing side effects of the drug, it is necessary to stop using and notify the doctor or go to the nearest medical facility for timely treatment.

Warnings

Contraindicated

Misenbo 62.5 contraindications in the following cases:

Hypersensitivity to Bosentan or any ingredients of the drug. 3 x ULN).

Be cautious when using

Do not start treatment with bosentan if the systolic blood pressure is below 85 mmHg.

Bosentan is contraindicated for medium and severe liver failure patients. Aminotransferase concentration should be measured before starting treatment, 1 time/month during treatment and 2 weeks after increasing dose.

Aminotransferase> 3 x ULN: Do not start treatment.

When being treated:

Aminotransferase concentration increases from 3-5 times ULN: Stop bosentan or dose reduction and monitor Aminotransferase levels every 2 weeks. If the Aminotransferase level returns to the value before treatment, it is possible to continue therapy or start over, but the concentration of aminotransferase should be tested after 3 days, after 2 weeks and every month.

Aminotransferase concentration increases from 5 to 8 times ULN: Stop bosentan and monitor Aminotransferase levels every 2 weeks. When the Aminotransferase level returns the value before treatment, consider the treatment again.

Aminotransferase concentration increases more than 8 times ULN or there are symptoms of liver poisoning, total bilirubin increased by 2 times so stop treatment and did not consider treatment again with Bosentan.

Monitor hemoglobin concentration after 1-3 months of treatment, then every 3 months during the treatment process. If hemoglobin concentration is significantly reduced, further evaluation should be assessed to determine the cause and demand for specific therapy.

Do not use bosentan in patients with hypotension. If used, bosentan should be stopped by reducing the dose slowly.

Bosentan may cause pulmonary edema, it is necessary to consider the possibility of a combined pulmonary disease and stop bosentan.

Be cautious in elderly patients because of high risk of reducing liver, kidney and heart function, simultaneous diseases or treatment with other drugs.

The ability to drive and operate machinery

The drug can cause headaches, dizziness should be cautious when driving and operating machinery.

Pregnancy

Misenbo 62.5 can be toxic to the fetus, so contraindicated for pregnancy. Pregnancy must be excluded before starting treatment with Misenbo 62.5. Only start treatment in women who are likely to get pregnant after pregnancy tests and apply adequate contraceptive methods in addition to endocrine contraceptives, including oral contraceptives, injections or subcutaneous implants.

Breastfeeding period

It is not known whether the drug is excreted in milk or not, so do not use Misenbo 62.5 for breastfeeding women.

Drug interaction

cytochrom p450

Bosentan is CYP2C9 and CYP3A touch agents. Therefore, the plasma concentration of the substance is metabolized by these two iszymes will decrease when used with bosentan.

Simultaneously use CYP2C9 inhibitors (fluconazole or amiodaron) and strong CYP3A inhibitors (ketoconazol, iTraconazole) or medium inhibitor CYP3A (Amprenavir, Erythromycin, Fluconazole, Diltiazem) with bosentane in plasma. There is no simultaneous use of the above drugs.

cyclosporin a

Increasing bosentane concentration while cyclosporin concentration decreases, so contraindications shared these two drugs.

tacrolimus

Increases the concentration of bosentan in plasma on animals, so it is necessary to be careful to coordinate.

glybid

Simultaneously used with bosentan causes liver aminotransferase so contraindicated use of these two drugs at the same time.

ketoconazole

Increases the plasma concentration of Bosentan, no need to adjust the dose of Bosentan but need to consider Bosentan's ability to act.

simvastatin and other statins

bosentan reduces plasma concentrations of statins metabolized by CYP3A4. It is necessary to consider the ability to reduce the effect of statin, monitor blood cholesterol levels after starting bosentan and adjust the dose of statin if necessary.

warfarin

Bosentan reduces the plasma concentration of warfarin. Because warfarin has a narrow treatment range, it is necessary to monitor blood clots and adjust the dose of warfarin if needed.

Sildenafil

Concentrated with Bosentan will reduce Sildenafil's plasma concentrations and increase bosentan plasma concentrations. Be careful when combining these 2 drugs.

rifampicin

Increases the bottom concentration of the first dose bosentan but reduces the concentration of bosentane in a stable state. Track the weekly liver function for the first 4 weeks, then monthly.

Hormone contraceptives

Bosentan reduces the concentration of norethindron and ethinylelestradiol of hormone contraceptives. Women need to apply additional methods of contraception when using bosentan.

lopinavir/ ritonavir or HIV treatment regimen has another Ritonavir

Bosentan is the substrate of organic anion transport protein (OATP), CYP3A, CYP2C9. Ritonavir inhibits OATP and CYP2C9. Need to adjust the dose of bosentan when starting Lopinavir/ Ritonavir.

Storage

Leave a cool place, avoid light, temperature below 30⁰C.

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