Misenbo 125 Hasan tablets treat hypertension (3 blisters x 10 tablets)

Dosage form Box of 3 blisters x 10 tablets
Specifications Bonsentan

Ingredient

Composition information	Content
Bonsentan	125mg

Uses

Indications

Misenbo 125 mg Hasan 3x10 medicine is indicated for treatment of pulmonary hypertension (Group I World Health Organization) in patients with symptoms of Group III or IV of the World Health Organization, to improve the ability to practice and reduce the rate of bad cases of clinical.

Pharmacokic

endothelin - 1 (et - 1) is a neurological hormone acting by the cohesion of ETA and ETB receptors in the 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

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

Absorption: Bosentan's absolute bioavailability in normal volunteers is about 50% and is not affected by food. The peak concentration of plasma is reached about 3-5 hours after taking 1 dose.

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

Metabolic: Bosentan 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 and CYP3A4 and may both CYP2C19.

Elimination: Total clearance after 1 dose of intravenous injection is about 4 iodine/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 125 Hasan tablets treat hypertension (3 blisters x 10 tablets)

How to use

oral drugs. Must take pills in the morning and afternoon, or not with food.

Dosage

Patients over 12 years of age: Start treatment at a dose of 62.5 mg x 2 times/day for 4 weeks. Then increase to the maintenance dose of 125 mg 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 x 2 times/day.

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

Over 40 kg: Start 62.5 mg x 2 times/day, after 4 weeks increasing to maintenance dose 125 mg 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? Large 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

When using Misenbo 125 mg Hasan 3x10, you may experience unwanted effects (ADR).

Side effects are reported including headache, rhinitis - throat, blushing, edema, hypotension, dizziness, chest drum, digestive disorders, itching, rash, fatigue, cramps, anemia.

Anaphylaxis and angioedema are rarely reported.

Increased liver enzyme depends on the dose may occur, abnormalities of liver function, cirrhosis and liver failure have been reported.

bosentan causes teratogenic animals.

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

Before using the drug you need to read the instructions carefully and refer to the information below.

Contraindicated

Misenbo 125 mg Hasan 3x10 contraindications in the following cases:

Hypersensitivity to Bosentan or any ingredients of the drug.

Pregnant women.

Concentrated with cyclosporin A (significantly increases the plasma concentration of bosentan), glyburic (increasing the risk of increasing liver enzymes).

Moderate or severe liver failure, patients with high aminotransferase (> 3 x ULN).

Be cautious when using

Do not start treatment with bosentan if the systolic blood pressure collects 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.

Do not start treatment with Bosentan in patients with aminotransferase levels 3 times higher than the above limit.

If the concentration of aminotransferase is 3-5 times higher during treatment, bosentan should be stopped or reduced and monitor Aminotransferase levels every 2 weeks. If the Aminotransferase level returns to the values before treatment, it is possible to continue the treatment or begins again, but the concentration of aminotransferase should be tested after 3 days, after 2 weeks and every month.

If the concentration of aminotransferase increases 5-8 times, it is advisable to stop using bosentan and monitor the concentration of aminotransferase every 2 weeks. When aminotransferase levels return to the value before treatment consideration.

If the concentration increases more than 8 times or there are symptoms of liver poisoning or increased bilirubin, totaling 2 times higher, stop treatment and do not consider the treatment back to bosentan.

Need to monitor hemoglobin concentration after 1 and 3 months of treatment and then every 3 months during treatment. If the hemoglobin concentration is significantly reduced, further evaluation is needed to determine the cause and demand for specific therapy.

Do not use bosentan in patients with hypotension. Although there is no evidence of acute response after stopping Bosentan, to avoid clinical deterioration, slow dose should be reduced.

If the signs of pulmonary edema occur when using Bosentan, it is necessary to consider the possibility of a combined venous disease and stop using Bosentan.

Be cautious to choose the dose for elderly patients, considering high frequency to reduce liver, kidney or heart function, simultaneous diseases or treatment with other drugs.

Bosentan and endothelin receptor antagonists cause teratogenicity in mice and should not be used for pregnant women or women who have the ability to give birth but do not use reliable contraception; Hormonal contraception may be incomplete.

The ability to drive and operate machinery

Because the side effects of the drug can cause headaches, dizziness should be cautious when driving and operating machinery.

Pregnancy

bosentan can be toxic to the fetus, so contraindications for pregnancy. Pregnancy must be eliminated before starting treatment with Bosentan, then prophylaxis with firm contraception. Only start treatment with Bosentan in women who are likely to be pregnant after a negative pregnancy test and only in women who apply adequate contraceptive methods in addition to hormonal contraceptives, including oral contraceptives, injected through the legs or implant under the skin. Pregnancy tests for urine or subsequent serum must be done monthly in women who are likely to get pregnant bosentan.

Breastfeeding period

Whether the drug is excreted in the milk or not. Because many drugs are excreted in human milk, do not breastfeed during medication.

Drug interaction

cyclosporin A: Bosentane concentration in plasma increases while cyclosporin levels decrease, so contraindicated when using bosentane and cyclosporin a.

tacrolimus: simultaneous use of bosentan and tacrolimus on animals significantly increases the plasma concentration of bosentan. Need to be cautious if used simultaneously.

glyburid: Increased risk of liver aminotransferase in patients with Bosentan simultaneously with glyburid. Contraindications for combination and consideration of other hypoglycemic drugs. The use of simultaneously reduces the concentration of bosentan plasma, glyburid as well as other oral hypoglycemic drugs metabolized mainly by CYP2G9 or CYP3A4. It is necessary to consider the possibility of reducing blood sugar control in patients taking these drugs.

Azol antifungal drugs: Increases bosentan plasma concentrations. No need to adjust the dose of Bosentan but must consider the possibility of increasing the effect of bosentan.

Simvastatin and other statins: simultaneously reducing plasma concentrations of simvastatin and other statins metabolized by CYP3A4. It is necessary to consider the ability to reduce the effect of statin, monitor blood cholesterol levels after starting to use bosentan and adjust the dose of statin if necessary.

warfarin: Use simultaneously reduces the plasma concentration of warfarin. Clinical experience does not show clinical changes in Inr or Warfarin dose. Because Warfarin has a narrow treatment index, it is necessary to monitor blood coagulation parameters and adjust the dose of warfarin if needed.

digoxin, nimodipine and losartan: Bosentan has no pharmacokinetic interactions meaningful to digoxin and nimodipine; Losartan has no significant effect on the plasma concentration of Bosentan.

Sildenafil: Simultaneously reduces Sildenafil's plasma concentrations and increases Bosentan's plasma concentrations. Caution should be careful when using, monitoring clinical reactions and side effects, adjusting the dose if necessary.

rifampicin: simultaneously used to increase the bottom concentration of bosentan after the dose at the same time but reduce the concentration of bosentan in a stable state. Track the weekly liver function for the first 4 weeks, then monthly.

Hormone contraceptives: A interactive study has shown that simultaneous use of bosentan with oral oral contraceptive oral contraceptives causes an average reduction in norethindron and ethinyl estradiol, equivalent to 14% and 31%. However, the corresponding exposure reduction is 56% and 66%. Therefore, hormonal contraceptives include oral medications, legs and subcutaneous implants may be uncertain when used with bosentan. Women need to apply additional methods of contraception when using bosentan.

Lopinavir/Ritonavir or other Ritonavir treatment regimen: In vitro data shows that Bosentan is a substrate of organic anion transport protein (OATP), CYP3A, CYP2C9. Ritonavir inhibits OATP and CYP3A. However, the impact of ritonavir on Bosentan pharmacokinetics is largely due to its influence on OATP. On normal volunteers, simultaneously use Bosentan 125 mg 2 times/day with Lopinavir 400 mg/ritonavir 100 mg x 2 times/day increasing the bottom concentration of Bosentan on Wednesday and 10, equivalent about 48 times and 5 times compared to those who only use Bosentan. Therefore, it is necessary to adjust the dose of Bosentan when starting to use Lopinavir/Ritonavir. Simultaneously indicated Bosentan 125 mg x 2 times/day does not have a significant impact on pharmacokinetics of Lopinavir 400 mg/ritonavir 100 mg x 2 times/day.

Storage

Where dry, less than 30 ° C.

Other drugs

Disclaimer

Every effort has been made to ensure that the information provided by Drugslib.com is accurate, up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. Drugslib.com information has been compiled for use by healthcare practitioners and consumers in the United States and therefore Drugslib.com does not warrant that uses outside of the United States are appropriate, unless specifically indicated otherwise. Drugslib.com's drug information does not endorse drugs, diagnose patients or recommend therapy. Drugslib.com's drug information is an informational resource designed to assist licensed healthcare practitioners in caring for their patients and/or to serve consumers viewing this service as a supplement to, and not a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners.

The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. Drugslib.com does not assume any responsibility for any aspect of healthcare administered with the aid of information Drugslib.com provides. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist.