Bidiphar

DRUG

MEDICAL EQUIPMENT

BIRESORT 20

COMPOSITION:

Diluted Isosorbid dinitrate powder 25%....................80 mg

corresponding to Isosorbid dinitrate 5mg.

PHARMACEUTICAL FORM:tablets.

INDICATIONS:

-Prevention and long-term treatment of angina pectoris.

-Treatment of severe congested heart failure (in combination with other drugs).

DOSAGE AND ADMINISTRATIONS:

Treatment of angina pectoris:

- Keeping Biresort 5 under tongue or chewing 2,5-10mg/ time every 2-3 hours until the pain covered.

- Prevention of angina pactoris: 10-20mg/time, divided 3-4 times/day.

Treatment of congested heart failure:

- Keeping the drug under the tongue or chewing 5-10mg/ time;divided 3-4 times/day and then the dose should be reduced to maintenance dose.

- Or taking 10-20mg/time; divided 3-4 times/day and then the dose should be reduced to the maintenance dose.

CONTRAINDICATIONS:

- Low blood pressure.

- Cardiogenic shock.

- Severe anemia.

- Increase the pressure of intra-cranium, glocome.

- Right ventricle coronary.

- Artery stenosis and myocardium thrombosis.

- Cardiac sphincter inflammation.

- Allergy to organic nitrate.

PHARMACOKYNETICS:

- Mechanism: nitrate going to the body has been converted into oxyde nitric (NO) due to Glutathion - S - reductase and cystein; NO combines with thiol group into nitrosothiol (R-SNO), this activates cyclase guanylate to convert guanosine tri - phosphate (GTP) to guanosine 3'5 'monophosphat rounds (GMPc). GMPc causes myosine in the artery wall fibers non-activated, and non-ability of combination with actin, making a vasodilation.

- Nitrate has mainly effects on cardiac- artery system, high doses could vasodilate both artery system or coronary artery.

- Vasodilation could make a blood stagnancy in periphery and in viscera system, the blood to cardiac has been reduced, then lead to reduce pressure in cardiac. Vasodilation also makes to reduce periphery resistance, the results will lead to reduce blood pressure, especially in systole that could cause sympathetic reflex causing rapid pulse and increased systalic ability of cardiac. Nitrates also have the effect glomerules inhibitors.

- The drug will reduce oxygen using in cardiac, the supply and need of oxygen in cardiac will be balance. This will has an effect on disappearing the intense cardiac pains.

PHARMACODYNAMICS:

- Oral administration has been given, absorption will be more quickly if keeping Isosorbid dinitrat (ISDN) under the tongue or chewing. Medicine is metabolized mostly at first in liver. Two active metabolism substances are isosorbid - 2 mononitrat (2-ISMN) with short effect time and Isosorbid – 5 nitratmono (5 - ISMN) with longer effect time.

- Drug is bound with plasma protein to 28 ± 12%, is excreted mainly through urine.

- Half life elimination through plasma of ISDN is 50 ± 20 minutes, this of 2 - ISMN is about 2 hours, this of 5-ISMN is about 5 hours. Effect time is depended on usage:

+ Keeping under the tongue: Start working after 2 minutes. Maximum effect after 15-45 minutes. Prolong 1-3 hours.

+ Chewing: Start working after 5-20 minutes, prolong 1-3 hours

+ Oral administration: Start working after 15-45 minutes, maximum effect after 45 to 120 minutes and prolong 2-6 hours

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