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Isosorbide Mononitrate (Isomin)

Description

Isosorbide mononitrate is designed to prevent angina attacks; deal with chronic heart failure, some forms of pulmonary hypertension and pulmonary heart disease (all the 3 above - in a combination therapy).

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The course of action

The drug is well absorbed when taken orally. The bioavailability equals approximately 100% as it is not metabolized in the first pass through the liver. After ingestion it is built in the blood after 3.5 min; the maximum concentration is observed in 35-65 minutes. The volume of distribution is estimated at 600l, minimal therapeutic blood concentration 100 ng/ml. There is a direct relationship between the concentration in the blood, AUC and the dose of drug received. The drug almost does not bind to plasma proteins (less than 4%). It is metabolized in the kidney to form two pharmacologically inactive glucuronide (elimination half-life of these compounds 6-8 hours). Kidneys are displayed mainly as metabolites (98%). Renal clearance equals 1.8 l/min. A sustained-release of the active compound in the blood maximum concentration is achieved in 5 hours and the average timeframe to maintain a therapeutic concentration (100+ ng/ml) equals 17 hours.

Dosage regimen

Isosorbide mononitrate is taken orally 1 hour before or 2 hours after eating. Capsules should be taken without chewing, with a full glass of water (240ml). Initial dose 10-20 mg 2 times a day (for the PM intermediate-acting) or 40-50 mg 1 time per day (tablets and capsules). Starting from 3-4 day dose can be increased up to 20-40 mg two times a day(for PM average duration), if necessary, increasing the dose to 60-80 mg day. When taken 2 times a day is recommended to Ďasymmetricí scheme: the first reception should be initiated immediately after awakening, the second one - 7 hours later. The maximum dosage must not exceed 80 mg/24 hours

Side effects

Cardio-vascular system: at the beginning of treatment nitrate headache (usually disappears after a few days with continued treatment); hypotension, dizziness, tachycardia,weakness are possible. Rarely in severe hypotension increased symptoms of angina are manifested (nitrates paradoxical impact); in some cases collapse, bradyarrhythmia, syncope.

From the digestive system: rarely nausea, vomiting.

Dermatological reactions: transient redness of the skin; in some cases exfoliative dermatitis.

Allergic reactions: skin manifestations.

Other: in some cases reducing the rate of psychomotor reactions.

Contraindications

The medication course must not be initiated in the following cases: acute circulatory disorders (shock, circulatory collapse); cardiogenic shock in cases where a high end-diastolic pressure in the left ventricle is provided through the use of intra-aortic counterpulsation or by the administration of drugs that have a positive inotropic effect; severe hypotension (systolic blood pressure less than 90 mm Hg, diastolic less than 60 mm Hg); concomitant use of PDE-group drugs and in case of hypersensitivity to nitrates.

Special notes

The drug is not used for the relief of angina attacks. During the period of treatment it is not recommended to drive vehicles and engage in other activities that require rapid psychomotor reactions.

During treatment monitoring of blood pressure and heart rate is required. In case of necessity to use the drug on a background of arterial hypotension the drugs that have a positive inotropic effect should be simultaneously administered (or circulatory support remedies needed to be taken).

A part of the assignment, and high doses can cause the development of tolerance; in this case it is recommended to cancel the treatment within 24-48 hours or after 3-6 weeks of regular admission to make a break for 3-5 days.

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