DILASIDOM

Active material: Molsidomin
When ATH: C01DX12
CCF: Peripheral vasodilators. Antianginal drug
ICD-10 codes (testimony): i20, I50.0
When CSF: 01.06.01.02
Manufacturer: WARSAW PHARMACEUTICAL WORK POLFA S.A. (Poland)

Pharmaceutical form, composition and packaging

Excipients: potato starch, lactose, magnesium stearate, sucrose, paint orange, Kollidon 25.

15 PC. – blisters (2) – packs cardboard.
30 PC. – blisters (1) – packs cardboard.

Excipients: potato starch, lactose, magnesium stearate, sucrose, red lacquer, Kollidon 25.

15 PC. – blisters (2) – packs cardboard.
30 PC. – blisters (1) – packs cardboard.

Pharmacological action

Antianginal drug from the group sydnonimine. Effect of the drug is realized by forming in the metabolism of nitrogen oxide molsidomine (NO), which stimulates the soluble guanylate cyclase. As a result, there is an accumulation of cGMP, which relaxes smooth muscle walls of blood vessels. Relaxation of smooth muscles causes, in particular, increasing the capacity of the veins, thereby reducing venous return, which reduces both ventricular filling pressure. It, in turn, reducing myocardial oxygen consumption and improves hemodynamic conditions in the coronary circulation in the subendocardial layer. Expansion of the arteries causes a decrease in systemic vascular resistance, leading to the immediate reduction of the heart and reduce the intraventricular pressure. Besides, Dilasidom relieves spasm of the coronary arteries.

Onset of action is manifested through Dilasidoma 20 min after oral administration, when sublingual – through 5-10 m, and the duration of action is approximately 6 no.

Unlike nitrates causes development of tolerance with a decrease in effectiveness during prolonged therapy.

Pharmacokinetics

Absorption and distribution

After oral administration, molsidomine is almost completely absorbed from the gastrointestinal tract. Bioavailability is 60-70%. C_max achieved through 1 h and is 4.4 ug / ml. When administered after a meal slows absorption, but not reduced. Thus C_max in the blood is on 30-60 minutes later, than in the fasting. The minimum effective concentration in the blood plasma molsidomine is 3-5 ng / ml.

Molsidomine almost bound to plasma proteins. Not accumulates in the body (incl. in patients with renal insufficiency).

Metabolism

Molsidomine biotransformed in the liver to the active metabolite SIN-1 (3-morfolino-sidnonimin), from which it is formed by non-enzymatic unstable compound SIN-1A (N-morpholino-N-aminosynthonitrile), releasing NO to form a pharmacologically inactive compound SIN-1C. The metabolism and other compounds formed.

Deduction

T_1/2 is 0.85-2.35 no. Metabolites are excreted by the kidneys (90%), 9% – through the intestine.

Pharmacokinetics in special clinical situations

In severe hepatic insufficiency (increase the sample to bromsulfaleinovoy 20-50%) marked slowing clearance and increase in the concentration of molsidomine in plasma.

Testimony

- Chronic congestive heart failure (in combination with cardiac glycosides and / or diuretics);

- Prevention of angina attacks.

Dosage regimen

The drug is administered orally, regardless of the meal. The tablets should be swallowed whole, without chewing, drinking plenty of fluids.

To prevent strokes Dilasidom appoint 1-4 mg 2-3 times / day.

To relief of angina attacks – sublingually 1-2 mg.

Side effect

Cardio-vascular system: at the beginning of therapy – headache (stops during therapy); decrease in blood pressure, collapse (with initially elevated blood pressure decrease greater severity, than the baseline standard and reduced blood pressure).

CNS: dizziness, slowing of mental and motor responses (usually, at the beginning of treatment).

From the digestive system: nausea.

Allergic reactions: skin rash, itch, bronchospasm.

Contraindications

- Cardiogenic shock;

- Severe hypotension (systolic BP below 100 mmHg.);

- Glaucoma (particularly closure);

- Vascular collapse;

- Low pressure filling of the left ventricle;

- I trimester of pregnancy;

- Lactation (breast-feeding);

- Hypersensitivity to the drug.

Pregnancy and lactation

Application Dilasidoma contraindicated in the I trimester of pregnancy.

If necessary, use Dilasidoma lactation should decide the issue of termination of breastfeeding.

Cautions

With care use in patients with myocardial infarction (in acute stage – only under medical supervision and monitoring functions of the cardiovascular system).

With caution and under the control of BP appointed the first dose.

Elderly patients with impaired liver and kidney function and hypotension requires correction mode.

During treatment should avoid alcohol.

Effects on ability to drive vehicles and management mechanisms

During treatment (especially early in treatment) should refrain from driving vehicles and Occupation potentially hazardous activities, require increased attention and psychomotor speed reactions.

Overdose

Symptoms: Strong headache, a sharp decrease in blood pressure, tachycardia.

Treatment: if necessary, symptomatic therapy.

Drug Interactions

In an application with vasodilating Dilasidoma, antihypertensives and ethanol enhanced the severity of the hypotensive action.

In an application with acetylsalicylic acid Dilasidoma intensified antiplatelet effect.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

List B. The drug should be stored in a dry, protected from light and away from children at a temperature of 15 ° to 25 ° C. Shelf life – 3 year.