Vazonimid (Solution) Instructions for Use

Marketing Authorization Holder

Pharmasintez-Tyumen, LLC (Russia)

ATC Code

C08CA06 (Nimodipine)

Active Substance

Nimodipine (Rec.INN registered by WHO)

Dosage Form

Vazonimid

Solution for infusion 0.2 mg/ml: fl. 50 ml 1 or 5 pcs.

Dosage Form, Packaging, and Composition

Solution for infusion transparent, from colorless to light yellow.

Excipients: ethanol 96% (ethyl alcohol) – 200 mg, macrogol 400 – 170 mg, sodium citrate (dihydrate) – 2 mg, anhydrous citric acid – 0.3 mg, water for injections – up to 1 ml.

50 ml – dark glass bottle (1) – cardboard packs.
50 ml – dark glass bottle (1) – cardboard packs (with connecting tube for infusion pump).
50 ml – dark glass bottle (5) – cardboard packs.
50 ml – dark glass bottle (5) – cardboard packs (with connecting tube for infusion pump).

Clinical-Pharmacological Group

A drug that improves cerebral circulation

Pharmacotherapeutic Group

Calcium channel blockers; selective calcium channel blockers with predominant vascular action; dihydropyridine derivatives

Pharmacological Action

Selective class II calcium channel blocker, a dihydropyridine derivative. Selectively interacts with L-type calcium channels and blocks the transmembrane influx of calcium ions. It has a vasodilating effect primarily on the vessels of the brain. Prevents or eliminates vasospasm caused by various vasoconstrictive biologically active substances. Causes a more pronounced increase in perfusion in areas of the brain with insufficient blood supply (compared to areas with normal blood supply). Improves cerebral circulation in subarachnoid hemorrhage.

It stabilizes the functional state of brain neurons. Improves memory and ability to concentrate.

It does not have a significant effect on systemic blood pressure, practically does not affect conduction in the AV and sinoatrial nodes and myocardial contractility. Reflexively increases heart rate in response to vasodilation.

Pharmacokinetics

When taken orally, it is rapidly absorbed from the gastrointestinal tract, C_max in plasma is reached within 1 hour. It undergoes intensive metabolism during the “first pass” through the liver. Bioavailability is low. Plasma protein binding is 95%. T_1/2 in the initial phase is 1-2 hours, in the terminal phase is 8-9 hours. It is excreted by the kidneys (less than 1% unchanged) and through the intestines.

Indications

Cerebrovascular insufficiency (including acute cerebral ischemia, decreased memory and ability to concentrate, mood lability). Treatment of residual effects of cerebrovascular accident and conditions after surgery for subarachnoid hemorrhage.

ICD codes

Dosage Regimen

For intravenous infusion only. Do not administer by intracardiac or any other route.

Initiate therapy within 96 hours of a confirmed subarachnoid hemorrhage. Administer via a central venous catheter to minimize local irritation and venous complications.

Prepare the infusion solution by transferring the contents of one 50 ml vial (containing 10 mg nimodipine) into a three-layer PVC infusion bag. Use only compatible infusion solutions: 0.9% Sodium Chloride, Ringer’s solution, 5% Dextrose, 10% Dextrose, or 6% Hydroxyethyl Starch in 0.9% Sodium Chloride.

Do not mix with other medications in the same infusion line or container. Protect the prepared solution from light.

For continuous infusion, administer at an initial rate of 1 mg/hour (equivalent to 5 ml of the prepared solution per hour). If well tolerated after two hours, increase the infusion rate to 2 mg/hour.

For patients with unstable blood pressure or body weight below 70 kg, initiate therapy at a reduced rate of 0.5 mg/hour (2.5 ml/hour). Increase to 1 mg/hour after two hours if tolerated.

The recommended duration of intravenous therapy is 5 to 14 days. Monitor blood pressure and heart rate continuously, especially during dose titration. Reduce the infusion rate or temporarily discontinue if a significant hypotensive effect occurs.

Following the intravenous course, transition to oral nimodipine therapy at a dose of 60 mg every 4 hours for 7 days, unless otherwise contraindicated.

Adverse Reactions

From the cardiovascular system: decreased blood pressure, bradycardia, flushing, occurrence or worsening of existing heart failure, extrasystole, angina pectoris (up to the development of myocardial infarction, especially in patients with severe obstructive coronary artery disease), arrhythmias (including short-term ventricular flutter, torsades de pointes arrhythmia); rarely – excessive decrease in blood pressure, tachycardia, transient visual impairment.

From the digestive system: nausea, diarrhea, discomfort in the gastrointestinal tract, dyspeptic symptoms, transient increase in the activity of transaminases, GGT and alkaline phosphatase in blood plasma, gingival hyperplasia (bleeding, soreness, swelling), constipation, dry mouth, increased appetite.

From the central nervous system: dizziness, headache, asthenia, extrapyramidal disorders, symptoms of CNS excitation (insomnia, increased psychomotor activity, agitation, aggressiveness), depression, fatigue, drowsiness.

From the respiratory system: difficulty breathing, cough, pulmonary edema, stridor breathing.

From the hematopoietic system: thrombocytopenia, agranulocytosis.

Allergic reactions: rarely – skin rash.

Other: joint pain and swelling, increased sweating, decreased renal function (increased urea concentration, hypercreatininemia), galactorrhea, weight gain, swelling of the feet and legs.

Contraindications

Severe arterial hypertension, pregnancy, lactation, hypersensitivity to nimodipine.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and during the lactation (breastfeeding) period.

Use in Renal Impairment

In case of impaired renal function, dose adjustment is required.

Geriatric Use

Elderly patients require dose adjustment.

Special Precautions

Use with caution in severe bradycardia, chronic heart failure, mild or moderate arterial hypotension, myocardial infarction with left ventricular failure, intracranial hypertension, with generalized cerebral edema.

In case of impaired renal function and in elderly patients, dose adjustment is required.

Effect on the ability to drive vehicles and operate machinery

Patients taking Nimodipine should refrain from engaging in potentially hazardous activities that require increased attention and speed of psychomotor reactions.

Drug Interactions

With simultaneous use with antihypertensive agents, an increase in the antihypertensive effect is possible.

With simultaneous use with beta-blockers, severe arterial hypotension and an increased risk of developing heart failure are possible.

With simultaneous use with aminoglycosides, cephalosporins, furosemide, impaired renal function is possible.

With simultaneous use with sodium valproate, the concentration of nimodipine in the blood plasma increases; with phenobarbital, phenytoin, carbamazepine, the bioavailability of nimodipine is significantly reduced.

With simultaneous use with cimetidine, a slight increase in the concentration of nimodipine in the blood plasma and an enhancement of its antihypertensive effect are possible.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.