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Ipidacrine

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2019-03-25
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$37.01
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Clinical Pharmacology

Pharmacotherapeutic group: Anticholinesterase agents.

ATC CODE: N07AA

Pharmacological properties

Pharmacodynamics

Ipidacrine is a reversible inhibitor of cholinesterase. It directly stimulates the conduction of impulses in the central nervous system (CNS) and neuromuscular synapses, blocking the potassium channels of the membranes. Enhances the effect on smooth muscles not only of the mediator acetylcholine, but also of adrenaline, serotonin, histamine and oxytocin.

Main pharmacological effects of ipidacrine:

- restoration and stimulation of neuromuscular conduction;

- restoration of impulse conduction in the peripheral nervous system after blockade caused by certain factors (for example, trauma, inflammation, local anesthetics, antibiotics, toxins and potassium chloride);

- increased contractility and tone of the smooth muscles of the internal organs;

- specific moderate stimulation of the CNS in combination with individual manifestations of sedative action;

- memory improvement.

In preclinical studies, ipidacrine had no teratogenic, embryotoxic, mutagenic, carcinogenic, or immunotoxic effects, and did not affect the endocrine system.

Sufficient data from clinical studies of the safety of ipidacrine in children are not available.

Pharmacokinetics

Absorption

After oral administration, ipidacrine is rapidly absorbed from the gastrointestinal tract. The maximum concentration in plasma after subcutaneous or intramuscular administration is achieved within 25-30 minutes. About 40-55% of the active substance is bound to plasma proteins. The therapeutic effect appears 15–20 minutes after parenteral administration. The duration of the drug is 3-5 hours.

Distribution

The drug penetrates the blood-brain barrier. Ipidacrine rapidly enters the tissue, only 2% of the drug is found in the plasma in an equilibrium state.

Metabolism and excretion

The drug is metabolized in the liver. Ipidacrine excretion is renal and extrarenal (through the gastrointestinal tract), excretion with urine prevails. The half-life of ipidacrine is 40 min. After parenteral administration, 34.8% of the applied dose of ipidacrine is excreted unchanged in the urine. This indicates a rapid metabolism of the drug in the body.

Indications

- Diseases of the central nervous system: bulbar paralysis and paresis.

- Diseases of the peripheral nervous system (neuritis, polyneuritis, polyneuropathy, polyradiculopathy, myasthenia gravis and myasthenic syndrome of various etiologies).

- The period of recovery after organic lesions of the central nervous system, accompanied by motor impairment.

Composition

1 ml of solution contains:

active ingredient: ipidacrine hydrochloride monohydrate - 5.4 mg or 16.2 mg (in terms of ipidacrine hydrochloride - 5.0 mg or 15.0 mg);

excipients: 1 M solution of hydrochloric acid to pH 2.8-4.0, water for injection to 1 ml.

Description

Transparent colorless liquid.

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Ipidacrine

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