Droperidol (solution for injections 0.25%)

Solutio Droperidoli 0.25% pro injectionibus

International not patented name

Droperidol

Pharmacotherapeutic group

Neuroleptics

Preparation composition

1 ml of the solution for injections contains 2.5 mg of droperidol.

Pharmacologic action

Pharmacodynamics

Neuroleptic, anti-psychotic, sedateive, anti-vomiting, anti-shock preparation. It blocks the dofamine receptors (mostly D₂) in the subcortical areas of the brain, suppresses the central alpha-adrenergic structures, violates the reverse neurons capture and noradrenalin deposition.

After the preparation injection psychic indifference develops. It possesses a strong cataleptogenic activity. The preparation potentiates the narcotics and analgesics effect. Being injected parenteral it acts in 3 – 10 minutes the maximal effect being observed in 30 minutes.

Pharmacokinetics

When injected intravenous and intramuscular the preparation plasma maximal concentration is achieved in 15 minutes. 85 – 95% of the preparation is fixed with the plasma proteins. The period of droperidol half elimination is about 134 minutes. It is metabolized in the liver. It is excreted mainly as its metabolites and in the unchanged form by the kidneys and through the intestine (in the unchanged form – 1% and 11% respectively).

Indications

Need in neuroleptanalgesia, psychomotor excitement in the postoperative period, poisoning, preparing patients to narcosis, to surgical interferences, hallucinations, hypertonic crises, traumas, myocardial infarction, shock.

Mode of appliance and dosing regime

The preparation is injected subcutaneous, intramuscular and intravenous.

For pre-medication the preparation is injected intramuscular 15 – 45 minutes before the surgical interference beginning the droperidol dose being 2.5 – 5 mg (1 – 2 ml of 0.25% solution). Children are injected droperidol in dose of 100 µg/kg of the body mass.

For the initial narcosis  the preparation is injected intravenous in dose 15 – 20 mg (6 – 8 ml) to adults and intravenous in dose 200 – 400 µg/kg of the body mass or intramuscular in dose 300 – 600 µg/kg of the body mass to children.

For hypertonic crisis cupping the preparation is infused intravenous in dose 0.1 mg/kg (usually 2 ml of 0.25% solution).

In the postoperative period adults are prescribed 2.5 – 5 mg ( 1- 2 ml of the preparation) intramuscular the intervals between the injections being 6 hours.

Special warnings

The preparation is applied under the in-hospital conditions exclusively.

Contraindications

Hypersensitivity, extra-pyramidal disturbances, operative interferences in the late terms of pregnancy (cesarean section), early childish age (younger 2 years).

Side effects

Arterial pressure reducing, breathing suppression, depressive states, dysphoria, extra-pyramidal symptoms.

Safety measures

For preventing orthostatic hypotension the patient is recommended to be transported with care. The elderly and physically weak patients should be prescribed smaller initial doses. The preparation should be applied with care in case the liver and kidneys functions are changed.

The preparation should be applied with care in case it is prescribed in combination with corticosteroids and insulin.

Interaction with other medicines

The benzodiazepine derivatives enhance and the dofamine receptors agonists (bromocriptine) reduce the droperidol effect. The preparation increases the opioid analgesics, soporific and narcotic drugs activities.

Overdosing

Symptoms: the side effects severity increase on the background of arterial hypertension.

Treatment: in case the extra-pyramidal disturbances appear anti-parkinsonic drugs are applied. The arterial pressure reduction is cupped by analeptic and sympathomimetic drugs. In case of hypovolemia the OCK restoration is recommended.

Dosage form

0.25% solution in 2 ml or 5 ml vials, in 5 ml bottles. Ten vials in a pack, 10 bottles in a pack.