Vero-Pipecuronium - instructions for use, dose, side effects, contraindications

Pharmacodynamics:Nondepolarizing long-acting muscle relaxant. Due to the competitive link with the nicotine-sensitive acetylcholine receptors located in the motor endings of the striated muscle fibers, it blocks the transmission of the signal from the nerve endings to the muscle fibers.

In contrast to depolarizing muscle relaxants pipecuronium bromide does not cause muscle fascination.

Even at doses several times greater than its effective dose, which is necessary for a 90% reduction in muscle contractility (ED₉₀), does not have ganglion blocking, vagolytic and symptomatic activity. Piperecuronium bromide does not have a hormonal effect, does not cause the release of histamine from mast cells.

With a balanced dose of ED anesthesia₅₀ and ED₉₀pipecuronium bromide are 30 and 50 μg / kg body weight, respectively. A dose of 50 mcg / kg provides 40-50 minutes of muscle relaxation.

The maximum effect of pipecuronium bromide depends on the dose and occurs after 1.5-5 minutes, with the effect developing most rapidly at doses of 70-80 μg / kg.

A further increase in the dose reduces the time required for the development of the effect, and significantly prolongs the effect of the drug.

Pharmacokinetics:With intravenous administration, the initial volume of distribution (Vd_c) is 110 ml / kg, the volume of distribution in the saturation phase (Vd_ss) - 300 ± 78 ml / kg, plasma clearance (Cl) -2.4 ± 0.5 ml / min / kg, mean half-life (T_1/2_β) - 121 ± 45 min, the average time spent in the blood plasma (MRT) is 140 min. It penetrates insignificantly through the placenta.
With the repeated administration of maintenance doses, the cumulative effect is unimportant,if at the time of 25% recovery of baseline contractility, doses of 10 and 20 μg / kg are used. It is excreted mainly by the kidneys, the liver also participates in elimination. One third is unchanged, the rest is in the form of 3-deacetyl-pipecuronium.

Indications:Relaxation of skeletal muscles and relief of endotracheal intubation in surgical interventions of various nature and diagnostic procedures in conditions of mechanical ventilation (IVL) requiring more than 20-30 minutes of muscle relaxation.

Contraindications:Children up to 3 months. Hypersensitivity to pipecuronium and / or bromine.

Carefully:Obstruction of biliary tract, edematic syndrome, dehydration, disturbance of water electrolyte metabolism, hypothermia, myasthenia gravis, respiratory failure, renal and / or hepatic insufficiency, decompensated heart failure.

Pregnancy and lactation:Experience sufficient to prove the safety of pipecuronium bromide for pregnant and fetus is absent.

In case of application for general anesthesia with Caesarean section pipecuronium bromide does not change the Apgar score, muscle tone and cardiovascular adaptation of newborns.

Data on the use of pipecuronium bromide during lactation are absent.

Dosing and Administration:Intravenously.

Immediately before the administration of 4 mg (1 bottle) of the lyophilized powder is diluted in 2 ml of 0.9% sodium chloride solution.

The dose of Vero-pipecurony is selected for each patient individually, taking into account the type of anesthesia, the estimated duration of the surgical intervention, possible interactions with other medications used before or during anesthesia, concomitant diseases and the general condition of the patient. It is recommended to use a stimulator of peripheral nerves to provide control of the neuromuscular block.

Recommended doses for adults and children over 14 years of age

The initial dose for intubation and subsequent surgical intervention: 60-80 μg / kg body weight, provides good / excellent conditions for intubation for 150-180 sec, while the duration of muscle relaxation is 60-90 minutes. The initial dose for miorelaxation with intubation with succinylcholine: 50 μg / kg, provides 30-60-minute muscle relaxation.

The maintenance dose: 10-20 μg / kg, provides a 30-60-minute relaxation during a surgical operation.

In chronic renal insufficiency, the amount of the administered dose is calculated depending on the creatinine clearance (CC): at a CC of 100 ml / min - 85 mcg / kg; at a CC of 80 ml / min - 70 mkg / kg; with SC 60 ml / min - 55 μg / kg; with SC less than 40 ml / min -50 μg / kg.
With obesity, the dose is calculated based on the "ideal" body weight.

Doses in children:

from 3 to 12 months - 40 mkg / kg (which provides muscle relaxation lasting 10-44 min), from 1 year to 14 years - 57 mkg / kg (muscle relaxation - 18-52 min).

Termination of the effect:

At the time of 80-85% of the blockade, measured with a stimulant of peripheral nerve fibers, or at the time of partial blockade, determined by clinical signs, the use of atropine (0.5-1.25 mg) in combination with neostigmine (1-3 mg) or galantamine (10-30 mg) stops the muscle-relaxing effect of Vero-pipecuronium.

Side effects:From the nervous system: oppression of the central nervous system (CNS), hypoesthesia.

From the musculoskeletal system: muscle weakness after cessation of muscle relaxation, muscle atrophy.

From the respiratory system: hypopnea, apnea, atelectasis of the lung, respiratory depression.

From the cardiovascular system: myocardial ischemia (up to myocardial infarction) and the brain, atrial fibrillation, ventricular extrasystole, bradycardia, lowering of blood pressure (BP).

On the part of the organs of hematopoiesis and the system of hemostasis: thrombosis, reduction of partial thromboplastin and prothrombin time.

From the side of the urinary system: anuria.

Allergic reactions: skin rash, hives, laryngospasm, angioedema.

Laboratory indicators: hyperkreatinemia, hypoglycemia, hyperkalemia.

Overdose:Symptoms: paralysis of the respiratory musculature, apnea, marked decrease in blood pressure.

In case of an overdose, the effects of Vero-pipecuronium are eliminated by the introduction of an acetylcholinesterase inhibitor-neostigmine (1-3 mg) in combination with atropine (0.5-1.25 mg) or galanthamine (10-30 mg). Simultaneously, an artificial ventilation of the lungs should be performed until spontaneous breathing is restored.

Interaction:The intensification and / or prolongation of the action of Vero-pipecuronium can cause:

- Means for inhalation anesthesia (halothane, methoxyflurane, diethyl ether, enflurane, isoflurane, cyclopropane);

- Means for intravenous anesthesia (ketamine, fentanyl, propanidide, barbiturates, etomidate, Υ-hydroxybutyric acid);

-suxamethonium chloride or other nondepolarizing muscle relaxants;

-Some antibiotics and chemotherapeutic drugs (aminoglycosides, tetracyclines, polypeptides, imidazole and its derivatives, clindamycin, lincomycin, polymyxin), antifungal medications (amphotericin B), quinidine, magnesium preparations, procainamide, diuretics; beta and alpha-blockers; thiamine, monoamine oxidase (MAO) inhibitors, guanidine, protamine, phenytoin, calcium antagonists, lidocaine (for intravenous administration).

Patients taking magnesium salts, capable of potentiating neuromuscular blockade, pipecuronium bromide should be administered in reduced doses.

Weakening the effect of Vero-pipecuronium:

Long-term preliminary use of glucocorticosteroids, neostigmine, pyridostigmine, norepinephrine, edrophonia, azathioprine, theophylline, potassium chloride, sodium chloride, calcium chloride.

Strengthen or weaken the effect of Vero-pipecuronium:

The preliminary use of depolarizing muscle relaxants can both strengthen and weaken the effect of Vero-pipecuronium; the effect depends on the dose, time of application and individual sensitivity to the drugs.

In the case of simultaneous use of halothane or fentanyl, blood pressure can be reduced.

Special instructions:Vero-pipecuronium can be used only in a specialized hospital with appropriate equipment for endotracheal intubation, mechanical ventilation, oxygen therapy, and specific antidotes.

Before the beginning of anesthesia, electrolyte balance, acid-base state and dehydration should be normalized.

Doses of Vero-pipecuronium, which cause muscle relaxation, do not have a significant cardiovascular effect and, unlike some anesthetics, practically do not cause a bradycardia due to the vagal effect. In this regard, the use and dosage of vagolytic drugs for premedication are subject to a thorough preliminary assessment; should also take into account the stimulating effect on the vagus of other, simultaneously used drugs, and the type of operation.

Due to possible precipitation, Vero-pipecuronium should be mixed with other injectable solutions or infusions. The only exception is isotonic sodium chloride solution, 5% glucose solution, Ringer's solution.

Patients with disorders of neuromuscular transmission, obesity, renal insufficiency, liver and biliary tract, with indications of a history of polio transferred should be administered the drug in smaller doses. Some conditions (hypokalemia, digitalisation, hypermagnesia, hypocalcaemia, hypercapnia, cachexia, hypothermia) may promote prolongation or enhancement of the Vero-pipecuronium effect.

The therapeutic effect in infants from 3 months to 1 year is practically indistinguishable from that in adults. Children aged 1 to 14 years are less sensitive to pipecuronium bromide and the duration of their therapeutic effect is shorter than in adults and infants (under 1 year of age).

Effect on the ability to drive transp. cf. and fur:In the first 24 hours after the termination of the muscle relaxant effect of Vero-pipecuronium, it is not recommended to drive and engage in other potentially dangerous activities requiring an increased concentration of psychomotor reactions.

Form release / dosage:Lyophilizate for the preparation of a solution for intravenous administration of 4 mg in vials.

Packaging:1 bottle with instructions for use in a pack of cardboard.

For 5, 10 or 25 bottles together with instructions for use in a pack of cardboard with partitions or special nests.

For 1, 5, 10 or 25 vials complete with 1, 5, 10 or 25 ampoules with sodium chloride solution isotonic 0.9% for injections of 2 ml together with instructions for use in a pack of cardboard with septums or special nests. In the case of a solvent package, an ampoule knife or scarifier, or a volcanic disc, is inserted into each bundle. When using ampoules with incisions or a fracture ring, the ampoule opener or scarifier, or volcanic disc, is not inserted.

For 50, 85 or 100 bottles together with an equal number of instructions for use in a cardboard box (for hospitals).

Storage conditions:List A. In a dry, the dark place at a temperature of 2 to 8 ° C.

Keep out of the reach of children.

Shelf life:2 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:P N002517 / 01

Date of registration:19.09.2008 / 04.08.2016

Expiration Date:Unlimited

The owner of the registration certificate:VEROPHARM SA VEROPHARM SA Russia

Manufacturer: & nbsp

VEROPHARM SA Russia

Information update date: & nbsp01.02.2017

Illustrated instructions

Instructions

Vero-Pipecuronius (Vero-Pipecuronium)