Aperomide - instructions for use, dose, side effects, contraindications

Pharmacodynamics:Aperomide® is a bis-quaternary ammonium compound of the steroid structure, a non-depolarizing muscle relaxant. Competitively blocks N-holinoretseptory skeletal muscles, preventing the acetylcholine-induced depolarization of the end plate and the excitation of muscle fibers.
Neuromuscular blockade is achieved within 5.5-6 minutes after the administration of a single dose of 50 μg / kg and 3-5 minutes - a dose of 70-85 μg / kg. Conduction of intubation of the trachea is possible after 2.5-3 min after administration of 70-100 mcg / kg; when using a smaller dose, the time to reach a level of muscle relaxancy sufficient for intubation is prolonged.The duration of the effect depends on the dose and type of anesthesia performed. When using the recommended doses, the effective relaxation of skeletal muscles is maintained for 50-70 minutes.
In medium doses it does not cause significant changes in the activity of the cardiovascular system; in large doses has a weak ganglion blocking, M-cholinoblocking activity.

Pharmacokinetics:The volume of distribution is 0.25 l / kg, with renal insufficiency 0.37 l / kg. It penetrates insignificantly through the placental barrier. The half-life is 1.7 hours (0.9-2.7 hours), with renal failure 4 hours (2-8.2 hours). Metabolized in tissues with the formation of an active metabolite (40-50% of the activity of pipecuronium bromide) and inactive derivatives.
It is excreted by the kidneys in unchanged form 75%, the rest in the form of metabolites. Clearance - 0.12-0.15 l / kg / h, with renal insufficiency - 0.08 l / kg / h.

Indications:Relaxation of skeletal muscles and facilitation of endotracheal intubation during surgery and diagnostic procedures in conditions of mechanical ventilation.

Contraindications:Hypersensitivity. Age to 3 months (doses in children under 3 months of age are not defined).

Carefully:Bile duct obstruction, edematous syndrome, increased circulating blood volume or dehydration, disturbed water-electrolyte metabolism, hypothermia, myasthenia gravis, myasthenic syndrome, respiratory depression, renal / hepatic insufficiency, decompensated chronic heart failure, children (under 14 years).

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 in cesarean 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:Only intravenously!
Immediately before administration, the contents of the ampoule are diluted with water for injection or 0.9% solution of sodium chloride.
Adults and children 14 years and over for complete miorelaxation, 70-80 μg / kg is administered. The maximum single dose is 100 μg / kg. To maintain muscle relaxancy for a long time should be re-introduced at doses of 15% of the original (10-15 μg / kg).When intubation with suksamethonium, the initial dose is -40-50 μg / kg.
In chronic renal insufficiency, the amount of the administered dose is determined by the values of creatinine clearance (CC): when the SC is below 100 ml / min, 85 μg / kg is injected, at a CC below 80 ml / min - 70 μg / kg, at a CC below 60 ml / min - 55 mkg / kg, with a SC less than 40 ml / min - 50 mcg / kg.
Doses in children aged 3 months to 12 months - 40 μg / kg (provides muscle relaxation lasting from 10 to 44 minutes); from 1 year to 14 years - 57 mkg / kg (muscle relaxation - from 18 to 52 minutes).

Side effects:From the musculoskeletal system: weakness of skeletal musculature after cessation of muscle relaxation, muscle atrophy.
From the nervous system: oppression of the central nervous system, hypoesthesia.
From the respiratory system: respiratory depression, hypopnea, apnea after cessation of muscle relaxation, lung atelectasis, laryngospasm.
From the cardiovascular system: bradycardia, lowering blood pressure; myocardial ischemia (up to the development of myocardial infarction) and the brain, atrial fibrillation, ventricular extrasystole.
On the part of the organs of hematopoiesis and the system of hemostasis: reduction of partial thromboplastin and prothrombin time, thrombosis.
From the side of the urinary system: anuria.
Laboratory indicators: hyperkreatinemia, hypoglycemia, hyperkalemia. Allergic reactions: skin rash, hives.

Overdose:Symptoms: prolonged paralysis of skeletal musculature and apnea, marked decrease in blood pressure, shock.
Treatment: neostigmine 1-3 mg in combination with atropine 0,5-1,25 mg or galantamine 10-30 mg (against the background of continuing artificial ventilation of the lungs).

Interaction:Means for inhalation (halothane, methoxyflurane, diethyl ether) and intravenous general anesthesia (ketamine, fentanyl propanidide, barbiturates), depolarizing and nondepolarizing muscle relaxants, antibiotics (aminoglycosides, tetracyclines), imidazole and metronidazole, antifungal agents (amphotericin B), diuretics, beta-blockers, thiamine, MAO inhibitors, guanethidine, protamine, phenytoin, alpha-adrenoblockers, blockers of "slow" calcium channels, lidocaine when used intravenously, reinforce and / or lengthen the action.
Drugs that reduce the concentration of K + in the blood, aggravate respiratory depression (until it stops).
Opioid analgesics increase respiratory depression.
When applying glucocorticosteroids, neostigmine, epinephrine, theophylline, potassium chloride, sodium chloride, calcium chloride before surgery, the effect may be weakened.
Depolarizing muscle relaxants can both enhance and weaken the action of pipecuronium bromide (depends on the dose, time of application and individual sensitivity).
With simultaneous application with quinidine, magnesium salts, procainamide, an increase in the severity of myorelaxation is possible.
Due to possible precipitation, mixing of pipecuronium bromide with other solutions for injection or infusion should be avoided. The exception is 0.9% solution of sodium chloride, 5% dextrose solution and Ringer's solution.

Special instructions:Apply only under the supervision of an experienced anesthesiologist, in the presence of conditions for intubation, artificial ventilation, oxygen therapy.
Careful monitoring during the operation and in the early postoperative period is necessary to maintain vital functions until the restoration of an adequate vital tonus is complete.
When calculating the dose, one should take into account the technique of anesthesia used, possible interactions with drugs administered before or during anesthesia, the condition and sensitivity of the patient.
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 states (hypokalemia, digitalization, gipermagniemiya, hypocalcemia, hypoproteinemia, dehydration, acidosis, hypercapnia, cachexia, hypothermia) can contribute to elongation or strengthening effect.
Before the beginning of anesthesia, it is necessary to correct electrolyte balance, acid-alkaline state and eliminate dehydration.
Pregnant women who, for the treatment of toxicosis, took magnesium salts (capable of strengthening the neuromuscular blockade), pipecuronium bromide prescribe in reduced doses.
Efficacy and safety of use in the neonatal period have not been studied. The therapeutic effect in infants from 3 months to 1 year practically does not differ from that in adults.Children aged 1 to 14 years are less sensitive to pipecuronium bromide and the duration of the therapeutic effect is shorter in them than in adults and infants (under 1 year of age).

Effect on the ability to drive transp. cf. and fur:Within 24 hours after complete recovery of neuromuscular conduction, it is not recommended to drive and engage in potentially hazardous activities in terms of injury.

Form release / dosage:Lyophilizate for the preparation of a solution for intravenous administration of 4 mg in ampoules with a capacity of 2 ml with a ring or break point.

Packaging:1 or 5 ampoules per contour cell package. 1 contour cell package with 1 ampoule or 1, 2 or 5 contour packs with 5 ampoules together with instructions for use in a cardboard package.

Storage conditions:In a dry, 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 printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N001197 / 01

Date of registration:06.03.2009

The owner of the registration certificate:RUSSIAN CARDIOLOGICAL NPK FGU ROSMEDTEKHNOLOGIY - EXPERIMENTAL PRODUCTION OF MEDICAL AND BIOLOGICAL PREPARATIONS RUSSIAN CARDIOLOGICAL NPK FGU ROSMEDTEKHNOLOGIY - EXPERIMENTAL PRODUCTION OF MEDICAL AND BIOLOGICAL PREPARATIONS Russia

Information update date: & nbsp13.01.2014

Illustrated instructions

Instructions

Aperomide® (Aperomid®)