equipoise

Aperomid ® is bischetvertichnym ammonium compounds of steroid structure, non-depolarizing muscle relaxant. Competitive blocking N-cholinergic receptors of the skeletal muscles, preventing the acetylcholine-induced depolarization of the end plate and the excitation of the muscle fiber.

Neuromuscular blockade reached within 5.5-6 minutes after administration of a single dose of 50 mg / kg and 5.3 min – a dose of 70-85 mg / kg. Carrying intubation possible within 2.5-3 minutes after administration of 70-100 mg / kg; using at the time to reach miorelaxation dose level sufficient for intubation lengthened. Duration of the effect is dependent on dose and type of anesthesia. When using the recommended dosages effective relaxation of skeletal muscles is maintained for 50-70 minutes.

In moderate doses does not cause significant changes in the cardiovascular system; in large doses it has ganglioblokiruyuschimi weak, M-anticholinergic activity.

Pharmacokinetics

The volume of distribution – 0.25 l / kg in renal failure – 0.37 l / kg. To a small extent crosses the placental barrier. The half-life – 1.7 hours (0.9-2.7 hours) in renal failure -. 4 hours (2-8,2 hours)
is metabolized in the tissues with the formation of the active metabolite (40-50% of the activity pipekuroniya equipoise) and inactive derivatives.
excreted by the kidneys unchanged to 75%, the rest is in the form of metabolites. Clearance – 0.12-0.15 l / kg / h in renal impairment – 0.08 l / kg / h.

Indications

The relaxation of skeletal muscles and to facilitate endotracheal intubation during operations and diagnostic procedures in a ventilator.

Contraindications

Hypersensitivity. Age up to 3 months (dose in children under the age of 3 months to be determined).

Carefully

Obstruction of the biliary tract, edema syndrome, increased blood volume, or dehydration, disruption of water and electrolyte metabolism, hypothermia, myasthenia gravis, myasthenic syndrome, respiratory depression, kidney / liver failure, decompensated chronic heart failure, children’s age (14 years).

Pregnancy and lactation

Experience sufficient to prove the safety pipekuroniya equipoise for pregnant women and fetus, there is no.
In the case of general anesthesia for cesarean section pipekuroniya equipoise does not change the index of Apgar, muscle tone and cardiovascular adaptation neonatal.
Data on the use of pipekuroniya equipoise during lactation are not available.

Dosing and Administration

Only intravenously!
Immediately before administration the contents of the vial is diluted with water for injection or 0.9% sodium chloride solution.

Adults and children from 14 years and above for the complete muscle relaxation is administered 70-80 mg / kg. The maximum single dose – 100 mg / kg. To maintain muscle relaxation in a long time to be administered repeatedly at doses of 15% of the original (10-15 mg / kg). During the intubation, suxamethonium on the background of the initial dose -40-50 mg / kg.

In chronic renal failure value of the dose administered is determined by the values of creatinine clearance (CC): QA below 100 ml / min administered 85 mg / kg, QC below 80 ml / min – 70 g / kg, QC below 60 ml / min – 55 ug / kg, while RC least 40 ml / min – 50 g / kg.

The doses in children aged 3 months to 12 months – 40 mg / kg (provides muscle relaxation lasting 10 to 44 minutes); from 1 year to 14 years – 57 mg / kg (muscle relaxation – from 18 to 52 min.)

Side effect

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

From the nervous system: central nervous system depression, hypoesthesia.

The respiratory system: respiratory depression, hypopnea, apnea, muscle relaxation after cessation, pulmonary atelectasis, laryngospasm.

Since the cardiovascular system: bradycardia, decreased blood pressure; myocardial ischemia (up to the development of myocardial infarction) and brain, atrial fibrillation, ventricular arrythmia.

From the side of hematopoiesis and hemostasis system: decrease in partial thromboplastin time, prothrombin and thrombosis.

From the urinary system: anuria.

Laboratory findings: hypercreatininemia, hypoglycemia, hyperkalemia.

Allergic reactions: skin rash, urticaria.

Overdose

Symptoms: prolonged paralysis of skeletal muscles, and sleep apnea, marked reduction in blood pressure, shock.
Treatment: neostigmine 1-3 mg in combination with atropine 0.5-1.25 mg or 10-30 mg of galantamine (against the background of continued mechanical ventilation).

Interaction with other drugs

Means for inhalation (halothane, methoxyflurane, diethyl ether) and intravenous general anesthesia (ketamine, fentanyl, propanidid, barbiturates) depolarizing and non-depolarizing muscle relaxants, antibiotics (aminoglycosides, tetracyclines), imidazole and metronidazole, antifungals (amphotericin B), diuretics, beta-blockers, thiamine, MAO inhibitors, guanethidine, protamine, phenytoin, alpha-blockers, blockers “slow” calcium channels, for intravenous use lidocaine enhance and / or prolong 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 to a surgical intervention glucocorticosteroids, neostigmine, epinephrine, theophylline, potassium chloride, sodium chloride, ammonium chloride, calcium effect may weaken.

Depolarizing muscle relaxants can both strengthen and weaken the action pipekuroniya equipoise (depending on the dose, application time and individual sensitivity).

In an application with quinidine, magnesium salts, procainamide may increase the severity of muscle relaxation.

Because of the possible precipitation should not be mixed with other pipekuroniya equipoise solution for injection or infusion. The exception is 0.9% sodium chloride solution, 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, mechanical ventilation, oxygen therapy.

Careful monitoring during surgery and in the early postoperative period in order to maintain vital functions to the full restoration of adequate vitality.

In calculating the dosage should be considered a technique applied anesthesia, possible interactions with drugs administered before or during anesthesia, the patient’s condition and sensitivity.

Patients with disorders of neuromuscular transmission, obesity, renal failure, liver disease and biliary tract, with indications of a history of myocardial polio should be prescribed the drug in smaller doses.Some states (hypokalemia, digitalization, gipermagniemiya, hypocalcemia, hypoproteinemia, dehydration, acidosis, hypercapnia, cachexia, hypothermia) may contribute to lengthening or enhancing effect.
Before the start of anesthesia should be carried out correction of electrolyte balance, acid-base balance and correct dehydration.

Pregnant women, who for the treatment of toxemia took magnesium salt (capable of enhancing neuromuscular blockade) pipekuroniya equipoise is administered in small 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 is virtually identical from that of adults.
children aged 1 year to 14 years are less sensitive to pipekuroniya equipoise and duration of the therapeutic effect they are shorter than in adults and infants (under 1 year).

Effects on ability to drive and use machinery

Within 24 hours after the full recovery of neuromuscular conduction is not recommended to transport and deal with potentially dangerous in terms of injury prevention activities.

release Form

Valium for drug of a solution for intravenous administration of 4 mg vials with a capacity of 2 ml with ring or point of fracture.
1 or 5 vials in blisters.
1 blisters 1 ampoule or 1, 2 or 5 contour cell packages of 5 ampoules together with instructions for use in paper cartons.

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