Pharmacological properties buy equipoise is a long-acting muscle relaxant nedepolyariziruyuschim. Due to the competition due to the n-cholinergic receptors, located on the endplate of the neuromuscular synapse of skeletal muscles, blocks the transmission of the signal from the nerve to the muscle fibers. It does not cause muscle fasciculations, has no hormonal action. Even at doses several times greater than its effective dose required for 90% reduction in muscle contractility . The dose equal to 0.05 mg / kg body weight, provides a 40-50 minute muscle relaxation during various operations . The maximum effect pipekuroniya buy equipoise dose-dependent and occurs within 1.5-5 min. The effect is faster at all doses of 0.07-0.08 mg / kg. A further increase in the dose reduces the time required for the development of the effect, and significantly prolongs the action of the drug. When administered intravenously, the initial volume of distribution (the V dc ) is 110 ml / kg body weight, volume of distribution in the saturation phase (the V dss ) is 300 (± 78 ) ml / kg, the plasma clearance (Cl) is approximately equal to 2,4 (± 0.5) ml / min / kg, the mean elimination half-life (T 1/2 ) is 121 (± 45) minutes. the average residence time in the blood plasma (MRT) – 140 min. Repeated administration of maintenance doses cumulative effect is insignificant, if at the time of 25% recovery of the original muscle contractility used doses of 0.01-0.02 mg / kg. Write mainly by the kidneys, while 56% of the drug – the first 24 hours. One-third of output unchanged, and the remaining amount -. In the form of 3-desacetyl pipekuroniya buy equipoise According to preclinical studies liver is also involved in the elimination pipekuroniya buy equipoise. Penetrates through the placental barrier.
Indications for use of
endotracheal intubation and relaxation of skeletal muscles with a total benzocaine during various surgical procedures requiring more than a 20-30 minute muscle relaxation and in the conditions of ventilation.
– Hypersensitivity to pipekuroniya buy equipoise and / or bromine and.
– Children under the age of 3 months.
– Severe hepatic impairment.
of biliary tract obstruction, edema syndrome, increased blood volume, or dehydration, diuretics, disturbance of acid-base balance (acidosis, hypercapnia) and water and electrolyte metabolism (gipokaliemiya. gipermagniemiya, hypocalcemia), hypothermia, digitalization, hypoproteinemia, cachexia, myasthenia gravis (including myasthenia gravis, Eaton-Lambert syndrome) due to the possible in cases such as amplification and attenuation of the drug. Small doses Arduana with severe myasthenia gravis or Lambert-Eaton syndrome can cause very pronounced effect. Such patients the drug is administered in very low doses, after careful assessment of the potential risk of respiratory depression, kidney failure (prolongs the action of the drug and time postanesthesia depression), decompensated chronic heart failure, children under the age of 14, malignant hyperthermia, anaphylactic reaction caused by any muscle relaxant to the patient’s history (because of possible cross-allergy).
Pregnancy and lactation
No clinical studies to prove the safety of Arduana in pregnant women and the fetus is not enough. Use of the drug during pregnancy is not recommended.
Clinical data on the safe use Arduana lactation is not enough. Use of the drug is not recommended during breast-feeding.
Dosing and Administration
As was the case with other non-depolarizing muscle relaxants, dose Arduana selected individually for each patient, taking into account the type of anesthesia, the proposed surgery duration, possible interactions with other drugs, used prior to or during anesthesia, comorbidities, and general condition of the patient .
It is recommended to use the stimulator peripheral nerve fibers to monitor neuromuscular block.
use only intravenously. Immediately before the administration of 4 mg of dry substance supplied diluted solvent.
The recommended dose for adults and children over 14 years:
– initial dose for intubation and subsequent surgery: 0.06-0.08 mg / kg body weight, provides a good / excellent conditions for tracheal intubation within 150-180 seconds, and the duration 60-90 minutes of muscle relaxation;
– miorelaxation initial dose for intubation using suxamethonium: 0.05 mg / kg. provides a 30-60-minute muscle relaxation;
– the maintenance dose: 0.01-0.02 mg / kg, provides a 30-60-minute muscle relaxation during surgery;
– chronic renal insufficiency is not recommended doses in excess of 0.04 mg / kg (in high doses may increase the duration of muscle relaxation);
– with overweight and obesity possible extension of Arduana, so you should use a dose designed for ideal weight.
Doses for children: from 3 to 12 months. – 0.04 mg / kg (which provides muscle relaxation lasting 10 to 44 min.). From 1 to 14 years – 0.05-0.06 mg / kg (muscle relaxation – from 18 to 52 min.).
Termination effect: when 80-85% blockade measured by stimulator peripheral nerve fibers, or partial blockade at the time determined by clinical signs, the application of atropine (0.5-1.25 mg) in combination with neostigmine methyl sulfate (1 -3 mg), or galantamine (10-30 mg) stops muscle relaxant action Arduana.
Side effect On the part of the nervous system: rare (less than 1%): depression of the central nervous system (CNS), somnolence, hypoesthesia. paralysis of skeletal muscles. From the musculoskeletal system: rarely (less than 1%): the weakness of the skeletal muscles after the cessation of muscle relaxation, muscle atrophy. The respiratory system: rarely (less than 1%): apnea, pulmonary atelectasis, respiratory depression, laryngospasm in a result of an allergic reaction, bronchospasm, cough. On the part of the cardiovascular system: rarely (less than 1%): myocardial ischemia (up to a myocardial infarction) and brain, arrhythmia, tachycardia, bradycardia, decreased or increased blood pressure, atrial fibrillation, ventricular premature beats , ventricular tachycardia. From the side of hematopoiesis and hemostasis system: rare (less than 1%): thrombosis, reduction of activated partial thromboplastin and prothrombin time. From the urinary system: rarely (less than 1%): anuria. Allergic reactions: rare (less than 1 %): skin rashes, allergic reactions, angioedema. Laboratory findings: rare (less than 1%): hypercreatininemia, hyperglycemia, hypokalemia, hypomagnesemia, hypocalcemia. Other: blepharitis, ptosis.
Symptoms: prolonged paralysis of skeletal muscles, and sleep apnea, marked reduction of blood pressure (BP), a shock.
In case of overdose or prolonged neuromuscular block of mechanical ventilation was continued until recovery of spontaneous breathing. Early recovery of spontaneous breathing as an antidote is administered an acetylcholinesterase inhibitor (e.g., neostigmine methylsulfate, pyridostigmine buy equipoise, edrophonium chloride): 0.5-1.25 mg atropine in combination with neostigmine (1.3 mg), or galantamine (10-30 mg). Until a satisfactory recovery of spontaneous breathing should be close monitoring of respiratory function.
Interaction with other drugs
inhaled anesthetics (halothane, methoxyflurane, ether diethyl ether, enflurane, isoflurane, cyclopropane), anesthetics for intravenous administration (ketamine propanidid. Barbiturates, etomidate, in-hydroxy and butyric acid), depolarizing and non-depolarizing muscle relaxants, some antibiotics (aminoglycosides, nitroimidazole derivatives, including metronidazole, tetracyclines, bacitracin, capreomycin, clindamycin, polymyxins, including colistin, lincomycin, amphotericin B), nitrate, anticoagulants, mineralocorticoid and steroids, diuretics, including . bumetanide, carbonic anhydrase inhibitors, ethacrynic acid, corticotropin, .alpha.-and β-blockers, thiamine, monoamine oxidase inhibitors (MAOIs), guanidine, protamine sulfate, phenytoin, blockers “slow” calcium channels, magnesium salts, procainamide, quinidine, lidocaine and procaine for intravenous enhance and / or prolong the action.
Drugs that decrease blood levels of potassium, aggravate respiratory depression (until it stops).
Opioid analgesics increase respiratory depression. High doses of sufentanil reduces the need for high initial doses of non-depolarizing muscle relaxants. Non-depolarizing muscle relaxants to prevent or reduce muscle tension caused by high doses of analgesics opiondnyh (including alfentanilom, fentanyl, sufentanil). Do not reduce the risk of bradycardia and hypotension caused by opiondnymi analgesics (especially against the background of vasodilators and / or beta-blockers).
During intubation with suxamethonium Arduan introduced after the disappearance of clinical signs of suxamethonium action. As is the case with other nedepolyariziruyuschimi relaxants introduction Arduana can shorten the time required for the onset of muscle relaxation, and increase the duration of maximal effect;
Prolonged preliminary application of glucocorticosteroids, neostigmine, edrophonium chloride, pyridostigmine, norepinephrine, azathioprine, epinephrine, theophylline, potassium chloride chloride, sodium chloride may weaken the effect of calcium.
Depolyariziruyuschie relaxants can both strengthen and weaken the action pipekuroniya buy equipoise (depending on the dose, time of use and individual sensitivity).
Doxapram temporarily masks the residual effects of muscle relaxants.
Use only in a specialized hospital with proper equipment for artificial respiration and in the presence of a specialist to conduct artificial respiration due to the impact of the drug on the respiratory muscles.
Close supervision is necessary during surgery and in the early postoperative period in order to maintain vital functions to the full recovery of muscle contractility.
The calculation should take into account the dose applied anesthetic technique, possible interactions with drugs administered before or during anesthesia, the patient’s condition and sensitivity to the drug.
cases anaphylactic and anaphylactoid reactions when used muscle relaxants are described in the medical literature. Despite the absence of such action messages Arduana, the drug can be used only under conditions that allow to proceed immediately to these states treatment.
Caution must be especially careful in applying Arduana with a history of the patient’s anaphylactic reaction caused by a muscle relaxant because of possible cross allergy .
Doses Arduana, causing muscle relaxation, does not have a significant cardiovascular effect and hardly cause bradycardia.
Application and dose m-holinoblokatorov sedation in order to be careful preliminary assessment; It should also take into account the stimulating effect by n. vagus other simultaneously used drugs and type of surgery.
In order to avoid relative overdosing and ensure proper control over the recovery of muscle activity is recommended to use the stimulator peripheral nerve fibers.
Patients with disorders of neuromuscular transmission, obesity, renal failure, liver disease and biliary tract under guidance of a history of myocardial polio, should be prescribed the drug in smaller doses.
in the case of liver disease Arduana application is possible only in cases where the risk is justified. This dose should be minimal.
Some states (hypokalemia, digitalization, gipermagniemiya, diuretics, hypocalcemia, hypoproteinemia, dehydration, acidosis, hypercapnia, cachexia, hypothermia) may contribute to lengthening or enhancing effect.
As is the case with other muscle relaxants, prior to use Arduana should normalize the electrolyte balance and acid-base status, eliminate dehydration.
Like other muscle relaxants Arduan can reduce the activated partial thromboplastin and prothrombin time.
Children aged 1 year to 14 years are less sensitive to pipekuroniya buy equipoise and duration miorelaksiruyushego effect they are shorter than in adults and children aged up to 1 year.
Efficacy and safety of use in the neonatal period have not been studied.
Myorelaxation effect in infants from 3 months. up to 1 year does not differ from that in adults.
Only use fresh solution.
The impact on the car and the working mechanisms of management capacity
in the first 24 hours after the termination of the action miorelaksiruyuschego Arduana advised not to drive and engage in potentially hazardous activities that require high concentration and psychomotor speed reactions.
. Lyophilisates for solution for intravenous administration of 4 mg / together with the solvent – sodium chloride solution 0.9%
10 mg of the freeze-dried in a vial of colorless glass (hydrolytic class 1) contain 4 mg pipekuroniya buy equipoise; 2 ml of solvent in a colorless glass ampoule (hydrolytic class 1) 5 5 vials and ampoules in a plastic tray, the plastic pallet 5 in the carton box with instructions for use.