Atracurium besilate

Chemical name

2,2'-[1,5-Пентандиил-бис-[��кси(3-оксо-3,1-пропанди��л)]]-бис-[1-[(3,4-диметокс��фенил)метил]-1,2,3,4-тетр агидро-6,7-диметокси-2-м етил]изохинолиния dibenzolsulfonat

Gross

C65-H82-N2-O18-S2

Characteristics

Net biscetverticnoe ammoniewoye compound benzylisoquinoline derivative, a mixture of 10 stereoisomers (in the equivalent ratios). Molecular mass 1243.49. Solution-apirogennaya, transparent bledno-jeltogo color liquid with pH 3,25-3,65. Contains 0.9% benzyl alcohol (as a preservative).

Of drugs

The drugs-miorelaksirutee (nedepoliarizutee). Competitive miorelaxant nedepoliarizutego type action. Does n-holinoretseptora tip plates nervno-mysherngo sinapsa and prevents linking them acetylcholine type competitive antagonism and membrane depolarization cells skeletal muscles. Oppressing neuromuscular transmission and the initiation of relaxation skeletal muscles. It is a quick and legkoobratimy miorelaksantny effect. The evolving within 1-2 minutes; The on / in a dose of 0.4-0.5 mg / kg and brings mg / kg intubation possible via 2-2.5 min and 1.5 min, respectively. The maximum effect of a dose in the range of 0,11-0,6 mg / kg achieved through 1,7-10 mines and depends on the input dose (dose of 0.4-0.5 mg / kg through 3-5 minutes). The average effective dose causing miorelaksaciu 95% - 0.26 mg / kg Length effect dose 0.3-0.6 mg / kg, a balanced anaesthesia is 15-35 minutes; Miorelaxation length is not correlated with the level псевдохолинэстеразно й Activity blood plasma and is not dependent on the functional state of the liver and kidney. And little cumulative power, the duration of the re-entry does not increase. Additional introduction of a balanced anesthesia may at intervals of 15 to 25 minutes (a few intervals longer when combined with izofluranom or anfluranom). Restoring neuromuscular transmission by 25% through a 45 mines and 95% of the 60 to 70 minutes after the balanced anaesthesia or after 40 minutes from the beginning of the process of recovery, with the inhalation anesthesia. Is moderate gistamina release. Provides gipotenzivne effect. In therapeutic doses does not affect the consciousness senses bolevu sensitivity, it is a sedative and amnestic effect malignant Gipertermii.v experiments in rabbits has embriotoksicescoe and teratogenic effect : increasing the number postimplantaih losses is viszerle and skeletal Narushenia.posle caesarean sections is a new side effects (even when the mothers of large and repeated doses), but does not exclude the possibility of respiratory depression or lower steel skeletal muscles. And mutagenna Aguostew.v highly associated with plasma proteins. Distribution following in / with the introduction of 2-3,4 mines. Poor permeates through GEB, placental barrier. Biotransformiroetsa by hydrolysis broadcasting with the participation of non-esterz blood plasma and spontaneously by nefermentativogo passive becoming inactive form. The ethyl-- laudanosin has miorelaksiruta activity, but it hypotension. Write for 20 minutes with the urine (approximately 90% in the form of metabolites), and jelchew (less than 10% in an unmodified form). Older patients slightly lowered overall Cl and increasing distribution, according to the duration of effect and the recovery nervous conductivity can be changed.

Indications

Relaxation of the muscles of surgical interventions, endotrahealna intubations, IVL (as a complement to general anesthesia).

Restrictions on the use of

Gipotenzia, hypothermia; Serious violations elektrolitnogo balance, including gipokaliemia and gipocalziemia; acidosis; kartsinomatos; pregnancy; Pediatric practices : children under the age of 1 month, preterm.

Pregnancy and lactation

Perhaps if the effect of therapy than the potential risk to the fetus and newborn.

Contraindications

Hypersensitivity, incl. mivakuriya to hydrogen, etc. miorelaxantham - benzylisoquinoline derivatives; male.

Side-Effects

Allergic reactions : from the release gistamina - hyperemia skin because vazodilatace (5%), skin eritematosnye (0.5%), urticaria, itching (0.2%), bronhospazm with bronchial hyper (0.2%), laringospazm, anaphylactoidnye Reaktion.so the circulatory system and blood (blood, gemostaz) : tranzitornaya arterial hypertension (2.1%) or gipotenzia (1.9%), tachycardia (2.1%) or aetiology (0.6%), until stopping Serdza.prochie : adults, inadequate dose strength or duration of the blockade neuromuscular transmission, rarely convulsions (in the face of intensive care trauma to the head, oedema of the brain, hypoxic encephalopathy, viral encephalitis, uremia).

Specific guidance

Solution slowly loses activity (about 6% per year) in the store, with 5 ^ degrees. About 5% of business lost during one month at a temperature of 25 degrees ^ (may be used if it contained at room temperature continuously, but no more than 14 days), not frozen. The fragmentation and / or change the color solution is not suitable for the introduction.

Patient interaction

Increases and the effect prolong 73.21 general anaesthetics : diethyl ether, alothane (20%), and izofluran anfluran (35%), ketamine, benzogexoni, chlorpromazine, propranolol, some antibiotics (aminoglikozida, tetratziklin, polimiksin, linkomicin, clindamycin, spectinomycin), magnesium salts, including sulfate (with Injecting a), procainamide, quinidine, lidocaine, etc. antiaritmicescie means dioretiki (tiazidnye, furosemide, mannit, acetazolamide) Preparations lithium (with a long introduction). Increases risk of bradikardii and / or hypotension against narcotic analgesics. The cross allergic reaction with tubokurarinom etc. miorelaxanthami contributing gistamina release, the development of a sustainable neuromuscular blockade to the anticholinesterase means in the face of suksametonia. Farmatsevticeski compatible (it is not possible to confuse one sprite, and to introduce / in the same), with barbituratami, including tiopental-natri and alkaline solutions drugs (possibly changing neutral pH solution atrakuriya, his inachtiwation or pretipitation free acid).

Overdosing

Symptoms : prolonged respiratory depression, or patients, gipotenzia, collapse, prolonged paralysis (similar mioplegii) Shok.lechenie : introduction antagonists - antiholinesteraznah means, preferably neostigmina metilsulfata, in the dose of 1-3 mg in / in the 0.5-2.0 min after in / in the 0,25-0,7 mg atropine (for the side effects m-holinomimeticakih) in the patients and the long-paralysis IVL (up to the full restoration of respiration); with a development hypotension or shock-vazokonstrictora. There is a need to re-survey after one hour after the heavily neuromuscular blockade to exclude miorelaxation.

Precautions

Extreme caution is needed in patients with neuromuscular violation of the transfer. Is only in the presence of antagonists, and the means for transporting voice and data-IVL. Severe neuromuscular blockade antiholinesteraznami means is not earlier than 8-35 minutes.

Dosing and Administration

In / in, adults and children older than 2 years 0.3-0.6 mg / kg bolusno further to 0.1-0.2 mg / kg or Batches infuzionno continuously at a speed of 0.3-0.6 mg / kg / h (dose reduced by 20% against a backdrop of galotana and 30% against the backdrop of anflurana or izoflurana). In endotrahealna mouth : traditional, first 0.4-0.5 mg / kg and then 0.25 mg / kg (perhaps brings mg / kg within 90 c). When гиперчувствительност и gistaminu to-0.3-0.4 mg / kg slow or divided dose for 1 min. Children from one month to two years of 0.3-0.4 mg / kg against galotana.

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