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Fármacos anestésicos locales

» productos farmaceuticos » Fármacos anestésicos locales

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Nombre del producto: Levobupivacaine hydrochloride,Levobupivacaine Hcl
Sinónimos: (S)-(-)-Clorhidrato de bupivacaína
No.: 27262-48-2
Packing: 25kg/drum
M. F.: C18H29ClN2O
MW: 324.8887
Apariencia: polvo cristalino blanco

Levobupivacaína (rINN) is a local anaesthetic drug belonging to the amino amide group. It is the S-enantiomer of bupivacaine.The hydrochloride salt of levobupivacaine, an amide derivative with anesthetic property. Levobupivacaine reversibly binds voltage-gated sodium channels to modulate ionic flux and prevent the initiation and transmission of nerve impulses (stabilizing neuronal membrane), thereby resulting in analgesia and anesthesia. In comparison with racemic bupivacaine, levobupivacaine is associated with less vasodilation and has a longer duration of action.

Levobupivacaine is an amide-type local anaesthetic. Levobupivacaine acts via blockade of voltage-sensitive ion channels in neuronal membranes, preventing transmission of nerve impulses. Localised and reversible anaesthesia is produced by interference with the opening of the sodium channel, which inhibits conduction of the action potential in nerves involved in sensory and motor activity and sympathetic activity. [1] Levobupivacaine displaces 3H-BTX from sodium channels of rat brain synaptosomes with IC50 of 2.9 μM and Hill coefficients of 1.2. When cell membrane is held at -80 mV, -70 mV, -60 mV or -100 mV, Levobupivacaine shows tonic inhibition of sodium channel in GH3 cells with IC50s of 132.1, 37.6, 21.6 and 264 μM, respectivamente. [2] Levobupivacaine depresses action potential of isolated axon in vitro.

Levobupivacaine HCl is intended for single use and does not contain preservatives; any solution remaining from an open container should be discarded. For specific techniques and procedures, refer to standard contemporary textbooks. Levobupivacaine Compatibility and Admixtures: Levobupivacaine may not be compatible with alkaline solutions having a pH greater than 8.5. Studies have shown that levobupivacaine is compatible with 0.9% Sodium Chloride Injection USP and with saline solutions containing morphine, fentanyl and clonidine. Compatibility studies with other parenteral products have not been studied. Dilution Stability: Levobupivacaine diluted to levobupivacaine 0.625 a 2.5 mg/mL in 0.9% sodium chloride injection is physically and chemically stable when stored in polyvinyl chloride (CLORURO DE POLIVINILO) bags at ambient room temperature for up to 24 hours. Aseptic technique should be used to prepare the diluted products. Admixtures of levobupivacaine should be prepared for single patient use only and used within 24 hours of preparation. The unused portion of diluted levobupivacaine should be discarded after each use.

Test Items Especificación Test Results
Apariencia Fine, white, crystalline, odorless powder confirm
Identificación ABC in Pass confirm
Solubilidad Very soluble in water, soluble in Alcohol;
insoluble in Ether and Benzene
confirm
USP Reference standards USP Tetracaine Hydrochloride RS.
USP Endotoxin RS.
confirm
Punto de fusion 145~150 degree 146.0~147.5
degree
Chromatographic purity In Pass confirm
Related substance Not more than the reference solution 0.05% confirm
Heavy metals ≤10 ppm confirm
PH 4.5-6.5 5.8
Residuos en ignición ≤0.10% 0.05%
Pérdida por secado ≤ 0.5% 0.19%
Ensayo 98.0 -101.0% 100.1%
Conclusión Confirms USP 32

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