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Local Anesthetic Drugs

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Chemical name: Bupivacaine
MF: C18H28N2O
MW: 288.43
CAS: 2180-92-9
Appearance: white powder
Purity: over 99%

Bupivacaine is only found in individuals that have used or taken this drug. It is a widely used local anesthetic agent. [PubChem]Bupivacaine blocks the generation and the conduction of nerve impulses, presumably by increasing the threshold for electrical excitation in the nerve, by slowing the propagation of the nerve impulse, and by reducing the rate of rise of the action potential. Bupivacaine binds to the intracellular portion of sodium channels and blocks sodium influx into nerve cells, which prevents depolarization. In general, the progression of anesthesia is related to the diameter, myelination and conduction velocity of affected nerve fibers. Clinically, the order of loss of nerve function is as follows: pain, temperature, touch, proprioception, and skeletal muscle tone. The analgesic effects of Bupivicaine are thought to potentially be due to its binding to the prostaglandin E2 receptors, subtype EP1 (PGE2EP1), which inhibits the production of prostaglandins, thereby reducing fever, inflammation, and hyperalgesia.

Bupivacaine is indicated for local infiltration, peripheral nerve block, sympathetic nerve block, and epidural and caudal blocks. It is sometimes used in combination with epinephrine to prevent systemic absorption and extend the duration of action. The 0.75% (most concentrated) formulation is used in retrobulbar block. It is the most commonly used local anesthetic in epidural anesthesia during labor, as well as in postoperative pain management.Liposomal formulations of buipivacaine are no more effective than plain solutions of bupivacaine.

Bupivacaine is contraindicated in patients with known hypersensitivity reactions to bupivacaine or amino-amide anesthetics. It is also contraindicated in obstetrical paracervical blocks and intravenous regional anaesthesia (Bier block) because of potential risk of tourniquet failure and systemic absorption of the drug and subsequent cardiac arrest. The 0.75% formulation is contraindicated in epidural anesthesia during labor because of the association with refractory cardiac arrest.

Items of analysis Specification Results
Appearance White or off white crystalline powder Complies
Solubility reely soluble in Dichloromethane, soluble in ethanol, and Ethyl acetate, insoluble in water. Complies
IdentifIcation IR ;The retention time of the major peak in the choramtogram of the Assay preparation corresponds to that in the Complies
Melting point 106℃~110℃ 106.6℃~109.2℃
Loss on drying ≤ 0.5% 0.03%
any individual impurity not more than 0.3% 0.05%
total impurities not more than 0.5% 0.06%
Limit of residual solvents Conform to standard Complies
Residue on ignition ≤0.1% 0.03%
Assay ≥98.5% 99.67%
Conclusion Qualified

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