BUPIVACAINE

BUPIVACAINE 

USE

BRAND NAME:- MARCAIN 0.5%,1%, SENSORCAINE 0.25%,0.5% inj.

BUPIVACAINE is a potent and long -acting amidelinked LA : used for infiltration,nerve block, epidural and spinal anaesthesia of long duration.  

PHARMACODYNAMIC :-

Bupivacaine binds to the intracellular portion of voltage-gated sodium channels and blocks sodium influx into nerve cells, which prevents depolarization. Without depolarization, no initiation or conduction of a pain signal can occur.

PHARMACOKINETICS:- 

The rate of systemic absorption of bupivacaine and other local anesthetics is dependent upon the dose and concentration of drug administered, the route of administration, the vascularity of the administration site, and the presence or absence of epinephrine in the preparation.

1.Onset of action (route and dose-dependent): 1–17 min.

2.Duration of action (route and dose-dependent): 2–9 hr

3.Half life: neonates, 8.1 hr, adults: 2.7 hr.

4.Time to peak plasma concentration (for peripheral, epidural, or caudal block): 30–45 min.

5.Protein binding: about 95%.

6.Metabolism: hepatic .

7.Excretion: renal (6% unchanged).

MECHANISM OF ACTION:-

BUPIVACAINE block the generation and conduction of nerve impulses by increasing the threshold for electrical excitation in the nerve, by slowing the propagation of the nerve impulses , and by reducing the rate of rise of the action potential . It long acting local anaesthetic . It has a slow  onset as compared to other local  anaesthetic hence is predominantly used as an epidural anaesthetics.

In addition to blocking Na+ channels, bupivacaine affects the activity of many other channels, including NMDA receptors. Importantly, bupivacaine inhibits NMDA receptor-mediated synaptic transmission in the dorsal horn of the spinal cord, an area critically involved in central sensitization. 

USED:-

used for infiltration,nerve block, epidural and spinal anaesthesia of long duration.  

SIDE EFFECTS:-

signs of an allergic reaction: hives, red rash, itching; sneezing, difficulty breathing; severe dizziness, vomiting; swelling of your face, lips, tongue, or throat.

•feeling anxious, restless, confused, dizzy, drowsy, or like you might pass out;

•ringing in your ears, problems with speech or vision;

•metallic taste in your mouth, numbness or tingling around your mouth;

•muscle twitching, tremors, seizure (convulsions);

•weak or shallow breathing;

•fast heart rate, gasping, feeling unusually hot;

•slow heart rate, weak pulse; 

•little or no urination.

DOSE:-  DIRECTION BY PHYSICIAN.