Bupivacaine Pharmacology


About Bupivacaine
Amino amide group local Anesthetic
Mechanism of Action of Bupivacaine
It blocks the generation and conduction of nerve impulses 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. In general, the progression of anesthesia is related to the diameter, myelination and conduction velocity of affected nerve fibers. It causes the loss of function in the order as follows i.e. pain, temperature, touch, propioception and skeletal muscle tone. The analgesic effects of Bupivacaine are thought to 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
Pharmacokinets of Bupivacaine
Absorption - The rate of systemic absorption of local anesthetics is dependent upon the total dose and concentration of drug administered, the route of administration, the vascularity of the administration site, and the presence or absence of epinephrine(A dilute concentration of epinephrine (1:200,000 or 5 [micro ]g/mL) usually reduces the rate of absorption and peak plasma concentration of bupivacaine, permitting the use of moderately larger total doses and sometimes prolonging the duration of action) in the anesthetic solution
Distribution - Its distribution depending upon the route of administration, local anesthetics are distributed to some extent to all body tissues, with high concentrations found in highly perfused organs such as the liver, lungs, heart, and brain. 95% bound to the plasma proteins. Crosses the placental barrier
Metabolism - Metabolized in the liver via conjugation with glucuronic acid. The major metabolite of bupivacaine is 2, 6-pipecoloxylidine
Excretion - Excreted through urine
Onset of Action for Bupivacaine
Duration of Action for Bupivacaine
Half Life of Bupivacaine
3.5 hours (adults)
8.1 hours (neonates)
Side Effects of Bupivacaine
1. Cardiac arrest.
2. Cardiac arrhythmias.
3. Respiratory failure.
4. Bradycardia.
5. Hypotension.
6. Arrhythmias.
7. Methemoglobinaemia.
8. Seizures.
9. Restlessness.
12.Prolonged block
Contra-indications of Bupivacaine
1. Hypersensitivity to the drug.
2. Digital block.
3. I.V. regional anaesthesia.
4. Para cervical block in obstetrics.
5. Spinal anaesthesia
Special Precautions while taking Bupivacaine
1. Heart block.
2. Hepatic dysfunction.
3. Shock.
4. Heart disease.
5. Debilitated patients.
Pregnancy Related Information
Old Age Related Information
Use with caution.
Breast Feeding Related Information
Use with caution.
Children Related Information
Use with caution.
Indications for Bupivacaine
1. Infiltration anaesthesia.
2. Epidural anaesthesia.
3. Spinal anaesthesia.
4. Nerve block.
Interactions for Bupivacaine
Cimetidine & Ranitidine: Clearance of Bupivacaine decreased.
Lignocaine & Mepivacaine: Efficacy potentiated by bupivacaine.
Typical Dosage for Bupivacaine
Dose varies with procedure, depth of anesthesia, vascularity of tissues, duration of anesthesia, and condition of patient
Caudal block:
INJ 15-30ml of 0.25% or 0.5%
Epidural block:
INJ 10-20ml of 0.25% or 0.5%
Peripheral nerve block:
INJ 5ml of 0.25% or 0.5% (12.5-25mg)
2.5 mg/kg or 400mg daily
Sympathetic nerve block:
INJ 20-50ml of 0.25%
Caudal block:
INJ 1-3.7 mg/kg
Epidural block:
INJ 1.25 mg/kg/dose
Schedule of Bupivacaine
Storage Requirements for Bupivacaine
Solutions should be stored at controlled room temperature 15-30?C (59-86?F)
Effects of Missed Dosage of Bupivacaine
The doctor should be informed immediately if a dose is missed
Effects of Overdose of Bupivacaine
Give symptomatic and supportive treatment. There is evidence that Intralipid, a commonly available intravenous lipid emulsion, can be effective in treating severe cardiotoxicity.

Home Delivery for Bupivacaine in Your City

Medicine India is just a publishing medium for medicine related information and does not provide services or sales of medicines including bupivacaine.

However, we do publish a comprehensive directory of Pharmacies, Chemists and Druggists in cities all over India. You can use this directory to find the medicine stores in your city (or area) that provide home delivery services for bupivacaine and other medicines and health products. Home delivery services for bupivacaine may be free or they may cost you depending on the pharmacy and the minimum order requirements. It would be best to get this clarified while placing the order.

Please be aware that you should take bupivacaine only if a doctor has recommended or prescribed it. Some or all pharmacies who provide a home delivery service for medicines might insist on a prescription for bupivacaine before they complete the sale. You can get this information while placing the order for bupivacaine with the pharmacy.

Bupivacaine is a generic medicine name and there are several brands available for it. Some of the brands for bupivacaine might be better known than bupivacaine itself. If the pharmacy that's willing to deliver medicines to your home doesn't have bupivacaine in stock, you can ask for one of the branded alternatives for bupivacaine.