Drug information of Bupivacaine

Bupivacaine

Drug group:

A widely used local anesthetic agent.

Mechanism of effect

Local anesthetics block 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.

Pharmacodynamic

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: (1) pain, (2) temperature, (3) touch, (4) proprioception, and (5) skeletal muscle tone.

Pharmacokinetics

 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 in the anesthetic solution.

The onset of action with Bupivacaine Hydrochloride is rapid and anesthesia is long lasting. The duration of anesthesia is significantly longer with Bupivacaine Hydrochloride than with any other commonly used local anesthetic. It has also been noted that there is a period of analgesia that persists after the return of sensation, during which time the need for strong analgesics is reduced. Local anesthetics are bound to plasma proteins in varying degrees.

Generally, the lower the plasma concentration of drug the higher the percentage of drug bound to plasma proteins. 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. Local anesthetics appear to cross the placenta by passive diffusion. The kidney is the main excretory organ for most local anesthetics and their metabolites.

Dosage

Adults

local anesthesia

Max: 2 mg/kg or 175 mg/dose, 400 mg/24h; Info: onset 2-10min, peak 30-45min, duration 3-6h; some concentrations preservative-free; all conc. available w/ epinephrine 1:200,000

regional anesthesia

Max: 2 mg/kg or 175 mg/dose, 400 mg/24h

spinal anesthesia

Info: onset <1min, peak 15min, duration 3-6h; some concentrations preservative-free; all conc. available w/ epinephrine 1:200,0000

Alerts

Local anesthetic solutions containing antimicrobial preservatives, i.e., those supplied in multiple-dose vials, should not be used for epidural or caudal anesthesia because safety has not been established with regard to intrathecal injection, either intentionally or unintentionally, of such preservatives.

The safety and effectiveness of local anesthetics depend on proper dosage, correct technique, adequate precautions, and readiness

for emergencies. Resuscitative equipment, oxygen, and other resuscitative drugs should be available for immediate use. 

perform retrobulbar blocks should be aware that there have been reports of respiratory arrest following local anesthetic injection. Prior to retrobulbar block, as with all other regional procedures, the immediate availability of equipment, drugs, and personnel to manage respiratory arrest or depression, convulsions, and cardiac stimulation or depression should be assured.

Points of recommendation

To make sure this medicine is safe for you, tell your doctor if you have:

  • If you have an allergy to bupivacaine, epinephrine, or any other part of bupivacaine and epinephrine.
  • If you are allergic to any drugs like this one, any other drugs, foods, or other substances. Tell your doctor about the allergy and what signs you had, like rash; hives; itching; shortness of breath; wheezing; cough; swelling of face, lips, tongue, or throat; or any other signs.
  • If you are taking any of these drugs: Dihydroergotamine, ergonovine, ergotamine, or methylergonovine. 

To make sure bupivacaine is safe for you, tell your doctor if you have:

  • anemia (lack of red blood cells);
  • kidney or liver disease;
  • a bleeding or blood clotting disorder;
  • syphilis, polio, a brain or spinal cord tumor;
  • numbness or tingling;
  • chronic back pain, headache caused by surgery;
  • low or high blood pressure;
  • abnormal curvature of the spine; or 

It is not known whether bupivacaine passes into breast milk or if it could harm a nursing baby. Tell your doctor if you are breast-feeding a baby. 

Avoid driving and doing other tasks or actions that call for you to be alert until you see how bupivacaine and epinephrine affects you.

If you have a sulfite allergy, talk with your doctor.

If you are 65 or older, use this medicine with care. You could have more side effects.

Do not give to a child younger than 12 years of age.

Tell your doctor if you are pregnant or plan on getting pregnant. You will need to talk about the benefits and risks of using bupivacaine and epinephrine while you are pregnant.

Tell your doctor if you are breast-feeding. You will need to talk about any risks to your baby.

Mouth:

Do not eat while your mouth feels numb. You may bite your tongue.

Spinal:

This medicine may cause short-term loss of feeling and motor activity in the lower half of your body. Do not try to get out of bed or do other tasks or actions until feeling and motor activity have returned to normal.

Pregnancy level

C

Related drugs

Lidocaine , prilocaine , Procaine


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