B-CAINE

Local Anesthetic

(Bupivacaine Hydrochloride Injection USP 0.5% W/V)

DESCRIPTION

B-CAINE (Bupivacaine Hydrochloride Injection USP 0.5% w/v) is used as a local or regional anesthetic for various procedures. Its safety and effectiveness depend on proper dosage, correct administration and readiness for emergencies. Bupivacaine is a prescription medication used to prevent pain and induce spinal anesthesia. Bupivacaine belongs to a group of drugs called local anesthetics. These work by numbing one small area of the body (local) or blocking pain in an area of the body (regional). This medication is available in an injection form to be administered by injection via local infiltration, peripheral nerve block, or caudal and lumbar blocks by a healthcare professional.

COMPOSITION

Each ML Contains:

Bupivacaine Hydrochloride USP
Eq. to anhydrous
• Bupivacaine Hydrochloride......... 5.0 mg
• Methylparaben USP............. 1.0 mg
(As preservative)
• Water for Injection USP......... q.s.

PHARMACOLOGICAL ACTION

Pharmacodynamic :

Bupivacaine has a similar mechanism of action to other local anesthetic in nerve axons in the peripheral nervous system. It also interferes with the function of all organs in which conduction or transmission of impulses occur. These include effects on the CNS, the autonomic ganglia, the neuromuscular junction and all forms of muscle fibres. At high doses it produces surgical anaesthesia, while at lower doses it produces sensory block (analgesia) with less pronounced motor block. Following absorption, Bupivacaine may cause stimulation of the CNS followed by depression and, in the cardiovascular system, it acts primarily on the myocardium where it may decrease electrical excitability, conduction rate, force of contraction and eventually cardiac arrest.

Pharmacokinetic Properties:

Like other local anesthetic, the rate of systemic absorption of Bupivacaine is dependent upon the total dose and concentration administered, the route of administration and the vascularity of the tissue locally. Bupivacaine is about 95% bound to plasma proteins, mainly to alpha-1- acid glycoprotein at low concentrations and to albumin at high concentrations. In adults, the terminal half-life of Bupivacaine is 2.7 hours. In neonates and some young infants, terminal elimination half-lives could be as long as 8 to 12 hours. The maximum blood concentration varies with the site of injection.
Amide local anesthetic including Bupivacaine have been shown to have diminished clearance in neonates and infants less than 3 months of age, with steady maturation until they reach levels of adult clearance at about 8 months of age. Foetal concentrations are lower than maternal concentrations because only the free, unbound drug is available for placental transfer. Local anesthetic are distributed to some extent to all body tissues, with higher concentrations found in highly perfused organs such as liver, heart and brain. In children the pharmacokinetics is similar to that in adults. Bupivacaine is metabolised in the liver and is excreted in the urine mainly as metabolites, with only 5 to 6% as unchanged drug.

CLINICAL PHARMACOLOGY

Indications And Usage:

B-CAINE (Bupivacaine Hydrochloride Injection USP 0.5% w/v) is available in an injection form to be administered by injection via local infiltration, peripheral nerve block, or caudal and lumbar blocks by a healthcare professional. The dose, frequency and route of administration will vary, depending on the indication for use.

Dosage And Administration:

Take B-CAINE (Bupivacaine Hydrochloride Injection USP 0.5% w/v) exactly as prescribed by your doctor. Follow the directions on your prescription label carefully. The dose your doctor recommends may be based on the following:
• The condition being treated
• Other medical conditions you have
• Other medications you are taking
• How you respond to this medication
• Your weight
• Your height
• Your age
• Your gender

Contraindications:

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 because of potential risk of tourniquet failure and systemic absorption of the drug and subsequent The 0.75% formulation is contraindicated in epidural anesthesia during labor because of the association with refractory cardiac arrest.

Over Dosage:

The dose, frequency, and route of administration will vary, depending on the indication for use.
Accidental intravascular injections of local anesthetic may cause immediate (within seconds to a few minutes) systemic toxic reactions. In the event of overdose, systemic toxicity appears later (15-60 minutes after injection) due to the slower increase in local anesthetic blood concentration.

Special Warnings And Precautions For Use:

There have been reports of cardiac arrest during the use of bupivacaine for epidural anaesthesia. or peripheral nerve blockade where resuscitative efforts have been difficult, and were required to be prolonged before the patient responded. However, in some instances resuscitation has proven impossible despite apparently adequate preparation and appropriate management.
Like all local anaesthetic drugs, bupivacaine may cause acute toxicity effects on the central nervous and cardiovascular systems if utilised for local anaesthetic procedures resulting in high blood concentrations of the drug. This is especially the case after unintentional intravascular administration or injection into highly vascular areas. Ventricular arrhythmia, ventricular fibrillation, sudden cardiovascular collapse and death have been reported in connection with high systemic concentrations of bupivacaine.
Adequate resuscitation equipment should be available whenever local or general anaesthesia is administered. The clinician responsible should take the necessary precautions to avoid intravascular injection .
Before any nerve block is attempted, intravenous access for resuscitation purposes should be established. Clinicians should have received adequate and appropriate training in the procedure to be performed and should be familiar with the diagnosis and treatment of side effects, systemic toxicity or other complications.
Major peripheral nerve blocks may require the administration of a large volume of local anaesthetic in areas of high vascularity, often close to large vessels where there is an increased risk of intravascular injection and/or systemic absorption. This may lead to high plasma concentrations.

Interaction With Other Medicinal Products And Other Forms Of Interaction :

Bupivacaine should be used with caution in patients receiving other local anesthetic or agents structurally related to amide-type local anesthetic, e.g. certain anti-arrhythmics, such as Lidocaine and Mexiletine, since the systemic toxic effects are additive.
Specific interaction studies with Bupivacaine and anti-arrhythmic drugs class III (e.g. amiodarone) have not been performed, but caution should be advised.

Pregnancy And Lactation :

There is no evidence of untoward effects in human pregnancy. In large doses there is evidence of decreased pup survival in rats and an embryological effect in rabbits if Bupivacaine is administered in pregnancy. Bupivacaine should not therefore be given in early pregnancy unless the benefits are considered to outweigh the risks.Foetal adverse effects due to local anesthetic, such as foetal bradycardia, seem to be most apparent in paracervical block anaesthesia. Such effects may be due to high concentrations of anesthetic reaching the foetus. Bupivacaine enters the mother's milk, but in such small quantities that there is no risk of affecting the child at therapeutic dose levels.

Effects On Ability To Drive And Use Machines :

In general, it is sufficient to allow 2 - 4 hours post nerve block or until full functions have returned following regional nerve block. In many situations, patients receive a sedative or other CNS depressant drug e.g., Diazepam, Midazolam to allow the block to be performed. One must allow adequate time for the effects of these drugs to clear.Depending on dosage, local anesthetic may have a very mild effect on mental function and coordination even in the absence of overt CNS toxicity and may temporarily impair locomotion and alertness.

Undesirable Effects :

Accidental sub-arachnoid injection can lead to very high spinal anaesthesia possibly with apnoea and severe hypotension.
The adverse reaction profile for Bupivacaine Hydrochloride is similar to those for other long acting local anesthetic. Adverse reactions caused by the drug per se are difficult to distinguish from the physiological effects of the nerve block (e.g., decrease in blood pressure, bradycardia), events caused directly (e.g., nerve trauma) or indirectly (e.g., epidural abscess) by needle puncture.
Neurological damage is a rare but well recognised consequence of regional and particularly epidural and spinal anaesthesia. It may be due to several causes, e.g. direct injury to the spinal cord or spinal nerves, anterior spinal artery syndrome, injection of an irritant substance, or an injection of a non-sterile solution. These may result in localised areas of paraesthesia or anaesthesia, motor weakness, loss of sphincter control and paraplegia. Occasionally these are permanent.
The adverse reactions considered at least possibly related to treatment with Bupivacaine Hydrochloride from clinical trials with related products and post-marketing experience are listed below by body system organ class and absolute frequency. Frequencies are defined as very common (1/10), common (1/100, <1/10), uncommon (1/1,000, < 1/100), rare (1/10,000, < 1/1,000), including isolated reports, or not known (identified through post-marketing safety surveillance and the frequency cannot be estimated from the available data).

Table Of Adverse Drug Reaction (ADR)

Hepatic dysfunction, with reversible increases of SGOT, SGPT, alkaline phosphatase and bilirubin, have been observed following repeated injections or long-term infusions of Bupivacaine. If signs of hepatic dysfunction are observed during treatment with Bupivacaine, the drug should be discontinued.

STORAGE

Store below 30°C. Protected from light. Do not allow to freeze. Keep out of reach of children.

SHELF LIFE

24 Months.

HOW SUPPLIED

B-CAINE (Bupivacaine Hydrochloride Injection USP 0.5% w/v) supplied in 10 mL glass vial.