Presentation
Bupi™ Heavy Injection: Each 4 ml contains 20 mg Bupivacaine Hydrochloride (as anhydrous) USP and 320 mg Dextrose BP.

 

Description
Bupivacaine Hydrochloride is 1-Butyl-2′ 6′-pipecoloxylidide monochloride, monohydrate, a white crystalline powder that is freely soluble in 95 percent ethanol, soluble in water, and slightly soluble in chloroform or acetone. Dextrose is D-glucopyranose monohydrate. Bupivacaine (Bupivacaine in Dextrose Injection, USP) is available in sterile, hyperbaric solution for subarachnoid injection (spinal block).Bupivacaine hydrochloride is related chemically and pharmacologically to the aminoacyl local anaesthetics. It is a homologue of mepivacaine and is chemically related to lidocaine. All three of these anaesthetics contain an amide linkage between the aromatic nucleus and the amino or piperidine group. They differ in this respect from the procaine-type local anaesthetics, which have an ester linkage. Each 1 ml of Bupivacaine Heavy contains 5 mg Bupivacaine hydrochloride, anhydrous and 80 mg dextrose, anhydrous.

 

Indications
Bupivacaine Heavy is indicated for the production of spinal anaesthesia for
Urological surgery
Lower limb surgery
Abdominal surgery

 

Dosage and Administration
The doses recommended below should be regarded as a guide for use in the average adult Spinal anaesthesia for surgery: 2-4 ml (10-20 mg Bupivacaine hydrochloride). The spread of anaesthesia obtained with Bupivacaine depends on several factors including the volume of the solutions and the position if the patients during and following the injection. When injected in the L3-L4 intervertebral space with the patient in the sitting position, 3 ml of Bupivacaine spreads to the T7- T10 spinal segments. With the patient receiving the injection in the horizontal position and then turned supine, the blockade spine spreads to T4-T7 spinal segments. It should be understood that the level of spinal anaesthetic can be unpredictable in a given patient.

 

Side Effects
Reactions to Bupivacaine are characteristic of those associated with other amide-type local anaesthetics. The most commonly encountered acute adverse experiences which demand immediate countermeasures following the administration of spinal anaesthesia are hypotension due to loss of sympathetic tone and respiratory paralysis or under ventilation due to cephalic extension of the motor level of anaesthesia. These may lead to cardiac arrest if untreated. In addition, dose-related convulsions and cardiovascular collapse may result from diminished tolerance, rapid absorption from the injection site or from unintentional intravascular injection of a local anaesthetic solution. Factors influencing plasma protein binding, such as acidosis, systemic diseases which alter protein production, or competition of other drugs for protein binding sites, may diminish individual tolerance.

 

Contraindications
Bupivacaine (Bupivacaine in Dextrose Injection, USP) is contraindicated in patients with a known hypersensitivity to it or to any local anaesthetic agent of the amide-type. The following conditions preclude the use of spinal
anaesthesia:

Severe hemorrhage, severe hypotension or shock and arrhythmias, such
as complete heart block, which severely restrict cardiac output
Local infection at the site of proposed lumbar puncture
Septicemia

 

Drug Interactions
Bupivacaine should be used with care in patients receiving antiarrhythmic drugs with local anaesthetic activity, as their toxic effects may be additive. Phenothiazines and Butyrophenones may reduce or reverse the pressor effect of epinephrine.

 

Precautions
The safety and effectiveness of spinal anaesthetics 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. The patient should have I.V. fluids running viaan indwelling catheter to assure a functioning intravenous pathway. The lowest dosage of local anaesthetic that results in effective anaesthesia should be used. Aspiration for blood should be performed before injection and injection should be made slowly. Tolerance varies with the status of the patient. Debilitated, elderly patients and acutely ill patients may require reduced doses. Reduced doses may also be indicated in patients with increased intra-abdominal pressure (including obstetrical patients), if otherwise suitable for spinal anaesthesia.

There should be careful and constant monitoring of cardiovascular and respiratory (adequacy of ventilation) vital signs and the patient’s state of consciousness after local anaesthetic injection. Restlessness, anxiety, incoherent speech, lightheadedness, numbness and tingling of the mouth and lips, metallic taste, tinnitus, dizziness, blurred vision, tremors, depression or drowsiness may be early warning signs of central nervous system toxicity. Spinal anaesthetics should be used with caution in patients with severe disturbances of cardiac rhythm, shock, or heart block.

Sympathetic blockade occurring during spinal anaesthesia may result in peripheral vasodilation and hypotension, the extent depending on the number of dermatomes blocked. Blood pressure should, therefore, be carefully monitored especially in the early phases of anaesthesia. Hypotension may be controlled by vasoconstrictors in dosages depending on the severity of hypotension and response of treatment. The level of anaesthesia should be carefully monitored because it is not always controllable in spinal techniques.

 

Use in Pregnancy

There are no adequate and well-controlled studies in pregnant women of the effect of Bupivacaine on the developing fetus. Bupivacaine Hydrochloride should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. This does not exclude the use of Bupivacaine Heavy at term for obstetrical anaesthesia.

 

Use in Lactation

It is not known whether local anaesthetic drugs are excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when local anaesthetic drugs are administered to a nursing woman.

 

Use in Children

Until further experience is gained in patients younger than 18 years, administration of Bupivacaine Heavy in this age group is not recommended.

 

Over Dosage
Acute emergencies from local anaesthetics are generally related to high plasma levels encountered during therapeutic use or to underventilation (and perhaps apnea) secondary to upward extension of spinal anaesthesia. Hypotension is commonly encountered during the conduct of spinal anaesthesia due to relaxation of sympathetic tone, and sometimes, contributory mechanical obstruction of venous return.

 

Pharmaceutical Precautions
The solution must not be stored in contact with metals e.g. needles or metal parts of syringes , a dissolved metal ions may cause swelling at the site of injection. The solution is preservative free. The solution should be used immediately after opening of the ampoule. Any remaining solution should be discarded.

 

Commercial Pack
Bupi™ Heavy Injection: Each box contains 1 x 5 ampoules in blister pack .