Bupicasan

Each mL contains: Bupivacaine Hydrochloride Monohydrate equivalent to Bupivacaine Hydrochloride 5 mg, Dextrose Monohydrate 80 mg.

Pharmacology: Bupivacaine Hydrochloride is a long acting local anaesthetic agent of the amide type. Bupivacaine Hydrochloride has rapid onset of action and long duration. The duration of analgesia in the T10-T12 segments is 2-3 hours.
Bupivacaine Hydrochloride is a hyperbaric solution and its initial spread in the subarachnoid space is considerable affected by gravity. Moreover, its spread cephalad more extensively than the isobaric solutions, even in the horizontal position when the effect gravity is minimal. Due to the larger intrathecal distribution and the consequently lower mean concentration the duration of anaesthesia tends to be shorter. In the isobaric solution without added dextrose produces a lower level of block, but of longer duration than the hyperbaric solution.
Bupivacaine Hydrochloride, like the other local anaesthetics, causes a reversible blockade of impulse propagation along nerve fibers by preventing the inward movement of sodium ions through the nerve membrane. Local anaesthetics of the amide type are thought to act within the sodium channels of the nerve membrane.
Bupivacaine Hydrochloride has a pKa of 8.1 at 25°C and an oil/water partition coefficient of 27.5.
Absorption from the subarachnoid space is relative slow and this, together with the small dose required for spinal anaesthesia, limits the maximum plasma concentration, which is approximately 0.4 mg/mL for every 100 mg injected. This means that the maximum recommended dose (20 mg) would result in plasma levels of less than 0.1 mg/mL.
After IV Injection Bupivacaine Hydrochloride has a total plasma clearance of 0.58 L/min, a volume of distribution at steady state of 73 L, an elimination half-life of 2.7 h and a hepatic extraction ratio 0.40. Clearance of Bupivacaine Hydrocloride is almost entirely due to liver metabolism, and depends upon both liver blood flow and the activity of the metabolizing enzymes.
Bupivacaine Hydrochloride readily crosses the placenta and equilibrium in regards of free drug will be reached. Because the degree protein binding in the foetus is less than in the mother, the total plasma will be greater in the mother, although the free concentration will be the same. Bupivacaine is excreted in breast milk, but in such small quantities that there is no risk to the child.
Only 8% of Bupivacaine excreted in unchanged form, primary metabolite which becomes 2,6 pipecolyxylidine (PPX), and its derivates.

BUPICASAN SPINAL 0.5% HEAVY is spinal anaesthesia for surgery (urological and lower limb surgery lasting 2-3 hours, abdominal surgery lasting 45-60 minutes).

Dosage recommendation: The dosage in the table are those thought to be necessary for the production of a successful block and should be regarded as guideline for use in the average adult. Regarding spread and duration times, there are wide individual variations and it is impossible to be precise. (See table.)


Click on icon to see table/diagram/image


Spinal injections should only be made after the subarachnoid space has been clearly identified by lumbar puncture. No drug should be injected until clear cerebrospinal fluid (CSF) is seen to escape from the spinal needle, or is detected by aspiration.
Failure of spinal anaesthesia has been reported in 1-5% of the patients. One reason for failure could be intrathecal maldistribution of the local anaesthetic e.g. entrapment in the caudal end of the dural sack or within a "pocket" with restricted communication to the major CSF space. In such cases a better spread, i.e. a sufficient block, may be achieved after temporary change(s) in the patient's position. If a supplementary block is necessary, it should be performed at a different level and with a reduced volume of the local anaesthetic. Only one extra attempt should be made.
The following dosage recommendations should be regarded as guide for use in the average adult. The effects of spinal administration of BUPICASAN SPINAL 0.5% HEAVY exceeding 20 mg have not been reported.
The use of spinal anaesthesia in children requires a through knowledge of differences between adults and children to enable the administration of adequate doses of the drug used. A relatively a high CSF volume is found in infants and neonates. They therefore require a relatively larger dose/Kg to produce the same level of block.
In small children the nerves are less myelinated, allowing easier diffusion and a more rapid onset of anaesthesia.
The hypotension usually seen after spinal blocks in adults is uncommon in children under the age of 8.
BUPICASAN SPINAL 0.5% HEAVY may be used in children. The following doses are recommended: 0.40-0.50 mg/kg for infants up to 5 kg.
0.30-0.40 mg/kg for children weighing between 5 and 15 kg.
0.25-0.30 mg/kg for children weighing more than 15 kg.
As the solutions are free from preservatives, they should be used immediately after opening of the container. Any remaining solution should be discarded.
Since BUPICASAN SPINAL 0.5% HEAVY contains dextrose/glucose, caramelization may occur during autoclaving. This preparation should therefore not be resterilized.

Known hypersensitivity to local anaesthetics of the amide type.
Acute active disease of the central nervous system, such as meningitis, poliomyelitis and cranial haemorrhage.
The presence of active tuberculosis or metastatic lesions in the vertebral column is also a contraindication.
Septicaemia.
Pernicious anemia with subacute combined degeneration of the spinal cord.
Pyrogenic infection of the skin or adjacent to the site of puncture.
Cardiogenic or hypovolaemic shock.
Coagulation disorders or ongoing anticoagulant treatment.

Spinal anaesthesia should only be undertaken by or under the supervision of clinicians with the necessary knowledge and experience. Spinal anaesthesia should only be given in a fully equipped operating suite where all the necessary resuscitative equipment and drugs are immediately available. The anaesthetist must remain in constant attendance until the operation is finished and must supervise the recovery until the anaesthesia has worn off.
Intravenous access, e.g. and IV infusion, should be in place before starting the spinal anaesthesia.
Regardless of the local anaesthetic used hypotension and bradycardia may occur. This should be prevented either by pre-loading the circulation with the crystalloidal or colloidal solutions, or by injecting a vasopressor, such as Ephedrine 20-40 mg IM, or treated promptly with, for example Ephedrine 5-10 mg intravenously and repeated as necessary.
Hypotension is common in patients with hypovolemia due to haemorrhage or dehydration and in those with aortocaval occlusion due to abdominal tumours or the pregnant uterus in late pregnancy. Hypotension is poorly tolerated by patients with coronary or cerebrovascular disease.
Spinal anaesthesia can be unpredictable and very high blockades are sometimes encountered with paralysis of the intercostals muscles and even the diaphragm, especially in pregnancy. On rare occasions it will be necessary to assist or control ventilation.
Chronic neurological disorders, such as multiple sclerosis, old hemiplegia due to stroke etc., are not thought to be adversely affected by spinal anaesthesia, but call for caution.
NB. Because spinal anaesthesia may be preferable to general anaesthesia in some high-risk patients, attempts should be made to optimize their general condition pro-operatively when time allows.
Effects on ability to drive cars and use machines: Spinal anaesthesia per se has little effect on mental function and coordination but will temporarily impair locomotion and alertness.

It is reasonable to assume that a large number of pregnant women and women of child-bearing age have been given Bupivacaine Hydrochloride. No specific disturbances to the reproductive process have so far been reported, e.g. no increased incidence of malformations.
Bupivacaine Hydrochloride enters the mother's milk, but in such small amounts that there is generally no risk of this affecting the neonate.

In general, almost all the side effects seen with spinal anaesthesia are due to the nerve blockade itself and not to the drug used. These effects include hypotension, bradycardia and post-spinal headache. Other undesirable effects in connection with spinal anaesthesia are: High or total spinal blockade: A rare, though severe, adverse reaction following spinal anaesthesia is high or total spinal blockade resulting in cardiovascular and respiratory depression. The cardiovascular depression is caused by extensive sympathetic blockade which may result in profound hypotension and bradycardia, or even cardiac arrest. Respiratory depression is caused by blockade of the innervation of the respiratory muscles, including diaphragm.
Neurological complication: Neurological damage is a rare, though recognized, consequence of spinal anaesthesia. It may have one of several causes such as direct injury to the spinal cord or spinal nerves, anterior spinal artery syndrome, injection of an irritant substance, injection of a non-sterile solution or the development of a space occupying lesion (haematoma or abscess) within the spinal canal. These may result in localized areas paraesthesia or anaesthesia, motor weakness, loss of sphincter control and paraplegia. Occasionally these are permanent. Neurological complications of this type have been reported with all local anaesthetics used for spinal anaesthesia.
Allergic reactions: Allergic reactions (in the most severe instances anaphylactic shock) to local anaesthetics of the amide type are rare.
Acute systemic toxicity: Like all local anaesthetic drugs, Bupivacaine Hydrochloride may have acute toxic effects on the central nervous and cardiovascular system, if given in high doses. This is especially the case if the injection is made intravascularly. However, the dose required for spinal anaesthesia is so small (20% or less than that required for epidural anaesthesia) that acute systemic toxicity is extremely unlikely and has not been reported.

Bupivacaine Hydrocloride should be used with caution in patients receiving agents structurally related to local anaesthetics, since the toxic effect are additive.

Store below 30°C. Protect from light. Do not freeze.

Anaesthetics - Local & General

N01BB51 - bupivacaine, combinations ; Belongs to the class of amides. Used as local anesthetics.

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