Bupivacaine spinal

BUPIVACAINE SPINAL

Solution for injection 5 mg/ml 4 ml in ampoules No.5

1 ml of the solution contains 5 mg of bupivacaine hydrochloride.

Highly-effective product for spinal anesthesia.

Marketing Authorization No. UA/13417/01/01

Composition

Active ingredient: bupivacaine hydrochloride;

1 ml of the solution contains  5 mg of bupivacaine hydrochloride;

Excipients: glucose monohydrate, hydrochloric acid or sodium hydroxide, water for injections.

Pharmaceutical form

Solution for injection.

Pharmacotherapeutic group

Local anesthetics. Code АТС  N01В В01.

Clinical performance

Indications.

Spinal anesthesia in surgery (for example, urologic surgery, lower limb surgery lasting 2-3 hours, abdominal surgery lasting 45-60 minutes).

Contraindications

Hypersensitivity to the local anesthetics of amide type or to any other component of the product.

Intrathecal anesthesia has its own general contraindications, which include:

  • active and acute central nervous system diseases, such as meningitis, brain tumors, poliomyelitis, intracranial hemorrhage;
  • spinal stenosis and active disease (spondylitis, tumors) or recent vertebral trauma (e.g., fracture);
  • septicemia;
  • malignant anemia with subacute compound degeneration of spinal cord;
  • pyogenic infection of the skin at or adjacent to the site of puncture;
  • cardiogenic or hypovolemic shock;
  • coagulation diseases or ongoing anticoagulation treatment.

Posology and method of administration

Bupivacaine should be applied only by the doctors having the relevant experience in conduction anesthesia. Administer the minimum doses which enable to reach the proper degree of anesthesia. Below are the recommended doses for adult patients; a dose should be adjusted for each patient individually.

The dosage should be reduced for elderly patients and women with late pregnancy.

The recommended site of injection is intervertebral space at L3-L4 segments.

At this time, there is no evidence of applying the doses over 20 mg.

Children up to  40 kg

Bupivacaine may be used in children.

The difference between small children and adults is the relatively high CFS volume in infants and neonates. Thus, it requires a relatively larger dose/kg to produce the same level of block as compared to adults.

The product should be injected only after detection of the subarachnoid cavity through lumbar puncture (until clear CSF is obtained through aspiration or puncture needle). In the event of weak anesthetic effect, another injection should be made at other level with the less anesthetic volume. One of the reason of such weak effect is incorrect distribution of the product in intrathecal cavity. In that case, the needed effect may be reached with the change of patient’s body position.

Instruction for use of  ampule

1. Separate one ampoule from the block and shake the contents gently, holding the ampoule by its neck.

2.Squeeze the ampoule in your hand (the product leakage shall not occur) and remove the cap by rotating it.

3.Immediately put a syringe in the ampoule through the obtained hole.

4.Turn the ampoule over and slowly suck the liquid in the syringe.

5.Put a needle on the syringe.

Adverse reactions

The adverse reaction profile for Bupivacaine is similar to those for other long acting local anesthetics used for intrathecal anesthesia. Adverse reactions caused by the drug are difficult to distinguish from the physiological effects of the nerve block (e.g. decrease in blood pressure, bradycardia, temporary urinary retention). Moreover, it is difficult to distinguish the events caused directly (e.g. spinal hematoma) or indirectly (e.g. meningitis, epidural abscess) by needle puncture or events associated to cerebrospinal leakage (e.g. postdural puncture headache).

Immune system disorders: allergic reactions, anaphylactic shock.

Cardiac disorders: hypotension, bradycardia, cardiac arrest.

Nervous system disorders: postdural puncture headache, paresthesia, paresis, dysesthesia, total unintentional spinal block, paraplegia, paralysis, neuropathy, arachnoiditis.

Gastrointestinal disorders: nausea, vomiting.

Respiratory, thoracic and mediastinal disorders: respiratory depression

Renal and urinary disorders: urinary retention, urinary incontinence

Musculoskeletal and connective tissue disorders: muscle weakness, back pain

Overdose

When used in large doses, bupivacaine may cause toxic effects on central nervous and cardio-vascular system, especially when it is administered intravenously. However, small doses are applied in connection with spinal anesthesia (≤ 20 % of the dose applied in connection with epidural anesthesia). Therefore, the product is not likely to cause overdose. However, if other local anesthetics are concomitantly administered, toxic effects are additive and may cause systemic toxic reactions.

Treatment of complications

Total spinal blockade should be treated by ensuring sufficient ventilation (maintaining a patent airway and giving oxygen by intubation or controlled ventilation, if needed). Hypotension shall be treated with vasopressors (those having inotropic effect are preferable), e.g. ephedrine 10–15 mg intravenously.

In case of acute systemic toxicity, immediately discontinue the use of local anesthetics. The treatment should be aimed at maintenance of the proper ventilation, oxygenation and blood circulation. Always ensure proper oxygen delivery and controlled ventilation, if needed. Should convulsions last more than 15-20 seconds, inject 1-3 mg/kg of thiopental sodium in order to facilitate ventilation, or  0.1 mg/kg of diazepam (which has much slower effect). Long-lasting convulsions carry a threat for normal respiration and oxygenation. Injection of neuromuscular blockers (e.g. succinylcholine 1mg/kg) helps to ensure lung ventilation and oxygenation, however, it requires the relevant experience in tracheal intubation and  controlled ventilation.

Hypotension/bradycardia should be treated with  vasopressors (e.g. ephedrine 10–15 mg intravenously, if needed, repeated the injection 2-3 minutes later).  Cardiac arrest should be immediately treated with cardiopulmonary measures. Among with the acidosis elimination, it is vital to ensure blood oxygenation, respiration and blood circulation.

In case of treatment of systemic toxicity in children, use the doses based on  children’s age and body weight.

Pregnancy and lactation

There is no evidence of untoward effects in human pregnancy. The dose shall be reduced for women with late pregnancy.

Bupivacaine enters the mother's milk, but in such small quantities that there is generally no risk of affecting the child at therapeutic dose levels.

Children.

Bupivacaine may be used in children

Special warnings and precautions for use

Before conducting the treatment, sensitivity test is required.

Intrathecal anesthesia should only be undertaken by specialists with the relevant knowledge and experience.

Regional anesthetic procedures should always be performed in a properly equipped and staffed area where resuscitative equipment and drugs should be immediately available.

Intravenous access should be in place before starting the intrathecal anesthesia. The clinician responsible should be appropriately trained and familiar with the diagnosis and treatment of side effects, systemic toxicity and other complications.

Patients in poor general condition due to ageing or other factors such as partial or complete heart conduction block, advanced liver or renal dysfunction require special attention, as regional anesthesia may be the optimal choice for surgery in these patients.

Patients treated with anti-arrhythmic drugs class III (e.g. amiodarone) should be kept under close surveillance and ECG monitoring considered, since cardiac effects may be additive.

Like all local anesthetic drugs, bupivacaine may cause acute toxicity effects on the central nervous and cardiovascular systems, if utilized for local anesthetic procedures resulting in high blood concentrations of the drug. This is especially the case after unintentional intravascular administration.

Ventricular arrhythmia, ventricular fibrillation, sudden cardiovascular collapse and death have been reported in connection with high systemic concentrations of bupivacaine. However, high concentrations are not expected with doses normally used for intrathecal anesthesia.

A very rare, but serious complication of the spinal anesthesia is high or total spinal blockade, resulting in cardiovascular and respiratory depression. Cardiovascular depression is caused by the advanced sympathetic block which in its turn may result in advanced arterial hypotension and bradycardia or even cardiac arrest. Respiratory depression may be caused by the block of innervation of respiratory muscles, including diaphragm.

Elderly patients or women with late pregnancy are in the risk group of developing high or total spinal blockade. The dose should be reduced in these patients.

Patients with hypovolemia due to any cause can develop sudden and severe hypotension during intrathecal anesthesia, regardless the kind of anesthetic used. Hypotension occurring after intrathecal anesthesia is rare among the children under 8 years old.

Neurological injury is a rare consequence of intrathecal anesthesia and may result in paresthesia, anesthesia, motor weakness and paralysis. Occasionally these are permanent.

The complications related to the following neurological diseases are not likely to happen during  intrathecal anesthesia: multiple sclerosis, hemiplegia, paraplegia and neuromuscular diseases. However, the patients having the mentioned diseases require special attention.  Before treatment is instituted, consideration should be taken if the benefits outweigh the possible risks for the patient.

Effects on ability to drive and use machines.

Local anesthetics have a minor influence on motion coordination resulting in temporary motor dysfunction and impairment of psychomotor action while driving the machines.

Interaction with other medicinal products and other forms of interaction.

Bupivacaine should be used with caution in patients receiving other local anesthetics or agents structurally related to local anesthetics of amide type, 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 is advised

Pharmacological properties

Pharmacodynamic properties. Bupivacaine is  the long acting local anesthetic of amide type.

Bupivacaine has revertible action and blocks the impulses which  pass through nerve fibers by  inhibiting the transport of sodium ions through neural membranes. Similar affects may be observed in activated membranes of the brain and cardiac muscle.

Bupivacaine is used for hyperbaric spinal anesthesia. Relative thickness of the solution at 20 ºС is 1.026 (or 1.021 at 37 ºС). The spread of Bupivacaine in the intrathecal space is affected by gravity.

Pharmacokinetic properties. Bupivacaine is the lipid-soluble substance and its coefficient of water/oil distribution is 27.5.

The substance is absorbed within two phases. Half-life period is 50 and 400 minutes respectively. Slow absorption phase limits recovery of Bupivacaine and this is the reason why the final phase of half-life period requires more time than intrathecal injection, as compared to intravenous injection. During intrathecal injection, Bupivacaine concentration in blood is significantly lower, as compared to the other regional anesthetic procedures. It is explained by the smaller dose needed for intrathecal anesthesia. In general, the maximum plasma concentration is increased to 0.4 mg/l per 100 mg injected. It means that plasma concentration should be 0.1 mg/l after injection of 20 ml of the solution. When administered intravenously, the general plasma clearance of bupivacaine is 0.58 l/min, steady state volume distribution is 73 l, final half-life period is 0.40. Usually, bupivacaine binds with alpha1-acid glycoprotein, binding with the proteins is 96%. Bupivacaine is metabolized in liver. Its clearance depends on changes occurring within ferments of the liver, rather than its perfusion.

Metabolites are considered to be pharmacologically active too, but less active, as compared ti bupivacaine.

Bupivacaine passes the placental barrier. Concentration of free bupivacaine is the same in mother and fetus. However, the general plasma concentration is lower in fetus having the lower degree of binding with the proteins.

Physical and chemical properties

Clear colorless liquid.

Incompatibilities

Mixture with other  solutions is not recommended.

Shelf life

2 years.

The ampules are not stored when opened.

Storage conditions

Store in original package at the temperature not above 25°C. Keep away from children. Do not freeze.

Package

4 ml in ampule  No. 5.

Prescription category

Following the  doctor’s prescription.

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