Universal reference book for medicines
Product name: BUPIVACAINE (BUPIVACAINE)

Active substance: bupivacaine

Type: Local anesthetic

Manufacturer: VELFARM (Russia) produced SYNTHESIS (Russia)
Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..

PHARMACHOLOGIC EFFECT
Local anesthetic of amide type.
The anesthetic effect occurs quickly (within 5-10 min). The mechanism of action is due to the stabilization of neuronal membranes and the prevention of the occurrence and conduct of a nerve impulse. The analgesic effect continues after anesthesia has ceased, which reduces the need for postoperative analgesia. With spinal anesthesia, bupivacaine causes a mild relaxation of the muscles of the lower extremities of 2-2.5 hours duration. With intercostal blockade, the action of bupivacaine lasts 7-14 hours; with epidural blockade - 3-4 hours; with blockade of abdominal muscles - 45-60 minutes. Some medicinal forms of bupivacaine include epinephrine.
PHARMACOKINETICS
Binding to plasma proteins is 95%.

Metabolised in the liver.

T 1/2 in adults is 1.5-5.5 h, in newborns - about 8 h.

It is excreted in the urine mainly in the form of metabolites and 5-6% - in unchanged form.

Bupivacaine penetrates into the cerebrospinal fluid.

INDICATIONS
Spinal anesthesia in surgery (for surgical interventions in urology or nizhnetorakalnoy surgery lasting up to 3-5 hours, in abdominal surgery - with a duration of 45-60 minutes).
Blockade of the trigeminal nerve, sacral, brachial plexus, pudendal nerve, intercostal, caudal anesthesia and epidural anesthesia in cesarean section.Anesthesia in the direction of dislocation of the joints of the upper and lower extremities.
DOSING MODE
The dose depends on the type of anesthesia.
To anesthetize in surgery (diagnostic and therapeutic manipulation) apply 2.5-100 mg. For blockade of the trigeminal nerve - 2.5-12.5 mg; of the stellate node - 25-50 mg; sacral, brachial plexus - 75-150 mg; intercostal blockade - 10-25 mg; blockade of peripheral nerves - 25-150 mg.For long-term epidural spinal anesthesia, the initial dose is 50 mg, supporting 15-25-40 mg every 4-6 hours. When epidural and caudal anesthesia is performed in obstetric practice, the dose is 15-50 mg. Epidural anesthesia with caesarean section - 75-150 mg. With blockade of the pudend nerve - 12.5-25 mg on each side.
The maximum dose is 2 mg / kg.

SIDE EFFECT
From the central nervous system and peripheral nervous system: numbness of the tongue, dizziness, blurred vision, muscle tremor, drowsiness, convulsions, loss of consciousness.
In the field of anesthesia, paresthesias, weakening of the sphincter tone are possible.
From the cardiovascular system: reduction of cardiac output, heart block, arterial hypotension, bradycardia, ventricular arrhythmias, cardiac arrest.

From the respiratory system: apnea.

Allergic reactions: skin manifestations, in severe cases - anaphylactic shock.

Side effects are rare, the likelihood of their development is increased when using an inadequate dose and disturbing the technique of bupivacaine administration.

CONTRAINDICATIONS
Meningitis, tumors, poliomyelitis, intracranial bleeding, osteochondrosis, spondylitis, tuberculosis, metastatic spinal lesions, pernicious anemia with neurologic symptoms, heart failure in decompensation phase, massive pleural effusion, significantly increased intra-abdominal pressure, expressed ascites, abdominal tumors, severe arterial hypotension (cardiogenic or hypovolemic shock), septicemia, coagulation disorder, or anticoagulant therapy, intravenous regional anesthesia
Yeru, paracervical block in obstetrics, in the form of 0.75% solution for epidural block in obstetrics, pustular skin lesions at the injection site, increased sensitivity to local anesthetics of amide type.
PREGNANCY AND LACTATION
Application in pregnancy and during lactation is possible in cases where the expected benefit to the mother exceeds the potential risk to the fetus or child.

Penetrates through the placental barrier, but the ratio of concentrations in the blood of the fetus and the mother is very low.

Isolated with breast milk in small amounts.
It is believed that the risk of adverse effects on the infant is almost non-existent.
SPECIAL INSTRUCTIONS
Spinal anesthesia should be performed only under the supervision of an experienced anesthesiologist.

When spinal anesthesia is performed in patients with hypovolemia, the risk of sudden and severe arterial hypotension is increased.

Caution is used in patients who receive antiarrhythmic drugs with local anesthetic activity.

It should be strictly observed that the used bupivacaine dosage form is in compliance with the indications for use.

DRUG INTERACTION
When used simultaneously with antiarrhythmic drugs with local anesthetic activity, the risk of additive toxic effects increases.

With simultaneous use with barbiturates, a decrease in the concentration of bupivacaine in the blood is possible.

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