Grindeks bupivacaine Spinal
Producer: AS Grindex (JSC Grindeks) Latvia
Code of automatic telephone exchange: N01BB01
Release form: Liquid dosage forms. Solution for injections.
General characteristics. Structure:
Active ingredient: 5 mg of bupivacaine of a hydrochloride of monohydrate in terms of hydrochloride bupivacaine.
Excipients: sodium chloride, 0,1 M acid solution hydrochloric or 0,1 M solution of sodium of hydroxide to pH 4,0-6,5, water for injections.
Solution for intrathecal introduction (local anesthetic for spinal anesthesia).
Pharmacological properties:
Pharmacodynamics. Anesthetic of long action of amide type, is 4 times more powerful than lidocaine. Reversibly blocks carrying out an impulse on nerve fibril due to influence on natrium channels, has hypotensive effect, slows down ChSS.
At intrakostalny postoperative to blockade the analgesia is supported during 7-14 h. After single epidural introduction to concentration of 5 mg/ml duration of effect makes 2-5 h, to 12 h - at a peripheral nerve block.
The drug solution containing a dextrose hyperbaric and in a subarachnoid space influences its distribution gravity.
The small volume of distribution in a subarachnoid space results in smaller average concentration and reduction of duration of effect of drug in comparison with isobaric solution. Use of solutions in concentration of 2.5 mg/ml renders smaller effect on motor nerves.
Pharmacokinetics. Concentration of bupivacaine in plasma depends on a dose, a way of introduction and the number of veins in the place of an injection. The bupivacaine elimination half-life after the general and two-phase absorption respectively makes 7 minutes and 6 hours of an epidural space. The slow phase of absorption is a factor which limits bupivacaine removal speed. Therefore the bupivacaine elimination half-life at epidural introduction is longer, than after an intravenous injection.
The general clearance in/in an injection makes later of plasma 580 ml/min., distribution volume – 73 l, an elimination half-life – 2,7 h, an indicator of hepatic extraction – 0,4. Linkng with proteins of plasma makes 96 %. Bupivacaine is well dissolved in fats.
Bupivacaine is metabolized in a liver, by a hydroxylation in 4-hydroxy-bupivacaine and by N-dealkylation in 2,6-pipekoloksilidin (RRH), a mediator of both processes is P4503A4 cytochrome.
After epidural introduction in urine about 0,2% of not changed bupivacaine, 1% of a pipekoloksilidin and about 0,1% 4 hydroxybupivacaines are found.
Bupivacaine gets through a placenta. Linkng with proteins of plasma in an organism of a fruit is lower, than in mother's organism, concentration of untied fraction in an organism of a fruit and mother is identical. Cosecretes with mother's milk. It is removed mainly by kidneys, only 5-6% of bupivacaine are removed in not changed view with urine.
Indications to use:
Spinal anesthesia in surgery (for operative measures in urology or nizhnetorakalny surgery lasting up to 3-5 h; in abdominal surgery - lasting 45-60 min.). Blockade of a trifacial, sacral, humeral textures, a pudental nerve, intercostal, caudal anesthesia and epidural anesthesia at Cesarean section. Anesthesia at reposition of dislocations of joints of upper and lower extremities.
Route of administration and doses:
The dose depends on a type of anesthesia. In surgery (diagnostic and medical manipulations) apply 2.5-100 mg to anesthesia.
For carrying out blockade of a trifacial - 2.5-12.5 mg; a star-shaped node - 25-50 mg; a sacral, brachial plexus - 75-150 mg; intercostal blockade - 10-25 mg; blockade of peripheral nerves - 25-150 mg.
For carrying out long epidural spinal anesthesia an initial dose - 50 mg, supporting - 15-25-40 mg each 4-6 h.
When carrying out epidural and caudal anesthesia in obstetric practice the dose makes 15-50 mg.
Epidural anesthesia at Cesarean section - 75-150 mg. At blockade of a pudental nerve - 12.5-25 mg from each party.
The maximum dose makes 2 mg/kg.
Features of use:
Spinal anesthesia should be carried out only under observation of the experienced anesthesiologist.
When carrying out spinal anesthesia at patients with a hypovolemia the risk of development of sudden and heavy arterial hypotension is increased.
With care apply at patients who receive antiarrhytmic drugs with mestnoanesteziruyushchy activity.
It is necessary to observe strictly compliance of the used dosage form of bupivacaine to indications to use.
Use at pregnancy and in the period of a lactation perhaps in cases when the expected advantage for mother exceeds potential risk for a fruit or the child.
Very low gets through a placental barrier, but a ratio of concentration into blood of a fruit and mother.
It is allocated with breast milk in insignificant quantities. It is considered that the risk of an adverse effect on the baby is practically absent.
Side effects:
From TsNS and peripheral nervous system: numbness of language, dizziness, sight illegibility, muscular tremor, drowsiness, spasms, loss of consciousness. In the field of anesthesia paresthesias, weakening of a tone of sphincters are possible.
From cardiovascular system: reduction of cordial emission, heart block, arterial hypotension, bradycardia, ventricular arrhythmias, cardiac standstill.
From respiratory system: apnoea.
Allergic reactions: skin manifestations, in hard cases - an acute anaphylaxis.
Side effects are observed seldom, the probability of their development increases at use of an inadequate dose and disturbance of the technology of administration of bupivacaine.
Interaction with other medicines:
Contraindications:
Meningitis, tumors, poliomyelitis, intracranial bleeding, osteochondrosis, spondylites, tuberculosis, metastatic damages of a backbone, pernicious anemia with neurologic symptomatology, heart failure in a decompensation phase, a massive pleural exudate, the increased intra belly pressure, the expressed ascites, tumors of an abdominal cavity, the expressed arterial hypotension (cardiogenic or hypovolemic shock), a septicaemia, disturbance of a fibrillation or therapy by anticoagulants, in/in regional anesthesia on Biyera, paracervical blockade in obstetrics, in the form of 0.75% of solution for epidural blockade in obstetrics, pustulous damages of skin in the place of an injection, hypersensitivity to mestnoanesteziruyushchy means of amide type is considerable.
Overdose:
System toxic reactions are mainly shown in work to the central nervous system (CNS) and in cardiovascular system. Similar reactions arise because of high concentration of drug in blood and at accidental overdose of an intra vascular injection, or at especially bystry absorption of a medicine from areas with good blood circulation. Reactions of TsNS are similar at all anesthetics of amide type of long action, and reactions from cardiovascular system more depend on properties of the entered medicine.
Central nervous system. Toxic influence of drug on TsNS is shown by gradual increase in symptoms. The first symptoms are paresthesia around a mouth and numbness of language, an oglushennost, a sharpening of hearing, a sonitus and deterioration in sight. More serious violations are shown in the form of a dysarthtia, a tremor of muscles which appears before spasms. These side effects cannot be mixed with neurotic behavior. Further there can come the loss of consciousness and a big epileptic seizure which can last from several seconds to several minutes. After spasms quickly there comes the hypoxia and a hypercapnia because of the strengthened muscle work. Therefore breath is broken and there is an impassability of respiratory tracts. In hard cases the apnoea is possible. Acidosis, a hypopotassemia and a hypoxia increase toxic reaction even more.
Reduction of toxic reaction depends on the speed of redistribution of medicine from TsNS, and also on his metabolism.
In case of spasms therapy is necessary. The treatment purpose – to provide oxygen access, to stop spasms and to support blood supply. If spasms spontaneously do not stop within 15-20 seconds, in/in 100-150 mg of thiopental ili5-10 are entered by diazepam mg.
Cardiovascular system. Toxic reactions from cardiovascular system can be observed only in hard cases of overdose of medicine. Prodromal symptoms of TsNS can remain unnoticed if the patient is hard paralyzed by sedative medicines or is under the general anesthesia. Toxic reactions are shown in the form of hypotension, bradycardia, arrhythmia, and even the cardiac standstill is possible.
If observe dangerous oppression of cardiovascular system (hypotension, bradycardia), in/in enter 5-10 mg of ephedrine and, in case of need, repeat administration of ephedrine in 2-3 minutes. In case of a blood circulation stop immediately begin kardiopulmonarny resuscitation.
Storage conditions:
Not to freeze. To store in places unavailable to children at a temperature of 25 degrees Celsius.
Issue conditions:
According to the recipe
Packaging:
Ampoules on 4 ml from colourless glass of a hydrolytic class No. 1 with the line or a point of a break. On 5 ampoules in a strip packaging from a PVC film without covering. On 1 strip packaging in a cardboard box.
