Bupivacaine Grindeks Spinal - instructions for use, dose, side effects, contraindications

Excipients: sodium chloride - 8.0 mg, 0.1 M sodium hydroxide solution or 0.1 M hydrochloric acid solution to pH 4.0-6.5, water for injection up to 1 ml.

Description:

A clear, colorless liquid.

Pharmacotherapeutic group:Local anesthetic

ATX: & nbsp

N.01.B.B.01 Bupivacaine

Pharmacodynamics:

Bupivacaine is a long-acting anesthetic, an amide type, 4 times more potent than lidocaine. Reversibly blocks the impulse on the nerve fiber due to the effect on the sodium channels, has an antihypertensive effect, slows the heart rate. With intrathecal injection, the effect occurs quickly, and its duration varies from medium to long. The duration of the effect depends on the dose.

Solution Bupivacaine Grindeks Spinal is isobaric.

Pharmacokinetics:

Bupivacaine is well soluble in lipids with a partition coefficient between oil and water equal to 27.5.

Bupivacaine is completely absorbed from the subarachnoid space into two phases with a half-life of 50-400 minutes. Slow absorption is the limiting factor in the elimination of bupivacaine, which explains its longer half-life than with intravenous administration.

Absorption from the subarachnoid space is slow, which, combined with the administration of a low dose required for spinal anesthesia, results in a relatively low maximum plasma concentration (0.4 mg / L for every 100 mg administered).

Indications:

Spinal anesthesia during surgical operations on the lower extremities, including operations on the hip joint, lasting 3-4 hours and not requiring a pronounced motor block.

Contraindications:

- Hypersensitivity to any of the components of the drug or to other local anesthetics of the amide type;

- severe arterial hypotension (cardiogenic or hypovolemic shock).

Conditions that are contraindications to intrathecal anesthesia:

- diseases of the central nervous system (CNS) (eg, meningitis, tumors, poliomyelitis, intracranial hemorrhage);

- purulent skin infections at or near the lumbar puncture;

- spinal stenosis, active diseases (eg, spondylitis, tumors, tuberculosis) or trauma (for example, fracture) of the spine;

- sepsis, subacute combined degeneration of the spinal cord due to pernicious anemia and tumors of the brain and spinal cord;

- cardiogenic or hypovolemic shock;

- a clotting disorder or active anticoagulant therapy.

Carefully:

Cardiovascular failure (possibly progressing), heart block,inflammatory diseases or infection of the injection site (with infiltration anesthesia), cholinesterase deficiency, kidney failure, advanced age (over 65 years), late pregnancy (III (for example, chronic heart failure, liver diseases), simultaneous administration of antiarrhythmic agents (including beta-blockers ), children's age (1-12 years).

Bupivacaine should be used with caution in patients receiving other local anesthetics or preparations structurally similar to local anesthetic agents of the amide type, such as antiarrhythmics (eg, lidocaine, mexiletine).

Pregnancy and lactation:

Data on adverse effects on pregnancy are absent. When used in pregnant animals in large doses, a decrease in the survival of offspring in rats and embryological effects in rabbits were observed. Concerning bupivacaine should not be used in the early stages of pregnancy, unless the benefits exceed the risks.

In late pregnancy, the dose should be reduced (see section "Special instructions"),

Bupivacaine penetrates into breast milk, but when applied in therapeutic doses, the effect on the baby is negligible.

Dosing and Administration:

Use bupivacaine can only doctors who have experience in conducting local anesthesia or under their supervision.

To achieve the required degree of anesthesia, the minimum possible dose should be administered.

The following doses are for adults. Selection of the dose is carried out individually.

Elderly patients and patients in late pregnancy, the dose should be reduced.

Indications for use

Dose

Start actions

Duration actions

Surgical operations on the lower extremities, including operations on the hip joint

2-4 ml

10-20 mg

5-8 min

1,5-4 hours

The recommended injection site is at the level of L3.

Clinical experience with a dose exceeding 20 mg is not available. Prior to the administration of the drug, intravenous access should be provided.

The introduction is carried out only after confirmation of entry into the subarachnoid space (the flow out of the needle of the transparent cerebrospinal fluid or during aspiration).If an unsuccessful attempt is made, only one additional attempt should be made at a different level and less. One of the reasons for the lack of effect can be a poor distribution of the drug in the subarachnoid space, which can be corrected by changing the patient's position.

Children with body weight less than 40 kg

BUPIVACAIN GREENDEX SPINAL is allowed to be used in children.

The main difference between adults and children is that in newborns and infants the volume of cerebrospinal fluid is greater, that to achieve the same degree of blockade requires a relatively high dose per kilogram of body weight compared to adults.

Regional anesthesia should be performed by a doctor who has experience working with children and who has the appropriate technique of administration.

Doses in children, given in the table, are indicative. Variability is possible. In determining the methods of anesthesia and taking into account the individual characteristics of patients should use the generally accepted guidelines for anesthesia. It is necessary to enter the minimum dose necessary to achieve sufficient anesthesia.

Body weight, kg	Dose, mg / kg
<5	0,4-0,5
5-15	0,3-0,4
15-40	0,25-0,3

Side effects:

The frequency of unwanted reactions is determined by the following categories: very frequent (> 1/10), frequent (≥1 / 100, <1/10), infrequent (≥1 / 1,000, <1/100), rare (≥1 / 10 000, <1/1 000), very rare (<1/10 000).

Very Frequent

(≥1/10)

From the gastrointestinal tract (GIT): nausea.

From the side of the cardiovascular system: lowering blood pressure, bradycardia.

Frequent

(≥1/100, <1/10)

From the nervous system: headache after puncture of the dura mater.

From the digestive tract: vomiting.

From the genitourinary system: urinary retention, urinary incontinence.

Infrequent

(≥1/1 000 , <1/100)

From the nervous system: paresthesia, paresis, dysesthesia.

From the side of skeletal muscles, connective tissue and bones: muscle weakness, back pain.

Rare

(≥1/10 000, <1/1 000)

From the cardiovascular system: heart failure.

From the immune system: allergic reactions, anaphylactic shock.

From the nervous system: complete unintentional spinal block, paraplegia, paralysis, neuropathy, arachnoiditis.

From the respiratory system: respiratory depression.

Undesirable reactions in children are similar to those in adults, however, early signs of local anesthetic toxicity in children are more difficult to recognize if the blockade is performed under sedation or anesthesia.

Overdose:

Acute systemic intoxication

Symptoms

Toxic reactions are manifested mainly from the central nervous and cardiovascular systems. They arise due to the high concentration of local anesthetic in the blood, which can be caused by accidental intravascular injection, overdose or extremely fast absorption from the area of highly vascularized tissues (see section "Special instructions").

Symptoms of CNS damage for all local anesthetics of the amide type are similar, whereas the symptoms of cardiovascular damage differ qualitatively and quantitatively.

Unintentional intravascular injection of a local anesthetic can lead to immediate systemic toxic reactions (within a few seconds-minutes). Signs of systemic toxicity in case of an overdose appear later (15-60 minutes after administration), as the concentration of local anesthetic in the blood plasma increases slowly.

From the central nervous system

Intoxication of the central nervous system manifests itself gradually. The initial signs of intoxication, as a rule, are: dizziness, paresthesia around the mouth, numbness of the tongue, hyperacusis, tinnitus and visual impairment.More serious manifestations are dysarthria and myofasciculation, which may precede the onset of generalized seizures. These phenomena should not be mistaken for a neurotic disorder. Following them, loss of consciousness and the development of a large convulsive fit lasting from a few seconds to several minutes are possible. In connection with increased muscular activity and insufficient ventilation (disruption of the normal breathing process), hypoxia and hypercapnia rapidly build up during seizures. In severe cases, breathing may stop. Concomitant acidosis increases the toxic effect of local anesthetics.

The resolution of symptoms is due to the metabolism of the local anesthetic and its redistribution from the central nervous system. The described phenomena quickly stop, if the overdose was not excessive.

From the side of the cardiovascular system

The defeat of the cardiovascular system, as a rule, indicates more severe intoxication. It is usually preceded by signs of central nervous system damage that can be erased if the patient is in anesthesia or deep sedation caused by drugs such as benzodiazepines or barbiturates.Due to the high concentration of local anesthetics in blood plasma, there may be a drop in blood pressure, bradycardia, arrhythmias and cardiac arrest.

Toxic manifestations of the cardiovascular system are often caused by myocardial depression and myocardial conduction disturbance, which cause a decrease in cardiac output, lowering of arterial pressure, atrioventricular blockade (AV blockade), bradycardia, ventricular arrhythmia, including ventricular tachycardia and ventricular fibrillation, cardiac arrest. These phenomena are often preceded by severe signs of CNS involvement, including convulsions, but in rare cases, cardiac arrest occurs without concomitant signs from the CNS. After a very rapid intravenous injection, the concentration of bupivacaine in the blood plasma can be quite high. In this case, he quickly reaches the coronary arteries, and the symptoms of circulatory disorders occur earlier than signs of CNS damage. This mechanism causes myocardial depression and may be the first manifestation of intoxication.

When the blockade is performed under general anesthesia in children, the early signs of intoxication are difficult to detect, and careful monitoring is therefore required.

Treatment

If a spinal block arises, adequate ventilation should be provided (ensure airway patency, oxygen supply, if necessary, intubation and artificial ventilation). With a decrease in blood pressure and / or bradycardia, it is necessary to introduce a vasopressor with an inotropic effect.

When symptoms of acute systemic intoxication appear, the administration of the drug should be stopped immediately. It is necessary to ensure proper ventilation, oxygenation and maintain blood circulation.

In all cases, it is necessary to adjust the supply of oxygen, if necessary, intubation and controlled ventilation (in some cases with hyperventilation). When convulsions are injected diazepam, with bradycardia - atropine. With circulatory failure - dobutamine intravenously, the administration of norepinephrine is allowed (starting from 0.05 μg / kg / min, if necessary, the dose is increased by 0.05 μg / kg / min every 10 minutes), in more severe cases, the dose is titrated according to the results of monitoring hemodynamics. The administration of ephedrine is possible. With severe damage to the cardiovascular system, resuscitation can continue for several hours. Any acidosis is subject to elimination.

When cupping systemic intoxication in children, the dose of the drug should be selected according to their age and body weight.

Interaction:

Caution should be exercised while using bupivacaine with other local anesthetics or antiarrhythmics Ib class, since they can enhance the toxic effects of each other.

A separate study of the interaction of local anesthetics and antiarrhythmic drugs of the third class (for example, amiodarone) was not carried out, nevertheless, it is advisable to use caution when using them simultaneously (see section "Special instructions").

The alkalinization can lead to precipitation, since the solubility of bupivacaine at pH> 6.5 decreases.

When preparing for the introduction, it is necessary to avoid prolonged contact of the drug with metal objects, since metal ions can cause reactions at the site of administration, manifested by soreness and edema.

Special instructions:

Spinal anesthesia can cause severe blockade and paralysis of the intercostal muscles and diaphragm, especially in pregnant women.

Care should be taken in patients with AV blockade II and III degree, as local anesthetics can disrupt intracardiac patency.

Care should be taken when administering the drug to elderly patients and patients with severe liver disease, severe renal failure, or a general unsatisfactory condition.

It is necessary to carry out careful monitoring and continuous ECG monitoring in patients receiving Class III antiarrhythmic drugs (for example, amiodarone), since the summation of their cardiovascular effects with those of bupivacaine is possible.

Like other local anesthetics, bupivacaine can cause acute toxic reactions from the central nervous and cardiovascular systems, if during the procedure of local anesthesia there is a high concentration in the blood. Most often this is manifested in the case of unintentional intravascular injection or with a good blood supply to the site of administration.

Against the background of a high concentration of bupivacaine in the plasma, cases of ventricular arrhythmia, ventricular fibrillation, sudden cardiovascular collapse and death were documented.At the same time, the doses used for spinal anesthesia, as a rule, do not lead to the achievement of a high systemic concentration.

A rare but serious unwanted reaction to spinal anesthesia is a high or complete spinal block, leading to cardiovascular and respiratory depression. The oppression of the cardiovascular system, caused by extensive sympathetic blockade, can lead to arterial hypotension and bradycardia, or even cardiac arrest.

Inhibition of respiration may be due to blockade of the innervation of the respiratory muscles, including the diaphragm.

In elderly patients and patients in late pregnancy, the risk of a high or complete spinal block, leading to oppression of blood circulation and respiration, is increased. These patients should lower the dose.

Spinal anesthesia can lead to lower blood pressure and bradycardia. This risk can be reduced by the introduction of crystalloid solutions. With a decrease in blood pressure, it must immediately be quenched, for example, by intravenous administration of 5-10 mg of ephedrine.

Neurological complications are a rare consequence of spinal anesthesia and can lead to paresthesia, anesthesia,muscle weakness and paralysis. In some cases, these complications are permanent.

Care must be taken in patients with multiple sclerosis, hemiplegia, paraplegia and neuromuscular disorders. Before the start of treatment, the benefits and risks for the patient should be correlated.

Effect on the ability to drive transp. cf. and fur:

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Solution for intrathecal administration, 5 mg / ml.

Packaging:

For 4 ml in an ampoule of colorless glass of hydrolytic class No. 1 with a line or break point, as well as two marking rings of blue color (for the manufacturer HS MB Pharma sr.o.).

5 ampoules per cell pack of PVC film without coating (pallet). One cell pack together with the instruction for use is placed in a pack of cardboard.

Storage conditions:

Store at a temperature not exceeding 25 ° C. Do not freeze.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-006092/10

Date of registration:29.06.2010 / 17.10.2016

Expiration Date:Unlimited

The owner of the registration certificate:GRINDEX, JSC GRINDEX, JSC Latvia

Manufacturer: & nbsp

HBM PHARMA, s.r.o. The Slovak Republic

Santonika, UAB Lithuania

Representation: & nbspGrindeks Rus, Open CompanyGrindeks Rus, Open CompanyRussia

Information update date: & nbsp20.04.2017

Illustrated instructions

Instructions

Bupivacaine Grindeks Spinal (Bupivacaine Grindeks Spinal)