Lidocaine injections 20mg/ml 2ml #10

Instruction for Lidocaine injections

You can buy Lidocaine injections on this page

Composition

One ampoule contains:
active ingredient: lidocaine hydrochloride 40 mg in 2 ml or 50 mg in 5 ml of solution;
excipients: sodium chloride, solution of sodium hydroxide 1 M (up to pH 5.0-7.0), water for injection.

Pharmacokinetics

When administered parenterally, the degree of absorption depends on the site of administration and dose. When administered intravenously, the maximum concentration of lidocaine in the blood plasma is created in 3-5 minutes, with intramuscular - in 5-15 minutes. Communication with plasma proteins - 50 - 80%. Distributed quickly (T1 / 2 distribution phase - 6-9 min). It first enters well-supplied blood tissues (heart, lungs, brain, liver, spleen), then into adipose and muscle tissues. It penetrates the blood-brain barrier, the placental barrier and into breast milk (40% of the concentration in the mother's plasma).
Metabolized in the liver (90-95%) with the participation of microsomal enzymes by deamination with the formation of active metabolites (monoethylglycine and glycinexidine), T1 / 2 of which is 2 hours and 10 hours, respectively. In diseases of the liver, the metabolic rate decreases and ranges from 50% to 10% of the normal value.
The elimination half-life after intravenous bolus administration is 1.5-2 hours, in newborns it is 3 hours, with prolonged intravenous infusions up to 3 hours or more. With abnormal liver function, the half-life may increase by 2 times or more.
Excreted in the bile and kidneys (up to 10% unchanged). In chronic renal failure, accumulation of metabolites is possible. Acidification of urine increases injections lidocaine clearance.

Pharmacodynamics

Lidocaine injections are an amide-type anesthetic. It has a local anesthetic effect, stabilizing the membranes of neurons, reducing their permeability to sodium ions, which prevents the generation and conduction of nerve impulses. A similar effect is observed on the excitable membranes of the cells of the heart muscle and brain. Lidocaine is characterized by rapid onset of action, high anesthetic activity and low toxicity. In lower concentrations, lidocaine has less effect on motor nerve fibers. When applied topically expands blood vessels, does not irritate the tissue.

Indications for use

- local anesthesia (terminal, infiltration, conduction) in surgery, ophthalmology, dentistry, otolaryngology
- blockade of peripheral nerves and nerve nodes

Dosage and administration

Before using injections lidocaine, it is imperative to carry out a skin test for an increased individual sensitivity to the drug, which is indicated by edema and redness of the injection site.
For anesthesia, the amount of the drug and the total dose depends on the type of anesthesia and the nature of the surgery.
In case of infiltration anesthesia, up to 30 ml of solution with a concentration of 10 mg / ml (1%) is used.
For conduction anesthesia, solutions with a concentration of 10 mg / ml (1%) and 20 mg / ml (2%) are used; The maximum total dose is up to 400 mg (40 ml of 1% solution and 20 ml of 2% lidocaine solution).
In dental practice, use 1 - 5 ml (20 - 100 mg) 2% solution; with intercostal nerve blockade, 3-5 ml (30-50 mg) of a 1% solution; in case of paracervical anesthesia - 10 ml (100 mg) of a 1% solution in each direction (repeated administration is possible not less than 1.5 hours later); with the blockade of Oberst-Lukashevich - 2 - 3 ml of 2% solution.
Vagosympathetic blockade: cervical - 5 ml (50 mg) of 1% solution, lumbar block - 5 to 10 ml (50 - 100 mg) of 1% solution.
Epidural anesthesia - 200 - 300 mg (10-15 ml) of a 2% lidocaine solution is used. It is not recommended to use continuous introduction of anesthetic with the help of a catheter; maximum dose should not be repeated more than 90 minutes.
For anesthesia of the mucous membranes (with tracheal intubation, bronchoesophagoscopy, fibrogastroduodenoscopy, removal of polyps, punctures of the maxillary sinus, etc.) use a 2% solution in a volume of not more than 20 ml. The duration of anesthesia is 15-30 minutes.
In ophthalmology: 2 drops of a 2% solution are instilled into the conjunctival sac 2 to 3 times with an interval of 30 to 60 seconds immediately before surgery or examination.
The maximum dose for adults is no more than 4.5 mg / kg or 300 mg.
To lengthen the action of lidocaine injections, it is possible to add an ex tempore 0.1% solution of adrenaline (1 drop per 5-10 ml of lidocaine solution, but not more than 5 drops). The maximum permissible dose of lidocaine is increased to 500 mg.
Note: after intravenous administration, lidocaine has a short duration of action (lasting 15-20 minutes). If intravenous infusion is not available by drip infusion, after immediate initial intravenous administration, 50–100 mg can be repeated if necessary once or twice with an interval of at least 10 minutes.
To prepare an infusion solution, 1 g or 2 g of lidocaine is added to 1 l of 5% dextrose solution for injection and a solution of lidocaine is obtained at a concentration of 1 mg / ml or 2 mg / ml.
In elderly patients, a dose reduction is recommended, especially with prolonged intravenous infusion. In chronic renal failure, dose adjustment is not required. In diseases of the liver (cirrhosis, hepatitis) and in patients with reduced hepatic blood flow (for example, against the background of chronic heart failure), the dose should be reduced by 40-50%.

Attention!

With rapid intravenous administration, a sharp decrease in blood pressure can occur and collapse develops. In these cases, phenylephrine, ephedrine and other vasoconstrictor agents are used.
1% lidocaine solution is used as a solvent for the preparation of injection solutions for the intramuscular injection of -lactam antibiotics of the cephalosporins group at the rate of 3 ml of lidocaine per vial containing 1.0 g of antibiotic.

Side effects

Nervous system disorders:
often - paresthesia, dizziness;
infrequently, signs of systemic neurotoxicity (convulsions, paresthesia around the mouth, numbness of the tongue, tremor, delirium, drowsiness, dysarthria, loss of consciousness), rarely - neuropathy, damage to peripheral nerves, arachnoiditis.
Violations by the organ of vision:
rarely - diplopia (double vision).
Heart disorders:
often - bradycardia;
rarely - arrhythmia, cardiac arrest.
Vascular disorders:
very often hypotension;
often - hypertension.
Disorders of the respiratory system, chest and mediastinal organs:
rarely - respiratory failure, depression and respiratory arrest.
Immune system disorders:
rarely - allergic reactions (urticaria, skin rashes, angioedema, in more severe cases - anaphylactic shock).
Disorders of the gastrointestinal tract:
very often nausea;
often - vomiting.

Contraindications

- hypersensitivity to any of the components of the drug or other amide local anesthetic drugs in history
- sick sinus syndrome (especially in elderly patients), a significant reduction in left ventricular function
- Wolff-Parkinson-White syndrome
- heart block: atrioventricular stage II - III (with the exception of cases when a probe for stimulation of the ventricles is inserted), intraventricular; sinus atrial
- intraventricular conduction disorders
- cardiogenic shock
- retrobulbar injection (especially for patients with glaucoma)
- porphyria
- Morgagni-Adams-Stokes syndrome
- for anesthesia in obstetric practice - violations of intrauterine development of the fetus, placental insufficiency, prematurity, delayed exposure, preeclampsia
- for epidural anesthesia - severe hypotension, cardiogenic shock and hypovolemic shock, neurological diseases, septicemia, inability to perform puncture due to spinal deformity
- for subarachnoid anesthesia - back pain, brain infections, benign and malignant neoplasms of the brain, coagulopathy of various genesis, migraine, subarachnoid hemorrhage, arterial hypertension and hypotension, paresthesia, psychosis, hysteria, non-contact insanity, hypotension, non-contact hypertension and hypotension, paresthesia, psychosis, hysteria, noncontact sufferance spine
- epileptiform convulsions in the previous application of lidocaine injections (in history)
- children's and teenage age up to 18 years
With care: in severe heart failure, severe hepatic and / or renal failure, in debilitated patients, in hypovolemia, AV block, sinus bradycardia, hypotension, severe myasthenia, pregnancy and lactation.

Drug interactions

Joint appointment with beta-blockers increases the risk of bradycardia and toxic effects of lidocaine injections.
Cimetidine and propranolol reduce hepatic clearance of lidocaine injections (reduced metabolism due to inhibition of microsomal oxidation and reduced hepatic blood flow) and increase the risk of toxic effects.
Barbiturates, phenytoin, rifampicin (inducers of liver microsomal enzymes) reduce efficacy (may require an increase in dose).
When administered with amamalin, phenytoin, verapamil, quinidine, amiodarone, the negative inotropic effect may be enhanced.
Cardiac glycosides weaken the cardiotonic effect, while curative drugs enhance muscle relaxation.
Procainamide increases the risk of developing excitation of the central nervous system, hallucinations.
With the simultaneous appointment of lidocaine injections, barbiturates, other hypnotic and sedative drugs may increase their inhibitory effects on the central nervous system.
Under the influence of monoamine oxidase inhibitors, it is possible to enhance the local anesthetic effect of lidocaine injections. Patients taking monoamine oxidase inhibitors should not be given parenteral injections lidocaine.
With simultaneous use of lidocaine injections and polymyxin B, it is possible to increase the inhibitory effect on neuromuscular transmission (monitoring of respiratory functions is necessary).

Pharmaceutical incompatibility

Lidocaine injections are precipitated when mixed with amphotericin, methohexitone or sulfadiazine. Depending on the pH of the solution, lidocaine injections may be incompatible with ampicillin.

special instructions

Regional and local anesthesia should be carried out by experienced professionals in an appropriately equipped room with the availability of ready-for-use equipment and preparations needed for cardiac monitoring and resuscitation. Anesthesia personnel must be qualified and trained in anesthesia techniques, must be familiar with the diagnosis and treatment of systemic toxic reactions, adverse events and reactions, and other complications.
In patients with acute myocardial infarction, administration of lidocaine injections may increase the risk of death by increasing the incidence of asystole. Intramuscular injections of lidocaine injections can increase the activity of creatinine phosphokinase, which can make it difficult to diagnose myocardial infarction. It is not recommended to use lidocaine with supraventricular arrhythmias (due to inefficiency and the risk of increased ventricular contractions - with atrial flutter and atrial fibrillation).
The introduction of lidocaine injections requires special care and dose reduction in cases of circulatory failure, hypotension, hypovolemia, hypokalemia, impaired liver function and / or kidneys. Before using injections lidocaine, potassium levels in plasma should be normalized.
Epidural anesthesia can lead to hypotension and bradycardia, this risk can be reduced by prior administration of colloid and crystalloid solutions. Paracervical blockade can cause bradycardia or fetal tachycardia, in connection with which monitoring of its cardiac activity is necessary.
Special care should be taken when administering the drug to elderly patients.
Patients predisposed to malignant hypertension require special attention, since they may be resistant to amide local anesthetics.
When retrobulbar injection lidocaine rarely reaches the subarachnoid space, causing serious adverse reactions, including cardiovascular failure, apnea, convulsions and temporary blindness. It is forbidden to inject lidocaine solutions in retrobulbar patients with glaucoma.
Lidocaine should be carefully injected into highly vascularized tissues to avoid intravasal ingestion of the drug. With the introduction of vascularized tissue is recommended aspiration test. Accidental injection of the drug into the artery of the head and neck can lead to the appearance of cerebral symptomatology. With rapid intravenous administration, blood pressure can dramatically decrease and collapse develops.
Alcohol abuse enhances the depressant effect of lidocaine on breathing.
MAO inhibitors must be discontinued at least 10 days prior to planned subarachnoid anesthesia with lidocaine injections.

Pregnancy and lactation

Lidocaine injections passes through the placental barrier, in connection with which during pregnancy (especially in the first trimester) its purpose is not recommended, only after a thorough analysis of the benefit / risk. A small amount of lidocaine can be excreted into breast milk, so when prescribing lidocaine, breastfeeding should be stopped.
Use in pediatrics. There is no data on the use of the drug in pediatric practice, and therefore, its use in children is not recommended.
Features the influence of the drug on the ability to drive vehicles and potentially dangerous machinery.
During the period of treatment, it is not recommended to control the transport and work with mechanisms that require concentration of attention and quickness of psychomotor reactions.

Overdose

Symptoms: initial signs of intoxication - dizziness, nausea, vomiting, euphoria, asthenia, low blood pressure; then - convulsions of the facial muscles of the face, tonic-clonic convulsions of skeletal muscles, psychomotor agitation, bradycardia, collapse; when used in childbirth in a newborn - bradycardia, depression of the respiratory center, respiratory arrest.
Treatment: when the first signs of intoxication appear, the administration is stopped, the patient is transferred to the horizontal position; spend inhalation of oxygen. For convulsions, intravenous administration of diazepam is indicated, for bradycardia, m-anticholinergics (atropine), vasoconstrictors (norepinephrine, phenylephrine) are indicated. If necessary, conduct intubation, artificial respiration, resuscitation. Dialysis is not effective.

Release form and packaging

On 5 ml or on 2 ml in ampoules from glass.
10 ampoules with a knife or scarifier for opening ampoules in a cardboard box with corrugated liner made of corrugated paper.
The boxes together with instructions for medical use in the state and Russian languages ​​are packaged in group packaging.
The number of instructions for medical use in the state and Russian languages ​​should correspond to the number of packages.
10 ampoules of 2 ml each or 5 ampoules of 5 ml each are placed in a polyvinyl chloride film insert. 1 liner with 10 ampoules or 2 liners with 5 ampoules with a knife or scarifier for opening ampoules and instructions for medical use in the state and Russian languages ​​are placed in a pack of cardboard.
10 ampoules with a knife or scarifier for opening ampoules and instructions for medical use in the state and Russian languages ​​are placed in a pack of cardboard with a cardboard insert for fixing the ampoules.
In the case of using ampoules with a fracture ring or with a notch and a break point, the attachment of a knife for opening ampoules is not provided.

Storage conditions

Store in a dark place at a temperature not higher than 25 ° C.
Keep out of the reach of children!
Shelf life - 2 years
Do not use after expiration date.

Terms of sell

You can buy Lidocaine injections without a prescription.