Lidocaine, 100 mg/ml 2 ml 10 pcs
Anesthetic effect of lidocaine is 2-6 times stronger than procaine (effect is faster and longer – up to 75 minutes, and after adding epinephrine – more than 2 hours). When applied topically, it dilates blood vessels and has no local irritant effect on tissues.
During parenteral administration the degree of absorption depends on the site of administration and the dose. At a concentration of 20 mg/ml intravenous is not used. Time to reach maximum concentration (Tcmax) in epidural injection is less than 30 minutes.
Binding with plasma proteins is 50-80 %. It is administered quickly (half-life period of distribution phase is 6-9 minutes). Firstly the drug enters into well supplied with blood tissues (heart, lungs, brain, liver, spleen), then into fat and muscle tissues. It penetrates through the blood-brain barrier (BBB), placental barrier and is secreted with breast milk (40 % of concentration in mother’s plasma).
Metabolized in liver (90-95 %) with microsomal enzymes by dealkylation of amino group and breaking the amide bond to form active metabolites (monoethylglycystylidine and glycystylidine) with half-life (T1/2) of 2 and 10 hours, respectively. Metabolism intensity decreases and makes 50 % to 10 % of the normal value if liver function is disturbed.
It is eliminated in the bile (part of the dose is reabsorbed in the gastrointestinal tract) and the kidneys (up to 10 % unchanged). Cumulation of metabolites is possible in chronic renal failure. Urine acidification increases lidocaine excretion.
– local infiltration anesthesia;
– conduction anesthesia (including retrobulbar, parabulbar);
– spinal anesthesia;
– epidural anesthesia.
How to take, the dosage
The amount of lidocaine solution and the total dose depends on the type of anesthesia, the nature and duration of the surgical intervention.
The method of diluting 20 mg/ml (2%) lidocaine solution to obtain the desired solution concentration:
To prepare 10 mg/mL (1%) lidocaine solution, take 1 part 20 mg/mL lidocaine solution and 1 part water for injection, that is, mix 2 mL 20 mg/mL lidocaine solution with 2 mL water for injection (for a 2-mL ampoule), or mix 5 mL 20 mg/mL lidocaine solution with 5 mL water for injection (for a 5-mL ampoule).
To prepare 5 mg/ml (0.5%) lidocaine solution, use 1 part 20 mg/ml lidocaine solution and 3 parts water for injection, i.e. mix 2 ml 20 mg/ml lidocaine solution with 6 ml water for injection (for 2 ml ampoule), or mix 5 ml 20 mg/ml lidocaine solution with 15 ml water for injection (for 5 ml ampoule).
To prepare 2.5 mg/ml (0.25%) lidocaine solution, take 1 part 20 mg/ml lidocaine solution and 7 parts water for injection, i.e. Mix 2 ml of 20 mg/ml lidocaine solution with 14 ml of water of injection (for 2 ml ampoule), or mix 5 ml of 20 mg/ml lidocaine solution with 35 ml of water of injection (for 5 ml ampoule).
To prepare 1.25 mg/ml (0.125%) lidocaine solution, take 1 part 20 mg/ml lidocaine solution and 15 parts water for injection, i.e. Mix 2 ml of 20 mg/ml lidocaine solution with 30 ml of water of injection (for 2 ml ampoule), or mix 5 ml of 20 mg/ml lidocaine solution with 75 ml of water of injection (for 5 ml ampoule).
For infiltration anesthesia (intradermal, subcutaneous) 0.125%, 0.25%, 0.5% solutions are used; to achieve infiltration anesthesia up to 60 ml (5-300 mg) of 0.5% solution or up to 30 ml of 1% solution is used.
For peripheral nerve conduction anesthesia (anesthesia of peripheral nerves including plexus blockade) 1% and 2% solutions are used; the maximum total dose is up to 400 mg (40 ml of 1% solution or 20 ml of 2% solution). For plexus blockade 10-20 ml of 1% solution or 5-10 ml of 2% solution.
For peripheral nerve conduction anesthesia: brachial – 15-20 ml (225-300 mg) 1.5% solution; in dental practice – 1-5 ml (20-100 mg) 2% solution; intercostal nerve blockade – 3 ml (30 mg) 1% solution.
For paracervical anesthesia: 10 ml (100 mg) of 1% solution in each side, if necessary, it is possible to reintroduce at least 1.5 hours later.
For paravertebral anaesthesia: 3 to 5 ml (30-50 mg) of 1% solution. Retrobulbar anesthesia: 3.0 to 4.0 (60-80 mg) 2% solution.
Parabulbar anesthesia – 1.0-2.0 (20-40 mg) 2% solution. Vagosympathetic blockade: cervical (stellate node) – 5 ml (50 mg) of 1% solution, lumbar – 5-10 ml (50-100 mg) of 1% solution.
Spinal anesthesia – 3.0-4.0 ml (60-80 mg) of 2% solution.
Epidural anesthesia – 25-30 ml (250-300 mg) of 1% solution is used to obtain analgesia; 15-20 ml (225-300 mg) of 1.5% solution or 10-15 ml (200-300 mg) of 2% solution to obtain anesthesia; 20-30 ml (200-300 mg) of 1% solution is used for thoracic epidural anesthesia. Continuous administration of the anesthetic with a catheter is not recommended; the maximum dose should not be repeated more often than 90 minutes.
When using caudal anesthesia: in surgical practice, 15-20 ml (225-300 mg) of 1.5% solution. Continuous administration of the anesthetic with a catheter is not recommended; the maximum dose should not be repeated more often than 90 min later. Recommended doses in children for neuromuscular blockade are up to 4.5 mg/ml 0.25-1.0% solution.
The maximum dose for children is 4.5 mg/kg, but no more than 100 mg; the maximum dose for adults is no more than 4.5 mg/kg or 300 mg. These doses must be repeated within 24 hours.
The effect of lidocaine may be prolonged by adding 0.1% epinephrine solution (0.1 ml per 20 ml lidocaine). In this case, in regional anesthesia the dose of lidocaine may be increased to 600 mg.
Polymer ampoule procedure:
1.Take the ampoule and shake it, holding it by the neck.
2.Squeeze the ampoule with your hand, taking care not to release the product, and with a twisting motion, turn and separate the valve.
3.Through the hole that is created, immediately connect the syringe to the ampoule.
4. Turn the ampoule over and slowly draw the contents into the syringe.
5. Slide the needle onto the syringe.
Vasoconstrictors (epinephrine, methoxamine, phenylephrine) prolong the local anesthetic effect.
Cimetidine reduces hepatic clearance of lidocaine (reduced metabolism due to inhibition of microsomal oxidation) and increases the risk of toxic effects.
Reduces the effect of antimyasthenic drugs. When treating the injection site of local anesthetic with disinfectant solutions containing heavy metals, the risk of a local reaction in the form of pain and swelling increases.
When using local anesthetic drugs for spinal and epidural anesthesia with guanadrel, guanethidine, mecamylamine, trimethophane camsylate the risk of severe hypotension and bradycardia increases.
Beta-andrenoblockers slow the metabolism of lidocaine, increasing its toxicity (decreased hepatic blood flow). Cardiac glycosides weaken the cardiotonic effect. It enhances and prolongs the effect of myorelaxing drugs. Simultaneous administration of lidocaine and hypnotics and sedatives may increase their depressant effect on the central nervous system.
When combined with narcotic analgesics an additive effect is developed that is used during epidural anesthesia, but respiratory depression increases.
Use with monoamine oxidase inhibitors (furazolidone, procarbazine, selegiline) increases the risk of decreased blood pressure.
Anticoagulants (including Sodium ardeparin, sodium dalteparin, sodium danaparoid, sodium enoxaparin, sodium heparin, warfarin and others) increase the risk of bleeding.
Does not reduce the antimicrobial activity of sulfonamides (PABA (paraaminobenzoic acid) is not metabolized).
The use of lidocaine, injection solution (2%), as an antiarrhythmic agent is inadmissible.
Particular caution should be exercised during local anesthesia of organs rich in blood vessels; intravascular injection during administration should be avoided. An aspiration test is recommended when injecting into vascularized tissues. Monoamine oxidase inhibitors (MAOIs) should be discontinued at least 10 days before planning subarachnoid anesthesia with lidocaine.
A rapid intravenous injection may result in a sharp decrease in blood pressure and collapse. In these cases, phenylephrine, ephedrine and other vasoconstrictors are used.
During treatment, caution should be exercised when driving motor vehicles and engaging in other potentially hazardous activities that require increased concentration and rapid psychomotor reactions.
– history of hypersensitivity to other amide local anesthetic drugs;
– Infection of the intended injection site;
– Syndrome of weak sinus node;
– Grade II-III atrioventricular block (except for cases when an artificial pacemaker is installed);
– sinoauricular block;
– Wolf-Parkinson-White syndrome (WPW syndrome);
– cardiogenic shock;
– intraventricular conduction disorders;
Chronic heart failure of New York Heart Association (NYHA) functional class II-III, severe hepatic failure, severe renal failure, hypovolemia, grade I atrioventricular block, sinus bradycardia, arterial hypotension, Severe myasthenia, history of epileptiform convulsions (including those caused by lidocaine), children under 12 years of age (due to slow metabolism drug accumulation is possible), critically ill and frail patients, elderly (over 65), local anesthesia in areas with rich blood vessels.
For spinal (subarachnoid) and epidural anesthesia – diseases of the central nervous system (CNS) (including infections, tumors), the presence of blood in the cerebrospinal fluid, parasthesias, psychosis, spinal deformity, peripheral neuropathy, aortic stenosis, antiplatelet therapy (including acetylsalicylic acid).
The frequency of side effects is given in accordance with the classification of the World Health Organization: very common – at least 10%; common – at least 1% and less than 10%; rare – at least 0.01% and less than 0.1%; very rare – less than 0.01%, including isolated cases.
From the central nervous system and sensory organs: frequent – dizziness, headache, weakness, infrequent – motor restlessness, rare – nystagmus, loss of consciousness, drowsiness, visual and auditory disturbances, tremor, trism, seizures (the risk of their development increases against a background of hypercapnia and acidosis), very rare – paralysis of respiratory muscles, respiratory arrest, motor and sensory block, respiratory paralysis (develops more often in subarachnoid anesthesia).
The cardiovascular system: often – increase or decrease of blood pressure, rarely – bradycardia, arrhythmia, tachycardia – when administered with a vasoconstrictor, very rarely – peripheral vasodilation, collapse, pain in the chest.
Gastrointestinal tract: frequently – nausea, vomiting, involuntary defecation.
Blood: infrequent – methemoglobinemia.
Local reactions: often – in spinal anesthesia – back pain, in epidural anesthesia – accidental penetration into the subarachnoid space.
Allergic reactions: often – skin rash, urticaria (on the skin and mucous membranes), skin itching, very rarely – angioedema, anaphylactic shock.
Others: infrequent – persistent anesthesia, very rare – respiratory depression, up to and including respiratory arrest, hypothermia.
Symptoms: initial signs of intoxication – dizziness, nausea, vomiting, euphoria, drowsiness, headache, paresthesias, disorientation, visual disturbances; later – convulsions of facial mimic muscles with transition to tonic-clonic convulsions of skeletal muscles, psychomotor agitation, asthenia, apnea, bradycardia, decreased blood pressure, collapse, methemoglobinemia; when used in childbirth, in the newborn – bradycardia, respiratory center depression, apnea.
Treatment: if the first signs of intoxication appear the administration is stopped, the patient is transferred to the horizontal position and oxygenation is carried out. In case of convulsions, intravenous diazepam 10 mg, in case of bradycardia – m-cholinoblockers (atropine), vasoconstrictors (norepinephrine, phenylephrine). Intubation, artificial lung ventilation, resuscitation measures are indicated if necessary. Dialysis is ineffective.
Lidocaine, Versatis, Lidocaine-Vial
3 years. Do not use after the expiration date shown on the package.
|Conditions of storage|
Store in a dark place at a temperature not exceeding 25°C. Keep out of reach of children.
solution for injection
Buy Lidocaine, 100 mg/ml 2 ml 10 pcs with delivery to USA, UK, Europe and over 120 other countries.