Pharmacological action Lidocaine Jelly
Lidocaine Jelly Antiarrhythmic agent Class IB, local anesthetic, a derivative of acetanilide. It has a membrane stabilizing activity. Causes blockade of sodium channels of excitable membranes of neurons and cardiomyocytes membrane.
Reduces the duration of the action potential and effective refractory period in Purkinje fibers, inhibits their automaticity. At the same time suppresses the electrical activity of lidocaine depolarized, arrhythmogenic sites, but minimal effect on the electrical activity of normal tissues. When used in the medium therapeutic doses practically no effect on myocardial contractility and slows AV-conduction. When applied as anti-arrhythmic agent for / in the introduction of the beginning of a 45-90 sec duration – 10-20 minutes, with a / m, the introduction of the top 5-15 minutes, duration – 60-90 minutes.
Causes all kinds of local anesthesia: a terminal, infiltration, conductor.
Pharmacokinetics Lidocaine Jelly
After i / m administration absorption is almost complete. Rapid distribution, Vd is about 1 l / kg (in patients with heart failure, below). Protein binding is dependent on the concentration of active substance in plasma and 60-80%. Metabolized primarily in the liver with the formation of active metabolites that may contribute to the manifestation of the therapeutic and toxic effects, especially after the infusion for 24 hours or more.
T1 / 2 tends to be two phases with the phase distribution of 9.7 min. In general, T1 / 2 is dependent on the dose is 1-2 hours and can grow up to 3 hours or more during the long in / infusion (over 24 h). Excreted by the kidneys as metabolites, 10% unchanged.
Statement Lidocaine Jelly
In cardiological practice: treatment and prevention of ventricular arrhythmias (extrasystoles, tachycardia, atrial flutter, atrial fibrillation), including in acute myocardial infarction, pacemaker implantation, and the glycoside intoxication, narcosis.
For anesthesia: a terminal, infiltration, conduction, spinal (epidural) anesthesia in surgery, obstetrics and gynecology, urology, ophthalmology, dentistry, otolaryngology, blockade of peripheral nerves and ganglia.
Dosage regimen Lidocaine Jelly
As an anti-arrhythmic means an adult with the introduction of a loading dose in / – 1.2 mg / kg over 3-4 minutes, with an average single dose of 80 mg. Then immediately transferred to a dropping infusion at 20-55 mg / kg / min. Drip infusion can be performed within 24-36 h. If necessary, against the background of the drop infusion can be repeated in / bolus administration of lidocaine 40 mg after 10 minutes after the first loading dose.
V / m is introduced to 2-4 mg / kg, if necessary, re-introduction may in 60-90 minutes.
Children with a / in a loading dose – 1 mg / kg, if necessary, may re-introduction after 5 minutes. For continuous in / infusion (usually after the administration of a loading dose) – 20-30 mg / kg / min.
For use in surgery and obstetrics, dentistry, ENT practice, the dosage is determined individually, depending on the evidence, the clinical situation and used the dosage form.
Maximum dose: adults with a / in a loading dose – 100 mg, with subsequent drop infusion – 2 mg / min, with a / m administration – 300 mg (about 4.5 mg / kg) for 1 h.
Children in the event of repeated administration of a loading dose every 5 minutes total dose of 3 mg / kg, in a continuous in / infusion (usually after the administration of a loading dose) – 50 mg / kg / min.
Side effect Lidocaine Jelly
From the central and peripheral nervous system: dizziness, headache, weakness, restlessness, nystagmus, loss of consciousness, drowsiness, visual and auditory disturbances, tremors, lockjaw, convulsions (risk of increased against the background of hypercapnia and acidosis), a syndrome of “horse tail “(paralysis of the legs, paresthesias), paralysis of respiratory muscles, respiratory arrest, motor block and sensitive, respiratory paralysis (usually develops in the subarachnoid anesthesia), numb tongue (when used in dentistry).
Cardio-vascular system: an increase or decrease blood pressure, tachycardia – the introduction of a vasoconstrictor, peripheral vasodilation, collapse, chest pain.
Part of the digestive system: nausea, vomiting, involuntary defecation.
Allergic reactions: skin rash, hives (on skin and mucous membranes), itching, angioedema, anaphylactic shock.
Local reactions: with spinal anesthesia – back pain, with epidural anesthesia – a random hit in the subarachnoid space, the local application in urology – urethritis.
Other: incontinent, methemoglobinemia, persistent anesthesia, decreased libido and / or potency, respiratory depression, up to a stop, hypothermia during anesthesia in dentistry: numbness and paresthesia of the lips and tongue, the lengthening of anesthesia.
Contraindications Lidocaine Jelly
Severe bleeding, shock, hypotension, infection, injection site expected, marked bradycardia, cardiogenic shock, severe congestive heart failure, SSS in elderly patients, AV-block II and III degree (except when introduced probe to stimulate the ventricles) , severe liver problems.
For subarachnoid anesthesia – a complete heart block, bleeding, hypotension, shock, infection, place of lumbar puncture, septicemia.
Increased sensitivity to lidocaine and other amide local anesthetic type.
Pregnancy and breastfeeding Lidocaine Jelly
During pregnancy and lactation only use for emergencies. Lidocaine is excreted in breast milk.
In obstetric practice with caution paracervical for violations of fetal development, fetoplacental insufficiency, prematurity, postmaturity, gestosis.
Cautions
C caution should be used for conditions associated with decreased hepatic blood flow (including chronic heart failure, liver disease), advanced cardiovascular failure (usually due to blockages of the heart and shock), the heavy and debilitated patients, elderly patients age (65 years) for epidural anesthesia – with neurological diseases, septicemia, failure of the puncture for spinal deformity, and for subarachnoid anesthesia – with back pain, infection of the brain, both benign and malignant tumors of the brain, with coagulopathies of various origins , migraine, subarachnoid hemorrhage, hypertension, hypotension, paresthesias, psychosis, hysteria, a non-contact patients, the impossibility of a puncture for spinal deformity.
Care should be injected lidocaine into the tissue with abundant vascularization (eg, in the neck area during operations on the thyroid gland), in such cases, lidocaine is used in smaller doses.
With the simultaneous use of beta-blockers, cimetidine required to decrease the dose of lidocaine, with polymyxin B – should control the function of breathing.
In treatment of MAO inhibitors should not be applied lidocaine administered parenterally.
Injectable solutions, which include epinephrine and norepinephrine, are not designed for on / in a.
Lidocaine can not be added to transfused blood.
Effects on ability to drive and control mechanisms
After application of lidocaine is not recommended to engage in activities that require high concentration and rapid psychomotor reactions.
Drug Interactions Lidocaine Jelly
While the use of barbiturates (including with phenobarbital) may increase the metabolism of lidocaine in the liver, decreased plasma concentrations and, therefore, reducing its therapeutic efficacy.
With the simultaneous use of beta-blockers (including with propranolol, nadolol) may increase the effects of lidocaine (including toxic), apparently due to slow its metabolism in the liver.
With the simultaneous use of MAO inhibitors may increase the local anesthetic action of lidocaine.
With the simultaneous use with drugs that cause blockade of neuromuscular transmission (including with suxamethonium chloride) may increase the action of drugs that cause blockade of neuromuscular transmission.
With the simultaneous use of hypnotics and sedatives may increase the inhibitory action on the central nervous system with aymalin, quinidine – may increase cardiodepressive action; with amiodarone – described the cases of seizures and SSS.
In an application with geksenalom, tiopentalom sodium (w / w) possible respiratory depression.
In an application with mexiletine increases toxicity of lidocaine, with midazolam – a moderate decrease in the concentration of lidocaine in plasma morphine – increased analgesic effect of morphine.
In an application with prenylamine growing risk of ventricular arrhythmias such as “pirouette”.
We describe the cases of excitation, hallucinations, while the use of procainamide.
While the use of propafenone may increase the duration and increase the severity of side effects from the CNS.
It is believed that under the influence of rifampicin may decrease the concentration of lidocaine in plasma.
With the simultaneous in / infusion of lidocaine and phenytoin may increase the side effects of central origin, described the case sinoatrial block due to the additive action of lidocaine cardiodepressive and phenytoin.
Patients receiving phenytoin as anticonvulsant, may decrease the concentration of lidocaine in plasma, due to the induction of microsomal liver enzymes influenced by phenytoin.
While the use of cimetidine moderately reduced clearance of lidocaine and increases its concentration in blood plasma, there is risk of increasing the side effects of lidocaine.
