DRUGS & SUPPLEMENTS

Lidocaine

Rating: 2.5 - 2 review(s)
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Lidocaine uses


Pharmacological action

Lidocaine is an antiarrhythmic agent of class IB, local anesthetic, a derivative of acetanilide. This medication has membrane stabilizing activity. Lidocaine causes a blockade of sodium channels of excitable membranes of neurons and the membrane of cardiomyocytes.

This drug reduces the duration of the action potential and effective refractory period in Purkinje fibers, inhibits their automaticity. In this case, Lidocaine inhibits electrical activity in depolarized, arrhythmogenic sites, but minimally affects the electrical activity of normal tissues. When used in the medium therapeutic doses virtually no effect on myocardial contractility and slows AV-conduction. When applied as an antiarrhythmic agent in IV injection it begin to act in 45-90 seconds, the duration of action is 10-20 minutes; for IM administration the onset of action is in 5-15 minutes, the duration - 60-90 minutes.

Lidocaine causes all kinds of local anesthesia: a terminal, infiltration and wires.

Pharmacokinetics

After IM administration absorption of Lidocaine is almost complete. The distribution is rapid, Vd is about 1 L/kg. The protein binding depends on the concentration of the active substance in the plasma and is 60-80%. Lidocaine metabolized mainly 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 depends on the dose is 1-2 hours and can grow up to 3 hours or more during prolonged intravenous infusion (over 24 h). Lidocaine excreted by the kidneys as metabolites, 10% unchanged.

Why is Lidocaine prescribed?

In cardiological practice: treatment and prevention of ventricular arrhythmias (extrasystoles, tachycardia, atrial flutter, atrial fibrillation), including in acute myocardial infarction, implantation of artificial pacemaker in the glycoside intoxication, narcosis.

Anaesthesia: terminal, infiltration, conduction, spinal (epidural) anesthesia in surgery, obstetrics and gynecology, urology, ophthalmology, dentistry, otolaryngology, blockade of peripheral nerves and ganglion.

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Dosage and administration

As an anti-arrhythmic medicine for adult with the introduction of a loading dose by IV - 1-2 mg / kg over 3-4 minutes; the average single dose is 80 mg. Then immediately transferred to drip infusion at a rate of 20-55 mg / kg / min. Drip infusion can be carried out within 24-36 hours. If necessary, against the background of drop infusions can repeat IV jet injection of Lidocaine 40 mg after 10 minutes after the first loading dose.

IM is introduced to 2-4 mg / kg, if necessary, repeated administration is possible through 60-90 minutes.

For children with IV injection loading dose - 1 mg / kg, if necessary, it may be repeated administration in 5 min.

For continuous intravenous infusion - 20-30 mg / kg / min.

For use in surgical and obstetric practice, dentistry, ENT practice, dosing regimen set individually, depending on the evidence, the clinical situation and used the dosage form.

Maximum dose: for adults for IV injections the loading dose is 100 mg, in a subsequent drop infusion it is 2 mg / min; when IM administration - 300 mg (about 4.5 mg / kg) for 1 h.

For children in case of reintroduction the loading dose every 5 minutes, the total dose is 3 mg / kg; by continuous intravenous infusion (usually following the introduction of a loading dose) - 50 mg / kg / min.

Lidocaine side effects, adverse reactions

CNS and peripheral nervous system: dizziness, headache, weakness, motor restlessness, nystagmus, loss of consciousness, drowsiness, visual and auditory disturbances, tremor, trismus, seizures (risk of their development against the backdrop of increasing hypercapnia and acidosis), a syndrome of "cauda equina" (paralysis of the legs, paresthesia), paralysis of respiratory muscles, respiratory arrest, a block of motor and sensitive, respiratory paralysis (usually develops in the subarachnoid anesthesia), numb tongue (when used in dentistry).

Cardiovascular system: increased or decreased blood pressure, tachycardia if used with a vasoconstrictor, peripheral vasodilatation, collapse, chest pain.

Digestive system: nausea, vomiting, involuntary defecation.

Allergic reactions: skin rash, hives (on skin and mucous membranes), itching, angioedema, anaphylactic shock.

Local reactions: during spinal anesthesia - a pain in the back, with an epidural anesthesia - a random hit in the subarachnoid space, when applied topically in urology - urethritis.

Other: incontinent, methemoglobinemia, persistent anesthesia, decreased libido and / or potency, respiratory depression, until the stop, hypothermia; during anesthesia in dentistry: numbness and paresthesia of the lips and tongue, the lengthening of anesthesia.

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Lidocaine contraindications

Severe bleeding, shock, hypotension, infection of the proposed injection site, marked bradycardia, cardiogenic shock, severe forms of chronic heart failure, SSS in elderly patients, AV-block II and III degree, severe liver function abnormalities.

For subarachnoid anesthesia - complete heart block, bleeding, hypotension, shock, infection of the venue lumbar puncture, septicemia.

Increased sensitivity to Lidocaine and other amide type local anesthetics.

Using during pregnancy and breastfeeding

During pregnancy and lactation be used only for health reasons. Lidocaine is excreted in breast milk.

In obstetric practice used with caution in paracervical for violations of fetal development, placental insufficiency, prematurity, postmaturity, gestosis.

Category effects on the fetus by FDA - B.

Special instructions

Use with caution in liver disease and kidney failure, hypovolemia, severe heart failure, in violation of the contractility of genetic susceptibility to malignant hyperthermia. In children, debilitated patients, elderly patients are required in dosage adjustment in accordance with the age and physical status. When injected into vascularized tissue it is recommended an aspiration test.

Lidocaine drug interactions

Beta-blockers increase the risk of bradycardia and hypotension. Norepinephrine and beta-blockers by reducing hepatic blood flow decrease, isadrine and glucagon - increase the clearance of Lidocaine. Cimetidine increases the plasma concentration of Lidocaine (displaces from its association with proteins and slows inactivation in the liver). Barbiturates causing induction of microsomal enzymes stimulate the degradation of Lidocaine and reduce its activity. Anticonvulsants (hydantoin derivatives) accelerate the biotransformation in the liver (decreased concentration in the blood), for IV injections it may increases cardiodepressive action of Lidocaine. Antiarrhythmics (amiodarone, verapamil, quinidine, aymalin) potentiate cardiac depression. Combination with novocainamide may cause CNS excitement and hallucinations. Lidocaine strengthens the inhibitory effect of anesthesia (hexobarbital, thiopental sodium), hypnotics and sedatives on the respiratory center, weakens the cardiac effects of digitoxin, enhances muscle relaxation caused by drugs curare like (possible paralysis of respiratory muscles). MAO inhibitors prolong local anesthesia.

Lidocaine in case of emergency / overdose

Symptoms: psychomotor agitation, dizziness, weakness, decreased blood pressure, tremors, tonic-clonic convulsions, coma, collapse, possible AV blockade, CNS depression, respiratory arrest.

Treatment: discontinuation, pulmonary ventilation, oxygen therapy, anticonvulsants, vasoconstrictors (norepinephrine, mezaton), when bradycardia - anticholinergics (atropine). It is possible to carry out intubation, mechanical ventilation, resuscitation. Dialysis is ineffective.

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Lidocaine pharmaceutical active ingredients containing related brand and generic drugs:

infoActive ingredient is the part of the drug or medicine which is biologically active. This portion of the drug is responsible for the main action of the drug which is intended to cure or reduce the symptom or disease. The other portions of the drug which are inactive are called excipients; there role is to act as vehicle or binder. In contrast to active ingredient, the inactive ingredient's role is not significant in the cure or treatment of the disease. There can be one or more active ingredients in a drug.


Lidocaine available forms, composition, doses:

infoForm of the medicine is the form in which the medicine is marketed in the market, for example, a medicine X can be in the form of capsule or the form of chewable tablet or the form of tablet. Sometimes same medicine can be available as injection form. Each medicine cannot be in all forms but can be marketed in 1, 2, or 3 forms which the pharmaceutical company decided based on various background research results.
Composition is the list of ingredients which combinedly form a medicine. Both active ingredients and inactive ingredients form the composition. The active ingredient gives the desired therapeutic effect whereas the inactive ingredient helps in making the medicine stable.
Doses are various strengths of the medicine like 10mg, 20mg, 30mg and so on. Each medicine comes in various doses which is decided by the manufacturer, that is, pharmaceutical company. The dose is decided on the severity of the symptom or disease.

Price
Akten 3.5% drops7.5 USD
Drops; Ophthalmic; Lidocaine Hydrochloride 2%
Drops; Ophthalmic; Lidocaine Hydrochloride 4%
EMLA 2.5-2.5% Cream 30 gm Tube58.4 USD
Gel; Local; Lidocaine Hydrochloride 5%
Injectable; Injection; 1%
Injectable; Injection; 1.5%
Injectable; Injection; 2%
Injectable; Injection; 20%
Injectable; Injection; 4%
Injectable; Injection; Lidocaine Hydrochloride 0.5%
Injectable; Injection; Lidocaine Hydrochloride 1%
Injectable; Injection; Lidocaine Hydrochloride 10 mg / ml
Injectable; Injection; Lidocaine Hydrochloride 10%
Injectable; Injection; Lidocaine Hydrochloride 15 mg / ml
Injectable; Injection; Lidocaine Hydrochloride 2%
Injectable; Injection; Lidocaine Hydrochloride 20 mg / ml
Injectable; Injection; Lidocaine Hydrochloride 20%
Injectable; Injection; Lidocaine Hydrochloride 4%
Injectable; Injection; Lidocaine Hydrochloride 5 mg / ml
Jelly; Topical; 2%
Jelly; Topical; Lidocaine Hydrochloride 2%
Lidamantle 3% cream2.03 USD
Lidocaine 2% viscous solution0.03 USD
Lidocaine 3% cream2.91 USD
Lidocaine 5% in d7.5w ampul3.06 USD
Lidocaine HCl 1% Solution0.24 USD
Lidocaine HCl 2% Gel 10ml Syringe17.99 USD
Lidocaine HCl 2% Gel 30ml Tube17.99 USD
Lidocaine HCl 3% Lotion 177ml Bottle230.3 USD
Lidocaine HCl 4% Solution 4ml Bottle9.42 USD
Lidocaine HCl 4% Solution 50ml Bottle16.99 USD
Lidocaine Viscous 2% Solution 100ml Bottle13.99 USD
Lidocaine base powder0.22 USD
Lidocaine hcl 0.5% vial0.08 USD
Lidocaine hcl 1% syringe9.76 USD
Lidocaine hcl 10% vial0.55 USD
Lidocaine hcl 4% solution0.18 USD
Lidocaine hcl powder0.24 USD
Lidocaine-Prilocaine 2.5-2.5% Cream 30 gm Tube47.79 USD
Lidodan 5 % Ointment0.16 USD
Lidodan Viscous 2 % Liquid0.06 USD
Lidoderm 1 Box = 30 Patches8.03 USD
Liquid; Block / Infiltration; Lidocaine Hydrochloride 2%
Rocephin 1 gm vial62.02 USD
Rocephin 10 gm vial478.32 USD
Rocephin 2 gm vial97.5 USD
Solarcaine aerosol0.06 USD
Solution; Block / Infiltration; Lidocaine Hydrochloride 1%
Solution; Oral; Lidocaine Hydrochloride 2%
Solution; Topical; Lidocaine Hydrochloride 4%
Xylocaine 0.5% vial0.18 USD
Xylocaine 2% Solution0.34 USD
Xylocaine 2% jelly0.68 USD
Xylocaine 5 % Ointment0.29 USD
Xylocaine 5% ointment0.42 USD
Xylocaine Jelly 2 % Jelly0.41 USD
Xylocaine Viscous 2 % Liquid0.1 USD
Zilactin-l cold sore liquid0.99 USD

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Lidocaine destination | category:

infoDestination is defined as the organism to which the drug or medicine is targeted. For most of the drugs what we discuss, human is the drug destination.
Drug category can be defined as major classification of the drug. For example, an antihistaminic or an antipyretic or anti anginal or pain killer, anti-inflammatory or so.


Lidocaine Anatomical Therapeutic Chemical codes:

infoA medicine is classified depending on the organ or system it acts [Anatomical], based on what result it gives on what disease, symptom [Therapeutical], based on chemical composition [Chemical]. It is called as ATC code. The code is based on Active ingredients of the medicine. A medicine can have different codes as sometimes it acts on different organs for different indications. Same way, different brands with same active ingredients and same indications can have same ATC code.


Lidocaine pharmaceutical companies:

infoPharmaceutical companies are drug manufacturing companies that help in complete development of the drug from the background research to formation, clinical trials, release of the drug into the market and marketing of the drug.
Researchers are the persons who are responsible for the scientific research and is responsible for all the background clinical trials that resulted in the development of the drug.


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References

  1. Dailymed."GIGI ANESTHETIC NUMBING (LIDOCAINE) AEROSOL [220 LABORATORIES INC]". https://dailymed.nlm.nih.gov/dailym... (accessed August 28, 2018).
  2. Dailymed."PHARMAPURERX LIDOCAINE HCL 4.12% (LIDOCAINE HYDROCHLORIDE) CREAM [PURETEK CORPORATION]". https://dailymed.nlm.nih.gov/dailym... (accessed August 28, 2018).
  3. Dailymed."LIDOCAINE; TETRACAINE: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailym... (accessed August 28, 2018).

Frequently asked Questions

Can i drive or operate heavy machine after consuming Lidocaine?

Depending on the reaction of the Lidocaine after taken, if you are feeling dizziness, drowsiness or any weakness as a reaction on your body, Then consider Lidocaine not safe to drive or operate heavy machine after consumption. Meaning that, do not drive or operate heavy duty machines after taking the capsule if the capsule has a strange reaction on your body like dizziness, drowsiness. As prescribed by a pharmacist, it is dangerous to take alcohol while taking medicines as it exposed patients to drowsiness and health risk. Please take note of such effect most especially when taking Primosa capsule. It's advisable to consult your doctor on time for a proper recommendation and medical consultations.

Is Lidocaine addictive or habit forming?

Medicines are not designed with the mind of creating an addiction or abuse on the health of the users. Addictive Medicine is categorically called Controlled substances by the government. For instance, Schedule H or X in India and schedule II-V in the US are controlled substances.

Please consult the medicine instruction manual on how to use and ensure it is not a controlled substance.In conclusion, self medication is a killer to your health. Consult your doctor for a proper prescription, recommendation, and guidiance.

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Review

sDrugs.com conducted a study on Lidocaine, and the result of the survey is set out below. It is noteworthy that the product of the survey is based on the perception and impressions of the visitors of the website as well as the views of Lidocaine consumers. We, as a result of this, advice that you do not base your therapeutic or medical decisions on this result, but rather consult your certified medical experts for their recommendations.

Visitor reports

One visitor reported useful

How is the drug Lidocaine useful in reducing or relieving the symptoms? How useful is it?
According to the survey conducted by the website sDrugs.com, there are variable results and below are the percentages of the users that say the medicine is useful to them and that say it is not helping them much. It is not ideal to continue taking the medication if you feel it is not helping you much. Contact your healthcare provider to check if there is a need to change the medicine or if there is a need to re-evaluate your condition. The usefulness of the medicine may vary from patient to patient, depending on the other diseases he is suffering from and slightly depends on the brand name.
Visitors%
Not useful1
100.0%

One visitor reported side effects

Did you get side effects while taking the Lidocaine drug, or were there no side effects?
According to the survey conducted by website sDrugs.com users, the below-mentioned percentages indicate the number of people experiencing the side effects and the number of people not experiencing the side effects when taking Lidocaine medicine. Every drug produces minimal side effects, and they are negligible most times, when compared to the desired effect [use] of the medicine. Side effects depend on the dose you are taking, any drug interactions that happen when you are on other medications, if the patient is sensitive, and other associated conditions. If you cannot tolerate the side effects, consult your doctor immediately, so he can either adjust the dose or change the medication.
Visitors%
No side effects1
100.0%

Three visitors reported doses

What is the dose of Lidocaine drug you are taking?
According to the survey conducted among sDrugs.com website users, the maximum number of people are using the following dose 101-200mg. Few medications come in only one or two doses. Few are specific for adult dose and child dose. The dose of the medicine given to the patient depends on the severity of the symptom/disease. There can be dose adjustments made by the doctor, based on the progression of the disease. Follow-up is important.
Visitors%
101-200mg1
33.3%
11-50mg1
33.3%
1-5mg1
33.3%

One visitor reported time for results

What is the time duration Lidocaine drug must be taken for it to be effective or for it to reduce the symptoms?
Most chronic conditions need at least some time so the dose and the drug action gets adjusted to the body to get the desired effect. The stastistics say sDrugs.com website users needed 1 month to notice the result from using Lidocaine drug. The time needed to show improvement in health condition after using the medicine Lidocaine need not be same for all the users. It varies based on other factors.
Visitors%
1 month1
100.0%

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The information was verified by Dr. Arunabha Ray, MD Pharmacology

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