XYLOCAINE Lidocaine 10mg / dose (10.0%) Pump Spray 50mL
RXDRUG-DR-1860
Discreet Packaging
FDA-registered Products
FDA-licensed Pharmacies
Indications/Uses
Xylocaine Injection: Local or regional anesthesia by infiltration techniques including percutaneous injection; IV regional anesthesia; peripheral nerve block techniques eg, brachial plexus and intracostal blocks; central neural techniques including epidural and caudal blocks.
Xylocaine Pump Spray: Nasal procedures eg, puncture of the maxillary sinus; oral and dental procedures eg, prior to injection; procedures in the oropharynx eg, gastrointestinal endoscopy; procedures in the respiratory tract eg, insertion of instruments and tubes; procedures in the larynx, trachea and bronchi; procedures in obstetrics and gynecology eg, vaginal delivery, suturing of ruptures in the mucosa and cervical biopsies.
Xylocaine Pump Spray: Nasal procedures eg, puncture of the maxillary sinus; oral and dental procedures eg, prior to injection; procedures in the oropharynx eg, gastrointestinal endoscopy; procedures in the respiratory tract eg, insertion of instruments and tubes; procedures in the larynx, trachea and bronchi; procedures in obstetrics and gynecology eg, vaginal delivery, suturing of ruptures in the mucosa and cervical biopsies.
Dosage/Direction for Use
Xylocaine Injection: Injections should always be made slowly with frequent aspiration to avoid accidental rapid IV injection which may produce toxic effects.
For epidural anesthesia, a test dose of 3-5 mL Xylocaine containing adrenaline should be administered, since an IV injection of adrenaline may be recognized by an increase in heart rate of short duration. Verbal contact and repeated measurements of heart rate should be maintained throughout a period of 5 min following the test dose. Aspiration should be repeated prior to administration of the total dose. The main dose should be injected slowly, 25-30 mg/min, in incremental doses under continual monitoring of the patient. If mild toxic symptoms occur, the injection should be stopped immediately.
The lowest dosage that will produce the desired effect should be given. Dosages should be reduced in children and in elderly or debilitated patients and patients with cardiac and/or liver disease.
For epidural anesthesia, a test dose of 3-5 mL Xylocaine containing adrenaline should be administered, since an IV injection of adrenaline may be recognized by an increase in heart rate of short duration. Verbal contact and repeated measurements of heart rate should be maintained throughout a period of 5 min following the test dose. Aspiration should be repeated prior to administration of the total dose. The main dose should be injected slowly, 25-30 mg/min, in incremental doses under continual monitoring of the patient. If mild toxic symptoms occur, the injection should be stopped immediately.
The lowest dosage that will produce the desired effect should be given. Dosages should be reduced in children and in elderly or debilitated patients and patients with cardiac and/or liver disease.
Xylocaine Pump Spray: It is intended for use on mucous membranes and provides efficient surface anesthesia, which lasts for approximately 10-15 min. The anesthesia usually occurs within 1-3 min depending on the area of application.
As with any local anesthetics, the safety and effectiveness of lidocaine depend on the proper dosage, the correct technique, adequate precautions and readiness for emergencies.
As with any local anesthetics, the safety and effectiveness of lidocaine depend on the proper dosage, the correct technique, adequate precautions and readiness for emergencies.
Since absorption is variable and especially high in the trachea and bronchi (see Adverse Reactions and Pharmacokinetics under Actions) the maximum recommended doses vary depending on the area of application.
In children, doses should not exceed 3 mg/kg for laryngotracheal use and 4-5 mg/kg for nasal, oral and oropharyngeal use.
In neonates and infants less concentrated lidocaine solutions are recommended.
In children, doses should not exceed 3 mg/kg for laryngotracheal use and 4-5 mg/kg for nasal, oral and oropharyngeal use.
In neonates and infants less concentrated lidocaine solutions are recommended.
Overdosage
Symptoms: Pump Spray: Acute Systemic Toxicity: Toxic reactions originate mainly in the CNS and CVS.
Central nervous system toxicity is a graded response, with symptoms and signs of escalating severity. The 1st symptoms are circumoral paresthesia, numbness of the tongue, lightheadedness, hyperacusis and tinnitus. Visual disturbance and muscular tremors are more serious and precede the onset of generalized convulsions. Unconsciousness and grand mal convulsions may follow, which may last from a few seconds to several minutes. Hypoxia and hypercarbia occur rapidly following convulsions due to increased muscular activity, together with the interference with normal respiration. In severe cases apnea may occur.
Acidosis increases the toxic effects of local anesthetics.
Recovery is due to redistribution and metabolism of the local anesthetic drug from the CNS. Recovery may be rapid unless large amounts of the drug have been administered.
Cardiovascular effects are only seen in cases with high systemic concentrations. Severe hypotension, bradycardia, arrhythmia and cardiovascular collapse may be the result in such cases.
Cardiovascular toxic effects are generally preceded by signs of toxicity in the CNS unless patient is receiving a general anesthetic or is heavily sedated with drugs eg, benzodiazepine or barbiturate.
However, should systemic toxicity occur, the signs are anticipated to be similar in nature to those following the administration of local anaesthetics by other routes.
Local anaesthetics toxicity is manifested by symptoms of nervous system excitation and, in severe cases, central nervous and cardiovascular depression.
Treatment: Injection: Treatment of a patient with toxic manifestations consists in ensuring adequate ventilation and arresting convulsions. Ventilation should be maintained with oxygen by assisted or controlled respiration as required. If convulsions occur, they should be treated rapidly by the IV administration of succinylcholine; 50-100 mg and/or diazepam 5-15 mg. Thiopentone may also be used to abort convulsions in the dosage 100-200 mg. If ventricular fibrillation or cardiac arrest occurs, effective cardiovascular resuscitation must be instituted.
Pump Spray: Treatment of Acute Toxicity: Treatment of acute toxicity should be instituted at the latest when twitches occur. The necessary drugs and equipment should be immediately available. The objectives of treatment are to maintain oxygenation, stop the convulsions and support the circulation.
Oxygen must be given and, if necessary, assisted ventilation (mask and bag). An anticonvulsant should be given IV if the convulsions do not stop spontaneously in 15-30 sec. Thiopentone 100-150 mg IV will abort the convulsions rapidly.
Alternatively diazepam 0.1/kg body weight may be used, although its action will be slow.
Prolonged convulsions may jeopardise the patient's ventilation and oxygenation. If so, injection of a muscle relaxant (eg, succinylcholine 1 mg/kg body weight) will facilitate ventilation and oxygenation can be controlled. Early endotracheal intubation must be considered in such situations.
If cardiovascular depression is evident (hypotension, bradycardia), ephedrine; 5-10 mg IV should be given and may be repeated, if necessary after 2-3 min.
Should circulatory arrest occur, immediate cardiopulmonary resuscitation (CPR) should be instituted. Optimal oxygenation and ventilation and circulatory support as well as acidosis are of vital importance since hypoxia and acidosis will increase the systemic toxicity of local anesthetics. Adrenaline (0.1-0.2 mg as IV or intracardiac injections) should be given as soon as possible and repeated, if necessary.
Children should be given doses commensurate with their age and weight.
Central nervous system toxicity is a graded response, with symptoms and signs of escalating severity. The 1st symptoms are circumoral paresthesia, numbness of the tongue, lightheadedness, hyperacusis and tinnitus. Visual disturbance and muscular tremors are more serious and precede the onset of generalized convulsions. Unconsciousness and grand mal convulsions may follow, which may last from a few seconds to several minutes. Hypoxia and hypercarbia occur rapidly following convulsions due to increased muscular activity, together with the interference with normal respiration. In severe cases apnea may occur.
Acidosis increases the toxic effects of local anesthetics.
Recovery is due to redistribution and metabolism of the local anesthetic drug from the CNS. Recovery may be rapid unless large amounts of the drug have been administered.
Cardiovascular effects are only seen in cases with high systemic concentrations. Severe hypotension, bradycardia, arrhythmia and cardiovascular collapse may be the result in such cases.
Cardiovascular toxic effects are generally preceded by signs of toxicity in the CNS unless patient is receiving a general anesthetic or is heavily sedated with drugs eg, benzodiazepine or barbiturate.
However, should systemic toxicity occur, the signs are anticipated to be similar in nature to those following the administration of local anaesthetics by other routes.
Local anaesthetics toxicity is manifested by symptoms of nervous system excitation and, in severe cases, central nervous and cardiovascular depression.
Treatment: Injection: Treatment of a patient with toxic manifestations consists in ensuring adequate ventilation and arresting convulsions. Ventilation should be maintained with oxygen by assisted or controlled respiration as required. If convulsions occur, they should be treated rapidly by the IV administration of succinylcholine; 50-100 mg and/or diazepam 5-15 mg. Thiopentone may also be used to abort convulsions in the dosage 100-200 mg. If ventricular fibrillation or cardiac arrest occurs, effective cardiovascular resuscitation must be instituted.
Pump Spray: Treatment of Acute Toxicity: Treatment of acute toxicity should be instituted at the latest when twitches occur. The necessary drugs and equipment should be immediately available. The objectives of treatment are to maintain oxygenation, stop the convulsions and support the circulation.
Oxygen must be given and, if necessary, assisted ventilation (mask and bag). An anticonvulsant should be given IV if the convulsions do not stop spontaneously in 15-30 sec. Thiopentone 100-150 mg IV will abort the convulsions rapidly.
Alternatively diazepam 0.1/kg body weight may be used, although its action will be slow.
Prolonged convulsions may jeopardise the patient's ventilation and oxygenation. If so, injection of a muscle relaxant (eg, succinylcholine 1 mg/kg body weight) will facilitate ventilation and oxygenation can be controlled. Early endotracheal intubation must be considered in such situations.
If cardiovascular depression is evident (hypotension, bradycardia), ephedrine; 5-10 mg IV should be given and may be repeated, if necessary after 2-3 min.
Should circulatory arrest occur, immediate cardiopulmonary resuscitation (CPR) should be instituted. Optimal oxygenation and ventilation and circulatory support as well as acidosis are of vital importance since hypoxia and acidosis will increase the systemic toxicity of local anesthetics. Adrenaline (0.1-0.2 mg as IV or intracardiac injections) should be given as soon as possible and repeated, if necessary.
Children should be given doses commensurate with their age and weight.
Contraindications
Known history of hypersensitivity to local anesthetics of the amide type or other components of Xylocaine injection/spray.
Xylocaine Injection: General contraindications for the different local and regional anesthetic techniques should be taken into consideration.
Xylocaine Injection: General contraindications for the different local and regional anesthetic techniques should be taken into consideration.
Special Precautions
Injection: The following precautions apply to the use of local anesthetics in general and should be taken into consideration before administration.
Before administration of the drug make sure that resuscitative equipment eg, equipment required for maintaining a free airway and oxygenation and drugs for use in the treatment of toxic reactions, are immediately available.
The possibility of hypotension and bradycardia following central neural block should be anticipated and appropriate precautions taken.
Since amide-type local anesthetics are metabolized by the liver, such drugs, especially in repeated doses, should be used with caution in patients with hepatic disease.
Local anesthetics should be used with caution for epidural anesthesia in patients with impaired cardiovascular function since they may be less able to compensate for functional changes associated with prolongation of A-V conduction produced by these drugs.
Small doses of local anesthetics injected into the head and neck area, including retrobulbar, dental and stellate ganglion blocks, may produce adverse reactions similar to systemic toxicity seen with accidental intravascular injections of larger doses.
Clinicians who perform retrobulbar blocks should be aware that there have been reports of respiratory arrest following the injection of local anesthetics. Prior to retrobulbar block, the necessary equipment, drugs and personnel should be immediately available as with all other regional procedures.
Paracervical block may affect the fetus to a higher degree than other obstetric blocks. The fetal heart rate should always be monitored during paracervical anesthesia since fetal bradycardia frequently follows paracervical block may be associated with fetal acidosis and hypoxia. The potential undesired consequences of paracervical block should be weighed against its advantages when fetal distress is expected or when factors predisposing to fetal distress are present (eg, toxemia, prematurity, diabetes).
Pump Spray: Excessive dosage or short intervals between doses may result in high plasma levels and serious adverse effects. Absorption from mucous membranes is variable but is especially high from the bronchial tree. Such applications may therefore result in rapidly rising or excessive plasma concentrations, with an increased risk of toxic symptoms eg, convulsions. Lidocaine spray should be used with caution in patients with wounds or traumatized mucosa in the region of the proposed application. A damaged mucosa will permit increased systemic absorption. The management of serious adverse reactions may require the use of resuscitative equipment, oxygen and other resuscitative drugs (see Overdosage).
In paralysed patients under general anesthesia, higher blood concentrations may occur than in spontaneously breathing patients. Unparalysed patients are more likely to swallow a large proportion of the dose which then undergoes considerable first-pass hepatic metabolism following absorption from the gut.
The oropharyngeal use of topical anesthetic agents may interfere with swallowing and thus enhance the danger of aspiration. Numbness of the tongue or buccal mucosa may increase the danger of biting trauma.
If the dose or administration is likely to result in high blood levels, some patients will require special attention to prevent potentially dangerous side effects: Patients with cardiovascular disease and heart failure; patients with partial or complete heart block; the elderly and patients in poor general health; patients with severe renal dysfunction; patients with severe renal liver disease.
Patients treated with antiarrhythmic drugs class III (eg, amiodarone) should be under close surveillance and ECG monitoring considered since cardiac effects may be additive.
Xylocaine pump spray should not be used on cuffs of endotracheal tubes (ETT) made of plastic. Lidocaine base in contact with both PVC and non-PVC cuffs of endotracheal tubes may cause damage of the cuff. This damage is described as pinholes which may cause leakage that could lead to pressure loss in the cuff.
Lidocaine pump spray is probably porphyrinogenic and should only be prescribed to patients with acute porphyria on strong or urgent indications. Appropriate precautions should be taken for all porphyic patients.
Effects on the Ability to Drive and Operate Machinery: Depending on the dose, local anesthetics may have a very mild effect on mental function and may temporarily impair locomotion and coordination.
Use in pregnancy & lactation: Lidocaine crosses the placental barrier. Lidocaine concentrations in umbilical veins are lower than those found in the maternal circulation. It is reasonable to assume that a large number of pregnant women and women of childbearing age have been given lidocaine. No specific disturbances to the reproductive process have so far been reported eg, an increased incidence of malformations or direct or indirect harmful effects on the fetus.
Lidocaine has been used extensively for obstetric procedures during labor and delivery which is an indication of its safety.
Like other local anesthetics, lidocaine is excreted in the breast milk, but in such small quantities that there is generally no risk of affecting the child at therapeutic dose levels.
Before administration of the drug make sure that resuscitative equipment eg, equipment required for maintaining a free airway and oxygenation and drugs for use in the treatment of toxic reactions, are immediately available.
The possibility of hypotension and bradycardia following central neural block should be anticipated and appropriate precautions taken.
Since amide-type local anesthetics are metabolized by the liver, such drugs, especially in repeated doses, should be used with caution in patients with hepatic disease.
Local anesthetics should be used with caution for epidural anesthesia in patients with impaired cardiovascular function since they may be less able to compensate for functional changes associated with prolongation of A-V conduction produced by these drugs.
Small doses of local anesthetics injected into the head and neck area, including retrobulbar, dental and stellate ganglion blocks, may produce adverse reactions similar to systemic toxicity seen with accidental intravascular injections of larger doses.
Clinicians who perform retrobulbar blocks should be aware that there have been reports of respiratory arrest following the injection of local anesthetics. Prior to retrobulbar block, the necessary equipment, drugs and personnel should be immediately available as with all other regional procedures.
Paracervical block may affect the fetus to a higher degree than other obstetric blocks. The fetal heart rate should always be monitored during paracervical anesthesia since fetal bradycardia frequently follows paracervical block may be associated with fetal acidosis and hypoxia. The potential undesired consequences of paracervical block should be weighed against its advantages when fetal distress is expected or when factors predisposing to fetal distress are present (eg, toxemia, prematurity, diabetes).
Pump Spray: Excessive dosage or short intervals between doses may result in high plasma levels and serious adverse effects. Absorption from mucous membranes is variable but is especially high from the bronchial tree. Such applications may therefore result in rapidly rising or excessive plasma concentrations, with an increased risk of toxic symptoms eg, convulsions. Lidocaine spray should be used with caution in patients with wounds or traumatized mucosa in the region of the proposed application. A damaged mucosa will permit increased systemic absorption. The management of serious adverse reactions may require the use of resuscitative equipment, oxygen and other resuscitative drugs (see Overdosage).
In paralysed patients under general anesthesia, higher blood concentrations may occur than in spontaneously breathing patients. Unparalysed patients are more likely to swallow a large proportion of the dose which then undergoes considerable first-pass hepatic metabolism following absorption from the gut.
The oropharyngeal use of topical anesthetic agents may interfere with swallowing and thus enhance the danger of aspiration. Numbness of the tongue or buccal mucosa may increase the danger of biting trauma.
If the dose or administration is likely to result in high blood levels, some patients will require special attention to prevent potentially dangerous side effects: Patients with cardiovascular disease and heart failure; patients with partial or complete heart block; the elderly and patients in poor general health; patients with severe renal dysfunction; patients with severe renal liver disease.
Patients treated with antiarrhythmic drugs class III (eg, amiodarone) should be under close surveillance and ECG monitoring considered since cardiac effects may be additive.
Xylocaine pump spray should not be used on cuffs of endotracheal tubes (ETT) made of plastic. Lidocaine base in contact with both PVC and non-PVC cuffs of endotracheal tubes may cause damage of the cuff. This damage is described as pinholes which may cause leakage that could lead to pressure loss in the cuff.
Lidocaine pump spray is probably porphyrinogenic and should only be prescribed to patients with acute porphyria on strong or urgent indications. Appropriate precautions should be taken for all porphyic patients.
Effects on the Ability to Drive and Operate Machinery: Depending on the dose, local anesthetics may have a very mild effect on mental function and may temporarily impair locomotion and coordination.
Use in pregnancy & lactation: Lidocaine crosses the placental barrier. Lidocaine concentrations in umbilical veins are lower than those found in the maternal circulation. It is reasonable to assume that a large number of pregnant women and women of childbearing age have been given lidocaine. No specific disturbances to the reproductive process have so far been reported eg, an increased incidence of malformations or direct or indirect harmful effects on the fetus.
Lidocaine has been used extensively for obstetric procedures during labor and delivery which is an indication of its safety.
Like other local anesthetics, lidocaine is excreted in the breast milk, but in such small quantities that there is generally no risk of affecting the child at therapeutic dose levels.
Adverse Reactions
Injection: Serious systematic adverse reactions are rare but may arise from high plasma concentrations resulting from excessive dosage, rapid absorption or accidental intravascular injection (see Dosage & Administration).
Systematic toxicity caused by lidocaine HCl is similar in nature to that observed with other local anesthetic agents. Pronounced acidosis or hypoxia in the patient may increase the risk and severity of toxic reactions. Such reactions involve the CNS and the CVS.
Central Nervous System Reactions: Characterized by numbness of the tongue, lightheadedness, dizziness, blurred vision and tremors, followed by drowsiness, convulsions, unconsciousness and possibly respiratory arrest.
Cardiovascular Reactions: Severe hypotension and bradycardia may occur following sympathetic block with central neural blocks. Cardiovascular reactions following high doses or the accidental intravascular injection of lidocaine are related to depression of the myocardium, decreased cardiac output, heart block hypotension, bradycardia, ventricular arrhythmias, including ventricular tachycardia and ventricular fibrillation and cardiac arrest. Hypoxia caused by convulsions and apnea may be a contributory factor in the cardiovascular reactions.
Neurological Reactions: The incidence of adverse neurological reactions associated with the use of local anesthetics is very low. Neurological reactions may be a function of the total dose of local anesthetic administered and are also dependent upon the particular drug used, the route of administration and the physical status of the patient. Many of these effects may be linked to local anesthetic techniques, with or without contribution by the drug. Neurological reactions following regional anesthesia have included persistent anesthesia, paresthesia, weakness, paralysis of the lower extremities and loss of sphincter control.
In rare cases, local anesthetic preparations have been associated with allergic reactions (in the most severe instances anaphylactic shock).
Pump Spray: Local irritation at the application site has been described. Following application to laryngeal mucosa before endotracheal intubation, reversible symptoms eg, sore throat, hoarseness and loss of voice have been reported. The use of lidocaine pump spray provides surface anesthesia during an endotracheal procedure but does not prevent post-intubation soreness.
Allergic Reactions: Allergic reactions (in the most severe instances anaphylactic shock) to local anesthetics of the amide type are rare (<0.1%).
Acute Systemic Toxicity: Lidocaine may cause acute toxic effects of high systemic levels occur due to rapid absorption eg, application to areas below the vocal chords or overdosage (see Pharmacokinetics under Actions and Overdosage).
Systematic toxicity caused by lidocaine HCl is similar in nature to that observed with other local anesthetic agents. Pronounced acidosis or hypoxia in the patient may increase the risk and severity of toxic reactions. Such reactions involve the CNS and the CVS.
Central Nervous System Reactions: Characterized by numbness of the tongue, lightheadedness, dizziness, blurred vision and tremors, followed by drowsiness, convulsions, unconsciousness and possibly respiratory arrest.
Cardiovascular Reactions: Severe hypotension and bradycardia may occur following sympathetic block with central neural blocks. Cardiovascular reactions following high doses or the accidental intravascular injection of lidocaine are related to depression of the myocardium, decreased cardiac output, heart block hypotension, bradycardia, ventricular arrhythmias, including ventricular tachycardia and ventricular fibrillation and cardiac arrest. Hypoxia caused by convulsions and apnea may be a contributory factor in the cardiovascular reactions.
Neurological Reactions: The incidence of adverse neurological reactions associated with the use of local anesthetics is very low. Neurological reactions may be a function of the total dose of local anesthetic administered and are also dependent upon the particular drug used, the route of administration and the physical status of the patient. Many of these effects may be linked to local anesthetic techniques, with or without contribution by the drug. Neurological reactions following regional anesthesia have included persistent anesthesia, paresthesia, weakness, paralysis of the lower extremities and loss of sphincter control.
In rare cases, local anesthetic preparations have been associated with allergic reactions (in the most severe instances anaphylactic shock).
Pump Spray: Local irritation at the application site has been described. Following application to laryngeal mucosa before endotracheal intubation, reversible symptoms eg, sore throat, hoarseness and loss of voice have been reported. The use of lidocaine pump spray provides surface anesthesia during an endotracheal procedure but does not prevent post-intubation soreness.
Allergic Reactions: Allergic reactions (in the most severe instances anaphylactic shock) to local anesthetics of the amide type are rare (<0.1%).
Acute Systemic Toxicity: Lidocaine may cause acute toxic effects of high systemic levels occur due to rapid absorption eg, application to areas below the vocal chords or overdosage (see Pharmacokinetics under Actions and Overdosage).
Drug Interactions
With large doses of lidocaine, consideration should be given to the risk of additional systemic toxicity in patients receiving other local anesthetics or agents structurally related to local anesthetics eg, tocainide.
Lidocaine should be used with caution in patients receiving other local anesthetics or agents structurally related to amide-type local anesthetics eg, antiarrhythmics eg, mexiletin and tocainide since the toxic effects are additive.
Specific interaction studies with lidocaine and antiarrhythmic drug class III (eg, amiodarone) have not been performed, but caution is advised (see Cautions for Usage).
Drugs that reduce the clearance of lidocaine (eg, cimetidine or β-blockers) may cause potentially toxic plasma concentrations when lidocaine is given in repeated high doses over a long time period. Such interactions should therefore be of no clinical importance following short-term treatment with lidocaine (eg, Xylocaine Pump Spray) at recommended doses.
Lidocaine should be used with caution in patients receiving other local anesthetics or agents structurally related to amide-type local anesthetics eg, antiarrhythmics eg, mexiletin and tocainide since the toxic effects are additive.
Specific interaction studies with lidocaine and antiarrhythmic drug class III (eg, amiodarone) have not been performed, but caution is advised (see Cautions for Usage).
Drugs that reduce the clearance of lidocaine (eg, cimetidine or β-blockers) may cause potentially toxic plasma concentrations when lidocaine is given in repeated high doses over a long time period. Such interactions should therefore be of no clinical importance following short-term treatment with lidocaine (eg, Xylocaine Pump Spray) at recommended doses.
Caution For Usage
Instructions for Use, Handling and Disposal: Pump Spray: The spray nozzle is already bent to its final appearance and no further actions should be done before using the spray nozzle. The nozzle must not be shortened otherwise the spray function will be destroyed.
If cleaning of the nozzle is desired, the entire nozzle can be submerged in boiling water for 5 min. The nozzle can be autoclaved (20 min at 120°C).
If cleaning of the nozzle is desired, the entire nozzle can be submerged in boiling water for 5 min. The nozzle can be autoclaved (20 min at 120°C).
Storage
Injection: Store below 25 °C.
Pump Spray: Store at a temperature not exceeding 25°C. During storage at temperature below +8°C precipitation may occur. This precipitation is dissolved when warming up in room temperature.
Pump Spray: Store at a temperature not exceeding 25°C. During storage at temperature below +8°C precipitation may occur. This precipitation is dissolved when warming up in room temperature.
Action
Pharmacotherapeutic Group: Local Anesthethics. ATC Code: N01BB02.
Pharmacology: Injection: Xylocaine contains lidocaine which is a local anesthetic of the amide type. Lidocaine stabilizes the neuronal membrane and reversibly prevents the initiation and conduction of nerve impulses, thereby producing the local anesthetic action.
The onset time is 1-5 min following infiltration and 5-10 (to 15) min following other methods of administration. The duration of anesthesia is 1-2 (to 4) hrs, depending on the type of blockade and concentration of lidocaine. The addition of adrenaline will prolong the duration by up to 50%.
Lidocaine is metabolized mainly in the liver and excreted via the kidneys. Approximately 90% of administered lidocaine is excreted in the form of various metabolites while <10% is excreted unchanged. The principal metabolites, monoethylglycinexylidide and glycinexylidide also possess pharmacological activity. In normal adults the elimination t½ is 1.5-2 hrs after an IV dose.
Pump Spray: Lidocaine 10 mg/dose pump spray is intended for use on mucous membranes and provides an efficient surface anesthesia, which lasts approximately 10-15 min. The anesthesia usually occurs within 1-3 min depending on the area of application.
Local anesthesia is defined as a loss of sensation that is confined to a certain area of the body. All local anesthesia have a common mode of action. To produce their effect, they must block the propagation of impulses along nerve fibers. Such impulses are transmitted by rapid depolarization and repolarization within the nerve axons. These changes in polarity are due to the passage of sodium and potassium ions across the nerve membrane, through ionic channels within the membrane. Local anesthetics prevent the inward movement of sodium ions which initiate depolarization and as a consequence, the nerve fiber cannot propagate any impulses. The mechanism behind the activity of local anesthetics are not fully understood but a possible explanation is that the lipid-soluble base form diffuses across the lipid membrane into the cell. Inside the cell, a proportion of lidocaine ionizes again and enters the sodium channel to exert an inhibitory effect on sodium influx and consequently, on impulse conduction.
Pharmacokinetics: Lidocaine is absorbed following topical administration to mucus membranes, its rate and extent of absorption being dependent upon concentration and the total dose administered, the specific site of application and the duration of exposure. In general, the rate of absorption of local anesthetic agents following topical application is most rapid after intratracheal and bronchial administration. Such application may therefore result in rapidly rising or excessive plasma concentrations, with an increased risk of toxic symptoms eg, convulsions.
Lidocaine is also well-absorbed from the GIT, although little intact drug appears in the circulation because of biotransformation in the liver.
Normally about 64% of the lidocaine is bound to plasma proteins. Amide local anesthetics are mainly bound to α-1-acid glycoprotein but also to albumin. The α1 acid glycoprotein has high-affinity, low capacity sites and albumin has quantitatively less important low-affinity, high-capacity sites.
Lidocaine crosses the blood-brain and placental barriers, presumably by passive diffusion.
The main elimination pathway of lidocaine is by liver metabolism. The primary route of lidocaine in human is N-dealkylation to monoethylglycine xylidide (MEGX), followed by hydrolysis to 2,6-xylidine and hydroxylation to 4-hydroxy-2,6-xylidine. MEGX can also be further dealkylated to glycine xylidine (GX). The pharmacological/toxicological actions of MEGX and GX are similar to, but less potent than, those of lidocaine. GX has a longer t½ (about 10 hrs) than lidocaine and may accumulate during long-term administration. Approximately 90% of the lidocaine administered IV is excreted in the form of various metabolites and <10% is excreted unchanged in the urine.
The primary metabolite in urine is a conjugate of 4-hydroxy-2,6-xylidine, accounting for about 70-80% of the dose excreted in the urine.
The elimination t½ of lidocaine following an IV bolus injection is typically 1.5-2 hrs. Because of the rapid rate at which lidocaine is metabolized, any condition that affects liver function may alter lidocaine kinetics.
The t½ may be prolonged 2-fold or more in patients with liver dysfunction. Renal dysfunction does not affect lidocaine kinetics but may increase the accumulation of metabolites.
Factors eg, acidosis and the use of CNS stimulants and depressants affect the CNS levels of lidocaine required to produce overt systemic effects. Objective adverse manifestations become increasingly apparent with increasing venous plasma levels from 5-10 mg/L.
Toxicity: Preclinical Safety Data: In animal studies, the toxicity noted after high doses of lidocaine consisted of effects on the central nervous and cardiovascular systems. No drug related adverse effects were seen in reproduction toxicity studies, neither did lidocaine show a mutagenic potential in either in vitro or in vivo mutagenicity tests. Cancer studies have not been performed with lidocaine, due to the area and duration of therapeutic use for lidocaine.
Pharmacology: Injection: Xylocaine contains lidocaine which is a local anesthetic of the amide type. Lidocaine stabilizes the neuronal membrane and reversibly prevents the initiation and conduction of nerve impulses, thereby producing the local anesthetic action.
The onset time is 1-5 min following infiltration and 5-10 (to 15) min following other methods of administration. The duration of anesthesia is 1-2 (to 4) hrs, depending on the type of blockade and concentration of lidocaine. The addition of adrenaline will prolong the duration by up to 50%.
Lidocaine is metabolized mainly in the liver and excreted via the kidneys. Approximately 90% of administered lidocaine is excreted in the form of various metabolites while <10% is excreted unchanged. The principal metabolites, monoethylglycinexylidide and glycinexylidide also possess pharmacological activity. In normal adults the elimination t½ is 1.5-2 hrs after an IV dose.
Pump Spray: Lidocaine 10 mg/dose pump spray is intended for use on mucous membranes and provides an efficient surface anesthesia, which lasts approximately 10-15 min. The anesthesia usually occurs within 1-3 min depending on the area of application.
Local anesthesia is defined as a loss of sensation that is confined to a certain area of the body. All local anesthesia have a common mode of action. To produce their effect, they must block the propagation of impulses along nerve fibers. Such impulses are transmitted by rapid depolarization and repolarization within the nerve axons. These changes in polarity are due to the passage of sodium and potassium ions across the nerve membrane, through ionic channels within the membrane. Local anesthetics prevent the inward movement of sodium ions which initiate depolarization and as a consequence, the nerve fiber cannot propagate any impulses. The mechanism behind the activity of local anesthetics are not fully understood but a possible explanation is that the lipid-soluble base form diffuses across the lipid membrane into the cell. Inside the cell, a proportion of lidocaine ionizes again and enters the sodium channel to exert an inhibitory effect on sodium influx and consequently, on impulse conduction.
Pharmacokinetics: Lidocaine is absorbed following topical administration to mucus membranes, its rate and extent of absorption being dependent upon concentration and the total dose administered, the specific site of application and the duration of exposure. In general, the rate of absorption of local anesthetic agents following topical application is most rapid after intratracheal and bronchial administration. Such application may therefore result in rapidly rising or excessive plasma concentrations, with an increased risk of toxic symptoms eg, convulsions.
Lidocaine is also well-absorbed from the GIT, although little intact drug appears in the circulation because of biotransformation in the liver.
Normally about 64% of the lidocaine is bound to plasma proteins. Amide local anesthetics are mainly bound to α-1-acid glycoprotein but also to albumin. The α1 acid glycoprotein has high-affinity, low capacity sites and albumin has quantitatively less important low-affinity, high-capacity sites.
Lidocaine crosses the blood-brain and placental barriers, presumably by passive diffusion.
The main elimination pathway of lidocaine is by liver metabolism. The primary route of lidocaine in human is N-dealkylation to monoethylglycine xylidide (MEGX), followed by hydrolysis to 2,6-xylidine and hydroxylation to 4-hydroxy-2,6-xylidine. MEGX can also be further dealkylated to glycine xylidine (GX). The pharmacological/toxicological actions of MEGX and GX are similar to, but less potent than, those of lidocaine. GX has a longer t½ (about 10 hrs) than lidocaine and may accumulate during long-term administration. Approximately 90% of the lidocaine administered IV is excreted in the form of various metabolites and <10% is excreted unchanged in the urine.
The primary metabolite in urine is a conjugate of 4-hydroxy-2,6-xylidine, accounting for about 70-80% of the dose excreted in the urine.
The elimination t½ of lidocaine following an IV bolus injection is typically 1.5-2 hrs. Because of the rapid rate at which lidocaine is metabolized, any condition that affects liver function may alter lidocaine kinetics.
The t½ may be prolonged 2-fold or more in patients with liver dysfunction. Renal dysfunction does not affect lidocaine kinetics but may increase the accumulation of metabolites.
Factors eg, acidosis and the use of CNS stimulants and depressants affect the CNS levels of lidocaine required to produce overt systemic effects. Objective adverse manifestations become increasingly apparent with increasing venous plasma levels from 5-10 mg/L.
Toxicity: Preclinical Safety Data: In animal studies, the toxicity noted after high doses of lidocaine consisted of effects on the central nervous and cardiovascular systems. No drug related adverse effects were seen in reproduction toxicity studies, neither did lidocaine show a mutagenic potential in either in vitro or in vivo mutagenicity tests. Cancer studies have not been performed with lidocaine, due to the area and duration of therapeutic use for lidocaine.
MedsGo Class
Anaesthetics - Local & General
Features
Brand
Xylocaine
Full Details
Dosage Strength
10 mg / dose (10%)
Drug Ingredients
- Lidocaine
Drug Packaging
Pump Spray 50mL
Generic Name
Lidocaine
Dosage Form
Pump Spray
Registration Number
DR-1860
Drug Classification
Prescription Drug (RX)
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