Source:http://www4.wiwiss.fu-berlin.de/dailymed/resource/drugs/1263
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Lidocaine Hydrochloride (Solution)
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| dailymed-instance:dosage |
When Lidocaine Hydrochloride Topical Solution is used concomitantly with other products containing lidocaine, the total dose contributed by all formulations must be kept in mind. The dosage varies and depends upon the area to be anesthetized, vascularity of the tissues, individual tolerance, and the technique of anesthesia. The lowest dosage needed to provide effective anesthesia should be administered. Dosages should be reduced for children and for elderly and debilitated patients. The maximum dose should not exceed 4.5 mg/kg (2 mg/lb) of body weight. Although the incidence of adverse effects with Lidocaine Hydrochloride is quite low, caution should be exercised, particularly when employing large volumes, since the incidence of adverse effects is directly proportional to the total dose of local anesthetic agent administered. The dosages recommended below are for normal, healthy adults: When used as a spray, or when applied by means of cotton applicators or packs, as when instilled into a cavity, the suggested dosage of Lidocaine Hydrochloride Topical Solution is 1 to 5 mL (40 to 200 mg lidocaine hydrochloride), i.e., 0.6���3.0 mg/kg or 0.3���1.5 mg/lb body weight. NOTE: The solution may be applied with a sterile swab which is discarded after a single use. When spraying, transfer the solution from the original container to an atomizer.
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Lidocaine Hydrochloride Topical Solution, USP 4% contains a local anesthetic agent and is administered topically. See INDICATIONS for specific uses. Lidocaine Hydrochloride Topical Solution contains lidocaine hydrochloride monohydrate, which is chemically designated as 2-(Diethylamino)-2',6'-acetoxylidide monohydrochloride monohydrate and has the following structural formula: Each mL contains:Lidocaine Hydrochloride Monohydrate, USP . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 40 mg Inactive Ingredients: methylparaben, propylene glycol and purified water. It may also contain sodium hydroxide for pH adjustment. The pH range is between 5.0 and 7.0. An aqueous solution for topical use only. NOT FOR INJECTION.
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Mechanism of Action: Lidocaine stabilizes the neuronal membrane by inhibiting the ionic fluxes required for the initiation and conduction of impulses, thereby effecting local anesthetic action.<br/>Hemodynamics: Excessive blood levels may cause changes in cardiac output, total peripheral resistance, and mean arterial pressure. These changes may be attributable to a direct depressant effect of the local anesthetic agent on various components of the cardiovascular system.<br/>Pharmacokinetics and Metabolism: Lidocaine may be absorbed following topical administration to mucous membranes, its rate of absorption and percent of dose absorbed depending upon concentration and total dose administered, the specific site of application and duration of exposure. In general, the rate of absorption of local anesthetic agents following topical application occurs most rapidly after intratracheal administration. Lidocaine is well-absorbed from the gastrointestinal tract, but little intact drug appears in the circulation because of biotransformation in the liver. Lidocaine is metabolized rapidly by the liver, and metabolites and unchanged drug are excreted by the kidney. Biotransformation includes oxidative N-dealkylation, ring hydroxylation, cleavage of the amide linkage, and conjugation. N-dealkylation, a major pathway of biotransformation, yields the metabolites monoethylglycinexylidide and glycinexylidide. The pharmacological/toxicological actions of these metabolites are similar to, but less potent than, those of lidocaine. Approximately 90% of lidocaine administered is excreted in the form of various metabolites, and less than 10% is excreted unchanged. The primary metabolite in urine is a conjugate of 4-hydroxy-2, 6-dimethylaniline. The plasma binding of lidocaine is dependent on drug concentration, and the fraction bound decreases with increasing concentration. At concentrations of 1 to 4 mcg of free base per mL, 60 to 80 percent of lidocaine is protein bound. Binding is also dependent on the plasma concentration of the alpha-1-acid glycoprotein. Lidocaine crosses the blood-brain and placental barriers, presumably by passive diffusion. Studies of lidocaine metabolism following intravenous bolus injections have shown that the elimination half-life of this agent is typically 1.5 to 2.0 hours. Because of the rapid rate at which lidocaine is metabolized, any condition that affects liver function may alter lidocaine kinetics. The half-life may be prolonged two-fold or more in patients with liver dysfunction. Renal dysfunction does not affect lidocaine kinetics but may increase the accumulation of metabolites. Factors such as 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 above 6.0 mcg free base per mL. In the rhesus monkey arterial blood levels of 18���21 mcg/mL have been shown to be threshold for convulsive activity.
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Lidocaine is contraindicated in patients with a known history of hypersensitivity to local anesthetics of the amide type, or to other components of Lidocaine Hydrochloride Topical Solution.
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Lidocaine Hydrochloride Topical Solution, USP 4% is supplied in 50 mL and 100 mL bottles. An aqueous solution for topical application. NOT FOR INJECTION.
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| dailymed-instance:overdosag... |
Acute emergencies from local anesthetics are generally related to high plasma levels encountered during therapeutic use of local anesthetics. .<br/>Management of Local Anesthetic Emergencies: The first consideration is prevention, best accomplished by careful and constant monitoring of cardiovascular and respiratory vital signs and the patient's state of consciousness after each local anesthetic administration. At the first sign of change, oxygen should be administered. The first step in the management of convulsions consists of immediate attention to the maintenance of a patent airway and assisted or controlled ventilation with oxygen and a delivery system capable of permitting immediate positive airway pressure by mask. Immediately after the institution of these ventilatory measures, the adequacy of the circulation should be evaluated, keeping in mind that drugs used to treat convulsions sometimes depress the circulation when administered intravenously. Should convulsions persist despite adequate respiratory support, and if the status of the circulation permits, small increments of an ultra-short acting barbiturate (such as thiopental or thiamylal) or a benzodiazepine (such as diazepam) may be administered intravenously. The clinician should be familiar, prior to use of local anesthetics, with these anticonvulsant drugs. Supportive treatment of circulatory depression may require administration of intravenous fluids and, when appropriate, a vasopressor as directed by the clinical situation (e.g., ephedrine). If not treated immediately, both convulsions and cardiovascular depression can result in hypoxia, acidosis, bradycardia, arrhythmias and cardiac arrest. If cardiac arrest should occur, standard cardiopulmonary resuscitative measures should be instituted. Dialysis is of negligible value in the treatment of acute overdosage with lidocaine. The intravenous LDof lidocaine hydrochloride in female mice is 26 (21���31) mg/kg and the
subcutaneous LDis 264 (203���304) mg/kg.
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Lidocaine Hydrochloride
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Lidocaine Hydrochloride (Solution)
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| dailymed-instance:adverseRe... |
Adverse experiences following the administration of lidocaine are similar in nature to those observed with other amide local anesthetic agents. These adverse experiences are, in general, dose-related and may result from high plasma levels caused by excessive dosage or rapid absorption, or may result from a hypersensitivity, idiosyncrasy or diminished tolerance on the part of the patient. Serious adverse experiences are generally systemic in nature. The following types are those most commonly reported:<br/>Central Nervous System: CNS manifestations are excitatory and/or depressant and may be
characterized by lightheadedness, nervousness, apprehension, euphoria, confusion, dizziness, drowsiness, tinnitus, blurred or double vision, vomiting, sensations of heat, cold or numbness, twitching, tremors, convulsions, unconsciousness, respiratory depression and arrest. The excitatory manifestations may be very brief or may not occur at all, in which case the first manifestation of toxicity may be drowsiness merging into unconsciousness and respiratory arrest. Drowsiness following the administration of lidocaine is usually an early sign of a high blood level of the drug and may occur as a consequence of rapid absorption.<br/>Cardiovascular System: Cardiovascular manifestations are usually depressant and are characterized by bradycardia, hypotension, and cardiovascular collapse, which may lead to cardiac arrest.<br/>Allergic: Allergic reactions are characterized by cutaneous lesions, urticaria, edema or anaphylactoid reactions. Allergic reactions may occur as a result of sensitivity either to the local anesthetic agent or to other ingredients in the formulation. Allergic reactions as a result of sensitivity to lidocaine are extremely rare and, if they occur, should be managed by conventional means. The detection of sensitivity by skin testing is of doubtful value.
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Lidocaine Hydrochloride Topical Solution is indicated for the production of topical anesthesia of accessible mucous membranes of the oral and nasal cavities and proximal portions of the digestive tract.
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Lidocaine Hydrochloride
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