Levonordefrin — Active Pharmaceutical Ingredient

Levonordefrin is an active pharmaceutical ingredient found in 7 FDA-approved drug products. Forms: INJECTABLE. Routes: INJECTION.

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Levonordefrin (7 brand names, 1 dosage form, 1 route)

Available dosage forms: INJECTABLE.

Routes of administration: INJECTION.

Brand Names

  • ARESTOCAINE HYDROCHLORIDE W/ LEVONORDEFRIN
  • CARBOCAINE W/ NEO-COBEFRIN
  • ISOCAINE HYDROCHLORIDE W/ LEVONORDEFRIN
  • MEPIVACAINE HYDROCHLORIDE W/ LEVONORDEFRIN
  • POLOCAINE W/ LEVONORDEFRIN
  • RAVOCAINE AND NOVOCAIN W/ NEO-COBEFRIN
  • SCANDONEST L

Indications and Usage

ISOCAINE is indicated for production of local anesthesia for dental procedures by infiltration or nerve block in adults and pediatric patients.

Dosage and Administration

As with all local anesthetics, the dose varies and depends upon the area to be anesthetized, the vascularity of the tissues, individual tolerance and the technique of anesthesia. The lowest dose needed to provide effective anesthesia should be administered. For specific techniques and procedures refer to standard dental manuals and textbooks.For infiltration and block injections in the upper or lower jaw, the average dose of 1 cartridge will usually suffice.Each cartridge contains 1.8 mL (36 mg of 2% or 54 mg of 3%).Five cartridges (180 mg of the 2% solution or 270 mg of the 3% solution) are usually adequate to effect anesthesia of the entire oral cavity. Whenever a larger dose seems to be necessary for an extensive procedure, the maximum dose should be calculated according to the patient’s weight. A dose of up to 3 mg per pound of body weight may be administered. At any single dental sitting the total dose for all injected sites should not exceed 400 mg in adults.The maximum pediatric dose should be carefully calculated.Maximum dose for Pediatric Patient =Pediatric Patient’s Weight (lbs.) × Maximum Recommended Dose 150 for Adults (400 mg.)The following table, approximating these calculations, may also be used as a guide. Maximum Allowable Dosage 3% Mepivacaine (Plain)2% Mepivacaine 1:20,000 Levonordefrin 3 mg/lb 270 mg max.)3 mg/lb (180 mg max.) Weight (lb.)MgNumber of CartridgesMgNumber of Cartridges 20601.1601.6 30901.7902.5 401202.21203.3 501502.81504.2 601803.31805.0 802404.41805.0 1002705.01805.0 1202705.01805.0 Adapted from Malamed, Stanley F: Handbook of medical emergencies in the dental office, ed. 2, St. Louis, 1982. The C.V. Mosby Co.When using ISOCAINE for infiltration or regional block anesthesia, injection should always be made slowly and with frequent aspiration.Any unused portion of a cartridge should be discarded.Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution

Contraindications

ISOCAINE is contraindicated in patients with a known hypersensitivity to amide type local anesthetics.

Adverse Reactions

Systemic adverse reactions involving the central nervous system and the cardiovascular system usually result from high plasma levels due to excessive dosage, rapid absorption, or inadvertent intravascular injection.A small number of reactions may result from hypersensitivity, idiosyncrasy or diminished tolerance to normal dosage on the part of the patient.Reactions involving the central nervous system are characterized by excitation and/or depression. Nervousness, dizziness, blurred vision, or tremors may occur followed by drowsiness, convulsions, unconsciousness, and possible respiratory arrest. Since excitement may be transient or absent, the first manifestations may be drowsiness merging into unconsciousness and respiratory arrest.Cardiovascular reactions are depressant. They may be the result of direct drug effect or more commonly in dental practice, the result of vasovagal reaction, particularly if the patient is in the sitting position. Failure to recognize premonitory signs such as sweating, feeling of faintness, changes in pulse or sensorium may result in progressive cerebral hypoxia and seizure or serious cardiovascular catastrophe. Management consists of placing the patient in the recumbent position and administration of oxygen. Vasoactive drugs such as Ephedrine or Methoxamine may be administered intravenously.Allergic reactions are rare and may occur as a result of sensitivity to the local anesthetic and are characterized by cutaneous lesions of delayed onset or urticaria, edema and other manifestations of allergy. The detection of sensitivity by skin testing is of limited value. As with other local anesthetics, anaphylactoid reactions to ISOCAINE have occurred rarely. The reaction may be abrupt and severe and is not usually dose related. Localized puffiness and swelling may occur.

Drug Interactions

The administration of local anesthetic solutions containing vasopressors, such as Levonordefrin, Epinephrine or Norepinephrine, to patients receiving tricyclic antidepressants or monoamine oxidase inhibitors may produce severe, prolonged hypertension. Concurrent use of these agents should generally be avoided. In situations when concurrent therapy is necessary, careful patient monitoring is essential.Concurrent administration of vasopressor drugs and of ergot-type oxytocic drugs may cause severe, persistent hypertension or cerebrovascular accidents.Phenothiazines and butyrophenones may reduce or reverse the pressor effect of Epinephrine.Solutions containing a vasoconstrictor should be used cautiously in the presence of disease which may adversely affect the patient’s cardiovascular system. Serious cardiac arrhythmias may occur if preparations containing a vasoconstrictor are employed in patients during or following the administration of potent inhalation anesthetics.MEPIVACAINE SHOULD BE USED WITH CAUTION IN PATIENTS WITH KNOWN DRUG ALLERGIES AND SENSITIVITIES. A thorough history of the patient’s prior experience with Mepivacaine or other local anesthetics as well as concomitant or recent drug use should be taken (see CONTRAINDICATIONS). Patients allergic to methylparaben or para-aminobenzoic acid derivatives (procaine, tetracaine, benzocaine, etc.) have not shown cross-sensitivity to agents of the amide type such as Mepivacaine. Since Mepivacaine is metabolized in the liver and excreted by the kidneys, it should be used cautiously in patients with liver and renal disease.

Overdosage

Treatment of a patient with toxic manifestations consists of assuring and maintaining a patient airway and supporting ventilation (respiration) as required. This usually will be sufficient in the management of most reactions. Should a convulsion persist despite ventilatory therapy, small increments of anticonvulsive agents may be given intravenously, such as benzodiazephine (e.g., diazepam) or ultrashort-acting barbiturates (e.g., thiopental or thiamylal) or short-acting barbiturates (e.g., pentobarbital or secobarbital). Cardiovascular depression may require circulatory assistance with intravenous fluids and/or vasopressor (e.g., Ephedrine) as dictated by the clinical situation. Allergic reactions should be managed by conventional means.IV and SC LD50’s in mice for Mepivacaine Hydrochloride 3% are 33 and 258 mg/kg respectively. The acute IV and SC LD50’s in mice for Mepivacaine Hydrochloride 2% with Levonordefrin 1:20,000 are 30 and 184 mg/kg respectively.

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