Version May 2024
Note: Dosage varies with the anesthetic procedure, degree of anesthesia needed, vascularity of tissue, duration of anesthesia required, and physical condition of patient. Always use the lowest effective dose along with careful aspiration.
Dental anesthesia, infiltration, or conduction block: Usual dose: Mepivacaine 34 mg (1.7 mL) per site or mepivacaine 180 mg (9 mL) for entire oral cavity; maximum cumulative mepivacaine dose: 6.6 mg/kg or 400 mg (whichever is less) during any single dental sitting.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
There are no dosage adjustments provided in the manufacturer's labeling; use with caution.
There are no dosage adjustments provided in the manufacturer's labeling; use with caution. Patients with severe hepatic disease, because of their inability to metabolize local anesthetics normally, are at a greater risk of developing toxic plasma concentrations.
Refer to adult dosing; reduce dose consistent with age and physical status.
Note: Dosage varies with the anesthetic procedure, degree of anesthesia needed, vascularity of tissue, duration of anesthesia required, and physical condition of patient. Always use the lowest effective dose along with careful aspiration.
Dental anesthesia, infiltration, or conduction block: Children and Adolescents: Maximum dosage must be carefully calculated on the basis of patient's weight. Manufacturer recommends a maximum mepivacaine dose of 6.6 mg/kg, but must not exceed 180 mg as a 2% solution. The American Academy of Pediatric Dentistry (AAPD) recommends a maximum mepivacaine dose of 4.4 mg/kg or a maximum total dose of 300 mg in any single dental sitting (Ref).
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
There are no dosage adjustments provided in the manufacturer's labeling; use with caution.
There are no dosage adjustments provided in the manufacturer's labeling; use with caution. Patients with severe hepatic disease, because of their inability to metabolize local anesthetics normally, are at a greater risk of developing toxic plasma concentrations.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Degree of adverse effects in the CNS and cardiovascular system is directly related to the blood levels of mepivacaine. The effects below are more likely to occur after systemic administration rather than infiltration. Also see mepivacaine.
Frequency not defined:
Central nervous system: Disorientation, dizziness, drowsiness, excitement, loss of consciousness, nervousness, seizure
Hypersensitivity: Hypersensitivity reaction
Neuromuscular & skeletal: Tremor
Ophthalmic: Blurred vision
<1%, postmarketing, and/or case reports: Nonimmune anaphylaxis
Hypersensitivity to mepivacaine, levonordefrin, local anesthetics of the amide-type, or any component of the formulation
Concerns related to adverse effects:
• CNS toxicity: Careful and constant monitoring of the patient's state of consciousness should be done following each local anesthetic injection; at such times, restlessness, anxiety, tinnitus, dizziness, blurred vision, tremors, depression, or drowsiness may be early warning signs of CNS toxicity. Treatment is primarily symptomatic and supportive.
• Methemoglobinemia: Has been reported with local anesthetics; clinically significant methemoglobinemia requires immediate treatment along with discontinuation of the anesthetic and other oxidizing agents. Onset may be immediate or delayed (hours) after anesthetic exposure. Patients with glucose-6-phosphate dehydrogenase deficiency, congenital or idiopathic methemoglobinemia, cardiac or pulmonary compromise, exposure to oxidizing agents or their metabolites, or infants <6 months of age are more susceptible and should be closely monitored for signs and symptoms of methemoglobinemia (eg, cyanosis, headache, rapid pulse, shortness of breath, light-headedness, fatigue).
• Respiratory arrest: Local anesthetics have been associated with rare occurrences of sudden respiratory arrest.
• Seizures: Convulsions due to systemic toxicity leading to cardiac arrest have also been reported, presumably following unintentional intravascular injection.
Disease-related concerns:
• Cardiovascular disease: Use with caution in patients with arteriosclerotic heart disease, cerebral vascular insufficiency, heart block, hypertension, and ischemic heart disease; minimal amounts of vasoconstrictor should be used in this patient population.
• Diabetes: Use with caution in patients with diabetes.
• Hepatic impairment: Use with caution in patients with hepatic impairment.
• Hyperthyroidism: Use with caution in patients with hyperthyroidism.
• Renal impairment: Use with caution in patients with renal impairment.
Special populations:
• Acutely ill patients: Use with caution in acutely ill patients; reduce dose consistent with age and physical status.
• Debilitated patients: Use with caution in debilitated patients; reduce dose consistent with age and physical status.
• Older adult: Use with caution in the elderly; reduce dose consistent with age and physical status.
• Pediatric: Use with caution in children; reduce dose consistent with age and physical status.
Dosage form specific issues:
• Potassium metabisulfite: Some preparations may contain potassium metabisulfite which may cause severe hypersensitivity reactions (anaphylaxis) in some individuals; use caution in patients with asthma.
Other warnings/precautions:
• Administration: Intravascular injections should be avoided; aspiration should be performed prior to administration; the needle must be repositioned until no return of blood can be elicited by aspiration; however, absence of blood in the syringe does not guarantee that intravascular injection has been avoided. Use with caution when there is inflammation and/or sepsis in the region of the proposed injection.
• Appropriate dosing: To avoid serious adverse effects and high plasma levels, the lowest dosage resulting in effective anesthesia should be administered. Repeated doses may cause significant increases in blood levels with each repeated dose due to the possibility of accumulation of the drug or its metabolites. Tolerance to elevated blood levels varies with patient status.
• Trained personnel: Dental practitioners using local anesthetic agents should be well trained in diagnosis and management of emergencies that may arise from the use of these agents. Resuscitative equipment, oxygen, and other resuscitative drugs should be available for immediate use.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Injection, solution [for dental use]:
Carbocaine 2% with Neo-Cobefrin: Mepivacaine hydrochloride 2% and levonordefrin 1:20,000 (1.7 mL) [contains edetate disodium, potassium metabisulfite]
Scandonest 2% L: Mepivacaine hydrochloride 2% and levonordefrin 1:20,000 (1.7 mL) [contains edetate disodium, potassium metabisulfite]
No
Administer slowly, with frequent aspirations before and during the injection to avoid intravascular injection. Use with caution when there is inflammation and/or sepsis in the region of the proposed injection.
Dental injection: Administer slowly, with frequent aspirations before and during the injection to avoid intravascular injection. Use with caution when there is inflammation and/or sepsis in the region of the proposed injection.
Dental anesthesia: Production of local anesthesia for dental procedures by infiltration or nerve block in adult and pediatric patients
None known.
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Alpha1-Blockers: May diminish the vasoconstricting effect of Alpha-/Beta-Agonists. Similarly, Alpha-/Beta-Agonists may antagonize Alpha1-Blocker vasodilation. Risk C: Monitor therapy
Atomoxetine: May enhance the hypertensive effect of Sympathomimetics. Atomoxetine may enhance the tachycardic effect of Sympathomimetics. Risk C: Monitor therapy
Benzylpenicilloyl Polylysine: Alpha-/Beta-Agonists may diminish the diagnostic effect of Benzylpenicilloyl Polylysine. Management: Consider use of a histamine skin test as a positive control to assess a patient's ability to mount a wheal and flare response. Risk D: Consider therapy modification
Bromocriptine: May enhance the hypertensive effect of Alpha-/Beta-Agonists. Management: Consider alternatives to this combination when possible. If combined, monitor for hypertension and tachycardia, and do not coadminister these agents for more than 10 days. Risk D: Consider therapy modification
BUPivacaine: Local Anesthetics may enhance the adverse/toxic effect of BUPivacaine. Management: Avoid using any additional local anesthetics within 96 hours after insertion of the bupivacaine implant (Xaracoll) or bupivacaine and meloxicam periarticular solution (Zynrelef) or within 168 hours after subacromial infiltration (Posimir brand). Risk C: Monitor therapy
BUPivacaine (Liposomal): Local Anesthetics may enhance the adverse/toxic effect of BUPivacaine (Liposomal). Management: Liposomal bupivacaine should not be administered with local anesthetics, but may be administered 20 minutes or more after lidocaine. Avoid all local anesthetics within 96 hours after administration of liposomal bupivacaine. Risk X: Avoid combination
Cannabinoid-Containing Products: May enhance the tachycardic effect of Sympathomimetics. Risk C: Monitor therapy
Chloroprocaine (Systemic): May enhance the hypertensive effect of Alpha-/Beta-Agonists. Risk C: Monitor therapy
Cocaine (Topical): May enhance the hypertensive effect of Sympathomimetics. Management: Consider alternatives to use of this combination when possible. Monitor closely for substantially increased blood pressure or heart rate and for any evidence of myocardial ischemia with concurrent use. Risk D: Consider therapy modification
Doxofylline: Sympathomimetics may enhance the adverse/toxic effect of Doxofylline. Risk C: Monitor therapy
Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates): May enhance the vasoconstricting effect of Alpha-/Beta-Agonists. Risk X: Avoid combination
Guanethidine: May enhance the arrhythmogenic effect of Sympathomimetics. Guanethidine may enhance the hypertensive effect of Sympathomimetics. Risk C: Monitor therapy
Hyaluronidase: May enhance the vasoconstricting effect of Alpha-/Beta-Agonists. Management: Do not use hyaluronidase to enhance the dispersion or absorption of alpha-/beta-agonists. Use of hyaluronidase for other purposes in patients receiving alpha-/beta-agonists may be considered as clinically indicated. Risk D: Consider therapy modification
Kratom: May enhance the adverse/toxic effect of Sympathomimetics. Risk X: Avoid combination
Levothyroxine: May enhance the adverse/toxic effect of Sympathomimetics. Specifically, the risk of coronary insufficiency may be increased in patients with coronary artery disease. Levothyroxine may enhance the therapeutic effect of Sympathomimetics. Sympathomimetics may enhance the therapeutic effect of Levothyroxine. Risk C: Monitor therapy
Lisuride: May enhance the hypertensive effect of Alpha-/Beta-Agonists. Risk X: Avoid combination
Methemoglobinemia Associated Agents: May enhance the adverse/toxic effect of Local Anesthetics. Specifically, the risk for methemoglobinemia may be increased. Risk C: Monitor therapy
Monoamine Oxidase Inhibitors: May enhance the hypertensive effect of Levonordefrin. Risk X: Avoid combination
Neuromuscular-Blocking Agents: Local Anesthetics may enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents. Risk C: Monitor therapy
Ozanimod: May enhance the hypertensive effect of Sympathomimetics. Risk C: Monitor therapy
Pergolide: May enhance the hypertensive effect of Alpha-/Beta-Agonists. Risk C: Monitor therapy
Propranolol: May increase the serum concentration of Mepivacaine. Risk C: Monitor therapy
Serotonin/Norepinephrine Reuptake Inhibitors: May enhance the tachycardic effect of Alpha-/Beta-Agonists. Serotonin/Norepinephrine Reuptake Inhibitors may enhance the vasopressor effect of Alpha-/Beta-Agonists. Management: If possible, avoid coadministration of direct-acting alpha-/beta-agonists and serotonin/norepinephrine reuptake inhibitors. If coadministered, monitor for increased sympathomimetic effects (eg, increased blood pressure, chest pain, headache). Risk D: Consider therapy modification
Solriamfetol: Sympathomimetics may enhance the hypertensive effect of Solriamfetol. Sympathomimetics may enhance the tachycardic effect of Solriamfetol. Risk C: Monitor therapy
Spironolactone: May diminish the vasoconstricting effect of Alpha-/Beta-Agonists. Risk C: Monitor therapy
Sympathomimetics: May enhance the adverse/toxic effect of other Sympathomimetics. Risk C: Monitor therapy
Technetium Tc 99m Tilmanocept: Local Anesthetics may diminish the diagnostic effect of Technetium Tc 99m Tilmanocept. Management: Avoid mixing and simultaneously co-injecting technetium Tc 99m tilmanocept with local anesthetics. This interaction does not appear to apply to other uses of these agents in combination. Risk C: Monitor therapy
Tedizolid: May enhance the hypertensive effect of Sympathomimetics. Tedizolid may enhance the tachycardic effect of Sympathomimetics. Risk C: Monitor therapy
Tricyclic Antidepressants: May enhance the vasopressor effect of Alpha-/Beta-Agonists. Management: Avoid, if possible, the use of alpha-/beta-agonists in patients receiving tricyclic antidepressants. If combined, monitor for evidence of increased pressor effects and consider reductions in initial dosages of the alpha-/beta-agonist. Risk D: Consider therapy modification
Vasopressin: Alpha-/Beta-Agonists (Direct-Acting) may enhance the hypertensive effect of Vasopressin. The effect of other hemodynamic parameters may also be enhanced. Risk C: Monitor therapy
Animal reproduction studies have not been conducted with this combination.
It is not known if mepivacaine or levonordefrin is present in breast milk. The manufacturer recommends that caution be exercised when administering mepivacaine/levonordefrin to breastfeeding women. Usual infiltration doses of mepivacaine with levonordefrin given to breastfeeding mothers has not been shown to affect the health of the breastfed infant.
Mepivacaine: Local anesthetics bind selectively to the intracellular surface of sodium channels to block influx of sodium into the axon. As a result, depolarization necessary for action potential propagation and subsequent nerve function is prevented. The block at the sodium channel is reversible. When drug diffuses away from the axon, sodium channel function is restored and nerve propagation returns.
Levonordefrin: Prolongs the duration of the anesthetic actions of mepivacaine by causing vasoconstriction (alpha-adrenergic receptor agonist) of the vasculature surrounding the nerve axons. This prevents the diffusion of mepivacaine away from the nerves resulting in a longer retention in the axon.
Onset of action: Upper jaw: 30 to 120 seconds; Lower jaw: 1 to 4 minutes
Duration: Upper jaw: 1 to 2.5 hours; Lower jaw: 2.5 to 5.5 hours
Protein binding: Mepivacaine: ~75%
Metabolism: Mepivacaine: Primarily hepatic via N-demethylation, hydroxylation, and glucuronidation
Excretion: Mepivacaine: Urine (90% to 95% as metabolites)
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