MEDICAINE AVEC ADRENALINE

A local anesthetic that is chemically related to bupivacaine but pharmacologically related to lidocaine.

It is indicated for infiltration, nerve block, and epidural anesthesia.

Mepivacaine is effective topically only in large doses and therefore should not be used by this route. (From AMA Drug Evaluations, 1994, p168).

For production of local or regional analgesia and anesthesia by local infiltration, peripheral nerve block techniques, and central neural techniques including epidural and caudal blocks.

Mepivicaine is an amide local anesthetic.

Mepivicaine as a reasonably rapid onset and medium duration and is known by the proprietary names as Carbocaine and Polocaine.

Mepivicaine is used in local infiltration and regional anesthesia.

Systemic absorption of local anesthetics produces effects on the cardiovascular and central nervous systems.

At blood concentrations achieved with normal therapeutic doses, changes in cardiac conduction, excitability, refractoriness, contractility, and peripheral vascular resistance are minimal.

Absorbed locally.

The rate of systemic absorption of local anesthetics is dependent upon the total dose and concentration of drug administered, the route of administration, the vascularity of the administration site, and the presence or absence of epinephrine in the anesthetic solution.

Rapidly metabolized, with only a small percentage of the anesthetic (5 percent to 10 percent) being excreted unchanged in the urine.

The liver is the principal site of metabolism, with over 50% of the administered dose being excreted into the bile as metabolites.

It is rapidly metabolized, with only a small percentage of the anesthetic (5 percent to 10 percent) being excreted unchanged in the urine.The liver is the principal site of metabolism, with over 50% of the administered dose being excreted into the bile as metabolites.

The half-life of mepivacaine in adults is 1.9-3.2 hours and in neonates 8.7-9 hours.

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The mean seizure dosage of mepivacaine in rhesus monkeys was found to be 18.8 mg/kg with mean arterial plasma concentration of 24.4 µg/mL.

The intravenous and subcutaneous

LD in mice is 23 mg/kg to 35 mg/kg and 280 mg/kg respectively.

Reactions resulting in fatality have occurred on rare occasions with the use of local anesthetics, even in the absence of a history of hypersensitivity.

Fatalities may occur with use of local anesthetics in the head and neck region as the result of retrograde arterial flow to vital CNS areas even when maximum recommended doses are observed.

The practitioner should be alert to early evidence of alteration in sensorium or vital signs.

The solution which contains a vasoconstrictor (Mepivacaine HCl 2% (20 mg/mL)) should be used with extreme caution for patients whose medical history and physical evaluation suggest the existence of hypertension, arteriosclerotic heart disease, cerebral vascular insufficiency, heart block, thyrotoxicosis and diabetes, etc.

The solution which contains a vasoconstrictor (Mepivacaine HCl 2% (20 mg/mL)) also contains potassium metabisulfite, a sulfite that may cause allergic-type reactions including anaphylactic symptoms and lifethreatening or less severe asthmatic episodes in certain susceptible people.

The overall prevalence of sulfite sensitivity in the general population is unknown and probably low.

Sulfite sensitivity is seen more frequently in asthmatic than in non-asthmatic people.

HCl 3% (30 mg/mL) is SULFITE FREE.

Mepivacaine, along with other local anesthetics, is capable of producing methemoglobinemia.

The clinical signs of methemoglobinemia are cyanosis of the nail beds and lips, fatigue and weakness.

If methemoglobinemia does not respond to administration of oxygen, administration of methylene blue intravenously 1-2 mg/kg body weight over a 5 minute period is recommended.

Association has made the following recommendations regarding the use of local anesthetics with vasoconstrictors in patients with ischemic heart disease: “Vasoconstrictor agents should be used in local anesthesia solutions during dental practice only when it is clear that the procedure will be shortened or the analgesia rendered more profound.

When a vasoconstrictor is indicated, extreme care should be taken to avoid intravascular injection.

The minimum possible amount of vasoconstrictor should be used.” (Kaplan, EL, editor: Cardiovascular disease in dental practice, Dallas 1986, American Heart Association). Methemoglobinemia: Cases of methemoglobinemia have been reported in association with local anesthetic use; MEPIVACAINE, along with other local anesthetics, is capable of producing this condition.

Although all patients are at risk for methemoglobinemia, patients with glucose-6-phosphate dehydrogenase deficiency, congenital or idiopathic methemoglobinemia, cardiac or pulmonary compromise, infants under 6 months of age, and concurrent exposure to oxidizing agents or their metabolites are more susceptible to developing clinical manifestations of the condition.

If local anesthetics must be used in these patients, close monitoring for symptoms and signs of methemoglobinemia is recommended.

Signs of methemoglobinemia may occur immediately or may be delayed some hours after exposure, and are characterized by cyanosis of the skin, nail beds and lips, and/or abnormal coloration of the blood, fatigue and weakness.

Methemoglobin levels may continue to rise; therefore, immediate treatment is required to avert more serious central nervous system and cardiovascular adverse effects, including seizures, coma, arrhythmias, and death.

MEPIVACAINE and any other oxidizing agents.

Depending on the severity of the signs and symptoms, patients may respond to supportive care, i.e., oxygen therapy, hydration.

If methemoglobinemia does not respond to administration of oxygen, a more severe clinical presentation may require treatment with methylene blue exchange transfusion, or hyperbaric oxygen.

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

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 1.7 mL (34 mg of 2% or 51 mg of 3%). 5.3 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 population = Child's Weight (lbs). 150 × Maximum Recommended Dose for Adults (400 mg) The following table, approximating these calculations, may also be used as a guide.

This table is based upon a recommended maximum for larger pediatric population of 5.3 cartridges (the maximum recommended adult dose) during any single dental sitting, regardless of the pediatric patient's weight or (for 2% mepivacaine) calulated maximum amount of drug: Maximum Allowable Dosage 3% Mepivacaine 2% Mepivacaine 1:20,000 Levonordefrin 3 mg/lb 3mg/lb (270 mg max). (180 mg max). Weight (lb). mg Number of Cartridges mg Number of Cartridges 20 60 1.2 60 1.8 30 90 1.8 90 2.6 40 120 2.3 120 3.5 50 150 2.9 150 4.4 60 180 3.5 180 5.3 80 240 4.7 180 5.3 100 270 5.3 180 5.3 120 270 5.3 180 5.3 Adapted from Malamed, Stanley F. Handbook of medical emergencies in the dental office, ed. 2, St.

Louis, 1982.

When using Mepivacine HCl Injection

USP 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 and container permit.

HCl 3% (30 mg/mL); (Mepivacaine Hydrocholoride Injection USP) is available in cardboard boxes containing 5 blisters of 10 x 1.7 mL single-dose dental cartridges, 50 per carton.

HCl 2% (20 mg/mL) (Mepivacaine Hydrochloride and Levonordefrin Injection; USP) is available in cardboard boxes containing 5 blisters of 10 x 1.7 mL single-dose dental cartridges, 50 per carton.

Both solutions should be stored at controlled room temperature, below 25° C (77° F).

Protect from light.

Do not permit to freeze.

For protection from light, retain in box until time of use.

Once opened, the box should be reclosed by closing the top flap.

Mepivacaine 2% (20 mg/mL) solution should not be used if its color is pinkish or darker than slightly yellow or it contains a precipitate.

Cartridge warmers should not be used with Mepivacaine HCl Injection USP products.

Both solutions should be stored at controlled room temperature, below 25° C (77° F).

Protect from light.

Do not permit to freeze.

For protection from light, retain in box until time of use.

Once opened, the box should be reclosed by closing the top flap.

Mepivacaine 2% (20 mg/mL) solution should not be used if its color is pinkish or darker than slightly yellow or it contains a precipitate.

Cartridge warmers should not be used with Mepivacaine HCl Injection USP products.

Animal reproduction studies have not been conducted with this solution.

It is also not known whether this solution can cause fetal harm when administered to a pregnant woman or can effect reproductive capacity.

This solution should be given to a pregnant woman only if clearly needed.

It is not known whether this drug is excreted in human milk.

Because many drugs are excreted in human milk, caution should be exercised when this solution is administered to a nursing woman.

Great care must be exercised in adhering to safe concentrations and dosages for pedodontic administration See DOSAGE AND ADMINISTRATION.