DailyMed Label: POLOCAINE (MEPIVACAINE HCl)

DailyMed Label: Polocaine

2024

DailyMed Prescription

Polocaine

Mepivacaine Hydrochloride

Dentsply Pharmaceutical

NDC: 66312-441

NDC: 66312-441

NDC: 66312-441

Mepivacaine Hydrochloride, a tertiary amine used as a local anesthetic, is 1-methyl-2,' 6' - pipecoloxylidide monohydrochloride with the following structural formula: It is a white, crystalline, odorless powder soluble in water, but very resistant to both acid and alkaline hydrolysis. Levonordefrin, a sympathomimetic amine used as a vasoconstrictor in local anesthetic solution, is (-)-α-(1-Aminoethyl)-3, 4-dihydroxybenzyl alcohol with the following structural formula: It is a white or buff-colored crystalline solid, freely soluble in aqueous solutions of mineral acids, but practically insoluble in water. DENTAL CARTRIDGES MAY NOT BE AUTOCLAVED. 3% (30 mg/mL) Polocaine ® DENTAL (mepivacaine hydrochloride injection 3% (30 mg/mL)) and 2% (20 mg/mL) Polocaine ® DENTAL with Levonordefrin 1:20,000 (mepivacaine hydrochloride 2% (20 mg/mL) with levonordefrin 1:20,000 injection) are sterile solutions for injection. COMPOSITION: CARTRIDGE The pH of the 2% cartridge solution is adjusted between 3.3 and 5.5 with NaOH. The pH of the 3% cartridge solution is adjusted between 4.5 and 6.8 with NaOH. Each mL contains: 2% 3% Mepivacaine Hydrochloride 20 mg 30 mg Levonordefrin 0.05 mg - Sodium Chloride 4 mg 6 mg Potassium metabisulfite 1.2 mg - Edetate disodium 0.25 mg - Sodium Hydroxide q.s. ad pH; Hydrochloric Acid 0.5 mg - Water For Injection, qs. ad. 1 mL 1 mL Chemical Structure Chemical Structure

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

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.) × Maximum Recommended Dose for Adults (400 mg) 150 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) calculated maximum amount of drug: Maximum Allowable Dosage Adapted from Malamed, Stanley F: Handbook of medical emergencies in the dental office, ed. 2, St. Louis, 1982. The C.V. Mosby Co. 3% Mepivacaine Plain 2% Mepivacaine 1:20,000 Levonordefrin 3 mg/lb (270 mg max.) 3 mg/lb (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 When using Polocaine ® 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.

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

The safety and effectiveness of mepivacaine depend upon proper dosage, correct technique, adequate precautions, and readiness for emergencies. The lowest dose that results in effective anesthesia should be used to avoid high plasma levels and possible adverse effects. Injection of repeated doses of mepivacaine may cause significant increase in blood levels with each repeated dose due to slow accumulation of the drug or its metabolites, or due to slower metabolic degradation than normal. Tolerance varies with the status of the patient. Debilitated, elderly patients, acutely ill patients, and children should be given reduced doses commensurate with their weight and physical status. Mepivacaine should be used with caution in patients with a history of severe disturbances of cardiac rhythm or heart block. INJECTIONS SHOULD ALWAYS BE MADE SLOWLY WITH ASPIRATION TO AVOID INTRAVASCULAR INJECTION AND THEREFORE SYSTEMIC REACTION TO BOTH LOCAL ANESTHETIC AND VASOCONSTRICTOR. If sedatives are employed to reduce patient apprehension, use reduced doses, since local anesthetic agents, like sedatives, are central nervous system depressants which in combination may have an additive effect. Young children should be given minimal doses of each agent. Changes in sensorium such as excitation, disorientation or drowsiness may be early indications of a high blood level of the drug and may occur following inadvertent intravascular administration or rapid absorption of mepivacaine. Local anesthetic procedures should be used with caution when there is inflammation and/or sepsis in the region of the proposed injection. The patient should be cautioned against loss of sensation and possibility of biting trauma should the patient attempt to eat or chew gum prior to return of sensation. Inform patients that use of local anesthetics may cause methemoglobinemia, a serious condition that must be treated promptly. Advise patients or caregivers to seek immediate medical attention if they or someone in their care experience the following signs or symptoms: pale, gray, or blue colored skin (cyanosis); headache; rapid heart rate; shortness of breath; lightheadedness; or fatigue. 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 diseases 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. Patients who are administered local anesthetics are at increased risk of developing methemoglobinemia when concurrently exposed to the following drugs, which could include other local anesthetics: EXAMPLES OF DRUGS ASSOCIATED WITH METHEMOGLOBINEMIA: Class Examples Nitrates/Nitrites nitric oxide, nitroglycerin, nitroprusside, nitrous oxide Local anesthetics articaine, benzocaine, bupivacaine, lidocaine, mepivacaine, prilocaine, procaine, ropivacaine, tetracaine Antineoplastic Agents cyclophosphamide, flutamide, hydroxyurea, ifosfamide, rasburicase Antibiotics dapsone, nitrofurantoin, para-aminosalicylic acid, sulfonamides Antimalarials chloroquine, primaquine Anticonvulsants phenobarbital, phenytoin, sodium valproate Other drugs acetaminophen, metoclopramide, quinine, sulfasalazine 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. Studies of mepivacaine HCl in animals to evaluate the carcinogenic and mutagenic potential or the effect on fertility have not been conducted. 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 affect 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 ).

Reactions to Polocaine

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 diseases 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. Patients who are administered local anesthetics are at increased risk of developing methemoglobinemia when concurrently exposed to the following drugs, which could include other local anesthetics: EXAMPLES OF DRUGS ASSOCIATED WITH METHEMOGLOBINEMIA: Class Examples Nitrates/Nitrites nitric oxide, nitroglycerin, nitroprusside, nitrous oxide Local anesthetics articaine, benzocaine, bupivacaine, lidocaine, mepivacaine, prilocaine, procaine, ropivacaine, tetracaine Antineoplastic Agents cyclophosphamide, flutamide, hydroxyurea, ifosfamide, rasburicase Antibiotics dapsone, nitrofurantoin, para-aminosalicylic acid, sulfonamides Antimalarials chloroquine, primaquine Anticonvulsants phenobarbital, phenytoin, sodium valproate Other drugs acetaminophen, metoclopramide, quinine, sulfasalazine 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.

3% (30 mg/mL) Polocaine ® DENTAL (Mepivacaine Hydrochloride Injection USP) (NDC 66312-441-16) is available in cardboard boxes containing 5 blisters of 10 × 1.7 mL single-dose dental cartridges, 50 per carton. 2% (20 mg/mL) Polocaine ® DENTAL with Levonordefrin 1:20,000 (Mepivacaine Hydrochloride and Levonordefrin Injection USP) (NDC 66312-461-16) is available in cardboard boxes containing 5 blisters of 10 × 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. The 2% (20 mg/mL) Polocaine ® DENTAL with Levonordefrin 1:20,000 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 Polocaine ® products.

Polocaine ® stabilizes the neuronal membrane and prevents the initiation and transmission of nerve impulses, thereby effecting local anesthesia. Polocaine ® is rapidly metabolized, with only a small percentage of the anesthetic (5 to 10 percent) being excreted unchanged in the urine. Polocaine ® because of its amide structure, is not detoxified by the circulating plasma esterases. The liver is the principal site of metabolism, with over 50 percent of the administered dose being excreted into the bile as metabolites. Most of the metabolized mepivacaine is probably resorbed in the intestine and then excreted into the urine since only a small percentage is found in the feces. The principal route of excretion is via the kidney. Most of the anesthetic and its metabolites are eliminated within 30 hours. It has been shown that hydroxylation and N-demethylation, which are detoxification reactions, play important roles in the metabolism of the anesthetic. Three metabolites of mepivacaine have been identified from adult humans: two phenols, which are excreted almost exclusively as their glucuronide conjugates, and the N-demethylated compound (2,' 6' - pipecoloxylidide). The onset of action is rapid (30 to 120 seconds in the upper jaw; 1 to 4 minutes in the lower jaw) and 3% (30 mg/mL) Polocaine ® DENTAL will ordinarily provide operating anesthesia of 20 minutes in the upper jaw and 40 minutes in the lower jaw . 2% (20 mg/mL) Polocaine ® DENTAL with Levonordefrin 1:20,000 provides anesthesia of longer duration for more prolonged procedures, 1 hour to 2.5 hours in the upper jaw and 2.5 hours to 5.5 hours in the lower jaw . Polocaine ® does not ordinarily produce irritation or tissue damage. Levonordefrin is a sympathomimetic amine used as a vasoconstrictor in local anesthetic solutions. It has pharmacologic activity similar to that of Epinephrine but it is more stable than Epinephrine. In equal concentrations, Levonordefrin is less potent than Epinephrine in raising blood pressure, and as a vasoconstrictor.

NDC 66312-441-16 Reorder # 34416 3% Polocaine® DENTAL Mepivacaine Hydrochloride 3% (30mg/mL) (Mepivacaine HCl Injection, USP) For dental block and infiltration injections only. 50 Single-Dose Cartridges, 1.7 mL each Sterile aqueous Solution for Injection Rx Only principal display panel carton