Mepivacaine

What is Mepivacaine?

• Mepivacaine (Carbocaine; Polocaine) is a tertiary amine used as a local anesthetic.

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Mepivacaine

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Mepivacaine Formulae Enantiomers

What are the uses of this medicine?

• Mepivacaine (Carbocaine; Polocaine) is used for production of local or regional analgesia and anesthesia by local infiltration, peripheral nerve block techniques, and central neural techniques including epidural and caudal block.
• Mepivacaine (Carbocaine; Polocaine) is indicated for production of local anesthesia for dental procedures by infiltration or nerve block in adults and pediatric patients.

How does this medicine work?

• An amide-type local anesthetic agent.
• At the injection site, mepivacaine binds to specific voltage-gated sodium ion channels in neuronal cell membranes, which inhibits both sodium influx and membrane depolarization.
• This leads to a blockage of nerve impulse initiation and conduction and results in a reversible loss of sensation.
• Compared to other local anesthetics, this agent has a more rapid onset and moderate duration of action.

Who Should Not Use this medicine ?

This medicine cannot be used in patients:

• with a known hypersensitivity to amide-type local anesthetics.

What drug interactions can this medicine cause?

Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements. Be sure to mention any of the following:

• tricyclic antidepressants or monoamine oxidase inhibitors
• nitric oxide, nitroglycerin, nitroprus-side, nitrous oxide
• articaine, benzocaine, bupivacaine, lidocaine, mepivacaine, prilocaine, procaine, ropivacaine, tetracaine
• cyclophosphamide, flutamide, hy-droxyurea, ifosfamide, rasburicase
• dapsone, nitrofurantoin, para-aminosalicylic acid, sulfonamides
• chloroquine, primaquine
• Phenobarbital, phenytoin, sodium valproate
• acetaminophen, metoclopramide, quinine, sulfasalazine

Is this medicine FDA approved?

• Yes, it was FDA approved.
• Mepivacaine became available in the United States in the 1960s.

How should this medicine be used?

Recommended dosage:

• 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.

Administration:

• When using Mepivacaine 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.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Mepivacaine hydrochloride injection 3% (30 mg/mL) and Mepivacaine hydrochloride 2% (20 mg/mL)

This medicine is available in fallowing brand namesː

• Carbocaine; Polocaine

What side effects can this medication cause?

The most common side effects of this medicine include:

• hypersensitivity
• idiosyncrasy
• paresthesias of the lips, tongue, and oral tissues
• excitation
• depression
• Nervousness
• dizziness
• blurred vision
• tremors
• drowsiness
• convulsions
• unconsciousness
• respiratory arrest
• sweating
• feeling of faintness
• changes in pulse
• cerebral hypoxia
• seizure
• urticaria
• edema and other manifestations of allergy

What special precautions should I follow?

• 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 life-threatening or less severe asthmatic episodes in certain susceptible people.
• 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.
• Mepivacaine should be used with caution in patients with a history of severe disturbances of cardiac rhythm or heart block.
• 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.
• 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.
• 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.
• Mepivacaine have not been linked to serum enzyme elevations, but when given as constant infusions or repeated injections have been occasionally mentioned as possible causes of clinically apparent liver injury.

What to do in case of emergency/overdose?

Symptoms of overdose may include:

• convulsion
• cardiovascular depression
• Allergic reactions

Management of overdosage:

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.
• Treatment of a patient with toxic manifestations consists of assuring and maintaining a patent airway and supporting ventilation as required.
• This usually will be sufficient in the management of most reactions.
• If 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.

Can this medicine be used in pregnancy?

• Pregnancy Category C.
• 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.

Can this medicine be used in children?

• Great care must be exercised in adhering to safe concentrations and dosages for pedodontic administration.

What are the active and inactive ingredients in this medicine?

Active ingredient:

• Mepivacaine Hydrochloride

Inactive ingredients:

• Sodium Chloride
• Sodium Hydroxide
• Water

Who manufactures and distributes this medicine?

Manufactured and Distributed by:

• Novocol Pharmaceutical of Canada, Inc.
• Cambridge, Ontario, Canada

What should I know about storage and disposal of this medication?

• Solutions should be stored at controlled room temperature, below 25° C (77° F).
• Protect from light.
• Do not permit to freeze.
• Once opened, the box should be reclosed by closing the top flap.
• The 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.

• Dailymed label info on Mepivacaine
• FDA Mepivacaine

Mepivacaine Resources
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