Mepivacaine and levonordefrin is a combination product of a local anesthetic and vasoconstrictor drugs used as a local anesthetic in dental procedures. Levonordefrin is one-sixth as potent as norepinephrine.
Mepivacaine and levonordefrin Uses:
- Dental anesthesia:
- It is used as a local anesthetic for dental procedures by infiltration or nerve block in adult and pediatric patients.
Mepivacaine and levonordefrin Dose in Adults:
Note:
- The right amount of drug to use changes depending on the dental work, how numb you need to be, blood flow in the area, how long the numbness should last, and the patient's health.
- Always use the smallest amount that works and check carefully before injecting.
Mepivacaine and levonordefrin Dose in the Dental anesthesia, infiltration, or conduction block:
- For one specific spot: They usually use about 34 mg of Mepivacaine, which is equal to 1.7 mL of the solution.
- For the whole mouth: They might use up to 180 mg of Mepivacaine, which is equal to 9 mL of the solution.
- But, there's a limit! During one dental visit, they should not use more than 6.6 mg of Mepivacaine for every kg of the patient's weight, OR 400 mg in total, whichever amount is smaller.
Mepivacaine and levonordefrin Dose in Children:
Note: Dosage varies alongside the anesthetic procedure, degree of anesthesia needed, vascularity of tissue, duration of anesthesia required, and physical condition of the patient.
- It is advised here to use the lowest effective dose along with careful aspiration.
Mepivacaine and levonordefrin Dose in the Dental anesthesia, infiltration, or conduction block:
When using Mepivacaine and Levonordefrin to numb areas in the mouth for children and teenagers:
- How much you can use depends on the child's weight.
- The company that makes the drug suggests not using more than 6.6 mg for every kg the child weighs. But no matter how much the child weighs, they say you shouldn't use more than 180 mg in total if you're using the 2% solution.
- On the other hand, a group of kid's dentists (called the AAPD) says you shouldn't use more than 4.4 mg for every kg the child weighs. And even if the child is heavier, you shouldn't use more than 300 mg in one dentist visit.
Pregnancy Risk Factor C
- There haven't been any studies done to see how this drug combination affects pregnant animals.
Use of levonordefrin and mepivacaine during lactation
- We don't know if mepivacaine or levonordefrin gets into breast milk.
- The company that makes them advises being careful when giving them to mothers who are breastfeeding.
- But so far, the normal doses given to breastfeeding moms haven't been shown to harm the baby.
Dose in Kidney Disease:
- The company that makes the drug doesn't give any special instructions for adjusting the dose if someone has kidney problems.
- So, be careful when using it in such cases.
Mepivacaine and levonordefrin Dose in Liver disease:
- The company that makes the drug doesn't give special instructions for dosage.
- Be careful when using it.
- People with serious liver problems may have trouble processing the drug, so they're at a higher risk of it building up to unsafe levels in their blood.
- The degree of severe effects in the CNS and cardiovascular system is directly linked to the blood levels of mepivacaine.
- The effects mentioned below are more likely to occur after systemic administration rather than infiltration. Also, see mepivacaine.
Side effects of Mepivacaine and levonordefrin
- Central nervous system:
- Disorientation
- Dizziness
- Drowsiness
- Excitement
- Loss of consciousness
- Nervousness
- Seizure
- Hypersensitivity:
- Hypersensitivity reaction
- Neuromuscular & skeletal:
- Tremor
- Ophthalmic:
- Blurred vision
Contraindications to Mepivacaine and levonordefrin:
If someone is allergic to mepivacaine, levonordefrin, or other similar local numbing drugs, or any ingredient in this medicine, they shouldn't use it.
Warnings and precautions
CNS toxicity:
- Brain side effects: After giving the numbing shot, keep a close watch on the patient.
- If they seem restless, worried, hear ringing in the ears, feel dizzy, see blurry, shake, feel down, or sleepy, these could be early signs that the medicine is affecting their brain.
- If this happens, mainly help and comfort them.
Methemoglobinemia:
- Methemoglobinemia: This condition can be caused by some local numbing drugs.
- If it gets severe, you need to treat it right away, stop the numbing medicine, and avoid other drugs that can make it worse.
- It can show up right after the drug is given or even hours later.
- People with certain health conditions, babies under 6 months old, or those exposed to certain chemicals are more at risk.
- Watch closely for symptoms like bluish skin, headaches, fast heartbeat, breathing trouble, feeling dizzy, or tiredness.
Respiratory arrest
- Breathing issues: Sometimes, numbing drugs can very rarely cause sudden stops in breathing.
Seizures:
- There have been reports of fits (seizures) which can lead to heart stoppage, likely because the drug accidentally got into the bloodstream.
Cardiovascular disease
- Be careful using this in people with certain heart issues.
- If the medicine has something to tighten blood vessels (vasoconstrictor), use as little as possible for these patients.
Diabetes:
- Be careful when using this medicine in people with diabetes.
Hepatic impairment
- Be careful when using this medicine in people with liver issues.
Hyperthyroidism:
- Be careful when using this medicine in people with an overactive thyroid.
Renal impairment
- Be careful when using this medicine in people with kidney issues.
Mepivacaine and levonordefrin: Drug Interaction
Risk Factor C (Monitor therapy) |
|
Alpha1-Blockers |
May diminish the vasoconstricting effect of Alpha-/Beta-Agonists. Similarly, Alpha-/Beta-Agonists may antagonize Alpha1-Blocker vasodilation. |
AtoMOXetine |
May enhance the hypertensive effect of Sympathomimetics. AtoMOXetine may enhance the tachycardic effect of Sympathomimetics. |
Beta-Blockers |
May increase the serum concentration of Mepivacaine. |
Cannabinoid-Containing Products |
May enhance the tachycardic effect of Sympathomimetics. Exceptions: Cannabidiol. |
Chloroprocaine |
May enhance the hypertensive effect of Alpha-/Beta-Agonists. |
Doxofylline |
Sympathomimetics may enhance the adverse/toxic effect of Doxofylline. |
Guanethidine |
May enhance the arrhythmogenic effect of Sympathomimetics. Guanethidine may enhance the hypertensive effect of Sympathomimetics. |
Methemoglobinemia Associated Agents |
May enhance the adverse/toxic effect of Local Anesthetics. Specifically, the risk for methemoglobinemia may be increased. |
Neuromuscular-Blocking Agents |
Local Anesthetics may enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents. |
Solriamfetol |
Sympathomimetics may enhance the hypertensive effect of Solriamfetol. |
Spironolactone |
May diminish the vasoconstricting effect of Alpha-/Beta-Agonists. |
Sympathomimetics |
May enhance the adverse/toxic effect of other Sympathomimetics. |
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. |
Tedizolid |
May enhance the hypertensive effect of Sympathomimetics. Tedizolid may enhance the tachycardic effect of Sympathomimetics. |
Risk Factor D (Consider therapy modification) |
|
Benzylpenicilloyl Polylysine |
Alpha-/Beta-Agonists may diminish the diagnostic effect of Benzylpenicilloyl Polylysine. Management: Consider the use of a histamine skin test as a positive control to assess a patient's ability to mount a wheal and flare response. |
Cocaine (Topical) |
May enhance the hypertensive effect of Sympathomimetics. Management: Consider alternatives to the 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. |
Hyaluronidase |
May enhance the vasoconstricting effect of Alpha-/Beta-Agonists. Management: Avoid the use of hyaluronidase to enhance dispersion or absorption of alpha-/beta-agonists. The use of hyaluronidase for other purposes in patients receiving alpha-/beta-agonists may be considered as clinically indicated. |
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. |
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 Factor X (Avoid combination) |
|
Bupivacaine (Liposomal) |
Local Anesthetics may enhance the adverse/toxic effect of Bupivacaine (Liposomal). Management: Liposomal bupivacaine should not be administered with local anesthetics. Liposomal bupivacaine may be administered 20 minutes or more after the administration of lidocaine, but the optimal duration of dose separation for other local anesthetics is unknown |
Ergot Derivatives |
May enhance the hypertensive effect of Alpha-/Beta-Agonists. Ergot Derivatives may enhance the vasoconstricting effect of Alpha-/Beta-Agonists. Exceptions: Ergoloid Mesylates; Nicergoline. |
Monoamine Oxidase Inhibitors |
May enhance the hypertensive effect of Levonordefrin. |
Monitoring parameters:
None mentioned.
How to administer Mepivacaine and levonordefrin?
- Go Slow: Inject the medicine slowly.
- Check Often: Regularly pull back on the syringe before and as you're injecting to make sure you're not in a blood vessel.
- Be Extra Careful If:
- There's swelling or redness in the area where you're going to inject.
- There's an infection in that area.
Mechanism of action of Mepivacaine and levonordefrin:
How Mepivacaine Works:
- Sodium Channels: Mepivacaine does its job by latching onto special "sodium channels" inside nerve cells.
- Blocking Signals: This latch blocks sodium from getting into the nerve, which is necessary for nerve signals to work.
- Stopping Nerve Activity: By blocking sodium, it stops nerve signals and prevents them from doing their job.
- Reversible: Importantly, this block is not permanent. When the drug moves away from the nerve, the sodium channels start working again, and the nerve signals come back.
How Levonordefrin Helps Mepivacaine:
- Vasoconstriction: Levonordefrin does something extra. It narrows blood vessels around the nerve.
- Locking Mepivacaine In: This "squeeze" on the blood vessels keeps mepivacaine around the nerve longer.
- Extended Numbness: So, thanks to levonordefrin, mepivacaine stays in place for a longer time, keeping the area numb for an extended period.
How Fast it Works:
- Upper jaw: Starts numbing in 30 seconds to 2 minutes.
- Lower jaw: Takes a bit longer, between 1 to 4 minutes.
How Long it Lasts:
- Upper jaw: Numbs the area for 1 to 2.5 hours.
- Lower jaw: Numbs longer, for 2.5 to 5.5 hours.
Inside the Body:
- Protein Binding: About 75% of Mepivacaine attaches to proteins in the blood.
- Processing (Metabolism): The liver processes Mepivacaine by breaking it down in various ways like N-demethylation, adding an oxygen (hydroxylation), and attaching it to a molecule (glucuronidation).
- Getting Rid of the Drug (Excretion): The body mostly gets rid of Mepivacaine through urine. About 90% to 95% of it is excreted this way, but it's mostly in a changed form (as metabolites).
International Brands of Mepivacaine and levonordefrin:
- Carbocaine 2% with Neo-Cobefrin
- Polocaine Dental
- Scandonest 2% L
- Polocaine 2% and Levonordefrin 1:20,000
Mepivacaine and levonordefrin Brands Names in Pakistan:
No Brands are Available in Pakistan yet.