Mentocaína

Uses

For the temporary relief of pain due to minor injury or irritation of the mouth and gums like Toothache, Sore gums, Canker sores, Braces, Minor dental procedures, Dentures

Tyrothricin is a topical antibiotic with broad spectrum activity against Gram positive bacteria and some fungal infections.

Tyrothricin is used as an over the counter topical antibiotic.

Mentocaína is also used to associated treatment for these conditions: Acute Sore Throat Pain, Dental Pain, Gangrene Stomatitis, Gingivitis, Hemorrhoids, Laryngitis, Pharyngitis, Premature Ejaculation, Secondary Bacterial Infection caused by Tonsillectomy, Secondary Bacterial Infection caused by Tooth Extractions, Skin Irritation, Sore Throat, Stomatitis, Sunburn, Teething pain, Tonsillitis, Tooth Pain, Vomiting, Pruritic dermatosis, Ulceration of the mouth, Buccopharyngeal anesthesiaBacterial Sinusitis, Bacterial rhinitis, Gingivitis, Inflammation of Mouth, Oral Infection, Oral bacterial infection, Pharyngitis, Skin Infections, Sore Throat, Stomatitis, Tonsillar inflammation, Tonsillitis, Trichomonal Vaginitis, Vaginal Infections, Mouth infection, Throat infections, Throat inflammation, Tongue inflammation, Ulceration of the mouth

How Mentocaína works

Benzocaine diffuses into nerve cells where it binds to sodium channels, preventing the channels from opening, and blocking the influx of sodium ions. Nerve cells unable to allow sodium into cells cannot depolarize and conduct nerve impulses.

Tyrocidines have a β-sheet structure containing both L and D amino acids . These structural features contribute to the formation of a curved dimer in which most amino acid side chains are located on the convex surface. The dimer orients itself at the membrane-water interface on bacterial cells with the relatively hydrophilic back-bone on the concave side facing the external environment and the many hydrophobic side chains on the convex side facing into the cell's lipid bilayer. The tyrocidine dimer is able to disrupt the cell membrane producing leakage of cell contents but the exact mechanism of this permeabilization is unclear.

Tyrocidines appear to act as reversible non-competitive inhibitors of acetylcholinesterase and β-galactosidase . The relation of this to their antibacterial action is unknown.

Gramcidins adopt similar β-sheet structures but are capable of forming β-helices . They can either form a double helix, running either parallel or anti-parallel, or a helical dimer wherein the N-termini of each polypeptide meets in the middle of the lipid bilayer. The alternating L and D amino acid structure allows the hydrophobic side chains to point outwards into the lipid bilayer, leaving the more hydrophilic backbone to form the lumen of the pore. The carbonyl oxygen atoms aid in the transport of cations through the pore. In both double helix and helical dimer conformations, gramcidins are capable of transporting monovalent cations through the membrane. Divalent cations result in blockage of the pore or channel when bound. Loss of potassium ions through membrane permeabilization seems to inhibit bacterial growth.

Gramcidin also appears to be able to insert into the mitochondial membrane and conduct hydrogen ions . This results in an uncoupling of oxidative phosphorylation from ATP generation due to the loss of the hydrogen ion gradient necessary for H+ATPase function.

Dosage

Mentocaína dosage

Apply to the affected area up to 4 times daily or as directed by a doctor/dentist. Children under 12 years of age should be supervised during the use of this product. Children under 2 years of age should be consulted to a doctor/dentist prior to the use of this product. An easy application might be done by fixing applicator on the tube’s nozzle. After application, supplied cap should be fixed on top of the applicator.

Side Effects

Side effects are less common. The side effects include allergies, swelling in the mouth or throatetc.

Toxicity

Patients experiencing an overdose may present with local anesthetic systemic toxicity syndrome, decreased cardiovascular function, decreased central nervous system function, cardiac arrest, bradycardia, hypotension, cardiac arrhythmias, syncope, and seizures. Patients should be treated with symptomatic and supportive measures which include airway maintenance, controlling seizures, and hemodynamic stabilization.

The components of tyrothricin are capable of disrupting eukaryotic cell membranes at high concentrations resulting in toxicity . This manifests as hemolysis in systemic administration. It is thought that the cholesterol present in eukaryotic cells affords some resistance to the toxic mechanisms of tyrothricin . Loss of olfactory function has been noted and topical administration to the nasal mucous membranes is not recommended .

Precaution

Patient with asthma, bronchitis, emphysema, heart disease; smokers. Children, Pregnancy and lactation.

Interaction

May antagonise the therapeutic effect of sulfonamides. Anticholinesterases may inhibit the metabolism benzocaine.

Elimination Route

The lack of water solubility prevents absorption of tyrothricin through the skin. It is not used through other routes due to toxicity concerns .

Pregnancy & Breastfeeding use

Pregnancy Category C. Either studies in animals have revealed adverse effects on the fetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the fetus.

Contraindication

Epiglottis (oral spray), methaemoglobinaemia.

Acute Overdose

Symptom: Methaemoglobinaemia, manifested by cyanotic (greyish) skin discolouration, unusual breathing or breathlessness.

Management: Symptomatic and supportive treatment. IV methylene blue 1% may be administered.

Storage Condition

Store between 15-30° C.

Innovators Monograph

You find simplified version here Mentocaína