Mepivacaine

Chemical name

N-(2,6-Диметилфенил)-1-ме��ил-2-пиперидинкарбокс амид (as hydrochloride)

Gross

C15-H22-N2-O

Characteristics

Anestetik amide Tipa.mepiwakaina hydrochloride, a white crystalline powder odourless. Rat in the water, as resistant to acid, and to schelocnomu hydrolysis.

Of drugs

The drugs - местноанестезирующее . As weak lipofilnam grounds passes through the lipid membrane layer nervous cells, and then move kationnuu form, has been associated with the receptor (residues S6 transmembrannah helical domains) sodium channels membranes located in okonchaniah sensitive nerves. Reversible potencialzawisimae blocks sodium channels from current sodium ions through the cell membrane stabilizes membrane increases the threshold electric nerve stimulation, reduces the capacity of action and lowers his body, eventually blocking depoliarizatia membranes, and the emergence of the momentum from the nerve Voloknam.vazavaet all local anaesthesia : terminal, infiltration, provodnikovuyu. Provides quick and strong Actie.pri ingestion systemic blood (and the toxic concentrations in the blood) may have a dampening effect on the central nervous system and miocard (but in the application of therapeutic doses changes conductivity, excitability, mechanical and other functions are minimal). Dissociation constant (pK_a) - 7.6; Solubility in fats average. The systemic absorption and concentration in the plasma depends on the dose, as a way of introduction, vascularization of injections, and the presence or absence of epinephrine in the anaesthetic solution. Adding to the solution mepiwakaina dilute solution epinephrine (1:200000 or 5 µ g / ml) usually reduces absorption mepiwakaina and its concentration in plasma. Linking plasma protein level (about 75%). Penetrates through the placenta. Not subjected to a esterz plasma. Rapidly metabolized in the liver, the main road metabolism, and gidrauxilirovnie N-demetilirovanie. In adults identified three metabolita two phenolic derivatives (excretiruyutza of glukuronidov) and metabolite N-demetilirovanny (2',6'-пипеколоксилидид) .T_1/2 in adults, 1.9-3.2 hours; Newborn - 8,7-9 hours More than 50% of dose in the form of metabolites excreted in mere then reabsorbiruetsa in the gut (in the faeces found small percentage), and presented with the urine within 30 hours, including unchanged to (5-10%). Koumouliruet if there is a violation of the liver (cirrhosis, hepatitis). Loss of sensitivity in the 3-20 min. Anaesthesia continues 45-180 min. The timing anaesthesia (start and duration) depending on the type of anesthesia used teniki it, a solution (dosage) and the individual patient. Adding solutions vazokonstrictorov by extension анестезии.Исследован��я Assessment carcinogenicity, mutagennosti, the effect on fertility in animals and humans at all.

Indications

Local anaesthesia with the aim of the oral cavity (all types), tracheal intubations, and bronho- ezofagoskopia, tonzillacktomii et al.

Restrictions on the use of

Pregnancy, breast-feeding.

Pregnancy and lactation

When pregnancy is possible if the expected effect of therapy outweighs the potential risk to the fetus (can be reduced uterine artery and hypoxia fruit). With caution in the period of breast-feeding (no data on the penetration of breast milk).

Contraindications

Hypersensitivity, incl. from other anestetikam amide; old age, male heavy expressed human liver (including cirrhosis of the liver), porphyria.

Side-Effects

From the nervous system and sensory organs : the initiation and / or depression, headache, ringing in the ears, weakness; The speech, glotania, view; Convulsions, Koma.so the circulatory system and blood (blood, gemostaz) : gipotenzia (or sometimes hypertension), aetiology, irregular ventricular possible stops Serdza.allergicakie reactions : sneeze, urticaria, prurit, erythema, vomiting, increased body temperature, swelling Kwinke.prochie : oppression respiratory centre, nausea, vomiting.

Specific guidance

Not recommended for subarahnoidalna (spinal) anaesthesia.

Patient interaction

Beta-adrenoblokatora, calcium blockers channels protiwaritmicescie to make a dampening effect on conductivity and airway diseases.

Overdosing

Symptoms : gipotenzia, Already, the muscular stiffness, loss of consciousness, convulsions, hypoxia, gipercapnia, respiratory and metabolic acidosis, despnoe, patients, stopping Serdza.lechenie : giperventilatia, maintaining adequate oksigenation, auxiliary breath mild convulsions and convulsing (nomination tiopentala 50-100 mg in / in or diazepam 10 mg in / in), the normalization of blood, azidoza correction.

Precautions

Be wary appoint patients with hepatitis, cirrhosis, liver failure expressed by the human kidney azidozom.

Dosing and Administration

Number solution and the total dose depend on the type of anaesthesia and the nature of intervention. For injection using a 3% solution mepiwakaina (maximum dose for adults-4.4 mg / kg, but not more than 300 mg per visit), or 2% solution in combination with epinefrinom (1:80000, 1:100000), or norapinefrinom (1:200000) (maximum dose, 6.6 mg / kg, but not more than 400 mg mepiwakaina per visit). The maximum dose mepiwakaina (in mg) for children calculated from the mass of the body of a child.

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