Artikain

General characteristics. Structure:

Active ingredient: 40 mg of an artikain of a hydrochloride.

Excipients: sodium chloride, water for injections.

Local anesthetic (derivative thiophene) for infiltration and conduction anesthesia, has the expressed mestnoobezbolivayushchy effect.

Pharmacological properties:

Pharmacodynamics. Local anesthetic (derivative thiophene) for infiltration and conduction anesthesia, has the expressed mestnoobezbolivayushchy effect. In fabrics (in the alkalescent environment) is exposed to hydrolysis and releases the basis having lipophilic properties and easily getting through a membrane in nerve fibril. Blocks current of ions of sodium (Na+) in a cell in a phase of depolarization and blocks carrying out impulses on nerve fibril. The beginning of action - right after introduction.

Action duration - from 1 to 3 h. In acid medium the effect decreases.

Pharmacokinetics. Time of achievement of the maximum concentration of an artikain in plasma after intramuscular introduction - 20-40 min. At submucosal introduction to oral cavities has high diffusion capacity.

Communication with proteins of plasma – 95%. The elimination half-life of an artikain - 1.2 h is metabolized in a liver. It is removed by kidneys - 54-63% (for 6 h). Gets through a placental barrier (in much smaller degree, than other local anesthetics), in insignificant quantity gets through a blood-brain barrier, it is practically not allocated with breast milk.

Indications to use:

In stomatology as local anesthesia.

Route of administration and doses:

At an uncomplicated exodontia of an upper jaw in a noninflammatory stage - 1,7 ml on tooth, if necessary - in addition 1-1,7 ml; a palatal section or a seam - 0,1 ml.

During removal of premolar tooths of a mandible (5-5) in an uncomplicated stage the infiltration anesthesia gives effect of a conduction anesthesia.

At preparation of cavities and turning of teeth for crowns, except for painters of a mandible, - a vestibular injection of 0,5-1,7 ml on tooth.

The maximum dose for adults - 7 mg/kg, for children is more senior than 4 years - 5 mg/kg. Meal is allowed only after sensitivity recovery.

Features of use:

Has no effect on a fruit (except for possible bradycardia) at any technology of use and a dose. During removal of premolar tooths of a mandible in an uncomplicated stage the infiltration anesthesia gives effect of a conduction anesthesia.

Infiltration mandibular anesthesia, infiltration anesthesia of language is inefficient, a soft palate - anesthesia by means of conduction anesthesia is required. It is not necessary to enter intravenously. Patients need control of functions of cardiovascular system, respiratory system and the central nervous system.

It is necessary to cancel monoamine oxidase inhibitors in 10 days prior to administration of local anesthetic. During treatment it is necessary to be careful during the driving of motor transport and occupation other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Use at pregnancy and during feeding by a breast. Artikain passes through a placental barrier to a lesser extent, than other anesthetics. In need of use of drug for the nursing mother there is no need to interrupt breastfeeding as артикаин it is not allocated in breast milk in clinically significant quantities.

Side effects:

From the central and peripheral nervous system: a headache, dizziness, drowsiness, weakness, motive concern, consciousness disturbance, up to its loss, a spasm, a lockjaw, a tremor, visual and acoustical disturbances, sight loss, opacification in eyes, a diplopia, a nystagmus, a syndrome of a horse tail (paralysis of legs, paresthesias), paralysis of respiratory muscles (develops at subarachnoidal anesthesia more often), the block motor and sensitive. 

From cardiovascular system: lowering of arterial pressure, collapse (peripheral vazodilatation), bradycardia, arrhythmias, thorax pain.

From an urinary system: involuntary urination.

From the alimentary system: nausea, vomiting, involuntary defecation.

From blood: methemoglobinemia.

From a respiratory organs: short wind, apnoea. Allergic reactions: a skin itch, skin rash, a Quincke's disease, other anaphylactic reactions (the acute anaphylaxis), a small tortoiseshell (on skin and mucous membranes is more often).

Others: hypothermia, impotence; at anesthesia in stomatology: nonsensitivity and paresthesias of lips and language, anesthesia lengthening, fruit bradycardia.

Local reactions: hypostasis and an inflammation in the place of an injection. If any of the side effects specified in the instruction are aggravated, or you noticed any other side effects which are not specified in the instruction, report about it to the doctor.

Interaction with other medicines:

Local anesthetics strengthen the oppression of the central nervous system caused by the medicines oppressing the central nervous system.

Anticoagulants (ардепарин sodium, далтепарин sodium, данапароид sodium, эноксапарин sodium, heparin sodium, warfarin) increase risk of development of hemorrhages and bleedings.

When processing the place of an injection of local anesthetic the disinfecting solutions containing heavy metals the risk of development of local reaction in the form of painful sensitivity, hypostasis increases. At use of mestnoanesteziruyushchy medicines for spinal and epidural anesthesia with guanadrely, guanetidiny, mekamilaminy, the trimetafana kamzilaty raises risk of a sharp lowering of arterial pressure and bradycardia.

Use with monoamine oxidase inhibitors (furasolidone, Procarbazinum, селегилин) increases risk of development of hypotension; it is necessary to cancel monoamine oxidase inhibitors in 10 days prior to administration of local anesthetic.

Strengthen and extend effect of myorelaxation medicines. With narcotic analgetics - the additive effect develops that is used when carrying out spinal and epidural anesthesia, however respiratory depression amplifies.

Mestnoanesteziruyushchy action of an artikain is strengthened and extend vasoconstrictive medicines.

Show antagonism with anti-myasthenic medicines on action on skeletal muscles, especially at use in high doses that demands additional correction of treatment of a myasthenia.

Cholinesterase inhibitors (anti-myasthenic medicines, cyclophosphamide, a demekariya bromide, an ecothiostalemate iodide, Thiotepum) reduce metabolism of mestnoanesteziruyushchy medicines.

Contraindications:

Hypersensitivity (including to other mestnoanesteziruyushchy medicines of group of amides), megaloblastny B12 - scarce anemia, a Bouveret's disease, fibrillation of auricles, closed-angle glaucoma, diseases of the central nervous system, a chronic hypoxia, bronchial asthma, children's age up to 4 years.

With care. To women in labor with a preeclampsia, bleedings in the last trimester of pregnancy, an amnionitis for carrying out juxtaspinal blockade.

Overdose:

Symptoms: dizziness, motive excitement, loss of consciousness, lowering of arterial pressure, bradycardia.

Treatment: to give to the patient horizontal position, to provide free passability of respiratory tracts, control of heart rate and arterial pressure. At short wind, an apnoea - oxygen, an endotracheal intubation, artificial ventilation of the lungs (the central analeptics are contraindicated); at spasms - intravenously slowly barbiturates of short action with simultaneous supply of oxygen and control of a hemodynamics; at heavy disturbances of blood circulation and shock - intravenous infusion of electrolytes, glucocorticosteroids, plasma substitutes, albumine; at a collapse and the increasing bradycardia - intravenously slowly Epinephrinum of 0.1 mg, further intravenously kapelno under control of heart rate and arterial pressure; at the expressed tachycardia and a tachyarrhythmia - intravenously β-adrenoblockers. Supply of oxygen and control of blood circulation are necessary in all cases.

Storage conditions:

In the dry, protected from light place at a temperature not above 25 °C. To store the Period of validity of 5 years in the place, unavailable to children. Not to use after the expiry date specified on packaging

Issue conditions:

According to the recipe

Packaging:

Solution for injections of 40 mg/ml. 2 ml in ampoules of neutral glass. 5 ampoules place in a blister strip packaging. 2 blister strip packagings place in a pack from a cardboard. Put the application instruction, a knife in each pack or a box ampoule or the scarificator ampoule. In case of use of ampoules with notches, rings of a break or points of a break the knife ampoule or the scarificator ampoule is not put.