Septanest

Septanest is a complex medicine, the effect of which is provided by its constituent elements. The medication has a local anesthetic effect.

[1], [2]

Indications Septanesta

It is used for conducting conductive or infiltration anesthesia (the drug is also used in dentistry - for procedures for filling or extirpation of teeth, and also for grinding teeth before installing crowns).

[3]

Release form

The release is realized as an injection liquid, in glass cartridges having a volume of 1 or 1.7 ml. Inside the pack there are 50 such cartridges (5 plates of 10 cartridges) with a volume of 1 or 1.7 ml of liquid, or 10 cartridges (1 plate) with a volume of 1.7 ml of the drug.

Pharmacodynamics

The medication contains an element of articaine, which is a local anesthetic amide type. It is used for dental procedures. The substance provokes a temporary delay in the sensitivity of individual nerve fibers (sensory, as well as vegetative and motor). It is believed that articaine acts by blocking the potential-dependent Na channels inside the walls of nerve fibers.

The drug has a rapid analgesic effect (it occurs in 1-3 minutes), has a good local tolerance, and also a powerful and reliable analgesic effect.

Adrenaline added to the articaine solution inhibits its penetration into the systemic circulation, so that the substance retains active indices inside the tissues for a longer time. Thanks to this, it is possible to achieve reduced bleeding in the operating area.

The medicine begins to act after 1.5-1.8 minutes, blocking the sensitivity of the nerve after 1.4-3.6 minutes.

The anesthetic effect lasts 45-75 minutes (if the pulp is anesthetized), or 120-360 minutes (if the soft tissue layer is anesthetized). A more accurate figure depends on the size of the portion used.

[4], [5],

Pharmacokinetics

The drug is absorbed at high speed and almost completely.

Peak values of articaine within the blood plasma after intraoral administration are noted after 10-15 minutes. The distribution volume is 1.67 l / kg, and the half-life of the element is about 20 minutes. Protein synthesis of the substance inside the blood plasma is approximately 95%.

The element quickly undergoes hydrolysis involving cholinesterase of the blood plasma. It is transformed into primary products of decomposition of articin acid, which are then metabolized to its glucuronide.

Most of the articaine, along with its metabolic products, is excreted through the kidneys. Adrenaline breaks down at high speed inside the liver and other tissues, and then, together with metabolites, is excreted through the kidneys.

Dosing and administration

Application of the infiltration form of anesthesia:

• before tonsillectomy (in the area of each amygdala) - the administration of 5-10 ml LS;
• when correcting fractures of bones - the introduction of 5-20 ml of the drug;
• when applying sutures in the perineal region - injection of 5-15 ml of the drug.

When performing a conductive form of anesthesia:

• anesthesia procedure according to the Lukashevich-Oberst method - introduction of 2-4 ml LS;
• retrobulbar procedure - use of 1-2 ml of the drug;
• intercostal procedure - injection of 2-4 ml of substance (in the area of each of the segments);
• paravertebral procedure - 5-10 ml of drugs;
• peridural procedure - the introduction of 10-30 ml of medication;
• caudal procedure - use of 10-30 ml of the drug;
• for blockade of the trigeminal nerve - the administration of 1-5 ml LS;
• for blockade of the cervicodial node - injection of 5-10 ml of liquid;
• for blockade of the area of the brachial plexus - the introduction of 10-30 ml of substance (in the axillary or supraclavicular part);
• for blockade of the external part of the genitals - 7-10 ml of the preparation (on both sides);
• for blockade of paracervical type - injection of 6-10 ml LS (on both sides).

During the procedures for the removal of teeth in the area of the upper jaw (uncomplicated) in the non-inflammatory stage, the drug is administered under the mucosa in the area of the transitional fold - the volume of the vestibular depot is 1.7 ml for one tooth (if necessary, 1-1.7 ml of LS ). When performing a palatine incision or suture - the volume of the palatine depot is 0.1 ml.

During the removal (in the uncomplicated phase) of premolars located in the lower jaw (5-5), analgesia, having an infiltration form, causes the development of a conductive anesthesia.

During the turning of teeth for the installation of crowns and procedures of cavity preparation (except molars in the area of the lower jaw), the size of the vestibular portion is 0.5-1.7 ml for one tooth. The maximum allowable dosage is 7 mg / kg.

[7]

Use Septanesta during pregnancy

There is no data on the use of articaine in pregnancy (except for use in childbirth). Artikain with adrenaline is able to pass through the placenta, although the first penetrates in a much smaller volume in comparison with other local anesthetics. Serum articaine in neonates was approximately 30% of its level recorded by the mother. Accidentally introduced into the vessels of adrenaline is able to slow the intra-uterine circulation.

The safety of the use of local anesthetics in pregnant women given their effects on the fetus has not yet been established.

Animal tests using articaine showed no direct or indirect adverse effect of drugs on the course of pregnancy and the process of delivery, as well as on fetal and fetal or postnatal development of the fetus. These tests also demonstrated that adrenaline has reproductive toxicity. At the same time, the level of potential risk to the human body remains unknown. Therefore, it is recommended that pregnant women refuse to use drugs.

Lactation period.

Clinical tests regarding the possibility of using Septanest during breastfeeding were not conducted.

There is no data on whether articaine with its metabolic products can pass into breast milk. At the same time preclinical information on drug safety suggests that the level of the substance inside the mother's milk does not reach a clinically significant level. Adrenaline is able to pass into milk, but quickly dissolves there.

Therefore, lactating women should refrain from breastfeeding for a period of 10 hours after the introduction of anesthesia.

Contraindications

The main contraindications:

• the presence of hypersensitivity to the elements of the drug;
• methemoglobinemia;
• pernicious anemia;
• tachycardia of ventricles of paroxysmal nature;
• atrial fibrillation;
• glaucoma of the closed type;
• hypoxia;
• hypersensitivity to sulfo groups (especially in people with bronchial asthma).

Caution is required in such cases:

• presence of diabetes or asthma;
• lack of cholinesterase inside the body;
• tireotoksikoz;
• kidney failure;
• increased blood pressure.

Side effects Septanesta

The use of medication can cause the development of certain side-effects:

• disorders of the central nervous system (depending on the size of the portion): a disorder of consciousness (sometimes before its loss), tremor, headaches, respiratory disorders (sometimes reaching apnea), cramps and muscle twitching;
• disorders of the digestive function: diarrhea, nausea, or vomiting;
• problems with the work of the senses: occasionally there are temporary visual disorders (sometimes reaching the blindness), as well as diplopia;
• lesions affecting the function of SSS: the development of tachycardia, and in addition to arrhythmia or bradycardia, as well as a decrease in blood pressure;
• manifestations of allergy: skin itching or hyperemia, runny nose and conjunctivitis, and in addition, Quincke edema, which has a different degree of severity (puffiness in the upper or lower lip area is possible, and in addition to the glottis (leads to difficulty in swallowing), as well as cheeks, and besides urticaria and difficulty in the respiratory process), and anaphylaxis;
• local signs: inflammation or swelling at the site of injection, the appearance of ischemic areas in the area of administration (tissue necrosis may even develop - if the drug was accidentally inserted into the vessels) and nerve damage (later paralysis may develop), which appears only when the technique of injection is not observed.

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Overdose

Among the signs of poisoning: a sense of excitement, which has a motor character, loss of consciousness, severe dizziness, tachycardia with bradycardia, and a decrease in blood pressure.

If the first symptoms of intoxication have occurred during the injection procedure, it is necessary to stop the procedure, put the patient in a horizontal position, and then provide free air access to the respiratory ducts and monitor the indicators of blood pressure and heart rate.

Additional procedures:

• with the development of apnea or dyspnea - endotracheal intubation, as well as ventilation and oxygen supply (use analeptics with a central type of exposure is prohibited);
• to eliminate seizures - intravenous injection at a slow speed of barbiturates, which have a short type of exposure, and at the same time, oxygen supply and monitoring of hemodynamics;
• if there is a shock condition and severe stages of circulatory disorders - intravenous infusion of electrolyte liquids with plasma substitutes, as well as albumin together with GCS;
• with progressive bradycardia and the onset of vascular collapse - at low speed, intravenously inject 0.1 mg of epinephrine, and then through the intravenous drip (while monitoring the values of blood pressure along with heart rate);
• when there is tachyarrhythmia or tachycardia, which have a pronounced character - intravenous introduction of selective β-adrenoblockers;
• with increased values of AD, use peripheral-type vasodilators.

Carrying out oxygen therapy and monitoring the circulatory processes should be carried out for any violations.

Interactions with other drugs

MMAO and tricyclics potentiate the hypertensive effect of the drug.

The local anesthetic effect of articaine is potentiated and prolonged with time when combining drugs with vasoconstrictor drugs.

Non-selective β-adrenoblockers increase the likelihood of hypertensive crisis, and besides bradycardia in pronounced form.

[8], [9]

Storage conditions

Septanest should be kept in a place where moisture does not penetrate. The temperature level is a maximum of 25 ° C.

Shelf life

Septanest is allowed to be applied within 24 months from the date of release of the drug.

Application for children

With care, the drug is prescribed to children (for children younger than 4 years, no drug safety, as well as the effectiveness of the exposure).

Analogues

The analogues of the drug are the drugs Alfacaine, Articaine 4% with Epinephrine INIBSA, Brilokain-adrenaline, Brilokain-adrenaline forte, Primacaine, Septonast with adrenaline, Ubistezin, Ubistezin forte, Ultrakaine DS, Ultracaine D-S Forte, Ultrakaine supragenin, Cytokartin.