Septanest

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

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Indications Septanesta

It is used to perform conduction or infiltration anesthesia procedures (the medicine is also used in dentistry - during procedures for filling or extracting teeth, and also when grinding teeth before installing crowns).

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Release form

The product is sold in the form of injection liquid, in glass cartridges with a volume of 1 or 1.7 ml. The pack contains 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 medicine.

Pharmacodynamics

The drug contains the element articaine, which is a local anesthetic of the 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 potential-dependent Na channels inside the walls of nerve fibers.

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

Adrenaline added to the articaine solution inhibits its penetration into the systemic circulation, due to which the substance maintains active indicators inside the tissues for a longer period of time. Due to this, it is possible to achieve reduced bleeding in the surgical area.

The drug begins to act after 1.5-1.8 minutes, blocking nerve sensitivity 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 precise figure depends on the size of the portion used.

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Pharmacokinetics

The drug is absorbed at high speed and almost completely.

Peak values of articaine in 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 in blood plasma is approximately 95%.

The element is rapidly hydrolyzed by plasma cholinesterase. It is transformed into primary breakdown products of articainic acid, which are then metabolized to its glucuronide.

Most of the articaine along with its metabolic products is excreted through the kidneys. Adrenaline is rapidly broken down in the liver and other tissues and then excreted through the kidneys along with its metabolites.

Dosing and administration

Application in infiltration anesthesia:

• before tonsillectomy (into the area of each tonsil) – administration of 5-10 ml of the drug;
• when reducing bone fractures – administer 5-20 ml of the drug;
• when applying stitches in the perineal area – injection of 5-15 ml of medication.

When performing conduction anesthesia:

• anesthesia procedure using the Lukashevich-Oberst method – administration of 2-4 ml of the drug;
• retrobulbar procedure – use of 1-2 ml of the drug;
• intercostal procedure – injection of 2-4 ml of the substance (into the area of each of the segments);
• paravertebral procedure – 5-10 ml of LS;
• epidural procedure – administration of 10-30 ml of medication;
• caudal procedure – application of 10-30 ml of the drug;
• for trigeminal nerve block – administration of 1-5 ml of the drug;
• for blockade of the cervicothoracic node – injection of 5-10 ml of liquid;
• for blockade of the brachial plexus area – introduction of 10-30 ml of the substance (into the axillary or supraclavicular part);
• for blocking the external part of the genitals - 7-10 ml of the drug (on both sides);
• for paracervical blockade – injection of 6-10 ml of drug (on both sides).

During procedures for removing teeth in the upper jaw (uncomplicated) at the non-inflammatory stage, the drug is injected 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, an additional 1-1.7 ml of the drug can be injected). When performing a palatal incision or suture - the volume of the palatal depot is 0.1 ml.

During the extraction (in the uncomplicated phase) of premolars located in the lower jaw (5-5), anesthesia, which has an infiltration form, causes the development of conduction anesthesia.

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

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Use Septanesta during pregnancy

There are no data on the use of articaine during pregnancy (except for cases of use during childbirth). Articaine and adrenaline are able to cross the placenta, although the former penetrates in a significantly smaller volume compared to other local anesthetics. Serum articaine levels in newborns were approximately 30% of its level recorded in the mother. Accidentally injected adrenaline into the vessels can slow down the intrauterine blood flow.

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

Animal tests using articaine have not shown any direct or indirect negative effects of the drug on the course of pregnancy and the birth process, as well as on the embryonic and fetal or postnatal development of the fetus. These tests also demonstrated that adrenaline has reproductive toxicity. However, the level of potential risk to the human body remains unknown. Therefore, pregnant women are advised to refrain from using the drug.

Lactation period.

There are no clinical trials to determine whether Septanest can be used during breastfeeding.

There is no data on whether articaine and its metabolic products can pass into breast milk. At the same time, preclinical data on drug safety suggest that the level of the substance in breast milk does not reach a clinically significant level. Adrenaline can pass into milk, but quickly disintegrates there.

Therefore, nursing women should refrain from breastfeeding for 10 hours after the administration of anesthesia.

Contraindications

Main contraindications:

• the presence of hypersensitivity to the components of the medication;
• methemoglobinemia;
• pernicious anemia;
• paroxysmal ventricular tachycardia;
• atrial fibrillation;
• closed-angle glaucoma;
• hypoxia;
• hypersensitivity to sulfo groups (especially in people with bronchial asthma).

Caution is required in the following cases:

• presence of diabetes mellitus or bronchial asthma;
• cholinesterase deficiency in the body;
• thyrotoxicosis;
• renal failure;
• elevated blood pressure.

Side effects Septanesta

The use of the medication may cause the development of certain side effects:

• CNS disorders (depending on the portion size): disturbances of consciousness (sometimes to the point of loss of consciousness), tremors, headaches, respiratory disorders (sometimes leading to apnea), convulsions and muscle twitching;
• digestive disorders: diarrhea, nausea or vomiting;
• problems with the functioning of the sense organs: temporary visual impairments (sometimes leading to blindness) and diplopia are occasionally observed;
• lesions affecting the function of the cardiovascular system: development of tachycardia, as well as arrhythmia or bradycardia, as well as a decrease in blood pressure;
• manifestations of allergies: skin itching or hyperemia, runny nose and conjunctivitis, and in addition to this, Quincke's edema, which has varying degrees of severity (swelling is possible in the area of the upper or lower lips, and in addition the glottis (leads to difficulty in the swallowing process), as well as cheeks, and in addition urticaria and difficulty in the breathing process), and anaphylaxis;
• local signs: inflammation or swelling at the injection site, the appearance of ischemic areas in the injection area (tissue necrosis may even develop if the drug was accidentally injected into the vessels) and nerve damage (paralysis may develop later), which only appears if the injection technique is not followed.

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Overdose

Signs of poisoning include: a feeling of excitement of a motor nature, loss of consciousness, severe dizziness, tachycardia with bradycardia, and a decrease in blood pressure.

If the first symptoms of intoxication occur during the injection procedure, it is necessary to stop the procedure, place the patient in a horizontal position, and then ensure free access of air to the respiratory tract and monitor blood pressure and heart rate.

Additional procedures:

• if apnea or dyspnea develops, endotracheal intubation is performed, as well as mechanical ventilation and oxygen supply (the use of analeptics with a central type of action is prohibited);
• to eliminate convulsions - intravenous injection at a slow rate of barbiturates with a short type of action, and simultaneously with this, oxygen supply and monitoring of hemodynamic parameters;
• if a state of shock and severe stages of circulatory disorders are observed – intravenous infusion of electrolyte fluids with plasma substitutes, as well as albumin together with GCS;
• in case of progressive bradycardia and the occurrence of vascular collapse, administer 0.1 mg of epinephrine intravenously at a low rate, and then intravenously through a drip (while monitoring blood pressure values along with heart rate);
• in the event of tachyarrhythmia or tachycardia of a pronounced nature – intravenous administration of selective β-blockers;
• in case of increased blood pressure values, use peripheral vasodilators.

Oxygen therapy and monitoring of blood circulation processes should be performed in case of any disturbances.

Interactions with other drugs

MAOIs and tricyclics potentiate the hypertensive effect of the drug.

The local anesthetic effect of articaine is potentiated and prolonged in time when the drug is combined with vasoconstrictor drugs.

Non-selective β-blockers increase the likelihood of hypertensive crisis, as well as severe bradycardia.

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Storage conditions

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

Shelf life

Septanest is approved for use within 24 months from the date of manufacture of the drug.

Application for children

The medicine is prescribed to children with caution (for children under 4 years of age, the drug's safety and effectiveness have not been established).

Analogues

The analogs of the drug are Alphacaine, Articaine 4% with Epinephrine INIBSA, Brilocaine-adrenaline, Brilocaine-adrenaline forte, Primacaine, Septonest with adrenaline, Ubistesin, Ubistesin forte, Ultracaine D-S, Ultracaine D-S forte, Ultracaine suprarenin, Cytokartin.