Ultracaine D-S forte
Ultracaine D-S forte: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Ultracain DS forte
ATX code: N01BB58
Active ingredient: articaine + epinephrine (Articaine + Epinephrine)
Manufacturer: Sanofi-Aventis Deutschland, GmbH (Germany); Sanofi-Winthrop Industrie (France)
Description and photo updated: 2018-29-11
Prices in pharmacies: from 904 rubles.
Buy
Ultracaine D-S forte is an α- and β-adrenergic agonist, a local anesthetic with a vasoconstrictor component used in dentistry.
Release form and composition
The dosage form of the drug is a solution for injection: a colorless transparent liquid, practically free of particles (1.7 ml each in colorless glass cartridges, 10 cartridges in corrugated cardboard blocks, 10 blocks in a cardboard box; 2 ml each in ampoules made of colorless glass, 10 ampoules in a pack of cardboard; each pack also contains instructions for the use of Ultracaine D-S forte).
1 ml of solution contains:
- active ingredients: articaine hydrochloride - 40 mg, epinephrine hydrochloride - 0.012 mg (corresponds to the content of epinephrine base - 0.01 mg, which is equivalent to the content of epinephrine in a solution of 1: 100,000);
- auxiliary ingredients: sodium chloride, sodium metabisulfite (sodium disulfite), water for injection.
Pharmacological properties
Pharmacodynamics
Ultracaine D-S forte is a local anesthetic with a combined composition used in dentistry for local infiltration and conduction anesthesia. The active components of the drug are epinephrine (a vasoconstrictor) and articaine (an amide-type substance with local anesthetic properties). Epinephrine provides a prolonged anesthetic effect. Articaine, through the blockade of voltage-gated sodium channels in the cell membrane of ions, leading to reversible inhibition of impulse conduction along the nerve fiber and reversible loss of sensitivity, has a local anesthetic effect directly at the injection site and around it.
The amide structure of articaine is similar to the structure of other local anesthetic substances, however, its molecule contains one additional ether group, which is rapidly hydrolyzed by esterases in the human body. The rapid destruction of articaine to articainic acid (an inactive metabolite of the substance) provides a very low systemic toxicity of the drug, which allows repeated injections of the solution.
The drug has good tissue tolerance and has a strong and fast (latency period - 1-3 minutes) anesthetic effect. The duration of anesthesia is not less than 75 minutes.
In children who took part in a clinical study (210 children aged 3.5–16 years old participated), when performing maxillary conduction or mandibular infiltration anesthesia, the use of Ultracaine D-S forte at a dose of 7 mg / kg body weight made it possible to provide a sufficient local anesthetic effect … The duration of anesthesia depended on the injected volume of the drug and was comparable in all age groups.
Pharmacokinetics
- absorption: after submucosal administration of 2 ml of the drug for articaine, the average Cmax (maximum concentration) in blood plasma is approximately 0.4 mg / l; T Cmax (time to reach maximum concentration) - 10-15 minutes. For articainic acid, the average Cmax value is 2 mg / l; indicator T Cmax - 45 min. Pharmacokinetic data obtained in children are comparable to those in adult patients. The differences between the plasma concentrations of articaine and articainic acid indicate the rapid hydrolysis of the substance in the blood and tissues, due to which the introduced articaine into the systemic circulation mainly enters the form of an inactive metabolite;
- distribution: after submucosal administration, the concentration of articaine in the blood in the area of the tooth alveoli is many times higher than those in the systemic circulation. There is an inverse relationship between the concentration of articaine in the dental alveolus and the time elapsed since the injection. Articaine binds to plasma proteins by 95%. It penetrates through the placental barrier in minimal quantities, practically is not excreted into breast milk;
- metabolism: articaine is inactivated in blood and tissues by nonspecific plasma esterases by hydrolysis in the carboxyl group. Since hydrolysis occurs very quickly and begins immediately after administration, approximately 90% of articaine is inactivated by this method. The remaining 10% are metabolized by liver microsomal enzymes. As a result, the main metabolite of articaine, articainic acid, is formed, which does not possess local anesthetic activity, its systemic toxicity has not been identified;
- excretion: after submucosal administration, articaine is excreted exponentially, the half-life (T 1/2) is approximately 25 minutes. Excretion occurs mainly by the kidneys: in the form of unchanged articaine - 1.45 ± 0.77%; articainic acid - 64.2 ± 14.4%; articainic acid glucuronide - 13.4 ± 5%. After injections of the solution into the oral mucosa, the total clearance of articaine is 235 ± 27 l / h.
Indications for use
Ultracaine D-S forte is used for local anesthesia (infiltration and conduction) during the following dental operations on the mucous membrane or bones with the aim of more pronounced hemostasis, or to improve the visualization of the operating field:
- operations on the tooth pulp (extirpation or amputation);
- long-term surgical interventions (for example, Caldwell-Luke operation);
- removal of a broken (osteotomy) or affected by apical periodontitis tooth;
- root apex resection;
- percutaneous osteosynthesis;
- interventions on the mucous membrane of the gums;
- excision of cysts;
- processing of cavities and grinding of highly sensitive teeth before prosthetics.
Contraindications
It is forbidden to use Ultracaine D-S forte with hypersensitivity to articaine or other local anesthetics of the amide type. An exception may be cases when, in the presence of hypersensitivity to these substances, an allergy to articaine was excluded with the help of studies carried out in compliance with all the necessary rules and requirements.
Ultracaine D-S forte is also contraindicated in patients with hypersensitivity to epinephrine and auxiliary components of the solution, including sulfites (including sensitivity, manifested in the form of bronchial asthma).
Contraindications related to articaine:
- severe dysfunction of the sinus node or severe conduction disturbances (severe bradycardia, AV block II and III degrees);
- acute decompensated heart failure;
- severe arterial hypotension;
- anemia (including B 12 deficiency anemia);
- methemoglobinemia;
- hypoxia;
- age up to 4 years (due to lack of sufficient clinical experience).
Contraindications related to epinephrine:
- paroxysmal tachycardia, tachyarrhythmia;
- joint intake of non-cardioselective β-blockers, for example, propranolol (the risk of developing hypertensive crisis and severe bradycardia increases);
- myocardial infarction in the last 3-6 months;
- pheochromocytoma;
- hyperthyroidism;
- coronary artery bypass grafting performed no more than 3 months ago;
- severe arterial hypertension;
- angle-closure glaucoma.
With caution, Ultracaine D-S forte is used in patients with the following diseases: CHF (chronic heart failure), IHD (ischemic heart disease), angina pectoris, atherosclerosis, postinfarction cardiosclerosis, cerebral circulation disorders, heart rhythm disturbances, myocardial infarction in history, stroke in anamnesis, cerebrovascular disorders, arterial hypertension, chronic bronchitis, pulmonary emphysema, diabetes mellitus (due to the risk of changes in the concentration of glucose in the blood), cholinesterase deficiency (it is allowed to use only if absolutely necessary, since prolonged and excessively strong action of the drug is not excluded), bleeding disorders, severe hepatic / renal dysfunction, severe agitation, a history of epilepsy,joint reception with halogen-containing agents during inhalation anesthesia.
Ultracaine D-S forte, instructions for use: method and dosage
Ultracaine D-S forte is intended for use in the oral cavity.
It is prohibited to inject into inflamed tissues.
Do not administer the solution intravenously (IV).
In order to prevent the development of major systemic reactions, it is important to avoid accidental ingestion of the drug into the blood vessels. For this, a two-stage aspiration test is performed before each injection. After it is carried out, Ultracaine D-S forte is slowly injected in a volume of 0.1–0.2 ml, and the remaining dose is also slowly injected after 20–30 seconds. The injection pressure must match the sensitivity of the tissues.
Recommended dosages to achieve adequate anesthesia:
- uncomplicated extraction of the teeth of the upper jaw (without inflammation): as a rule, it is enough to create a depot of the drug in the area of the transitional fold by introducing it into the submucosa from the vestibular side (1.7 ml per tooth). To achieve complete anesthesia, some patients are injected with Ultracaine D-S forte repeatedly at a dose of 1–1.7 ml, which in most cases avoids painful palatal injection. If you need to remove several teeth located nearby, then the number of injections is usually limited;
- incisions and sutures in the palatine region to create a palatal depot: each injection accounts for approximately 0.1 ml of the drug;
- removal of premolars of the lower jaw (without inflammation): it is usually enough to carry out infiltration anesthesia (instead of mandibular), for which an injection of Ultracaine D-S forte is performed at a dose of 1.7 ml per tooth. If the desired effect is absent, the anesthetic is re-injected at a dose of 1–1.7 ml into the submucosa in the region of the transitional fold of the lower jaw from the vestibular side. If it was not possible to achieve complete anesthesia after two injections, a conduction block of the mandibular nerve is performed.
When carrying out surgical interventions, the dose of anesthetic is selected individually, depending on the duration and severity of the intervention.
A sufficient dose of articaine to perform one treatment procedure in adult patients is up to 7 mg / kg of body weight. There is evidence of good tolerance for doses up to 500 mg (equivalent to 12.5 ml of solution for injection).
In children (over 4 years old), it is recommended to use the minimum dose of Ultracaine D-S Forte, which is necessary to achieve adequate anesthesia. The dose depends on the age and body weight of the child, but should not be higher than 5 mg / kg body weight.
In patients with severe renal / hepatic impairment and elderly patients, an increase in plasma articaine concentrations is possible, therefore, they should use Ultracaine D-S forte in the minimum dose required to achieve a sufficient depth of anesthesia.
Side effects
The incidence of the following side effects is determined in accordance with the following gradation: very often -> 1/10; often - from> 1/100 to 1/1000 to 1/10 000 to <1/1000; very rarely - <1/10 000, including individual messages; frequency is unknown - it is impossible to determine the frequency of occurrence from the available data:
- central nervous system (CNS): often - hypesthesia, paresthesia, headache, mainly due to the presence of epinephrine in the composition of Ultracaine D-S forte; infrequently - dizziness; the frequency is unknown - dose-dependent reactions from the central nervous system (nervousness, agitation, respiratory disorders up to respiratory arrest, stupor, in some cases progressing to loss of consciousness, coma, muscle tremor, muscle twitching, sometimes progressing to generalized seizures). There are reports that a violation of the correct injection technique with the introduction of a local anesthetic in dental practice led to damage to the facial nerve, which in turn was the cause of the development of facial nerve paralysis;
- organ of vision: frequency is unknown - visual disorders (mydriasis, blurred vision, blindness, double vision), as a rule, are reversible and occur during the injection of anesthetic or a short time after it;
- Gastrointestinal tract (gastrointestinal tract): often - nausea, vomiting;
- heart and blood vessels: very rarely - the development of tachycardia, cardiac arrhythmias, increased blood pressure (due to the presence of epinephrine in the composition of Ultracaine D-S forte); the frequency is unknown - bradycardia, decreased blood pressure (blood pressure), heart failure, shock;
- immune system: frequency unknown - allergic and allergic-like reactions (may appear at the injection site in the form of mucosal inflammation or swelling), angioedema (swelling of the lower and / or upper lips, cheeks, vocal cords with a feeling of "lump in the throat" and difficulty swallowing, urticaria and difficulty breathing; any of these effects can progress to anaphylactic shock), flushing of the skin, itching, conjunctivitis, rhinitis (reactions not associated with the injection site);
- general disorders and disorders at the injection site: the frequency is unknown - in some cases, with unintentional intravascular injection at the injection site, ischemic zones appeared, up to tissue necrosis.
In the course of the studies, the safety profile in children and adolescents aged 4–18 years was comparable to that in adult patients. However, in 16% of children, especially at the age of 3–7 years, due to prolonged anesthesia of the soft tissues of the oral cavity, their more frequent damage was noted. A retrospective study, which involved 211 children aged 1–4 years, revealed that dental interventions performed using 0.01 mg / ml of epinephrine and 4.2 ml of 4% articaine did not cause adverse reactions.
Overdose
Symptoms of toxic effects: first manifestations - dizziness, motor agitation or stupor; possibly - a sharp decrease in blood pressure, muscle twitching, bradycardia, severe circulatory disorders, respiratory failure, generalized convulsions, shock.
Treatment: when the first symptoms appear during the injection of the anesthetic, you should immediately stop administering it, lay the patient on a horizontal surface, leave the lower limbs in an elevated position; ensure airway patency and monitor hemodynamic parameters such as heart rate (heart rate) and blood pressure; put an intravenous catheter (even if the symptoms of intoxication seem mild; this will allow, if necessary, to quickly administer the necessary drugs).
Recommendations for eliminating violations resulting from the toxic action of Ultracaine D-S forte:
- breathing disorders: depending on their severity, oxygen is supplied, and if necessary, artificial respiration - endotracheal intubation and mechanical ventilation (artificial lung ventilation). Central analeptics are contraindicated;
- muscle twitching and generalized convulsions: stop intravenous administration of short-acting or ultra-short-acting barbiturates (these drugs are administered slowly under the constant supervision of a physician due to the risk of respiratory depression and hemodynamic disorders), while simultaneously supplying oxygen and monitoring hemodynamic parameters;
- bradycardia or a sharp decrease in blood pressure: the patient is placed on a horizontal surface, leaving the lower limbs in an elevated position;
- severe circulatory disorders and shock: regardless of the cause of the appearance of these symptoms, the administration of the drug is immediately stopped, the patient is transferred to a horizontal position with the lower limbs raised. Oxygen is supplied, intravenous administration of electrolyte solutions, GCS (glucocorticosteroids) (for example, methylprednisolone at a dose of 250-1000 mg), if necessary - albumin, plasma substitutes;
- circulatory collapse and increased bradycardia: while controlling heart rate and blood pressure, a solution of epinephrine is injected at a dose of 0.002 5–0.1 mg slowly intravenously, if necessary, higher doses (above 0.1 mg) - by infusion, adjusting the rate of administration;
- severe tachycardia and tachyarrhythmias: stop with the introduction of antiarrhythmic drugs (with the exception of noncardioselective β-blockers);
- increased blood pressure in patients with arterial hypertension: vasodilators are used if necessary.
special instructions
It is forbidden to inject Ultracaine D-S forte into the inflamed area.
Intravenous administration of the solution is not allowed.
The physician should always perform an aspiration test to prevent intravascular administration of the drug.
The injection pressure must match the sensitivity of the tissue.
When taking a solution from ampoules, only new sterile syringes and needles should be used, this will help prevent infection (including hepatitis virus).
Opened cartridges must not be reused for other patients!
A cartridge with signs of damage cannot be used for injection.
It is advisable to replace Ultracaine D-S forte with drugs such as Ultracaine D or Ultracaine D-S (contains smaller doses of epinephrine), for patients with the following diseases: diseases of the cardiovascular system (CHF, arterial hypertension, heart rhythm disturbances, coronary artery disease, angina pectoris, a history of myocardial infarction), atherosclerosis, a history of stroke, cerebrovascular disorders, diabetes mellitus, hyperthyroidism, severe anxiety, chronic bronchitis, emphysema.
Due to the content of sodium disulfite in the preparation, the anesthetic is contraindicated in patients with bronchial asthma and hypersensitivity to sulfites, since they may develop acute allergic reactions, such as bronchospasm.
The risk of adverse reactions can be minimized by using the lowest effective doses of the drug and conducting a two-stage aspiration test before the injection of Ultracaine D-S forte.
It is allowed to take food only after the cessation of the effect of local anesthesia, to the moment of full restoration of sensitivity.
The doctor should warn children and their parents that due to the prolonged decrease in tissue sensitivity due to the action of Ultracaine D-S forte, the risk of accidental damage to soft tissues by teeth (biting) increases.
It should be borne in mind that 1 ml of Ultracaine D-S forte contains less than 23 mg (1 mmol) of sodium.
The anesthetic is intended for use in dentistry. It is forbidden to use it for anesthesia of the distal extremities due to the risk of ischemia (since the drug contains epinephrine).
Influence on the ability to drive vehicles and complex mechanisms
Ultracaine D-S forte, used for local anesthesia, does not cause noticeable deviations from the usual ability to drive vehicles and work with complex mechanisms. Nevertheless, the decision to return the patient after dental intervention to driving a car and engaging in potentially hazardous activities that require speed of psychomotor reactions and high concentration of attention is made by the doctor.
Application during pregnancy and lactation
Articaine crosses the placental barrier.
There is not enough clinical data on the use of the drug during pregnancy, therefore, the decision to prescribe Ultracaine D-S forte by the dentist can be made provided that the benefits to the mother exceed the risk to the fetus. If during gestation it becomes necessary to use this drug, it is recommended to prefer drugs that do not contain epinephrine (Ultracaine D), or have a lower concentration (Ultracaine D-S).
Since no pharmacologically significant concentrations of articaine are found in breast milk, you can not interrupt breastfeeding if you need to use the drug.
Pediatric use
Due to the lack of clinical experience, Ultracaine D-S forte is contraindicated in children under 4 years of age.
With impaired renal function
Patients with severe renal impairment are recommended to use Ultracaine D-S forte with caution.
In patients of this category, plasma articaine concentrations may increase, so they need to use the drug in the minimum dose required to achieve a sufficient depth of anesthesia.
For violations of liver function
Patients with severe hepatic impairment are recommended to use Ultracaine D-S forte with caution.
In patients of this category, plasma articaine concentrations may increase, so they need to use the drug in the minimum dose required to achieve a sufficient depth of anesthesia.
Use in the elderly
In elderly patients, an increase in plasma articaine concentrations is possible, therefore, they should use Ultracaine D-S forte in the minimum dose that is required to achieve a sufficient depth of anesthesia.
Drug interactions
The combination of Ultracaine D-S forte with noncardioselective β-adrenergic blockers (for example, propranolol) is contraindicated, since the risk of developing severe bradycardia and hypertensive crisis increases.
Combinations to be taken into account:
- tricyclic antidepressants or monoamine oxidase (MAO) inhibitors: increase the effect of blood pressure-increasing vasoconstrictors (adrenomimetics), including epinephrine (similar observations have been described for concentrations of epinephrine 1:80 000 and norepinephrine 1:25 000 when used as vasoconstrictors). Although epinephrine in the drug is contained in a significantly lower concentration (1: 100,000), it is necessary to take into account the possibility of enhancing its action;
- muscle relaxants: the intensity and duration of their action increases;
- drugs that depress the central nervous system: under the influence of anesthetics, their effectiveness increases; opioid (narcotic) analgesics, on the contrary, enhance the effect of the drug, while increasing the risk of respiratory depression;
- acetylsalicylic acid, heparin: bleeding may develop at the injection site;
- cholinesterase inhibitors: likely prolongation and a pronounced increase in the action of articaine due to a slowdown in metabolism;
- drugs for the treatment of myasthenia gravis: additional correction of the treatment of myasthenia gravis is required when using Ultracaine D-S forte, especially in high doses, since it antagonizes the effect on skeletal muscles;
- oral hypoglycemic agents: their effectiveness may decrease due to the inhibition of insulin release from β-cells of the pancreas by epinephrine;
- means for inhalation anesthesia (halothane): after anesthetic injections, the risk of cardiac arrhythmias increases, since halothane can increase myocardial sensitivity to catecholamines;
- disinfectant solutions containing heavy metals: the risk of developing local reactions, such as swelling and soreness, increases when the injection site is treated with disinfectant solutions containing heavy metals;
- other local anesthetics: their metabolism slows down.
Analogs
Analogues of Ultracaine D-S forte are: Articaine DF, Ultracaine D-S, Articaine with adrenaline, Articaine with adrenaline forte, Articaine INIBSA, Alfakaine SP, Artifrin, Artifrin forte, Orablok, Septanest with adrenaline, Brilocaine-adrenaline, Brylokaine adrenaline forte, Primacaine with adrenaline, Ubistezin, Ubistezin forte, Articaine-Binergia with adrenaline, Cytokartin, Articaine-EGEN with adrenaline, etc.
Terms and conditions of storage
Store in a place out of the reach of children and protected from light, cartridges - at temperatures up to 30 ° С, ampoules - up to 25 ° С.
The shelf life of the drug in cartridges is 2.5 years, in ampoules - 3 years.
It is prohibited to use the drug after the expiration date.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews of Ultracaine D-S forte
Reviews of Ultracaine D-S Forte by both doctors and patients are positive. Experts note that the drug is well tolerated, has a pronounced duration of action and is suitable for all dental interventions, for example, such as depulpation of teeth, opening of boils, abscesses, atheroma, suturing, etc. Moreover, all doctors recommend injections in the dental office equipped with a first-aid kit with anti-shock therapy, and it is imperative to test the sensitivity of patients to this drug.
Patients characterize Ultracaine D-S forte as a powerful pain reliever that allows them to painlessly tolerate any dental intervention, even in particularly difficult cases. It is reported that after the injection, the drug begins to act within the first 5-10 minutes and retains the anesthetic effect for a long time. There are practically no reports of overdose or side effects.
Price for Ultracaine D-S forte in pharmacies
The price for Ultracain D-S forte in pharmacies is 5079–5800 rubles. (10 cartridges per 1.7 ml in the package) or 1108-1420 rubles. (10 ampoules of 2 ml in the package).
Ultracaine D-S forte: prices in online pharmacies
|
Drug name Price Pharmacy |
|
Ultracaine D-S forte 40 mg + 10 μg / ml solution for injection with epinephrine 2 ml 10 pcs. 904 RUB Buy |
|
Ultracaine D-S forte solution for in. 2ml 10 pcs. 1249 RUB Buy |
|
Ultracaine D-S forte 40 mg + 10 μg / ml solution for injection with epinephrine 1.7 ml 100 pcs. 5566 RUB Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
