Pharmacological properties of the drug Ultracain d-s forte
Ultracaine D-S forte is a combined drug for local anesthesia (infiltration and regional) in dentistry. Articaine is a local anesthetic of the amide type of the tiaprofen group. Epinephrine (adrenaline) has a vasoconstrictor effect, preventing the systemic absorption of articaine and the development of its side effects. The drug is characterized by a rapid onset of action (after 1–3 minutes), as well as a rapid and reliable analgesic effect with good tissue tolerance. The duration of effective surgical anesthesia is at least 75 minutes. The drug does not interfere with wound healing, which is due to its good tissue tolerance and minimal vasoconstrictor effect. Articaine is 95% bound to plasma proteins. Practically does not penetrate the placenta and is not excreted in breast milk. T1/2 is 25.3±3.3 hours. It is excreted mainly by the kidneys.
Ultracaine during pregnancy and breastfeeding
The optimal form of this anesthetic during pregnancy is Ultracaine DS with an epinephrine concentration of 1:200,000. The use of anesthetics without epinephrine (or adrenaline) in pregnant and lactating women is generally not recommended. This is due to the fact that adrenaline, by constricting blood vessels at the injection site, slows down the absorption of the main component (articaine) into the blood, and accordingly this will reduce the peak concentrations of articaine in the blood, and therefore its possible side effects on the fetus.
Ultracaine during breastfeeding - after anesthesia with Ultracaine, the content of articaine in breast milk is possible, but the concentration is so low that it cannot cause any harm. Therefore, there is no need to give up breastfeeding. The epinephrine content in Ultracaine DS is also very small and cannot adversely affect either the mother or the child.
Sources:
1. Higher prof. the author's education in surgical dentistry, 2. Based on personal experience as a dental surgeon, 3. National Library of Medicine (USA), 4. “Local anesthesia in dentistry” (Baart J.), 5. https://dental.sanofi .de/.
Use of the drug Ultracain d-s forte
Intravascular administration is contraindicated. Before administering the drug, a test aspiration should be performed to exclude the possibility of intravascular injection. Injection into inflamed tissue should be avoided. For uncomplicated forceps extraction of the upper tooth (in the absence of inflammation), a vestibular injection in a dose of 1.7 ml per tooth is usually adequate. In some cases, an additional vestibular injection in a dose of 1 to 1.7 ml may be required to ensure complete anesthesia. In most cases there is no need to inject through a painful palatal approach. In cases where it is necessary to cut or suture the palate, a palatal depot injection in a dose of about 0.1 ml is adequate. With multiple extractions of adjacent teeth, the number of vestibular injections can usually be limited. In the case of uncomplicated forceps extractions of the lower premolars in the absence of inflammation, it is possible to do without anesthesia of the lower jaw, since infiltration anesthesia provided by an injection in a dose of 1.7 ml per tooth is usually sufficient. If the desired effect cannot be achieved in this way, then an additional vestibular injection is performed in a dose of 1 to 1.7 ml. Only if complete anesthesia cannot be achieved by these methods, conventional anesthesia using the mandibular blockade method is necessary. For surgical interventions, Ultracaine D-S forte is indicated in an individual dose, depending on the severity and duration of the operation. During one treatment procedure, adults can be administered up to 7 mg of articaine per 1 kg of body weight. Doses up to 500 mg (12.5 ml injection solution) are well tolerated. Before injection, a test aspiration should always be performed to exclude the possibility of intravascular injection. Aspiration is made easier when using the Uniject K injection syringe in combination with cartridges (carpules). The injection pressure should correspond to the sensitivity of the tissue.
ULTRACAINE D-S
Directions for use and doses
The drug is intended for use in the oral cavity and can only be injected into tissues where there is no inflammation.
It is impossible to inject into inflamed tissues.
The drug cannot be administered intravenously. In order to avoid accidental release of the drug into the blood vessels, an aspiration test (in two stages) should always be performed before its administration.
The main systemic reactions that may develop as a result of accidental intravascular administration of the drug can be avoided by following the injection technique: after an aspiration test, slowly inject 0.1-0.2 ml of the drug, then, no earlier than 20-30 seconds later, slowly inject the remaining dose of the drug. The injection pressure should correspond to the sensitivity of the tissue.
For anesthesia during uncomplicated extraction of teeth in the upper jaw in the absence of inflammation, it is usually sufficient to create a depot of the drug Ultracaine®
D-S in the area of the transitional fold by introducing it into the submucosa from the vestibular side (1.7 ml of the drug per tooth). In rare cases, an additional injection of 1 ml to 1.7 ml may be required to achieve complete anesthesia. In most cases, this eliminates the need for a painful palatal injection. When removing several adjacent teeth, the number of injections can usually be limited.
For anesthesia for incisions and sutures in the palate to create a palatal depot, about 0.1 ml of the drug is required for each injection.
In the case of removal of mandibular premolars in the absence of inflammation, mandibular anesthesia can be dispensed with, since infiltration anesthesia provided by an injection of 1.7 ml per tooth is usually sufficient. If in this way it was not possible to achieve the desired effect, an additional injection of 1-1.7 ml of anesthetic should be performed into the submucosa in the area of the transitional fold of the mandible on the vestibular side. If in this case it was not possible to achieve complete anesthesia, it is necessary to conduct a conduction block of the mandibular nerve.
When treating cavities and grinding teeth for crowns, with the exception of the lower molars, depending on the volume and duration of treatment, the administration of the drug Ultracaine is indicated®
D-S in the area of the transitional fold on the vestibular side in a dose of 0.5-1.7 ml per tooth.
When performing one treatment procedure, adults can be administered articaine in a dose of up to 7 mg per 1 kg of body weight. It was noted that patients tolerated doses up to 500 mg (corresponding to 12.5 ml of solution for injection) well.
For pediatric patients (over 4 years of age), the minimum doses necessary to achieve adequate anesthesia should be used, the dose of Ultracaine®
D-S is selected depending on the age and body weight of the child, but the dose of articaine should not exceed 7 mg per 1 kg of body weight (0.175 ml/kg). The use of the drug in children under 1 year of age has not been studied.
For elderly patients and all patients with severe renal and hepatic insufficiency, it is possible to create increased plasma concentrations of articaine. For these patients, the minimum doses necessary to achieve a sufficient depth of anesthesia should be used.
Contraindications to the use of the drug Ultracain d-s forte
Hypersensitivity to the components of the drug or other amide-type anesthetics. For patients with paragroup allergies, only cartridges and ampoules can be used (multi-dose vials contain methylparaben as a preservative). Due to the content of epinephrine (adrenaline), the drug is contraindicated in paroxysmal tachycardia and other tachyarrhythmias, closed-angle glaucoma, hyperthyroidism, pheochromocytoma, simultaneous terminal anesthesia, and taking non-selective β-adrenergic receptor blockers. The drug should not be used in patients with asthma, hypersensitivity to sulfites, in patients with acute heart failure, cardiac rhythm or conduction disorders (2nd-3rd degree AV block, severe bradycardia), severe hypertension (arterial hypertension).
Side effects of the drug Ultracain d-s forte
As with the use of other local anesthetics, dose-dependent disorders of the central nervous system of varying degrees of severity (from stupor to loss of consciousness), breathing disorders (up to apnea), muscle tremors, involuntary muscle contractions (up to generalized convulsive seizures), nausea, vomiting are possible. . During or shortly after injection, in rare cases, short-term visual impairment (blurred contours, diplopia, blindness) may develop. Circulatory disorders such as decreased blood pressure, tachycardia or bradycardia when using Ultracaine are usually mild. The use of local anesthetics can also cause the development of heart failure or shock, in some cases life-threatening. The development of hypersensitivity reactions (allergic or pseudo-allergic in nature) cannot be excluded. They manifest themselves as local reactions in the form of swelling, erythema, itching, as well as conjunctivitis, rhinitis, angioedema of the face, including swelling of the upper and/or lower lip, cheeks, tongue with asphyxia, urticaria, anaphylactic shock. Headache, mainly caused by the action of epinephrine, is often noted. Other side effects caused by epinephrine (tachycardia, cardiac arrhythmias, increased blood pressure) at low concentrations of 1:200,000 (0.5 mg/100 ml) and 1:100,000 (1 mg/100 ml) are rare. With submucosal administration of the contents of 2 cartridges (carpules) of Ultracaine D-S in the oral cavity, no changes in systolic or diastolic blood pressure were observed in healthy adult test participants; Heart rate in these cases also remained virtually unchanged. In some cases, areas of ischemia may develop at injection sites, sometimes progressing to the point of tissue necrosis, due to unintentional intravascular injection. Paresis of the facial nerve is possible only if the injection technique is violated. In some cases, particularly in patients with asthma, a hypersensitivity reaction may occur due to the metabisulfite contained in the sodium preparation. In this case, vomiting, diarrhea, wheezing, asthma attacks, impaired consciousness or shock may develop.
Forms of release of the anesthetic Ultracaine -
Ultracaine: the composition, regardless of the release form, 1 carpool of anesthetic contains 40 mg of articaine, and the volume of anesthetic solution in the carpul will be 1.7 ml. As for the content of epinephrine, as we said above, each of the three forms will have its own concentration of this vasoconstrictor component (vasoconstrictor). It should also be noted that ultracaine anesthetic contains the preservative sodium disulfite, which is designed to stabilize epinephrine in the drug. Moreover, since Ultracain D is produced without epinephrine, it will not contain preservatives.
Ultracaine DS forte (epinephrine 1:100.000) –
An excellent anesthetic for achieving a pronounced and long-lasting analgesic effect during surgical interventions in the oral cavity, for depulping teeth, etc. However, this form cannot be used for high blood pressure, severe cardiovascular diseases, thyroid disease and bronchial asthma.
For detailed instructions from the manufacturer, read: → “Ultracain DS Forte – instructions for use”
Ultracaine DS (epinephrine 1:200.000) –
The best option for use in patients at risk - pregnant and lactating women, patients with compensated cardiovascular diseases. It is undesirable to use for bronchial asthma. Cannot be used for thyroid diseases.
For detailed instructions from the manufacturer, read: → “Ultracain DS – instructions for use”
Ultracaine D (without epinephrine) –
The optimal choice if there is a high risk of allergic reactions, because... This anesthetic is completely free of any preservatives that are necessary to stabilize anesthetics containing adrenaline. In this regard, it is a good choice also for patients with bronchial asthma. Due to the absence of adrenaline, it can be used for diseases of the thyroid gland. The absence of adrenaline allows its use in patients with severe cardiovascular disorders, but it must be taken into account that the duration of action of the anesthetic without epinephrine/adrenaline will be no more than 20 minutes.
For detailed instructions from the manufacturer, read: → “Ultracain D – instructions for use”
Side effects of the drug Ultracain d-s forte
The drug cannot be administered intravenously, or injected into the site of inflammation. Eating food or liquids before anesthesia is prohibited. The drug should not be prescribed to patients with cholinesterase deficiency, since in this case there is a greater likelihood of an increase in the duration, and in some cases, of an undesirable increase in its effect. The drug should be prescribed with caution to patients with angina pectoris, arteriosclerosis, blood clotting disorders, and severe renal and liver dysfunction. During pregnancy, local anesthesia is a non-stressful method of achieving analgesia or anesthesia for surgical procedures. Articaine penetrates the placental barrier to a lesser extent than other anesthetics. Due to its rapid breakdown and elimination from the body, articaine does not accumulate in breast milk in clinically significant concentrations, and therefore there is no need to interrupt breastfeeding. The question of how long after surgery the patient can again drive vehicles or work with potentially dangerous mechanisms is determined individually. Maximum safety of destruction of the cartridge glass, as well as their optimal use, is achieved by using an appropriate injection syringe (Uniject or Uniject K for infiltration anesthesia, Ultraject K for intraligamentary anesthesia). Damaged cartridges should not be used for injection. Partially used cartridges cannot be used to treat other patients (risk of infection with viral hepatitis, etc.). The date of first withdrawal from the multi-dose vial should be noted on the label. Eating is allowed only after sensitivity has been restored.
Ultracain® ds (Ultracain® ds)
The drug is intended for use in the oral cavity and can only be injected into tissues where there is no inflammation. Do not inject into inflamed tissue.
The drug cannot be administered intravenously.
For anesthesia during uncomplicated extraction of teeth of the upper jaw in the absence of inflammation
Usually it is enough to create a depot of the drug Ultracain® D-S (Ultracain® D-S forte) in the area of the transitional fold by introducing it into the submucosa from the vestibular side - 1.7 ml of the drug per tooth. In rare cases, an additional injection of 1 ml to 1.7 ml may be required to achieve complete anesthesia. In most cases, this eliminates the need for a painful palatal injection. When removing several adjacent teeth, the number of injections can usually be limited.
For anesthesia during incisions and suturing in the palate to create a palatal depot
About 0.1 ml of the drug is needed for each injection.
In case of removal of mandibular premolars in the absence of inflammation
You can do without mandibular anesthesia, because Usually, infiltration anesthesia provided by injection of 1.7 ml of the drug per tooth is sufficient. If in this way it was not possible to achieve the desired effect, an additional injection of 1-1.7 ml of the drug should be performed into the submucosa in the area of the transitional fold of the mandible on the vestibular side. If in this case it was not possible to achieve complete anesthesia, it is necessary to conduct a conduction block of the mandibular nerve.
When treating cavities and grinding teeth for crowns, with the exception of the lower molars
, depending on the volume and duration of treatment, administration of the drug Ultracain® D-S with a lower content of epinephrine into the area of the transitional fold on the vestibular side is indicated in a dose of 0.5-1.7 ml per tooth.
When performing one treatment procedure for adults
Articaine can be administered at a dose of up to 7 mg per 1 kg of body weight. It was noted that patients tolerated doses up to 500 mg (corresponding to 12.5 ml of solution for injection) well.
In children over 4 years old
the dose of the drug is selected depending on the age and body weight of the child; the dose should not exceed 5 mg of articaine per 1 kg of body weight.
In elderly patients
and
patients with severe renal and hepatic insufficiency,
increased plasma concentrations of articaine may be achieved. In these patients, the drug should be used in the minimum dose necessary to achieve a sufficient depth of anesthesia.
In order to avoid accidental intravascular administration of the drug, an aspiration test should always be performed before its administration.
The injection pressure should correspond to the sensitivity of the tissue.
Interactions of the drug Ultracain d-s forte
The vasoconstrictor effect of adrenaline may be enhanced by concomitant use of tricyclic antidepressants or MAO inhibitors. Interactions of this type have been described for norepinephrine (norepinephrine) and epinephrine when used at concentrations of 1:25,000 and 1:80,000, respectively. Although the concentration of adrenaline in Ultracaine D-S forte (1:100,000) is significantly lower, this possibility should nevertheless be taken into account. Epinephrine can block the pancreas from releasing insulin, thereby reducing the effectiveness of oral antidiabetic medications. Some inhalational anesthetics (for example, halothane) can increase the sensitivity of the myocardium to catecholamines, contributing to the development of arrhythmia. With the simultaneous use of antithrombotic agents (heparin, acetylsalicylic acid), the incidence of bleeding increases. Accidental puncture of a vessel during local anesthesia can cause serious bleeding. The drug should not be prescribed simultaneously with non-selective beta-adrenergic receptor blockers.
Overdose of the drug Ultracain d-s forte, symptoms and treatment
If, during the administration of the drug, initial manifestations of an undesirable effect develop (dizziness, restlessness, stupor), the drug should be stopped and the patient should be placed in a horizontal position. It is necessary to ensure airway patency, monitor heart rate and blood pressure. It is recommended to start IV infusion of crystalloid solutions even if the symptoms do not seem severe, to ensure IV access. For breathing problems, oxygen should be prescribed depending on the severity of the condition; if necessary, perform artificial respiration or tracheal intubation to perform mechanical ventilation. Centrally acting analeptics are contraindicated. Involuntary muscle contractions or generalized convulsions are stopped by intravenous administration of short-acting or ultra-short-acting barbiturates. It is recommended to administer barbiturates slowly, depending on the effect, while continuing oxygen inhalation and cardiac monitoring. The administration of barbiturates should be accompanied by infusional delivery of fluid through a previously installed cannula. For tachycardia and arterial hypotension, it is often sufficient to place the patient in a horizontal position with slightly elevated lower limbs. In case of severe circulatory disorders, including shock, after stopping the administration of the drug, the patient should be in a horizontal position with slightly elevated lower limbs, airway patency, administration of oxygen, intravenous infusion of a balanced electrolyte solution, plasma replacement solutions, albumin, intravenous administration of corticosteroids (for example, 250–1000 mg of methylprednisolone). With a pronounced decrease in blood pressure and bradycardia - intravenous administration of adrenaline: 1 ml of 1:1000 solution is dissolved in 10 ml of solvent and slowly 0.25–1 ml of this solution is administered intravenously (0.025–0.1 ml of adrenaline ). Monitor heart rate and blood pressure. Do not administer more than 1 ml of solution (0.1 mg of adrenaline) at a time. If this dose is insufficient, it is necessary to add adrenaline to the infusion solution (the infusion rate is adjusted taking into account heart rate and blood pressure levels). In case of severe sinus tachycardia or tachyarrhythmia, β-adrenergic receptor blockers are administered intravenously under the control of circulatory parameters. For hypertension (arterial hypertension), peripheral vasodilators are prescribed.
Ultracaine D-S, 40 mg+5 mcg/ml, solution for injection, 1.7 ml, 100 pcs.
The drug is intended for use in the oral cavity and can only be injected into tissues where there is no inflammation. Do not inject into inflamed tissue.
The drug cannot be administered intravenously.
For anesthesia for uncomplicated extraction of teeth in the upper jaw in the absence of inflammation, it is usually sufficient to create a depot of the drug Ultracain® D-S (Ultracain® D-S forte) in the area of the transitional fold by introducing it into the submucosa from the vestibular side - 1.7 ml of the drug per tooth. In rare cases, an additional injection of 1 ml to 1.7 ml may be required to achieve complete anesthesia. In most cases, this eliminates the need for a painful palatal injection. When removing several adjacent teeth, the number of injections can usually be limited.
For anesthesia for incisions and sutures in the palate in order to create a palatal depot, about 0.1 ml of the drug is required for each injection.
In the case of removal of mandibular premolars in the absence of inflammation, mandibular anesthesia can be dispensed with, because Usually, infiltration anesthesia provided by injection of 1.7 ml of the drug per tooth is sufficient. If in this way it was not possible to achieve the desired effect, an additional injection of 1-1.7 ml of the drug should be performed into the submucosa in the area of the transitional fold of the mandible on the vestibular side. If in this case it was not possible to achieve complete anesthesia, it is necessary to conduct a conduction block of the mandibular nerve.
When treating cavities and grinding teeth for crowns, with the exception of the lower molars, depending on the volume and duration of treatment, it is recommended to administer the drug Ultracain® D-S with a lower content of epinephrine into the area of the transitional fold on the vestibular side in a dose of 0.5-1.7 ml per tooth.
When performing one treatment procedure, adults can be administered articaine in a dose of up to 7 mg per 1 kg of body weight. It was noted that patients tolerated doses up to 500 mg (corresponding to 12.5 ml of solution for injection) well.
In children over 4 years of age, the dose of the drug is selected depending on the age and body weight of the child; the dose should not exceed 5 mg of articaine per 1 kg of body weight.
In elderly patients and patients with severe renal and hepatic impairment, increased plasma concentrations of articaine may occur. In these patients, the drug should be used in the minimum dose necessary to achieve a sufficient depth of anesthesia.
In order to avoid accidental intravascular administration of the drug, an aspiration test should always be performed before its administration.
The injection pressure should correspond to the sensitivity of the tissue.
