ULTRACAINE® DS FORTE
Hoechst Marion Roussel
Articaine HCl – Epinephrine
Action And Clinical Pharmacology: Ultracaine has been shown to block conduction by interfering with the process fundamental to the generation of the nerve action potential, namely, the large transient increase in the permeability of the membrane to sodium ions that is produced by a slight depolarization of the membrane.
Ultracaine kinetics were determined in man by radioassay following a single i.m. dose of 5 mg/kg and a single i.v. dose of 1 mg/kg of 5-labelled articaine HCl. The maximal blood concentration was reached 45 to 60 minutes after the i.m. injection. The elimination from the blood occurred in 2 phases with the following half-lives: 1.2 and 69.7 hours, and 2.0 and 31.5 hours after i.v. and i.m. injection, respectively. Ultracaine is excreted mainly via the kidneys, in 3 phases, with the following half-lives: 2.5, 4.4 and 210 hours, and 1.6, 4.6 and 39 hours after i.v. and i.m. injection, respectively. The total excretion of radioactivity, through the kidneys, was 89% after i.v. injection and 76% after i.m. injection while 1.5% (i.v.) and 1.3% (i.m.) were excreted with the feces. After the i.m. injection, 2 metabolites (M1 and M2) accounting for 87% and 2%, respectively, of the administered dose were found. No metabolite was detected in the blood following an i.v. injection. In the urine, only metabolites were found.
A study in male volunteers demonstrated that a single submucosal injection of 80 mg articaine 4% with epinephrine (1:200 000) resulted in a mean maximum serum concentration of 326±158 ng/mL. The Cmax was reached an average of 17.7±6.6 minutes after injection. Articaine is rapidly hydrolysed to its primarily inactive principal metabolite, articaine carboxylic acid. Maximum concentrations of the metabolite were reached 46.2±9.2 minutes after injection.
Indications And Clinical Uses: For infiltration anesthesia and nerve block anesthesia in clinical dentistry.
Contra-Indications: Known hypersensitivity to any of its components (see Supplied) and/or local anesthetics of the amide group; in the presence of inflammation and/or sepsis near the proposed injection site; in patients with severe shock; in patients with any degree of heart block; in patients with paroxysmal tachycardia; in patients with known arrhythmia with rapid heart rate; in patients with narrow-angle glaucoma; in patients with cholinesterase deficiency; in patients with existing neurologic disease and in patients with severe hypertension.
When articaine with epinephrine is used, the caution required of any vasopressor drug is in order.
Manufacturers’ Warnings In Clinical States: As with other local anesthetics applied to the head and neck area, life-threatening or fatal shock, respiratory or cardiac arrest may rarely occur with Ultracaine.
Methemoglobinemia: As with any local anesthetic, articaine HCl with epinephrine may rarely produce methemoglobinemia: this has been observed when an i.v. regional anesthesia technique was used. When used as directed in dental procedures, Ultracaine was not associated with methemoglobinemia.
Methemoglobinemia values of less than 20% usually do not produce any clinical symptoms. The usual clinical signs of methemoglobinemia are cyanosis of the nail beds and lips. Although the possibility of methemoglobinemia occurring in dental patients is extremely rare it can be rapidly reversed by the use of 1 to 2 mg/kg body weight of methylene blue administered i.v. over a 5 minute period.
Pregnancy and Lactation: Animal studies have not demonstrated teratogenic or embryotoxic effects of Ultracaine. However, safe use in pregnant women has not been established. Ultracaine is unlikely to be transferred to the mother’s milk since it is rapidly decomposed and eliminated.
As with other local anesthetics, Ultracaine has been shown to cross the placental barrier after peridural administration.
Precautions: General: Resuscitative equipment and drugs should be readily available when any local anesthetic is used. The safety and effectiveness of local anesthetics depend upon proper dosage, correct technique, adequate precautions, and readiness for emergencies. Ultracaine should be used cautiously in persons with known drug allergies or sensitivities, or suspected sensitivity to the amide-type local anesthetics.
The following precautions apply to all anesthetics: avoid excessive premedications with sedatives, tranquilizers, and anti-emetic agents, especially in infants, small children and elderly patients. Inject slowly with frequent aspirations and if blood is aspirated, relocate needle. Keep dosage, including the concentration and total volume of solution, as low as possible, with due regard to the age, weight, and physical status of the patient and the vascularity of the area injected. Absorption is greater when injections are made into a highly vascular tissue. The lowest dosage that gives effective anesthesia should be used to avoid high plasma levels and serious systemic side effects.
In children and elderly patients, as well as in patients of all ages with chronic or debilitating disease, the response to local anesthetics may be modified (see Dosage).
Patients with Special Diseases and Conditions: The use of a local anesthetic containing a vasoconstrictor in areas with a limited blood supply or in patients with peripheral vascular disease, will depend on an appraisal of the relative advantages and risks.
Ultracaine should be used with extreme caution in patients whose medical history and physical evaluation suggest the existence of thyrotoxicosis or diabetes.
Owing to the sulfite component, hypersensitivity reactions may occur occasionally in patients with bronchial asthma and, very rarely, in other patients (see Adverse Effects).
Drug Interactions: Solutions containing a vasoconstrictor, e.g. epinephrine, should be used with caution, if at all, in patients who are receiving MAO inhibitors or tricyclic antidepressants, because severe, prolonged hypertension may result.
Dose-related cardiac arrhythmias may occur if preparations containing epinephrine are employed in patients during, or immediately following, the administration of enflurane, halothane, or other halogenated anesthetics.
Adverse Reactions: Persistent paresthesia of the lips and oral tissues have been reported after blocking the inferior alveolar nerve.
Reactions to Ultracaine are characteristic of those associated with amide-type local anesthetics and/or vasoconstrictors.
A major cause of adverse effects to this group of drugs is excessive plasma levels, which may be due to overdosage, inadvertent intravascular injection, or slow metabolic degradation. Other causes of reactions to these local anesthetics may be hypersensitivity, idiosyncrasy, or diminished tolerance.
Reactions at the site of injection may include swelling, a burning sensation, and in insolated cases, ischemic zones, sometimes progressing to tissue necrosis.
As with all local anesthetics of this type, excessive plasma levels cause systemic reactions involving the CNS and cardiovascular systems. The CNS effects are characterized by excitation and/or depression. The first manifestation may be nervousness, dizziness, headache, tremors, or temporary visual disturbances (blurred vision, blindness, double vision) followed by drowsiness, convulsions, unconsciousness and possibly life-threatening or fatal respiratory arrest. Since excitement may be transient or absent, the first manifestation may be drowsiness, sometimes merging into unconsciousness and rarely fatal respiratory arrest. Other CNS effects may be nausea, vomiting, chills, constriction of the pupils, or tinnitus. The cardiovascular manifestations of excessive plasma levels may include depression of the myocardium, cardiac arrhythmia, tachycardia, bradycardia, blood pressure changes (usually hypotension) and possibly fatal cardiac arrest.
Allergic reactions are characterized by cutaneous lesions (e.g., urticaria, edema, itching, reddening of the skin), nausea, diarrhea, wheezing respirations, acute asthmatic attacks, impaired consciousness and anaphylactic shock which may be life-threatening or fatal.
Symptoms And Treatment Of Overdose: The type of toxic reaction is unpredictable and depends on factors such as dosage, rate of absorption and clinical status of patient. These reactions call for extreme preparedness, symptoms occurring rapidly and with little warning.
Reactions due to systemic absorption are primarily of 2 types and related to stimulation and/or depression of the CNS. Symptoms: CNS stimulation may include nervousness, dizziness, blurred vision, nausea, vomiting, tinnitus, tremor, generalized convulsions, hypertension with facial flushing and tachycardia.
CNS depression may include drowsiness, loss of consciousness, pallor, and dyspnea ranging to possibly fatal respiratory arrest.
Depression of cardiac and circulatory function can lead to cardiac arrhythmias, bradycardia, hypotension, cyanosis, cardiovascular collapse and possible fatal cardiac arrest.
Treatment: Toxic effects of local anesthetics require symptomatic treatment; there is no specific cure. 1) For all symptoms: resuscitate with oxygen 2) Circulatory collapse: immediately resuscitate with oxygen and maintain blood pressure with i.v. vasopressor agents; if cardiac arrest occurs, cardiac massage or external cardiac stimulation is indicated 3) Respiratory failure: resuscitate with oxygen, keep airway open and support respiration 4) Severe convulsions: the use of curare-like drugs, e.g. succinylcholine chloride, 40 mg, i.v. is preferred to i.v. administration of ultrashort-acting barbiturates, e.g. thiopental, 30 to 50 mg per minute, because of their depressant effect. I.V. muscle relaxants and barbiturates should only be administered by those familiar with their use.
Dosage And Administration: As with all local anesthetics, the dosage varies and depends upon the area to be anesthetized, the vascularity of the tissues, the number of neuronal segments to be blocked, individual tolerance and the technique of anesthesia. The lowest dosage needed to provide effective anesthesia should be administered. A test aspiration should always be performed before injection, in order to avoid intravascular injection. The pressure of the injection must be adapted to the sensitivity of the tissue.
It is recommended that the dosage should not exceed 7 mg/kg body weight in adults.
To date, Ultracaine has not been administered to children under 4 years of age, nor in doses greater than 5 mg/kg in children between the ages of 4 and 12.
Availability And Storage: Ultracaine DS: Each cartridge contains: articaine HCl 4% with epinephrine 1/200 000. Nonmedicinal ingredients: sodium metabisulfite (0.50 mg/mL) as antioxidant and water for injection. Cartridges of 1.7 mL, boxes of 50.
Ultracaine DS Forte: Each cartridge contains: articaine 4% with epinephrine 1/100 000. Nonmedicinal ingredients: sodium metabisulfite (0.50 mg/mL) as antioxidant and water for injection. Cartridges of 1.7 mL, boxes of 50.
Store at room temperature, below 25°C. Protect from light. Do not freeze.
ULTRACAINE® DS FORTE Hoechst Marion Roussel Articaine HCl – Epinephrine Local Anesthetic