Septocaine

Name: Septocaine

Warnings

Contraindications

Hyperensitivity to amide-type local anesthetics, sulfites

Cautions

Vasoconstrictor epinephrine, will promote local hemostasis, decrease systemic absorption, increase duration of action

Local anesthetics may produce cardiovascular effects when absorbed

Risk of methemoglobinemia and sudden respiratory arrest

CNS toxicity may occur; monitor state of consciousness, drowsiness, restlessness, anxiety, tinnitus, tremors, blurred vision following local injections of the anesthetic

Avoid IV use

What Is Articaine Epinephrine?

Articaine and epinephrine are anesthetics (numbing medicines). They work by blocking nerve signals in your body.

Articaine and epinephrine is a combination medicine used to numb your mouth for a dental procedure.

Articaine and epinephrine may also be used for purposes not listed in this medication guide.

You should not receive articaine and epinephrine if you have ever had an allergic reaction to any type of numbing medicine.

You should not receive this medicine if you are allergic to any type of numbing medicine.

To make sure articaine and epinephrine is safe for you, tell your doctor if you have:

  • a heart rhythm disorder;
  • low or high blood pressure;
  • asthma or a sulfite allergy; or
  • a history of seizures.

FDA pregnancy category C. It is not known whether articaine and epinephrine will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant while using this medicine.

It is not known whether articaine and epinephrine passes into breast milk or if it could harm a nursing baby. Tell your doctor if you are breast-feeding a baby.

Articaine Epinephrine Side Effects

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficult breathing; swelling or puffiness of your face, lips, tongue, or throat.

Tell your caregivers right away if you have:

  • weak or shallow breathing;
  • a slow heart rate;
  • a light-headed feeling, like you might pass out;
  • blurred vision, ringing in your ears; or
  • anxiety, confusion, restless feeling, or tremors.

Call your doctor or dentist at once if you have any swelling, pain, or heavy bleeding after your procedure.

Common side effects may include:

  • tongue pain or swelling, red or swollen gums;
  • mild swelling in your face;
  • headache; or
  • numbness and tingling.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

What is the most important information I should know about Septocaine (articaine and epinephrine)?

You should not receive articaine and epinephrine if you have ever had an allergic reaction to any type of numbing medicine.

How is Septocaine (articaine and epinephrine)given?

Articaine and epinephrine is given as an injection that is usually placed into the gum area inside your mouth. You will receive this injection in a dentist's office or oral surgical setting.

Septocaine Dosage and Administration

General Dosing Information

Table 1 (below) summarizes the recommended volumes and concentrations of Septocaine® for various types of anesthetic procedures. The dosages suggested in this table are for normal healthy adults, administered by submucosal infiltration or nerve block.

Table 1: Recommended Dosages for Both Strengths
Procedure Septocaine® Injection
Volume (mL) Total dose of articaine HCl (mg)
Infiltration 0.5 – 2.5 20 – 100
Nerve block 0.5 – 3.4 20 – 136
Oral surgery 1.0 – 5.1 40 – 204

The recommended doses serve only as a guide to the amount of anesthetic required for most routine procedures. The actual volumes to be used depend on a number of factors such as type and extent of surgical procedure, depth of anesthesia, degree of muscular relaxation, and condition of the patient. In all cases, the smallest dose that will produce the desired result should be given.

The onset of anesthesia and the duration of anesthesia are proportional to the volume and concentration (i.e., total dose) of local anesthetic used. Caution should be exercised when employing large volumes because the incidence of side effects may be dose-related.

For most routine dental procedures, Septocaine® containing epinephrine 1:200,000 is preferred. However, when more pronounced hemostasis or improved visualization of the surgical field are required, Septocaine® containing epinephrine 1:100,000 may be used.

Maximum Recommended Dosages

  • Adults: For normal healthy adults, the maximum dose of articaine HCl administered by submucosal infiltration or nerve block should not exceed 7 mg/kg (0.175 mL/kg).
  • Pediatric Patients Ages 4 to 16 Years: The quantity of articaine HCl in children ages 4 to 16 years of age to be injected should be determined by the age and weight of the child and the magnitude of the operation. The maximum dose of articaine HCl 4% should not exceed 7 mg/kg (0.175 mL/kg) [see Use in Specific Populations (8.4)].
  • Safety and effectiveness of Septocaine® in pediatric patients below the age of 4 years have not been established.

Dosing in Special Populations

Dose reduction may be required in debilitated patients, acutely ill patients, elderly patients, and pediatric patients commensurate with their age and physical condition. No studies have been performed in patients with renal or liver dysfunction. Caution should be used in patients with severe liver disease. [see Warnings and Precautions (5.2), Use in Specific Populations (8.4, 8.5, and 8.6)]

Adverse Reactions

Reactions to articaine are characteristic of those associated with other amide-type local anesthetics. Adverse reactions to this group of drugs may also result from excessive plasma levels (which may be due to overdosage, unintentional intravascular injection, or slow metabolic degradation), injection technique, volume of injection, or hypersensitivity or they may be idiosyncratic.

Clinical Studies Experience

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

The reported adverse reactions are derived from clinical trials in the United States and the United Kingdom. Table 2 displays the adverse reactions reported in clinical trials where 882 individuals were exposed to Septocaine® containing epinephrine 1:100,000. Table 3 displays the adverse reactions reported in clinical trials where 182 individuals were exposed to Septocaine® containing epinephrine 1:100,000 and 179 individuals were exposed to Septocaine® containing epinephrine 1:200,000.

Adverse reactions observed in at least 1% of patients:

Table 2: Adverse Reactions in Controlled Trials with an Incidence of 1% or Greater in Patients Administered Septocaine® containing Epinephrine 1:100,000
Body System/Reaction Septocaine® containing epinephrine 1:100,000 (N=882) Incidence
Body as a whole
Face Edema 13 (1%)
Headache 31 (4%)
Infection 10 (1%)
Pain 114 (13%)
Digestive system
Gingivitis 13 (1%)
Nervous system
Paresthesia 11 (1%)
Table 3: Adverse Reactions in Controlled Trials with an Incidence of 1% or Greater in Patients Administered Septocaine® containing Epinephrine 1:200,000 and Septocaine® containing Epinephrine 1:100,000
Reaction Septocaine® with epinephrine 1:200,000
(N=179)
Incidence
Septocaine® with epinephrine 1:100,000
(N=182)
Incidence
Any adverse reaction 33 (18%) 35 (19%)
Pain 11 (6.1%) 14 (7.6%)
Headache 9 (5%) 6 (3.2%)
Positive blood aspiration into syringe 3 (1.6%) 6 (3.2%)
Swelling 3 (1.6%) 5 (2.7%)
Trismus 1 (0.5%) 3 (1.6%)
Nausea and emesis 3 (1.6%) 0 (0%)
Sleepiness 2 (1.1%) 1 (0.5%)
Numbness and tingling 1 (0.5%) 2 (1%)
Palpitation 0 (0%) 2 (1.%)
Ear symptoms (earache, otitis media) 1 (0.5%) 2 (1%)
Cough, persistent cough 0 (0%) 2 (1%)

Adverse reactions observed in less than 1% of patients:

Table 4: Adverse Reactions in Controlled Trials with an Incidence of Less than 1% but Considered Clinically Relevant in Patients Administered Septocaine®
Body System Reactions
Body as a Whole Asthenia; back pain; injection site pain; burning sensation above injection site; malaise; neck pain
Cardiovascular System Hemorrhage; migraine; syncope; tachycardia; elevated blood pressure
Digestive System Dyspepsia; glossitis; gum hemorrhage; mouth ulceration; nausea; stomatitis; tongue edemas; tooth disorder; vomiting
Hemic and Lymphatic System Ecchymosis; lymphadenopathy
Metabolic and Nutritional System Edema; thirst
Musculoskeletal System Arthralgia; myalgia; osteomyelitis
Nervous System Dizziness; dry mouth; facial paralysis; hyperesthesia; increased salivation; nervousness; neuropathy; paresthesia; somnolence; exacerbation of Kearns-Sayre Syndrome
Respiratory System Pharyngitis; rhinitis; sinus pain; sinus congestion
Skin and Appendages Pruritus; skin disorder
Special Senses Ear pain; taste perversion

Postmarketing Experience

The following adverse reactions have been identified during postapproval use of Septocaine®. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a casual relationship to drug exposure.

Persistent paresthesias of the lips, tongue, and oral tissues have been reported with use of articaine hydrochloride, with slow, incomplete, or no recovery. These postmarketing events have been reported chiefly following nerve blocks in the mandible and have involved the trigeminal nerve and its branches.

Hypoesthesia has been reported with use of articaine, especially in pediatric age groups, which is usually reversible. Prolonged numbness can result in soft tissue injuries such as that of the lips and tongue in these age groups.

Ischemic injury and necrosis have been described following use of articaine with epinephrine and have been postulated to be due to vascular spasm of terminal arterial branches.

Paralysis of ocular muscles has been reported, especially after posterior, superior alveolar injections of articaine during dental anesthesia. Symptoms include diplopia, mydriasis, ptosis, and difficulty in abduction of the affected eye. These symptoms have been described as developing immediately after injection of the anesthetic solution and persisting one minute to several hours, with generally complete recovery.

Use in specific populations

Pregnancy

Teratogenic Effects - Pregnancy Category C.

There are no adequate and well-controlled studies in pregnant women with Septocaine®. Articaine hydrochloride and epinephrine (1:100,000) has been shown to increase fetal deaths and skeletal variations in rabbits when given in doses approximately 4 times the maximum recommended human dose (MRHD). Septocaine® should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

In embryo-fetal toxicity studies in rabbits, 80 mg/kg, subcutaneously (approximately 4 times the MRHD based on body surface area) caused fetal death and increased fetal skeletal variations, but these effects may be attributable to severe maternal toxicity, including seizures, observed at this dose. In contrast, no embryo-fetal toxicities were observed when articaine and epinephrine (1:100,000) was administered subcutaneously throughout organogenesis at doses up to 40 mg/kg in rabbits and 80 mg/kg in rats (approximately 2 times the MRHD based on body surface area).

In pre- and postnatal developmental studies subcutaneous administration of articaine hydrochloride to pregnant rats throughout gestation and lactation, at a dose of 80 mg/kg (approximately 2 times the MRHD based on body surface area) increased the number of stillbirths and adversely affected passive avoidance, a measure of learning, in pups. This dose also produced severe maternal toxicity in some animals. A dose of 40 mg/kg (approximately equal to the MRHD on a mg/m2 basis) did not produce these effects. A similar study using articaine and epinephrine (1:100,000) rather than articaine hydrochloride alone produced maternal toxicity, but no effects on offspring.

Nursing Mothers

It is not known whether Septocaine® is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Septocaine® is administered to a nursing woman. When using Septocaine®, nursing mothers may choose to pump and discard breast milk for approximately 4 hours (based on plasma half life) following an injection of Septocaine® (to minimize infant ingestion) and then resume breastfeeding.

Pediatric Use

Safety and effectiveness of Septocaine® in pediatric patients below the age of 4 years have not been established. Safety of doses greater than 7 mg/kg (0.175 mL/kg) in pediatric patients has not been established. Safety and effectiveness was established in clinical trials with 61 pediatric patients between the ages of 4 and 16 years administered articaine hydrochloride 4% and epinephrine 1:100,000 injections. Fifty-one of these patients received doses from 0.76 mg/kg to 5.65 mg/kg (0.9 to 5.1 mL) for simple dental procedures and 10 patients received doses between 0.37 mg/kg and 7.48 mg/kg (0.7 to 3.9 mL) for complex dental procedures. Approximately 13% of these pediatric patients required additional injections of anesthetic for complete anesthesia. Dosages in pediatric patients should be reduced, commensurate with age, body weight, and physical condition [see Dosage and Administration (2.2)].

Geriatric Use

In clinical trials, 54 patients between the ages of 65 and 75 years, and 11 patients 75 years and over received Septocaine® containing epinephrine 1:100,000. Among all patients between 65 and 75 years, doses from 0.43 mg/kg to 4.76 mg/kg (0.9 to 11.9 mL) were administered to 35 patients for simple procedures and doses from 1.05 mg/kg to 4.27 mg/kg (1.3 to 6.8 mL) were administered to 19 patients for complex procedures. Among the 11 patients ≥ 75 years old, doses from 0.78 mg/kg to 4.76 mg/kg (1.3 to 11.9 mL) were administered to 7 patients for simple procedures and doses of 1.12 mg/kg to 2.17 mg/kg (1.3 to 5.1 mL) were administered to 4 patients for complex procedures.

Approximately 6% of patients between the ages of 65 and 75 years and none of the 11 patients 75 years of age or older required additional injections of anesthetic for complete anesthesia compared with 11% of patients between 17 and 65 years old who required additional injections.

No overall differences in safety or effectiveness were observed between elderly subjects and younger subjects, and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out.

Renal/Hepatic Insufficiency

No studies have been performed with articaine hydrochloride 4% and epinephrine 1:200,000 injection or articaine hydrochloride 4% and epinephrine 1:100,000 injection in patients with renal or hepatic dysfunction [see Warnings and Precautions (5.2)].

Overdosage

Acute emergencies from local anesthetics are generally related to high plasma levels encountered during therapeutic use of local anesthetics or to unintended subarachnoid injection of local anesthetic solution [see Warnings and Precautions (5.1, 5.2)].

The first consideration is prevention, best accomplished by careful and constant monitoring of cardiovascular and respiratory vital signs and the patient's state of consciousness after each local anesthetic injection. At the first sign of change, oxygen should be administered.

The first step in the management of convulsions, as well as hypo-ventilation, consists of immediate attention to the maintenance of a patent airway and assisted or controlled ventilation as needed. The adequacy of the circulation should be assessed. Should convulsions persist despite adequate respiratory support, treatment with appropriate anticonvulsant therapy is indicated. The practitioner should be familiar with the use of anticonvulsant drugs, prior to the use of local anesthetics. Supportive treatment of circulatory depression may require administration of intravenous fluids and, when appropriate, a vasopressor.

If not treated immediately, both convulsions and cardiovascular depression can result in hypoxia, acidosis, bradycardia, arrhythmias, and/or cardiac arrest. If cardiac arrest should occur, standard cardiopulmonary resuscitative measures should be instituted.

For additional information about overdose treatment, call a poison control center (1-800-222-1222).

For the Consumer

Applies to articaine / epinephrine: parenteral injection

Side effects include:

Pain, headache, facial edema, gingivitis, paresthesia, infection.

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