Articane HCl and Epinephrine Injection

Name: Articane HCl and Epinephrine Injection

Description

Septocaine® (articane hcl and epinephrine injection) injection is a sterile, aqueous solution that contains articaine HCl 4% (40 mg/mL) and epinephrine bitartrate in an epinephrine 1:200,000 or epinephrine 1:100,000 strength. Articaine HCl is an amino amide local anesthetic, chemically designated as 4-methyl-3-[2-(propylamino)-propionamido]-2-thiophenecarboxylic acid, methyl ester hydrochloride and is a racemic mixture. Articaine HCl has a molecular weight of 320.84 and the following structural formula:

Articaine HCl has a partition coefficient in n-octanol/Soerensen buffer (pH 7.35) of 17 and a pKa of 7.8.

Epinephrine bitartrate, (-)-1-(3,4-Dihydroxyphenyl)-2-methylamino-ethanol (+) tartrate (1:1) salt, is a vasoconstrictor that is added to articaine HCl in a concentration of 1:200,000 or 1:100,000 (expressed as free base). It has a molecular weight of 333.3 and the following structural formula:

Septocaine® (articane hcl and epinephrine injection) contains articaine HCl (40 mg/mL), epinephrine (1:200,000 or 1:100,000) (as epinephrine bitartrate), sodium chloride (1.6 mg/mL), and sodium metabisulfite (0.5 mg/mL). The product is formulated with a 15% overage of epinephrine. The pH is adjusted with sodium hydroxide.

Side effects

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® (articane hcl and epinephrine injection) containing epinephrine 1:100,000. Table 3 displays the adverse reactions reported in clinical trials where 182 individuals were exposed to Septocaine® (articane hcl and epinephrine injection) containing epinephrine 1:100,000 and 179 individuals were exposed to Septocaine® (articane hcl and epinephrine injection) 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® (articane hcl and epinephrine injection) 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® (articane hcl and epinephrine injection) containing Epinephrine 1:200,000 and Septocaine® (articane hcl and epinephrine injection) containing Epinephrine 1:100,000

Reaction Septocaine® (articane hcl and epinephrine injection) withe
pinephrine 1:200,000
(N=179) Incidence
Septocaine® (articane hcl and epinephrine injection) withe
pinephrine 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® (articane hcl and epinephrine injection)

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® (articane hcl and epinephrine injection) . 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.

Overdose

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].

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).

What is the most important information i should know about articaine and epinephrine (septocaine)?

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

Before receiving this medication, tell your dentist if you have high or low blood pressure, asthma or a sulfite allergy, or a history of seizures.

This medication can cause numbness for an extended period of time. Avoid eating, chewing gum, or drinking hot liquids until the feeling in your mouth has returned completely. Chewing while your mouth is numb could result in a bite injury to your tongue, lips, or inside of your cheek.

What should i discuss with my health care provider before receiving articaine and epinephrine (septocaine)?

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

Before receiving articaine and epinephrine, tell your dentist if you are allergic to any drugs, or if you have:

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

FDA pregnancy category C. This medication may be harmful to an unborn baby. Before you receive articaine and epinephrine, tell your dentist if you are pregnant.

It is not known whether articaine and epinephrine passes into breast or if it could harm a nursing baby. Before you receive articaine and epinephrine, tell your dentist if you are breast-feeding a baby.

What happens if i miss a dose (septocaine)?

Since articaine and epinephrine is given as needed before a dental procedure, you are not likely to be on a dosing schedule.

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