Akten

Dosage forms and Strength

%medicine_name%™ (lidocaine hydrochloride ophthalmic gel) Ophthalmic Gel, 3.5% contains 35 mg per mL of lidocaine hydrochloride for topical ophthalmic administration.

Storage And Handling

%medicine_name%™ (lidocaine hydrochloride ophthalmic gel) 3.5% is supplied as a clear gel for single patient use as follows:

5mL fill in a 10mL natural, round plastic dropper bottle

(NDC 17478-792-10).

Storage

Store at 15° to 25° C (59° to 77° F)

Keep container closed and protected from light in the original carton until use. Discard after use.

Manufactured by: Akorn Inc., Lake Forest, IL 60045. Rev. 09/08. FDA revision date: 10/7/2008

%medicine_name%™ (lidocaine hydrochloride ophthalmic gel) is a local anesthetic indicated for ocular surface anesthesia during ophthalmologic procedures.

The recommended dose of %medicine_name%™ (lidocaine hydrochloride ophthalmic gel) is 2 drops applied to the ocular surface in the area of the planned procedure. %medicine_name%™ (lidocaine hydrochloride ophthalmic gel) may be reapplied to maintain anesthetic effect.

None

WARNINGS

Included as part of the PRECAUTIONS section.

PRECAUTIONS

• Not for Injection.
• Corneal Opacification. Prolonged use of a topical ocular anesthetic may produce permanent corneal opacification and ulceration with accompanying visual loss.

Nonclinical Toxicology

Carcinogenesis, mutagenesis, Impairment of fertility

Long-term studies in animals have not been performed to evaluate the carcinogenic potential of %medicine_name%™ (lidocaine hydrochloride ophthalmic gel).

Use In Specific Populations

Pregnancy. Pregnancy Category B.

Reproduction< studies for lidocaine have been performed in both rats and rabbits. There was no evidence of harm to the fetus at subcutaneous doses up to 50 mg/kg lidocaine (more than 800 fold greater than the human dose on a body weight basis) in the rat model. There are however, no adequate and well controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, this drug should be used in pregnancy only if clearly needed.

Nursing Mothers

Lidocaine is secreted in human milk. The clinical significance of this observation is unknown. Although no systemic exposure is expected with administration of %medicine_name%™ (lidocaine hydrochloride ophthalmic gel) , caution should be exercised when %medicine_name%™ (lidocaine hydrochloride ophthalmic gel) is administered to a nursing woman.

Pediatric Use

Safety and efficacy in pediatric patients has been extrapolated from studies in older subjects and studies in pediatric patients using different formulations of lidocaine.

Geriatric Use

No overall clinical differences in safety or effectiveness were observed between the elderly and other adult patients.

SIDE EFFECTS

Most common adverse reactions are conjunctival hyperemia, corneal epithelial changes, headache, and burning upon instillation.

DRUG INTERACTIONS

No information provided.

Most common adverse reactions are conjunctival hyperemia, corneal epithelial changes, headache, and burning upon instillation.

Prolonged use of a topical ocular anesthetic may produce permanent corneal opacification and ulceration with accompanying visual loss.

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. However, topical ocular application of %medicine_name%™ (lidocaine hydrochloride ophthalmic gel) is not expected to result in systemic exposure.

Lidocaine may be absorbed following topical administration to mucous membranes. Its rate and extent of absorption depend upon various factors such as concentration, the specific site of application, viscosity of the agent, and duration of exposure.

The plasma binding of lidocaine is dependent on drug concentration, and the fraction bound decreases with increasing concentration. At concentrations of 1 to 4 mcg of free base per mL, 60 to 80 percent of lidocaine is protein bound. Binding is also dependent on the plasma concentration of the alpha-1-acid glycoprotein.

Lidocaine is metabolized rapidly by the liver, and metabolites and unchanged drug are excreted by the kidneys. Biotransformation includes oxidative Ndealkylation, ring hydroxylation, cleavage of the amide linkage, and conjugation. N-dealkylation, a major pathway of biotransformation, yields the metabolites monoethylglycinexylidide and glycinexylidide. The pharmacologic/toxicologic actions of these metabolites are similar to, but less potent than, those of lidocaine. Approximately 90% of lidocaine administered is excreted in the form of various metabolites, and less than 10% is excreted unchanged. The primary metabolite in urine is a conjugate of 4-hydroxy-2, 6-dimethylaniline.

Studies of lidocaine metabolism following intravenous bolus injections have shown that the elimination half-life of this agent is typically 1.5 to 2 hours. Because of the rate at which lidocaine is metabolized, any condition that affects liver function may alter lidocaine kinetics. The half-life may be prolonged twofold or more in patients with liver dysfunction. Renal dysfunction does not affect lidocaine kinetics but may increase the accumulation of metabolites.