DORZOLAMIDE HYDROCHLORIDE solution/ drops

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

DORZOLAMIDE HYDROCHLORIDE (UNII: QZO5366EW7) (DORZOLAMIDE - UNII:9JDX055TW1)

Available from:

Golden State Medical Supply, Inc.

INN (International Name):

DORZOLAMIDE HYDROCHLORIDE

Composition:

DORZOLAMIDE 20 mg in 1 mL

Administration route:

OPHTHALMIC

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Dorzolamide hydrochloride ophthalmic solution is indicated in the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma. Dorzolamide hydrochloride ophthalmic solution is contraindicated in patients who are hypersensitive to any component of this product [ see Warnings and Precautions (5.1) ]. Risk Summary There are no adequate and well-controlled studies in pregnant women with dorzolamide hydrochloride ophthalmic solution. Dorzolamide caused fetal vertebral malformations when administered orally to rabbits at 2.5 mg/kg/day (37 times the clinical exposure). Dorzolamide administered during the period of organogenesis was not teratogenic in rabbits dosed up to 1 mg/kg/day (15 times the clinical exposure). Dorzolamide hydrochloride administered orally to rats during late gestation and lactation caused growth delays in offspring at 7.5 mg/kg/day (52 times the clinical exposure). Growth was not delayed at 1 mg/kg/day (8.0 times the clinical exposure). The background risk of major birth defects and miscarriage for the indicated population is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively. Data Animal Data Developmental toxicity studies were conducted in pregnant rabbits administered dorzolamide hydrochloride orally during the period of organogenesis from gestation days 6 through 18 at doses of 0.2, 1, 2.5, 5, and 10 mg/kg/day. The developmental lowest observed adverse effect level (LOAEL) was 2.5 mg/kg/day, based on vertebral malformations and decreased fetal body weight. The maternal LOAEL was 2.5 mg/kg/day, based on metabolic acidosis and reduced weight gain. The maternal and developmental no adverse effect levels (NOAELs) were 1 mg/kg/day. The rabbit doses of 1 and 2.5 mg/kg/day represent estimated plasma C max levels in rabbits 15 and 37 times higher than the lower limit of detection in human plasma following ocular administration, respectively. Dorzolamide hydrochloride was administered orally to rats during late gestation and lactation (gestation day 17 through postpartum day 20) at doses of 0.1, 1, or 7.5 mg/kg/day. The developmental LOAEL was 7.5 mg/kg/day, based on reduced birth weight, reduced weight gain, and a slight delay in postnatal development (incisor eruption, vaginal canalization and eye openings) secondary to lower offspring body weight. This 7.5 mg/kg/day dose represents an estimated plasma C max level in rats 52 times higher than the lower limit of detection in human plasma following ocular administration. The developmental NOAEL was 1 mg/kg/day. The maternal LOAEL was 1 mg/kg/day, based on reduced body weight gain. The maternal NOAEL was 0.1 mg/kg/day. The rat doses of 1 and 0.1 mg/kg/day represent estimated plasma C max levels in rats approximately 8.0 times and approximately equal (1x), respectively to the lower limit of detection in human plasma following ocular administration. Risk Summary There are no data on the presence of dorzolamide hydrochloride ophthalmic solution in human milk, the effects on the breastfed infant, or the effects on milk production. The developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for dorzolamide hydrochloride ophthalmic solution and any potential adverse effects on the breast-fed child from dorzolamide hydrochloride ophthalmic solution. Dorzolamide is present in the milk of lactating rats (see Data) . Data Animal Data Lactating rats were dosed orally with 7.5 mg/kg/day of dorzolamide hydrochloride; dorzolamide and the N-desethyl metabolite were detected in the milk. Safety and effectiveness of dorzolamide hydrochloride ophthalmic solution have been demonstrated in pediatric patients in a 3-month, multicenter, double-masked, active-treatment-controlled trial. No overall differences in safety or effectiveness have been observed between elderly and younger patients. Dorzolamide has not been studied in patients with severe renal impairment (CrCl < 30 mL/min). Because dorzolamide and its metabolite are excreted predominantly by the kidney, dorzolamide hydrochloride ophthalmic solution is not recommended in such patients. Dorzolamide has not been studied in patients with hepatic impairment and should therefore be used with caution in such patients.

Product summary:

Dorzolamide Hydrochloride Ophthalmic Solution 2% is supplied sterile in 10 mL white LDPE plastic dropper bottles with white LDPE dropper tips and orange P/P caps of the following sizes: 10 mL Storage Store Dorzolamide Hydrochloride Ophthalmic Solution at 20°-25°C (68°-77°F). Protect from light. After opening, Dorzolamide Hydrochloride Ophthalmic Solution can be used until the expiration date on the bottle.

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

DORZOLAMIDE HYDROCHLORIDE- DORZOLAMIDE HYDROCHLORIDE SOLUTION/ DROPS
GOLDEN STATE MEDICAL SUPPLY, INC.
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HIGHLIGHTS OF PRESCRIBING INFORMATION
DORZOLAMIDE HYDROCHLORIDE OPHTHALMIC SOLUTION. THESE HIGHLIGHTS DO NOT
INCLUDE ALL THE
INFORMATION NEEDED TO USE DORZOLAMIDE HYDROCHLORIDE OPHTHALMIC
SOLUTION SAFELY AND
EFFECTIVELY. SEE FULL PRESCRIBING INFORMATION FOR DORZOLAMIDE
HYDROCHLORIDE OPHTHALMIC
SOLUTION.
DORZOLAMIDE HYDROCHLORIDE OPHTHALMIC SOLUTION, FOR TOPICAL OPHTHALMIC
USE
INITIAL U.S. APPROVAL: 1994
INDICATIONS AND USAGE
Dorzolamide hydrochloride ophthalmic solution is a carbonic anhydrase
inhibitor indicated for the
treatment of elevated intraocular pressure in patients with ocular
hypertension or open-angle glaucoma.
(1) (1)
DOSAGE AND ADMINISTRATION
The dose is one drop of dorzolamide hydrochloride ophthalmic solution
in the affected eye(s) three times
daily. Dorzolamide hydrochloride ophthalmic solution may be used
concomitantly with other topical
ophthalmic drug products to lower intraocular pressure. (2) (2)
DOSAGE FORMS AND STRENGTHS
Ophthalmic solution containing dorzolamide 2% (20 mg/mL). (3) (3)
CONTRAINDICATIONS
Dorzolamide hydrochloride ophthalmic solution is contraindicated in
patients who are hypersensitive to
any component of this product. (4, 5.1) (4)
WARNINGS AND PRECAUTIONS
1. Sulfonamide Hypersensitivity (5.1)
2. Bacterial Keratitis (5.2)
3. Corneal Endothelium (5.3)
4. Allergic Reactions (5.4)
5. Acute Angle-Closure Glaucoma (5.5)
ADVERSE REACTIONS
The most frequently reported adverse reactions associated with
dorzolamide hydrochloride ophthalmic
solution were ocular burning, stinging, or discomfort immediately
following ocular administration
(approximately one-third of patients). Approximately one-quarter of
patients noted a bitter taste following
administration. Superficial punctate keratitis occurred in 10 to 15%
of patients and signs and symptoms of
ocular allergic reaction in approximately 10%. (6)
TO REPORT SUSPECTED ADVERSE REACTIONS, CONTACT AKORN OPERATING COMPANY
LLC