Trusopt

Trusopt

dorzolamide

Manufacturer:

Santen

Distributor:

Metro Drug
Full Prescribing Info
Contents
Dorzolamide hydrochloride.
Description
Each mL of DORZOLAMIDE HCl (TRUSOPT) 2% contains 20 mg dorzolamide (22.3 mg of dorzolamide hydrochloride).
DORZOLAMIDE HCl (TRUSOPT) is a clear, colorless to nearly colorless, slightly viscous solution containing 22.26 mg of dorzolamide hydrochloride equivalent to 20 mg of dorzolamide as an active ingredient in each mL.
It also contains benzalkonium chloride, hydroxyethyl cellulose, mannitol, sodium citrate and sodium hydroxide as additives.
Action
DORZOLAMIDE HCl (TRUSOPT) Ophthalmic Solution is a novel carbonic anhydrase inhibitor formulated for topical ophthalmic use. Unlike oral carbonic anhydrase inhibitors, DORZOLAMIDE HCl (TRUSOPT), which is administered topically, exerts its effects directly in the eye.
Pharmacology: Pharmacodynamics: Mechanism of Action: DORZOLAMIDE HCL (TRUSOPT) is a potent inhibitor of human carbonic anhydrase II. Following topical ocular administration, DORZOLAMIDE HCL (TRUSOPT) reduces elevated intra-ocular pressure, whether or not associated with glaucoma. Elevated intraocular pressure is a major risk factor in the pathogenesis of optic nerve damage and visual field loss. DORZOLAMIDE HCL (TRUSOPT) does not cause pupillary constriction and reduces intra-ocular pressure without side effects such as night blindness, accommodative spasm. DORZOLAMIDE HCL (TRUSOPT) has minimal or no effect on pulse rate or blood pressure.
In patients with glaucoma or ocular hypertension, the efficacy of dorzolamide given t.i.d. as monotherapy (baseline IOP ≥23 mmHg) or given b.i.d. as adjunctive therapy while receiving ophthalmic beta-blockers (baseline IOP ≥22 mmHg) was demonstrated in large-scale clinical studies of up to one-year duration. The IOP-lowering effect of dorzolamide as monotherapy and as adjunctive therapy was demonstrated throughout the day and this effect was maintained during long-term administration. Efficacy during long-term monotherapy was similar to betaxolol and slightly less than timolol. When used as adjunctive therapy to ophthalmic beta-blockers, dorzolamide demonstrated additional IOP lowering similar to pilocarpine 2% q.i.d.
In addition, a clinical study was undertaken in 184 (122 for dorzolamide) paediatric patients from 1 week of age to <6 years of age with glaucoma or elevated intraocular pressure (baseline IOP > 22 mmHg) to assess the safety of DORZOLAMIDE HCl (TRUSOPT) when administered topically t.i.d (three times a day). Efficacy results in paediatric patients suggest that the mean IOP decrease observed in the dorzolamide group was comparable to the mean IOP decrease observed in the timolol group even if a slight numeric advantage was observed for timolol.
Longer-term efficacy studies (>12 weeks) are not available.
Pharmacokinetics: When topically applied, dorzolamide reaches the systemic circulation.
To assess the potential for systemic carbonic anhydrase inhibition following topical administration, active substance and metabolite concentrations in red blood cells (RBCs) and plasma and carbonic anhydrase inhibition in RBCs were measured. Dorzolamide accumulates in RBCs during chronic dosing as a result of selective binding to CA-II while extremely low concentrations of free active substance in plasma are maintained. The parent active substance forms a single N-desethyl metabolite that inhibits CA-II less potently than the parent active substance but also inhibits a less active isoenzyme (CA-I). The metabolite also accumulates in RBCs where it binds primarily to CA-I. Dorzolamide binds moderately to plasma proteins (approximately 33%). Dorzolamide is primarily excreted unchanged in urine; the metabolite is also excreted in urine. After dosing ends, dorzolamide washes out of RBCs slower elimination phase with a half-life of about four months.
Indications/Uses
DORZOLAMIDE HCl (TRUSOPT) Ophthalmic Solution is indicated in the treatment of elevated intraocular pressure in patients with ocular hypertension; open-angle glaucoma, pseudoexfoliative glaucoma and other secondary open-angle glaucomas.
Dosage/Direction for Use
When used as monotherapy, the dose is one drop of DORZOLAMIDE HCl (TRUSOPT) Ophthalmic Solution in the affected eye(s) three times daily.
When used as adjunctive therapy with an ophthalmic beta-blocker, the dose is one drop of DORZOLAMIDE HCl (TRUSOPT) in the affected eye(s) two times daily.
When substituting DORZOLAMIDE HCl (TRUSOPT) for another ophthalmic antiglaucoma agent, discontinue the other agent after proper dosing on one day, and start DORZOLAMIDE HCl (TRUSOPT) on the next day.
If more than one topical ophthalmic drug is being used, the drugs should be administered at least ten minutes apart.
Overdosage
Treatment should be symptomatic and supportive. Electrolyte imbalance, development of an acidotic state and possible central nervous system effects may occur. Serum electrolyte levels (particularly potassium) and blood pH levels should be monitored.
Contraindications
DORZOLAMIDE HCl (TRUSOPT) is contraindicated in patients who are hypersensitive to any component of this product.
Special Precautions
DORZOLAMIDE HCl (TRUSOPT) has not been studied in patients with severe renal impairment (CrCl <30 mL/min). Because DORZOLAMIDE HCl (TRUSOPT) and its metabolite are excreted predominantly by the kidney, DORZOLAMIDE HCl (TRUSOPT) is not recommended in such patients.
The management of patients with acute angle-closure glaucoma requires therapeutic interventions in addition to ocular hypotensive agents. DORZOLAMIDE HCl (TRUSOPT) has not been studied in patients with acute angle-closure glaucoma.
DORZOLAMIDE HCl (TRUSOPT) has not been studied in patients with hepatic impairment and should therefore be used with caution in such patients.
DORZOLAMIDE HCl (TRUSOPT) is a sulfonamide and although administered topically, is absorbed systemically. Therefore the same types of adverse reactions that are attributable to sulfonamides may occur with topical administration. If signs of serious reactions or hypersensitivity occur, discontinue the use of this preparation.
In clinical studies, local ocular adverse effects, primarily conjunctivitis and lid reactions, were reported with chronic administration of DORZOLAMIDE HCl (TRUSOPT). Some of these reactions had the clinical appearance and course of an allergic-type reaction that resolved upon discontinuation of drug therapy. If such reactions are observed, discontinuation of treatment with DORZOLAMIDE HCl (TRUSOPT) should be considered.
There is a potential for an additive effect on the known systemic effects of carbonic anhydrase inhibition in patients receiving an oral carbonic anhydrase inhibitor and DORZOLAMIDE HCl (TRUSOPT). The concomitant administration of DORZOLAMIDE HCl (TRUSOPT) and oral carbonic anhydrase inhibitors has not been studied and is not recommended.
Choroidal detachment has been reported with administration of aqueous suppressant therapy (e.g., dorzolamide) after filtration procedures.
Choroidal detachment has been reported with administration of aqueous suppressant therapy (e.g., dorzolamide) after filtration procedures.
Ophthalmic Solution contains the preservative benzalkonium chloride, which may be absorbed by soft contact lenses. Therefore, DORZOLAMIDE HCl (TRUSOPT) should not be administered while wearing soft contact lenses. The contact lenses should be removed before application of the drops and not be reinserted earlier than 15 minutes after use.
Use in Children: Safety and effectiveness in children have not been established.
Use In Pregnancy & Lactation
Pregnancy: There are no adequate and well-controlled studies in pregnant women. DORZOLAMIDE HCl (TRUSOPT) should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Lactation: It is not known whether this drug is excreted in human milk. A decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
Side Effects
In the previous long-term clinical studies of 1108 patients treated with DORZOLAMIDE HCl (TRUSOPT) Ophthalmic Solution alone or as adjunctive therapy with ophthalmic beta-blockers, the most frequently reported drug-related adverse effects and local symptoms were: Bitter taste, burning and stinging, blurred vision, eye itching, tearing, headache, conjunctivitis, eyelid inflammation, nausea, eyelid irritation and asthenia/fatigue. The most frequent cause of discontinuation (approximately 3%) from treatment with Ophthalmic Solution was drug-related ocular adverse effects, primarily conjunctivitis and lid reactions. Iridocyclitis and rash were each reported rarely. There was one report of urolithiasis.
The following adverse reactions have been reported in post-marketing experience: Hypersensitivity: Signs and symptoms of local reactions including palpebral reactions and systemic allergic reactions including angioedema, bronchospasm, urticaria and pruritus.
Nervous System: Dizziness, paresthesia.
Ocular: Pain, redness, superficial punctate keratitis, transient myopia (which resolved upon discontinuation of therapy), eyelid crusting, choroidal detachment following filtration surgery.
Skin/ Mucous Membranes: Contact dermatitis epistaxis, throat irritation, dry mouth.
Urogenital: Urolithiasis.
Laboratory Findings: DORZOLAMIDE HCl (TRUSOPT) was not associated with clinically meaningful electrolyte disturbances.
Drug Interactions
Specific drug interaction studies have not been performed with DORZOLAMIDE HCl (TRUSOPT) Ophthalmic Solution. In clinical studies, DORZOLAMIDE HCl (TRUSOPT) was used concomitantly with the following medications without evidence of adverse interactions: Timolol ophthalmic solution, betaxolol ophthalmic solution and systemic medications, including ACE-inhibitors, calcium channel blockers, diuretics, non-steroidal anti-inflammatory drugs including aspirin, and hormones (e.g. estrogen, insulin, thyroxine).
DORZOLAMIDE HCl (TRUSOPT) is a carbonic anhydrase inhibitor and although administered topically, is absorbed systemically. In clinical studies, DORZOLAMIDE HCl (TRUSOPT) was not associated with acid-base disturbances. However, these disturbances have been reported with oral carbonic anhydrase inhibitors and have in some instances, resulted in drug interactions (e.g. toxicity associated with high-dose salicylate therapy). Therefore, the potential for such drug interactions should be considered in patients receiving DORZOLAMIDE HCl (TRUSOPT).
Storage
Store at temperatures not exceeding 30°C. Avoid freezing. Protect from light.
ATC Classification
S01EC03 - dorzolamide ; Belongs to the class of carbonic anhydrase inhibitors. Used in the treatment of glaucoma.
Presentation/Packing
Ophth soln 2% x 5 mL x 1's.
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