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APO-DORZOLAMIDE is a brand name for Dorzolamide, supplied as a solution. The medicine, its uses, side effects and dosage are the same regardless of brand.
Used for: AND CLINICAL USE............................................................... 3 CONTRAINDICATIONS .................................................................................... 3 WARNINGS AND PRECAUTIONS................................................................... 4 ADVERSE REACTIONS…
Verbatim from this product's HC label. Tap a section to expand.
Recommended Dose and Dosage Adjustment When used as monotherapy, the dose is one drop of APO-DORZOLAMIDE (dorzolamide hydrochloride) Ophthalmic Solution 2% in the affected eye(s) three times daily. When used as adjunctive therapy with an ophthalmic beta-blocker, the dose is one drop of APO- DORZOLAMIDE Ophthalmic Solution in the affected eye(s) two times daily.
When substituting APO-DORZOLAMIDE Ophthalmic Solution for another ophthalmic antiglaucoma agent, discontinue the other agent after proper dosing on one day, and start APO- DORZOLAMIDE Ophthalmic Solution on the next day. If more than one topical ophthalmic drug is being used, the drugs should be administered at least ten minutes apart.
Missed Dose If a dose is missed, it should be applied as soon as possible. However, if it is almost time for the next dose, the missed dose should be skipped and the next dose should be taken as usual. OVERDOSAGE No data are available in humans in regard to overdosage by accidental or deliberate ingestion.
The most common signs and symptoms to be expected with overdosage of dorzolamide are electrolyte imbalance, development of an acidotic state, and possibly central nervous system effects (see ADVERSE REACTIONS). Treatment should be symptomatic and supportive.
Serum electrolyte levels (particularly potassium) and blood pH levels should be monitored. Significant lethality was observed in female rats and mice after single oral doses of dorzolamide hydrochloride of 11369 mg/m2 or 1927 mg/kg (24000 times the maximum recommended human ophthalmic dose) and 3960 mg/m2 or 1320 mg/kg (16000 times the maximum recommended human ophthalmic dose), respectively.
For management of a suspected drug overdose, contact your regional Poison Control Centre. _____________________________________________________________________________________________ APO-DORZOLAMIDE Product Monograph Page 9 of 20 ACTION AND CLINICAL PHARMACOLOGY Mechanism of Action Dorzolamide hydrochloride ophthalmic solution is a carbonic anhydrase inhibitor formulated for topical ophthalmic use.
Inhibition of carbonic anhydrase in the ciliary processes of the eye decreases aqueous humor secretion, presumably by slowing the formation of bicarbonate ions with subsequent reduction in sodium and fluid transport. The result is a reduction in intraocular pressure (IOP).
General Dorzolamide hydrochloride ophthalmic solution 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, including severe reactions such as Stevens-Johnson syndrome and toxic epidermal necrolysis.
If signs of serious reactions or hypersensitivity occur, discontinue the use of this preparation. The management of patients with acute angle-closure glaucoma requires therapeutic interventions in addition to ocular hypotensive agents.
Dorzolamide hydrochloride ophthalmic solution has not been studied in patients with acute angle-closure glaucoma. Immune Immunology and Hypersensitivity In clinical studies, local ocular adverse effects, primarily conjunctivitis and eyelid reactions, were reported with chronic administration of dorzolamide hydrochloride ophthalmic solution.
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 hydrochloride ophthalmic solution should be considered.
Ophthalmologic Corneal Edema There is an increased risk of developing irreversible corneal edema in a subset of glaucoma patients with endothelial abnormalities including cellular density and/or morphology. In this group of patients evaluation of the cornea with particular attention to the corneal endothelium is recommended prior and during treatment with dorzolamide hydrochloride ophthalmic solution.
Corneal Edema and Irreversible Corneal Decompensation Corneal edema and irreversible corneal decompensation has been reported in patients with pre- existing chronic corneal defects and/or a history of intraocular surgery while using dorzolamide.
Dorzolamide hydrochloride ophthalmic solution should be used with caution in such patients. , dorzolamide) after filtration procedures. Management of eyes with chronic or recurrent choroidal detachment should include stopping all forms of aqueous suppressant therapy and treating endogenous inflammation vigorously.
Not medical advice. Always read the patient information leaflet and follow your prescriber or pharmacist.
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Pharmacokinetics Unlike oral carbonic anhydrase inhibitors, topically-applied dorzolamide hydrochloride ophthalmic solution exerts its effects at substantially low doses and therefore with less systemic exposure. When applied topically, dorzolamide reaches the systemic circulation.
To assess the potential for systemic carbonic anhydrase inhibition following topical administration, drug and metabolite concentrations in 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 drug in plasma are maintained.
The parent drug forms a single N-desethyl metabolite that inhibits CA-II less potently than the parent drug 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 excreted unchanged in the urine; the metabolite is also excreted in urine. After dosing ends, dorzolamide washes out of RBCs in a non-linear manner, resulting in a rapid decline of drug concentration initially, followed by a slower elimination phase with a half-life of about four months.
To simulate the maximum systemic exposure after long term topical ocular administration, dorzolamide was given orally to eight healthy subjects for up to 20 weeks. d. Dorzolamide and metabolite reached steady state by 4 and 13 weeks, respectively, and the following observations were noted: • In plasma, concentrations of dorzolamide and metabolite were generally below the assay limit of quantitation (15nM) indicating almost no free drug or metabolite; • In RBCs, dorzolamide concentrations approached the binding capacity of CA-II (20-25 μM) and metabolite concentrations approached 12-15 μM, well below the binding capacity of CA- I (125-155 μM); _____________________________________________________________________________________________ APO-DORZOLAMIDE Product Monograph Page 10 of 20 • In RBCs, inhibition of CA-II activity and total carbonic anhydrase activity was below the degree of inhibition anticipated to be necessary for a pharmacological effect on renal function and respiration.
STORAGE AND STABILITY APO-DORZOLAMIDE Ophthalmic Solution:
Store at room temperature 15°-30°C (59° - 86°F). Protect from light. DOSAGE FORMS, COMPOSITION AND PACKAGING APO-DORZOLAMIDE Ophthalmic Solution is supplied as a sterile, isotonic, buffered, slightly viscous, aqueous solution of dorzolamide hydrochloride.
3 mg of dorzolamide hydrochloride). Non-medicinal ingredients: hydroxyethyl cellulose, mannitol, sodium citrate dihydrate, sodium hydroxide (to adjust pH) and water for injection. 0075% is added as a preservative. APO-DORZOLAMIDE Ophthalmic Solution is a clear to slightly opalescent, colourless to nearly colourless, slightly viscous solution supplied in a white, opaque LDPE bottle with controlled drop tip.
Available in bottles of 5 mL (partial fill in an 11 mL bottle) and 10 mL. _____________________________________________________________________________________________ APO-DORZOLAMIDE Product Monograph Page 11 of 20 PART II: SCIENTIFIC INFORMATION PHARMACEUTICAL INFORMATION Drug Substance Proper name: dorzolamide hydrochloride Chemical name: […]
_____________________________________________________________________________________________ APO-DORZOLAMIDE Product Monograph Page 5 of 20 Contact Lenses Dorzolamide hydrochloride ophthalmic solution has not been studied in patients wearing contact lenses.
The preservative in dorzolamide hydrochloride ophthalmic solution, benzalkonium chloride, may be absorbed by soft contact lenses. Patients should be instructed to remove their lenses before application of the drops and not to re-insert the lenses earlier than 15 minutes after use.
Hepatic Hepatic Impairment Dorzolamide hydrochloride ophthalmic solution has not been studied in patients with hepatic impairment and should therefore be used with caution in such patients.
Special Populations Pregnant Women:
There are no adequate and well-controlled studies in pregnant women. Dorzolamide hydrochloride ophthalmic solution should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Nursing Women:
It is not known whether dorzolamide is excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions from dorzolamide hydrochloride ophthalmic solution in nursing infants, 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.
5 mg/kg/day (94 times the maximum recommended human ophthalmic dose) were seen during lactation. 5 mg/kg/day (94 times the maximum recommended human ophthalmic dose).
Pediatrics:
Safety and effectiveness in children have not been established.
Geriatrics (>65 years of age):
Of the total number of patients in clinical studies of dorzolamide hydrochloride ophthalmic solution, 44% were 65 years of age and over, while 10% were 75 years of age and over. No overall differences in effectiveness or safety were observed between these patients and younger patients, but greater sensitivity of some older individuals to the product cannot be ruled out.
_____________________________________________________________________________________________ APO-DORZOLAMIDE Product Monograph Page 6 of 20 Monitoring and Laboratory Tests Dorzolamide hydrochloride ophthalmic solution was not associated with clinically meaningful electrolyte disturbances.
ADVERSE REACTIONS Adverse Drug Reaction Overview In long-term studies of 1108 patients treated with dorzolamide hydrochloride ophthalmic solution as monotherapy or as adjunctive therapy with an ophthalmic beta-blocker, the most frequent cause of discontinuation (approximately 3%) from treatment with dorzolamide hydrochloride ophthalmic solution was drug-related ocular adverse effects, primarily conjunctivitis and eyelid reactions (see WARNINGS AND PRECAUTIONS).
In clinical studies, the most common ocular complaints were burning and stinging, blurred vision, itching and tearing. Bitter taste was also frequently reported. If these local symptoms were considered clinically important by investigators they also appear as adverse experiences in the listing below.
For dorzolamide hydrochloride ophthalmic solution the most frequently reported ocular drug related adverse events were burning and stinging 38%, taste perversion 13%, conjunctival injection 5%, corneal erosion 4%, follicular conjunctivitis 3%, and blurred vision 3%.
Clinical Trial Adverse Drug Reactions Adverse experiences that […]