Dorzolamid

When ATH:
S01EC03

Characteristic.

Carbonic anhydrase inhibitors. Dorzolamida hydrochloride is a white or almost white crystalline powder, soluble in water, slightly soluble in methanol and ethanol. Molecular weight 360,90.

Pharmacological action.
Protivoglaukomnoe.

Application.

According to Physicians Desk Reference (2009), dorzolamida hydrochloride in the form 2% ophthalmic solution is indicated for the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma.

Contraindications.

Hypersensitivity.

Pregnancy and breast-feeding.

When pregnancy is possible, if the effect of therapy outweighs the potential risk to the fetus (adequate and well-controlled studies of the safety of use in pregnant women were not conducted).

Category actions result in FDA - C. (The study of reproduction in animals has revealed adverse effects on the fetus, and adequate and well-controlled studies in pregnant women have not held, However, the potential benefits, associated with drugs in pregnant, may justify its use, in spite of the possible risk.)

Teratogenic effects. In studies of the toxic impact of dorzolamida hydrochloride during pregnancy in rabbits when administered in doses ≥ 2,5 mg / kg / day (in 31 times the recommended human ophthalmic use in the) were marked malformations of the vertebral bodies (were observed at doses, causing metabolic acidosis) and reduced weight gain in females and fetuses. There was no occurrence of malformations, associated with the use of dorzolamida hydrochloride, in studies in rats with doses up to 10 mg / kg / day (in 125 times the recommended human dose in the ophthalmic use).

Dorzolamida hydrochloride studies from lactating rats was decreased weight gain at 5-7% in offspring with the introduction of its rats in lactation at dose 7,5 mg / kg / day (in 94 times higher than the recommended human ophthalmic dose for application). There was a slight delay in postnatal development, incl. the eruption of incisors and open eye combined with a reduction in weight of fruit.

Unknown, whether dorzolamida hydrochloride in breast milk of lactating women. Considering, that it can cause serious side effects in children, breastfed, nursing mothers should stop breast-feeding or, or use dorzolamida.

Side effects.

Data from controlled clinical trials

From the nervous system and sensory organs: approximately 1/3 patients is burning, tingling or discomfort in the eyes after instillation; 10-15% — pinpoint superficial keratitis; about 10% -signs and symptoms of ocular allergic reactions; 1-5%-conjunctivitis and eyelid reactions from (cm. Precautions), blurred vision, eye redness, lacrimation, dry eyes, photophobia; seldom - a headache, fatigue/tiredness.

From the digestive tract: approximately 1/4 patients — a bitter taste in the mouth after use; rarely - nausea.

Other: in rare cases, skin rashes, urolithiasis, iridocyclitis.

In a three-month clinical study in children profile of side effects when applying dorzolamida hydrochloride as ophthalmic solution was comparable with that in adult patients.

Clinical practice

Side effects, who either observed in clinical trials with a frequency of less than 1%, or experienced in clinical practice in applying 2% ophthalmic solution dorzolamida hydrochloride (and the frequency of their manifestation is not defined): signs and symptoms of systemic allergic reactions (incl. angioedema, bronchospasm, itch, hives), dizziness, paraesthesia, eye pain, transient myopia, choroidal detachment after trabekuljektomii, coalescence age, dyspnoea, contact dermatitis, nose bleed, dry mouth, irritation in the throat.

Cooperation.

While conducting clinical trials of dorzolamida hydrochloride in the form 2% ophthalmic solution is not reported on violations of acid-base and electrolyte balance, such violations were reported when oral carbonic anhydrase inhibitors and in some cases caused a number of drug interactions, incl. manifestation of toxicity, associated with the reception of high doses of salicylates). Therefore, you should consider the possibility of drug interaction in patients, using ophthalmic solution dorzolamida.

There is a chance of increasing the known systemic effects, associated with the inhibition of carbonic anhydrase, patients, receiving carbonic anhydrase inhibitors interior and local (combined use not recommended).

Overdose.

You may experience the following symptoms: electrolyte imbalance, Acidosis, disorders of the nervous system.

Treatment: symptomatic, requires monitoring of electrolytes (especially potassium) levels and control the pH value of blood.

Dosing and Administration.

Konъyunktyvalno. Buried at 1 drop into the affected eye (or eyes) 3 once a day. If you use other local ophthalmic means the interval between instilljacijami should be not less than 10 m.

Precautions.

Dorzolamida hydrochloride is a sulfonamide and although applied topically, subjected to systemic absorption. In this regard, in applying dorzolamida in the form of eye drops may experience adverse reactions, characteristic of sulfonamides. There were, Although rarely, deaths due to severe reactions to sulfonamides, including Stevens-Johnson Syndrome, toxic epidermal necrolysis, fulminant gepatonekroz, agranulocytosis, aplastic anemia, etc.. blood diskrazii. Sensitization to sulfonamides may occur with repeated use, regardless of the route of administration. When serious adverse reactions or hypersensitivity manifestation of the use should be discontinued.

In patients with acute angle-closure glaucoma in addition to funds, applies when ocular, needed additional therapeutic measures. Application 2% ophthalmic solution dorzolamida hydrochloride in patients with acute attack zakratougolna glaucoma was not investigated.

Be careful to use 2% ophthalmic solution dorzolamida hydrochloride in patients, with low corneal endothelial cell density, because this category of patients have increased risk of developing corneal edema.

Features of use in patients with severe renal impairment (Cl creatinine less than 30 ml / min) not determined. As dorzolamida hydrochloride (like its metabolite) write mainly via the kidneys, not recommended to appoint him in this pathology.

Features of the application in patients with impaired liver function is not defined (should be used with caution).

In clinical studies with prolonged use of dorzolamida hydrochloride in the form 2% ophthalmic solution, reported on the development of local side effects, mainly conjunctivitis and eyelid reactions from the. Many of these reactions had clinical manifestations and over by type of allergic and took place after the cancellation HP. When such reactions drug should be lifted and assess the condition of the patient before resuming therapy.

Cases were reported of development of bacterial keratitis, associated with the use of ophthalmic funds in mul'tidoznyh bottles. When you use nenamerennaja possible contamination of the contents of the vial and the emergence of ophthalmic infections.

You should not use the ophthalmic solution dorzolamida hydrochloride while wearing contact lenses.