The instruction for medical use
of DORZASOPT medicine
Trade names
of Dorzasopt
the International unlicensed name
Is not present
the Dosage form
of the Drop eye 5 ml
Structure
1 ml of drug contains
active agents: a dorzolamida (in the form of a hydrochloride) 20 mg,
Timololum (in the form of a maleate) 5 mg,
excipients: hydroxyethylcellulose, Mannitolum, citric acid monohydrate, sodium hydroxide 1M solution, a benzalkoniya chloride, 1M acid chlorohydrogen, 1M hydroxide sodium solution, the water purified.
Description
Transparent, colourless or almost colourless slightly viscous solution.
Pharmacotherapeutic group
Protivoglaukomny drugs and miotik. Beta blockers. Timololum in a combination with other drugs.
The code of automatic telephone exchange S01ED51
the Pharmacological
Dorzolamid's Pharmacokinetics properties a hydrochloride
At topical administration dorzolamid gets into a system blood stream.
At prolonged use dorzolamid collects in erythrocytes
as a result of selection binding from karboangidrazy the II type, maintaining extremely low concentration of free drug in plasma. As a result of metabolism of a dorzolamid the only N-desetilny is formed the metabolite which is less expressed blocks a karboangidraza of the II type in comparison with initial substance, however at the same time inhibits a karboangidraza of the I type (less active isoenzyme). The metabolite also collects in erythrocytes where contacts mainly karboangidrazy the I type. About 33% of a dorzolamid contact proteins of blood plasma. Dorzolamid is brought with urine in not changed look and in the form of a metabolite. After drug phase-out dorzolamid it is not linearly washed away from erythrocytes that at first leads to fast decrease in its concentration, and then elimination slows down. T1/2 makes about 4 months.
Timololum a maleate
At topical administration of Timololum the maleate gets into a system blood stream. The average Cmax value after morning use was 0.46 ng/ml, after use in the afternoon – 0.35 ng/ml.
Joint effect of these substances results in more significant therapeutic effect. Decrease in intraocular pressure occurs in 20 min. after instillation, reaches a maximum in 2 h and not less than 24 Parts proceed.
A pharmacodynamics
of Dorzasopt - the combined protivoglaukomny drug. Effect of medicine is directed to reduction of the increased intraocular pressure which is a major factor of risk in pathogenesis of injury of an optic nerve and glaukomatozny deterioration in visual functions (loss of fields of vision).
Dorzolamid - selection inhibitor of a karboangidraza of the II type. The karboangidraza inhibition in a ciliary body promotes reduction of formation of ions of bicarbonate with the subsequent delay of transfer of sodium and liquid that leads to decrease in secretion of intraocular liquid. Does not cause an accommodation spasm, a miosis, a hemeralopia.
Timololum is a blocker β1- and β2 - adrenoceptors (non-selective), has no significant internal sympathomimetic activity, has no direct depressive impact on a myocardium and has no membrane stabilizing properties. Effect of Timololum is connected with decrease in formation of watery moisture in a ciliate epithelium.
The indication to use
- the increased intraocular pressure
- an open angle glaucoma (including pseudo-exfoliative glaucoma and other
types of a secondary open angle glaucoma)
the Route of administration and doses
Only for topical administration.
Dorzasopt appoint on 1 drop in a conjunctival sac of the affected eye 2 times a day.
At simultaneous use of other local ophthalmologic means the interval between instillations has to be not less than 10 minutes.
If pass from treatment with other ophthalmologic drug to Dorzasopt, then the previous drug is cancelled after a usual daily dosage, and the Dorzasopt drug treatment begins next day.
It is necessary to avoid touch of a tip of a dropper to any surfaces to avoid microbic pollution of contents of a bottle.
Side effects
Drug in general is well transferred. In clinical trials of side effects concerning this combined drug it was not observed. Side reactions were limited to already known side effects of a dorzolamid of a hydrochloride and/or Timololum of a maleate. In general system side effects were mild and did not lead to drug withdrawal.
The following possible side effects of components of drug are known:
Dorzolamida hydrochloride:
- inflammation of a century, irritation and peeling of a century, an iridocyclitis, a dot
keratitis, the tranzitorny shortsightedness (passing after drug withdrawal)
- a headache, asthenia/fatigue, paresthesias
- a Quincke's disease, a bronchospasm, a small tortoiseshell, an itching
- nasal bleeding, irritation of a throat, dryness in a mouth, skin rash
of Timololum a maleate:
At topical administration:
- conjunctivitis, blepharitis, a keratitis, decrease in sensitivity of a cornea,
reduction of formation of plaintive liquid, visual disturbances
including changes of refractivity of an eye (in some cases because of cancellation of miotik), a diplopia, a ptosis
- a ring in ears, paresthesia, a headache, an asthenia, fatigue,
dizziness, a depression, insomnia, nightmares, decrease
in memory, increase of symptoms of a myasthenia
- arrhythmia, hypotension, a faint, cardiovascular disturbances,
disturbances of a rhythm, cardiac arrest, hypostases, Reynaud's syndrome, decrease
in temperature of hands and legs
- a bronchospasm (mainly at patients with the previous
bronkhoobstruktivny pathology), cough, a stethalgia
- an alopecia, psoriazopodobny rashes or exacerbation of psoriasis
- an anaphylaxis, a Quincke's disease, a small tortoiseshell, local or
generalized rashes
- diarrhea, dyspepsia, dryness in a mouth
- decrease in a libido, Peyroni's disease, a system lupus erythematosus
At system use:
- extremity pain, decrease in tolerance to physical activities, AV-
blockade of II and III degree, sinoauricular block, a fluid lungs, deterioration
in disturbances of peripheric circulation, deterioration in a course
of stenocardia, a vazodilatation
- itch, the increased sweating, exfoliative dermatitis
- dizziness, weakness, decrease in concentration of attention, the increased
drowsiness
- vomiting, a hyperglycemia, a hypoglycemia, not Werlhof's disease,
rattles, an arthralgia, impotence, urination disturbances
- clinically significant changes at system use of Timololum
of a maleate were noted extremely seldom. Easy increase in size
of residual nitrogen, level of potassium, uric acid and triglycerides
of blood plasma, easy decrease in hemoglobin, a hematocrit, cholesterol, LPVP are described,
however the specified changes did not progress and clinically
were not shown.
Use of beta blockers can cause aggravation of a pseudoparalytic myasthenia.
Contraindications
- hypersensitivity to drug components
- a heavy renal failure (by KK less than 30 ml/min.)
- giperkhloremichesky acidosis
- sinus bradycardia
- AV-blockade of II and III degree
- the profound heart failure
- cardiogenic shock
- dystrophic processes in a cornea
- bronchial asthma (including in the anamnesis)
- a heavy chronic obstructive pulmonary disease
- heavy allergic inflammations of a mucous membrane of a nose
- children's and teenage age up to 18 years
- pregnancy and the period of a lactation
Medicinal interactions
of Specific researches of interaction of Dorzasopt with other medicines was not carried out.
At simultaneous use of blockers of β-adrenoceptors strengthening as local (decrease in intraocular pressure), and systemic action (influence on a cardiovascular system) is possible. If eye drops apply along with antihypertensive or others is warm - vascular means (for example, antagonists of calcium, reserpine, blockers of β-adrenoceptors), arterial hypotension and bradycardia can develop. It should be considered also concerning means which were accepted recently and did not manage to eliminirovatsya completely.
At combined use of Timololum and CYP2D6 inhibitors (for example, quinidine or selective serotonin reuptake inhibitors) it was reported about the potentiated effect of system blockade of beta adrenoceptors (for example, decrease in frequency of ChSS, a depression).
System beta blockers can enhance hypoglycemic effect of antidiabetic drugs and the arterial hypertension which is effect of cancellation of a clonidine (clonidine).
In spite of the fact that at monotherapy by drug the effect on a pupil is minimum or is absent, there are single descriptions of development of a mydriasis at combined use of Timololum of a maleate and adrenaline. At simultaneous use of the eye drops containing epinephrine the mydriasis is possible.
Simultaneous use of the eye drops containing epinephrine and pilocarpine strengthens effect of Timololum.
Dorzolamid exponentiates effect of other antiglaukomny drugs. Acetazoleamide at intake increases risk of development of system side effects of drug.
Effect of such inhibitors of acetylcholinesterase as fiziostigmin, Galantaminum, neostigmin or pyridostigmine (often applied at a myasthenia) can be reduced dorzolamidy.
At the combined use together with diuretics the considerable loss of potassium is possible.
Appointment along with Phenytoinum can aggravate osteoporosis.
The salicylic acid accepted together with drug can lead to development of acidosis.
Special instructions
Eye drops of Dorzasopt contain preservative a benzalkoniya chloride therefore the persons carrying rigid contact lenses should remove them before use of drug and to insert them anew not earlier than in 15 min. after instillation.
It is impossible to use drug when carrying soft contact lenses as a benzalkoniya chloride is capable to collect on lenses and to have negative impact approximately.
Features of use of the drug Dorzasopt for patients with the profound abnormal liver functions are not defined (it is necessary to use with care).
In clinical trials differences in efficiency and safety of use of drug were not observed by different age groups, however it is not necessary to exclude possibilities of higher sensitivity to drug at some elderly patients.
At topical administration dorzolamid and Timololum get into a system blood stream. In this regard side reactions can be similar to reactions which are characteristic of sulfonamides and beta blockers. At emergence of those or hypersensitivity to drug it is necessary to stop its appointment.
Before use of the drug Dorzasopt it is necessary to provide adequate control of heart failure. Patients with heavy pathology of heart in the anamnesis and symptoms of heart failure have to be under careful observation. At emergence of the first signs or symptoms of heart failure the use of drug should be stopped.
Messages about a lethal outcome as a result of a bronchospasm at patients with bronchial asthma and heart failure against the background of use of the eye drops containing Timololum a maleate are registered.
Risk of development of an urolithiasis at patients with an urolithiasis in the anamnesis can increase at Dorzasopt's use since karboangidraza inhibitor which at topical administration can be absorbed and get into a system blood stream is its part.
Therapy by beta blockers can distort some symptoms of a hypoglycemia at patients with diabetes or a hypoglycemia.
Beta blockers can smooth a hyperthyroidism course. The termination of intake of beta blockers can be the cause of aggravation of symptoms.
In case of the forthcoming surgery using the general anesthesia it is necessary to cancel drug for 48 h before operation since Timololum strengthens action of muscle relaxants and the general anesthetics.
Features of influence of medicine on ability to run the vehicle or potentially dangerous mechanisms
At use of drug development of side reactions is possible, it is necessary to avoid potentially dangerous types of activity connected with need of concentration of attention and the increased speed of psychomotor reactions.
Overdose
Symptoms: strengthening of symptoms of side effect.
Treatment: carry out symptomatic and maintenance therapy. It is necessary to control the level of electrolytes (first of all sodium) and rn blood plasma. In researches it is also shown that Timololum is not removed at dialysis.
A form of release and packing
On 5 ml in a plastic bottle with a stopper dropper and the screwing-up protective cap supplied with a safety ring.
On 1 bottle together with the instruction for medical use in the state and Russian languages put in a box of cardboard.
To Store storage conditions at a temperature not above 25ºC in the place protected from light.
To store out of children's reach!
2 years
After opening of a bottle drug to use a period of storage within 4 weeks.
Not to apply after a period of storage.
Prescription status
According to the prescription
the Producer
the Owner of a trademark and the certificate of registration of a yavlyaetsyakompaniye "UORLD MEDITSIN", Great Britain ('WORLD MEDICINE', Great Britain).
Made "RomfarmKompaniS.RL.", Otopen, St. Eroilor1A, Romania ('Rompharm Company S.R.L.', Otopeni, Eroilorstreet 1 A, Romania).
The owner of the registration certificate the UORLD MEDITSIN company, Great Britain
the Address of the organization accepting in the territory of the Republic of Kazakhstan claims from consumers on quality of products
of RK, Almaty, Turksibsky district, Suyunbaya Ave., 222
Ph. / fax: 8 (7272) 529090
To develop
of DORZASOPT medicine
Trade names
of Dorzasopt
the International unlicensed name
Is not present
the Dosage form
of the Drop eye 5 ml
Structure
1 ml of drug contains
active agents: a dorzolamida (in the form of a hydrochloride) 20 mg,
Timololum (in the form of a maleate) 5 mg,
excipients: hydroxyethylcellulose, Mannitolum, citric acid monohydrate, sodium hydroxide 1M solution, a benzalkoniya chloride, 1M acid chlorohydrogen, 1M hydroxide sodium solution, the water purified.
Description
Transparent, colourless or almost colourless slightly viscous solution.
Pharmacotherapeutic group
Protivoglaukomny drugs and miotik. Beta blockers. Timololum in a combination with other drugs.
The code of automatic telephone exchange S01ED51
the Pharmacological
Dorzolamid's Pharmacokinetics properties a hydrochloride
At topical administration dorzolamid gets into a system blood stream.
At prolonged use dorzolamid collects in erythrocytes
as a result of selection binding from karboangidrazy the II type, maintaining extremely low concentration of free drug in plasma. As a result of metabolism of a dorzolamid the only N-desetilny is formed the metabolite which is less expressed blocks a karboangidraza of the II type in comparison with initial substance, however at the same time inhibits a karboangidraza of the I type (less active isoenzyme). The metabolite also collects in erythrocytes where contacts mainly karboangidrazy the I type. About 33% of a dorzolamid contact proteins of blood plasma. Dorzolamid is brought with urine in not changed look and in the form of a metabolite. After drug phase-out dorzolamid it is not linearly washed away from erythrocytes that at first leads to fast decrease in its concentration, and then elimination slows down. T1/2 makes about 4 months.
Timololum a maleate
At topical administration of Timololum the maleate gets into a system blood stream. The average Cmax value after morning use was 0.46 ng/ml, after use in the afternoon – 0.35 ng/ml.
Joint effect of these substances results in more significant therapeutic effect. Decrease in intraocular pressure occurs in 20 min. after instillation, reaches a maximum in 2 h and not less than 24 Parts proceed.
A pharmacodynamics
of Dorzasopt - the combined protivoglaukomny drug. Effect of medicine is directed to reduction of the increased intraocular pressure which is a major factor of risk in pathogenesis of injury of an optic nerve and glaukomatozny deterioration in visual functions (loss of fields of vision).
Dorzolamid - selection inhibitor of a karboangidraza of the II type. The karboangidraza inhibition in a ciliary body promotes reduction of formation of ions of bicarbonate with the subsequent delay of transfer of sodium and liquid that leads to decrease in secretion of intraocular liquid. Does not cause an accommodation spasm, a miosis, a hemeralopia.
Timololum is a blocker β1- and β2 - adrenoceptors (non-selective), has no significant internal sympathomimetic activity, has no direct depressive impact on a myocardium and has no membrane stabilizing properties. Effect of Timololum is connected with decrease in formation of watery moisture in a ciliate epithelium.
The indication to use
- the increased intraocular pressure
- an open angle glaucoma (including pseudo-exfoliative glaucoma and other
types of a secondary open angle glaucoma)
the Route of administration and doses
Only for topical administration.
Dorzasopt appoint on 1 drop in a conjunctival sac of the affected eye 2 times a day.
At simultaneous use of other local ophthalmologic means the interval between instillations has to be not less than 10 minutes.
If pass from treatment with other ophthalmologic drug to Dorzasopt, then the previous drug is cancelled after a usual daily dosage, and the Dorzasopt drug treatment begins next day.
It is necessary to avoid touch of a tip of a dropper to any surfaces to avoid microbic pollution of contents of a bottle.
Side effects
Drug in general is well transferred. In clinical trials of side effects concerning this combined drug it was not observed. Side reactions were limited to already known side effects of a dorzolamid of a hydrochloride and/or Timololum of a maleate. In general system side effects were mild and did not lead to drug withdrawal.
The following possible side effects of components of drug are known:
Dorzolamida hydrochloride:
- inflammation of a century, irritation and peeling of a century, an iridocyclitis, a dot
keratitis, the tranzitorny shortsightedness (passing after drug withdrawal)
- a headache, asthenia/fatigue, paresthesias
- a Quincke's disease, a bronchospasm, a small tortoiseshell, an itching
- nasal bleeding, irritation of a throat, dryness in a mouth, skin rash
of Timololum a maleate:
At topical administration:
- conjunctivitis, blepharitis, a keratitis, decrease in sensitivity of a cornea,
reduction of formation of plaintive liquid, visual disturbances
including changes of refractivity of an eye (in some cases because of cancellation of miotik), a diplopia, a ptosis
- a ring in ears, paresthesia, a headache, an asthenia, fatigue,
dizziness, a depression, insomnia, nightmares, decrease
in memory, increase of symptoms of a myasthenia
- arrhythmia, hypotension, a faint, cardiovascular disturbances,
disturbances of a rhythm, cardiac arrest, hypostases, Reynaud's syndrome, decrease
in temperature of hands and legs
- a bronchospasm (mainly at patients with the previous
bronkhoobstruktivny pathology), cough, a stethalgia
- an alopecia, psoriazopodobny rashes or exacerbation of psoriasis
- an anaphylaxis, a Quincke's disease, a small tortoiseshell, local or
generalized rashes
- diarrhea, dyspepsia, dryness in a mouth
- decrease in a libido, Peyroni's disease, a system lupus erythematosus
At system use:
- extremity pain, decrease in tolerance to physical activities, AV-
blockade of II and III degree, sinoauricular block, a fluid lungs, deterioration
in disturbances of peripheric circulation, deterioration in a course
of stenocardia, a vazodilatation
- itch, the increased sweating, exfoliative dermatitis
- dizziness, weakness, decrease in concentration of attention, the increased
drowsiness
- vomiting, a hyperglycemia, a hypoglycemia, not Werlhof's disease,
rattles, an arthralgia, impotence, urination disturbances
- clinically significant changes at system use of Timololum
of a maleate were noted extremely seldom. Easy increase in size
of residual nitrogen, level of potassium, uric acid and triglycerides
of blood plasma, easy decrease in hemoglobin, a hematocrit, cholesterol, LPVP are described,
however the specified changes did not progress and clinically
were not shown.
Use of beta blockers can cause aggravation of a pseudoparalytic myasthenia.
Contraindications
- hypersensitivity to drug components
- a heavy renal failure (by KK less than 30 ml/min.)
- giperkhloremichesky acidosis
- sinus bradycardia
- AV-blockade of II and III degree
- the profound heart failure
- cardiogenic shock
- dystrophic processes in a cornea
- bronchial asthma (including in the anamnesis)
- a heavy chronic obstructive pulmonary disease
- heavy allergic inflammations of a mucous membrane of a nose
- children's and teenage age up to 18 years
- pregnancy and the period of a lactation
Medicinal interactions
of Specific researches of interaction of Dorzasopt with other medicines was not carried out.
At simultaneous use of blockers of β-adrenoceptors strengthening as local (decrease in intraocular pressure), and systemic action (influence on a cardiovascular system) is possible. If eye drops apply along with antihypertensive or others is warm - vascular means (for example, antagonists of calcium, reserpine, blockers of β-adrenoceptors), arterial hypotension and bradycardia can develop. It should be considered also concerning means which were accepted recently and did not manage to eliminirovatsya completely.
At combined use of Timololum and CYP2D6 inhibitors (for example, quinidine or selective serotonin reuptake inhibitors) it was reported about the potentiated effect of system blockade of beta adrenoceptors (for example, decrease in frequency of ChSS, a depression).
System beta blockers can enhance hypoglycemic effect of antidiabetic drugs and the arterial hypertension which is effect of cancellation of a clonidine (clonidine).
In spite of the fact that at monotherapy by drug the effect on a pupil is minimum or is absent, there are single descriptions of development of a mydriasis at combined use of Timololum of a maleate and adrenaline. At simultaneous use of the eye drops containing epinephrine the mydriasis is possible.
Simultaneous use of the eye drops containing epinephrine and pilocarpine strengthens effect of Timololum.
Dorzolamid exponentiates effect of other antiglaukomny drugs. Acetazoleamide at intake increases risk of development of system side effects of drug.
Effect of such inhibitors of acetylcholinesterase as fiziostigmin, Galantaminum, neostigmin or pyridostigmine (often applied at a myasthenia) can be reduced dorzolamidy.
At the combined use together with diuretics the considerable loss of potassium is possible.
Appointment along with Phenytoinum can aggravate osteoporosis.
The salicylic acid accepted together with drug can lead to development of acidosis.
Special instructions
Eye drops of Dorzasopt contain preservative a benzalkoniya chloride therefore the persons carrying rigid contact lenses should remove them before use of drug and to insert them anew not earlier than in 15 min. after instillation.
It is impossible to use drug when carrying soft contact lenses as a benzalkoniya chloride is capable to collect on lenses and to have negative impact approximately.
Features of use of the drug Dorzasopt for patients with the profound abnormal liver functions are not defined (it is necessary to use with care).
In clinical trials differences in efficiency and safety of use of drug were not observed by different age groups, however it is not necessary to exclude possibilities of higher sensitivity to drug at some elderly patients.
At topical administration dorzolamid and Timololum get into a system blood stream. In this regard side reactions can be similar to reactions which are characteristic of sulfonamides and beta blockers. At emergence of those or hypersensitivity to drug it is necessary to stop its appointment.
Before use of the drug Dorzasopt it is necessary to provide adequate control of heart failure. Patients with heavy pathology of heart in the anamnesis and symptoms of heart failure have to be under careful observation. At emergence of the first signs or symptoms of heart failure the use of drug should be stopped.
Messages about a lethal outcome as a result of a bronchospasm at patients with bronchial asthma and heart failure against the background of use of the eye drops containing Timololum a maleate are registered.
Risk of development of an urolithiasis at patients with an urolithiasis in the anamnesis can increase at Dorzasopt's use since karboangidraza inhibitor which at topical administration can be absorbed and get into a system blood stream is its part.
Therapy by beta blockers can distort some symptoms of a hypoglycemia at patients with diabetes or a hypoglycemia.
Beta blockers can smooth a hyperthyroidism course. The termination of intake of beta blockers can be the cause of aggravation of symptoms.
In case of the forthcoming surgery using the general anesthesia it is necessary to cancel drug for 48 h before operation since Timololum strengthens action of muscle relaxants and the general anesthetics.
Features of influence of medicine on ability to run the vehicle or potentially dangerous mechanisms
At use of drug development of side reactions is possible, it is necessary to avoid potentially dangerous types of activity connected with need of concentration of attention and the increased speed of psychomotor reactions.
Overdose
Symptoms: strengthening of symptoms of side effect.
Treatment: carry out symptomatic and maintenance therapy. It is necessary to control the level of electrolytes (first of all sodium) and rn blood plasma. In researches it is also shown that Timololum is not removed at dialysis.
A form of release and packing
On 5 ml in a plastic bottle with a stopper dropper and the screwing-up protective cap supplied with a safety ring.
On 1 bottle together with the instruction for medical use in the state and Russian languages put in a box of cardboard.
To Store storage conditions at a temperature not above 25ºC in the place protected from light.
To store out of children's reach!
2 years
After opening of a bottle drug to use a period of storage within 4 weeks.
Not to apply after a period of storage.
Prescription status
According to the prescription
the Producer
the Owner of a trademark and the certificate of registration of a yavlyaetsyakompaniye "UORLD MEDITSIN", Great Britain ('WORLD MEDICINE', Great Britain).
Made "RomfarmKompaniS.RL.", Otopen, St. Eroilor1A, Romania ('Rompharm Company S.R.L.', Otopeni, Eroilorstreet 1 A, Romania).
The owner of the registration certificate the UORLD MEDITSIN company, Great Britain
the Address of the organization accepting in the territory of the Republic of Kazakhstan claims from consumers on quality of products
of RK, Almaty, Turksibsky district, Suyunbaya Ave., 222
Ph. / fax: 8 (7272) 529090
To develop
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