

Travoprost, a synthetic analogue of prostaglandin P2-alpha, is a highly selective agonist of prostaglandin FP receptors and reduces intraocular pressure by increasing the outflow of aqueous humor. The main mechanism of drug action is associated with an increase in uveoscleral outflow. Does not have a significant impact on the production of aqueous humor.
Timolol is a non-selective blocker of beta-adrenoreceptors without sympathomimetic activity, does not have a direct depressive effect on the myocardium, does not possess membrane stabilizing activity. When applied topically reduces intraocular pressure by reducing the formation of aqueous humor and a small increase in its outflow.
Intraocular pressure decreases approximately 2 hours after application, and the maximum effect is achieved after 12 hours. A significant reduction in intraocular pressure may persist for 24 hours after a single use of the drug.
Pharmacokinetics
Travoprost and timolol are absorbed through the cornea. In the cornea hydrolysis of travoprost to the biologically active form - travoprost occurs.
Travoprost after topical administration is rapidly removed from the plasma within an hour — the plasma concentration decreases below the detection threshold — less than 0.01 ng / ml (can vary from 0.011 ng / ml to 0.02 ng / ml).
Maximum concentration (C max a) plasma timolol is 0.692 ng / ml and persists up to the detection threshold for 12 hours, and T max timolol is achieved within an hour after topical administration.
T 1/2 timolol is 4 hours after topical application of DuoTrav.
Travoprost is excreted in the form of inactive metabolites mainly with bile (61%). Travoprost free acid and its metabolites are excreted by the kidneys. Less than 2% of travoprost is found in the urine in the form of free acid.
Timolol and formed metabolites are excreted mainly by the kidneys. About 20% of timolol is excreted unchanged, the rest in the form of metabolites.
Reducing elevated intraocular pressure in open-angle glaucoma and intraocular hypertension in patients resistant to monotherapy with beta-blockers or analogues.
1 ml of the solution contains:
The main active substances: travoprost - 40 mcg; timolol - 5 mg;
Auxiliary components: benzalkonium chloride, boric acid, edetate disodium, macrogol glyceryl hydroxystearate, mannitol, trometamol and / or hydrochloric acid, purified water.
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The drug is taken orally 30 minutes before a meal or 2-4 hours after a meal. The prescribed dose of the pill should be taken whole, without chewing and drinking plenty of water.
For adults prescribed in the initial dose of 100 mg 1 time / day after meals before bedtime. On the 4th day, you can increase the dose to 150 mg. In the future, in order to achieve the optimal therapeutic effect, the dose is increased by 50 mg / day every 3-4 days until the optimum dose is reached. The daily dose of more than 150 mg should be divided into 2 doses, with a lower dose taken after lunch, and the main dose at bedtime. The maximum daily dose for outpatients is 450 mg. The maximum daily dose for inpatients is 600 mg.
In the treatment of libido disorders The recommended daily dose is 50 mg.
In the treatment of impotencein the case of drug monotherapy, the recommended daily dose of more than 200 mg, with combination therapy - 50 mg.
In the treatment of benzodiazepine addiction The recommended treatment regimen is based on a gradual, sometimes over several months, reduction of the dose of benzodiazepine. Each time, reducing the dose of benzodiazepine by 1/4 or 1/2 tablet, 50 mg of trazodone are simultaneously added. This ratio is left unchanged for 3 weeks, then proceed to a further gradual reduction of the dose of benzodiazepines until their complete abolition. After that, the daily dose of trazodone is reduced by 50 mg every 3 weeks.
For elderly and debilitated patients initial dose - up to 100 mg / day in fractional doses or 1 time / day before bedtime. The dose may be increased under the supervision of a physician, depending on the effectiveness and tolerability of the drug. Usually do not require a dose in excess of 300 mg / day.
Children aged 6-18 years: The initial daily dose of 1.5-2 mg / kg / day, divided into several doses. If necessary, gradually increase the dose to 6 mg / kg / day with an interval of 3-4 days.
From the side of the central nervous system: fatigue, drowsiness, agitation, headache, dizziness, weakness, myalgia, discoordination, paresthesia, disorientation, tremor.
Since the cardiovascular system and blood (hematopoiesis, hemostasis): decrease in blood pressure, orthostatic hypotension due to adrenolytic action (especially in individuals with vasomotor lability), arrhythmia, conduction disturbance, bradycardia.
From the hemopoietic system: leukopenia and neutropenia (usually minor).
From the digestive system: dry and bitter mouth, nausea, vomiting, diarrhea, loss of appetite.
Other: allergic reactions, eye irritation, priapism (you should immediately stop taking the drug and consult a doctor).
- Pregnancy.
- Lactation period.
- Children's age up to 6 years.
- Hypersensitivity to the drug.
Precautions should be prescribed to patients with:
- AV blockade.
- Myocardial infarction (early recovery period).
- Arterial hypertension (may require correction of doses of antihypertensive drugs).
- Ventricular arrhythmia.
- Priapism in history.
- Renal and / or liver failure.
- As well as patients under the age of 18 years.
Trazodone may enhance the effect of certain antihypertensive drugs and usually requires a reduction in their doses. The simultaneous appointment with drugs that depress the central nervous system (including clonidine, methyldopa), enhances the effect of the latter. Antihistamines and drugs with anticholinergic activity enhance the anticholinergic effect of trazodone.
The drug is contraindicated for use during pregnancy and lactation (breastfeeding).
Since the drug has some adrenolytic activity, the development of bradycardia and a decrease in blood pressure are possible. Therefore, it should be carefully prescribed the drug to patients with impaired cardiac conduction, AV-blockade of varying severity, in patients with recent myocardial infarction. When using trazodone, there may be some decrease in the number of leukocytes, which does not require specific treatment, except in cases of severe leukopenia. Therefore, during the period of treatment it is recommended to conduct studies of peripheral blood, especially in the presence of sore throat when swallowing and the appearance of fever.The drug does not have an anticholinergic effect, so it can be administered to elderly patients suffering from prostatic hypertrophy, angle-closure glaucoma, impaired cognitive functions.
With the appearance of long and inadequate erections, the patient should consult a doctor. During the period of treatment, the patient should refrain from drinking alcohol.
Use in pediatrics: there are no studies on the effectiveness of the drug in pediatrics, so the drug should be used with caution in children and adolescents under the age of 18 years. Doses for children under 6 years of age have not been established.
Influence on ability to drive motor transport and control mechanisms: since the drug has anxiolytic and sedative activity, a decrease in the ability to concentrate and the speed of psychomotor reactions is possible. During treatment, the patient should avoid practicing potentially hazardous activities, including driving vehicles and driving mechanisms.
Symptoms: nausea, drowsiness, hypotension, increased frequency and severity of side effects.
Treatment: There is no specific antidote to the drug. In cases of overdose, symptomatic treatment is carried out (including gastric lavage, forced diuresis).