Combigan eye drops 5ml

Combigan eye drops - is a combined medicinal product containing two active substances: brimonidine and timolol, which can reduce increased intraocular pressure (IOP) by mutual enhancement of the effect, which contributes to more pronounced hypotensive effect.

Combigan is a combined drug that includes 2 active substances: brimonidine - adrenomimetic, which stimulates alpha2-adrenoreceptors, and timolol - a blocker of beta adrenoreceptors. Both active substances reduce intraocular pressure (IOP) due to the combined interaction, leading to a much more pronounced hypotensive effect compared to the effect of each of the components alone.

Brimonidine is an alpha-adrenergic receptor agonist, and it has a 1000-fold greater selectivity for alpha2-adrenergic receptors compared to alpha1-adrenergic receptors. Selectivity is expressed in the absence of mydriasis and vasoconstriction of the vessels of the microcirculatory bed. The hypotensive effect of brimonidine is provided by reducing the formation of intraocular fluid and increasing its outflow along the uveoscleral pathway.

Timolol is a non-selective beta-blocker, it does not possess internal sympathomimetic and membrane-stabilizing activity. Timolol reduces IOP by reducing the formation of intraocular fluid. The exact mechanism of action is not established, it may be associated with inhibition of the synthesis of cyclic adenosine monophosphate (cAMP) and is caused by endogenous stimulation of beta-adrenergic receptors.

Pharmacokinetics

The mean values of the maximum concentration of the drug in the blood plasma (Cmax) of brimonidine and timolol after the application of the Kombigan prepatare were 0.0327 and 0.406 ng / ml, respectively.

Brimonidine

When installing 0.2% solution in the form of eye drops, the concentration of brimonidine in the blood plasma is very low. Brimonidine is slightly exposed to metabolism in the eye tissues, the association with plasma proteins is about 29%. The half-life (T1 / 2) of the drug after topical application on average is about 3 hours.

The main part of the drug (about 74% of the dose absorbed into the systemic bloodstream) is excreted by the kidneys in the form of metabolites for 5 days, unchanged drug in the urine is not detected. In vitro studies on liver cells of animals and humans, it has been shown that aldehyde oxidase and cytochrome P450 are largely involved in the metabolism process. Consequently, systemic induction is determined, first of all, by the metabolism of the drug in the liver.

Timolol

80% of timolol, used in the form of eye drops, enters the systemic bloodstream by absorption through the vessels of the conjunctiva, the nasal mucosa and the lacrimal tract. After the installation of eye drops, the maximum concentration of timolol in the aqueous humor of the eye is achieved after 1-2 hours. The half-life (T1 / 2) of timolol in the blood plasma is about 7 hours. Timolol slightly binds to blood plasma proteins. Timolol is partially metabolized in the liver; the active substance and its metabolites are excreted by the kidneys.

Indications:

• open-angle glaucoma;
• ophthalmogypertension (with insufficient effectiveness of local therapy with beta-blockers).

Contraindications:

• Hypersensitivity to the components of the drug.
• Increased respiratory tract reactivity, including:
• Bronchial asthma.
• Bronchoobstruction, incl. in the anamnesis, severe chronic obstructive pulmonary disease.
• Sinus bradycardia.
• Atrioventricular blockade of II-III degree without implanted artificial pacemaker.
• Heart failure.
• Cardiogenic shock.
• Concomitant therapy with monoamine oxidase (MAO) inhibitors, antidepressants - tricyclic and tetracyclic (including mianserin).
• Age to 18 years.
• The period of breastfeeding.

Carefully:

• Renal / hepatic insufficiency (the use of the drug is not sufficiently studied in this group of patients).
• Depression
• Cerebral or coronary insufficiency.
• Reynaud's syndrome.
• Orthostatic hypotension
• Obliterating thromboangiitis.
• Severe cardiovascular diseases of unstable course.
• Diabetes.
• Episodes of hypoglycemia (in the absence of therapy).
• Pheochromocytoma (without previous treatment).
• Metabolic acidosis.
• Simultaneous use of radiocontrast preparations.
• Intravenous injection of lidocaine, blockers of "slow" calcium channels (verapamil, diltiazem) in connection with the risk of suppression of atrioventricular conduction, the development of bradycardia, heart failure and lowering blood pressure.
• Simultaneous prescribing or changing the dose of drugs taken from groups of adrenomimetics (isoprenaline) and adrenoblockers (prazosin), as well as other agents that affect adrenergic transmission - because of their possible interaction with the active components of the drug or changes in their therapeutic potential.

Special instructions:

It is impermissible to touch the tip of the bottle to any surfaces to avoid infection of the eye and the contents of the vial. Like all ophthalmic drugs used locally, Combigan can be absorbed systemically.

When allergic reactions occur, treatment with Combigan should be stopped.

In patients with severe impairment of kidney function on hemodialysis, treatment with timolol is accompanied by a marked decrease in blood pressure.

Against the background of taking a group of beta-adrenoblockers in patients with agonizing manifestations and severe anaphylactic reactions to various allergens in an anamnesis, it is possible to reduce or lack efficiency from the introduction of epinephrine in the usual doses. Beta-adrenoblockers can also hide symptoms of hyperthyroidism and worsen the course of Prinzmetal angina, vascular diseases, both peripheral and central, as well as arterial hypotension.

Signs indicating acute hypoglycemia, in particular tachycardia, palpitation and sweating, may be masked against a background of beta-blocker therapy.

If it is necessary to stop therapy with Combigan, as well as in the treatment of cardiovascular diseases with beta-blockers of systemic action, therapy is gradually phased out, in order to avoid the development of cardiac arrhythmias, myocardial infarction and / or sudden death, the risk of which increases with the abrupt withdrawal of this drug group.

The benzalkonium chloride auxiliary contained in the Combigan preparation may be irritating to the eye mucosa. Before the installation of Kombigan, it is necessary to remove contact lenses, they can be re-used after 15 minutes. Shelf life of the drug after the first opening of the bottle-dropper is 28 days. After the specified time has elapsed, the dropper should be discarded, even if it contains a residual amount of the drug. This is necessary in order to avoid the risk of infection. On a cardboard package, patients are advised to record the date the vial is opened.

Impact on the ability to manage vehicles and mechanisms

Combigan has little effect on the ability to drive vehicles and mechanisms. Against the backdrop of treatment with the drug Kombigan, transient visual impairment (fuzzy), the development of episodes of weakness and drowsiness, which may have an adverse effect if the patient's work is associated with potentially hazardous activities is possible. In case of occurrence of the specified symptomatology it is necessary to refrain from performance of dangerous kinds of activity.

Suggested Use:

In adults, including elderly patients:

Locally, instilled in the conjunctival sac of the affected eye 1 drop 2 times / day at intervals of 12 hours.

Combigan can be used with other ophthalmic drugs to reduce intraocular pressure. If you use more than 2 drugs, then you need to do a 5-minute break between instillation.

As with the use of other eye drops, to reduce the possible systemic absorption, it is recommended that the tear sack is pressed briefly (for 1 minute) in the area of the projection of the lacrimal sac at the inner corner of the eye.

Packaging:

• Comes in original packaging. Item is brand new and unopened.

Storage:

• Keep away from direct sunlight.
• Keep locked and away from children.
• Store in dry place at room temperature.
• Do not exceed storage temperature higher than 25 C

Important notice- the outer box design may vary before prior notice!