1 ml prolonged-release eye drops contain 20 mg of cardolol hydrochloride. The preparation contains benzalkonium chloride (10 mg / 100 ml).
Action:
Non-cardiac selective β-blocker with partial agonist activity (moderate, intrinsic sympathomimetic activity - ISA) and slight stabilizing effect of membranes. The preparation reduces intraocular pressure (regardless of the presence of glaucoma) by reducing the secretion of aqueous humor. The effect of the drug is usually visible about 30 minutes after instillation. The maximum effect occurs between 2 and 4 h after administration and persists after 24 h. The stable effect of lowering the intraocular pressure does not change over time: it can last for a year. However, sensitivity to cardiolol hydrochloride may be reduced, especially after prolonged use. The drug practically does not change the diameter of the pupil and does not affect the accommodation. The preparation contains a water-soluble polymer (alginic acid) with physical properties (such as bioadhesion and ionic interactions) that allow a reduction in the frequency of once daily administration. Mean plasma concentrations after 2 months of multiple administrations in glaucoma patients are lower after sustained release drops once daily than after regular drops twice a day.
Contraindications:
Hypersensitivity to the active substance or any of the excipients. Reactive respiratory diseases, including current or previous bronchial asthma or severe chronic obstructive pulmonary disease. Public heart failure. Cardiogenic shock. Atrio-ventricular block IIst. and III. uncontrolled starter. Sick sinoatrial node syndrome (including sinoatrial block). Sinus bradycardia. Untreated phaeochromocytoma (pheochromocytoma). Contraindications to the use of β-adrenergic drugs with a general effect should be considered, despite the fact that systemic side effects of beta-adrenergic drugs administered to the eye occur only in exceptional cases.
Precautions:
Patients taking systemic β-blockers may experience an increase in intra-ocular pressure or known effects due to general blocking of β-adrenergic receptors. You should carefully monitor the response of these patients to treatment. Co-administration of two beta-adrenergic blockers administered topically is not recommended. If drops are used to lower the intraocular pressure in patients with acute angle-closure glaucoma, the eye constrictor should be used concurrently. In these patients, the immediate goal of treatment is to reopen the angle of perception. This requires the simultaneous use of myotic drugs to narrow the pupil because cardolol has little or no effect on the pupil. During the administration of drugs that reduce the production of aqueous humor (eg, Timolol, acetazolamide) cases of choroidal detachment after filtration have been reported. During long-term treatment, the sensitivity to cardolol may be reduced, so to ensure the effectiveness of long-term treatment, check for tachyphylaxis once a year. Ophthalmic β-blockers may cause dry eye - care should be taken in patients with corneal diseases. The same cardiovascular and lung side effects may occur with the medicine, as well as other side effects that are observed when using β-blockers with a general effect. The incidence of general adverse reactions after topical ocular administration is lower than after systemic administration. In patients with cardiovascular disease (eg ischemic heart disease, Prinzmetal angina pectoris and heart failure) and hypotension, β-blocker therapy should be evaluated with particular care and consideration should be given to the use of other active substances.Patients with cardiovascular disease should be monitored for symptoms of the severity of these diseases and for side effects. Due to the prolonged duration of conduction, β-blockers should be administered with caution to patients with atrioventricular block Ist. The dose should be reduced if the heart rate at rest falls below 50-55 / min and patients have symptoms associated with it. with bradycardia. Patients with severe peripheral circulation disorders (such as severe Raynaud's disease or Raynaud's syndrome) should be treated with caution. It should be used with caution in patients with mild or moderate chronic obstructive pulmonary disease (COPD) and only if the expected benefit outweighs the potential risk. Β-blockers should be administered with caution to patients with a tendency to have spontaneous hypoglycaemia or patients with unstable diabetes because these drugs may mask the signs and symptoms of acute hypoglycaemia. The use of β-blockers in the treatment of hypertension caused by the pheochromocytoma requires close monitoring of blood pressure. In elderly patients or patients with renal and / or hepatic impairment, when β-blockers in the form of eye drops are used concomitantly with β-adrenergic agents given in general, dosage adjustment is often necessary. An exacerbation of psoriasis has been reported during the use of β-blockers. The indications for use in patients with psoriasis should be duly considered. When beta-blockers are used, patients with a history of atopy or severe anaphylactic reaction to multiple allergens may experience increased reactivity when re-exposed to these allergens. In patients prone to severe anaphylactic reaction, regardless of its cause, the use of β-blockers may exacerbate the anaphylactic reaction and resistance to treatment with epinephrine at normal doses, especially when using floctafenine, iodinated contrast agents, anesthetics or desensitization. Β-blockers administered to the eyes may block the action of β-adrenergics acting in general, e.g. adrenaline. The anesthetist should be informed about the patient's use of karteolol. If it is necessary to stop treatment, a 48-hour break should be enough to regain sensitivity to catecholamines. In some situations, treatment with β-blockers should not be interrupted: in patients with coronary insufficiency, it is recommended to continue the treatment for surgery because there is a risk of symptoms associated with sudden discontinuation of β-blockers; in urgent cases or when interruption of treatment is impossible, patients should be protected against increased vagal activity by administering atropine in premedication and at a later time, if necessary; should be used anesthetics with the least possible depressive effect on the myocardium and supplement the volume of circulating blood. Β-blockers can also mask the symptoms of hyperthyroidism, especially cardiovascular symptoms. When using β-blocker drugs, there is a risk of contact lens intolerance due to decreased tear production. The benzalkonium chloride contained in the preparation may cause eye irritation, accumulate on the lenses and discolour soft contact lenses - soft contact lenses should not be used while the preparation is being used. Before use, the lenses should be removed and not placed earlier than 15 minutes after application.
Pregnancy and lactation:
It should not be used during pregnancy unless clearly necessary. If the preparation is administered until delivery, the newborn should be carefully monitored during the first days of life. When using cardamolol hydrochloride in therapeutic doses in the form of eye drops, it is unlikely that sufficient milk will be obtained in milk to cause clinical signs of β-adrenergic blockade in the infant.
Side effects:
Common: signs and symptoms of eye irritation (eg burning, burning, itching, tearing, redness), conjunctival hyperaemia, conjunctivitis, keratitis, taste disturbances.Uncommon: dizziness, muscle aches, muscle spasms. Rare: positive test for anti-nuclear antibodies. Not known: systemic allergic reactions (including angioneurotic edema), urticaria, local and generalized rashes, pruritus, anaphylactic reaction, hypoglycaemia, insomnia, depression, nightmares, memory loss, syncope, cerebrovascular accident, cerebral ischemia, worsening of signs and symptoms post-operative myasthenia gravis, paresthesia and headache, blepharitis, blurred vision and choroidal detachment after filtration, reduced corneal sensitivity, dry eye, corneal erosion, eyelid droop, diplopia, refractive changes (in some cases due to discontinuation of a pupil that constricts the pupils), bradycardia, chest pain, palpitations, edema, arrhythmia, congestive heart failure, atrioventricular block, cardiac arrest, heart failure, hypotension, Raynaud's sign, cold hands and feet, bronchospasm (especially in patients with previously diseases spastic bronchi), shortness of breath, cough, nausea, indigestion, diarrhea, dry mouth, abdominal pain, vomiting, alopecia, psoriasis-like rash or worsening of psoriasis, skin rash, systemic lupus erythematosus, claudication, sexual dysfunction, decreased libido, impotence, asthenia /fatigue. In some patients with severe corneal damage, very rare cases of corneal calcification associated with the use of eye drops with phosphate content have been reported.
Dosage:
Adults: 1 drop into the conjunctival sac of the affected eye (eyes) once a day, in the morning. Stabilization of intraocular pressure using drops containing carteolol sometimes requires several weeks. Evaluation of treatment, which must include intraocular pressure measurement and cornea examination, should be performed at the beginning of treatment and then at regular intervals after approximately 4 weeks of treatment. An ophthalmologist may, if it deems it necessary, prescribe the use of one or more additional anti-glaucoma medications (topically or generally) in combination with carteolol in the form of drops. Other eye drops used simultaneously must be administered at least 15 minutes prior to the application of the preparation. Compression of the nasolabial canal or closing of the eyelids for 2 min reduces the systemic absorption of the drug. This can lead to a reduction in systemic side effects and increase local effects.Replacement of other medicines. If prolonged-release prolonged-release eye-drops for prolonged-release eye-drops, the use of an already-prescribed drug must be discontinued after the end of a full treatment day. The use of karteolol in the form of prolonged release drops starts from the Next day, giving 1 drop to the affected eye once a day. If we replace several anti-glaucoma medications with carteolol, discontinue the treatment with the previously used drugs one at a time. If we substitute for cardamolol in the form of drops, pupil-narrowing drugs, then after reflux of the effects of lympics, refractive examination may be necessary. The decision to use the medicine must be accompanied by the measurement of intraocular pressure, especially at the beginning of treatment. Children and adolescents (<18 years) - no clinical trials have been conducted in children and adolescents, therefore these drops are not recommended for use in this age group.