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ATC code:S SENSORY DRUGS; S01 DRUGS USED IN OPHTHALMOLOGY; S01E ANTIGLAUCOMA DRUGS AND MIOTICS; S01E D Beta-adrenergic blockers; S01E D51 Timolol, combinations
Country of manufacture:Romania
Diabetics:Can
Delivery
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Payment
Bimoptic Plus eye drops 0.3 + 5 mg / ml bottle 3 ml No. 1
588.30 грн.
Description
Instructions for use Bimoptic Plus eye drops 0.3 + 5 mg / ml bottle 3 ml No. 1
Composition
active ingredients: bimatoprost, timolol (in the form of timolol maleate);
1 ml of eye drops, solution contains bimatoprost 0.3 mg; timolol 5.0 mg (in the form of timolol maleate 6.8 mg);
Excipients: citric acid, monohydrate; disodium hydrogen phosphate heptahydrate; sodium chloride; benzalkonium chloride; 1 M solution of sodium hydroxide or hydrochloric acid; purified water.
Dosage form
Eye drops, solution.
Main physicochemical properties: transparent colorless or light yellow solution.
Pharmacotherapeutic group
Drugs used in ophthalmology. Antiglaucoma and miotic drugs. Beta-blockers. Timolol, combinations. ATX code S01E D51.
Pharmacological properties
Pharmacodynamics
Bimoptic Plus Rompharm is a combination drug that contains bimatoprost and timolol maleate, which reduce high intraocular pressure (IOP) due to their combined action, which allows for a more pronounced effect compared to the effect of each substance separately. Bimoptic Plus Rompharm is a fast-acting drug.
Bimatoprost is an ophthalmic agent that lowers IOP and belongs to the synthetic prostamide group, and by chemical structure it belongs to prostaglandin F2α (PGF2α); bimatoprost does not affect any of the known types of prostaglandin receptors.
Bimatoprost selectively mimics the effects of newly discovered biosensitized substances, prostamides. However, prostamide receptors have not yet been structurally identified.
The mechanism of IOP-lowering by bimatoprost involves increased outflow of intraocular fluid through the trabecular nasolacrimal ducts and from the uveoscleral compartments of the eye.
Timolol is a non-selective beta1- and beta2-adrenergic blocker without intrinsic sympathomimetic and membrane-stabilizing activity.
Timolol lowers IOP by reducing the production of intraocular fluid. The exact mechanism of action of timolol has not been established, it is probably associated with inhibition of the synthesis of cyclic adenosine monophosphate (c-AMP) and is caused by endogenous stimulation of beta-adrenergic receptors.
Clinical effects
The IOP-lowering ability of bimatoprost/timolol is not inferior to the results obtained during adjunctive therapy with bimatoprost (once daily) and timolol (twice daily).
Published data on bimatoprost/timolol suggest that evening administration may be more effective in lowering IOP than morning administration. However, the likelihood of adherence should be considered when choosing morning or evening dosing.
Pharmacokinetics
The drug Bimoptic Plus Rompharm
Plasma concentrations of bimatoprost and timolol were determined in a crossover study comparing monotherapy with bimatoprost/timolol in healthy volunteers.
Systemic absorption of the drug is minimal and does not differ either with combined treatment or when each of the components of the drug is taken separately.
In two 12-month studies measuring systemic absorption, no accumulation of any component was observed.
Bimatoprost
In in vitro studies, bimatoprost penetrated well into the cornea and sclera. With topical application of bimatoprost eye drops, the total systemic exposure is very low, without cumulation. When instilling 0.03% bimatoprost solution 1 drop in both eyes 1 time per day for 2 weeks in healthy volunteers, the maximum concentration of bimatoprost in the blood plasma was achieved within 10 minutes after application and within 1.5 hours its concentration in the blood plasma decreased below the level of detection (0.025 ng/ml). The mean values of Cmax and area under the concentration-time curve (AUC0-24 h) of bimatoprost were similar on the 7th and 14th day of application and were 0.08 ng/ml and 0.09 ng•h/ml, respectively, indicating that the equilibrium concentration of bimatoprost was achieved within the first week of topical application.
Bimatoprost is moderately distributed in tissues, and the volume of systemic distribution in humans at steady state was 0.67 l/kg. Bimatoprost is predominantly found in plasma. Bimatoprost is approximately 88% bound to plasma proteins.
Bimatoprost is not extensively metabolized in the human eye and is one of the major circulating substances in the blood when it enters the systemic circulation after topical application. Bimatoprost is then subjected to glucuronidation, oxidation, N-diethylation and deamidation to form various metabolites.
Bimatoprost is primarily excreted in the urine: approximately 67% of an intravenous dose of bimatoprost was excreted in the urine, and 25% of the dose was excreted via the gastrointestinal tract. The elimination half-life determined after intravenous administration was approximately 45 minutes; total plasma clearance was 1.5 L/h/kg.
After twice daily administration, the mean area under the concentration-time curve (AUC0-24 h) was 0.0634 ng h/ml in elderly subjects (≥65 years) and was statistically significantly higher than in young subjects (0.0218 ng h/ml). However, this is not considered clinically significant as systemic exposure in both young and elderly subjects was negligible when using eye drops. No accumulation of bimatoprost in the blood was observed over time, and the drug was equally effective and safe in both young and elderly subjects.
Timolol
In patients undergoing cataract surgery, after instillation of eye drops in the form of a 0.5% solution, the peak concentration of timolol in the intraocular fluid after 1 hour was 898 ng/ml.
Some of the drug enters the systemic circulation and is metabolized by the liver. The half-life of timolol in plasma is approximately 4–6 hours. Timolol is partially metabolized by the liver, and its metabolites are excreted by the kidneys. Timolol binds to plasma proteins to a small extent.
Indication
Reduction of intraocular pressure (IOP) in adult patients with open-angle glaucoma and intraocular hypertension when monotherapy with beta-blockers or prostaglandin analogues for topical use is insufficient.
Contraindication
Hypersensitivity to timolol, bimatoprost and/or excipients included in the preparation.
Respiratory tract hyperreactivity syndrome, including bronchial asthma in the acute stage and a history of episodes, severe chronic obstructive bronchopulmonary (COPD) diseases.
Sinus bradycardia, sick sinus syndrome, sinoatrial block, second and third degree atrioventricular block not controlled by a pacemaker, clinically pronounced heart failure, cardiogenic shock.
Interaction with other medicinal products and other types of interactions
No interaction studies have been conducted with the fixed combination of bimatoprost/timolol.
There is a possibility of additive effects, which can lead to arterial hypotension and/or pronounced bradycardia, with the simultaneous use of eye drops containing beta-blockers and calcium channel blockers, guanethidine, beta-blockers, parasympathomimetics, antiarrhythmics (including amiodarone) and digitalis glycosides.
Cases of increased systemic beta-blockade (e.g., decreased heart rate, depression) have been reported during combination treatment with CYP2D6 inhibitors (e.g., quinidine, fluoxetine, paroxetine) and timolol.
Mydriasis has been observed rarely as a result of the concomitant use of ophthalmic beta-blockers and adrenaline (epinephrine).
Application features
Like other ophthalmic drugs, Bimoptic Plus Rompharm can penetrate the systemic circulation. Due to the presence of timolol, a beta-adrenergic component, various types of adverse reactions (cardiovascular and respiratory) may occur, as with the use of systemic beta-blockers. The frequency of adverse reactions with topical administration of the drug is lower than with systemic administration.
The drug Bimoptic Plus Rompharm should be prescribed with caution:
patients with acute eye inflammation (e.g. uveitis) due to the possibility of increased inflammation; patients at risk of macular edema, including cystoid macular edema. Bimoptic Plus Rompharm should be used with caution in patients with aphakia, pseudophakia with posterior lens capsule rupture, patients with a known risk of macular edema (e.g. after intraocular surgery, retinal vein occlusion, inflammatory eye diseases and diabetic retinopathy).
Cardiac disease: Patients with cardiovascular disease (e.g. coronary artery disease, Prinzmetal's angina and heart failure) and antihypertensive therapy with beta-blockers should be carefully monitored. It is recommended that therapy with other active substances be considered.
Patients with cardiovascular disease should be monitored for signs of worsening of these conditions and adverse reactions.
Due to the negative effect on impulse conduction time, beta-blockers should be used with great caution in patients with first-degree heart block.
Vascular disorders: The drug should be used with caution in patients with severe peripheral circulatory disorders (e.g., severe forms of Raynaud's disease or Raynaud's syndrome).
Respiratory disorders: Respiratory disorders, including fatal cases due to bronchospasm, have been reported in patients with asthma following the use of some ophthalmic beta-blockers.
Endocrine disorders: Beta-adrenergic receptor blocking agents should be used with caution in patients with spontaneous hypoglycemia or in patients with unstable diabetes, as beta-blockers may mask the symptoms of acute hypoglycemia.
Beta-adrenergic blockers may also mask the symptoms of hyperthyroidism.
Corneal diseases: Ophthalmic beta-blockers may cause dry eyes and should be used with caution in patients with corneal diseases.
Anaphylactic reactions: When beta-blockers are used in patients with atopic diseases or with severe anaphylactic reactions to a wide range of allergens, doses usually used to interrupt anaphylactic reactions may be ineffective in the presence of beta-blockers.
Surgical anesthesia: Beta-blocking ophthalmic drugs may block the effects of systemic beta-agonists, such as adrenaline. If the patient is taking timolol, the anesthesiologist should be informed.
Liver and kidney function. The use of Bimoptic Plus Rompharm in patients with impaired liver and kidney function has not been studied, therefore caution should be exercised when treating patients in these groups.
In patients with mild liver disease or baseline elevated liver enzymes – alanine transaminase (ALT), aspartate transaminase (AST) and/or total bilirubin – bimatoprost did not affect liver function over a study period of more than 24 months.
There are no known adverse liver reactions when timolol is used in the eyes.
Visual disturbances. Before starting treatment, patients should be informed about the possible growth of eyelashes, darkening of the eyelids or periocular area and increased pigmentation of the iris (brown color), as such reactions have been observed during treatment with bimatoprost and Bimoptic Plus Rompharm. Increased pigmentation of the iris may become permanent and may lead to differences in the appearance of the eyes if only one eye is treated.
As a result of 12 months of treatment with the drug, iris pigmentation was noted in 0.2% of patients. And as a result of 12 months of treatment with bimatoprost eye drops alone, it was observed in 1.5%, and no further increase in the frequency of this effect was observed during 3 years of therapy. Increased iris pigmentation is due to increased production of melanocytes, and not just an increase in their number. The long-term effect of increased iris pigmentation has not been reported. Changes in iris color during treatment with bimatoprost eye drops may not appear for several months to several years. Treatment does not affect birthmarks and iris spots. In some patients, pigmentation of the skin around the eyes disappeared.
Retinal detachment: Retinal detachment has been reported with the use of aqueous suppressant therapy (e.g., timolol, acetazolamide) following filtration procedures.
Skin disorders
Hair growth is possible in areas where Bimoptic Plus Rompharm repeatedly comes into contact with the skin surface. Therefore, it is important to use Bimoptic Plus Rompharm as directed to avoid it running down the cheek or other areas of the skin.
Other beta-blockers. The effect on IOP or the known effects of systemic beta-blockade may be potentiated if timolol is administered to patients already receiving systemic beta-blocking agents. The response of such patients to treatment should be closely monitored. The concomitant use of two topical beta-adrenergic blocking agents is not recommended.
Excipients
The preservative benzalkonium chloride, which is part of the drug Bimoptic Plus Rompharm, may cause eye irritation.
Patients who wear soft contact lenses should be advised to remove them before instillation of the drug and to reinsert them 15 minutes after using the eye drops.
Benzalkonium chloride may discolor soft contact lenses. Contact with soft contact lenses should be avoided.
Benzalkonium chloride has been reported to cause punctate keratopathy and/or toxic ulcerative keratopathy. Therefore, patients with dry eye syndrome or corneal damage should be monitored if they use Bimoptic Plus Rompharm frequently or for long periods.
The use of the drug in patients with inflammatory eye diseases, neovascular, inflammatory, angle-closure glaucoma, congenital glaucoma, and narrow-angle glaucoma has not been studied.
Studies of 0.03% bimatoprost ophthalmic solution in patients with glaucoma and ocular hypertension have shown that frequent use of more than one dose of bimatoprost per day may reduce the hypotensive effect. Patients using Bimoptic Plus Rompharm with other prostaglandin analogues should be monitored for changes in IOP.
As with the topical use of other ophthalmic drugs, systemic absorption of the active substances of Bimoptic Plus Rompharm (bimatoprost and timolol) is possible, although no increase in systemic absorption of individual active substances has been observed. Due to the beta-adrenergic component - timolol - the same types of cardiovascular, pulmonary and other adverse reactions are possible as with the use of systemic beta-blockers.
Ability to influence reaction speed when driving vehicles or other mechanisms
Bimoptic Plus Rompharm has a minor influence on the ability to drive or use machines. As with other ophthalmic drugs, if temporary blurred vision occurs during instillation, you should wait until your vision clears before driving or using machines.
Use during pregnancy or breastfeeding
Pregnancy
There are no adequate data from the use of bimatoprost/timolol fixed combination in pregnant women. Bimoptic Plus Rompharm should be used during pregnancy only if clearly needed. Regarding reduced systemic absorption, see section “Dosage and administration”.
Bimatoprost
There are no adequate clinical data on use in pregnant women. Animal studies have shown reproductive toxicity at high doses.
Timolol
Epidemiological studies have not revealed any malformative effects, but have shown a risk of intrauterine growth retardation with oral beta-blockers. In addition, symptoms of beta-blockade (e.g. bradycardia, hypotension, respiratory failure and hypoglycaemia) have been observed in neonates when beta-blockers have been administered before delivery. Therefore, the neonate should be closely monitored during the first days of life. Animal studies with timolol have shown reproductive toxicity at doses considerably higher than those used in clinical practice.
Breast-feeding
Timolol
Beta-blockers are excreted in breast milk. However, when using therapeutic doses of timolol in the form of eye drops, the presence of a significant amount of the substance in breast milk that would cause clinical symptoms of beta-adrenergic receptor blockade in the newborn is unlikely.
Bimatoprost
It is not known whether bimatoprost is excreted in human milk, but studies in rats have shown the presence of bimatoprost in the milk of lactating rats. Bimoptic Plus Rompharm should not be used by women who are breastfeeding.
Fertility
There is no data on the effect of the drug on human fertility.
Method of administration and doses
Bimoptic Plus Rompharm is applied topically to the eye.
The recommended dose is 1 drop in the conjunctival sac of the affected eye once daily, in the morning or evening. It should be used at the same time each day.
If a dose is missed, the next dose should be taken as scheduled. It is not recommended to exceed the dose of 1 injection once a day.
Nasolacrimal occlusion or eye closure for 2 minutes may reduce systemic absorption. This, in turn, may reduce systemic side effects and increase local drug activity.
If the drug is used with other ophthalmic drugs, it is necessary to take a 5-minute break between instillations of each of the drugs.
Use in elderly patients
The safety and efficacy data in elderly patients are similar to those in adult patients.
Children
The safety and efficacy of Bimoptic Plus Rompharm in children have not been studied.
The drug should not be prescribed to patients under 18 years of age.
Overdose
There have been no reports of overdoses of the drug Bimoptic Plus Rompharm in humans.
In case of overdose, symptomatic and supportive therapy should be applied.
No symptoms of toxic effects of bimatoprost were observed in cases of accidental ingestion of Bimoptic Plus Rompharm at doses up to 100 mg/kg/day. This dose is at least 36 times higher than the dose (7.5 ml vial of 0.03% bimatoprost solution) that can be accidentally ingested by a child weighing 10 kg.
In case of an overdose of timolol, the following symptoms are observed: bradycardia, hypotension, bronchospasm, headache, dizziness, shortness of breath, cardiac arrest. In case of renal failure, timolol is not completely removed by hemodialysis.
Adverse reactions
Results of the drug safety study.
The majority of adverse reactions observed in clinical trials with bimatoprost/timolol were ocular and mild in severity. None of the adverse reactions were serious. Based on 12-month clinical data, the most common adverse reaction was conjunctival hyperemia (mostly very mild or moderate and probably non-inflammatory in nature), which occurred in approximately 26% of patients and led to discontinuation in 1.5% of patients.
Table 1 lists adverse reactions reported during clinical trials with bimatoprost/timolol or in the post-marketing period (for each frequency, adverse reactions are listed by form of manifestation - from severe to mild).
The frequency of adverse reactions was determined using the following criteria:
Very common >1/10
Common ≥1/100 to <1/10
Uncommon ≥1/1000 to <1/100
Rare ≥1/10,000 to <1/1,000
Very rare <1/10,000
Not known Frequency cannot be estimated from the available data.
Table 1
Organ system class
Frequency
Adverse reaction
On the part of the immune system
Unknown
Hypersensitivity reactions, including symptoms of allergic dermatitis, angioedema, eye allergy
Mental disorders
Unknown
Insomnia, nightmares
Central nervous system
Often
Headache, dizziness
Unknown
Dysgeusia
From the organs of vision
Very often
Conjunctival hyperemia
Often
Superficial keratitis, corneal erosion, burning sensation, itching, burning pain in the eyes, foreign body sensation, dry eye, redness of the eyelashes, eye pain, photophobia, eye discharge, visual impairment, itching of the eyelid skin, visual acuity reduced, blepharitis, eyelid swelling, eye irritation, tearing, eyelash growth
Infrequently
Irritation of the mucous membrane of the eyes, iritis, conjunctival edema, eyelid pain, asthenopia, trichiasis, iris hyperpigmentation, deepening of the palpebral sulcus, eyelid refraction.
Bronchospasm (predominantly in patients with pre-existing bronchospastic syndrome), asthma
From the skin and subcutaneous fat
Often
Pigmentation of the skin of the eyelashes, hirsutism, pigmentation of the skin around the eye
Unknown
Alopecia
General violations
Unknown
Increased fatigue
Like other topical ophthalmic drugs, Bimoptic Plus Rompharm (bimatoprost/timolol) enters the systemic circulation. Absorption of timolol may cause the same adverse reactions as with systemic beta-blockers. The incidence of systemic adverse reactions to the drug after topical ocular administration is lower than with systemic administration. Regarding reduced systemic absorption, see section “Dosage and Administration”.
Additional adverse reactions that have been observed with the active substances (bimatoprost or timolol) and may potentially occur with the drug are listed in Table 2.
Table 2.
Decreased corneal sensitivity1, diplopia1, ptosis1, retinal detachment after surgical treatment1 (see section "Special instructions"), keratitis1, blepharospasm2, retinal hemorrhage2, uveitis2, darkening of eyelashes, periorbital erythema
Organ system class
Adverse reaction
On the part of the immune system
Systemic allergic reactions including anaphylaxis1
General disorders and administration site conditions
Asthenia1,2
Laboratory indicators
Liver enzyme changes2
1 - adverse reactions observed with the use of timolol
2 - adverse reactions observed with the use of bimatoprost
Adverse reactions to eye drops containing phosphates
Very rare cases of corneal calcification associated with the use of eye drops containing phosphates have been reported in patients with significantly damaged corneas.
Reporting of suspected adverse reactions
Reporting of suspected adverse reactions after the marketing authorisation of a medicinal product is of great importance. This allows for continuous monitoring of the benefit-risk balance of the medicinal product. Healthcare professionals should report any suspected adverse reactions via the national reporting system.
Expiration date
3 years.
The shelf life after first opening the bottle is 28 days.
Storage conditions
Store in the original packaging at a temperature not exceeding 25 °C.
Keep out of reach of children.
Packaging
3 ml in a bottle with a dropper cap and a cardboard box.
Vacation category
According to the recipe.
Producer
K.T. Rompharm Company S.R.L.
Location of the manufacturer and its business address
Eroilor St. No. 1A, Otopeni, 075100, Ilfov County, Romania.
Specifications
Characteristics
Active ingredient
Timolol, Bimatoprost
Adults
Can
ATC code
S SENSORY DRUGS; S01 DRUGS USED IN OPHTHALMOLOGY; S01E ANTIGLAUCOMA DRUGS AND MIOTICS; S01E D Beta-adrenergic blockers; S01E D51 Timolol, combinations
Country of manufacture
Romania
Diabetics
Can
Drivers
With caution
For allergies
With caution
For children
It is impossible.
Form
Drops
Method of application
For the eyes
Nursing
It is impossible.
Pregnant
It is impossible.
Producer
Rompharm Company
Quantity per package
3 ml
Trade name
Bimoptic
Vacation conditions
By prescription
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