Cabastin
UkraineTable of Contents
INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT CABASTINE (CABASTINE)
Composition:
Active substance: levocabastine;
1 ml of solution contains 0.543 mg of levocabastine hydrochloride, equivalent to 0.500 mg of levocabastine;
Excipients: hydroxypropylbetadex, sodium dihydrogen phosphate dihydrate, sodium hydrogen phosphate dodecahydrate, sodium chloride, purified water.
Pharmaceutical form. Eye drops, solution.
Main physicochemical properties: almost clear, colorless solution.
Pharmacotherapeutic group.
Medicinal products used in ophthalmology. Anti-inflammatory and antiallergic agents. ATC code S01GX02.
Pharmacological properties.
Pharmacodynamics.
Mechanism of action. Levocabastine is a selective, potent, fast-acting H1-antihistamine with prolonged activity.
After instillation into the eyes, it rapidly relieves symptoms of allergic conjunctivitis (itching, erythema, lacrimation, eyelid swelling, chemosis) for several hours.
Children. Studies conducted in children aged 6 to 18 years confirmed the efficacy of levocabastine administered as eye drops.
Pharmacokinetics.
Absorption. After ocular instillation, levocabastine is gradually and partially absorbed through the mucous membrane.
In patients with allergic conjunctivitis, the absolute bioavailability is approximately 30% after single ocular administration of levocabastine eye drops, suspension; following repeated ocular administration of one drop in each eye up to four times daily for 4 weeks, steady-state plasma concentrations ranged from 0.24 to 0.83 ng/mL.
Biotransformation. After single oral administration (0.5 mg, 1 mg, and 2 mg), levocabastine is rapidly and completely absorbed (Tmax = 2 hours). Following oral administration of 0.5 mg of levocabastine solution, the mean bioavailability is 112%. The elimination half-life (35–45 hours) remains unchanged after repeated dosing.
Excretion. After 9 days of repeated oral administration (0.5 mg/day), mean steady-state plasma concentrations were 12.3 ng/mL. Levocabastine is excreted primarily via the kidneys, mainly in unchanged form.
Non-clinical safety data
Non-clinical data from the literature on levocabastine revealed no special risk to humans following intravenous, oral, or topical administration. After ocular instillation in rabbits, measured plasma concentrations of levocabastine were low, suggesting that systemic effects are unlikely.
Tolerance studies of the medicinal product Kabastin in rabbits revealed no special risk to humans following administration four times daily for 4 weeks.
Clinical characteristics.
Indications.
Allergic conjunctivitis.
Contraindications.
Hypersensitivity to the active substance or to any of the excipients of the medicinal product.
Interaction with other medicinal products and other types of interactions.
Not expected.
Special precautions for use
Cavastin, eye drops, must not be administered by injection.
Each 5 ml of the medicinal product contains 39.65 mg of phosphates.
Use during pregnancy or breastfeeding
Pregnancy
There is a lack of data on the use of the medicinal product in pregnant women.
Due to the minimal systemic exposure and the absence of reports on fetotoxic or teratogenic effects in animal studies, Cavastin eye drops should be used during pregnancy only if clearly needed and with caution.
Breastfeeding period
Due to the lack of data, levocabastine should not be used during breastfeeding.
Effect on ability to drive vehicles or operate machinery
Transient visual discomfort due to slight irritation following instillation of Cavastin eye drops may occur. In such cases, it is recommended to wait until vision has normalized before driving or operating machinery.
Method of Administration and Dosage.
Doses. Adults and children aged 6 years and older: the usual recommended dose is 1 drop in each eye twice daily.
If necessary, the dose may be increased to 1 drop 3–4 times daily.
Eye drops should be administered at regular intervals.
Treatment should not be continued for more than 5 days without consulting a physician.
Method of Administration.
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Wash hands thoroughly.
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Before first use, remove the safety ring.
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Remove the protective cap.
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Before the first instillation into the eye: hold the bottle upside down and gently squeeze it in the middle to dispense 1–2 drops of the medicinal product.
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Look upward, gently pull the lower eyelid downward, position the bottle above the eye, and gradually squeeze the bottle until a drop appears.
Avoid touching the eye or eyelid with the tip of the bottle.
- Blink once to spread the eye drops over the entire surface of the eye.
Keep eyes closed and wipe away excess liquid.
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To minimize systemic effects, it is recommended to press gently on the inner corner of the eye (tear duct) and hold for 1 minute after each instillation, keeping the eyes closed.
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After each use, to remove residual drops: hold the bottle vertically by the middle and quickly tilt it downward to shake off the remaining drop.
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After use, replace the cap on the bottle.
If drops do not appear, repeat the steps described in points 3 and 4.
If using other eye drops simultaneously, wait 15 minutes between administrations.
These eye drops do not contain preservatives.
Children.
The safety and efficacy of Cabastin eye drops in children under 6 years of age have not been established.
Overdose.
Sedative effects cannot be ruled out following accidental overdose.
In case of overdose, thoroughly rinse the eye with sterile physiological saline solution.
Adverse reactions
Adverse reactions, based on clinical trial results, epidemiological studies, and post-marketing data, are classified according to frequency as follows: very common (≥1/10), common (≥1/100, <1/10), uncommon (≥1/1000, <1/100), rare (≥1/10000, <1/1000), and very rare (<1/10000). The frequency of reactions observed during the post-marketing period is unknown.
Eye disorders
Common: eye pain, blurred vision.
Uncommon: eyelid edema.
Very rare: conjunctivitis, eye swelling, blepharitis, ocular hyperemia, lacrimation.
In very rare cases, corneal calcification has been reported with the use of phosphate-containing eye drops in some patients with severely damaged corneas.
Cardiac disorders
Very rare: tachycardia.
General disorders and administration site conditions
Common: application site reactions, including burning/stinging sensation, eye irritation.
Very rare: application site reactions, including eye redness, eye itching.
Immune system disorders
Very rare: angioedema, hypersensitivity, anaphylactic reaction.
Skin and subcutaneous tissue disorders
Very rare: contact dermatitis, urticaria.
Nervous system disorders
Very rare: headache.
Shelf life. 24 months.
Shelf life after first opening: 3 months.
Storage conditions.
Store at a temperature not exceeding 25 °C. Keep out of reach and sight of children.
Packaging.
5 ml in a bottle with a dropper and cap; 1 bottle with dropper and cap in a cardboard box.
Prescription category. Prescription only.
Manufacturer.
Laboratoires Chauvin.
Manufacturer's address and place of business.
Zone Industrielle Ripoteau, 07200 Aubenas, France.