Cetadrope - instructions for use, dose, side effects, contraindications

Excipients: benzalkonium chloride in terms of 100% substance 0.1 mg, hypromellose 1.0 mg, sodium chloride 7.5 mg, disodium edetate 1.0 mg, sodium hydroxide - q.s. up to pH 6.0-7.5, water for injection up to 1 ml.

Description:

A clear, colorless solution.

Pharmacotherapeutic group:Non-steroidal anti-inflammatory drug (NSAID)

ATX: & nbsp

M.01.A.B.15 Ketorolac

Pharmacodynamics:

Ketorolac (ketorolac trometamol) is a non-steroidal anti-inflammatory drug (NSAID) with analgesic and anti-inflammatory activity. It is believed that it inhibits the cyclooxygenase necessary for the biosynthesis of prostaglandins involved in the inflammation reaction and the onset of pain syndrome. After a local ophthalmic application ketorolac reduces the content of prostaglandins in aqueous humor.

With systemic application ketorolac does not cause a narrowing of the pupil. According to the results of clinical studies ketorolac does not have a significant effect on intraocular pressure.

Pharmacokinetics:

Solutions of ketorolac trometamol (0.1% and 0.5%) or placebo were instilled in patients 12 and 1 h before surgery. Using a 0.1% solution, the concentration of ketorolac in aqueous humor at the time of surgery was one patient at the lower limit of detection (40 ng / ml), in 7 patients below the detection limit. With the application of a 0.5% solution, the average ketorolac trometamol content in the aqueous humor of patients was 95 ng / ml. Concentrations of prostaglandin E2 (PGE2) in watery moisture were: 80, 40 and 28 pg / ml when administered to patients placebo, 0.1% and 0.5% solutions of ketorolac trometamol, respectively.

In a 21-day study of tolerability with multiple administration (3 times a day) in healthy volunteers, only 1 in 13 subjects before the introduction of a regular dose ketorolac was detected in plasma (0.021 μg / ml). In another group of 13 people, only 4 subjects had a very low plasma concentration of ketorolac (0.011-0.023 μg / ml) 15 minutes after instillation.

Thus, a higher content of ketorolac in aqueous humor and a very low concentration or a completely undetectable plasma content after ophthalmic administration suggests,that the use of ketorolac trometamol in the ophthalmologic route of administration for the treatment of eye diseases manifests itself in sufficiently low systemic absorption in patients.

Indications:

Temporary relief of pruritus with seasonal allergic conjunctivitis.

Treatment of postoperative inflammation in patients who underwent cataract extraction.

Contraindications:

Hypersensitivity to ketorolac trometamol, as well as to the components that make up the drug.

Hypersensitivity (including in the anamnesis) to acetylsalicylic acid, derivatives of phenylacetic acid, such as diclofenac or other NSAIDs used in ophthalmology, as well as other systemic NSAIDs.

Children under 18 years.

Carefully:

Hypersensitivity to acetylsalicylic acid, phenylacetic acid derivatives and other NSAIDs due to possible cross-sensitivity with ketorolac.

The tendency to bleeding and the concomitant use of drugs that increase bleeding time.

In patients with ophthalmologic complications in the postoperative period, with violation of innervation of the cornea, defects in the epithelium of the cornea, diabetes mellitus,diseases of the mucous membrane of the eyes (for example, dry eye syndrome), with concomitant rheumatoid arthritis, as well as with small intervals between repeated ophthalmologic operations due to the high risk of developing unwanted corneal reactions that may threaten vision loss.

Pregnancy and lactation:

The drug is not recommended for use during pregnancy. Controlled studies of ketorolac in pregnant women have not been conducted.

In connection with the known effect of drugs that inhibit the synthesis of prostaglandins on the development of the fetal cardiovascular system (closure of the arterial duct), the use of ketorolac preparations during pregnancy should be avoided.

If necessary, use during lactation should stop breastfeeding.

The effect of the drug on fertility has not been studied.

Dosing and Administration:

Intended for topical application in ophthalmology:

In order to temporarily relieve itching with seasonal allergic conjunctivitis - 1 drop 4 times a day with a 6 hour interval.

In order to prevent and treat the inflammatory process of the eye: locally,to the affected eye 24 hours before and within 2-3 weeks after the operation for cataract removal 4 times a day at intervals of 6-8 hours.

After instillation, a slight pressure is recommended in the projection of the nasolacrimal canal or a slight closure of the eyelid. This reduces the systemic absorption of drugs injected into the conjunctival sac, which can reduce the likelihood of systemic side effects.

In case of application of the preparation together with other eye drops, it should be instilled in 5 minutes before using another drug.

Side effects:

The frequency of side effects detected during the studies was evaluated according to the following gradations: very often (> 10%), often (> 1% and <10%), infrequently (> 0.1% and <1%), rarely (> 0.01% and <0.1%).

In clinical studies of the drug Ketadrop® the following side effects are revealed.

From the side of the organ of vision: very often - eye irritation, pain in the eyes, a brief burning sensation, foreign body sensation and blurring of vision; often - congestion hyperemia, superficial keratitis, iritis, eye swelling and (or) century, eye infection; infrequently - an ulcer of the cornea,corneal infiltrate, epiphore, dry eyes, iritis, temporary blurring of vision; rarely - corneal damage (thinning, erosion, rupture of the epithelium or perforation).

From the immune system: often - hypersensitivity reactions, urticaria, rash, itching, angioedema, anaphylactic reactions.

From the respiratory system: the frequency is unknown - bronchospasm, exacerbation of bronchial asthma.

From the nervous system: infrequently - headache.

Systemic reactions: frequency unknown - increased blood pressure (BP), nasal congestion, increased heart rate (HR), as well as prolonged clotting time and increased bleeding of the operated eye with intraocular use of NSAIDs.

Effects of the cornea. The use of local forms of NSAIDs can lead to the development of keratitis. In some sensitive patients, prolonged use of NSAIDs can lead to destruction of the corneal epithelium, thinning of the cornea, development of erosion, ulcers or perforation of the cornea, which can threaten vision. Patients with signs of corneal abnormalities should immediately stop using NSAIDs, including ketorolac, and carry out a thorough monitoring of the condition of the cornea.

Postmarketing experience with the use of NSAIDs indicates that patients with complications after eye surgeries, with corneal denervation, corneal epithelial defects, diabetes mellitus, certain syndromes (eg, dry eye syndrome), rheumatoid arthritis or repeated eye surgery for a short period of time there may be an increased risk of developing corneal side effects that may pose a threat to vision. Care should be taken to use local forms of NSAIDs in these patients.

Postmarketing experience with the use of NSAIDs also indicates that the use of local NSAIDs more than 1 day before surgery or for more than 14 days after surgery may increase the risk of occurrence and severity of corneal side effects.

A cross-over hypersensitivity to acetylsalicylic acid, phenylacetic acid and other NSAIDs is possible. Therefore, caution should be exercised when using ketorolac in patients who have previously shown hypersensitivity to these drugs.

Overdose:

Usually does not lead to the development of symptoms that threaten vital organs and systems.

If swallowed accidentally, a large amount of liquid should be taken.

Interaction:

Ketorolaka trometamol can be used in combination with antibiotics, β-adrenoblockers, carbonic anhydrase inhibitors, cycloplegics and mydriatics.

With the simultaneous use of the drug Ketadrop® with other eye drops, it is necessary to make a break between instillations for at least 5 minutes.

Delayed healing. NSAIDs for topical use, including ketorolac, can slow the healing. Local forms of corticosteroids, as is known, can also slow or delay healing. Simultaneous use of NSAIDs and steroids for topical application can cause healing problems after surgery.

Special instructions:

With a tendency to bleeding and concomitant administration of drugs that increase bleeding time, the use of ophthalmic forms of NSAIDs after ophthalmic surgical interventions may increase the risk of bleeding in the eye tissues, including the accumulation of blood in the anterior chamber of the eye (hyphema).

Patients with signs of destruction of the corneal epithelium should immediately stop taking the drug and carefully monitor the condition of the cornea. Patients with complications in the postoperative period with impaired innervation corneal defects corneal epithelium, diabetic mucosal diseases eyes (e.g., "dry eye" syndrome), with concomitant rheumatoid arthritis, as well as at small intervals between repeated ophthalmological operations, due high risk of adverse reactions on the part of the cornea that can threaten vision loss should be used with caution. The use of local NSAIDs for 24 hours or more before surgery on the cornea and more than 14 days after it can increase the risk of complications from the cornea and their severity.

It is not recommended to wear contact lenses during treatment with Catadrop®, t. preservative benzalkonium chlorideContained in a preparation, may be deposited in soft contact lenses and have an adverse effect on the eye tissue. Hard contact lenses should be removed before instillation and then reinstall after 15 minutes.With frequent or prolonged use of the drug, benzalkonium chloride can cause the emergence of point keratitis or toxic ulcerative keratopathy in patients with the syndrome of "dry eyes" or corneal pathology.

In patients with complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid or other non-steroidal anti-inflammatory drugs (including anamnesis), the drug may provoke the development of an attack of bronchial asthma. When developing an allergic reaction, the drug should be discontinued.

Do not touch the tip of the dropper bottle to any surface to avoid contamination of the dropper and its contents.

Safety of use in children and among the elderly is not established.

Effect on the ability to drive transp. cf. and fur:

After the application of eye drops, it is possible to reduce the clarity of visual perception, so immediately after instillation it is not recommended to drive and engage in activities requiring increased attention and speed of psychomotor reactions.

Form release / dosage:

Eye drops, 0,5%.

Packaging:

By 5 ml of the drug into the bottles-droppers of low-density polyethylene (PPP) sealed with a screw cap of high-density polyethylene (PEP) with a point for piercing the dropper.

One bottle together with the instruction for use is placed in a cardboard box.

Storage conditions:

In a dry, the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Shelf life of the drug after the first opening of the bottle-dropper is 28 days.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-002422

Date of registration:07.04.2014 / 22.09.2014

Expiration Date:07.04.2019

The owner of the registration certificate:Micro Labs LimitedMicro Labs Limited India

Manufacturer: & nbsp

MICRO LABS, Limited India

Representation: & nbspMICRO LABS LIMITED MICRO LABS LIMITED India

Information update date: & nbsp02.01.2018

Illustrated instructions

Instructions

Cetadrope® (Ketadrop®)