Cirelax

INSTRUCTION FOR MEDICAL USE OF THE MEDICINAL PRODUCT CIRELAX (CIRELAX)

Composition:

Active substance: cyclopentolate hydrochloride;

1 ml of solution contains cyclopentolate hydrochloride 10 mg;

Excipients: boric acid, benzalkonium chloride, potassium chloride, disodium edetate, hydrochloric acid or sodium carbonate solution, purified water.

Pharmaceutical form. Eye drops, solution.

Main physicochemical properties: clear, colorless solution.

Pharmacotherapeutic group.
Mydriatic and cycloplegic agents. Anticholinergic agents. ATC code S01F A04.

Pharmacological properties.

Pharmacodynamics.

Cyclopentolate blocks M-cholinoreceptors, thereby preventing the action of the mediator of cholinergic synapses — acetylcholine.

As a result of blocking cholinergic synapses located in the iris sphincter and ciliary muscle, the pupil dilates due to predominant tone of the muscle dilating the pupil and relaxation of the muscle constricting the pupil. Simultaneously, due to relaxation of the ciliary (accommodative) muscle, paralysis of accommodation (cycloplegia) occurs.

Pupil dilation occurs within 15–30 minutes after a single instillation. Mydriasis persists for 6–12 hours; in particularly sensitive patients, mild mydriasis may last significantly longer. Residual effects of cycloplegia persist for 6–24 hours. The drug exerts a weak spasmolytic effect, reduces secretion of salivary, gastric, bronchial, sweat, and pancreatic glands; increases intraocular pressure; reduces vagus nerve tone, leading to increased heart rate with slight elevation of blood pressure.

It penetrates the blood-brain barrier; at medium therapeutic doses, it produces a moderate stimulating effect on the central nervous system and stimulates respiration.

Pharmacokinetics.

Cyclopentolate is well absorbed through the conjunctiva. A significant concentration in the central nervous system is reached within 0.5–1 hour. Plasma protein binding is moderate. The elimination half-life is 2 hours.

Clinical characteristics.

Indications.

The medicinal product is used to achieve mydriasis and cycloplegia.

Contraindications.

Hypersensitivity to the active substance or to other components of the medicinal product; closed-angle glaucoma; anatomically narrow anterior chamber angle of the eye.

Interaction with other medicinal products and other forms of interaction.

The effects of cyclopentolate may be enhanced when used concomitantly with anticholinergic agents such as amantadine, certain antihistamines, phenothiazines, neuroleptics, and tricyclic antidepressants.

The antiglaucoma effect of carbachol, pilocarpine, and the antiglaucoma and miotic effects of ophthalmic cholinesterase inhibitors may be reduced when used concomitantly with cyclopentolate.

Special precautions for use.

Complete recovery of accommodation occurs within 24 hours, although in some cases recovery may take several days.

Individuals with darkly pigmented irises and/or dark skin are less sensitive to the effects of cyclopentolate; therefore, the dose of the medicinal product should be adjusted accordingly.

To reduce systemic absorption and the risk of systemic adverse reactions, it is recommended to press the nasolacrimal punctum during and for 2–3 minutes after instillation (especially when used in children). Children should be observed for at least 45 minutes after administration.

Hands should be thoroughly washed after administration, as there is a risk of systemic toxicity if the medicinal product is accidentally ingested orally. In case of accidental oral ingestion, seek immediate medical attention.

Parents should ensure that the medicinal product does not enter the child's mouth and should wash the child's hands after administration.

To prevent contamination of the solution, the dropper tip should not touch any surface.

Increased sensitivity to light may occur during cyclopentolate use; therefore, eyes should be protected from bright light.

Psychotic reactions, behavioral disturbances, and other neurological disorders may occur in patients who are hypersensitive to anticholinergic agents. These effects may occur at any age, but are most commonly observed in young children (under 3 years of age).

In patients predisposed to elevated intraocular pressure and in elderly patients, the risk of induced angle-closure glaucoma is increased. The medicinal product should be used with caution in such patients and in patients with Down's syndrome. The depth of the anterior chamber should be evaluated before administration, especially if prolonged or intensive therapy is required.

Due to the risk of hyperthermia, the medicinal product should be used with caution in patients (especially children) exposed to high ambient temperatures or who have fever.

The medicinal product should be used with caution in patients with prostatic hypertrophy, intestinal obstruction, coronary insufficiency, cardiac failure, or ataxia due to the possibility of atropine-like reactions, and in patients hypersensitive to belladonna alkaloids or in debilitated patients due to the risk of systemic toxic effects.

The medicinal product should be used with caution in patients with eye inflammation, as hyperemia significantly increases the rate of systemic absorption through the conjunctiva.

Seizures and psychotic reactions may occur during cyclopentolate use, especially in children. The medicinal product should be used with caution in children with epilepsy.

Use in children.

Increased sensitivity to cyclopentolate has been reported in infants, young children (under 3 years), children with Down's syndrome, spastic paralysis, or brain damage. Due to systemic absorption of cyclopentolate, these patients may experience toxic effects on the central nervous system, cardiovascular system, and respiratory system.

The medicinal product is contraindicated in children under 1 year of age and should be used with particular caution in young children (under 3 years), children with Down's syndrome, spastic paralysis, or brain damage.

In cases of partial or complete accommodative spasm during cycloplegia, a course of atropine sulfate instillations is preferable.

Fair-skinned children with blue eyes have an increased risk of adverse reactions.

Use in elderly patients.

Elderly patients have an increased risk of induced glaucoma, elevated intraocular pressure, and psychiatric or behavioral disturbances. The medicinal product should be used with caution in these patients, and intraocular pressure should be monitored.

Use in patients with renal and/or hepatic impairment.

There are no studies on the use of cyclopentolate in patients with renal or hepatic impairment.

The medicinal product contains the preservative benzalkonium chloride, which may be absorbed by soft contact lenses, cause discoloration, or lead to eye irritation. Contact lenses must be removed before instillation. Lenses may be reinserted no sooner than 15 minutes after administration of the medicinal product.

When using other ophthalmic drops concurrently, an interval of at least 15 minutes between instillations should be maintained.

Use during pregnancy or breastfeeding.

Currently, there is insufficient data on the safety of cyclopentolate use during pregnancy. It is unknown whether cyclopentolate is excreted in breast milk. The medicinal product should be used during pregnancy or breastfeeding only if the expected benefit to the mother outweighs the potential risk to the fetus/infant. During cyclopentolate use, feeding intolerance in infants may occur. It is recommended to avoid breastfeeding for at least 4 hours after administration of the medicinal product.

Ability to affect reaction speed when driving or operating machinery.

Cyclopentolate may cause transient blurred vision. Patients should refrain from driving or operating machinery until visual acuity is restored.

Method of Administration and Dosage

The medicinal product is intended for ophthalmic use only. Eye drops should be instilled into the conjunctival sac of the eye.

Adults: instill 1–2 drops of the solution. Instillation may be repeated after 5–10 minutes if necessary.

Children aged 1 year and older: instill 1–2 drops of the solution. Instillation may be repeated after 5–10 minutes if necessary.

Maximum effect of the medicinal product is achieved within 30–60 minutes after administration.

To reduce systemic absorption and the risk of systemic adverse reactions, it is recommended to press the nasolacrimal punctum during the procedure and for 2–3 minutes afterwards (especially when used in children). Children should be observed for at least 45 minutes after the procedure.

After administration of the medicinal product, hands must be thoroughly washed. Parents should ensure that the medicinal product does not enter the child's mouth and should wash the child's hands after administration.

Children.

The medicinal product should not be used in children under 1 year of age and should be used with particular caution in younger children (under 3 years of age), children with Down's syndrome, spastic paralysis, or brain damage.

Increased sensitivity to cyclopentolate has been reported in infants, young children (under 3 years), and children with Down's syndrome, spastic paralysis, or brain damage. Due to systemic absorption of cyclopentolate, toxic effects on the central nervous system, cardiovascular system, and respiratory system may occur in such patients.

Overdose.

Symptoms.

Exaggeration of adverse reactions. Systemic adverse reactions may also occur after local administration of cyclopentolate, especially in children, and include flushing and dryness of the skin and mucous membranes, rash (in children), blurred vision, tachycardia, fever, abdominal distension in infants, seizures, hallucinations, excitement, disturbances in mental reactions (incoherent speech, increased fatigue, impaired recognition of nearby objects, spatial disorientation, changes in emotional state), and impaired neuromuscular coordination. Significant overdose may lead to central nervous system depression, coma, cardiovascular and respiratory failure, cerebral paralysis, and even death. Symptoms appear within 20–30 minutes after cyclopentolate instillation and may last up to 12–24 hours.

Treatment.

In case of local overdose, rinse eyes with warm water. If symptoms of overdose occur, discontinue use of the medicinal product and administer symptomatic and supportive therapy. In case of severe manifestations, intravenous administration of a specific antidote—physostigmine—is indicated. For adults, administer 2 mg of the antidote; if no effect is observed within 20 minutes, repeat administration at a dose of 1–2 mg. For children, administer 0.5 mg of the antidote; if no effect is observed within 5 minutes, repeat the dose (total dose should not exceed 2 mg).

Side effects.

Local reactions (ophthalmological disorders): increased intraocular pressure, transient burning sensation, irritation, conjunctival hyperemia, photophobia, blurred vision, conjunctivitis, blepharoconjunctivitis, punctate keratitis, synechiae, swelling, eye pain, mydriasis, lacrimation.

Central nervous system and psychiatric disorders: psychotic reactions and behavioral disturbances, including ataxia, incoherent speech, anxiety, hallucinations, hyperactivity, seizures, disorientation, prosopagnosia, confusion, agitation; retrograde amnesia, dizziness, headache, somnolence. In children, the following may occur: ataxia, epileptic seizures, speech disorders, excitement, incoherent speech, hallucinations, disorientation in time and space, impaired recognition of familiar people, amnesia, dysarthria, cerebral manifestations or dysfunctions, increased activity, anxiety, fear, central anticholinergic syndrome, somnolence, tearfulness.

Cardiovascular system disorders: tachycardia, bradycardia alternating with tachycardia, arterial hypotension or hypertension, tachyarrhythmia, arrhythmia, vasodilation, facial and extremity flushing, palpitations.

Gastrointestinal disorders: nausea, vomiting, dry mouth, decreased gastrointestinal motility, abdominal distension (in infants), stomach discomfort, intestinal obstruction, food intolerance, necrotizing enterocolitis, constipation, hypersalivation.

Immune system, skin and subcutaneous tissue disorders: hypersensitivity reactions, including severe anaphylactic reactions, respiratory failure; rash, erythema, urticaria (including contact urticaria), contact dermatitis, sensation of warmth and dryness of the skin.

Urinary system disorders: urinary retention, imperative urges to urinate, difficulty urinating.

Other: fever, gait disturbances, fatigue, decreased secretion of salivary and sweat glands, pharynx, bronchi, and nasal passages.

Reporting suspected adverse reactions.

Reporting of suspected adverse reactions after drug registration is highly important. It enables continuous monitoring of the benefit-risk balance of the medicinal product. Healthcare and pharmacy professionals, as well as patients or their legal representatives, should report all suspected adverse reactions and lack of efficacy via the Automated Pharmacovigilance Information System at the following link: https://aisf.dec.gov.ua.

Shelf life.

3 years. After opening the bottle, the medicinal product can be used for up to 28 days.

Storage conditions.

Store at 2–8 °C, protected from light and out of reach of children. After opening, store the bottle at a temperature not exceeding 25 °C.

Packaging.

5 mL of solution in a dropper bottle; 1 dropper bottle per cardboard box.

Prescription category.

Prescription only.

Manufacturer.

C.O. Rompharm Company S.R.L., Romania /
S.C. Rompharm Company S.R.L., Romania.

Manufacturer's address and place of business.

Otopeni, Eroilor str. № 1A, 075100, jud. Ilfov /
Otopeni city, Eroilor str. № 1A, 075100, jud. Ilfov.

Marketing authorization holder.

WORLD MEDICINE, LLC, Ukraine /
WORLD MEDICINE, LLC, Ukraine.