Iriphrin

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT IRIFRIN (IRIFRIN)

Composition:

active substance: phenylephrine;

1 ml of the preparation contains phenylephrine hydrochloride 25 mg;

excipients: benzalkonium chloride, disodium edetate, hypromellose, sodium metabisulfite (E 223), sodium citrate, anhydrous citric acid, water for injections.

Pharmaceutical form. Eye drops.

main physicochemical properties: clear, colorless solution or slightly yellow liquid.

Pharmacotherapeutic group. Agents used in ophthalmology. Mydriatic and cycloplegic agents. ATC code S01F B01.

Pharmacological properties.

Pharmacodynamics.

The drug has a pronounced stimulating effect on postsynaptic alpha-adrenergic receptors, while its effect on cardiac beta-adrenergic receptors is almost negligible. The drug exerts a vasoconstrictor effect similar to that of norepinephrine; however, it has virtually no chronotropic or inotropic effect on the heart. The vasopressor effect of the drug is less pronounced than that of norepinephrine but significantly longer-lasting. When used in usual doses, it does not produce a significant stimulating effect on the central nervous system. After instillation, phenylephrine contracts the iris dilator muscle, thereby causing pupil dilation, as well as constricting the smooth muscles of conjunctival arterioles. There is no effect on the ciliary muscle, so mydriasis occurs without cycloplegia.

Pharmacokinetics.

Phenylephrine readily penetrates ocular tissues; pupil dilation occurs within 10–60 minutes after a single instillation. Mydriasis persists for 4–6 hours. Due to significant contraction of the iris dilator muscle, pigment particles from the iris pigment layer may appear in the aqueous humor of the anterior chamber 30–45 minutes after instillation. This phenomenon should be differentiated from signs of anterior uveitis or the presence of formed blood elements in the aqueous humor of the anterior chamber.

Clinical characteristics.

Indications.

• Iridocyclitis, anterior uveitis (for treatment and prevention of posterior synechiae formation and reduction of exudation from the iris of the eye).
• Diagnostic dilation of the pupil during ophthalmoscopy and other diagnostic procedures necessary for assessing the condition of the posterior segment of the eye.
• Performance of provocative testing in patients with narrow anterior chamber angle and suspected closed-angle glaucoma.
• Differential diagnosis of the type of ocular injection.
• Pupil dilation during laser interventions on the fundus and vitreoretinal surgery.
• "Red eye" syndrome (to reduce hyperemia and irritation of ocular membranes).
• Complex therapy of accommodative spasm in school-age children.
• Treatment and prevention of asthenopia.

Contraindications.

─ Hypersensitivity to any component of the drug.

─ Narrow-angle or closed-angle glaucoma.

─ Significant cardiovascular disorders (heart diseases, arterial hypertension, aneurysm, tachycardia), especially in elderly patients.

─ Insulin-dependent diabetes mellitus.

─ Thyrotoxicosis.

─ Hyperthyroidism.

─ Concomitant use with monoamine oxidase inhibitors (MAOIs) and use within 2 weeks after discontinuation of MAOIs.

─ Additional pupil dilation during surgery in patients with impaired integrity of the eyeball or impaired tear secretion function.

─ Concomitant use with tricyclic antidepressants and antihypertensive agents (including β-blockers).

─ Congenital glucose-6-phosphate dehydrogenase deficiency.

─ Hepatic porphyria.

─ Contraindicated in newborns with low body weight.

─ Contraindicated in newborns and infants with cardio- or cerebrovascular disorders.

─ Contraindicated in elderly patients with severe atherosclerotic, cardiovascular, or cerebrovascular diseases.

Interaction with other medicinal products and other types of interactions.

The mydriatic effect of phenylephrine is enhanced by local application of atropine, and reduced by local application of other ophthalmic preparations containing miotics. The drug may inhibit the ability of miotics to reduce intraocular pressure.

The mydriatic effect of phenylephrine is enhanced by local application of atropine.

Antihypertensive medicinal products (including β-adrenergic blockers) are contraindicated for concomitant use with phenylephrine for topical application, as arterial hypertension or reversal of antihypertensive effects with fatal outcomes may occur.

MAO inhibitors. Concomitant use of phenylephrine with monoamine oxidase inhibitors is contraindicated, as well as use within 2 weeks after discontinuation of MAO inhibitors. Use of phenylephrine within 21 days after stopping MAO inhibitors should be performed with caution due to the possible development of systemic adrenergic effects.

Tricyclic antidepressants are contraindicated for concomitant use with phenylephrine. The vasoconstrictor action of adrenergic agents may be potentiated by tricyclic antidepressants (risk of cardiac arrhythmia, including within several days after discontinuation of their use), propranolol, reserpine, guanethidine, methyldopa, and muscarinic cholinergic blockers.

Inhalation anesthesia. The drug may potentiate cardiovascular depression during inhalation anesthesia. Due to the increased risk of ventricular fibrillation, the drug should be used with caution during general anesthesia with anesthetics such as, for example, halothane (fluothane), which increase myocardial sensitivity to sympathomimetics.

Cardiac glycosides or quinidine. Increased risk of arrhythmia.

Special precautions for use.

Phenylephrine hydrochloride is an adrenergic agent used in ophthalmology primarily to achieve mydriatic effect. The drug has minimal effect on the ciliary muscle of the eye, so significant impact on accommodation is not observed, although pupil dilation may reduce depth of focus and cause blurred vision.

Systemic effects can be minimized by applying digital pressure to the inner canthus of the eye for 1 minute after instillation (this blocks passage of the drops through the nasolacrimal duct to the nasal mucosa and pharynx, and is especially recommended for infants, children, and elderly patients).

Since the pupil-dilating effect may last 1–3 hours, patients may experience photophobia; therefore, the eye(s) should be protected from bright sunlight, including the use of sunglasses, until vision fully returns to normal. Activities requiring visual concentration (e.g., reading, watching television, etc.) should be avoided until residual mydriasis resolves.

Increased absorption and enhanced systemic adverse effects may occur in the presence of conjunctival hyperemia or corneal epithelial defects.

To prevent acute angle-closure glaucoma, the anterior chamber angle should be evaluated prior to drug administration. To minimize discomfort during phenylephrine instillation, anesthetic eye drops may be administered a few minutes beforehand.

Elderly patients. Reactive miosis may occur. Reactive miosis has been observed in elderly patients one day after administration of phenylephrine solution, and repeated application led to reduced pupil dilation. Use with caution in patients with cerebral atherosclerosis, cardiovascular disorders, chronic bronchial asthma, arterial hypertension, or insulin-dependent diabetes mellitus. Due to the pronounced effect of the drug on pupil dilation, temporary appearance of floating pigment spots in the intraocular fluid may occur in elderly patients within 30–45 minutes after instillation of phenylephrine solution.

Pediatric use. Always use the smallest dose necessary to achieve the desired effect. Parents should be informed about the need to prevent the drug from entering the child’s mouth or contacting the cheeks, and about the necessity of washing their own hands as well as the child’s hands and cheeks after instillation. In general, children, especially low-birth-weight infants and premature neonates, are at increased risk of developing systemic adverse reactions, including transient increase in blood pressure, which may increase the risk of intraventricular hemorrhage. Infants should be monitored after instillation, and appropriate resuscitative measures should be available if needed.

Contact lenses. Since the preparation contains the preservative benzalkonium chloride, it may cause irritation and discoloration of soft contact lenses. Therefore, patients should remove contact lenses before instillation and wait 15 minutes after instillation before reinserting contact lenses.

Use during pregnancy or breastfeeding.

Not studied. Use may be considered if the anticipated benefit to the mother outweighs the potential risk to the fetus or infant. Breastfeeding should be discontinued during treatment with this drug.

Ability to affect reaction rate when driving or operating machinery.

Do not drive or operate machinery until visual acuity has fully recovered.

Method of Administration and Dosage.

For ophthalmoscopy, administer a single instillation of the 2.5% solution. Usually, one drop of the 2.5% solution instilled into the conjunctival sac is sufficient to achieve mydriasis. Maximum mydriasis is reached within 15–30 minutes and remains adequate for 1–3 hours. If prolonged maintenance of mydriasis is required, a repeat instillation may be performed after 1 hour.

For diagnostic procedures, a single instillation of the 2.5% solution is used:

─ as a provocative test in patients with a narrow anterior chamber angle and suspected angle-closure glaucoma. If the difference in intraocular pressure before and after pupil dilation is between 3 and 5 mm Hg, the provocative test is considered positive;

─ for differential diagnosis of the type of ocular injection: if within 5 minutes after instillation a narrowing of ocular blood vessels is observed, the injection is classified as superficial; if ocular redness persists, a thorough examination for iridocyclitis or scleritis should be performed, as this indicates vasodilation in deeper ocular tissue layers.

In iridocyclitis and anterior uveitis, the drug is used for treatment and prevention of posterior synechiae formation, as well as for reducing exudation into the anterior chamber of the eye. For this purpose, one drop of the drug is instilled into the conjunctival sac of the affected eye(s) 2–3 times daily.

Complex therapy of accommodative spasm and asthenopia in school-aged children.

In mild myopia, administer 1 drop of the 2.5% solution before bedtime on days with high visual strain; in moderate myopia — 1 drop of the 2.5% solution 3 times per week before bedtime; in emmetropia (absence of myopia) — daily, regardless of visual load.

In hyperopic patients with a tendency to develop spasm, use the 2.5% solution in combination with 1 drop of 1% cyclopentolate before bedtime during periods of high visual strain, and 3 times per week under normal conditions.

Use in elderly patients. Dose adjustment is not required in elderly patients. Repeated instillations may produce a less pronounced mydriatic effect.

Before first use, rotate the cap clockwise until it stops. The scarifier inside the cap will puncture the nozzle of the bottle. After this, the bottle can be opened in the usual way by rotating the cap counterclockwise. During instillations, standard sanitary and hygienic precautions must be observed: hands should be washed with soap, and the dropper tip should not be touched with fingers.

Children.

In pediatric practice, the drug may be used from the first days of life for diagnostic procedures (ophthalmoscopy, retinography). Use in premature infants should be cautious and based on a physician's risk-benefit assessment: no more than 1 drop in each eye.

Overdose.

Even with topical application, systemic effects of phenylephrine may occur. The most common are significant increase in blood pressure and reflex bradycardia.

Treatment: administration of alpha-adrenergic blockers. In case of reflex bradycardia, atropine should be used (in children — at a dose of 0.01–0.02 mg/kg body weight).

Adverse Reactions

Immune system disorders: hypersensitivity, allergic conjunctivitis.

Eye disorders: eye pain, burning sensation (at the beginning of administration, in some cases), reactive hyperemia, blurred vision, eye irritation, ocular discomfort, photophobia, lacrimation, increased intraocular pressure in patients with narrow-angle or closed-angle glaucoma, reactive miosis (on the following day after administration; with repeated instillations, less pronounced mydriasis may occur compared to the previous day; this effect is more commonly observed in elderly patients). Periocular pallor may occur in premature newborns.

Cardiovascular system disorders: tachycardia, cardiac arrhythmias including ventricular arrhythmias, arterial hypertension, reflex bradycardia, coronary artery occlusion, pulmonary artery embolism, myocardial infarction.

Reporting of suspected adverse reactions. Reporting suspected adverse reactions after marketing authorization is an important procedure. It allows continuous monitoring of the benefit-risk balance of the medicinal product. Healthcare professionals are encouraged to report any suspected adverse reactions through the national reporting system.

Patients who experience any undesirable effects, adverse reactions, or lack of therapeutic effect should contact the Company Contact Person of «Sentiss Pharma Private Limited», India in Ukraine by phone +38044 585-04-60 or via email: [email protected].

Shelf life. 2 years.

Shelf life after opening the bottle – 1 month.

Do not use after the expiry date stated on the packaging.

Storage conditions. Store at a temperature not exceeding 25 °C in a place protected from light. Do not freeze.

Keep out of reach and sight of children.

Packaging. 5 ml in a dropper bottle with a tamper-evident cap, 1 bottle in a carton.

Prescription status. Prescription only.

Manufacturer.

SENTISS PHARMA PVT. LTD., India / SENTISS PHARMA PVT. LTD., India.

Address of manufacturer and location of operations.

Village Khera Nihla, Tehsil Nalagarh, Distt. Solan, Himachal Pradesh, 174 101, India / Village Khera Nihla, Tehsil Nalagarh, Distt. Solan, Himachal Pradesh, 174 101, India.

Marketing Authorization Holder.

SENTISS PHARMA PVT. LTD., India / SENTISS PHARMA PVT. LTD., India.

Address of Marketing Authorization Holder.

212/D-1, Ashirwad Commercial Complex, Green Park, New Delhi, 110016, India / 212/D-1, Ashirwad Commercial Complex, Green Park, New Delhi, 110016, India.