Fenikamid (Drops) Instructions for Use

Marketing Authorization Holder

Grotex, LLC (Russia)

ATC Code

S01FA56 (Tropicamide in combination with other drugs)

Active Substances

Phenylephrine (Rec.INN registered by WHO)

Tropicamide (Rec.INN registered by WHO)

Dosage Form

Fenikamid

Eye drops 8 mg+50 mg/1 ml: 10 ml bottle 1 pc.

Dosage Form, Packaging, and Composition

Eye drops as a clear, colorless to yellow or brownish-yellow liquid.

Excipients: benzalkonium chloride – 0.1 mg, sodium phosphate dibasic dihydrate – 0.28 mg, sodium phosphate monobasic dihydrate – 0.005 mg, sodium chloride – 4.5 mg, disodium edetate dihydrate (Trilon B) – 0.5 mg, 1M hydrochloric acid solution or 1M sodium hydroxide solution – to adjust pH to 3.0-5.8, water for injections – to 1 ml.

10 ml – polyethylene terephthalate bottles (1) with a dropper – foil film bags (1) – cardboard packs.

Clinical-Pharmacological Group

Diagnostic agent for topical use in ophthalmology (m-cholinoblocker + alpha-adrenomimetic)

Pharmacotherapeutic Group

Agents used in ophthalmology; mydriatic and cycloplegic agents; anticholinergic agents

Pharmacological Action

Combined agent for use in ophthalmology.

Tropicamide. An M-cholinoblocking agent, it blocks M-cholinergic receptors of the pupillary sphincter and the ciliary muscle, causing short-term mydriasis and cycloplegia. Slightly increases intraocular pressure. Mydriasis with the use of tropicamide develops within 5-10 minutes and reaches a maximum by 20-45 minutes. Maximum pupil dilation persists for 1 hour and normalizes after 6 hours.

Phenylephrine. A non-selective alpha-adrenomimetic. It has a pronounced stimulating effect on postsynaptic α-adrenergic receptors, weakly affects cardiac β₁-adrenergic receptors. It has a vasoconstrictor effect (the vasopressor action of phenylephrine is weaker than that of norepinephrine but more prolonged), and has practically no chronotropic or inotropic effect on the heart. After instillation, phenylephrine contracts the pupillary dilator and the smooth muscles of the conjunctival arterioles, thereby causing pupil dilation and conjunctival vasoconstriction, and improves the outflow of intraocular fluid. Pupil dilation occurs within 10-60 minutes after a single instillation and persists for 4-6 hours. Mydriasis caused by phenylephrine is not accompanied by cycloplegia.

Phenylephrine complements the action of tropicamide since their mechanisms of action are different. The combined use of tropicamide and phenylephrine reduces or eliminates the ability of tropicamide to increase intraocular pressure.

Pharmacokinetics

Tropicamide. Easily penetrates into the eye tissues, is rapidly absorbed into the bloodstream. When using a modified radioreceptor assay, the lower limit of quantitation for tropicamide in plasma is less than 240 ng/ml, the quantitation range is 240 ng/ml – 10 ng/ml. The mean C_max in plasma at the 5th minute after administration was 2.8±1.7 ng/ml. At the 60th minute, the concentration of tropicamide in plasma was 0.46±0.51 ng/ml, and at the 120th minute – below 240 ng/ml.

Phenylephrine. Easily penetrates into the eye tissues, C_max in plasma is observed 10-20 minutes after topical application. Phenylephrine is excreted by the kidneys unchanged (< 20%) or as inactive metabolites.

Indications

Pupil dilation: for diagnostic ophthalmological procedures; before surgical and laser operations.

ICD codes

Dosage Regimen

For diagnostic pupil dilation, instill one drop into the conjunctival sac of each eye 15-30 minutes before the procedure.

For preoperative mydriasis prior to surgical or laser interventions, instill one drop into the conjunctival sac of the eye to be operated on.

Apply gentle pressure to the lacrimal sac area at the inner corner of the eye for 1-2 minutes immediately after instillation to minimize systemic absorption.

Avoid allowing the dropper tip to contact the eye or any other surface to prevent contamination of the solution.

Do not use the preparation in patients under 12 years of age due to contraindication.

In elderly patients or those with cardiovascular risk factors, administer with extreme caution and monitor for systemic effects.

Maximum mydriasis is typically achieved within 20-45 minutes after instillation.

Do not exceed the single recommended dose of one drop per eye for the indicated procedures.

Adverse Reactions

Local reactions: increased intraocular pressure, transient pain, burning in the eye, photophobia, transient decreased vision, release of pigment into the aqueous humor with a temporary increase in intraocular pressure, blockage of the anterior chamber angle (with narrow angle), pain in the brow area, lacrimation, conjunctival hyperemia, keratitis; rarely – reactive miosis the day after application (repeated instillations of the agent at this time may produce less pronounced mydriasis than the day before; this effect is more common in elderly patients).

Systemic side effects: pallor of the skin, dry mouth, redness and dryness of the skin, contact dermatitis, headache, fainting, decreased blood pressure, sensation of palpitations, tachycardia, arrhythmia, bradycardia, ventricular occlusion of the coronary arteries, pulmonary embolism; disorders of the central nervous system, muscle rigidity, frequent urge to urinate, difficulty urinating, decreased gastrointestinal tone and peristalsis leading to constipation; sometimes – vomiting, dizziness; in elderly patients with cardiovascular diseases – ventricular arrhythmias, myocardial infarction.

Contraindications

Hypersensitivity to this combination; angle-closure glaucoma, increased intraocular pressure; cardiovascular diseases (including coronary sclerosis, angina pectoris, arrhythmia, hypertensive crisis); thyrotoxicosis; type 1 diabetes mellitus; concurrent use (as well as within 3 weeks after their discontinuation) of MAO inhibitors; pregnancy, breastfeeding period; age under 12 years.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and breastfeeding.

Pediatric Use

Contraindicated for use in children under 12 years of age.

Special Precautions

Use with caution in patients with type 2 diabetes, elderly patients (risk of ventricular arrhythmias and myocardial infarction in patients with cardiovascular diseases), in patients with cerebrovascular diseases, conditions after surgery (reduced conjunctival healing).

The drops should be instilled into the lower conjunctival sac. To reduce the risk of systemic side effects, gentle pressure with a finger on the projection area of the lacrimal sacs at the inner corner of the eye for 1-2 minutes after instillation is recommended.

Due to significant contraction of the pupillary dilator 30-45 minutes after instillation, pigment particles from the pigment layer of the iris may be detected in the aqueous humor of the anterior chamber. The suspension in the aqueous humor must be differentiated from manifestations of anterior uveitis or from the entry of blood cells into the aqueous humor of the anterior chamber.

Cycloplegics may increase intraocular pressure and provoke the development of angle-closure glaucoma in predisposed individuals, which must be taken into account and a thorough assessment performed before starting treatment; Tropicamide may induce the occurrence of psychoses.

Effect on the ability to drive vehicles and operate machinery

During treatment, driving vehicles and engaging in other hazardous activities requiring increased concentration and speed of psychomotor reactions are not recommended, as changes in accommodation and pupil width may lead to decreased visual acuity.

Drug Interactions

Adrenomimetics enhance, and M-cholinomimetics weaken the effect of tropicamide.

Tricyclic antidepressants, phenothiazines, amantadine, quinidine, antihistamine drugs increase the likelihood of systemic side effects of tropicamide.

Atropine enhances the mydriatic effect of phenylephrine.

Concomitant use with MAO inhibitors, as well as within 21 days after their discontinuation, increases the risk of systemic adrenergic effects.

The vasopressor effect of alpha-adrenomimetics may also be enhanced when used concomitantly with tricyclic antidepressants, propranolol, guanethidine, methyldopa, and M-cholinoblockers. Beta-blockers increase the risk of a sharp increase in blood pressure. Phenylephrine increases the risk of suppression of cardiovascular activity during inhalational general anesthesia.

When prescribing beta-blockers, enhancement of the vasoconstrictor action of phenylephrine is possible due to their suppression of vasodilation.

Due to the risk of a hypertensive crisis, concomitant use of phenylephrine and guanethidine, as well as any other adrenergic blocker or monoamine reuptake inhibitor, is not recommended.

Preliminary instillation of local anesthetics may increase the systemic absorption of the active substances and prolong mydriasis.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.