Inocaine

Inocaine is a local anesthetic drug for ophthalmologic procedures. Contains the component oxybuprocaine.

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Indications Inocaine

It is used for short-term local anesthesia in ophthalmological disorders:

• removal of foreign objects from the conjunctiva, and also the cornea;
• performing gonioscopy or ocular tonometry procedures, as well as other diagnostic tests;
• preparation for retrobulbar or subconjunctival injections.

Release form

The substance is released in the form of eye drops, inside a dropper bottle with a capacity of 5 ml. There is 1 such bottle in the box.

Pharmacodynamics

A local anesthetic that blocks the activity of nerve receptors. It acts by blocking the activity of Na+ channels in the walls of nerve fibers, as well as slowing down the generation of potentials (initially inside small vegetative fibers, then in the area of larger fibers (sensory) and at the final stage - inside the neural fibers themselves). After local administration, it penetrates well into the tissues.

Compared with Tetracaine and other local anesthetics, the drug has a weaker irritating effect on the cornea and conjunctiva. Superficial anesthesia of these areas develops after half a minute and lasts for a 15-minute period. After the end of the local anesthetic effect, sensitivity of the conjunctiva and cornea is restored.

The drug does not affect the accommodation function and the width of the pupil.

Pharmacokinetics

The drug easily penetrates the corneal stroma with a single instillation of the drug into the conjunctival sac. Over the next 15 minutes, a significant decrease in the stromal parameters of the drug is observed, which leads to the development of a 12-15 minute period of anesthesia.

The substance is absorbed into the circulatory system in small quantities, immediately undergoing metabolism there with the formation of inactive metabolic products.

Key metabolic products are 80% excreted via the kidneys in combination with glucuronic acid.

Dosing and administration

The drug is used locally.

When removing foreign objects that have entered the conjunctiva with the cornea: to remove a chalazion, you need to drip 1 drop of the drug with a 1.5-minute interval (pain relief for 5 minutes).

Before starting gonioscopy or ocular tonometry procedures, and other diagnostic procedures: 1 drop of the substance into the conjunctival eye sac. The development of surface anesthesia in the cornea with conjunctiva area begins after 60 seconds. For prolonged anesthesia (up to 1 hour), 3-time instillation with a 4-5-minute interval is required.

Before performing a retrobulbar or subconjunctival injection: 3-fold application of 1 drop of the substance with a 5-minute interval.

During instillation, it is necessary to press lightly on the inner area of the lacrimal sac before starting the procedure and release it after 60 seconds from the moment of instillation – to reduce systemic absorption.

Keep your eyes closed between successive instillations.

Before the drug is administered, the lenses must be removed. After the anesthetic effect of Inocaine has ended, they can be put back on.

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Use Inocaine during pregnancy

Inocaine may be used during pregnancy or breastfeeding only in emergency situations when the potential benefit to the woman is more likely to outweigh the risk of developing negative symptoms in the fetus or infant.

Contraindications

Main contraindications:

• the presence of severe heart failure;
• signs of allergy;
• hyperthyroidism;
• having an open form of penetrating eye injury;
• eye infections;
• severe intolerance to the components of the drug or other local anesthetics from the group of esters such as PABA or the amide category.

Side effects Inocaine

The use of eye drops may cause the following disorders:

• local ophthalmologic manifestations: discomfort, keratitis (also discoid, toxic, candidal and superficial small-spotted), burning in the eye area, keratopathy (including its ulcerative necrotizing, toxic and postoperative forms), fibrinosis affecting the iris, periorbital form of contact dermatitis (including the allergic type of disorder). In addition, there is suppression of the precorneal film (only in people with blue eyes), weakening of the sensitivity of the cornea or a change in its thickness, direct cytotoxic effect on corneal cells (for example, a significant decrease in oxygen consumption by the corneal epithelium) and moderate damage to the epithelial layer of the cornea. False positive readings, decreased spontaneous blinking frequency, tingling sensation, spontaneous eye movements, stromal infiltration, corneal ulcers, peripheral corneal ring formation, cataracts, fibrinous iritis, and decreased tear film stability also occur;
• nervous system disorders: feeling of excitement, severe confusion, disorientation or euphoria, sedative effects, speech, visual or auditory dysfunction, seizures, loss of consciousness and paresthesia;
• lesions of the musculoskeletal structure: muscle cramps;
• respiratory dysfunction: respiratory arrest;
• problems with the gastrointestinal tract: vomiting, nausea or dysphagia;
• symptoms caused by the action of the preservative (benzalkonium chloride): a feeling of irritation or discoloration of soft eye lenses;
• disorders of the cardiovascular system: comatose state or severe sinus bradycardia;

Immune disorders: signs of allergy - for example, urticaria, anaphylaxis or hyperemia, swelling of the eyelids, severe itching, and in addition, contact allergies and Quincke's edema.

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Overdose

If the drug is used in excessively large doses or for too long, general negative symptoms may occur. The systemic toxic effect, in particular, leads to disruption of the cardiovascular system and central nervous system.

Manifestations of intoxication include sedation, euphoria, severe confusion, marked irritability or disorientation, as well as visual, auditory or speech disorders, muscle twitching, hypotension, paresthesia and respiratory disorders. In addition, cardiovascular failure, severe excitability, nausea, insomnia, vomiting, shock or coma, convulsions, loss of consciousness and cardiac arrest may develop.

To eliminate the disorder, you should immediately rinse your eyes with plain water or 0.9% NaCl, and also carry out symptomatic procedures.

Interactions with other drugs

There is no information on the development of any negative or positive reactions in connection with the combined introduction of oxybuprocaine into the conjunctiva with other commonly used eye drops. In theory, the drug may weaken the antibacterial properties of sulfonamides.

Inocaine potentiates the effectiveness of sympathomimetics with succinylcholine, and along with this, β-blockers.

Not compatible with fluorescent solutions (due to the formation of sediment), mercury salts, silver nitrate and alkali solutions.

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Storage conditions

Inocaine should be stored in a place closed to small children. It is forbidden to freeze drops. Temperature indicators are a maximum of 25°C.

Shelf life

Inocaine is allowed to be used within a 2-year period from the date of release of the pharmaceutical substance. An opened bottle has a 1-month shelf life.

Application for children

The drug cannot be prescribed in pediatrics because there is no information regarding its medicinal safety and effectiveness in this group.

Analogues

Analogues of the drug are Dicaine and Lidocaine with Tetracaine.

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Reviews

Inocaine gets pretty good reviews from people on forums. Its positive properties are noted as simplicity and ease of use, speed of action, high-quality anesthetic effect, the ability to buy without a prescription and low cost.

The disadvantages include the appearance of a slight burning sensation in the eyes after instillation, the short-term analgesic effect and the impossibility of long-term use of the drug.