Maxitrol

Maxitrol is used in the treatment of ophthalmological diseases. It is a combination drug that contains antibacterial substances and corticosteroids.

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Indications Maxitrol

It is indicated for inflammation of the eye tissues (in cases where the use of corticosteroids is required) with an existing infectious process of bacterial origin (superficial type) or with the risk of its occurrence. Among these are the inflammatory process in the area of the conjunctiva of the eyelids or bulbar conjunctiva, as well as in the area of the cornea, as well as the anterior part of the eyeball; this also includes chronic anterior uveitis and corneal trauma caused by thermal, radiation or chemical burns or penetration of a foreign object into it.

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Release form

It is produced in the form of eye drops in special dropper bottles with a volume of 5 ml.

Pharmacodynamics

Maxitrol has a dual effect - it suppresses signs of inflammation (this is facilitated by the GCS substance dexamethasone), and also has an antimicrobial effect (this is provided by 2 antibiotics - neomycin with polymyxin B).

Dexamethasone is an artificial GCS with powerful anti-inflammatory properties. Polymyxin B is a cyclic lipopeptide that can pass through the cell walls of gram-negative microbes and destroy the cytoplasmic membrane. However, this substance is less active against gram-positive microbes.

Neomycin is an aminoglycoside that acts on bacterial cells by inhibiting the process of synthesis within ribosomes, as well as the connection between polypeptides.

Bacterial resistance to polymyxin B develops at the chromosomal level and occurs quite rarely. A very important element of this process is the modification of phospholipids in the cytoplasmic membrane.

Resistance to neomycin develops in several different ways, including:

• changes in ribosome subunits inside microbial cells;
• disruption of the processes of neomycin movement into cells;
• inactivation of enzymes through the processes of phosphorylation, adenylation, and acetylation.

Genetic data that promote the production of inactivating enzymes can be transported via bacterial plasmids or chromosomes.

Gram-positive aerobes that are sensitive to the drug: Bacillus simplex, wax bacillus, cabbage bacillus and Bacillus pumilus. In addition, also Corynebacterium accolens and Corynebacterium macginleyi, Corynebacterium bovis with Corynebacterium pseudodiphtheriticum and Corynebacterium propinquum. In addition, it affects methicillin-sensitive Staphylococcus aureus and Staphylococcus epidermidis, as well as Staphylococcus capitis, Staphylococcus warneri and Staphylococcus pasteuri. Together with this, the drug acts on Streptococcus mutans.

Gram-negative aerobes susceptible to drug action: influenza bacillus, Klebsiella pneumoniae, Moraxella catarrhalis and Moraxella lacunata, as well as Pseudomonas aeruginosa.

Conditionally drug-resistant bacterial species: methicillin-resistant Staphylococcus epidermidis, as well as Staphylococcus lugdunensis and Staphylococcus hominis.

Gram-positive drug-resistant aerobes: Enterococcus faecalis, methicillin-resistant Staphylococcus aureus, Streptococcus mitis, and Streptococcus pneumoniae.

Gram-negative drug-resistant aerobes: Serratia species.

Maxitrol-resistant anaerobes: Propionibacterium acnes.

Dexamethasone is a moderate-strength corticosteroid that penetrates well into the eye tissue. Corticosteroids have vasoconstrictor and anti-inflammatory properties. They also suppress the inflammatory response along with the symptoms of various disorders, but often do not eliminate the disorder itself.

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Pharmacokinetics

The effect of dexamethasone after local use (dropping into the eyes) of a medicinal suspension containing 0.1% of this substance was studied in people who had undergone cataract surgery. The drug reached its peak value in the eye fluid (about 30 ng/ml) over a period of 2 hours. Then this level decreased with a half-life of 3 hours.

Excretion of dexamethasone occurs via metabolic processes. About 60% of the drug is excreted in the urine as 6-β-hydrodexamethasone. No unchanged dexamethasone is found in the urine.

The half-life is quite short – approximately 3-4 hours.

About 77-84% of the substance is synthesized with serum albumin. The clearance rate is within 0.111-0.225 l/hour/kg, and the distribution volume varies in the range of 0.576-1.15 l/kg. After internal administration of the active component, its bioavailability is approximately 70%.

The pharmacokinetics of neomycin are similar to those of other aminoglycosides.

Neomycin could not be detected in urine or serum after application of 0.5% neomycin sulfate ointment to up to 47.4 g of volunteer skin and leaving it on for 6 hours.

Polymyxin B is poorly absorbed through mucous membranes - this indicator varies from unstable low to completely absent. The substance is not detected in urine or serum after treating large areas of skin with burns, as well as the maxillary sinuses with conjunctiva.

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Dosing and administration

Drops are used to treat ophthalmological disorders. Before starting the procedure, shake the bottle thoroughly. To prevent contamination of the suspension and the dropper tip, the instillation procedure should be carried out with caution, without touching the eyelids or other surfaces.

Use in adults and elderly patients.

During treatment of mild forms of pathologies, it is necessary to instill 1-2 drops into the affected eye per procedure (4-6 procedures are allowed per day). The frequency of instillation should be gradually reduced as the health condition improves. It is necessary to pay close attention to the manifestations of the disease and not to terminate treatment prematurely.

In case of severe course of the disease, it is necessary to carry out procedures every hour (1-2 drops), gradually reducing their frequency as the inflammatory process ceases.

After the instillation procedure, it is necessary to close the eyes tightly or perform nasolacrimal occlusion. This method allows to weaken the systemic absorption of the drug administered through the eyes, thereby reducing the risk of developing systemic side effects.

When treating simultaneously with other local ophthalmic drugs, it is necessary to observe at least a 5-minute interval between procedures. In this case, eye ointments should be used last.

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Use Maxitrol during pregnancy

There is limited information about the use of neomycin, dexamethasone, or polymyxin B in pregnant women.

Animal tests have shown that the drug has reproductive toxicity, which is why these eye drops should not be used during pregnancy.

Contraindications

Among the contraindications:

• hypersensitivity to the active components of the drug or other of its components;
• herpes simplex keratitis;
• cowpox and chickenpox, as well as other viral infectious processes affecting the conjunctiva and cornea;
• pathologies of eye structures of fungal origin;
• mycobacterial eye infections.

It is also prohibited to use in children, since the efficacy and safety of the drug in this group of patients has not been established.

Side effects Maxitrol

Most often, the use of drops during the clinical trials led to the development of side effects such as irritation and discomfort in the eyes, as well as the appearance of keratitis.

Other adverse reactions:

• immune system: manifestations of intolerance have rarely developed;
• ophthalmologic disorders: occasionally increased intraocular pressure, photophobia or mydriasis developed, drooping of the upper eyelid, ocular itching, pain, sensation of a foreign body, as well as swelling and discomfort in the eyes, blurred vision, increased lacrimation, and ocular hyperemia occurred.

Additional adverse reactions that have occurred as a result of using dexamethasone and may develop as a result of using Maxitrol include: headaches or dizziness, scaly patches on the edges of the eyelids, conjunctivitis, dysgeusia, corneal erosion and dry keratoconjunctivitis, and decreased visual acuity.

Some patients may have intolerance to topical aminoglycosides. In addition, neomycin applied topically (in the eyes) can provoke a skin hypersensitivity reaction.

Long-term topical (eye drops) use of corticosteroids can increase intraocular pressure, resulting in damage to the optic nerve. In addition, visual acuity is weakened, the visual field is impaired, and cup-shaped cataracts are formed.

Combining the drug with other antimicrobial drugs and corticosteroids may provoke the development of secondary infections.

Since the drops contain corticosteroids, if the patient has pathologies that cause thinning of the sclera or cornea, their prolonged use increases the likelihood of perforation.

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Interactions with other drugs

When combined with topical steroids and NSAIDs, the likelihood of complications during corneal wound healing may increase.

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Storage conditions

The drops must be kept out of the reach of children. The bottle must be tightly sealed and stored in an upright position. Temperature values are a maximum of 30°C. The medicine must not be frozen.

Shelf life

Maxitrol is suitable for use within 2 years from the date of its release. The shelf life of an opened bottle is 1 month.

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