Maxitrol

Maxitrol is used in the treatment of ophthalmic diseases. This is a combination medicine, which contains antibacterial substances and corticosteroids.

[1]

Indications of the maxitrola

It is indicated for inflammation of the eye tissues (in cases where the use of corticosteroids is required) with the existing bacterial infection (surface type) infection or the risk of its appearance. Among them - an inflammatory process in the area of the connective membrane of the eyelids or bulbar conjunctiva, and in addition in the area of the cornea, as well as the anterior part of the eyeball; This includes also the anterior uveitis in chronic form and the trauma of the cornea, which was caused by a thermal, radiation or chemical burn or penetration of a foreign object into it.

[2]

Release form

Produced in the form of eye drops in special flacon-droppers with a volume of 5 ml.

Pharmacodynamics

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

Dexamethasone is an artificial SCS with powerful anti-inflammatory properties. Polymyxin B is a cyclic-type lipopeptide capable of passing through the cell walls of gram-negative microbes, as well as destroying the cytoplasmic membrane. In this case, relative to Gram-positive microbes this substance shows less activity.

Neomycin is an aminoglycoside that acts on bacterial cells, inhibiting the synthesis process inside the ribosome, as well as the connection between polypeptides.

Stability of bacteria with respect to polymyxin B develops at the chromosomal level and occurs rarely. A very important element of this process is the modification of the phospholipids entering the cytoplasmic membrane.

Resistance to neomycin develops in several different ways, among which:

• change of ribosomal subunits inside microbial cells;
• violation of the processes of moving neomycin into cells;
• inactivation of enzymes through phosphorylation, adenylation, and acetylation.

Genetic data that contribute to the production of inactivating enzymes can be transported using bacterial plasmids or chromosomes.

Gram-positive aerobes that are sensitive to the action of the drug: Bacillus simplex, wax bacillus, cabbage stick and Bacillus pumilus. In addition, also Corynebacterium accolens and Corynebacterium macginleyi, Corynebacterium bovis with Corynebacterium pseudodiphtheriticum and Corynebacterium propinquum. In addition, it affects the sensitive to methicillin, golden and epidermal staphylococci, as well as Staphylococcus capitis, staphylococcus varvers and Staphylococcus pasteuri. Along with this, the drug acts on streptococcus mutants.

Gram-negative aerobes exposed to drugs: Influenza wand, Klebsiella pneumonia, Moraxella cataralis and Moraxella lacunata, as well as Pseudomonas aeruginosa.

Conditionally resistant to the action of LS types of bacteria: methicillin-resistant epidermal staphylococcus, and in addition Staphylococcus lugdunensis and Staphylococcus hominis.

Gram-positive aerobes resistant to the effects of drugs: enterococcus fecal, methicillin-resistant Staphylococcus aureus, streptococcus mitis and pneumococcus.

Gram-negative aerobes resistant to the drug: Serratia species.

Resistant to Maxitrol anaerobes: propionibacterium acne.

Dexamethasone is a SCS with a moderate impact strength, it perfectly passes inside the eye tissues. Corticosteroids have vasoconstrictive and anti-inflammatory properties. In addition, they inhibit the inflammatory reaction together with the manifestation of symptoms in a variety of disorders, but often the disorder itself does not eliminate it.

[3], [4], [5],

Pharmacokinetics

The effect of dexamethasone after local use (instillation in the eyes) of a drug suspension containing 0.1% of this substance was investigated in people who underwent a cataract surgery. Peak value within the eye fluid (about 30 ng / ml) the drug reached within 2 hours. Then this level decreased with a half-life, which is equal to the 3-m clock.

Excretion of dexamethasone occurs through metabolic processes. About 60% of the drug is excreted in the urine in the form of substance 6-β-hydrodexamethasone. There is no unchanged dexamethasone in the urine.

The half-life is rather short - about 3-4 hours.

About 77-84% of the substance is synthesized with serum albumin. The clearance level is in the range of 0,111-0,225 l / h / kg, and the distribution volume varies in the range of 0.576-1.15 l / kg. After internal reception of the active component, its bioavailability is approximately 70%.

The pharmacokinetics of neomycin is similar to that of other aminoglycosides.

It was not possible to determine neomycin in urine or serum after treatment with 0.5% ointment of neomycin sulfate in an amount up to 47.4 g of the skin of volunteers, and leaving it for 6 hours.

Polymyxin B is slightly absorbed through the mucous membranes - this index varies from the unstable low to the completely absent. The substance is not found inside urine or serum after treatment with large areas of skin with burns, as well as maxillary sinuses with conjunctiva.

[6], [7], [8]

Dosing and administration

Drops are used in the treatment of ophthalmic disorders. Before starting the procedure, you need to shake the bottle thoroughly. To prevent contamination of the suspension and the tip of the dropper, care should be taken to perform the instillation procedure without touching the eyelids and other surfaces.

Use in adults, as well as in elderly patients.

During the treatment of mild forms of pathology, it is necessary to instill 1-2 drops per procedure into the affected eye (for a total of 4-6 procedures in a day). The frequency of instillation should be gradually reduced as the state of health improves. It is necessary to treat attentively the manifestations of the disease and not finish the treatment prematurely.

In the case of a severe course of the disease, it is required to conduct the procedures hourly (1-2 drops each), gradually reducing their frequency as the inflammatory process stops.

After the instillation procedure, it is required to close the eyes tightly or to perform nasolacrimal occlusion. This method allows us to weaken the systemic absorption of the medication introduced through the eyes, thereby reducing the risk of systemic side effects.

With simultaneous treatment with the use of other local ophthalmic drugs, a minimum of 5-minute interval between procedures is required. In this case ointments for the eyes should be used in the last place.

[10], [11]

Use of the maxitrola during pregnancy

There are only limited information on the use of pregnant substances neomycin, dexamethasone or polymyxin B.

Animal tests showed that the drug has reproductive toxicity, so you can not use these eye drops during pregnancy.

Contraindications

Among the contraindications:

• hypersensitivity to the active components of the drug or other of its constituent elements;
• provoked by herpes simplex keratitis;
• cowpox and chicken pox, as well as other viral infectious processes affecting the conjunctiva with the cornea;
• pathology of the eye structures, having a fungal origin;
• mycobacterial eye infections.

It is also forbidden to use in children, since the efficacy and safety of the use of drugs in the indicated group of patients is not established.

Side effects of the maxitrola

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

Other negative reactions:

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

Among the additional negative manifestations due to the use of dexamethasone, which can develop as a result of the use of Maxitrol: the appearance of headaches or dizziness, the appearance of scales on the edges of the eyelids, the development of conjunctivitis, dysgeusia, erosion in the cornea and dry keratoconjunctivitis, and deterioration of visual acuity.

Individual patients may have an intolerance to local aminoglycosides. In addition, the locally used (buried in the eye) neomycin is capable of provoking a reaction of skin hypersensitivity.

Long-term local (instillation into the eye) use of corticosteroids can increase intraocular pressure, resulting in damage to the optic nerve. In addition, the visual acuity is weakened, the visual field is violated and a cup-shaped cataract is formed.

Combination of the drug with other antimicrobial drugs and corticosteroids can trigger the occurrence of secondary infections.

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

[9]

Interactions with other drugs

When combined with local steroid agents, as well as NSAIDs, the risk of complications in wound healing in the cornea may increase.

[12],

Storage conditions

Drops should be kept out of the reach of children. The bottle should be tightly sealed and kept in an upright position. Temperature values are a maximum of 30 ° C. The medicine is not allowed to be frozen.

Shelf life

Maxitrol is suitable for use in the period of 2 years from the date of its release. In this case, the expiration date of the opened bottle is 1 month.

[13],