Dexamytrex Ophtiole

Dexamethasone Sodium Phosphate:

• Pharmacological action
• Pharmacokinetics
• Why is Dexamytrex Ophtiole prescribed?
• Dosage and administration
• Dexamytrex Ophtiole (Dexamethasone Sodium Phosphate) side effects, adverse reactions
• Dexamytrex Ophtiole contraindications
• Using during pregnancy and breastfeeding
• Dexamytrex Ophtiole (Dexamethasone Sodium Phosphate) in case of emergency / overdose
• Dexamytrex Ophtiole (Dexamethasone Sodium Phosphate) reviews

Pharmacological action

Dexamytrex Ophtiole is a glucocorticosteroid. This medication Inhibits the function of leukocytes and tissue macrophages. Dexamytrex Ophtiole (Dexamethasone Sodium Phosphate) restricts the migration of leukocytes in the area of inflammation. This drug violates the ability of macrophages to phagocytosis and the formation of interleukin-1. Dexamytrex Ophtiole (Dexamethasone Sodium Phosphate) decreases capillary permeability caused by histamine release. This medicine inhibits the activity of fibroblasts and collagen formation.

Dexamytrex Ophtiole (Dexamethasone Sodium Phosphate) inhibits the activity of phospholipase A2, which leads to suppression of the synthesis of prostaglandins and leukotrienes.

With direct application to the vessels this drug has a vasoconstrictor effect.

Dexamytrex Ophtiole (Dexamethasone Sodium Phosphate) has a pronounced dose-dependent effect on the metabolism of carbohydrates, proteins and fats.

In high doses Dexamytrex Ophtiole (Dexamethasone Sodium Phosphate) may increase the excitability of brain tissue and contributes to lowering the threshold of convulsive readiness.

With systemic use of therapeutic activity of Dexamytrex Ophtiole (Dexamethasone Sodium Phosphate) is due to anti-inflammatory, antiallergic, immunosuppressive and antiproliferative action.

For external and local use of therapeutic activity of Dexamytrex Ophtiole (Dexamethasone Sodium Phosphate) is due to anti-inflammatory, antiallergic and antiexudative (due to vasoconstrictor effect) effect.

Pharmacokinetics

The plasma protein binding is 60-70%. This medication penetrates histohematic barriers. In a small amount it is excreted in breast milk. Dexamytrex Ophtiole (Dexamethasone Sodium Phosphate) metabolized in a liver. T_1/2 is 2-3 hours. This drug is excreted by kidneys.

When Dexamytrex Ophtiole (Dexamethasone Sodium Phosphate) applied topically in ophthalmology it absorbed through the cornea with intact epithelium in moisture anterior chamber. When inflammation of the tissues of the eye or mucosal damage and corneal absorption rate of Dexamytrex Ophtiole (Dexamethasone Sodium Phosphate) significantly increased.

Why is Dexamytrex Ophtiole prescribed?

For oral administration: Biermer's disease; acute and subacute thyroiditis, hypothyroidism, progressive ophthalmopathy associated with thyrotoxicosis; bronchial asthma; rheumatoid arthritis in the acute phase; ulcerative colitis; connective tissue disease; autoimmune hemolytic anemia, thrombocytopenia, aplasia and hypoplasia of hematopoiesis, agranulocytosis, serum sickness; acute erythroderma, pemphigus (normal), acute eczema (early treatment); malignant tumor (as a palliative therapy); congenital adrenogenital syndrome; cerebral edema (usually after a preliminary parenteral corticosteroids).

For parenteral administration: shock of various origins; swelling of the brain (with brain tumors, head injury, neurosurgical intervention, brain hemorrhage, encephalitis, meningitis, radiation damage); asthmatic status; severe allergic reactions (angioedema, bronchospasm, dermatosis, acute anaphylactic reaction to medication, transfusion serum, pyrogenic reactions); acute hemolytic anemia, thrombocytopenia, acute lymphoblastic leukemia, agranulocytosis; serious infectious diseases (in combination with antibiotics); acute adrenal insufficiency, acute croup; arthropathy (scapulohumeral periarthritis, epicondylitis, styloiditis, bursitis, tenosynovitis, compression neuropathy, osteochondrosis, arthritis of various etiologies, osteoarthritis).

For use in ophthalmic practice: not purulent and allergic conjunctivitis, keratitis, keratoconjunctivitis without damaging the epithelium, iritis, iridocyclitis, blefaroconjuntivitis, blepharitis, episcleritis, scleritis, inflammation of injuries and eye surgeries, sympathetic ophthalmia.

Dosage and administration

The dosing regimen is individual. Orally for severe disease at the beginning of treatment it is prescribed to 10-15 mg / day, maintenance dose may be 2-4.5 mg / day or more. The daily dose divided into 2-3 doses. In small doses Dexamytrex Ophtiole is taken 1 time in the morning.

For parenteral administration this medication is administered IV slowly bolus or infusion (acute and urgent conditions); IM; it is possible also periarticular and intraarticular injection. During the day it can be administered from 4 to 20 mg of Dexamytrex Ophtiole (Dexamethasone Sodium Phosphate) 3-4 times / day. The duration of parenteral administration is usually 3-4 days, then move on to maintenance therapy of oral form. In the acute period in various diseases and early treatment Dexamytrex Ophtiole (Dexamethasone Sodium Phosphate) used in higher doses. Upon reaching the effect the dose is decreased within a few days before reaching the maintenance dose or until discontinuation of treatment.

When used in ophthalmology for acute conditions this drug instilled into conjunctival sac 1-2 drops every 1-2 hours, then with a decrease in inflammation after every 4-6 hours. The duration of treatment is from 1-2 days to several weeks depending on the clinical course of disease.

Dexamytrex Ophtiole (Dexamethasone Sodium Phosphate) side effects, adverse reactions

Endocrine system: impaired glucose tolerance, steroid diabetes mellitus or manifestation of latent diabetes mellitus, suppression of adrenal function, Itsenko-Cushing syndrome (including moon face, obesity, pituitary type, hirsutism, increased blood pressure, dysmenorrhea, amenorrhea, myasthenia gravis, striae), delayed sexual development in children.

Metabolism: increased excretion of calcium, hypocalcemia, weight gain, negative nitrogen balance (increased protein breakdown), increased sweating, hypernatremia, hypokalemia.

CNS: delirium, disorientation, euphoria, hallucinations, manic-depressive psychosis, depression, paranoia, increased intracranial pressure, nervousness or anxiety, insomnia, dizziness, vertigo, pseudotumor cerebellum, headache, convulsions.

Cardio-vascular system: arrhythmia, bradycardia (up to cardiac arrest); development (in predisposed patients) or increased severity of chronic heart failure, ECG changes typical of hypokalemia, increased blood pressure, hypercoagulability, thrombosis. In patients with acute and subacute myocardial infarction - spread necrosis, slowing the formation of scar tissue that can lead to rupture of the heart muscle; with intracranial introduction - nosebleeds.

Digestive system: nausea, vomiting, pancreatitis, steroid gastric and duodenal ulcers, erosive esophagitis, bleeding and perforation of the gastrointestinal tract, increase or decrease in appetite, flatulence, hiccups; rarely - increased activity of hepatic transaminases and alkaline phosphatase.

Sensory organs: posterior subcapsular cataracts, increased intraocular pressure with possible damage to the optic nerve, propensity to develop secondary bacterial, fungal or viral infections of the eye, trophic changes of the cornea, exophthalmos.

Musculoskeletal system: growth retardation and ossification processes in children (premature closure of epiphyseal growth zones), osteoporosis (very rare - a pathological bone fractures, aseptic necrosis of head of humerus and femur), rupture of tendons of muscles, steroid myopathy, reduced muscle mass (atrophy).

Dermatological reactions: delayed wound healing, petechiae, ecchymosis, skin thinning, hyper or hypopigmentation, steroid acne, stretch marks, susceptibility to the development of pyoderma and candidiasis.

Allergic reactions: generalized (including skin rash, itching, anaphylactic shock) and when applied topically.

Effects associated with immunosuppressive action: development or worsening of infection (the appearance of this side effect contribute jointly used immunosuppressive drugs, and vaccinations).

Local reactions: when Dexamytrex Ophtiole (Dexamethasone Sodium Phosphate) administered parenteral - tissue necrosis.

For external use: rarely - itching, redness, burning, dryness, folliculitis, acne, hypopigmentation, perioral dermatitis, allergic dermatitis, maceration of the skin, secondary infection, skin atrophy, striae, miliaria. With prolonged use or application to large areas of skin may develop systemic side effects characteristic of SCS.

Dexamytrex Ophtiole contraindications

For short-term use for health reasons - increased sensitivity to Dexamytrex Ophtiole (Dexamethasone Sodium Phosphate).

For intra-articular injection and injection directly into the lesion: previous arthroplasty, abnormal bleeding (endogenous or caused by the use of anticoagulants), intra-articular fracture, infection (sepsis) inflammation in the joints and periarticular infections (including in history), as well as general infectious disease, pronounced juxta-articular osteoporosis, no signs of inflammation in the joints ("dry" joint, such as osteoarthritis without synovitis), severe bone destruction and deformity of the joint (a sharp narrowing of joint space, ankylosis), instability of the joint as a result of arthritis, aseptic necrosis of the epiphyses of bones forming the joint.

For external use: bacterial, viral, fungal skin diseases, tuberculosis, skin, cutaneous manifestations of syphilis, skin tumors, post-vaccination period, violation of the integrity of the skin (ulcers, wounds), children's age (up to 2 years, with itching in the anal area - up to 12 years), rosacea, acne vulgaris, perioral dermatitis.

For use in ophthalmology: bacterial, viral, fungal eye diseases, tuberculosis eye damage, tampering with the ocular epithelium, acute form of purulent eye infection in the absence of specific therapy, diseases of the cornea, combined with defects in the epithelium, trachoma, glaucoma.

Using during pregnancy and breastfeeding

During pregnancy and lactating Dexamytrex Ophtiole (Dexamethasone Sodium Phosphate) is used taking into account the expected therapeutic effect and adverse effect on the fetus. Long-term therapy during pregnancy does not exclude the possibility of violations of fetal growth. In the case of the end of pregnancy there is a danger of atrophy of the adrenal cortex of the fetus, which may require replacement therapy in the newborn.

Category effects on the fetus by FDA - C.

Dexamytrex Ophtiole (Dexamethasone Sodium Phosphate) in case of emergency / overdose

Symptoms: increased side effects.

Treatment: the development of adverse reactions - symptomatic therapy, the Itsenko-Cushing syndrome - the prescription of aminoglutethimide.

Gentamicin Sulfate:

• Dexamytrex Ophtiole (Gentamicin Sulfate) reviews

F-27078915

NADA #141-177, Approved by FDA.

PRODUCT

INFORMATION

VETERINARY

For Otic Use in Dogs Only

CAUTION Federal law restricts this drug to use by or on the order of a licensed veterinarian.

Keep this and all drugs out of the reach of children.

DESCRIPTION Each gram of Dexamytrex Ophtiole (Gentamicin Sulfate) Otic Suspension contains Dexamytrex Ophtiole (Gentamicin Sulfate) sulfate, USP equivalent to 3 mg Dexamytrex Ophtiole (Gentamicin Sulfate) base; mometasone furoate monohydrate equivalent to 1 mg mometasone; and 10 mg clotrimazole, USP in a mineral oilbased system containing a plasticized hydrocarbon gel.

PHARMACOLOGY

Dexamytrex Ophtiole (Gentamicin Sulfate): Dexamytrex Ophtiole (Gentamicin Sulfate) sulfate is an aminoglycoside antibiotic active against a wide variety of gram-negative and grampositive bacteria. In vitro tests have determined that Dexamytrex Ophtiole (Gentamicin Sulfate) is bactericidal and acts by inhibiting normal protein synthesis in susceptible microorganisms. In clinical trials, Dexamytrex Ophtiole (Gentamicin Sulfate) was shown to have a range of activity against the following organisms commonly isolated from infected canine ears:

Pseudomonas spp. (including P. aeruginosa), coagulasepositive staphylococci, Enterococcus faecalis, Proteus mirabilis and beta-hemolytic streptococci.

Mometasone: Mometasone furoate monohydrate is a synthetic adrenocorticoid characterized by a novel (2') furoate 17-ester having chlorine at the 9 and 21 positions, which have shown to possess high topical potency.

Systemic absorption of mometasone furoate ointment was found to be minimal (2%) over 1 week when applied topically to dogs with intact skin. In a 6-month dermal toxicity study using 0.1% mometasone ointment on healthy intact skin in dogs, systemic effects typical of corticosteroid therapy were noted.

The extent of percutaneous absorption of topical corticosteroids is determined by many factors including the integrity of the epidermal barrier. Topical corticosteroids can be absorbed from normal, intact skin. Inflammation can increase percutaneous absorption. Once absorbed through the skin, topical corticosteroids are handled through pharmacokinetic pathways similar to systemically administered corticosteroids.

Clotrimazole: Clotrimazole is a broad-spectrum antifungal agent that is used for the treatment of dermal infections caused by various species of dermatophytes and yeast. The primary action of clotrimazole is against dividing and growing organisms.

In vitro, clotrimazole exhibits fungistatic and fungicidal activity against isolates of Trichophyton rubrum, Trichophyton mentagrophytes, Epidermophyton floccosum, Microsporum canis, Candida spp., and Malassezia pachydermatis. Resistance to clotrimazole is very rare among the fungi that cause superficial mycoses. In an induced otitis externa study using dogs infected with Malassezia pachydermatis, 1% clotrimazole in the vehicle formulation was effective both microbiologically and clinically in terms of reduction of exudate, odor, and swelling.

In studies of the mechanism of action, the minimum fungicidal concentration of clotrimazole caused leakage of intracellular phosphorus compounds into the ambient medium with concomitant breakdown of cellular nucleic acids and accelerated potassium efflux. These events began rapidly and extensively after addition of the drug. Clotrimazole is very poorly absorbed following dermal application.

Gentamicin-Mometasone-Clotrimazole: By virtue of its three active ingredients, Dexamytrex Ophtiole (Gentamicin Sulfate) Otic Suspension has antibacterial, anti-inflammatory, and antifungal activity. In clinical field trials, Dexamytrex Ophtiole (Gentamicin Sulfate) Otic Suspension was effective in the treatment of otitis externa associated with bacteria and Malassezia pachydermatis. Dexamytrex Ophtiole (Gentamicin Sulfate) Otic Suspension reduced discomfort, redness, swelling, exudate, and odor.

INDICATIONS Dexamytrex Ophtiole (Gentamicin Sulfate) Otic Suspension is indicated for the treatment of otitis externa in dogs caused by susceptible strains of yeast (Malassezia pachydermatis) and bacteria (Pseudomonas spp. [including P. aeruginosa], coagulasepositive staphylococci, Enterococcus faecalis, Proteus mirabilis, and beta-hemolytic streptococci).

CONTRAINDICATIONS If hypersensitivity to any of the components occurs, treatment should be discontinued and appropriate therapy instituted. Concomitant use of drugs known to induce ototoxicity should be avoided. Do not use in dogs with known perforation of eardrums.

WARNINGS The use of these components has been associated with deafness or partial hearing loss in a small number of sensitive dogs (eg, geriatric). The hearing deficit is usually temporary. If hearing or vestibular dysfunction is noted during the course of treatment, discontinue use of Dexamytrex Ophtiole (Gentamicin Sulfate) Otic Suspension immediately and flush the ear canal thoroughly with a nonototoxic solution.

Corticosteroids administered to dogs, rabbits, and rodents during pregnancy have resulted in cleft palate in offspring. Other congenital anomalies including deformed forelegs, phocomelia, and anasarca have been reported in offspring of dogs that received corticosteroids during pregnancy.

Field and experimental data have demonstrated that corticostroids administered orally or parenterally to animals may induce the first stage of parturition if used during the last trimester of pregnancy and may precipitate premature parturition followed by dystocia, fetal death, retained placenta, and metritis.

PRECAUTIONS Before instilling any medication into the ear, examine the external ear canal thoroughly to be certain the tympanic membrane is not ruptured in order to avoid the possibility of transmitting infection to the middle ear as well as damaging the cochlea or vestibular apparatus from prolonged contact.

Administration of recommended doses of Dexamytrex Ophtiole (Gentamicin Sulfate) Otic Suspension beyond 7 days may result in delayed wound healing. If overgrowth of nonsusceptible bacteria or fungi occurs, treatment should be discontinued and appropriate therapy instituted.

Avoid ingestion. Adverse systemic reactions have been observed following the oral ingestion of some topical corticosteroid preparations. Patients should be closely observed for the usual signs of adrenocorticoid overdosage which include sodium retention, potassium loss, fluid retention, weight gain, polydipsia, and/or polyuria. Prolonged use or overdosage may produce adverse immunosuppressive effects.

Use of corticosteroids, depending on dose, duration, and specific steroid, may result in endogenous steroid production inhibition following drug withdrawal. In patients presently receiving or recently withdrawn from corticosteroid treatments, therapy with a rapidly acting corticosteroid should be considered in especially stressful situations.

TOXICOLOGY Field and safety studies with Dexamytrex Ophtiole (Gentamicin Sulfate) Otic Suspension have shown a wide safety margin at the recommended dose level in dogs (see PRECAUTIONS/ADVERSE REACTIONS ).

ADVERSE REACTIONS

Dexamytrex Ophtiole (Gentamicin Sulfate): While aminoglycosides are absorbed poorly from skin, intoxication may occur when aminoglycosides are applied topically for prolonged periods of time to large wounds, burns, or any denuded skin, particularly if there is renal insufficiency. All aminoglycosides have the potential to produce reversible and irreversible vestibular, cochlear, and renal toxicity.

Mometasone: ALP (SAP) and ALT (SGPT) enzyme elevations, weight loss, anorexia, polydipsia, polyuria, neutrophilia, and lymphopenia have occurred following the use of parenteral, high-dose, and/or prolonged or systemic synthetic corticosteroids in dogs. Cushing's syndrome in dogs has been reported in association with prolonged or repeated steroid therapy.

Clotrimazole: The following have been reported occasionally in humans in connection with the use of clotrimazole: erythema, stinging, blistering, peeling, edema, pruritus, urticaria, and general irritation of the skin not present before therapy.

Dexamytrex Ophtiole (Gentamicin Sulfate) Otic Suspension: In field studies following once daily teatment with Dexamytrex Ophtiole (Gentamicin Sulfate) Otic Suspension, ataxia, proprioceptive deficits, and increased water consumption were observed in less than 1% of 164 dogs. In a field study following twice-daily treatment with Dexamytrex Ophtiole (Gentamicin Sulfate) Otic Suspension, inflammation of the pinna and diarrhea were observed in less than 1% of 141 dogs.

DOSAGE AND ADMINISTRATION

The external ear canal should be thoroughly cleaned and dried before treatment. Verify that the eardrum is intact. For dogs weighing less than 30 lbs, instill 4 drops from the 7.5 g, 15 g, and 30 g bottles (2 drops from the 215 g bottle) of Dexamytrex Ophtiole (Gentamicin Sulfate) Otic Suspension once daily into the ear canal. For dogs weighing 30 lbs or more, instill 8 drops from the 7.5 g, 15 g, and 30 g bottles (4 drops from the 215 g bottle) once daily into the ear canal. Therapy should continue for 7 consecutive days.

HOW SUPPLIED Dexamytrex Ophtiole (Gentamicin Sulfate) Otic Suspension is available in 7.5 g (NDC 14043-120-75), 15 g (NDC 14043-120-15), 30 g (NDC 14043-120-30), and 215 g (NDC 14043-120-21) plastic bottles.

Store between 2° and 25°C (36° and 77°F). Shake well before use.

U.S. Patent No. 6,127,353.

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