Elzhina

Uses

Econazole Cream: All fungal skin infections due to dermatophytes, yeasts, moulds and other fungi. These include Vulvo-vaginal candidiasis, Candidial napkin rash, and other candidial infection, Ringworm (tinea) infections, Athlete's foot, Paronychia, Pityriasis versicolor and Balanitis.

Econazole-G Cream: Vulvo-vaginal candidiasis or any other fungal infection of vagina.

Econazole VT: Vulvo-vaginal candidiasis or any other fungal infection of vagina.

For the treatment of onychomycosis, local therapy with Econazole cream, combined with an oral antimycotic, is recommended.

Neomycin is an aminoglycoside antibiotic agent used orally and topically to treat a wide variety of infections in the body.

Oral neomycin sulfate is indicated as an adjunctive therapy in hepatic coma (portal-system encephalopathy) by reducing ammonia-forming bacteria in the intestinal tract. It is strongly recommended that oral neomycin is only used in infections that are proven or strongly suspected to be caused by susceptible bacteria to reduce the risk of the development of drug-resistant bacteria.

Neomycin, in combination with polymyxin B sulfates and hydrocortisone in otic suspensions, is used in the treatment of superficial bacterial infections of the external auditory canal caused by organisms susceptible to the antibiotics. This otic formulation is also used in the treatment of infections of mastoidectomy and fenestration cavities caused by organisms susceptible to the antibiotics.

The ophthalmic solution containing neomycin in combination with polymyxin B sulfates and dexamethasone is used to treat steroid-responsive inflammatory ocular conditions for which a corticosteroid is indicated and where bacterial infection or a risk of bacterial infection exists.

Ornidazole is used for Amoebiasis (Intestinal and hepatic), Giardiasis, Trichomoniasis, Bacterial vaginosis, Treatment of susceptible anaerobic infections

Prednisolone eye drops is used for the treatment of steroid-responsive inflammation of the palpebral and bulbar conjunctiva, cornea and anterior segment of the globe.

Prednisolone tablet, Injection is used forAllergy and anaphylaxis: bronchial asthma, drug hypersensitivity reactions, serum sickness, angioneurotic oedema, anaphylaxis.

Respiratory disease: allergic pneumonitis, asthma, occupational asthma, pulmonary aspergillosis, pulmonary fibrosis, pulmonary alveolitis, aspiration of foreign body, aspiration of stomach contents, pulmonary sarcoid, drug induced lung disease, adult respiratory distress syndrome, spasmodic croup.

Rheumatic disorders: rheumatoid arthritis, polymyalgia rheumatica, juvenile chronic arthritis, systemic lupus erythematosus, dermatomyositis, mixed connective tissue disease.

Arteritis/collagenosis: giant cell arteritis/polymyalgia rheumatica, mixed connective tissue disease, polyarteritis nodosa, polymyositis.

Blood disorders: haemolytic anaemia (auto-immune), leukaemia (acute and chronic lymphocytic), lymphoma, multiple myeloma, idiopathic thrombocytopenic purpura.

Cardiovascular disorders: post-myocardial infarction syndrome, rheumatic fever with severe carditis.

Endocrine disorders: primary and secondary adrenal insufficiency, congenital adrenal hyperplasia.

Gastro-intestinal disorders: Crohn's disease, ulcerative colitis, persistent coeliac syndrome (coeliac disease unresponsive to gluten withdrawal), auto-immune chronic active hepatitis, multisystem disease affecting liver, biliary peritonitis.

Infections (with appropriate chemotherapy): helminthic infestations, Herxheimer reaction, infectious mononucleosis, miliary tuberculosis, mumps orchitis (adult), tuberculous meningitis, rickettsial disease.

Muscular disorders: polymyositis, dermatomyositis.

Neurological disorders: infantile spasms, Shy-Drager syndrome, sub-acute demyelinating polyneuropathy.

Ocular disease: scleritis, posterior uveitis, retinal vasculitis, pseudo-tumours of the orbit, giant cell arteritis, malignant ophthalmic Graves disease.

Renal disorders: lupus nephritis, acute interstitial nephritis, minimal change glomerulonephritis.

Skin disorders: pemphigus vulgaris, bullous pemphigoid, systemic lupus erythematosus, pyoderma gangrenosum.

Miscellaneous: sarcoidosis, hyperpyrexia, Behçets disease, immunosuppression in organ transplantation.

Prednisolone is used for the treatment of steroid-responsive inflammation of the palpebral and bulbar conjunctiva, cornea and anterior segment of the globe.

Elzhina is also used to associated treatment for these conditions: Allergy Skin, Balanitis candida, Dermatitis, Fungal infectious disorders of the Beard, Fungal skin infection, Herpes Zoster, Intertrigo, Mycotic Eczema, Pityriasis versicolor, Ringworm, Skin candida, Tinea Corporis, Tinea Cruris, Tinea Pedis, Tinea pedis of the interdigital, Vulvovaginal mycotic infection, Cutaneous candidiasis, Cutaneous dermatophyte infectionAcne pustular, Allergic Contact Dermatitis, Allergy Skin, Atopic Dermatitis (AD), Atopic Dermatitis (AD) of the external ear canal, Bacterial diarrhoea, Burns, Carbuncle, Cradle Cap, Dermatitis, Dermatitis, Contact, Dermatitis, Eczematous, Diarrhoea, Discoid Lupus Erythematosus (DLE), Ear infection bacterial, Ear infection bacterial caused by susceptible bacteria, Gastrointestinal Infections, Hepatic coma, Hidradenitis Suppurativa (HS), Hot Water Burns (Scalds), Impetigo, Impetigo contagious, Infantile Eczema, Infected Wounds, Infected skin ulcer, Infection of the outer ear caused by susceptible bacteria, Infectious diarrhea, Inflammatory Reaction caused by Acne, Intertrigo, Itching caused by Infection, Lichen Planus (LP), Localized Infection caused by susceptible bacteria, Nail infection, Neurodermatitis, Otitis Externa, Postoperative Wound Infection, Psoriasis Vulgaris (Plaque Psoriasis), Pustular Dermatosis, Radiodermatitis, Secondarily Infected Eczema, Secondary Bacterial Infection, Skin Burns, Skin Infections, Skin Infections, Bacterial, Skin Irritation, Skin Ulcer, Solar erythema, Abrasions, Blistering caused by Staphylococcus, Erythematous eruptions, Intertriginous erythema of the anogenital, Ocular bacterial infections caused by susceptible bacteria, Resistant to other corticosteroids Dermatosis, Susceptible Bacterial InfectionsAmebiasis, Anaerobic Bacterial Infection, Chlamydial Infections, Gastrointestinal Infections caused by entamoeba histolytica, Giardiasis, Mixed Vaginal Infections, Surgical Site Infections, Trichomonal Vaginitis, TrichomoniasisInflammation, Inflammatory Conditions, Ocular Infections, Irritations and Inflammations, Ocular Inflammation, Organ Transplant Rejection

How Elzhina works

Econazole interacts with 14-α demethylase, a cytochrome P-450 enzyme necessary to convert lanosterol to ergosterol. As ergosterol is an essential component of the fungal cell membrane, inhibition of its synthesis results in increased cellular permeability causing leakage of cellular contents. Econazole may also inhibit endogenous respiration, interact with membrane phospholipids, inhibit the transformation of yeasts to mycelial forms, inhibit purine uptake, and impair triglyceride and/or phospholipid biosynthesis.

Like other aminoglycoside antibiotic drugs, neomycin inhibits bacterial ribosomes by binding to the 30S ribosomal subunit of susceptible bacteria and disrupting the translational machinery of bacterial protein synthesis. Bacterial translation is normally initiated by the mRNA binding to the 30S ribosomal subunit and subsequent binding with 50S subunit for elongation.

The short term effects of corticosteroids are decreased vasodilation and permeability of capillaries, as well as decreased leukocyte migration to sites of inflammation. Corticosteroids binding to the glucocorticoid receptor mediates changes in gene expression that lead to multiple downstream effects over hours to days.

Glucocorticoids inhibit neutrophil apoptosis and demargination; they inhibit phospholipase A2, which decreases the formation of arachidonic acid derivatives; they inhibit NF-Kappa B and other inflammatory transcription factors; they promote anti-inflammatory genes like interleukin-10.

Lower doses of corticosteroids provide an anti-inflammatory effect, while higher doses are immunosuppressive. High doses of glucocorticoids for an extended period bind to the mineralocorticoid receptor, raising sodium levels and decreasing potassium levels.

Dosage

Elzhina dosage

Econazole Cream is applied to the affected skin areas once or twice daily, in the morning and/or in the evening and gently rubbed in with the clean finger.

For mycoses of the hands, application is recommended following each washing of the hands. For the treatment of onychomycosis, occlusive dressings are recommended.

Econazole-G Cream is applied with the applicator par vaginally once or twice daily.

Econazole VT is applied with the applicator par vaginally one tablet once or twice daily.

In order to prevent relapse, treatment should be continued for 2 weeks after clinical cure.

Amoebiasis:

• Adults: 500 mg twice a day for 5 days.
• Children: 10-25 mg per kg body weight in two divided doses.

Amoebic dysentery:

• Adults: 1.5 gm once a day for 3 days.
• Children: 40 mg per kg body weight, once a day for 3 days.

Giardiasis:

• Adults: 1.5 gm once daily for 1-2 days.
• Children: 40 mg per kg body weight for 2 days.

Trichomoniasis: 1.5 gm once or 500 mg twice a day for 5 days. Sexual partner should also be treated at the same time.

Bacterial vaginosis: 3 tablets of 500 mg each as a single dose or one tablet of 500 mg once daily for 5-7 days.

The initial dosage of Prednisolone may vary from 5 mg to 60 mg daily depending on the disorder being treated. Divided daily dosage is usually used.

The appropriate individual dose must be determined by trial and error and must be re-evaluated regularly according to activity of the disease.

In general, initial dosage shall be maintained or adjusted until the anticipated response is observed. The dose should be gradually reduced until the lowest dose, which will maintain an adequate clinical response is reached.

During prolonged therapy, dosage may need to be temporarily increased during periods of stress or during exacerbations of the disease. When the drug is to be stopped, it must be withdrawn gradually and not abruptly.

Intermittent dosage regimen: A single dose of Prednisolone in the morning on alternate days or at longer intervals is acceptable therapy for some patients. When this regimen is practical, the degree of pituitary-adrenal suppression can be minimized.

Use in children: Corticosteroids cause growth retardation in infancy, childhood and adolescence, which may be irreversible. Treatment should be administered where possible as a single dose on alternate days.

Specific dosage guidelines-

Allergic and skin disorders: initial doses of 5-15 mg daily are commonly adequate.

Collagenosis: Initial doses of 20-30 mg daily are frequently effective. Those with more severe symptoms may require higher doses.

Rheumatoid arthritis: The usual initial dose is 10-15 mg daily. The lowest daily maintenance dose compatible with tolerable symptomatic relief is recommended.

Blood disorders and lymphoma: An initial daily dose of 15-60 mg is often necessary with reduction after an adequate clinical or haematological response. Higher doses may be necessary to induce remission in acute leukaemia.

Adult: Instill one drop into the conjunctival sac two to four times daily. During the initial 24 to 48 hours, the dosing frequency may be increased if necessary. Care should be taken not to discontinue the therapy before completing the course.

Paediatri: Safety and effectiveness in pediatric patients have not been established.

Side Effects

Rarely, transient local mild irritation, itching & redness may occur immediately after application. Econazole has minimal allergic effect. It is well tolerated, even by delicate skin. Local irritations are not likely to occur, except in rare cases, e.g., in eczematous skin areas. In such cases, anti-eczematous treatment is recommended for several days before therapy with Econazole is initiated.

Side effects of Ornidazole have been mainly limited to the gastrointestinal tract (nausea, vomiting, epigastric pain) and central nervous system (dizziness, headache, lassitude). Unlike other nitroimidazoles, Ornidazole does not interact with alcohol, although this requires further study.

Leukopenia has been described occasionally during therapy. Adverse central nervous system (CNS) effects of Ornidazole have mainly included headache, dizziness, lassitude or somnolence, fatigue and weakness. Adverse CNS effects of Ornidazole may be less than that happens with metronidazole. Seizures have not been reported with Ornidazole in studies available to date.

Elevation of intraocular pressure (IOP) with possible development of glaucoma and infrequent optic nerve damage, posterior subcapsular cataract formation and delayed wound healing. Fungal and viral infections of the cornea are particularly may develop coincidentally with long-term applications of steroid.

General side-effects include leucocytosis, hypersensitivity including anaphylaxis, thromboembolism, nausea, and malaise.

Toxicity

Overdosage of econazole in humans has not been reported to date. In mice, rats guinea pigs and dogs, the oral LD 50 values were found to be 462, 668, 272, and > 160 mg/kg, respectively.

The oral LD₅₀ of neomycin sulfate in mouse is > 8 g/kg. The subcutaneous LD₅₀ is 200 mg/kg in rat and 190 mg/kg in mouse. The intraperitoneal LD₅₀ in mouse is 305 mg/kg. The oral Lowest published toxic dose (TDLo) in woman is 12600 mg/kg/7D.

Because of low absorption, acute overdosage from oral neomycin is not likely to occur. However, prolonged administration of neomycin should be avoided because of the possibility of some systemic absorption and the risk of neurotoxicity, ototoxicity, and/or nephrotoxicity. Hemodialysis will remove neomycin from the blood. While nephrotoxicity and ototoxicity have been reported in otherwise patients without compromised renal function, the risk for developing these toxicities is increased in patients with renal impairment. Like other aminoglycosides, neomycin may cause fetal harm and total irreversible bilateral congenital deafness when administered in pregnant women.

The oral LD₅₀ of prednisolone acetate in mice is 1680 mg/kg. Patients experiencing an overdose of oral prednisolone acetate may experience an increased severity in the adverse effects of corticosteroids. Overdose of oral prednisolone acetate may be treated by gastric lavage or inducing vomiting if the overdose was recent, as well as supportive and symptomatic therapy. Chronic overdosage may be treated by dose reduction or treating patients on alternate days. An overdose by the ophthalmic route is not expected to cause problems.

Precaution

Hypersensitivity has rarely been recorded. If something like this occur, administration of the product should be discontinued. The infected area should be kept clean and dry during treatment.

In patient with ataxia, vertigo, and mental confusion, Ornidazole should be prescribed with caution. During prolonged treatment with Ornidazole, blood dyscrasia namely mild leukopenia have been reported rarely. In case leukopenia occurs, the decision to discontinue the therapy should depend upon the gravity of infection.

Shake the bottle well before use. Prolonged use of corticosteroids may result in damage to the optic nerve and defects in vision. If this product is used for longer period of time, intraocular pressure should be routinely monitored.

Caution is necessary when oral corticosteroids, including Prednisolone, are prescribed in patients with the following conditions like-Tuberculosis, Hypertension, Congestive heart failure, Liver failure, Renal insufficiency, Diabetes mellitus or in those with a family history of diabetes, Osteoporosis, Patients with a history of severe affective disorders and particularly those with a previous history of steroid-induced psychoses, Epilepsy, Peptic ulceration, Previous Steroid Myopathy.

Undesirable effects may be minimized by using the lowest effective dose for the minimum period and by administering the daily requirement as a single morning dose on alternate days. Frequent patient review is required to titrate the dose appropriately against disease activity.

Interaction

Although not studied, based on the chemical similarity of enconazole with other imidazole compounds, a theoretical potential for competitive interaction with compounds metabolized by CYP3A4/2C9 exists. Due to the limited systemic availability after vaginal application (see Pharmacokinetics under Actions), clinically relevant interactions are unlikely to occur, in patients on oral anticoagulants eg, warfarin and acenocoumarol, caution should be exercised and monitoring of the anticoagulant effect should be considered.

Like other imidazoles, Ornidazole has a mild potential to cause disulfiramlike reactions. Concomitant administration of oral anticoagulants may increase the risk of haemorrhage due to diminished hepatic metabolism. Ornidazole has been reported to decrease the clearance of 5-fluorouracil.

Hepatic microsomal enzyme inducers: Drugs which can cause liver enzyme induction such as phenobarbitone, phenytoin, rifampicin, rifabutin, carbamazepine, primidone and aminoglutethimide may reduce the therapeutic efficacy of corticosteroids by increasing the rate of metabolism.

Non-steroidal anti-inflammatory drugs: Concomitant administration of ulcerogenic drugs such as indomethacin during corticosteroid therapy may increase the risk of Gl ulceration.

Anticoagulants: Response to anticoagulants may be reduced or, less often, enhanced by corticosteroids.

Vaccines: Live vaccines should not be given to individuals with impaired immune responsiveness. The antibody response to other vaccines may be diminished.

Oestrogens: Oestrogens may potentiate the effects of glucocorticoids and dosage adjustment may be required if oestrogens are added to or withdrawn from a stable dosage regimen.

Other: The desired effects of hypoglycaemic agents (including insulin), anti-hypertensives and diuretics are antagonised by corticosteroids and the hypokalaemic effect of acetazolamide, loop diuretics, thiazide diuretics and carbenoxolone are enhanced.

Volume of Distribution

The small fraction of absorbed neomycin is rapidly distributed in the tissues. The amount of systemically absorbed neomycin is reported to increase cumulatively with each repeated dose administered until a steady state is reached.

The volume of distribution of the active metabolite, prednisolone, is 0.22/0.7L/kg.

Elimination Route

After topical application to the skin of normal subjects, systemic absorption of econazole nitrate is extremely low. Although most of the applied drug remains on the skin surface, drug concentrations were found in the stratum corneum which, by far, exceeded the minimum inhibitory concentration for dermatophytes.

Neomycin is poorly absorbed from the gastrointestinal tract. Gastrointestinal absorption of the drug may be increased if inflammatory or ulcerative gastrointestinal disease is present.

Prednisolone acetate oral suspension given at a dose equivalent to 15mg prednisolone has a C_max of 321.1ng/hr, a T_maxof 1-2 hours, and an AUC of 1999.4ng*hr/mL. The absorption pharmacokinetics of prednisolone acetate are not significantly different from a comparable dose of prednisolone.

Half Life

There is limited information on the half-life of neomycin.

Oral prednisolone acetate has a plasma half life of 2-3 hours.

Clearance

There is limited information on the clearance rate of neomycin.

Data regarding the clearance of prednisolone acetate is not readily available.

Elimination Route

The small absorbed fraction of neomycin is excreted by the kidney. The unabsorbed portion of the drug is excreted unchanged in the feces.

Prednisolone acetate is predominantly excreted in the urine.

Pregnancy & Breastfeeding use

During pregnancy: There is no information of any abnormality or adverse event in neonates while Econazole Cream / VT had been used during pregnancy.

During lactation: As the systemic absorption of Econazole Nitrate cream is extremely low after topical/vaginal use, excretion in breast milk is likely to be negligible. So, it can be used topically/vaginally during lactation if needed.

Adequate clinical trials have not been conducted. Ornidazole should be prescribed only if the potential benefit justifies the potential risk to fetus/neonate.

Pregnancy: Prednisolone Acetate is pregnancy category C. So, this drug should be used during pregnancy only if clearly needed.

Lactation: Corticosteroids are excreted in small amounts in breast milk and infants of mothers taking pharmacological doses of steroids should be monitored carefully for signs of adrenal suppression.

Contraindication

Hypersensitivity to any component of Econazole.

Previous hypersensitivity to Ornidazole and to other nitroimidazoles. Ornidazole is contraindicated in central nervous system disorders, particularly in epilepsy or in peripheral neuropathy.

Prednisolone (Eye drops) is contraindicated in viral diseases of the cornea, conjunctiva and known hypersensitivity to any of the ingredients of Prednisolone (Eye drops) or other corticosteroids.

Systemic infections unless specific anti-infective therapy is employed. Hypersensitivity to any ingredient. Ocular herpes simplex because of possible perforation.

Special Warning

Use in the elderly: Treatment of elderly patients, particularly if long term, should be planned bearing in mind the more serious consequences of the common side effects of corticosteroids in old age, especially osteoporosis, diabetes, hypertension, hypokalemia, susceptibility to infection and thinning of the skin. Close clinical supervision is required to avoid life-threatening reactions.

May need to increase dose in patients with hyperthyroidism to achieve therapeutic effects.

Acute Overdose

Econazole Cream / VT is intended for topical and vaginal use. If accidental ingestion of large quantities of the product occurs, an appropriate method of gastric emptying may be used if considered desirable.

Renal Impairment Haemodialysis patients: Give a supplemental dose (50% of the usual dose) before dialysis.

Hepatic Impairment Severe: Double the interval between doses.

A one-time accidental overdose of Prednisolone Ophthalmic Suspension generally will not cause acute problems. Long time overdose may show general side-effects. In accidental overdose sufficient water should be taken to dilute the medication.

Report of acute toxicity and/or death following overdose of glucocorticoids are rare. No specific antidote is available; treatment is supportive and symptomatic. Serum electrolytes should be monitored.

Storage Condition

Store at room temperature and protect from light and moisture.

Store in a cool, dry place and protect from light. Keep out of the reach of children. Protect from freezing. Shake well before using.

Innovators Monograph

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