Dexacort (Drops) Instructions for Use

Marketing Authorization Holder

Daru Pahsh Pharmaceutical Mfg. The Company (Iran)

ATC Code

S01BA01 (Dexamethasone)

Active Substance

Dexamethasone (Rec.INN registered by WHO)

Dosage Form

Dexacort

Eye and ear drops 0.1%: dropper bottle 5 ml

Dosage Form, Packaging, and Composition

5 ml – polyethylene dropper bottles (1) – cardboard packs.

Clinical-Pharmacological Group

Topical corticosteroids for ophthalmology

Pharmacotherapeutic Group

Topical glucocorticosteroid

Pharmacological Action

Corticosteroid. Suppresses the functions of leukocytes and tissue macrophages. Limits the migration of leukocytes to the area of inflammation. Impairs the ability of macrophages to phagocytose and to form interleukin-1. Promotes stabilization of lysosomal membranes, thereby reducing the concentration of proteolytic enzymes in the area of inflammation. Reduces capillary permeability caused by the release of histamine. Suppresses fibroblast activity and collagen formation.

Inhibits the activity of phospholipase A₂, leading to suppression of the synthesis of prostaglandins and leukotrienes. Suppresses the release of COX (mainly COX-2), which also contributes to a reduction in prostaglandin production.

Reduces the number of circulating lymphocytes (T- and B-cells), monocytes, eosinophils, and basophils due to their movement from the vascular bed into the lymphoid tissue; suppresses antibody formation.

Dexamethasone suppresses the release of ACTH and β-lipotropin by the pituitary gland but does not reduce the level of circulating β-endorphin. Inhibits the secretion of TSH and FSH.

When applied directly to blood vessels, it has a vasoconstrictor effect.

Dexamethasone has a pronounced dose-dependent effect on the metabolism of carbohydrates, proteins, and fats. Stimulates gluconeogenesis, promotes the uptake of amino acids by the liver and kidneys, and increases the activity of gluconeogenesis enzymes. In the liver, Dexamethasone enhances glycogen storage by stimulating the activity of glycogen synthase and the synthesis of glucose from protein metabolism products. The increase in blood glucose levels stimulates insulin secretion.

Dexamethasone suppresses glucose uptake by fat cells, which leads to activation of lipolysis. However, due to increased insulin secretion, lipogenesis is stimulated, leading to fat accumulation.

It has a catabolic effect in lymphoid and connective tissue, muscles, adipose tissue, skin, and bone tissue. Osteoporosis and Cushing’s syndrome are the main factors limiting long-term corticosteroid therapy. As a result of the catabolic effect, growth suppression in children is possible.

In high doses, Dexamethasone may increase the excitability of brain tissue and contribute to a lowering of the seizure threshold. Stimulates excessive production of hydrochloric acid and pepsin in the stomach, which contributes to the development of peptic ulcer.

When used systemically, the therapeutic activity of dexamethasone is due to its anti-inflammatory, anti-allergic, immunosuppressive, and anti-proliferative effects.

When used externally and locally, the therapeutic activity of dexamethasone is due to its anti-inflammatory, anti-allergic, and anti-exudative (due to the vasoconstrictor effect) effects.

Its anti-inflammatory activity is 30 times greater than that of hydrocortisone and it does not possess mineralocorticoid activity.

Pharmacokinetics

Plasma protein binding is 60-70%. Penetrates through histohematic barriers. A small amount is excreted in breast milk.

Metabolized in the liver.

T_1/2 is 2-3 hours. Excreted by the kidneys.

When applied topically in ophthalmology, it is absorbed through the cornea with intact epithelium into the aqueous humor of the anterior chamber of the eye. In case of inflammation of the eye tissues or damage to the mucous membrane and cornea, the absorption rate of dexamethasone significantly increases.

Indications

For oral administration Addison-Biermer disease; acute and subacute thyroiditis, hypothyroidism, progressive ophthalmopathy associated with thyrotoxicosis; bronchial asthma; rheumatoid arthritis in the acute phase; ulcerative colitis; connective tissue diseases; autoimmune hemolytic anemias, thrombocytopenia, aplasia and hypoplasia of hematopoiesis, agranulocytosis, serum sickness; acute erythroderma, pemphigus (vulgaris), acute eczema (at the beginning of treatment); malignant tumors (as palliative therapy); congenital adrenogenital syndrome; cerebral edema (usually after preliminary parenteral administration of corticosteroids).

For parenteral administration shock of various origins; cerebral edema (in brain tumor, traumatic brain injury, neurosurgical intervention, cerebral hemorrhage, encephalitis, meningitis, radiation injury); status asthmaticus; severe allergic reactions (angioedema, bronchospasm, dermatosis, acute anaphylactic reaction to drugs, serum transfusion, pyrogenic reactions); acute hemolytic anemias, thrombocytopenia, acute lymphoblastic leukemia, agranulocytosis; severe infectious diseases (in combination with antibiotics); acute adrenal cortex insufficiency; acute croup; joint diseases (scapulohumeral periarthritis, epicondylitis, styloiditis, bursitis, tenosynovitis, compression neuropathy, osteochondrosis, arthritis of various etiologies, osteoarthritis).

For use in ophthalmological practice non-purulent and allergic conjunctivitis, keratitis, keratoconjunctivitis without epithelial damage, iritis, iridocyclitis, blepharoconjunctivitis, blepharitis, episcleritis, scleritis, inflammatory process after eye injuries and surgical interventions, sympathetic ophthalmia; macular edema due to occlusion of the central retinal vein or its branches, visual impairment due to diabetic macular edema in patients with aphakia, in patients with an insufficient response to therapy, or those for whom therapy with drugs other than corticosteroids is not suitable, inflammation of the posterior segment of the uvea, representing non-infectious uveitis.

For topical use in ENT practice (as part of combination drugs) external otitis without damage to the tympanic membrane, infected eczema of the external auditory canal; inflammatory and infectious diseases of the nasal cavity, pharynx, paranasal sinuses.

ICD codes

Dosage Regimen

Individual. Orally, for severe diseases at the beginning of treatment, up to 10-15 mg/day is prescribed; the maintenance dose may be 2-4.5 mg or more per day. The daily dose is divided into 2-3 doses. In small doses, it is taken once a day in the morning.

For parenteral use, it is administered intravenously slowly by bolus or drip (in acute and emergency conditions); intramuscularly; periarticular and intra-articular administration is also possible. From 4 to 20 mg of dexamethasone can be administered 3-4 times within 24 hours. The duration of parenteral use is usually 3-4 days, after which maintenance therapy with the oral form is started. In the acute period of various diseases and at the beginning of treatment, Dexamethasone is used in higher doses. Upon achieving the effect, the dose is reduced at intervals of several days until the maintenance dose is reached or until treatment is discontinued.

In ophthalmology, the method of use depends on the dosage form used. The treatment regimen depends on the indications for use.

In ENT practice, it is used topically in accordance with the recommended dosing regimen of the drug used.

Adverse Reactions

From the endocrine system decreased glucose tolerance, steroid diabetes mellitus or manifestation of latent diabetes mellitus, suppression of adrenal function, Cushing’s syndrome (including moon face, pituitary-type obesity, hirsutism, increased blood pressure, dysmenorrhea, amenorrhea, myasthenia, striae), delayed sexual development in children.

From the metabolism increased excretion of calcium ions, hypocalcemia, weight gain, negative nitrogen balance (increased protein breakdown), increased sweating, hypernatremia, hypokalemia.

From the central nervous system delirium, disorientation, euphoria, hallucinations, manic-depressive psychosis, depression, paranoia, increased intracranial pressure, nervousness or anxiety, insomnia, dizziness, vertigo, pseudotumor cerebelli, headache, convulsions.

From the cardiovascular system arrhythmias, bradycardia (up to cardiac arrest); development (in predisposed patients) or increased severity of chronic heart failure, ECG changes characteristic of hypokalemia, increased blood pressure, hypercoagulation, thrombosis. In patients with acute and subacute myocardial infarction – spread of the necrosis focus, slowing of scar tissue formation, which can lead to rupture of the heart muscle; with intracranial administration – nosebleed.

From the digestive system nausea, vomiting, pancreatitis, steroid ulcer of the stomach and duodenum, erosive esophagitis, gastrointestinal bleeding and perforation, increase or decrease in appetite, flatulence, hiccups; rarely – increased activity of hepatic transaminases and alkaline phosphatase.

From the sensory organs posterior subcapsular cataract, increased intraocular pressure with possible damage to the optic nerve, tendency to develop secondary bacterial, fungal or viral eye infections, trophic changes in the cornea, exophthalmos.

From the musculoskeletal system slowing of growth and ossification processes in children (premature closure of epiphyseal growth zones), osteoporosis (very rarely – pathological bone fractures, aseptic necrosis of the humeral and femoral head), muscle tendon rupture, steroid myopathy, decrease in muscle mass (atrophy).

Dermatological reactions delayed wound healing, petechiae, ecchymoses, thinning of the skin, hyper- or hypopigmentation, steroid acne, striae, tendency to develop pyoderma and candidiasis.

Allergic reactions generalized (including skin rash, skin itching, anaphylactic shock) and with topical application.

Effects associated with immunosuppressive action : development or exacerbation of infections (concomitant use of immunosuppressants and vaccination contribute to the appearance of this side effect).

Local reactions with parenteral administration – tissue necrosis.

With topical application rarely – itching, hyperemia, burning, dryness, folliculitis, acne, hypopigmentation, perioral dermatitis, allergic dermatitis, skin maceration, secondary infection, skin atrophy, striae, miliaria. With prolonged use or application to large areas of the skin, the development of systemic side effects characteristic of corticosteroids is possible.

Contraindications

For short-term use for vital indications – hypersensitivity to dexamethasone.

For intra-articular administration and administration directly into the lesion site previous arthroplasty, pathological bleeding (endogenous or caused by the use of anticoagulants), intra-articular bone fracture, infectious (septic) inflammatory process in the joint and periarticular infections (including in the anamnesis), as well as general infectious disease, severe periarticular osteoporosis, absence of signs of inflammation in the joint (“dry” joint, for example, in osteoarthritis without synovitis), severe bone destruction and joint deformity (sharp narrowing of the joint space, ankylosis), joint instability as an outcome of arthritis, aseptic necrosis of the epiphyses of the bones forming the joint.

For topical application bacterial, viral, fungal skin diseases, skin tuberculosis, skin manifestations of syphilis, skin tumors, post-vaccination period, violation of the integrity of the skin (ulcers, wounds), children’s age (up to 2 years, for itching in the anal area – up to 12 years), rosacea, acne vulgaris, perioral dermatitis.

For use in ophthalmology bacterial, viral, fungal eye diseases, tuberculous eye lesions, violation of the integrity of the ocular epithelium, acute form of purulent eye infection in the absence of specific therapy, corneal diseases combined with epithelial defects, trachoma, glaucoma with decompensated increase in intraocular pressure, not controlled by medications, aphakia with rupture of the posterior lens capsule; age under 18 years (for some dosage forms).

Use in Pregnancy and Lactation

During pregnancy (especially in the first trimester), as well as during lactation, Dexamethasone is used taking into account the expected therapeutic effect and the negative impact on the fetus. With long-term therapy during pregnancy, the possibility of fetal growth disorders cannot be excluded. In case of use at the end of pregnancy, there is a risk of atrophy of the adrenal cortex in the fetus, which may require replacement therapy in the newborn.

Use in Hepatic Impairment

Should be used with caution in severe chronic liver failure.

Use in Renal Impairment

Should be used with caution in severe chronic renal failure.

Pediatric Use

Contraindications for topical application children under 2 years of age, for itching in the anal area – under 12 years of age.

For use in ophthalmology children and adolescents under 18 years of age for some dosage forms.

Geriatric Use

When used in ophthalmology, dose adjustment is not required.

Special Precautions

Should be used with caution in parasitic and infectious diseases of viral, fungal or bacterial nature (current or recently suffered, including recent contact with a patient) – herpes simplex, herpes zoster (viremic phase), chickenpox, measles, amoebiasis, strongyloidiasis (established or suspected), systemic mycosis; active and latent tuberculosis. Use in severe infectious diseases is permissible only against the background of specific therapy.

Should be used with caution within 8 weeks before and 2 weeks after vaccination, with lymphadenitis after BCG vaccination, with immunodeficiency states (including AIDS or HIV infection).

Should be used with caution in gastrointestinal diseases: gastric and duodenal ulcer, esophagitis, gastritis, acute or latent peptic ulcer, recently created intestinal anastomosis, ulcerative colitis with threat of perforation or abscess formation, diverticulitis.

Should be used with caution in diseases of the cardiovascular system, including after a recent myocardial infarction (in patients with acute and subacute myocardial infarction, spread of the necrosis focus, slowing of scar tissue formation and, as a result, rupture of the heart muscle may occur), with decompensated chronic heart failure, arterial hypertension, hyperlipidemia), with endocrine diseases – diabetes mellitus (including impaired carbohydrate tolerance), thyrotoxicosis, hypothyroidism, Itsenko-Cushing’s disease, with severe chronic renal and/or hepatic failure, nephrourolithiasis, with hypoalbuminemia and conditions predisposing to its occurrence, with systemic osteoporosis, myasthenia gravis, acute psychosis, obesity (III-IV degree), with poliomyelitis (except for the form of bulbar encephalitis), open-angle and closed-angle glaucoma.

If intra-articular administration is necessary, it should be used with caution in patients with a general severe condition, ineffectiveness (or short duration) of the action of 2 previous administrations (taking into account the individual properties of the corticosteroids used).

Before starting and during corticosteroid therapy, it is necessary to monitor the complete blood count, blood glucose level and plasma electrolyte content.

In case of intercurrent infections, septic conditions and tuberculosis, simultaneous antibiotic therapy is necessary.

Dexamethasone-induced relative adrenal insufficiency may persist for several months after its discontinuation. Taking this into account, during stressful situations that arise during this period, hormone therapy is resumed with the simultaneous administration of salts and/or mineralocorticoids.

When using dexamethasone in patients with corneal herpes, the possibility of its perforation should be kept in mind. During treatment, intraocular pressure and the condition of the cornea should be monitored.

With sudden withdrawal of dexamethasone, especially in case of prior use in high doses, a so-called withdrawal syndrome (not due to hypocorticism) occurs, manifested by anorexia, nausea, lethargy, generalized musculoskeletal pain, and general weakness. After discontinuation of dexamethasone, relative adrenal cortex insufficiency may persist for several months. If stressful situations arise during this period, corticosteroids are prescribed (according to indications) for the duration, if necessary in combination with mineralocorticoids.

During treatment, control of blood pressure, water-electrolyte balance, peripheral blood picture and blood glucose level is required, as well as observation by an ophthalmologist.

In children during long-term treatment, careful monitoring of the dynamics of growth and development is necessary. Children who were in contact with patients with measles or chickenpox during the treatment period are prophylactically prescribed specific immunoglobulins.

Drug Interactions

With simultaneous use with antipsychotic agents, bucarban, azathioprine, there is a risk of developing cataracts; with agents that have an anticholinergic effect – risk of developing glaucoma.

With simultaneous use with dexamethasone, the effectiveness of insulin and oral hypoglycemic drugs is reduced.

With simultaneous use with hormonal contraceptives, androgens, estrogens, anabolic steroids, hirsutism and acne are possible.

With simultaneous use with diuretics, increased potassium excretion is possible; with NSAIDs (including acetylsalicylic acid) – the frequency of erosive and ulcerative lesions and bleeding from the gastrointestinal tract increases.

With simultaneous use with oral anticoagulants, a weakening of the anticoagulant effect is possible.

With simultaneous use with cardiac glycosides, tolerance to cardiac glycosides may worsen due to potassium deficiency.

With simultaneous use with aminoglutethimide, a decrease or suppression of the effects of dexamethasone is possible; with carbamazepine – a decrease in the action of dexamethasone is possible; with ephedrine – increased excretion of dexamethasone from the body; with imatinib – a decrease in the concentration of imatinib in blood plasma is possible due to induction of its metabolism and increased excretion from the body.

With simultaneous use with itraconazole, the effects of dexamethasone are enhanced; with methotrexate – increased hepatotoxicity is possible; with praziquantel – a decrease in the concentration of praziquantel in the blood is possible.

With simultaneous use with rifampicin, phenytoin, barbiturates, a weakening of the effects of dexamethasone is possible due to increased excretion from the body.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.