diprofos inj.

Uses

Indicated in atopic, infantile & discoid eczema; prurigo nodularis; Psoriasis (excluding widespread plague psoriasis); lichen simplex or planus; contact sensitivity reactions; seborrhoeic dermatitis; discoid lupus erythematosus & adjunct to systemic steroid therapy in generalized erythroderma.

Short-term treatment of steroid responsive in inflammatory conditions of the eye after clinical exclusion of bacterial, viral or fungal infections. Non-infected inflammatory conditions of the ear or nose.

diprofos inj. is also used to associated treatment for these conditions: Acute Gouty Arthritis, Adrenal cortical hypofunctions, Alopecia Areata (AA), Ankylosing Spondylitis (AS), Berylliosis, Blepharitis allergic, Blepharoconjunctivitis, Bullous dermatitis herpetiformis, Bursitis, Congenital Adrenal Hyperplasia (CAH), Congenital Hypoplastic Anemia, Conjunctivitis, Corneal Inflammation, Dermatitis, Eczematous, Dermatomyositis, Dermatosis, Discoid Lupus Erythematosus (DLE), Edema of the cerebrum, Epicondylitis, Episcleritis, External ear inflammation, Eye allergy, Hypercalcemia of Malignancy, Inflammatory Reaction of the ear, Iridocyclitis, Iritis, Itching caused by Allergies, Keloid Scars, Keratitis interstitial, Keratoconjunctivitis, Leukemias, Lichen Planus (LP), Lichen simplex chronicus, Lupus Erythematosus, Malignant Lymphomas, Multiple sclerosis exacerbation, Mycosis Fungoides (MF), Necrobiosis lipoidica diabeticorum, Nephrotic Syndrome, Ocular Inflammation, Ocular injuries, Ophthalmia, Sympathetic, Pemphigus, Plaque psoriasis of the body, Plaque psoriasis of the scalp, Polymyositis, Post-Surgical Ocular Inflammation, Pruritus, Psoriasis, Psoriasis Vulgaris (Plaque Psoriasis), Psoriatic Arthritis, Psoriatic plaque, Pulmonary Tuberculosis (TB), Pure Red Cell Aplasia, Regional Enteritis, Rheumatoid Arthritis, Rheumatoid Arthritis, Juvenile, Scleritis, Secondary thrombocytopenia, Severe Asthma, Severe Atopic Dermatitis, Skin Infections, Stevens-Johnson Syndrome, Systemic Lupus Erythematosus (SLE), Temporal Arteritis, Trichinosis, Tuberculous Meningitis, Ulcerative Colitis, Uveitis, Verrucous Lichen Planus (LP), Acquired immune hemolytic anemia, Acute nonspecific tenosynovitis, Acute rheumatic carditis, Bacterial blepharitis, Corticosteroid-responsive dermatoses, Eczematous rash, Exfoliative erythroderma, Granuloma annulare lesions, Idiopathic eosinophilic pneumonias, Non-suppurative Thyroiditis, Ocular bacterial infections, Severe Allergic rhinitis, Severe Contact dermatitis, Severe Serum sickness, Severe Transfusion Reactions, Severe drug hypersensitivity reactions, Superficial ocular infections, Symptomatic Sarcoidosis, Synovitis of osteoarthritisAcute Gouty Arthritis, Allergic Conditions, Alopecia Areata (AA), Dermatological Disease, Discoid Lupus Erythematosus (DLE), Endocrine Disorders, Epicondylitis, Gastrointestinal Diseases, Haematological disorders, Keloid Scars, Kidney Diseases, Lichen Planus (LP), Lichen simplex chronicus, Necrobiosis lipoidica diabeticorum, Neoplastic Disease, Nervous System Disorders, Ophthalmic Diseases, Psoriatic plaque, Respiratory Diseases, Rheumatism, Rheumatoid Arthritis, Acute Bursitis, Acute nonspecific tenosynovitis, Cystic tumors of aponeurosis, Cystic tumors of tendon, Localized Hypertrophic, Inflammatory, Infiltrated granuloma annulare lesions, Subacute Bursitis, Synovitis of osteoarthritis

How diprofos inj. works

Glucocorticoids inhibit neutrophil apoptosis and demargination, and inhibit NF-Kappa B and other inflammatory transcription factors. They also inhibit phospholipase A2, leading to decreased formation of arachidonic acid derivatives. In addition, glucocorticoids promote anti-inflammatory genes like interleukin-10.

Corticosteroids like betamethasone can act through nongenomic and genomic pathways. The genomic pathway is slower and occurs when glucocorticoids activate glucocorticoid receptors and initiate downstream effects that promote transcription of anti-inflammatory genes including phosphoenolpyruvate carboxykinase (PEPCK), IL-1-receptor antagonist, and tyrosine amino transferase (TAT). On the other hand, the nongenomic pathway is able to elicit a quicker response by modulating T-cell, platelet and monocyte activity through the use of existing membrane-bound receptors and second messengers.

Betamethasone phosphate is a soluble ester prodrug of betamethasone. Betamethasone is rapidly de-esterified, allowing betamethasone to act as an agonist of the glucocorticoid receptor. 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

diprofos inj. dosage

Apply sparingly to the affected area 2 to 3 times daily until an improvement occurs.

Eye: 1 or 2 drops to each affected eye every 1 or 2 hours until control is achieved, then the frequency may be reduced.
Ear: 2 or 3 drops to each affected ear every 2 or 3 hours until control is achieved, then the frequency may be reduced.
Nose: 2 or 3 drops instilled into each nostril 2 or 3 times daily.

Side Effects

Burning, itching, irritation, dryness, folliculitis, hypertrychosis acneiform eruptions, perioral dermatitis, allergic contact dermatitis, maceration of the skin, secondary infection, skin atrophy, striae and miliariamay be reported.

Hypersensitivity reactions may occur leading to irritation, burning, stinging, itching and dermatitis. Topical corticosteroid use may result in corneal ulceration, increased intraocular pressure leading to optic nerve damage, reduced visual acuity. Intensive or prolonged use of topical corticosteroids may lead to formation of posterior subcapsular cataracts. In those diseases causing thinning of the cornea or sclera, corticosteroid therapy may result in thinning of the globe leading to perforation. Mydriasis, ptosis and epithelial punctate keratitis have also been reported following ophthalmic use of corticosteroids.

Toxicity

Chronic high doses of glucocorticoids can lead to the development of cataracts, glaucoma, hypertension, water retention, hyperlipidemia, peptic ulcer, pancreatitis, myopathy, osteoporosis, mood changes, psychosis, dermal atrophy, allergy, acne, hypertrichosis, immune suppression, decreased resistance to infection, moon face, hyperglycemia, hypocalcemia, hypophosphatemia, metabolic acidosis, growth suppression, and secondary adrenal insufficiency. Overdose may be treated by adjusting the dose or stopping the corticosteroid as well as initiating symptomatic and supportive treatment.

Patients experiencing an acute overdose should be treated with symptomatic and supportive treatment. Chronic overdoses where patients require continued therapy can be treated through temporary dose reduction or alternate day treatment.

The oral, intraperitoneal, and intravenous LD₅₀ values in rats are 1877 mg/kg, 1179 mg/kg, and 1276 mg/kg, respectively.

Precaution

Avoid long-term therapy particularly in infant & children; the treated area should not be bandaged or otherwise covered or wrapped as to be occlusive unless directed by the physician. Avoid contact with eyes.

Topical corticosteroids should never be given for an undiagnosed red eye. Ophthalmic treatment with corticosteroid preparations should not be repeated or prolonged without regular review to exclude raised intraocular pressure, cataract formation or unsuspected infections.

Interaction

Increased hyperglycaemia and hypokalaemia with thiazide diuretics. Increased incidence of peptic ulcer or GI bleeding with concurrent NSAIDs admin. Response to anticoagulants altered. Dose of antidiabetics and antihypertensives needs to be increased. Decreases serum concentration of salicylates and antimuscarinic agents.

Potentially Fatal: Reduced efficacy with concurrent use of carbamazepine, phenytoin, primidone, barbiturates and rifampicin. Enhanced effect in women taking oestrogens or oral contraceptives.

Specific drug interaction studies have not been conducted.

Volume of Distribution

In a study that included Indian women of reproductive age, the volume of distribution following a single intramuscular dose of betamethasone phosphate was 94,584±23,539 mL(s).

The volume of distribution of betamethasone in an intramuscular injection of 3mg betamethasone acetate and 3mg betamethasone phosphate is 226.00 ± 61.64 L.

Elimination Route

The absorption and potency of any topical corticosteroid including betamethasone depends on the vehicle in which the steroid is delivered. For example, betamethasone dipropionate 0.05% ointment is classified as a highly potent topical steroid, while betamethasone dipropionate 0.05% cream or lotion is considered to be moderately potent.

There are several structural modifications that can determine the potency of a topical corticosteroid. For example, corticosteroids containing a halogen at specific carbons, or that contain esters are more potent due to enhanced lipophilicity. As such, there is a marked difference between topical products containing betamethasone dipropionate vs. betamethasone valerate. Betamethasone dipropionate contains 2 esters which enhances its potency, while betamethasone valerate has only one ester and is less potent.

It should be noted that the use of occlusive dressings with topical steroids significantly increases the absorption, increasing the risk for adverse effects.

An intramuscular injection of 3mg betamethasone acetate and 3mg betametasone phosphate reaches a betamethasone C_max 33.21 ± 8.71 ng/mL, with a T_max of 1.56 ± 1.32 h, and an AUC of 506.95 ± 125.03 ng*h/mL.

Half Life

In a study that included Indian women of reproductive age, the half-life following a single intramuscular dose of betamethasone phosphate was 10.2 ± 2.5 hours.

The half life of betamethasone in an intramuscular injection of 3mg betamethasone acetate and 3mg betamethasone phosphate is 12.47 ± 1.91 h.

Clearance

In a study that included Indian women of reproductive age, the CL/F following a single intramuscular dose of betamethasone phosphate was 6,466 ± 805 mL/hour.

The clearance of betamethasone in an intramuscular injection of 3mg betamethasone acetate and 3mg betamethasone phosphate is 12.62 ± 3.45 L/h.

Elimination Route

Corticosteroids are eliminated predominantly in the urine.

Corticosteroids are eliminated predominantly in the urine.

Pregnancy & Breastfeeding use

There are no adequate and well controlled studies in pregnant women on teratogenic effects from topically applied corticosteroids and should not be used extensively for a prolonged period. Caution should be excercised when topical corticosteroids are administered in nursing women.

There are no adequate and well controlled studies for pregnant woman. It should not be used extensively in pregnant woman. There is no information available whether it is secreted in the milk or not.

Contraindication

Betamethasone is contraindicated in patients with a history of hypersensitivity to any of the components of the preparation. Betamethasone Eye/Ear/Nasal Drops is contraindicated in Herpes simplex virus infection of the eye; known sensitivity or allergy to any ingredient; red eye due to unknown causes; viral or fungal infections in the treatment area; tuberculosis, glaucoma etc.

Acute Overdose

Long-term intensive topical use may lead to systemic effects

Long-term intensive topical use may lead to systemic effects.

Storage Condition

Protect from light. Do not freeze. Store between 15 °C and 30 °C.

This should be protected from light, store below 25°C. Keep out of reach of children. Do not use more than 4 weeks after opening.

Innovators Monograph

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