Betol Ointment 0.05%+0.005%

Uses

Ointment is used for the topical treatment of plaque-type psoriasis vulgaris amenable to topical therapy. Topical Suspension is used for the topical treatment of plaque psoriasis of the scalp and body.

Betol Ointment 0.05%+0.005% 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 osteoarthritisPlaque psoriasis of the scalp, Psoriasis Vulgaris (Plaque Psoriasis)

How Betol Ointment 0.05%+0.005% 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.

The precise mechanism of calcipotriol in remitting psoriasis is not well-understood, however, it has been shown to have comparable affinity with calcitriol for the Vitamin D receptor while being less than 1% the activity in regulating calcium metabolism. The Vitamin D receptor (VDR) belongs to the steroid/thyroid receptor superfamily, and is found on the cells of many different tissues including the thyroid, bone, kindney, and T cells of the immune system. T cells are known to play a role in psoriasis and are believed to undergo modulation of gene expression with binding of calcipotriol to the VDR. This modulation is thought to affect gene products related to cell differentiation and proliferation.

Dosage

Betol Ointment 0.05%+0.005% dosage

Ointment: This Ointment is indicated for topical use only. The phototoxic effects have not been studied in psoriasis patients. All psoriasis-affected areas treated with this Ointment should be, where possible, protected from direct sunlight and UV-light with items of clothing.

• Adults: This ointment should be applied topically to the affected area once daily. The maximum daily dose should not exceed 15 gm. The maximum recommended weekly dose of ointment is 100 gm/week. The treated area should not be more than 30% of the body surface. The use of this ointment should be intermittent for up to one year under close medical supervision. Treatment should be limited to four week periods with Calcipotriol used alone for one month between periods of use of this ointment as needed.
• Children: This ointment is not recommended for use in children and adolescents below the age of 18 years.

Topical Suspension: Apply required quantity of spray of Topical Suspension once daily to the affected areas and gently rub in using the tips of the fingers. Treatment may be continued for up to 8 weeks. Treatment may be discontinued earlier, if symptoms arecleared. The maximum weekly dose should not exceed 100 gm. Shake before use. This Topical Suspension is not for oral, ophthalmic or intravaginal use.

Side Effects

Itching, burning, redness, or irritation of the skin may occur.

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.

Topically applied calcipotriene can be absorbed in sufficient amounts to produce systemic effects. Elevated serum calcium has been observed with excessive use of calcipotriene.

Precaution

Hypercalcemia and hypercalciuria have been reported. If either occurs, discontinue until parameters of calcium metabolism normalize. Topical corticosteroids can produce reversible hypothalamic-pituitary-adrenal (HPA) axis suppression, Cushing’s syndrome and unmask latent diabetes. Rate of adrenal suppression increased with treatment duration. Systemic absorption may require evaluation for HPA axis suppression. Modify use if HPA axis suppression develops. Potent corticosteroids, use on large areas, prolonged use or occlusive use may increase systemic absorption. Local adverse reactions may include atrophy, striae, irritation, acne form eruptions, hypopigmentation, and allergic contact dermatitis and may be more likely with occlusive use or more potent corticosteroids. Use is not recommended on face, axillae, groin or where atrophy is present. Children may be more susceptible to systemic toxicity when treated with topical corticosteroids.

Interaction

Additive adverse effects when used with other steroids.

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).

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.

Clinical studies with radiolabeled ointment indicate that approximately 6% (+3%, SD) of the applied dose of calcipotriene is absorbed systemically when the ointment is applied topically to psoriasis plaques or 5% (+2.6%, SO) when applied to normal skin.

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.

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.

Elimination Route

Corticosteroids are eliminated predominantly in the urine.

The active form of the vitamin, 1,25-dihydroxy vitamin D3 (calcitriol), is known to be recycled via the liver and excreted in the bile. There is evidence that maternal 1,25-dihydroxy vitamin D3 (calcitriol) may enter the fetal circulation, but it is not known whether it is excreted in human milk.

Pregnancy & Breastfeeding use

There are no adequate and well-controlled studies in pregnant women. Ointment or suspension should be used during pregnancy only if the potential benefit to the patient justifies the potential risk to the fetus. Systemically administered corticosteroids appear in human milk and could suppress growth, interfere with endogenous corticosteroid production, or cause other untoward effects. It is not known whether topically administered calcipotriene or corticosteroids could result in sufficient systemic absorption to produce detectable quantities in human milk. Because many drugs are excreted in human milk, caution should be exercised when Calcipotriol and Betamethasone ointment or suspension is administered to a nursing woman.

Contraindication

Betamethasone and Calcipotriol containing preparation is contraindicated in those patients with a history of hypersensitivity to any of the components of the preparation. It is also contraindicated in patients with known disorders of calcium metabolism. Patients with severe renal insufficiency or severe hepatic disorders are also contraindicated.

Acute Overdose

Symptoms: Polyuria, constipation, muscle weakness, confusion, and coma; adrenal insufficiency.

Management: Symptomatic treatment.

Storage Condition

Store between 20-25° C.

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