Betamethasone dipropionate was developed by Merck in the 1980s, with specific formulations such as the Diprolene cream and lotion patented in 1987. Although betamethasone, the parent compound, was approved for medical use back in 1961, the dipropionate ester form was patented later, with patents expiring around 2003 and 2007. This expiration paved the way for the introduction of generic versions. Since then, betamethasone dipropionate has been incorporated into various topical products, including combination medications like Lotrisone, which combi Betamethasone dipropionate is a powerful topical corticosteroid used to manage inflammatory skin conditions such as eczema and psoriasis by alleviating redness, itching, and swelling.
BRAND NAMES
The generic medication betamethasone dipropionate is sold under several brand names, including Diprolene, Sernivo, and Diprosone. It is a potent topical corticosteroid used to treat various inflammatory and itchy skin conditions.
Diprolene is available in multiple forms such as cream, gel, lotion, and ointment. An enhanced version called Diprolene AF ("augmented formulation") offers greater potency for stronger treatment effects.
Sernivo is a spray specifically formulated for the treatment of mild to moderate plaque psoriasis, providing a convenient application method.
Diprosone is a brand name used for betamethasone dipropionate in Europe and other regions, offering the same corticosteroid treatment under a different label.
Alphatrex is another brand name under which betamethasone dipropionate is marketed, available in various markets.
MECHANISM OF ACTION
Betamethasone dipropionate exerts its effects by binding to glucocorticoid receptors within cells, which then enter the nucleus to alter gene expression. This leads to an increase in the production of anti-inflammatory proteins and a decrease in inflammatory mediators, resulting in reduced swelling, redness, and itching. Additionally, it suppresses the movement of certain white blood cells and decreases capillary permeability, helping to regulate the body's inflammatory response.
PHARMACOKINETICS:
Absorption
The absorption and effectiveness of topical corticosteroids, including betamethasone, are influenced by the formulation or vehicle used. For instance, betamethasone dipropionate 0.05% ointment is classified as a highly potent topical steroid, whereas the same concentration in cream or lotion form is regarded as moderately potent.
Distribution
In a study involving Indian women of reproductive age, the volume of distribution after a single intramuscular dose of betamethasone phosphate was reported to be 94,584 ± 23,539 mL.
Metabolism
Betamethasone is metabolized into six different metabolites. The metabolic pathways involve 6β-hydroxylation, 11β-hydroxyl oxidation, and reduction of the C-20 carbonyl group, followed by the removal of the side chain.
Elimination: Corticosteroids are primarily excreted through the urine.
PHARMACODYNAMICS
Corticosteroids work by binding to glucocorticoid receptors, which suppress pro-inflammatory signals and enhance anti-inflammatory responses. They have a broad therapeutic range, allowing patients to take doses much higher than the body’s natural production when needed. However, patients undergoing long-term corticosteroid therapy should be informed about the risks of hypothalamic-pituitary-adrenal (HPA) axis suppression and a greater vulnerability to infections.
ADMINISTRATION
Betamethasone dipropionate is typically applied topically in the form of a cream, gel, ointment, or lotion to treat skin conditions, or administered by injection for systemic or localized issues. The method of administration is determined by the type of condition being treated and the specific formulation prescribed by a healthcare provider.
DOSAGE AND STRENGTH
Betamethasone dipropionate is a potent topical corticosteroid available in various formulations, including creams, ointments, lotions, and gels. These preparations are commonly found in a 0.05% concentration. The potency can differ based on whether the formulation is "augmented," which is designed for enhanced skin penetration.
DRUG INTERACTIONS
Betamethasone dipropionate, a topical corticosteroid, has fewer drug interactions than oral or injectable forms. Significant interactions are more likely with systemic (oral, injected, or absorbed through large areas of damaged skin) exposure rather than from typical topical use. The following categories of drugs may interact with betamethasone:
Hepatic enzyme inducers
These medications can increase the metabolism of corticosteroids like betamethasone, potentially decreasing its effectiveness.
Barbiturates (phenobarbital)
Phenytoin
Rifampin
Carbamazepine
FOOD INTERACTIONS
There are no known direct food interactions with topical forms of betamethasone dipropionate, such as creams or ointments. However, dietary considerations are more relevant for oral or injectable forms, as these can influence blood sugar levels and cause fluid retention, similar to other corticosteroids.
CONTRAINDICATIONS
Topical betamethasone dipropionate should not be used if you have a known hypersensitivity or allergic reaction to the drug, any of its ingredients, or other corticosteroids. It is also contraindicated for use on the eyes, face, groin, or armpits, and for certain skin conditions, such as rosacea and perioral dermatitis.
SIDE EFFECTS
Abdominal swelling or bloating
Fat accumulation around the abdomen
Unusual or excessive hair growth
Formation of abscesses
Acne or skin breakouts
Suppression of adrenal gland function
Vision loss or blindness
Blood clot formation
Blurred or distorted vision
Bowel or bladder control issues
Ulcers or erosion in the stomach lining
Fragile bones or increased risk of fractures
Protruding or bulging eyes
Calcium buildup in the skin
Sudden cardiac arrest
Development of cataracts
Bone tissue damage or necrosis
OVER DOSE
Overdose with betamethasone dipropionate, especially from topical use, is uncommon. However, excessive or prolonged application over large skin areas, use under occlusive dressings, or ingestion can lead to systemic corticosteroid effects.
TOXICITY
Prolonged use of high doses of glucocorticoids can lead to a range of adverse effects, including cataracts, glaucoma, high blood pressure, fluid retention, elevated lipid levels, peptic ulcers, pancreatitis, muscle weakness, osteoporosis, mood disturbances, psychosis, thinning of the skin, allergic reactions, acne, excessive hair growth, immune suppression, increased risk of infections, characteristic "moon face," high blood sugar, low calcium and phosphate levels, metabolic acidosis, growth suppression, and secondary adrenal insufficiency. Management of overdose typically involves adjusting the dosage or discontinuing the corticosteroid, along with providing appropriate symptomatic and supportive care.
