Betamethasone phosphate API Manufacturers

General Description:

Betamethasone phosphate, identified by CAS number 360-63-4, is a notable compound with significant therapeutic applications. Betamethasone phosphate is a prodrug that is rapidly hydrolyzed, providing rapidly accessible to agonize glucocorticoid receptors. Betamethasone provides greater anti-inflammatory activity than with less sodium and water retention. Betamethasone sodium phosphate was granted FDA approval on 3 March 1965.

Indications:

This drug is primarily indicated for: Betamethasone phosphate is indicated intramuscularly to treat allergic states, dermatologic diseases, endocrine disorders, gastrointestinal diseases, hematologic disorders, neoplastic diseases, nervous system conditions, ophthalmic diseases, renal diseases, respiratory diseases, rheumatic disorders, trichinosis with neurologic or myocardial involvement, and tuberculous meningitis with subarachnoid block or impending block. It is also used intra-articularly in the treatment of acute gouty arthritis, acute and subacute bursitis, acute nonspecific tenosynovitis, epicondylitis, rheumatoid arthritis, and synovitis of osteoarthritis. Intralesional betamethasone phospahte is indicated in the treatment of alopecia areata, discoid lupus erythematosus, keloids, lichen planus, lichen simplex chronicus, psoriatic plaques, necrobiosis lipoidica diabeticorum, and localized hypertrophic, infiltrated, inflammatory lesions of granuloma annulare. Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Metabolism:

Betamethasone phosphate undergoes metabolic processing primarily in: Betamethasone phosphate is rapidly de-esterified to betamethasone. This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.

Absorption:

The absorption characteristics of Betamethasone phosphate are crucial for its therapeutic efficacy: 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. The drug's ability to rapidly penetrate into cells ensures quick onset of action.

Half-life:

The half-life of Betamethasone phosphate is an important consideration for its dosing schedule: The half life of betamethasone in an intramuscular injection of 3mg betamethasone acetate and 3mg betamethasone phosphate is 12.47 ± 1.91 h. This determines the duration of action and helps in formulating effective dosing regimens.

Protein Binding:

Betamethasone phosphate exhibits a strong affinity for binding with plasma proteins: Corticosteroids are generally bound to corticosteroid binding globulin and serum albumin in plasma. This property plays a key role in the drug's pharmacokinetics and distribution within the body.

Route of Elimination:

The elimination of Betamethasone phosphate from the body primarily occurs through: Corticosteroids are eliminated predominantly in the urine. Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.

Volume of Distribution:

Betamethasone phosphate is distributed throughout the body with a volume of distribution of: The volume of distribution of betamethasone in an intramuscular injection of 3mg betamethasone acetate and 3mg betamethasone phosphate is 226.00 ± 61.64 L. This metric indicates how extensively the drug permeates into body tissues.

Clearance:

The clearance rate of Betamethasone phosphate is a critical factor in determining its safe and effective dosage: The clearance of betamethasone in an intramuscular injection of 3mg betamethasone acetate and 3mg betamethasone phosphate is 12.62 ± 3.45 L/h. It reflects the efficiency with which the drug is removed from the systemic circulation.

Pharmacodynamics:

Betamethasone phosphate exerts its therapeutic effects through: Corticosteroids bind to the glucocorticoid receptor, inhibiting pro-inflammatory signals, and promoting anti-inflammatory signals. Betamethasone phosphate has a short duration of action as it is rapidly hydrolyzed to betamethasone. Corticosteroids have a wide therapeutic window as patients may require doses that are multiples of what the body naturally produces. Patients taking corticosteroids should be counselled regarding the risk of hypothalamic-pituitary-adrenal axis suppression and increased susceptibility to infections. The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Betamethasone phosphate functions by: 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. This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Toxicity:

Classification:

Betamethasone phosphate belongs to the class of organic compounds known as gluco/mineralocorticoids, progestogins and derivatives. These are steroids with a structure based on a hydroxylated prostane moiety, classified under the direct parent group Gluco/mineralocorticoids, progestogins and derivatives. This compound is a part of the Organic compounds, falling under the Lipids and lipid-like molecules superclass, and categorized within the Steroids and steroid derivatives class, specifically within the Pregnane steroids subclass.

Categories:

Betamethasone phosphate is categorized under the following therapeutic classes: Adrenal Cortex Hormones, Corticosteroids, Cytochrome P-450 CYP3A Inducers, Cytochrome P-450 CYP3A Substrates, Cytochrome P-450 CYP3A4 Inducers, Cytochrome P-450 CYP3A4 Inducers (strength unknown), Cytochrome P-450 CYP3A4 Substrates, Cytochrome P-450 CYP3A5 Inducers, Cytochrome P-450 CYP3A5 Inducers (strength unknown), Cytochrome P-450 Enzyme Inducers, Cytochrome P-450 Substrates, Fused-Ring Compounds, Glucocorticoids, Hormones, Hormones, Hormone Substitutes, and Hormone Antagonists, OAT3/SLC22A8 Substrates, P-glycoprotein inducers, P-glycoprotein substrates, Pregnadienes, Pregnadienetriols, Pregnanes, Steroids, Steroids, Fluorinated. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.