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Betamethasone

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From Pharmacopedia
Betamethasone (valerate, dipropionate, sodium phosphate, acetate)
Celestone (oral/injectable), Diprolene/Diprosone (topical), Luxiq (foam), Celestone Soluspan (depot IM)

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Summary
Common uses
Antenatal lung maturation (24-34 weeks gestation)0, Severe corticosteroid-responsive dermatoses (topical)0, Intra-articular and soft-tissue injection0, Autoimmune disease flare (oral)0
Pharmacy
Starting dose
Antenatal: Celestone Soluspan 12 mg IM q24h × 2 doses; topical: pea-sized amount BID; intra-articular varies by joint
Preparations
0.6 mg/5 mL oral solution; Celestone Soluspan 6 mg/mL IM/IA (mix of sodium phosphate + acetate); 0.05% and 0.1% topical cream/ointment/lotion/foam (various salts); augmented betamethasone 0.05% (super-high potency)
US FDA Max
Indication-specific
Pharmacology
Routes
Oral, IM, IA, topical
Onset
Hours
Duration
Biologic 36-54 hours (long-acting)
Half-life
Plasma ~5 hours; biologic ~36-54 hours[1]
Bioavailability
Oral ~70%; depot IM provides sustained release over weeks[1]
Pregnancy
Antenatal use (12 mg IM × 2 doses 24h apart) is one of the most evidence-based interventions in obstetrics — reduces neonatal respiratory distress syndrome and mortality in threatened preterm delivery between 24 and 34 weeks. Other uses weigh benefit against fetal HPA suppression.[citation needed]
Legal status
Rx-only in US
Purported mechanism
Betamethasone is a synthetic fluorinated glucocorticoid (the 9α-fluoro group enhances activity), structurally similar to dexamethasone with ~25× the potency of hydrocortisone, virtually no mineralocorticoid activity, and one of the longest biologic half-lives in routine use.0 Activates the glucocorticoid receptor to broadly remodel inflammatory, immune, and metabolic transcription. The dipropionate, valerate, and augmented dipropionate ester forms determine topical potency (high to super-high)[1].

References

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  1. 1.0 1.1 1.2 FDA Prescribing Information, Celestone Soluspan (betamethasone sodium phosphate/acetate), Organon, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/014602s086lbl.pdf