Synonyms
Bromocriptine mesilate
Molecular Formula
C33H44BrN5O8S
Smiles
CC(C)C[C@H]1C(=O)N2CCC[C@H]2[C@]3(N1C(=O)[C@](O3)(C(C)C)NC(=O)[C@H]4CN([C@@H]5CC6=C(NC7=CC=CC(=C67)C5=C4)Br)C)O.CS(=O)(=O)O
General Description
Bromocriptine Mesylate is the mesylate salt of bromocriptine, a semisynthetic ergot alkaloid derivative with potent dopamine D2 receptor agonist activity. It is derived from ergocryptine and possesses a complex pharmacological profile affecting multiple neurotransmitter systems.
Mechanism of Action
Bromocriptine Mesylate acts as a potent agonist at dopamine D2 receptors in the pituitary and central nervous system, suppressing prolactin secretion from lactotroph cells. It also exhibits antagonist activity at serotonin 5-HT2 receptors and partial agonist activity at alpha-1 and alpha-2 adrenergic receptors.
Application
Indicated for the treatment of Parkinson's disease, hyperprolactinemia, and acromegaly. Bromocriptine Mesylate is a dopamine D2 receptor agonist and ergot alkaloid derivative that effectively suppresses prolactin secretion and improves motor function in Parkinsonian patients through dopaminergic pathway modulation.
A bromocriptine mesylate nanoemulsion was prepared by spontaneous emulsification and incorporated into a transdermal gel. The optimized nanoemulsion exhibited a mean globule size of 160 nm, zeta potential of -20.4 mV, and drug content of 99.45%. Ex vivo permeation studies showed enhancement ratios of 7.4 for the nanoemulsion and 5.86 for the nanoemulsion gel compared to aqueous suspension gel. In vivo pharmacokinetic evaluation in rats demonstrated a 274% increase in relative bioavailability for the nanoemulsion gel compared to oral suspension, with prolonged drug release and improved safety confirmed by histopathological studies.
Fig. 2 Texture profile analysis of blank gel and BCM-NE gel: a spreadability and b adhesiveness. (Sita V G, Vavia P. 2020)
References
- Sita V G, Vavia P. Bromocriptine nanoemulsion-loaded transdermal gel: optimization using factorial design, in vitro and in vivo evaluation. AAPS PharmSciTech, 2020, 21(3): 80.
What distinguishes Bromocriptine Mesylate from other dopamine agonists?
Bromocriptine Mesylate has a shorter duration of action and different receptor subtype selectivity compared to cabergoline, with additional serotonergic and adrenergic receptor activities valuable for complex endocrine management.
What storage conditions are required?
Bromocriptine Mesylate should be stored at 2-8℃ in a tightly sealed container, protected from light and moisture.
What purity grade is available?
Bromocriptine Mesylate is supplied as a high-purity grade suitable for neurological and endocrine R&D and pharmaceutical manufacturing.
Can packaging be customized?
Custom packaging options and flexible order quantities can be tailored to customer R&D and production requirements.