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Drug

D0815 | bromocriptine

Molecular Formula C32H40BrN5O5
Molecular Weight 654.6
Structure
State solid
Route of elimination Parent drug and metabolites are almost completely excreted via the liver, and only 6% eliminated via the kidney.
Protein binding 90-96% bound to serum albumin
Half life 2-8 hours
Absorption Approximately 28% of the oral dose is absorbed; however due to a substantial first pass effect, only 6% of the oral dose reaches the systemic circulation unchanged. Bromocriptine and its metabolites appear in the blood as early as 10 minutes following oral administration and peak plasma concentration are reached within 1-1.5 hours. Serum prolactin may be decreased within 2 hours or oral administration with a maximal effect achieved after 8 hours. Growth hormone concentrations in patients with acromegaly is reduced within 1-2 hours with a single oral dose of 2.5 mg and decreased growth hormone concentrations persist for at least 4-5 hours.
Trade names Parlodel
Description a dopamine 2 receptor (D2R) agonist; ergoline derivative

G

N

N04BC01 Bromocriptine


[N04BC] Dopamine agonists


[N04B] DOPAMINERGIC AGENTS


[N04] ANTI-PARKINSON DRUGS


[N] Nervous system

G02CB01 Bromocriptine


[G02CB] Prolactine inhibitors


[G02C] OTHER GYNECOLOGICALS


[G02] OTHER GYNECOLOGICALS


[G] Genitourinary system and reproductive hormones

Toxicity Dose Time Species Model Method Action Positive criterion Reference
MEMBRANE POTENTIAL 11.44±1.58 human qHTS-HepG2 MMP assay decrease IC50 163
MEMBRANE POTENTIAL 21.82 human HepG2 MMP assay decrease IC50 163
MEMBRANE POTENTIAL 13.20±10.83 rat hepatocytes MMP assay decrease IC50 163
MITOCHONDRIA TRANSPORT 5 µM 2h rat Hippocampal Neurons time-lapse imaging experiments decrease 216

Pictogram Signal Statements Precautionary Statement Codes
Warning

The GHS information provided by 1 company from 1 notification to the ECHA C&L Inventory.


H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]


H361 (100%): Suspected of damaging fertility or the unborn child [Warning Reproductive toxicity]


H362 (100%): May cause harm to breast-fed children [Reproductive toxicity, effects on or via lactation]


 P201, P202, P260, P263, P264, P270, P281, P301+P312, P308+P313, P330, P405, and P501; (The corresponding statement to each P-code can be found at the GHS Classification page.)

Organism Test type Route Dose (normalized dose) Effect Source
women TDLo oral 650ug/kg/9D-I (0.65mg/kg) Annals of Internal Medicine. Vol. 118, Pg. 199, 1993.
rat LD50 intravenous 10500ug/kg (10.5mg/kg) Yakkyoku. Pharmacy. Vol. 29, Pg. 1231, 1978.
mouse LD50 intravenous 189mg/kg (189mg/kg) Yakkyoku. Pharmacy. Vol. 30, Pg. 809, 1979.
child TDLo oral 375ug/kg (0.375mg/kg) Journal of Pediatrics. Vol. 105, Pg. 838, 1984.
man TDLo oral 52mg/kg/35W-I (52mg/kg) brain and coverings: changes in cerebral spinal fluid Neurology. Vol. 35, Pg. 1193, 1985.
rat LD50 oral > 2gm/kg (2000mg/kg) Yakkyoku. Pharmacy. Vol. 30, Pg. 809, 1979.
rabbit LD50 intravenous 8200ug/kg (8.2mg/kg) Iyakuhin Kenkyu. Study of Medical Supplies. Vol. 10, Pg. 232, 1979.
women TDLo oral 50ug/kg (0.05mg/kg) sense organs and special senses: other: eye Lancet. Vol. 340, Pg. 1410, 1992.
women TDLo oral 1mg/kg/20D-I (1mg/kg) behavioral: toxic psychosis American Journal of Psychiatry. Vol. 143, Pg. 935, 1985.
mouse LD50 oral 2502mg/kg (2502mg/kg) Yakkyoku. Pharmacy. Vol. 30, Pg. 809, 1979.
rat LD50 subcutaneous > 1gm/kg (1000mg/kg) Yakkyoku. Pharmacy. Vol. 30, Pg. 809, 1979.
rabbit LD50 oral > 1gm/kg (1000mg/kg) Yakkyoku. Pharmacy. Vol. 30, Pg. 809, 1979.


  • (4R,7R)-10-bromo-N-[(1S,2S,4R,7S)-2-hydroxy-7-(2-methylpropyl)-5,8-dioxo-4-(propan-2-yl)-3-oxa-6,9-diazatricyclo[7.3.0.0^{2,6}]dodecan-4-yl]-6-methyl-6,11-diazatetracyclo[7.6.1.0^{2,7}.0^{12,16}]hexadeca-1(16),2,9,12,14-pentaene-4-carboxamide (5'alpha)-2-bromo-12'-hydroxy-2'-(1-methylethyl)-5'-(2-methylpropyl)-3',6',18-trioxoergotaman (5'alpha)-2-bromo-12'-hydroxy-2'-(1-methylethyl)-5'-(2-methylpropyl)ergotaman-3',6',18-trione
    (5'alpha)-2-bromo-12'-hydroxy-5'-(2-methylpropyl)-2'-(propan-2-yl)-3',6',18-trioxoergotaman (5'alpha)-2-bromo-12'-hydroxy-5'-(2-methylpropyl)-3',6',18-trioxo-2'-(propan-2-yl)ergotaman (5'alpha)-2-bromo-12'-hydroxy-5'-isobutyl-2'-isopropyl-3',6',18-trioxoergotaman
    (5alpha,5'beta)-2-bromo-12'-hydroxy-5'-(2-methylpropyl)-3',6',18-trioxo-2'-(propan-2-yl)ergotaman (6aR,9R)-5-Bromo-N-((2R,5S,10aS,10bS)-10b-hydroxy-5-isobutyl-2-isopropyl-3,6-dioxooctahydro-2H-oxazolo[3,2-a]pyrrolo[2,1-c]pyrazin-2-yl)-7-methyl-4,6,6a,7,8,9-hexahydroindolo[4,3-fg]quinoline-9-carboxamide (6aR,9R)-5-bromo-N-((2R,5S,10aS,10bS)-
    08Y 10b-hydroxy-5-isobutyl-2-isopropyl-3,6- 13177-EP2272832A1
    13177-EP2275420A1 13177-EP2277876A1 13177-EP2280008A2
    13177-EP2287165A2 13177-EP2287166A2 13177-EP2292614A1
    13177-EP2292620A2 13177-EP2295412A1 13177-EP2295413A1
    13177-EP2295439A1 13177-EP2298731A1 13177-EP2298738A1
    13177-EP2298779A1 13177-EP2311808A1 13177-EP2311818A1
    13177-EP2311829A1 13177-EP2311837A1 13177-EP2316470A2
    13177-EP2316834A1 2-Bromo-12'-hydroxy-2'-(1-methylethyl)-5'-alpha-(2-methylpropyl)ergotamin-3',6',18-trione 2-Bromo-alpha-ergocryptine
    2-Bromo-alpha-ergokryptin 2-Bromo-alpha-ergokryptine 2-Bromoergocryptine
    2-Bromoergocryptine Methanesulfonate 2-Bromoergokryptine 25614-03-3
    3A64E3G5ZO 88085-EP2298415A1 88085-EP2298742A1
    88085-EP2305648A1 AC-13601 AKOS015961273
    BDBM81993 BIDD:GT0464 BPBio1_001131
    BRD-K14496212-001-01-1 BRD-K14496212-066-04-8 Biomol-NT_000005
    Bromergocryptine Bromocriptin Bromocriptina
    Bromocriptina [INN-Spanish] Bromocriptine (USAN/INN) Bromocriptine [BAN]
    Bromocriptine [USAN:BAN:INN] Bromocriptine [USAN:INN:BAN] Bromocriptine methanesulfonate
    Bromocriptine+ (GTP-) Bromocriptinum Bromocriptinum [INN-Latin]
    Bromocryptin Bromocryptine Bromoergocriptine
    Bromoergocryptine C06856 C32H40BrN5O5
    CAS-25614-03-3 CB-154 CCG-204266
    CCRIS 3244 CHEBI:3181 CHEMBL493
    Carboprost Methylate,(S) D03165 DB01200
    DSSTox_CID_2687 DSSTox_GSID_22687 DSSTox_RID_76692
    DTXSID1022687 EINECS 247-128-5 Ergocryptine, 2-bromo-
    Ergocryptine, 2-bromo- (8CI) Ergoset Ergotaman-3',6',18-trione, 2-bromo-12'-hydroxy-2'-(1-methylethyl)-5'-(2-methylpropyl)-, (5'alpha)-
    Ergotaman-3',6',18-trione, 2-bromo-12'-hydroxy-2'-(1-methylethyl)-5'-(2-methylpropyl)-,(5'-alpha)- Ergotaman-3',6',18-trione, 2-bromo-12'-hydroxy-2'-(1-methylethyl)-5'alpha-(2-methylpropyl)- GTPL35
    J-016067 LS-64540 Lopac0_000171
    N-[(2R,5S,10aS,10bS)-10b-hydroxy-5-isobutyl-2-isopropyl-3,6-dioxo-8,9,10,10a-tetrahydro-5H-oxazolo[[?]]pyrrolo[[?]]pyrazin-2-yl]-bromo-methyl-[?]carboxamide; NCGC00024584-03 NCGC00024584-04
    NCGC00024584-05 NCI60_001365 NSC169774
    OZVBMTJYIDMWIL-AYFBDAFISA-N PDSP2_001500 Parlodel
    Prestwick0_000121 Prestwick1_000121 Prestwick2_000121
    Q413581 SANDOZ 15-754 SCHEMBL25297
    SPBio_002101 SR-01000075356 SR-01000075356-5
    Tox21_110907 UNII-3A64E3G5ZO ZINC53683151
    [2,1-c]pyrazin-2-yl)-7-methyl-4,6,6a,7,8,9- bromocriptine dioxooctahydro-2H-oxazolo[3,2-a]pyrrolo
    hexahydroindolo[4,3-fg]quinoline-9-carboxamide

    DrugBank Name bromocriptine
    DrugBank DB01200
    CAS Number 22260-51-1, 25614-03-3
    PubChem Compound 31101
    KEGG Compound ID C06856
    KEGG Drug D03165
    ChEBI 3181