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1. 2 Bromo Alpha Ergocryptine
2. 2 Bromo Alpha Ergokryptine
3. 2 Bromoergocryptine
4. 2 Bromoergocryptine Mesylate
5. 2 Bromoergocryptine Methanesulfonate
6. 2 Bromoergokryptine
7. 2-bromo-alpha-ergocryptine
8. 2-bromo-alpha-ergokryptine
9. 2-bromoergocryptine
10. 2-bromoergocryptine Mesylate
11. 2-bromoergocryptine Methanesulfonate
12. 2-bromoergokryptine
13. Bromocriptin
14. Bromocriptine Mesylate
15. Bromocryptin
16. Cb 154
17. Cb-154
18. Cb154
19. Mesylate, 2-bromoergocryptine
20. Mesylate, Bromocriptine
21. Methanesulfonate, 2-bromoergocryptine
22. Parlodel
1. Bromocryptine
2. 25614-03-3
3. Bromocriptin
4. Bromoergocryptine
5. Bromergocryptine
6. Bromoergocriptine
7. 2-bromo-alpha-ergocryptine
8. 2-bromo-alpha-ergokryptine
9. Bromocriptina
10. Bromocriptinum
11. 2-bromo-alpha-ergokryptin
12. Bromocriptinum [inn-latin]
13. Bromocriptina [inn-spanish]
14. Ergocryptine, 2-bromo-
15. Cb-154
16. Bagren
17. 2-bromoergocryptine
18. 2-bromo-.alpha.-ergocryptine
19. 3a64e3g5zo
20. Chebi:3181
21. Ergotaman-3',6',18-trione, 2-bromo-12'-hydroxy-2'-(1-methylethyl)-5'-(2-methylpropyl)-, (5'alpha)-
22. Ergoset
23. Sandoz 15-754
24. Bromergon
25. (+)-bromocriptine
26. Cb 154
27. 22260-51-1
28. (5'alpha)-2-bromo-12'-hydroxy-2'-(1-methylethyl)-5'-(2-methylpropyl)-3',6',18-trioxoergotaman
29. Ergotaman-3',6',18-trione, 2-bromo-12'-hydroxy-2'-(1-methylethyl)-5'-(2-methylpropyl)-, (5'.alpha.)-
30. Bromocriptine (mesylate)
31. (6ar,9r)-5-bromo-n-[(1s,2s,4r,7s)-2-hydroxy-7-(2-methylpropyl)-5,8-dioxo-4-propan-2-yl-3-oxa-6,9-diazatricyclo[7.3.0.02,6]dodecan-4-yl]-7-methyl-6,6a,8,9-tetrahydro-4h-indolo[4,3-fg]quinoline-9-carboxamide
32. Ccris 3244
33. Nsc169774
34. Einecs 247-128-5
35. Bromocriptine (usan/inn)
36. Unii-3a64e3g5zo
37. Sr-01000075356
38. Bromocriptine [usan:inn:ban]
39. Ncgc00024584-03
40. 08y
41. 2-bromo-12'-hydroxy-2'-(1-methylethyl)-5'-alpha-(2-methylpropyl)ergotamin-3',6',18-trione
42. Bromocriptine+ (gtp-)
43. Prestwick0_000121
44. Prestwick1_000121
45. Prestwick2_000121
46. Carboprost Methylate,(s)
47. Dsstox_cid_2687
48. Bromocriptine [mi]
49. Biomol-nt_000005
50. Chembl493
51. Gtpl35
52. Bromocriptine [inn]
53. (5'alpha)-2-bromo-12'-hydroxy-5'-isobutyl-2'-isopropyl-3',6',18-trioxoergotaman
54. Bromocriptine [usan]
55. Dsstox_rid_76692
56. Dsstox_gsid_22687
57. Lopac0_000171
58. Schembl25297
59. Bromocriptine [vandf]
60. (5'alpha)-2-bromo-12'-hydroxy-2'-(1-methylethyl)-5'-(2-methylpropyl)ergotaman-3',6',18-trione
61. Bidd:gt0464
62. Spbio_002101
63. Bromocriptine [who-dd]
64. Bpbio1_001131
65. Dtxsid1022687
66. Bdbm81993
67. Tox21_110907
68. Pdsp2_001500
69. Zinc53683151
70. Akos015961273
71. Ccg-204266
72. Db01200
73. Sdccgsbi-0050159.p003
74. Dioxooctahydro-2h-oxazolo[3,2-a]pyrrolo
75. Ncgc00024584-04
76. Ncgc00024584-05
77. Ncgc00024584-07
78. Ncgc00024584-09
79. (5'alpha)-2-bromo-12'-hydroxy-5'-(2-methylpropyl)-2'-(propan-2-yl)-3',6',18-trioxoergotaman
80. (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
81. Ac-13601
82. Nci60_001365
83. 10b-hydroxy-5-isobutyl-2-isopropyl-3,6-
84. Cas-25614-03-3
85. C06856
86. D03165
87. Hexahydroindolo[4,3-fg]quinoline-9-carboxamide
88. Q413581
89. J-016067
90. Sr-01000075356-5
91. (6ar,9r)-5-bromo-n-((2r,5s,10as,10bs)-
92. [2,1-c]pyrazin-2-yl)-7-methyl-4,6,6a,7,8,9-
93. Brd-k14496212-001-01-1
94. Brd-k14496212-066-04-8
95. (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
96. (5alpha,5'beta)-2-bromo-12'-hydroxy-5'-(2-methylpropyl)-3',6',18-trioxo-2'-(propan-2-yl)ergotaman
97. 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
| Molecular Weight | 654.6 g/mol |
|---|---|
| Molecular Formula | C32H40BrN5O5 |
| XLogP3 | 3.8 |
| Hydrogen Bond Donor Count | 3 |
| Hydrogen Bond Acceptor Count | 6 |
| Rotatable Bond Count | 5 |
| Exact Mass | 653.22128 g/mol |
| Monoisotopic Mass | 653.22128 g/mol |
| Topological Polar Surface Area | 118 Ų |
| Heavy Atom Count | 43 |
| Formal Charge | 0 |
| Complexity | 1230 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 6 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| Covalently Bonded Unit Count | 1 |
| 1 of 2 | |
|---|---|
| Drug Name | Parlodel |
| PubMed Health | Bromocriptine (By mouth) |
| Drug Classes | Antidiabetic, Antiparkinsonian, Prolactin Secretion Inhibitor |
| Drug Label | Parlodel (bromocriptine mesylate) is an ergot derivative with potent dopamine receptor agonist activity. Each Parlodel (bromocriptine mesylate) SnapTabs tablet for oral administration contains 2 mg and each capsule contains 5 mg bromocriptine... |
| Active Ingredient | Bromocriptine mesylate |
| Dosage Form | Tablet; Capsule |
| Route | Oral |
| Strength | eq 5mg base; eq 2.5mg base |
| Market Status | Prescription |
| Company | Us Pharms Holdings I |
| 2 of 2 | |
|---|---|
| Drug Name | Parlodel |
| PubMed Health | Bromocriptine (By mouth) |
| Drug Classes | Antidiabetic, Antiparkinsonian, Prolactin Secretion Inhibitor |
| Drug Label | Parlodel (bromocriptine mesylate) is an ergot derivative with potent dopamine receptor agonist activity. Each Parlodel (bromocriptine mesylate) SnapTabs tablet for oral administration contains 2 mg and each capsule contains 5 mg bromocriptine... |
| Active Ingredient | Bromocriptine mesylate |
| Dosage Form | Tablet; Capsule |
| Route | Oral |
| Strength | eq 5mg base; eq 2.5mg base |
| Market Status | Prescription |
| Company | Us Pharms Holdings I |
For the treatment of galactorrhea due to hyperprolactinemia, prolactin-dependent menstrual disorders and infertility, prolactin-secreting adenomas, prolactin-dependent male hypogonadism, as adjunct therapy to surgery or radiotherapy for acromegaly or as monotherapy is special cases, as monotherapy in early Parksinsonian Syndrome or as an adjunct with levodopa in advanced cases with motor complications. Bromocriptine has also been used off-label to treat restless legs syndrome and neuroleptic malignant syndrome.
FDA Label
Bromocriptine stimulates centrally-located dopaminergic receptors resulting in a number of pharmacologic effects. Five dopamine receptor types from two dopaminergic subfamilies have been identified. The dopaminergic D1 receptor subfamily consists of D1 and D5 subreceptors, which are associated with dyskinesias. The dopaminergic D2 receptor subfamily consists of D2, D3 and D4 subreceptors, which are associated with improvement of symptoms of movement disorders. Thus, agonist activity specific for D2 subfamily receptors, primarily D2 and D3 receptor subtypes, are the primary targets of dopaminergic antiparkinsonian agents. It is thought that postsynaptic D2 stimulation is primarily responsible for the antiparkinsonian effect of dopamine agonists, while presynaptic D2 stimulation confers neuroprotective effects. This semisynthetic ergot derivative exhibits potent agonist activity on dopamine D2-receptors. It also exhibits agonist activity (in order of decreasing binding affinity) on 5-hydroxytryptamine (5-HT)1D, dopamine D3, 5-HT1A, 5-HT2A, 5-HT1B, and 5-HT2C receptors, antagonist activity on α2A-adrenergic, α2C, α2B, and dopamine D1 receptors, partial agonist activity at receptor 5-HT2B, and inactivates dopamine D4 and 5-HT7 receptors. Parkinsonian Syndrome manifests when approximately 80% of dopaminergic activity in the nigrostriatal pathway of the brain is lost. As this striatum is involved in modulating the intensity of coordinated muscle activity (e.g. movement, balance, walking), loss of activity may result in dystonia (acute muscle contraction), Parkinsonism (including symptoms of bradykinesia, tremor, rigidity, and flattened affect), akathesia (inner restlessness), tardive dyskinesia (involuntary muscle movements usually associated with long-term loss of dopaminergic activity), and neuroleptic malignant syndrome, which manifests when complete blockage of nigrostriatal dopamine occurs. High dopaminergic activity in the mesolimbic pathway of the brain causes hallucinations and delusions; these side effects of dopamine agonists are manifestations seen in patients with schizophrenia who have overractivity in this area of the brain. The hallucinogenic side effects of dopamine agonists may also be due to 5-HT2A agonism. The tuberoinfundibular pathway of the brain originates in the hypothalamus and terminates in the pituitary gland. In this pathway, dopamine inhibits lactotrophs in anterior pituitary from secreting prolactin. Increased dopaminergic activity in the tuberoinfundibular pathway inhibits prolactin secretion making bromocriptine an effective agent for treating disorders associated with hypersecretion of prolactin. Pulmonary fibrosis may be associated bromocriptines agonist activity at 5-HT1B and 5-HT2B receptors.
Antiparkinson Agents
Agents used in the treatment of Parkinson's disease. The most commonly used drugs act on the dopaminergic system in the striatum and basal ganglia or are centrally acting muscarinic antagonists. (See all compounds classified as Antiparkinson Agents.)
Dopamine Agonists
Drugs that bind to and activate dopamine receptors. (See all compounds classified as Dopamine Agonists.)
Hormone Antagonists
Chemical substances which inhibit the function of the endocrine glands, the biosynthesis of their secreted hormones, or the action of hormones upon their specific sites. (See all compounds classified as Hormone Antagonists.)
G02CB01
S76 | LUXPHARMA | Pharmaceuticals Marketed in Luxembourg | Pharmaceuticals marketed in Luxembourg, as published by d'Gesondheetskeess (CNS, la caisse nationale de sante, www.cns.lu), mapped by name to structures using CompTox by R. Singh et al. (in prep.). List downloaded from https://cns.public.lu/en/legislations/textes-coordonnes/liste-med-comm.html. Dataset DOI:10.5281/zenodo.4587355
G - Genito urinary system and sex hormones
G02 - Other gynecologicals
G02C - Other gynecologicals
G02CB - Prolactine inhibitors
G02CB01 - Bromocriptine
N - Nervous system
N04 - Anti-parkinson drugs
N04B - Dopaminergic agents
N04BC - Dopamine agonists
N04BC01 - Bromocriptine
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.
Route of Elimination
Parent drug and metabolites are almost completely excreted via the liver, and only 6% eliminated via the kidney.
Completely metabolized by the liver, primarily by hydrolysis of the amide bond to produce lysergic acid and a peptide fragment, both inactive and non-toxic. Bromocriptine is metabolized by cytochrome P450 3A4 and excreted primarily in the feces via biliary secretion.
Bromocriptine has known human metabolites that include 5-bromo-N-[2,10-dihydroxy-7-(2-methylpropyl)-5,8-dioxo-4-propan-2-yl-3-oxa-6,9-diazatricyclo[7.3.0.02,6]dodecan-4-yl]-7-methyl-6,6a,8,9-tetrahydro-4H-indolo[4,3-fg]quinoline-9-carboxamide and 5-bromo-N-[2,11-dihydroxy-7-(2-methylpropyl)-5,8-dioxo-4-propan-2-yl-3-oxa-6,9-diazatricyclo[7.3.0.02,6]dodecan-4-yl]-7-methyl-6,6a,8,9-tetrahydro-4H-indolo[4,3-fg]quinoline-9-carboxamide.
S73 | METXBIODB | Metabolite Reaction Database from BioTransformer | DOI:10.5281/zenodo.4056560
2-8 hours
The dopamine D2 receptor is a 7-transmembrane G-protein coupled receptor associated with Gi proteins. In lactotrophs, stimulation of dopamine D2 receptor causes inhibition of adenylyl cyclase, which decreases intracellular cAMP concentrations and blocks IP3-dependent release of Ca2+ from intracellular stores. Decreases in intracellular calcium levels may also be brought about via inhibition of calcium influx through voltage-gated calcium channels, rather than via inhibition of adenylyl cyclase. Additionally, receptor activation blocks phosphorylation of p42/p44 MAPK and decreases MAPK/ERK kinase phosphorylation. Inhibition of MAPK appears to be mediated by c-Raf and B-Raf-dependent inhibition of MAPK/ERK kinase. Dopamine-stimulated growth hormone release from the pituitary gland is mediated by a decrease in intracellular calcium influx through voltage-gated calcium channels rather than via adenylyl cyclase inhibition. Stimulation of dopamine D2 receptors in the nigrostriatal pathway leads to improvements in coordinated muscle activity in those with movement disorders.
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