Details
Stereochemistry | RACEMIC |
Molecular Formula | C20H33N3O3S.ClH |
Molecular Weight | 432.02 |
Optical Activity | ( + / - ) |
Defined Stereocenters | 3 / 3 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.[H][C@@]12C[C@H](CN(CCC)[C@@]1([H])CC3=C(C2)C(O)=CC=C3)NS(=O)(=O)N(CC)CC
InChI
InChIKey=DVLKVIJLALMCBQ-VENMBWNLSA-N
InChI=1S/C20H33N3O3S.ClH/c1-4-10-22-14-17(21-27(25,26)23(5-2)6-3)11-16-12-18-15(13-19(16)22)8-7-9-20(18)24;/h7-9,16-17,19,21,24H,4-6,10-14H2,1-3H3;1H/t16-,17+,19-;/m0./s1
CV-205502 (Quinagolide, Norprolac), a small molecule, dopamine 2-receptor agonist was developed by Novartis for the treatment of prolactinoma and hyperprolactinaemia. It is is a long-acting dopamine agonist with potent D2 and weak D1 activity. Quinagolide exists as a racemate and its relevant clinical activity is mediated predominantly by the (-) enantiomer. It is typically present in the hydrochloride salt form and is marketed as oral tablets under the brand name Norprolac contained as a racemate. Quinagolide is currently available in several countries including Canada, but not approved for treatment in the United States. Owing to its dopaminergic action, the drug exerts a strong inhibitory effect on the secretion of the anterior pituitary hormone prolactin, but does not reduce normal levels of other pituitary hormones. Long-term treatment with Norprolac was found to reduce the size or limit the growth of prolactin-secreting pituitary macroadenomas. In some patients the reduction of prolactin secretion may be accompanied by short- lasting, small increases in plasma growth hormone levels, the clinical significance of which is unknown. As a specific inhibitor of prolactin secretion with a prolonged duration of action, Norprolac has been shown to be effective and suitable for once-a- day oral treatment of patients presenting with hyperprolactinaemia and its clinical manifestations such as galactorrhoea, oligomenorrhoea, amenorrhoea, infertility and reduced libido.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: P14416 Gene ID: 1813.0 Gene Symbol: DRD2 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/2521863 |
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0.52 nM [Ki] |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.medicines.org.uk/emc/product/7369/smpc
Adults
The optimal dose must be titrated individually on the basis of the prolactin- lowering effect and tolerability.
With the 'starter pack' treatment begins with 25 micrograms/day for the first 3 days, followed by 50 micrograms/day for a further 3 days. From day 7 onwards, the recommended dose is 75 micrograms/day.
If necessary, the daily dose may then be increased stepwise until the optimal individual response is attained. The usual maintenance dosage is 75 to 150 micrograms/day.
Daily doses of 300 micrograms or higher doses are required in less than one- third of the patients.
In such cases, the daily dosage may be increased in steps of 75 to 150 micrograms at intervals not shorter than 4 weeks until satisfactory therapeutic effectiveness is achieved or reduced tolerability, requiring the discontinuation of treatment, occurs.
Route of Administration:
Oral
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94424-50-7
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DTXSID20241478
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SUB04163MIG
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33474X943Y
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C046650
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m9431
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100000090012
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236233
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DBSALT001152
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76966248
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ACTIVE MOIETY
SUBSTANCE RECORD