◉ Summary of Use during Lactation:The consensus opinion is that women taking a statin should not breastfeed because of a concern with disruption of infant lipid metabolism. However, others have argued that children homozygous for familial hypercholesterolemia are treated with statins beginning at 1 year of age, that statins have low oral bioavailability, and risks to the breastfed infant are low, especially with rosuvastatin and pravastatin. Some evidence indicates that atorvastatin can be taken by nursing mothers with no obvious developmental problems in their infants. Until more data become available, an alternate drug may be preferred, especially while nursing a newborn or preterm infant.
◉ Effects in Breastfed Infants:In a case series of patients with homozygous familial hypercholesterolemia, 6 patients breastfed 11 infants after restarting statin therapy postpartum. The specific statin used by these women was not reported, most of the women on statin therapy were using atorvastatin, either 40 or 80 mg, daily. Normal early child development was reported for all offspring. Children started school at the appropriate age and no learning difficulties were reported.
◉ Effects on Lactation and Breastmilk:Gynecomastia has been reported in men taking atorvastatin. Serum prolactin was normal in one case where it was measured. In another case, possible rosuvastatin-induced gynecomastia resolved after the patient’s medication was changed to atorvastatin.
来源:Drugs and Lactation Database (LactMed)
制备方法与用途
生物活性
(3S,5S)-Atorvastatin 是 Atorvastatin 的无活性对映异构体,可以激活孕烷 X 受体 (PXR)。Atorvastatin 是一种具有口服活性的 HMG-CoA 还原酶抑制剂,能够有效降低血脂。
[EN] METHODS FOR PROVIDING INTERMEDIATES IN THE SYNTHESIS OF ATORVASTATIN. [FR] PROCÉDÉS POUR PRODUIRE DES INTERMÉDIAIRES DANS LA SYNTHÈSE DE L'ATORVASTATINE.
BOOSTING THE EFFECT OF METHOTREXATE THROUGH THE COMBINED USE WITH LIPOPHILIC STATINS
申请人:DALANA3, S.L.
公开号:US20160175310A1
公开(公告)日:2016-06-23
The invention relates to the use of an inhibitor of the dihydrofolate reductase enzyme selected from the group that consists of methotrexate, trimetrexate and pemetrexed; or a pharmaceutically acceptable salt thereof, for the preparation of a drug for the treatment or prevention of recurrences of a disease selected from the group that consists of cancer, psoriasis, psoriatic arthritis, juvenile polyarticular arthritis, rheumatoid arthritis, Crohn's disease, polymyositis, dermatomyositis and sarcoidosis, wherein said treatment or prevention includes administering to a patient, simultaneously, separately or sequentially, a lipophilic statin and the inhibitor of the dihydrofolate reductase enzyme. The invention also relates to a pharmaceutical composition which includes the inhibitor of the dihydrofolate reductase enzyme and the lipophilic statin together with pharmaceutically acceptable carriers and/or vehicles.
USRE40667E1
申请人:——
公开号:USRE40667E1
公开(公告)日:2009-03-17
[EN] METHODS FOR PROVIDING INTERMEDIATES IN THE SYNTHESIS OF ATORVASTATIN.<br/>[FR] PROCÉDÉS POUR PRODUIRE DES INTERMÉDIAIRES DANS LA SYNTHÈSE DE L'ATORVASTATINE.
申请人:UNIV GRONINGEN
公开号:WO2016122325A1
公开(公告)日:2016-08-04
The invention relates to the field of medicinal chemistry, In particular, it relates to methods for providing intermediates in the synthesis of Atorvastatin, a competitive inhibitor of HMG-Co A reductase. Provided is a process for providing a compound having a Formula (I) or a pharmaceutically acceptable salt, ester, amide or stereoisomer thereof, comprising reacting in a 4 component Ugi-reaction in a single reaction mixture the compounds of formula A, formula B, formula C and formula D.
Synthesis of some impurities and/or degradation products of atorvastatin, calcium (3R,5R)-7- [2-(4-fluorophenyl)-5-isopropyl-3-phenyl-4-(phenylcarbamoyl)pyrrol-1-yl]-3,5-dihydroxyheptanoate, is described. These include its desfluoro analog, the corresponding (3S,5S)- and (3S,5R)-epimers, atorvastatin lactone, and some other potential impurities. The synthesized compounds as well as the corresponding intermediates were characterized by 1H NMR, 13C NMR and MS.