Drugs online research references
J Assoc Physicians India. 1994 Jun;42(6):468-9.
Repeated blood donation effective in treating hyperlipidemia.
Kumar H.
Indira Gandhi Institute of Cardiology, Juhi Nursing Home.
Effectiveness of repeated blood donation in lowering blood lipids has been studied. Ten patients of hyperlipidaemia who donated blood 300 ml every month for 3 months and received gemfibrozil 1200 mg/day (Group B) had nearly 2 fold greater fall in serum total cholesterol, LDL and triglyceride levels in comparison to 17 patients of group A who were treated with gemfibrozil alone in similar dose for the same period. HDL level remained almost unchanged. Thus, a non-pharmacological way of treating hyperlipidaemia has emerged from this study. Moreover donated blood will be available as by-product for use by others. This method may be especially suitable in obese persons.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=7852232&dopt=Abstract
Pol Arch Med Wewn. 1994 Jan;91(1):9-18.
[Evaluation of the efficiency of gemfibrozil in treating hyperlipidemia type IIb and IV]
[Article in Polish]
Polakowska M, Broda G, Rywik S, Piotrowski W, Bednarska M, Kuzminska A, Pytlak A, Chotkowska E.
Zakladu Epidemiologii i Prewencji Chorob Ukladu Krazenia Instytutu Kardiologii, Warszawie.
Analysis of the efficacy and tolerability of gemfibrozil (Gevilon-Parke Davis) was performed including 29 patients aged 19-69 years with primary hyperlipoproteinemia (HLP) type IIb-16 persons, IV-13 persons. All patients got dietary recommendations and received gemfibrozil 450-900 mg/day for 3 months. In both types of HLP a significant reduction of serum cholesterol (TCh)--15.5% triglycerides (TG)--32.1% VLDL-Ch--34.9% and VLDL-TG concentration--36.6% was observed as well as an increase of HDL3 fraction-16.3%. The greatest reduction of serum TCh concentration and VLDL-Ch were observed in type IIb, while that of TG and VLDL-TG in type IV HLP. The best therapeutic effect was obtained during the first month of treatment. The percent of TCh, TG, VLDL-Ch, VLDL-TG reduction correlated with their initial level. Tolerability of gemfibrozil was very good. Only in 2 patients transient abdominal pain was observed.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=8190659&dopt=Abstract
Drug Metab Dispos. 1997 Jan;25(1):55-60.
Interaction of human serum albumin with the electrophilic metabolite 1-O-gemfibrozil-beta-D-glucuronide.
Sallustio BC, Fairchild BA, Pannall PR.
Department of Clinical Pharmacology, Queen Elizabeth Hospital, Woodville, South Australia.
Acyl glucuronides are electrophilic metabolites that are readily hydrolyzed, undergo intramolecular rearrangement, and bind covalently to endogenous proteins. Gemfibrozil is a fibrate lipid-lowering agent that is extensively metabolized to an acyl glucuronide conjugate in humans. The aims of this study were to examine the interactions of 1-O-gemfibrozil-beta-D-glucuronide with human serum albumin. The degradation of 1-O-gemfibrozil-beta-D-glucuronide (approximately 200 microM) was examined in vitro during incubations at 37 degrees C with phosphate buffer (pH 7.4 or 9.0), solutions of human serum albumin (pH 7.4), or fresh human plasma (pH 7.4). The effects of diazepam, oxyphenbutazone, and gemfibrozil on the degradation of 1-O-gemfibrozil-beta-D-glucuronide, and its reversible binding to albumin were also studied. A pilot in vivo study was performed on two patient volunteers administered 1 g/day p.o. gemfibrozil. 1-O-Gemfibrozil-beta-D-glucuronide was unstable, with degradation half-lives in buffer of 4.1 hr and 44 hr at pH 9.0 and 7.4, respectively; and 8.5 hr and 5.5 hr in pH 7.4 solutions of human serum albumin or fresh plasma, respectively. Degradation was dependent on pH and the presence of albumin, which seemed to accelerate the intramolecular rearrangement and hydrolysis of the conjugate. 1-O-Gemfibrozil-beta-D-glucuronide was highly reversibly bound to albumin, with a mean unbound fraction of 0.028, and its degradation seemed to be related to the degree of reversible binding. Hydrolysis and covalent binding were associated with the site II binding domain on albumin, because only diazepam inhibited these reactions. However, intramolecular rearrangement was increased when binding to the site I domain was inhibited. Covalent binding was also detected in vivo to human plasma proteins. The half-life of the gemfibrozil-protein adducts was 2.5-3 days. Albumin plays an important role in the disposition of acyl glucuronides by acting as: i) a transporter protein; ii) a potential catalyst for their degradation and, therefore, clearance; and iii) a target for covalent adduct formation.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=9010630&dopt=Abstract
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