Human in vivo competitive inhibition of P450 substrates: increased plasma concentrations as a function of hepatic extraction ratio and percent inhibition.

نویسنده

  • H Boxenbaum
چکیده

The purpose of this note is to posit and discuss the concept of "competitive inhibition potential" (CIP), which is an in vivo index of the ability of a competitive inhibitor to elevate plasma concentrations of drug substrates, when the competitive inhibitor is administered at its usual and customary dose.

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

Cytochrome P450 3A4 in vivo ketoconazole competitive inhibition: determination of Ki and dangers associated with high clearance drugs in general.

Assuming complete hepatic substrate metabolism and system linearity, quantitative effects of in vivo competitive inhibition are investigated. Following oral administration of a substrate in the presence of a competitive inhibitor, determination of the inhibition constant (Ki) is possible when plasma concentration-time profiles of both substrate and inhibitor are available. When triazolam is the...

متن کامل

In Vitro Inhibition of Human Sperm Creatine Kinase by Nicotine, Cotinine and Cadmium, as a Mechanism in Smoker Men Infertility

Background Nicotine, cotinine and cadmium are harmful components of cigarettes that have an effect on human reproductive function. Although the effects of cigarette smoke on male reproductive function is characterized in several articles its mechanism of action is still unknown. In the present study, we investigate the effect of nicotine, cotinine and cadmium on human sperm creatine kinase acti...

متن کامل

Dmd053991 2166..2174

Plasma concentrations of orally administered methadone are reduced by the human immunodeficiency virus protease inhibitor combination ritonavir and lopinavir, but the mechanism is unknown. Methadone metabolism, clearance, and drug interactions have been attributed to CYP3A4, but this remains controversial. This investigation assessed the effects of acute (2 days) and steady-state (2 weeks) rito...

متن کامل

Paraoxonase Inhibition by Propranolol

There are many evidences that human serum paraoxonase activity modifies plasma lipid profile and paraoxonase has an antiatherogenic property. Non-selective beta-blockers affect plasma lipid profile too, but they have atherogenic property when patients take these drugs in long term. In this study the effect of propranolol, a non-selective beta-blocker, on paraoxonase activity was investigated. L...

متن کامل

Paraoxonase Inhibition by Propranolol

There are many evidences that human serum paraoxonase activity modifies plasma lipid profile and paraoxonase has an antiatherogenic property. Non-selective beta-blockers affect plasma lipid profile too, but they have atherogenic property when patients take these drugs in long term. In this study the effect of propranolol, a non-selective beta-blocker, on paraoxonase activity was investigated. L...

متن کامل

ذخیره در منابع من


  با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

عنوان ژورنال:
  • Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques

دوره 2 3  شماره 

صفحات  -

تاریخ انتشار 1999