This video is about Raloxifene
Welcome to our video on raloxifene where we will be discussing the motive side of action routes of exposure administrations and of course adme our first topic will be pharmacokinetics absorption so relax a fitness administered orally 60 to 150 milligrams per day it is then rapidly absorbed in the gastrointestinal tract in this concentration time graph the
Absolute bioavailability is 2% and ranges from 1.3 to 2.7 percent it has a relatively long t max and low bioavailability to inter conversion of reversible systemic metabolism and entró hepatic cycling of firlock season and the metabolites and there’s an increased absorption by the administration of a high-fat meal now we’re on distribution rollag – is extensively
Distributed after oral administration the volume of distribution is 2348 liters per kilogram for a dose of 30 to 150 milligrams this means that most of the drug is distributed to the organ tissue 95% is bound to the human plasma protein also known as alpha acid glycoprotein and albumin however it does not find to the sex hormone-binding globulin and now we’re on to
Metabolism raloxifene has an extensive first pass glucuronidation you can say the liver is a champion and here i’m drawing the structure of the raloxifene for prime glue quran i’d which predominates in this case along with that the six for prime glue quran i’d and the six prime glue quran i’d was also detected raloxifene does not undergo a briar transformation by the
Cytochrome p450 system and now finally excretion total plasma clearances attributed to karana dacian 5% is excreted from the kidney while 90% or more is extruded through feces within five days the plasma elimination half-life is twenty seven point seven hours and the oral clearance is forty four point one liters per hour and it ranges from 40 to 60 liters per hour
Five percent is excreted in the urine as glue quran id conjugates and less than 0.2% of experiences unchanged drug sing aunty pharmacodynamics so we’ll be talking about osteoporosis and the mechanism first so that’s a dissolved material the plasma protein being drawn it’s gonna go through now i’m drawing the raloxifene er and transcription factor so transcription
Is initiated and that results in an increased intracellular specific protein expression resulting in increased bone mineral density increased anti-thyroid genetic activity and increase venous thromboembolism or talking about breast cancer the transcription is repressed which results in lower endometrial tissue and decreased breast cell proliferation and this is
Just to conclude all the positive effects of raloxifene for both breast cancer and osteoporosis and now we will be comparing to breast cancer drugs and the criteria used for choosing one over the other based on individual patient cases so sponge bob will represent raloxifene and squidward tamoxifen so here is a risk criteria premenopausal versus postmenopausal
Starring kim kardashian here but we will be focusing on pre menopausal first of a pre menopausal if you have a history of blood clots then you go away from tamoxifen otherwise choose tamoxifen and then if you’re postmenopausal you go through with this chart and the ser m refers to the relax of in and the risk criteria continues and that concludes this video thanks for watching
Transcribed from video
Raloxifene By Shanu Bhandari