Fall, 2021

LET'S TALK
STATINS
Gwendoline Balto
Esther Birkey
Iulia Ciubotariu
Sophia Cook
Presentation Overview
Introduction to the drug Excretion

Absorption Risks

Distribution Summary
 Introduction
What is this drug?
3,5-dihydroxyglutaric acid moiety
Substituents on the ring define
solubility and properties=various
forms
 Introduction
What does this drug do?
Blocks the active site of HMG-CoA
reductase which blocks the STATINS
conversion of HMG-CoA to
mevalonic acid = reduction in
hepatic cholesterol synthesis
Question
How do statins reduce cholesterol?
A.) Because cholesterol is an essential nutrient, statins only
remove small chunks of cholesterol particles from the
circulatory system

B.) Increases absorption of dietary cholesterol in the small

intestine

C.) Stops the production of cholesterol by blocking an enzyme

that makes cholesterol, which results in lower cholesterol
levels in the blood

D.) None of the above

 If the individual LDL cholesterols
has had a heart is 190 mg/dL or
attack higher
Who is
recommended
to take statin
medication?
40-75 with 40-75 with risk
diabetes and factors and an
LDL cholesterol LDL cholesterol
of 70 mg/dL or level of 70
higher mg/dL or higher
How many
people
take
statins?
over 200
million
globally
Why do so 23% reduction in heart
attacks
many
17% reduction in fatal or non-
people fatal stroke
take this 19% reduction in death from
cardiovascular causes
drug? 12% reduction in all-cause
It's effective! mortality
Statin
Dropped to $12.2
Market billion in 5 years.
Value
Biggest threat =
$19.7 billion generic variants
(2012)
 The History of Statins

1950s 1976 1987

Cholesterol
becomes an First statin FDA approved
obvious risk discovered by
Akira Endo
Statin Medications
Water solibility
Affects Affects

Similarities
chemical structure
pharmacokinetic profile
lipid motility efficacy

Mechanisms of Absorption Excretion

functioning in the
body Distribution
Differences Metabolism
 Absorption and Food

Different statin medications have different absorption rates.

Some should be taken before eating and some should be taken

with food. This will help make the medication more bioavailable.

An individual should check the medication’s instructions

Absorption
Intestinal lumen

Enterocyte

Bloodstream

Hepatocytes
Absorption

Absorbed through active and passive

transport in the intestinal cell
More hydrophilic medications enter the
liver cells through active transport
Less hydrophilic medications enter the
cell through passive diffusion
Distribution

Selectively distributed by the liver

Some statins can directly enter cells
Other statins inhibit P-glycoprotein
Hydrophillic nature of drug prevents wide
distribution across tissues
 Elimination
The main pathway of elimination is ABC transporter
mediated biliary excretion.

Excretion is related to the hydrophilicity of the

medication
More hydrophilic medications enter the liver cells
through active transport and are excreted mostly by
the kidney
Less hydrophilic medications enter the cell through
passive diffusion and are and excreted mostly in the
liver
Risks
There is an increased risk of developing Type 2
Diabetes.

Some people complain of muscle issues.

Gastrointestinal hemorrhage

Typically, the risks of taking statins are low and the

benefits of taking the medication far outweigh the
potential risks.
Summary
Statins help a lot of people by reducing their
cholesterol levels, which in turn reduces risk of
cardiovascular diseases and the rate of mortality.

The benefits of statins far outweigh the negative

side effects and there is a low risk of serious
complications.