Statins - Hypolipidaemic drugs, Summaries of Pharmacology

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STATINS

PRESENTED BY:- DIVYA (23045)

MODERATOR :- DR. ADITI

DR. HIMANSHU

agenda

INTRODUCTION

MECHANISM OF

ACTION

USES

SIDE EFFECTS

DRUG INTERACTIONS

STATINS INCLUDE :-

Lovastatin

Atorvastatin

Rosuvastatin

Pravastatin

Simvastatin

Pitavastatin

POTENCY OF STATINS

EFFICACY LDL-CH

REDUCTION (%)

NOTE

LOVASTATIN Low -

Moderate

20 –45 First clinically used statin

Lipophilic

Given orally in precursor

lactone form

Has maximum CNS

penetration

ATORVASTATI

N

High Upto 55 Long plasma half life (14-18hr)

Additional antioxidant

property

Most commonly used statin

ROSUVASTATI High Upto 55 Raises HDL-CH by 10-15%

ENHANCING YOUR PRESENTATION

MECHANISM OF ACTION

Statins competitively inhibit HMG-CoA reductase

enzyme in cholesterol biosynthesis

decrease Cholesterol synthesis

Increase LDL receptors in the Liver

Receptor mediated uptake and catabolism of LDL

Reduce plasma LDL levels

USES

Statins are commonly used drugs for treatment of :

o

Primary hyperlipidaemias

o

Secondary ( Diabetes Mellitus, Nephrotic

Syndrome ) hypercholesterolaemia

o

Atherosclerotic cardiovascular disease like

Myocardial infarction, angina, peripheral arterial

disease

o

Prophylaxis of Myocardial Infarction who already

had a attack.

o

Rosuvastatin is used post hip/knee replacement

Pleiotropic effect :- Plaque stabilization

Decrease endothelial dysfunction

Due to NO production

Anti-inflammatory

Reduce oxidative stress

Decrease platelet aggregation

DRUG INTERACTION

Gemfibro

zil

Inhibits

hepatic

uptake of

statins

By

Organic

anion

transport

er OATP

2

Statins x Nicotinic acid/ gemfibrozil/ CYP3A4 inhibitors –

Ketoconazole, Erythromycin, Cyclosporine, HIV protease

inhibitors

Inhibit metabolism of statins

Increased incidence of Myopathy and liver injury

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