USE OF STATINS IN MI

PRESENTED BY PHARM. MAMZA JOSHUA3rd, OCT., 2014

Myocardial infarction also known as Heart attack is a medical condition that occurs when blood stops flowing properly to a part of the heart

Usually this is because one of the coronary arteries that supplies blood to the heart develops a blockage due to an unstable buildup of white blood cells, cholesterol and fat. 

OVERVIEW OF MYOCARDIAL INFARCTI ON

Chest painDypsnoea Diaphoresis, weakness, light-

headedness, nausea, vomiting, and palpitations

Loss of consciousnessSudden death

SIGNS AND SYMPTOMS

The most common triggering event is the disruption of an atherosclerotic plaque in an epicardial coronary artery, which leads to a clotting cascade, sometimes resulting in total occlusion of the artery

Atherosclerosis is the gradual buildup of cholesterol and fibrous tissue in plaques

PATHOPHYSIOLOGY

PATHOPHYSIOLOGY cont.

Lovastatin Simvastatin Pravastatin Atorvastatin Fluvastatin Rosuvastatin Mevastatin Cerivastatin 

STATINS EXAMPLES OF DRUGS UNDER THIS CLASS

MECHANISM OF ACTION

MECHANISM OF ACTION cont.

SAR

SAR cont.

BreastfeedingHigh alcohol intakeMyopathy Increase in liver enzymesActive liver disease or persistent

abnormal liver function testPregnancy

PRECAUTIONS AND CONTRAINDICATION

RhabdomyolysisKidney injuryLiver damageNeuropathyMemory defectsAcceleration of ageing Infection and CancerDiabetes Increase in liver enzymes

ADVERSE DRUG REACTION

Taking a statin drug with amiodarone, clarithromycin, cyclosporine, erythromycin, fluconazole, gemfibrozil, itraconazole, ketoconazole, or niacin increases the risk of myopathy or rhabdomyolysis

Lovastatin, rosuvastatin and simvastatin may increase the risk of bleeding when administered with warfarin

INTERRACTIONS

Most of the statins (lovastatin, simvastatin, and atorvastatin, ) are metabolized by the cytochromal P450 3A4. Drugs that inhibit P450 3A4, such as itraconazole, cyclosporine, and erythromycin, increases plasma statin level

Grapefruit juice can inhibit intestinal metabolism of the statins and can result in an increase in artovastatin, lovastatin, and simvastatin serum levels.

INTERRACTIONS cont.

Co-administration of fluvastatin with warfarin increases warfarin toxicity, because they are both metabolised by cytochrome P450 2C9

food increases the bioavailability of lovastatin Conversely bioavailability of pravastatin,

atorvastatin, and fluvastatin is decreased by food

INTERRACTIONS cont.

SIGNIFICANCE OF CHOLESTEROL LEVEL

Statin equivalent dosages

% LDL reduction (approx.)

Atorvastatin Fluvastatin Lovastatin Pravastatin Rosuvastatin Simvastatin

10–20% – 20 mg 10 mg 10 mg – 5 mg

20–30% – 40 mg 20 mg 20 mg – 10 mg

30–40% 10 mg 80 mg 40 mg 40 mg 5 mg 20 mg

40–45% 20 mg – 80 mg 80 mg 5–10 mg 40 mg

46–50% 40 mg – – – 10–20 mg 80 mg*

50–55% 80 mg – – – 20 mg –

56–60% – – – – 40 mg –

* 80-mg dose no longer recommended due to increased risk of rhabdomyolysis

Starting dose

Starting dose 10–20 mg 20 mg 10–20 mg 40 mg 5–10 mg 20 mg

If higher LDL reduction goal

40 mg if >45%

40 mg if >25%

20 mg if >20%

-- 20 mg if LDL >190 mg/dL (4.87 mmol/L)

40 mg if >45%

Optimal timing

Anytime Evening With evening meals

Evening Anytime Evening

DOSES

Primary prevention: prevention of heart disease in those with high cholesterol

Secondary prevention: decreasing mortality in people with pre-existing CVD

Familial hypercholesterolemia In children: statins are effective at reducing their cholesterol level when lifestyle changes are not enough

Meanwhile statins in children should be started at age 8

INDICATIONS

Researchers hypothesize that statins prevent cardiovascular disease via four proposed mechanisms

Improve endothelial functionModulate inflammatory responsesMaintain plaque stabilityPrevent thrombus formation

OTHER EFFECTS OF STATINS

Oyster mushroomRed yeast riceFish oilFlax seeds

OTHER SOURCES OF STATINS

The statins that produce the greatest percentage change in LDL cholesterol levels are atorvastatin and simvastatin

Atorvastatin and fluvastatin are least affected by alterations in renal function

Fewer pharmacokinetic drug interactions are likely to occur with pravastatin and fluvastatin, because they are not metabolized through the cytochrome P450 (3A4) system

The most cost-effective statins, based on cost per percentage change in LDL cholesterol levels, are fluvastatin and atorvastatin

IMPORTANT THINGS TO NOTE

CIPRIDE: Simvastatin tablet 10mg, marketed by VIXA Pharmaceutical

LIPIVASTIN: Atorvastatin tablet 10mg, marketed by NEROS Pharmaceutical

STATINS STOCKED IN THE HOSPITAL

THANK YOU!

THANK YOU!!

THANK YOU!!!