Atorvastatin

Atorvastatin was the best-selling drug for lowering lipid level in early 2000s, this drug

has role in lowering Cholesterol level in the blood, and increase the blood level of good

Cholesterol. the available dose in pharmacy is called atorvastatin calcium in tablet form.

(kogawa., etal 2019). Atorvastatin is one of the statin family and widely used in USA,

Atorvastatin is the prototype of the class of drug that is called hydroxymethylglutaryl -Coenzyme

A (HMG-COA) reductase inhibitors or statin. this drug acts on decreasing the level of the bad

Cholesterol which is LDL and VLDL Cholesterol, in addition to triglycerides.it takes two weeks

to reduce the level of LDL and the maximal effect of decreasing LDL happen within 4-6 weeks,

about HDL which is good Cholesterol it may still the same level that the patient has or it may

increase (Frandsen, G., & Pennington,2018).

Pharmacokinetics and pharmacodynamic

Atorvastatin is absorbed directly after administration, reaching the peak plasma level

within four hours, the time need and extent of atorvastatin for absorption is affected by the time-

of-day administration, in addition Food intake while taking the atorvastatin will decrease its

effect, Metabolism occurs in the liver and the major forms after metabolism are 2-hydroxy- and

4-hydroxy-atorvastatin acid , the excretion of Atorvastatin is via bile after is metabolized by the

liver , so if the patient have liver disease it must be administered with caution . Atorvastatin is

metabolized to 2-hydroxy- and 4-hydroxy-atorvastatin acid by (CYP450) family of enzymes,

composed of over 30 isoenzymes and this enzyme that is responsible for metabolism is the

reason for increasing the drug-to-drug interaction and problem with certain foods. (Schachter, M.

(2005).
 Indication and Clinical implications

Atorvastatin is used to treat Hypercholesterolemia so it will decrease the risk of

developed cardiovascular morbidity and mortality in patient with or without history of

cardiovascular disease. (Bellosta, S., Paoletti, R., & Corsini,. (2004). Atorvastatin is used with

adjunct to diet and life style modification for decreasing the risk of MI, CVA, angina and in DM

patients who don’t have cardiovascular disease to prevent develop of cardiovascular diseases in

those patients. That is related to patient with Type 2 DM has high opportunity to develop

atherosclerotic disease related to increase the risk factor to happen like Hypertension and hyper

dyslipidemia, this is Characterized by increasing in LDL, triglycerides and low level of HDL. (,

Ginsberg, H.,et al 2010).

Drug dose

Atorvastatin used In Conjunction with life Style modification like Diet with low fat and

increase the Activity level, and based on Age, baseline LDL, Cholesterol level, if there is history

of Atherosclerosis cardiovascular diseases, based on patient other medications we can select if

there is need to use atorvastatin for this patient or not,Statin therapy classified according to the

level of LDL to three types: high intensity, moderate and low intensity, Atorvastatin used in high

intensity with the dose of 40 -80 mg/day generally LDL reduced by more than50%, in case of

moderate intensity statin therapy Atorvastatin 10-20 mg/day this dose decreases the LDL by

30%-49%, the response of the dose monitored every 1-3 months. (stone.,et al 2014).

Side effect:
 In patient on statin there is Suspension to increase the level of fasting serum glucose

concentration and glycosylated hemoglobin so the risk to develop DM is high. (FDA.2012).

Atorvastatin is associated with increase the risk for develop liver injury and sometimes has sever

hepatotoxicity and it leads to fatal outcomes at the end (Björnsson,2017). The Clinical picture of

liver injury induced by Statin happen after many months or years after imitation of statin, the

Clinical presentation for Statin induced Liver injury include Cholestatic, there is suspension to

develop autoimmune Hepatitis positive histology, and raised serum immunoglobulin level

(Russo et al.,2014). Statin induced myopathy may happen that is related to FDA definition is

unexplained muscle pain or weakness when the Creatinine Kinase concentration is more than 10

times of upper limit of normal range, the sever form of Myopathy induced by Statin is

Rhabdomyolysis when the Creatinine Kinase is more than 40 times of the upper limit of Normal

range which require hospitalization and may muscle Fiber necrosis happen. (Newman., et al

2019).

Contraindications

Atorvastatin contraindications include patients with hypersensitivity to any of its

components, in addition it is Contraindicated in pregnant women according to FDA

categorization of statin as X drugs. (Zarek & Koren 2014).

Drug -drug interaction:

In related to drugs that increase the risk of rhabdomyolysis which is one of the important

side effects to avoid, Cyclosporine increases the risk of rhabdomyolysis, that inhibits the uptake

and metabolism. (Carter et al.,2019). in addition, patient with coronary heart disease or heart
failure may take different drug to manage the Symptoms of disease one of the drugs that if it

given with Atorvastatin, it will increase the side effect Rhabdomyolysis is Sacubitril /Valsartan

with Atorvastatin. (Siew.,at al 2022).

Atorvastatin approval and Cost:

On November 30,2011 the FDA approved Atorvastatin to trat hypercholesterolemia, the

first trade name for Atorvastatin is Lipitor, with best selling that reached more than 125$ Billion

in 1997, the price in USA is around 11$ for a supply of 15 tab of 20 mg, in Jordan related to the

Jordan food drug administration the average price is around 31 JD.

Toxicity:

The risk of Atorvastatin Toxicity increases in patient with Liver disease, Atorvastatin is not

preferred to be used in liver disease patient that is way this drug metabolized in liver so there will

be histological and biochemical Changes in liver. In Comparison between Atorvastatin and

Pitavastatin the result Shows that patient on Atorvastatin has an increasement in ALT and AST

levels those enzymes reflect the liver Function, this is due to Atorvastatin is taken up by liver

more Selectively and efficiently in Comparison with another Statin. (Al-kareem et al.,2020).

Nursing Implications and patient teaching:

One of the advantages of Atorvastatin over other statin that is safe on renal system, but there is

risk to develop liver injury so there is importance to monitor the liver Functions test, Lipid panel

and liver function test must be taken as baseline before starting on Atorvastatin, and lipid panel
teat taken again after 6 weeks of therapy and after that it taken every 6 to 12 months, the

adherence of the Atorvastatin is the key to lowering lipids and preventing the cardiovascular

event , in addition to Atorvastatin it is very important to lifestyle modification in treating

hyperlipidemia , that is include eating healthy diet, losing weight ,increase physical activity

(Lindsey &. Siddique.2022).

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