Essay: Lovastatin And Tumor Necrosis Factor - An Overview.

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Discuss about the Lovastatin and Tumor Necrosis Factor.

Heart diseases are common. According to the University of Minnesota, John Hunter, a great physician in the eighteenth centurypainted the medical image of angina pectoris in order to explainhow suddendeaths occur. The account of coronary disorders, stroke, and sudden death can be traced back to ancient times and how specialists have treated it thoroughly from different disciplines(Means 2012). It is in this light that the following discussion will cover a widely used medicine to prevent heart attacks and diseases known as Lovastatin.

Lovastatin is scientifically known as(HMG-CoA) Hydroxymethylglutaryl-coenzyme A.It is a reductase and an enzyme that limits the rate in the cholesterol biosynthetic pathway. It also lowers the cholesterol in the body. This drug was the first HMG-CoA reductaseinhibitor that was used in treating hypercholesterolemia. This is aprescription drug available in the form of an immediate release tablet as well as extended release tablet. Lovastatin prescription is a combination therapy whereby it is accompanied together with weight loss, exercise, and diet, in order to decrease the menace of stroke and heart attack. In addition, it is used to moderate the quantity of cholesterol in the blood by slackening the production of cholesterol to cut a numberoffacts that may accumulate on the arterial walls and block the flow of blood to the heart, brains, and other parts of the body.

Lovastatin is administered in the evening. The drug is taken orally. This is a tradition that been followed by many physicians. This comes from the fact that cholesterol biosynthesis hepatic HMG-CoA reductase is highest at night and the half-life of statins is usually very short. Lovastatin has half-lives of sixhours or less. For maximum lowering of LDL, lovastatin has to be administered in the evening. This is important to exhibit these enzymes when they are mostly active. After carrying out a study, it was realized that when administering this drug in the evening there were high chances of reducing cholesterol than when compared to administering it during the day(Lewis 2014). Taking of statins in the morning can lead to the rise of cholesterol and low level of lipoprotein. Cholesterol levels are usually very high in the morning and are highest in the afternoon. For a patient who is mostly awake at night, the medication intake of lovastatin is carried after twelve hours of work. The drug should be taken as directed without taking more or less of it or often than the doctor’s prescription. The tablet should be swallowed whole without splitting, chewing or crushing it and a patient should only stop using the tablet after talking with his/her doctor. Many are times when medicine have allergic reactions on our bodies hence it is crucial to disclose allergies to certain medication or any ingredients in lovastatin. Therefore, it is very important for one to follow instructions when using the drug (Leibowitz 2010).When on lovastatin medication the patient should not tale alcohol , the patient should also avoid taking a lot of grapejuice, this is because the risks of the side effects can be increased. Lovastatin reduces the effects of the following drugs when taken together. These drugs include: ketoconazole, intraconazole, nefazodone, HIV inhibitors, blood thinners, some of cholesterol lowering drugs such as niacin and gemfibrozil. One should inform the doctor on the medication they are on to avoid such risks

Mechanism of Action

Lovastatin is hydrolyzed to lactone in vivo. In pharmacokinetics studies, the inhibition of HMG-CoA is usually the basis of this study. After lovastatin was administered orally in a man, .10% of this drug was in urine while 83% was excreted in feces. Excretion in feces indicates that the drug was absorbed and excreted in bile and the presence of theunabsorbed drug. The concentration of plasma of the lovastatin metabolites was high after 2 hours of dosage and declined to 10% after 24hours of dosage. After oral dosage, lovastatin highly selected the liver where it had high concentration than its target tissues. Lovastatin usually undergoes high selectivity of the liver where it was more concentrated than in the target tissues. Extensive first-pass extraction usually happens in the liver. There is also subsequent of the drug equivalent in the bile. Due totheextensive hepatic extraction of this drug, its availability to circulate as active inhibitor is very low. Lovastatin is highly bound to plasma proteins in humans. This drug crosses the placenta and blood-brain barriers. The most active metabolites in the human plasma are β-hydroxyacid of Lovastatin, and two other metabolites(Due and Wroblewski2013).

The liver usually controls hypercholesterolemia and Dyslipidemia. An increase of the LDL receptor can cause the decrease in the levels of cholesterol. Lovastatin is meant to inhibit HMG-CoA reductase.This is the enzymethatchanges HMG-CoA to mevalonic acid. The statin competes withthesubstrate in the active sites of the enzymes. Lovastatin works by stamping down fatty acids and cholesterol in the body. Reduction of this cholesterol can lead to the prevention of vascular disease, heart failure, and strokes. The statin works in the liver in order so as to prevent or inhibit HMG-CoA reductase. After discharging bad cholesterol from the liver, it is discharged in the blood artery vessels. Therefore, the lovastatin works to lower the cholesterol so that they fats cannot clog up the arteries (Herrick 2012).

Lovastatin is used in treating coronary heart diseases.It prevents both secondary and primary effects on the heart. The drug is used in managing cardiovascular risk in individuals with levels of plasma cholesterol that are normal. Lovastatin is also used in treating patients that have progressive renal diseases. Application of lovastatin has proved to slow renal function loss and in the prevention of cretonne clearance decline. Lovastatin is used in treating cancer. In the inhabitation of cell growth, the drug may be independent of Ras function. In the bone fraction treatment, it works by stimulating the formation of bones in vivo and invitro. When administered in long doses it leads to the healing of bone fractures. The drug is used in the inhibition of the nitric oxide (Riekes et al. 2017). Therefore, it is important for patients to use the drug only under the doctor’s prescription and the patient should stop using the drug incase the above side effect is experienced.

Lovastatin as a Therapy Drug

Lovastatin belongs to a therapy class. Lovastatin belongs to a class of therapy known as the statins. Statins are administered so as to reduce cholesterol that is found in the blood .This is done by blocking the enzyme that is required to make cholesterol.  It is used in treating heart diseases by lowering the cholesterollevel. It is not an anti-inflammatory drug.It is a therapy drug, which is associated with asymptomatic and mild elevations. These elevations are brought by higher dosage of lovastatin (Liu et al. 2017).

Just like most medical drugs, lovastatin has its own side effects, which are grouped into side effects that are common and side effects that are serious. The side effects that are common occur with the use of lovastatin areapain in the abdomen (stomach area), heartburn, nausea, headache, constipation, memory loss, confusion, insomnia, muscle pain and lack of energy in the body (Fye 2014). The serious side effects and their symptoms may include muscle problem where one experiences muscle pain, tenderness, and weakness. In addition, the drug leads to liver problems, which make one pass urine dark in color and yellowing skin, or eyes turn white.It also causes the problem of the central nervous system, which is characterized byalack of energy, weakness, and extreme tiredness. In addition, one may experience flu- like symptoms that are, body aches, fever, tiredness, cough, and hoarseness, also, bleeding problems may be experienced with symptoms like unusual bleeding and bruising (Joseph &Majd2012). Therefore, it is very important for patients using this drug to seek immediate medical attention if the above discussed side effects prolong.

References List

Joseph, L, &Majd, A 2012, 'A brief review: history to understand fundamentals of electrocardiography', Journal Of Community Hospital Internal Medicine Perspectives, Vol 2, Iss 1, Pp 1-5 (2012), viewed 30 March 2017. Retrieved from https://doaj.org/article/34c8a98d7c3e4a51a353c92ee7b31881

Fye, W. B. 2014. A history of the origin, evolution and impact of electrocardiography.

The American Journal of Cardiology 73 (13):937-949.

Herrick, J. B. 2012. Certain clinical features of sudden obstruction of the coronary arteries. Journal of the American Medical Association 27:100-116.

La Due, J. S., and F. Wroblewski. 2013. The significance of serum glutamic oxalacetic transaminase activity following acute myocardial infarction. Circulation 2:871-877.

Leibowitz, J. O. 2010. The history of coronary heart disease. Berkeley: University of California Press

Lewis, T.2014. Diseases of the heart. 4th ed. London: Macmillan.

Means, J. H. 2012. The Association of American Physicians: Its first seventy-five years. New York: McGraw-Hill.

Liu, P.C., Lu, G., Deng, Y., Wang, C.D., Su, X.W., Zhou, J.Y., Chan, T.M., Hu, X. and Poon, W.S., 2017. Inhibition of NF-κB Pathway and Modulation of MAPK Signaling Pathways in Glioblastoma and Implications for Lovastatin and Tumor Necrosis Factor-Related Apoptosis Inducing Ligand (TRAIL) Combination Therapy. PloS one, 12(1), p.e0171157.

Riekes, M.K., Dereymaker, A., Berben, P., Augustijns, P., Stulzer, H.K. and Van den Mooter, G., 2017. Development of enteric-coated fixed dose combinations of amorphous solid dispersions of ezetimibe and lovastatin: Investigation of formulation and process parameters. International journal of pharmaceutics, 520(1), pp.49-58.

Langert, K.A., Goshu, B. and Stubbs, E.B., 2017. Attenuation of experimental autoimmune neuritis with locally administered lovastatin?encapsulating poly (lactic?co?glycolic) acid nanoparticles. Journal of Neurochemistry, 140(2), pp.334-346.