Cholesterol is a long chain polycyclic alcohol, usually called a steroid, that plays several structural and metabolic roles vitals to human biology. Body cholesterol is derived from two sources, de novo biosynthesis and diet and its metabolism homeostasis depend on absorption, synthesis and excretion mechanisms. Aging is a physiological process influenced by the interaction of multiple endogenous and exogenous factors and the genetic component characterized by loss of homeostasis that leads to changes in the biochemical composition of tissues, reduced adaptive responsiveness to environmental stimuli and increased susceptibility to disease. Various aspects of cholesterol metabolism, including its synthesis and excretion, are compromised in aging. Several studies indicate that serum cholesterol levels increase in adulthood but tend to decrease in the older adult. A trend of increase plasma cholesterol with aging was observed, namely low-density lipoprotein cholesterol, however in very old age a decrease in total cholesterol was observed that was associated with poor health and multi-morbidity. Appropriate prevention of chronic conditions such as cardiovascular disease and associated risk factors in older patients is becoming increasingly important to enable sustainable health care and maintain quality of life. Age and plasma cholesterol concentration are well-recognized cardiovascular risk factors, together with the wide availability of safe and effective pharmacological cholesterol lowering agents is assumed that the treatment is highly recommended for the older population, providing significant protection in these individuals. However, in this population there are other aspects to consider, such as age-related changes in pharmacokinetic and pharmacodynamic properties of drugs. Direct experimental evidence is very limited, especially in the older strata of the population.