Kaletra leads to significant increases in some blood lipids in HIV-negative men

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A study involving HIV-negative men has found that taking Kaletra can result in significant increases in some blood lipids, and suggests that the metabolic effects of protease inhibitors are drug-specific rather than a class effect. The study is published in the March 5th edition of AIDS.

Investigators from the University of California, San Francisco, examined the impact of four weeks of Kaletra on the lipid profiles of ten HIV-negative men. The investigators conducted the study in HIV-negative men because they wished to see if it was treatment with Kaletra rather than factors associated with HIV infection which were causing lipid abnormalities in HIV-positive patients taking Kaletra and other protease inhibitors.

The men had a mean age of 43.8 years and had a confirmed negative HIV test result. They were admitted as in-patients for five days and were placed on a carefully controlled diet to minimise dietary effects on the metabolism. They were then discharged and provided with four week's supply of Kaletra, and were instructed to eat their normal diet and engage in their normal exercise habits. After four weeks of Kaletra they were again admitted for blood tests and other examinations.

Glossary

glucose

A simple form of sugar found in the bloodstream. All sugars and starches are converted into glucose before they are absorbed. Cells use glucose as a source of energy. People with a constant high glucose level might have a disease called diabetes.

p-value

The result of a statistical test which tells us whether the results of a study are likely to be due to chance and would not be confirmed if the study was repeated. All p-values are between 0 and 1; the most reliable studies have p-values very close to 0. A p-value of 0.001 means that there is a 1 in 1000 probability that the results are due to chance and do not reflect a real difference. A p-value of 0.05 means there is a 1 in 20 probability that the results are due to chance. When a p-value is 0.05 or below, the result is considered to be ‘statistically significant’. Confidence intervals give similar information to p-values but are easier to interpret. 

metabolism

The physical and chemical reactions that produce energy for the body. Metabolism also refers to the breakdown of drugs or other substances within the body, which may occur during digestion or elimination.

cholesterol

A waxy substance, mostly made by the body and used to produce steroid hormones. High levels can be associated with atherosclerosis. There are two main types of cholesterol: low-density lipoprotein (LDL) or ‘bad’ cholesterol (which may put people at risk for heart disease and other serious conditions), and high-density lipoprotein (HDL) or ‘good’ cholesterol (which helps get rid of LDL).

lipid

Fat or fat-like substances found in the blood and body tissues. Lipids serve as building blocks for cells and as a source of energy for the body. Cholesterol and triglycerides are types of lipids.

The investigators found that after four weeks of Kaletra treatment, fasting triglycerides increased three-fold (0.89 mmol/l at baseline to 1.63 mmol/l, p=0.007), that levels of VLDL cholesterol increased by a third (0.39mmol/l at baseline to 0.53mmol/l, p=0.05), and that free fatty acids (0.33mmol/l at baseline to 0.43mmol/l, p=0.001) also increased significantly.

No significant change was seen in LDL, HDL, or total cholesterol levels, nor in blood levels of fasting glucose levels, insulin, or insulin resistance. However, a two-hour oral glucose tolerance test revealed that there was an increase in glucose (p=0.05) and insulin (p=0.04) levels.

No changes in body shape were observed.

The investigators attribute the increase in triglycerides to ritonavir, and they note that increased VLDL production is thought to be involved in the mechanism associated with triglyceride elevation.

Elevated LDL cholesterol is seen in HIV-positive patients taking a protease inhibitor-containing HAART regimen. However, this was not seen in the ten HIV-negative men in this study, leading the investigators to speculate that increased LDL cholesterol in HIV-positive patients could be due to improving health or because of an interaction between HIV and HAART. The investigators admit to being uncertain if the mild impairment of glucose tolerance revealed by the two-hour glucose tolerance test was of any clinical significance.

The investigators also compared their results to a similar study involving the use of indinavir in HIV-negative individuals. They noted that indinavir had little effect on lipids in HIV-negative individuals, but significantly increased insulin resistance. They conclude that the metabolic effects of protease inhibitors appear to be “drug specific, not class specific.”

Further information on this website

Lopinavir - overview

Body fat and metabolic changes on treatment - menu

Lipodystrophy - factsheets

References

Grace AL et al. The metabolic effects of lopinavir/ritonavir in HIV-negative men. AIDS 18: 641 – 649, 2004.