Role of antioxidant property of carvedilol in mild to moderate hypertensive patients: A prospective open-label study.

OBJECTIVE: Carvedilol is a nonselective third generation β-blocker that does not display the negative effects of traditional β-blockers. Regarding the antioxidant, anti-inflammatory and distinct metabolic properties of carvedilol which are similar to that of high-density lipoprotein (HDL) and paraoxonase 1 (PON1), the present study intends to investigate the effects of carvedilol treatment on malondialdehyde (MDA) and soluble lectin-like ox-low-density lipoprotein (LDL) receptor (sLOX-1) as markers of oxidative stress in association to lipid profiles, apolipoproteins (apo), and PON1 activity in hypertensive patients.

PATIENTS AND METHODS: This clinical trial study was performed on forty patients with mild to moderate essential hypertension. Subjects were studied before and after 2 months treatment with carvedilol, 25 mg daily. Lipids and lipoproteins were measured using a biochemistry analyzer. PON and arylesterase activity were assayed using paraoxon and phenyl acetate as substrates, respectively. MDA was quantified using a chemical colorimetric assay. ELISA was used to measure sLOX-1.

RESULTS: Our results showed that carvedilol treatment decreased systolic and diastolic blood pressure as much as forty and 16 mmHg, respectively ( P < 0.001). It also increased HDL, total cholesterol, and serum PON1 activity ( P < 0.05), but the levels of triglyceride, LDL, apo A-I, and apo B did not significantly change. There was an inverse correlation between serum PON1 activity and serum MDA.

CONCLUSION: This study confirmed the antihypertensive effect of the drug and its beneficial metabolic effects through augmenting HDL and PON1 activity. We propose that the antioxidant effects of carvedilol can be partially attributed to increased PON-1 activity.