BACKGROUND: Eplerenone is a selective mineralocorticoid receptor antagonist which effectively blocks mineralocorticoid receptors in various tissues throughout the body. The addition of eplerenone to optimal medical therapy reduces morbidity and mortality among patients post acute myocardial infarction complicated by left ventricular dysfunction and heart failure. The aim of this study was to evaluate pharmacokinetic characteristics and tolerability after multiple oral administration of eplerenone 100 mg for 7 days in healthy Korean volunteers. METHODS: A double-blind, randomized, placebo-controlled, parallel study was conducted in 22 healthy Korean subjects. Healthy males and females between age of 20 and 55 years were enrolled. Each subject received 100 mg eplerenone (N=16) or placebo (N=6) for 7 days. Blood samples for pharmacokinetic parameter determination on day 7 were collected pre-dose and up to 36 hours after last drug administration. Adverse events were reported throughout the treatment period. RESULTS: The steady-state concentration of eplerenone reached after multiple administration of eplerenone 100 mg for 7 days. The mean eplerenone Cmax of 1620.1 ng/mL was obtained at 1.0 hour (range 0.5 to 2 hours). The mean AUC0-24h,ss at day 7 was 8763.6 ng/mL*h. The mean oral clearance and mean terminal half-life of eplerenone were 13.0 L/h and 3.4 hours. There were some drug-related mild adverse events after eplerenone administration, but all adverse events recovered without any treatment. CONCLUSION: In this study, the pharmacokinetic parameters after multiple oral doses of eplerenone 100 mg for 7 days were evaluated and eplerenone at these doses were well tolerated in healthy Korean subjects.
Administration, Oral ; Female ; Half-Life ; Heart Failure ; Humans ; Male ; Myocardial Infarction ; Receptors, Mineralocorticoid ; Spironolactone ; Ventricular Dysfunction, Left

OBJECTIVETo observe the clinical efficacy of Chibixiao Recipe (CBX) in combination with minocycline and spironolactone in treating rosacea in females.

METHODSSixty-eight women with rosacea were randomly assigned to the treated group (48 cases) and the control group (20 cases), both of which were treated with minocycline and spironolactone taken orally, but to the treated group, the Chinese herbal recipe, CBX was given additionally. Besides, cryotherapy with liquid nitrogen was applied to those with apparent capillary dilatation. The therapeutic course for both groups was 8 weeks. The levels of serum testosterone before and after treatment were determined by radioimmunoassay (RIA), and a 4-month follow-up was conducted.

RESULTSIn the treated group the cure-markedly effective rate was 87.5% and the recurrent rate was 6.5%, while in the control group, they were 45.0% and 41.2% respectively. Comparisons in the indexes between the two groups all showed significant difference (both P<0.01), with the cure-markedly effective rate higher, and the recurrent rate lower in the treated group. The serum level of testosterone got lowered in both groups ( P<0.05 and P<0.01), but the lowering in the treated group was more significant, showing significance when compared with that in the control group ( P<0.01).

CONCLUSIONCBX in combination with Western medicine has effect in treating rosacea superior to that of Western medicine alone, and could effectively reduce recurrent rate and the serum level of testosterone. female rosacea, testosterone, Chibixiao Recipe, minocycline, spironolactone

Adult ; Drug Therapy, Combination ; Female ; Humans ; Medicine, Chinese Traditional ; Middle Aged ; Minocycline ; administration & dosage ; Recurrence ; Rosacea ; blood ; drug therapy ; Spironolactone ; administration & dosage ; Testosterone ; blood

NAD(P)H oxidase plays an important role in hypertension and its complication in aldosterone-salt rat. We questioned whether NAD(P)H oxidase subunit expression and activity are modulated by aldosterone and whether this is associated with target- organ damage. Rats were infused with aldosterone (0.75 microgram/hr/day) for 6 weeks and were given 0.9% NaCl+/-losartan (30 mg/kg/day), spironolactone (200 mg/kg/ day), and apocynin (1.5 mM/L). Aldosterone-salt hypertension was prevented completely by spironolactone and modestly by losartan and apocynin. Aldosterone increased aortic NAD(P)H oxidase activity by 34% and spironolactone and losartan inhibited the activity. Aortic expression of the subunits p47(phox), gp91(phox), and p22(phox) increased in aldosterone-infused rats by 5.5, 4.7, and 3.2-fold, respectively, which was decreased completely by spironolactone and partially by losartan and apocynin. Therefore, the increased expression of NAD(P)H oxidase may contribute to cardiovascular damage in aldosterone-salt hypertension through the increased expression of each subunit.
Acetophenones/administration & dosage ; Aldosterone/administration & dosage/*toxicity ; Aldosterone Antagonists/administration & dosage ; Angiotensin II Type 1 Receptor Blockers/administration & dosage ; Animals ; Anti-Inflammatory Agents, Non-Steroidal/administration & dosage ; Aorta/metabolism/pathology ; Blood Pressure/drug effects ; Hypertension/chemically induced/drug therapy/*enzymology ; Kidney/metabolism/pathology ; Losartan/administration & dosage ; Male ; NADPH Oxidase/antagonists & inhibitors/*metabolism ; Organ Size ; Oxidative Stress ; Protein Subunits/metabolism ; RNA, Messenger/metabolism ; Rats ; Rats, Sprague-Dawley ; Sodium Chloride/administration & dosage ; Spironolactone/administration & dosage ; Superoxides/metabolism