In a randomized, crossover study, the absorption, distribution, and elimination of intravenous and oral felodipine were investigated in eight healthy men 22 to 31 years old. Felodipine was given as a 2.5 mg iv infusion over 30 minutes and as a 27.5 mg oral solution. Both doses were labeled with 25 microCi 14C-felodipine. Given as an oral solution, felodipine is rapidly (mean time to peak concentration 64 minutes; range 30 to 90 minutes) and completely absorbed. Presystemic elimination reduced the availability to 16% (range 10% to 25%). Felodipine kinetics can be described by a multicompartmental model with three distinct phases. The t1/2 for the initial phase was 6.4 minutes (range 1.7 to 10.4 minutes) and felodipine was distributed to a volume of 0.6 L/kg (range 0.4 to 0.9 L/kg), which approximately corresponds to the total body water. The second distribution phase reached pseudoequilibrium with a t1/2 of 1.6 hours (range 1.3 to 2.2 hours). The volume of distribution at the end of this phase was 9.7 L/kg (range 6.0 to 18.2 L/kg). The terminal phase had t1/2 of 10.2 hours (range 6.7 to 20.7 hours). The contribution of the three phases to the AUC was 15%, 40%, and 45% in the order of increased t1/2. Total body clearance of felodipine was 1.2 L/min (range 0.9 to 1.6 L/min). Within 72 hours after drug dosing, 62% to 81% of the felodipine doses were excreted in the urine and feces as metabolites. The rate of excretion by the kidneys had a biphasic pattern, with t1/2 values of 4 and 18 hours. Approximately 10% of the doses was excreted in the feces.

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Sex hormones are suggested to influence energy intake (EI) and metabolic hormones. This study investigated the influence of menstrual cycle (MC) and hormonal contraceptive (HC) cycle phases on EI, energy availability (EA), and metabolic hormones in recreational athletes (eumenorrheic, NHC = 15 and monophasic HC-users, CHC = 9). In addition, 72-h dietary and training logs were collected in addition to blood samples, which were analyzed for 17β-estradiol (E2), progesterone (P4), leptin, total ghrelin, insulin, and tri-iodothyronine (T3). Measurements were completed at four time-points (phases): Bleeding, mid-follicular (FP)/active 1, ovulation (OVU)/active 2, mid-luteal (LP)/inactive in NHC/CHC, respectively. As expected, E2 and P4 fluctuated significantly in NHC (p < 0.05) and remained stable in CHC. In NHC, leptin increased significantly between bleeding and ovulation (p = 0.030) as well as between FP and OVU (p = 0.022). No group differences in other measured hormones were observed across the MC and HC cycle. The mean EI and EA were similar between phases, with no significant differences observed in macronutrient intake over either the MC or HC. While the MC phase might have a small, but statistically significant effect on leptin, the findings of the present study suggest that the MC or HC phase does not significantly alter ad libitum EI or EA in recreational athletes.

Purpose: The aim of this study was to investigate within-cycle differences in nocturnal heart rate (HR) and heart rate variability (HRV) in naturally menstruating women (NM) and women using combined hormonal contraceptives (CU) or progestin-only hormonal contraceptives (PU). Methods: Physically active participants were recruited into three groups: NM (n = 19), CU (n = 11), and PU (n = 12). Participants' HR and HRV (with Bodyguard 2 HRV monitor) and blood hormones were monitored during one menstrual cycle (MC) (NM group) or for 4 wk (CU and PU groups). Estradiol, progesterone, and luteinizing hormone were analyzed from fasting blood samples collected four times in the NM (M1 = bleeding, M2 = follicular phase, M3 = ovulation, and M4 = luteal phase) and PU groups (M1 = lowest E 2 , M2 = M1 + 7 d, M3 = M1 + 14 d, and M4 = M1 + 21 d) and twice in the CU group (active and inactive pill phases). After every blood sample, nightly HR and HRV were recorded and examined as an average from two nights. Results: Hormonal concentrations differed (P < 0.05) between MC phases in the NM and PU groups, but not (P ≥ 0.116) between the active and the inactive phases in the CU group. In the NM and PU groups, some of the HRV values were higher, whereas in the NM group, HR was lower during M2 compared with M3 (P < 0.049) and M4 (P < 0.035). In the CU group, HRV values (P = 0.014-0.038) were higher, and HR was lower (P = 0.038) in the inactive phase compared with the first week of the active phase. Conclusions: The MC and the hormonal cycle phases influence autonomic nervous system balance, which is reflected in measurements of nocturnal HR and HRV. This should be considered when monitoring recovery in physically active individuals.