Quote from: JoanneB on December 18, 2016, 09:44:17 AMIt's also best to take spiro after a little something to eat to avoid a grumbly tummy.
Food also increases its bioavailability.
Clin Pharmacol Ther. 1986 Nov;40(5):531-6."The mean (+/- SD) percent increase in AUC (0 to 24 hours) of spironolactone when it was given with food, compared with the ingestion on an empty stomach (95.4% +/- 66.9%), was much more pronounced than the corresponding increase of 7 alpha-thiomethylspirolactone (45.4% +/- 33.7%), 6 beta-hydroxy-7 alpha-thiomethylspiro-lactone (21.8% +/- 21.5%), and canrenone (40.7% +/- 26.3%). These observations indicate that food promotes the absorption of spironolactone and possibly decreases its first-pass metabolism."
Clin Pharmacol Ther. 1977 Jul;22(1):100-3."The influence of food intake on the bioavailability of canrenone, the major and active metabolite of spironolactone, was explored in 8 healthy male volunteers."
"The results indicate that more canrenone enters the general circulation when spironolactone in ingested together with a meal."
Canrenone is supposedly a weaker anti-androgen than spironolactone and since this study, other metabolites of Spiro have been found to have a major effect on the body and be responsible for much of its anti-mineralocorticoid effects.
QuoteI also do the spiro sub-lingually. It's a bit nasty at first but I readily got used to it as it dissolves quickly
Its bioavailability is already quite high, around 80-90% and even higher when taken with a meal. Why take it sublingually? Do you find a difference vs. orally? Reports of adverse effects of spironolactone on liver in humans are extremely rare. Spironolactone is even prescribed to individuals with liver cirrhosis.
Regarding spironolactone, taken once or twice daily...
Med J Aust. 1980 Feb 9;1(3):124-5."Once-a-day therapy with spironolactone has been compared with a twice-a-day regimen in an open crossover trial in patients with essential hypertension. When compared with placebo, both treatments significantly lowered blood pressure. Twice-a-day therapy provided slightly better blood pressure control than the once-a-day dosing schedule. There were only minor differences in biochemical findings between the two regimens. Three of the 17 patients developed reversible gynaecomastia."
Br J Clin Pharmacol. 1981 Oct; 12(4): 585–588."There was no indication of improved blood pressure control throughout the 24 h while receiving spironolactone in divided doses compared to the once a day regime. Previous studies of patients with mild hypertension maintained on a daily dose of (...) spironolactone have come to similar conclusions (Hennigsen, 1978; Ludbrook et al., 1980; Madwar, 1980)."
