This is in contradiction with widespread statements that spironolactone increases free estradiol levels by displacing estradiol from SHBG.Spironolactone appears to cross the blood–brain barrier. Metabolism
Spironolactone is rapidly and extensively metabolized in the liver upon oral administration and has a very short terminal half-life of 1.4 hours. The major metabolites of spironolactone are 7α-thiomethylspironolactone (7α-TMS), 6β-hydroxy-7α-thiomethylspironolactone (6β-OH-7α-TMS), and canrenone (7α-desthioacetyl-δ6-spironolactone). These metabolites have much longer elimination half-lives than spironolactone of 13.8 hours, 15.0 hours, and 16.5 hours, respectively, and are responsible for the therapeutic effects of the medication. As such, spironolactone is a prodrug. The 7α-thiomethylated metabolites of spironolactone were not known for many years and it was originally thought that canrenone was the major active metabolite of the medication, but subsequent research identified 7α-TMS as the major metabolite. Other known but more minor metabolites of spironolactone include 7α-thiospironolactone (7α-TS), which is an important intermediate to the major metabolites of spironolactone, as well as the 7α-methyl ethyl ester of spironolactone and the 6β-hydroxy-7α-methyl ethyl ester of spironolactone.Spironolactone is hydrolyzed or deacetylated at the thioester of the C7α position into 7α-TS by carboxylesterases. Following formation of 7α-TS, it is S-oxygenated by flavin-containing monooxygenases to form an electrophilic sulfenic acid metabolite. This metabolite is involved in the CYP450 inhibition of spironolactone, and also binds covalently to other proteins. 7α-TS is also S-methylated into 7α-TMS, a transformation catalyzed by thiol S-methyltransferase. Unlike the related medication eplerenone, spironolactone is said to not be metabolized by CYP3A4. However, hepatic CYP3A4 is likely responsible for the 6β-hydroxylation of 7α-TMS into 6β-OH-7α-TMS.
The FDA warns against use in people with a history of uncontrolled seizure disorders and cautious use in infants, children, the elderly, and individuals with other skin conditions (e.g., atopic dermatitis, psoriasis) and in those who weigh less than 110 lbs (50 kg). Carbaryl has been used since 1976 but found to have the potential to cause cancer in rodents and not to be as effective as previously thought. It is either not used at all or its use is restricted.Sexual partners should be evaluated and treated, and sexual contact should be avoided until all partners are better. Because of the strong association between the presence of pubic lice and sexually transmitted infections (STIs), affected people require investigation for other STIs. Eyes
Infestation of the eyes is treated differently than other parts of the body. Lice can be removed with forceps or by removing or trimming the lashes. Eyelashes may be treated with a gentle petroleum jelly for occlusion. Complications
Complications are usually as a result of persistent scratching and include thickening of the skin, darkened skin, and secondary bacterial infection including impetigo, conjunctivitis and blepharitis. Epidemiology
Infestation with pubic lice is found in all parts of the world, occurs in all ethnic groups and all levels of society.Current worldwide prevalence has been very approximately estimated at two percent of the human population. Accurate numbers are difficult to acquire, because pubic lice infestations are not considered a reportable condition by many governments.