Oral contraceptives male contraception

TP, a 22 year-old woman, presents to your office for a routine gynecologic examination. She entered menarche at the age of 12. Her last menstrual period was 3 months ago. Her periods are often irregular and occur about every 2 to 3 months. She has had all normal Pap smears in the past and no history of sexually transmitted infections. She is currently in a monogamous relationship with a male partner. She has had a total of four sexual partners. She is not taking oral contraceptives and does not routinely use condoms. She has never been pregnant in the past, but she plans on starting a family in the near future. As you examine the patient, you note facial and chest acne, increased facial and abdominal hair, and obesity. 

The catabolism and the amount remaining in the body of males and females is given in Table 1. Females on oral contraceptives have more caffeine left in the body than females not on contraceptives in all periods, but this is especially noticeable in the 12- to 24-h period. 

Ethinyloestradiol Synthetic oestrogen Used for oestrogen replacement therapy in deficient states, both pre- and postmenopausal. Treatment of prostate cancer (male), breast cancer (post-menopausal women). Component of many oral contraceptives... 

Cimetidine (for treatment of peptic ulcers) competes with dihydrotestosterone for receptors in the testis and accessory sex glands. The more common sequelae are low sperm count and gynacomastia. Epidemiological evidence has shown that occupation exposure to oral contraceptives can induce gynacomastia in exposed males. Diethylstilbestrol (DES) antagonizes the activity of fetal testosterone. In the male offspring, testicular hypoplasia, abnormal semen parameters, and infertility result. Ketoconazole has be shown to be transported to the seminal fluid and to immobilize the sperm. 

Prominent among toxicants that adversely affect both male and female reproductive systems are endocrine disruptors (see Section 9.7). Toxicants that mimic the actions of sex hormones are agonists, and those that prevent hormonal action or bind competitively to hormone receptor sites are antagonists,12 Male patients treated with cimetidine for peptic ulcers have exhibited low sperm counts and abnormal breast enlargement, a condition called gynecomastia. Gynecomastia has also been caused in men working in oral contraceptive production. Ketoconozole inhibits the enzymes required to produce hormones involved in sperm production and can immobilize sperm in seminal fluid. 

In the human female, whose pituitary hormones may be suppressed by the use of oral contraceptives, the ratio of testosterone to creatinine in urine may be used. Alternatively, a method suitable for both males and females is to measure the ratio of total testosterone to epitestosterone using gas chromatography—mass spectrometry. In this method, the bis(trimethylsilyl) derivative is formed and the intensity of the molecular ions at m/z 432, under electron impact conditions for both of the steroid derivatives, is used to determine the ratio (M. Donike and J. Zimmermann, J. Chromat, 1980, 202, 483-486). The internationally accepted limit for the ratio is currently 6. 

The structure of steroids—cholesterol, female sex hormones, male sex hormones, adrenal cortical steroids, anabolic steroids, and oral contraceptives (Section 29.8)... 

Materials and Methods. Subjects ranging in age between 21-89 years were randomly selected from the Domiciliary Care Veterans Facility at the Central State Hospital. Determination of copper and ceruloplasmin was made on venous blood drawn from 180 males and 44 females. We have made no attempt to exclude from this study patients with chronic illnesses since it would be highly unlikely that such aged populations would be completely free of these conditions. However, patients with acute intercurrent illnesses and hepatic renal or symptomatic cardiovascular diseases were eliminated from this study. Individuals with acute illnesses as well as pregnant females or females on oral contraceptive agents also have been excluded. Some of the older patients did have evidence of atherosclerosis, mild diabetes mellitus, or compensated heart failure. 

Hyperlipidemia Hypertension Smoking yfDUVJ Diabetes IUl 1 Male gender Obesity Sedentary lifestyle Stress (type A personality) Elevated homocysteine Oral contraceptive use Increasing age Familial/genetic factors... 

The polyphenolic binaphthyl gossypol 94 displays interesting pharmacological applications like male oral contraceptive, treatment of bronchitis, total inhibitor of HIV 1, and in vitro antiviral activity against herpes type 2 virus and influenza virus (Scheme 26.28). Apogossypol 95, a degradation derivative of gossypol that lacks the aldehyde functions, still has the potent pan-active inhibitor activity of antiapoptotic Bcl-2 family proteins. The naphthoic acid precursor can be obtained by... 

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