Bioavailability and LH-Suppressing Effect of Different Testosterone Preparations in Normal and Hypogonadal Men

Nieschlag, Eberhard; Cüppers, H J; Wiegelmann, W.; Wickings, E. Jean

doi:10.1159/000178721

Cited by 76 publications

(43 citation statements)

References 7 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Until recently, the available intramuscular injections were designed for use at a frequency of between weekly and once every four weeks. These preparations are the cheapest mode of testosterone treatment available, but often cause supraphysiological testosterone levels in the days immediately following injection and/or low trough levels prior to the next injection during which time the symptoms of hypogonadism may return (Nieschlag et al 1976). More recently, a commercial preparation of testosterone undecanoate for intramuscular injection has become available.…”

Section: Testosterone Preparationsmentioning

confidence: 99%

Testosterone for the aging male; current evidence and recommended practice

Stanworth

Jones²

2008

CIA

125

View full text Add to dashboard Cite

An international consensus document was recently published and provides guidance on the diagnosis, treatment and monitoring of late-onset hypogonadism (LOH) in men. The diagnosis of LOH requires biochemical and clinical components. Controversy in defi ning the clinical syndrome continues due to the high prevalence of hypogonadal symptoms in the aging male population and the non-specifi c nature of these symptoms. Further controversy surrounds setting a lower limit of normal testosterone, the limitations of the commonly available total testosterone result in assessing some patients and the unavailability of reliable measures of bioavailable or free testosterone for general clinical use. As with any clinical intervention testosterone treatment should be judged on a balance of risk versus benefi t. The traditional benefi ts of testosterone on sexual function, mood, strength and quality of life remain the primary goals of treatment but possible benefi cial effects on other parameters such as bone density, obesity, insulin resistance and angina are emerging and will be reviewed. Potential concerns regarding the effects of testosterone on prostate disease, aggression and polycythaemia will also be addressed. The options available for treatment have increased in recent years with the availability of a number of testosterone preparations which can reliably produce physiological serum concentrations.

show abstract

Section: Testosterone Preparationsmentioning

confidence: 99%

Testosterone for the aging male; current evidence and recommended practice

Stanworth

Jones²

2008

CIA

125

View full text Add to dashboard Cite

show abstract

“…Transdermal gel also gives stable testosterone levels while injectable testosterone esters are associated with "roller-coaster" pharmacokinetics where serum testosterone levels rise into the high normal or supraphysiological range immediately following injection, but fall into the hypogonadal range within two weeks. 63,64 This is reflected in fluctuations in mood, energy, and sexual function. Injectable testosterone esters also result in a high incidence of polycythemia compared with gels due to higher circulating testosterone levels.…”

Section: Dovepressmentioning

confidence: 99%

Safety and efficacy of testosterone gel in the treatment of male hypogonadism

Lakshman¹,

Basaria²

2009

CIA

View full text Add to dashboard Cite

Transdermal testosterone gels were first introduced in the US in 2000. Since then, they have emerged as a favorable mode of testosterone substitution. Serum testosterone levels reach a steady-state in the first 24 hours of application and remain in the normal range for the duration of the application. This pharmacokinetic profile is comparable to that of testosterone patch but superior to injectable testosterone esters that are associated with peaks and troughs with each dose. Testosterone gels are as efficacious as patches and injectable forms in their effects on sexual function and mood. Anticipated increases in prostate-specific antigen with testosterone therapy are not significantly different with testosterone gels, and the risk of polycythemia is lower than injectable modalities. Application site reactions, a major drawback of testosterone patches, occur less frequently with testosterone gels. However, inter-personal transfer is a concern if appropriate precautions are not taken. Superior tolerability and dose flexibility make testosterone gel highly desirable over other modalities of testosterone replacement. Androgel and Testim, the two currently available testosterone gel products in the US, have certain brandspecific properties that clinicians may consider prior to prescribing. Keywords: testosterone gel, Androgel, Testim, hypogonadism Physiology of hypothalamic-pituitary-gonadal axisTesticular function is dependent on the hypothalamic secretion of gonadotropin-releasing hormone (GnRH) which in turn stimulates the secretion of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) from the pituitary to act on the testis. This results in spermatogenesis and testosterone production via stimulation of seminiferous tubules and Sertoli cells, and Leydig cells, respectively. Testosterone is secreted at adult levels during three periods of male life: transient surge during the first trimester of intrauterine life, perinatal surge during early neonatal life, and continually after puberty to maintain androgenization. Testosterone exerts negative feedback both at the level of the hypothalamus and the pituitary gland. Additionaly, sertoli cells produce inhibin that exerts a negative feedback on FSH secretion. Diagnosis of androgen deficiencyThe estimates of the prevalence of androgen deficiency, defined solely in terms of serum testosterone concentrations below the lower limit of the normal range for healthy young men, vary greatly among different studies. Longitudinal data from the Massachusetts Male Aging Study (MMAS) indicate that the prevalence of symptomatic androgen deficiency (Total testosterone 300 ng/dL) in men aged between 40-69 years is between 6% and 12%.

show abstract

“…Administration of a suppository containing 40 mg testosterone results in an immediate and steep rise of serum testosterone lasting for about 4 h. Effective serum levels can be achieved by repeated applications (Nieschlag et al 1976). This therapy, however, never gained much popularity probably because the patients find it unacceptable to use suppositories three times daily on a long-term routine basis.…”

Section: Rectal Applicationmentioning

confidence: 99%

“…In short, for substitution purposes testosterone propionate must be injected every 2 to 3 days while testosterone enanthate, when given in doses of 200 to 250 mg, allows spacing of the injections at about 2 week intervals. Two other clinically available testosterone esters, testosterone cypionate and testosterone cyclohexanecarboxylate have very similar kinetic properties so that they can be used in the same doses and intervals (Nieschlag et al 1976, Schulte-Beerbiihl and Nieschlag 1980, Snyder et al 1980, Sokol and Swerdloff1980, Schiirmeyer and Nieschlag 1984, Gooren 1987.…”

Section: Testosterone Estersmentioning

confidence: 99%

“…Testosterone substitution is started when the diagnosis is established and serum testosterone levels are found below the normal range, taking into account the various influences on serum testosterone levels including diurnal variations. For full substitution pharmacokinetic and clinical studies show that 200 to 250 mg testosterone enanthate or testosterone cypionate must be injected every 2 weeks (Nieschlag et al 1976, Davidson et al 1979, Schulte-Beerbiihl and Nieschlag 1980, Snyder and Lawrence 1980, Sokol et al 1982, Gooren 1987, Cunningham et al 1990.…”

Section: Clinical Practice Of Substitution Therapymentioning

confidence: 99%

See 1 more Smart Citation