Testosterone and Esters

Testosterone is the most well known androgen and is a sex steroid hormone. Androgens cause masculinisation and are used to replace testosterone in patients with absent or low levels of the hormone. They are also used commercially by normal males as they have anabolic effects.

• Masculinisation
• Inhibition of pituitary gonadotrophins and spermatogenesis in normal males
• Anabolic action

• Hypogonadism (primary or secondary) with androgen deficiency e.g. castrated patients. Testosterone esters are usually used and treatment is usually lifelong.¹ The hypogonadism must be thoroughly investigated to begin with by a specialist with an interest in this area. If the cause is hypopituitarism then therapy can result in normal sexual development but infertility remains.
• Breast cancer in females.
• Delayed puberty - but can lead to short stature.
• Prevention of infertility secondary to chemotherapy treatment.²
• Treatment of weight loss in HIV infected patients.³
• Anabolic steroids: these have some androgenic activity but cause less virilisation in women. Used in aplastic anaemia and osteoporosis. Enhancement of body build has not been proven to be beneficial.

Testosterone is not useful as a male contraception, nor for menopausal symptoms or lower limb atherosclerosis. Other unlicensed uses include anaemia, development of male features in transsexuals,⁴ microphallus and lichen sclerosus.⁵

• Breast cancer in men
• Prostate cancer
• Primary hepatic malignancy - or a strong family history of this
• Hypercalcaemia
• Breast feeding
• Pregnancy
• Nephrotic syndrome

• Short stature in boys treated for delayed puberty, due to rapid fusion of the epiphyses
• Cardiac disease e.g. ischaemic heart disease
• Renal impairment
• Hepatic impairment - dose related toxicity e.g. cholestasis with some androgens and fluid retention
• Elderly
• Hypertension
• Epilepsy
• Migraine - headaches may worsen
• Diabetes mellitus
• Bony metastases - may result in hypercalcaemia
• Examine prostate and breasts regularly

• Effect of anticoagulants are increased e.g. warfarin.
• Possible increased risk of hypoglycaemia in patients on oral medications for diabetes.

• Prostatic enlargement and malignant change
• Headache
• Psychiatric disturbance e.g. depression, anxiety
• Gastrointestinal side effects e.g. nausea, haemorrhage
• Liver effects e.g. cholestatic jaundice and liver tumours (rare)
• Cardiovascular effects e.g. hypertension
• Electrolyte disturbances e.g. sodium retention with fluid overload, hypercalcaemia
• Sexual dysfunction e.g. change in libido
• Androgenic effects e.g. hirsutism, male-pattern baldness, seborrhoea, acne, precocious sexual development, virilism in women
• Other adverse effects include gynaecomastia, polycythaemia, weight gain and increased bone growth

• Capsules
• Buccal
• Intramuscular injections - preferred when used for replacement, depot versions are available
• Implants - replaced every 4-5 months
• Transdermal patches - can lead to transfer of testosterone to female sexual partner¹
• Gel formulation

Patients should be referred to specialists and treatment is usually started and managed under their supervision. Factors that need to be included in any assessment are:

• Full medical and psychiatric history
• Exclude active breast cancer in females
• Prostate examination and prostate specific antigen (PSA) to rule out prostate cancer¹
• Diabetes mellitus - may get hypo- or hyperglycaemia
• Worsens fluid retention in liver and kidney disease

Monitor by measuring hormone levels and watch out for side effects, such as polycythaemia and irritation at injection sites.

As age increases testosterone levels decline. At the same time some men may experience non-specific symptoms such as depression, fatigue and loss of libido. Replacement of testosterone has been suggested in older men; however, the clinical diagnosis of lack of testosterone is not easily made in older men. To date there is no clear evidence of the benefit of treating older men with testosterone.¹

A number of studies have observed that as testosterone levels reduce so does bone density in men. Similarly, the lower the level of testosterone the increased risk of bone fractures.⁶ To date there have only been a few trials with small numbers of patients producing inconsistent results. Therefore the use of testosterone in men for bone protection is not recommended.