Testosterone Undecanoate

Registered South African indications:

• Male hypogonadism

Contraindications

Injection

• Hypersensitivity to the active ingredient or any of its excipients
• Androgen-dependent carcinoma of the prostate or of the male mammary gland
• Past or present hepatic tumours
• Hypercalcaemia accompanying malignant tumours
• The use of testosterone undecanoate in women is contraindicated
  - Pregnancy
  - Breastfeeding

Capsule

• Hypersensitivity to the active ingredient or any of its excipients
• Impaired hepatic function and hypercalcaemia
• Known or suspected mammary or prostatic carcinoma

Cautions

• Pregnancy (cap)
• Breastfeeding (cap)
• Renal impairment
• Hepatic impairment (inj)
• Elderly
• Children and adolescents
• Cancer patients at risk of hypercalcaemia
• Severe cardiac disease
• Ischaemic heart disease
• Patients predisposed to oedema
• Hypertension
• Acquired or inherited bleeding disorders 
• Clotting disorders
• Thrombophilia
• Epilepsy
• Migraine
• Pre-existing sleep apnoea
• Diabetes mellitus
• Benign prostatic hyperplasia

Forms avail. in SA and covered in this monograph: inj, cap

Male hypogonadism

• Oral (cap): Initial: 120-160mg; Maintenance: 40-120mg, dly; Treatment duration: 2-3 weeks

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Take with a meal

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It is preferable to take half the dose in the morning, and half at night; if an uneven number of capsule to be taken, take larger dose in morning

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Do not cut/crush/chew/dissolve

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• IM: 1000mg, as a slow injection, every 10-14 weeks

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Serum testosterone levels should be measured before the start of treatment. Depending on the levels, the first injection interval may be reduced to a minimum of 6 weeks

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See additional prescribing points

Not established for use in children below 18 years

Pregnancy

Injection

• Contraindicated
• Testosterone undecanoate is not indicated for use in women and must not be used in pregnant women

Capsule

• Caution; not recommended
• Testosterone undecanoate must not be used during pregnancy

Breastfeeding

Injection

• Contraindicated
• Testosterone undecanoate is not indicated for use in women and must not be used in breastfeeding women

Capsule

• Caution; not recommended
• Testosterone undecanoate  must not be used during lactation

Fertility

• Testosterone replacement therapy may reversibly reduce spermatogenesis

Renal Impairment

• Caution; no dose adjustment recommended

Hepatic Impairment

Injection

• Caution; no information available
  No formal studies have been performed in patients with hepatic impairment
• Past or present liver tumours: Contraindicated 

Capsules

• Impaired hepatic function and hypercalcaemia: Contraindicated

Elderly

• Caution; no dose adjustment recommended
  Consider a lower testosterone target, at lower end of normal testosterone range

Porphyria Information

• Probably not porphyrinogenic (PNP)

Drugs in Sport

• Prohibited - At all times

Central Nervous System Disorders

• Depression
• Emotional disorder
• Insomnia
• Restlessness
• Aggression
• Irritability
• Headache
• Migraine
• Tremor
• Fatigue

Cardiovascular Disorders

• Hot flush
• Cardiovascular disorder
• Hypertension
• Dizziness

Respiratory Disorders

• Bronchitis
• Sinusitis
• Cough
• Dyspnoea
• Snoring
• Dysphonia

Gastrointestinal Disorders

• Diarrhoea
• Nausea

Hepatobiliary Disorders

• Abnormal hepatic function tests
• Increased aspartate aminotransferase 

Genitourinary Disorders

• Decreased urine flow 
• Urinary retention
• Urinary tract disorder
• Nocturia
• Dysuria
• Increased prostate specific antigen 
• Abnormal prostate examination 
• Benign prostate hyperplasia
• Prostatic intraepithelial neoplasia
• Prostate induration
• Prostatitis
• Prostatic disorder
• Change in libido 
• Testicular pain
• Breast induration
• Breast pain
• Gynaecomastia
• Increased oestradiol 
• Increased testosterone 

Endocrine and Metabolic Disorders

• Increased weight
• Increased appetite
• Increased glycosylated haemoglobin 
• Hyperhidrosis

Musculoskeletal Disorders

• Arthralgia
• Pain in extremity
• Muscle disorders
• Musculoskeletal stiffness
• Increased creatine phosphokinase 

Skin and Subcutaneous Tissue Disorders

• Acne
• Alopecia
• Erythema
• Rash
• Pruritus
• Dry skin

Immune, Blood and Lymphatic System Disorders

• Polycythaemia
• Increased haematocrit 
• Increased red blood cell count 
• Increased haemoglobin
• Hypersensitivity
• Hypercholesterolaemia
• Increased triglycerides 
• Increased cholesterol 

Others

• Pulmonary oil microembolism

• Oral anticoagulants
• Adrenocorticotropic hormone 
• Corticosteroids
• Thyroxin-binding globulin
• Hepatic enzyme-inducing agents
• Antidiabetic agents

• Breast examination
• Testosterone levels
• Full blood count
• Hepatic function
• Lipid profile

Specific cases may require

• Prothrombin time
• International normalized ratio
• Prostate-specific antigen 
• Prostate examination
• Glucose monitoring

It is advisable to occasionally measure testosterone serum levels at the end of an injection interval. Serum levels below normal range would indicate the need for a shorter injection interval. In the case of high serum levels, an extension of the injection interval may be considered. The injection interval should remain within the recommended range of 10 to 14 weeks.

Testosterone undecanoate is a fatty acid ester of the natural androgen testosterone. Therapy increases plasma levels of testosterone and its active metabolites.

Capsule 40mg

• Androxon (Adcock) originator

Injection (per 4ml) 1000mg

• Nebido (Bayer) originator