Sustanon 250 mg/ml solution for injection

(equivalent to a total of 176mg of Testosterone)

For excipients, see 6.1

Solution for injection.

Testosterone replacement therapy in male hypogonadal disorders, for example:

after castration;

eunuchoidism;

hypopituitarism;

endocrine impotence;

male climacteric symptoms like decreased libido;

certain types of infertility due to disorders of spermatogenesis.

Testosterone therapy may also be indicated for the prevention and treatment of osteoporosis in hypogonadal males.

Testosterone administration may also be used as supportive therapy for female-to-male transsexuals.

Dosage

In general, dosage should be adjusted to the individual response of the patient.

Adults:

Usually, one injection of 1ml per three weeks is adequate.

Elderly:

It should be noted that smaller and less frequent doses may achieve the same response.

Children:

It should be noted that smaller and less frequent doses may achieve the same response.

Female-to-male transsexuals:

Different specialist centres have used doses varying from one injection of 1ml every two weeks to one injection of 1ml every four weeks.

Administration

Deep intramuscular injection

Known or suspected prostatic or mammary carcinoma;

Pregnancy

Breast-feeding

Hypersensitivity to the active substance or to any of the excipients.

Patients, especially the elderly, with the following conditions should be monitored:

▪ ischaemic heart disease, since androgens may produce hypercholesterolaemia.

▪ latent or overt cardiac failure, renal dysfunction, hypertension, epilepsy or migraine (or a history of these conditions), since androgens may occasionally induce fluid and sodium retention.

▪ skeletal metastases, since androgens may induce hypercalcaemia or hypercalciuria in these patients.

Long term monitoring should include measurement of haemoglobin.

The use of steroids may influence the results of certain laboratory tests.

Androgens should be used cautiously in prepubertal boys to avoid premature epiphyseal closure or precocious sexual development.

If androgen-associated adverse reactions occur, Sustanon 250 treatment should be interrupted and, after disappearance of the symptoms, be resumed at a lower dosage.

Sustanon 250contains Arachis oil (peanut oil) and should not be taken / applied by patients known to be allergic to peanut. As there is a possible relationship between allergy to peanut and allergy to Soya, patients with Soya allergy should also avoid Sustanon 250.

Female-to-male transsexual supportive therapy

Before initiating Sustanon for female-to-male transsexuals, specialist assessment should be undertaken, including psychiatric assessment. A complete personal and medical history should be taken. During treatment, periodic check-ups are recommended of a frequency and nature adapted to the individual. The following should be monitored:

▪ signs of osteoporosis,

▪ changes in lipid profile.

In patients with a personal or family history of breast cancer and with a personal history of endometrial cancer, careful monitoring should be undertaken.

Subject to specialist advice, hysterectomy and bilateral oophorectomy should be considered after 18-24 months of testosterone treatment, to reduce the possible increased risk of endometrial and ovarian cancer.

Continued surveillance is required to detect osteoporosis in patients who have undergone oophorectomy, as testosterone may not fully reverse the decline in bone density in these patients.

Continued surveillance is required to detect endometrial and ovarian cancer in patients on long term treatment who have not proceeded to hysterectomy and bilateral oophorectomy.

Enzyme-inducing agents may exert increasing or decreasing effects on testosterone levels. Therefore adjustment of the dose, and/or intervals between injections may be required.

On the basis of its pharmacological effect, Sustanon 250 is suspected to cause birth defects and/or other irreversible adverse effects on pregnancy outcome. Therefore, Sustanon 250 is contraindicated during pregnancy and lactation.

As far as is known Sustanon 250 has no influence on alertness and concentration.

The following adverse reactions have been associated with androgen therapy in general:

• In prepubertal boys, precocious sexual development, an increased frequency of erections, phallic enlargement and premature epiphyseal closure;

• Priapism and other signs of excessive sexual stimulation;

• Water and sodium retention;

• Oligospermia and a decreased ejaculatory volume.

Treatment should be interrupted until these symptoms have disappeared, after which it should be continued at a lower dosage.

Hoarseness of the voice may be the first symptom of vocal change which may lead to irreversible lowering of the voice. If signs of virilisation develop, particularly lowering of the voice, treatment should be discontinued unless the effects are desired treatment outcomes.

The following undesirable effects have also been observed:

● acne

● disturbance of liver function

● polycythaemia

● hypertension

● weight gain (in female-to-male transsexuals)

The acute intramuscular toxicity of Sustanon 250 is very low. Priapism in men is a symptom of chronic overdose. If this occurs, Sustanon treatment should be interrupted and, after disappearance of the symptom, be resumed at a lower dose.

ATC code: GO3B A urogenital system (including sex hormones)

Testosterone is the principal endogenous hormone essential for normal growth and development of the male sex organs and male secondary sex characteristics. During adult life testosterone is essential for the functioning of the testes and accessory structures, and for the maintenance of libido, sense of well-being, erectile potency, prostate and seminal vesicle function.

Treatment of hypogonadal males with Sustanon 250 results in a clinically significant rise of plasma concentrations of testosterone, dihydrotestosterone and androstenedione, as well as a decrease of SHBG (sex hormone binding globulin). In the males with primary (hypergonadotropic) hypogonadism treatment with Sustanon results in a normalisation of pituitary function.

Sustanon 250 contains a number of esters of testosterone with different durations of action. The esters are hydrolysed into the natural hormone testosterone, as soon as they enter the general circulation.

A single dose of Sustanon 250 in males leads to an increase of total plasma testosterone, with peak level reached approximately 24-48hrs (t_max) after administration. Plasma testosterone levels return to the lower limit of the normal range in males after approximately 21 days.

In female-to-male transsexuals, a single dose of Sustanon 250 repeated every two weeks resulted in mean trough testosterone levels towards the upper end of the normal male range at 2, 4 and 12 months.

Testosterone is metabolised via the normal pathways. Excretion mainly takes place via the urine as conjugates of etiocholanolone and androsterone.

Not applicable

Benzyl Alcohol Ph. Eur.

Arachis Oil Ph. Eur.

Not applicable.

5 years.

Do not store above 25^oC

Do not refrigerate (or freeze)

Store the ampoules in the outer carton

1ml ampoules in boxes of 1, 3, or 6.

No special requirements.

Organon Laboratories Limited

Cambridge Science Park

Milton Road

Cambridge

CB4 0FL

PL 0065/5086R

28 February 1973

January 2006

Ref: USSU250v4.3