1. Name Of The Medicinal Product
Sustanon 250, 250 mg/ml solution for injection
2. Qualitative And Quantitative Composition
Testosterone propionate | 30 mg/ml |
| 60 mg/ml |
Testosterone isocaproate | 60 mg/ml |
Testosterone decanoate | 100 mg/ml |
(equivalent to a total of 176mg of Testosterone)
Sustanon 250 contains 1 ml Arachis oil. For a full list of excipients, see section 6.1
3. Pharmaceutical Form
Solution for injection.
A clear, pale yellow solution.
4. Clinical Particulars
4.1 Therapeutic Indications
Testosterone replacement therapy in males for conditions associated with primary and secondary hypogonadism, either congenital or acquired.
Testosterone administration may also be used as supportive therapy for female-to-male transsexuals.
4.2 Posology And Method Of Administration
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.
Children:
Safety and efficacy have not been adequately determined in children.
Sustanon contains benzyl alcohol and should not be given to children under 3 years of age.
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
4.3 Contraindications
Known or suspected carcinoma of the prostate or breast
Pregnancy
Breast-feeding
Hypersensitivity to the active substance or to any of the excipients.
4.4 Special Warnings And Precautions For Use
Physicians should consider monitoring subjects receiving Sustanon before the start of treatment, at quarterly intervals for the first 12 months and yearly thereafter for the following parameters:
• digital rectal examination (DRE) of the prostate and PSA to exclude benign prostate hyperplasia or a sub-clinical prostate cancer,
• hematocrit and hemoglobin to exclude polycythemia.
Patients, especially the elderly, with the following conditions should be also be monitored:
• 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.
In patients with pre-existing cardiac, renal or hepatic disease, or hypertension androgen treatment may cause complications characterized by oedema with or without congestive heart failure.
Caution should be applied when treating men with sleep apnea. There have been reports that testosterone can cause or exacerbate pre-existing sleep apnea. However, there is a lack of evidence regarding the safety of testosterone in men with the condition. Good clinical judgment and caution should be employed in subjects with risk factors such as adiposity or chronic lung diseases.
In pre-pubertal children statural growth and sexual development should be monitored since androgens in general and Sustanon in high dosages may accelerate epihyseal closure and sexual maturation.
If androgen-associated adverse reactions occur, treatment with Sustanon should be discontinued and upon resolution of the complaints resumed with lower dosages.
The misuse of androgens to enhance ability in sports carries serious health risks and is to be discouraged.
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.
Sustanon 250 contains benzyl alcohol (0.1 ml benzyl alcohol per ml). Must not be given to premature babies or neonates. May cause toxic reactions and anaphylactoid reactions in infants and children up to 3 years old.
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.
4.5 Interaction With Other Medicinal Products And Other Forms Of Interaction
Enzyme-inducing agents may decrease and enzyme-inhibiting drugs may increase testosterone levels. Therefore, adjustment of the dose of Sustanon may be required. Androgens may improve glucose tolerance and decrease the need for insulin or other anti-diabetic medicines in diabetic subjects (see section 4.4).
High doses of androgens may enhance the anticoagulant action of coumarin type agents allowing a reduction of the dose of these agents (see section 4.4).
Sustanon use may result in decreased levels of thyroxine-binding globulin, resulting in decreased total T4 serum levels and increased resin uptake of T3 and T4. Free thyroid hormone levels remain unchanged, and there is no clinical evidence of thyroid dysfunction.
4.6 Pregnancy And Lactation
There are no adequate data for the use of Sustanon in pregnant women. In view of the risk of virilization of the fetus, Sustanon should not be used during pregnancy. Treatment with Sustanon should be discontinued when pregnancy occurs.
There are no adequate data for the use of Sustanon during lactation. Therefore, Sustanon should not be used during lactation.
4.7 Effects On Ability To Drive And Use Machines
As far as is known Sustanon 250 has no influence on alertness and concentration.
4.8 Undesirable Effects
Due to the nature of Sustanon side effects cannot be quickly reversed by discontinuing medication. Injectables in general, may cause a local reaction at the injection site.
The following adverse reactions have been associated with androgen therapy in general.
Since the undesirable effects described below are derived from post marketing surveillance and based on general androgenic class labelling, the frequency could not be calculated.
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Paediatric population
The following undesirable effects have been reported in prepubertal boys using androgens in general (see section 4.4): precocious sexual development, an increased frequency of erections, phallic enlargement and premature epiphyseal closure.
4.9 Overdose
The acute toxicity of testosterone is low.
If symptoms of chronic overdose occur (e.g. polycythemia, priapism) treatment should be discontinued and after disappearance of the symptoms, be resumed at lower dosage.
5. Pharmacological Properties
5.1 Pharmacodynamic Properties
Pharmacotherapeutic group: Androgens. ATC code G03B A03
Treatment of hypogonadal men with Sustanon results in a clinically significant rise of plasma concentrations of testosterone, dihydrotestosterone, estradiol and androstenedione. Luteinizing hormone (LH) and follicle-stimulating hormone (FSH) are restored to the normal range. In hypogonadal men, treatment with Sustanon results in an improvement of testosterone deficiency symptoms. Moreover, treatment increases bone mineral density and lean body mass, and decreases body fat mass. Treatment also improves sexual function, including libido and erectile function. Treatment increases hemoglobin and hematocrit, which may lead to polycytaemia. Testosterone also produces systemic effects, such as increasing the retention of sodium, potassium and chloride leading to an increase in water retention. Treatment may result in an increase in prostate size and PSA levels, and worsening of lower urinary tract symptoms. In boys with constitutional delay of growth and puberty, treatment with androgens accelerates growth and induces development of secondary sex characteristics. In female-to-male transsexuals, treatment with androgens/Sustanon induces masculinization.
5.2 Pharmacokinetic Properties
Sustanon 250 contains four esters of testosterone with different durations of action. The esters are hydrolyzed into the natural hormone testosterone as soon as they enter the general circulation.
Absorption:
A single dose of Sustanon 250 leads to an increase of total plasma testosterone with peak levels of approximately 70 nmol/l (Cmax), which are reached approximately 24-48 h (tmax) after administration. Plasma testosterone levels return to the lower limit of the normal range in males in 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.
Distribution:
Testosterone displays a high (over 97%) non-specific binding to plasma proteins and sex hormone binding globulin in in vitro tests.
Biotransformation:
Testosterone is metabolized to dihydrotestosterone and estradiol, which are further metabolized via the normal pathways.
Elimination:
Excretion mainly takes place via the urine as conjugates of etiocholanolone and androsterone.
5.3 Preclinical Safety Data
Not applicable
6. Pharmaceutical Particulars
6.1 List Of Excipients
Benzyl Alcohol Ph. Eur.
Arachis Oil Ph. Eur.
6.2 Incompatibilities
Not applicable.
6.3 Shelf Life
5 years.
6.4 Special Precautions For Storage
Do not store above 25oC
Do not refrigerate (or freeze)
Store the ampoules in the outer carton
6.5 Nature And Contents Of Container
Colorless glass ampoule filled with 1 ml of Sustanon in boxes of 1, 3, or 6.
Not all pack sizes may be marketed. In correspondence please quote batch number.
6.6 Special Precautions For Disposal And Other Handling
Any unused product or waste material should be disposed of in accordance with local requirements.
7. Marketing Authorisation Holder
Organon Laboratories Limited
Cambridge Science Park
Milton Road
Cambridge
CB4 0FL
8. Marketing Authorisation Number(S)
PL 0065/5086R
9. Date Of First Authorisation/Renewal Of The Authorisation
28 February 1973
10. Date Of Revision Of The Text
18 January 2011
Ref: USSU250v5.5
Sustanon/01-11/1
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