T 500 (Testosterone blend)

02 Details

 

 

T 500

(Testosterone blend)

 

 

 

Testosterone Cypionate (cipionate)

 

 

Cipionato de testosterona; Testostérone, Cipionate de; Testosterone Cyclopentylpropionate; Testosterone Cypionate; Testosteroni Cipionas. 3-Oxoandrost-4-en-17β-yl 3-cyclopentylpropionate; 17β-Hydroxyandrost-4-en-3-one cyclopentanepropionate; 17β-(3-Cyclopentyl-1-oxopropoxy)androst-4-en-3-one. Тестостерона Ципионат

 

C27H40O3 = 412.6.

CAS — 58-20-8.

ATC — G03BA03.

ATC Vet — QG03BA03.

 

USP 31(Testosterone Cypionate). A white or creamy-white, crystalline powder, odourless or has a slight odour. Insoluble in water; freely soluble in alcohol, in chloroform, in dioxan, and in ether; soluble in vegetable oils. Protect from light.

 

Testosterone Enantate (enanthate)

 

 

Enantato de testosterona; NSC-17591; Testosteron enantát; Testostérone, enantate de; Testosterone Enanthate; Testosterone Heptanoate; Testosterone Heptylate; Testosteronenantat; Testosteroni enantas; Testosteronienantaatti; Testosterono enantatas; Testosteronu enantan; Tesztoszteronönantát. 3-Oxoandrost-4-en-17β-yl heptanoate; 17β-Hydroxyandrost-4-en-3-one heptanoate. Тестостерона Энантат

 

C26H40O3 = 400.6.

CAS — 315-37-7.

ATC — G03BA03.

ATC Vet — QG03BA03.

 

USP 31(Testosterone Enanthate). A white or creamy-white crystalline powder. It is odourless or has a faint odour characteristic of heptanoic acid. Insoluble in water; very soluble in ether; soluble in vegetable oils. Store at a temperature of 2°to 8°. Protect from light.

 

Testosterone Propionate

 

 

NSC-9166; Propionato de testosterona; Testosteron Propiyonat; Testostérone, propionate de; Testosteroni propionas; Testosteronipropionaatti; Testosteronopropionatas; Testosteronpropionat; Testosteron-propionát; Testosteronu propionian; Tesztoszteronpropionát. 3-Oxoandrost-4-en-17β-yl propionate; 17β-Hydroxyandrost-4-en-3-one propionate. Тестостерона Пропионат

 

C22H32O3 = 344.5.

CAS — 57-85-2.

ATC — G03BA03.

ATC Vet — QG03BA03.

 

USP 31(Testosterone Propionate). White or creamy-white, odourless, crystals or crystalline powder. Insoluble in water; freely soluble in alcohol, in dioxan, in ether, and in other organic solvents; soluble in vegetable oils. Protect from light

 

Test 500 contains a mixture of three testosterone compounds, which were modified with the addition of carboxylic acid esters at the 17-beta hydroxyl group. Esterified forms of testosterone are absorbed more slowly from the area of injection. Once in the bloodstream, the ester is removed to yield free (active) testosterone.

 

T 500 contains:500mg

• 200mg/ml Testosterone cypionate
• 200mg/ml Testosterone enanthate
• 100mg/ml Testosterone propionate

 

 

Pharmacologic Category

Androgen

Dosing: Adult

500mg every week.

Dosing: Geriatric

Refer to adult dosing

Dosing: Pediatric

Safety and efficacy have not been adequately determined in children and adolescents.

Dosing: Renal Impairment

No dosage adjustment provided in manufacturer’s labeling; use with caution.

Dosing: Hepatic Impairment

No dosage adjustment provided in manufacturer’s labeling; use with caution.

Use

Testosterone replacement therapy for male hypogonadism, when testosterone deficiency has been confirmed by clinical features and biochemical tests.

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

Storage/Stability

Store at room temperature. Protect from light.

Contraindications

• Pregnancy.
• Known or suspected carcinoma of the prostate or breast.
• Breast-feeding.
• Hypersensitivity to the active substance or to any of the excipients.

Warnings/Precautions

Medical examination:

Testosterone level should be monitored at baseline and at regular intervals during treatment. Clinicians should adjust the dosage individually to ensure maintenance of eugonadal testosterone levels.

Physicians should consider monitoring patients receiving test400 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.
• Haematocrit and haemoglobin to exclude polycythaemia.

In patients receiving long-term androgen therapy, the following laboratory parameters should also be monitored regularly: haemoglobin, and haematocrit, liver function tests and lipid profile.

Conditions that need supervision:

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

• Tumours – Mammary carcinoma, hypernephroma, bronchial carcinoma and skeletal metastases. In these patients hypercalcaemia or hypercalciuria may develop spontaneously, also during androgen therapy. The latter can be indicative of a positive tumour response to the hormonal treatment. Nevertheless, the hypercalcaemia or hypercalciuria should first be treated appropriately and after restoration of normal calcium levels, hormone therapy can be resumed.
• Pre-existing conditions –

In patients suffering from severe cardiac, hepatic or renal insufficiency or ischaemic heart disease, treatment with testosterone may cause severe complications characterised by oedema with or without congestive cardiac failure. In such cases treatment must be stopped immediately. Patients who experienced myocardial infarction, cardiac-, hepatic- or renal insufficiency, hypertension, epilepsy, or migraine should be monitored due to the risk of deterioration of or reoccurrence of disease. In such cases treatment must be stopped immediately.

Testosterone may cause a rise in blood pressure and T500 should be used with caution in men with hypertension.

• Epilepsy or Migraine – (or a history of these conditions), since androgens may occasionally induce fluid and sodium retention.
• Diabetes mellitus – Androgens in general and T 500 can improve glucose tolerance in diabetic patients.
• Anti-coagulant therapy – Androgens in general and T 500 can enhance the anti-coagulant action of coumarin-type agents.
• Sleep apnea- 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 patients with risk factors such as adiposity or chronic lung diseases.

Pregnancy Risk Factor

X

Category X: Studies in animals or human beings have demonstrated fetal abnormalities, or there is evidence of fetal risk based on human experience, or both, and the risk of the use of the drug in pregnant women clearly outweighs any possible benefit. The drug is contraindicated in women who are or may become pregnant.

 

Pregnancy Considerations

Use is contraindicated in women who are or may become pregnant; masculinization of the fetus has been reported.

Lactation

Excreted in breast milk.

Breast-Feeding Considerations

T500 is excreted in breast milk. Due to the potential for serious adverse reactions in the nursing infant, breast-feeding is not recommended.

Adverse Reactions

Frequency unknown.

Cardiovascular: Edema

Central nervous system: Depression, excitation, insomnia

Dermatologic: Acne (females and prepubertal males)

Also reported in females: Hirsutism, male-pattern baldness

Endocrine & metabolic: Electrolyte imbalances, glucose intolerance, gonadotropin secretion inhibited, gynecomastia, HDL decreased, LDL increased, libido changes

Also reported in females: Clitoral enlargement, menstrual irregularities

Genitourinary:

Prepubertal males: Increased or persistent erections, penile enlargement

Postpubertal males: Bladder irritation, epididymitis, impotence, oligospermia, priapism (chronic), testicular atrophy, testicular function inhibited

Hematologic: Prothrombin time increased, suppression of clotting factors

Hepatic: Alkaline phosphatase increased, ALT increased, AST increased, bilirubin increased, cholestatic jaundice, hepatic necrosis (rare), hepatocellular neoplasms, peliosis hepatis (with long-term therapy)

Neuromuscular & skeletal: CPK increased, premature closure of epiphyses (in children)

Renal: Creatinine excretion increased

Drug Interactions

Enzyme-inducing agents may decrease and enzyme-inhibiting drugs may increase testosterone levels. Therefore, adjustment of the dose of T 500 may be required.

Insulin and other anti-diabetic medicines:

Androgens may improve glucose tolerance and decrease the need for insulin or other anti-diabetic medicines in diabetic patients.

Patients with diabetes mellitus should therefore be monitored especially at the beginning or end of treatment and at periodic intervals during T 500 treatment.

Anti-coagulant therapy:

High doses of androgens may enhance the anticoagulant action of coumarin type agents. Therefore, close monitoring of prothrombin time and if necessary a dose reduction of the anti-coagulant is required during therapy.

ACTH or Corticosteroids:

The concurrent administration of testosterone with ACTH or corticosteroids may enhance oedema formation therefore these active substances should be administered cautiously, particularly in patients with cardiac or hepatic disease or in patients predisposed to edema.

Test Interactions

Androgens may decrease 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.

Monitoring Parameters

Liver function tests, cholesterol profile, hemoglobin/hematocrit; INR/PT in patients on anticoagulant therapy

Children: Radiographs of left wrist and hand every 6 months (to assess bone maturation)

Adult females: Signs of virilization (deepening voice, hirsutism, acne, clitoromegaly); urine and serum calcium in women with breast cancer.

Dosage Forms

500mg/ml in a Multi-dose vial with 10ml.

Multi dosing vial: 500mg/1 ml

Mechanism of Action

Testosterone is the principal endogenous androgen responsible for promoting the growth and development of the male sex organs and maintaining secondary sex characteristics in androgen-deficient males. It has anabolic properties over skeletal muscle that increase with the dosing. Enanthate, Propionate and Cypionate offer varying pharmacokinetics making this a useful compound.

Pharmacodynamics/Kinetics

T 500 contains three 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.

Absorption:

A single dose of T500 leads to an increase of total plasma testosterone with peak reached approximately 24-48 h (tmax) after administration.

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 metabolised to dihydrotestosterone and estradiol, which are further metabolised via the normal pathways.

Elimination:

Excretion mainly takes place via the urine as conjugates of etiocholanolone and androsterone.