MESTEROLONE TABLETS 25mg TAJ PHARMA

MESTEROLONE TABLETS 25mg TAJ PHARMA
(
Mesterolone)

COMPOSITION
Mesterolone Tablets 25mg Taj Pharma

Each tablet contains:
Mesterolone.                                        25 mg
Excipients                                            q.s

ACTION

-dihydro-testosterone, which is a-methyl compound of 5aMesterolone is the 1 considered to be the proper active androgen in many androgen-dependent target organs.

Mesterolone is an oral androgen preparation which has only a slight central inhibitory effect and, consequently, no restrictive effect on testicular function.

Mesterolone balances a deficiency of androgen formation which begins to fall gradually with increasing age. Therefore, Mesterolone is suitable for the treatment of all conditions caused by deficient endogenous androgen formation. In the recommended therapeutic dosage, Mesterolone will not impair spermatogenesis. Mesterolone is especially well tolerated by the liver.

PHARMACOKINETICS AND METABOLISM

Following oral ingestion mesterolome is rapidly and almost completely absorbed in a wide dose range of 10 – 100 mg. The intake of Mesterolone generates maximum serum drug levels of 3.1 ± 1.1 mg/ml after 1.6 ± 0.2 hours. Thereafter drug levels in serum decrease with a terminal half-life of 12 13 hours. Mestorelone is bound to serum proteins by 98%. Binding to albumin accounts for 40% and binding to SHBG to 58%.

Mestorelone is rapidly inactivated by metabolism. The metabolic clearance rate from serum accounts for 4.4 ± 1.6 ml. min -1.kg-1 .

There is no renal excretion of unchanged drug. The main metabolite has been identified as 1a – methyl-androsterone, which – in conjugated form – accounts for 55 – 70% of renally excreted metabolites. The ratio of main metabolite glucoronide to sulphate was about 12:1. As a further metabolite 1a – methyl- 5a androstane-3a, 17b- diol has been recognized, which accounted for about 3% of renally eliminated metabolites. No metabolic conversion into estrogens or corticoids has been observed. In form of metabolites mesterolone is excreted by about 85% of dose with the urine and by about 14% of dose with the faeces. Within 7 days 93% of dose have been recovered in excreta, the half of which had been excreted within 24 hours.

The absolute bioavailability of mesterolone was determined to about 3% of the oral dose.

The daily intake of Mesterolone will lead to an about 30% increase in drug serum levels.

INDICATIONS

Androgen deficiency or male infertility when associated with primary or secondary male hypogonadism.

Reduced efficiency in middle and advanced age

Complaints attributable to androgen-deficiency, such as reduced efficiency, easy fatigability, lack of concentration, weak memory, disturbances of libido and potency, irritability, disturbances of sleep, depressive moods, and general vegetative complaints, can be overcome or improved by the use of Mesterolone tablets.

Potency disturbances

Potency disorders based on an androgen deficiency are eliminated by administration of Mesterolone. If other factors are the sole cause or if they contribute to the disorders, Mesterolone may be administered in support of other therapeutic measures.

Hypogonadism
Growth, development and function of androgen-dependent target organs are stimulated by Mesterolone. It promotes development of secondary male sex characteristics in cases of prepuberal androgen-deficiency.

Mesterolone eliminates deficiency symptoms in cases where a loss of gonadal function has occurred postpuberally.

Infertility
Oligozoospermia and deficient Leydig-cell secretion may be the cause of infertility. With Mesterolone, sperm count and sperm quality as well as the fructose concentration in the ejaculate can be improved or normalized, thus increasing the chances of procreation.

CONTRAINDICATIONS

Prostatic carcinoma.
Previous or existing liver tumours.

WARNINGS

Androgens are not suitable for enhancing muscular development in healthy individuals or for increasing physical ability.

Risk of carcinoma
The occasionally expressed fear that prostatic carcinoma can be induced by the use of androgens is unfounded. Androgens have no carcinogenic action.

Observations made over many years have shown that the risk of carcinoma in men treated with androgens was no greater than in an untreated control group.

Specific studies of male patients under long-term and high-dosed therapy with testosterone produced no signs of prostatic carcinoma and, hence, no evidence that the exogenous supply of testosterone activates any atypical cells which may be present.

The regular check-ups during the therapy failed to reveal a single case of carcinoma among patients with prostatic adenoma, whose complaints were favourably influenced by Mesterolone.

Since androgens can exacerbate a clinically manifest carcinoma of the  prostate, malignant tumours of the prostate must be ruled out before the start of

Mesterolone treatment. As in prophylactic examinations of men, regular rectal and – if required to confirm the diagnosis – biopsy examinations must be carried out during the therapy.

Liver tumours            ·

In rare cases, benign, and in even rarer cases, malignant liver tumours leading

in isolated cases to life-threatening intra-abdominal haemorrhage have been observed after the use of hormonal substances such as the one contained in Mesterolone. A liver tumour should be included in the differential-diagnostic considerations if severe upper abdominal complaints, a liver enlargement or signs of an intra-abdominal haemorrhage occur. If necessary, the preparation must be withdrawn.

ADVERSE REACTIONS

Mesterolone is well tolerated even as regards liver function. Laboratory tests conducted during high-dosed and long-term treatment produced no evidence for an injurious effect. If, in individual cases, frequent or persistent erections occur, the dose should be reduced or the treatment discontinued in order to avoid injury to the penis.

DRUG INTERACTIONS

None recorded so far.

DOSAGE AND ADMINISTRATION

The tablets should be swallowed whole with some liquid.

The following dosages are recommended:

Reduced efficiency and potency disturbances:      ·

Commencement of treatment:

1 Mesterolone tablet 3 times per day.

After satisfactory clinical improvement, it can be tried to reduce the dose.

Continuation of treatment:

1 Mesterolone tablet twice or once per day.

According to the type and severity of the complaints, the dose for further treatment is to be adjusted to individual requirements. Continuous treatment over a period of several months is recommended.

Hypogonadism requires continuous therapy:       

For development of secondary male sex characteristics, 1 – 2 Mesterolone tablets 3 times per day for several months.

As maintenance dose, 1 Mesterolone tablet 2 – 3 times per day will often be sufficient.

Infertility – for the improvement of sperm quantity and quality:           

1 Mesterolone tablet 2 – 3 times per day for a cycle of spermatogenesis, i.e. for about 90 days. If necessary, Mesterolone treatment is to be repeated after an interval of several weeks.

To achieve a higher fructose concentration in the ejaculate in cases of postpuberal Leydig-cell insufficiency: 1 Mesterolone tablet twice per day over several months.

OVERDOSAGE

Acute toxicity studies using single administration showed that Mesterolone is to be classified as practically non-toxic. No risk of toxicity is to be expected even after inadvertent single administration of a multiple of the dose required for therapy.

PRESENTATION

Blisters of 50 tablets.

EXCIPIENTS

lactose monohydrate, maize starch, polyvidone 25,000, magbesium stearate, methyl- 4-hydroxybenzoate, propyl-4-hydroxybenzoate

STORAGE

No special storage conditions are required.

Manufactured in India by:

TAJ PHARMACEUTICALS LTD.
Mumbai, India
Unit No. 214.Old Bake House,
Maharashtra chambers of  Commerce Lane,
Fort, Mumbai – 400001
at:Gujarat, INDIA.
Customer Service and Product Inquiries:
1-800-TRY-FIRST (1-800-222-434 & 1-800-222-825)
Monday through Saturday 9:00 a.m. to 7:00 p.m. EST
E-mail: tajgroup@tajpharma.com

 

 

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Taj Generics (Taj Pharma) provides a wide range of products to the Indian market, including an extensive range of generics and specialty products; Our products cover a vast array of therapeutic categories, and we offer an extensive range of dosage forms and delivery systems including oral solids, controlled-release, steriles, injectables, topicals, liquids, transdermals, semi-solids and high-potency products. Our Generics portfolio offers over 1500 products in the major therapeutic areas of gastro-intestinal, cardiovascular, pain management, oncology, anti-infectives, paediatrics and dermatology.