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Uses and Administration
Mesterolone has androgenic properties (see Testosterone, Refer to ) but is reported to have less inhibitory effect on intrinsic testicular function than testosterone.
Mesterolone is given orally in the treatment of androgen deficiency or male infertility associated with hypogonadism ( Refer to ). Initial treatment with 75 to 100 mg daily, in 3 or 4 divided doses, is given for several months, followed by 50 to 75 mg daily for maintenance.
(last reviewed 2010-06-30; last modified 2010-06-14)
Adverse Effects, Treatment and Precautions
Adverse Effects and Precautions
As for androgens in general (see Testosterone, Refer to ).
Mesterolone is reported not to inhibit gonadotrophin secretion or spermatogenesis.
(last reviewed 2010-06-30; last modified 2010-06-14)
Pharmacokinetics
Mesterolone is rapidly and almost completely absorbed after an oral dose and peak serum concentrations occur after about 1.6 hours. It is rapidly metabolised, with an absolute bioavailability of about 3% of the oral dose, and a terminal half-life of 12 to 13 hours. Unlike other androgens (see Testosterone, Refer to ), mesterolone is not metabolised to oestrogenic compounds. Mesterolone is bound to serum proteins; about 40% to albumin and 58% to sex-hormone binding globulin. About 77% of the metabolites are excreted in the urine, and about 13% in the faeces.
(last reviewed 2010-06-30; last modified 2010-06-14)
Preparations: Single-Ingredient
The following preparations list represents a compilation of all available salt forms or related substances for this drug product.
The symbol ¤ denotes a preparation which is discontinued or no longer actively marketed.
AUSTRALIA: Proviron;AUSTRIA: Proviron¤;BELGIUM: Proviron;BRAZIL: Proviron;CHILE: Proviron¤;CZECH REPUBLIC: Proviron¤;DENMARK: Mestoranum¤;FINLAND: Proviron¤;FRANCE: Proviron¤;GERMANY: Proviron¤; Vistimon¤;GREECE: Proviron;HONG KONG: Proviron¤;HUNGARY: Proviron;INDIA: Mestilon; Provironum;INDONESIA: Androlon; Infelon; Proviron;ISRAEL: Proviron;ITALY: Proviron;MALAYSIA: Malvinum; Provironum; Vistimon¤;MEXICO: Proviron;NETHERLANDS: Proviron¤;NORWAY: Mestoranum¤;PHILIPPINES: Proviron; Restore¤;POLAND: Proviron¤;PORTUGAL: Proviron;RUSSIAN FEDERATION: Proviron (Провирон)¤;SOUTH AFRICA: Proviron;SINGAPORE: Provironum; Restore;SPAIN: Proviron;SWEDEN: Mestoranum¤;SWITZERLAND: Proviron¤;THAILAND: Mesviron; Provironum;TURKEY: Proviron;UNITED KINGDOM: Proviron;UKRAINE: Proviron (Провирон);VENEZUELA: Proviron¤;
Preparations: Multi-Ingredient
The following preparations list represents a compilation of all available salt forms or related substances for this drug product.
The symbol ¤ denotes a preparation which is discontinued or no longer actively marketed.
GERMANY: Pluriviron¤;
Therapeutic Use
- Sex Hormones and their Modulators
Last Updated 1/21/20
The format of this leaflet was determined by the Ministry of Health and its
content was checked and approved by it in July 2012
PRESCRIBING INFORMATION
PROVIRON
Tablets
COMPOSITION
Each tablet contains 25 mg mesterolone.
ACTION
-dihydro-testosterone, which is -methyl compound of 5Mesterolone is the 1
considered to be the proper active androgen in many androgen-dependent target
organs.
Proviron is an oral androgen preparation which has only a slight central inhibitory
effect and, consequently, no restrictive effect on testicular function.
Proviron balances a deficiency of androgen formation which begins to fall gradually
with increasing age. Therefore, Proviron is suitable for the treatment of all conditions
caused by deficient endogenous androgen formation. In the recommended therapeutic
dosage, Proviron will not impair spermatogenesis. Proviron 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 Proviron 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.kg1 .
There is no renal excretion of unchanged drug. The main metabolite has been
identified as 1 - 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 1 - methyl- 5 androstane-3, 17-
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 Proviron 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 Proviron tablets.
Potency disturbances
Potency disorders based on an androgen deficiency are eliminated by
administration of Proviron. If other factors are the sole cause or if they contribute to
the disorders, Proviron may be administered in support of other therapeutic measures.
Hypogonadism
Growth, development and function of androgen-dependent target organs are
stimulated by Proviron. It promotes development of secondary male sex
characteristics in cases of prepuberal androgen-deficiency.
Proviron 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 Proviron, 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 Proviron.
Since androgens can exacerbate a clinically manifest carcinoma of the
prostate, malignant tumours of the prostate must be ruled out before the start of
Proviron 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 Proviron. 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
Proviron 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 Proviron tablet 3 times per day.
After satisfactory clinical improvement, it can be tried to reduce the dose.
Continuation of treatment:
1 Proviron 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 Proviron tablets
3 times per day for several months.
As maintenance dose, 1 Proviron tablet 2 - 3 times per day will often be
sufficient.
Infertility - for the improvement of sperm quantity and quality:
1 Proviron tablet 2 - 3 times per day for a cycle of spermatogenesis, i.e. for
about 90 days. If necessary, Proviron 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 Proviron tablet twice per day over
several months.
OVERDOSAGE
Acute toxicity studies using single administration showed that Proviron 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, methyl4-hydroxybenzoate, propyl-4-hydroxybenzoate
STORAGE
No special storage conditions are required.
MANUFACTURER
Bayer Weimar GmbH und CO.KG., Germany
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