Androgens are male hormones which cause development of secondary sex characteristics in male. Indeed, testosterone is responsible for all the changes that occur in a boy at puberty. The testes of an adult male produce 5-12 mg of testosterone (later converted into more active dihydrotestosterone) daily.
In women, ovary produces small quantity of testosterone. Adrenal cortex produces small quantities of dehydroepiandrosterone and androstenedione which are called weak androgens. Besides, a good number of synthetic androgens have been produced.
Methyltestosterone and fluoxymesterone are derivatives of testosterone which are orally active with submaximal androgenic efficacy. In addition, there are some lipid-soluble esters of testosterone which are suitable for injection.
Androgens are used in a variety of clinical cases such as:
Testicular failure: It may be primary –in children, resulting in delayed puberty. Treatment with parenteral testosterone esters or transdermal testosterone or dihydrotestosterone in courses of 4-6 months at a time is highly satisfactory. Secondary testicular failure is corrected gradually over months by androgen treatment.
Hypopituitarism: Hypogonadism is one of the features of hypopituitarism. Androgens are added at the time of puberty to other hormonal replacement.
AIDS related muscle wasting: Testosterone therapy has been shown to improve weakness and muscle wasting in AIDS patients with low testosterone levels.
Hereditary angioneurotic edema: This genetic disorder can be prevented by 17α-alkylated androgens (e.g. methyltestosterone, stanozolol, danazol) but not by testosterone.
Ageing: Because testosterone levels decline in old age, it has been administered elderly males to improve bone mineralization and muscle mass. Occasionally small amount of androgen is added to postmenopausal hormone replacement.
Androgens are available only with your doctor's prescription in the following dosage forms:
Tablet, Extended Release
Capsule, Extended Release
Capsule, Liquid Filled
Patch, Extended Release
2 What to Know Before Using
If you are about to start a drug therapy, the risk-benefit ratio of taking the drug should be considered carefully. Here, the suitable drug therapy is chosen with active participation of both the doctor and the patient.
There are some important factors such as drug interactions, metabolic impairment, hypersensitivity reaction, pregnancy, lactation etc. which may alter the desired therapeutic effects of such medications.
Sometimes the presence of other health disorders affects the beneficial effects of this medicine and even may cause serious toxic effects. If you have had any allergic reactions to any medicine then you must inform your doctor about that.
Further, androgens are contraindicated in carcinoma of prostate and male breast, liver and kidney disease and during pregnancy (because of masculinization of female fetus). They should not be given to men aged more than 65 years, and to those with coronary artery disease or congestive heart failure. Androgen therapy can worsen sleep apnoea, migraine, and epilepsy.
Moreover, certain drugs should not be used concurrently with such medications. It is always recommended to consult with your doctor if you are in need of some other medications or even any over-the-counter medicine for another health problem in order to avoid unwanted toxic effects.
Using androgens with any of the following drugs is not recommended:
You should use this medicine following the directions given by your doctor. The dosage schedule and the duration of drug therapy depend on the particular medical problem for which you are using this medicine.
The therapeutic dose may also vary with patient’s condition or requirement and the strength of the medicine as well. However, different preparations and doses are listed below:
Testosterone (free): 25 mg i.m. daily to twice weekly.
Testosterone propionate: 25-50 mg i.m. daily to twice weekly.
Testosterone propionate 25 mg + testosterone enanthate 100 mg in 1 ml ampoule; 1 ml i.m. weekly.
Testosterone propionate 250 mg + testosterone enanthate 250 mg in 1 ml ampoule; 1 ml i.m. every 2-4 weeks.
Testosterone propionate 20 mg + testosterone phenyl propionate 40 mg + testosterone isocaproate 40 mg in 1 ml ampoule; 1 ml i.m. every 2-3 weeks.
Testosterone propionate 30 mg + testosterone phenyl propionate 60 mg + testosterone isocaproate 60 mg + testosterone decanoate 100 mg in 1 ml ampoule; 1 ml i.m. every 3-4 weeks.
Mesterolone: 1 to 3 tablets of 25 mg daily for androgen deficiency, oligozoospermia and male infertility.
Dihydrotestosterone 25mg/g gel (100 g tube): 5-10 g to be applied over nonscrotal skin once daily. This gel formulation has become the preferred method of androgen replacement for hypogonadism and impotence.
Further, it is advised to store the medicine in a closed container at room temperature away from heat, moisture, and direct light. All kinds of medicines should be kept out of the reach of children. However, outdated medicines should be disposed by an appropriate way.
4 Precautions to Take
Firstly, regular visits to your doctor are recommended to check that this medicine is working properly or not. In case of pregnant women, the use of such medications is not safe because of masculinization of female fetus.
Further, the lactating mothers should not use these drugs, since androgens may pass through the breast milk and may cause premature sexual development in male babies and development of male features in female babies.
In addition, when this drug is used by the patients with diabetes mellitus, the blood sugar levels should be investigated at frequent intervals. If any change in the blood and/or urine sugar tests is noticed, you should check with your doctor immediately.
On the contrary, you should apply the gel (e.g. androgel) 5 to 6 hours before having a bath.
5 Potential Side Effects
There are some unwanted side effects associated with each drug that usually do not need medical attention. These side effects usually go away during the treatment episode as your body adjusts to the medicine.
Your healthcare professional may advise you about the ways how to prevent or reduce those unwanted side effects. Sometimes you may need to consult with the doctor if you notice any of the following toxic effects:
Acne may occur in both males and females. Virilization, excess body hair and menstrual irregularities may occur in women.
Frequent, sustained and often painful erections in males in the beginning of therapy; subside spontaneously after sometime.
Oligozoospermia can occur with moderate doses given for a few weeks to men with normal testosterone levels.
Precocious puberty, premature sexual behavior, and stunting of stature due to early closure of epiphysis –if testosterone is given continuously to young boys for increasing stature.
Gynaecomastia may occur, especially in children and in patients with liver disease. This is due to peripheral conversion of testosterone to estrogens.
Salt retention and edema occur especially when large doses are used in patients with heart and kidney disease. It is rare with the doses used for hypogonadism.
Lowering of HDL and rise in LDL levels, especially with methyltestosterone, fluoxymesterone and other 17α-alkylated analogues.
Cholestatic jaundice occurs with methyltestosterone, fluoxymesterone and some other anabolic steroids in a dose dependent manner, but not with parenterally used esters of testosterone. However, jaundice is reversible on discontinuation.
Incidence of hepatic carcinoma is higher in patients who have received long-term methyltestosterone or other oral androgens.
Prolonged use may produce testicular atrophy. Besides, many effects, e.g. voice change may be permanent after long-term therapy.
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