Malestrone - General Information
A potent androgenic steroid and major product secreted by the leydig cells of the testis. Its production is stimulated by luteinizing hormone from the pituitary gland. In turn, testosterone exerts feedback control of the pituitary LH and FSH secretion. Depending on the tissues, testosterone can be further converted to dihydrotestosterone or estradiol. [PubChem]
Pharmacology of Malestrone
Malestrone is a steroid hormone from the androgen group. Malestrone is primarily secreted in the testes of males and the ovaries of females although small amounts are secreted by the adrenal glands. It is the principal male sex hormone and an anabolic steroid. In both males and females, it plays key roles in health and well-being. Examples include enhanced libido, energy, immune function, and protection against osteoporosis. On average, the adult male body produces about twenty times the amount of testosterone than an adult female's body does.
Malestrone for patients
AndroGel (testosterone gel) is a clear, colorless gel medicine that delivers testosterone into your body through your skin. Once AndroGel is absorbed through your skin, it enters your bloodstream and helps your body reach normal testosterone levels. The type of testosterone delivered by AndroGel is the same as the testosterone produced in your body.
- AndroGel should not be applied to the scrotum.
- AndroGel should be applied once daily to clean dry skin.
- After application of AndroGel, it is currently unknown for how long showering or swimming should be delayed. For optimal absorption of testosterone, it appears reasonable to wait at least 5-6 hours after application prior to showering or swimming. Nevertheless, showering or swimming after just 1 hour should have a minimal effect on the amount of AndroGel absorbed if done very infrequently.
- Since alcohol based gels are flammable, avoid fire, flame or smoking until the gel has dried.
Oxyphenbutazone: Concurrent administration of oxyphenbutazone and androgens may result in elevated serum levels of oxyphenbutazone.
Insulin: In diabetic patients, the metabolic effects of androgens may decrease blood glucose and, therefore, insulin requirements.
Propranolol: In a published pharmacokinetic study of an injectable testosterone product, administration of testosterone cypionate led to an increased clearance of propranolol in the majority of men tested.
Corticosteroids: The concurrent administration of testosterone with ACTH or corticosteroids may enhance edema formation; thus, these drugs should be administered cautiously, particularly in patients with cardiac or hepatic disease.
Drug/Laboratory Test Interactions
Androgens may decrease levels of thyroxin-binding globulin, resulting in decreased total T4 serum levels and increased resin uptake of T3 and T4. Free thyroid hormone levels remain unchanged, however, and there is no clinical evidence of thyroid dysfunction.
Androgens are contraindicated in men with carcinoma of the breast or known or suspected carcinoma of the prostate.
AndroGel® is not indicated for use in women, has not been evaluated in women, and must not be used in women.
Pregnant women should avoid skin contact with AndroGel® application sites in men. Testosterone may cause fetal harm. In the event that unwashed or unclothed skin to which AndroGel® has been applied does come in direct contact with the skin of a pregnant woman, the general area of contact on the woman should be washed with soap and water as soon as possible. In vitro studies show that residual testosterone is removed from the skin surface by washing with soap and water.
AndroGel® should not be used in patients with known hypersensitivity to any of its ingredients, including testosterone USP that is chemically synthesized from soy.
Additional information about Malestrone
Malestrone Indication: For replacement therapy in males for conditions associated with a deficiency or absence of endogenous testosterone.
Mechanism Of Action: The effects of testosterone in humans and other vertebrates occur by way of two main mechanisms: by activation of the androgen receptor (directly or as DHT), and by conversion to estradiol and activation of certain estrogen receptors. Free testosterone (T) is transported into the cytoplasm of target tissue cells, where it can bind to the androgen receptor, or can be reduced to 5α-dihydrotestosterone (DHT) by the cytoplasmic enzyme 5α-reductase. DHT binds to the same androgen receptor even more strongly than T, so that its androgenic potency is about 2.5 times that of T. The T-receptor or DHT-receptor complex undergoes a structural change that allows it to move into the cell nucleus and bind directly to specific nucleotide sequences of the chromosomal DNA. The areas of binding are called hormone response elements (HREs), and influence transcriptional activity of certain genes, producing the androgen effects.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Testosterone
Synonyms: Testosterona [Inn-Spanish]; Testosteronum [Inn-Latin]; TES; Testosterone Hydrate; Testosterone Enanthate; Testosterone Cypionate; Testostosterone; Testosteron; Trans-Testosterone; Dea No. 4000
Drug Category: Androgens
Drug Type: Small Molecule; Approved; Investigational
Absorption: Approximately 10% of the testosterone dose applied on the skin surface is absorbed into systemic circulation
Toxicity (Overdose): Side effects include amnesia, anxiety, discolored hair, dizziness, dry skin, hirsutism, hostility, impaired urination, paresthesia, penis disorder, peripheral edema, sweating, and vasodilation.
Protein Binding: 40% of testosterone in plasma is bound to sex hormone-binding globulin and 2% remains unbound and the rest is bound to albumin and other proteins.
Biotransformation: Testosterone is metabolized to 17-keto steroids through two different pathways. The major active metabolites are estradiol and dihydrotestosterone (DHT).
Half Life: 10-100 minutes
Dosage Forms of Malestrone: Gel Topical
Chemical IUPAC Name: (8R,9S,10R,13S,14S,17S)-17-hydroxy-10,13-dimethyl-1,2,6,7,8,9,11,12,14,15,16,17-dodecahydrocyclopenta[a]phenanthren-3-one
Chemical Formula: C19H28O2
Testosterone on Wikipedia: https://en.wikipedia.org/wiki/Testosterone
Organisms Affected: Humans and other mammals