How Do Androgens Work?

Androgens are a class of drugs used to treat symptoms of low testosterone in adult men who have hypogonadism (a condition in which the body does not produce enough natural testosterone) in males and metastatic breast cancer in females. Androgens are a group of hormones that play a key role in male traits and reproductive activity. The predominant and most active androgen is testosterone, which is produced by the male testes. The other androgens that support the functions of testosterone are produced mainly by the adrenal cortex—the outer portion of the adrenal glands—in relatively small quantities. In males, testosterone is responsible for many normal functions, including the growth and development of the genitals, muscles, and bones and maintenance of secondary sex characteristics. It is also present in the female body (produced in the ovaries, adrenal glands, and fat cells), although in small amounts.

Some of the functions of testosterone in the male body including:

• Starting and completing the process of puberty
• Bone and muscle development
• Growth of body hair, including facial hair
• Change of vocal cords to produce the adult male voice
• Sex drive (libido) and sexual function
• Growth and function of the prostate gland
• Sperm production

Androgens (testosterone) are used only for men with low testosterone levels (normal total testosterone range is approximately 300 ng/dL) caused by certain medical conditions, including disorders of the testicles, pituitary gland (a small gland in the brain), or hypothalamus (a part of the brain) that causes hypogonadism.

Some of the symptoms of androgen deficiency in males include:

• Reduced sexual desire
• Hot flushes and sweating
• Breast development (gynecomastia)
• Lethargy and fatigue
• Depression
• Reduced muscle mass and strength
• Increased body fat, particularly around the abdomen
• Weaker erections and orgasms
• Reduced amount of ejaculate
• Loss of body hair
• Reduced bone mass; therefore, increased risk of osteoporosis

Androgens are administered via oral, topical (gels and transdermal patch), and intranasal routes.

Androgens work in the following ways:

• They supplement or replace the natural production of testosterone and reverse the symptoms of low testosterone.
• They imitate the properties of the naturally occurring hormone “testosterone” and activate the body’s testosterone receptors.
• They suppress the pituitary-ovarian axis by inhibiting the output of pituitary gonadotropins.
• They depress the preovulatory surge in output of follicle-stimulating hormone and luteinizing hormone, thereby reducing ovarian estrogen production. 
• In fibrocystic breast disease, they suppress estrogenic stimulation as a result of decreased ovarian production of estrogen.
• In addition, they increase the amount of protein made by the body. This protein is used to build more muscle and increase body weight.

Androgens are used in the following conditions:

In males

• Primary hypogonadism in males because of:
  • Testicular failure due to cryptorchidism (a condition in which one or both of the testes fail to descend from the abdomen into the scrotum)
  • Bilateral testicular torsion (a rare condition with a majority of cases occurring in neonates)
  • Orchitis (inflammation of one or both testicles)
  • Vanishing testis syndrome (a developmental anomaly characterized by the absence of one or both testicles with partial or complete absence of testicular tissue)
  • Orchidectomy (a surgical procedure in which one or both testicles are removed)
  • Klinefelter syndrome (a chromosomal condition in boys and men which can affect physical and intellectual development)
  • Chemotherapy
  • Toxic damage from alcohol or heavy metals
• Hypogonadotropic hypogonadism because of:
  • Idiopathic gonadotropin or luteinizing-hormone releasing hormone deficiency
  • Pituitary-hypothalamic injury from tumors, trauma, or radiation (a small gland in the brain)
• Androgen deficiency
• Hypogonadism, climacteric, and impotence (persistent difficulty achieving and maintaining an erection sufficient to have sex)
• Postpubertal cryptorchidism (both the testes remain within the abdominal cavity)

In females

• Inoperable breast carcinoma
• Endometriosis (a condition in which tissue similar to that which lines the inside of the uterine wall grows outside the uterus)
• Postpartum breast pain and engorgement (pain and fullness in breasts postdelivery)
• Fibrocystic breast disease (swollen, tender breasts with noncancerous lumps)

In both sexes

• Hereditary angioedema (an inherited condition that causes episodes of swelling in the hands, feet, face, airway, or intestines)
• Bone pain due to osteoporosis (a condition in which the bones become thin and weak and break easily) 
• Promotes weight gain after:
  • Weight loss following extensive surgery
  • Chronic infections
  • Severe trauma
  • Weight loss due to unknown etiology
• HIV wasting syndrome (progressive, involuntary weight loss which is not attributable to any condition other than HIV infection itself)
• Muscular dystrophy (a group of diseases that cause progressive weakness and loss of muscle mass)

Some of the common side effects include:

• Headache
• Diarrhea
• Nausea
• Vomiting
• Itching/burning at the application site
• Oily skin or hair
• Acne
• Flushing
• Rash
• Skin color changes
• Nasal discomfort/dryness

Other rare side effects include:

• Dizziness (feeling faint, weak, or unsteady)
• Allergic contact dermatitis
• Hair loss
• Insomnia (trouble falling and/or staying asleep)
• Hypertension (high blood pressure)
• Increased/decreased sexual interest
• New or worsening acne (especially in women and prepubertal men)
• Enlargement of the breasts
• Increase in facial hair
• Abnormal or absent menstrual periods
• Frequent, difficult, or painful urination
• Weight gain
• Vaginal dryness/irritation
• Deepening of voice
• Increased serum prostate-specific antigen level
• Mental/mood changes (such as anxiety, depression, increased anger)
• Allergic reactions
• Rash
• Hives (itchy, raised welts that are found on the skin)
• Itching
• Swelling of face, lips, tongue, or throat

Information contained herein is not intended to cover all possible side effects, precautions, warnings, drug interactions, allergic reactions, or adverse effects. Check with your doctor or pharmacist to make sure these drugs do not cause any harm when you take them along with other medicines. Never stop taking your medication and never change your dose or frequency without consulting your doctor.

Generic and brand names of androgens include:

• Androderm
• AndroGel
• Android
• Aveed
• Axiron
• Danazol
• Depo-Testosterone
• Fortesta
• Jatenzo
• Methitest
• Methyltestosterone
• Natesto
• Oxandrin
• Oxandrolone
• Striant
• Testim
• Testopel
• Testosterone
• Testosterone buccal system
• Testosterone intranasal
• Testosterone topical
• Testred
• Vogelxo
• Xyosted