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Pharmacology for Nurses

37.3 Masculinizing Hormonal Therapy

Pharmacology for Nurses37.3 Masculinizing Hormonal Therapy

Learning Outcomes

By the end of this section, you should be able to:

  • 37.3.1 Identify the characteristics of masculinizing hormonal drugs used for transgender and nonbinary therapy.
  • 37.3.2 Explain the indications, actions, adverse reactions, and interactions of masculinizing hormonal drugs used for transgender and nonbinary therapy.
  • 37.3.3 Describe nursing implications of masculinizing hormonal drugs used for transgender and nonbinary therapy.
  • 37.3.4 Explain the client education related to masculinizing hormonal drugs used for transgender and nonbinary therapy.

The hormones used for reproductive health, covered in Reproductive Health Drugs, are also discussed in this chapter; complete information for the drugs can be found there. Discussion in this chapter focuses on use of the medications to develop male secondary sex characteristics in individuals who were assigned female at birth and choose to undergo female-to-male (FTM) transition. Further transition would include chest masculinization surgery, hysterectomy, and creation of external male genitalia (Mount Sinai, n.d.-a).

The overall effects of masculinizing hormonal drugs on the female body include the growth of facial hair and increased body hair, deepening of the voice, redistribution of subcutaneous fat, increased muscle mass, hairline recession, and, possibly, male pattern baldness (Figure 37.3). Sexual and gonadal effects include an increase in libido, clitoral growth, vaginal dryness, and cessation of menses (Deutsch, 2016; Hembree et al., 2017; Mayo Clinic, 2021b; Unger, 2016).

Although male hormone therapy produces some of the secondary male characteristics in females who are transitioning to males, it also has adverse effects that may be problematic. Possible complications include weight gain, acne, male pattern baldness, sleep apnea, elevated cholesterol, hypertension, polycythemia, type 2 diabetes, infertility, deep vein thrombosis, pulmonary embolism, increased risk for heart disease, drying and thinning of the vaginal lining, pelvic pain, and clitoral discomfort (Mayo Clinic, 2021b).

One major consideration for any transgender male is the danger the hormones pose to a fetus. Testosterone in particular is teratogenic, but other hormones are as well (Rodriguez-Wallberg et al., 2022). Thus, the nurse must ensure that a female client transitioning to male has had a negative pregnancy test.

A diagram shows the areas of the body that are altered by drugs used for F T M transition. There is hair loss at the scalp, increased oiliness in the skin, and acne. Increased muscle mass and strength occur in the arms. The voice deepens. Facial and body hair grows. Fat redistribution occurs in the stomach. Clitoral enlargement and vaginal atrophy also occur.
Figure 37.3 Drugs used for female-to-male transition affect many areas of the body. (attribution: Copyright Rice University, OpenStax, under CC BY 4.0 license)


Androgens are a group of male hormones, including testosterone. They can be endogenous (produced in the body) or synthetic (developed in a laboratory). All forms of androgens assist with the development of male secondary sex characteristics (Deutsch, 2016; Hembree et al., 2017; Mayo Clinic, 2021b; T’Sjoen et al., 2019; Unger, 2016). In the case of FTM transition, synthetic androgens must be administered exogenously because the female body does not produce them.

Androgens increase the retention of nitrogen, sodium, potassium, and phosphorous and decrease the urinary excretion of calcium. Therefore, a female client transitioning to male should be evaluated for any underlying condition that would be affected by increased levels of these electrolytes, primarily cardiac and renal disorders (DailyMed, Testosterone cypionate, 2018).

Safety Alert

Androgens and Diabetic Medication

Androgens can decrease blood glucose levels in clients with diabetes. Dosages of insulin and other hypoglycemic medications must be monitored and possibly decreased to prevent dangerous hypoglycemic events.

(Source: DailyMed, Testopel, 2018)


Danazol is a synthetic androgen that inhibits pituitary gonadotropins and in turn suppresses ovarian response to the pituitary. Danazol has weak properties and acts similarly to testosterone. In females it causes masculinization effects. Generally, the pituitary-suppressive action of danazol is reversible.

Contraindications to danazol include hypersensitivity; undiagnosed abnormal genital bleeding; markedly impaired hepatic, renal, or cardiac function; pregnancy; breastfeeding; androgen-dependent tumor; and active thrombosis or thromboembolic disease or a history of such events. Danazol may cause some fluid retention, so it should be used cautiously in clients with conditions that may be affected by excess fluid, including epilepsy, migraine, cardiac or renal dysfunction, polycythemia, and hypertension. Danazol should also be used with caution inclients with diabetes (DailyMed, Danazol, 2023).


Testosterone is a hormone responsible for the development of male sex organs and secondary sex characteristics. These characteristics include the male pattern of hair distribution (pubic area, axillae, face, and chest), deepening of the voice, heavier bone structure, increased hematocrit, and differences in fat distribution (T’Sjoen et al., 2019). Testosterone undecanoate is an androgen and anabolic steroid medication used mainly to treat low testosterone levels in male clients. It is also used to promote secondary sex characteristics in females transitioning to males (DailyMed, Aveed, 2021; T’Sjoen et al., 2019).

A realistic target for hormone therapy for FTM transition is to administer testosterone until testosterone levels are within the typical male physiologic range (320–1000 ng/dL).

Table 37.7 lists common forms of testosterone and typical routes and dosing for adult clients.

Drug Routes and Dosage Ranges
Testopel pellet 75 mg subcutaneous implant (6 pellets implanted every 3–4 months).
Testosterone enanthate
Testosterone cypionate
50–100 mg intramuscularly/subcutaneously weekly or 100–200 mg intramuscularly every 2 weeks.
Testosterone gel 50–100 mg daily.
Testosterone patch
(AndroGel, Androderm)
2.5–7.5 mg daily transdermally.
Testosterone undecanoate 1000 mg intramuscularly every 12 weeks or 750 mg intramuscularly every 10 weeks.
Table 37.7 Drug Emphasis Table: Testosterone (sources:; Coleman et al., 2022)

Fluoxymesterone and Methyltestosterone

Fluoxymesterone and methyltestosterone are anabolic steroids. Their use in FTM transition is to assist in the development of secondary male sex characteristics. Contraindications and precautions include pregnancy; diabetes; and liver, renal, or cardiac disease. Adverse effects include acne, heart or blood vessel problems, stroke, liver problems, mental or mood problems, and infertility. For more information regarding anabolic steroids, see Reproductive Health Drugs.


Progesterone has some minor anabolic and adrenergic properties that can help with development of male characteristics (increased hair growth) and suppression of female characteristics (decreased breast size). See Reproductive Health Drugs for more information about progesterone. For individuals who do not want therapies that contain estrogen, are at risk for thromboembolic complications, or have other contraindications, progesterone is an alternative to estrogen.

Clinical Tip

Target for Hormone Therapy

A practical target for hormone therapy for FTM transition is to administer testosterone until testosterone levels reach the typical cisgender male physiologic range (320–1000 ng/dL).

(Source: Hembree et al., 2017)

Table 37.8 is a drug prototype table for masculinizing hormones featuring the testosterone patch. It lists drug class, mechanism of action, adult dosage, indications, therapeutic effects, drug and food interactions, adverse effects, and contraindications.

Drug Class
Masculinizing hormone

Mechanism of Action
Suppresses estrogen and enhances testosterone
Drug Dosage
2.5–7.5 mg daily transdermally.
For use in FTM transgender transition

Therapeutic Effects
Increased muscle mass
Increased body hair
Increased libido
Voice deepening
Cessation of menses
Drug Interactions
Oral anticoagulants
Hyperglycemic drugs (doses may need to be decreased because the testosterone patch may decrease blood glucose levels inclients with diabetes)

Food Interactions
No significant interactions
Adverse Effects
Application site pruritus, blistering, erythema
Back pain
Gastrointestinal bleeding
Pelvic pain
Decreased libido
Presence of a hormone-sensitive cancer
History of blood clots (deep vein thrombosis or pulmonary embolism)
Serious cardiac, hepatic, or renal disease
Significant mental health conditions, such as severe depression or psychosis, that have not been addressed
Table 37.8 Drug Prototype Table: Testosterone Patch (sources:; Coleman et al., 2022)

Nursing Implications

The nurse should do the following for clients who are taking masculinizing hormones:

  • Assess baseline health, including underlying medical conditions, current medications, and pertinent laboratory and diagnostic results.
  • Be cognizant of the client’s feelings, values, and culture in order to render sensitive care.
  • Be knowledgeable about drug actions, side effects, contraindications, and precautions and assess the client’s knowledge and understanding.
  • Obtain a hematocrit and lipid profile before the client starts hormone therapy and at follow-up visits.
  • Monitor virilizing and adverse effects every 3 months for the first year and then every 6–12 months.
  • Assess serum testosterone at follow-up visits, with a practical target in the male range of 400–700 ng/dL. Peak levels for clients taking parenteral testosterone can be measured 24–48 hours after injection. Trough levels can be measured immediately before injection.
  • Screen for bone mineral density before clients at risk for osteoporosis start hormone therapy. Otherwise, screening can start at age 60 or, if sex hormone levels are consistently low, earlier.
  • Screen clients with cervixes or breasts appropriately.
  • Ensure that the client understands issues related to family planning and has had an opportunity to meet with a family planning specialist. Resources are available for various options, such as freezing eggs or donating eggs to a partner or gestational surrogate.
  • Ensure that the client is aware of and has access to resources such as community organizations, specialty clinics and hospitals, and support groups.
  • Provide client teaching regarding the drug and when to call the health care provider. See below for client teaching guidelines.

Client Teaching Guidelines

The client taking a masculinizing hormone should:

  • Know the names, actions, effects, side effects, contraindications, and precautions related to each medication.
  • Understand the schedule for medication administration—time, dosage, and route.
  • Know how to self-administer parenteral or transdermal medication.
  • Be aware of drug–drug, drug–food, and drug–herbal interactions as indicated for specific drugs, such as testosterone and warfarin and diabetes medications.
  • Notify the health care provider if any of the following occur:
    • Serious reactions to any drug, including swelling of the mouth, lips, or tongue; respiratory problems; or skin rash
    • Any adverse effect that becomes too uncomfortable (e.g., clitoral enlargement, acne)
    • New onset of diabetes or a thyroid disorder; substantial weight changes; subjective or objective evidence of regression of virilization; or new symptoms potentially precipitated or exacerbated by hormone imbalances, such as hot flashes, pelvic cramping, or bleeding
  • Be aware of fertility considerations and the available options.
  • Continue to attend wellness visits and schedule routine diagnostic procedures such as for prostate and breast cancer prevention.

FDA Black Box Warning


Danazol can result in androgenic effects on the female fetus. If a client becomes pregnant while on therapy, the drug should be discontinued. A pregnancy test is required before clients of childbearing age begin therapy, and a nonhormonal method of contraception should be used during therapy.


Virilization has been reported in children who were secondarily exposed to topical testosterone gel/solutions. Children should avoid contact with adult application sites for these products.

Serious reactions, involving urge to cough, dyspnea, throat tightening, chest pain, dizziness, syncope, and episodes of anaphylaxis, have been reported to occur during or immediately after the administration of testosterone undecanoate injection. This product is available through a REMS program and requires that clients be observed in the health care setting for 30 minutes in order to provide appropriate medical treatment in the event of serious reactions or anaphylaxis.

Testosterone enanthate (subcutaneous) and testosterone undecanoate (oral) can cause blood pressure increases that can increase the risk for major adverse cardiovascular events, including nonfatal myocardial infarction, nonfatal stroke, and cardiovascular death, especially in clients with cardiovascular risk factors or established cardiovascular disease. Before initiating testosterone enanthate, consider the client’s baseline cardiovascular risk and ensure blood pressure is adequately controlled. Additionally, blood pressure should be monitored throughout the treatment period and risk versus benefits evaluated for clients who develop cardiovascular risk factors or disease while on treatment.


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