TESTOSTERONE

In Ontario, options for testosterone administration include injectable and transdermal preparations (patch or gel). Injectable formulations are most commonly used, due to their better efficacy and affordability. While intramuscular (IM) injection is the most common means of administering testosterone, subcutaneous (SC) delivery has also been used with clinical efficacy and is very well-tolerated. Often SC formulations are less painful and preferential for self-administration. A dose reduction of 10-15% can be considered if switching from IM to SC.

CONTRAINDICATIONS

• Pregnancy or breastfeeding.

• Active known sex hormone-sensitive cancer (e.g. breast, endometrial).

• Unstable ischemic cardiovascular disease.

• Poorly controlled psychosis or acute homicidality.

• Psychiatric conditions that limit the ability to provide informed consent.

• Hypersensitivity to one of the components of the formulation
  (recall cypionate is in cottonseed oil-base, and enanthate is in a sesame oil-base).

FORMULATIONS & RECOMMENDED DOSES OF TESTOSTERONE

* Price quotes provided by www.pharmacy.ca. The prices listed above are accurate as of June 2018 and represent the price of the generic brand of medication unless otherwise indicated (ranging from low dose to maximum dose). Prices include a usual and customary dispensing fee of $9 99, which may vary from pharmacy to pharmacy.

a)  Testosterone enanthate is compounded in sesame oil, and testosterone cypionate is compounded in cottonseed oil; patients with allergy to either of these compounds should use the alternative agent

b)  Androderm brand, per drug monograph the 12.2 mg patch delivers 2.5 mg/day while the 24.3 mg patch delivers 5 mg per day

c)  Each pump bottle provides 60 pumps, 1 pump = 1.25 g of gel, equivalent to 12.5 mg of testosterone

NB: Testosterone (in all forms) is considered a controlled substance in Canada; prescriptions should be written in accordance with provincial requirements for controlled substances.

SAFETY

Gel formulations have the risk of inadvertent exposures to others who come into contact with the patient’s skin. This is of particular importance for patients with young children and/or with intimate partners who are pregnant or considering pregnancy.

Keep in mind: Testosterone therapy does not prevent pregnancy even if amenorrhea is achieved. Testosterone is a teratogen thus reliable contraception may be required depending on sexual practices.

PREVENTIVE CARE

Transmasculine patients maintained on masculinizing hormone therapy have unique preventive care needs and recommendations. An adapted Preventive Care Checklist for transmasculine patients can be used at the point of care can be found in the full Sherbourne Health Guidelines.

EFFECTS AND EXPECTED TIME COURSE OF TESTOSTERONE

The degree and rate of physical effects are dependent on the dose and route of administration(2), as well as patient-specific factors such as age, genetics, body habitus and lifestyle.

Hormone therapy results in both reversible and irreversible masculinization.

Keep in mind: Use patient-preferred terminology. Terminology such as “clitoral” and “vaginal” may be upsetting to some but not all.

Desired androgenic effects of testosterone therapy include deepened voice, cessation of menses, clitoral growth, increased muscle mass, and hair growth in androgen-dependent areas including facial hair. Breast tissue may lose glandularity, but generally does not lose mass or hemi circumference. Typically, patients taking testosterone will experience masculinizing changes over a period

of months to years. The timeframe of physiologic changes may be slightly slower with the use of transdermal preparations.

a)  Estimates represent published and unpublished clinical observations 3-6

b)  Significantly dependent on the amount of exercise

c)  Highly dependent on age and inheritance; may be minimal

MONITORING STRATEGIES & DOSE ADJUSTMENTS

• Standard monitoring of testosterone should be employed at baseline, 3, 6, and 12 months; and yearly thereafter if dosing is stable.

• Some clinicians prefer to see patients monthly until an effective dose is established.

• Follow up visits should include a functional inquiry, targeted physical exam, blood work, and health promotion/disease prevention counselling as indicated.

• Titration of doses will generally occur in the early phases of treatment. For example, with injectable testosterone, a starting dose of 30 mg injected weekly could be increased by 10–20 mg every 4–6 weeks, but is typically reviewed and increased q3 months. Speed of titration will depend on lab results, patient goals, response, and side effects.

• For those using an injectable route, there may be utility in varying the timing of blood work to gather information regarding serum hormone levels throughout the cycle (peak, mid-cycle, and trough), especially if a patient is reporting cyclic symptoms.

• Hormone levels for those seeking a more androgynous appearance may intentionally be mid-range between male and female norms.

• Supraphysiologic levels should be avoided due to the increased risk of adverse events and side effects, as well as the potential for the aromatization of excess testosterone into estrogen (this excess aromatization has the potential to lead to gynecomastia as an unwanted side effect). Dose reduction is warranted if supraphysiologic doses are measured at mid-cycle or trough levels.

• There may be some irregular bleeding or spotting in the first few months of treatment. However, once sustained menstrual cessation is achieved, any vaginal bleeding without explanation (e.g. missed dose(s) or lowered dose of testosterone) warrants a full workup for endometrial hyperplasia/cancer.

Keep in mind lab reference ranges:

Clinical effects are the goal of therapy, not specific lab values. If the sex marker associated with the patient’s health card has not been changed, the reported reference ranges will refer to the sex assigned at birth. Reference ranges vary between laboratories - refer to reference ranges from the specific laboratory (often available online or by request from the lab).

HORMONE MONITORING SUMMARY FOR TRANSMASCULINE PATIENTS

In this table, smaller and white check-marks indicate parameters that are measured under particular circumstances.

Non-hormone labs:

Cis-Male reference ranges should be used for Hb/Hct (lower limit of cis-female range can be used if menstruating, but clinical goal is often to suppress the menstrual cycle).

NB: Individual parameters should be considered more frequently if concerns identified or existing factors are present

• a)  Post-gonadectomy: Elevated LH may have implications regarding bone mineral density (See full Guidelines)

• b)  During the first year of treatment only

• c)  Once at either 6- or 12-month mark