ANDRODERM
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ANDRODERM (ANDRODERM).
Testosterone is an androgen receptor agonist; it binds to androgen receptors, leading to changes in gene expression that promote male secondary sexual characteristics and maintain libido, muscle mass, and bone density.
| Metabolism | Testosterone is metabolized primarily in the liver via CYP3A4 and CYP2C9 isoenzymes, as well as by 5α-reductase to dihydrotestosterone (DHT) and by aromatase to estradiol. |
| Excretion | Approximately 90% of testosterone metabolites are excreted in urine as glucuronide and sulfate conjugates; 6% are excreted in feces via bile. |
| Half-life | Terminal elimination half-life is approximately 10–100 minutes (rapid), but due to transdermal absorption, effective half-life is extended to about 8–10 hours after patch application. |
| Protein binding | Approximately 98–99% bound: primarily to sex hormone-binding globulin (SHBG, ~40%) and albumin (~60%). |
| Volume of Distribution | Volume of distribution is approximately 0.2–0.8 L/kg, reflecting distribution into steroid-sensitive tissues and binding proteins. |
| Bioavailability | Transdermal bioavailability is approximately 10–15% of the nominal dose (based on 24-hour application), with interindividual variability due to skin permeability. |
| Onset of Action | Following transdermal application, serum testosterone levels rise within 30–60 minutes; clinical effects (e.g., libido, mood) may be noticed within days to weeks. |
| Duration of Action | The transdermal patch provides sustained testosterone levels for 24 hours with once-daily dosing; continuous use is required for maintenance of effects. |
Apply one 2.5 mg or 5 mg transdermal system to clean, dry, intact skin on the abdomen, upper arms, or thighs once daily, preferably in the morning. Starting dose is 5 mg daily; adjust based on serum testosterone levels.
| Dosage form | FILM, EXTENDED RELEASE |
| Renal impairment | No specific dose adjustment recommended for renal impairment. Use with caution in patients with severe renal impairment due to potential fluid retention. |
| Liver impairment | Contraindicated in patients with severe hepatic impairment (Child-Pugh class C). In mild to moderate impairment (Child-Pugh A or B), use with caution and monitor liver function; no specific dose adjustment guidelines. |
| Pediatric use | Not indicated for use in pediatric patients. Safety and efficacy have not been established in children <18 years. |
| Geriatric use | Initiate at 2.5 mg once daily in elderly patients due to increased risk of adverse effects, particularly prostatic hyperplasia and cardiovascular events. Monitor serum testosterone levels and adjust as needed. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ANDRODERM (ANDRODERM).
| Breastfeeding | Testosterone is excreted into human milk; M/P ratio not established. Potential for virilization of female infants and early puberty in male infants. Risk of suppression of maternal lactation (androgen-induced decrease in prolactin). Contraindicated during breastfeeding; alternative therapies recommended. |
| Teratogenic Risk | Androderm (testosterone) is contraindicated in pregnancy due to virilization of female fetus. First trimester: high risk of pseudohermaphroditism in female fetuses (labial fusion, clitoromegaly) with androgen exposure during critical period of genital differentiation (weeks 8-12). Second and third trimesters: risk of clitoral enlargement, advanced bone age, and potential long-term behavioral effects. Male fetuses may experience premature sexual development. No adequate studies; USP pregnancy category X. |
■ FDA Black Box Warning
WARNING: Cardiovascular risk - Increased risk of myocardial infarction, stroke, and cardiovascular death has been reported with testosterone replacement therapy. Only use in men with confirmed hypogonadism.
| Serious Effects |
["Men with carcinoma of the breast or known or suspected carcinoma of the prostate.","Women who are pregnant or may become pregnant (risk of virilization of fetus).","Hypersensitivity to testosterone or any component of the product.","Severe renal or hepatic impairment (risk of fluid retention)."]
| Precautions | ["Elderly patients and those with known cardiovascular risk factors should be monitored for cardiovascular events.","May exacerbate sleep apnea in predisposed individuals.","Can cause erythrocytosis; monitor hematocrit.","May accelerate growth of prostate cancer and benign prostatic hyperplasia; monitor prostate-specific antigen (PSA).","Monitor for signs of virilization in women if used off-label.","Possible hypercalcemia in immobilized patients."] |
| Food/Dietary | No known food interactions. Take with or without food. |
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| Fetal Monitoring | If inadvertent use in pregnancy: fetal ultrasound to assess genital development (female fetus) and growth parameters (bone age). Maternal serum testosterone levels (though not validated for monitoring). Monitor for signs of maternal virilization (hirsutism, voice deepening, clitoromegaly). After delivery, assess infant for any androgen-related anomalies. |
| Fertility Effects | Testosterone suppresses endogenous gonadotropins (LH, FSH), leading to oligospermia or azoospermia in men; may impair spermatogenesis. In women, high doses can disrupt ovulatory cycles and reduce fertility. Reversible upon discontinuation, but recovery may take months. May also impair semen quality and reduce testicular volume. |
| Clinical Pearls | Apply to clean, dry, intact skin on the abdomen, thighs, upper arms, or back. Rotate application sites to minimize skin reactions. Do not apply to genitals or scrotum. Avoid showering or swimming for at least 3-4 hours after application to ensure absorption. Monitor serum testosterone levels 14 days after starting therapy or dose adjustment, drawn in the morning before application. Use with caution in patients with known or suspected prostate cancer or breast cancer. Warn patients about the risk of transfer to women and children through skin contact; cover application site with clothing or wash skin before contact. |
| Patient Advice | Apply the gel to clean, dry, intact skin once daily in the morning. · Rotate application sites to prevent skin irritation. · Avoid direct skin contact with women and children; wash hands thoroughly after application and cover the site with clothing. · Do not apply to the genitals or scrotum. · Do not shower or swim for at least 3-4 hours after application. · Monitor for signs of skin irritation, such as redness or itching. · Report any swelling of the ankles, difficulty breathing, or changes in mood or sleep. · Keep the medication away from children and pets. |