Dosing & Uses
Dosage Forms & Strengths
tablet, buccal: Schedule III
- 30mg
Testosterone Replacement Therapy
Primary hypogonadism (congenital or acquired): Testicular failure due to conditions such as cryptorchidism, bilateral torsion, orchitis, vanishing testis syndrome, orchiectomy, Klinefelter Syndrome, chemotherapy, or toxic damage from alcohol or heavy metals; these men usually have low serum testosterone concentrations and gonadotropins (FSH, LH) above normal range
Hypogonadotropic hypogonadism (congenital or acquired): Gonadotropin or luteinizing hormone-releasing hormone (LHRH) deficiency or pituitary-hypothalamic injury from tumors, trauma, or radiation; these men have low testosterone serum concentrations but have gonadotropins in the normal or low range
1 buccal system (30 mg) to gum region q12hr; place above incisor on alternate sides of mouth
Dosing Considerations
Prior to initiating therapy, confirm the diagnosis of hypogonadism by ensuring that serum testosterone concentrations have been measured in the morning on at least 2 separate days and that these serum testosterone concentrations are below the normal range
Limitations of use
- Safety and efficacy of testosterone in men with “age-related hypogonadism” (also referred to as “late-onset hypogonadism”) have not been established
- Safety and efficacy of testosterone in males aged <18 years have not been established
Safety and efficacy not established
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (0)
Serious - Use Alternative (5)
- cyclosporine
testosterone buccal system increases effects of cyclosporine by decreasing metabolism. Avoid or Use Alternate Drug.
- lonafarnib
testosterone buccal system will increase the level or effect of lonafarnib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration of lonafarnib (a sensitive CYP3A substrate) with weak CYP3A inhibitors is unavoidable, reduce to, or continue lonafarnib at starting dose. Closely monitor for arrhythmias and events (eg, syncope, heart palpitations) since lonafarnib effect on QT interval is unknown.
- pexidartinib
testosterone buccal system and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.
- pretomanid
testosterone buccal system, pretomanid. Either increases toxicity of the other by Other (see comment). Avoid or Use Alternate Drug. Comment: Pretomanid regimen associated with hepatotoxicity. Avoid alcohol and hepatotoxic agents, including herbal supplements and drugs other than bedaquiline and linezolid.
- sotorasib
sotorasib will decrease the level or effect of testosterone buccal system by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If use is unavoidable, refer to the prescribing information of the P-gp substrate for dosage modifications.
Monitor Closely (16)
- atogepant
testosterone buccal system will increase the level or effect of atogepant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- avapritinib
testosterone buccal system will increase the level or effect of avapritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- axitinib
testosterone buccal system increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- carbamazepine
testosterone buccal system increases toxicity of carbamazepine by decreasing metabolism. Use Caution/Monitor.
- finerenone
testosterone buccal system will increase the level or effect of finerenone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Monitor serum potassium during initiation and dosage adjustment of either finererone or weak CYP3A4 inhibitors. Adjust finererone dosage as needed.
- insulin degludec
testosterone buccal system increases effects of insulin degludec by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Androgens may decrease blood glucose and, therefore, may necessitate a decrease in the dose of antidiabetic medication.
- insulin degludec/insulin aspart
testosterone buccal system increases effects of insulin degludec/insulin aspart by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Androgens may decrease blood glucose and, therefore, may necessitate a decrease in the dose of antidiabetic medication.
- insulin inhaled
testosterone buccal system increases effects of insulin inhaled by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Androgens may decrease blood glucose and, therefore, may necessitate a decrease in the dose of antidiabetic medication.
- isavuconazonium sulfate
testosterone buccal system will increase the level or effect of isavuconazonium sulfate by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- ivacaftor
testosterone buccal system increases levels of ivacaftor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Monitor when coadministered with weak CYP3A4 inhibitors .
- lemborexant
testosterone buccal system will increase the level or effect of lemborexant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Lower nightly dose of lemborexant recommended if coadministered with weak CYP3A4 inhibitors. See drug monograph for specific dosage modification.
- lomitapide
testosterone buccal system increases levels of lomitapide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Lomitapide dose should not exceed 30 mg/day.
- midazolam intranasal
testosterone buccal system will increase the level or effect of midazolam intranasal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Coadministration of mild CYP3A4 inhibitors with midazolam intranasal may cause higher midazolam systemic exposure, which may prolong sedation.
- mipomersen
mipomersen, testosterone buccal system. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- stiripentol
stiripentol will increase the level or effect of testosterone buccal system by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. Consider reducing the dose of P-glycoprotein (P-gp) substrates, if adverse reactions are experienced when administered concomitantly with stiripentol.
- tinidazole
testosterone buccal system will increase the level or effect of tinidazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
Minor (39)
- acarbose
testosterone buccal system increases effects of acarbose by pharmacodynamic synergism. Minor/Significance Unknown.
- androstenedione
androstenedione increases effects of testosterone buccal system by pharmacodynamic synergism. Minor/Significance Unknown.
- budesonide
testosterone buccal system, budesonide. Either increases effects of the other by pharmacodynamic synergism. Minor/Significance Unknown. May enhance edema formation.
- chlorpropamide
testosterone buccal system increases effects of chlorpropamide by pharmacodynamic synergism. Minor/Significance Unknown.
- cortisone
testosterone buccal system, cortisone. Either increases effects of the other by pharmacodynamic synergism. Minor/Significance Unknown. May enhance edema formation.
- deflazacort
testosterone buccal system, deflazacort. Either increases effects of the other by pharmacodynamic synergism. Minor/Significance Unknown. May enhance edema formation.
- dexamethasone
testosterone buccal system, dexamethasone. Either increases effects of the other by pharmacodynamic synergism. Minor/Significance Unknown. May enhance edema formation.
- epoetin alfa
testosterone buccal system increases effects of epoetin alfa by pharmacodynamic synergism. Minor/Significance Unknown. Androgens may be used to decrease necessary dose of epoetin alfa.
- fludrocortisone
testosterone buccal system, fludrocortisone. Either increases effects of the other by pharmacodynamic synergism. Minor/Significance Unknown. May enhance edema formation.
- glimepiride
testosterone buccal system increases effects of glimepiride by pharmacodynamic synergism. Minor/Significance Unknown.
- glipizide
testosterone buccal system increases effects of glipizide by pharmacodynamic synergism. Minor/Significance Unknown.
- glyburide
testosterone buccal system increases effects of glyburide by pharmacodynamic synergism. Minor/Significance Unknown.
- hydrocortisone
testosterone buccal system, hydrocortisone. Either increases effects of the other by pharmacodynamic synergism. Minor/Significance Unknown. May enhance edema formation.
- insulin aspart
testosterone buccal system increases effects of insulin aspart by pharmacodynamic synergism. Minor/Significance Unknown.
- insulin detemir
testosterone buccal system increases effects of insulin detemir by pharmacodynamic synergism. Minor/Significance Unknown.
- insulin glargine
testosterone buccal system increases effects of insulin glargine by pharmacodynamic synergism. Minor/Significance Unknown.
- insulin glulisine
testosterone buccal system increases effects of insulin glulisine by pharmacodynamic synergism. Minor/Significance Unknown.
- insulin lispro
testosterone buccal system increases effects of insulin lispro by pharmacodynamic synergism. Minor/Significance Unknown.
- insulin NPH
testosterone buccal system increases effects of insulin NPH by pharmacodynamic synergism. Minor/Significance Unknown.
- insulin regular human
testosterone buccal system increases effects of insulin regular human by pharmacodynamic synergism. Minor/Significance Unknown.
- metformin
testosterone buccal system increases effects of metformin by pharmacodynamic synergism. Minor/Significance Unknown.
- methylprednisolone
testosterone buccal system, methylprednisolone. Either increases effects of the other by pharmacodynamic synergism. Minor/Significance Unknown. May enhance edema formation.
- miglitol
testosterone buccal system increases effects of miglitol by pharmacodynamic synergism. Minor/Significance Unknown.
- nateglinide
testosterone buccal system increases effects of nateglinide by pharmacodynamic synergism. Minor/Significance Unknown.
- pioglitazone
testosterone buccal system increases effects of pioglitazone by pharmacodynamic synergism. Minor/Significance Unknown.
- prednisolone
testosterone buccal system, prednisolone. Either increases effects of the other by pharmacodynamic synergism. Minor/Significance Unknown. May enhance edema formation.
- prednisone
testosterone buccal system, prednisone. Either increases effects of the other by pharmacodynamic synergism. Minor/Significance Unknown. May enhance edema formation.
- repaglinide
testosterone buccal system increases effects of repaglinide by pharmacodynamic synergism. Minor/Significance Unknown.
- rosiglitazone
testosterone buccal system increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown.
- ruxolitinib
testosterone buccal system will increase the level or effect of ruxolitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- ruxolitinib topical
testosterone buccal system will increase the level or effect of ruxolitinib topical by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- saw palmetto
saw palmetto decreases effects of testosterone buccal system by pharmacodynamic antagonism. Minor/Significance Unknown.
- saxagliptin
testosterone buccal system increases effects of saxagliptin by pharmacodynamic synergism. Minor/Significance Unknown.
- sitagliptin
testosterone buccal system increases effects of sitagliptin by pharmacodynamic synergism. Minor/Significance Unknown.
- tacrolimus
testosterone buccal system increases effects of tacrolimus by decreasing metabolism. Minor/Significance Unknown.
- tolazamide
testosterone buccal system increases effects of tolazamide by pharmacodynamic synergism. Minor/Significance Unknown.
- tolbutamide
testosterone buccal system increases effects of tolbutamide by pharmacodynamic synergism. Minor/Significance Unknown.
- triamcinolone acetonide injectable suspension
testosterone buccal system, triamcinolone acetonide injectable suspension. Either increases effects of the other by pharmacodynamic synergism. Minor/Significance Unknown. May enhance edema formation.
- vildagliptin
testosterone buccal system increases effects of vildagliptin by pharmacodynamic synergism. Minor/Significance Unknown.
Adverse Effects
1-10%
Gum or mouth irritation
Abnormal taste
Gum pain or tenderness
Gum edema
Headache
Postmarketing Reports
Vascular Disorders: Venous thromboembolism
Myocardial infarction, stroke
Warnings
Contraindications
Male breast or prostate cancer
Hypersensitivity to ingredients, including soy
Women who are breast feeding, may become pregnant or are pregnant
Cautions
Edema with or without congestive heart failure, may be a complication in patients with pre-existing cardiac, renal, or hepatic disease
Testosterone has been subject to abuse, typically at doses higher than recommended for the approved indication and in combination with other anabolic androgenic steroids; anabolic androgenic steroid abuse can lead to serious cardiovascular and psychiatric adverse reactions
Potential for gynecomastia
Risk of sleep apnea in susceptible patients
Increase risk of BPH and prostate cancer in elderly; monitor patients with benign prostatic hyperplasia (BPH) for worsening of signs and symptoms of BPH
Increased hematocrit (polycythemia), reflective of increased red blood cell mass, may require discontinuation; increases risk for thromboemolism; monitor serum testosterone, prostate specific antigen (PSA), liver function, lipid concentrations, hematocrit and hemoglobin periodically
Skin burns reported at application site in patients wearing an aluminized transdermal system during a magnetic resonance imaging scan (MRI); because transdermal testosterone patch contains aluminum, it is recommended to remove system before undergoing MRI
Venous thromboembolism, including DVT and PE reported in patients using testosterone products; these observations have included patients with and without polycythemia; evaluate signs or symptoms consistent with DVT or PE; if venous thromboembolic event suspected, discontinue treatment with testosterone and initiate appropriate workup and management
Cardiovascular risks
- Some postmarketing studies have shown an increased risk of myocardial infarction and stroke associated with the use of testosterone replacement therapy
- January 31, 2014: The FDA is investigating the risk of stroke, MI, and death in men taking prescription testosterone drugs
- The investigationwas prompted by findings from 2 studies that suggest an increased risk of MI in men who take testosterone
- PLOS ONE (Jan 29, 2014): Analysis of men with a history of MI (N=55,593)showed men >65 yr had a 2-fold increase in the risk of MI within 90 days of filling an initial prescription for a testosterone drug; among younger men (<65 yr) with a history of heart disease, there was a 2- to 3-fold increased risk of MI
- The PLOS ONE study confirmed results of a much smaller study (JAMA November 6, 2013) which found that older men, many with underlying heart disease, had a 30% increased chance of death, MI, and stroke after taking testosterone therapy
Pregnancy & Lactation
Pregnancy Category: X
Lactation: Contraindicated
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Androgen that promotes the growth and development of male sex organs and maintains secondary sex characteristics in androgen deficient males.
Pharmacokinetics
Peak plasma time: 10-12 hr
Half-Life: 10-100 min
Protein binding: 98%
Concentration: 520-550 ng/dL
Excretion: Urine (90%); feces (6%)
Absorption: 10% of applied dose
Metabolism: Liver
Metabolites: Estradiol, dihydrotestosterone
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