Testosterone (buccal)

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Testosterone (buccal)
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Turky Alkathery, M.D. [2]

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Overview

Testosterone (buccal) is a steroid hormone from the androgen group that is FDA approved for the treatment of deficiency or absence of endogenous testosterone. Common adverse reactions include gum or mouth irritation, bitter taste, gum pain, gum tenderness, headache, gum edema and taste perversion.

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Indications

  • Testosterone (buccal) is indicated for replacement therapy in adult males for conditions associated with a deficiency or absence of endogenous testosterone:
  • Primary hypogonadism (congenital or acquired) – testicular failure due to cryptorchidism, bilateral torsion, orchitis, vanishing testis syndrome, orchiectomy, Klinefelter’s syndrome, chemotherapy, or toxic damage from alcohol or heavy metals. These men usually have low serum testosterone levels and gonadotropins (follicle-stimulating hormone [FSH], luteinizing hormone [LH]) above the normal range.
  • Hypogonadotropic hypogonadism (congenital or acquired) – idiopathic gonadotropin or luteinizing hormone-releasing hormone (LHRH) deficiency, or pituitary hypothalamic injury from tumors, trauma, or radiation. These patients have low serum testosterone levels but have gonadotropins in the normal or low range.
  • Limitations of use:
  • Safety and efficacy of testosterone (buccal) in males less than 18 years old have not been established.

Dosage

Dosage Information

  • The recommended dosage for testosterone (buccal) is the application of one buccal system (30 mg) to the gum region twice daily; morning and evening (about 12 hours apart).
  • To ensure proper dosing, serum testosterone concentrations should be measured. Morning, pre-dose serum testosterone concentrations should be measured at 4 to 12 weeks after initiation of therapy to ensure proper serum testosterone concentrations are achieved. Testosterone (buccal) therapy should be discontinued if serum testosterone concentrations are consistently outside of the normal range (300 to 1050 ng/dL) despite the use of one buccal system applied twice daily.

Administration Instructions

  • Testosterone (buccal) should be placed in a comfortable position just above the incisor tooth (on either side of the mouth). With each application, testosterone (buccal) should be rotated to alternate sides of the mouth.
  • Upon opening the packet, the rounded side surface of the buccal system should be placed against the gum and held firmly in place with a finger over the lip and against the product for 30 seconds to ensure adhesion. Testosterone (buccal) is designed to stay in position until removed. If the buccal system fails to properly adhere to the gum or should fall off during the 12-hour dosing interval, the old buccal system should be removed and a new one applied.
  • If the buccal system falls out of position within the first 8 hours of dosing, replace with a new system and continue for a total of 12 hours from the placement of the first system. If the system falls out of position after 8 hours of dosing, a new buccal system should be applied and it may remain in place for 12 hours then continue with the next regularly scheduled dosing.
  • Patients should take care to avoid dislodging the buccal system. Patients should check to see if testosterone (buccal) is in place following consumption of food or alcoholic/non-alcoholic beverages. Testosterone (buccal) should not be chewed or swallowed. To remove testosterone (buccal), gently slide it downwards from the gum toward the tooth to avoid scratching the gum. The testosterone (buccal) buccal system should be removed before routine morning and evening oral care is performed, followed by application of a new buccal system.

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

  • There is limited information regarding Off-Label Guideline-Supported Use of Testosterone (buccal) in adult patients.

Non–Guideline-Supported Use

  • There is limited information regarding Off-Label Non–Guideline-Supported Use of Testosterone (buccal) in adult patients.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

  • Safety and effectiveness of testosterone (buccal) in males less than 18 year of age have not been established. Improper use may result in acceleration of bone age and premature closure of the epiphyses.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

  • There is limited information regarding Off-Label Guideline-Supported Use of Testosterone (buccal) in pediatric patients.

Non–Guideline-Supported Use

  • There is limited information regarding Off-Label Non–Guideline-Supported Use of Testosterone (buccal) in pediatric patients.

Contraindications

  • Testosterone (buccal) is contraindicated in men with carcinoma of the breast or known or suspected carcinoma of the prostate.
  • Testosterone (buccal) is contraindicated in women who are or may become pregnant, or who are breastfeeding. Testosterone (buccal) may cause fetal harm when administered to a pregnant woman. Testosterone (buccal) may cause serious adverse reactions in nursing infants. Exposure of a fetus or nursing infant to androgens may result in varying degrees of virilization.

Warnings

Gum-Related Adverse Reactions and Limited Long-Term Information on Oral Safety

  • Gum-related adverse reactions, including severe gum irritation, were reported in clinical trials of testosterone (buccal). Long-term clinical trial data on gum safety is available in only a limited number of patients (117 patients, 51 patients and 48 patients with at least 6 months, 1 year, and 2 years of exposure, respectively). It is recommended that patients regularly inspect their own gum region where testosterone (buccal) is applied. Any abnormal finding should be brought promptly to the attention of the patient’s physician. In such circumstances, dental consultation may be appropriate.

Worsening of Benign Prostatic Hyperplasia (BPH) and Potential Risk of Prostate Cancer

  • Patients with BPH treated with androgens are at an increased risk for worsening of signs and symptoms of BPH. Monitor patients with BPH for worsening signs and symptoms.
  • Patients treated with androgens may be at increased risk for prostate cancer. Evaluate patients for prostate cancer prior to initiating and during treatment with androgens.

Polycythemia

  • Increases in hematocrit, reflective of increases in red blood cell mass, may require lowering or discontinuation of testosterone. Check hematocrit prior to initiating treatment. It would also be appropriate to re-evaluate the hematocrit 3 to 6 months after starting treatment, and then annually. If hematocrit becomes elevated, stop therapy until hematocrit decreases to an acceptable concentration. An increase in red blood cell mass may increase the risk of thromboembolic events.

Venous Thromboembolism

  • There have been postmarketing reports of venous thromboembolic events, including deep vein thrombosis (DVT) and pulmonary embolism (PE), in patients using testosterone products, such as testosterone (buccal). Evaluate patients who report symptoms of pain, edema, warmth and erythema in the lower extremity for DVT and those who present with acute shortness of breath for PE. If a venous thromboembolic event is suspected, discontinue treatment with testosterone (buccal) and initiate appropriate workup and management.

Use in Women

  • Due to lack of controlled evaluations in women and potential virilizing effects, testosterone (buccal) is not indicated for use in women.

Potential for Adverse Effects on Spermatogenesis

  • With large doses of exogenous androgens, including testosterone (buccal), spermatogenesis may be suppressed through feedback inhibition of pituitary follicle-stimulating hormone (FSH) which could possibly lead to adverse effects on semen parameters including sperm count.

Hepatic Adverse Effects

  • Prolonged use of high doses of orally active 17-alpha-alkyl androgens (e.g., methyltestosterone) has been associated with serious hepatic adverse effects (peliosis hepatis, hepatic neoplasms, cholestatic hepatitis, and jaundice). Peliosis hepatis can be a life-threatening or fatal complication. Long-term therapy with testosterone enanthate, which elevates blood levels for prolonged periods, has produced multiple hepatic adenomas. Testosterone is not known to produce these adverse effects. Nonetheless, patients should be instructed to report any signs or symptoms of hepatic dysfunction (e.g., jaundice). If these occur, promptly discontinue testosterone (buccal) while the cause is evaluated.

Edema

  • Androgens, including testosterone (buccal), may promote retention of sodium and water. Edema with or without congestive heart failure may be a serious complication in patients with preexisting cardiac, renal, or hepatic disease. In addition to discontinuation of the drug, diuretic therapy may be required.

Gynecomastia

  • Gynecomastia may develop and persist in patients being treated with androgens, including testosterone (buccal), for hypogonadism.

Sleep Apnea

  • The treatment of hypogonadal men with testosterone may potentiate sleep apnea in some patients especially those with risk factors such as obesity or chronic lung diseases.

Lipids

  • Changes in the serum lipid profile may occur. Monitor the lipid profile periodically, particularly after starting therapy.

Hypercalcemia

  • Androgens, including testosterone (buccal), should be used with caution in cancer patients at risk of hypercalcemia (and associated hypercalciuria). Regular monitoring of serum calcium concentrations is recommended in these patients.

Decreased Thyroxine-binding Globulin

  • Androgens, including testosterone (buccal), may decrease concentrations of thyroxine-binding globulins, resulting in decreased total T4 concentrations and increased resin uptake of T3 and T4. Free thyroid hormone concentrations remain unchanged, however, and there is no clinical evidence of thyroid dysfunction.

Adverse Reactions

Clinical Trials Experience

  • Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug can not be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

Twelve Week Clinical Trials in Hypogonadal Men

  • In the Phase 3, open-label study, 98 patients received testosterone (buccal) for up to 12 weeks. Adverse reactions to testosterone (buccal) reported by ≥1% of patients are listed in Table 1.
This image is provided by the National Library of Medicine.
  • Gum irritation generally resolved in 1 to 8 days. Gum tenderness resolved in 1 to 14 days.
  • The following adverse reactions to testosterone (buccal) occurred in 1 patient each: acne, anxiety, breast enlargement, breast pain, buccal mucosal roughening, difficulty in micturition, fatigue, gingivitis, gum blister, gustatory sense diminished, hematocrit increased, lipids serum increased, liver function tests abnormal, nose edema, stinging of lips, and toothache.
  • There was one additional 12-week study in 12 patients. In this study, additional adverse reactions to testosterone (buccal) and reported by 1 patient each included emotional lability and hypertension.

Long-Term Extension Clinical Trials in Hypogonadal Men

  • In two extension trials, a total of 117 and 51 patients received testosterone (buccal) for at least 6 months and 1 year, respectively.
  • Of 117 patients treated for at least 6 months, adverse reactions reported by 1 patient each included: anxiety, buccal inflammation, depression, dry mouth, gum redness, hypertension, infection, medication error, nausea, pruritus, renal function abnormal, stomatitis, taste bitter, taste perversion and toothache. Polycythemia and increased serum prostate specific antigen (PSA) were reported in three and two patients, respectively.
  • In these two extension studies, a total of 48 patients received testosterone (buccal) for at least 2 years. In these patients, adverse reactions included: gingival recession, lip ulceration, stomatitis, rash, prostate cancer, increased PSA, abdominal pain, diarrhea, hypertension aggravated, headache, nervousness, polycythemia, taste perversion, aggressiveness, hyperlipidemia, peripheral edema, and anxiety.

Gum-related adverse events and gum examinations

  • In the open-label study, all reported gum-related adverse events were collected and gum examinations were conducted at Baseline and every month thereafter.
  • A total of 16 patients reported 19 gum-related adverse reactions. Of these, ten patients (10.2%) reported 12 reactions of mild intensity, four patients (4.1%) reported 5 reactions of moderate intensity, and two patients (2.0%) reported 2 reactions of severe intensity. Four patients (4.1%) discontinued treatment with testosterone (buccal) due to gum or mouth-related adverse reactions including two with severe gum irritation, one with mouth irritation, and one with “bad taste in mouth.” Gum irritation generally resolved in 1 to 8 days. Gum tenderness resolved in 1 to 14 days.
  • Monthly gum examinations were conducted to assess for gingivitis, gum edema, oral lesions, ulcerations or leukoplakia. No cases of ulceration or leukoplakia were observed. No new oral lesions were observed. The incidence of gingivitis and gum edema was not increased during treatment.
  • In the two extension trials, gum examinations were conducted every 3 months while on treatment. In one of these trials, no patient had a gum abnormality, and in the other trial, moderate gingivitis and mild gum edema were reported by 1 patient each.
  • In these two extension studies, patient-reported information on testosterone (buccal) gum adherence was collected every 3 months for 1 year. At each visit, 37% to 52% of patients reported problems with testosterone (buccal) adhering to the gum. Circumstances surrounding testosterone (buccal) detachment included eating, drinking and oral care. Hot foods and hot beverages were more likely to be associated with detachment than cold food and cold beverages.

Postmarketing Experience

  • The following adverse reactions have been identified during post approval use of testosterone (buccal). Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure: dry mouth, gingival swelling, lip swelling, mouth ulceration, stomatitis, red blood cell increased, dysgeusia, and venous thromboembolism.

Drug Interactions

Insulin

  • Changes in insulin sensitivity or glycemic control may occur in patients treated with androgens. In diabetic patients, the metabolic effects of androgens may decrease blood glucose and, therefore, may necessitate a decrease in the dose of anti-diabetic medication.

Oral Anticoagulants

  • Changes in anticoagulant activity may be seen with androgens, therefore more frequent monitoring of the international normalized ratio (INR) and prothrombin time are recommended in patients taking warfarin, especially at the initiation and termination of androgen therapy.

Corticosteroids

  • The concurrent use of testosterone with corticosteroids may result in increased fluid retention and requires careful monitoring, particularly in patients with cardiac, renal or hepatic disease.


Drug Abuse and Dependence

Controlled Substance

  • Testosterone (buccal) contains testosterone, a Schedule III controlled substance in the Controlled Substances Act.

Abuse

  • Anabolic steroids, such as testosterone, are abused. Abuse is often associated with adverse physical and psychological effects.

Dependence

  • Although drug dependence is not documented in individuals using therapeutic doses of anabolic steroids for approved indications, dependence is observed in some individuals abusing high doses of anabolic steroids. In general, anabolic steroid dependence is characterized by any three of the following:
  • Taking more drug than intended
  • Continued drug use despite medical and social problems
  • Significant time spent in obtaining adequate amounts of drug
  • Desire for anabolic steroids when supplies of the drugs are interrupted
  • Difficulty in discontinuing use of the drug despite desires and attempts to do so
  • Experience of a withdrawal syndrome upon discontinuation of anabolic steroid use

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA): X

  • Testosterone (buccal) is contraindicated in pregnant women or in women who may become pregnant. Testosterone is teratogenic and may cause fetal harm. Exposure of a fetus to androgens such as testosterone may result in varying degrees of virilization. If a woman becomes pregnant while taking testosterone (buccal), she should be apprised of the potential hazard to the fetus.


Pregnancy Category (AUS): There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Testosterone (buccal) in women who are pregnant.

Labor and Delivery

There is no FDA guidance on use of Testosterone (buccal) during labor and delivery.

Nursing Mothers

  • Although it is not known how much testosterone transfers into human milk, testosterone (buccal) is contraindicated in nursing women because of the potential for virilization in nursing infants. Testosterone and other androgens may adversely affect lactation.

Pediatric Use

  • Safety and effectiveness of testosterone (buccal) in males less than 18 year of age have not been established. Improper use may result in acceleration of bone age and premature closure of the epiphyses.

Geriatic Use

  • Of the total number of subjects in clinical studies of testosterone (buccal), 51 patients (17%) were 65 years of age and older. There is insufficient long-term safety data in geriatric patients to assess the potentially increased risks of cardiovascular disease and prostate cancer.

Gender

There is no FDA guidance on the use of Testosterone (buccal) with respect to specific gender populations.

Race

There is no FDA guidance on the use of Testosterone (buccal) with respect to specific racial populations.

Renal Impairment

  • No studies were conducted in patients with renal impairment.

Hepatic Impairment

  • No studies were conducted in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Testosterone (buccal) in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Testosterone (buccal) in patients who are immunocompromised.

Administration and Monitoring

Administration

  • Buccal

Monitoring

  • Monitor patients with benign prostatic hyperplasia (BPH) for worsening of signs and symptoms of BPH.
  • Monitor prostate specific antigen (PSA), hematocrit, and lipid concentrations periodically.
  • More frequent monitoring of International Normalized Ratio (INR) and prothrombin time is recommended in patients taking warfarin.
  • Monitoring of serum calcium concentrations is recommended in cancer patients.

IV Compatibility

  • There is limited information regarding IV Compatibility.

Overdosage

  • There is one report of acute overdosage with testosterone enanthate injection: testosterone levels of up to 11,400 ng/dL were implicated in a cerebrovascular accident.
  • Oral ingestion of testosterone (buccal) is not expected to result in clinically significant serum testosterone concentrations due to extensive first-pass (hepatic) metabolism.
  • Treatment of overdosage would consist of discontinuation of testosterone (buccal) together with appropriate symptomatic and supportive care.

Pharmacology

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Testosterone (buccal)
Systematic (IUPAC) name
(8R,9S,10R,13S,14S,17S)- 17-hydroxy-10,13-dimethyl- 1,2,6,7,8,9,11,12,14,15,16,17- dodecahydrocyclopenta[a]phenanthren-3-one
Identifiers
CAS number 58-22-0

57-85-2 (propionate ester)
ATC code G03BA03
PubChem 6013
DrugBank DB00624
Chemical data
Formula C19H28O2 
Mol. mass 288.42
SMILES eMolecules & PubChem
Physical data
Melt. point 155 °C (311 °F)
Spec. rot +110.2°
SEC Combust −11080 kJ/mol
Pharmacokinetic data
Bioavailability Low (due to extensive first pass metabolism)
Metabolism Liver, testis and prostate
Half life 2–4 hours
Excretion Urine (90%), feces (6%)
Therapeutic considerations
Licence data

US

Pregnancy cat.

X(US) Contraindicated due to teratogenic effects

Legal status

Schedule IV(CA) Schedule III(US) Prescription only

Routes Intramuscular injection, transdermal (cream, gel, or patch), sub-'Q' pellet

Mechanism of Action

  • Endogenous androgens, including testosterone and dihydrotestosterone (DHT), are responsible for the normal growth and development of the male sex organs and for maintenance of secondary sex characteristics. These effects include the growth and maturation of prostate, seminal vesicles, penis and scrotum; the development of male hair distribution, such as facial, pubic, chest and axillary hair; laryngeal enlargement, vocal chord thickening, alterations in body musculature and fat distribution. Testosterone and DHT are necessary for the normal development of secondary sex characteristics. Male hypogonadism results from insufficient secretion of testosterone and is characterized by low serum testosterone concentrations. Signs/symptoms associated with male hypogonadism include erectile dysfunction and decreased sexual desire, fatigue and loss of energy, mood depression, regression of secondary sexual characteristics and osteoporosis.
  • Male hypogonadism can present as primary hypogonadism caused by defects of the gonads, such as Klinefelter’s Syndrome or Leydig cell aplasia while secondary hypogonadism is the failure of the hypothalamus or pituitary to produce sufficient gonadotropins (FSH, LH).

Structure

  • testosterone (buccal) mucoadhesive is for buccal administration only. It contains testosterone, an androgen.
  • Testosterone (buccal) is designed to adhere to the gum or inner cheek. It provides a controlled and sustained release of testosterone through the buccal mucosa as the buccal system gradually hydrates. Application of testosterone (buccal) twice a day, in the morning and in the evening, provides continuous systemic delivery of testosterone.
  • Testosterone (buccal) is a white to off-white colored, monoconvex, tablet-like, mucoadhesive buccal system. Testosterone (buccal) adheres to the gum tissue above the incisors, with the flat surface facing the cheek mucosa.
  • The active ingredient in testosterone (buccal) is testosterone (SEE FIGURE 1). Each buccal system contains 30 mg of testosterone. Testosterone USP is practically white crystalline powder chemically described as 17-beta hydroxyandrost-4-en-3-one.

Figure 1: Chemical Structure of Testosterone

This image is provided by the National Library of Medicine.
  • Other pharmacologically inactive ingredients in testosterone (buccal) are anhydrous lactose NF, carbomer 934P, hypromellose USP, magnesium stearate NF, lactose monohydrate NF, polycarbophil USP, colloidal silicon dioxide NF, starch NF and talc USP.

Pharmacodynamics

  • No pharmacodynamic studies were conducted using testosterone (buccal).

Pharmacokinetics

Absorption

  • When applied to the buccal mucosa, testosterone (buccal) releases testosterone, allowing for absorption of testosterone through gum and cheek surfaces that are in contact with the buccal system. Since venous drainage from the mouth is to the superior vena cava, trans-buccal delivery of testosterone circumvents first-pass (hepatic) metabolism.
  • Following the initial application of testosterone (buccal), the serum testosterone concentration rises to a maximum within 10-12 hours. The mean maximum (Cmax) and mean average serum total testosterone concentrations for the 12 hour dosing period (Cavg(0-12)) are within the normal physiologic range.
  • Testosterone (buccal) is intended for twice daily dosing. Serum concentrations of testosterone reach steady-state levels after the second dose of twice daily testosterone (buccal) dosing. Following removal of testosterone (buccal), the serum testosterone concentration decreases to a level below the normal range within 2-4 hours.
  • Figure 2. Mean (SD) total testosterone concentration-time curves on Day 7 (after 7 days of testosterone (buccal) treatment, n=29)
This image is provided by the National Library of Medicine.
  • Although no specific food effect study was conducted, Phase 3 study results showed that consumption of food and beverage did not significantly affect the absorption of testosterone from testosterone (buccal).
  • The effects of toothbrushing, mouthwashing, chewing gum and alcoholic beverages on the use and absorption of testosterone (buccal) were not investigated in controlled studies. However, Phase 3 clinical studies permitted patients to do these activities indicating the use of testosterone (buccal) was not significantly affected by these activities.

Distribution

  • Circulating testosterone is chiefly bound in the serum to sex hormone-binding globulin (SHBG) and albumin. Approximately 40% of testosterone in plasma is bound to SHBG, 2% remains unbound (free) and the rest is bound to albumin and other proteins.

Metabolism

  • Testosterone is metabolized to various 17-keto steroids through two different pathways, and the major active metabolites are estradiol and dihydrotestosterone (DHT).
  • Mean DHT concentrations increased in parallel with testosterone concentrations during testosterone (buccal) treatment. After 24 hours of treatment, mean (SD) DHT serum concentrations was approximately 80 (50) ng/dL. The mean steady-state T/DHT ratio during treatment with testosterone (buccal) ranged approximately 9-12.

Excretion

  • There is considerable variation in the half-life of testosterone as reported in the literature, ranging from ten to 100 minutes. About 90% of a dose of testosterone given intramuscularly is excreted in the urine as glucuronic and sulfuric acid conjugates of testosterone and its metabolites; about 6% of a dose is excreted in the feces, mostly in the unconjugated form. Inactivation of testosterone occurs primarily in the liver.

Geriatrics

  • In patients 65 years of age and older, the total testosterone Cavg(0-24) value was higher by 13% compared to patients <65 years of age. In addition, the total T to DHT area-under-the curve ratio was lower in the older population compared to the younger population by 16%. These differences may not be clinically significant.

Nonclinical Toxicology

Carcinogenesis, Mutagenesis, Impairment of Fertility

  • Carcinogenicity
  • Testosterone has been tested by subcutaneous injection and implantation in mice and rats. In mice, the implant induced cervical-uterine tumors, which metastasized in some cases. There is suggestive evidence that injection of testosterone into some strains of female mice increases their susceptibility to hepatoma. Testosterone is also known to increase the number of tumors and decrease the degree of differentiation of chemically induced carcinomas of the liver in rats.
  • Mutagenesis
  • Testosterone was negative in the in vitro Ames and in the in vivo mouse micronucleus assays.
  • Impairment of Fertility
  • The administration of exogenous testosterone has been reported to suppress spermatogenesis in the rat, dog and non human primates, which was reversible on cessation of the treatment.

Clinical Studies

  • testosterone (buccal) was evaluated in a multicenter, open-label Phase 3 trial in 98 hypogonadal men. In this study, 30 mg of testosterone (buccal) was administered buccally twice daily for 12 weeks. The mean age was 53.6 years (range 20 to 75 years). Overall, 69% of patients were Caucasian, 9% were African-American, 15% were Hispanic, 4% were Asian, and 2% were of another ethnic origin. At baseline, 10% of patients reported current use of tobacco and 42% drank alcohol.
  • Of 82 patients who completed the trial and had sufficient data for full analysis, 86.6% had mean serum testosterone concentration (Cavg(0-24)) values within the physiologic range (300-1050 ng/dL).
  • The mean (±SD) time-averaged steady-state daily testosterone concentration (Cavg(0-24)) at Day 84 was 520 (±205) ng/dL compared with a mean of 149 (±99) ng/dL at Baseline. The mean (±SD) maximum testosterone concentration (Cmax) at Day 84 was 970 (±442) ng/dL. At Day 84, the mean percentage of time over the 24-hour sampling period that total testosterone concentrations remained within the normal range of 300-1050 ng/dL was 76%.
  • FIGURE 3 shows the mean total testosterone serum concentration versus time curves on Day 84 (after 12 weeks of testosterone (buccal) treatment).

Figure 3. Mean (SD) total testosterone concentration-time curves on Day 84 (after 12 weeks of Striant treatment, n=82)

This image is provided by the National Library of Medicine.
  • Mean DHT concentrations increased in parallel with testosterone concentrations, with the total testosterone/DHT ratio (9-12) indicating no alteration in metabolism of testosterone to DHT in testosterone deficient men treated with testosterone (buccal).
  • During continuous treatment there was no accumulation of testosterone, and mean total testosterone, free testosterone, and DHT were maintained within their physiologic ranges.

How Supplied

  • Testosterone (buccal) mucoadhesive is supplied in transparent blister packs containing 10 doses. It is white to off-white colored with a flat edge on one side and a convex surface on the other.
  • Testosterone (buccal) is debossed on its flat side, as shown below:
This image is provided by the National Library of Medicine.
  • Each testosterone (buccal) contains 30 mg of testosterone and is supplied as follows:
This image is provided by the National Library of Medicine.

Storage

  • Store at 20-25°C (68-77°F) [see USP Controlled Room Temperature]. Protect from heat and moisture. Damaged blister packages should not be used. Discard used testosterone (buccal) in household trash in a manner that prevents accidental application or ingestion by children or pets.

Images

Drug Images

Package and Label Display Panel

This image is provided by the National Library of Medicine.
This image is provided by the National Library of Medicine.
This image is provided by the National Library of Medicine.

Patient Counseling Information

Men with Known or Suspected Prostate or Breast Cancer

  • Men with known or suspected prostate or breast cancer should not use testosterone (buccal).

Gum-Related Adverse Reactions

  • Gum-related adverse reactions, including severe gum irritation, were reported in clinical trials of Striant. Advise patients to regularly inspect the gum region where they apply Striant and to report any abnormality to their health care professional.

Potential Adverse Reactions with Androgens

  • Patients should be informed that treatment with androgens, such as Striant, may lead to adverse reactions that include:
  • Changes in urinary habits such as increased urination at night, trouble starting their urine stream, passing urine many times during the day, having an urge that they have to go to the bathroom right away, having a urine accident, being unable to pass urine and having a weak urine flow
  • Breathing disturbances, including those associated with sleep, or excessive daytime sleepiness
  • Too frequent or persistent erections of the penis
  • Nausea, vomiting, changes in skin color, or ankle swelling

Patients Should be Advised of these Application Instructions

  • Advise patients to carefully read the patient information accompanying each carton of Striant blister packaged tablets.
  • Morning and evening oral care should be timed to coincide with removal of the residual old system and application of a new buccal system.
  • Before morning and evening oral care, the residual Striant buccal system residual should be removed, then oral care should be performed.
  • Following oral care, a new buccal system should be applied.
  • Upon opening the packet, the rounded side surface of the buccal system should be placed against the gum and held firmly in place with a finger over the lip and against the product for 30 seconds to ensure adhesion.
  • Striant should be placed in a comfortable position just above the incisor tooth (on either side of the mouth). With each application, Striant should be rotated to alternate sides of the mouth.
  • Striant is designed to stay in position until removed. If the buccal system fails to properly adhere to the gum or falls off within the first 8 hours of dosing, replace with a new system and continue for a total of 12 hours for the placement of the first system. If the system falls out of position after 8 hours of dosing, a new buccal system should be applied and it may remain in place for 12 hours then continue with the next regularly scheduled dosing.
  • Patients should take care to avoid dislodging the buccal system. Patients should check to see if Striant is in place following consumption of food or alcoholic/non-alcoholic beverages. Striant should not be chewed or swallowed.

Patient Information

This image is provided by the National Library of Medicine.

Precautions with Alcohol

  • Alcohol-Testosterone (buccal) interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

Look-Alike Drug Names

  • Testoderm - Testoderm TTS[2]
  • Testoderm - Testoderm with Adhesive[2]
  • Testoderm with Adhesive - Testoderm TTS[2]

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.

  1. "STRIANT - testosterone tablet".
  2. 2.0 2.1 2.2 "https://www.ismp.org". External link in |title= (help)

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