A-Z Drug Facts > Testosterone

Testosterone

Pronouncation: (teh-STAHS-tuh-RONE)
Class: Androgen Testosterone

Trade Names:
Androderm
- Transdermal system 5 mg per 24 h, 44 cm ² surface area, 24.3 mg total testosterone
- Transdermal system 2.5 mg per 24 h, 37 cm ² surface area, 12.2 mg total testosterone

Trade Names:
Testopel
- Implant Pellets 75 mg

Testosterone Cypionate

Trade Names:
Depo-Testosterone
- Injection 100 mg/mL
- Injection 200 mg/mL

Testosterone Enanthate

Trade Names:
Delatestryl
- Injection 200 mg/mL

Testosterone Gel

Trade Names:
AndroGel
- Gel 1%

Trade Names:
Testim
- Gel 1%

Testosterone Buccal System

Trade Names:
Striant
- Mucoadhesive 30 mg

Pharmacology

Feedback for Testosterone As a treatment for... Avg User Ratings [?] Hypogonadism -- Male 7.8 6 comments  Rate it! Breast Cancer -- Palliative Be the first to rate it 0 comments   Delayed Puberty -- Male Be the first to rate it 0 comments   Showing 3 of 4 conditions - Show All... Compare with other drugs.

Promotes growth and development of male reproductive organs, maintains secondary sex characteristics, increases protein anabolism and decreases protein catabolism.

Pharmacokinetics

Absorption

Testosterone transdermal T _max is 2 to 4 h. Slowly released following buccal application, reaching the C _max within 10 to 12 h.

Distribution

After transdermal administration, steady-state testosterone levels occur in 3 to 4 wk; 98% is bound to proteins.

Metabolism

Transdermal testosterone is metabolized in the liver.

Elimination

Transdermal testosterone t _½ is 10 to 100 min. Approximately 90% is excreted in urine, and approximately 6% is excreted in feces.

Indications and Usage

Men

Replacement therapy in primary hypogonadism and hypogonadotropic hypogonadism (testosterone enanthate [ Delatestryl ], testosterone pellets [ Testopel ], testosterone gel [ AndroGel , Testim ], testosterone transdermal system [ Androderm ], testosterone buccal system [ Straint ], testosterone cypionate [ Depo-Testosterone ]. Stimulation of puberty (testosterone enanthate [ Delatestryl ], testosterone pellets [ Testopel ]).

Women

Ablation of ovaries in metastatic breast cancer (testosterone enanthate [ Delatestryl ]).

Contraindications

Hypersensitivity to product; serious cardiac, hepatic, or renal disease; men with carcinoma of breast or prostate; women who are or may become pregnant; testosterone gel and buccal system are contraindicated in women.

Dosage and Administration

Androgen Replacement Therapy
Adults

IM 50 to 400 mg every 2 to 4 wk (testosterone enanthate, testosterone cypionate). Subcutaneous 150 to 450 mg every 3 to 6 mo (testosterone pellets). Transdermal 5 mg applied daily ( Androderm ). Topical Start by applying entire packet of testosterone gel 5 g (containing 50 mg testosterone systemically) to clean, dry skin of shoulders and/or upper arms or abdomen. Based on measurements of serum testosterone levels and clinical response 14 days after initiation of therapy, dose may be increased from 5 to 10 g ( Testim ) or from 5 to 7.5 g and from 7.5 to 10 g ( AndroGel ). Buccal 30 mg applied to the gum region twice daily, morning and evening (about 12 h apart). Place in a comfortable position just above 1 of the incisor teeth.

Delayed Puberty
Adolescents

IM 50 to 200 mg every 2 to 4 wk for limited duration (testosterone enanthate). Subcutaneous 150 to 450 mg every 4 to 6 mo (testosterone pellets).

Breast Cancer
Adults

IM 200 to 400 mg every 2 to 4 wk (testosterone enanthate).

General Advice

• Injection
• For deep IM administration into gluteal muscle only. Not for intradermal, subcutaneous, IV, or intra-arterial administration.
• Rotate injection sites.

Storage/Stability

Store AndroGel at controlled room temperature (68° to 77°F). Store Testim at room temperature (59° to 86°F). Store transdermal systems in protective pouch at controlled room temperature (59° to 86°F). Protect systems from excessive heat or pressure, which can cause bursting of the drug reservoir. Store blister packs at controlled room temperature (68° to 77°F). Protect from heat and moisture. Do not remove buccal system from blister pack until ready to apply. Store vials and prefilled syringes at controlled room temperature (68° to 77°F). Store pellets in a cool place.

Drug Interactions

Anticoagulants

May potentiate anticoagulant effects.

Insulin, oral hypoglycemics

May decrease glucose levels and antidiabetic drug requirements.

Propranolol

Coadministration of an injectable testosterone may increase propranolol Cl, resulting in decreased plasma levels.

Laboratory Test Interactions

Clotting factors II, V, VII, X

Testosterone may suppress expression.

Thyroid function tests

Testosterone may cause decreased levels of thyroid hormones.

Adverse Reactions

Cardiovascular

Edema.

Topical

Decreased and increased BP (1%).

CNS

Depression; headache; increased or decreased libido; anxiety; generalized paresthesia.

Topical

Insomnia, mood swings, asthenia, emotional lability, nervousness.

Dermatologic

Acne; hirsutism; male pattern baldness; seborrhea; rash.

Topical

Hot flushes.

Transdermal

Pruritus at application site (37%); burn like blister reaction under system (12%); erythema at application site (7%); vesicles at application site (6%); prostate abnormalities (5%); allergic contact dermatitis (4%); burning and induration at application site (3%).

EENT

Topical

Increased lacrimation, smell disorder (1%).

GI

Transdermal

GI bleeding (2%).

Buccal

Gum or mouth irritation (9%); bitter taste (4%); gum pain and tenderness (3%); gum edema, taste perversion (2%).

Genitourinary

Gynecomastia, penile erections, decreased ejaculatory volume, excessive frequency and duration of penile erections (men); amenorrhea, virilization (deepening of voice and clitoral enlargement), menstrual irregularities, inhibition of gonadotropin secretion (women).

Topical

Breast pain, testis disorder, impaired urination (3%); spontaneous penile erection; taste disorder (1%).

Hematologic

Suppression of clotting factors II, V, VII, and X; polycythemia.

Hepatic

Cholestatic jaundice (elevated LFT results); hepatocellular neoplasm; peliosis hepatitis.

Metabolic

Increased cholesterol; decreased serum glucose.

Topical

Increased hematocrit/hemoglobin (2%).

Miscellaneous

Inflammation and pain at injection or implantation site; fluid and electrolyte retention; hypersensitivity; application site reactions (topical).

Precautions

Pregnancy

Category X .

Lactation

Undetermined. Testosterone gel, cypionate, buccal, and transdermal are not indicated for women.

Children

Use drug with great caution; may effect bone maturation.

Testosterone gel and buccal system

Safety and efficacy not established.

Androderm

Safety and efficacy not established in children younger than 15 yr of age.

Testosterone cypionate

Safety and efficacy not established in children younger than 12 yr of age.

Elderly

Elderly men may be at increased risk of developing prostatic hypertrophy or carcinoma.

Acute intermittent porphyria

Acute intermittent porphyria has been reported. Use drug with caution in patients known to have this condition.

Athletic performance

Abuse of these agents to enhance athletic performance has potential risk of serious adverse reactions.

Breast cancer and immobilized patients

May develop hypercalcemia.

Edema

Use drug with caution in patients with conditions that might be affected by fluid retention (eg, asthma, cardiac or renal function impairment, epilepsy).

Gynecomastia

Frequently occurs and may persist. Use drug with caution in patients with preexisting gynecomastia.

Hepatic effects

Prolonged use of high doses of androgens may result in potentially life-threatening peliosis, cholestatic jaundice, hepatitis, hepatic neoplasms, or hepatocellular carcinoma.

Oligospermia and reduced ejaculatory volume

May occur after prolonged use.

Product interchange

Do not interchange products because of their differences in duration of action.

Serum cholesterol

Levels may increase with androgen use; use drug with caution in patients with history of MI or coronary artery disease.

Sleep apnea

Treatment of hypogonadal men may potentiate sleep apnea, particularly in patients with risk factors (eg, obesity, chronic lung diseases).

Overdosage

Symptoms

Cerebrovascular accident (testosterone enanthate).

Patient Information

• Advise patient to read patient information brochure before using the first time and with each refill.
• Caution patient not to change the dose or stop taking unless advised by health care provider.
• Instruct diabetic patient to monitor blood glucose more frequently when drug is started or dose is changed, and to inform health care provider of significant changes in readings.
• Caution patient that testosterone has not been shown to be safe or effective for enhancing athletic performance and, because of potential for serious health risks, should not be used for this purpose.
• Instruct patient to inform health care provider if any of the following occur: too frequent or persistent erections of the penis; ankle swelling; unexplained nausea and/or vomiting; difficulty urinating; breast enlargement; mood changes; any change in skin color; breathing problems, including any associated with sleep; changes in body hair distribution, increase in acne, or other unusual changes in female partner.

• Gel
• Instruct patient to apply gel once daily at about the same time each day. Advise patient that application every morning is preferred. Advise patient that if bathing or showering in the morning, to apply the gel afterward.
• Caution patient that gel is flammable and not to use near fire or open flame.
• Instruct patient in proper application of gel: open tube ( Testim ) by piercing end of tube using top part of cap or open foil packet ( AndroGel ) by folding top edge at perforation and tearing completely across the packet along the perforation; squeeze entire contents into palm of hand and immediately apply gel to clean, dry skin of the shoulders and/or upper arms ( Testim ), or shoulders and upper arms and/or abdomen ( AndroGel ); use circular motion to rub gel into skin for several seconds until the gel is well rubbed in and the area feels dry; immediately and thoroughly wash hands with soap and water; allow application site to dry for a few minutes before dressing; discard used medication tube or foil packet in household trash in manner that prevents accidental application or ingestion by children or pets.
• Caution patient not to apply Testim or AndroGel to scrotum, penis, abdomen, or skin that is not normal (eg, inflamed or irritated).
• Advise patient to rinse eyes with warm, clean water if gel accidentally gets into the eyes and to notify health care provider if eye irritation develops.
• Advise patient not to swim or bathe within 2 h of applying Testim , or within 5 to 6 h of applying AndroGel , because swimming or bathing too soon after application of gel may reduce effectiveness.
• Instruct patient to wash application site thoroughly with soap and water to remove drug residue before any situation in which direct skin-to-skin contact is anticipated.
• Advise patient that in the event that unwashed or unclothed skin to which the gel has been applied does not come in contact with the skin of another person, especially a pregnant or breast-feeding partner, that the general area of contact on the other person should be washed thoroughly with soap and water as soon as possible.
• Advise patient that if a dose is missed and it is more than 12 h before the next scheduled dose, to apply the dose and resume the regular dose the next day. If it is less than 12 h before the next scheduled dose, advise patient to skip that dose and apply the next dose at the regularly scheduled time. Caution patient not to double the dose to catch up.

• Transdermal System
• Instruct patient to apply patch once daily at about the same time each day. Advise patient that application at night is preferred.
• Instruct patient in proper application of patch: open packet and remove patch immediately prior to application; remove release liner to expose adhesive side of patch; apply to clean, dry skin area of back, abdomen, thigh, or upper arm using firm pressure with fingers or palm, making sure there is good contact with the skin, especially around the edge of the patch.
• Caution patient not to apply patch to scrotum, penis, skin that is not normal (eg, inflamed or irritated), skin over a bony prominence, or skin that could be subject to prolonged pressure during sleep or sitting.
• Instruct patient to discard used patches in household trash in manner that prevents accidental ingestion by children or pets.
• Advise patient that patch does not have to be removed during sexual intercourse, nor while showering, bathing, or swimming.
• Advise patient that mild skin irritation can be relieved by using OTC hydrocortisone. Instruct patient to notify health care provider if irritation persists or worsens.

• Buccal System
• Review application and removal process with patient.
• Instruct patient to apply buccal system twice daily, morning and evening (about 12 h apart).
• Caution patient not to chew or swallow the buccal system.
• Advise patient to avoid dislodging the buccal system and check to see if the system is in place following brushing teeth, use of mouthwash, and eating or drinking.
• Advise patient that if the buccal system fails to properly adhere to the gum or falls off during the 12-dosing interval, the old system should be discarded and a new one applied. If the buccal system falls out of position within 4 h of the next dose, a new system should be applied and may remain in place until the time of the next regularly scheduled dose.
• Advise patient to regularly inspect gum region where buccal system is applied and to report any abnormality (including gum tenderness or irritation) to health care professional.

• Injection and Pellets
• Advise patient that medication will be prepared and administered by a health care provider in a medical setting.
• Advise patient to report pain, tenderness, or signs of inflammation at injection/implantation site to health care provider.

Link to this page

Printable Version

Email Page

Add to my drug list