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Pronunciation |
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(tes
TOS ter
one) |
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U.S. Brand
Names |
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Androderm® Transdermal System;
AndroGel®; Andro-L.A.® Injection; Andropository®
Injection; Delatest® Injection; Delatestryl® Injection;
depAndro® Injection; Depotest® Injection;
Depo®-Testosterone Injection; Duratest® Injection;
Durathate® Injection; Everone® Injection; Histerone®
Injection; Testex®; Testoderm® Transdermal System;
Testopel®
Pellet |
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Generic
Available |
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Yes |
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Synonyms |
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Aqueous Testosterone; Testosterone Cypionate; Testosterone Enanthate;
Testosterone Propionate |
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Pharmacological Index |
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Androgen |
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Use |
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Androgen replacement therapy in the treatment of delayed male puberty;
postpartum breast pain and engorgement; inoperable breast cancer; male
hypogonadism |
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Restrictions |
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C-III |
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Pregnancy Risk
Factor |
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X |
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Contraindications |
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Severe renal or cardiac disease, benign prostatic hypertrophy with
obstruction, undiagnosed genital bleeding, males with carcinoma of the breast or
prostate; hypersensitivity to testosterone or any component;
pregnancy |
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Warnings/Precautions |
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Perform radiographic examination of the hand and wrist every 6 months to
determine the rate of bone maturation. May accelerate bone maturation without
producing compensating gain in linear growth. Has both androgenic and anabolic
activity, the anabolic action may enhance hypoglycemia. Prolonged use has been
associated with serious hepatic effects (hepatitis, hepatic neoplasms,
cholestatic hepatitis, jaundice). May potentiate sleep apnea in some male
patients (obesity or chronic lung disease) or exacerbate heart failure due to
fluid retention. |
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Adverse
Reactions |
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>10%:
Dermatologic: Acne
Endocrine & metabolic: Menstrual problems (amenorrhea), virilism, breast
soreness
Genitourinary: Epididymitis, priapism, bladder irritability
1% to 10%:
Cardiovascular: Flushing, edema
Central nervous system: Excitation, aggressive behavior, sleeplessness,
anxiety, mental depression, headache
Dermatologic: Hirsutism (increase in pubic hair growth)
Gastrointestinal: Nausea, vomiting, GI irritation
Genitourinary: Prostatic hypertrophy, prostatic carcinoma, impotence,
testicular atrophy
Hepatic: Hepatic dysfunction
<1%: Cholestatic hepatitis, gynecomastia, hepatic necrosis, hypercalcemia,
hypersensitivity reactions, hypoglycemia, leukopenia, polycythemia, suppression
of clotting factors |
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Drug
Interactions |
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CYP3A3/4 and 3A5-7 enzyme substrate |
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Mechanism of
Action |
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Principal endogenous androgen responsible for promoting the growth and
development of the male sex organs and maintaining secondary sex characteristics
in androgen-deficient males |
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Pharmacodynamics/Kinetics |
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Duration of effect: Based upon the route of administration and which
testosterone ester is used; the cypionate and enanthate esters have the longest
duration, up to 2-4 weeks after I.M. administration
Distribution: Crosses the placenta; appears in breast milk
Protein binding: 98% (to transcortin and albumin)
Metabolism: In the liver
Half-life: 10-100 minutes
Elimination: In urine (90%) and feces via bile (6%) |
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Usual Dosage |
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Children: I.M.:
Male hypogonadism:
Initiation of pubertal growth: 40-50 mg/m2/dose (cypionate or
enanthate ester) monthly until the growth rate falls to prepubertal levels
Terminal growth phase: 100 mg/m2/dose (cypionate or enanthate
ester) monthly until growth ceases
Maintenance virilizing dose: 100 mg/m2/dose (cypionate or
enanthate ester) twice monthly
Delayed puberty: 40-50 mg/m2/dose monthly (cypionate or enanthate
ester) for 6 months
Adults: Inoperable breast cancer: I.M.: 200-400 mg every 2-4 weeks
Male: Short-acting formulations: Testosterone Aqueous/Testosterone Propionate
(in oil): I.M.:
Androgen replacement therapy: 10-50 mg 2-3 times/week
Male hypogonadism: 40-50 mg/m2/dose monthly until the growth rate
falls to prepubertal levels (~5 cm/year); during terminal growth phase: 100
mg/m2/dose monthly until growth ceases; maintenance virilizing dose:
100 mg/m2/dose twice monthly or 50-400 mg/dose every 2-4 weeks
Male: Long-acting formulations: Testosterone enanthate (in oil)/testosterone
cypionate (in oil): I.M.:
Male hypogonadism: 50-400 mg every 2-4 weeks
Male with delayed puberty: 50-200 mg every 2-4 weeks for a limited duration
Male greater than or equal to 18 years: Transdermal: Primary hypogonadism
or hypogonadotropic hypogonadism:
Testoderm®: Apply 6 mg patch daily to scrotum (if
scrotum is inadequate, use a 4 mg daily system)
Testoderm-TSS®: Apply 5 mg patch daily to clean, dry
area of skin on the arm, back or upper buttocks. Do not apply
Testoderm-TSS® to the scrotum
Androderm®: Apply 2 systems nightly to clean, dry area
on the back, abdomen, upper arms or thighs for 24 hours for a total of 5 mg/day
AndroGel®: Males >18 years of age: 5 g (to deliver
50 mg of testosterone) applied once daily (preferably in the morning) to clean,
dry, intact skin of the shoulder and upper arms and/or abdomen. Upon opening the
packet(s), the entire contents should be squeezed into the palm of the hand and
immediately applied to the application site(s). Application sites should be
allowed to dry for a few minutes prior to dressing. Hands should be washed with
soap and water after application. Do not apply
AndroGel® to the genitals
Dosing adjustment/comments in hepatic disease: Reduce dose
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Monitoring
Parameters |
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Periodic liver function tests, radiologic examination of wrist and hand every
6 months (when using in prepubertal children) |
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Reference Range |
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Testosterone, urine: Male: 100-1500 ng/24 hours; Female: 100-500 ng/24
hours |
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Test
Interactions |
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May cause a decrease in creatinine and creatine excretion and an increase in
the excretion of 17-ketosteroids, thyroid function tests |
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Mental Health: Effects
on Mental Status |
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May cause anxiety, insomnia, aggressive behavior, or
depression |
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Mental Health:
Effects on Psychiatric
Treatment |
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May rarely cause neutropenia; use caution with clozapine and
carbamazepine |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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No information available to require special precautions |
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Dental Health:
Effects on Dental Treatment |
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No effects or complications reported |
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Patient
Information |
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Diabetics should monitor serum glucose closely and notify prescriber of
changes; this medication may alter hypoglycemic requirements. You may experience
acne, growth of body hair, loss of libido, impotence, or menstrual irregularity
(usually reversible); nausea or vomiting (small frequent meals, frequent mouth
care, sucking lozenges, or chewing gum may help). Report changes in menstrual
pattern; enlarged or painful breasts; deepening of voice or unusual growth of
body hair; persistent penile erection; fluid retention (swelling of ankles,
feet, or hands, difficulty breathing or sudden weight gain); unresolved changes
in CNS (nervousness, chills, insomnia, depression, aggressiveness); altered
urinary patterns; change in color of urine or stool; yellowing of eyes or skin;
unusual bruising or bleeding; or other persistent adverse reactions.
Pregnancy/breast-feeding precautions: Inform prescriber if you are
pregnant. Do not get pregnant during or for 1 month following therapy. Male: Do
not cause a female to become pregnant. Male/female: Consult prescriber for
instruction on appropriate barrier contraceptive measures. This drug may cause
severe fetal defects. Do not breast-feed. |
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Nursing
Implications |
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Warm injection to room temperature and shaking vial will help redissolve
crystals that have formed after storage; administer by deep I.M. injection into
the upper outer quadrant of the gluteus maximus. Transdermal system should be
applied on clean, dry, scrotal skin. Dry-shave scrotal hair for optimal skin
contact. Do not use chemical depilatories. |
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Dosage Forms |
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Injection:
Aqueous suspension: 25 mg/mL (10 mL, 30 mL); 50 mg/mL (10 mL, 30 mL); 100
mg/mL (10 mL, 30 mL)
In oil, as cypionate: 100 mg/mL (1 mL, 10 mL); 200 mg/mL (1 mL, 10 mL)
In oil, as enanthate: 100 mg/mL (1 mL, 5 mL, 10 mL); 200 mg/mL (1 mL, 5 mL,
10 mL)
In oil, as propionate: 100 mg/mL (10 mL, 30 mL)
Pellet: 75 mg (1 pellet per vial)
Transdermal system:
Androderm®: 2.5 mg/day; 5 mg/day
Testoderm®: 4 mg/day; 6 mg/day
Testoderm-TTS®: 5 mg/day
Transdermal gel: AndroGel®: 1%: 50 mg (5 g gel); 75 mg
(7.5 g gel) |
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References |
|
Borhan-Manesh F and Farnum JB,
"Methyltestosterone-Induced Cholestasis. The Importance of Disproportionately Low Serum Alkaline Phosphatase Level,"
Arch Intern Med, 1989, 149(9):2127-9.
Cunningham GR, Cordero E, and Thornby JI,
"Testosterone Replacement With Transdermal Therapeutic Systems. Physiological Serum Testosterone and Elevated Dihydrotestosterone Levels,"
JAMA, 1989, 261(17):2525-30.
Daigle RD, "Anabolic Steroids," J Psychoactive Drugs, 1990,
22(1):77-80.
Moller BB and Ekelund B,
"Toxicity of Cyclosporine During Treatment With Androgens," N Engl J Med,
1985, 313(22):1416.
Ruch W and Jenny P,
"Priapism Following Testosterone Administration for Delayed Male Puberty," Am
J Med, 1989, 86(2):256. |
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