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MethylTESTOSTERone


General


Pronunciation

(meth il tes TOS te rone)


Brand Names: U.S.

  • Android
  • Methitest
  • Testred

Indications


Use: Labeled Indications

Males:

Delayed puberty: To stimulate puberty in carefully selected males with clearly delayed puberty.

Hypogonadotropic hypogonadism (congenital or acquired): Treatment of idiopathic gonadotropin or luteinizing hormone-releasing hormone (LHRH) deficiency, or pituitary hypothalamic injury from tumors, trauma, or radiation.

Primary hypogonadism (congenital or acquired): Treatment of testicular failure caused by cryptorchidism, bilateral torsion, orchitis, vanishing testis syndrome; or orchidectomy.

Females:

Breast cancer, metastatic: Secondarily in women with advancing inoperable metastatic (skeletal) mammary cancer who are 1 to 5 years postmenopausal; has also been used in premenopausal women with breast cancer who have benefited from oophorectomy and are considered to have a hormone-responsive tumor.


Contraindications


Men with breast cancer or with known or suspected prostate cancer; women who are or may become pregnant.

Documentation of allergenic cross-reactivity for androgens is limited. However, because of similarities in chemical structure and/or pharmacologic actions, the possibility of cross-sensitivity cannot be ruled out with certainty.


Dosing and Administration


Dosing: Adult

Breast cancer, metastatic (females): Oral: 50 to 200 mg daily

Delayed puberty (males): Oral: 10 to 50 mg daily; limit treatment duration to 4 to 6 months; use lower range of dosing and individualize dose based on response and tolerability.

Hypogonadotropic hypogonadism (congenital or acquired) and primary hypogonadism (congenital or acquired) (males): Oral: Initial: 10 to 50 mg daily; individualize dose based on response and tolerability.


Dosing: Geriatric

Refer to adult dosing.


Dosing: Pediatric

Delayed puberty: Adolescent males: Oral: Refer to adult dosing.

Hypogonadotropic hypogonadism (congenital or acquired) and primary hypogonadism (congenital or acquired): Adolescent males: Oral: Refer to adult dosing.


Dosing: Renal Impairment

There are no dosage adjustments provided in the manufacturer 's labeling. However, patients with renal disease may be at an increased risk of fluid retention.


Dosing: Hepatic Impairment

There are no dosage adjustments provided in the manufacturer 's labeling. However, patients with hepatic disease may be at an increased risk of fluid retention.


Administration

Administer orally. Hazardous agent; use appropriate precautions for handling and disposal (NIOSH 2014 [group 3]).


Storage

Store at 15 � �C and 30 � �C (59 � �F and 86 � �F). Protect from light, moisture, and heat.


Dosage Forms/Strengths


Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Capsule, Oral:

Android: 10 mg [contains brilliant blue fcf (fd&c blue #1), fd&c red #40]

Testred: 10 mg [contains brilliant blue fcf (fd&c blue #1), fd&c red #40]

Generic: 10 mg

Tablet, Oral:

Methitest: 10 mg [scored]


Drug Interactions

Ajmaline: Androgens may enhance the adverse/toxic effect of Ajmaline. Specifically, the risk for cholestasis may be increased. Monitor therapy

Blood Glucose Lowering Agents: Androgens may enhance the hypoglycemic effect of Blood Glucose Lowering Agents. Monitor therapy

C1 inhibitors: Androgens may enhance the thrombogenic effect of C1 inhibitors. Monitor therapy

Corticosteroids (Systemic): May enhance the fluid-retaining effect of Androgens. Monitor therapy

CycloSPORINE (Systemic): Androgens may enhance the hepatotoxic effect of CycloSPORINE (Systemic). Androgens may increase the serum concentration of CycloSPORINE (Systemic). Consider therapy modification

Vitamin K Antagonists (eg, warfarin): Androgens may enhance the anticoagulant effect of Vitamin K Antagonists. Consider therapy modification


Monitoring Parameters

Liver function tests (periodically); hemoglobin and hematocrit (periodically in patients receiving high doses). In prepubertal children, perform radiographic examination of the hand and wrist every 6 months to determine the rate of bone maturation and to assess the effect of treatment on the epiphyseal centers. In women receiving methyltestosterone for breast cancer, monitor urine and serum calcium concentrations frequently.


Lab Test Interferences


Test Interactions

Testosterone may decrease thyroxine-binding globulin, resulting in decreased total T4; free thyroid hormone levels are not changed.


Adverse Reactions


Frequency not defined.

Male: Gynecomastia, impotence, oligospermia (at high doses), priapism, prostatic carcinoma, prostatic hyperplasia, testicular atrophy, virilism

Female: Atrophy, breast soreness, hirsutism, menstrual problems (amenorrhea), virilism

Cardiovascular: Edema

Central nervous system: Anxiety, depression, headache

Dermatologic: Acne, "male pattern " � baldness

Endocrine & metabolic: Hypercalcemia, hypercholesterolemia, libido (changes in)

Gastrointestinal: Nausea, vomiting

Hematologic: Polycythemia, suppression of clotting factors

Hepatic: Cholestatic hepatitis, hepatic dysfunction, hepatic necrosis, hepatocellular neoplasm (rare), jaundice, liver function tests (abnormal), peliosis hepatitis

Neuromuscular & skeletal: Paresthesia

Miscellaneous: Anaphylactoid reactions (rare)

Postmarketing and/or case reports (Limited to important or life-threatening): Hepatotoxicity (idiosyncratic) (Chalasani, 2014)


Warnings/Precautions


Concerns related to adverse effects:

- Cardiovascular events: Studies have suggested an increased risk of cardiovascular events among groups of men prescribed testosterone therapy (Basaria 2010; Finkle 2014; Vigen 2013). The Endocrine Society suggests it may be prudent to avoid testosterone therapy in men who have experienced a cardiovascular event (eg, MI, stroke, acute coronary syndrome) in the past six months (The Endocrine Society 2014 ). These risks are currently under review by the FDA (Drug Safety Communication 2014).

- Gynecomastia: Gynecomastia may develop and persist in patients being treated for hypogonadism.

- Hepatic effects: Prolonged use and/or high doses may cause peliosis hepatis, hepatic neoplasms including hepatocellular carcinoma, cholestatic hepatitis, and jaundice. Discontinue in case of cholestatic hepatitis with jaundice or abnormal liver function tests.

- Oligospermia: May cause oligospermia and reduced ejaculatory volume after prolonged administration or excessive dosage.

- Priapism: Priapism or excessive sexual stimulation may occur.

- Venous thromboembolism: Venous thromboembolic events, including deep vein thrombosis (DVT) and pulmonary embolism (PE), have been reported with testosterone products. Evaluate patients with symptoms of pain, edema, warmth, and erythema in the lower extremity for DVT and those with acute shortness of breath for PE. Discontinue therapy if a venous thromboembolism is suspected.

Disease-related concerns:

- Breast cancer: May cause hypercalcemia (by stimulating osteolysis) in patients with breast cancer; discontinue if hypercalcemia occurs.

- Edematous conditions: Use with caution in patients with conditions influenced by edema (eg, cardiovascular disease, renal or hepatic impairment); may cause fluid retention.

Concurrent drug therapy issues:

- Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

Special populations:

- Elderly: Elderly patients treated with androgens may be at an increased risk for the development of prostatic hypertrophy and prostatic carcinoma; use is contraindicated in men with prostate cancer. In addition, elderly patients may be at greater risk for fluid retention, transaminase elevations, and excessive sexual stimulation.

- Pediatric: Androgen therapy should be used very cautiously in children and only by specialists who are aware of the adverse effects on bone maturation. May accelerate bone maturation without producing compensatory gain in linear growth in children; in prepubertal children, perform radiographic examination of the hand and wrist every 6 months to determine the rate of bone maturation and to assess the effect of treatment on the epiphyseal centers.

- Women: During treatment for metastatic breast cancer, women should be monitored for signs of virilization; discontinue if mild virilization is present to prevent irreversible symptoms.

Special handling:

- Hazardous agent: Use appropriate precautions for handling and disposal (NIOSH 2014 [group 3]).


Pregnancy Risk Factor

X


Pregnancy Considerations

Use is contraindicated in women who are or may become pregnant. May cause virilization of the external genitalis of the female fetus, including clitoromegaly, abnormal vaginal development, and fusion of genital folds to form a scrotal-like structure. The degree of masculinization is dose related and most likely to occur when androgens are administered in the first trimester. If a patient becomes pregnant while taking androgens, she should be counseled on the potential hazard to the fetus.


Actions


Pharmacology

Stimulates receptors in organs and tissues to promote growth and development of male sex organs and maintains secondary sex characteristics in androgen-deficient males


Metabolism

Hepatic


Excretion

Urine (~90%); feces (~6%)


Half-Life Elimination

Variable: 10 to 100 minutes


Protein Binding

98% bound to sex hormone-binding globulin


Patient and Family Education


Patient Education

- Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

- Patient may experience emotional instability, headache, sexual dysfunction, or enlarged breasts (males). Have patient report immediately to prescriber signs of liver problems (dark urine, feeling tired, lack of appetite, nausea, abdominal pain, light-colored stools, vomiting, or yellow skin or eyes), signs of severe cerebrovascular disease (change in strength on one side is greater than the other, trouble speaking or thinking, change in balance, or change in eyesight), signs of DVT (edema, warmth, numbness, change in color, or pain in the extremities), signs of virilization (in females a deep voice, facial hair, pimples, or period changes, angina, arm pain, shoulder pain, shortness of breath, excessive weight gain, swelling of arms or legs, priapism, nausea, vomiting, severe anxiety, lump in breast, breast pain or soreness, skin discoloration, or coughing up blood (HCAHPS).

- Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.

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