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Metribolone  Steroid use:

Labeled indications

Androgens are primarily indicated in males as replacement therapy when congenital or acquired endogenous androgen absence or deficiency is associated with primary or secondary hypogonadism. Primary hypogonadism includes conditions such as: testicular failure due to cryptorchidism, bilateral torsion, orchitis, or vanishing testis syndrome; orchidectomy, Klinefelter’s syndrome, chemotherapy, or toxic damage from alcohol or heavy metals. Hypogonadotropic hypogonadism (secondary hypogonadism) conditions include idiopathic gonadotropin or LHRH deficiency, or pituitary-hypothalamic injury as a result of tumors, trauma, or radiation and are the most common forms of hypogonadism seen in older adults.

Storage/Stability

Store at room temperature. Protect from light.

Contraindications from Metribolone steroid

Hypersensitivity to Methyltrienolone or any component of the formulation; males with carcinoma of the breast or known or suspected carcinoma of the prostate; women who are breast-feeding, pregnant, or who may become pregnant.

Pregnancy Risk Factor X

Category X: Studies in animals or human beings have demonstrated fetal abnormalities, or there is evidence of fetal risk based on human experience, or both, and the risk of the use of the drug in pregnant women clearly outweighs any possible benefit. The drug is contraindicated in women who are or may become pregnant.

Pregnancy considerations

Methyltrienolone may cause adverse effects, including masculinization of the female fetus, if used during pregnancy. Females who are or may become pregnant should also avoid skin-to-skin contact to areas where testosterone has been applied topically on another person.

Lactation

Contraindicated Breast-Feeding Considerations.

High levels of endogenous maternal testosterone, such as those caused by certain ovarian cysts, suppress milk production. Maternal serum testosterone levels typically decrease after pregnancy and revert to normal upon discontinuing breast-feeding. We do not know the quantity of testosterone in breast milk or its impact on nursing infants after maternal supplementation. Some products should not be used during breast-feeding. Nursing females should refrain from skin-to-skin contact with areas where another person has topically applied testosterone.

Adverse reactions from Metribolone steroid

This compound is highly hepatotoxic.

Cardiovascular

Hypertension (≥3%), increased blood pressure (1%), decreased blood pressure, deep vein thrombosis, edema, vasodilatation.

Central nervous system

Headache (1% to ≥3%), fatigue (2%), irritability (2%), insomnia (≤2%), mood swings (≤2%), aggressive behavior (1%), taste disorder (1%), altered sense of smell (≤1%), abnormal dreams, amnesia, anxiety, chills, depression, dizziness, emotional lability, excitement, hostility, malaise, nervousness, outbursts of anger, paresthesia, seizure, sleep apnea, suicidal ideation

Dermatologic

Acne vulgaris (5%), hyperhidrosis (1%), alopecia, contact dermatitis, diaphoresis, erythema, folliculitis, hair discoloration, pruritus, seborrhea, skin rash, xeroderma.

Endocrine & metabolic

Increased plasma estradiol concentration (3%), weight gain (1%), gynecomastia (≤1%), hot flash (≤1%), change in libido, decreased gonadotropin, fluid retention, hirsutism (increase in pubic hair growth), hypercalcemia, hyperchloremia, hypercholesterolemia, hyperglycemia, hyperkalemia, hyperlipidemia, hypernatremia, hypoglycemia, hypokalemia, inorganic phosphate retention, menstrual disease (including amenorrhea).

Gastrointestinal

Diarrhea (≥3%), gastroesophageal reflux disease, gastrointestinal hemorrhage, gastrointestinal irritation, increased appetite, nausea, vomiting.

Following buccal administration (most common): Dysgeusia, gingival pain, gingival swelling, mouth irritation (including gums), unpleasant taste.

Genitourinary

Prostate specific antigen increase (5% to 11%), prostatitis (≥3%), ejaculatory disorder (1%), prostate induration (1%), spontaneous erections (≤1%), benign prostatic hypertrophy, difficulty in micturition, hematuria, impotence, irritable bladder, mastalgia, oligospermia, priapism, testicular atrophy, urinary tract infection, virilization.

Hepatic

Abnormal hepatic function tests, cholestatic hepatitis, cholestatic jaundice, hepatic insufficiency, hepatic necrosis hepatocellular neoplasms, increased serum bilirubin, peliosis hepatis.

Hematologic & oncologic

Increased hematocrit (1% to 3%), increased hemoglobin (2%), malignant neoplasm of prostate (1%), anemia, clotting factors suppression, hemorrhage, leukopenia, polycythemia, prostate carcinoma.

Hypersensitivity

Anaphylactoid reaction, hypersensitivity reaction (including pulmonary oil microembolism).

Local

Pain at injection site (5%), erythema at injection site (1%), application site reaction (gel, solution), inflammation at injection site.

Transdermal system

Application site pruritus (17% to 37%), application site vesicles (including burn-like blisters under system; 6% to 12%), application site erythema (≤7%), local allergic contact dermatitis (4%), application site burning (3%), application site induration (3%), local skin exfoliation (<3%).

Neuromuscular & skeletal

Arthralgia (≥3%), back pain (≥3%), abnormal bone growth (accelerated), hemarthrosis, hyperkinesia, weakness.

Ophthalmic

Increased lacrimation.

Renal

Increased serum creatinine, polyuria.

Respiratory

Bronchitis (≥3%), nasopharyngitis (≥3%), sinusitis (≥3%), upper respiratory tract infection (≥3%), dyspnea

Drug interactions

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

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

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

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

Dehydroepiandrosterone: May enhance the adverse/toxic effect of Testosterone. Risk X: Avoid combination.

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

Test interactions

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

Monitoring parameters

Liver function tests, cholesterol profile, hemoglobin/hematocrit; INR/PT in patients on anticoagulant therapy.

Children: Radiographs of left wrist and hand every 6 months (to assess bone maturation).

Adult females: Signs of virilization (deepening voice, hirsutism, acne, clitoromegaly); urine and serum calcium in women with breast cancer.

Dosage forms

Oral Tablets, 500mcg.
Injectable, 1100mcg.
Anatomic Therapeutic Chemical (ATC) Classification Not available.

Mechanism of action

Anabolic steroid derived from Trenbolone, sharing some properties. Characterized by its androgenic and anti-glucocorticoid activity. They have modified the molecule of trenbolone to make it orally active by 17-alpha-alkylating it.

Pharmacodynamics/Kinetics from Metribolone steroid

Well absorbed after ingestion with an empty stomach.
Active life: 4-6 hours.
Metabolism: Hepatic.

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