Metribolone (Metribolone)

02 Details

Metribolone

1100mcg/ml 2 ml 5 vials

 

Metribolone

(Metribolone)

Methyltrienolone; METRIBOLONE; 965-93-5; R1881; Metribolona; 17alpha-Methyltrienolone

C19H24O2

CAS – 965-93-5

 

A synthetic non-aromatizable androgen and anabolic steroid. It binds strongly to the androgen receptor and has therefore also been used as an affinity label for this receptor in the prostate and in prostatic tumors.

 

Metribolone contains: 1100mcg

• 1100 mcg / ml Methyltrienolone

 

 

Pharmacologic Category

Androgen

Dosing: Adult

1100 mcg every 24 hours.

Dosing: Geriatric

Refer to adult dosing

Dosing: Pediatric

Has not been tested in pediatric population.

Dosing: Renal Impairment

No dosage adjustment provided in manufacturer’s labeling; use with caution.

Dosing: Hepatic Impairment

No dosage adjustment provided in manufacturer’s labeling; use with caution.

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

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 generally fall following pregnancy and return to normal once breast-feeding is stopped. The amount of testosterone present in breast milk or the effect to the nursing infant following maternal supplementation is not known. Some products are contraindicated while breast-feeding. Females who are nursing should avoid skin-to-skin contact to areas where testosterone has been applied topically on another person.

Adverse Reactions

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. A modified molecule of trenbolone that is 17-alfa-alkylated to make it orally active.

 

Pharmacodynamics/Kinetics

 

Well absorbed after ingestion with an empty stomach.

Active life: 4-6 hours

Metabolism: Hepatic