Primobolan Depot (Methenolone Enanthate)

02 Details

Primobolan Depot

 (Methenolone Enanthate)

 

Metenolone Enantate; Enantato de metenolona; Enantato de metilandrostenolona;

Méténolone, Enantate de; Metenoloni Enantas; Methenolone; Enanthate (USAN); Methenolone Oenanthate; NSC-64967; SH-601; SQ-16374. 17β-Hydroxy-1-methyl-5α-androst-1-en-3-one-heptanoate. Метенолона Энантат

 

C27H42O3 = 414.6.

CAS — 303-42-4.

ATC — A14AA04.

ATC Vet — QA14AA04.

Pharmacopoeias. In Jpn.

 

Primobolan Depot : 100mg

• 100 mg / ml Metenolone Enantate

 

Pharmacologic Category

Androgen

Dosing: Adult

 

Intramuscular depot injections of metenolone enantate have been given for osteoporosis in doses of 100 mg every 2 weeks, reducing to once every 3 to 4 weeks after an initial response.

Intramuscular injections of 100 mg of the enantate every 1 to 2 weeks, or 200 mg every 2 to 3 weeks, have been used in progressive breast cancer.

Dosing: Geriatric

 

Refer to adult dosing.

 

Dosing: Pediatric

No information available in pediatric population

Dosing: Renal Impairment

No dosage adjustment provided in manufacturer’s labeling; use with caution due to propensity to cause edema.

Dosing: Hepatic Impairment

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

Use: Labeled Indications

 

Has been used in treating aplastic anemia, breast cancer, and postmenopausal osteoporosis

 

Storage/Stability

 

Store in a dry cool place. Protect from light and moisture.

 

Contraindications

Hypersensitivity to metenolone or any component of the formulation.

Men with carcinomas of the breast or with known or suspected carcinomas of the prostate; 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.

Warnings/Precautions

• Hepatic effects: Prolonged use and/or high doses may cause peliosis hepatis or liver cell tumors, which may not be apparent until liver failure or intra-abdominal hemorrhage develops. Discontinue in case of cholestatic hepatitis with jaundice or abnormal liver function tests.
• 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: Use with caution in patients with breast cancer; may cause hypercalcemia by stimulating osteolysis.
• Edematous conditions: Use with caution in patients with conditions influenced by edema (eg, cardiovascular disease, migraine, seizure disorder, renal impairment); may cause fluid retention.
• Hepatic impairment: Use with caution in patients with hepatic impairment.

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

Use is contraindicated in women who are or may become pregnant; masculinization of the fetus has been reported.

Lactation

Excretion in breast milk unknown/not recommended

Breast-Feeding Considerations

It is not known if metenolone is excreted in breast milk. Due to the potential for serious adverse reactions in the nursing infant, breast-feeding is not recommended.

Adverse Reactions

Frequency unknown.

Cardiovascular: Edema

Central nervous system: Depression, excitation, insomnia

Dermatologic: Acne (females and prepubertal males)

Also reported in females: Hirsutism, male-pattern baldness

Endocrine & metabolic: Electrolyte imbalances, glucose intolerance, gonadotropin secretion inhibited, gynecomastia, HDL decreased, LDL increased, libido changes

Also reported in females: Clitoral enlargement, menstrual irregularities

Genitourinary:

Prepubertal males: Increased or persistent erections, penile enlargement

Postpubertal males: Bladder irritation, epididymitis, impotence, oligospermia, priapism (chronic), testicular atrophy, testicular function inhibited

Hematologic: Prothrombin time increased, suppression of clotting factors

Hepatic: Alkaline phosphatase increased, ALT increased, AST increased, bilirubin increased, cholestatic jaundice, hepatic necrosis (rare), hepatocellular neoplasms, peliosis hepatis (with long-term therapy)

Neuromuscular & skeletal: CPK increased, premature closure of epiphyses (in children)

Renal: Creatinine excretion increased

Metabolism/Transport Effects

 

None known.

 

Drug Interactions

Corticosteroids, Warfarin and Antidiabetic agents.

Test Interactions

 

May suppress factors II, V, VII, and X; may increase PT; may decrease thyroxine-binding globulin and radioactive iodine uptake

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

 

1mL ampule with 100mg of methenolone enanthate.

Multi dosing vial: 100mg/1 ml

Anatomic Therapeutic Chemical (ATC) Classification

• A14AA04

Mechanism of Action

Synthetic testosterone derivative with similar androgenic and anabolic actions

Pharmacodynamics/Kinetics

 

Metabolism: Hepatic

Elimination: Urine and Feces

Half-life: 1-2 weeks.

 

Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions

Effects on Dental Treatment

No significant effects or complications reported

Effects on Bleeding

No information available to require special precautions