Nandrolone Phenpropionate
Indications: Carcinoma, breast
DESCRIPTION:
Nandrolone Phenopropionate injection is a sterile solution of nandrolone phenpropionate, a short acting anabolic agent in sesame oil for intramuscular injection. Each ml contains: 25 mg or 50 mg nandrolone phenpropionate in sterile sesame oil. Preservative: 5% benzyl alcohol (25 mg); or 10% (50 mg). Chemically it is Estr-4-en-3-one, 17-(1-oxo-3-phenylpropoxy)-, (17 beta)-
CLINICAL PHARMACOLOGY:
Anabolic steroids are synthetic derivatives of testosterone. Androgens have been reported to increase protein anabolism and decrease protein catabolism. Nitrogen balance is improved with anabolic agents but only when there is sufficient intake of calories and protein. Whether this positive nitrogen balance is of primary benefit in the utilization of protein building dietary substances has not been established.
Certain clinical effects and adverse reactions demonstrate the androgenic properties of this class of drugs. The deletion of the CH3 group from the C-19-position has resulted in reduction of its androgenic properties and retention and enhancement of its anabolic properties.
Thus it is possible to employ doses that provide significant anabolic effects without undesired androgenic effects. Complete dissociation of anabolic and androgenic effects has not been achieved. The actions of anabolic steroids are therefore similar to those of male sex hormones with the possibility of causing serious disturbances of growth and sexual development if given to young children. Anabolic steroids suppress the gonadotropic functions of the pituitary and may exert a direct effect upon the testis.
INDICATIONS AND USAGE:
Effective: For the control of metastatic breast cancer.
CONTRAINDICATIONS:
1. Male patients with carcinoma of the breast or with known or suspected carcinoma of the prostate.
2. Carcinoma of the breast in some females.
3. Pregnancy because of masculinization of the fetus.
4. Nephrosis or the nephrotic phase of nephritis.
WARNINGS:
1. Anabolic steroids do not enhance athletic ability.
2. Hypercalcemia may develop both spontaneously and as a result of hormonal therapy in women with disseminated breast carcinoma. If it develops while on this agent, the drug should be discontinued.
3. Caution is required in administering these agents to patients with cardiac, renal or hepatic disease. Edema may occur occasionally with or without congestive heart failure. Concomitant administration with adrenal steroids or ACTH may add to the edema.
4. There have been rare reports of hepatocellular neoplasms and peliosis hepatitis in association with long-term androgenic-anabolic steroid therapy. (See PRECAUTIONS, Carcinogenesis, Mutagenesis, and Impairment of Fertility.)
5. Anabolic steroids should be used with caution in patients with benign prostatic hypertrophy.
6. In children, anabolic treatment may accelerate bone maturation without producing compensatory gain in linear growth. This adverse effect may result in compromised adult stature. The younger the child the greater the risk of compromising final mature height. The effect on maturation should be monitored by assessing bone age of the wrist and hand every six months.
PRECAUTIONS:
General
Women should be observed for signs of virilization (deepening of the voice, hirsutism, acne, clitoromegaly and menstrual irregularities.) Discontinuation of drug therapy at the time of evidence of mild virilism is necessary to prevent irreversible virilization. Such virilization is usual following anabolic use in high doses.
Information for the Patient
The physician should instruct patients to report any of the following side effects of androgenic anabolic steroids:
Women: Hoarseness, acne, changes in menstrual periods, more hair on the face, nausea, vomiting, changes in the skin color or ankle swelling.
Laboratory Tests
1. Women with disseminated breast carcinoma should have frequent determination of urine and serum calcium levels during the course of anabolic therapy.
2. Periodic (every 6 months) x-ray examinations of bone age should be made during treatment of children to determine the rate of bone maturation and the effects of anabolic therapy on the epiphyseal centers.
3. Hemoglobin and hematocrit should be checked periodically for polycythemia in patients who are receiving high doses of anabolics.
4. Because of the hepatotoxicity associated with the use of 17-alpha-alkylated anabolic steroids, liver function tests should be obtained periodically.
Drug/Laboratory Test Interactions
1. Anabolics may decrease levels of the PBI in thyroxine binding capacity and radioactive iodine uptake.
2. Anabolics may cause alterations in the glucose tolerance test and metyrapone test.
Carcinogenesis, Mutagenesis, and Impairment of Fertility
Human Data. Long term studies in animals have not been performed to evaluate carcinogenic potential of nandrolone phenpropionate. There are rare reports of hepatocellular carcinoma in patients receiving long-term therapy with anabolics in high doses. Withdrawal of the drugs did not lead to repression of the tumors in all cases. Geriatric patients treated with anabolics may be at an increased risk for the development of prostatic hypertrophy and prostatic carcinoma.
Pregnancy, Teratogenic Effects, Pregnancy Category X
(See CONTRAINDICATIONS.)
Nursing Mothers
It is not known whether anabolics are excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants from anabolics, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
Pediatric Use
Safety and effectiveness of nandrolone phenopropionate in children have not been established.
DRUG INTERACTIONS:
1. Anticoagulants: Anabolic steroids may increase sensitivity to oral anticoagulants. Dosage of the anticoagulant may have to be decreased in order to maintain the prothrombin time at the desired therapeutic level. Patients receiving oral anticoagulant therapy require close monitoring, especially when anabolics are started or stopped.
2. Oxyphenbutazone: Concurrent administration of oxyphenbutazone and androgens may result in elevated serum levels of oxyphenbutazone.
3. Insulin: In diabetic patients the metabolic effects of anabolics may decrease blood glucose and insulin requirements.
ADVERSE REACTIONS:
The following adverse reactions are listed in order of decreasing severity:
1. In Males
a) Prepubertal
1. Phallic enlargement.
2. Increased frequency of erections.
b) Post-pubertal
1. Inhibition of testicular function and oligospermia.
2. Gynecomastia.
2. In Females
a) Hirsutism, male pattern baldness, deepening of the voice and clitoral enlargement. These changes are usually irreversible even after prompt discontinuance of therapy and are not prevented by concomitant usage of estrogens.
b) Menstrual irregularities.
3. In Both Sexes
a) Bleeding of patients on concomitant anticoagulant therapy.
b) Premature closure of epiphyses in children.
c) Inhibition of gonadotropin secretion.
d) Increased or decreased libido.
e) Acne (especially in females and prepubertal males).
f) Nausea.
g) The electrolytes: retention of sodium, chlorides, water, potassium phosphates and calcium.
h) Increased serum cholesterol.
i) Suppression of clotting factors II, V, VII, X.
4. There have been rare reports of hepatocellular neoplasm and peliosi hepatitis in association with long-term androgenic-anabolic steroid therapy. (See WARNINGS.)
OVERDOSAGE:
There have been no reports of acute overdosage with the anabolics.
DOSAGE AND ADMINISTRATION:
The recommended dosage of nandrolone phenpropionate injection in metastatic breast cancer is 50-100 mg/weekly based on therapeutic response, and consideration of the benefit to risk ratio. Duration of therapy will depend on the response of the condition and appearance of adverse reactions. If possible, therapy should be intermittent. Nandrolone is intended only for deep intramuscular injection, into the gluteal muscle preferably.
Store at 15-30Β°C (59-86Β°F). Protect from bright light.