Fluoxymesterone Tablets USP 5mg Taj Pharma
DESCRIPTION
Fluoxymesterone, an androgenic hormone.
Fluoxymesterone is a white or nearly white, odorless, crystalline powder, melting at or about 240° C, with some decomposition. It is practically insoluble in water, sparingly soluble in alcohol, and slightly soluble in chloroform.
The chemical name for fluoxymesterone is androst-4-en-3-one, 9-fluoro-11,17- dihydroxy-17-methyl-, (11β,17β)-. The molecular formula is C20H29FO3 and the molecular weight 336.45.
CLINICAL PHARMACOLOGY
Endogenous androgens are responsible for the normal growth and development of the male sex organs and for maintenance of secondary sex characteristics. These effects include growth and maturation of prostate, seminal vesicles, penis, and scrotum; development of male hair distribution, such as beard, pubic, chest, and axillary hair; laryngeal enlargement; vocal cord thickening; alterations in body musculature; and fat distribution.
Androgens also cause retention of nitrogen, sodium, potassium, and phosphorus, and decreased urinary excretion of calcium. Androgens have been reported to increase protein anabolism and decrease protein catabolism. Nitrogen balance is improved only when there is sufficient intake of calories and protein.
Androgens are responsible for the growth spurt of adolescence and for the eventual termination of linear growth which is brought about by fusion of the epiphyseal growth centers. In children, exogenous androgens accelerate linear growth rates but may cause a disproportionate advancement in bone maturation. Use over long periods may result in fusion of the epiphyseal growth centers and termination of growth process. Androgens have been reported to stimulate the production of red blood cells by enhancing the production of erythropoietic stimulating factor.
During exogenous administration of androgens, endogenous testosterone release is inhibited through feedback inhibition of pituitary luteinizing hormone (LH). At large doses of exogenous androgens, spermatogenesis may also be suppressed through feedback inhibition of pituitary follicle stimulating hormone (FSH).
There is a lack of substantial evidence that androgens are effective in fractures, surgery, convalescence, and functional uterine bleeding.
Pharmacokinetics
Testosterone given orally is metabolized by the gut, and 44 percent is cleared by the liver in the first pass. Oral doses as high as 400 mg per day are needed to achieve clinically effective blood levels for full replacement therapy. The 17-alpha-alkylated derivatives (fluoxymesterone and methyltestosterone) are less extensively metabolized by the liver and have longer half lives. They are more suitable for oral administration than testosterone.
Testosterone in plasma is 98 percent bound to a specific testosterone-estradiol binding globulin, and about two percent is free. Generally, the amount of this sex-hormone binding globulin in the plasma will determine the distribution of testosterone between free and bound forms, and the free testosterone concentration will determine its half-life.
About 90 percent of a dose of testosterone is excreted in the urine as glucuronic and sulfuric acid conjugates of testosterone and its metabolites; about six percent of a dose is excreted in the feces, mostly in the unconjugated form. Inactivation of testosterone occurs primarily in the liver. Testosterone is metabolized to various 17-keto steroids through two different pathways. There are considerable variations of the half-life of testosterone as reported in the literature, ranging from 10 to 100 minutes. The half-life of fluoxymesterone is reported to be 10 hours.
In responsive tissues the activity of testosterone appears to depend on reduction to dihydrotestosterone, which binds to cytosol receptor proteins. The steroid-receptor complex is transported to the nucleus where it initiates transcription events and cellular changes related to androgen action.
INDICATIONS
In the male— fluoxymesterone Tablets are indicated for:
- Replacement therapy in conditions associated with symptoms of deficiency or absence of endogenous testosterone.
- Primary hypogonadism (congenital or acquired)— testicular failure due to cryptorchidism, bilateral torsion, orchitis, vanishing testis syndrome; or orchidectomy.
- Hypogonadotropic hypogonadism (congenital or acquired)—idiopathic gonadotropin or LHRH deficiency, or pituitary-hypothalamic injury from tumors, trauma, or radiation.
- Delayed puberty, provided it has been definitely established as such, and is not just a familial trait.
In the female— fluoxymesterone Tablets are indicated for palliation of androgen-responsive recurrent mammary cancer in women who are more than one year but less than five years postmenopausal, or who have been proven to have a hormone-dependent tumor as shown by previous beneficial response to castration.
DOSAGE AND ADMINISTRATION
The dosage will vary depending upon the individual, the condition being treated, and its severity. The total daily oral dose may be administered singly or in divided (three or four) doses.
Male hypogonadism: For complete replacement in the hypogonadal male, a daily dose of 5 to 20 mg will suffice in the majority of patients. It is usually preferable to begin treatment with full therapeutic doses which are later adjusted to individual requirements. Priapism is indicative of excessive dosage and is indication for temporary withdrawal of the drug.
Delayed puberty: Dosage should be carefully titrated utilizing a low dose, appropriate skeletal monitoring, and by limiting the duration of therapy to four to six months.
Inoperable carcinoma of the breast in the female: The recommended total daily dose for palliative therapy in advanced inoperable carcinoma of the breast is 10 to 40 mg. Because of its short action, fluoxymesterone should be administered to patients in divided, rather than single, daily doses to ensure more stable blood levels. In general, it appears necessary to continue therapy for at least one month for a satisfactory subjective response, and for two to three months for an objective response.
SIDE EFFECTS
Endocrine and urogenital
Female: the most common side effects of androgen therapy are amenorrhea and other menstrual irregularities; inhibition of gonadotropin secretion; and virilization, including deepening of the voice and clitoral enlargement. The latter usually is not reversible after androgens are discontinued. When administered to a pregnant woman, androgens can cause virilization of external genitalia of the female fetus.
Male: Gynecomastia, and excessive frequency and duration of penile erections. Oligospermia may occur at high dosage.
Skin and appendages
Hirsutism, male pattern of baldness, seborrhea, and acne.
Fluid and electrolyte disturbances
Retention of sodium, chloride, water, potassium, calcium, and inorganic phosphates.
Gastrointestinal
Nausea, cholestatic jaundice, alterations in liver function tests, rarely hepatocellular neoplasms and peliosis hepatis (See WARNINGS).
Hematologic
Suppression of clotting factors II, V, VII, and X, bleeding in patients on concomitant anticoagulant therapy, and polycythemia.
Nervous system
Increased or decreased libido, headache, anxiety, depression, and generalized paresthesia.
Allergic
Hypersensitivity, including skin manifestations and anaphylactoid reactions.
Drug Abuse And Dependence
Controlled Substance Class: Fluoxymesterone is a controlled substance under the Anabolic Steroids Control Act, and (fluoxymesterone) Tablets has been assigned to Schedule III.
DRUG INTERACTIONS
Androgens may increase sensitivity to oral anticoagulants. Dosage of the anticoagulant may require reduction in order to maintain satisfactory therapeutic hypoprothrombinemia.
Concurrent administration of oxyphenbutazone and androgens may result in elevated serum levels of oxyphenbutazone.
In diabetic patients, the metabolic effects of androgens may decrease blood glucose and, therefore, insulin requirements.
Drug/Laboratory test interferences
Androgens may decrease levels of thyroxine-binding globulin, resulting in decreased total T4 serum levels and increased resin uptake of T3 and T4. Free thyroid hormone levels remain unchanged, however, and there is no clinical evidence of thyroid dysfunction.
WARNINGS
Hypercalcemia may occur in immobilized patients and in patients with breast cancer. If this occurs, the drug should be discontinued.
Prolonged use of high doses of androgens (principally the 17-α alkyl-androgens) has been associated with development of hepatic adenomas, hepatocellular carcinoma, and peliosis hepatis—all potentially life-threatening complications.
Cholestatic hepatitis and jaundice may occur with 17-α-alkyl-androgens. Should this occur, the drug should be discontinued. This is reversible with discontinuation of the drug.
Geriatric patients treated with androgens may be at an increased risk of developing prostatic hypertrophy and prostatic carcinoma although conclusive evidence to support this concept is lacking.
Edema, with or without congestive heart failure, may be a serious complication in patients with pre-existing cardiac, renal or hepatic disease.
Gynecomastia may develop and occasionally persists in patients being treated for hypogonadism.
Androgen therapy should be used cautiously in males with delayed puberty. Androgens can accelerate bone maturation without producing compensatory gain in linear growth. The effect on bone maturation should be monitored by assessing bone age of the wrist and hand every six months.
This drug has not been shown to be safe and effective for the enhancement of athletic performance. Because of the potential risk of serious adverse health effects, this drug should not be used for such purpose.
PRECAUTIONS
General
Women should be observed for signs of virilization which is usual following androgen use at high doses. Discontinuation of drug therapy at the time of evidence of mild virilism is necessary to prevent irreversible virilization. A decision may be made by the patient and the physician that some virilization will be tolerated during treatment for breast carcinoma.
Patients with benign prostatic hypertrophy may develop acute urethral obstruction. Priapism or excessive sexual stimulation may develop. Oligospermia may occur after prolonged administration or excessive dosage. If any of these effects appear, the androgen should be stopped and if restarted, a lower dosage should be utilized.
Laboratory tests
Women with disseminated breast carcinoma should have frequent determination of urine and serum calcium levels during the course of androgen therapy (See WARNINGS).
Because of the hepatotoxicity associated with the use of 17-alpha-alkylated androgens, liver function tests should be obtained periodically.
Periodic (every six months) X-ray examinations of bone age should be made during treatment of prepubertal males to determine the rate of bone maturation and the effects of androgen therapy on the epiphyseal centers.
Hemoglobin and hematocrit levels (to detect polycythemia) should be checked periodically in patients receiving long-term androgen administration.
Serum cholesterol may increase during androgen therapy.
Carcinogenesis, mutagenesis, impairment of fertility
Animal data: Testosterone has been tested by subcutaneous injection and implantation in mice and rats. The implant induced cervical-uterine tumors in mice, which metastasized in some cases. There is suggestive evidence that injection of testosterone into some strains of female mice increases their susceptibility to hepatoma. Testosterone is also known to increase the number of tumors and decrease the degree of differentiation of chemically-induced carcinomas of the liver in rats.
Human data: There are rare reports of hepatocellular carcinoma in patients receiving long-term therapy with androgens in high doses. Withdrawal of the drugs did not lead to regression of the tumors in all cases. Geriatric patients treated with androgens may be at an increased risk of developing prostatic hypertrophy and prostatic carcinoma although conclusive evidence to support this concept is lacking.
This compound has not been tested for mutagenic potential. However, as noted above, carcinogenic effects have been attributed to treatment with androgenic hormones. The potential carcinogenic effects likely occur through a hormonal mechanism rather than by a direct chemical interaction mechanism.
Impairment of fertility was not tested directly in animal species. However, as noted below under Adverse Reactions, oligospermia in males and amenorrhea in females are potential adverse effects of treatment with fluoxymesterone Tablets. Therefore, impairment of fertility is a possible outcome of treatment with fluoxymesterone.
Pregnancy
Teratogenic effects: Pregnancy Category X. (See CONTRAINDICATIONS.)
Nursing mothers
Fluoxymesterone is not recommended for use in nursing mothers.
Pediatric use
Androgen therapy should be used very cautiously in children and only by specialists aware of the adverse effects on bone maturation. Skeletal maturation must be monitored every six months by an X-ray of the hand and wrist (See WARNINGS).
OVERDOSE
There have been no reports of acute overdosage with the androgens.
CONTRAINDICATIONS
- Known hypersensitivity to the drug
- Males with carcinoma of the breast
- Males with known or suspected carcinoma of the prostate gland
- Women known or suspected to be pregnant
- Patients with serious cardiac, hepatic or renal disease
SHELF-LIFE
3 Years
STORAGE AND HANDLING
Keep this medication in the container it came in, tightly closed, and out of reach of children. Store it at room temperature and away from light, and excess heat and moisture (not in the bathroom).
Unneeded medications should be disposed of in special ways to ensure that pets, children, and other people cannot consume them. However, you should not flush this medication down the toilet. Instead, the best way to dispose of your medication is through a medicine take-back program. Talk to your pharmacist or contact your local garbage/recycling department to learn about take-back programs in your community. See the FDA’s Safe Disposal of Medicines website for more information if you do not have access to a take-back program.
It is important to keep all medication out of sight and reach of children as many containers (such as weekly pill minders and those for eye drops, creams, patches, and inhalers) are not child-resistant and young children can open them easily. To protect young children from poisoning, always lock safety caps and immediately place the medication in a safe location – one that is up and away and out of their sight and reach.
PATIENT INFORMATION
Patients should be instructed to report any of the following: nausea, vomiting, changes in skin color, and ankle swelling. Males should be instructed to report too frequent or persistent erections of the penis and females any hoarseness, acne, changes in menstrual periods or increase in facial hair.
Manufactured in India by:
TAJ PHARMACEUTICALS LTD.
Mumbai, India
Unit No. 214.Old Bake House,
Maharashtra chambers of Commerce Lane,
Fort, Mumbai – 400001
at:Gujarat, INDIA.
Customer Service and Product Inquiries:
1-800-TRY-FIRST (1-800-222-434 & 1-800-222-825)
Monday through Saturday 9:00 a.m. to 7:00 p.m. EST
E-mail: tajgroup@tajpharma.com
Fluoxymesterone Tablets USP 5mg Taj Pharma
Patient Information Leaflet
1.What is fluoxymesterone?
Fluoxymesterone is a man-made form of testosterone, a naturally occurring sex hormone that is produced in a man’s testicles. Small amounts of testosterone are also produced in a woman’s ovaries and adrenal system.
Fluoxymesterone is used in men and boys to treat conditions caused by a lack of this hormone, such as delayed puberty or other hormonal imbalances.
Fluoxymesterone is also used in women to treat breast cancer that has spread to other parts of the body. Fluoxymesterone treats only the symptoms of metastatic breast cancer but does not treat the cancer itself.
Fluoxymesterone may also be used for purposes not listed in this medication guide.
2.What is the most important information I should know about fluoxymesterone?
This medicine can cause birth defects.
Do not use fluoxymesterone if you are pregnant.
You should not use fluoxymesterone if you have prostate cancer or male breast cancer.
Fluoxymesterone will not enhance athletic performance and should not be used for that purpose or shared with another person.
What should I discuss with my healthcare provider before taking fluoxymesterone?
You should not use fluoxymesterone if you are allergic to it, or if you have:
prostate cancer;
male breast cancer; or if you are pregnant.
Fluoxymesterone will not enhance athletic performance and should not be used for that purpose or shared with another person.
To make sure fluoxymesterone is safe for you, tell your doctor if you have:
- benign prostatic hypertrophy (BPH);
- breast cancer;
- delayed puberty (unless you are taking fluoxymesterone to treat it);
- liver or kidney disease;
- diabetes;
- any debilitating condition; or
- heart disease, coronary artery disease (hardened arteries), congestive heart failure, or a history of heart attack.
This medication can harm an unborn baby or cause birth defects. Do not use fluoxymesterone if you are pregnant. Use effective birth control to avoid pregnancy during your treatment with fluoxymesterone. Follow your doctor’s instructions about how long to prevent pregnancy after your treatment ends.
It is not known whether fluoxymesterone passes into breast milk or if it could harm a nursing baby. You should not breast-feed while you are taking fluoxymesterone.
Fluoxymesterone can affect bone growth in boys who are treated for delayed puberty. Bone development may need to be checked with X-rays every 6 months during treatment.
3.How should I take fluoxymesterone?
Follow all directions on your prescription label. Your doctor may occasionally change your dose to make sure you get the best results. Do not take this medicine in larger or smaller amounts or for longer than recommended.
While using fluoxymesterone, you may need frequent blood tests.
Store at room temperature away from moisture, heat, and light.
Read all patient information, medication guides, and instruction sheets provided to you. Ask your doctor or pharmacist if you have any questions.
4.What happens if I miss a dose?
Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.
What happens if I overdose?
Seek emergency medical attention.
What should I avoid while taking fluoxymesterone?
This medicine can pass into body fluids (urine, feces, vomit). Caregivers should wear rubber gloves while cleaning up a patient’s body fluids, handling contaminated trash or laundry or changing diapers. Wash hands before and after removing gloves.
Wash soiled clothing and linens separately from other laundry.
Fluoxymesterone will not enhance athletic performance and should not be used for that purpose or shared with another person.
5.Fluoxymesterone side effects
Get emergency medical help if you have signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.
Stop using fluoxymesterone and call your doctor at once if you have:
shortness of breath (even with mild exertion), swelling, rapid weight gain;
increased or ongoing erection of the penis;
nausea, vomiting, loss of appetite, increased thirst, muscle weakness, confusion, and feeling tired or restless; or
upper stomach pain, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes).
Women receiving fluoxymesterone may develop male characteristics, which could be irreversible if testosterone treatment is continued. Stop taking this medication and call your doctor at once if you notice any of these signs of excess testosterone:
changes in menstrual periods;
male-pattern hair growth (such as on the chin or chest);
hoarse voice; or
enlarged clitoris.
Common side effects (in men or women) may include:
acne, changes in skin color;
increased hair growth;
male pattern baldness;
increased or decreased interest in sex;
breast swelling;
headache, anxiety, depression; or
numbness, burning, pain, or tingly feeling.
This is not a complete list of side effects and others may occur.
Fluoxymesterone dosing information
Usual Adult Dose for Hypogonadism — Male:
-5 to 20 mg orally per day
-Usually preferable to start therapy at a higher level within the range (e.g., 10 mg) with subsequent adjustment as required.
Comments:
-This drug may be given as a single dose or in divided doses.
-Dosage and duration of therapy will depend on age, sex, diagnosis, patient response to treatment, and appearance of adverse effects.
Uses: This drug is indicated for replacement therapy in conditions associated with a deficiency or absence of endogenous testosterone.
Males:
-Primary hypogonadism (congenital or acquired)
-Hypogonadotropic hypogonadism (congenital or acquired)
-Testicular failure due to cryptorchidism, bilateral torsion, orchitis, vanishing testis syndrome, or orchidectomy
-Idiopathic gonadotropin or luteinizing hormone-releasing hormone (LHRH) deficiency, or pituitary-hypothalamic injury from tumors, trauma, or radiation
Usual Adult Dose for Breast Cancer–Palliative:
Palliation of Inoperable Mammary Cancer:
-10 to 40 mg orally per day in divided doses for 3 months or more
Palliation of Advanced Mammary Carcinoma:
-Hormone therapy is adjunctive to and not a replacement for conventional therapy; therapy duration will depend on the response of the condition and the appearance of adverse reactions.
Comments:
-Androgen therapy appears to occasionally accelerate the disease; patients should be followed closely.
-This treatment has been used in premenopausal women with breast cancer who have benefited from oophorectomy and are considered to have a hormone-responsive tumor.
Use: Secondary treatment in women with advancing inoperable metastatic (skeletal) mammary cancer who are 1 to 5 years postmenopausal.
Usual Pediatric Dose for Delayed Puberty — Male:
2.5 to 20 mg orally per day; generally in the lower range of 2.5 to 10 mg orally per day, taken in one single dose or in divided doses for a limited duration (e.g., 4 to 6 months).
Comments:
-Various dosage regimens have been used: some call for lower dosages initially with gradual increases as puberty progresses, with or without a decrease to maintenance level; other regimens call for higher dosage to induce pubertal changes and lower dosage for maintenance after puberty.
-The chronological and skeletal ages should be taken into consideration in determining the initial dose and when adjusting the dose.
-Brief treatment with conservative doses may occasionally be justified in these male patients if they do not respond to psychological support.
-Patients and parents should be advised of the potential adverse effect on bone maturation prior to treatment.
-Hand and wrist x-rays to determine bone age should be obtained every 6 months to assess the effect of treatment on the epiphyseal centers.
Use: Stimulate puberty in adolescent males with clearly delayed puberty
6.What other drugs will affect fluoxymesterone?
Other drugs may interact with fluoxymesterone, including prescription and over-the-counter medicines, vitamins, and herbal products. Tell each of your health care providers about all medicines you use now and any medicine you start or stop using.
See also:
Fluoxymesterone drug interactions (in more detail)
Further information
Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.
Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.
- Manufactured in India by:
TAJ PHARMACEUTICALS LTD.
Mumbai, India
Unit No. 214.Old Bake House,
Maharashtra chambers of Commerce Lane,
Fort, Mumbai – 400001
at:Gujarat, INDIA.
Customer Service and Product Inquiries:
1-800-TRY-FIRST (1-800-222-434 & 1-800-222-825)
Monday through Saturday 9:00 a.m. to 7:00 p.m. EST
E-mail: tajgroup@tajpharma.com
