Nandrolone Decanoate – Detailed Information

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General Information

Nandrolone decanoate, also known as 19-nortestosterone, is an injectable medication that belongs to the group of drugs called class II anabolic androgenic steroids (AAS). The drugs that fall under class II AAS are all known as 19-nortestosterone derivatives; they are all synthetic derivatives of the endogenous male hormone testosterone. The primary role of testosterone in the human male is to aid the development of secondary sexual characteristics (androgenic effects) during puberty and the development as well as maintenance of muscle mass (anabolic effects).

 Drugs, such as Nandrolone decanoate, that fall under the AAS category were synthesized to have more anabolic and less androgenic properties.

Originally synthesized and described by Birch in 1950, nandrolone is similar in chemical composition and structure to testosterone.

The only difference in chemical composition between testosterone and nandrolone is that nandrolone lacks a methyl group at carbon C-19. 

Due to its demethylation at C-19, nandrolone decanoate has very strong anabolic effects but weak androgenic effects; its anabolic effects are much stronger than testosterone.

One of the main indications for the clinical use of injectable nandrolone decanoate is in the management of refractory anemia that is not responsive to other treatment modalities.

Nandrolone triggers the production of erythropoietin by the kidneys, which results in an increased red blood cell mass and volume. 

Additionally, in patients suffering from chronic wasting diseases such as cancer, nandrolone may promote tissue development with the subsequent building of muscle mass. 

Nandrolone may also be used in the medical management of postmenopausal women who have osteoporosis.

anabolics

Mechanism of Action

Nandrolone is an androgen receptor agonist, and its actions are mediated through the same receptors that regulate the action and activity of endogenous testosterone

It exerts its effects at the genetic level by altering the transcriptional activities of specific genes that control the expression of the relevant proteins. 

After parenteral administration, nandrolone binds to androgen receptors and forms receptor complexes.

These receptor complexes can then enter the cell nucleus and bind to the relevant nucleotide sequence of the chromosomal DNA. 

Once bound to chromosomal DNA, nandrolone is then able to promote the expression of the needed proteins through the modification of nuclear transcription in the cells.

Nandrolone decanoate shares the actions of endogenous androgens such as testosterone. Exogenous androgens such as nandrolone decanoate promote protein anabolism and stimulate appetite which results in a reversal of catabolic processes and negative nitrogen balance. 

Increases in lean body mass in patients with cachexia (e.g. malnourished dialysis patients) and decreased bone resorption and increased bone density in patients with osteoporosis are often noted. 

Blood glucose, erythrocyte production, and the balance of calcium are also affected by androgens. 

Increased erythrocyte production is apparently due to enhanced production of erythropoietic stimulating factors. 

Patients with anemia associated with the renal disease will have increases in red blood cell volume and hemoglobin after receiving nandrolone decanoate.

Since nandrolone decanoate has actions similar to endogenous androgens, administration of nandrolone decanoate has the possibility of causing serious disturbances of growth and sexual development if given to young children and causing unwanted adverse effects in women. 

Exogenous androgens suppress gonadotropin-releasing hormone, thereby reducing the gonadotropic function of the pituitary through a negative feedback mechanism. 

This results in a reduction of endogenous testosterone, luteinizing hormone, and follicle-stimulating hormone. Exogenous androgens may also have a direct effect on the testes. 

Reversible increases in low-density lipoproteins (LDL) and decreases in high-density lipoproteins (HDL) also occur.

Pharmacokinetics

Nandrolone decanoate is typically administered parenterally as an intramuscular injection. It undergoes an extensive hepatic first-pass metabolism in the liver and therefore has very low bioavailability when administered orally. 

In contrast, nandrolone administered parenterally as an intramuscular injection has a very high bioavailability.

Whether through oral or parenteral administration, nandrolone binds to androgen receptors within the body after its absorption. The androgen receptors, which are ligand-dependent nuclear transcription factors and located on the X chromosome, are expressed in a wide variety of tissues within the human body, such as bone, muscle, prostate, and adipose tissue, among others. Parenterally administered nandrolone has a half-life of about 6 – 12 days. This half-life maybe even longer under some circumstances, such as liver or renal disease.

In the systemic circulation, nandrolone decanoate is rapidly hydrolyzed to free nandrolone by plasma esterases. 

Nandrolone has high lipid solubility and can rapidly diffuse into cells. Nandrolone is subsequently metabolized in the liver via reduction and oxidation which is similar to the metabolism of testosterone. 

Data on the excretion of the parent compound and metabolites are lacking. The plasma clearance of nandrolone is approximately 1.6 L/hour/kg and the elimination half-life of the parent compound is 6 to 8 days.

Metabolism of nandrolone decanoate occurs primarily in the liver and happens in two phases: phase I and phase II. 

In phase I, the enzymatic reactions involve the actions of the enzymes 5-alpha and 5-beta reductases, 3-alpha and 3-beta hydroxysteroid dehydrogenases, and 17-beta hydroxysteroids dehydrogenases. 

Phase II of nandrolone decanoate metabolism occurs after the conclusion of phase I and involves the conjugation of the phase I metabolites with glucuronic acid or sulfate. 

The primary breakdown product that arises from the metabolism of nandrolone is 19-norandrosterone. 

Other breakdown compounds that may also be produced due to the metabolism of nandrolone decanoate include 5-alpha-dihydro nandrolone, 19-norandrosterone, and 19-norethiocholanolone.

Following its metabolism in the liver, nandrolone decanoate is excreted from the body in the urine through the kidneys. 

The metabolites of nandrolone can be detected for a long time following the administration of parenteral nandrolone injection to the individual. 

The approximate length of time that nandrolone metabolites can be detected in urine is 33 days.

However, some studies have shown that these metabolites may persist in the urine for up to 60 days after receiving an intramuscular injection of nandrolone.

Route-Specific Pharmacokinetics

Intramuscular Route: Following intramuscular injection, nandrolone decanoate is slowly released from the intramuscular depot at a relatively constant rate over approximately 4 days. A 100-mg dose produces peak serum concentrations in 3—6 days.

Indications of Use

Nandrolone Decanoate is used in the treatment of anemia resultant of renal insufficiency, as well as off-label for cachexia, osteoporosis, and wasting syndrome.

Nandrolone decanoate is a medication that is available only by prescription due to its high likelihood of being abused, as well as the severe side effects that may arise if it is improperly administered. 

Some indications for receiving intramuscular nandrolone decanoate injections include the following:

Aplastic anemia: 

Studies have shown that nandrolone decanoate injections may be of benefit in the management of patients with aplastic anemia, a condition that arises from the damage to the bone marrow cells within the body. 

The research done revealed a positive correlation between the long-term administration of the nandrolone decanoate injection and improvement in symptoms of aplastic anemia, in some subjects, the red blood cell levels returned to normal.

Hemodialysis: 

Patients on chronic hemodialysis as a result of end-stage renal disease are predisposed to developing anemia due to reduced production of erythropoietin; exogenous erythropoietin may be administered to these individuals to boost their production of red blood cells. 

Several studies have indicated that nandrolone decanoate injections enhance the sensitivity of erythroid precursor cells to erythropoietin, patients on hemodialysis who received a combination of exogenous erythropoietin and nandrolone injections as part of their treatment regimen showed a significant improvement in their hematocrit and hemoglobin values. 

Additionally, nandrolone injections increased the nutritional status and the lean body mass of patients on hemodialysis as they experienced marked improvements in serum albumin levels as well as other markers of nutritional status. 

Osteoporosis: 

Nandrolone decanoate injections have been shown to help minimize and even reverse the loss of bone density that is associated with osteoporosis. 

It acts by inhibiting bone resorption resulting in a corresponding increase in bone formation. In addition, it causes an increase in the content of bone minerals at the proximal and distal radius, as well as at the lumbar spine. 

All these effects significantly reduce the incidence of fractures that are typically associated with osteoporosis. 

Precautions and contraindications 

Your health care provider needs to know if you have any of these conditions: breast cancer; diabetes; heart disease; kidney disease; liver disease; prostate trouble; an unusual or allergic reaction to nandrolone, other medicines, foods, dyes, or preservatives; pregnant or trying to get pregnant; breast-feeding. 

You will need to have blood work done while you are taking this medicine. This drug may affect blood sugar in patients with diabetes.

Nandrolone decanoate injections are administered intramuscularly only. Do not inject via intravenous administration. Nandrolone decanoate contains benzyl alcohol. 

Do not use this formulation in patients with benzyl alcohol hypersensitivity.

Androgen therapy (such as nandrolone) can result in loss of diabetic control and should be used with caution in patients with diabetes mellitus. Close monitoring of blood glucose is recommended.

The use of androgens (such as nandrolone) in children should be undertaken only with extreme caution. Androgens may accelerate bone maturation without stimulating compensatory linear growth, sometimes resulting in compromised adult stature. Radiographic examinations of the hand and wrist should be performed every 6 months to assess the rate of bone maturation and the effect of the drug on epiphyseal centers. 

Once the epiphyses have closed, growth is terminated. Even after discontinuation of treatment, epiphyseal closure can be enhanced for several months.

Nandrolone decanoate can stimulate the growth of cancerous tissue and should not be used in male patients with prostate cancer or breast cancer. 

Patients with prostatic hypertrophy should be treated with caution because of the possible development of malignancy.

Androgens (such as nandrolone) can induce osteolysis and should be used with caution in patients with hypercalcemia. 

Androgen-induced hypercalcemia occurs especially in immobile patients and those with metastatic breast cancer.

Alterations in the serum lipid profile consisting of decreased HDL and increased LDL occur with anabolic steroids including nandrolone.

The drug should be used cautiously in patients with hypercholesterolemia and in those with cardiac disease especially in those with arteriosclerosis, coronary artery disease, and myocardial infarction. 

Monitoring of lipoprotein concentrations is recommended. During treatment with androgens, edema can occur because of sodium retention. 

Thus, this is another reason to use nandrolone cautiously in patients with heart failure, peripheral edema, or severe cardiac disease.

During treatment with androgens, edema occurs because of fluid retention in association with sodium retention. Nandrolone decanoate is, therefore, contraindicated in patients with severe hepatic disease and should be avoided in patients with severe renal disease because of possible exacerbation of these conditions. 

In addition, patients with nephrosis or the nephrotic phase of nephritis should be treated with caution. Because androgenic anabolic steroids have been associated with the development of peliosis hepatis and benign and malignant liver tumors (e.g., hepatocellular cancer), further cautions are warranted for patients with hepatic disease. 

Patients with hepatic disease or hepatic dysfunction also can be at risk of drug accumulation because of reduced clearance.

There are certain conditions under which nandrolone decanoate should not be administered or administered with extreme caution. 

Some of these circumstances include the following:

  • Pregnancy: Pregnancy is an absolute contraindication for nandrolone decanoate administration. This drug can cause masculinization of the fetus and should not be administered to pregnant women.
  • Cancer: Men with cancer of the breast or prostate or women who have breast cancer with associated hypercalcemia should not receive nandrolone decanoate injection. In women, this may cause the resorption of bones, making them more prone to fractures.
  • Children: Nandrolone injections may speed up bone maturation in children without a corresponding increase in their vertical growth. These kids may suffer from a compromised physical stature such that they do not achieve their full growth potential.
  • Women: Extreme care should be exercised if administering nandrolone decanoate injections to women. These women should be monitored closely for signs of virilization such as acne, clitoromegaly, hirsutism, and deepening of the voice. If any of these features are detected, the nandrolone injections should be discontinued immediately.
  • Individuals with hepatic, renal, or cardiac diseases should be monitored very closely while receiving nandrolone decanoate injections.

This list may not include all possible contraindications.

Pregnancy

Nandrolone decanoate belongs to the Food and Drug Administration (FDA) category X. This means that studies done in humans or animals have demonstrated a positive risk of fetal abnormalities if this drug is administered to pregnant women and that the risks outweigh any benefits that may be gained through the administration of this drug. 

As such, nandrolone is absolutely contraindicated in pregnancy; women on this medication should stop receiving it as soon as possible if they become pregnant. 

Administration of nandrolone injections to pregnant women may lead to virilization of the fetus; this risk is especially high during the first trimester of pregnancy.

Nandrolone decanoate is absolutely contraindicated during pregnancy because of probable adverse effects on the fetus.

Androgenic anabolic steroids are known to cause embryotoxicity, fetotoxicity, and masculinization of female animal offspring. Nandrolone decanoate is contraindicated in females who are or may become pregnant. 

If nandrolone decanoate is used during pregnancy, or if the patient becomes pregnant while taking this drug, she should be apprised of the potential hazard to the fetus.

Breast – Feeding

It is not known if anabolic steroids are excreted in human milk. Nandrolone is not indicated in females of childbearing potential; use during breastfeeding should be avoided because of the potential for serious adverse reactions in nursing infants. 

Alternative methods to breastfeeding are recommended.

Interactions

Possible interactions include: goserelin; leuprolide; medicines for diabetes; medicines for the prostate like dutasteride, finasteride, saw palmetto; warfarin. 

This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. 

Some items may interact with your medicine.

Androgens can enhance the effects of anticoagulants.

The dosage of the anticoagulant may have to be decreased in order to maintain the prothrombin time at the desired therapeutic level. 

When anabolic steroid or androgen therapy is started or stopped in patients on anticoagulant therapy, close monitoring is required. 

Additionally, nandrolone decanoate may generate a pharmacodynamic interaction with warfarin by independently affecting the activity of circulating coagulation proteins. 

Androgens reduce the amount or activity of circulating coagulant proteins thereby enhancing the anticoagulant effect of warfarin.

The actions of androgens could be antagonized by 5-alpha reductase inhibitors.

Avoid concurrent use of androgens with 5-alpha-reductase inhibitors.

Exogenously administered androgens (testosterone derivatives or anabolic steroids) have variable effects on blood glucose control in patients with diabetes mellitus. In general, low testosterone concentrations are associated with insulin resistance. 

Further, when hypogonadal men (with or without diabetes) are administered exogenous androgens, glycemic control typically improves as indicated by significant reductions in fasting plasma glucose concentrations and HbA1c.

Increased fluid retention may occur with concomitant nandrolone decanoate and corticosteroid use. Corticosteroids with greater mineralocorticoid activity such as fludrocortisone are more likely to cause edema.

Androgens may be necessary to assist in the growth response to human growth hormone, but excessive doses of androgens in prepubescent males can accelerate epiphyseal maturation.

Goserelin and leuprolide inhibit steroidogenesis. Concomitant use of nandrolone decanoate with goserelin or leuprolide is relatively contraindicated and would defeat the purpose of goserelin or leuprolide therapy.

Androgens are known to stimulate erythropoiesis.

Despite the fact that endogenous generation of erythropoietin is depressed in patients with chronic renal failure, other tissues besides the kidney can synthesize erythropoietin, albeit in small amounts.

Concurrent administration of androgens can increase the patient’s response to epoetin alfa, reducing the amount required to treat anemia. Because adverse reactions to epoetin alfa have been associated with an abrupt increase in blood viscosity, this drug combination should be avoided, if possible.

In vitro, both genistein and daidzein inhibit 5 alpha-reductase isoenzyme II, resulting in decreased conversion of testosterone to the potent androgen 5-alpha-dihydrotestosterone (DHT) and a subsequent reduction in testosterone-dependent tissue proliferation.

The action is similar to that of finasteride but is thought to be less potent. 

Theoretically, because the soy isoflavones appear to inhibit type II 5-alpha-reductase, the soy isoflavones may counteract the activity of the androgens.

This list may not include all possible drug interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.

Side Effects

There are a variety of side effects that could occur in individuals who receive nandrolone decanoate injections. Some of these reactions include, but are not limited to, the following:

  • Enlargement of the prostate in elderly men.
  • Reduced sperm count and volume in men.
  • Hepatitis and hepatocellular carcinoma may occur at high doses. A rare but life-threatening liver disease known as peliosis hepatis may also occur.
  • Females may experience the signs of virilization previously mentioned as well as menstrual abnormalities. These effects are reversible if the medication is discontinued promptly.
  • In prepubertal children, nandrolone may cause premature closing of the growth plates, which may result in stunted growth.
  • There may be alterations in blood clotting factors in individuals receiving nandrolone decanoate injections, which may impair clotting times. Patients on anticoagulants should be closely monitored for bleeding abnormalities while receiving nandrolone decanoate injections.
  • Patients may exhibit psychiatric effects such as depression, insomnia, and mania while on nandrolone injections.
  • In the renal system, there may be increased retention of water, potassium, nitrogen, chloride, and calcium. The retention of these electrolytes may result in edema.
  • Some patients may experience gastrointestinal disturbances, such as nausea, vomiting, and diarrhea.
  • Significant increases in low-density lipoproteins (LDL) with a corresponding decrease in high-density lipoproteins may occur in individuals receiving nandrolone injections.
  • Change in sex drive or performance; diarrhea; hair loss; headache; trouble sleeping.

This list may not describe all possible side effects. Call your health care provider immediately if you are experiencing any signs of an allergic reaction: allergic reactions like

  • Skin rash.
  • Itching or hives.
  • Swelling of the face.
  • Lips or tongue. 
  • Breast lump.
  • Breathing problems. 
  • Changes in mood especially anger-depression or rage. 
  • Change in voice.
  • Dark urine. 
  • Increase in facial hair. 
  • Irregular menstrual periods.
  • Acne.
  • Nausea, vomiting.
  • Stomach pain.
  • Swelling in ankles or legs.
  • Trouble passing urine or change in the amount of urine. 
  • Yellowing of the eyes or skin.

Menstrual irregularity can occur with nandrolone decanoate therapy in females. Disruption of the regular menstrual cycle secondary to nandrolone decanoate-induced suppression of gonadotropin secretion can lead to amenorrhea or oligomenorrhea.

When androgens (such as nandrolone) are given to women, virilization, manifested by acne, hirsutism, clitoromegaly, male pattern baldness, reduced breast size, and deepening of the voice or hoarseness, can occur. 

If treatment is discontinued when these symptoms first appear, they usually subside. Prolonged treatment can lead to irreversible masculinity, so the benefit of treatment should be measured against the risk.

In males:

Male patients can experience feminization during prolonged therapy with nandrolone decanoate, which is believed to result from inhibition of gonadotropin secretion and conversion of androgens to estrogens.

These effects are more pronounced in patients with concurrent hepatic disease and include mastalgia and gynecomastia. 

Feminizing effects are generally reversible. Inhibition of testicular function, testicular atrophy, impotence (erectile dysfunction), epididymitis, and bladder irritation can also occur.

Priapism and excessive sexual stimulation, more common in geriatric males, are generally the effect of excessive nandrolone decanoate dosage. Oligospermia and decreased ejaculate volume may occur in patients receiving long-term therapy or excessive doses. 

Alopecia resembling male pattern baldness has also occurred.

Prostate cancer as a secondary malignancy or prostatic hypertrophy can develop during prolonged therapy with nandrolone decanoate and are more likely to occur in elderly males. 

Signs of acute epididymitis (e.g., fever, chills, pain in the inguinal region) and/or urinary urgency should prompt withdrawal of the drug and reevaluation of dosage.

In prepubescent males

When androgens (such as nandrolone) are used in the treatment of immature males, early virilism can be a disadvantage because it is accompanied by premature epiphyseal closure. 

Monitoring of skeletal maturation should be undertaken at about 6-month intervals. Once the epiphyses have closed, growth is terminated. 

Even after discontinuation of treatment, epiphyseal closure can be enhanced for several months. Penile enlargement and an increased frequency of erections can also occur.

Storage

Store this medication at 68°F to 77°F (20°C to 25°C) and away from heat, moisture and light. 

Keep all medicine out of the reach of children. Throw away any unused medicine after the beyond-use date. Do not flush unused medications or pour down a sink or drain.


Surajit jana

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