Stanozolol Cream

Overview of Stanozolol Cream

Dosage Strength of Stanozolol Cream

2% 30 mL Pump

General Information

Stanozolol is an oral anabolic steroid used to treat hereditary angioedema. Stanozolol prophylactically decreases the frequency and severity of attacks. Anabolic steroids promote body tissue-building processes and reverse catabolic or tissue-depleting processes. When using this product, it is important to provide adequate calorie and protein intake to maintain a positive nitrogen balance. This drug was approved by the FDA in 1962. In July 2003, Ovation acquired the US marketing and distribution rights for several products from Sanofi-Synthelabo, Inc, including Winstrol; however, the product had already been in short supply due to manufacturing issues at the time of the acquisition.

Mechanism of Action

Stanozolol binds to androgen receptors, such as membrane bound receptor proteins LAGS and stanozolol-binding protein (STBP).

The anabolic steroid, stanozolol, is used therapeutically to treat a number of pathological conditions and its clinical effects suggest that it can modulate connective tissue breakdown. The ability of this compound to stimulate prostaglandin E2 (PGE2), collagenase, gelatinase and stromelysin production by human synovial and skin fibroblasts in vitro was examined. The results showed that stanozolol significantly stimulated, in a dose dependent manner, PGE2, collagenase and stromelysin production by skin fibroblasts. However, no stimulation was seen in the synovial cell lines. In contrast, no effect on gelatinase production was seen in either cell type, following exposure to stanozolol. The synovial and skin lines both exhibited a significant stimulation of PGE2 and all three metalloproteinases in response to interleukin-1 beta (IL-1 beta).

Steroid-binding proteins unrelated to the classical nuclear receptors have been proposed to play a role in non-genomic actions of the 17alpha-alkylated testosterone derivative (17alpha-AA) stanozolol (ST). We have previously reported that male rat liver endoplasmic reticulum contains two steroid-binding sites associated with high molecular mass oligomeric proteins: (1) the ST-binding protein (STBP); and (2) the low-affinity glucocorticoid-binding protein (LAGS). To further explore the role of LAGS on the mechanism of action of ST, we have now studied: (1) the interaction of ST and its hydroxylated metabolites with solubilized LAGS and the cytosolic glucocorticoid receptor (GR); and (2) the effects of hormones on the capability of STBP to bind ST. We found that, unlike 17alpha-methyltestosterone, neither ST nor its hydroxylated metabolites bind to GR. However, the 16beta-hydroxylation of ST significantly increases the capability of LAGS to bind ST. Interestingly, 3'-hydroxylation of ST abrogates the capability of LAGS to bind ST. ST (k(i)=30 nM) and 16beta-hydroxystanozolol (k(i)=13 nM) bind with high affinity to LAGS, and are capable of accelerating the rate of dissociation of previously bound dexamethasone from the LAGS. STBP and LAGS are strongly induced by ethinylestradiol. However, unlike STBP, LAGS is regulated by thyroid hormones and growth hormone, which proves that these steroid-binding activities are associated with different binding sites. These findings seem to suggest a novel mechanism for ST whereby membrane-associated glucocorticoid-binding activity is targeted by the 16beta-hydroxylated metabolite of ST. ST and its 16beta-hydroxylated metabolite modulate glucocorticoid activity in the liver through negative allosteric modulation of LAGS, with the result of this interaction an effective increase in classical GR-signaling by increasing glucocorticoid availability to the cytosolic GR.

Pharmacokinetics

Stanozolol has high oral bioavailability, due to the presence of its C17α alkyl group and the resistance to gastrointestinal and liver metabolism that it results in. The medication has very low affinity for human serum sex hormone-binding globulin (SHBG), about 5% of that of testosterone and 1% of that of DHT. Stanozolol is metabolized in the liver, ultimately becoming glucuronide and sulfate conjugates. Its biological half-life is reported to be 9 hours when taken by mouth and 24 hours when given by intramuscular injection in the form of an aqueous suspension. It is said to have a duration of action of one week or more via intramuscular injection.

Contraindications/Precautions

The use of Stanozolol is contraindicated in the following:

  • Male patients with carcinoma of the breast, or with known or suspected carcinoma of the prostate
  • Carcinoma of the breast in females with hypercalcemia; androgenic anabolic steroids may stimulate osteolytic resorption of bone
  • Nephrosis or the nephrotic phase of nephritis

Stanozolol can cause fetal harm when administered to a pregnant woman. Stanozolol is contraindicated in women who are or may become pregnant. If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be apprised of the potential hazard to the fetus.

Pregnancy

Stanozolol has been assigned to pregnancy category X. The use of stanozolol is considered contraindicated during pregnancy. Anabolic steroid use, particularly during the first trimester of pregnancy, may cause virilization of the external genitalia of the female fetus.

Reversible oligospermia may occur after prolonged administration or excessive dosage. If this effect occurs, the anabolic steroid can be discontinued and if restarted, a lower dosage should be utilized.1

Breast-feeding

There are no data on the excretion of anabolic steroids into human milk. Because many drugs are excreted into human milk and because of the potential for adverse effects on the nursing infant, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the woman. 1

Adverse Reactions/Side Effects

In rare cases, serious and even fatal cases of liver problems have developed during treatment with stanozolol. Contact your doctor immediately if you experience abdominal pain, light colored stools, dark colored urine, unusual fatigue, nausea or vomiting, or yellowing of the skin or eyes. These may be early signs of liver problems.

If you experience any of the following serious side effects, contact your doctor immediately or seek emergency medical attention:

  • an allergic reaction (difficulty breathing; closing of the throat; swelling of the lips, tongue, or face; or hives);
  • swelling of the arms or legs (especially ankles);
  • frequent or persistent erections, or breast tenderness or enlargement (male patients); or
  • voice changes (hoarseness, deepening), hair loss, facial hair growth, clitoral enlargement, or menstrual irregularities (female patients).

Other less serious side effects may also occur. Talk to your doctor if you experience:

  • new or worsening acne;
  • difficulty sleeping;
  • headache; or
  • changes in sexual desire.

Side effects other than those listed here may also occur. Talk to your doctor about any side effect that seems unusual or that is especially bothersome.

Cardiovascular effects may be precipitated in patients adversely affected by fluid retention. Edema, with and without congestive heart failure, has occurred during anabolic steroid therapy.

Genitourinary effect following chronic administration and/or large dosages of anabolic steroids can result in oligospermia and decreased ejaculatory volume. Elderly male patients may experience prostatic enlargement resulting in urinary obstruction. Priapism and excessive stimulation may develop.

In female patients the use of anabolic steroids may result in virilization including deepening voice, hirsutism, acne, clitomegaly (not reversible), and menstrual abnormalities. Discontinuation of medication at signs of mild virilization may prevent irreversible virilization.
Alterations in libido may occur (increased/decreased).

Life-threatening peliosis hepatis and hepatic abnormalities including hepatic neoplasms and hepatocellular carcinomas have occurred following prolonged therapy with high doses of anabolic steroids. Tumor regression did not occur in all cases following medication withdrawal.

Cholestatic hepatitis, jaundice, and abnormal liver function tests occur at relatively low doses.

In female patients the use of anabolic steroids has resulted in virilization including deepening voice, hirsutism, acne, clitomegaly (not reversible), and menstrual abnormalities. Discontinuation of stanozolol at signs of mild virilization may prevent irreversible virilization.

Androgenic activity associated with anabolic steroids is involved in termination of linear bone growth by closure of the epiphyseal growth centers. Appropriate monitoring of bone age is recommended during stanozolol use in prepubertal patients.

Oncologic effects following prolonged therapy with large doses of anabolic steroids have included hepatic neoplasms and hepatocellular carcinomas.

Hematologic effects occurring during anabolic steroid therapy include alteration in clotting factors II, V, VII and X , prolonged prothrombin time (PT), and increased red cell production.

During exogenous administration of anabolic steroids, endogenous testosterone release is inhibited through feedback inhibition of pituitary luteinizing hormone (LH). Large doses of exogenous anabolic steroids may suppress spermatogenesis through inhibition of pituitary follicle stimulating hormone (FSH).

Decreased glucose tolerance requiring adjustments in hyperglycemic control has occurred in diabetic patients during anabolic steroid therapy.

Metabolic effects occurring during anabolic steroid therapy in immobilized patients or those with metastatic breast disease include osteolytic-induced hypercalcemia.

Anabolic steroids effect electrolyte balance, nitrogen retention, and urinary calcium excretion. Edema, with and without congestive heart failure, has occurred during anabolic steroid therapy.
The androgenic activity of anabolic steroids may decrease levels of thyroxin-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.

Significant increases in low density lipoproteins (LDL) and decreases in high density lipoproteins (HDL) have occurred.

Anabolic steroids cause retention of nitrogen, sodium, potassium, chloride, water and phosphorus, and decrease urinary excretion of calcium. Patients should be instructed to report edema.

Gastrointestinal effects occurring during stanozolol therapy include nausea and vomiting.

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.

  • 1. a. b. Product Information. Stanozolol (stanozolol)." Sanofi Winthrop Pharmaceuticals, New York, NY.

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