Basic information Pharmacology and mechanism of action Indications Side effects Preparations References Safety Related Supplier
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PYRVINIUM PAMOATE

Basic information Pharmacology and mechanism of action Indications Side effects Preparations References Safety Related Supplier
PYRVINIUM PAMOATE Basic information
PYRVINIUM PAMOATE Chemical Properties
  • Melting point:210-215° (softens at 190°)
  • Boiling point:829.27°C (rough estimate)
  • Density 1.0104 (rough estimate)
  • refractive index 1.6400 (estimate)
  • storage temp. 2-8°C
  • solubility DMSO: >10mg/mL
  • form powder
  • color red
  • EPA Substance Registry SystemPyrvinium pamoate (3546-41-6)
Safety Information
PYRVINIUM PAMOATE Usage And Synthesis
  • Pharmacology and mechanism of action Pyrvinium is a quaternary ammonium derivative of a cyanine dye with marked effect against Enterobius vermicularis.
    The mechanism of action is not well known. The drug inhibits oxidative metabolism in the worms and interferes with the absorption of glucose in intestinal helminths. Since most intestinal worms are dependent on anaerobic carbohydrate metabolism, this may be an important action of the drug[1].
     
  • IndicationsInfections caused by Enterobius vermicularis. Pyrvinium is largely replaced today by more effective and safer drugs such as albendazole and mebendazole.
     
  • Side effects Gastrointestinal disturbances such as nausea, vomiting, dyspepsia, indigestion and abdominal pain are frequent. Allergic reactions and photosensitivity have been reported. Pyrvinium stains the stool bright red and may stain clothing if vomiting occurs. Patients should be informed about this.
     
  • PreparationsPyrvinium pamoate (embonate): 450 mg of the pamoate is equivalent to 300 mg of pyrvinium.
    • Povanyl ® (Parke-Davis). Oral solution 10 mg pyrvinium per ml. Tablets 50 mg pyrvinium.
    • Vanquin® (Parke-Davis). Oral solution 10 mg pyrvinium per ml. Tab pyrvinium.
  • References1. Buchanan RA, Barrow WB, Heffelfinger JC, Kinkel AW, Smith TC, Turner JL (1974). Pyrvinium pamoate. Clin Pharmacol Ther, 16, 716–719.
  • Usesanthelmintic
  • UsesPyrvinium Pamoate is a potent noncompetitive inhibitor of the androgen receptor, with the application towards prostate cancer treatment. Antihelmintic.
  • brand namePovan (Parke-Davis).
  • General DescriptionOdorless bright orange or orange-red to brownish red or almost black fluffy powder. Melting point 210-215°C. Insoluble in water. Tasteless.
  • Air & Water ReactionsInsoluble in water.
  • Reactivity ProfilePYRVINIUM PAMOATE is light sensitive. Incompatible with strong oxidizing agents, strong acids and bases .
  • Fire HazardFlash point data for PYRVINIUM PAMOATE are not available; however, PYRVINIUM PAMOATE is probably combustible.
  • Biochem/physiol ActionsPyrvinium pamoate is a potent androgen receptor inhibitor. Androgen receptors (ARs) are nuclear hormone receptors/transcription factors that reside in the cytoplasm and activated by testosterone and dihydrotestosterone. AR inhibitors have potential therapeutic benefit in prostate cancer; competitive inhibitors and chemical castration methods have been discovered, but both therapies have undesirable side effects and/or resistance potential. A screen for non-competitive inhibitors was performed, resulting in the discovery of pyrvinium as an AR inhibitor. In comparison to competitive inhibitors, this compound does not bind to the ligand-binding domain of AR or block DNA occupancy by AR, but it inhibits AR-dependent gene expression via a distinct signaling mechanism. It is more potent than classical competitive AR antagonists and exhibits synergy with other AR inhibitors.
PYRVINIUM PAMOATE(3546-41-6)Related Product Information
PYRVINIUM PAMOATESupplierMore
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