Peringatan Keamanan

Stomatitis, gastric disturbance, vertigo, febrile reactions, skin eruptions, and irritation may occur with overdose. Thrombocytopenia, neutropenia, and agranulocytosis. Intravenous administration may cause severe hypotension and cardiac arrhythmias, which has been followed by sudden death L1579.

Mercury mainly affects the nervous system. Exposure to high levels of metallic, inorganic, or organic mercury can permanently damage the brain, kidneys, and developing fetus. Effects on brain functioning may result in irritability, shyness, tremors, changes in vision or hearing, and memory problems. Acrodynia, a type of mercury poisoning in children, is characterized by pain and pink discoloration of the hands and feet. Mercury poisoning can also cause Hunter-Russell syndrome and Minamata disease L1582.

Mersalyl

DB09338

small molecule experimental

Deskripsi

Mersalyl is the sodium salt form of mersalyl acid, a mercurial diuretic. It is an outdated drug, and its approval has been discontinued by the FDA. Mersalyl acid is currently replaced by less toxic non-mercury containing diuretics L1575, L1577. The sodium salt of a mercury-containing derivative of salicylamide, was formerly used (often in combination with theophylline) to treat edema, due to its powerful diuretic properties L1577. Interestingly, it has been found to have antiviral properties in mice L1584.

Struktur Molekul 2D

Berat 483.87
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) -
Volume Distribusi -
Klirens (Clearance) The hepatobiliary excretion of mersayl was studied in the isolated perfused rat liver and in isolated rat liver plasma membrane vesicles. In the isolated perfused liver, mersalyl was found to be immediately absorbed by the perfusion medium and concentratively excreted into bile. Uptake is characterized by saturation kinetics (S)0.5 = 20 microM, Vmax = 117 nmoles/min/g liver, cooperatively of mersalyl binding sites, stimulation by extracellular sodium and temperature dependence. Uptake of mersalyl into basolateral membrane vesicles also demonstrates characteristics of a carrier-mediated transport, dependence on extravesicular sodium, cooperativity of mersalyl binding sites, temperature dependence and trans-stimulation by intravesicular non-radioactive mersalyl. Uptake was found to be inhibited by alpha-naphthylacetic acid and mercapto group reagents, suggesting involvement of mercapto groups on the carrier and a binding site for carboxylic anions. Data from the isolated perfused liver and from isolated basolateral vesicles suggest that mersalyl uptake into the liver is carrier mediated. Uptake mechanism and driving forces appear analogous to those for the uptake of chemically related compounds such as taurocholic acid. It is, therefore, speculated that mersalyl may be transported by carrier molecules which accept various chemically unrelated compounds [L1584].

Absorpsi

Data absorpsi tidak tersedia.

Metabolisme

Organic mercury is absorbed primarily in the gastrointestinal tract, followed by distribution throughout the body via the bloodstream. Organic mercury forms a complex with free cysteine and the cysteine and sulfhydryl groups on proteins such as hemoglobin (Hgb). These complexes function to mimic methionine and, as a result, are transported throughout the body. This includes travel across the blood-brain barrier and across the placenta L1582.

Rute Eliminasi

Organic mercury is metabolized into inorganic mercury, which is eventually excreted in the urine and feces L1582.

Interaksi Obat

851 Data
Sodium phosphate, monobasic Mersalyl may increase the nephrotoxic activities of Sodium phosphate, monobasic.
Acemetacin The therapeutic efficacy of Mersalyl can be decreased when used in combination with Acemetacin.
Lactulose The risk or severity of dehydration can be increased when Mersalyl is combined with Lactulose.
Magnesium sulfate The risk or severity of dehydration can be increased when Mersalyl is combined with Magnesium sulfate.
Tegaserod The risk or severity of dehydration can be increased when Mersalyl is combined with Tegaserod.
Magnesium oxide The risk or severity of dehydration can be increased when Mersalyl is combined with Magnesium oxide.
Magnesium cation The risk or severity of dehydration can be increased when Mersalyl is combined with Magnesium cation.
Dantron The risk or severity of dehydration can be increased when Mersalyl is combined with Dantron.
Oxyphenisatin The risk or severity of dehydration can be increased when Mersalyl is combined with Oxyphenisatin.
Phenolphthalein The risk or severity of dehydration can be increased when Mersalyl is combined with Phenolphthalein.
Emodin The risk or severity of dehydration can be increased when Mersalyl is combined with Emodin.
Linaclotide The risk or severity of dehydration can be increased when Mersalyl is combined with Linaclotide.
Bisacodyl The risk or severity of dehydration can be increased when Mersalyl is combined with Bisacodyl.
Polyethylene glycol The risk or severity of dehydration can be increased when Mersalyl is combined with Polyethylene glycol.
Polycarbophil The risk or severity of dehydration can be increased when Mersalyl is combined with Polycarbophil.
Magnesium acetate tetrahydrate The risk or severity of dehydration can be increased when Mersalyl is combined with Magnesium acetate tetrahydrate.
Monopotassium phosphate The risk or severity of dehydration can be increased when Mersalyl is combined with Monopotassium phosphate.
Dipotassium phosphate The risk or severity of dehydration can be increased when Mersalyl is combined with Dipotassium phosphate.
Glycerin The risk or severity of dehydration can be increased when Mersalyl is combined with Glycerin.
Potassium lactate The risk or severity of dehydration can be increased when Mersalyl is combined with Potassium lactate.
Sodium fluorophosphate The risk or severity of dehydration can be increased when Mersalyl is combined with Sodium fluorophosphate.
Mineral oil The risk or severity of dehydration can be increased when Mersalyl is combined with Mineral oil.
Carboxymethylcellulose The risk or severity of dehydration can be increased when Mersalyl is combined with Carboxymethylcellulose.
Docusate The risk or severity of dehydration can be increased when Mersalyl is combined with Docusate.
Plantago seed The risk or severity of dehydration can be increased when Mersalyl is combined with Plantago seed.
Magnesium citrate The risk or severity of dehydration can be increased when Mersalyl is combined with Magnesium citrate.
Castor oil The risk or severity of dehydration can be increased when Mersalyl is combined with Castor oil.
Magnesium glycinate The risk or severity of dehydration can be increased when Mersalyl is combined with Magnesium glycinate.
Methylcellulose The risk or severity of dehydration can be increased when Mersalyl is combined with Methylcellulose.
Sennosides The risk or severity of dehydration can be increased when Mersalyl is combined with Sennosides.
Lactitol The risk or severity of dehydration can be increased when Mersalyl is combined with Lactitol.
Plecanatide The risk or severity of dehydration can be increased when Mersalyl is combined with Plecanatide.
Gluconic Acid The risk or severity of dehydration can be increased when Mersalyl is combined with Gluconic Acid.
Magnesium peroxide The risk or severity of dehydration can be increased when Mersalyl is combined with Magnesium peroxide.
Pentaerithrityl The risk or severity of dehydration can be increased when Mersalyl is combined with Pentaerithrityl.
Sodium tartrate The risk or severity of dehydration can be increased when Mersalyl is combined with Sodium tartrate.
Magnesium acetate The risk or severity of dehydration can be increased when Mersalyl is combined with Magnesium acetate.
Deacetylbisacodyl The risk or severity of dehydration can be increased when Mersalyl is combined with Deacetylbisacodyl.
Sodium ascorbate The risk or severity of dehydration can be increased when Mersalyl is combined with Sodium ascorbate.
Sodium phosphate, dibasic The risk or severity of dehydration can be increased when Mersalyl is combined with Sodium phosphate, dibasic.
Sodium phosphate, monobasic, unspecified form The risk or severity of dehydration can be increased when Mersalyl is combined with Sodium phosphate, monobasic, unspecified form.
Sodium phosphate, dibasic, unspecified form The risk or severity of dehydration can be increased when Mersalyl is combined with Sodium phosphate, dibasic, unspecified form.
Magnesium The risk or severity of dehydration can be increased when Mersalyl is combined with Magnesium.
Sodium cation The risk or severity of dehydration can be increased when Mersalyl is combined with Sodium cation.
Plantago ovata seed The risk or severity of dehydration can be increased when Mersalyl is combined with Plantago ovata seed.
Oxyphenisatin acetate The risk or severity of dehydration can be increased when Mersalyl is combined with Oxyphenisatin acetate.
Calcium polycarbophil The risk or severity of dehydration can be increased when Mersalyl is combined with Calcium polycarbophil.
Konjac mannan The risk or severity of dehydration can be increased when Mersalyl is combined with Konjac mannan.
Mannitol The risk or severity of dehydration can be increased when Mersalyl is combined with Mannitol.
Alloin The risk or severity of dehydration can be increased when Mersalyl is combined with Alloin.
Frangula purshiana bark The risk or severity of dehydration can be increased when Mersalyl is combined with Frangula purshiana bark.
Dehydrocholic acid The risk or severity of dehydration can be increased when Mersalyl is combined with Dehydrocholic acid.
Sulfate ion The risk or severity of dehydration can be increased when Mersalyl is combined with Sulfate ion.
Cyclosporine Cyclosporine may decrease the excretion rate of Mersalyl which could result in a higher serum level.
Icosapent Icosapent may decrease the excretion rate of Mersalyl which could result in a higher serum level.
Cefotiam Cefotiam may decrease the excretion rate of Mersalyl which could result in a higher serum level.
Mesalazine Mesalazine may decrease the excretion rate of Mersalyl which could result in a higher serum level.
Cefmenoxime Cefmenoxime may decrease the excretion rate of Mersalyl which could result in a higher serum level.
Cefmetazole Cefmetazole may decrease the excretion rate of Mersalyl which could result in a higher serum level.
Pamidronic acid Pamidronic acid may decrease the excretion rate of Mersalyl which could result in a higher serum level.
Cefpiramide Cefpiramide may decrease the excretion rate of Mersalyl which could result in a higher serum level.
Loracarbef Loracarbef may decrease the excretion rate of Mersalyl which could result in a higher serum level.
Cefalotin Cefalotin may decrease the excretion rate of Mersalyl which could result in a higher serum level.
Nabumetone Nabumetone may decrease the excretion rate of Mersalyl which could result in a higher serum level.
Ketorolac Ketorolac may decrease the excretion rate of Mersalyl which could result in a higher serum level.
Tenoxicam Tenoxicam may decrease the excretion rate of Mersalyl which could result in a higher serum level.
Celecoxib Celecoxib may decrease the excretion rate of Mersalyl which could result in a higher serum level.
Cefotaxime Cefotaxime may decrease the excretion rate of Mersalyl which could result in a higher serum level.
Tolmetin Tolmetin may decrease the excretion rate of Mersalyl which could result in a higher serum level.
Foscarnet Foscarnet may decrease the excretion rate of Mersalyl which could result in a higher serum level.
Rofecoxib Rofecoxib may decrease the excretion rate of Mersalyl which could result in a higher serum level.
Fenoprofen Fenoprofen may decrease the excretion rate of Mersalyl which could result in a higher serum level.
Valdecoxib Valdecoxib may decrease the excretion rate of Mersalyl which could result in a higher serum level.
Diclofenac Diclofenac may decrease the excretion rate of Mersalyl which could result in a higher serum level.
Sulindac Sulindac may decrease the excretion rate of Mersalyl which could result in a higher serum level.
Bacitracin Bacitracin may decrease the excretion rate of Mersalyl which could result in a higher serum level.
Amphotericin B Amphotericin B may decrease the excretion rate of Mersalyl which could result in a higher serum level.
Cephaloglycin Cephaloglycin may decrease the excretion rate of Mersalyl which could result in a higher serum level.
Adefovir dipivoxil Adefovir dipivoxil may decrease the excretion rate of Mersalyl which could result in a higher serum level.
Pentamidine Pentamidine may decrease the excretion rate of Mersalyl which could result in a higher serum level.
Mefenamic acid Mefenamic acid may decrease the excretion rate of Mersalyl which could result in a higher serum level.
Naproxen Naproxen may decrease the excretion rate of Mersalyl which could result in a higher serum level.
Sulfasalazine Sulfasalazine may decrease the excretion rate of Mersalyl which could result in a higher serum level.
Phenylbutazone Phenylbutazone may decrease the excretion rate of Mersalyl which could result in a higher serum level.
Carprofen Carprofen may decrease the excretion rate of Mersalyl which could result in a higher serum level.
Tacrolimus Tacrolimus may decrease the excretion rate of Mersalyl which could result in a higher serum level.
Ceforanide Ceforanide may decrease the excretion rate of Mersalyl which could result in a higher serum level.
Salicylic acid Salicylic acid may decrease the excretion rate of Mersalyl which could result in a higher serum level.
Balsalazide Balsalazide may decrease the excretion rate of Mersalyl which could result in a higher serum level.
Cefditoren Cefditoren may decrease the excretion rate of Mersalyl which could result in a higher serum level.
Atazanavir Atazanavir may decrease the excretion rate of Mersalyl which could result in a higher serum level.
Colistimethate Colistimethate may decrease the excretion rate of Mersalyl which could result in a higher serum level.
Cefuroxime Cefuroxime may decrease the excretion rate of Mersalyl which could result in a higher serum level.
Cefapirin Cefapirin may decrease the excretion rate of Mersalyl which could result in a higher serum level.
Cefprozil Cefprozil may decrease the excretion rate of Mersalyl which could result in a higher serum level.
Olsalazine Olsalazine may decrease the excretion rate of Mersalyl which could result in a higher serum level.
Lumiracoxib Lumiracoxib may decrease the excretion rate of Mersalyl which could result in a higher serum level.
Cefamandole Cefamandole may decrease the excretion rate of Mersalyl which could result in a higher serum level.
Cefazolin Cefazolin may decrease the excretion rate of Mersalyl which could result in a higher serum level.
Cefonicid Cefonicid may decrease the excretion rate of Mersalyl which could result in a higher serum level.

Target Protein

Alkaline phosphatase, tissue-nonspecific isozyme ALPL
Aquaporin-1 AQP1
Monocarboxylate transporter 1 SLC16A1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 1850465
    Park CS, Doh PS, Lee CJ, Han DS, Carraway RE, Miller TB: Cellular mechanism of stimulation of renin secretion by the mercurial diuretic mersalyl. J Pharmacol Exp Ther. 1991 Apr;257(1):219-24.
  • PMID: 2818621
    Thalhammer T, Graf J: Hepatobiliary transport of the anionic organomercury compound (mersalyl) is carrier mediated. Biochem Pharmacol. 1989 Oct 1;38(19):3223-31.
  • PMID: 7408902
    Steven FS, Griffin MM: Studies on the molecular mechanism of mersalyl and 4-aminophenylmercuric acetate re-activation of trypsin-thiol complexes. Eur J Biochem. 1980 Aug;109(2):567-73.

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