Pyrimethamin Produkt Beschreibung

Pyrimethamine Struktur
58-14-0
  • CAS-Nr.58-14-0
  • Bezeichnung:Pyrimethamin
  • Englisch Name:Pyrimethamine
  • Synonyma:Pyrimethamin
    wr2978;RP 4753;WR 2978;bw50-63;Malacid;Malocid;nsc3061;4753r.p.;Tindurin;BW 50-63
  • CBNumber:CB8461315
  • Summenformel:C12H13ClN4
  • Molgewicht:248.71
  • MOL-Datei:58-14-0.mol
Pyrimethamin physikalisch-chemischer Eigenschaften
  • Schmelzpunkt: :233-234°C
  • Siedepunkt: :393.35°C (rough estimate)
  • Dichte :1.2171 (rough estimate)
  • Brechungsindex :1.6110 (estimate)
  • storage temp.  : 0-6°C
  • Löslichkeit :Prepare the solution immediately before use. Dissolve 0.25 g in a mixture of 1 volume of methanol R and 3 volumes of methylene chloride R and dilute to 10 mL with the same mixture of solvents. The solution is clear (2.2.1) and not more intensely coloured than reference solution BY6 (2.2.2, Method II).
  • Aggregatzustand :neat
  • pka :pKa 7(t=20.0) (Uncertain)
  • Wasserlöslichkeit :<0.01 g/100 mL at 21 ºC
  • maximale Wellenlänge (λmax) :276nm(lit.)
  • Merck  :14,7985
  • BRN  :219864
  • Stabilität: :Stable, but light sensitive. Combustible. Incompatible with strong oxidizing agents.
  • CAS Datenbank :58-14-0(CAS DataBase Reference)
  • NIST chemische Informationen :Pyrimethamine(58-14-0)
  • EPA chemische Informationen :2,4-Pyrimidinediamine, 5-(4-chlorophenyl)-6-ethyl- (58-14-0)
Sicherheit
  • Kennzeichnung gefährlicher :Xn
  • R-Sätze: :22-36
  • S-Sätze: :26
  • RIDADR  :3249
  • WGK Germany  :3
  • RTECS-Nr. :UV8140000
  • HazardClass  :6.1(b)
  • PackingGroup  :III
  • HS Code  :29335990

Pyrimethamine Chemische Eigenschaften,Einsatz,Produktion Methoden

  • R-Sätze Betriebsanweisung: R22:Gesundheitsschädlich beim Verschlucken.
  • Chemische Eigenschaften White Solid
  • Verwenden For the treatment of toxoplasmosis and acute malaria; For the prevention of malaria in areas non-resistant to pyrimethamine.
    Pyrimethamine is a dihydrofolate reductase inhibitor, like the biguanides, and is structurally related to trimethoprim. It is seldom used alone. Pyrimethamine in fixed combinations with dapsone or sulfadoxine is used for treatment and prophylaxis of chloroquine-resistant falciparum malaria. The synergistic activities of pyrimethamine and sulfonamides are similar to those of trimethoprim/sulfonamide combinations. Resistant strains of Plasmodium falciparum have appeared world wide. Prophylaxis against falciparum malaria with pyrimethamine alone is therefore not recommended. Most strains of Plasmodium vivax have remained sensitive. Pyrimethamine is also used in combination with a sulfonamide for the treatment of Toxoplasmosis. It is slowly absorbed from the gastrointestinal tract with peak plasma levels 4–6 hours after dosing. Pyrimethamine is bound to plasma proteins and is extensively metabolized before excretion. Its elimination half-life is 3–5 days.
  • Verwenden Dihydrofolate reductase inhibitor; generally used in combination with other antimicrobial agents. Antiprotozoal (Toxoplasma); antimalarial
  • Indications Pyrimethamine (Daraprim) is the best of a number of 2,4- diaminopyrimidines that were synthesized as potential antimalarial and antibacterial compounds. Trimethoprim (Proloprim) is a closely related compound.
    Pyrimethamine is well absorbed after oral administration, with peak plasma levels occurring within 3 to 7 hours. An initial loading dose to saturate nonspecific binding sites is not required, as it is with chloroquine. However, the drug binds to tissues, and therefore, its rate of renal excretion is slow. Pyrimethamine has a half-life of about 4 days. Although the drug does undergo some metabolic alterations, the metabolites formed have not been totally identified.
  • Definition ChEBI: An aminopyrimidine that is pyrimidine-2,4-diamine which is substituted at position 5 by a p-chlorophenyl group and at position 6 by an ethyl group. It is a folic acid antagonist used as an antimalarial or with a sulfonamide to treat toxoplasmo is.
  • Trademarks Daraprim (GlaxoSmithKline).
  • Allgemeine Beschreibung Odorless white crystalline powder. Tasteless. An antimalarial drug.
  • Air & Water Reaktionen Pyrimethamine is a diaminopyrimidine which is structurally related to trimethoprim. It is effective against erythrocytic stage of Plasmodium (P) falciparum and less so against P. vivax, P. ovale and P. malariae. Pyrimethamine also inhibits the sporogony in the mosquito, resulting in a decrease of transmission of the infection within the community[1].
    The mechanism of action of pyrimethamine is related to its inhibition of dihydrofolic reductase necessary for the folic acid synthesis in the parasite. Pyrimethamine acts slowly and is not recommended as monotherapy for acute malaria attacks. Resistance to pyrimethamine developed soon when the drug was used on a large scale as monoprophylaxis [1]. In resistant strains, the enzyme dihydrofolic reductase binds to pyrimethamine several hundred times less than in sensitive strains [2]. This high grade resistance is probably a onestep mutation and cannot be overcome by increasing the dose. However, when combined with long-acting sulphonomides (sulphadoxine), the effect of pyrimethamine is potentiated and the risk of developing resistant strains is far less.
     
  • Reaktivität anzeigen Pyrimethamine together with sulphadoxine (Fansidar) is used in the treatment of P. falciparum malaria (cf. Sulphadoxine: Indications). Pyrimethamine is also valuable in the treatment of toxoplasmosis.
  • Brandgefahr Pyrimethamine in combination with sulphadoxine (Fansidar) can cause severe cutaneous adverse reactions (cf. Sulphadoxine: Side effects). Agranulocytosis occurs quite frequently (1/2000) and fatalities have been reported when pyrimethamine is combined with dapsone [3]. When given alone, life-threatening adverse reactions are very rare and the drug is generally well tolerated. Megaloblastic anaemia may, however, occur during long-term treatment with high doses (i.e. for toxoplasmosis) and can be prevented by folinic acid supplementation [4].
  • Biologische Aktivität During long-term treatment with high doses, folinic acid supplement is usually given.
  • Clinical Use Pyrimethamine has been recommended for prophylactic use against all susceptible strains of plasmodia; however, it should not be used as the sole therapeutic agent for treating acute malarial attacks. As mentioned previously, sulfonamides should always be coadministered with pyrimethamine (or trimethoprim), since the combined antimalarial activity of the two drugs is significantly greater than when either drug is used alone. Also, resistance develops more slowly when they are used in combination. Sulfonamides exert little or no effect on the blood stages of P. vivax, and resistance to the dihydrofolate reductase inhibitors is widespread.
    In addition to its antimalarial effects, pyrimethamine is indicated (in combination with a sulfonamide) for the treatment of toxoplasmosis.The dosage required is 10 to 20 times higher than that employed in malarial infections.
  • Nebenwirkungen Relatively few side effects are associated with the usual antimalarial dosages. However, signs of toxicity are evident at higher dosages, particularly those used in the management of toxoplasmosis. Many of these reactions reflect the interference of pyrimethamine with host folic acid metabolism, especially that occurring in rapidly dividing cells. Toxic symptoms include anorexia, vomiting, anemia, leukopenia, thrombocytopenia, and atrophic glossitis. CNS stimulation, including convulsions, may follow an acute overdose.The side effects associated with the pyrimethamine–sulfadoxine combination include those associated with the sulfonamide and pyrimethamine alone. In addition, there is evidence of a greater incidence of allergic reactions, particularly toxic epidermal necrolysis and Stevens-Johnson syndrome, with the combination. This carries an estimated mortality of 1:11,000 to 1:25,000 when used as a chemoprophylactic.
  • Sicherheitsprofil Poison by ingestion, subcutaneous, and intraperitoneal routes. Experimental teratogenic and reproductive effects. Questionable carcinogen. Human mutation data reported. When heated to decomposition it emits very toxic fumes of Cland NOx. Used as an antimalarial drug for humans and to treat toxoplasmosis in hogs.
  • Veterinary Drugs and Treatments In veterinary medicine, pyrimethamine is used to treat Hepatozoon americanum infections, and toxoplasmosis in small animals (often in combination with sulfonamides). In horses, it is used to treat equine protozoal myeloencephalitis, sometimes called equine toxoplasmosis.
    In humans, pyrimethamine is used for the treatment of toxoplasmosis and as a prophylactic agent for malaria.
Pyrimethamine Upstream-Materialien And Downstream Produkte
Upstream-Materialien
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58-14-0, Pyrimethamine Verwandte Suche:
  • 2,4-Diamino-5-(4-chlorophenyl)-6-ethylpyrimidine
  • 2,4-Diamino-5-chlorophenyl-6-ethylpyrimidine
  • 2,4-Pyrimidinediamine, 5-(4-chlorophenyl)-6-ethyl-
  • 2,4-Pyrimidinediamine, 5-(p-chlorophenyl)-6-ethyl-
  • 2,4-Pyrimidinediamine,5-(4-chlorophenyl)-6-ethyl-
  • 4753 R.P.
  • 4753r.p.
  • 5-(4’-chlorophenyl)-2,4-diamino-6-ethylpyrimidine
  • 5-(4'-Chlorophenyl)-2,4-diamino-6-ethylpyrimidine
  • 5-(4-Chlorophenyl)-2,4-diamino-6-ethylpyrimidine
  • 5-(4-chlorophenyl)-6-ethylpyrimidine-2,4-diyldiamine
  • 5-(P-Chlorophenyl)-6-ethyl-2,4-diaminopyrimidine
  • Pyrimidine,2,4-diamino-5-(p-chlorophenyl)-6-ethyl-
  • RP 4753
  • Tindurin
  • Tinduring
  • WR 2978
  • wr2978
  • PYRIMETHAMIN
  • PYRIMETHAMINE
  • 5-(4-CHLOROPHENYL)-6-ETHYL-2,4-PYRIMIDINEDIAMINE
  • 5-(4-CHLOROPHENYL)-6-ETHYL-PYRIMIDINE-2,4-DIAMINE
  • 2,4-diamino-5-(p-chlorophenyl)-6-ethylpyrimidine
  • PYRIMETHAMINE HCL
  • Pyrimeigamine
  • Pyrimethamine BP98 USP23
  • PYRIMETHAMINE VETRANAL, 250 MG
  • 5(4-Chloro Phenyl)-6-Ethyl-2,4-pyridine diamine
  • PYRIMETHAMINEUM
  • PYRIMETHAMINE,USP
  • Pyrimethamine (base and/or unspecified salts)
  • Pirimetmin
  • 5-(p-chlorophenyl)-6-ethyl-4-pyrimidinediamine
  • BW 50-63
  • bw50-63
  • Chloridin
  • Chloridine
  • Chloridyn
  • Darachlor
  • Daraclor
  • Darapram
  • Daraprim
  • Daraprime
  • Diaminopyritamin
  • Erbaprelina
  • Fansidar
  • Khloridin
  • Malacid
  • Malocid
  • Malocide
  • Maloprim
  • NCI-C01683
  • nsc3061
  • NSC-3061
  • Pirimecidan
  • Pirimetamin
  • Pirimetamina
  • Primethamine