chemspider StdInChIKey WKSAUQYGYAYLPV UHFFFAOYSA N Pyrimethamine Daraprim is a medication used ... in immunocompromise d patients, such as HIV positive individuals. Mechanism of action Pyrimethamine ... , including protozoa. Mechanism of resistance Resistance to pyrimethamine is widespread. Mutations in the malarial gene for dihydrofolate reductase may reduce the effectiveness of pyrimethamine. ref ... pyrimethamine in Plasmodium falciparum journal Antimicrob Agents Chemother volume 48 issue ... decrease the binding affinity between pyrimethamine and dihydrofolate reductase via loss of hydrogen ... ref Clinical use Pyrimethamine is typically given with a sulfonamide medicine sulfonamide and folinic ... Citation needed date January 2009 with pyrimethamine by blocking a different enzyme needed for folic ... related to folate deficiency. Use in mass drug administrations Pyrimethamine has been extensively ... contributed to the emergence and spread of pyrimethamine resistant Plasmodium falciparum strains. Side effects Pyrimethamine may deplete folic acid in humans, resulting in hematology hematologic side ... when used with a sulfonamide Contraindications Pyrimethamine is contraindicated in patients with hypersensitivity to pyrimethamine megaloblastic anemia &ndash depletion of folic acid may aggravate ... and pyrimethamine Antimalarials Category Antimalarial agents Category Dihydrofolate reductase ... more details
Drugbox verifiedrevid 447624347 type combo drug name Sulfadoxine pyrimethamine component1 Sulfadoxine class1 Sulfonamide medicine Sulfonamide component2 Pyrimethamine class2 Antiparasitic Clinical data tradename Fansidar Drugs.com MedlinePlus licence EU EMA requires brand name licence US FDA may use generic name DailyMedID preference to licence US pregnancy AU A B1 B2 B3 C D X pregnancy US C pregnancy category legal AU S2, S3, S4, S5, S6, S7, S8, S9 or Unscheduled legal CA OTC, Rx only, Schedule I, II, III, IV, V, VI, VII, VIII legal UK GSL, P, POM, CD, CD Lic, CD POM, CD No Reg POM, CD Benz POM, CD Anab POM or CD Inv POM legal US OTC Rx only Schedule I, II, III, IV, V legal status dependency liability routes of administration Oral Identifiers CAS number Ref cascite correct ?? CAS number CAS supplemental ATCvet ATC prefix P01 ATC suffix BD51 ATC supplemental PubChem PubChemSubstance IUPHAR ligand DrugBank Ref drugbankcite correct drugbank DrugBank ChemSpiderID Ref chemspidercite correct chemspider ChemSpiderID UNII Ref fdacite correct FDA UNII KEGG Ref keggcite correct kegg KEGG ChEBI Ref ebicite correct EBI ChEBI ChEMBL Ref ebicite correct EBI ChEMBL Sulfadoxine pyrimethamine Fansidar ... antibacterial sulfadoxine and the antiparasitic pyrimethamine . Both drugs are antifolate s they inhibit ... Activity of Pyrimethamine and Sulfadoxine against Plasmodium falciparum In Vitro Chulay ... of a species specific diagnosis the sulfadoxine pyrimethamine combination may be indicated. ref http jama.ama assn.org cgi content abstract 297 20 2201 JAMA Abstract Sulfadoxine Pyrimethamine ... and Pyrimethamine Bot generated title . ref but only to treat serious malaria infections ... information DR600357 Pyrimethamine and Sulfadoxine Oral Route MayoClinic.com Bot generated title . ref Programmatic use Sulfadoxine pyrimethamine has been used in mass drug administration s as well as in intermittent preventive therapy . See Also Sulfadoxine Pyrimethamine . References references Antimalarials ... more details
Diaminopyrimidines are a class of organic chemical compounds that include two amine groups on a pyrimidine ring. Image Iclaprim.svg thumb right 250px Iclaprim Image Trimethoprim.svg thumb right 250px Trimethoprim They include many dihydrofolate reductase inhibitor drug s such as pyrimethamine , trimetrexate , and piritrexim ref http aac.asm.org cgi content full 45 12 3293 Dicyclic and Tricyclic Diaminopyrimidine Derivatives as Potent Inhibitors of Cryptosporidium parvum Dihydrofolate Reductase Structure Activity and Structure Selectivity Correlations Nelson et al. 2001 ref and the antibiotic s Iclaprim and trimethoprim . Some have been patented as anti cancer drugs. ref http www.wipo.int pctdb en wo.jsp?IA GB1998000111&DISPLAY DESC ref See also 2,4 Diaminopyrimidine 4,5 Diaminopyrimidine References reflist Category Pyrimidines Category Aromatic amines organic compound stub de Diaminopyrimidine fr Diaminopyrimidine ... more details
using the antimalarial drug sulfadoxine pyrimethamine S P was pioneered in Ifakara, Tanzania in 1999 ... K, et al. Seasonal intermittent preventive treatment with artesunate and sulfadoxine pyrimethamine for prevention ... preventive treatment with sulphadoxine pyrimethamine targeting the transmission season on the incidence ... care ANC visits. Sulfadoxine pyrimethamine is the drug currently recommended by the WHO because ... K, Bulmer JN, Peshu N, et al. Intermittent sulphadoxine pyrimethamine to prevent severe anaemia ... of sulphadoxine pyrimethamine to reduce prevalence of pregnancy malaria in southern Mozambique. Trop ... and sulfadoxine pyrimethamine in a highly malarious area of Kenya a randomized controlled trial. Trans ... JM, Misore A, et al. Efficacy of sulfadoxine pyrimethamine for prevention of placental malaria in an area ... ME. Intermittent sulfadoxine pyrimethamine in pregnancy effectiveness against malaria morbidity ... treatment with sulphadoxine pyrimethamine for control of malaria in pregnancy in western Kenya a hospital ... P, Russell WB, Broadhead RL. An evaluation of the effects of intermittent sulfadoxine pyrimethamine ... groups and 157 deaths in the sulfadoxine pyrimethamine groups a protective efficacy of 2 ... now that resistance to sulfadoxine pyrimethamine has worsened. A recent trial of S P conducted in Tanzania ... pyrimethamine in northern Tanzania and the emergence of dhps resistance mutation at Codon ... effects, notably the cutaneous reactions that stopped the use of sulfadoxine pyrimethamine as prophylaxis ..., the WHO recommended the co administration of the antimalarial drug sulfadoxine pyrimethamine with routine ... ref Gesase, S., et al., High resistance of Plasmodium falciparum to sulphadoxine pyrimethamine in northern ... the phased implementation of artesunate plus sulfadoxine pyrimethamine in Maputo Province, Southern ... more details
Drugbox Verifiedfields changed verifiedrevid 408901454 IUPAC name 4 Amino N 5,6 dimethoxy 4 pyrimidinyl benzenesulfonamide image Sulfadoxine.png Clinical data tradename Drugs.com drugs.com international sulfadoxine pregnancy AU A B1 B2 B3 C D X pregnancy US A B C D X pregnancy category legal AU S2, S3, S4, S5, S6, S7, S8, S9 or Unscheduled legal CA Schedule I, II, III, IV, V, VI, VII, VIII legal UK GSL, P, POM, CD, or Class A, B, C legal US OTC Rx only Schedule I, II, III, IV, V legal status routes of administration Pharmacokinetic data bioavailability protein bound metabolism elimination half life excretion Identifiers CASNo Ref cascite CAS number Ref cascite correct ?? CAS number 2447 57 6 CAS supplemental ATCvet yes ATC prefix J01 ATC suffix EQ13 ATC supplemental PubChem 17134 DrugBank Ref drugbankcite changed drugbank DrugBank DB01299 ChemSpiderID Ref chemspidercite changed chemspider ChemSpiderID 16218 NIAID ChemDB 007816 UNII Ref fdacite changed FDA UNII 88463U4SM5 KEGG Ref keggcite correct kegg KEGG D00580 ChEMBL Ref ebicite changed EBI ChEMBL 1539 Chemical data chemical formula C 12 H 14 N 4 O 4 S 1 molecular weight 310.33 g mol smiles COC1 C N CN C1OC NS O O C2 CC C C C2 N Sulfadoxine also spelled sulphadoxine is an ultra long lasting Sulfonamide medicine sulfonamide often used in combination with pyrimethamine to treat or prevent malaria . ref name autogenerated1 http www.malaria ipca.com sulphadoxine pyrimethamine.html Medical Treatment Sulphadoxine and Pyrimethamine Bot generated title . ref It is also used, usually in combination with other drugs, to treat or prevent various infections in livestock. ref http en.scientificcommons.org 19483411. ref See also Sulfadoxine pyrimethamine References reflist Nucleic acid inhibitors Category Anilines Category Ethers Category Pyrimidines Category Sulfonamide antibiotics Category Dihydropteroate synthetase inhibitors Category Antimalarial agents antibiotic stub de Sulfadoxin es Sulfadoxina it Sulfadossina ... more details
List of drugs P Ps Pz ps pv Pseudo 12 pseudoephedrine International Nonproprietary Name INN Pseudofrin Pseudovent psilocybine International Nonproprietary Name INN Psorcon PsoriGel psyllium hemicellulose United States Adopted Name USAN Pulmicort Pulmolite pulmonol International Nonproprietary Name INN Pulmozyme pumaprazole International Nonproprietary Name INN pumitepa International Nonproprietary Name INN pumosetrag International Nonproprietary Name INN Purge drug Purge Purified Cortrophin Gel Purinethol Purinethol GlaxoSmithKline puromycin International Nonproprietary Name INN PVF K py pyl pyo Pylori Chek Breath Test Pyocidin Pyopen pyr pyrantel International Nonproprietary Name INN pyrazinamide International Nonproprietary Name INN pyricarbate International Nonproprietary Name INN Pyridamal 100 pyridarone International Nonproprietary Name INN pyridofylline International Nonproprietary Name INN pyridostigmine bromide International Nonproprietary Name INN pyridoxine International Nonproprietary Name INN pyrimethamine International Nonproprietary Name INN pyrimitate International Nonproprietary Name INN pyrinoline International Nonproprietary Name INN Pyrinyl pyrithione zinc International Nonproprietary Name INN pyrithyldione International Nonproprietary Name INN pyritidium bromide International Nonproprietary Name INN pyritinol International Nonproprietary Name INN Pyrolite pyronaridine United States Adopted Name USAN pyrophendane International Nonproprietary Name INN pyrovalerone International Nonproprietary Name INN pyroxamine International Nonproprietary Name INN pyrrocaine International Nonproprietary Name INN pyrrolifene International Nonproprietary Name INN pyrrolnitrin International Nonproprietary Name INN pyrvinium chloride International Nonproprietary Name INN pyt pytamine International Nonproprietary Name INN Pytest ... more details
Drugbox Verifiedfields changed verifiedrevid 408892547 IUPAC name 4 amino N pyrimidin 2 yl benzenesulfonamide image Sulfadiazine 2D skeletal.png width 250 image2 Sulfadiazine 3D vdW.png width2 250 Clinical data tradename Drugs.com drugs.com monograph sulfadiazine MedlinePlus a682130 pregnancy category ? legal status Approved Drug routes of administration Cream Pharmacokinetic data bioavailability ? metabolism ? elimination half life ? excretion ? Identifiers CASNo Ref cascite CAS number Ref cascite correct ?? CAS number 68 35 9 ATC prefix J01 ATC suffix EC02 ATC supplemental ATCvet J01 EQ10 PubChem 5215 DrugBank Ref drugbankcite changed drugbank DrugBank DB00359 ChemSpiderID Ref chemspidercite changed chemspider ChemSpiderID 5026 UNII Ref fdacite changed FDA UNII 0N7609K889 KEGG Ref keggcite correct kegg KEGG D00587 ChEMBL Ref ebicite changed EBI ChEMBL 439 Chemical data C 10 H 10 N 4 O 2 S 1 molecular weight 250.278 g mol Sulfadiazine is a Sulfonamide medicine sulfonamide antibiotic . Uses It eliminates bacteria that cause infections by stopping the production of folic acid inside the bacterial cell, and is commonly used to treat urinary tract infection s UTIs . In combination, sulfadiazine and pyrimethamine , can be used to treat toxoplasmosis , a disease caused by Toxoplasma gondii . Side effects Side effects reported for sulfadiazine include nausea , upset stomach , loss of appetite , and dizziness . Brand names Lantrisul Neotrizine Sulfa Triple 2 Sulfadiazine Sulfaloid Sulfonamides Duplex Sulfose Terfonyl Triple Sulfa Triple Sulfas Triple Sulfoid See also Silver sulfadiazine External links http www.meds help.com sulfadiazine Sulfadiazine patient information Category Aromatic amines Category Pyrimidines Category World Health Organization essential medicines Category Sulfonamide antibiotics Category Anilines Sulfonamides and trimethoprim Antiprotozoal agent antiinfective drug stub es Sulfadiazina it Sulfadiazina ja pt Sulfadiazina ru ... more details
Refimprove date December 2009 Antiprotozoal agents Anatomical Therapeutic Chemical Classification System ATC code ATC P01 is a class of pharmaceutical s used in treatment of protozoan infection . Protozoans have little in common with each other for example, Entamoeba histolytica is less closely related to Naegleria fowleri than it is to Homo sapiens and so agents effective against one pathogen may not be effective against another. However, metronidazole is selective for anaerobic organisms, and so it is effective against many though not all of these pathogens. They can be grouped by mechanism ref name Webster2001 cite book author Cynthia R. L. Webster title Clinical pharmacology url http books.google.com books?id NmR00leAkt8C&pg PA86 accessdate 2 May 2010 date 15 June 2001 publisher Teton NewMedia isbn 9781893441378 pages 86 ref or by organism. ref name TrevorKatzung2007 cite book author1 Anthony J. Trevor author2 Bertram G. Katzung author3 Susan B. Masters title Katzung & Trevor s pharmacology examination & board review url http books.google.com books?id Bvtkl3XUC5AC&pg PA435 accessdate 2 May 2010 date 11 December 2007 publisher McGraw Hill Professional isbn 9780071488693 pages 435 ref Examples Eflornithine Furazolidone Melarsoprol Metronidazole Ornidazole Paromomycin sulfate Pentamidine Pyrimethamine Tinidazole References Reflist Major Drug Groups Antiprotozoal agent Excavata antiparasitics Agents against amoebozoa DEFAULTSORT Antiprotozoal Agent Category Antiprotozoal agents Antimicrobial stub de Antiprotozoikum es Antiprotozoario ja ... more details
suspected drugs Isotab was contaminated. The report also showed that Isotab contained Pyrimethamine which is in fact used for the treatment of malaria . The presence of pyrimethamine proved ... Drugs Laboratory in Karachi also verified the presence of pyrimethamine used in certain combinations ... title Isotab Contamination with pyrimethamine issu FIA seals three firms manufacturing deadly Isotab ... more details
The Garki Project was a non profit study conducted by the World Health Organization from 1969 to 1976 in the Garki, Nigeria Garki Local Government Area of the Jigawa State then part of the Kano State , Nigeria . Its purpose was to study epidemiology and control of malaria in the lowland rural Sudan savanna in northern Nigeria. The main objectives of the project were to measure the effects of indoor residual spraying and mass drug administration and to construct and test a mathematical model of malaria transmission. ref cite book last Molineaux first L. last2 Gramiccia first2 G. title The Garki Project Research on the Epidemiology and Control of Malaria in the Sudan Savanna of West Africa publisher World Health Organization year 1980 isbn 9241560614 ref The project was funded by both the World Health Organization and the Federal Government of Nigeria. The project concluded that indoor spraying with Propoxur had a very limited impact on malaria and the mass administration of Antimalarial medication sulfalene pyrimethamine in combination with the residual spraying failed to interrupt the transmission of malaria for any length of time. However, the mathematical model used was found to simulate the epidemiology of Plasmodium falciparum fairly realistically and was considered fit for use in planning control of malaria. ref cite journal last Molineaux first L. last2 Deitz first2 K. last3 Thomas first3 A. title Further Epidemiological Evaluation of a Malaria Model journal Bull. World Health Organ. volume 56 issue 4 pages 565 71 year 1978 ref References Reflist External Links http www.swisstph.ch fr ressources epidemiological databases.html The Swiss TPH Epidemiological Databases Page with references to the Garki project and data Category Malaria Category Jigawa State ... more details
A dihydrofolate reductase inhibitor is a molecule that inhibits the function of dihydrofolate reductase , and is a type of antifolate . Since folate is needed by rapidly dividing cells to make thymine , this effect may be used to therapeutic advantage. For example, methotrexate is used as cancer chemotherapy because it can prevent neoplastic cells from dividing. ref name pmid7942284 cite journal author Huennekens FM title The methotrexate story a paradigm for development of cancer chemotherapeutic agents journal Adv. Enzyme Regul. volume 34 issue pages 397 419 year 1994 pmid 7942284 doi 10.1016 0065 2571 94 90025 6 url ref ref name pmid14529544 cite journal author McGuire JJ title Anticancer antifolates current status and future directions journal Curr. Pharm. Des. volume 9 issue 31 pages 2593 613 year 2003 pmid 14529544 doi 10.2174 1381612033453712 url ref Bacteria also need DHFR to grow and multiply and hence inhibitors selective for bacterial vs. host DHFR have found application as antibacterial agents. ref name pmid16359642 cite journal author Hawser S, Lociuro S, Islam K title Dihydrofolate reductase inhibitors as antibacterial agents journal Biochem. Pharmacol. volume 71 issue 7 pages 941 8 year 2006 month March pmid 16359642 doi 10.1016 j.bcp.2005.10.052 url ref Image THFsynthesispathway.png thumb 400px center Tetrahydrofolate synthesis pathway A variety of drugs act as enzyme inhibitor inhibitors of dihydrofolate reductase the antibiotic trimethoprim and its derivatives brodimoprim , tetroxoprim , and iclaprim . the antimalarial drugs pyrimethamine and proguanil . the experimental new antimalarial drug JPC 2056 , which may also be more effective and better tolerated than current treatments against toxoplasmosis . ref cite journal author Mui EJ, Schiehser GA, Milhous WK, et al. editor1 last Matlashewski editor1 first Greg title Novel Triazine JPC 2067 B Inhibits Toxoplasma gondii In Vitro and In Vivo journal PLoS Negl Trop Dis volume 2 issue 3 pages e190 year ... more details
doi url ref The target population of 83,000 received a single dose of pyrimethamine at the beginning ... malaria epidemics. In the following three years, 1955 to 1957, pyrimethamine administration was replaced ... of chloroquine pyrimethamine was combined with spraying of residual insecticides DDT . ref name pmid13720940 ... with propoxur , a residual insecticide. In addition, in 60 villages, MDA with sulfalene pyrimethamine ... in 33 of 42 villages in the catchment area received a single dose of sulfadoxine pyrimethamine ... administration of sulfadoxine pyrimethamine combined with artesunate on malaria incidence a double ... chloroquine base and 45 mg pyrimethamine weekly for nine weeks. An additional 300 mg chloroquine and 75 mg pyrimethamine plus 1500 mg sulfadoxine was added to this regimen in the first ... pages 245 55 year 1964 month September pmid 14208125 doi url ref Salt crystals were mixed with pyrimethamine so as to provide a 0.07 pyrimethamine salt. As there were no shops in the catchment area ... levels of pyrimethamine resistance were reported. It was then decided to mix the remaining ... a population of approximately 20,000. Sea salt was mixed with pyrimethamine at a concentration ... pyrimethamine resistance was reported, pyrimethamine was replaced by chloroquine . From 1961 ... that MDA would cause pyrimethamine and later chloroquine resistance was first raised in the early ... more details
, mefloquine , and sulfa drug combinations with pyrimethamine . Quinine is also used in post ... Health Organisation. Combination with sulfadoxine pyrimethamine is no longer recommended WHO ... have also been seen in a small number of patients. PyrimethaminePyrimethamine is used in the treatment ... pyrimethamine , most commonly as fixed dose sulfadoxine pyrimethamine Fansidar , produces synergism ... . Chloroquine proguanil or sulfa drug pyrimethamine combinations should be used in all other ... and pyrimethamine. Two gene mutations are thought to be responsible, allowing synergistic ... Dose Sulfadoxine pyrimethamine SP Fansidar This fixed dose combination has been used for many ... malaria. 25 mg kg of sulfadoxine and 1.25 mg kg of pyrimethamine. SP plus chloroquine ... plus sulfadoxine pyrimethamine for the treatment of uncomplicated P. falciparum malaria. ref ... for uncomplicated falciparum malaria. ref name who2010 Artesunate and sulfadoxine pyrimethamine ... depends on the level of resistance to sulfadoxine and pyrimethamine thus limiting is usage. It is recommended ... more details
such as trimethoprim and pyrimethamine . Folinic acid may be prescribed in the treatment of toxoplasmosis retinitis , in combination with the folic acid antagonists pyrimethamine and sulfadiazine ... more details
otheruses Ion trap The term ion trapping is used to describe the build up of a higher concentration of a chemical across a cell membrane due to the pKa value of the chemical and difference of pH across the cell membrane. Generally speaking, this results in basic chemicals accumulating in acidic bodily fluids such as the cytosol , and acidic chemicals accumulating in basic fluids such as mastitic milk. Many Cell biology cells have other mechanisms to pump a molecule inside or outside the cell against the concentration gradient , but these processes are active ones, meaning that they require enzymes and consume cellular energy . In contrast, ion trapping does not require any enzyme or energy. It is similar to osmosis in that they both involve the semipermeable nature of the cell membrane. Cells have a more acidic pH inside the cell than outside gastric mucosa l cells being an exception . Therefore basic drugs like bupivacaine , pyrimethamine are more charged inside the cell than outside. The cell membrane is permeable to non ionized fat soluble molecules ionized water soluble molecules cannot cross it easily. Once a non charged molecule of a basic chemical crosses the cell membrane to enter the cell, it becomes charged due to gaining a hydrogen ion because of the lower pH inside the cell, and thus becomes unable to cross back. Because transmembrane equilibrium must be maintained, another unionized molecule must diffuse into the cell to repeat the process. Thus its concentration inside the cell increases many times that of the outside. The non charged molecules of the drug remain in equal concentration on either side of the cell membrane. The charge of a molecule depends upon the pH of its solution. In an acidic medium, basic drugs are more charged and acidic drugs are less charged. The converse is true in a basic medium. For example, Naproxen is a non steroidal anti inflammatory drug that is a weak acid its pKa value is 5.0 . The gastric juice has a pH of 2.0. It is a ... more details
Antifolates are drug s that impair the function of folic acid s. ref name urlNCI antifolate cite web url http www.jamesline.com cancertypes glossary index.cfm?action Display&ID 44814&Letter A title NCI antifolate format work accessdate ref Many are used in cancer chemotherapy , some are used as antibiotics or antiprotozoal agents. A well known example is methotrexate . This is a folic acid analogue, and owing to structural similarity with it binds and inhibits the enzyme dihydrofolate reductase DHFR , and thus prevents the formation of tetrahydrofolate . Because tetrahydrofolate is essential for purine and pyrimidine synthesis, its deficiency can lead to inhibited production of DNA , RNA , and proteins as tetrahydrofolate is also involved in the synthesis of amino acids serine and methionine . Since antifolates interfere with metabolism of nucleotide s , they are categorized as antimetabolite s. Other antifolates include trimethoprim , pyrimethamine , and pemetrexed . Many are primarily DHFR inhibitors, but raltitrexed is an inhibitor of thymidylate synthase , and pemetrexed inhibits both and a third enzyme. Indications Low dose methotrexate is used to treat a wide variety of non cancerous diseases such as rheumatoid arthritis , Lupus erythematosus lupus , scleroderma , psoriasis , asthma , sarcoidosis , primary biliary cirrhosis , polymyositis , and inflammatory bowel disease . ref name Oldref 52 cite book author Morgan SL, Baggott JE year 1995 title Folate antagonists in nonneoplastic disease proposed mechanisms of efficacy and toxicity editor Bailey LB pages 405 33 publisher New York Marcel Dekker isbn 0 8247 9280 7 work Folate in Health and Disease ref Mechanism Antifolates act specifically during DNA and RNA synthesis, and thus are cytotoxic during the S phase of the cell cycle. Thus, they have a greater toxic effect on rapidly dividing cells such as malignant and myeloid cells, and GI & oral mucosa , which replicate their DNA more frequently, and thus inhibits ... more details
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