MyMedR

Toxic effects of the suplhanilamide group

Landor JV

Journal of the Malaya Branch of the British Medical Association, 1939;3:98-99.

Matched MeSH terms: Sulfanilamides

The treatment of pneumonia with M & B 693

Monteiro ES

Journal of the Malaya Branch of the British Medical Association, 1939;3:52-79.

Matched MeSH terms: Sulfanilamides

Severe cutaneous adverse reactions and sulphadoxine-pyrimethamine in Sabah, Malaysia

Lyn PC, Fernandez E

Med J Aust, 1987 Mar 16;146(6):335-6.

PMID: 2950306

Matched MeSH terms: Sulfanilamides/adverse effects*

Single dose kinetic study of the triple combination mefloquine/sulphadoxine/pyrimethamine (Fansimef) in healthy male volunteers

Mansor SM, Navaratnam V, Mohamad M, Hussein S, Kumar A, Jamaludin A, et al.

Br J Clin Pharmacol, 1989 Mar;27(3):381-6.

PMID: 2785812

A single dose pharmacokinetic study of a combined antimalarial formulation of mefloquine, sulphadoxine and pyrimethamine (Fansimef) has been performed in 10 healthy adult male Malaysian volunteers. The dose consisted of two tablets containing 250 mg mefloquine base, 500 mg sulphadoxine base and 25 mg pyrimethamine base each. Plasma concentrations of mefloquine and pyrimethamine were measured by GC-ECD, those of sulphadoxine by h.p.l.c. Time to peak concentrations (mean +/- s.d. for mefloquine (5.70 +/- 0.95 h), sulphadoxine (3.75 +/- 2.03 h) and pyrimethamine (3.30 +/- 1.98 h) were similar to those observed by others after administration of the single compounds. This was also true for elimination half-lives (t1/2). The t1/2s for mefloquine, sulphadoxine and pyrimethamine were 387 +/- 98 h, 255 +/- 61 h and 114 +/- 42 h, respectively.

Matched MeSH terms: Sulfanilamides/pharmacokinetics*

Physicochemical modulation of skin barrier by microwave for transdermal drug delivery

Wong TW, Nor Khaizan A

Pharm Res, 2013 Jan;30(1):90-103.

PMID: 22890987 DOI: 10.1007/s11095-012-0852-z

PURPOSE: To investigate mechanism of microwave enhancing drug permeation transdermally through its action on skin.

METHODS: Hydrophilic pectin-sulphanilamide films, with or without oleic acid (OA), were subjected to drug release and skin permeation studies. The skins were untreated or microwave-treated, and characterized by infrared spectroscopy, Raman spectroscopy, thermal, electron microscopy and histology techniques.

RESULTS: Skin treatment by microwave at 2450 MHz for 5 min promoted drug permeation from OA-free film without incurring skin damage. Skin treatment by microwave followed by film loaded with drug and OA resulted in permeation of all drug molecules that were released from film. Microwave exerted spacing of lipid architecture of stratum corneum into structureless domains which was unattainable by OA. It allowed OA to permeate stratum corneum and accumulate in dermis at a greater ease, and synergistically inducing lipid/keratin fluidization at hydrophobic C-H and hydrophilic O-H, N-H, C-O, C=O, C-N regimes of skin, and promoting drug permeation.

CONCLUSION: The microwave technology is evidently feasible for use in promotion of drug permeation across the skin barrier. It represents a new approach in transdermal drug delivery.

Matched MeSH terms: Sulfanilamides/administration & dosage*; Sulfanilamides/pharmacokinetics

Erythema exudativum multiforme following sulphonamide therapy

D'ABRERA VS

Med J Malaya, 1957 Dec;12(2):427-34.

PMID: 13515874

Matched MeSH terms: Sulfanilamides

Fulltext Oral lichenoid reactions during antimalarial prophylaxis with sulphadoxine-pyrimethamine combination

Zain RB

Southeast Asian J. Trop. Med. Public Health, 1989 Jun;20(2):253-6.

PMID: 2609215

The prevalence of clinically observed oral lichenoid reaction in 186 Malay army personnel using Fansidar for 9 weeks was found to be 4.8%. The prevalence was found to be 0.5% in 186 army personnel who had stopped using Fansidar for 2 months and 0% in 143 army personnel (control group) who had not used Fansidar for at least 4 months. The lesion showed a higher prevalence for the gingiva. There was no correlation between cigarette smoking and the occurrence of these lesions in each group.

Matched MeSH terms: Sulfanilamides/adverse effects*

Fansidar resistant falciparum malaria acquired in South East Asia

Black F, Bygbjerg I, Effersøe P, Gomme G, Jepsen S, Jensen GA

Trans R Soc Trop Med Hyg, 1981;75(5):715-6.

PMID: 7036431

A case of Plasmodium falciparum malaria resistant to Fansidar (sulphadoxine plus pyrimethamine) at a level corresponding to R III and resistant to chloroquine is reported. The infection was most certainly acquired in Malaysia, but diagnosed and treated in a non-malarious area. Normal resorption and elimination rates of the Fansidar components excludes cure failure due to abnormal drug fate in the host. P. falciparum parasites from the patient have been maintained in vitro cultures. The patient was permanently cured with mefloquine.

Matched MeSH terms: Sulfanilamides/therapeutic use*

Fulltext Falciparum malaria resistant to Fansidar (sulphadoxine-pyrimethamine) occurring in three children of the same family

Ponnampalam JT

Singapore Med J, 1982 Feb;23(1):37-8.

PMID: 7051329

Three cases of multiple drug resistant falciparum malaria in the same family are described. It is interesting to note that faIciparum malaria resistant to Fansidar has not as yet been reported in adults from West Malaysia up to the present time, although resistance to the drug in children is being encountered not infrequently. This presents a serious paediatric problem because malaria causes the highest incidence of mortality and morbidity in this age group in a proportion of the rural population.

Matched MeSH terms: Sulfanilamides/pharmacology*

Fulltext Treatment failure of falciparum malaria with Fansidar in Tawau Sabah. January-June, 1982

Tan HS, Tan PE

Med J Malaysia, 1983 Sep;38(3):217-23.

PMID: 6369092

One hundred and ten consecutive patients with falciparum malaria were treated with Fansidar and primaquine. Of the 61 patients who were followed up at one week, 4 (6.5%) failed to clear their parasitemia (1 R III and 3 R Il treatment failures). Of the subsequent 40 patients who were seen again at one month, another 3 (7.5%) had recrudesced (R 1 treatment failure). A total of 7 patients thus experienced some form of treatment failure in the cohort of 40 who completed the one month follow up. Only 1 of these 7patients (with R III treatment) failure) failed to respond to repeat Fansidar treatment, and may be the only one with true Fansidar resistance. The overall treatment failure rate of 17.5% (95% confidence interval: 6-29%) in the cohort who completed the study is consistent with the known clinical efficacy of Fansidar. These results suggest no significant Fansidar resistance in falciparum malaria found in Sabah.

Matched MeSH terms: Sulfanilamides/therapeutic use*

Clinical efficacy of sulfadoxine-pyrimethamine in the treatment of falciparum malaria in Sabah, Malaysia

Tan HS, Tan PE

Ann Acad Med Singap, 1984 Apr;13(2):170-4.

PMID: 6388486

One hundred and ten consecutive patients with falciparum malaria were treated with Fansidar and primaquine. Of the 61 patients who were followed up at one week, 4 (6.6%) failed to clear their parasitaemia (1 R III and 3 R II treatment failures). Of the subsequent 40 patients who were seen again at one month, another 3 (7.5%) had recrudesced (R I treatment failure). A total of 7 patients thus experienced some form of treatment failure in the cohort of 40 who completed the one month follow up. Only 1 of these 7 patients (with R III treatment failure) failed to respond to repeat Fansidar treatment, and may be the only one with true Fansidar resistance. The overall treatment failure rate of 17.5% (95% confidence interval: 6-29%) in the cohort who completed the study is consistent with the known clinical efficacy of Fansidar. These results suggest no significant Fansidar resistance in falciparum malaria found in Sabah.

Matched MeSH terms: Sulfanilamides/therapeutic use*

Chemosuppression of malaria by the triple combination mefloquine/sulfadoxine/pyrimethamine: a field trial in an endemic area in Malaysia

Navaratnam V, Mohamad M, Hussain S, Kumar A, Jamaludin A, Sulaiman I, et al.

Trans R Soc Trop Med Hyg, 1989 11 1;83(6):755-9.

PMID: 2694509

Malaria, particularly that due to chloroquine-resistant Plasmodium falciparum, which requires management with antimalarial drugs capable of protecting against multiresistant strains, has emerged in Malaysia. A study was carried out to assess the efficacy and tolerability of 2 dosages of mefloquine/sulfadoxine/pyrimethamine (MSP; RO 13-5112) compared to Fansidar in a malaria endemic area. 914 subjects in 3 random groups were studied. Occurrence of malaria was assessed both clinically as well as by blood films. Plasma drug levels were also measured. The results showed that the low dose of MSP was completely effective in suppressing parasitaemia. 2.7% of the study population reported adverse drug reactions, the lowest incidence being in subjects on the low dose; their blood chemical profiles were also the least affected. The plasma levels of pyrimethamine and sulfadoxine achieved in the low dose group were slightly higher than expected, but there was no significant difference in bioavailability. The study showed that, for chemoprophylaxis, a low dose of MSP provided effective protection with minimal side effects.

Matched MeSH terms: Sulfanilamides/therapeutic use*

The effect of various drugs on the glucuronidation of zidovudine (azidothymidine; AZT) by human liver microsomes

Sim SM, Back DJ, Breckenridge AM

Br J Clin Pharmacol, 1991 Jul;32(1):17-21.

PMID: 1909542

1. Zidovudine (3'-azido-3'-deoxythymidine; AZT) is the drug of proven efficacy available for the treatment of patients with AIDS or ARC. It is eliminated mainly by hepatic glucuronidation. Therefore, interference with this metabolic pathway may lead to enhancement of AZT effect or to increased toxicity of the drug. We have examined the effect of a number of drugs which themselves undergo glucuronidation on AZT conjugation by human liver microsomes in vitro. 2. AZT glucuronidation followed Michaelis-Menten kinetics. The apparent Km and Vmax values (mean +/- s.d., n = 5), were 2.60 +/- 0.52 mM and 68.0 +/- 23.4 nmol h-1 mg-1, respectively, as determined from Eadie-Hofstee plots. 3. Dideoxyinosine, sulphanilamide and paracetamol were essentially non-inhibitory at concentrations up to 10 mM (4 times the concentration of AZT in the incubation). The most marked inhibitory effects were seen with indomethacin, naproxen, chloramphenicol, probenecid and ethinyloestradiol, with enzyme activity decreased by 97.7, 94.9, 88.7, 83.4% and 79.0%, respectively, at a concentration of 10 mM. Other compounds producing some inhibition of AZT conjugation were oxazepam, salicylic acid and acetylsalicylic acid. 4. Further studies are necessary to characterise the inhibition observed but the method described enables a screen of potentially important drug interactions to be carried out.

Matched MeSH terms: Sulfanilamides/pharmacology

A comparative study of malaria prophylaxis in peninsular Malaysia using chloroquine and a combination of sulphadoxine and pyrimethamine

Ponnampalam JT

J Trop Med Hyg, 1978 Oct;81(10):198-203.

PMID: 366165

Matched MeSH terms: Sulfanilamides/therapeutic use*

Suppression of malaria with monthly administration of combined sulphadoxine and pyrimethamine

Lewis AN, Ponnampalam JT

Ann Trop Med Parasitol, 1975 Mar;69(1):1-12.

PMID: 1092276

A trial of suppression of malaria by administration of combined sulphadoxine-pyrimethamine tablets every 28 days was undertaken in West Malaysia during 1972. One thousand subjects were followed over a 10-month period, including control groups on placebo and on weekly chloroquine. Subjects were examined monthly for parasitaemia, drug reactions, leucopenia, teratogenicity and haemolysis among the subjects deficient in glucose-6-phosphate dehydrogenase. Rates of new infections in the placebo group were 8.0% with Plasmodium falciparum and 6.2% with P. vivax; in the group receiving weekly chloroquine, 5.1% P. falciparum and 0.3% P. vivax; and in the group receiving monthly sulphadoxine-pyrimethamine, 0.3% P. Falciparum and 1.0% P. vivax. The effective rate of cure of new infections with P. falciparum by a single suppressive dose of combined sulphadoxine-pyrimethamine given the following month was 88.7%. No serious side effects were observed.

Matched MeSH terms: Sulfanilamides/administration & dosage*

Pharmacokinetic rationale for a malarial suppressant administered once monthly

Peck CC, Lewis AN, Joyce BE

Ann Trop Med Parasitol, 1975 Jun;69(2):141-5.

PMID: 1155986

Serum was collected from six adults participating in a field trial of sulfadoxine and pyrimethamine in combination which was being administered once monthly for malaria suppression. Samples were drawn during each of two consecutive months three hours, and 7, 14 and 28 days following a dose of 1 500 mg sulfadoxine. Serum sulfadoxine concentration was measured using the method of Bratton and Marshall (1939). Initial serum concentrations averaged 19-9 plus or minus 2-4 (SD) mg/100 ml and decayed to 6-2 plus or minus 2-8 mg/100 ml at 14 days. Serum sulfadoxine concentrations were still detectable at 28 days following a dose (2-1 plus or minus 1-5 mg/100 ml). Elimination half-time averaged 195 plus or minus 44 hours. The presistent serum concentrations of sulfadoxine following monthly doses documented here during field-use of this drug are in agreement with the successful clinical results reported for such a regimen (Lewis and Ponnampalam, 1974; O'Holohan and Hugoe-Mathews, 1971; Wolfensberger, 1971).

Matched MeSH terms: Sulfanilamides/pharmacology*

Synthesis and biological evaluation of curcumin-like diarylpentanoid analogues for anti-inflammatory, antioxidant and anti-tyrosinase activities

Lee KH, Ab Aziz FH, Syahida A, Abas F, Shaari K, Israf DA, et al.

Eur J Med Chem, 2009 Aug;44(8):3195-200.

PMID: 19359068 DOI: 10.1016/j.ejmech.2009.03.020

A series of 46 curcumin related diarylpentanoid analogues were synthesized and evaluated for their anti-inflammatory, antioxidant and anti-tyrosinase activities. Among these compounds 2, 13 and 33 exhibited potent NO inhibitory effect on IFN-gamma/LPS-activated RAW 264.7 cells as compared to L-NAME and curcumin. However, these series of diarylpentanoid analogues were not significantly inhibiting NO scavenging, total radical scavenging and tyrosinase enzyme activities. The results revealed that the biological activity of these diarylpentanoid analogues is most likely due to their action mainly upon inflammatory mediator, inducible nitric oxide synthase (iNOS). The present results showed that compounds 2, 13 and 33 might serve as a useful starting point for the design of improved anti-inflammatory agents.

Matched MeSH terms: Sulfanilamides

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