Methicillin

Douthwaite, A. H.; Trafford, J. A. P.; McGill, D. A. F.; Evans, I. E.

doi:10.1136/bmj.2.5243.6

Cited by 27 publications

(4 citation statements)

References 3 publications

(5 reference statements)

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“…aureus became resistant to penicillin treatment relatively soon after its discovery. Methicillin (the first designer anti-resistance antibiotic) was introduced in 1960 in the defense against penicillinases,[ 23 ] with the emergence of methicillin-resistant S. aureus (MRSA) arising shortly thereafter. [ 24 25 ] The establishment of MRSA within the community may be due to the overuse of antibacterial-containing substances in common household and hospital cleaning products to achieve a “super clean” environment.…”

Section: Evolution Of Bacterial Resistancementioning

confidence: 99%

Developing new antimicrobial therapies: Are synergistic combinations of plant extracts/compounds with conventional antibiotics the solution?

Cheesman¹,

Ilanko²,

Blonk³

et al. 2017

Phcog Rev

360

169

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The discovery of penicillin nearly 90 years ago revolutionized the treatment of bacterial disease. Since that time, numerous other antibiotics have been discovered from bacteria and fungi, or developed by chemical synthesis and have become effective chemotherapeutic options. However, the misuse of antibiotics has lessened the efficacy of many commonly used antibiotics. The emergence of resistant strains of bacteria has seriously limited our ability to treat bacterial illness, and new antibiotics are desperately needed. Since the discovery of penicillin, most antibiotic development has focused on the discovery of new antibiotics derived from microbial sources, or on the synthesis of new compounds using existing antibiotic scaffolds to the detriment of other lines of discovery. Both of these methods have been fruitful. However, for a number of reasons discussed in this review, these strategies are unlikely to provide the same wealth of new antibiotics in the future. Indeed, the number of newly developed antibiotics has decreased dramatically in recent years. Instead, a reexamination of traditional medicines has become more common and has already provided several new antibiotics. Traditional medicine plants are likely to provide further new antibiotics in the future. However, the use of plant extracts or pure natural compounds in combination with conventional antibiotics may hold greater promise for rapidly providing affordable treatment options. Indeed, some combinational antibiotic therapies are already clinically available. This study reviews the recent literature on combinational antibiotic therapies to highlight their potential and to guide future research in this field.

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Section: Evolution Of Bacterial Resistancementioning

confidence: 99%

Developing new antimicrobial therapies: Are synergistic combinations of plant extracts/compounds with conventional antibiotics the solution?

Cheesman¹,

Ilanko²,

Blonk³

et al. 2017

Phcog Rev

360

169

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“…Methicillin penetration of the BBB is not much better, the CSF /serum ratio in normal human subjects being 0.5 %. [18][19][20][21] By application of the CDS approach an improved CNS penetration and a prolonged release of these drugs are expected. Their use in the treatment of brain infections would be in this way permitted.…”

mentioning

confidence: 99%

Chemical delivery systems for some penicillinase-resistant semisynthetic penicillins

Pop¹,

Wu²,

Bodor³

1989

J. Med. Chem.

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Chemical delivery systems (CDS's) based on a dihydropyridine----quaternary pyridinium ion redox system analogous to the naturally occurring NADH----NAD+ system were synthesized for a group of staphylococcal penicillinase resistant penicillins, including methicillin, oxacillin, cloxacillin, and dicloxacillin, in order to improve their penetration of the central nervous system (CNS). The CDS's are penicillin monoesters of gem-diols in which the other hydroxyl group is esterified by the dihydrotrigonelline carrier. The CDS's were found to be much more lipopholic than the parent drugs by comparing their log k' values used as lipophilicity indexes. A study of the chemical oxidation of the CDS's performed by a UV spectrophotometric method showed relatively slow reaction. Stability studies were performed in buffers and different animal tissues for both the CDS's and the quaternary salt type derivatives. These studies showed that the CDS's were oxidized to the quaternary salt forms at neutral and basic pH and added water at lower pH. The quaternary salts released the parent drugs both in buffers and in vitro. A preliminary in vivo distribution study in the rat and rabbit demonstrated blood-brain barrier (BBB) penetration by the CDS, whereas no drug was detected by administering the drug itself.

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“…In analyzing reported cases of staphylococcal endocarditis, chiefly in the American literature, I have restricted our attention to 29 cases where success or failure could be attributed specifically to a penicillinase resistant penicillin (Bunn, 1960;Campeau et al, 1961;Douthwaite et al, 1961;Allen et al, 1962;Sabath et al, 1962;Simon and Rantz, 1962;Doyle, 1964;and Quinn, 1964). The duration of treatment seems to be more important than the daily dosage.…”

Section: Clinical Observationsmentioning

confidence: 99%

The New Penicillins in Endocarditis

Hamburger

1964

Postgraduate Medical Journal

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Methicillin

Cited by 27 publications

References 3 publications

Developing new antimicrobial therapies: Are synergistic combinations of plant extracts/compounds with conventional antibiotics the solution?

Developing new antimicrobial therapies: Are synergistic combinations of plant extracts/compounds with conventional antibiotics the solution?

Chemical delivery systems for some penicillinase-resistant semisynthetic penicillins

The New Penicillins in Endocarditis

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