Metacyclin Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
Methacycline was synthesized by Pfizer Research Laboratories in 1961 starting with oxytetracycline. It shows two to fivefold greater in vitro antibacterial activity and in vivo protective activity than tetracycline. Methacycline has been given orally to treat infections by Rickettsia, Chlamydiae, Staphyloccus, Streptococcus, Neisseria, Klebsiella, Proteus, Escherichia coli, and Haemophilus influenzae.
Verwenden
Methacycline is a semi-synthetic tetracycline prepared by dehydration of the 6-hydroxy group of oxytetracycline to yield an exocyclic 6-methylene. Like all tetracyclines, methacycline shows broad spectrum antibacterial and antiprotozoan activity and acts by binding to the 30S and 50S ribosomal subunits, blocking protein synthesis. Methacycline has been extensively cited in the literature with over 400 references.
Definition
ChEBI: A tetracycline that is the 6-methylene analogue of oxytetracycline, obtained by formal dehydration at position 6.
Pharmazeutische Anwendungen
6-Methylene-5-hydroxy-tetracycline. A semisynthetic derivative
supplied as the hydrochloride for oral administration.
Mean peak plasma concentrations of 2–6 mg/L are found
about 4 h after a 300 mg oral dose. Both food and milk reduce
uptake by half. Protein binding is 80–90%. The plasma elimination
half-life varies between 7 and 15 h and increases to 44 h
in severe renal impairment. It is widely distributed, producing
lung concentrations similar to, or greater than, the simultaneous
plasma concentration. About one-third is excreted in the urine.
Gastrointestinal intolerance is reported to be less frequent
than with other tetracyclines, largely because of the lower dosages
used. There are no unique adverse drug reactions,
although skin and conjunctival pigmentation have been
reported.
Metacyclin Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
