Avtor/Urednik		Golmajer, Andrej; Kozjek, Franc
Naslov		Makrolidi in njihove farmakodinamične lastnosti
Prevedeni naslov		Macrolides and their pharmacodynamic properties
Tip		članek
Vir		Farm Vestn
Vol. in št.		Letnik 51, št. 4
Leto izdaje		2000
Obseg		str. 561-6
Jezik		slo
Abstrakt		Macrolides have proven to be valuable alternatives to penicilines and cephalosporins for the treatment of a number of infections. The mechanism of action of macrolides has been studied for more than 30 years but is still unclear. All macrolides inhibit bacterial protein synthesis by binding to the 50S ribosomal subunit with a specific target in the 23S ribosomal RNA molecule and various ribosomal proteins. The chemical structure of macrolides is characterized by large lactone ring containing between 12 and 16 atoms, to which are attached one or more sugars via glycoside bonds. The most useful classification is that which divides tha macrolides in terms of the size of the lactone ring. When choosing a particular macrolide, the type of microorganisms causing the infection, the tolerability of the drug, convenience of dosing and possible drug interactions all must be taken into account. Some new indications appeared that discriminate semysinthetic macrolided in favour over erythromycin. Clarithromycin and azythromycin are becoming more and more important for the treatment and prophylaxis of Mycobacterium avium complex (MAC) in patients with AIDS. Clarythromycin is themacrolide of choice tor the treatment of ulcer disease caused by Helicobacter pylori, azithromycin is preffered macrolide of choice for the treatment of Chlamydia trachomatis infections. The major factor limiting the use of zyhromycin and clarithromycin has been their cost. However, these drugs may be cost effective in comparison with erythromycin if compliance is improved.
Izvleček		Nekatere neugodne lastnosti eritromicina (nestabilnost v zelodčnem soku, kratka biološka razpolovna doba, manjša absorpcija na prazen želodec) so vodile k odkritju novih makrolidov. Makrolidi se precej razlikujejo po farmakokinetičnih lastnostih, afiniteti do tkiv in intracelularni penetraciji.Novejši polsintetični makrolidi (klaritromicin, azitromicin, roksitromicin, diritromicin) imajo bistveno boljše farmakokinetične lastnosti kot eritromicin. Ker imajo daljšo biološko razpolovno dobo je terapija z njimi krajša. Jemlje se jih le 1-krat ali 2-krat dnevno, kar povečuje sodelovanje pacientov pri terapiji. Zaradi inhibicije citokroma P-450 IIIA4 v jetrih in enterocitih se lahko pri posameznih makrolidih (predvsem eritromicinu) pojavijo interakcije z nekaterimi zdravili, ki so pogosto v uporabi.
Deskriptorji		ANTIBIOTICS, MACROLIDE INFECTION CONTROL CLARITHROMYCIN AZITHROMYCIN