Author/Editor		Golmajer, Andrej; Kozjek, Franc
Title		Farmakokinetične lastnosti makrolidov
Translated title		Pharmacokinetic properties of macrolides
Type		članek
Source		Farm Vestn
Vol. and No.		Letnik 51, št. 4
Publication year		2000
Volume		str. 567-73
Language		slo
Abstract		In the recent years new macrolides have been developed to try overcome the problems (unstability in gastric fluid, short elimination half-life, reduced absorption when given with meals) associated with erythromycin. Macrolides show marked variation in their pharmacokinetic parameters, tissue affinity and intracellular penetration. Newer semisynthetic macrolides (clarythromycin, azithromycin, roxithromycin, dirithromycin) exhibit better pharmacokinetic properties than erythromycin. Because they have longer elimination half-life the therapy is shorte. They only need to be taken once or twice a day, which is likely to improve patient compliance. Macrolides (erytromicin, above all) can interact adversly with commonly used drugs, ussualy by inhibition of cytochrome P-450 IIA4 in the liver and enterocytes.
Summary		Nekatere neugodne lastnosti eritromicina (nestabilnost v zelod nem soku, kratka biolo ka razpolovna doba, manj a absorpcija na prazen elodec) 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.
Descriptors		ANTIBIOTICS, MACROLIDE CLARITHROMYCIN AZITHROMYCIN ERYTHROMYCIN DRUG INTERACTIONS