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Penicillin antibiotics are time-dependent bactericidal agents. Most of them have very short elimination half-life. As regards their bioavailability, benzylpenicillins are not absorbed following oral administration, while oral ampicillin and cloxacilin are poorly absorbed, and amoxicillin is almost completely absorbed. These drugs are suited for intravenous to oral switch provided that plasma concentrations after oral administration are comparable to those following intravenous application. The assessment is made by calculating the average steady-state plasma concentration. Consequently, the same bactericidal activity can be expected. Oral therapy has many advantages over intravenous administration, including lower treatment costs, shorter hospital stay, lower incidence of phlebitis and sepsis, and greater patient convenience. However, switch therapy is not possible in critically-ill patients, and in patients with fever, increased inflammatory parameters, or malabsorption syndrome. This paper presents two cases of intravenous to oral antibiotic switch therapy. On the basis of pharmacokinetic simulations and evaluation of the efficacy of antibacterial treatment, oral amoxicillin therapy was found to be comparable to intravenous amplicillin treatmentthe suitability of switching intravenous to oral cloxacillin for the treatment of osteomyelitis.Penicilinski antibiotiki delujejo baktericidno in spadajo med časovno odvisne antibiotike. Za večino penicilinov je značilna kratka razpolovna doba eliminacije. Benzilpenicilini se po peroralni aplikaciji ne absorbirajo, ampicilin in kloksacilin se sicer absorbirata, vendar slabo, medtem ko se amoksicilin skoraj v celoti absorbira. Pri slednjem je smotrno z intravenske terapije preklopiti na peroralno, če lahko s peroralno aplikacijo dosežemo plazemske koncentracije penicilina, primerljive s tistimi po intravenski aplikaciji, t. j. enako povprečno plazemsko koncentracijo penicilina v stacionarnem stanju. Posledično lahko pričakujemo enako učinkovitost obeh aplikacij. Smiselnost preklopne terapije je treba proučiti predvsem s stališa bolnika, saj ni primerna za bolnike, ki so v kritičnem stanju in imajo močno zvišano telesno temperaturo ali malabsorbcijski sindrom. Prednost preklopne terapije pa je v tem, da zmanjša pojavnost flebitisa in seps. V članku sta obravnavana dva primera preklopne terapije. Na osnovi farmakokinetičnih simulacij in indeksov učinkovitosti protibakterijskega zdravljenja je pokazana primerljivost intravenske terapije z ampicilinom in peroralne terapije z amoksicilinom, medtem ko preklopna terapija pri zdravljenju osteomielitisa s kloksacilinom ostaja nedorečena. Na podlagi predstavljenih primerov članek ilustrativno prikazuje, da ustrezna razlaga farmakokinetičnih parametrov bistveno pripomore k pravočasnemu preklopu z intravenske na peroralno terapijo s penicilinom. Takšna terapija je bolniku bolj prijazna, poleg tega pa prispeva k zniževanju stroškov za zdravljenje z zdravili v bolnišnicah ob že vedno varni in učinkoviti farmakoterapiji bakterijskih okužb

Pharmacokinetics of penicillin antibiotics: intravenous-to-oral switch therapy