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Penicillins<br />

■■<br />

Introduction to Penicillins<br />

Penicillins are one of the largest and oldest classes<br />

of antimicrobial agents. Since the development<br />

of the natural penicillins in the 1930s, further<br />

penicillin development has been directed by the<br />

need to combat increasing antimicrobial resistance.<br />

Classes of penicillins with expanded Gramnegative<br />

spectra overcome the shortfalls of natural<br />

penicillins, and they can be grouped fairly easily by<br />

spectrum of activity.<br />

Penicillins have several things in common:<br />

• Penicillins have very short half-lives (< 2 hours)<br />

and must be dosed multiple times per day. The<br />

half-lives of most of them are prolonged in the<br />

presence of renal dysfunction.<br />

• Like other beta-lactams, penicillins can cause<br />

hypersensitivity reactions. If a patient has a<br />

true hypersensitivity reaction to a penicillin,<br />

other penicillins should be avoided, even if they<br />

are from different subclasses of penicillins. If<br />

the reaction is not severe, cephalosporins or<br />

carbapenems may be useful.<br />

• Many penicillins are relatively poorly absorbed,<br />

even those available as oral formulations.<br />

This can lead to diarrhea when oral therapy<br />

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