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Route of Administration

Route of Administration. Depot forms. Procaine penicillin G benzathine penicillin G IM and serve as depot forms. They are slowly absorbed into the circulation and persist at low levels over a long time period. Pharmacokineics. Absorption:

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Route of Administration

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  1. Route of Administration

  2. Depot forms • Procaine penicillin G • benzathine penicillin G • IM and serve as depot forms. • They are slowly absorbed into the circulation and persist at low levels over a long time period.

  3. Pharmacokineics • Absorption: • Food decreases the absorption of all the penicillinase-resistant penicillins because as gastric emptying time increases. • The drugs are destroyed by stomach acid should be taken on an empty stomach. • Distribution: • The β-lactam antibiotics distribute well throughout the body. • All the penicillins cross the placental barrier • No teratogenic effects. • Penetration into bone or cerebrospinal fluid (CSF) is insufficient for therapy unless these sites are inflamed. • Penicillin levels in the prostate are insufficient to be effective against infections.

  4. Metabolism: Host metabolism of the β-lactam antibiotics is usually insignificant. • Excretion: The primary route of excretion is through kidney • Patients with impaired renal function must have dosage regimens adjusted. • Probenecid inhibits the secretion of penicillins by competing for active tubular secretion via the organic acid transporter increase blood levels. • The penicillins are also excreted in breast milk.

  5. Adverse reactions • Hypersensitivity: • Approximately 5% percent • Cross-allergic reactions occur among the β-lactam antibiotics. • Patient history

  6. Nephritis: • Acute interstitial nephritis ( Methicillin ) • Neurotoxicity: • Seizures if injected intrathecally • GABAergic inhibition. • Hematologic toxicities: • Decreased coagulation

  7. Cephalosporins • Cephalosporinsare β-lactam antibiotics that are closely related both structurally and functionally to the penicillins. • Most cephalosporinsare produced semisynthetically by the chemical attachment of side chains to 7-aminocephalosporanic acid. • Cephalosporinshave the same mode of action as penicillins, and they are affected by the same resistance mechanisms. • More resistant than the penicillins to certain β-lactamases.

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