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Antibiotics

Penicillins
Mechanism of action
Structurally, penicillins are -lactam antibiotics. Bacterial cell walls are consisting of a protective peptidoglycan layer, which is continuously undergoing remodeling. The remodelling process involves the breaking of the -(1,4) linked N-acetylmuramic acid and N-acetylglucosamine; as well as the breaking of the cross-linking peptide chains. This cross-linking peptide chains is what provides the rigidity, to the otherwise fluid cell wall. The breaking of this peptide cross-linking is performed by an enzyme called transpeptidase. The transpeptidase also helps in reforming the peptide bonds once the restructuring of the cell wall is done. The penicillins act by inhibiting this particular enzyme. By inhibiting this enzyme the penicillin prevents the reformation of the peptide bonds and thus makes the cell wall less strong. This loss of cell wall integrity causes the bacteria to leak out its cellular contents and perish. This beta-lactam ring of the penicillin is generally not very stable and therefore it participates in the inactivation of bacterial cell enzymes which are essential for synthesis of peptidoglycan. Transpeptidase attacks the beta-lactam ring which opens up to give a more stable compound. When this happens the drug remains bound to the transpeptidase via covalent linkage and thereby inhibits the enzyme by acylation of the active site. The resistance to penicillin arises due to mutations in the active site of the transpeptidase enzyme. Thus there are many variants of the transpeptidase enzyme which need the use of newer penicillin antibiotics.

Side effect

diarrhea that is watery or bloody; urinating less than usual or not at all; fever, swollen glands, sore throat, rash or itching, joint pain, general ill feeling; skin rash, bruising, severe tingling, numbness, pain, muscle weakness; pale or yellowed skin, dark colored urine, fever, confusion or weakness; or easy bruising, unusual bleeding (nose, mouth, vagina, or rectum), purple or red pinpoint spots under your skin.

Indication
Infections caused by Streptococcus pyogenes Tonsillitis Pharyngitis Skin infections Prophylaxis of rheumatic fever Moderate-to-severe gingivitis (with metronidazole) Penicillin V is the first choice in the treatment of odontogenic infections.

Contraindication

Cephalosporins
Mechanism of action
Cephalosporins are bactericidal and have the same mode of action as other beta-lactam antibiotics (such as penicillins) but are less susceptible topenicillinases. Cephalosporins disrupt the synthesis of the peptidoglycan layer of bacterial cell walls Cephalosporins have the same mode o action as the penicillins, but they are more resistant than the penicillins to -lactamases.

Side Effects
Allergic manifestations. Intolerance to ingested ethanol, because cephalosporins block the alcohol oxidation, which results in the accumulation of acetaldehyde.

Bleeding, because of anti-vitamin K effects.

Indication

Contraindication

Carbapenems

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