Lipopeptides and Lipoglycopeptides
Chemistry and Pharmacodynamics Lipopeptides Daptomycin: only member of its class Structure: 13 amino acids, with 10 forming an ester-linked amino acid ring With a terminal L-tryptophan bonded to decanoic acid Mechanism of action of lipopeptides Bactericidal (concentration-dependent killing): Lipophilic tail binds to bacterial membranes (calcium-dependent) → creates a hole or channel in the membrane, causing […]
Cephalosporins
Chemistry Cephalosporin structure Cephalosporins are members of the beta-lactam drug family and consist of: A beta-lactam ring: a 4-membered ring containing 2 carbons (α and β carbons), a nitrogen, and a carbonyl group (a carbon double-bonded to oxygen) The group in the compound responsible for antibacterial activity Can be hydrolyzed (i.e., broken down) by beta-lactamases, […]
Penicillins
Chemistry Penicillins are members of the beta-lactam family of drugs and consist of: A beta-lactam ring: a 4-membered ring containing 2 carbons (α and β carbons), a nitrogen, and a carbonyl group (a carbon double-bonded to oxygen) The beta-lactam group in the compound is responsible for antibacterial activity. Can be hydrolyzed (i.e., broken down) by […]
Antispasmodics
Overview Definition Antispasmodics are a group of medications used to reduce excessive GI smooth muscle contractility and spasm. Classification Antispasmodic agents are classified based on their action: Indications This group of medications is used in individuals with abdominal discomfort from bowel spasm, such as that due to irritable bowel syndrome (IBS). Anticholinergics Mechanism of action […]
Nonsteroidal Antiinflammatory Drugs (NSAIDs)
Pharmacodynamics Mechanism of action Nonsteroidal antiinflammatory drugs (NSAIDs) exert their therapeutic effects by interrupting fatty acid metabolism, primarily the action of cyclooxygenase (COX) on arachidonic acid (AA). Pharmacokinetics NSAIDs are generally very similar: Classification NSAIDs can be divided into groups based on their ability to inhibit the isoforms of cyclooxygenase (COX-1 and COX-2). Indications Adverse […]
Chloramphenicol
Pharmacodynamics and Pharmacokinetics Chemical structure Mechanism of action Pharmacokinetics Indications Antimicrobial coverage Types of infections Because of chloramphenicol’s side effects, use is generally limited to severe infections where resistance has developed against alternative agents: Adverse Effects and Contraindications Adverse effects Contraindications Drug interactions Mechanisms of Resistance Resistance mechanisms to chloramphenicol in bacteria include: Comparison of […]
Lincosamides
Chemistry and Pharmacodynamics Chemical structure Mechanism of action Pharmacokinetics Since lincomycin is rarely used, the pharmacokinetics of clindamycin are have been listed: Absorption and distribution Metabolism and excretion Indications Antimicrobial coverage Type of infections Adverse Effects and Contraindications Adverse effects Contraindications Drug interactions Mechanisms of Resistance There are 3 main routes of resistance: Comparison of […]
Aminoglycosides
Chemistry and Pharmacodynamics Chemical structure Contains a hexose-ring nucleus Glycosidic linkages to various amino sugars Gentamicin is the prototypical drug. Mechanism of action Aminoglycosides bind to the bacterial 30S ribosomal subunit. Disruption of bacterial protein synthesis by: Prevention of initiation complex formation Misreading of mRNA → production of faulty protein → damage to the cell […]
Oxazolidinones
Chemistry and Pharmacodynamics Chemical structure Mechanism of action Pharmacokinetics Absorption and distribution Metabolism Excretion Indications Antimicrobial coverage Types of infections These medications are FDA-approved for: Adverse Effects Adverse effects Warnings Linezolid may cause a hypertensive crisis in the following conditions: Drug interactions Comparison of Antibiotics Table: Comparison of several classes of bacterial protein synthesis inhibitor […]
Macrolides and Ketolides
Chemistry and Pharmacodynamics Chemical structure Macrolides: characterized by a macrocyclic lactone ring Ring contains 14‒16 atoms 1 or more sugars are attached via glycosidic bonds Erythromycin is the prototype drug of the class. Ketolides (e.g., telithromycin): similar structure to macrolides 14-atom ring 1 of the sugars is substituted with a keto group Derived from erythromycin […]