Factors Affecting Drug Metabolism: It is influenced by biological, chemical, and stereochemical factors, affecting drug efficacy, clearance, and potential toxicity. Biological and Chemical Factors Affecting Drug Metabolism Genetic Polymorphisms Enzyme Variability: Differences in genes encoding drug-metabolizing enzymes (e.g., CYP450) lead to variations in metabolic rates. Metabolizer Phenotypes: Individuals can be poor, intermediate, extensive, or ultra-rapid … Read more

Drug Metabolism Principles Definition  Drug Metabolism Principles: Drug metabolism is the biochemical modification of pharmaceutical substances in the body, primarily carried out by liver enzymes. It occurs in two main phases: Phase I Metabolism Overview: Phase I reactions modify drug molecules via oxidation, reduction, or hydrolysis, often introducing or exposing functional groups (-OH, -NH₂, -SH). Common … Read more

Drug metabolism is the chemical transformation of pharmaceuticals, primarily in the liver, converting lipophilic compounds into water-soluble metabolites for easier excretion. Key Goals of Drug Metabolism Detoxification: Converts toxic compounds into less harmful forms. Excretion: Enhances drug elimination via urine or bile. Regulation of Drug Activity: Activates prodrugs or inactivates drugs, influencing their effect. Enzymatic … Read more

Optical and Geometrical Definition  Optical and Geometrical Isomerism: Stereoisomerism is a form of isomerism in which compounds have the same molecular formula and sequence of bonded atoms (constitution) but differ in the spatial arrangement of atoms or groups. It includes geometrical isomerism, which arises from restricted rotation around double bonds or ring structures leading to … Read more

Bioisosterism Definition: Bioisosterism are structurally similar chemical groups that mimic the biological activity of another. Importance in Drug Design: Improved Activity: Replacement of groups can enhance potency and reduce toxicity. Increased Stability: Bioisosteres improve metabolic stability. Reduced Side Effects: Modification helps improve drug safety. Examples: Sulfonamide (-SO₂NH₂) as a bioisostere of carboxyl (-COOH) in diuretics. Fluorine … Read more

Chelation Definition: Chelation is the formation of complexes between drugs and metal ions (e.g., Ca²⁺, Fe³⁺, Mg²⁺). Importance in Drug Action: Drug Absorption: Chelating with dietary minerals reduces absorption (e.g., tetracyclines + calcium). Toxicity Management: Chelating agents are used to remove heavy metals (e.g., lead, arsenic). Stability: It can enhance or reduce drug stability in … Read more

Protein Binding Definition: Protein Binding: Drugs bind to plasma proteins (e.g., albumin, globulins) in the bloodstream, affecting their distribution and activity. Importance in Drug Action: Free vs. Bound Drug: Only free drug is active; bound drug serves as a reservoir. Drug-Drug Interactions: Competition for binding sites can increase free drug concentration and toxicity. Duration of … Read more

Hydrogen Bonding Definition: Hydrogen bonding occurs when hydrogen (H) atoms interact with electronegative atoms (O, N, F). This contributes to a drug’s solubility and receptor binding. Importance in Drug Action: Water Solubility: More hydrogen bonds = better water solubility. Receptor Binding: Hydrogen bonds enhance drug-receptor interactions (enzyme active sites, DNA intercalation). Stability: Hydrogen bonds stabilize … Read more