Local Anesthetics

Local Anesthetics

Local anesthetics are drugs that block nerve conduction at the site of administration, causing temporary loss of sensation without unconsciousness. Definition: Local anesthetics are medications that temporarily block sensation in a specific area of the body without affecting consciousness. They are commonly used during surgical, dental, and diagnostic procedures to prevent or relieve pain. Mechanism … Read more

SAR of Local anaesthesia

SAR of Local anaesthesia

SAR of Local anaesthesia SAR of Local Anaesthesia shows how lipophilic group, intermediate chain, and amine group influence potency, duration, and activity. Aromatic Group (Lipophilic End): Typically, a benzene ring, responsible for lipophilicity, enabling penetration of nerve cell membranes. Potency is proportional to lipid solubility, influencing membrane penetration. Intermediate Chain (Linker): Connects the aromatic group … Read more

Voglibose

Voglibose is an alpha-glucosidase inhibitor antidiabetic drug that helps control post-meal blood sugar by delaying carbohydrate absorption. Structure of Voglibose It is an iminosugar derivative with a cyclitol backbone, structurally modified to enhance specificity for intestinal alpha-glucosidases. Chemical Formula: C₁₂H₂₀N₂O₈ Mode of Action Alpha-Glucosidase Inhibition: Specifically inhibits intestinal enzymes, delaying carbohydrate digestion. Postprandial Glycemic Control: … Read more

Acarbose

Acarbose is an alpha-glucosidase inhibitor antidiabetic drug that lowers blood sugar by delaying carbohydrate digestion and glucose absorption. Structure of Acarbose It is a pseudotetrasaccharide composed of glucose units linked by alpha-1,4 and alpha-1,6 glycosidic bonds, modified with a valienamine moiety. Chemical Formula: C₁₈H₃₄N₂O₁₄ Mode of Action Alpha-Glucosidase Inhibition: Blocks enzymes responsible for breaking down … Read more

Nateglinide

Nateglinide

Nateglinide is a meglitinide antidiabetic drug used in the treatment of type 2 diabetes mellitus. It lowers blood sugar by stimulating rapid insulin release from the pancreas, making it particularly effective in controlling post-meal glucose levels. With its fast onset and short duration of action, Nateglinide helps improve glycemic control while reducing the risk of … Read more

Repaglinide

Repaglinide

Repaglinide is a meglitinide antidiabetic drug commonly used in the management of type 2 diabetes mellitus. It lowers blood sugar by stimulating quick and short-acting insulin release from the pancreas, particularly effective in controlling postprandial (after-meal) glucose spikes. With its rapid onset and short duration of action, Repaglinide offers flexibility in dosing and is especially … Read more

Rosiglitazone

Rosiglitazone is a thiazolidinedione antidiabetic drug that enhances insulin sensitivity to help manage blood sugar in type 2 diabetes. Structure of Rosiglitazone It is a TZD with a similar core structure to pioglitazone but contains a different aromatic substituent, enhancing its potency. Chemical Formula: C₁₉H₂₅N₃O₃S Mode of Action PPAR-γ Agonism: Increases insulin sensitivity in peripheral … Read more

Pioglitazone

Pioglitazone

Pioglitazone is a thiazolidinedione antidiabetic drug that improves insulin sensitivity and controls blood sugar in type 2 diabetes. Structure of Pioglitazone Pioglitazone is a TZD with a thiazolidinedione ring substituted with a pyridine moiety, enhancing its binding affinity to PPAR-γ. Chemical Formula: C₁₄H₁₈N₂O₂S Mode of Action PPAR-γ Agonism: Enhances insulin sensitivity by modulating gene expression … Read more

Metformin

Metformin

Metformin is a biguanide antidiabetic drug that lowers blood sugar by reducing hepatic glucose production and improving insulin sensitivity. Structure of Metformin Metformin is a biguanide derivative with two guanidine groups attached to a dimethylamine backbone. Chemical Formula: C₄H₁₁N₅ Mode of Action AMP-Activated Protein Kinase (AMPK) Activation: Enhances insulin sensitivity and reduces hepatic gluconeogenesis. Intestinal … Read more

Glimepiride

Glimepiride

Glimepiride is a third-generation sulfonylurea antidiabetic drug widely used in type 2 diabetes treatment. It lowers blood sugar by stimulating pancreatic insulin secretion and is considered more effective and safer than earlier sulfonylureas, offering better glycemic control with a lower risk of side effects. Structure of Glimepiride Glimepiride is a third-generation sulfonylurea with a triazole … Read more

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