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Mechanism of Action of Tricyclic Antidepressants (TCAs)

TCA mechanism – serotonin and norepinephrine reuptake inhibition with receptor blockade

Introduction Tricyclic antidepressants (TCAs) are one of the oldest classes of antidepressant medications. Although largely replaced by SSRIs due to their improved safety profiles, TCAs are still widely used for treatment-resistant depression, neuropathic pain, and other off-label conditions. They work by inhibiting the reuptake of norepinephrine and serotonin, thereby increasing the levels of these neurotransmitters … Read more

Mechanism of Action of SSRIs (Selective Serotonin Reuptake Inhibitors)

SSRIs mechanism – serotonin reuptake inhibition in synaptic cleft

Mechanism of Action of SSRIs (Selective Serotonin Reuptake Inhibitors) Introduction Selective Serotonin Reuptake Inhibitors (SSRIs) are first-line antidepressants commonly used in the treatment of major depressive disorder, generalized anxiety disorder, panic disorder, and other psychiatric conditions. They act by increasing the availability of serotonin (5-HT) in the synaptic cleft and are preferred for their favorable … Read more

Mechanism of Action of SGLT2 Inhibitors

SGLT2 inhibitors mechanism – increased glucose excretion via renal tubules

Introduction SGLT2 Inhibitors, or sodium-glucose co-transporter 2 inhibitors, are a newer class of oral antidiabetic drugs that reduce blood glucose levels by promoting urinary glucose excretion. Unlike insulin-dependent drugs, they work via the kidneys and help in both glycemic control and weight reduction. Commonly used SGLT2 inhibitors include: These drugs are now also used for … Read more

Mechanism of Action of DPP-4 Inhibitors

DPP-4 inhibitors mechanism – incretin hormone enhancement via enzyme blockade

Introduction Dipeptidyl Peptidase-4 (DPP-4) Inhibitors, commonly referred to as gliptins, are oral antidiabetic drugs that enhance the action of incretin hormones, especially GLP-1 (glucagon-like peptide-1) and GIP (glucose-dependent insulinotropic peptide). They help regulate postprandial and fasting blood glucose levels in patients with type 2 diabetes mellitus. Commonly used DPP-4 inhibitors include: These agents are known … Read more

Mechanism of Action of Thiazolidinediones

TZD mechanism – PPAR gamma activation and insulin sensitivity improvement

Introduction Thiazolidinediones (TZDs), also known as glitazones, are oral antidiabetic drugs used to improve insulin sensitivity in patients with type 2 diabetes mellitus. Unlike insulin secretagogues, TZDs do not stimulate insulin release—they enhance the body’s response to insulin. Common examples include: They act by binding to PPAR-γ (peroxisome proliferator-activated receptor gamma) and modulating gene transcription, … Read more

Mechanism of Action of Meglitinides

Meglitinides mechanism – insulin secretion by SUR1-mediated KATP channel blockade

Introduction Meglitinides, also known as glinides, are short-acting insulin secretagogues used in the treatment of type 2 diabetes mellitus. They function similarly to sulfonylureas but have a more rapid onset and shorter duration of action, making them ideal for postprandial glucose control. Common meglitinides include: These drugs are especially useful for meal-time glucose spikes and … Read more

Mechanism of Action of Sulfonylureas

Sulfonylureas mechanism – insulin secretion via KATP channel inhibition

Introduction Sulfonylureas are one of the oldest and most widely used classes of oral antidiabetic agents. They are particularly effective in patients with type 2 diabetes mellitus who have residual pancreatic beta-cell function. They exert their effect by stimulating insulin secretion from pancreatic beta cells. Sulfonylureas are typically used in combination with other agents or … Read more

Mechanism of Action of Potassium-Sparing Diuretics

Potassium-sparing diuretics mechanism – aldosterone antagonism and ENaC blockade

Introduction Potassium-sparing diuretics are a unique subclass of diuretics that help conserve potassium levels while promoting mild diuresis. Unlike other diuretics, they do not cause hypokalemia, making them ideal as adjunct therapy with thiazide or loop diuretics. These drugs are grouped into two types: These drugs are tested frequently in USMLE, NCLEX, GPAT, NAPLEX, and … Read more

Mechanism of Action of Thiazide Diuretics

Thiazide diuretics mechanism – inhibition of sodium chloride symporter in the distal tubule

Introduction Thiazide diuretics are one of the most commonly prescribed classes of antihypertensive agents, especially in the U.S. They are highly effective in treating mild to moderate hypertension and are also useful in managing edema, calcium kidney stones, and heart failure. Examples include: Thiazides are recommended as first-line therapy for hypertension in JNC-8 and AHA/ACC … Read more

Mechanism of Action of Calcium Channel Blockers (CCBs)

Calcium channel blockers mechanism – L-type calcium channel inhibition and vasodilation

Introduction Calcium Channel Blockers (CCBs) are a major class of antihypertensive and anti-anginal medications. They work by blocking voltage-gated L-type calcium channels, leading to relaxation of smooth muscle in blood vessels and the heart. CCBs are divided into two major subtypes: They are widely prescribed in the U.S. and feature prominently in USMLE, NCLEX, NAPLEX, … Read more

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