Calcimimetics
Pharmacodynamics Medications in the class Mechanism of action Physiologic effects Calcimimetics prevent the progression of bone disease and adverse effects associated with hyperparathyroidism. Pharmacokinetics Absorption Distribution and metabolism Excretion Indications Adverse Effects and Contraindications Adverse effects Important adverse effects for the calcimimetic class include: Contraindications Drug interactions Monitoring Calcium levels should be monitored. Comparison of […]
Renin-Angiotensin-Aldosterone System Inhibitors
Overview Definition Renin-angiotensin-aldosterone system inhibitors constitute an important class of medications for the treatment of cardiovascular diseases, and are 1st-line agents for the treatment of hypertension. Review of the RAAS Drugs in the RAAS inhibitor class Drugs in the RAAS inhibitor class include: Overview of antihypertensive agents Table: Drugs used to treat hypertension Location of […]
Tetracyclines
Chemistry and Pharmacodynamics Chemical structure Contain a linear, fused 4-ring nucleus Have a variety of attached functional groups Mechanism of action Tetracyclines bind reversibly to the 30S ribosomal subunit: Block the attachment of aminoacyl-tRNA to the mRNA–ribosome complex Disrupt bacterial protein synthesis Bacteriostatic (inhibit but do not kill organisms) Demeclocycline is an antidiuretic hormone (ADH) […]
Benzodiazepines
Chemistry and Pharmacodynamics Chemical structure Mechanism of action Physiologic effects GABA: GABA receptors: Benzodiazepine therapeutic effects: Pharmacokinetics Absorption Lipophilic benzodiazepines have a more rapid absorption. Distribution Metabolism Excretion Elimination occurs through the kidney (glucuronides are excreted in the urine). Pharmacokinetics comparison table The table below highlights important benzodiazepine medications and addresses the properties of each. […]
Antiprogestins and Selective Progesterone Modulators
Overview Definition Antiprogestins are competitive inhibitors of progestins at the progesterone receptors (PRs). Selective progesterone receptor modulators (SPRMs) can act as either agonists or antagonists depending on the tissue type/cellular environment. Classification Antiprogestins: mifepristone Selective progesterone receptor modulators (SPRMs): ulipristal General indications Pregnancy termination: mifepristone Emergency contraception: ulipristal Common side effects Nausea Vomiting Abdominal pain […]
Triptans and Ergot Alkaloids
Overview Pathophysiology of migraine The pathophysiology of migraines is not completely understood. Involves: The trigeminovascular system: Neurons originate from trigeminal ganglion Innervate cerebral, pial, and dura vessels Vasoactive neuropeptide release Vasodilation Plasma protein extravasation Serotonin plays a role through 5-hydroxytryptamine (5-HT) 1B and 1D receptors in: Trigeminal neurons Cerebral and meningeal vessels The role of […]
Nitrates
Chemistry and Pharmacodynamics Chemistry Mechanism of action Exogenously administered nitrates are converted to NO after entering the cell: Physiologic effects Pharmacokinetics Absorption Distribution Metabolism Excretion Indications Table: Comparison of nitrates Medications Common formulations Indications Clinical pearls Nitroglycerin Sublingual Oral Transdermal IV Angina Acute MI (unless a right ventricular or inferior infarct) Heart failure Variant angina […]
Potassium-sparing Diuretics
Overview Definition Potassium-sparing diuretics are medications that act in the principal cells in the collecting ducts (CDs) to induce diuresis that does not result in excretion of potassium. Overview of antihypertensive agents Table: Drugs used to treat hypertension Location of action Class Subclasses Renal drugs Drugs affecting the RAAS ACEis ARBs Direct renin inhibitors Diuretics […]
Loop Diuretics
Overview Definition Loop diuretics are a group of medications primarily used to treat edema (and sometimes hypertension) by inhibiting sodium reabsorption through the NKCC2 cotransporter (as known as the Na+-K+-Cl– cotransporter) in the thick ascending limb of the loop of Henle (TAL), which lead to significant diuresis. Overview of antihypertensive agents Table: Drugs used to […]
Disease-Modifying Antirheumatic Drugs (DMARDs)
Overview of Antirheumatic Drugs Definition Antirheumatic drugs are used to treat rheumatoid arthritis by slowing the progression of the disease. General indications Antirheumatic drugs are given for: Classification Leflunomide Table: Leflunomide Mechanism of action Inhibits dihydroorotate dehydrogenase Interrupts de novo synthesis of pyrimidines Inhibits proliferation of immune cells Physiologic effects Antiinflammatory effect Antiproliferative effect Metabolism […]