Pharmacodynamics topics. What is affinity?

The following pharmacological definition has been taken from the Pharmacology and Experimental Therapeutics Department Glossary at Boston University School of Medicine. Affinity: The equilibrium constant of the reversible reaction of a drug with a receptor to form a drug-receptor complex; the reciprocal of the dissociation constant of a drug-receptor complex. Under the most general conditions, […]

Glucagon-like peptide-1 agonists (exenatide): consensus statement published on Diabetes Care

Below is a transcript of the latest statement (December 2008) published on Diabetes Care, about the role of Glucagon-like peptide-1 agonists (exenatide) in the medical management of hyperglycemia in type 2 diabetes. Glucagon-like peptide-1 agonists (exenatide). Glucagon-like peptide-1 (GLP-1) 7–37, a naturally occurring peptide produced by the L-cells of the small intestine, potentiates glucose-stimulated insulin […]

DPP-4 inhibitors: consensus statement published on Diabetes Care. Diagram of its mechanism of action.

Below is a transcript of the latest statement (December 2008) published on Diabetes Care about the role of dipeptidyl peptidase four inhibitors in the medical management of hyperglycemia in type 2 diabetes. Dipeptidyl peptidase four inhibitors. GLP-1 and glucose-dependent insulinotropic peptide (GIP), the main insulinotropic peptides of intestinal origin (incretins), are rapidly degraded by dipeptidyl peptidase four (DPP-4). […]

Sulfonylureas: consensus statement published on Diabetes Care

Below is a transcript of the latest statement (December 2008) published on Diabetes Care about the role of sulfonylureas in the medical management of hyperglycemia in type 2 diabetes. Sulfonylureas. Sulfonylureas lower glycemia by enhancing insulin secretion (see mechanism of action). In terms of efficacy,  they appear to be similar to metformin, lowering A1C levels by 1.5 percentage points (26,49). […]

Sildenafil still a drug subject to medical prescription

Pfizer withdraws its application to change the marketing authorisation for Viagra 50 mg (sildenafil) from prescription-only to non-prescription The European Medicines Agency (EMEA) has been formally notified by Pfizer Limited of its decision to withdraw its application for a change to the marketing authorisation for the medicine Viagra (sildenafil) 50 mg film-coated tablets. The change concerned switching […]

Varenicline psychiatric side effects: recommendations from the MHRA

The Medicines and Healthcare products Regulatory Agency has issued recommendations about the use of varenicline (Champix) as a smoking cessation drug. Advice for healthcare professionals: • Patients and their family or care-givers should be made aware of the possibility that trying to stop smoking might cause symptoms of depression • Patients who are taking varenicline […]

Rufinamide approved as adjunctive for Lennox Gastaut syndrome

The U.S. Food and Drug Administration has approved a new drug, Banzel (rufinamide), for use as an adjunctive (add-on) treatment for seizures associated with Lennox-Gastaut syndrome. “This approval offers another treatment option for patients who suffer from these debilitating, severe seizures,” said Russell Katz, M.D., director of the Division of Neurology Products in the FDA’s […]

Statins: mechanism of action and side effects

An overview on the mechanism of action of statins: HMG CoA reductase inhibitors,or statins are widely prescribed drugs. They are indicated for the treatment of hipercholesterolemia, a condition that increases cardiovascular risk. Currently, the drugs of this group that are available are: Atorvastatin Fluvastatin Lovastatin Mevastatin Pitavastatin Pravastatin Rosuvastatin Simvastatin Mechanism of action. Animation explained […]

Imatinib (Gleevec) pharmacology: mechanism of action and therapeutic considerations

Imatinib mesylate is a small-molecule tyrosine kinase inhibitor that was initially developed as a 2-phenylaminopyrimidine derivative specific for PDGFR. Imatinib was subsequently found to be a potent inhibitor of ABL kinases, including the BCR-ABL fusion protein generated as a result of the t(9;22) chromosomal translocation (Philadelphia chromosome) found in chronic myelogenous leukemia (CML), and was […]

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