Naproxen metabolism in man. 1975

E J Segre

In summary, naproxen is an acidic, highly albumin-bound drug. After oral administration, it is promptly and fully absorbed. The mean half-life of the drug in man is 13 hours, close to ideal for twice-daily administration. The only metabolite detected in man is the 6-desmethyl compound. Both it and naproxen itself are excreted in the urine, primarily as conjugates. The kinetics of naproxen binding to serum albumin tend to limit attainable plasma levels. They increase little if the dose is increased beyond 500 mg twice daily, since greater concentrations are rapidly cleared. Albumin binding and competitive displacement are also responsible for potential interactions of naproxen with drugs such as warfarin, sulfonylureas, and aspirin. Experience thus far does not indicate that any of the potential interactions are clinically meaningful.

UI MeSH Term Description Entries
D007408 Intestinal Absorption Uptake of substances through the lining of the INTESTINES. Absorption, Intestinal
D009280 Naphthaleneacetic Acids Naphthalene derivatives containing the -CH2CCO2H radical at the 1-position, the 2-position, or both. Compounds are used as plant growth regulators to delay sprouting, exert weed control, thin fruit, etc. Acids, Naphthaleneacetic
D009288 Naproxen An anti-inflammatory agent with analgesic and antipyretic properties. Both the acid and its sodium salt are used in the treatment of rheumatoid arthritis and other rheumatic or musculoskeletal disorders, dysmenorrhea, and acute gout. Aleve,Anaprox,Methoxypropiocin,Naprosin,Naprosyn,Naproxen Sodium,Proxen,Sodium Naproxenate,Synflex,Naproxenate, Sodium,Sodium, Naproxen
D004347 Drug Interactions The action of a drug that may affect the activity, metabolism, or toxicity of another drug. Drug Interaction,Interaction, Drug,Interactions, Drug
D004359 Drug Therapy, Combination Therapy with two or more separate preparations given for a combined effect. Combination Chemotherapy,Polychemotherapy,Chemotherapy, Combination,Combination Drug Therapy,Drug Polytherapy,Therapy, Combination Drug,Chemotherapies, Combination,Combination Chemotherapies,Combination Drug Therapies,Drug Polytherapies,Drug Therapies, Combination,Polychemotherapies,Polytherapies, Drug,Polytherapy, Drug,Therapies, Combination Drug
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000893 Anti-Inflammatory Agents Substances that reduce or suppress INFLAMMATION. Anti-Inflammatory Agent,Antiinflammatory Agent,Agents, Anti-Inflammatory,Agents, Antiinflammatory,Anti-Inflammatories,Antiinflammatories,Antiinflammatory Agents,Agent, Anti-Inflammatory,Agent, Antiinflammatory,Agents, Anti Inflammatory,Anti Inflammatories,Anti Inflammatory Agent,Anti Inflammatory Agents
D001682 Biological Availability The extent to which the active ingredient of a drug dosage form becomes available at the site of drug action or in a biological medium believed to reflect accessibility to a site of action. Availability Equivalency,Bioavailability,Physiologic Availability,Availability, Biologic,Availability, Biological,Availability, Physiologic,Biologic Availability,Availabilities, Biologic,Availabilities, Biological,Availabilities, Physiologic,Availability Equivalencies,Bioavailabilities,Biologic Availabilities,Biological Availabilities,Equivalencies, Availability,Equivalency, Availability,Physiologic Availabilities
D001692 Biological Transport The movement of materials (including biochemical substances and drugs) through a biological system at the cellular level. The transport can be across cell membranes and epithelial layers. It also can occur within intracellular compartments and extracellular compartments. Transport, Biological,Biologic Transport,Transport, Biologic
D013997 Time Factors Elements of limited time intervals, contributing to particular results or situations. Time Series,Factor, Time,Time Factor

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