Clinical pharmacokinetics of diclofenac. Therapeutic insights and pitfalls.

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Davies NM, Anderson KE

Clinical pharmacokinetics of diclofenac. Therapeutic insights and pitfalls.

Clin Pharmacokinet. 1997 Sep;33(3):184-213. doi: 10.2165/00003088-199733030-00003.

PubMed ID

9314611 [ View in PubMed

]

Abstract

Diclofenac is a nonsteroidal anti-inflammatory drug (NSAID) of the phenylacetic acid class. When given orally the absorption of diclofenac is rapid and complete. Diclofenac binds extensively to plasma albumin. The area under the plasma concentration-time curve (AUC) of diclofenac is proportional to the dose for oral doses between 25 to 150 mg. Substantial concentrations of drug are attained in synovial fluid, which is the proposed site of action for NSAIDs. Concentration-effect relationships have been established for total bound, unbound and synovial fluid diclofenac concentrations. Diclofenac is eliminated following biotransformation to glucoroconjugated and sulphate metabolites which are excreted in urine, very little drug is eliminated unchanged. The excretion of conjugates may be related to renal function. Conjugate accumulation occurs in end-stage renal disease; however, no accumulation is apparent upon comparison of young and elderly individuals. Dosage adjustments for the elderly, children or for patients with various disease states (such as hepatic disease or rheumatoid arthritis) may not be required. Significant drug interactions have been demonstrated for aspirin (acetylsalicylic acid), lithium, digoxin, methotrexate, cyclosporin, cholestyramine and colestipol.

DrugBank Data that Cites this Article

Drugs

Diclofenac

Drug Carriers

Drug	Carrier	Kind	Organism	Pharmacological Action	Actions
Diclofenac	Serum albumin	Protein	Humans	Unknown	Not Available	Details

Drug Reactions

Reaction
Diclofenac DB00586 Cytochrome P450 2C9 3'-Hydroxydiclofenac DBMET00146	Details
Diclofenac DB00586 Cytochrome P450 3A4 Cytochrome P450 1A2 Cytochrome P450 2B6 Cytochrome P450 2C8 Cytochrome P450 2C18 Cytochrome P450 2C19 Cytochrome P450 2C9 5-hydroxy diclofenac DBMET02613	Details

Drug Interactions

Drugs	Interaction
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Digoxin Diclofenac	The serum concentration of Digoxin can be increased when it is combined with Diclofenac.