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Chemical
nameBenzenearetic acid, 2 -
[(2, 6 - dichlorophenyl) amino] - , monosodium salt.
CategoryAntirheumatic; Analgesic; Antigout agent;
Antidysmenorrheal; Vascular headache suppressant.
Mechanism of
action
Diclofenac inhibits the activity of the enzyme cyclo -
oxygenase, resulting in decreased formation of precursors of
prostaglandins and thromboxanes from arachidonic acid. Diclofenac may
block pain impulse generation via a peripheral action that may involve
reduction of the activity of prostaglandins, and possibly inhibition of
the synthesis or actions of other substances that sensitize pain receptors
to mechanical or chemical stimulation.
Indications
Indicated for rheumatoid arthritis, osteoarthritis, and
ankylosing spondylitis. Immediate - release tablets only indicated for
pain and primary dysmenorrhea, and may also be used to relieve acute
attacks of gout or calcium pyrophosphate deposition disease (pseudogout)
and pain associated with nonrheumatic inflammatory conditions or vascular
headaches.
Precautions to
consider
This medication should not be used when the following
medical problems exist: Allergic reaction, severe, such as anaphylaxis or
angioedema, that induced by aspirin or other NSAIDs, history of; Nasal
polyps associated with bronchospasm, aspirin-induced (high risk of severe
allergic reactions because of cross - sensitivity); Blood dyscrasias,
active or history of; Bone marrow depression (diclofenac may induce or
exacerbate these conditions). Risk benefit should be considered when the
following medical problems exist: Allergic reaction, mild, such as
allergic rhinitis, urticaria, or skin rash, indured by aspirin or other
NSAIDs, history of (possibility of cross - sensitivity); Anemia; Asthma;
Hypertension; Edema; Inflammatory or ulcerative disease of the upper or
lower gastrointestinal tract; Diabetes mellitus; Hemophilia or other
bleeding problems; Hepatic or renal function impairment; Stomatitis;
Systemic lupus erythematosus; Porphyria, hepatic (diclofenac may
precipitate an acute attack).
Pregnancy
Embryotoxicity and other adverse effects, but not
teratogenicity, demonstrated in animal studies. FDA Pregnancy Category
B.
Breast -
feeding
Diclofenac is distributed into breast milk.
Drug
interactions
ln addition to the interactions listed below, the
possibility should be considered that additive or multiple effects leading
to impaired blood clotting and / or increased risk of bleeding may occur
if any NSAID is used concurrently with any medication having a significant
potential for causing hypoprothrombinemia, thrombocytopenia, or
gastrointestinal ulceration or hemorrhage. Acetaminophen, Alcohol,
Potassium supplements, Anticoagulants, Heparin, Thrombolytic agents,
Potassium-sparing diuretics, Lithium, Probenecid, Salicylates, Digoxin,
Antidiabetic agents or insulin, Corticosteroids, Cyclosporine, Valproic
acid.
Side / Adverse
effects
Hypersensitivity reactions such as: Rhinosinusitis /
asthma or angioedema / urticaria; Anaphylaxis. Gastrointestinal
problems; Dermatologic effects; Headache; Renal and hepatic function
impairment; Hearing problems; CNS effects; Hyperkalemia; Edema.
Administration and
dosage
Retard tablets: Usual adult dose: Antirheumatic
(nonsteroidal anti-inflammatory)-Oral, 1 Diclofenac retard (100 mg) tablet
once a day, in the moming or evening. Note: The retard dosage
form is not intended as initial therapy; the daily maintenance dose should
be determined using an immediate -or delayed -release formulation. The
retard dosage form may then be used, if desired, provided that the
required dose can be achieved with the available strengths. Usual
pediatric dose: Safety and efficacy have not been established.
How
suppliedTablets: Box of 100
enteric coated tablets. Each coated slow - release tablet contains 100
mg diclofenac sodium.
StorageStore below 30° C, protect from light and
moisture.
References1 - USP DI Vol: 1 (1997) pages:
379-395. 2 - Drug facts and comparisons (1994). 3 - USP 23 - Sixth
supplement / Page: 3670.
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