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Chemical
nameBenzeneacetic 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,
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, 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 dyscrasis,
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, induced by aspirin or other
NSAIDs, history of (possibility of cross - sensitivity); Anemia; Asthma;
Hypertension; Edema; Inftammatory 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
In 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
1 - Enteric coated tablets: Usual adult
dose: Rheumatoid arthritis - Oral, 150 to 200 mg per day in 3 or 4
divided doses, initially. Afther a satisfactory response has been
obtained, dosage should be reduced to the minimum dose that provides
continuing control of symptoms, usually 75 to 100 mg a day in 3 divided
doses. Osteoarthritis - Oral, 100 to 150 mg per day in 2 or 3 divided
doses, initially. After a satisfactory response has been obtained, dosage
should be reduced to the minimum dose that provides continuing control of
symptoms. Ankylosing spondylitis - Oral, 100 to 125 mg a day in 4 or 5
divided doses, initially. After a satisfactory response has been obtained,
dosage should be reduced to the minimum dose that provides continuing
control of symptoms. Usual adult prescribing limits: Rheumatoid
arthritis - 225 mg per day. Osteoarthritis - 150 mg per day; higher
doses have not been studied. Usual pediatric dose - Safety and efficacy
have not been established. 2 - Suppositories: Usual
adult dose: Antirheumatic (nonsteroidal anti - inflammatory) - Rectal, 50
or 100 mg, as a substitute for the last oral dose of the day. Usual
adult prescribing limits: Total daily dosage (oral and rectal) should
not exceed 150 mg. Usual pediatric dose: Safety and efficacy have
not been established.
How
suppliedBox of 5
suppositories. Each suppository contains 50 mg diclofenac sodium.
StorageStore below 30° C, protect from light and
moisture. Suppositories: Store in cold place.
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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