Source:http://www4.wiwiss.fu-berlin.de/dailymed/resource/drugs/2455
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Diclofenac Potassium (Tablet)
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Carefully consider the potential benefits and risks of diclofenac potassium tablets and other treatment options before deciding to use diclofenac potassium tablets. Use the lowest effective dose for the shortest duration consistent with individual patient treatment goals . After observing the response to initial therapy with diclofenac potassium tablets, the dose and frequency should be adjusted to suit an individual patient's needs. For treatment of pain or primary dysmenorrhea the recommended dosage is 50 mg t.i.d. With experience, physicians may find that in some patients an initial dose of 100 mg of diclofenac potassium tablets, followed by 50-mg doses, will provide better relief. For the relief of osteoarthritis the recommended dosage is 100-150 mg/day in divided doses, 50 mg b.i.d. or t.i.d. For the relief of rheumatoid arthritis the recommended dosage is 150-200 mg/day in divided doses, 50 mg t.i.d. or q.i.d. Different formulations of diclofenac (diclofenac sodium enteric-coated tablets; diclofenac sodium extended-release tablets; diclofenac potassium tablets) are not necessarily bioequivalent even if the milligram strength is the same.
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Diclofenac potassium is a benzene-acetic acid derivative, designated chemically as 2-[(2,6-dichlorophenyl) amino] benzeneacetic acid, monopotassium salt. The structural formula is: Diclofenac potassium, is a faintly yellowish white to light beige, virtually odorless, slightly hygroscopic crystalline powder. It is freely soluble in methanol, soluble in ethanol, sparingly soluble in water and practically insoluble in chloroform and in dilute acid. The n-octanol/water partition coefficient is 13.4 at pH 7.4 and 1545 at pH 5.2. Diclofenac potassium has a dissociation constant (pKa) of 4.0��0.2 at 25��C in water. Each diclofenac potassium tablet intended for oral administration contains 50 mg of diclofenac potassium. In addition, each tablet contains the following inactive ingredients: hydroxypropyl methylcellulose, lactose monohydrate, magnesium stearate, microcrystalline cellulose, polyethylene glycol, polysorbate 80, pregelatinized starch and titanium dioxide.
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Pharmacodynamics: Diclofenac potassium tablets are a nonsteroidal anti-inflammatory drug (NSAID) that exhibits anti-inflammatory, analgesic, and antipyretic activities in animal models. The mechanism of action of diclofenac potassium tablets, like that of other NSAIDs, is not completely understood but may be related to prostaglandin synthetase inhibition.<br/>Pharmacokinetics:<br/>Absorption: Diclofenac is 100% absorbed after oral administration compared to IV administration as measured by urine recovery. However, due to first-pass metabolism, only about 50% of the absorbed dose is systemically available (see Table 1). In some fasting volunteers, measurable plasma levels are observed within 10 minutes of dosing with diclofenac potassium tablets. Peak plasma levels are achieved approximately 1 hour in fasting normal volunteers, with a range of .33 to 2 hours. Food has no significant effect on the extent of diclofenac absorption. However, there is usually a delay in the onset of absorption and a reduction in peak plasma levels of approximately 30%.<br/>Distribution: The apparent volume of distribution (V/F) of diclofenac potassium is 1.3 L/kg. Diclofenac is more than 99% bound to human serum proteins, primarily to albumin. Serum protein binding is constant over the concentration range (0.15-105��g/mL) achieved with recommended doses. Diclofenac diffuses into and out of the synovial fluid. Diffusion into the joint occurs when plasma levels are higher than those in the synovial fluid, after which the process reverses and synovial fluid levels are higher than plasma levels. It is not known whether diffusion into the joint plays a role in the effectiveness of diclofenac.<br/>Metabolism: Five diclofenac metabolites have been identified in human plasma and urine. The metabolites include 4'-hydroxy-, 5-hydroxy-, 3'-hydroxy-, 4',5-dihydroxy- and 3'-hydroxy-4'-methoxy diclofenac. In patients with renal dysfunction, peak concentrations of metabolites 4'-hydroxy-and 5-hydroxy-diclofenac were approximately 50% and 4% of the parent compound after single oral dosing compared to 27% and 1% in normal healthy subjects. However, diclofenac metabolites undergo further glucuronidation and sulfation followed by biliary excretion. One diclofenac metabolite 4'-hydroxy-diclofenac has very weak pharmacologic activity.<br/>Excretion: Diclofenac is eliminated through metabolism and subsequent urinary and biliary excretion of the glucuronide and the sulfate conjugates of the metabolites. Little or no free unchanged diclofenac is excreted in the urine. Approximately 65% of the dose is excreted in the urine and approximately 35% in the bile as conjugates of unchanged diclofenac plus metabolites. Because renal elimination is not a significant pathway of elimination for unchanged diclofenac, dosing adjustment in patients with mild to moderate renal dysfunction is not necessary. The terminal half-life of unchanged diclofenac is approximately 2 hours.<br/>Special Populations:<br/>Pediatric: The pharmacokinetics of diclofenac potassium tablets has not been investigated in pediatric patients.<br/>Race: Pharmacokinetics differences due to race have not been identified.<br/>Hepatic Insufficiency: Hepatic metabolism accounts for almost 100% of diclofenac potassium tablet elimination, so patients with hepatic disease may require reduced doses of diclofenac potassium tablets compared to patients with normal hepatic function.<br/>Renal Insufficiency: Diclofenac pharmacokinetics has been investigated in subjects with renal insufficiency. No differences in the pharmacokinetics of diclofenac have been detected in studies of patients with renal impairment. In patients with renal impairment (inulin clearance 60-90, 30-60, and<30 mL/min; N=6 in each group), AUC values and elimination rate were comparable to those in healthy subjects.
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Diclofenac potassium tablets are contraindicated in patients with known hypersensitivity to diclofenac. Diclofenac potassium tablets should not be given to patients who have experienced asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs. Severe, rarely fatal, anaphylactic-like reactions to NSAIDs have been reported in such patients . Diclofenac potassium tablets are contraindicated for the treatment of perioperative pain in the setting of coronary artery bypass graft (CABG) surgery .
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Diclofenac potassium tablets 50 mg are white, round, film-coated, debossed GG977 on one side and plain on the reverse side are supplied as follows: NDC 0781-5017-01 in bottles of 100 tablets NDC 0781-5017-10 in bottles of 1000 tablets Store at 20��-25��C (68��-77��F) (see USP Controlled Room Temperature). Dispense in a tight container as defined in the USP. Protect from moisture.
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Cardiovascular Risk:<br/>Gastrointestinal Risk:
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Symptoms following acute NSAID overdoses are usually limited to lethargy, drowsiness, nausea, vomiting, and epigastric pain, which are generally reversible with supportive care. Gastrointestinal bleeding can occur. Hypertension, acute renal failure, respiratory depression and coma may occur, but are rare. Anaphylactoid reactions have been reported with therapeutic ingestion of NSAIDs, and may occur following an overdose. Patients should be managed by symptomatic and supportive care following an NSAID overdose. There are no specific antidotes. Emesis and/or activated charcoal (60 to 100 g in adults, 1 to 2 g/kg in children) and/or osmotic cathartic may be indicated in patients seen within 4 hours of ingestion with symptoms or following a large overdose (5 to 10 times the usual dose). Forced diuresis, alkalinization of urine, hemodialysis, or hemoperfusion may not be useful due to high protein binding.
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Diclofenac Potassium
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Diclofenac Potassium (Tablet)
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In 718 patients treated for shorter periods, i.e., 2 weeks or less, with diclofenac potassium tablets, adverse reactions were reported one-half to one-tenth as frequently as by patients treated for longer periods. In a 6-month, double-blind trial comparing diclofenac potassium tablets (N=196) versus diclofenac sodium delayed-release tablets (N=197) versus ibuprofen (N=197), adverse reactions were similar in nature and frequency. In patients taking diclofenac potassium tablets or other NSAIDs, the most frequently reported adverse experiences occurring in approximately 1%-10% of patients are: Gastrointestinal experiences including: abdominal pain, constipation, diarrhea, dyspepsia, flatulence, gross bleeding/perforation, heartburn, nausea, GI ulcers (gastric/duodenal) and vomiting. Abnormal renal function, anemia, dizziness, edema, elevated liver enzymes, headaches, increased bleeding time, pruritus, rashes and tinnitus. Additional adverse experiences reported occasionally include: Body as a Whole: fever, infection, sepsis Cardiovascular System: congestive heart failure, hypertension, tachycardia, syncope Digestive System: dry mouth, esophagitis, gastric/peptic ulcers, gastritis, gastrointestinal bleeding, glossitis, hematemesis, hepatitis, jaundice Hemic and Lymphatic System: ecchymosis, eosinophilia, leukopenia, melena, purpura, rectal bleeding, stomatitis, thrombocytopenia Metabolic and Nutritional: weight changes Nervous System: anxiety, asthenia, confusion, depression, dream abnormalities, drowsiness, insomnia, malaise, nervousness, paresthesia, somnolence, tremors, vertigo Respiratory System: asthma, dyspnea Skin and Appendages: alopecia, photosensitivity, sweating increased Special Senses: blurred vision Urogenital System: cystitis, dysuria, hematuria, interstitial nephritis, oliguria/polyuria, proteinuria, renal failure Other adverse reactions, which occur rarely are: Body as a Whole: anaphylactic reactions, appetite changes, death Cardiovascular System: arrhythmia, hypotension, myocardial infarction, palpitations, vasculitis Digestive System: colitis, eructation, liver failure, pancreatitis Hemic and Lymphatic System: agranulocytosis, hemolytic anemia, aplastic anemia, lymphadenopathy, pancytopenia Metabolic and Nutritional: hyperglycemia Nervous System: convulsions, coma, hallucinations, meningitis Respiratory System: respiratory depression, pneumonia Skin and Appendages: angioedema, toxic epidermal necrolysis, erythema multiforme, exfoliative dermatitis, Stevens-Johnson syndrome, urticaria Special Senses: conjunctivitis, hearing impairment.
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Carefully consider the potential benefits and risks of diclofenac potassium tablets and other treatment options before deciding to use diclofenac potassium tablets. Use the lowest effective dose for the shortest duration consistent with individual patient treatment goals . Diclofenac potassium tablets are indicated:
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Diclofenac Potassium
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