Frafenac 50 Diclofenac Potassium Tablets

FRAFENAC-50 TABLETS

(Diclofenac Potassium 50MG)

 

Description

FRAFENAC-50 contains 50mg Diclofenac, as the potassium salt, is a benzeneacetic acid derivative, designated chemically as 2-[(2,6-dichlorophenyl)amino]benzeneacetic acid, monopotassium salt.

Diclofenac, as the potassium salt, is a faintly yellowish white to light beige, virtually odourless, slightly hygroscopic crystalline powder. It is freely soluble in methanol, soluble in ethanol, and practically insoluble in chloroform and in dilute acid. Diclofenac Potassium is soluble in water. The n-octanol/water partition coefficient is 13.4 at pH 7.4 and 1545 at pH 5.2. It has a single dissociation constant (pKa) of 4.0 ± 0.2 at 25°C in water.
Diclofenac Potassium Tablets, USP for oral administration, contain 50mg of Diclofenac

Potassium. In addition, each tablet contains the following inactive ingredients: anhydrous lactose, colloidal silicon dioxide, crosscarmellose sodium, glyceryl triacetate, hypromellose, magnesium stearate, microcrystalline cellulose, polydextrose, polyethylene glycol, sodium lauryl sulfate, red oxide of iron and titanium dioxide.

 

Diclofenac Potassium – Clinical Pharmacology: Pharmacodynamics

Diclofenac Potassium is a non-steroidal anti-inflammatory drug (NSAID) that exhibits anti-inflammatory, analgesic, and antipyretic activities in animal models. The mechanism of action of Diclofenac Potassium, like that of other NSAIDs, is not completely understood but may be related to prostaglandin synthetase inhibition.

 

Pharmacokinetics

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 I). In some fasting volunteers, measurable plasma levels are observed within 10 minutes of dosing with Diclofenac Potassium. Peak plasma levels are achieved approximately 1 hour in fasting normal volunteers. 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%.

Table 1. Pharmacokinetic Parameters for Diclofenac
PK Parameter Normal Healthy Adults (20 to 52 years)
Absolute Bioavailability (%) [N=7] 55 40
Tmax (hr) [N=65] 76 1
Oral Clearance (CL/F; mL/min) 622 21
Renal Clearance (% unchanged drug in urine) [N=7] <1
Apparent Volume of Distribution (V/F; L/kg) [N=61] 1.3 3.3
Terminal Half-life (hr) [N=48] 1.9 29

 

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 to 105 mcg/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.

Metabolism: Five diclofenac metabolites have been identified inhuman 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.

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.

 

Special Populations

Pediatric: The pharmacokinetics of Diclofenac Potassium has not been investigated in pediatric patients.

Race: Pharmacokinetic differences due to race have not been identified.

Hepatic Insufficiency: Hepatic metabolism accounts for almost 100% of Diclofenac Potassium elimination, so patients with hepatic disease may require reduced doses of Diclofenac Potassium compared to patients with normal hepatic function.

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 to 90, 30 to 60, and <30 mL/min; N = 6 in each group), AUC values and elimination rate were comparable to those in healthy subjects.

 

Indications

Diclofenac Potassium tablets, are indicated:

For treatment of primary dysmenorrhea

For relief of mild to moderate pain

For relief of the signs and symptoms of osteoarthritis

For relief of the signs and symptoms of rheumatoid arthritis

 

Contra-Indications

Diclofenac Potassium tablets are contraindicated in patients with known hypersensitivity to diclofenac. Diclofenac Potassium 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

 

Side effect

Upset stomach, nausea, heartburn, diarrhoea, constipation, headache, tiredness, drowsiness, and dizziness may occur. If any of these effects persist or worsen, notify your doctor or pharmacist promptly.

 

Dosage and administration

50mg – 100mg tablets once or twice daily depending on the severity of pains. Take this medication by mouth with a full glass of water (8 ounces or 240 milliliters) unless your doctor directs you otherwise. Do not lie down for at least 30 minutes after taking this drug. To prevent stomach upset, take this medication with food, milk, or an antacid.

 

Presentation

FRAFENAC-50 contains 50mg Diclofenac potassium packed in Alu-PVC blister of 1 x 10’s & 10 x 10’s

 

Artwork No.: 5332101-00

 

Manufactured by

Saga Laboratories

Survey No. 198/2 & 198/3, Chachrawadi Vasna,

Ta.: Sanand, Dist.: Ahmedabad – 382 210 INDIA

 

Manufactured for

FRANPHINO PHARM. CO. LTD,

44, Mosalasi Street,

Mushin, Lagos, Nigeria.

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