Diclofenac

BRAND NAMES:

Cambia – It contains active ingredients such as diclofenac potassium. It is available in the form of 50mg powder for oral solution. It is used in the treatment of Migraine and Spondyloarthritis.

Cataflam – It contains active ingredients such as diclofenac potassium. It is available in the form of tablets. It is used in the treatment of analgesic and anti-inflammatory.

Voltaren XR- It contains active ingredients such as diclofenac sodium. It is available in the form of 100 mg extended-release tablets. 

Voltaren Emulgel– It is available in the form of a gel. It is available in 30g, 60g, and 100 grams strengths.

Zipsor- It contains active ingredients such as diclofenac potassium. It is available in the form of a liquid liquid-filled capsule. The strength of the capsules is 25mg.

MECHANISM OF ACTION:

Diclofenac has analgesic, anti-inflammatory, and antipyretic effects. Diclofenac's mode of action involves inhibiting cyclooxygenase. Diclofenac is a potent inhibitor of prostaglandin production in vitro. Diclofenac doses achieved during therapy produced in vivo effects. In animal models, prostaglandins sensitize afferent neurons and increase bradykinin's pain-inducing activity. Prostaglandins are inflammatory mediators. Because diclofenac inhibits prostaglandin synthesis, it may produce a reduction in prostaglandins in peripheral organs.

PHARMACOKINETICS:

Absorption: Diclofenac is completely absorbed after oral administration compared to IV treatment, as assessed by urine recovery. However, due to first-pass metabolism, only about half of the absorbed dosage is systemically accessible. Food has no discernible effect on the rate of diclofenac absorption. However, the commencement of absorption is frequently delayed by 1 to 4.5 hours, with a 20% drop in peak plasma levels.

Distribution: The apparent volume of distribution of diclofenac sodium is 1.4L/kg.

Metabolism: Before being eliminated in the bile, diclofenac and its oxidative metabolites are glucuronidated or sulfated. Diclofenac metabolism can also include acylglucuronidation by UGT2B7 and oxidation by CYP2C8. CYP3A4 is in charge of creating the minor metabolites 5-hydroxy- and 3-hydroxy-diclofenac. Following a single oral dose, peak concentrations of metabolites 4'-hydroxy- and 5-hydroxy diclofenac in patients with renal failure were roughly 50% and 4% of the parent substance, respectively, compared to 27% and 1% in healthy subjects.

Excretion: Diclofenac is removed by metabolism, followed by urine and biliary excretion of the glucuronide and sulfate conjugates of the metabolites. No free, unaltered diclofenac is eliminated in the urine. Approximately 65% of the dosage is eliminated in urine and 35% in bile as conjugates of unaltered diclofenac and metabolites. 

PHARMACODYNAMICS:

Diclofenac decreases inflammation, which lessens nociceptive pain and fever. It also raises the possibility of developing a gastrointestinal ulcer by decreasing the development of protective mucus in the stomach.

DOSAGE AND ADMINISTRATION:

Diclofenac oral pills are available in two different formats.

• Delayed-release tablets are available in three strengths: 25 mg, 50 mg, and 75 mg.
• Extended-release pills in a single strength (100 mg).

The recommended adult dose for osteoarthritis is 35mg of diclofenac-free acid capsules, taken orally three times daily.

Diclofenac potassium immediate-release tablets-50mg orally twice or three times per day

Diclofenac sodium enteric-coated tablets. 50 mg orally two or three times per day, or 75 mg twice daily.

Maximum daily dose: 150 mg.

Diclofenac sodium extended-release tablets (100mg) orally once daily

Usual adult dose for Ankylosing spondylitis.

Diclofenac sodium enteric-coated and delayed-release tablets -25 mg orally 4 times a day. An additional 25mg dose may be administered at bedtime, if necessary.

Maximum dose-125 mg per day

Usual adult dose for Rheumatoid Arthritis

Take 50 mg of Diclofenac Pottasum Instant-Release Tablets orally three or four times daily.

Enteric-coated and delayed-release tablets containing diclofenac sodium50 mg orally three to four times per day, or 75 mg twice per day

Maximum dosage per day: 225 mg

Extended-release Diclofenac sodium tablets: 100 mg taken once a day orally 

Maximum dosage: 100 mg taken twice a day; this would only be recommended for extremely uncommon patients whose advantages surpass the hazards to their health.

Diclofenac is available as a tablet, liquid-filled capsule, hard gelatin capsule, extended-release, delayed-release, and powder packs that may be used orally. To relieve the discomfort associated with migraine headaches, a single dose of diclofenac solution is administered without meals. Consume diclofenac precisely as prescribed. Never take more or less of it, or take it more frequently than your doctor prescribes.

DRUG INTERACTIONS:

Heart or blood pressure medication, including a diuretic or water pill

Blood thinner-warfarin, Coumadin, jantoven

Other NSAIDs- aspirin, ibuprofen, naproxen, celecoxib, indomethacin, meloxicam and others

CONTRAINDICATIONS:

An FDA-boxed warning states that individuals with a history of higher cardiovascular risk, such as MI or stroke, should not use diclofenac. Because diclofenac increases the risk of MI and stroke, it should not be administered during coronary artery bypass graft surgery. Because of the possible adverse consequences of reduced renal perfusion, diclofenac is not recommended for patients with mild or severe renal insufficiency.

SIDE EFFECTS:

• Skin rash
• Flu-symptoms
• Heart problems- swelling, rapid weight gain
• Kidney problems- no urination
• swelling in your arms or legs
• feeling tired 
• short of breath
• Liver problems
• nausea
• diarrhea 
• stomach pain
• dark urine
• jaundice
• Blood or tarry stools
• Coughing up blood
• Blood vomitings
• Indigestion
• Constipation
• headache, dizziness, drowsiness
• itching, sweating
• stuffy nose
• increased blood pressure

OVERDOSE:

Symptoms of overdose

•  Nausea

•  Vomiting

•  Stomach pains

•  Drowsiness

•  Slow, shallow, or irregular breathing

•  Loss of consciousness

TOXICITY:

Diclofenac's potential for toxicity is associated with polymorphisms of the cytochrome P450 gene family, which affects the patient's potential for drug metabolism. OTC NSAID toxicity is not uncommon but is generally limited to mild symptoms with a low risk of serious effects. These effects are usually limited to GI upset, nausea, and dizziness. Severe overdose may lead to more serious symptoms involving seizures, coma, cardiovascular events, and metabolic acidosis.

STORAGE:

Should be kept in a tightly sealed container away from light and at a room temperature of 20C to 25C (68F to 77F). Avoid storing this medication in areas where it might become damp.