CEP-MR

Mechanism of Action:

Diclofenac has analgesic, anti-inflammatory, and antipyretic properties. The mechanism of action of diclofenac, like other NSAIDs, is not fully understood but includes inhibition of cyclooxygenase (COX-1 and COX-2). Diclofenac is a potent inhibitor of prostaglandin synthesis in vitro.

Pharmacokinetic Properties:

Bioavailability – 100%; Protein – more than 99% binding; Metabolism – liver, no active metabolites exist; Half-life – 1.2–2 hr (35% of the drug enters enterohepatic recurrence); Excretion – bile, only 1% in urine.

Drug-Drug interactions:

Avoid concomitant aspirin, salicylates (eg, indistinguishable, crosslets), or other NSAIDs. The risk of GI increases with anticoagulants, antiplatelets, oral corticosteroids, SSRIs, SNRIs, smoking, alcohol, or prolonged NSAID therapy; track up. Diuretics (eg, loops or thiazides), with ACE inhibitors, ARBs or β-blockers may increase or increase the risk of renal failure; Monitor closely. Pentonates digoxin; Monitoring Level. Mayonant lithium, methotrexate, cyclosporine; Monitoring for toxicity. Concomitant pemetrexed-myelosuppression with pemetrexed may increase the risk of renal, and GI toxicity. Reinforced by CYP2C9 inhibitors (eg, voriconazole) and antagonists by CYP2C9 inducers (eg, rifampin); Dose adjustment may be required. Caution with other hepatotoxic drugs (eg, acetaminophen, some antibiotics, antipyretics).

Precautions/ warning:

• Not interchangeable with other forms of diclofenac.
• There is an increased risk of serious cardiac events (MI, including stroke).
• Avoid recent MI, severe heart failure; If necessary, monitor.
• There is an increased risk of serious GI adverse events (including swelling, bleeding, ulceration, perforation).
• History of ulcer disease and/or GI bleeding.
• High blood pressure; Monitor BP closely.
• Hepatic or renal impairment. Release if signs or symptoms of liver disease develop, or if abnormal LFTs persist or worsen.
• Dehydration.
• Hypovolemia.
• Advanced kidney disease: not recommended.
• Hyperkalemia.
• Coagulation disorders.
• Monitor CBC, blood chemistry, liver, and kidney function in prolonged therapy.
• Pre-existing asthma. May mask of infection or fever.
• Close at 1 sign of a rash or any other hypersensitivity.
• Elderly.
• Weakened Labor and Delivery.
• Pregnancy (abstinence from ancy30 weeks’ gestation).
• nursing mothers.

Breastfeeding: with caution

Fertility:

For those taking diclofenac, ovulation was reduced by an amazing 93%. The progesterone levels of women have also been reported to fall.

Dosage:

Adult Dose: Use the lowest effective dose for the shortest duration. Osteoarthritis: 50mg 2-3 times daily. Arthritis: 50mg 3–4 times daily.

Duration of action:

The terminal half-life of unchanged diclofenac is about 2 hours.

Adverse Reaction:

GI disturbances, anemia, dizziness, edema, headache, pruritus, rash (can be severe), tinnitus; Heart thrombotic events, GI ulcers/bleeding, hepatotoxicity, renal toxicity, hypersensitivity reactions.

Storage:

Keep in a cool and dry place

Overdosage:

Symptoms of an overdose may include severe abdominal pain, vomiting that looks like coffee grounds, excessive drowsiness, slow/shallow breathing, seizures.

Contraindications:

Aspirin allergy. Coronary artery bypass graft surgery.

Side effects:

Abdominal pain, nausea, heartburn, diarrhea, constipation, gas, headache, drowsiness, and dizziness may occur. If any of these effects persist or worsen, tell your doctor or pharmacist immediately.

Warnings:

If you are allergic to aspirin or other similar NSAIDs, such as ibuprofen or naproxen, you may have an allergic reaction to diclofenac. If you have any signs, call your doctor immediately: Wheezing, Difficulty breathing, Hives, itchy rash

Pregnancy: with caution

Old age-with caution