Mechanism Of Action:

Aceclofenac has a higher anti-inflammatory action than conventional NSAIDs. It is a cytokine inhibitor. Aceclofenac works by inhibiting the action of any substance in the body called cyclo-oxygenase. Cyclo-oxygenase is involved in the production of prostaglandins (chemicals in the body) that cause pain, swelling, and inflammation. Aceclofenac is the glycolic acid ester of diclofenac.

Paracetamol

Acetanilide derivative, Non narcotic Analgesic,Antipyretic.

Paracetamol has analgesic and antipyretic action.

It is more active on the cyclo-oxygenase enzyme in the brain. Seriously it is a poor inhibitor of prostaglandin synthesis.

Analgesic action: Paracetamol increases the pain threshold and produces analgesic effects.

Antipyretic action: Paracetamol reduces fever and inhibits the effects of endogenous pyrogens by direct action at the thermoregulatory center in the hypothalamus.

Half-Life of Aceclofenac:

The mean plasma elimination half-life is 4 – 4.3 hour

Indications for Aceclofenac:

1. Ankylosing spondylitis

2. Osteoarthritis

3. Symptomatic treatment of pain and inflammation in Post-Traumatic pain

4. Cervical pain

5. Low back pain

6. Acute gout

The onset of Action for Paracetamol:

30 – 60 minutes

Half-Life of Paracetamol:

1-4 hour

Indications for Paracetamol:

1. To relieve pain and fever

2. Acute gout

3. Migrain

Pharmacokinetic Properties:

Absorption – It is rapidly and completely absorbed after oral administration.

Distribution- Widely distributed in the body in protein-form. It is highly protein-bound (> 99.7%). Aceclofenac penetrates the synovial fluid, where concentrations reach about 60% in plasma.

Metabolism- Metabolites in the liver cause metabolism. The main metabolite is 4-hydroxycyclofenac.

Excretion – It is mainly excreted through urine.

Pharmacokinetics of Paracetamol:

Absorption: Paracetamol is rapidly and completely absorbed after oral administration.

Distribution: It is mostly distributed in the unbound form in the body.

Metabolism: It is extensively metabolized in the liver.

Excretion: Excreted in urine

Drug-Drug interactions:

Lithium, digoxin, and methotrexate: Aceclofenac may increase plasma concentrations of lithium, digoxin, and methotrexate.

Anticoagulants: The activity of anticoagulants may increase.

Diuretics: Aceclofenac inhibits the activity of diuretics. When potassium is administered concomitantly with sparing diuretics, serum potassium should be monitored.

Cyclosporine: Aceclofenac cyclosporine may increase nephrotoxicity.

Quinolones: Aceclofenac can exacerbate spasms when coadministered with quinolone antibiotics.

Precautions:

1. Hepatic impairment

2. Renal impairment

3. Hypertension

Special Precautions while taking Aceclofenac:

Hepatic porphyria, Bleeding tendencies, Blood disorders, Crohn`s disease, Decreased heart function, History of peptic ulcers, Inflammation of the bowel and back passage, Mildly decreased kidney function, Recent major surgery, Stomach disorders, Decreased liver function, Intestinal disorders

Breastfeeding: Use with caution/ Contraindicated.

Fertility:

The use of aceclofenac may impair female fertility and is not recommended in women attempting to conceive. In women who have difficulties conceiving or who are undergoing investigation of infertility, withdrawal of Aceclofenac 100 mg Film-coated Tablets should be considered.

Dosage:

Adult:

500 – 1000 mg in 3 times daily

Maximum dose: 4 g / day

For migraine: 500 mg to be taken at the first sign of migraine attack and repeated 4 – 6 hourly until suppress mild attacks.

Children:

60 mg / kg body weight /day in 4 divided doses.

Duration of action:

6 hours

Adverse Reaction:

Indigestion – including abdominal pain, feeling sick, and diarrhea. Stomach ulcers – can cause internal bleeding and anemia; Additional medication to protect your stomach may be prescribed to help reduce this risk. Headache, drowsiness, dizziness, allergic reaction

Storage:

 This medicinal product does not require any special storage conditions.

Overdosage:

Management of acute poisoning with NSAIDs essentially consists of supportive and symptomatic measures.

a) Symptoms

Symptoms include headache, nausea, vomiting, epigastric pain, gastrointestinal irritation, gastrointestinal bleeding, rarely diarrhea, disorientation, excitation, coma, drowsiness, dizziness, tinnitus, hypotension, respiratory depression, fainting, occasionally convulsions. In cases of significant poisoning, acute renal failure and liver damage are possible.

b) Therapeutic measure

Patients should be treated symptomatically as required.

Within one hour of ingestion of a potentially toxic amount, activated charcoal should be considered. Alternatively, in adults, gastric lavage should be considered within one hour of ingestion of a potentially life-threatening overdose

Contraindications:

Hypersensitivity to Paracetamol

Contra-indications of Aceclofenac:

1. Hypersensitivity to the drug

2. Bleeding from the stomach or intestines

3. Moderate to severely decreased kidney function

4. Hypersensitivity to other NSAIDs

5. Active peptic ulcer

Side Effects of Paracetamol:

1. Nausea

2. Abdominal distress

3. Allergic reactions

4. Rash

Side Effects of Aceclofenac:

Dyspepsia, Abdominal pain, Dizziness, Vertigo, Pruritis, Rash, Dermatitis, Nausea, Diarrhoea, Flatulence, Gastritis, Constipation, Vomiting, Ulcerative stomatitis, Elevation of circulating levels of hepatic enzymes.

Warnings:

This medicine should be used with caution in the elderly due to the increased risk of serious adverse effects. Treatment with this medicine should be started at low doses to check for tolerance. Depending on the clinical condition, close monitoring of renal and liver function may be necessary for such patients.

This medicine is not recommended for use in patients under 18 years of age as the safety and efficacy of the use are not clinically established.

Pregnancy: Use with caution/Contraindicated.

Children Related Information: Use with caution