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Ibuprofen + Paracetamol

Ibuprofen + Paracetamol Ibuprofen + Paracetamol
Ibuprofen + Paracetamol Ibuprofen + Paracetamol

Ibuprofen is an anti-inflammatory, antipyretic and analgesic drug which helps in reducing the pain, swelling and lowering high temperatures. Paracetamol is an analgesic as well as anti-pyretic which works in a different way from Ibuprofen to relieve pain and fever. 

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Introduction

Ibuprofen is an anti-inflammatory, antipyretic and analgesic drug which helps in reducing the pain, swelling and lowering high temperatures. Paracetamol is an analgesic as well as anti-pyretic which works in a different way from Ibuprofen to relieve pain and fever.

Pharmacological Class: NSAID 

Indications

  • Mild to moderate pain associated with migraine
  • Headache
  • Minor pain of arthritis
  • Common cold  
  • Muscular aches
  • Fever
  • Backache      
  • Toothache  
  • Menstrual cramps 

Pharmachologic action

The pharmacological actions of Ibuprofen and Paracetamol differ in their site and mode of action. Their complementary modes of action are synergistic which results in greater antinociception and antipyresis than the single active drug alone.

  • Ibuprofen elicits an analgesic effect through peripheral inhibition of the cycloxygenase-2 (COX-2) isoenzyme with a subsequent reduction in sensitization of nociceptive nerve terminals. It also inhibits induced leukocyte migration into inflamed areas. Ibuprofen antipyretic effects are produced by the central inhibition of prostaglandins in the hypothalamus. It reversibly inhibits platelet aggregation and reduces inflammatory pain, swelling, and fever

  • Paracetamol inhibits central COX-2 activity and also stimulate the activity of descending 5-hydroxytryptamine (serotonin) pathway that inhibits nociceptive signal transmission in the spinal cord. The antipyretic properties of acetaminophen are likely due to direct effects on the heat-regulating centers of the hypothalamus resulting in peripheral vasodilation, sweating and hence heat dissipation

Dosage

Adult: Ibuprofen 400 mg and paracetamol 325/500 mg: 1 tab 3- 4 times/day          

Note:  Not for use by children

Pharmacokinetics

Ibuprofen is well absorbed from the gastrointestinal tract and is extensively bound to plasma proteins.  Ibuprofen diffuses into the synovial fluid. Peak plasma concentrations achieved within 1-2 hrs after ingestion on an empty stomach. When taken with food, peak plasma levels are lower. It is broken down in the liver into two major metabolites with rapid and complete primary excretion via the kidneys. The elimination half life is approximately 2-4 hours Paracetamol is readily absorbed from the gastrointestinal tract. Plasma protein binding is 25% and peak plasma concentrations occurring at 0.5-067 hrs after ingestion on an empty stomach. When this product was taken with food, peak plasma levels were delayed. It is metabolized in liver and excreted in the urine mainly as the glucuronide and sulphate conjugates, with about 10% as glutathione conjugates. Less than 5% is excreted as unchanged paracetamol. The elimination half life is approximately 1-4 hours.

The bioavailability and pharmacokinetic profile of Ibuprofen and Paracetamol are not altered when taken in combination as a single or repeat dose.

Contraindications

  • Use in patients with active peptic ulcer
  • Patients with history of hypersensitivity to either of the drugs, Recent GI bleeding, Neonates

Drug interaction

      • Antagonizes the effects of furosemide & thiazides
      • Pethidine & propanthelene reduce absorption of paracetamol
      • Aspirin displaces ibuprofen from binding sites
      • Increased risk of GI ulceration & bleeding when taken with anticoagulants
      • Increases the risk of methotrexate toxicity & lithium toxicity when taken along

      Side effects

      Common (affecting between 1 in10 to 1 in 100)

      • Constipation, Diarrhea, gas or bloating
      • Dizziness, Nervousness
      • Nausea

       

      Uncommon (affecting 1 in 100 to 1 in 1000)

      • Ringing in the Ears
      • Unexplained weight gain
      • Fever, rashes, itching
      • Swelling of the eyes, face, throat, arms, hands, feet, ankles, or lower legs
      • Difficulty breathing or swallowing
      • Loss of appetite

      Very rare (affecting less than 1 in 10,000)

      • Yellowing of the skin or eyes
      • Flu-like symptoms
      • Fast heartbeat
      • Cloudy, discolored, or bloody urine
      • Difficult or painful urination
      • Blurred vision, changes in color vision, o other vision problems

      Precautions

      • Caution should be exercised in patients with asthma, especially in patients with frequent stuffed or runny nose or nasal polyps, swelling of the hands, arms, feet, ankles, or lower legs; lupus (a condition in which the body attacks many of its own tissues and organs, often including the skin, joints, blood, and kidneys); or liver or kidney disease or during pregnancy and breastfeeding
      • It may cause dizziness or drowsiness. Driving a car or operating a machinery while taking this medication is not advised
      • Alcohol consumption with these drugs should be avoided

      Clinical evidence

      • A combination of two analgesics in fixed dose in a single tablet have shown better pain relief than either drug alone in acute postoperative pain and migraine headache. It shows 73% efficacy with ibuprofen 400 mg + paracetamol 1000 mg. Doctors treating pain after surgery may consider using acetaminophen and ibuprofen together four times a day, provided there are no contraindications to either drug1.
      • Paracetamol is often used with a NSAID for acute pain after oral surgery but these drugs have to be given separately at different time intervals. The combination of paracetamol and ibuprofen provides superior pain relief after oral surgery as compare to paracetamol or ibuprofen alone 2.

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