Medznat

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

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.