Aspirin

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DRUGS
Aspirin

Aspirin is a nonsteroidal anti-inflammatory drug (NSAID). It has analgesic, antipyretic, antirheumatic, and anti-inflammatory properties. Its action may be due to inhibition of synthesis and release of prostaglandins.

It is used to treat pain, inflammation associated with various conditions (including rheumatoid arthritis, juvenile rheumatoid arthritis, systemic lupus erythematosus, osteoarthritis, and ankylosing spondylitis) and nonfatal myocardial infarction.

Introduction

Aspirin is a nonsteroidal anti-inflammatory drug (NSAID). It has analgesic, antipyretic, antirheumatic, and anti-inflammatory properties. Its action may be due to inhibition of synthesis and release of prostaglandins. It is used to treat pain, inflammation associated with various conditions (including rheumatoid arthritis, juvenile rheumatoid arthritis, systemic lupus erythematosus, osteoarthritis, and ankylosing spondylitis) and nonfatal myocardial infarction. 

Pharmacological Class:  NSIAD

Indications

  • Pain
  • Inflammation
  • Fever
  • Muscle pain
  • Toothaches
  • Common cold
  • Headache
  • Rheumatic fever
  • Menstrual pain
  • Ankylosing Spondylitis
  • Osteoarthritis
  • Rheumatoid arthritis

Pharamcological Action

Aspirin directly and irreversibly inhibits the activity of both types of cyclooxygenase (COX-1 and COX-2) to decrease the formation of precursors of prostaglandins and thromboxanes from arachidonic acid. It may competitively inhibit prostaglandin formation. The platelet aggregation-inhibiting effect of aspirin specifically involves its ability to act as an acetyl donor to cyclooxygenase.

Irreversible acetylation renders cyclooxygenase inactive, thereby preventing the formation of the aggregating agent thromboxane A2 in platelets. Since platelets lack the ability to synthesize new proteins, the effects persist for the life of the exposed platelets (7-10 days). Aspirin may also inhibit production of the platelet aggregation inhibitor, prostacyclin (prostaglandin I2), by blood vessel endothelial cells.

Dosage

Osteoarthritis: 3 grams per day in divided doses

Rheumatoid Arthritis: 3 grams per day in divided doses

Ankylosing Spondylitis: 3 grams per day in divided doses

Fever: 325 to 650 mg orally or rectally every 4 hours as needed

Rheumatic fever: 80 mg/kg/day orally in 4 equally divided doses, up to 6.5 g/day

SLE: 3 grams per day in divided doses

Pharmacokinetics

Aspirin is absorbed rapidly in gastrointestinal tract. It is rapidly hydrolyzed primarily in the liver to salicylic acid, which is conjugated with glycine (forming salicyluric acid) and glucuronic acid and excreted largely in the urine.

Contraindications

  • People who are allergic to aspirin, products containing aspirin, or aspirin-like products
  •  People with active reye's syndrome, kidney disease, gout, anemia, hemophilia and blood clotting disorder
  • Pregnant and breast feeding women
  • People who have habit of drinking too much of alcohol
  • Patient who are prescribed anticoagulation therapy

Drug Interactions

 

  • Aspirin when taken with leflunomide may increases risk of liver damage.
  • Concomitant use of aspirin and ibuprofen increases the risk of gastrointestinal ulcers, bleeding and reduces the effectiveness of aspirin.
  • When taken together with methotrexate, causes nausea, vomiting, diarrhea, sore throat, chills, fever, rash, unusual bruising or bleeding, pale skin, dark urine, swelling of the extremities, or shortness of breath.
  • Using omacetaxine together with aspirin may increase the risk of bleeding.
  • Concomitant use of aspirin and ketorolac causes nausea, vomiting, stomach pain, drowsiness, black or bloody stools, coughing up blood, urinating less than usual, and shallow breathing.

Side effects

Common (affecting between 1 in10 to 1 in 100)

  • Heartburn
  • Upset stomach
  • Drowsiness
  • Mild headache
  • Epigastric distress
  • Dyspepsia
  • Nausea

Uncommon (affecting 1 in 100 to 1 in 1000)

  • Black/tarry stools
  • Persistent or severe stomach/abdominal pain
  • Slurred speech
  • Weakness on one side of the body
  • Sudden vision changes or severe headache

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

  • Serious bleeding from the stomach/intestine
  • Serious allergic reaction
  • Trouble breathing
  • Difficulty hearing

Precautions

  • Avoid in patients who have or have ever had asthma, frequent stuffed or runny nose, or nasal polyps.
  • Avoid in patients who have three or more alcoholic drinks every day.
  • Avoid in pregnant or breastfeeding women as it may harm fetus.
  • Avoid in patients having heartburn, upset stomach, or stomach pain, ulcers, anemia, bleeding problems such as hemophilia, or kidney or liver disease.

Clinic Evidence

  • Seventy-two randomized single-dose trials with 3253 patients given aspirin, and 3297 were given placebo. Significant benefit of aspirin over placebo was shown for aspirin 600/650 mg, 1000 mg and 1200 mg, with numbers-needed-to-treat for at least 50% pain relief of 4.4 (4.0-4.9), 4.0 (3.2-5.4) and 2.4 (1.9-3.2) respectively. Type of pain model, pain measurement, sample size, quality of study design, and study duration had no significant impact on the results. There was a clear dose-response for pain relief with aspirin, even though these were single dose studies.1

References

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