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Ibuprofen Discovery, Uses, Side effects, Dosage and Brands

Ibuprofen Discovery, Uses, Side effects, Dosage and Brands

  • May 7, 2024
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Introduction

Ibuprofen is a nonsteroidal anti-inflammatory drug (NSAID) commonly used to relieve pain, reduce inflammation, and lower fever. It belongs to a class of medications known for their analgesic (pain-relieving), anti-inflammatory, and antipyretic (fever-reducing) properties. It is available over-the-counter in various forms, such as tablets, capsules, and liquid suspensions, as well as in prescription-strength formulations.

Discovery and Marketing

Ibuprofen was discovered in 1961 by Stewart Adams and John Nicholson while working at Boots UK Limited and initially marketed as Brufen. It is available under many brand names, including Nurofen, Advil, and Motrin. Ibuprofen was first sold in 1969 in the United Kingdom and in 1974 in the United States.

The discovery of ibuprofen resulted from extensive research and testing conducted by Adams and his team. They tested over 600 chemical compounds to find an alternative to existing pain relievers. After 10 years of perseverance, they found a compound worth trying on patients in the clinic. Adams initially tested the drug as a treatment for his hangover.

The success of ibuprofen led to its worldwide popularity. In recognition of their pioneering research work, Adams and Nicholson were inducted into the 2020 class of the National Inventors Hall of Fame.

Availability and Prescription Status

Ibuprofen was first made available by prescription in 1969 in the United Kingdom under the brand name Brufen. It was later marketed as Motrin in the United States in 1974

Over time, this drug has proven to be a safer and better-tolerated treatment for various conditions, including rheumatoid arthritis. As a result, it was approved for over-the-counter use in the 1980s in both the United Kingdom (as Nurofen) and the United States (as Advil).

The Mechanism of Action

Ibuprofen works by inhibiting the body’s production of prostaglandins, substances that the body produces in response to illness or injury. Prostaglandins cause pain, swelling, and fever. By reducing their production, Ibuprofen helps to alleviate these symptoms.

Ibuprofen Uses

Ibuprofen is a nonsteroidal anti-inflammatory drug (NSAID) that is commonly used for various purposes. Here are some of its main uses:

Pain Relief

Ibuprofen is widely used to reduce mild-to-moderate pain. It helps to relieve headaches, toothaches, menstrual cramps, muscle pain, back pain, and pain associated with arthritis.

Fever Reduction

It is also used to reduce fever. It helps bring down elevated body temperature caused by infections or other factors.

Arthritis Treatment

It is commonly used to manage symptoms of arthritis, including osteoarthritis, rheumatoid arthritis, and juvenile arthritis. It helps reduce inflammation, swelling, and pain associated with these conditions

Dysmenorrhea

It is often used to manage pain related to dysmenorrhea, which is the medical term for painful menstrual cramps

Headache and Migraine Relief

Ibuprofen is frequently used to alleviate headaches and migraines.

Postoperative Dental Pain

Ibuprofen is sometimes used to manage acute and chronic orofacial pain, including postoperative dental pain

Soft Tissue Disorder

It is sometimes used to treat pain associated with soft tissue disorders.

Benefits of Ibuprofen

Ibuprofen’s advantage lies in its dual action: it not only relieves pain but also reduces inflammation. This makes it particularly beneficial for conditions where inflammation is a key issue, like arthritis or sprains. Plus, its fever-reducing properties add to its versatility, making it a staple in many medicine cabinets.

Dosage

The dosage of ibuprofen varies depending on factors such as age, weight, the condition being treated, and the specific formulation of the medication. It’s essential to follow the instructions provided by your healthcare provider or those on the medication label. Here are some general dosage guidelines:

Adults

Pain and Fever: The typical dose for adults is 200 to 400 milligrams every 4 to 6 hours, as needed. Do not exceed 1200 milligrams in 24 hours unless directed by a healthcare professional.

Children

Pain and Fever: For children aged 6 months to 11 years, the dose is based on weight. It’s typically around 5 to 10 milligrams per kilogram (mg/kg) of body weight every 6 to 8 hours, as needed.

Special Considerations

Elderly: Elderly individuals are more susceptible to side effects and should use the lowest effective dose for the shortest duration possible.

Renal or hepatic impairment: Individuals with kidney or liver problems may require adjustments to their dosage. Consult a healthcare professional for personalized dosing recommendations.

Ibuprofen Use During Pregnancy

Ibuprofen is generally not advised during pregnancy, particularly after the 20th week, unless prescribed by a healthcare provider. This caution stems from its potential to impact fetal circulation and kidney function.

While short-term use, limited to three days, might be considered under certain circumstances, depending on the pregnancy stage, alternative treatments are often preferred. It’s essential to consult a doctor or pharmacist before using it during pregnancy to weigh its benefits against potential risks.

Consideration for Breastfeeding

When it comes to breastfeeding, ibuprofen is commonly deemed safe to use. It’s a preferred pain reliever for breastfeeding individuals since only minute amounts enter breast milk, posing minimal risk to the infant.

Despite its generally favorable profile, any noticeable changes in the baby’s feeding behavior or other concerns should be promptly addressed by reaching out to a midwife, health visitor, pharmacist, or doctor. They provide guidance and reassurance tailored to individual circumstances.

Understanding the Potential Side Effects of Ibuprofen

Some side effects of Ibuprofen include:

(1) Gastrointestinal Effects

  • Heartburn
  • Nausea
  • Stomach pain
  • Gastric ulcers
  • Gastrointestinal bleeding

(2) Cardiovascular Effects

Increased risk of heart attack and stroke, especially with long-term use or in high doses

(3) Renal Effects

  • Kidney damage or failure
  • Fluid retention

(4) Allergic Reactions

  • Rash
  • Itching
  • Swelling of the face, throat, or tongue
  • Difficulty breathing

(5) Hematologic Effects

  • Increased risk of bleeding
  • Decreased blood clotting ability

(6) Central Nervous System Effects

  • Headache
  • Dizziness
  • Drowsiness

(7) Other Side Effects

  • Ringing in the ears (tinnitus)
  • Liver damage, especially with long-term use or in high doses
  • Allergic reactions, including anaphylaxis (very rare),

Contraindications

Ibuprofen is contraindicated for the following health conditions:

Hypersensitivity or allergic reactions

It is contraindicated in patients with a known history of hypersensitivity or allergic reactions to ibuprofen itself, other NSAIDs, or aspirin.

Preterm Neonates

Ibuprofen lysine IV formulation is contraindicated in preterm neonates with:

  • Congenital heart diseases require patency of the PDA (Patent Ductus Arteriosus).
  • Active bleeding.
  • Thrombocytopenia.
  • Renal impairment.
  • Coagulation defects.
  • Proven or suspected necrotizing enterocolitis.

Additional Contraindications (Canada)

In Canada, ibuprofen has contraindications listed on drug labels for the following conditions:

  • Active gastrointestinal (GI) or cerebrovascular bleeding.
  • Uncontrolled heart failure.
  • Lupus.
  • Renal impairment.
  • Hepatic impairment or disease.

Pediatric Population

NSAIDs, including ibuprofen, are among the most frequently associated with hypersensitivity reactions in both adult and pediatric populations. Safe alternatives for cross-intolerant children and adolescents exist, including tolmetin, etoricoxib, paracetamol, and nimesulide.

Drug Interactions

To start ibuprofen, it is important to be aware of the following drug interactions to ensure the safe use and effectiveness of the medicine:

Anticoagulants

It increases the risk of bleeding when taken with ibuprofen.

Antiplatelet Drugs

It increases the risk of bleeding when taken with ibuprofen.

Corticosteroids

Increased risk of gastrointestinal ulcers and bleeding when taken with it.

Selective Serotonin Reuptake Inhibitors (SSRIs)

Increased risk of gastrointestinal bleeding when taken with this drug.

ACE Inhibitors

Decreased effectiveness of blood pressure control when taken with ibuprofen.

Warnings and Precautions

Before using ibuprofen, it is essential to be aware of the following warnings and precautions:

Avoid Use in Certain Conditions

  • History of gastrointestinal bleeding or ulcers
  • Kidney or liver disease
  • Heart disease or high blood pressure
  • Asthma or other respiratory conditions

Use with Caution in Specific Populations

  • Elderly individuals
  • Pregnant or breastfeeding women
  • Children under 12 years old

Limit Alcohol Consumption

Alcohol increases the risk of gastrointestinal bleeding and liver damage when taken with ibuprofen.

Long-Term Use

Long-term use of this NSAID increases the risk of serious cardiovascular and gastrointestinal events

Brands in Pakistan

In Pakistan, ibuprofen is marketed under the following brands:

  • Actifen by GlaxoSmithKline
  • Al-Fen by Alina Combine Pharmaceuticals (Pvt) Ltd.
  • Arufen by Progressive Laboratories
  • Baprofen by Batala Pharmaceuticals
  • Bludol by Standpharm Pakistan (Pvt) Ltd.
  • Boschofen by Bosch Pharmaceuticals (Pvt) Ltd.
  • BravoFen by Mega Pharmaceuticals (Pvt) Ltd
  • Brufen by Abbott Laboratories (Pakistan) Limited
  • Dolocol by Semos Pharmaceuticals (Pvt) Ltd.
  • Dorafen by Dosaco Laboratories
  • Advil by Pfizer Pharmaceuticals.

Brand Names in other countries

Ibuprofen is sold under many brand names all over the world Some common brand names include:

Brand names in Australia

  • Advil
  • Alaxan
  • Bugesic
  • Hedafen
  • Herron Blue
  • Panafen

Brand Names in India

  • Combiflam
  • Paraped Plus
  • Unafen

Brand Names in the USA

  • Addaprin
  • A-G Profen
  • Advil
  • Bufen
  • Genpril
  • Haltran
  • I-Prin
  • Ibuphm
  • Ibuprofen
  • Ibuprohm

Brand Names in the UK

  • Arthrofen
  • Brufen
  • Calprofen
  • Ebufac
  • Fenbid
  • Feverfen
  • Gelofen
  • Ibuleve
  • Ibugel
  • Ibufen

Conclusion

In conclusion, Ibuprofen has established itself as a reliable and effective over-the-counter medication in the management of pain, inflammation, and fever. However, as with any medication, it’s important to use it responsibly, understanding its benefits and potential side effects. Always consult with a healthcare provider to ensure that Ibuprofen is the right choice for your specific needs.

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