Description

Simple

A pain medication used to reduce fever, pain, and inflammation.

Clinical

An NSAID and non-selective COX inhibitor used to treat mild-moderate pain, fever, and inflammation.

Overview

Ibuprofen is a non-steroidal anti-inflammatory drug (NSAID) derived from propionic acid and it is considered the first of the propionics.[7] The formula of ibuprofen is 2-(4-isobutylphenyl) propionic acid and its initial development was in 1960 while researching for a safer alternative for aspirin.[8] Ibuprofen was finally patented in 1961 and this drug was first launched against rheumatoid arthritis in the UK in 1969 and USA in 1974. It was the first available over-the-counter NSAID.[9]

On the available products, ibuprofen is administered as a racemic mixture. Once administered, the R-enantiomer undergoes extensive interconversion to the S-enantiomer _in vivo_ by the activity of the alpha-methylacyl-CoA racemase. In particular, it is generally proposed that the S-enantiomer is capable of eliciting stronger pharmacological activity than the R-enantiomer.[Read more

Pharmacology

Indication

Ibuprofen is the most commonly used and prescribed NSAID. It is very common over the counter medication widely used as an analgesic, anti-inflammatory and antipyretic.[ Read more

Pharmacodynamic

Ibuprofen has multiple actions in different inflammatory pathways involved in acute and chronic inflammation. The main effects reported in ibuprofen are related to the control of pain, fever and acute inflammation by the inhibition of the synthesis of prostanoids by COX-1 and COX-2. Pain relief is a... Read more

Mechanism of action

The exact mechanism of action of ibuprofen is unknown. However, ibuprofen is considered an NSAID and thus it is a non-selective inhibitor of cyclooxygenase, which is an enzyme involved in prostaglandin (mediators of pain and fever) and thromboxane (stimulators of blood clotting) synthesis via the ar... Read more

Absorption

It is very well absorbed orally and the peak serum concentration can be attained in 1 to 2 hours after extravascular administration. When ibuprofen is administered immediately after a meal there is a slight reduction in the absorption rate but there is no change in the extent of the absorption.[ Read more

Protein binding

Ibuprofen dosage is more than 99% bound to plasma proteins and site II of purified albumin, binding appears to be saturable and becomes non-linear at concentrations exceeding 20 mcg/ml.[ Read more

Volume of distribution

The apparent volume of distribution of ibuprofen is of 0.1 L/kg.[25]

Clearance

The clearance rate ranges between 3-13 L/h depending on the route of administration, enantiomer type and dosage.[ Read more

Half life

The serum half-life of ibuprofen is 1.2-2 hours.[10] In patients with a compromised liver function, the h... Read more

Route of elimination

Ibuprofen is rapidly metabolized and eliminated in the urine thus, this via accounts for more than 90% of the administered dose. It is completely eliminated in 24 hours after the last dose and almost all the administered dose goes through metabolism, representing about 99% of the eliminated dose.[ Read more

Toxicity

The symptoms of overdose are presented in individuals that consumed more than 99 mg/kg. Most common symptoms of overdose are abdominal pain, nausea, vomiting, lethargy, vertigo, drowsiness (somnolence), dizziness and insomnia. Other symptoms of overdose include headache, loss of consciousness, tinni... Read more

Adverse Effects

Contraindications

  • Route:
    • Oral
  • Regions: US
  • With Therapies:
      • Name: Coronary artery bypass graft (CABG) surgery
      • Drugbank Id: DBCOND0107829
  • Hypersensitivity:
    • aspirin
    • Anti-Inflammatory Agents, Non-Steroidal
  • Regions: US

Food Interactions

  • Avoid alcohol
  • Food delays the time to reach peak plasma concentrations by 30-60 minutes and reduces peak plasma concentrations by 30-50%. Extent of absorption is unaffected.
  • Take with food to reduce gastric irritation.

Interactions

Type in a drug name to check for interaction with Ibuprofen
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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
(R)-warfarin
The metabolism of (R)-warfarin can be decreased when combined with Ibuprofen.
(S)-Warfarin
The metabolism of (S)-Warfarin can be decreased when combined with Ibuprofen.
1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid
The risk or severity of hypertension can be increased when Ibuprofen is combined with 1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid.
1-benzylimidazole
The risk or severity of hypertension can be increased when Ibuprofen is combined with 1-benzylimidazole.
2,5-Dimethoxy-4-ethylamphetamine
The risk or severity of hypertension can be increased when Ibuprofen is combined with 2,5-Dimethoxy-4-ethylamphetamine.
2,5-Dimethoxy-4-ethylthioamphetamine
The risk or severity of hypertension can be increased when Ibuprofen is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
4-Bromo-2,5-dimethoxyamphetamine
The risk or severity of hypertension can be increased when Ibuprofen is combined with 4-Bromo-2,5-dimethoxyamphetamine.
4-Methoxyamphetamine
The risk or severity of hypertension can be increased when Ibuprofen is combined with 4-Methoxyamphetamine.
5-methoxy-N,N-dimethyltryptamine
The risk or severity of hypertension can be increased when Ibuprofen is combined with 5-methoxy-N,N-dimethyltryptamine.
Abacavir
Ibuprofen may decrease the excretion rate of Abacavir which could result in a higher serum level.
Abatacept
The metabolism of Ibuprofen can be increased when combined with Abatacept.
Abciximab
The risk or severity of bleeding can be increased when Ibuprofen is combined with Abciximab.
Abediterol
The risk or severity of hypertension can be increased when Ibuprofen is combined with Abediterol.
Abemaciclib
The serum concentration of Abemaciclib can be increased when it is combined with Ibuprofen.
Abiraterone
The metabolism of Ibuprofen can be decreased when combined with Abiraterone.
Acarbose
Ibuprofen may decrease the excretion rate of Acarbose which could result in a higher serum level.
Acebutolol
Ibuprofen may decrease the antihypertensive activities of Acebutolol.
Aceclofenac
The risk or severity of adverse effects can be increased when Ibuprofen is combined with Aceclofenac.
Acemetacin
The risk or severity of adverse effects can be increased when Ibuprofen is combined with Acemetacin.
Acenocoumarol
The metabolism of Acenocoumarol can be decreased when combined with Ibuprofen.
27 References
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