Ibuprofen + Caffeine

Drug Reference 9 min 139

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Created On: 30/09/2019

Ibuprofen plus caffeine is a well-tolerated combination in which ibuprofen acts as an anti-inflammatory, antipyretic and analgesic drug. Caffeine is a central nervous system stimulant and smooth muscle relaxant which helps in increasing the blood flow.

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Introduction

Ibuprofen plus caffeine is a well tolerated combination in which ibuprofen acts as an anti-inflammatory, antipyretic and analgesic drug. Caffeine is a central nervous system stimulant and smooth muscle relaxant which helps in increasing the blood flow. Its combination with ibuprofen has shown better results in acute pain.

Pharmacological Class: NSAID and central nervous system stimulant

Indications

Tension type headache and migraine
Post oral surgery dental pain
Rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, cervical spondylitis, intervertebral disc syndrome, and sciatica
Non-articular rheumatic conditions including fibrositis, myositis, bursitis and low back pain
Soft tissue injuries such as sprains, strains and sports injuries
Painful inflammatory conditions in gynecology
Post-operative and post-traumatic inflammation
Acute gout

Pharmachologic action

Ibuprofen is a non-selective inhibitor of cyclooxygenase which is responsible for the synthesis of prostaglandin via arachidonic acid pathway. Cyclooxygenase-2 decreases the synthesis of prostaglandins required in mediating inflammation, pain, fever, and swelling. The antipyretic effects may arise due to action on the hypothalamus which further leads to vasodilation, subsequent heat dissipation, and an increase in the peripheral blood flow.

Caffeine works by stimulating central nervous system promoting bradycardia, increased respiratory rate, and vasoconstriction. It happens due to increased intracellular cyclic AMP following inhibition phosphodiesterase that degrades cyclic AMP. Sometimes, it is combined with some analgesics or with alkaloids to treat migraine and other headache related issues.

Dosage

The dose of ibuprofen range from 50-400 mg at every 6-8 hour and not more than three times a 24 hour period while the dose of caffeine is 400mg once daily.

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 hours 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.

Caffeine is well absorbed from the gastrointestinal tract and widely distributed throughout the body. The peak plasma level for caffeine range from 6-10mg/L and the mean time to reach peak concentration ranged from 30 minutes to 2 hours. It is metabolized in liver via oxidation, demethylation and acetylation. Excretion is done by the kidney and about 80% of a dose of caffeine is metabolized to paraxanthine (1,7-dimethylxanthine), 10% to theobromine (3,7-dimethylxanthine), and 4% to theophylline (1,3-dimethylxanthine). The elimination half life is approximately 3-7 hours.

Contraindications

The combination is contraindicated in the following conditions:

Tobacco Smoking
Increased Cardiovascular Event Risk
After Coronary Bypass Surgery
Acute Thromboembolic Stroke
High Blood Pressure
Heart Attack
Stomach or Intestinal Ulcer
Liver Problems
Bleeding of the Stomach or Intestine
Kidney Disease
Pregnancy
Blood Clotting Disorder

Drug interaction

It may cause interactions with the following drugs and not advised to be taken along them:

Aspirin
Aminoglycosides
ACE inhibitors
Azole antifungal agents
Beta-blockers
Bisphosphonates
Clopidogrel
Corticosteroids
Heparin
Loop diuretics
Methotrexate
Quinolones
Serotonin reuptake inhibitors
Warfarin

Side effects

Common (affecting between 1 in 10 to 1 in 100 people)

Nausea and Vomiting
Flatulence
Diarrhea

Uncommon (affecting between 1 in 100 to 1 in 1000 people)

Hypertension
Neutropenia
Anemia
Hemorrhage
Hypoproteinemia
Thrombocythemia

Precautions

Caffeine should not to be used as a substitute for sleep
Caffeine may alter blood sugar levels. So, use in diabetic patients is advised with caution
As ibuprofen may cause serious allergic reactions, knowledge of patient’s medical history is a must

Clinical evidence

Ibuprofen and caffeine if administered together provide greater analgesic activity than ibuprofen alone, caffeine, and placebo. Caffeine acts as an adjuvant to ibuprofen in acute pain. A double-blind study with this method indicates that ibuprofen and caffeine if administered together provides greater analgesic effectiveness than either component alone or also act as a pain reliever in tension-type headache ¹
The patients with upper respiratory tract illnesses (URTIs) have reduced alertness and have slower reaction times. The combination of ibuprofen and caffeine is the optimum treatment for malaise associated with URTIs as it provides significant effects on objective performance and subjective measures in comparison to the treatment with ibuprofen or caffeine alone ²

References

Diamond S, Balm TK, Freitag FG. Clin Pharmacol Ther. 2000 Sep;68(3):312-9 ncbi.nlm.nih.gov/pubmed/11014413
Smith AP, Nutt DJ. Psychopharmacology (Berl). 2014 May; 231(9):1963-74. ncbi.nlm.nih.gov/pubmed/24287602
Andrzej Polski, Regina Kasperek, Karolina Sobotka-Polska, Ewa Poleszak. Curr. Issues Pharm. Med. Sci., Vol. 27, No. 1, Pages 10-13
Diamond S, Balm TK, Freitag FG. Clin Pharmacol Ther 2000; 68:312-19. jfponline.com/home/article/is-the-combination-of-ibuprofen-and-caffeine-effective-for-the-treatment-of-a-tension-type-headache/bc0081b998e17a7059e56f9f3a7be9cf.html
Mc Quay HJ, Angell K, Carroll D, Moore RA, Juniper RP. Pain. 1996 Aug; 66(2-3):247-51. ncbi.nlm.nih.gov/pubmed/8880847
Springer : link.springer.com/article/10.1007%2Fs11916-001-0060-8
Wiley online library: onlinelibrary.wiley.com/
DrugLib.com: druglib.com/
PharmgKB: pharmgkb.org/pathway/PA165884757
Drug Bank drugbank.ca/drugs/DB00201