What is Diclofenac? What is Diclofenac used for?
Diclofenac is a Generic name for nonsteroidal anti-inflammatory drug (NSAID). This drug works by lowering substances (prostaglandins) in the body that are main cause of pain and inflammation.
Diclofenac is most commonly taken in order to relieve pain, swelling and inflammation that may be caused by injuries and different health conditions such as rheumatoid arthritis, osteoarthritis, painful menstruation periods, migraines, and ankylosing splondylitis. It is available in different dosages and forms on the market.
Most commonly it is used as delayed release tablet in dose of 25 mg and 50 mg and as extended release tablet in doses of 75 mg and 100 mg. It is also available in the form of solution and powder for injection, gel, cream, patch and suppository of 50 mg and 100 mg. FDA approved diclofenac in 1998.
It is originally manufactured by Novartis. This drug is also available under different brand names, such as Voltaren, Solaraze, Pennsaid, Cataflam, Zipsor and Zorvolex.
What is Ibuprofen? What is Ibuprofen used for?
Ibuprofen is a Generic name for nonsteroidal anti-inflammatory NSAID drug . It is used as a pain reliever and fever reducer for different conditions such as: headaches, dental and muscle pain, tendinitis, menstrual cramps, and for the treatment of swelling, pain and joint stiffness caused by arthritis, osteoarthritis, bursitis, ankylosing spondylitis, juvenile arthrits, psoriatic arthritis and gout.
It can also be used as a fever reducer and for the treatment of common cold. In some cases Ibuprofen may be used intravascular with opiates for relieving moderate to severe pain.
Ibuprofen is available on the market in following dosage forms and strengths: capsule, capsule liquid filled, capsule coated (200, 220 and 400 mg), tablet (200, 300, 400, 600 and 800 mg), oral liquid (100 mg/5mL and 50 mg/1.25mL), injection (100mg/ml), solution (100 mg, 100 mg/5mL), suspension (100 mg, 200 mg/10mL, 100 mg/5mL). FDA approved ibuprofen in 1797 under the Motrin brand in 1974 originally manufactured by McNeil.
Common Brand names for ibuprofen are: Advil, Motrin, Brufen, Calprofen, Genpril, Ibu, Midol, Nuprin, Cuprofen, Nurofen, Ibuprofen 800 and PediaCare Children’s Pain Reliever/Fever Reducer IB.
Difference between Diclofenac and Ibuprofen
Both drugs are classified as NSAID – nonsteroidal anti-inflammatory drugs and used with efficacy for the treatment of pain. They work by lowering the levels of hormones (prostaglandins) that are responsible for causing inflammation and pain in the body.
But there are also differences between these two drugs. Ibuprofen in doses of 200 mg is available as OTC product in many countries while diclofenac is only available as prescription medicine.
But, in some countries diclofenac 25 mg which is the lowest efficient dose is also available as OTC. Ibuprofen in doses higher than 400 mg is available as prescription medicine.
Chemically these two drugs are also different; however they have almost the same mechanism of action. Ibuprofen is derivative of phenylpropanoic acids compounds with a structure containing a benzene ring linked to a propanoic acid.
Diclofenac is derivative of chemical entities known as dichlorobenzenes, compounds that have benzene structure linked with two chlorine atoms. These chlorine atoms may be the reason of diclofenac’s more potent acitivity compared to ibuprofen. There is some evidence that diclofenac may also inhibit the lipoxygenase pathways, reducing the formation of the leukotrienes that are known as pro-inflammatory autacoids.
There is also speculation that diclofenac may inhibit enzyme phospholipase A2. These additional actions can explain diclofenac’s high potency of diclofenac as one the most potent NSAIDs, 6 times more potent than indomethacin and 40 times as potent as aspirin.
Diclofenac is completely absorbed from gastrointestinal tract, while ibuprofen is absorbed in 80 % of taken dose. Both drugs bind to plasma proteins with high affinity and percentage of dose. Diclofenac binds to plasma proteins in rate of 99% while ibuprofen’s rate is about 90%.
Both mostly bind to albumin. Ibuprofen is metabolized in the liver predominantly via CYP2C9 liver enzymes but also with CYP2C8, CYP2C19 and CYP3A4, but also with UDP glucuronil transferase enzymes. Diclofenac is metabolized in the liver via CYP2C9, CYP3A4 liver enzymes but also with UDP glucuronil transferase enzymes and Prostaglandin G/H synthase 1
Studies have been found that diclofenac is more potent analgesic than ibuprofen, while ibuprofen is much safer than diclofenac when it is used for a longer period of time. Ibuprofen also works better as fever reducer than diclofenac.
Ibuprofen is eliminated in the urine with elimination half-life time of 2-4 hours. Diclofenac is eliminated through urinary and biliary excretion of the glucuronide and the sulfate conjugates of the metabolites. Approximately 65% of received dose is excreted in the urine and approximately 35% in the bile. Diclofenac’s elimination half-life time is about 2 hours.
In side effects profiles, diclofenac and ibuprofen are also similar. Both drugs tend to risk stomach upset and cause rash, and may also cause serious allergy. It is also known that chronic use of these drugs may precipitate sudden heart attacks or severe gastrointestinal ulceration and gastrointestinal bleeding.
However, it has been found that diclofenac causing such side effects with higher incidence and severity compared to ibuprofen. Diclofenac use increases the risk of stroke and heart attack. Ibuprofen is considered as one of the safest analgesics after acetaminophen and selective COX-2 inhibitors.
Diclofenac is classified in pregnancy category C by the FDA pregnancy list of drugs which means that it should be Used with caution and only if benefits outweigh risks. Animal studies showed risk and human studies not are available or neither animal nor human studies done.
However, Diclofenac is classified in category D if gestation period is over 30 weeks. Category D means that diclfenac may cause negative effects on the fetus during these periods. It has been shown that diclofenac may cause premature closure of ductus arteriosus.
Ibuprofen is classified in pregnancy category C by the FDA pregnancy list of drugs which means that it should be Used with caution and only if benefits outweigh risks. Animal studies showed risk and human studies not are available or neither animal nor human studies done.
However, ibuprofen is classified in category D if gestation period is over 30 weeks. Category D means that diclofenac may cause negative effects on the fetus during these period. It has been shown that ibuprofen may also cause premature closure of ductus arteriosus.
Diclofenac Vs Ibuprofen side effects
Diclofenac possible side effects Ibuprofen possible side effects
Constipation Dizziness (3-9%)
Abdominal distention and flatulence Epigastric pain (3-9%)
Abdominal pain or cramps Heartburn (3-9%)
Diarrhea Constipation (1-3%)
Dizziness Rash (3-9%)
Dyspepsia Tinnitus (3-9%)
Edema Edema (1-3%)
Fluid retention Fluid retention (1-3%)
Headache Headache (1-3%)
Nausea Vomiting (1-3%)
Peptic ulcer or GI bleeding Pruritus Rash Tinnitus Acute hepatitis Agranulocytosis Asthma Aplastic anemia Asymptomatic hepatitis Blood urea nitrogen (BUN) >40 mg/dL (>14.3 mmol/L) Cholestasis Chronic active hepatitis Congestive heart failure (CHF) Decreased hemoglobin Epistaxis Fatal fulminant hepatitis Hemolytic anemia (may be autoimmune) Hepatocellular necrosis Hypertension Jaundice Leukopenia Nephrotoxicity Purpura Serum creatinine >2 mg/dL (>177 μmol/L)
The incidence of these side effects will be increrased if ibuprofen and diclofenac are taken together or overdosed.
Can you take Diclofenac and Ibuprofen together?
No, these drugs should not be used together, as they are from the same class, thus their effects will become additive increasing the risk of side effects such as bleeding and gastrointestinal ulcers to happen.
If you need additional medicine for your pain relieving treatment, and you already use diclofenac or ibuprofen consult your doctor. Your doctor may prescribe you acetaminophen of 500 mg as additional treatment, because it is much safer to be combined with ibuprofen or diclofenac.
Diclofenac vs Ibuprofen drug interactions
Diclofenac may have serious interaction with following drugs:
· aspirin rectal
· aspirin/citric acid/sodium bicarbonate
· ketorolac intranasal
Ibuprofen may have serious interaction with following drugs:
· ketorolac intranasal