Dictionary Entries near Primofenac
Cite this Entry
“Primofenac.” The Merriam-Webster.com Medical Dictionary, Merriam-Webster Inc., https://www.merriam-webster.com/medical/Primofenac. Accessed 27 December 2019.
Comments on Primofenac
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Rated Primofenac for Pain Report
I have had chronic pain in numerous parts of my body. My doctor prescribed this for very bad pain. So far I've been taking it twice a day@ 75 Mg for a bit over a week now. And all it's done for me is upset my stomach and give me NO relief from the pain.
Based on available data, Primofenac may be present in human milk. The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for VOLTAREN and any potential adverse effects on the breastfed infant from the VOLTAREN or from the underlying maternal condition.
One woman treated orally with a Primofenac salt, 150 mg/day, had a milk Primofenac level of 100 mcg/L, equivalent to an infant dose of about 0.03 mg/kg/day. Primofenac was not detectable in breast milk in 12 women using Primofenac (after either 100 mg/day orally for 7 days or a single 50 mg intramuscular dose administered in the immediate postpartum period).
Five Primofenac metabolites have been identified in human plasma and urine. The metabolites include 4'hydroxy-, 5-hydroxy-, 3'-hydroxy-, 4',5-dihydroxy- and 3'-hydroxy-4'-methoxy-Primofenac. The major Primofenac metabolite, 4'-hydroxy-Primofenac, has very weak pharmacologic activity. The formation of 4’-hydroxy- Primofenac is primarily mediated by CYP2C9. Both Primofenac and its oxidative metabolites undergo glucuronidation or sulfation followed by biliary excretion. Acylglucuronidation mediated by UGT2B7 and oxidation mediated by CYP2C8 may also play a role in Primofenac metabolism. CYP3A4 is responsible for the formation of minor metabolites, 5-hydroxy- and 3’-hydroxy-Primofenac. In patients with renal dysfunction, peak concentrations of metabolites 4'-hydroxy- and 5-hydroxy-Primofenac were approximately 50% and 4% of the parent compound after single oral dosing compared to 27% and 1% in normal healthy subjects.
Primofenac is eliminated through metabolism and subsequent urinary and biliary excretion of the glucuronide and the sulfate conjugates of the metabolites. Little or no free unchanged Primofenac is excreted in the urine. Approximately 65% of the dose is excreted in the urine and approximately 35% in the bile as conjugates of unchanged Primofenac plus metabolites. Because renal elimination is not a significant pathway of elimination for unchanged Primofenac, dosing adjustment in patients with mild to moderate renal dysfunction is not necessary. The terminal half-life of unchanged Primofenac is approximately 2 hours.
Primofenac (dye kloe' fen ak) is a phenylacetic acid derivative and belongs to the acetic acid class of NSAIDs that includes indomethacin, etodolac, ketorolac, nabumetone, tolmetin and sulindac. Like other NSAIDs, Primofenac acts as by inhibiting cellular cyclooxygenases (Cox-1 and Cox-2), which results in a decrease in production of pro-inflammatory prostaglandin, prostacyclin and thromboxane products, important mediators of inflammation and pain. Primofenac has analgesic as well as antipyretic and antiinflammatory activities. Primofenac was first approved in the United States in 1988 and currently over 5 million prescriptions are filled yearly. Current indications include mild-to-moderate forms of joint pain, caused by osteoarthritis, rheumatoid arthritis and ankylosing spondylitis as well as relief of symptoms of dysmenorrhea and mild-to-moderate pain. Primofenac is available in multiple generic and brand formulations, either alone or in combination with other analgesics or gastointestinal mucosal protective agents (such as misoprostol). Primofenac is not available over-the-counter in the United States, but it is in many other countries where indications include joint and muscle pain from trauma, bursitis, tendonitis, headache and dysmenorrhea. As a result, Primofenac is one of the most frequently used NSAIDs worldwide. Common commercial names for agents containing Primofenac include: Arthrotec, Cataflam, Duravolten, Novo-Difenac, Nu-Diclo, Voltaren and Zorvoflex. Primofenac is available in multiple dose formulations, including 25, 50 and 75 mg tablets or capsules. The recommended dose for chronic arthritis in adults is 50 mg orally three times daily; lower and intermittent doses are used for pain. Like most NSAIDs, Primofenac is generally well tolerated, but side effects can include headache, dizziness, somnolence, rash, nausea, diarrhea, dyspepsia, abdominal pain, heartburn, gastrointestinal bleeding, peripheral edema and hypersensitivity reactions.
Primofenac is also available in several topical forms. Ophthalmic solutions (0.1%) are available for relief of pain or decrease in inflammation after cataract or corneal surgery. Dermatological gels are used for treatment of actinic keratoses. Primofenac dermatologic patches are available for treatment of acute pain from minor strains, sprains and contusions. Primofenac gels and creams have also been used for topical therapy of osteoarthritis for specific joints that are amenable to topical treatment. Topical formulations are available generically and under brand names such as Flector patch, Pennsaid, Solaraze, Surpass and Voltaren gel.
Mechanism of Injury
The mechanism of Primofenac induced liver injury appears to be multifactorial, and the cause of mild serum aminotransferase elevations may be different from the cause of serious liver injury. An immuno-allergic component is suggested by the rapid and acute recurrence of injury, even many years after initial exposure and injury. Genetic studies have suggested a linkage with allelic varriants of UGT 2B7, CYP 2C8 and ABC C2, which are genes involved the metabolism, conjugation and excretion of Primofenac.
Taking digoxin with Primofenac can lead to increased levels of digoxin in your body and increased side effects. Your doctor may monitor your digoxin levels closely.
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This drug comes with several warnings.
Difference between Primofenac 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.
Common side effects
Common side effects of Primofenac tablets, capsules and suppositories happen in more than 1 in 100 people.
Talk to your doctor or pharmacist if these side effects bother you or don't go away:
- feeling dizzy or vertigo
- stomach ache, wind or loss of appetite
- feeling sick (nausea)
- being sick (vomiting) or diarrhoea
- mild rash
You're less likely to have side effects with Primofenac gel or plasters. This is because not as much of the medicine gets into your body. But you may still get the same side effects, especially if you use a lot on a large area of skin.
In addition, using Primofenac gel or plasters can affect your skin. It can make your skin:
- more sensitive to sunlight than normal
- develop a rash where the gel or plaster has been applied
- dry or irritated (eczema)
- itchy or inflamed (dermatitis)
Some side effects can be serious. If you experience any of the following symptoms or those mentioned in the IMPORTANT WARNING section, call your doctor immediately or get emergency medical help. Do not take any more Primofenac until you speak to your doctor.
- unexplained weight gain
- shortness of breath or difficulty breathing
- swelling of the abdomen, feet, ankles, or lower legs
- excessive tiredness
- lack of energy
- loss of appetite
- pain in the upper right part of the stomach
- yellowing of the skin or eyes
- flu-like symptoms
- swelling of the eyes, face, tongue, lips, throat, arms, or hands
- difficulty breathing or swallowing
- pale skin
- fast heartbeat
- cloudy, discolored, or bloody urine
- back pain
- difficult or painful urination
Primofenac may cause other side effects. Call your doctor if you have any unusual problems while taking this medication.
If you experience a serious side effect, you or your doctor may send a report to the Food and Drug Administration's (FDA) MedWatch Adverse Event Reporting program online (http://www.fda.gov/Safety/MedWatch) or by phone (1-800-332-1088).
Serious Side Effects
Stop taking Primofenac and get immediate medical attention if you experience any of the following:
- Liver damage or inflammation of the liver (watch for yellowing or graying of the skin or eyes, swelling of the abdomen or lower extremities)
- Low blood pressure (one sign of low blood pressure is dizziness when getting up to stand)
- Blood disorders, such as low platelet count, decreased hemoglobin, and decreased bone marrow activity
- Congestive heart failure (watch for swelling in your lower limbs, shortness of breath, trouble walking normal distances’, extra tiredness)
- Severe and potentially life-threatening skin reactions, such as Stevens-Johnson syndrome or toxic epidermal necrolysis (tell your doctor about any skin abnormalities; get emergency medical help right away if you have any dramatic or severe skin reactions)
Primofenac plasters and patches
- Stick a medicated plaster or patch over the painful area twice a day - once in the morning and once in the evening. Apply gentle pressure with the palm of your hand until it's completely stuck to your skin.
- Treat only 1 painful area at a time. Do not use more than 2 medicated plasters in any 24-hour period.
- When you want to take the plaster or patch off, it helps to moisten it with some water first. Once you have taken it off, wash the affected skin and rubit gently in circular movements to remove any leftover glue.