Non-steroidal anti-inflammatory drug(NSAIDs) Anti-inflammatory painkillers

‘Anti-inflammatories'

• Anti-inflammatory painkillers are sometimes called non-steroidal anti-inflammatory drugs (NSAIDs), or just 'anti-inflammatories'.

• There are over 20 types. They include: aceclofenac, acemetacin, aspirin, celecoxib, dexibuprofen, dexketoprofen, diclofenac, etodolac, etoricoxib, fenbufen, fenoprofen, flurbiprofen, ibuprofen, indometacin, ketoprofen, mefenamic acid, meloxicam, nabumetone, naproxen, piroxicam, sulindac, tenoxicam, and tiaprofenic acid. Each of these also comes as different brand names.

• You need a prescription to get anti-inflammatories, apart from ibuprofen and aspirin,

• Nonsteroidal anti-inflammatory drugs, usually abbreviated to NSAIDs—but also referred to as nonsteroidal anti-inflammatoryagents/analgesics (NSAIAs) or nonsteroidal anti-inflammatory medicines (NSAIMs)—are a class of drugs that

• provide analgesic and antipyretic (fever-reducing) effects, and,

• in higherdoses, antiinflammatory effects.

• NSAIDs are generally indicated for the symptomatic relief of the following conditions:

• Rheumatoid arthritis• Osteoarthritis• Inflammatory arthropathies (e.g. ankylosing spondylitis, psoriatic

arthritis,Reiter's syndrome)• Acute gout• Dysmenorrhoea (menstrual pain)• Metastatic bone pain• Headache and migraine• Postoperative pain• Mild-to-moderate pain due to inflammation and tissue injury• Muscle stiffness and pain due to Parkinson's disease• Pyrexia (fever)• Ileus• Renal colic• They are also given to neonate infants whose ductus arteriosus is not

closed within 24 hours of birth

• Anti-inflammatory painkillers are used to treat arthritis, sprains, painful periods, and other painful conditions.

• Most people have no trouble taking these tablets. However, some people develop side-effects which can sometimes be serious.

• In particular - if you have any cardiovascular (heart, stroke or blood vessel condition) or certain gut conditions, or are elderly, then these medicines are prescribed with caution and only where there are no alternatives and at the lowest doses and durations necessary.

• Note: if you develop upper abdominal pains, pass blood or black stools, or vomit blood, then stop taking the tablets and see your doctor as soon as possible or go to the nearest casualty department.

• As painkillers. Anti- inflammatories are used to ease pain in various conditions, including: joint pains, muscle and ligament pains (strains and sprains), period pain, pains after operations, headaches, migraines, and some other types of pain. After a single dose, they work at least as well as paracetamol to ease pain. A short course of an anti-inflammatory medicine is an option to ease short bouts of painful conditions.

• To reduce inflammation. With repeated regular doses, they also reduce inflammation. This can further reduce pain and stiffness that occurs with inflammatory conditions such as rheumatoid arthritis. When used to reduce inflammation, you might not notice the maximum effect for up to 1-3 weeks after starting a course of tablets.

• Ibuprofen and aspirin are also used to bring down a high temperature.

• Low-dose aspirin is also used to help prevent blood clots that can cause a heart attack or stroke.

• They work by inhibiting (blocking) the effect of cyclo-oxygenase (COX) enzymes. COX enzymes help to make prostaglandins. Some prostaglandins are involved in the production of pain and inflammation at sites of injury or damage. A reduction in prostaglandin production reduces pain and inflammation.

• There are two types of COX enzymes - COX-1 and COX-2. It is the COX-2 enzyme that is mainly involved in making the prostaglandins that are involved with pain and inflammation. Anti-inflammatory painkillers are sometimes classified into two main groups:

• Nonselective or standard NSAIDs. Most fall into this group, including diclofenac, ibuprofen, indometacin, and naproxen. These block both COX-1 and COX-2 enzymes.

• Coxibs. For example, celecoxib and etoricoxib. These mainly (selectively) block just the COX-2 enzyme.

Salicylates• Aspirin (acetylsalicylic acid)• Diflunisal• Salsalate

• Aspirin (USAN), also known as acetylsalicylicacid (abbreviated ASA), is a salicylate drug, often used as

• an analgesic to relieve minor aches and pains, as an

• antipyretic to reduce fever, and as• an antiinflammatory medication. • Aspirin was first isolated by

Felix Hoffmann, a chemist with the German company Bayer in 1897.[1]

[2]

• Diflunisal is a non-steroidal anti-inflammatory drug (NSAID). It was developed by Merck Sharp & Dohme in 1971 after showing promise in a research project studying more potent chemical analogs of aspirin. It was first sold under the brand name Dolobid, marketed by Merck & Co., but generic versions are now widely available. It is available in 250 mg and 500 mg tablets.

• Effectiveness of diflunisal is similar to other NSAIDs, but the duration of action is twelve hours or more. This means fewer doses per day are required for chronic administration. In acute use, it is popular in dentistry when a single dose after oral surgery can maintain analgesia until the patient is asleep that night.

• Salsalate is a non-steroidal anti-inflammatory drug (NSAID). Salsalate is in a class of drugs called salicylates. Salsalate may work by inhibiting the production of and release of prostaglandins. Salsalate is the generic name of a prescription drug marketed under the brandnames Mono- Gesic, Salflex, Disalcid, and Salsitab. Other generic and brand name formulations may be available.

• Salsalate is used to reduce pain and inflammation caused by conditions such as rheumatoid arthritis, osteoarthritis, and related rheumatic conditions. Salsalate is also recommended by physicians as an anti-inflammatory alternative to naproxen, and ibuprofen for patients that have had minor stomach bleeding or stomach upset. It has also been used as an alternative to narcotic pain medicine for people with spinal disc protrusion.

Propionic acid derivatives• Ibuprofen• Dexibuprofen• Naproxen• Fenoprofen• Ketoprofen• Dexketoprofen• Flurbiprofen• Oxaprozin• Loxoprofen

(RS)-2-(4-(2-methylpropyl)phenyl)-propanoic acid

• Ibuprofen (INN) (from iso-butyl- propanoic -phenolic acid) is a nonsteroidal anti-inflammatory drug (NSAID) used for pain relief, fever reduction, and against swelling.

• Ibuprofen has an antiplatelet effect, though relatively mild and somewhat short-lived compared with aspirin or prescription antiplatelet drugs. In general, ibuprofen also acts as a vasoconstrictor. Ibuprofen is a 'core' medicine in the World Health Organization's Model List of Essential Medicines necessary to meet the minimum medical needs of a basic healthcare system.

• Ibuprofen was derived from propanoic acid by the research arm of Boots Group during the 1960s and patented in 1961. Originally marketed as Brufen, ibuprofen is available under a variety of popular trademarks, including Motrin, Nurofen, Advil, and Nuprin. Generic formulations are available as well.

• In Europe, Australia, and New Zealand, ibuprofen lysine (the lysine salt of ibuprofen, sometimes called "ibuprofen lysinate" even though the lysine is in cationic form) is licensed for treatment of the same conditions as ibuprofen. The lysine salt increases water solubility

• Ibuprofen is produced industrially as a racemate. The compound, like other 2-arylpropionate derivatives (including ketoprofen, flurbiprofen, naproxen, etc.), does contain a chiral center in the α-position of the propionate moiety. So two enantiomers of ibuprofen occur, with the potential for different biological effects and metabolism for each enantiomer. Indeed, the (S)-(+)-ibuprofen (dexibuprofen) was found to be the active form both in vitro and in vivo.

• It was logical, then, to consider the potential for improving the selectivity and potency of ibuprofen formulations by marketing ibuprofen as a single enantiomer product (as occurs with naproxen, another NSAID). Further in vivo testing, however, revealed the existence of an isomerase (alpha- methylacyl - CoA racemase), which converted (R)-ibuprofen to the active (S)-enantiomer.

• Naproxen sodium (INN) is a nonsteroidal anti-inflammatory drug (NSAID). Naproxen and naproxen sodium are marketed under various trade names, including: Aleve, Anaprox, Antalgin, Apranax, Feminax Ultra, Flanax, Inza, Midol Extended Relief, Nalgesin, Naposin, Naprelan, Naprogesic, Naprosyn, Narocin, Proxen, Soproxen, Synflex and Xenobid.

• Naproxen was originally marketed as the prescription drug Naprosyn by Syntex in 1976, and naproxen sodium was first marketed under the trade name Anaprox in 1980. It remains a prescription-only drug in much of the world. In the United States, the Food and Drug Administration (FDA) approved its use as an over-the-counter (OTC) drug in 1994

2-(3-phenoxyphenyl)-propanoic acid

• Fenoprofen is a non-steroidal anti-inflammatory drug. Fenoprofen calcium is used for symptomatic relief for rheumatoid arthritis, osteoarthritis, and mild to moderate pain. Fenoprofen is marketed in the USA as Nalfon.

• Decreases inflammation, pain, and fever, probably through inhibition of cyclooxygenase activity and prostaglandin synthesis.

• History of significantly impaired renal function; patients with known hypersensitivity to any component of the product; patients who have experienced asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs; treatment of perioperative pain in the setting of coronary artery bypass graft (CABG) surgery.

Ketoprofen, (RS)2-(3-benzoylphenyl)-propanoic acid is one of the propionic acid class of nonsteroidal anti-inflammatory drug (NSAID) with analgesic and antipyretic

effects. It acts by inhibiting the body's production of prostaglandin.• Ketoprofen is generally prescribed for arthritis-related inflammatory pains or

severe toothaches that result in the inflammation of the gums.• Ketoprofen topical plasters are being extensively used for treatment of

musculoskeletal pain. The plasters have been shown to provide rapid and sustained delivery to underlying tissues without significantly increasing levels of drug concentration in the blood when compared to the traditional oral administration

• Dexketoprofen , (2S)-2-[3- ( benzoyl) phenyl]propanoic acid, is manufactured by Menarini, under the tradename Keral. It is available in the UK, as dexketoprofen trometamol, as a prescription-only drug and in Latin America as Enantyum, produced by Menarini. Also, in Italy it is available as an over the counter-drug under the tradename Enantyum. In Lithuania it is available as over the counter-drug under tradename Dolmen. In Mexico it is available in tablet form as "Stadium" made by Menarini in Luxemburg.

• Ketoprofen was available over-the-counter in the United States in the form of 12.5 mg coated tablets (Orudis KT and Actron), but this form has been discontinued. It is available by prescription as 50, 75, 100, 150, and 200 mg capsules.

• Ketoprofen is available also as a 2.5% gel for topical application and its so available as plasters in case of topical analgesic and anti inflammatory.

• Brand names in the US are Orudis and Oruvail. It is available in the UK as Ketoflam and Oruvail, in Finland as Ketorin, Keto, Ketomex, and Orudis'; in France as Profénid, Bi-Profénid and Ketum, in Italy as Ketodol, Fastum Gel, Lasonil, Orudis or Oki, in Poland, Serbia, Slovenia and Croatia as Knavon or Ketonal, in Romania as Ketonal, in Mexico as Arthril, in Norway as Zon or Orudis, in Russia as ОКИ (OKI), Fastum Gel and Ketonal,In Egypt, Gesiket "ATM", in Spain as Actron and in Venezuela as Ketoprofeno under an injectable solution of 100 mg and 150 mg capsules.

• Recent studies have found ketoprofen, like diclofenac, is a veterinary drug causing lethal effects in red-headed vultures. Vultures feeding on the carcasses of recently treated livestock suffer acute kidney failure within days of exposure.

• According to research, the vulture population has undergone a sharp decline on the Indian subcontinent, 95% decline in 2004, 99.9% decline as of 2008 due to the use of diclofenac in animals.

(RS)-2-(2-fluorobiphenyl-4-yl)propanoic acid

• Flurbiprofen is a member of the phenylalkanoic acid derivative family of non-steroidal anti-inflammatory drugs(NSAIDs) used to treat the inflammation and pain of arthritis. It is known by the following tradenames: Urbifen marketed by General Pharmaceuticals, Ansaid, marketed by Pfizer, Flurwood by W.Woodward and Froben, by Abbott.

• Flurbiprofen is also used as an active ingredient in some kinds of throat lozenges (Strepsils Intensive).

Acetic acid derivatives• Indomethacin• Tolmetin• Sulindac• Etodolac• Ketorolac• Diclofenac (Safety alert by FDA• Nabumetone (drug itself is non-acidic but the

active, principal metabolite has a carboxylic acid group)

2-{1-[(4-chlorophenyl)carbonyl]-5-methoxy-2-methyl-1H-indol-3-yl}acetic acid

• Indometacin (INN) or indomethacin (USAN and former BAN) is a non-steroidal anti-inflammatory drug (NSAID) commonly used as a prescription medication to reduce fever, pain, stiffness, and swelling. It works by inhibiting the production of prostaglandins, molecules known to cause these symptoms. It is marketed under more than seventy different trade names.

• Indomethacin was discovered in 1963 and it was first approved for use in the U.S. by the Food and Drug Administration in 1965. Its mechanism of action, along with several other NSAIDs that inhibit COX, was described in 1971.

[1-methyl-5-(4-methylbenzoyl)-1H-pyrrol-2-yl]acetic acid

• Tolmetin is a non-steroidal anti-inflammatory drug of the arylalkanoic acids. It is used primarily to reduce hormones that cause pain, swelling, tenderness, and stiffness in conditions such as osteoarthritis and rheumatoid arthritis, including juvenile rheumatoid arthritis. In the United States it is marketed as Tolectin and comes as a tablet or capsule.

• Diclofenac (INN ) is a nonsteroidal anti-inflammatory drug (NSAID) taken to reduce inflammation and as an analgesic reducing pain in certain conditions.

• The name is derived from its chemical name: 2-(2,6-dichloranilino) phenylacetic acid.

• In the United Kingdom, India, Brazil, and the United States, it may be supplied as either the sodium or potassium salt, in China most often as the sodium salt, while in some other countries only as the potassium salt. Diclofenac is available as a generic drug in a number of formulations, including diclofenac diethylamine applied topically. Over-the-counter (OTC) use is approved in some countries for minor aches and pains and fever associated with common infections.

1g of Voltarol Emulgel contains 11.6mg of the active substance diclofenac diethylammonium, which corresponds to 10mg diclofenac sodium. Excipients: Diethylamine, carbomer, macrogol cetostearyl ether, cocyl caprylocaprate, isopropyl alcohol, liquid paraffin heavy, perfume creme 45(containing benzyl benzoate), propylene glycol, and purified water.Aluminium tubes with protective inner coating.

Enolic acid (Oxicam) derivatives• Piroxicam• Meloxicam• Tenoxicam• Droxicam• Lornoxicam• Isoxicam

• Piroxicam is a non-steroidal anti-inflammatory drug of the oxicam class used to relieve the symptoms of rheumatoid and osteoarthritis, primary dysmenorrhoea, postoperative pain; and act as an analgesic, especially where there is an inflammatory component. It is manufactured by Pfizer under the tradename Feldene, and is available in the UK, Spain, Portugal, Belgium, Australia, Italy, Brazil and the United States. It is also manufactured by Bosnalijek under the tradename Roxam, and is available in Eastern Europe, Africa, and the Middle East. In India, it is available by the tradename Dolonex. In Thailand it is available by the tradename Fasden. It is manufactured as a patch by SK Chemicals Co., Ltd. in Korea (www.skchemicals.com.cn) for use in China under the trade name "Trast"; the Chinese name (in Pinyin) is Biluoxikang Tiepian".

• It is also used in veterinary medicine to treat certain neoplasias expressing cyclooxygenase (COX) receptors, such as bladder, colon, and prostate cancers.

• Other brand names for Piroxicam include "Arantil", "Brexidol", "Brexin", "Erazon", "Exipan", "Faxiden", "Felden", "Feldoral", "Flamexin", "Hawksone", "Hotemin", "Lubor", "Mobilis", "Pirox von ct", "Proponol", "Reumador", "Remox", "Roxam", "Sinartrol", "Toricam", "Tracam", "Ugesic", "Veral" and "Vurdon".

4-hydroxy-2-methyl-N-(5-methyl-2-thiazolyl)-2H-1,2-benzothiazine-3-carboxamide-1,1-dioxide.

• Meloxicam is a nonsteroidal anti-inflammatory drug (NSAID) with analgesic and fever reducer effects. It is a derivative of oxicam, closely related to piroxicam, and falls in the enolic acid group of NSAIDs. It was developed by Boehringer-Ingelheim. Meloxicam starts to relieve pain 30–60 minutes after administration.

Fenamic acid derivatives (Fenamates )• Mefenamic acid• Meclofenamic acid• Flufenamic acid• Tolfenamic acid

2-(2,3-dimethylphenyl)aminobenzoic acid• Mefenamic acid is a non-steroidal anti-inflammatory drug used to treat

pain, including menstrual pain. It is typically prescribed for oral administration. Mefenamic acid is marketed in the USA as Ponstel and is commonly known in UK as Ponstan.

• Mefenamic acid decreases inflammation (swelling) and uterine contractions by a still unknown mechanism. However it is thought to be related to the inhibition of prostaglandin synthesis. There is also evidence that supports the use of mefenamic acid for perimenstrual migraine headache prophylaxis, with treatment starting 2 days prior to the onset of flow or 1 day prior to the expected onset of the headache and continuing for the duration of menstruation.[1]

Sulphonanilides• Nimesulide (systemic preparations are banned by several countries for the

potential risk of hepatotoxicity)

Others• Licofelone acts by inhibiting LOX (lipooxygenase) & COX and hence known as 5-

LOX/COX inhibitor• Lysine clonixinate

Natural• Hyperforin• Figwort• Calcitriol(Vitamin D)[52]

A related drug, Paracetamol or "acetaminophen" is often considered in the same category as NSAIDS due to its use as a non-narcotic analgesic and fever-reducing agent, but is not classified as a NSAID because it only exerts weak anti-inflammatory effects.

• Selective COX-2 inhibitors (Coxibs)• Celecoxib (FDA alert)• Rofecoxib (withdrawn from market)• Valdecoxib (withdrawn from market)• Parecoxib FDA withdrawn, licenced in the EU• Lumiracoxib TGA cancelled registration• Etoricoxib not FDA approved, licenced in the EU• Firocoxib used in dogs and horses