NSAIDs - Revision history

Bhavisha: /* Oxicams */

2016-06-04T16:58:48Z

Oxicams

Kellizfrid: /* Introduction */

2014-10-23T19:07:00Z

Introduction

Bara at 21:04, 11 April 2012

2012-04-11T21:04:31Z

Jackiedvm: /* Carprofen */

2011-05-11T12:51:13Z

Carprofen

Bara at 23:15, 8 November 2010

2010-11-08T23:15:18Z

Suzannah.stacey at 17:41, 7 October 2010

2010-10-07T17:41:31Z

A.allison: Unprotected "NSAIDs"

2010-07-13T21:17:20Z

Unprotected "NSAIDs"

Bara: /* Paracetamol */

2010-06-07T22:38:44Z

Paracetamol

Bara: /* Drugs in This Group */

2010-06-04T11:43:28Z

Drugs in This Group

Raven: /* Flunixin */

2010-04-17T11:51:05Z

Flunixin

@@ Line 85: / Line 85: @@
 {{Learning
 |full text = [http://www.cabi.org/cabdirect/FullTextPDF/2009/20093115490.pdf ''' Review of NSAIDs: COX selectivity and systemic effects beyond analgesia.''' Budsberg, S. C.; The North American Veterinary Conference, Gainesville, USA, Small animal and exotics. Proceedings of the North American Veterinary Conference, Orlando, Florida, USA, 17-21 January, 2009, 2009, pp 1126-1128 - '''Full Text Article''']
 }}
 {{review}}
 [[Category:WikiDrugs]]

@@ Line 1: / Line 1: @@
 ==Introduction==
-The term "NSAIDs" stands for non-steroidal anti-inflammatory drugs. They were originially obtained from plant extracts such as willow bark, which contain agents known as salicylates. Aspirin was synthesised for the first time in 1893, and in 1972 the mode of NSAID action was discovered to be associated with cyclo-oxygenase inhibition.
+The term "NSAIDs" stands for non-steroidal anti-inflammatory drugs. They were originially obtained from plant extracts such as willow bark, which contain agents known as salicylates. Aspirin was synthesised for the first time in 1893, and in 1972 the mode of NSAID action was discovered to be associated with cyclo-oxygenase (COX) inhibition. There are three categories of clinically used NSAIDs: non-selective COX inhibitors, preferential COX-2 inhibitors, and specific COX-2 inhibitors. In short, they decrease the production of prostaglandins and thromboxanes, which are inflammatory mediators. NSAIDs are widely used since they are multi-purpose drugs that do not induce addiction. Such uses include pain relief, fever reduction, and inflammation management.
 ==Mechanism of Action==

@@ Line 1: / Line 1: @@
 ==Introduction==
 The term "NSAIDs" stands for non-steroidal anti-inflammatory drugs. They were originially obtained from plant extracts such as willow bark, which contain agents known as salicylates. Aspirin was synthesised for the first time in 1893, and in 1972 the mode of NSAID action was discovered to be associated with cyclo-oxygenase inhibition.
@@ Line 84: / Line 83: @@
 Meloxicam (Metacam) is commonly used in dogs and cats, and is now licensed in cattle, pigs and horses. It may have cartilage sparing effects in osteoarthritis, but this has only been tested under laboratory conditions. Other NSAIDs appear to be detrimental to cartilage.
-==Literature Search==
+{{Learning
-[[File:CABI logo.jpg|left|90px]]
+|full text = [http://www.cabi.org/cabdirect/FullTextPDF/2009/20093115490.pdf ''' Review of NSAIDs: COX selectivity and systemic effects beyond analgesia.''' Budsberg, S. C.; The North American Veterinary Conference, Gainesville, USA, Small animal and exotics. Proceedings of the North American Veterinary Conference, Orlando, Florida, USA, 17-21 January, 2009, 2009, pp 1126-1128 - '''Full Text Article''']
+{{review}}
-Use these links to find recent scientific publications via CAB Abstracts (log in required unless accessing from a subscribing organisation).
+[[Category:WikiDrugs]]

@@ Line 65: / Line 65: @@
 ===Carprofen===
-Carprofen (Rimadyl) is a poor COX inhibitor, yet a potent anti-inflammatory drug. It is generally well-tolerated and can be used as a peri-operative analgesic with a reduce risk of nephrotoxicity compared to other NSAIDs.
+Carprofen (Rimadyl) is a poor COX inhibitor, yet a potent anti-inflammatory drug. It is generally well-tolerated and can be used as a peri-operative analgesic with a reduced risk of nephrotoxicity compared to other NSAIDs.
 ===Ketoprofen===

← Older revision		Revision as of 23:15, 8 November 2010
Line 83:		Line 83:
	===Oxicams===		===Oxicams===
	Meloxicam (Metacam) is commonly used in dogs and cats, and is now licensed in cattle, pigs and horses. It may have cartilage sparing effects in osteoarthritis, but this has only been tested under laboratory conditions. Other NSAIDs appear to be detrimental to cartilage.		Meloxicam (Metacam) is commonly used in dogs and cats, and is now licensed in cattle, pigs and horses. It may have cartilage sparing effects in osteoarthritis, but this has only been tested under laboratory conditions. Other NSAIDs appear to be detrimental to cartilage.
		+
		+	==Literature Search==
		+	[[File:CABI logo.jpg\|left\|90px]]
		+
		+
		+	Use these links to find recent scientific publications via CAB Abstracts (log in required unless accessing from a subscribing organisation).
		+	<br><br><br>
		+	[http://www.cabi.org/cabdirect/FullTextPDF/2009/20093115490.pdf ''' Review of NSAIDs: COX selectivity and systemic effects beyond analgesia.''' Budsberg, S. C.; The North American Veterinary Conference, Gainesville, USA, Small animal and exotics. Proceedings of the North American Veterinary Conference, Orlando, Florida, USA, 17-21 January, 2009, 2009, pp 1126-1128 - '''Full Text Article''']

@@ Line 1: / Line 1: @@
 {{review}}
-{{toplink
+==Introduction==
 The term "NSAIDs" stands for non-steroidal anti-inflammatory drugs. They were originially obtained from plant extracts such as willow bark, which contain agents known as salicylates. Aspirin was synthesised for the first time in 1893, and in 1972 the mode of NSAID action was discovered to be associated with cyclo-oxygenase inhibition.
 ==Mechanism of Action==
 NSAIDs are defined as "''agents which inhibit the formation of eicosanoids from arachidonic acid''". Prostaglandins (PGs), thromboxanes (TXs) and leukotrienes (LTs) are all eicosanoids which have an inflammatory-mediating action.
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 ==Actions==
 Acting centrally, NSAIDs provide analgesia. The degree of analgesia provided is dependent on the type and cause of the pain in question. For example, NSAIDs are very effective at relieving post-operative pain. They also work well in instances of hyperalgesia, where inflammation causes sensitisation of pain receptors. This is because NSAIDs prevent the formation of pain-producing prostaglandins that would otherwise be formed under the influence of pro-inflammatory cytokines such as IL-1 and TNF-a.
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 ==Pharmacokinetic Considerations==
 Pharmacokinetics for NSAIDs differ greatly between species, meaning that data from one species cannot be used to reliably calculate a dose for another.
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 ==Side Effects and Contraindications==
 The side effects associated with the use of NSAIDs are related to their non-specific inhibition of COX enzymes. The constitutively expressed COX-1 has many functions within the normal body, and suppression of these may lead to adverse reactions.
 Gastro-intestinal prostaglandins (for example, PGI2 and PGE2) normally have a protective influence over the gastric mucosa, by inhibiting the secretion of gastric acid and promoting that of mucus. NSAID inhibition of COX-1 function leads to the reduced synthesis of these prostaglandins, causing '''ulceration of the gastro-intestinal tract'''. Lesions of the large intestine have also been demonstrated following the use of phenylbutazone in the horse. Although NSAIDs are normally absorbed in the stomach, phenylbutazone may bind to feed and become released in this more distal area of the tract resulting in ulceration.
 Prostaglandins have a vasodilatory action, and so local production in the kidney is important for maintaining normal renal perfusion. NSAID interference will therefore lower renal blood flow, giving rise to '''nephrotoxicity''', and so use in renal patients must be carefully considered. Care must also be taken when administering these drugs peri-operatively.
 Some NSAIDs, such as aspirin and ketoprofen, can also have '''negative effects on coagulation'''. Platelet aggregation is caused by prostaglandins and thromboxanes which are produced by platelets using a COX-1 pathway. Inhibition of this pathway can therefore cause bleeding.
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 ===Drug Interactions===
 The concurrent use of two COX inhibitors will result in both additive efficacy and toxicity.
@@ Line 62: / Line 49: @@
 ==Drugs in This Group==
 ===Aspirin===
 Aspirin is the common name for acetyl salicylic acid. This is hydrolysed to an active form, salicylate, which irreversibly binds COX by an acetylation reaction and has a high affinity for COX in platelets. Because of this affinity, the drug has an anti-thrombotic effect which is more pronounced at low doses where platelet production of TXA2 (aggregatory) is inhibited but that of PGI2 (disaggregatory) is not. At higher doses, PGI2 formation is also affected, reducing the dis-aggregatory influence it provides and therefore the anti-thrombotic effects of aspirin. Once COX is bound by salicylate, TXA2 production is inhibited for the life of that platelet, and so new platelets are required to raise body TXA2 levels again. At the low doses required for anti-thrombosis, aspirin has no analgesic or anti-inflammatory properties.
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 ===[[Paracetamol]]===
 ===Phenylbutazone===
 Phenylbutazone (colloquially known as "bute") has a more potent anti-inflammatory than analgesic action. It follows the standard NSAID mechanism of COX inhibition, and concentrates in inflammatory exudates. It is cheap and commonly used in veterinary practice.
@@ Line 82: / Line 65: @@
 ===Carprofen===
 Carprofen (Rimadyl) is a poor COX inhibitor, yet a potent anti-inflammatory drug. It is generally well-tolerated and can be used as a peri-operative analgesic with a reduce risk of nephrotoxicity compared to other NSAIDs.
 ===Ketoprofen===
 Ketoprofen has potent anti-inflammatory, analgesic and anti-pyretic actions. In addition to its effects on COX, ketoprofen may inhibit lipoxygenase and bradykinin to have a broader mechanism of action. The main side effect is gastro-intestinal erosion.
 ===Cinchophen===
 This drug has a primarily anti-inflammatory effect, though is analgesic and anti-pyretic at higher doses (similar to aspirin). Cinchophen also has uricosuric activity. Side effects include hepatotoxitiy and gastric ulceration.
@@ Line 96: / Line 76: @@
 ===Flunixin===
 Flunixin is of limited use in small animal practice due to its toxicity; however, it is commonly used in farm and equine practice. It has potent anti-inflammatory and analgesic effects and is used for such conditions as pneumonia, mastitis and endotoxic shock. Preparations are available in combination with anti-microbials (e.g. Resflor - florfenicol plus flunixin).
 ===Fenamates===
 Tolfenamic acid and meclofenamic acid are the fenamates used in veterinary medicine. In addition to the usual mechanism of action, they may provide some antagonism to the prostaglandin receptor.
 ===Oxicams===
 Meloxicam (Metacam) is commonly used in dogs and cats, and is now licensed in cattle, pigs and horses. It may have cartilage sparing effects in osteoarthritis, but this has only been tested under laboratory conditions. Other NSAIDs appear to be detrimental to cartilage.

← Older revision	Revision as of 21:17, 13 July 2010
(No difference)

@@ Line 71: / Line 71: @@
 Oxidisation is the main method of aspirin metabolisation, but some drug is also conjugated to glucuronide. Glucuronidation cannot be performed by the cat, accounting for the long half-life in this species.
-===Paracetamol===
+===[[Paracetamol]]===
 ===Phenylbutazone===

@@ Line 71: / Line 71: @@
 Oxidisation is the main method of aspirin metabolisation, but some drug is also conjugated to glucuronide. Glucuronidation cannot be performed by the cat, accounting for the long half-life in this species.
-===Paracetemol===
+===Paracetamol===
-Although paracetemol is rarely used in veterinary medicine, it is a common household drug and so problems may arise following owner administration.
+Although paracetamol is rarely used in veterinary medicine, it is a common household drug and so problems may arise following owner administration.
-Paracetemol is metabolised by three liver pathways: glucuronidation, sulphate conjugation and N-hydroxylation. N-hydroxylation produces a substance known as NABQI which binds glutathione. If glutathione binding is saturated, NABQI binds hepatic proteins and thereby leads to liver necrosis. The glucuronidation pathway is absent in the cat, meaning N-hydroxylation is used as an alternative. Relatively, this produces greater quantities of NABQI making glutathione saturation more probable. Cats are therefore more susceptible to paracetemol toxicity. Paracetemol toxicity may be treated with N-acetylcysteine, a glutathione precursor.
+Paracetamol is metabolised by three liver pathways: glucuronidation, sulphate conjugation and N-hydroxylation. N-hydroxylation produces a substance known as NABQI which binds glutathione. If glutathione binding is saturated, NABQI binds hepatic proteins and thereby leads to liver necrosis. The glucuronidation pathway is absent in the cat, meaning N-hydroxylation is used as an alternative. Relatively, this produces greater quantities of NABQI making glutathione saturation more probable. Cats are therefore more susceptible to paracetamol toxicity. Paracetamol toxicity may be treated with N-acetylcysteine, a glutathione precursor.
-Paracetemol is grouped as an NSAID, but actually has an alternative mechanism of action. It interferes with cyclic endoperoxidases, the intermediate stage of inflammatory mediator formation. Thus, it acts further down the pathway of mediator production and so has a narrower range of effects than other NSAIDs. The drug has good anti-pyretic and analgesic properties, but is inferior as an anti-inflammatory.
+Paracetamol is grouped as an NSAID, but actually has an alternative mechanism of action. It interferes with cyclic endoperoxidases, the intermediate stage of inflammatory mediator formation. Thus, it acts further down the pathway of mediator production and so has a narrower range of effects than other NSAIDs. The drug has good anti-pyretic and analgesic properties, but is inferior as an anti-inflammatory.
-Pardale-V is a preparation of paracetemol with codeine which is licensed in dogs (although not for long-term use). It has fewer gastro-intestinal side effects than other NSAIDs and is therefore good for animals which are particularly sensitve to these drugs.
+Pardale-V is a preparation of paracetamol with codeine which is licensed in dogs (although not for long-term use). It has fewer gastro-intestinal side effects than other NSAIDs and is therefore good for animals which are particularly sensitve to these drugs.
 ===Phenylbutazone===