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{{ | Diclofenac | ||
{{Short description|A nonsteroidal anti-inflammatory drug (NSAID) used to treat pain and inflammatory disorders}} | |||
{{Drugbox | |||
| Verifiedfields = changed | |||
| verifiedrevid = 477002646 | |||
| IUPAC_name = 2-(2,6-dichloroanilino)phenylacetic acid | |||
| image = Diclofenac.svg | |||
| width = 200 | |||
| image2 = Diclofenac ball-and-stick model.png | |||
| width2 = 200 | |||
| tradename = Voltaren, Cataflam, others | |||
| Drugs.com = | |||
| MedlinePlus = a689002 | |||
| pregnancy_AU = C | |||
| pregnancy_US = C | |||
| legal_AU = S4 | |||
| legal_CA = Rx-only | |||
| legal_UK = POM | |||
| legal_US = Rx-only | |||
| routes_of_administration = Oral, topical, rectal, intravenous, intramuscular | |||
| bioavailability = 50–60% | |||
| protein_bound = >99% | |||
| metabolism = Liver (CYP2C9) | |||
| elimination_half-life = 1.2–2 hours | |||
| excretion = Urine (65%), feces (35%) | |||
| CAS_number = 15307-86-5 | |||
| ATC_prefix = M01 | |||
| ATC_suffix = AB05 | |||
| PubChem = 3033 | |||
| DrugBank = DB00586 | |||
| ChemSpiderID = 2928 | |||
| UNII = 144O8QL0L1 | |||
| KEGG = D07893 | |||
| ChEBI = 47381 | |||
| ChEMBL = 661 | |||
| NIAID_ChemDB = 007680 | |||
| IUPHAR_ligand = 2718 | |||
| synonyms = | |||
}} | |||
==Introduction== | |||
'''Diclofenac''' is a [[nonsteroidal anti-inflammatory drug]] (NSAID) commonly used to treat pain and inflammatory disorders such as [[arthritis]]. It is available in various forms, including oral tablets, topical gels, and injections. Diclofenac works by inhibiting the production of [[prostaglandins]], which are chemicals in the body that promote inflammation, pain, and fever. | |||
==Pharmacology== | |||
===Mechanism of Action=== | |||
Diclofenac exerts its effects by inhibiting the enzyme [[cyclooxygenase]] (COX), which is responsible for the conversion of arachidonic acid to prostaglandins. There are two main isoforms of COX: COX-1 and COX-2. Diclofenac is a non-selective inhibitor, meaning it affects both COX-1 and COX-2, although it has a slightly higher affinity for COX-2. | |||
===Pharmacokinetics=== | |||
Diclofenac is well absorbed from the gastrointestinal tract, with a bioavailability of 50-60% due to first-pass metabolism in the liver. It is highly protein-bound (>99%) and is metabolized primarily by the liver enzyme [[CYP2C9]]. The elimination half-life of diclofenac is approximately 1.2 to 2 hours, and it is excreted in the urine (65%) and feces (35%). | |||
==Clinical Uses== | |||
===Indications=== | |||
Diclofenac is indicated for the treatment of various conditions, including: | |||
* [[Osteoarthritis]] | |||
* [[Rheumatoid arthritis]] | |||
* [[Ankylosing spondylitis]] | |||
* Acute pain, such as postoperative pain | |||
* [[Migraine]] | |||
* Dysmenorrhea (painful menstruation) | |||
===Dosage Forms=== | |||
Diclofenac is available in several formulations, including: | |||
* Oral tablets and capsules | |||
* Topical gels and creams | |||
* Transdermal patches | |||
* Rectal suppositories | |||
* Intramuscular and intravenous injections | |||
==Adverse Effects== | |||
===Common Side Effects=== | |||
Common side effects of diclofenac include: | |||
* [[Gastrointestinal]] discomfort, such as nausea and dyspepsia | |||
* Headache | |||
* Dizziness | |||
* Elevated liver enzymes | |||
===Serious Side Effects=== | |||
Serious side effects may include: | |||
* [[Gastrointestinal bleeding]] | |||
* [[Cardiovascular events]], such as myocardial infarction and stroke | |||
* [[Renal impairment]] | |||
* [[Hepatotoxicity]] | |||
==Contraindications== | |||
Diclofenac is contraindicated in patients with: | |||
* Known hypersensitivity to diclofenac or other NSAIDs | |||
* History of [[asthma]], urticaria, or allergic-type reactions after taking aspirin or other NSAIDs | |||
* Active [[peptic ulcer disease]] | |||
* Severe [[hepatic impairment]] | |||
* Severe [[renal impairment]] | |||
==Interactions== | |||
Diclofenac may interact with other medications, including: | |||
* [[Anticoagulants]] (e.g., warfarin) | |||
* [[Antihypertensives]] (e.g., ACE inhibitors, diuretics) | |||
* [[Lithium]] | |||
* [[Methotrexate]] | |||
==Conclusion== | |||
Diclofenac is a widely used NSAID with proven efficacy in treating pain and inflammation. However, its use must be carefully monitored due to potential adverse effects, particularly gastrointestinal and cardiovascular risks. It is important for healthcare providers to consider individual patient risk factors when prescribing diclofenac. | |||
==See Also== | |||
* [[Nonsteroidal anti-inflammatory drug]] | |||
* [[Cyclooxygenase]] | |||
* [[Prostaglandin]] | |||
==External Links== | |||
* [https://www.drugs.com/diclofenac.html Drugs.com: Diclofenac] | |||
* [https://medlineplus.gov/druginfo/meds/a689002.html MedlinePlus: Diclofenac] | |||
[[Category:Nonsteroidal anti-inflammatory drugs]] | |||
[[Category:Analgesics]] | |||
[[Category:World Health Organization essential medicines]] | |||
[[Category:Chlorobenzenes]] | |||
[[Category:Acetic acids]] | |||
Latest revision as of 17:14, 1 January 2025
Diclofenac
A nonsteroidal anti-inflammatory drug (NSAID) used to treat pain and inflammatory disorders
| Dic | |
|---|---|
| INN | |
| Drug class | |
| Routes of administration | Oral, topical, rectal, intravenous, intramuscular |
| Pregnancy category | |
| Bioavailability | 50–60% |
| Metabolism | Liver (CYP2C9) |
| Elimination half-life | 1.2–2 hours |
| Excretion | Urine (65%), feces (35%) |
| Legal status | |
| CAS Number | 15307-86-5 |
| PubChem | 3033 |
| DrugBank | DB00586 |
| ChemSpider | 2928 |
| KEGG | D07893 |
Introduction[edit]
Diclofenac is a nonsteroidal anti-inflammatory drug (NSAID) commonly used to treat pain and inflammatory disorders such as arthritis. It is available in various forms, including oral tablets, topical gels, and injections. Diclofenac works by inhibiting the production of prostaglandins, which are chemicals in the body that promote inflammation, pain, and fever.
Pharmacology[edit]
Mechanism of Action[edit]
Diclofenac exerts its effects by inhibiting the enzyme cyclooxygenase (COX), which is responsible for the conversion of arachidonic acid to prostaglandins. There are two main isoforms of COX: COX-1 and COX-2. Diclofenac is a non-selective inhibitor, meaning it affects both COX-1 and COX-2, although it has a slightly higher affinity for COX-2.
Pharmacokinetics[edit]
Diclofenac is well absorbed from the gastrointestinal tract, with a bioavailability of 50-60% due to first-pass metabolism in the liver. It is highly protein-bound (>99%) and is metabolized primarily by the liver enzyme CYP2C9. The elimination half-life of diclofenac is approximately 1.2 to 2 hours, and it is excreted in the urine (65%) and feces (35%).
Clinical Uses[edit]
Indications[edit]
Diclofenac is indicated for the treatment of various conditions, including:
- Osteoarthritis
- Rheumatoid arthritis
- Ankylosing spondylitis
- Acute pain, such as postoperative pain
- Migraine
- Dysmenorrhea (painful menstruation)
Dosage Forms[edit]
Diclofenac is available in several formulations, including:
- Oral tablets and capsules
- Topical gels and creams
- Transdermal patches
- Rectal suppositories
- Intramuscular and intravenous injections
Adverse Effects[edit]
Common Side Effects[edit]
Common side effects of diclofenac include:
- Gastrointestinal discomfort, such as nausea and dyspepsia
- Headache
- Dizziness
- Elevated liver enzymes
Serious Side Effects[edit]
Serious side effects may include:
- Gastrointestinal bleeding
- Cardiovascular events, such as myocardial infarction and stroke
- Renal impairment
- Hepatotoxicity
Contraindications[edit]
Diclofenac is contraindicated in patients with:
- Known hypersensitivity to diclofenac or other NSAIDs
- History of asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs
- Active peptic ulcer disease
- Severe hepatic impairment
- Severe renal impairment
Interactions[edit]
Diclofenac may interact with other medications, including:
- Anticoagulants (e.g., warfarin)
- Antihypertensives (e.g., ACE inhibitors, diuretics)
- Lithium
- Methotrexate
Conclusion[edit]
Diclofenac is a widely used NSAID with proven efficacy in treating pain and inflammation. However, its use must be carefully monitored due to potential adverse effects, particularly gastrointestinal and cardiovascular risks. It is important for healthcare providers to consider individual patient risk factors when prescribing diclofenac.