- Author: Kristine M Lohr, MD, MS; Chief Editor: Harris Gellman, MD more...
The goals of pharmacotherapy are to reduce morbidity and prevent complications. Medications used include nonsteroidal anti-inflammatory drugs (NSAIDs), corticosteroids, and topical anesthetics.
Nonsteroidal Anti-inflammatory Drugs
Nonsteroidal anti-inflammatory drugs (NSAIDs) are most commonly used for relief of mild to moderately severe pain. Although the pain-relieving effects tend to be patient-specific, ibuprofen is usually used for initial therapy. All NSAIDs now have the black box warning for increased cardiovascular risk, even with short-term use, with naproxen having the least risk. Topical diclofenac has been used and may be the only topical NSAID manufactured in the United States, although a compounding pharmacy can compound any NSAID into a topical form.
Ibuprofen is the drug of choice for mild to moderately severe pain. It inhibits inflammatory reactions and pain by decreasing prostaglandin synthesis.
Naproxen is used for relief of mild to moderately severe pain. It inhibits inflammatory reactions and pain by decreasing the activity of cyclooxygenase, which is responsible for prostaglandin synthesis.
Ketoprofen is used for the relief of mild to moderate pain and inflammation. Small doses are indicated initially in patients with small body size, elderly patients, and persons with renal or liver disease. Doses of over 75 mg do not increase therapeutic effects. Administer high doses with caution, and closely observe the patient for response.
Flurbiprofen may inhibit cyclooxygenase, thereby inhibiting prostaglandin biosynthesis. These effects may result in analgesic, antipyretic, and anti-inflammatory activities.
This is one of a series of phenylacetic acids that has demonstrated anti-inflammatory and analgesic properties in pharmacological studies. It is believed to inhibit the enzyme cyclooxygenase, which is essential in the biosynthesis of prostaglandins. Diclofenac can cause hepatotoxicity; hence, liver enzymes should be monitored in the first 8 weeks of treatment. It is absorbed rapidly; metabolism occurs in the liver by demethylation, deacetylation, and glucuronide conjugation. The delayed-release, enteric-coated form is diclofenac sodium, and the immediate-release form is diclofenac potassium. While all NSAIDs have the potential for hepatotoxicity, diclofenac has the greatest risk.
Tolmetin inhibits prostaglandin synthesis by decreasing the activity of the enzyme cyclooxygenase, which, in turn, decreases the formation of prostaglandin precursors. The pediatric dosage is 20 mg/kg/d PO divided tid/qid initially, then 15-30 mg/kg/d, not to exceed 30 mg/kg/d
Celecoxib inhibits primarily COX-2. Inhibition of COX-1 may contribute to NSAID GI toxicity. At therapeutic concentrations, COX-1 isoenzyme is not inhibited; thus, the incidence of GI toxicity, such as endoscopic peptic ulcers, bleeding ulcers, perforations, and obstructions, may be decreased when compared with nonselective NSAIDs.
Seek the lowest dose for each patient. The adult dosage is 100-200 mg PO bid; the pediatric dosage has not been established for patients younger than 2 years and is 50 mg PO bid for patients 2 years or older whose weight is at least 10 kg but up to 25 kg, and is 100 mg PO bid for patients 2 years or older whose weight is more than 25 kg.
Indomethacin is used for relief of mild to moderate pain; it inhibits inflammatory reactions and pain by decreasing the activity of COX, which results in a decrease of prostaglandin synthesis.
Meloxicam decreases the activity of cyclo-oxygenase, which, in turn, inhibits prostaglandin synthesis. These effects decrease the formation of inflammatory mediators.
Diclofenac is designated chemically as 2-[(2,6-dichlorophenyl) amino] benzeneacetic acid, monosodium salt, with an empirical formula of C14 H10 Cl2 NO2 NA. It is one of a series of phenylacetic acids that has demonstrated anti-inflammatory and analgesic properties in pharmacological studies. It is believed to inhibit the enzyme cyclooxygenase, which is essential in the biosynthesis of prostaglandins. Diclofenac can cause hepatotoxicity; hence, liver enzymes should be monitored in the first 8 weeks of treatment.
Corticosteroids have anti-inflammatory properties and cause profound and varied metabolic effects. In addition, they modify the body’s immune response to diverse stimuli.
Hydrocortisone decreases inflammation by suppressing migration of polymorphonuclear leukocytes (PMNs) and reversing increased capillary permeability.
Methylprednisolone decreases inflammation by suppressing migration of PMNs and reducing capillary permeability.
Dexamethasone is used for various inflammatory diseases. It decreases inflammation by suppressing migration of PMNs and reducing capillary permeability.
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