Meloxicam

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DRUGS
Meloxicam

Meloxicam is a NSAID (nonsteroidal anti-inflammatory drug) of oxicam family. It has anti-inflammatory, analgesic and antipyretic properties. It works by reducing hormones that cause inflammation and pain in the body. Meloxicam is used to treat pain or inflammation caused by rheumatoid arthritis and osteoarthritis in adults.

Introduction

Meloxicam is a NSAID (nonsteroidal anti-inflammatory drug) of oxicam family. It has anti-inflammatory, analgesic and antipyretic properties. It works by reducing hormones that cause inflammation and pain in the body. Meloxicam is used to treat pain or inflammation caused by rheumatoid arthritis and osteoarthritis in adults.

Pharmacological Class: NSAID

Indications

  • Osteoarthritis
  • Rheumatoid arthritis
  • Juvenile arthritis in people aged 2 years or older
  • Primary dysmenorrhea
  • Ankylosing spondylitis

Pharamcological Action

Anti-inflammatory effects of meloxicam are believed to be due to inhibition of prostaglandin synthetase (cyclooxygenase), leading to the inhibition of prostaglandin synthesis. As prostaglandins sensitize pain receptors, inhibition of their synthesis may be associated with the analgesic and antipyretic effects of meloxicam.

Dosage

Adult dose

  • Rheumatoid arthritis: 7.5 mg orally once daily up to the maximum of 15 mg once daily
  • Osteoarthritis: 7.5 mg orally once daily up to the maximum of 15 mg once daily

Pediatric dose

  • Juvenile rheumatoid arthritis: 0.125 mg/kg/day orally once daily

NOTE: Drug should not be given to cardiac/hypertensive patients, people suffering from kidney dysfunction and liver malfunction.

Pharmacokinetics

Plasma protein binding is 99% and it is metabolized to four biologically inactive main metabolites. Meloxicam undergoes roughly equal renal and faecal elimination, with <0.25% excreted unchanged in urine and 1.6% of the parent compound present in the faeces

Contraindications

  • Contraindicated in patients with known hypersensitivity to meloxicam.
  • It should not be given to patients who have experienced asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs.
  • Contraindicated in conditions like renal failure, hepatic failure, rectal bleeding, proctitis and hemorrhoids.

Drug Interactions

  • NSAIDs may diminish the antihypertensive effect of angiotensin-converting enzyme (ACE) inhibitors. This interaction should be given consideration in patients taking NSAIDs concomitantly with ACE inhibitors.
  • Voriconazole may increase the serum concentration of meloxicam by decreasing its metabolism.
  • Concomitant administration of aspirin (1000 mg TID) to healthy volunteers tended to increase AUC (10%) and Cmax (24%) of meloxicam. 
  • Pretreatment for four days with cholestyramine significantly increased the clearance of meloxicam by 50%. This resulted in a decrease in t1/2, from 19.2 hours to 12.5 hours, and a 35% reduction in AUC.

Side effects

Common (affecting between 1 in10 to 1 in 100)

  • Stomach upset including nausea, vomiting, heartburn, indigestion, belching and  pain
  • Headache
  • Sore mouth or throat, discomfort when swallowing
  • Constipation or diarrhea
  • Dizziness or light-headedness
  • Skin rash or itching

Uncommon (affecting 1 in 100 to 1 in 1000)

  • Blurred vision
  • Any change in the amount or color of your urine (red or brown)
  • Any pain or difficulty experienced when urinating
  • Severe pain or tenderness in the stomach
  • Severe dizziness
  • Yellowing of the skin

Very rare (affecting less than 1 in 10,000)

  • Vomiting of blood
  • Rectal bleeding, black stools or bloody diarrhea
  • Swelling of the face, lips or tongue which may make swallowing or breathing difficult
  • Asthma, wheezing or shortness of breath
  • Sudden or severe itching, skin rash or hives
  • Weakness in one part or side of body, slurred speech, blurred vision/visual disturbances

Precautions

  • It should not be given in case of nasal polyps associated with bronchospasm, aspirin induced (high risk of severe allergic reaction), previous allergic/anaphylactic reaction to aspirin or NSAIDs.
  • Risk benefits should be considered under the following problems: alcoholism, gastrointestinal bleeding, peptic ulcer disease, asthma, compromised cardiac function, congestive heart disease, edema, hypertension, hepatic and renal function impairment.
  • Should not be taken by the pregnant women, especially in the last few months of her pregnancy. Also, it should not be taken if one is planning to become pregnant.

Clinic Evidence

  • Relatively selective COX-2 inhibition exemplified by meloxicam may offer effective symptom relief with an improved GI tolerability profile. A global safety analysis of clinical trials, representing over 5,600 patients and comprising 170 and 1,100 patient-years of exposure for meloxicam 7.5 mg and 15 mg, respectively, showed that meloxicam caused less GI toxicity and fewer peptic ulcers and GI bleeds than naproxen, diclofenac, or piroxicam. The renal safety profile and incidence of liver function abnormalities with meloxicam is equivalent to other NSAIDs available for clinical use.1
  • Daily doses of meloxicam are comparable to 500 mg mefenamic acid t.i.d. in relieving dysmenorrhea symptoms, and meloxicam has a better gastrointestinal tolerability profile. A double blind randomized study showed that meloxicam 7.5 mg and 15 mg showed a similar profile in pain reduction and dysmenorrhea symptoms when compared with mefenamic acid.2

References

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