Transcript
..as a selective inhibitor for COX-2,
retains the anti-inflammatory, analgesic
& antipyretic actions without the harmful
side effects of COX-1 inhibitors.
Melocam(meloxicam)
..belongs to the oxicam derivatives and it is one of the most strong NSAIDs.
Membrane Phospholipids
Phospholipase A2
Arachidonic F.A.
Cyclooxygenase (COX)
Prostaglandins Thromboxan A2
Prostacyclins
cylooxygenase (COX)
COX-1 COX-2
Maintains normal physiological functions
Involved in inflammation &
pain
Non-Selective NSAIDs
COX-1 COX-1
Side effectsStomach Kidney
Platelets
Therapeutic effectsAnti-inflammatory
AnalgesicAntipyretic
pharmacokinetic profile of meloxicam
..Prolonged and complete absorption after oral administration.
..Bioavailability of 89%.
..Not affected by concomitant intake of food.
..More than 99 % bound to plasma protein.
..Elimination half-life is 20-24 hours.
..During distribution, meloxicam penetrates the synovial fluid, reaching concentrations are 45-57% of those in plasma.
..Meloxicam was found in synovial fluid 1 hour after administration and reached peak concentrations at approximately 6 hours.
…Intramuscular meloxicam is rapidly absorbed, reaches Cmax at 1.5 hours after injection, and its absolute bioavailability is 100%.
..90% of the Cmax is reached within 30 min of injection.
..Concentrations tend to remain stable for at least 5-6 hours, these data support the use of intramuscular meloxicam in patients with acute arthropathies, since it provides a fast relief of pain and inflammation.
pharmacokinetic profile of meloxicam is not altered in :
elderly patients
mild to moderate renal impairment
mild hepatic impairment
Indications Immunological
Rheumatoid arthritis
Ankylosing spondylitis
Degenerative
Osteoarthritis
Musculoskeletal injuries:-Skeletal trauma
FractureDislocation & subluxationSprains & StrainsTendinitis & bursitis
Muscle strains
Melocam Ampoules
Acute pain of any origin
efficacy safety
..Due to its selectivity on Cox 2 enzyme, Melocam doesn't create the usual problems of classic NSAIDs
Melocam is a selective Cox2 inhibitor whichshows high anti-inflammatory & analgesicpotency in the management of arthritis.
How to solve this chronic problem
without creating problems?
Proven Efficacy
….A multicentre, double-blind, study was conducted in patients with osteoarthritis (OA) of the hip or knee in order to compare the efficacy of Meloxicam, with Diclofenac sodium.
…336 patients were treated with oral Meloxicam 7.5 mg once daily or Diclofenac 100 mg slow release once daily for 6 months,-meloxicam (n = 169)-diclofenac (n = 167)
Thus, Meloxicam is beneficial for patients suffering from this chronic and disabling condition & demonstrates similar efficacy in pain relief & more rapid stiffness relief
GI effects
Meloxicam 7.5 and 15 mg (n = 893 and 3282)Piroxicam 20 mg (n = 906) Diclofenac 100 mg SR (n = 324) Naproxen 750–1000 mg (n = 243).
Method
{analysis of double-blind studies in rheumatoid arthritis (RA) and osteoarthritis (OA)}
When examining non-serious GI events (dyspepsia, abdominal pain), severe GI events (perforation, bleeding)
Both meloxicam doses were significantly better than comparator non-steroidal anti-inflammatory drugs (NSAIDs) in most cases.
Result
Renal Effect
…..In several trials, the percentage of patients recording abnormal elevations in the levels of serum urea & creatinine was significantly lower in Melocam®
(meloxicam) groups versus diclofenac & piroxicam.
Cycloxygenase inhibitors prevent the synthesis of prostaglandins that are responsible for maintaining renal blood flow.
soNo need for dose adjustment in patients with mild to moderate
renal failure.
In Geriatric patients
Pharmacokinetic Profile
Elderly men exhibited pharmacokinetic profile similar to young men.
In a long term study to evaluate the safety & efficacy of Melocam® (meloxicam) 15
mg once daily in patients with rheumatoid arthritis, for age up to 84
years old, proves to be effective & tolerable.
No Effect on Platelet Aggregation
…..As a result of the decrease in TXA2 by Coxinhibitors, platelet aggregation is reduced,producing a prolonged bleeding time.
Platelet aggregation was almost completely inhibited by indomethacin (-87%) as compared to control (100%), but remained unaffected by meloxicam (-1% )
….Meloxicam 7.5 mg per day is COX-1 sparing & has no effect on platelet aggregation & bleeding time.
Conclusions:
In Acute Arthropathies
This study was done to compare the efficacy & the local tolerability of an i.m. Meloxicam with i.m. Piroxicam
patients 210 with RA & OA.
-Meloxicam 15 mg (n = 144)
-Piroxicam 20 mg (n = 66)
-Duration= 7 days.
1-EfficacyIn patients with RA, global efficacy was rated as 'very good' or 'rather good' by 91% of those treated with Meloxicam and only 71% treated with Piroxicam
The corresponding ratings in patients withOA were achieved by 86% of those treatedwith Meloxicam and 82% treated withPiroxicam.
Conclusion
Melocam i.m. is effective & tolerable for thetreatment of acute rheumatic pain and showssuperiority over Piroxicam
Cost Effective
Melocam (once daily) is cost-effectiveversus vs classic NSAIDs in
management for chronic arthritis
Once daily
Which maintain compliance in patients receiving chronic treatment.
Dosage & administration
In rheumatoid arthritis
15 mg once daily.
According to the response, dose could be
reduced to 7.5 mg once daily.
In acute exacerbations of osteoarthritis
7.5 mg increased to a maximum of 15 mg
Once
In cases of acute pain
Start with ampoule form (1 ampoule /day) and
then maintain treatment with tablets or
suppositories.
e daily.
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