2. Melocam(meloxicam)
..belongs to the oxicam derivatives and it
is one of the most strong NSAIDs.
..as a selective inhibitor for COX-2,
retains the anti-inflammatory, analgesic
& antipyretic actions without the harmful
side effects of COX-1 inhibitors.
6. 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.
7. ..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.
8. …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.
9. pharmacokinetic profile of meloxicam is not altered in :
elderly patients
mild to moderate renal impairment
mild hepatic impairment
12. Melocam is a selective Cox2 inhibitor which
shows high anti-inflammatory & analgesic
potency in the management of arthritis.
..Due to its selectivity on Cox 2 enzyme,
Melocam doesn't create the usual
problems of classic NSAIDs
13.
14. How to solve this chronic
problem
without creating problems?
15. 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)
16. Thus, Meloxicam is beneficial for patients suffering from this
chronic and disabling condition & demonstrates similar
efficacy in pain relief & more rapid stiffness relief
18. GI effects
{analysis of double-blind studies in rheumatoid
arthritis (RA) and osteoarthritis (OA)}
Method
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).
19. Result
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.
20. Renal Effect
Cycloxygenase inhibitors prevent the synthesis
of prostaglandins that are responsible for
maintaining renal blood flow.
…..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.
21. so
No need for dose adjustment in
patients with mild to moderate
renal failure.
22. 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.
23. No Effect on Platelet Aggregation
…..As a result of the decrease in TXA2
inhibitors, platelet aggregation is
producing a prolonged bleeding time.
by Cox
reduced,
24. Platelet aggregation was almost completely inhibited
by indomethacin (-87%) as compared to control
(100%), but remained unaffected by meloxicam (-1% )
Conclusions:
….Meloxicam 7.5 mg per day is COX-1
sparing & has no effect on platelet
aggregation & bleeding time.
25. 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.
26. 1-Efficacy
In 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 with
OA were achieved by 86% of those treated
with Meloxicam and 82% treated with
Piroxicam.
27.
28. Conclusion
Melocam i.m. is effective & tolerable for the
treatment of acute rheumatic pain and shows
superiority over Piroxicam
29. Cost Effective
Melocam (once daily) is cost-effective
versus vs classic NSAIDs in
management for chronic arthritis
31. 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.
