MELOCOX-15

MELOCOX-15

- Meloxicam is a non-steroidal  anti-inflammatory drug (NSAID) , of the Oxicam family ,with 
  anti-inflammatory, analgesic and antipyretic properties 
- Meloxicam As other NSAIDS, its precise mechanism of action remains unknown , however, there is
  at least one common mode of action shared by all  NSAIDS, including Meloxicam, inhibition of  
  biosynthesis of prostaglandin, known  inflammation mediators.
- Meloxicam is well absorbed from the gastrointestinal tract ,which is reflected by a high absolute
  bioaviabiality of  89% following oral administration .
-Following single dose administration of meloxicam, mean maximum plasma concentrations are 
 achieved within 5- 6 hours with solid oral dosage forms .with multiple dosing , steady state 
 conditions were reached within 3 to 5 days .
-Extent of absorbtion for meloxicam following oral administration is not altered by concomitant food 
   intake.
-Meloxicam is 99.4 % bound to human plasma protien ( specialiy albumin ) within the theraputic
  range, and penetrates into synovial fluid to give concentrations approximately half of those in 
  plasma.
-Meloxicam undergoes extensive hepatic biotranformation .four different metabolites of meloxicam 
  were identified in urine, which are all pharmcodynamically inactive.the major metabolite, 
  5-carboxymeloxicam (60 %of dose )is formed by oxidation of an intermediate metabolite
  5-hydroxymethyl meloxicam , which is also excreted to a lesser extent (9% of dose).
- Meloxicam is excreted predominately in the form of metabolites and occur  to equal  extent in
  urine and faces . less than 5% of the daily dose is excreted unchanged in the faces , which only traces
  of the parent compound are excreted in urine. The mean elimination half –life is about 20 hours .
  Total plasma clearance amounts on average 8 ml/min.

 * Each  Tablet  of  Melocox®   15 Contains:
     Meloxicam       15 mg.
 * Each  Tablet  of  Melocox®   7. 5 Contains:
     Meloxicam      7. 5 mg.
 * Each  suppository of  Melocox®   15 Contains:
     Meloxicam       15 mg.

  Melocox® is contra-indicated in the following situations:
-Hypersensitivity to Melocox®,or hypersensitivity to substances with a similar
  action  e.g. : NSAIDs as Aspirin . Melocox®, should not be given to patients who have developed 
  signs of asthma , nasal polyps ,angionurtic edema or urticaria following the administration of Aspirin
  or other NSAIDs.
-History of gastrointestinal bleeding or perforation ,related to previous NSAIDs therapy .
-Active ,or history of recurrent peptic ulcer , hemorrhage (two or more distinct episodes of proven  
  ulceration  or bleeding ) .
-Severely impaired  liver function  and non – dialyzed sever renal failure .Gastrointestinal bleeding , 
  cerebrovascular  bleeding  or other bleeding disorders ,sever heart failure ,Children under 15 years .

-Administration of several NSAIDs together may increase the risk of gastrointestinal ulceration and 
  bleeding via synergistic action.
- Corticosteroids :increase risk of  gastrointestinal ulceration or bleeding .
- Anticoagulants ,antiplatlet drugs, systemically administrated heparin ,thrombolytic increased risk of 
  bleeding .
- Selective serotonin reuptake inhibitors :increased risk of gastrointestinal bleeding . 
- NSAIDs increase lithium plasma levels, which may reach toxic values.
-NSAIDs can reduce tubular secretion  of methotrexate therapy increasing plasma concentrations of  
 methotrexate. 
- NSAIDs decrease the efficacy intrauterine devices .
-Diuretics: patient treated  with NSAIDs and diuretics should be adequately hydrated and be 
  monitored for renal function prior initiating treatment  .
-Antihypertensive effect reduced by NSAID.
-In patients with pre-existing renal impairment this may lead to acute renal  failure,when  NSAID and
  angiotensin II are administered .
- Cholystyramine accelerated the elimination of  Meloxicam ,so that clearance for  Meloxicam 
  increase by  50% and half life of decrease to 13± 3hrs.

- is contraindicated during pregnancy ,especially during the third trimester .
- NSAIDs are known to pass into mother’s milk .administration should therefore be avoided in 
  women who are breast feeding .

 -Common : light –headedness , headache ,dyspepsia, nausea ,vomiting, abdominal pain, constipation
   flatulence, diarrhea , Edema including edema of lower limbs.
 -Uncommon : Anemia ,vertigo, tinnitus, drowsiness ,Palpitations (In this case, symptomatic and 
  supportive therapy should be given as appropriate.(ECG and blood ) potassium levels should be
  monitored, increase in blood pressure , flushes, gastrointestinal bleeding, gastrointestinal ulcers, 
  esophagitis,  stomatisis , Angioedema, pruritus , rash ,sodium and water retention, hyperkalaemia .
 -Rare : disturbances of blood count :leucocytopenia , thrombocytopenia, agranulocytosis , 
  anaphylactic / anaphylactoid reaction , Mood disorders, insomnia and nightmares,Confusion,
  Conjunctivitis , Visual disturbances including blurred  vision ,  onset of asthma attacks in certain
  individuals allergic to aspirin or other NSAIDs,  gastrointestinal perforation, gastritis, colitis ,peptic
  ulcers, perforation or gastrointestinal   bleeding that may occur  can be sometimes  sever , especially    
  in elderly patients , Hepatitis, Urticaria ,Steven –Johnson  syndrome and toxic epidermal necrolysis ,
  angioderma, bullous reactions , such as erythema  multiform , photosensitivity reactions, Acute
  functional renal failure  in patient with risk factors .
 -Others : isolated cases of agranulocytosis have been reported in patients treated with Melocox®  
  and other potentially myelotoxic drugs.

Over dosage :-
  In case  of overdose  the standard measures of gastric evacuation and general supportive  measures
  should be used as there is no known antidote .It has been shown in a clinical trial that cholystyramin
  accelerated the elimination of Melocox®

-Undesirable effects may be minimized by using the lowest effective dose for the shortest duration 
  necessary to control symptoms 
-The recommended maximum daily dose should not be exceeded in case of  insufficient therapeutic 
  effect , nor  an additional should  be added to the therapy because this may increase the toxicity  with   
 therapeutic advantage has been proven before starting treatment with Melocox®.
- Any history of esophagitis ,gastritis and peptic ulcer must be sought in order to ensure their total 
  cure , Attention should be paid to the possible onset of a recurrence in patient treated with  
 Melocox® and with a past history  of this type .
-The use of  Melocox®  with  Concomitant NSAIDS inclnding cyclo-oxygenase II selective  inhibitor 
 should be avoided 

 Melocox®   15   tablets   (blister  of 10 tablets ,pack of one  blister)    .
 Melocox®   7.5  tablets   (blister  of 10 tablets ,pack of two  blister)   .
 Melocox®   15  suppositories  (blister  of 6 suppositories , pack of one  blister)     .

 Tablets : Store at a temperature  below 30oC in a dry place .
 suppositories: Store below 25°C ,and Protect from heat .