PMS-meloxicam
PMS-meloxicam - General Information
PMS-meloxicam is a nonsteroidal anti-inflammatory drug (NSAID) used to relieve the symptoms of arthritis, primary dysmenorrhea, fever; and as an analgesic, especially where there is an inflammatory component. It is closely related to piroxicam. In Europe it is marketed under the brand names Movalis, Melox, and Recoxa. In North America it is generally marketed under the brand name Mobic. In Latin America, the drug is marketed as Tenaron. [Wikipedia]
Pharmacology of PMS-meloxicam
PMS-meloxicam is an nonsteroidal anti-inflammatory drug (NSAID) with analgesic and antipyretic properties. Prostaglandins are substances that contribute to inflammation of joints. PMS-meloxicam inhibits prostaglandin synthetase (cylooxygenase 1 and 2) and leads to a decrease of the synthesis of prostaglandins, therefore, inflammation is reduced.
PMS-meloxicam for patients
MOBIC, like other drugs of its class, can cause discomfort and, rarely, more serious side effects, such as gastrointestinal bleeding, which may result in hospitalization and even fatal outcomes. Although serious GI tract ulcerations and bleeding can occur without warning symptoms, patients should be alert for the signs and symptoms of ulcerations and bleeding, and should ask for medical advice when observing any indicative signs or symptoms. Patients should be made aware of the importance of this follow-up Effects - Risk of GI Ulceration, Bleeding and Perforation).
Patients should report to their physicians signs or symptoms of gastrointestinal ulceration or bleeding, skin rash, weight gain, or edema.
Patients should be informed of the warning signs and symptoms of hepatotoxicity (e.g., nausea, fatigue, lethargy, pruritus, jaundice, right upper quadrant tenderness, and "flu-like" symptoms). If these occur, patients should be instructed to stop therapy and seek immediate medical therapy.
Patients should also be instructed to seek immediate emergency help in the case of an anaphylactoid reaction.
In late pregnancy, as with other NSAIDs, MOBIC should be avoided because it may cause premature closure of the ductus arteriosus.
PMS-meloxicam Interactions
ACE inhibitors
Reports suggest that 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.
Aspirin
Concomitant administration of aspirin (1000 mg TID) to healthy volunteers tended to increase the AUC (10%) and Cmax (24%) of meloxicam. The clinical significance of this interaction is not known; however, as with other NSAIDs, concomitant administration of meloxicam and aspirin is not generally recommended because of the potential for increased adverse effects. Concomitant administration of low-dose aspirin with MOBIC may result in an increased rate of GI ulceration or other complications, compared to use of MOBIC alone. MOBIC is not a substitute for aspirin for cardiovascular prophylaxis.
Cholestyramine
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. This suggests the existence of a recirculation pathway for meloxicam in the gastrointestinal tract. The clinical relevance of this interaction has not been established.
Cimetidine
Concomitant administration of 200 mg cimetidine QID did not alter the single-dose pharmacokinetics of 30 mg meloxicam.
Digoxin
Meloxicam 15 mg once daily for 7 days did not alter the plasma concentration profile of digoxin after b-acetyldigoxin administration for 7 days at clinical doses. In vitro testing found no protein binding drug interaction between digoxin and meloxicam.
Furosemide
Clinical studies, as well as post-marketing observations, have shown that NSAIDs can reduce the natriuretic effect of furosemide and thiazide diuretics in some patients. This effect has been attributed to inhibition of renal prostaglandin synthesis. Studies with furosemide agents and meloxicam have not demonstrated a reduction in natriuretic effect. Furosemide single and multiple dose pharmacodynamics and pharmacokinetics are not affected by multiple doses of meloxicam. Nevertheless, during concomitant therapy with furosemide and MOBIC, patients should be observed closely for signs of declining renal function, as well as to assure diuretic efficacy.
Lithium
In clinical trials, NSAIDs have produced an elevation of plasma lithium levels and a reduction in renal lithium clearance. In a study conducted in healthy subjects, mean pre-dose lithium concentration and AUC were increased by 21% in subjects receiving lithium doses ranging from 804 to 1072 mg BID with meloxicam 15 mg QD as compared to subjects receiving lithium alone. These effects have been attributed to inhibition of renal prostaglandin synthesis by MOBIC. Patients on lithium treatment should be closely monitored when MOBIC is introduced or withdrawn.
Methotrexate
A study in 13 rheumatoid arthritis (RA) patients evaluated the effects of multiple doses of meloxicam on the pharmacokinetics of methotrexate taken once weekly. Meloxicam did not have a significant effect on the pharmacokinetics of single doses of methotrexate. In vitro, methotrexate did not displace meloxicam from its human serum binding sites.
Warfarin
Anticoagulant activity should be monitored, particularly in the first few days after initiating or changing MOBIC therapy in patients receiving warfarin or similar agents, since these patients are at an increased risk of bleeding. The effect of meloxicam on the anticoagulant effect of warfarin was studied in a group of healthy subjects receiving daily doses of warfarin that produced an INR (International Normalized Ratio) between 1.2 and 1.8. In these subjects, meloxicam did not alter warfarin pharmacokinetics and the average anticoagulant effect of warfarin as determined by prothrombin time. However, one subject showed an increase in INR from 1.5 to 2.1. Caution should be used when administering MOBIC with warfarin since patients on warfarin may experience changes in INR and an increased risk of bleeding complications when a new medication is introduced.
PMS-meloxicam Contraindications
MOBIC is 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. Severe, rarely fatal, anaphylactic-like reactions to NSAIDs have been reported in such patients.
Additional information about PMS-meloxicam
PMS-meloxicam Indication: For the treatment of arthritis and osteoarthritis.
Mechanism Of Action: Anti-inflammatory effects of meloxicam are believed to be due to inhibition of prostaglandin synthetase (cylooxygenase), 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.
Drug Interactions: Anisindione PMS-meloxicam increases the anticoagulant effect
Dicumarol PMS-meloxicam increases the anticoagulant effect
Acenocoumarol PMS-meloxicam increases the anticoagulant effect
Warfarin PMS-meloxicam increases the anticoagulant effect
Lithium PMS-meloxicam increases serum levels of lithium
Food Interactions: Take without regard to meals.
Generic Name: Meloxicam
Synonyms: Meloxicamum [latin]
Drug Category: Analgesics; Antineoplastic Agents; Antiemetics; Nonsteroidal Antiinflammatory Agents (NSAIDs); Cyclooxygenase Inhibitors; Growth Inhibitors
Drug Type: Small Molecule; Approved
Other Brand Names containing Meloxicam: Mobic; Mobicox; Movalis; Movatec; Novo-meloxicam; PHL-meloxicam; PMS-meloxicam; Parocin; Ratio-meloxicam; Tenaron; Metacam; Gen-meloxicam; Dom-meloxicam; Co Meloxicam; Apo-meloxicam;
Absorption: 89%
Toxicity (Overdose): LD50, Acute: 84 mg/kg (Rat); Oral 470 mg/kg (Mouse); Oral 320 mg/kg (Rabbit)
Protein Binding: 99.4%
Biotransformation: Hepatic
Half Life: 15-20 hours
Dosage Forms of PMS-meloxicam: Tablet Oral
Chemical IUPAC Name: (3E)-3-[hydroxy-[(5-methyl-1,3-thiazol-2-yl)amino]methylidene]-2-methyl-1,1-dioxobenzo[e]thiazin-4-one
Chemical Formula: C14H13N3O4S2
Meloxicam on Wikipedia: https://en.wikipedia.org/wiki/Meloxicam
Organisms Affected: Humans and other mammals
