Mecelxib
Mecelxib Uses, Dosage, Side Effects, Food Interaction and all others data.
Mecelxib is a nonsteroidal anti-inflammatory drug that exhibits anti-inflammatory, analgesic and antipyretic activities. The mechanism of action of Mecelxib is believed to be due to inhibition of prostaglandin synthesis, primarily via inhibition of cyclooxygenase-2 (COX-2) and at therapeutic concentrations in humans, Mecelxib does not inhibit the cyclooxygenase-1 (COX-1) isoenzyme.
Mecelxib inhibits cyclooxygenase 2 (COX-2) enzyme, reducing pain and inflammation. It is important to note that though the risk of bleeding with celecoxib is lower than with certain other NSAIDS, it exists nonetheless and caution must be observed when it is administered to those with a high risk of gastrointestinal bleeding.
A note on the risk of cardiovascular events
Significant concerns regarding the safety of COX-2 selective NSAIDs emerged in the early 2000s. Rofecoxib, another member of the COX-2 inhibitor drug class, also known as Vioxx, was withdrawn from the market due to prothrombotic cardiovascular risks. Following an FDA Advisory Committee meeting in 2005, in which data from large clinical outcome trials were evaluated, the FDA concluded that the risk for cardiovascular thrombotic events for both COX-2 selective NSAIDs and nonselective NSAIDs was evident. It was determined that the benefits of celecoxib treatment, however, outweighed the risks. Postmarketing cardiovascular outcomes trial (PRECISION) revealed that the lowest possible dose of celecoxib was similar in cardiovascular safety to moderate strength doses of both naproxen and ibuprofen. Patients who had previous cardiovascular events including acute MI, coronary revascularization, or coronary stent insertion were not evaluated in the trial. It is not advisable to administer NSAIDS to these groups of patients.
| Trade Name | Mecelxib |
| Availability | Prescription only |
| Generic | Celecoxib |
| Celecoxib Other Names | Celecoxib, Célécoxib, Celecoxibum |
| Related Drugs | Humira, Ubrelvy, Buprenex, Botox, aspirin, prednisone, ibuprofen, acetaminophen, tramadol, meloxicam |
| Type | |
| Formula | C17H14F3N3O2S |
| Weight | Average: 381.372 Monoisotopic: 381.075882012 |
| Protein binding | The protein binding of celecoxib is 97%, and it is primarily bound to albumin. |
| Groups | Approved, Investigational |
| Therapeutic Class | Drugs for Osteoarthritis, Drugs used for Rheumatoid Arthritis, Non-steroidal Anti-inflammatory Drugs (NSAIDs) |
| Manufacturer | |
| Available Country | Vietnam |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Mecelxib used for relief of the signs and symptoms of osteoarthritis, for relief of the signs and symptoms of rheumatoid arthritis; for relief of pain after dental extraction; for reduction of colorectal polyps in Familial Adenomatous Polyposis (FAP)
Mecelxib is also used to associated treatment for these conditions: Ankylosing Spondylitis (AS), Osteoarthritis (OA), Pain, Acute, Primary Dysmenorrhoea, Rheumatoid Arthritis, Rheumatoid Arthritis, Juvenile
How Mecelxib works
Unlike most NSAIDs, which inhibit both types of cyclooxygenases (COX-1 and COX-2), celecoxib is a selective noncompetitive inhibitor of cyclooxygenase-2 (COX-2) enzyme. COX-2 is expressed heavily in inflamed tissues where it is induced by inflammatory mediators. The inhibition of this enzyme reduces the synthesis of metabolites that include prostaglandin E2 (PGE2), prostacyclin (PGI2), thromboxane (TXA2), prostaglandin D2 (PGD2), and prostaglandin F2 (PGF2). Resultant inhibition of these mediators leads to the alleviation of pain and inflammation.
By inhibiting prostaglandin synthesis, non-steroidal anti-inflammatory drugs (NSAIDs) cause mucosal damage, ulceration and ulcer complication throughout the gastrointestinal tract. Mecelxib poses less of an ulceration risk than other NSAIDS, owing to its decreased effect on gastric mucosal prostaglandin synthesis when compared to placebo.
Mecelxib exerts anticancer effects by binding to the cadherin-11 (CDH11)protein, which is thought to be involved in the progression of tumors, and inhibiting the 3-phosphoinositide-dependent kinase-1 (PDK-1) signaling mechanism. In addition, celecoxib has been found to inhibit carbonic anhydrase enzymes 2 and 3, further enhancing its anticancer effects.
As mentioned in the pharmacodynamics section of this drug entry, celecoxib may cause an increased risk of thrombotic events. The risk of thrombosis resulting from COX-2 inhibition is caused by the vasoconstricting actions of thromboxane A2, leading to enhanced platelet aggregation, which is uncontrolled when the actions of prostacyclin, a platelet aggregation inhibitor, are suppressed through the inhibition of COX-2.
Dosage
Mecelxib dosage
Osteoarthritis: The recommended oral dose is 200 mg per day administered as a single dose or as 100 mg twice daily.
Rheumatoid arthritis: The recommended oral dose is 100 to 200 mg twice daily.
Familial adenomatous polyposis (FAP): The recommended oral dose is 400 mg twice daily to be taken with food.
Dental pain: Single dose of Mecelxib 100 mg to400 mg
Side Effects
Gastrointestinal side effects include abdominal pain, diarrhoea, dyspepsia, flatulence and nausea. Central nervous system side effects include dizziness, headache and insomnia. Other side effects include upper respiratory tract infection, skin rash, back pain and peripheral edema.
Toxicity
The oral TDLo in humans 5.71 mg/kg.
It is not advisable to administer celecoxib in patients with renal impairment or advanced hepatic impairment, as this may lead to increased serum concentrations, causing toxicity. Symptoms of overdose may include breathing difficulties, coma, drowsiness, gastrointestinal bleeding, high blood pressure, kidney failure, nausea, sluggishness, stomach pain, and vomiting. Because serious gastrointestinal tract ulceration and bleeding can occur without preceding symptoms, patients should be monitored for signs/symptoms of gastrointestinal bleeding. Symptomatic and supportive measures should be taken in a celecoxib overdose. The induction of emesis or administration of active charcoal should take place if the patient is seen within 4 hours of celecoxib ingestion. Diuresis, urinary alkalinization, hemodialysis, or hemoperfusion may not be useful in a celecoxib overdose due to its high level of protein binding.
Precaution
Mecelxib cannot be expected to substitute for corticosteroids or to treat corticosteroid insufficiency. Patients on prolonged corticosteroid therapy should have their therapy tapered slowly if a decision is made to discontinue corticosteroids. Mecelxib should be prescribed with extreme caution in patients with a prior history of G.I. ulcer-disease or G.I. bleeding, hepatic and renal insufficiency, heart failure, those taking diuretics and ACE inhibitors, pre-existing asthma, elderly patients.
Interaction
Furosemide: NSAIDs can reduce the matriuretic effect of furosemide and thiazides in some patients.
Fluconazole: Concomitant administration of fluconazole at 200 mg QD resulted in a two-fold increase in celecoxib plasma concentration.
Warfarin: Caution should be exercised when administering Mecelxib with warfarin since these patients are at increased risk of bleeding complications.
Food Interaction
- Avoid alcohol. Alcohol increases the risk of gastrointestinal irritation.
- Avoid multivalent ions. Separate the administration of aluminum and magnesium containing drugs by several hours.
- Take with or without food. Doses up to 200 mg can be taken without regard to food, but doses of 400mg or higher should be taken with food.
Mecelxib Hypertension interaction
[Moderate] Nonsteroidal anti-inflammatory drugs (NSAIDs), including topicals, can lead to new onset of hypertension or worsening of preexisting hypertension, either of which can contribute to the increased incidence of cardiovascular events.
NSAIDs should be used with caution in patients with hypertension.
Blood pressure should be monitored closely during the initiation of NSAID therapy and throughout the course of therapy.
Mecelxib Drug Interaction
Moderate: duloxetine, duloxetine, metoprolol, metoprololUnknown: omega-3 polyunsaturated fatty acids, omega-3 polyunsaturated fatty acids, pregabalin, pregabalin, acetaminophen, acetaminophen, acetaminophen, acetaminophen, cyanocobalamin, cyanocobalamin, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol, cetirizine, cetirizine
Mecelxib Disease Interaction
Major: asthma, GI toxicity, rash, renal toxicities, thrombosisModerate: anemia, heart failure, hepatotoxicity, hyperkalemia, hypertension
Volume of Distribution
The apparent volume of distribution of celecoxib at steady state (Vss/F) is about 429 L, which suggests wide distribution into various tissues. Mecelxib is not preferentially bound to red blood cells. Another resource reports a volume of distribution of 455 ± 166L.
Elimination Route
Mecelxib is absorbed rapidly in the gastrointestinal tract. When a single oral dose of 200 mg was given to healthy research subjects, the peak plasma levels of celecoxib occurred within 3 hours. The Cmax is 705 ng/mL. When multiple doses are given, steady-state concentrations are reached on or before day 5. When taken with a high-fat meal, peak plasma levels are delayed for about 1 to 2 hours with an increase in total absorption (AUC) of 10% to 20%. The AUC of celecoxib has been shown to be significantly lower in patients with chronic renal impairment. A meta-analysis of pharmacokinetic studies has suggested an approximately 40% higher AUC (area under the curve) of celecoxib in black patients compared to Caucasians for unknown reasons.
Half Life
The effective half-life of celecoxib is approximately 11 hours when a single 200 mg dose is given to healthy subjects. The terminal half-life of celecoxib varies because of its low solubility, which prolongs absorption.
Clearance
Apparent clearance (CL/F), single oral 200 mg dose, healthy subjects = 27.7 L/hr. Clearance may be decreased by about 47% in patients with chronic renal insufficiency, according to a pharmacokinetic study. Studies have not been performed in patients with severe renal impairment.
Elimination Route
Mecelxib is primarily eliminated by hepatic metabolism with small amounts (12 About 57% of an oral dose of celecoxib is excreted in the feces and 27% is found to be excreted into the urine in the form of metabolites. The main metabolite in urine and feces is identified as the carboxylic acid metabolite (73%). The amount of glucuronide in the urine is reported to be low.
Pregnancy & Breastfeeding use
Mecelxib should be used during pregnancy only if the potential benefit justifies the potential risk to fetus. But in late pregnancy Mecelxib should be avoided because it may cause premature closure of ductus arteriosus.
It is not known whether Mecelxib is excreted in human milk. Because many drugs are excreted in human milk and because of potential for serious adverse reactions in nursing infants from Mecelxib, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
Contraindication
Mecelxib is contraindicated in patients with known hypersensitivity to Mecelxib, who have demonstrated allergic type reactions to sulfonamide or who have experienced asthma, urticaria or allergic type reactions after taking aspirin or other NSAIDs.
Special Warning
Geriatric: Dose adjustment in the elderly is not generally necessary. However, for patients of less than 50 kg in body weight, initiate therapy at the lowest recommended dose.
Paediatric: The safety and efficacy of Mecelxib is not established in paediatric patients.
Hepatic insufficiency: Mecelxib should be introduced at a reduced dose in patients with moderate hepatic impairment. The use of Mecelxib in patients with severe hepatic impairment is not recommended.
Acute Overdose
Patients should be managed by symptomatic and supportive care following an NSAID overdose. No specific antidote is available.
Storage Condition
Store at 15 to 30° C.
Innovators Monograph
You find simplified version here Mecelxib
Mecelxib contains Celecoxib see full prescribing information from innovator Mecelxib Monograph, Mecelxib MSDS, Mecelxib FDA label
FAQ
What is Mecelxib used for?
It is used to treat the pain and inflammation in osteoarthritis, acute pain in adults, rheumatoid arthritis, ankylosing spondylitis, painful menstruation, and juvenile rheumatoid arthritis.
How safe is Mecelxib?
Mecelxib is no less safe than two other non-opioid painkillers. A prescription painkiller that has been under a cloud for more than a decade is apparently safer than previously believed, a Food and Drug Administration panel concluded Wednesday.
How does Mecelxib work?
Mecelxib works by stopping the body's production of a substance that causes pain and inflammation.
What are the common side effects of Mecelxib?
Common side effects of Mecelxib are include:
- stomach pain, heartburn, gas, diarrhea, constipation, nausea, vomiting;
- swelling in your hands or feet;
- dizziness; or.
- cold symptoms such as stuffy nose, sneezing, sore throat.
Is Mecelxib safe during pregnancy?
Mecelxib should not be used during pregnancy. Women who could get pregnant should use an effective method of contraception to prevent pregnancy while taking Mecelxib. If you think you could be pregnant, stop taking Mecelxib and consult your doctor.
Is Mecelxib safe during breastfeeding?
Because of the low levels of Mecelxib in breastmilk, amounts ingested by the infant are small and would not be expected to cause any adverse effects in breastfed infants. No special precautions are required.
Can I drink alcohol with Mecelxib?
Alcohol should be avoided if taking Mecelxib, in particular, because the medication already causes a higher risk of cardiovascular side effects, such as heart attacks and strokes, and alcohol increases that risk.
Can I drive after taking Mecelxib?
If you become drowsy, dizzy or light-headed after taking Mecelxib, do not drive or operate machinery.
Is Mecelxib used for back pain?
Mecelxib treats the pain, inflammation, and stiffness.
Is Mecelxib bad for kidneys?
Clinical Inquiry concludes that Mecelxib does not appear to worsen renal function, it should still be used with caution for patients who are elderly, hospitalized, or at risk of developing serious complications such as acute renal failure, heart failure, and gastrointestinal bleeding.
Can Mecelxib make me sleepy?
Mecelxib oral capsule does not cause drowsiness, but it can cause other side effects.
Is it safe to take Mecelxib every day?
Mecelxib may be taken at any time without regard to meals, particularly with lower doses (such as up to 200 mg twice daily). Higher doses (such as 400 mg twice daily) should be taken with food to reduced stomach upset.
How long does Mecelxib stay in my system?
The half-life of Mecelxib is about 11 to 12 hours which means that it is expelled from the body within about 2 1/2 to 3 days after discontinuing the medicine.
What is the best time of day to take Mecelxib?
Mecelxib may be taken at any time without regard to meals, particularly with lower doses (such as up to 200 mg twice daily). Higher doses (such as 400 mg twice daily) should be taken with food to reduced stomach upset.
How often can I take Mecelxib?
Mecelxib capsules are usually taken once or twice a day.
How long does Mecelxib take to work?
Mecelxib takes approximately 3 hours after oral administration to reach peak concentrations. The pain-relieving effects of Mecelxib last for approximately 12 hours.
How long does Mecelxib stay in my system?
The half-life of Mecelxib is about 11 to 12 hours which means that it is expelled from the body within about 2 1/2 to 3 days after discontinuing the medicine.
Can I take Mecelxib for a long time?
For safe and effective use of this Mecelxib, do not take more of it, do not take it more often, and do not take it for a longer time than your doctor ordered.
Who should not take Mecelxib?
You should not take Mecelxib if you have high blood pressure, a heart attack, chronic heart failure, abnormal bleeding in the brain resulting in damage to brain tissue, called a hemorrhagic stroke.
What happen If I missed dose of Mecelxib?
If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.
What happen if I take too much Mecelxib?
If you take too much Mecelxib call your healthcare provider or local Poison Control Center, or seek emergency medical attention right away. If Mecelxib is administered by a healthcare provider in a medical setting, it is unlikely that an overdose will occur. However, if overdose is suspected, seek emergency medical attention.
What happens if I suddenly stop taking Mecelxib?
Suddenly stopping your treatment with Mecelxib may lead to your symptoms getting worse. Do not stop taking Mecelxib unless your doctor tells you to. Your doctor may tell you to reduce the dose over a few days before stopping completely.
Can Mecelxib affect my heart?
Risk of heart failure may be lower with Mecelxib than with other NSAIDs.
Can Mecelxib affects my liver?
Mecelxib use liver problems, such as liver damage, hepatitis, and liver failure. These problems can affect how well your liver works. On rare occasions, liver problems can be fatal.
