Celecoxib

What is a Celecoxib?

Celecoxib is a medication that belongs to the class of drugs known as nonsteroidal anti-inflammatory drugs (NSAIDs). It is commonly prescribed to treat pain and inflammation associated with conditions such as osteoarthritis, rheumatoid arthritis, and ankylosing spondylitis.

Celecoxib works by inhibiting the production of prostaglandins, which are substances that play a role in the development of pain, inflammation, and fever. By blocking the action of prostaglandins, celecoxib can help to relieve pain, reduce inflammation, and lower fever.

Celecoxib is available in various strengths and forms, including capsules and tablets. The dosage and duration of treatment may vary depending on the specific condition being treated and the individual’s response to the medication.

As with all medications, celecoxib may cause side effects. Common side effects include stomach upset, nausea, vomiting, diarrhea, and headache. Rare but serious side effects may include gastrointestinal bleeding, liver damage, and cardiovascular events. It is important to discuss any potential risks and benefits of celecoxib with a healthcare provider before starting treatment.

Description

Celecoxib is a COX-2 inhibitor and nonsteroidal anti-inflammatory medication that is sold under the brand names Celebrex and others. It is utilized to treat mild to moderate pain and assist relieve symptoms of arthritis (eg, osteoarthritis, rheumatoid arthritis, or juvenile rheumatoid arthritis), such as inflammation, swelling, stiffness, and joint pain. Nevertheless, this restorative does not cure arthritis and will help you only as long as you restart taking it. Celecoxib is also employed to regale ankylosing spondylitis, which is a kind of arthritis that involves the joints in the spine of the human being. This medicine may also be used to feast acute pain and menstrual cramps. Celecoxib is also employed to treat acute migraine headaches with or without aura. Regardless, this drug is not used to control migraines. This drug is unrestricted only with your doctor’s prescription.

This consequence is available in the subsequent dosage forms:

• Capsule
• Solution

• ChemSpider ID: 2562
• ChEMBL Id: 118
• IUPHAR ID: 2892
• Pronunciation: /sɛlɪˈkɒksɪb/ SEL-i-KOK-sib
• Pregnancy category: : AU: B3;
• Metabolism: Liver (mainly CYP2C9)
• Routes of administration: By mouth
• Brand names – Celebrex®, Elyxyb®

Background

Celecoxib, a selective cyclooxygenase-2 (COX-2) inhibitor, is a nonsteroidal anti-inflammatory drug (NSAID) that is known for its decreased risk of causing gastrointestinal bleeding compared to other NSAIDs. It is utilized to manage symptoms of different styles of arthritis affliction and in family adenomatous polyposis (FAP) to reduce precancerous polyps in the colon. It is notable by Pfizer under the trademark name Celebrex and/or was initially granted Food and Drug Administration approval in 1998.

What is Celecoxib (Celebrex®)?

Celecoxib is generally known by the brand name Celebrex®. Celecoxib (Sell-e-COX-eb) is employed to lessen a few symptoms rendered by arthritis, such as inflammation, swelling, stiffness, and also joint ache. Yet, this cure does not cure arthritis and will help you only as long as you resume taking it.

How do I take it?

Celecoxib is taken once or twice a day. The pills are 100 or 200mg. each. The characteristic dose is 200 to 400 mg. per day. This drug is utilized for both rheumatoid arthritis and osteoarthritis. Your medic will advise you on how many pills to take and how often. Observe your doctor’s directions. For the best outcomes, take these pills at the same time every day. Do not take more or fewer drugs than ordered. This medicine might also be taken with or without food.

Celecoxib is less likely to induce stomach upset and ulcers than NSAIDS. However, in a few cases, patients have complained of upset stomachs, indigestion, or diarrhea. Stomach difficulties may be more likely to occur if you drink alcoholic beverages while being feasted with this medicine. If you have Comprehended allergy to sulfa drugs, Do not take this drug until you talk to your doctor. 

Mechanism of Action of Celecoxib

Contrasting most Nonsteroidal anti-inflammatory pharmaceuticals, which inhibit both types of categories of cyclooxygenases (COX-1 and COX-2), celecoxib is an exacting noncompetitive inhibitor of the cyclooxygenase-2 (COX-2) enzyme. COX-2 is illustrated heavily in inflamed tissues where it is induced by the inflammatory arbitrator. The inhibition of this enzyme lessens the synthesis of metabolites that possess prostaglandin E2 (PGE2), prostacyclin (PGI2), thromboxane (TXA2), prostaglandin D2 (PGD2), and prostaglandin F2 (PGF2). Consequential inhibition of these mediators guides the alleviation of pain and inflammation.

By inhibiting prostaglandin synthesis, non-steroidal anti-inflammatory drugs (NSAIDs) cause mucosal injury, ulceration, and ulcer complication throughout the gastrointestinal tract. Celecoxib poses more unreasonable ulceration trouble than other NSAIDs, owing to its diminished effect on gastric mucosal prostaglandin synthesis when compared to a placebo. Celecoxib wields anticancer effects by binding to the cadherin-11 (CDH11)protein, which is thought to be affected in the progression of tumors, and inhibiting the 3-phosphoinositide-dependent kinase-1 (PDK-1) signaling mechanism. In proliferation, celecoxib has been found to inhibit carbonic anhydrase enzymes 2 and 3, further improving its anticancer effects.

As cited in the pharmacodynamics excerpt of this medication entry, celecoxib might also generate an improved chance of thrombotic events. The risk of thrombosis resulting from COX-2 inhibition is induced 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 repressed through the inhibition of COX-2. Celecoxib is biochemically set as 4-[5-(4-methylphenyl)- 3-(trifluoromethyl)-1H-pyrazol-1-yl] benzenesulfonamide and is a diaryl-substituted pyrazole. The mechanism of action of celecoxib is due to the selective inhibition of cyclooxygenase-2 (COX-2), which is accountable for prostaglandin synthesis, an integral part of the pain and inflammation pathway. This pharmacologic activity gives celecoxib its analgesic, anti-inflammatory, and antipyretic results. Celecoxib ailing inhibits COX-1 and, therefore, may also affect platelet function less than aspirin.

Celecoxib also has anticancer properties concerned below and exerts its anticancer properties by binding cadherin-11 (CDH11), which likely plays an important role in the malignant progression of cancerous cells. Celecoxib is extensively metabolized through cytochrome P450 2C9 (CYP2C9) and may also have interchanges with other medications that are substrates of CYP2C9.

Structure-activity relationship

The Searle analysis corporation located the two suitably covered aromatic rings that must reside on adjacent functions about the central ring for acceptable COX-2 inhibition. Various modifications can also be made to the 1,5-diaryl pyrazole moiety to extrapolate the structure-activity relationship of celecoxib. A para-sulfamoyl phenyl at connection 1 of the pyrazole was found to have a better-elevated strength for COX-2 selective inhibition than a para-methoxyphenyl (see structures 1 and 2, beneath). In acquisition, a 4-(methylsulfonyl)phenyl or 4-sulfamoyl phenyl is known to be necessary for COX-2 inhibition. For representative, replacing either of these entities with a –SO2NHCH3 substituent dwindles COX-2 inhibitory activity as noted with a very high inhibitory concentration-50 (see structures 3 – 5). At the 3-position of the pyrazole, a trifluoromethyl or difluoromethyl furnishes superior selectivity and potency compared to a fluoromethyl or methyl substitution (see structures 6 – 9).

Celecoxib is incorporated 22; the 4-sulfamoylphenyl on the 1-pyrazole substituent is required for COX-2 inhibition and the 4-methyl on the 5-pyrazol technique has a lower steric impediment to maximizing force, while the 3-trifluoromethyl group supplies superior selectivity and/or potency. To elucidate the selectivity of celecoxib, it is needed to examine the free energy of binding discrepancy between the drug molecule and COX-1 corresponding to COX-2 enzymes. The structural modifications highlight the importance of binding to remains 523 in the side binding pocket of the cyclooxygenase enzyme, which is isoleucine in COX-1 and valine in COX-2. This variation arises to contribute to COX-2 selectivity by begetting a steric obstacle between the sulfonamide oxygen and the methyl group of Ile523 that destabilizes the celecoxib-COX-1 complex.

Pharmacodynamics

Celecoxib inhibits the cyclooxygenase 2 (COX-2) enzyme, relieving pain and inflammation. It is essential to note that though the risk of bleeding with celecoxib is more subordinate than with certain other NSAIDS, it exists nonetheless and caution must be observed when it is administered to those with a high chance of gastrointestinal bleeding.

A missive on the risk of cardiovascular events

Consequential circumstances regarding the safety of COX-2 selective NSAIDs emerged in the early 2000s. Rofecoxib, another component of the COX-2 inhibitor drug category, also known as Vioxx, was withdrawn from the market due to prothrombotic cardiovascular risks. Following a Food and Drug Administration Advisory Committee meeting in 2005, in which data from large clinical outcome trials were evaluated, the Food and Drug Administration terminated that the chance for cardiovascular thrombotic occasions for both COX-2 selective Nonsteroidal anti-inflammatory drugs and nonselective NSAIDs was evident. It was determined that the advantages of celecoxib treatment, however, outweighed the risks. The postmarketing cardiovascular consequences trial (PRECISION) revealed that the lowest possible dose of celecoxib was comparable in cardiovascular safety to moderate strength doses of both naproxen and ibuprofen. Patients who had earlier cardiovascular events including acute MI, coronary revascularization, and/or coronary stent insertion were not evaluated in the trial. It is not advisable to distribute NSAIDs to these groups of patients.

Absorption

Celecoxib is absorbed rapidly in the gastrointestinal tract. When a specific oral dose of 200 mg was given to healthy investigation subjects, the peak plasma levels of celecoxib occurred within 3 hours. The Cmax is 705 ng/mL. When numerous doses are given, steady-state engagements are reached on or before day 5. When tolerated with a high-fat meal, peak plasma levels are postponed for about 1 to 2 hours with an increase in total absorption (AUC) of 10% to 20%. The AUC of celecoxib is extremely lower in patients with chronic renal impairment. A meta-analysis of pharmacokinetic studies has suggested a roughly 40% higher AUC (area under the curve) of celecoxib in black patients corresponded to Caucasians for unknown motivations.

Volume of distribution

The conspicuous magnitude of diffusion of celecoxib at steady state (Vss/F) is about 429 L, which proposes wide diffusion into various tissues. Celecoxib is not preferentially attached to red blood cells. Another help conveys a volume of distribution of 455 ± 166L.

Protein binding

The protein binding of celecoxib drug is 97%, and it is especially affixed to albumin.

Metabolism

A broader part of celecoxib metabolism is mediated by cytochrome P450 2C9 in the liver with few contributions from CYP3A4 and CYP2C8 and/or possible contributions from CYP2D6. It is assimilated by biotransformation to carboxylic acid and/or glucuronide metabolites. Three metabolites, introductory alcohol, a carboxylic acid, and a glucuronide conjugate, have been encountered in human plasma after celecoxib administration. These are deemed inactive metabolites concerning COX enzyme inhibition. Patients who are understood or presumed to have decreased cytochrome P450 2C9 activity or function, based on their previous history, should be allocated celecoxib with warning as they may also have abnormally high serum concentrations resulting from reduced metabolism celecoxib.

Route of elimination

Celecoxib is primarily got rid of by hepatic metabolism with small amounts (<3%) of the unchanged drug found in both the urine and feces. 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.

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 on patients with severe renal impairment.

What about other medications?

When you are taking Celecoxib, your doctors must know if you are taking any other medicine. This includes pill and non-prescription medicines as well as vitamins and/or herbal supplements. Celecoxib can also be taken with other remedies, however, it is best to have your doctor’s recommendation before adding another drug to your day-to-day routine.

Administration of celecoxib

Celecoxib is a pill accepted orally and comes in 50, 100, 200, and 400 mg doses. In occasional cases, celecoxib can also be added to customized combinations for topical administration with or without the use of iontophoresis or other topical delivery instruments. It is not known via any other route of administration.

Dosing for approved indications is as follows:

• Osteoarthritis: 200 mg orally daily, or 100 mg twice daily.
• Rheumatoid Arthritis: 100 to 200 mg by mouth doubled daily, utilizing the lowest effective dose.
• Ankylosing Spondylitis: 200 mg by mouth daily. Dosing can increase to 400 mg. Always utilize the lowest effective dose for the shortest possible therapy duration. Prescribers should believe in discontinuing the drug if there is no reaction at the highest dose after six weeks.
• Dysmenorrhea: 200 mg by mouth twice daily. Dosing can increase to 400 mg. Always utilize the lowest effective dose for the shortest possible therapy duration. Prescribers should believe in discontinuing the pill if there is no response at the highest dose after six weeks.
• Acute Pain: 200 mg orally creased daily; patients can also start with 400 mg for a single dose on day one of treatment, with a supplementary 200 mg on the first day if necessary.

All doses should be given with food if GI upset happens. In patients who are deficient in CYP2C9 metabolizers, consider starting at 50% of the lowest dose. Avoid usage in renal impairment of creatinine clearance is less than 30 mL/s. Also, bypass use in hepatic insufficiency if the patient is Child-Pugh Class C.

Continuing Education Activity

The Food and Drug Administration suggests celecoxib and other NSAIDs (non-steroidal anti-inflammatory drugs), along with acetaminophen, as first-line painkillers for patients with osteoarthritis and rheumatoid arthritis. Celecoxib also has a Food and Drug Administration movement for the management of acute pain in adult women and primary dysmenorrhea. Similarly, the Food and Drug Administration also recommends utilizing celecoxib as an adjunct therapy in patients with household adenomatous polyposis to reduce the number of colorectal polyps. This activity examines the mechanism of action, damaging event profile, toxicity, dosing, pharmacodynamics, and monitoring of celecoxib, pertinent for clinicians and other interprofessional group members to allow for fitting utilization of celecoxib.

Objectives:

• Outline the mechanism of action of celecoxib.
• Remember the approved and off-label indications for celecoxib.
• Summarize the potential adverse effects of celecoxib.
• Establish interprofessional group processes for improving care coordination and contact to determine the appropriateness of celecoxib in the clinical background.

Important Warning:

Someone who takes nonsteroidal anti-inflammatory drugs (NSAIDs) (other than aspirin) such as celecoxib might also have a more elevated likelihood of carrying a heart attack or a stroke than people who do not take these medications. These possibilities might also happen without warning and may induce death. This chance may be higher for individuals who take NSAIDs for a long time. Do not take a Nonsteroidal anti-inflammatory drug such as celecoxib if you have newly had a heart attack unless instructed to do so by your medic. Inform your doctor if you or anyone in your family has or has ever had a heart disorder, a heart attack, or a stroke if you smoke and if you have or have ever had advanced cholesterol, high blood tension, and/or diabetes. Get emergency medical assistance right away if you encounter any of the following symptoms: chest ache, shortness of breath, weakness in one part or side of the body, or slurred speech. If you will be confronting a coronary artery bypass graft (CABG; a style of heart surgery), you must not take the celecoxib tablet right before or immediately after the surgery.

Nonsteroidal anti-inflammatory medications such as celecoxib may also induce ulcers, bleeding, or holes in the stomach or intestine. These tribulations might develop at any time during medicine, may happen without warning symptoms, and may also cause death. The opportunity may be higher for individuals who take NSAIDs for a lengthy time, are older, have poor health, or drink large amounts of alcohol while taking celecoxib. Convey your medic if you drink considerable quantities of alcohol or if you take any of the subsequent medications: anticoagulants (‘blood thinners’) such as warfarin (Coumadin, Jantoven); aspirin; other Nonsteroidal anti-inflammatory drugs such as ibuprofen (Advil, Motrin) or naproxen (Aleve, Naprosyn); and also verbal steroids like dexamethasone, methylprednisolone (Medrol), and also prednisone (Rayos); selective serotonin reuptake inhibitors (SSRIs) such as citalopram (Celexa), and also fluoxetine (Prozac, Sarafem, in Symbyax), fluvoxamine (Luvox), paroxetine (Brisdelle, Paxil, Pexeva), and sertraline (Zoloft); or serotonin-norepinephrine reuptake inhibitors (SNRIs) such as desvenlafaxine (Pristiq), duloxetine (Cymbalta), and venlafaxine (Effexor XR). Also, inform your medic if you have or have ever had also ulcers and/or bleeding in your stomach and/or intestines and/or other bleeding disorders. If you participate any of the subsequent symptoms, bypass taking the celecoxib drug and talk to your medic about stomach pain, heartburn, vomiting a substance that is bloody and/or looks such like coffee bases, blood in the stool, or black and/or tarry stools.

Maintain all interpretations with your medic and the laboratory. Your medic will monitor your symptoms carefully and will presumably order certain ordeals to check your body’s response to celecoxib. Be sure to announce to your medic how you are feeling so that your medic can determine the right amount of medication to treat your disorder with the lowest risk of serious side effects. Your medic and/or apothecary will give you the manufacturer’s patient knowledge sheet (Medication Manual) when you start the remedy with celecoxib each time you supply your prescription. Read the details carefully and ask your doctor and/or apothecary if you have any questions. You could also visit the Food and Drug Administration (FDA) website or the manufacturer’s website to receive the Medication Guide.

Why is Celecoxib medication prescribed?

Celecoxib is utilized to reduce pain, tenderness, swelling, and stiffness induced by osteoarthritis (arthritis induced by a breakdown of the lining of the joints), rheumatoid arthritis (arthritis caused by swelling of the lining of the joints), and ankylosing spondylitis (arthritis that mainly involves the spine). Celecoxib is also used to regale juvenile rheumatoid arthritis (a sort of arthritis that affects children) in children 2 years of age and older. Celecoxib is also employed to treat painful menstrual periods and to lessen other types of short-term pain including pain induced by injuries, surgery, and other medical or dental procedures, or medical essentials that last for a limited time. Celecoxib is in a category of NSAIDs called COX-2 inhibitors. It works by stopping the body’s production of a sense that causes pain and inflammation.

How should this medicine be used?

Celecoxib arrives as a capsule to take by mouth. Celecoxib capsules are usually taken once or double a day. If you are taking up to 200 mg of celecoxib capsules at a period, you may also take the medication with or without food. If you are taking more than 200 mg of celecoxib capsules at a moment, you should take the medication with food. Ask your medic or pharmacist if you are not sure if you require to take your medication with food. To assist you remember to take celecoxib capsules, take them around the same time(s) every day.

Observe the directions on your prescription label, and ask your physician or pharmacist to explain any part you do not understand. Take celecoxib exactly as demanded. Do not take more or small of it or take it more often than prescribed by your doctor.

If you cannot swallow the tablets or if you are giving this medication to a child, you may also open the capsules and sprinkle the contents over a teaspoon of cold or room-temperature applesauce. You may organize the mixture in advance and store it for up to 6 hours in a refrigerator. When you are willing to take your medication, swallow all of the mixtures. Then consume water to wash down the mixture and be sure that you have swallowed all of it.

Medical uses

Celecoxib is indicated for the therapy of osteoarthritis, rheumatoid arthritis, acute ache, musculoskeletal pain, painful menstruation, ankylosing spondylitis, juvenile rheumatoid arthritis, and to lower the number of colon and rectal polyps in individuals with familial adenomatous polyposis. It may also be used in youngsters with juvenile rheumatoid arthritis who are more senior than two years of age and weigh more than 10 kg (22 lb).

For postoperative aches, it is more or less equal to ibuprofen. For pain relief, it is equal to paracetamol (acetaminophen), which is the first-line medicine for osteoarthritis.

Proof of effects is not clear as several studies done by the manufacturer have not been released for an independent analysis.

Indications of Celecoxib

Celecoxib has considerable indications, both FDA approved, and non-FDA approved. The Food and Drug Administration suggests celecoxib and other NSAIDs (non-steroidal anti-inflammatory drugs), along with acetaminophen, as first-line analgesics for patients with osteoarthritis and rheumatoid arthritis. Celecoxib also has a Food and Drug Administration indication for the management of acute pain in adult women and primary dysmenorrhea. Similarly, the FDA also recommends utilizing celecoxib as an adjunct therapy in patients with household adenomatous polyposis to reduce the number of colorectal polyps.

Off-label, celecoxib can be utilized for a wide variety of musculoskeletal and rheumatologic diseases, including ankylosing spondylitis, juvenile idiopathic arthritis, and gout. It is also being employed increasingly in hospital protocols as part of a multimodal perioperative pain managing regimen, and repeatedly given pre-operatively along with adjunct ache medications, including acetaminophen and/or pregabalin.

Other uses for this medicine

Celecoxib is also sometimes employed with surgery and other treatments to decrease the number of polyps (abnormal growths) in the colon (large intestine) and rectum in patients with family adenomatous polyposis (a disorder in which hundreds or thousands of polyps form in the colon and/or cancer may also develop). Talk to your medic about the chances of utilizing this medication for your condition.

This medication may also be prescribed for other usages; ask your physician or pharmacist for more details.

Contraindications of Celecoxib

Due to its cardiovascular risk, celecoxib is contraindicated for the treatment of perioperative aches in the location of coronary artery bypass graph (CABG) surgery.

Celecoxib also includes a sulfonamide group and is contraindicated in patients who have demonstrated extreme allergic responses to drugs with a sulfonamide group, e.g., sulfamethoxazole. Investigations have shown that allergies to sulfonamide antimicrobials are indeed a risk factor for allergic reactions to the sulfonamide chemical group. Non-antimicrobial drugs that include a sulfonamide chemical company such as celecoxib, a history of penicillin allergy is at least as strong a chance factor for an allergic reaction. Therefore, providers should comprehend that this phenomenon is probably not solely due to the cross-reactivity of sulfonamide-containing antimicrobials and non-antimicrobials and that individual patients have an improved tendency to celecoxib allergy if they are allergic to any antimicrobial medicine.

Since CYP2C9 metabolizes celecoxib, its use requires caution in patients taking medications that inhibit CYP2C9, for example, fluconazole, which is an antifungal drug. Like all Nonsteroidal anti-inflammatory drugs, celecoxib drug should not be taken after 29 weeks of gestation.

What special precautions should I follow?

Before taking celecoxib,

• tell your physician and pharmacist if you are allergic to celecoxib, aspirin, or other NSAIDs such as ibuprofen (Advil, Motrin) and naproxen (Aleve, Naprosyn), sulfa medications, any other medications, or any of the inactive ingredients in celecoxib capsules. Ask your apothecary for a list of the inactive ingredients.
• tell your doctor and apothecary what prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Be certain to note the medications listed in the IMPORTANT WARNING section and any of the following: angiotensin-converting enzyme (ACE) inhibitors such as benazepril (Lotensin, in Lotrel), captopril, enalapril (Epaned, Vasotec, in Vaseretic), fosinopril, lisinopril (Qbrelis, in Zestoretic), moexipril (Univasc), perindopril (Aceon, in Prestalia), quinapril (Accupril, in Quinaretic), ramipril (Altace), and trandolapril (in Tarka); angiotensin receptor blockers such as candesartan (Atacand, in Atacand HCT), eprosartan, irbesartan (Avapro, in Avalide), and/or losartan (Cozaar, in Hyzaar), olmesartan (Benicar, in Azor, in Benicar HCT, in Tribenzor), and also telmisartan (Micardis, in Micardis HCT, in Twynsta), and valsartan (Dioavan, in Entresto, in Exforge HCT); atomoxetine (Strattera); beta blockers such as atenolol (Tenormin, in Tenoretic), labetalol (Trandate), metoprolol (Kapspargo Sprinkle, Lopressor, Toprol XL, in Dutoprol), nadolol (Corgard, in Corzide), and propranolol (Hemangeol, Inderal, Innopran); cyclosporine (Gengraf, Neoral, Sandimmune); digoxin (Lanoxin); diuretics (‘water pills’); fluconazole (Diflucan); lithium (Lithobid); methotrexate (Otrexup, Rasuvo, Reditrex, Trexall); and pemtrexed (Alimta, Pemfexy). Your doctor might also require you to vary the doses of your medications and/or monitor you carefully for side effects. Substantial other medications or drugs may also interact with celecoxib drug, so be sure to tell your medic about all the medications you are taking, even those that do not occur on this list.
• tell your physician if you have and/or have ever had any of the conditions noted in the IMPORTANT WARNING section or asthma, especially if you also have frequent stuffed and/or runny nose or nasal polyps (swelling of the lining of the nose); swelling of the hands, arms, feet, ankles, or lower legs; heart neglect; or liver or kidney disorder.
• tell your doctor if you are pregnant, plan to become pregnant, and/or are breastfeeding. Celecoxib may damage the fetus and cause problems with delivery if it is taken around 20 weeks or thereafter during gestation. Do not take celecoxib drugs roughly or after 20 weeks of pregnancy, unless you are told to do so by your physician. If you become expectant while taking celecoxib, call your physician.
• if you are having surgery, including dental surgery, advise the physician or dentist that you are taking celecoxib.

What special dietary teachings should I follow?

Unless your physician tells you otherwise, resume your normal diet.

What should I do if I overlook a quantity?

If you are taking celecoxib, take the forgotten dose as soon as you remember it. Regardless, if it is nearly time for the next dose, bypass the missed dose and continue your regular dosing program. Do not take a dual dose to make up for a missed one.

What side effects can this medication cause?

Celecoxib may also cause side effects. Advise your medic if any of these symptoms are severe or do not go away:

• gas and/or bloating
• sore throat
• cold symptoms
• constipation
• dizziness
• dysgeusia

Some side effects can also be serious. If you participate any of the following symptoms or those mentioned in the IMPORTANT WARNING province, call your doctor immediately. Do not take any more celecoxib until you speak to your medic.

• unexplained weight gain
• shortness of breath or difficulty breathing
• swelling of the abdomen, feet, ankles, and/or lower legs
• diarrhea
• nausea
• excessive tiredness
• unusual bleeding or bruising
• itching
• lack of energy
• loss of appetite
• ache in the upper right part of the stomach
• yellowing of the skin or eyes
• flu-like symptoms
• blisters
• fever
• rash
• hives
• swelling of the face, throat, tongue, lips, eyes, and/or hands
• hoarseness
• difficulty swallowing or breathing
• pale skin
• fast heartbeat
• cloudy, discolored, or bloody urine
• back pain
• difficult or painful urination
• frequent urination, especially at night

Celecoxib may cause other side effects. Contact your medic if you have any unusual problems while you are taking this medication. If you encounter a serious side effect, you or your doctor may send a report to the Food and Drug Administration’s (FDA) MedWatch Adverse Event Reporting schedule online or by phone.

What should I know about the storage and disposal of this drug?

Preserve this medicine in the container it arrived in, tightly closed, and out of reach of children. Keep it at room temperature and away from excess heat and dampness (not in the bathroom).

It is important to maintain all the drugs out of sight and/or reach of juveniles as many receptacles (such as weekly pill minders and those for eye drops, creams, patches, and inhalers) are not child-resistant and young youngsters can open them smoothly. To rescue young children from poisoning, always lock safety caps and instantly place the medicine in a safe location – one that is up and away and out of sight and contact.

Unneeded medicines should be disposed of in special ways to ensure that pets, youngsters, and other people cannot consume them. Still, you should not flush this drug down the toilet. Rather, the best way to dispose of your drug is through a medicine take-back program. Convey to your pharmacist or contact your local garbage or recycling department to learn about take-back programs in your community. See the Food and Drug Administrations Safe Disposal of Medicines website for more details if you do not have access to a take-back program.

In case of an emergency or overdose

In point of overdose, contact the poison control helpline. Information is also available online. If the victim has tumbled, had a seizure, has trouble breathing, or can not be awakened, immediately reach emergency services.

Symptoms of overdose may include:

• lack of energy
• drowsiness
• nausea
• vomiting
• stomach pain
• vomiting fabric that is bloody or looks like coffee grounds
• bloody or black, tarry stools
• loss of consciousness
• hives
• rash
• swelling of the eyes, face, tongue, lips, throat, arms, hands, feet, ankles, and/or lower legs
• difficulty breathing or swallowing
• Cardiovascular events: NSAIDs are associated with an improved risk of serious (and potentially fatal) adverse cardiovascular thrombotic events, including myocardial infarction and stroke. The danger may also be increased with the duration of use or pre-existing cardiovascular risk factors or condition. Individual cardiovascular risk profiles should be evaluated before prescribing. New-onset hypertension or exacerbation of hypertension may arise (NSAIDs may impair response to thiazide or loop diuretics), and may contribute to cardiovascular events; monitor blood pressure and use with caution in patients with hypertension. May cause sodium and fluid retention, use it with caution in patients with edema or heart failure. The long-term cardiovascular threat in youngsters has not been evaluated. Utilize the lowest effective dose for the shortest duration of time, consistent with individual patient goals, to reduce the risk of cardiovascular events; alternative therapies should be considered for patients at high risk. The increased risk is about 37%.
• Gastrointestinal events: NSAIDs may increase the risk of serious gastrointestinal (GI) ulceration, bleeding, and perforation (may be fatal). These possibilities may happen at any time during therapy and without warning. Use warning with a history of GI disease (bleeding or ulcers), concurrent medicine with aspirin, anticoagulants and/or corticosteroids, smoking, and use of alcohol, the elderly or debilitated patients. Use the lowest effective dose for the shortest duration of time, consistent with individual patient goals, to reduce the risk of GI adverse events; alternate therapies should be considered for patients at high risk. When utilized concomitantly with ≤325 mg of aspirin, a substantial expansion in the risk of gastrointestinal complications (e.g., ulcer) occurs; concomitant gastroprotective therapy (e.g., proton pump inhibitors) is recommended. The increased risk is about 81%.
• Hematologic effects: Anemia may also occur; monitor hemoglobin or hematocrit in individuals on long-term treatment. Celecoxib does not usually affect prothrombin time, partial thromboplastin time, or platelet computations; it does not inhibit platelet aggregation at authorized doses.

Individuals with prior history of ulcer disease or GI bleeding require special precautions. Moderate to a severe liver impairment or GI toxicity can also occur with or without warning symptoms in somebody treated with NSAIDs.

In October 2020, the U.S. Food and Drug Administration (FDA) mandated the drug label to be updated for all nonsteroidal anti-inflammatory medications to explain the chance of kidney problems in unborn babies that result in low amniotic fluid. They suggest avoiding NSAIDs in pregnant women at 20 weeks and/or later in pregnancy.

Allergy

Celecoxib includes a sulfonamide moiety and may also cause allergic reactions in those allergic to other sulfonamide-containing drugs. This is in complement to the contraindication in people with severe allergies to other NSAIDs. Nevertheless, it has a low (reportedly 4%) chance of inducing cutaneous responses among persons who have a history of such responses to aspirin or nonselective NSAIDs. NSAIDs may cause serious skin adverse events, including exfoliative dermatitis, Stevens-Johnson syndrome, and toxic epidermal necrolysis; events may happen without warning and in patients without prior known sulfa allergy. Use should be discontinued at the foremost sign of rash (or any other hypersensitivity).

Heart attack and stroke

A 2013 meta-analysis of hundreds of clinical difficulties or issues found that coxibs (the style of drugs that includes celecoxib) improve the chances of major cardiovascular problems by approx 37% over placebo. In 2016, a randomized trial delivered strong evidence that therapy with celecoxib drug is not more likely to result in poor cardiovascular outcomes than treatment with naproxen and/or ibuprofen. As a repercussion, in 2018 an Food and Drug Administration advisory panel concluded that celecoxib drug poses no greater risk for inducing heart attacks and strokes than the commonly-used NSAIDs ibuprofen or naproxen and recommended that the FDA consider revising its advice to physicians regarding celecoxib’s safety.

The COX-2 inhibitor rofecoxib (Vioxx) was extracted from the market in 2004 due to its risk. Like all NSAIDs on the US market, celecoxib preserves an FDA-mandated “black box warning” for cardiovascular and gastrointestinal trouble. In February 2007, the American Heart Association warned that interesting “patients with a prior history of or at high risk for cardiovascular disease usefulness of COX-2 inhibitors for pain relief should be limited to patients for whom there are no reasonable alternatives, and then, only in the lowest dose and for the shortest duration required.”

In 2005, a study disseminated in the Annals of Internal Medicine found that cardiovascular effects of COX-2 inhibitors differ, counting on the drug. Other COX-2-selective inhibitors, such as rofecoxib, have extremely higher myocardial infarction rates than celecoxib. In April 2005, after a comprehensive review of data, the Food and Drug Administration concluded it was likely “that there is a ‘class effect’ for increased CV trouble for all NSAIDs”. In a 2006 meta-analysis of randomized control investigations, the cerebrovascular events associated with COX-2 inhibitors were examined, but no considerable risks were found when corresponding to nonselective NSAIDs or placebos.

Drug interactions

Celecoxib is predominantly metabolized by cytochrome P450 2C9. Caution must be exercised with the simultaneous usage of 2C9 inhibitors, such as fluconazole, which can greatly elevate celecoxib serum levels. If utilized concomitantly with lithium, celecoxib advances lithium plasma levels. If utilized concomitantly with warfarin, celecoxib may result in an increased risk of bleeding difficulties. The risk of bleeding and gastric ulcers also increases further when SSRIs are used in combination with celecoxib. The drug may improve the risk of kidney defeat with angiotensin-converting enzyme inhibitors, such as lisinopril, and diuretics, such as hydrochlorothiazide.

Pregnancy

In the US FDA’s pregnancy categories, the drug is Category C before 30 weeks gestation, and Category D starting at 30 weeks gestation.

What other information should I know?

Do not let anyone else take your medication. Request your pharmacist any questions you have about supplying your prescription. Your blood pressure should be checked regularly during your restorative. You require to keep a documented list of all of the medicine and nonprescription (over-the-counter) medicines you are taking, as well as any results such as vitamins, minerals, or other dietary supplements. You should bring this checklist with you each time you visit a doctor or if you are admitted to an infirmary. It is also important information to carry with you in case of trouble.

Warnings

Celecoxib can improve your risk of fatal heart attack or stroke, even if you do not have any chance factors. Do not utilize this drug just before or after heart bypass surgery (coronary artery bypass graft, or CABG).

Celecoxib may also induce stomach or intestinal bleeding, which can be fatal. These disorders can occur without warning while you are using this medicine, especially in older adults. You should not take this drug if you already have bleeding in your stomach or intestines.

Before taking this medicine

You should not utilize celecoxib if you are allergic to it, or if you have:

• an allergy to sulfa drugs; or
• a narrative of an asthma attack or severe allergic response after taking aspirin or an NSAID.

To make sure celecoxib is safe for you, tell your physician if you have ever had:

• a stomach ulcer, bleeding in your stomach and/or intestines;
• heart disease, high blood pressure;
• asthma;
• bleeding issues;
• liver or kidney disease; or
• if you smoke or drink alcohol.

If you are expectant, you should not take celecoxib unless your physician signifies you to. Taking an NSAID during the last 20 weeks of pregnancy can also cause serious heart or kidney problems in the unborn baby and possible difficulties with your pregnancy. This medicine may also affect fertility (the ability to have children) in women. Ask your physician about this risk. It may not be secure to breastfeed while using this medicine. Ask your doctor about any troubles. Do not give this medication to a child without a medical recommendation.

Dosing information

• Usual Adult Dose for Pain: Acute pain: 400 mg initially, obeyed by 200 mg if required on the first day. Then, 200 mg twice daily as required.
• Usual Adult Dose for Dysmenorrhea: is 400 mg originally, followed by 200 mg if required on the first day. Then, 200 mg double daily as needed.
• Usual Adult Dose for Osteoarthritis: is 200 mg orally earlier daily or 100 mg orally twice daily.
• Usual Adult Dose for Rheumatoid Arthritis: 100 to 200 mg orally twice every day.
• Usual Adult Dose for Familial Adenomatous Polyposis: 400 mg orally twice every day with food.
• Usual Adult Dose for Ankylosing Spondylitis: is 200 mg orally once daily or 100 mg orally twice day-to-day. If after 6 weeks of treatment, no results are observed, a tribulation dose of 400 mg orally daily may be worthwhile. If no reaction is seen after 6 weeks, consideration should be given to alternate treatment choices.
• Usual Pediatric Dose for Juvenile Rheumatoid Arthritis: 2 years or older: 10 to less than and/or equivalent to 25 kg: 50 mg orally twice daily, Greater than 25 kg: 100 mg orally doubled every day.

Monitoring

Due to the chance for celecoxib to cause new or worsening hypertension, fluid retention in patients with congestive heart failure, renal toxicity, liver toxicity, anaphylactic responses, and skin changes ranging from a non-severe rash to more severe responses including Stevens-Johnson syndrome, prescribers require to monitor patients for adverse drug reactions. Prescribers should observe a patient’s blood pressure, and renal and liver function and monitor for signs and symptoms of GI bleeding.

Patients accepting such medications as lithium or warfarin should have the concentrations of these medications monitored more carefully as well due to celecoxib’s renal toxicity and inhibition of CYP2C9, respectively. Plasma attention of celecoxib is not routinely part of the monitoring to determine medicinal efficacy.

Toxicity

Unfortunately, no antidotes for celecoxib overdose are available. Nevertheless, celecoxib is a relatively safe medication overall. There were no registered overdoses of celecoxib during FDA difficulties, and doses up to 2400 mg per day for ten days did not result in severe toxicity.

Symptoms of celecoxib overdose would likely be comparable to overdoses of other NSAIDs, which include lethargy, drowsiness, nausea, vomiting, and epigastric pain. Activated charcoal may be allocated for overdose medicine at the constraint of emergency medical providers if the patient presents within 4 hours of known or suspected ingestion of substantial amounts of celecoxib. Due to high plasma protein binding, dialysis, urine alkalinization, or diureses are improbable to have a significant therapeutic effect on celecoxib overdose.

Enhancing Healthcare Team Outcomes

Significant possibilities are obtainable for improved interprofessional care coordination concerning celecoxib.

As mentioned above, in the inpatient setting, celecoxib is increasingly being utilized as a part of pre-operative and post-operative multimodal pain management algorithms. Analysis has shown in several little randomized trials that distributing celecoxib peri-operatively for elective methods such as total hip arthroplasties, total knee arthroplasties, and other procedures with some success in reducing pain and enhancing functions such as early ambulation. The usage of non-opioid drugs to enhance pain and function after surgery is becoming increasingly necessary due to societal and political pressure to reduce overall opioid analgesic consumption as a response to increasing rates of overdose deaths. It is, thus, important for clinicians (including MDs, DOs, PAs, and NPs), nurses, pharmacists, physical and also occupational therapists, and other support staff to correspond a concerted action to set patient-specific goals regarding pain and function in the acute care and rehabilitative settings and to reinforce how celecoxib use can assist to achieve these objectives to the patient. Clinicians and the interprofessional health care team must also maintain regular and open transmission while monitoring the patient for advancements in pain and function and possible adverse effects the patient may be experiencing. This interprofessional system will yield the best restorative results while minimizing the chance of adverse events. 

In outpatient conditions, prescribers of celecoxib must also correspond with pharmacists to prevent and monitor unsafe drug relations and with the patient, family associates, and caregivers to monitor medicinal benefits and possible adverse drug effects. When the guardian’s function as an interprofessional team, patients can also receive maximum benefit from celecoxib with minimal adverse effects.

Expert Advice For Celecoxib

• Celecoxib helps relieve pain and inflammation.
• It may generate fewer stomach problems as compared to other NSAIDs like Ibuprofen or Naproxen.
• It may cause dizziness and fatigue. Do not move and/or do anything demanding concentration until you know how it affects you.
• Do not swallow alcohol while on treatment with this medicine as it may induce excessive drowsiness.
• Regularly monitor your blood pressure while taking this drug, especially in the first two weeks after starting treatment.
• Notify your physician if you have a history of stomach ulcers, heart disorders, high blood pressure, and liver or kidney disease.
• During long-term treatment, your medic may want to take regular blood tests to observe your liver function.
• Do not take Celecoxib if you are pregnant, scheduling to conceive, and/or breastfeeding.

FAQ

Author: Dr. Prachi Patel