Celecoxib 100 mg Capsules

Brand Name

Celecoxib is both the brand name and generic designation for this medication, widely acknowledged in clinical settings for its utility in managing pain and inflammation. It is a prominent choice among healthcare providers for addressing specific musculoskeletal and inflammatory conditions.

International Nonproprietary Name (INN)

The active compound in this drug aligns with its International Nonproprietary Name (INN), celecoxib. This pyrazole derivative belongs to the class of selective cyclooxygenase-2 inhibitors, engineered to provide targeted relief in inflammatory states.

Forms of Release

Celecoxib is available primarily as oral capsules, offered in strengths of 50 mg, 100 mg, 200 mg, and 400 mg to cater to varying patient needs and treatment regimens. These capsules are designed for straightforward administration, ensuring consistent delivery of the active ingredient for pain and inflammation management. No alternative forms like tablets or solutions are widely marketed, focusing the formulation on this practical oral route.

Composition

The central active ingredient in Celecoxib is celecoxib itself, driving its anti-inflammatory and analgesic effects. Alongside this, the capsules contain several inactive components to support stability and bioavailability. These include lactose monohydrate, sodium lauryl sulfate, and povidone as fillers and stabilizers, with magnesium stearate facilitating capsule production. The capsule shell is composed of gelatin, titanium dioxide, and, in certain strengths, iron oxides or other colorants for differentiation. These auxiliary substances ensure the drug’s structural integrity and effective delivery upon ingestion.

Pharmacologic Properties

Pharmacodynamics

This medication operates by selectively targeting inflammatory pathways in the body. Celecoxib exerts its effects by inhibiting cyclooxygenase-2 (COX-2), an enzyme responsible for producing prostaglandins that mediate pain, swelling, and fever during inflammation. Unlike non-selective NSAIDs, it spares cyclooxygenase-1 (COX-1) at therapeutic doses, reducing interference with protective gastric mucosal functions and platelet activity. This selective inhibition dampens the inflammatory cascade, alleviating discomfort and joint stiffness in conditions like arthritis, while offering a gastrointestinal safety profile superior to traditional alternatives. Its action provides sustained relief without broadly disrupting normal physiological processes.

Pharmacokinetics

The pharmacokinetic profile of Celecoxib describes its journey through the body. After oral administration, it is absorbed from the gastrointestinal tract, with peak plasma concentrations achieved in about 2 to 3 hours, enhanced by high-fat meals which increase bioavailability to approximately 40–50%. It is highly bound to plasma proteins (97%), predominantly albumin, and distributes extensively into tissues, with a volume of distribution of around 400 L. Metabolism occurs primarily in the liver via cytochrome P450 2C9, producing inactive metabolites through oxidation and glucuronidation. Excretion is split between urine (27%) and feces (57%), with a half-life of 8 to 12 hours, prolonged in hepatic or renal impairment, necessitating tailored dosing in such cases.

Indications for Use

This medication is prescribed for conditions involving pain and inflammation, capitalizing on its ability to selectively mitigate these symptoms in various musculoskeletal disorders.

Diseases and Conditions

Celecoxib is indicated for the relief of osteoarthritis symptoms, reducing joint pain and stiffness in adults. It is also approved for rheumatoid arthritis management in adults, easing inflammation and improving mobility. For acute pain, such as post-surgical discomfort or menstrual cramps, and ankylosing spondylitis, it provides effective analgesia and anti-inflammatory support. Its targeted action makes it a valuable option for chronic and acute inflammatory states requiring symptom control.

Contraindications

While beneficial for many, certain conditions preclude the use of this medication due to significant risks, requiring careful evaluation prior to therapy.

Conditions Prohibiting Use

Celecoxib is contraindicated in patients with known hypersensitivity to celecoxib, sulfonamides, or any capsule components, as reactions could range from rash to anaphylaxis. It is prohibited in individuals with a history of asthma, urticaria, or allergic-type reactions triggered by aspirin or other NSAIDs, due to cross-sensitivity risks. Patients with active peptic ulcer disease, recent gastrointestinal bleeding, or severe heart failure should avoid it, given potential exacerbation of these conditions. It is also barred post-coronary artery bypass graft surgery due to increased cardiovascular event risk, ensuring safety in high-risk populations.

Method of Administration and Dosage

How to Take

This medication is taken orally as capsules, swallowed whole with a generous amount of water. It may be consumed with or without food, though taking it with a meal—especially a high-fat one—enhances absorption, which can be beneficial for acute pain relief. Timing should be consistent, typically once or twice daily, to maintain steady levels. Patients should avoid opening capsules, as this alters the intended release, ensuring optimal delivery and efficacy.

Dosages for Adults and Children

Dosing varies by condition and patient age, with use limited to adults and adolescents over 18 due to insufficient pediatric data. For osteoarthritis, adults typically take 200 mg daily, either as a single dose or 100 mg twice daily. In rheumatoid arthritis, the dose ranges from 100–200 mg twice daily, up to 400 mg/day. Acute pain or dysmenorrhea starts with 400 mg initially, followed by 200 mg if needed on day one, then 200 mg twice daily as required. For ankylosing spondylitis, 200 mg daily suffices, with an increase to 400 mg if response is inadequate. Celecoxib’s dosing flexibility supports tailored symptom management.

Dose Adjustment in Specific Conditions

Adjustments are necessary in hepatic or renal impairment. In moderate hepatic dysfunction (Child-Pugh Class B), the dose is halved (e.g., 100 mg daily for osteoarthritis), with severe cases avoiding use due to limited data. Renal impairment (creatinine clearance 30–60 mL/min) requires caution but no standard reduction, though severe cases (below 30 mL/min) warrant avoidance or specialist oversight. Elderly patients, especially those under 50 kg or with comorbidities, may start at the lowest effective dose (e.g., 100 mg daily), with monitoring for tolerability, balancing efficacy and safety.

Side Effects

This medication can provoke a range of adverse reactions, from mild to serious, and patients should be educated to recognize and address them promptly.

Possible Adverse Reactions

Common effects include gastrointestinal upset—abdominal pain, dyspepsia, or diarrhea—often mild and transient. Headache, dizziness, and peripheral edema may affect daily comfort, while hypertension occurs in some, particularly with prolonged use. Skin rashes or itching are reported, with rare progression to severe reactions like Stevens-Johnson syndrome. Cardiovascular risks, such as myocardial infarction or stroke, increase with higher doses or long-term therapy, especially in predisposed individuals. Renal effects, including reduced function or fluid retention, and rare hepatic enzyme elevations also occur, necessitating regular oversight to manage these potential issues.

Overdose

Symptoms of Overdose

Excessive intake of Celecoxib can lead to significant symptoms requiring immediate attention. These include severe nausea, vomiting, or abdominal pain from gastrointestinal irritation, alongside lethargy or drowsiness from systemic effects. Hypertension, tachycardia, or respiratory distress may signal cardiovascular strain, while acute kidney injury or oliguria could emerge in severe cases. Confusion or seizures are rare but possible with massive doses, highlighting the need for swift recognition and response.

First Aid Measures

In an overdose scenario, prompt action is crucial. If the patient is alert and ingestion was recent, contact emergency services or poison control without inducing vomiting unless instructed. Maintain airway and vital sign stability while awaiting assistance. In medical settings, activated charcoal may be given within an hour of ingestion to limit absorption, followed by supportive care—IV fluids, blood pressure management, and monitoring. Dialysis is ineffective due to high protein binding, but symptomatic treatment addresses complications effectively.

Drug Interactions

Effects on Other Medications

This medication can alter the effects of co-administered drugs through metabolic interactions. It inhibits CYP2C9, increasing levels of warfarin, phenytoin, or sulfonylureas, potentially enhancing their effects or toxicity, requiring close monitoring or dose tweaks. ACE inhibitors or diuretics may have reduced efficacy, raising blood pressure risks, while lithium levels can rise, necessitating adjustments. Aspirin co-use negates gastrointestinal benefits, increasing ulcer risk. Careful management ensures safe combination therapy.

Compatibility with Alcohol and Food

Alcohol should be minimized with Celecoxib, as it heightens gastrointestinal bleeding risk and may exacerbate side effects like dizziness. Food enhances absorption, making administration with meals advisable for tolerability, with no specific dietary restrictions beyond avoiding excess irritants. Consistency in intake supports predictable outcomes.

Special Precautions

Use During Pregnancy and Breastfeeding

This medication is Category C before 30 weeks gestation, used only if benefits outweigh risks due to potential fetal harm, shifting to Category D after 30 weeks due to premature ductus arteriosus closure risks, contraindicating late-term use. Celecoxib enters breast milk in trace amounts; breastfeeding is discouraged due to unknown infant effects, with alternatives preferred.

Impact on Driving and Operating Machinery

Celecoxib may affect alertness or coordination due to dizziness or drowsiness, particularly early in therapy. Patients should avoid driving or machinery until they assess its impact, ensuring safety in daily tasks.

Considerations for Elderly and Pediatric Patients

In elderly patients, this drug requires cautious dosing due to increased cardiovascular and gastrointestinal risks, starting at 100 mg daily with monitoring for adverse events. It’s not approved for children under 18, lacking pediatric safety data, with alternatives used for juvenile conditions. Adult dosing adjustments ensure tolerability across populations.