Celecoxib

Brand Names: Celecoxib

Drug Class: Nonsteroidal Anti-inflammatory Drug

Overview

11. DESCRIPTION Celecoxib capsule is a nonsteroidal anti-inflammatory drug, available as capsules containing 50 mg, 100 mg, 200 mg and 400 mg celecoxib for oral administration. The chemical name is 4-[5-(4-methylphenyl)- 3-(trifluoromethyl)-1H-pyrazol-1-yl] benzenesulfonamide and is a diaryl-substituted pyrazole. The molecular weight is 381.38.

Mechanism of Action

12. CLINICAL PHARMACOLOGY 12.1 Mechanism of Action Celecoxib has analgesic, anti-inflammatory, and antipyretic properties. The mechanism of action of celecoxib is believed to be due to inhibition of prostaglandin synthesis, primarily via inhibition of COX-2. Celecoxib is a potent inhibitor of prostaglandin synthesis in vitro . Celecoxib concentrations reached during therapy have produced in vivo effects. Prostaglandins sensitize afferent nerves and potentiate the action of bradykinin in inducing pain in animal models. Prostaglandins are mediators of inflammation. Since celecoxib is an inhibitor of prostaglandin synthesis, its mode of action may be due to a decrease of prostaglandins in peripheral tissues. 12.

Indications

  • 1. INDICATIONS AND USAGE Celecoxib is indicated Celecoxib is a nonsteroidal anti-inflammatory drug indicated for: Osteoarthritis (OA) ( 1.1 ) Rheumatoid Arthritis (RA) ( 1.2 ) Juvenile Rheumatoid Arthritis (JRA) in patients 2 years and older ( 1.3 ) Ankylosing Spondylitis (AS) ( 1.4 ) Acute Pain (AP) ( 1.5 ) Primary Dysmenorrhea (PD) ( 1.6 ) 1.1 Osteoarthritis For the management of the signs and symptoms of OA [ see Clinical Studies (14.1) ]. 1.2 Rheumatoid Arthritis For the management of the signs and symptoms of RA [ see Clinical Studies (14.2) ]. 1.

Common Doses

  • 200 mg
  • 100 mg
  • 50 mg
  • 400 mg

Dosage

2. DOSAGE AND ADMINISTRATION Use the lowest effective dosage for shortest duration consistent with individual patient treatment goals. ( 2.1 ) OA: 200 mg once daily or 100 mg twice daily. ( 2.2 , 14.1 ) RA: 100 mg to 200 mg twice daily. ( 2.3 , 14.2 ) JRA: 50 mg twice daily in patients 10 kg to 25 kg. 100 mg twice daily in patients more than 25 kg. ( 2.4 , 14.3 ) AS: 200 mg once daily single dose or 100 mg twice daily. If no effect is observed after 6 weeks, a trial of 400 mg (single or divided doses) may be of benefit. ( 2.5 , 14.

Black Box Warning

WARNING: RISK OF SERIOUS CARDIOVASCULAR AND GASTRO-INTESTINAL EVENTS Cardiovascular Thrombotic Events Nonsteroidal anti-inflammatory drugs (NSAIDs) cause an increased risk of serious cardiovascular thrombotic events, including myocardial infarction, and stroke, which can be fatal. This risk may occur early in the treatment and may increase with duration of use [ see Warnings and Precautions (5.1) ]. Celecoxib is contraindicated in the setting of coronary artery bypass graft (CABG) surgery [ see Contraindications (4) and Warnings and Precautions (5.1) ].

Contraindications

  • 4. CONTRAINDICATIONS Celecoxib is contraindicated in the following patients: Known hypersensitivity (e.g., anaphylactic reactions and serious skin reactions) to celecoxib, any components of the drug product [see Warnings and Precautions (5.7, 5.9) ]. History of asthma, urticaria, or other allergic-type reactions after taking aspirin or other NSAIDs. Severe, sometimes fatal, anaphylactic reactions to NSAIDs, have been reported in such patients [see Warnings and Precautions (5.7 , 5.8) ]. In the setting of CABG surgery [see Warnings and Precautions (5.1) ].

Side Effects

  • 6. ADVERSE REACTIONS The following adverse reactions are discussed in greater detail in other sections of the labeling: Cardiovascular Thrombotic Events [ see Warnings and Precautions ( 5.1 ) ] GI Bleeding, Ulceration and Perforation [ see Warnings and Precautions ( 5.2 ) ] Hepatotoxicity [ see Warnings and Precautions ( 5.3 ) ] Hypertension [ see Warnings and Precautions ( 5.4 ) ] Heart Failure and Edema [ see Warnings and Precautions ( 5.5 ) ] Renal Toxicity and Hyperkalemia [ see Warnings and Precautions ( 5.6 ) ] Anaphylactic Reactions [ see Warnings and Precautions ( 5.

Interactions

  • 7. DRUG INTERACTIONS See Table 3 for clinically significant drug interactions with celecoxib. Table 3: Clinically Significant Drug Interactions with Celecoxib Drugs That Interfere with Hemostasis Clinical Impact: Celecoxib and anticoagulants such as warfarin have a synergistic effect on bleeding. The concomitant use of celecoxib and anticoagulants have an increased risk of serious bleeding compared to the use of either drug alone. Serotonin release by platelets plays an important role in hemostasis.