Naproxen
From DrugPedia: A Wikipedia for Drug discovery
Pronouncation: (nay-PROX-ehn)
Class: NSAID
Trade Names:
EC Naprosyn
- Tablets, delayed-release 375 mg
- Tablets, delayed-release 500 mg
Trade Names:
Naprosyn
- Tablets 250 mg
- Tablets 375 mg
- Tablets 500ߙmg
- Suspension 125 mg/5 mL
Apo-Naproxen (Canada)
Apo-Naproxen SR (Canada)
Gen-Naproxen EC (Canada)
Naxen (Canada)
Novo-Naprox (Canada)
Novo-Naprox EC (Canada)
Nu-Naprox (Canada)
ratio-Naproxen (Canada)
Naproxen Sodium
Trade Names:
Aleve
- Tablets 200 mg (220 mg naproxen sodium)
Trade Names:
Anaprox
- Tablets 250 mg (275 mg naproxen sodium)
Trade Names:
Anaprox DS
- Tablets 500ߙmg (550 mg naproxen sodium)
Trade Names:
Naprelan
- Tablets, controlled-release 375 mg (412.5 mg naproxen sodium)
- Tablets, controlled-release 500 mg (550 mg naproxen sodium)
Apo-Napro-Na (Canada)
Apo-Napro-Na DS (Canada)
Novo-Naprox Sodium (Canada)
Novo-Naprox SR (Canada)
Novo-Naprox Sodium DS (Canada)
Contents |
[edit] Pharmacology
Decreases inflammation, pain, and fever, probably through inhibition of cyclooxygenase activity and prostaglandin synthesis.
[edit] Pharmacokinetics
Absorption
Naproxen is completely absorbed from the GI tract. Tablet T max is 2 to 4 h (immediate-release); suspension T max is 1 to 4ߙh; fasted patients' T max is 4 to 6 h (delayed-release); bioavailability is 95%; steady state is reached in 4 to 5 days.
Distribution
Vd is 0.16 L/kg and protein binding is 99% albumin-bound.
Elimination
Naproxen is eliminated in urine (95%), primarily as naproxen less than 1%, 6-0-desmethylnaproxen less than 1%, or their conjugates (66% to 92%). Naproxen t ½ is 12 to 17 h; Cl is 0.13ߙmL/min/kg; t ½ of metabolites and conjugates is less than 12 h.
Special Populations
Renal Function Impairment
Metabolites and conjugates may accumulate.
[edit] Indications and Usage
Rx
Management of mild to moderate pain, symptoms of rheumatoid or osteoarthritis, bursitis, tendonitis, ankylosing spondylitis, primary dysmenorrhea, acute gout. Naproxen (not naproxen sodium) also indicated for treatment of juvenile rheumatoid arthritis. Delayed-release naproxen is not recommended for initial treatment of acute pain because absorption is delayed compared to other naproxen formulations.
OTC
Temporary relief of minor aches and pains associated with the common cold, headache, toothache, muscular aches, backache, minor arthritis pain, pain of menstrual cramps, and reduction of fever.
Unlabeled Uses
Sunburn, migraine, PMS.
[edit] Contraindications
Allergy to aspirin, iodides or any NSAID; patients in whom aspirin or other NSAIDs induce symptoms of asthma, rhinitis or nasal polyps.
[edit] Dosage and Administration
Naproxen
Rheumatoid Arthritis, Osteoarthritis, Ankylosing Spondylitis Adults
PO 250 to 500 mg twice daily; max dose of 1.5 g/day should be used short term only.
Delayed-release
PO 375 to 500 mg twice daily.
Controlled release
PO 750 to 1,000 mg every daily. Individualize dosage. Do not exceed 1,500 mg/day.
Suspension
PO 250 mg (10 mL), 375 mg (15 mL), or 500 mg (20 mL) twice daily.
Pain, Dysmenorrhea, Bursitis, Tendinitis Adults
PO 500 mg initially, then 250ߙmg everyߙ6 to 8 h. Do not exceed 1,250ߙmg/day.
Juvenile Rheumatoid Arthritis Children
PO 10 mg/kg/day in 2 divided doses. For children requiring suspension, 2.5ߙmL twice daily can be given for weights of at least 13ߙkg; 5 mL twice daily for weights of at least 25 kg, or 7.5 mL twice daily for weights of at least 38 kg.
Acute Gout Adults
PO 750 mg, followed by 250 mg everyߙ8ߙh until the attack subsides.
Naproxen Sodium
Rheumatoid Arthritis, Osteoarthritis, Ankylosing Spondylitis Adults
PO 275 to 550 mg twice daily. May increase to 1.65 g for limited periods.
Acute Gout Adults
PO 825 mg initially, then 275ߙmg everyߙ8ߙh prn.
Controlled-release
PO 1,000 to 1,500 mg once daily on the first day, then 1,000 mg once daily until attack has subsided.
Pain, Dysmenorrhea, Tendinitis, Bursitis Adults
PO 500 mg initially, then 275 mg everyߙ6 to 8 h prn. Do not exceed 1,375 mg/day.
Controlled release
PO 750 to 1,000 mg once daily. Individualize dosage. Do not exceed 1,500 mg/day.
[edit] Storage/Stability
Store at controlled room temperature (59° to 86°F).
[edit] Drug Interactions
Anticoagulants
May increase effect of anticoagulants because of decreased plasma protein binding. May increase risk of gastric erosion and bleeding.
Lithium
May decrease lithium Cl.
Methotrexate
May increase methotrexate levels.
Laboratory Test Interactions
May falsely increase urinary 17-ketosteroid values; may interfere with urinary assays for 5-hydroxy-indoleacetic acid.
[edit] Adverse Reactions
Cardiovascular
Edema; weight gain; CHF; alterations in BP; vasodilation; palpitations; tachycardia; chest pain; bradycardia.
CNS
Headache; dizziness; drowsiness; vertigo; lightheadedness; mental depression; nervousness; irritability; fatigue; malaise; insomnia; sleep disorders; dream abnormalities; aseptic meningitis.
Dermatologic
Rash; urticaria; purpura; skin eruptions.
EENT
Visual changes; tinnitus; rhinitis; pharyngitis, stomatitis.
GI
Constipation; heartburn; abdominal pain; peptic ulceration and bleeding; nausea; dyspepsia; diarrhea; vomiting; anorexia; colitis; flatulence.
Genitourinary
Glomerulonephritis; interstitial nephritis; nephrotic syndrome; acute renal insufficiency and renal failure; dysuria; hyperkalemia; hyponatremia; renal papillary necrosis.
Hepatic
Increased LFT results.
Hematologic
Increased bleeding time; leukopenia; thrombocytopenia; granulocytopenia; eosinophilia; ecchymosis.
Respiratory
Bronchospasm; laryngeal edema; dyspnea; shortness of breath.
[edit] Precautions
Pregnancy
Category B .
Lactation
Excreted in breast milk.
Children
Safety and efficacy in children younger than 2 yr of age not established (Rx); do not give to children younger than 12 yr of age except under the advice and supervision of a health care provider (OTC).
Elderly
Increased risk of adverse reactions.
Renal Function
Assess function before and during therapy in patients with renal function impairment because NSAID metabolites are eliminated renally.
Hepatic Function
May need to reduce dose in patients with hepatic failure.
CV disease
Drug may worsen CHF and may decrease hypertension control.
Concomitant therapy
Do not use naproxen sodium and naproxen concomitantly; both drugs circulate as naproxen anion.
GI effects
Serious GI toxicity (eg, bleeding, ulceration, perforation) can occur at any time, with or without warning symptoms.
[edit] Overdosage
Symptoms
Drowsiness, nausea, heartburn, vomiting, indigestion, seizures.
[edit] Patient Information
- Tell patient to take with milk, meals or antacids; follow with ½ to 1 glass of water to reduce GI upset.
- Advise patient to shake oral suspension before measuring.
- Explain that it may take 2 to 4 wk with naproxen and 1 to 2 days with naproxen sodium for anti-inflammatory effects to occur. Peak analgesic effect may occur in 1 to 2 h.
- Caution patient that use with aspirin, alcohol, steroids, and other GI irritants may cause increased GI upset.
- Instruct patient to report the following symptoms to health care provider: visual problems, abdominal pain, symptoms of gastric bleeding.
- Caution patient to avoid intake of alcoholic beverages and smoking.
- Advise patient to use caution while driving or performing other activities that require coordinated motor movements and mental alertness.
