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Keywords
NSAIDS- Non-Steroidal Anti-Inflamatory Drugs
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NSAIDS- Non-Steroidal Anti-Inflamatory Drugs
NSAIDS
Prototype Non-Steroidal Anti-inflammatory Drugs
Acetaminophen (Tylenol)Allopurinol (Zyloprim)
Ibuprofen (Advil, Motrin)
Salicylates (Aspirin)
Mechanism of Action
Most function by triggering a metabolic process that results in decreased levels of prostaglandins. This is achieved by inhibiting cyclooxygenase (COX), an enzyme necessary to the synthesis of prostaglandinsProstaglandins serve a major role in the production of pain, inflammation, and fever (hyperpyrexia)
There are two isoforms of COX: COX-1 and COX-2
COX-1 is expressed in the gastrointestinal tract in high levels
COX-2 is the one expressed in the gastrointestinal in lower levels
NSAIDs may inhibit both COX-1 and COX-2, but target one isoform more than the other
COX-1-Selective NSAIDs
KetoprofenFlurbiprofen
COX-2-Selective NSAIDs
DiclofenacMefenamic acid
Side Effects and Adverse Reactions Associated With NSAIDs
Tinnitus, a sign of ototoxicityHepatotoxicity
Gastrointestinal bleeding
Increased predisposition to ulcers
Heartburn
Gastrointestinal disturbances, such as nausea
Drug Interactions Associated With NSAIDs
LithiumWarfarin
Oral hypoglycemic agents (OHAs)
Certain antihypertensives; angiotensin converting enzyme inhibitors, β-blockers
Diuretics
Methotrexate (high doses)
Desmopressin and NSAIDs (in patients with bleeding disorders)
Certain NSAIDs should not be used together (Eg: Ketoprofen and ibuprofen)
Acetaminophen (Tylenol, Paracetamol)
- Classification: antipyretic, non-opioid analgesic, non-steroidal anti-inflammatory drug
- Indications: mild to moderate pain, inflammation, and hyperpyrexia (fever)
- Availability: found in over 200 products; may be used in conjunction with opioid analgesics to potentiate pain relief
- Doses: 325 mg (regular strength), 500 mg (extra strength), and 650 mg (extended release)
- Route: enteral, parenteral, and intravenous
- Forms: tablet, liquid, elixir, suppository, suspension, and infusion
- Combination products: propoxyphene napsylate (Darvocet-N 100), oxycodone and acetaminophen (Percocet)
- Maximum pediatric dose: 10-15 mg/kg every 5 hours for children, and 10-15 mg/kg every 6 hours for newborns
- Toxic dose: 150 mg/kg
- Antidote: N-acetylcysteine (Mucomyst)
What is Allopurinol?
- Treats gouty arthritis
- Colchicine may cause hematuria
- Reduces uric acid levels
About Ibuprofen
Ibuprofen is widely used for its analgesic, antipyretic, and antiinflammatory roles. Its mechanism of action is associated with inhibition of cyclo-oxygenases, an enzyme necessary to the synthesis of prostaglandins, a chemical mediator involved in the production of pain, inflammation, and fever. Overdose can cause serious toxicity, especially for children that ingest over 400 mg/kg (Bushra & Aslam, 2010).Indications for Use of Ibuprofen
- Analgesic: Relieves mild to moderate pain, both acute and chronic
- Antipyretic: Fever reduction
- Antiinflammatory: Reduces inflammation associated with arthritis and injury
Common Analgesic Uses
- Dysmenorrhea
- Headache and migraine
- Postoperative dental pain
- Dysmenorrhea
- Headache and migraine
- Spondylitis
- Osteoarthritis, rheumatoid arthritis and soft tissue disorders
Side Effects/Adverse Reactions
- Thrombocytopenia
- Rashes
- Headache
- Blurred vision
- Dizziness
- Fluid retention/edema
- Toxic amblyopia (rare)
- Undetected gastric damage with prolonged use, especially in heavy doses
Contraindications
- Abnormal bleeding, evidenced by hematemesis, melena, or other signs
- Severe gastrointestinal disturbances such as intense gastric pain or vomiting
- Pregnancy: Pregnancy category C. Promoted to category D at ≥ 30 weeks’ gestation (increases risk of premature closure of the fetal ductus arteriosus in the heart)
- Infants less than 6 months old
- Ulcer or certain gastrointestinal diseases
Signs of Ibuprofen Toxicity
- Seizures
- Apnea
- Hypertension
- Renal and hepatic dysfunction
- Increased risk of myocardial infraction (Bushra & Aslam, 2010)
Indications for Use of Aspirin
- Prophylaxis of thrombolytic events and myocardial infarction
- Low-dose daily therapy for patients with heart failure
- Rheumatoid arthritis: provides inflammation relief
- Causes irreversible inhibition of the isoenzyme cyclooxygenase-1
Signs of Aspirin Toxicity
- Tinnitus and hearing loss
- Hyperventilation
- Behavioral changes
Contraindications of NSAID Use
- Anticoagulants
- Renal disease
- Rhinitis
- Peptic ulcer disease
- Pregnancy
Renal Disease and NSAID Use
- Use of NSAIDS is contraindicated in patients with renal disease\
- Renal transplants are required for serious cases
- Azathioprine (Imuran) is used to reduce the risk of rejection
- Leukopenia is a severe adverse reaction of Imuran
- Immunosuppressant therapy agents may need to be discontinued if the WBC count drops below 3,000
- Multiple sclerosis: Immunosuppressant therapy is performed through the drug glatiramer acetate (Copaxone)
The Connection Between Ulcers and NSAIDS
- Long-term use of NSAIDS may compromise the integrity of a gastric mucosa and increase the risk of developing an ulcer
- Misoprostol (Cytotec) may be used to reduce the risk of ulcers in patients on long-term NSAID therapy.
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