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NSAIDS- Non-Steroidal Anti-Inflamatory Drugs

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NSAIDS- Non-Steroidal Anti-Inflamatory Drugs

Post by Naseem Abbas Malik on Mon Oct 19, 2015 2:02 pm

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 prostaglandins
Prostaglandins 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

Ketoprofen
Flurbiprofen




COX-2-Selective NSAIDs

Diclofenac
Mefenamic acid




Side Effects and Adverse Reactions Associated With NSAIDs

Tinnitus, a sign of ototoxicity
Hepatotoxicity
Gastrointestinal bleeding
Increased predisposition to ulcers
Heartburn
Gastrointestinal disturbances, such as nausea




Drug Interactions Associated With NSAIDs

Lithium
Warfarin
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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Naseem Abbas Malik
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