Non –steroidal anti-inflammatory drugs (NSAIDS)-Salicylic Acids

Name of the NSAIDS- Salicylic Acids

• Aspirin
• Diflusinal
• Sodium salicylate

1.Aspirin

Mechanism of Action

 Blocks the activity of cyclooxygenase, the enzyme needed for prostaglandin synthesis. Prostaglandins, important mediators in the inflammatory response, cause local vasodilation with swelling and pain. With blocking of cyclooxygenase and inhibition of prostaglandins, inflammatory symptoms subside. Pain is also relieved because prostaglandins play a role in pain transmission from the periphery to the spinal cord. Aspirin inhibits platelet aggregation by interfering with production of thromboxane A2, a substance that stimulates platelet aggregation. Aspirin acts on the heatregulating center in the hypothalamus and causes peripheral vasodilation, diaphoresis, and heat loss.

Pharmacokinetics

• Bioavailability: 80-100%
• Onset: PO, 5-30 min; PR, 1-2 hr
• Duration: PO, 4-6 hr; PR, >7 hr
• Peak plasma time: PO, 0.25-3 hr
• Protein bound: ≤100 mcg/mL, 90-95%; 100-400 mcg/mL, 70-85%; higher concentrations, 25-60%
• Metabolized by liver via microsomal enzyme system
• Half-life: Low dose, 2-3 hr; higher dose, 15-30 hr
• Excretion: Urine (80-100%), sweat, saliva, feces

Adverse Reactions

• CNS: Confusion, CNS depression
• EENT: Hearing loss, tinnitus
• GI: Diarrhea, GI bleeding, heartburn, hepatotoxicity, nausea, stomach pain, vomiting
• HEME: Decreased blood iron level, leukopenia, prolonged bleeding time, shortened life span of RBCs, thrombocytopenia
• SKIN: Ecchymosis, rash, urticaria
• Other: Angioedema, Reye’s syndrome, salicylism (dizziness, tinnitus, difficulty hearing, vomiting, diarrhea, confusion, CNSdepression, diaphoresis, headache, hyperventilation, and lassitude) with regular use of large doses

Contraindications

Allergy to tartrazine dye, asthma, bleeding problems (such as hemophilia), hypersensitivity to aspirin or its components, peptic ulcer disease

Nursing Considerations

• Don’t crush timed-release or controlledrelease aspirin tablets unless directed.
• Ask about tinnitus. This reaction usually occurs when blood aspirin level reaches or exceeds maximum for therapeutic effect

Patient Teaching

• Advise adult patient taking low-dose aspirin not to also take ibuprofen because it may reduce the cardioprotective and stroke preventive effects of aspirin.
• Instruct patient to take aspirin with food or after meals because it may cause GI upset if taken on an empty stomach.
• Advise patient with tartrazine allergy not to take aspirin.
• Tell patient to consult prescriber before taking aspirin with any prescription drug for blood disorder, diabetes, gout, or arthritis.
• Tell patient not to use aspirin if it has a strong vinegar-like odor.

2.Diflusinal

Mechanism of Action

Blocks the activity of cyclooxygenase, the enzyme needed to synthesize prostaglandins, which mediate the inflammatory response and cause local vasodilation, swelling, and pain. By blocking cyclooxygenase and inhibiting prostaglandins, this NSAID reduces inflammatory symptoms. This mechanism also relieves pain because prostaglandins promote pain transmission from the periphery to the spinal cord.

Pharmacokinetics

• Bioavailability: 80-100%
• Peak Plasma Time: within 2-3 hr
• Protein Bound: at least 98-99%
• Metabolism: Liver (to glucuronide conjugates, not to salicylic acid)
• Half-life: 8-12 hr
• Excretion: Urine ~90%; feces <5%

Adverse Reactions

• CNS: Aseptic meningitis, cerebral hemorrhage, dizziness, drowsiness, headache, insomnia
• CV: Vasculitis
• EENT: Tinnitus ENDO: Hypoglycemia
• GI: Abdominal pain, constipation, diarrhea, esophageal irritation, GI bleeding or ulceration, hepatic failure, hepatitis, indigestion, jaundice, nausea, perforation of stomach or intestine, vomiting
• GU: Acute renal failure, interstitial nephritis HEME: Agranulocytosis, aplastic anemia, leukopenia, pancytopenia, thrombocytopenia
• SKIN: Erythema multiforme, exfoliative dermatitis, rash, Stevens-Johnson syndrome, toxic epidermal necrolysis
• Other: Anaphylaxis, angioedema, hyponatremia

Contraindications

Asthma attacks, rhinitis, or urticaria precipitated by aspirin or other NSAIDs; hypersensitivity to diflunisal; treatment of perioperative pain after coronary artery bypass graft surgery

Nursing Considerations

• Use diflunisal with extreme caution and for shortest time possible in patients with a history of GI bleeding or ulcer disease because NSAIDs such as diflunisal increase the risk.
• Serious GI tract ulceration and bleeding, as well as perforation of stomach or intestine, can occur without warning or symptoms. Elderly patients are at greater risk. To minimize risk, give diflunisal with food. If patient has GI distress, withhold drug and notify prescriber immediately.
• Use diflunisal cautiously in patients with hypertension, and monitor blood pressure closely during therapy; drug can cause or worsen hypertension.
• Use drug cautiously in elderly patients, those with renal dysfunction, and those who should avoid prolonged bleeding time increase the risk of these events.
•  Monitor BUN and serum creatinine levels in elderly patients, patients taking ACE inhibitors or diuretics, and patients with heart falure or impaired hepatic or renal function. These patients may have an increased risk of renal failure.
• Assess patient’s skin routinely for rash or other signs of hypersensitivity reaction; drug may cause serious skin reactions without warning. At first sign of reaction, stop drug and notify prescriber.
• Assess type, location, and intensity of pain before and 1 to 2 hours after giving drug.
• Assess patient carefully because long-term or high-dose therapy may mask fever.

Patient Teaching

• Teach patient not to crush or chew diflunisal tablets own for 30 minutes afterward to avoid esophageal irritation.
• Inform patient that drug will start working in about 1 week but that full effects may not occur for several weeks.
• Explain that diflunisal may increase the risk of serious adverse cardiovascular reactions; urge patient to seek immediate medical attention for such signs and symptoms as chest pain, shortness of breath, slurred speech, and weakness.
• Tell patient that diflunisal also may increase risk of serious adverse GI reactions; stress need to seek immediate medical attention for signs and symptoms such as abdominal or epigastric pain, black or tarry stools, indigestion, and vomiting blood or material that resembles coffee grounds.
• Alert patient about possibly serious skin reactions and the need to seek immediate medial attention for such as problems as blisters, fever, itching, rash, and other signs of hypersensitivity.
• Caution patient to avoid acetaminophen, alcohol, aspirin, and other salicylates during diflunisal therapy, unless directed otherwise by prescriber.
• Advise patient to avoid hazardous activities until drug’s CNS effects are known.
• Advise patient to tell health care providers about diflunisal therapy before surgery, including dental surgery. Therapy should stop for 1 week before procedure

3.Sodium salicylate

Mechanism of Action

 Hydrolyzes to formaldehyde and ammonia in an acidic environment, such as urine, producing greater amounts of formaldehyde as pH decreases. Formaldehyde has bactericidal action, possibly by denaturing proteins. To facilitate hydrolysis, methenamine is formulated with weak organic acid, such as hippuric acid or mandelic acid

Pharmacokinetics

• Half-Life: 3-6 hr
• Absorption: well absorbed; 10-30% hydrolyzed by gastric acid unless enteric coated tablet
• Peak Urine Time: (formaldehyde) 2 hr for hippurate salt, 3-8 hr for mandelate salt
• Metabolism: by liver (10-25%)
• Excretion: urine (90%)

Adverse Reactions

• CNS: Headache
• CV: Edema
• EENT: Stomatitis
• GI: Abdominal cramps, anorexia, diarrhea, nausea, vomiting
• GU: Bladder irritation, crystalluria, dysuria,hematuria, proteinuria, urinary frequency
• RESP: Pulmonary hypersensitivity (dyspnea, pneumonitis)
• SKIN: Pruritus, rash, urticaria

Contraindications

Concurrent therapy with sulfonamides, hypersensitivity to methenamine, renal insufficiency, severe dehydration, severe hepatic disease

Nursing Considerations

• Be aware that methenamine is used for prophylaxis; it isn’t recommended as primary treatment for UTI.
• Drug shouldn’t be given to patients with creatinine clearance less than 50 ml/min/ 1.73 m2.
• Before giving first dose, expect to obtain urine specimen for culture and sensitivity tests and to review test results if available.
• Plan to give methenamine mandelate around the clock to maintain a therapeutic blood level. • Make sure patient receives adequate fluids.
• Expect to repeat culture and sensitivity tests if patient fails to improve.

Patient Teaching

• Instruct patient to take methenamine with food to avoid GI distress.
• Direct patient to drink extra fluids; avoid alkaline foods, such as milk, milk products, and most fruits; and avoid antacids that contain sodium bicarbonate or carbonate during methenamine therapy.
• Instruct patient to report painful urination, rash, or severe GI distress.
• Urge patient to comply with urine testing before and during long-term therapy.

REFERENCES

1. Robert Kizior, Keith Hodgson, Saunders Nursing Drug handbook,1st edition 2024, Elsevier Publications. ISBN-9780443116070
2. McGraw Hill- Drug Handbook, Seventh Edition, 2013, McGraw Hill Education Publications,9780071799430.
3. April Hazard, Cynthia Sanoski, Davi’s Drug Guide for Nurses -Sixteenth Edition 2019, FA Davis Company Publications,9780803669451.
4. Jones and Bartlet, Pharmacology for Nurses, Second Edition, 2020, Jones and Bartlet Learning Publications, ISBN 9781284141986.
5. Nursebro.com, Search – Nursebro

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