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aspirin rectal

 

Classes: NSAIDs

Dosing and uses of Aspirin rectal

 

Adult dosage forms and strengths

suppository

  • 60mg
  • 120mg
  • 200mg
  • 300mg
  • 600mg

 

Antipyretic/Analgesic

300-600 mg PR q4-6hr PRn

 

Administration

Patient should lie on left side with knees bent

Remove protective wrap before inserting

Gently insert tip into rectum with slight side-to-side movement (tip of suppository pointing toward navel)

 

Pediatric dosage forms and strengths

suppository

  • 120mg
  • 200mg
  • 300mg
  • 600mg

 

Antipyretic/Analgesic

<12 years: 10-15 mg/kg/dose PR q4-6hr; not to exceed 4 g/day

>12 years: As adults; 300-600 mg PR q4-6hr PRn

 

Geriatric Dosing

Antipyretic/Analgesic

  • <12 years: 10-15 mg/kg/dose PR q4-6hr; not to exceed 4 g/day
  • >12 years: As adults; 300-600 mg PR q4-6hr PRN

 

Renal Impairment

CrCl<10 mL: Not recommended

 

Hepatic Impairment

Not recommended

 

Administration

Patient should lie on left side with knees bent

Remove protective wrap before inserting

Gently insert tip into rectum with slight side-to-side movement (tip of suppository pointing toward navel)

 

Geriatric dosage forms and strengths

 

Antipyretic/Analgesic

 

Aspirin rectal adverse (side) effects

Frequency not defined

Common

  • Rectal discomfort
  • Tinnitus (high or chronic dose)
  • Rash
  • Urticaria

Angioedema

DIC

Hypotension

Tachycardia

CNS alteration

Dizziness

Headache

Dermatologic problems

Hives

Electrolyte disturbances; dehydration, hyperkalemia, metabolic acidosis, respiratory alkalosis

Platelet aggregation inhibition

Prolonged prothrombin time

Thrombocytopenia

Hepatotoxicity

Hearing loss

Renal damage

Bronchospasm

Pulmonary edema (salicylate-induced/noncardiogenic)

Reye syndrome

 

Warnings

Contraindications

Hypersensitivity to aspirin or NSAIDs

Hepatitis or severe hepatic/renal impairment

Do not use in children or adolescents with viral infections (eg, influenza, chickenpox) because of risk of Reye syndrome

 

Cautions

Many dosage forms, check label carefully!

Gastrointestinal bleeding; particular caution in patients w/ history of GI bleed, alcoholism, or bleeding disorders

Avoid w/ active peptic ulcer disease

Avoid in severe renal impairment (ie, CrCl <10 mL/min)

Avoid in severe hepatic impairment

 

Pregnancy and lactation

Pregnancy category: D; avoid during pregnancy, particularly in third trimester because of risk for premature closure of the ductus arteriosus

Lactation: excreted in breast milk; do not breast feed

Pregnant or breastfeeding patients should seek advice of health professional before using OTC drugs

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Aspirin rectal

Mechanism of action

Inhibits prostaglandin synthesis by cyclooxygenase-1 and -2 via acetylation; inhibits formation of prostaglandin derivative, thromboxane A2 via acetylation of platelete cyclooxygenase, which in turn inhibits platelet aggregation

 

Pharmacokinetics

Absorption: 60%

Onset: 4-5 hr

Half-life: 4.7-9 hr

Protein Bound: 50-80%  

Volume of Distribution: 150 mL/kg

Metabolism: Hydrolyzed by esterases in liver (mostly) & erythrocytes to salicylic acid

Metabolites: salicyluric acid, salicyl acyl glucuronide, salicyl phenolic glucuronide, gentisic acid

Excretion: (urine) 5.6-35.6% Hemodialysis: Yes

 

Pharmacogenomics

Aspirin associated hypersensitivity reactions include:

Aspirin-induced urticaria: associated with HLA-DRB1*1302-DQB1*0609 haplotype

Aspirin-intolerant asthma: associated with HLA-DPB1*0301