Acetylsalicylic Acid (Aspirin)

Pharmachology
Definition

• Acetylsalicylic acid or also known as Aspirin is a non-

steroidal analgesic compound that is used as an analgesic,
antipyretic, anti-inflammatory and anti-platelet agent. In
small doses (80 mg - 100 mg), Acetylsalicylic acid, has
benefits as an anti-platelet or blood thinner which can be
used to prevent platelet aggregation (platelets or platelets)
in patients with myocardial infarction or blockage of the
heart muscle and other conditions. post stroke.
Presentation

• Acetylsalicylic Acid Tablet 500 mg (Aspirin)

• Acetylsalicylic Acid Tablet 80 mg
(Miniaspi)
 INDICATION and DOSAGE

• Acute ischaemic stroke, Angina pectoris, Myocardial

infarction
Adult: For primary prevention: Loading: 150-300 mg
(Chewed and Swalowed).
• Rheumatic disorders
Adult: 4-8 g daily in divided doses for acute disorders.
5.4 g daily in divided doses for chronic conditions.
• Fever, Mild to moderate pain
Adult: Initially, 300-900 mg, repeated 4-6 hourly
according to clinical needs. Max: 4 g daily.
 ACTION

• salicylate that exhibits analgesic, anti-

inflammatory, and antipyretic activities. It is a
selective and irreversible inhibitor of
cyclooxygenase-1 (COX-1) enzyme resulting in
direct inhibition of the biosynthesis of
prostaglandins and thromboxanes from
arachidonic acid. Additionally, it also inhibits
platelet aggregation.
 ONSET and DURATION

• Onset: Platelet inhibition: Within 1 hr (nonenteric-

coated); delayed (enteric-coated); 20 minutes (if
chewed).
• Duration: 4-6 hours (immediate-release); Platelet
inhibition: Approx 10 days
 PHARMACOKINETICS

• Absorption: Rapidly absorbed from the gastrointestinal

tract; less reliable (rectal); absorbed through the skin.
Partially hydrolysed by esterases to salicylate during
absorption in the GI tract. Bioavailability: 50-75%
(immediate-release). Time to peak plasma concentration:
Approx 1-2 hours (nonenteric-coated); 3-4 hours (enteric-
coated); Approx 2 hours (extended-release cap).
 PHARMACOKINETICS

• Distribution: Widely and rapidly distributed into most body tissues and

fluids. Crosses the placenta and enters breast milk. Volume of
distribution: 170 mL/kg. Plasma protein binding: 80-90%.
• Metabolism: Metabolised in the liver into salicyluric acid, salicyl
phenolic glucuronide, salicylic acyl glucuronide, gentisic acid, and
gentisuric acid. Undergoes first-pass metabolism.
• Excretion: Via urine (75% as salicyluric acid, 10% as salicylic acid).
Elimination half-life: 15-20 minutes.
 Adverse Reaction

• Significant: Salicylate sensitivity, tinnitus.

• Blood and lymphatic system disorders: Anaemia,
hypoprothrombinaemia, thrombocytopenia.
• Gastrointestinal disorders: Dyspepsia, gastric irritation, nausea,
vomiting.
• Nervous system disorders: Dizziness, confusion.
• Respiratory, thoracic and mediastinal disorders: Asthma,
bronchospasm, dyspnea, rhinitis.
• Skin and subcutaneous tissue disorders: Rash, urticaria.
 Special Precaution

• Patient with dyspepsia or lesion of the GI mucosa,

• asthma or allergic disorders
• Anaemia, dehydration, menorrhagia
• uncontrolled hypertension
• G6PD deficiency
• Thyrotoxicosis.
• Patients undergoing surgical procedures.
• Moderate hepatic and renal impairment.
• Pregnancy.
 references

• https://www.mims.com/indonesia/drug/info/epinephrine?mtype=generic
• https://www.medicines.org.uk/emc/files/pil.3673.pdf
• National Center for Biotechnology Information. PubChem Database. Aspirin, CID=2244,
https://pubchem.ncbi.nlm.nih.gov/compound/Aspirin (accessed on Jan. 21, 2020)