Acetylsalicylic acid

Author: Prof. Dr. med. Peter Altmeyer

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Last updated on: 12.11.2021

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Synonym(s)

Aspirin; ASS

Definition
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Frequently used remedy for mild to moderate pain.

ASA has analgesic, antipyretic, antiphlogistic effects and inhibits platelet aggregation. Prostaglandin synthesis is inhibited by irreversible inhibition of cyclooxygenase.

Half-life
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15 minutes.

Pharmacodynamics (Effect)
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ASA has an exceptional position within the COX inhibitors. The acetylation of salicylic acid (a development of the chemist Felix Hofmann) improved the tolerability and expanded the active profile of salicylic acid. This is because the acetyl group, which is rapidly cleaved in the portal circulation (HWZ of ASS only 15 -20 min!), has clinical effects that go beyond COX inhibition. ASA has still been shown to inhibit the proinflammatory ubiquitous transcription factor NFκB, iNOS, and COX-2 expression. These effects are probably independent of enzymatic COX inhibition.

Spectrum of action
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Pharmacokinetic data show that ASA is rapidly (HWZ: 15min) and presystemically (in the mucosa of stomach and dodenum) converted to the active metabolite salicylic acid (SS) by cleavage of the acyl moiety. COX inhibition by ASA is irreversible. PG synthesis is inhibited by SS inhibiting transcription of the inducible COX-2 gene and thus inhibiting COX-2 synthesis. SS is excreted directly or in the form of inactive (after conjugation with glucuronic acid or glycine in the liver) metabolites) in a pH-dependent manner via the kidneys.

Indication
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Acute pain

Acute treatment of the various forms of coronary heart disease, cerebrovascular diseases, PAD.

secondary prevention of myocardial and cerebral infarction

Follow-up treatment of crown interventions (balloon dilatation, stent implantation) and aortocronary bypass surgery (100mgASS+75mg clopedigrel)

Aftercare of venous thromboembolism

Polcythaemia vera (100mg/day)

Dosage and method of use
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Depending on the indication, the standard dosage varies greatly. Usual single doses for adults are:

  • 100 mg for blood thinning (1 x daily as a permanent treatment)
  • 300 - 1000 mg as analgesic (several times a day at intervals of 4-8 hours)
  • 1000 mg for migraine
  • The maximum daily dose is usually 3000 mg. For the treatment of acute and chronic inflammatory diseases such as rheumatoid arthritis, daily doses of 4-8 g may be used.

Undesirable effects
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Common: Mild gastrointestinal discomfort. Occasional: Hyperhidrosis, nausea, vomiting, diarrhoea. Rarely (especially after long-term therapy) gastric bleeding or gastric ulcers. Transaminases increase with high-dose therapy.

Notice. ASA can have a relapsing-active effect in approx. 20-30% of patients with chronic urticaria, but can also trigger angioedema or anaphylactic shock (see intolerance reaction below).

Rare: serious bleeding such as cerebral haemorrhage, haemolysis and haemolytic anaemia (in patients with severe glucose-6-phosphate dehydrogenase deficiency), haemorrhage such as. Nasal bleeding, gingival bleeding, skin bleeding, or urogenital tract bleeding with possible prolongation of bleeding time, hypersensitivity reactions of the respiratory tract, gastrointestinal tract, and cardiovascular system, especially in asthmatics (possible symptoms include: Drop in blood pressure, attacks of shortness of breath, rhinitis, nasal congestion, anaphylactic shock or Quincke's oedema), headache, dizziness, impaired hearing, ringing in the ears (tinnitus) (may be signs of overdose), mental confusion (may be signs of overdose), visual disturbances (may be signs of overdose), somnolence (may be signs of overdose), Gastrointestinal ulcers, which very rarely may lead to perforation, Gastrointestinal bleeding, which very rarely may lead to iron deficiency anemia, Gastrointestinal inflammation, Thrombocytopenia, Granulocytosis, Hemorrhagic vasculitis, Hypersensitivity reactions such as severe skin reactions (up to erythema multiforme), Menorrhagia, Reye's syndrome.

A syndromal combination with aspirin intolerance, asthma and polyposis nasi has been described as Widal 's disease and plays a role in ENT medicine.

Notice. Dizziness and tinnitus can be symptoms of an overdose (especially in children and elderly patients).

Interactions
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See Table 1.

Preparations
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Aspirin, ASS, Alka-Seltzer, Godamed, Thomapyrin acute, Togal ASS

Note(s)
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The biography of ASS already shows many elements of the modern pharmaceutical business at the end of the 19th century. First of all, the question of patenting: the Imperial Patent Office had rejected the application to patent the acetylation of salicylic acid. The question of the trade name had to be based on the biological origin of salicylaldehyde from flowers of meadowsweet (Spiraea syn. Filipendula ulmaria). The trade name "Euspirin" was also available. In the end, the vowel "A" (from acetyl) won the race. During World War I, Bayer lost company assets and protection for patents and trademarks, including that of Aspirin®, in the United States in 1917. It was not until 1994 that Bayer was able to reacquire the rights to its own name and to Aspirin® in the United States through the acquisition of Sterling-Winthrop.

Tables
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Major drug interactions of acetylsalicylic acid

ACE inhibitor

Effect of the ACE inhibitor ↓

Alcohol

Alcohol level ↑

Antihypertensives

antihypertensive effect ↓

Anti-inflammatory drugs, non-steroidal

reciprocal effect ↑

Acetazolamide

metabolic acidosis, CNS toxicity ↑

Benzbromarone

Benzbromarone action ↓

Benzoic acid

Cross-allergy

Cephalosporins

Bleeding tendency ↑

Coumarins

Bleeding tendency ↑

Digoxin

Digoxin level ↑

Dihydroergotamine

Bleeding tendency ↑

Fibrinolytics

Bleeding tendency ↑

Glucocorticoids

Acetylsalicylic acid levels ↓, risk of salicylate intoxication after sudden discontinuation of long-term corticosteroid therapy, gastrointestinal bleeding

Heparin

Bleeding tendency ↑, avoid combination

Imipramine

Deaths described in ASA overdose, avoid combination

Indometacin

Gastric bleeding, indomethacin effect ↓

Potassium iodide

Gastric mucosal damage, avoid combination

Caffeine

Drug abuse

Lithium salt

Lithium toxicity ↑

Metformin

Lactic acidosis

Midazolam

Midazolam effect ↑

Mucopolysaccharide polysulfate

Bleeding tendency ↑

Nitrazepam

Tear production ↓,

Cave: Sicca syndrome.

Penicillins i.v.

Bleeding tendency ↑

Prednimustine

Bleeding tendency ↑

Probenecid

Probenecid effect ↓

Saluretics

Saluretic effect ↓, CNS toxicity ↑

Thyroid hormones

Thyroid hormone levels ↑

Loop diuretics

Diuretic effect ↓ in renal failure or liver cirrhosis with ascites, CNS toxicity ↑

Sulfinpyrazone

Sulfinpyrazone effect ↓

Sulfonylureas

Hypoglycemia

Tartrazine

Cross-allergy

Thiazide diuretics

Diuretic effect ↓, CNS toxicity ↑.

Ticlopidine

Bleeding tendency ↑, avoid combination

Valproic acid

Bleeding tendency ↑, valproic acid levels ↑, avoid combination

Zidovudine

Zidovudine toxicity ↑

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Last updated on: 12.11.2021