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Karsten Schrör

Acetylsalicylic Acid

Second Edition

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After the remarkable success of the first edition of this book – a first comprehensive overview of all aspects of pharmacology, toxicology, and clinics of aspirin – both the author and the publisher felt that an updated edition is needed: More than 2500 entries on “aspirin” are found during the last 5 years alone in the publication data base “Pubmed” – every year. Here, a completely revised and actualized edition of the first version is presented, trying to consider all of the relevant information on this remarkable drug until the end of 2015.

A major new finding regarding the pharmacodynamics of aspirin was the detection of numerous hitherto unknown acetylation targets and the increasing awareness that the irreversible and essentially nonselective acetylation process, in case of proteins possibly associated with modifications of their steric structure and function, is the key mechanistic event in the pharmacology of aspirin at doses that are currently used. This is exactly opposite to the original concept at the time of clinical introduction of aspirin in 1899 when the metabolite salicylate was considered to be the active drug and unmetabolized aspirin just an inactive prodrug. The irreversibility of acetylation has also consequences for the duration of aspirin's action. This is determined by the turnover rate of the affected target (protein) rather than by the short half-life of aspirin in the circulation, amounting for only a few minutes.

Interesting news also came from the pharmacokinetics. A new fast-disintegrating aspirin formulation with a more rapid onset of action and about threefold higher peak plasma level was introduced in the market in Germany and some other countries and might replace the standard aspirin tablet in the future.

Significant new patient data have also been generated by the widespread clinical use of the compound. This includes thrombotic diseases such as prevention of arterial and venous thromboembolism and preeclampsia. Another exciting field of clinical research is the possible use of aspirin in chemoprevention of malignant diseases, most notably colorectal cancer. The US-PSTF has just filed a draft to recommend prophylactic aspirin for primary prevention in certain groups of patients at elevated risk. A final recommendation about the use of aspirin in primary prevention will be probably published within the next months. Finally, numerous new clinical trials on aspirin as a single drug or as comedication in several clinical indications have been published since 2010 and are discussed in some detail here.

As in the past, in the making of this new edition, many friends and colleagues worldwide have extended their considerable help and support. I am grateful to all of them. The technical help of Petra Rompel (Düsseldorf) in generating the illustrations is also gratefully acknowledged.

Düsseldorf, March 2016

Karsten Schrör

  1. 1 General Aspects
    1. 1.1 History
    2. 1.2 Chemistry
  2. 2 Pharmacology
    1. 2.1 Pharmacokinetics
    2. 2.2 Cellular Modes of Action
    3. 2.3 Actions on Organs and Tissues
  3. 3 Toxicity and Drug Safety
    1. 3.1 Systemic Side Effects
    2. 3.2 Organ Toxicity
    3. 3.3 Hypersensitivity to Aspirin and Reye's Syndrome
  4. 4 Clinical Applications of Aspirin
    1. 4.1 Thromboembolic Diseases
    2. 4.2 Pain, Fever, and Inflammatory Diseases
    3. 4.3 Further Potential Clinical Indications