Aspirin: A Comprehensive Pharmacological Overview

Aspirin, scientifically known as acetylsalicylic acid (ASA), is a cornerstone in the world of nonsteroidal anti-inflammatory drugs (NSAIDs). With its multifaceted roles as an analgesic, antipyretic, and anti-inflammatory agent, aspirin has secured its position as one of the most frequently administered medications worldwide.

Mechanism of Action

At the heart of aspirin’s mechanism is its ability to irreversibly inhibit the enzyme cyclooxygenase (COX). This action effectively blocks the synthesis of prostaglandins and thromboxanes, molecules that are instrumental in processes like inflammation, pain modulation, fever generation, and blood clotting.

Click here to learn more about COX enzymes.

Pharmacokinetics: Journey in the Body

1. Absorption: Once ingested, aspirin is swiftly absorbed from the stomach and upper part of the small intestine. While the presence of food might slow down this absorption slightly, it doesn’t notably alter the overall amount that enters the bloodstream.
2. Distribution: Post absorption, aspirin doesn’t confine itself to one area. It travels and distributes across all tissues and body fluids, including the central nervous system (CNS).
3. Metabolism: The body doesn’t let aspirin linger for long. It’s rapidly transformed in the plasma into salicylic acid. This metabolite, while echoing some properties of aspirin, is a tad less potent. The liver then takes charge, further metabolizing salicylic acid mainly via the glycine and glucuronic acid pathways.
4. Excretion: The final exit for aspirin and its metabolites is through the kidneys. The speed of this exit is influenced by the pH of the urine. Alkaline conditions hasten the process, whereas acidic conditions tend to slow it down.

Pharmacological Actions Across Organ Systems

• Cardiovascular System: Aspirin’s ability to curtail platelet aggregation is a boon for heart health, offering protection against heart attacks and strokes.
• Gastrointestinal System: It’s not all rosy; aspirin can irritate the stomach lining, heightening the risk of ulcers and associated bleeding.
• Renal System: Prolonged consumption, especially in those with compromised kidney function, might further deteriorate renal health.
• Respiratory System: A word of caution for asthma patients: aspirin might exacerbate symptoms or even trigger bronchospasm in some.

Therapeutic Uses and Doses

• Pain Relief: Aspirin is effective for mild to moderate pain. Typical dose: 325-650 mg every 4 to 6 hours.
• Fever Reduction: It’s a reliable antipyretic. Typical dose: 325-650 mg every 4 to 6 hours.
• Anti-inflammatory: Conditions like rheumatoid arthritis benefit from its anti-inflammatory effects. Typical dose: 2.4-5.4 g daily in divided doses.
• Cardiovascular Protection: A low dose can work wonders in preventing heart attacks and strokes. Typical dose: 75-325 mg daily.

Side Effects

• Gastrointestinal: Users might experience gastric irritation, ulcers, or even bleeding.
• Hematological: Expect prolonged bleeding time and increased susceptibility to bruising.
• Hypersensitivity Reactions: Some might develop rashes, angioedema, or bronchospasm.
• Overdose Symptoms: Overconsumption might lead to tinnitus, vertigo, hyperventilation, and metabolic acidosis.

Salicylism 

Salicylism: Salicylism is a syndrome that results from the chronic ingestion of salicylates, like aspirin, in amounts exceeding the body’s ability to metabolize them. It’s characterized by a constellation of symptoms rather than acute life-threatening toxicity.

Symptoms of Salicylism:

1. Tinnitus (ringing in the ears)
2. Vertigo
3. Decreased hearing
4. Nausea and vomiting
5. Headache
6. Dizziness
7. Hyperpnea (abnormally deep or rapid breathing)
8. Sweating

Treatment of Salicylism:

1. Discontinuation of Salicylate Intake: The first step in treating salicylism is to stop taking any products containing salicylates.
2. Supportive Care: This includes hydration and monitoring of vital signs.
3. Activated Charcoal: In cases of recent overdose, activated charcoal may be administered to reduce the absorption of salicylates from the stomach.
4. Alkalinization of the Urine: This can enhance the excretion of salicylates from the body.
5. Hemodialysis: In severe cases, especially when there are significant metabolic abnormalities or neurological symptoms, hemodialysis may be required to remove salicylates from the bloodstream.

Aspirin Poisoning

Aspirin Poisoning (Acute Salicylate Poisoning): Aspirin poisoning occurs when someone takes a larger amount of aspirin than the body can safely handle. This can be either from a one-time overdose or from chronic poisoning if someone takes large amounts of aspirin over time.

Symptoms of Aspirin Poisoning:

1. Rapid breathing
2. Hyperthermia (increased body temperature)
3. Sweating
4. Ringing in the ears
5. Dehydration
6. Lethargy or confusion
7. Seizures
8. Respiratory alkalosis (early stages) followed by metabolic acidosis (later stages)

Treatment of Aspirin Poisoning:

There is no specific antidote for treatment. However, the condition should be managed by the below procedure:-

1. Decontamination: If the ingestion was recent, activated charcoal may be administered to reduce further absorption of the aspirin from the stomach and intestines.
2. Alkalinization of the urine: Intravenous sodium bicarbonate can be given to alkalinize the urine, which enhances the excretion of salicylates. This is especially beneficial in patients with severe toxicity.
3. Fluids: Intravenous fluids are given to maintain hydration and to replace fluids lost from sweating, vomiting, and increased urination.
4. Hemodialysis: In cases of severe poisoning, hemodialysis can be used to rapidly remove salicylates from the blood, especially if there’s kidney failure or ongoing symptoms despite appropriate treatment.
5. Supportive care: This includes treating symptoms like seizures, fever, and respiratory or metabolic imbalances.
6. Monitoring: Frequent monitoring of blood salicylate levels, blood gases, and other laboratory tests are essential to guide treatment.

Prevention:

• Store medications out of reach of children.
• Always use child-resistant packaging.
• Avoid taking multiple medications that contain salicylates simultaneously.
• Always follow recommended dosages and guidelines.

If someone is suspected of having aspirin poisoning, it’s crucial to seek emergency medical attention immediately. The prognosis is generally good with early detection and treatment, but delays can lead to serious complications and can be fatal.

Contraindications

• Peptic Ulcer Disease: Given the risk of bleeding, those with ulcers should avoid aspirin.
• Asthma: Especially those diagnosed with aspirin-exacerbated respiratory disease.
• Children and Teenagers: Due to the potential development of Reye’s syndrome, especially during viral infections.

Drug Interactions

• Warfarin and other anticoagulants: Combining these can lead to a heightened risk of bleeding.
• Other NSAIDs: The risk of gastrointestinal side effects multiplies.
• Alcohol: A dangerous duo, as it significantly increases the risk of gastrointestinal bleeding.
• Antihypertensives: Aspirin might undermine their efficacy.

This article provides a detailed overview of aspirin’s pharmacology. Specialized pharmacology textbooks or primary research articles are recommended for those seeking an even deeper dive.

Disclaimer: This article is for informational purposes only and should not be taken as medical advice. Always consult with a healthcare professional before making any decisions related to medication or treatment.