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What is the half life of atropine in children? An In-Depth Pharmacological Review

4 min read

The elimination half-life of atropine is more than doubled in children under two years of age compared to older children and adults. So, what is the half life of atropine in children? The answer varies significantly with age, a critical factor in pediatric pharmacology.

Quick Summary

The half-life of intravenous atropine is 6.9 ± 3.3 hours in children under 2 and 2.5 ± 1.2 hours in children over 2. This variation highlights age-dependent pharmacokinetics.

Key Points

  • Age-Dependent Half-Life: The half-life of atropine is significantly longer in children under 2 years (6.9 hours) compared to those over 2 years (2.5 hours).

  • Adult Comparison: The half-life in children over 2 years is similar to that in adults (3.0 hours), while infants and the elderly show prolonged elimination.

  • Mechanism of Action: Atropine is an antimuscarinic agent that blocks acetylcholine receptors, inhibiting parasympathetic effects.

  • Pediatric Uses: Key uses in children include treating bradycardia, pre-anesthetic medication, an antidote for certain poisonings, and ophthalmic use for exams and myopia control.

  • Metabolism: Atropine is primarily metabolized by the liver, and a significant portion is excreted unchanged in the urine. Immature organ function in infants slows this process.

  • Dosing Considerations: Pediatric dosing requires careful calculation, typically weight-based, to ensure appropriate exposure and prevent adverse effects.

  • Side Effects: Common side effects are anticholinergic and include tachycardia, dry mouth, flushing, and blurred vision. Infants are at higher risk due to slower drug clearance.

In This Article

Understanding Atropine and Its Role in Pediatrics

Atropine is a naturally occurring alkaloid derived from the Atropa belladonna plant. It functions as a competitive antagonist of muscarinic acetylcholine receptors, effectively blocking the effects of parasympathetic nervous system stimulation. In clinical practice, this makes atropine an essential medication for various procedures and conditions. Its primary actions include increasing a slow heart rate, reducing secretions like saliva and bronchial mucus, and relaxing smooth muscles.

In pediatric medicine, atropine is used for several specific indications:

  • Symptomatic Bradycardia: It is a first-line treatment for a dangerously slow heart rate, especially when it persists despite adequate oxygenation and ventilation.
  • Anesthesia Premedication: Before surgery, atropine is given to reduce respiratory tract secretions and block cardiovagal reflexes that can occur during procedures.
  • Antidote for Poisoning: It is a crucial antidote for poisoning from organophosphates (found in some pesticides) and certain types of mushrooms. In these cases, large and repeated doses may be necessary to counteract the cholinergic crisis.
  • Ophthalmology: In eye care, atropine drops are used to dilate the pupil (mydriasis) and temporarily paralyze the focusing muscles (cycloplegia) for accurate eye exams in children, especially those with amblyopia (lazy eye) or strabismus (eye turn). Low-dose atropine has also gained significant attention for its effectiveness in slowing the progression of myopia (nearsightedness) in children.

What is the Half Life of Atropine in Children?

The half-life of a drug is the time it takes for the concentration of the drug in the body to be reduced by half. This pharmacokinetic parameter is vital for determining dosing intervals and understanding the duration of a drug's effect. For atropine, the half-life is not a single value but varies dramatically with age, especially in the pediatric population.

According to FDA data, the half-life of intravenous atropine shows significant age-related differences:

  • Children under 2 years: The mean half-life is 6.9 ± 3.3 hours.
  • Children over 2 years: The mean half-life is 2.5 ± 1.2 hours.

This prolonged elimination in infants and toddlers (under 2 years) is a critical consideration for clinicians, as it can lead to a higher risk of side effects if not dosed appropriately. The slower clearance in this age group may be due to immature hepatic (liver) metabolism and renal (kidney) excretion pathways.

Pharmacokinetics: How a Child's Body Processes Atropine

The journey of atropine through a child's body involves absorption, distribution, metabolism, and excretion (ADME).

  • Absorption: Atropine is well absorbed when administered via various routes, including intravenous (IV), intramuscular (IM), and endotracheal.
  • Distribution: After administration, atropine is distributed throughout the body and can cross the blood-brain barrier. Plasma protein binding is around 14% to 22%.
  • Metabolism: The liver is the primary site of metabolism, where atropine is broken down by enzymatic hydrolysis into metabolites like noratropine and atropine-n-oxide. This metabolic process is less efficient in very young children, contributing to the longer half-life.
  • Excretion: A significant portion of the drug, between 13% and 50%, is excreted unchanged in the urine.

Comparison of Atropine Half-Life Across Age Groups

To fully appreciate the pediatric differences, it's useful to compare the half-life of atropine across different age demographics.

Age Group Mean Half-Life (Hours) Standard Deviation Source
Children (< 2 years) 6.9 ± 3.3 hours
Children (> 2 years) 2.5 ± 1.2 hours
Adults (16-58 years) 3.0 ± 0.9 hours
Geriatric (65-75 years) 10.0 ± 7.3 hours

As the table illustrates, the half-life in children over 2 is similar to that of adults. However, both infants and geriatric patients exhibit a significantly prolonged elimination period, highlighting their increased sensitivity to the drug.

Potential Side Effects and Safety Considerations

Given its mechanism of action, atropine's side effects are primarily anticholinergic. In children, it is crucial to monitor for these effects, especially in infants who clear the drug more slowly. Common side effects include:

  • Fast heart rate (tachycardia)
  • Flushing (redness of the skin)
  • Dry mouth and skin
  • Blurred vision and sensitivity to light (photophobia)
  • Difficulty urinating
  • Restlessness or irritability
  • Fever

In cases of overdose, more severe symptoms like hallucinations, delirium, and coma can occur. The use of atropine in neonates and small infants requires careful consideration as the appropriate amount must be calculated precisely to avoid excessive exposure.

Conclusion

The half-life of atropine in children is a dynamic parameter heavily influenced by age. It is approximately 6.9 hours in children under two and shortens to about 2.5 hours in children over two, which is comparable to the adult half-life of 3.0 hours. This prolonged clearance in the youngest pediatric patients is attributed to immature metabolic and excretory functions, underscoring the need for careful, weight-based consideration and vigilant monitoring for anticholinergic side effects. Understanding these pharmacokinetic differences is paramount for the safe and effective use of atropine in the pediatric population, from managing cardiac emergencies to slowing myopia progression.

For more detailed information on drug pharmacokinetics, a valuable resource is the U.S. Food and Drug Administration (FDA) drug label database.

Read more on the FDA's website

Frequently Asked Questions

The mean half-life of intravenous atropine in pediatric subjects under 2 years of age is 6.9 ± 3.3 hours.

In a child over 2 years, like a 5-year-old, the mean half-life is 2.5 ± 1.2 hours, which is very similar to the mean half-life in adults (16-58 years), which is 3.0 ± 0.9 hours.

The elimination half-life of atropine is more than doubled in children under two years old, likely due to immature hepatic (liver) and renal (kidney) function, which leads to decreased drug metabolism and excretion.

In children, atropine is used to treat symptomatic bradycardia (slow heart rate), as a pre-anesthetic to reduce secretions, as an antidote for organophosphate poisoning, and in ophthalmic form for eye exams and to slow myopia progression.

Atropine dosing for symptomatic bradycardia in children is typically calculated based on their weight to ensure an appropriate amount is administered.

Yes, common side effects in children are related to its anticholinergic properties and include fast heart rate, flushing, dry mouth, blurred vision, and restlessness. The risk is higher in children under 2 due to the longer half-life.

Atropine is eliminated through a combination of enzymatic hydrolysis (metabolism) in the liver and excretion of the unchanged drug in the urine. About 13% to 50% of a dose is excreted unchanged by the kidneys.

References

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Medical Disclaimer

This content is for informational purposes only and should not replace professional medical advice.