Propylthiouracil

Generic name
Propylthiouracil
Brand name
ATC Code
H03BA02
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Propylthiouracil

Dosages
Side effects in children
Warnings & precautions in children
Contra-indications in children

Interactions
PK
Renal impairment
References

Pharmacokinetics in children

In a 1988 study of 7 children and adolescents with unknown doses [Hoffman 1988]: (1)
T½ = 1.47 hours (with hyperthyroidism) and 1.53 hours (with euthyroid status), not significantly different.
 

dose recommendation of formulary compared to licensed use (on-label versus off-label)

No information is present at this moment.

Available formulations

No information is present at this moment.

Dosages

Hyperthyroidism if alternative is not possible
  • Oral
    • Term neonate
      • Initial dose: 5 - 10 mg/kg/day in 3 doses. Until euthyroid status is achieved
        Maintenance dose: Adjust the maintenance dosage based on the hormone levels or add levothyroxine.

      • Under 10 years of age, there is little evidence about the optimum and safe doses. Read the warnings and precautions for use in children before administering.

    • 1 month up to 10 years
      • Initial dose: 5 - 7 mg/kg/day in 3 doses. Max: 300 mg/day. Until euthyroid status is achieved.
        Maintenance dose: Adjust the maintenance dosage based on the hormone levels or add levothyroxine.

      • Under 10 years of age, there is little evidence about the optimum and safe doses. Read the warnings and precautions for use in children before administering.

    • 10 years up to 12 years
      [11] [12]
      • Initial dose: 75 - 225 mg/day in 3 doses. 100–300 mg/day orally in 4 doses can possibly be given (observe a dosing interval of 6 hours strictly)
        Until euthyroid status is achieved.
        Maintenance dose: Adjust the maintenance dosage based on the hormone levels or add levothyroxine.
    • 12 years up to 18 years
      [11] [12]
      • Initial dose: 225 - 300 mg/day in 3 doses. 300–400 mg/day orally in 4 doses can possibly be given (observe a dosing interval of 6 hours strictly)
        Until euthyroid status is achieved.
        Maintenance dose: Adjust the maintenance dosage based on the hormone levels or add levothyroxine..

Renal impaiment in children > 3 months

GFR ≥10 ml/min/1.73m2: Dose adjustment not required.

GFR <10 ml/min/1.73m2: A general recommendation on dose adjustment cannot be provided.

The complete list of all undesirable drug reactions can be found in the national Summary of Product Characteristics (SmPC) – click here

Side effects in children

Using propylthiouracil can lead to liver damage and acute liver failure, which can be fatal. Monitoring the liver function and symptoms of liver damage is required, especially in the first 6 months after commencing treatment.

The complete list of all contra-indications can be found in the national Summary of Product Characteristics (SmPC) – click here

Contra-indications

No information available on specific contra indications in children.

The complete list of all warnings and precautions can be found in the national Summary of Product Characteristics (SmPC) – click here

Warnings & precautions in children

Because of the increased risk of serious and fatal liver damage, it should not be used in children unless other therapies are not possible or not tolerated (this also applies for adults, but the effect is more prominent in children). Primarily observed at doses of 300 mg/day upwards, but in some cases already at just 50 mg/day.

Interactions

The complete list of all interactions can be found in the national Summary of Product Characteristics (SmPC) – click here

ANTITHYROID PREPARATIONS

This pages provides a list of drugs from the same ATC class for comparison. This does not necessarily mean that these drugs are interchangeable.

Sulfur-containing imidazole derivatives
H03BB01
H03BB02

References

  1. Hoffman WH, et al, Pharmacokinetics of propylthiouracil in children and adolescents with Graves' disease in the hyperthyroid and euthyroid states, Dev Pharmacol Ther, 1988, 11(2), 73-81
  2. FDA, Black box warning propylthiouracil, http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm164162.htm
  3. Gao Y, et al, Long-term outcomes of patients with propylthiouracil-induced anti-neutrophil cytoplasmic auto-antibody-associated vasculitis, Rheumatology (Oxford)., 2008 , Oct;47(10), 1515-20
  4. Glaser NS, et al, Organization of Pediatric Endocrinologists of Northern California Collaborative Graves' Disease Study G. Predicting the likelihood of remission in children with Graves' disease: a prospective, multicenter study, Pediatrics, 2008, Mar;121(3), e481-8
  5. Gorton C, et al, Remission in children with hyperthyroidism treated with propylthiouracil. Long-term results, Am J Dis Child, 1987 , Oct;141(10), 1084-6
  6. Karras S, et al, Toxicological considerations for antithyroid drugs in children, Expert Opin Drug Metab Toxicol., 2011 , Apr;7(4), 399-410
  7. Lian XL, et al, [The clinical characteristics of symptomatic propylthiouracil-induced hepatic injury in patients with hyperthyroidism], Zhonghua Nei Ke Za Zhi, 2004, Jun;43(6), 442-6
  8. Malozowski S, et al, Propylthiouracil-induced hepatotoxicity and death. Hopefully, never more. . , J Clin Endocrinol Metab, 2010, Jul;95(7), 3161-3
  9. Rivkees SA, et al, Dissimilar hepatotoxicity profiles of propylthiouracil and methimazole in children, J Clin Endocrinol Metab, 2010 , Jul;95(7), 3260-7
  10. Sato H, et al, Comparison of methimazole and propylthiouracil in the management of children and adolescents with Graves' disease: efficacy and adverse reactions during initial treatment and long-term outcome., J Pediatr Endocrinol Metab, 2011, 24(5-6), 257-63
  11. Aurobindo Pharma B.V, SmPC Propylthiouracil (RVG 52546) 04-01-2024, www.geneesmiddeleninformatiebank.nl
  12. Admeda Artzneimittel GmHB, SmPC Propycil (6075593.00.00), 09/2019

Changes

Therapeutic Drug Monitoring


Overdose