Propylthiouracil

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Propylthiouracil
Black Box Warning
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Adeel Jamil, M.D. [2]

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Black Box Warning

WARNING
See full prescribing information for complete Boxed Warning.
* Severe liver injury and acute liver failure, in some cases fatal, have been reported in patients treated with propylthiouracil. These reports of hepatic reactions include cases requiring liver transplantation in adult and pediatric patients.
  • Propylthiouracil should be reserved for patients who can not tolerate methimazole and in whom radioactive iodine therapy or surgery are not appropriate treatments for the management of hyperthyroidism.
  • Because of the risk of fetal abnormalities associated with methimazole, proplythiouracil may be the treatment of choice when an antithyroid drug is indicated during or just prior to the first trimester of pregnancy.

Overview

Propylthiouracil is a thyroid hormone antagonist and anti thyroide drug that is FDA approved for the treatment of Graves' disease with hyperthyroidism or toxic multinodular goiter, and to ameliorate symptoms of [[hyperthyroidism]] in preparation for thyroidectomy. There is a Black Box Warning for this drug as shown here. Common adverse reactions include nausea, vomiting, epigastric distress, loss of taste, arthralgia, paresthesias, myalgia, headache, drowsiness, pruritus, skin rash and urticaria.

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

  • Propylthiouracil is indicated:
  • in patients with Graves' disease with hyperthyroidism or toxic multinodular goiter who are intolerant of methimazole and for whom surgery or radioactive iodine therapy is not an appropriate treatment option.
  • to ameliorate symptoms of hyperthyroidism in preparation for thyroidectomy or radioactive iodine therapy in patients who are intolerant of methimazole.

Dosing Information

  • Propylthiouracil is administered orally. The total daily dosage is usually given in 3 equal doses at approximately 8-hour intervals.
Adults
  • The initial dose is 300 mg daily. In patients with severe hyperthyroidism, very large goiters, or both, the initial dose may be increased to 400 mg daily; an occasional patient will require 400 to 900 mg daily initially. The usual maintenance dose is 100 to 150 mg daily. In general, dose selection for an elderly patient should be cautious, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.
Geriatric Use
  • Clinical studies of propylthiouracil did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should be cautious, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Propylthiouracil in adult patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Propylthiouracil in adult patients.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

  • Propylthiouracil is generally not recommended for use in the pediatric patient population except in rare instances in which other alternative therapies are not appropriate options. Studies evaluating appropriate dosing regimen have not been conducted in the pediatric population although general practice would suggest initiation of therapy in patients 6 years or older at a dosage of 50 mg daily with careful upward titration based on clinical response and evaluation of TSH and free T4 levels. Although cases of severe liver injury have been reported with doses as low as 50 mg/day, most cases were associated with doses of 300 mg/day and higher.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Propylthiouracil in pediatric patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Propylthiouracil in pediatric patients.

Contraindications

Warnings

WARNING
See full prescribing information for complete Boxed Warning.
* Severe liver injury and acute liver failure, in some cases fatal, have been reported in patients treated with propylthiouracil. These reports of hepatic reactions include cases requiring liver transplantation in adult and pediatric patients.
  • Propylthiouracil should be reserved for patients who can not tolerate methimazole and in whom radioactive iodine therapy or surgery are not appropriate treatments for the management of hyperthyroidism.
  • Because of the risk of fetal abnormalities associated with methimazole, proplythiouracil may be the treatment of choice when an antithyroid drug is indicated during or just prior to the first trimester of pregnancy.

Liver Toxicity

Agranulocytosis
Hypothyroidism

PRECAUTIONS

General

Adverse Reactions

Clinical Trials Experience

  • To report SUSPECTED ADVERSE REACTIONS, contact West-ward Pharmaceutical Corp. at 1-877-233-2001 or the FDA at 1-800-FDA-1088 or WWW.FDA.GOV/MEDWATCH.

Postmarketing Experience

There is limited information regarding Postmarketing Experience of Propylthiouracil in the drug label.

Drug Interactions

Anticoagulants (oral)=

Beta-adrenergic blocking agents
Digitalis Glycosides
Theophylline

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA): D


Pregnancy Category (AUS):

  • Australian Drug Evaluation Committee (ADEC) Pregnancy Category

There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Propylthiouracil in women who are pregnant.

Labor and Delivery

There is no FDA guidance on use of Propylthiouracil during labor and delivery.

Nursing Mothers

  • Propylthiouracil is transferred to breasdt milk to a small extent and therefore likely results in clinically insignificant doses to the suckling infant. One one study, nine lactating women were administered 400 mg of propylthiouracil by mouth. The mean amount of propylthiouracil excreted during 4 hours after drug administration was 0.025% of the administered dose.

Pediatric Use

Geriatic Use

There is no FDA guidance on the use of Propylthiouracil with respect to geriatric patients.

Gender

There is no FDA guidance on the use of Propylthiouracil with respect to specific gender populations.

Race

There is no FDA guidance on the use of Propylthiouracil with respect to specific racial populations.

Renal Impairment

There is no FDA guidance on the use of Propylthiouracil in patients with renal impairment.

Hepatic Impairment

There is no FDA guidance on the use of Propylthiouracil in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Propylthiouracil in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Propylthiouracil in patients who are immunocompromised.

Administration and Monitoring

Administration

Monitoring

Laboratory Tests
  • Thyroid function tests should be monitored periodically during therapy. Once clinical evidence of hyperthyroidism has resolved, the finding of an elevated serum TSH indicates that a lower maintenance dose of propylthiouracil should be employed.

IV Compatibility

There is limited information regarding IV Compatibility of Propylthiouracil in the drug label.

Overdosage

Signs and Symptoms
  • No information is available on the following: LD50: concentration of propylthiouracil in biologic fluids associated with toxicity and/or death; the amount of drug in a single dose usually associated with symptoms of overdosage; or the amount of propylthiouracil in a single dose likely to be life-threatening.
Treatment
  • In the event of an overdose, appropriate supportive treatment should be initiated as dictated by the patient's medical status.

Pharmacology

Propylthiouracil
Propylthiouracil.png
Propylthiouracil-3D-balls.png
Clinical data
AHFS/Drugs.comMonograph
MedlinePlusa682465
Pregnancy
category
  • D
Routes of
administration
Oral
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability80%-95%
Metabolism?
Elimination half-life2 hours
Excretion?
Identifiers
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
E number{{#property:P628}}
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Chemical and physical data
FormulaC7H10N2OS
Molar mass170.233 g/mol
3D model (JSmol)
  (verify)

Mechanism of Action

Structure

This image is provided by the National Library of Medicine.

Pharmacodynamics

There is limited information regarding Pharmacodynamics of Propylthiouracil in the drug label.

Pharmacokinetics

  • Propylthiouracil is readily absorbed and is extensively metabolized. Approximately 35% of the drug is excreted in the urine, in intact and in conjugated forms, within 24 hours.

Nonclinical Toxicology

There is limited information regarding Nonclinical Toxicology of Propylthiouracil in the drug label.

Clinical Studies

Carcinogenesis, Mutagenesis, Impairment of Fertility

How Supplied

Propylthiouracil Tablets, USP, 50 mg: White, Round, Scored Tablet, Debossed “West-ward 480”.

Bottles of 100 tablets.

Bottles of 1000 tablets.

Unit Dose Boxes of 100 tablets.

Dispense in a tight, light-resistant container as defined in the USP using a child-resistant closure.

Reference:

International Agency for Research on Cancer, IARC Monographs on the Evaluation of the Carcinogenic Risk of Chemicals to Man. 1974; 7:67-76.

Manufactured By: West-ward Pharmaceutical Corp. Eatontown, NJ 07724 Revised August 2011

Storage

  • Store at 20-25°C (68-77°F) [See USP Controlled Room Temperature]. Protect from light and moisture.

Images

Drug Images

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This pill image is provided by the National Library of Medicine's PillBox.

Package and Label Display Panel

Propylthiouracil Tablets, USP

50 mg

100 Tablets

NDC 0143-1480-01

Propylthiouracil drug lable.png
This image of the FDA label is provided by the National Library of Medicine.

Patient Counseling Information

Patients should be advised that if they become pregnant or intend to become pregnant white taking an antithyroid drug, they should contact their physician immediately about their therapy.

Patients should report immediately any evidence of illness, particularly sore throat, skin eruptions, fever, headache, or general malaise. They also should report symptoms suggestive of hepatic dysfunction (anorexia, pruritis, right upper quadrant pain, etc).

Precautions with Alcohol

  • Alcohol-Propylthiouracil interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

There is limited information regarding Propylthiouracil Brand Names in the drug label.

Look-Alike Drug Names

There is limited information regarding Propylthiouracil Look-Alike Drug Names in the drug label.

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.


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