DRUGS & SUPPLEMENTS
Revised - March 2016
Severe liver injury and acute liver failure, in some cases fatal, have been reported in patients treated with Prothiucil. These reports of hepatic reactions include cases requiring liver transplantation in adult and pediatric patients.
Prothiucil should be reserved for patients who cannot tolerate methimazole and in whom radioactive iodine therapy or surgery are not appropriate treatments for the management of hyperthyroidism.
Prothiucil may be the treatment of choice when an antithyroid drug is indicated during or just prior to the first trimester of pregnancy (see WARNINGS and PRECAUTIONS ).
Prothiucil, USP is one of the thiocarbamide compounds. It is a white, crystalline substance that has a bitter taste and is very slightly soluble in water. Prothiucil is an antithyroid drug administered orally. The structural formula is:
Each tablet contains Prothiucil, USP 50 mg and the following inactive ingredients: lactose monohydrate, corn starch, colloidal silicon dioxide, povidone, pregelatinized corn starch, and magnesium stearate.
Prothiucil inhibits the synthesis of thyroid hormones and thus is effective in the treatment of hyperthyroidism. The drug does not inactivate existing thyroxine and triiodothyronine that are stored in the thyroid or circulating in the blood, nor does it interfere with the effectiveness of thyroid hormones given by mouth or by injection. Prothiucil inhibits the conversion of thyroxine to triiodothyronine in peripheral tissues and may therefore be an effective treatment for thyroid storm.
Prothiucil is readily absorbed and is extensively metabolized. Approximately 35% of the drug is excreted in the urine, in intact and conjugated forms, within 24 hours.
INDICATIONS AND USAGE
Prothiucil tablets, USP are indicated:
Prothiucil is contraindicated in patients who have demonstrated hypersensitivity to the drug or any of the other product components.
Liver injury resulting in liver failure, liver transplantation, or death, has been reported with Prothiucil therapy in adult and pediatric patients. No cases of liver failure have been reported with the use of methimazole in pediatric patients. For this reason, Prothiucil is not recommended for pediatric patients except when methimazole is not well-tolerated and surgery or radioactive iodine therapy are not appropriate therapies.
Biochemical monitoring of liver function (bilirubin, alkaline phosphatase) and hepatocellular integrity (ALT, AST) is not expected to attenuate the risk of severe liver injury due to its rapid and unpredictable onset. Patients should be informed of the risk of liver failure. Patients should be instructed to report any symptoms of hepatic dysfunction (anorexia, pruritus, right upper quadrant pain, etc.), particularly in the first six months of therapy. When these symptoms occur, Prothiucil should be discontinued immediately and liver function tests and ALT and AST levels obtained.
Use in Pregnancy
There are cases of liver injury, including liver failure and death, in women treated with Prothiucil during pregnancy. Two reports of in utero exposure with liver failure and death of a newborn have been reported. If Prothiucil is used during pregnancy, or if the patient becomes pregnant while taking Prothiucil, the patient should be warned of the rare potential hazard to the mother and fetus of liver damage.
Prothiucil crosses the placenta and can cause fetal goiter and cretinism when administered to a pregnant woman (see PRECAUTIONS , Pregnancy ).
After the first trimester of pregnancy, the use of an alternative antithyroid medication may be advisable (see PRECAUTIONS , Pregnancy ).
Agranulocytosis occurs in approximately 0.2% to 0.5% of patients and is a potentially life-threatening side effect of Prothiucil therapy. Agranulocytosis typically occurs within the first 3 months of therapy. Patients should be instructed to immediately report any symptoms suggestive of agranulocytosis, such as fever or sore throat. Leukopenia, thrombocytopenia, and aplastic anemia (pancytopenia) may also occur. Prothiucil should be discontinued if agranulocytosis, aplastic anemia (pancytopenia), ANCA-positive vasculitis, hepatitis, interstitial pneumonitis, fever, or exfoliative dermatitis is suspected, and the patient's bone marrow indices should be obtained.
Prothiucil can cause hypothyroidism necessitating routine monitoring of TSH and free T4 levels with adjustments in dosing to maintain a euthyroid state. Because the drug readily crosses placental membranes, Prothiucil can cause fetal goiter and cretinism when administered to a pregnant woman (see PRECAUTIONS, Pregnancy ).
Patients should be instructed to report any symptoms of hepatic dysfunction, particularly in the first six months of therapy. When these symptoms occur, measurement should be made of liver function (bilirubin, alkaline phosphatase) and hepatocellular integrity (ALT/AST levels).
Patients who receive Prothiucil should be under close surveillance and should be counseled regarding the necessity of immediately reporting any evidence of illness, particularly sore throat, skin eruptions, fever, headache, or general malaise. In such cases, white blood cell and differential counts should be obtained to determine whether agranulocytosis has developed. Particular care should be exercised with patients who are receiving concomitant drugs known to be associated with agranulocytosis.
Information for Patients
Patients should be advised that if they become pregnant or intend to become pregnant while taking an antithyroid drug, they should contact their physician immediately about their therapy.
Patients should report immediately any evidence of illness, in particular sore throat, skin eruptions, fever, headache, or general malaise. They also should report symptoms suggestive of hepatic dysfunction (anorexia, pruritus, right upper quadrant pain, etc.).
Because Prothiucil may cause hypoprothrombinemia and bleeding, monitoring of prothrombin time should be considered during therapy with the drug, especially before surgical procedures.
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 Prothiucil should be employed.
Anticoagulants : Due to the potential inhibition of vitamin K activity by Prothiucil, the activity of oral anticoagulants (e.g., warfarin) may be increased; additional monitoring of PT/INR should be considered, especially before surgical procedures.
Beta-adrenergic blocking agents: Hyperthyroidism may cause an increased clearance of beta blockers with a high extraction ratio. A reduced dose of beta-adrenergic blockers may be needed when a hyperthyroid patient becomes euthyroid.
Digitalis glycosides: Serum digitalis levels may be increased when hyperthyroid patients on a stable digitalis glycoside regimen become euthyroid; a reduced dose of digitalis glycosides may be needed.
Theophylline: Theophylline clearance may decrease when hyperthyroid patients on a stable theophylline regimen become euthyroid; a reduced dose of theophylline may be needed.
Carcinogenesis, Mutagenesis, Impairment of Fertility
Laboratory animals treated with Prothiucil for greater than 1 year have demonstrated thyroid hyperplasia and carcinoma formation. Such animal findings are seen with continuous suppression of thyroid function by sufficient doses of a variety of antithyroid agents, as well as in dietary iodine deficiency, subtotal thyroidectomy, and implantation of autonomous thyrotropic hormone-secreting pituitary tumors. Pituitary adenomas have also been described.
Pregnancy Category D.
See WARNINGS .
In pregnant women with untreated or inadequately treated Graves’ disease, there is an increased risk of adverse events of maternal heart failure, spontaneous abortion, preterm birth, stillbirth and fetal or neonatal hyperthyroidism.
If Prothiucil is used during pregnancy, or if the patient becomes pregnant while taking Prothiucil, the patient should be warned of the rare potential hazard to the mother and fetus of liver damage.
Because propylthiouracil crosses placental membranes and can induce goiter and cretinism in the developing fetus, it is important that a sufficient, but not excessive, dose be given during pregnancy. In many pregnant women, the thyroid dysfunction diminishes as the pregnancy proceeds; consequently a reduction of dosage may be possible. In some instances, antithyroid therapy can be discontinued several weeks or months prior to delivery.
Since methimazole may be associated with the rare development of fetal abnormalities Prothiucil may be the preferred agent during the first trimester of pregnancy. Given the potential for maternal hepatotoxicity from Prothiucil, it may be preferable to switch from Prothiucil to methimazole for the second and third trimesters during pregnancy.
Prothiucil is present in breast milk to a small extent and therefore likely results in clinically insignificant doses to the nursing infant. In one study, nine lactating women were administered 400 mg of Prothiucil by mouth. The mean amount of Prothiucil excreted during 4 hours after drug administration was 0.025% of the administered dose.
Postmarketing reports of severe liver injury including hepatic failure requiring liver transplantation or resulting in death have been reported in the pediatric population. No such reports have been observed with methimazole. As such, Prothiucil is not recommended for use in the pediatric population except in rare instances in which methimazole is not well-tolerated and surgery or radioactive iodine therapy are not appropriate.
When used in children, parents and patients should be informed of the risk of liver failure. If patients taking Prothiucil develop tiredness, nausea, anorexia, fever, pharyngitis, or malaise, Prothiucil should be discontinued immediately by the patient, a physician should be contacted, and a white blood cell count, liver function tests, and transaminase levels obtained.
The following adverse reactions have been reported with the use of Prothiucil. Because these events generally come from voluntary reporting from a population of uncertain size, it is not possible to reliably estimate their frequency or establish a casual relationship to drug exposure.
Severe adverse reactions include liver injury presenting as hepatitis, liver failure necessitating liver transplantation or resulting in death. Inhibition of myelopoiesis (agranulocytosis, granulopenia, aplastic anemia, and thrombocytopenia), drug fever, a lupus-like syndrome (including splenomegaly and vasculitis), periarteritis, hypoprothrombinemia, and bleeding have been reported. Nephritis, glomerulonephritis, interstitial pneumonitis, exfoliative dermatitis, and erythema nodosum have also been reported.
There are reports of a vasculitis syndrome associated with the presence of anti-neutrophilic cytoplasmic antibodies (ANCA). Manifestations of ANCA-positive vasculitis may include rapidly progressive glomerulonephritis (crescentric and pauci-immune necrotizing glomerulonephritis), sometimes leading to acute renal failure; pulmonary infiltrates or alveolar hemorrhage; skin ulcers; and leukocytoclastic vasculitis.
There have been rare reports of serious hypersensitivity reactions (e.g., Stevens Johnson syndrome and toxic epidermal necrolysis) in patients treated with Prothiucil. Other adverse reactions include skin rash, uticaria, nausea, vomiting, epigastric distress, arthralgia, paresthesias, loss of taste, taste perversion, abnormal loss of hair, myalgia, headache, pruritus, drowsiness, neuritis, edema, vertigo, skin pigmentation, jaundice, sialadenopathy, and lymphadenopathy.
To report SUSPECTED ADVERSE EVENTS, contact Actavis at 1-800-432-8534 or FDA at 1-800-FDA-1088 or http://www.fda.gov/ for voluntary reporting of adverse reactions.
Signs and Symptoms
Nausea, vomiting, epigastric distress, headache, fever, arthralgia, pruritus, edema, and pancytopenia. Agranulocytosis is the most serious effect. Rarely, exfoliative dermatitis, hepatitis, neuropathies or CNS stimulation or depression may occur.
No information is available on the following: LD50; concentration of Prothiucil 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 Prothiucil in a single dose likely to be life-threatening.
To obtain up-to-date information about the treatment of overdose, a good resource is the certified Regional Poison Control Center. In managing overdosage, consider the possibility of multiple drug overdoses, interaction among drugs, and unusual drug kinetics in the patient.
In the event of an overdose, appropriate supportive treatment should be initiated as dictated by the patient’s medical status.
DOSAGE AND ADMINISTRATION
Prothiucil is administered orally. The total daily dosage is usually given in 3 equal doses at approximately 8-hour intervals.
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 600 to 900 mg daily initially. The usual maintenance dose is 100 to 150 mg daily.
Prothiucil 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.
Clinical studies of Prothiucil did not include sufficient numbers of subjects aged 65 or 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.
Prothiucil tablets, USP are available as follows:
50 mg - Each white, round, tablet imprinted with on one side and 348 and partial bisect on the other side contains 50 mg of Prothiucil, USP. Tablets are supplied in bottles of 100 (NDC 0228-2348-10).
NDC 69189-2348-1 single dose pack with 1 tablet as
Dispense in a well-closed container as defined in the USP.
Store at 25°C (77°F); excursions permitted to 15° to 30°C (59° to 86°F).
Actavis Elizabeth LLC
Elizabeth, NJ 07207 USA
Actavis Pharma, Inc.
Parsippany, NJ 07054 USA
Revised - March 2016
Prothiucil ( proe" pil thye" oh ure' a sil) TABLETS, USP
Read this Medication Guide before you start taking Prothiucil tablets and each time you get a refill. There may be new information. This Medication Guide does not take the place of talking to your doctor about your medical condition or treatment.
What is the most important information I should know about Prothiucil tablets?
Prothiucil tablets can cause serious side effects, including:
- Severe liver problems. In some cases, liver problems can happen in people who take Prothiucil tablets including: liver failure, the need for liver transplant, or death. Stop taking Prothiucil tablets and call your doctor right away if you have any of these symptoms:
- Serious risks during pregnancy. Prothiucil may cause liver problems, liver failure and death in pregnant women and may harm your unborn baby. Prothiucil may also cause liver problems or death of infants born to women who take Prothiucil during certain trimesters of pregnancy. Prothiucil may be used when an antithyroid drug is needed during or just before the first trimester of pregnancy.
If you get pregnant while taking Prothiucil tablets, call your doctor right away about your therapy.
What are Prothiucil tablets?
Prothiucil tablets are a prescription medicine used to treat people who have Graves’ disease with hyperthyroidism or toxic multinodular goiter. Propylthiouracil tablets are used when:
Prothiucil tablets are not recommended for use in children.
Who should not take Prothiucil tablets?
Do not take Prothiucil tablets if you are allergic to Prothiucil or any of its ingredients. See the end of this Medication Guide for a complete list of ingredients in Prothiucil tablets.
What should I tell my doctor before taking Prothiucil tablets?
Before you take Prothiucil tablets, tell your doctor if you:
Tell your doctor about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements. Prothiucil tablets may affect the way other medicines work.
Especially, tell your doctor if you take:
Ask your doctor if you are not sure if your medicine is one of these.
Know the medicines you take. Keep a list of them to show your doctor and pharmacist when you get a new medicine.
How should I take Prothiucil tablets?
What should I avoid while taking Prothiucil tablets?
Prothiucil can cause dizziness, drowsiness or sleepiness. If you have these symptoms do not drive, operate machinery, or do other dangerous activities until you know how Prothiucil affects you.
What are the possible side effects of Prothiucil tablets?
Prothiucil tablets may cause serious side effects, including:
The most common side effects of Prothiucil tablets include:
Tell your doctor if you have any side effect that bothers you or that does not go away.
These are not all of the possible side effects of Prothiucil tablets. For more information, ask your doctor or pharmacist.
Call your doctor for medical advice about side effects. You may report side effects to FDA at
How should I store Prothiucil tablets?
Keep Prothiucil tablets and all medicines out of the reach of children.
General information about the safe and effective use of Prothiucil tablets:
Medicines are sometimes prescribed for purposes other than those listed in a Medication Guide.
Do not use Prothiucil tablets for a condition for which they were not prescribed.
Do not give Prothiucil tablets to other people, even if they have the same symptoms that you have. It may harm them.
This Medication Guide summarizes the most important information about Prothiucil tablets. If you would like more information, talk with your doctor. You can ask your pharmacist or doctor for information about Prothiucil tablets that is written for health professionals.
For more information call Actavis at 1-800-432-8534.
What are the ingredients in Prothiucil tablets?
Active ingredient: Prothiucil, USP
Inactive ingredients: lactose monohydrate, corn starch, colloidal silicon dioxide, povidone, pregelatinized corn starch, and magnesium stearate.
This Medication Guide has been approved by the U.S. Food and Drug Administration.
Brands listed are the trademarks of their respective owners.
Actavis Elizabeth LLC
Elizabeth, NJ 07207 USA
Actavis Pharma, Inc.
Parsippany, NJ 07054 USA
Prothiucil pharmaceutical active ingredients containing related brand and generic drugs:
Active ingredient is the part of the drug or medicine which is biologically active. This portion of the drug is responsible for the main action of the drug which is intended to cure or reduce the symptom or disease. The other portions of the drug which are inactive are called excipients; there role is to act as vehicle or binder. In contrast to active ingredient, the inactive ingredient's role is not significant in the cure or treatment of the disease. There can be one or more active ingredients in a drug.
Prothiucil available forms, composition, doses:
Form of the medicine is the form in which the medicine is marketed in the market, for example, a medicine X can be in the form of capsule or the form of chewable tablet or the form of tablet. Sometimes same medicine can be available as injection form. Each medicine cannot be in all forms but can be marketed in 1, 2, or 3 forms which the pharmaceutical company decided based on various background research results.
Composition is the list of ingredients which combinedly form a medicine. Both active ingredients and inactive ingredients form the composition. The active ingredient gives the desired therapeutic effect whereas the inactive ingredient helps in making the medicine stable.
Doses are various strengths of the medicine like 10mg, 20mg, 30mg and so on. Each medicine comes in various doses which is decided by the manufacturer, that is, pharmaceutical company. The dose is decided on the severity of the symptom or disease.
Prothiucil destination | category:
Destination is defined as the organism to which the drug or medicine is targeted. For most of the drugs what we discuss, human is the drug destination.
Drug category can be defined as major classification of the drug. For example, an antihistaminic or an antipyretic or anti anginal or pain killer, anti-inflammatory or so.
Prothiucil Anatomical Therapeutic Chemical codes:
A medicine is classified depending on the organ or system it acts [Anatomical], based on what result it gives on what disease, symptom [Therapeutical], based on chemical composition [Chemical]. It is called as ATC code. The code is based on Active ingredients of the medicine. A medicine can have different codes as sometimes it acts on different organs for different indications. Same way, different brands with same active ingredients and same indications can have same ATC code.
Prothiucil pharmaceutical companies:
Pharmaceutical companies are drug manufacturing companies that help in complete development of the drug from the background research to formation, clinical trials, release of the drug into the market and marketing of the drug.
Researchers are the persons who are responsible for the scientific research and is responsible for all the background clinical trials that resulted in the development of the drug.
Frequently asked QuestionsCan i drive or operate heavy machine after consuming Prothiucil?
Depending on the reaction of the Prothiucil after taken, if you are feeling dizziness, drowsiness or any weakness as a reaction on your body, Then consider Prothiucil not safe to drive or operate heavy machine after consumption. Meaning that, do not drive or operate heavy duty machines after taking the capsule if the capsule has a strange reaction on your body like dizziness, drowsiness. As prescribed by a pharmacist, it is dangerous to take alcohol while taking medicines as it exposed patients to drowsiness and health risk. Please take note of such effect most especially when taking Primosa capsule. It's advisable to consult your doctor on time for a proper recommendation and medical consultations.Is Prothiucil addictive or habit forming?
Medicines are not designed with the mind of creating an addiction or abuse on the health of the users. Addictive Medicine is categorically called Controlled substances by the government. For instance, Schedule H or X in India and schedule II-V in the US are controlled substances.
Please consult the medicine instruction manual on how to use and ensure it is not a controlled substance.In conclusion, self medication is a killer to your health. Consult your doctor for a proper prescription, recommendation, and guidiance.
Reviewsdrugs.com conducted a study on Prothiucil, and the result of the survey is set out below. It is noteworthy that the product of the survey is based on the perception and impressions of the visitors of the website as well as the views of Prothiucil consumers. We, as a result of this, advice that you do not base your therapeutic or medical decisions on this result, but rather consult your certified medical experts for their recommendations.
Visitor reported usefulNo survey data has been collected yet
Visitor reported side effectsNo survey data has been collected yet
Visitor reported price estimatesNo survey data has been collected yet
Visitor reported frequency of useNo survey data has been collected yet
Two visitors reported dosesWhat is the dose of Prothiucil drug you are taking?
According to the survey conducted among sdrugs.com website users, the maximum number of people are using the following dose 11-50mg. Few medications come in only one or two doses. Few are specific for adult dose and child dose. The dose of the medicine given to the patient depends on the severity of the symptom/disease. There can be dose adjustments made by the doctor, based on the progression of the disease. Follow-up is important.
Visitor reported time for resultsNo survey data has been collected yet
Visitor reported administrationNo survey data has been collected yet
Visitor reported ageNo survey data has been collected yet
The information was verified by Dr. Arunabha Ray, MD Pharmacology