propylthiouracil

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Overview

What is propylthiouracil?

Propylthiouracil (6-propyl-2-thiouracil) is one of the thiocarbamide compounds. It is a white, crystalline substance that has a bitter taste and is very slightly soluble in water.

Each tablet contains propylthiouracil, 50 mg (293.7, µmol), lactose monohydrate, corn starch, colloidal silicon dioxide, povidone, pregelatinized starch, and magnesium stearate.

Propylthiouracil is an antithyroid drug administered orally. The molecular weight is 170.23. The molecular formula is CHNOS, and the structural formula is as follows:

What does propylthiouracil look like?

What are the available doses of propylthiouracil?

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What should I talk to my health care provider before I take propylthiouracil?

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How should I use propylthiouracil?

Propylthiouracil is indicated in the medical treatment of hyperthyroidism. Long-term therapy may lead to remission of the disease. Propylthiouracil may also be used to ameliorate hyperthyroidism in preparation for subtotal thyroidectomy or radioactive iodine therapy. Propylthiouracil is also used when thyroidectomy is contraindicated or not advisable.

Propylthiouracil is administered orally. The total daily dosage is usually given in 3 equal doses at approximately 8-hour intervals.

Adults:

:

What interacts with propylthiouracil?

Propylthiouracil is contraindicated in the presence of hypersensitivity to the drug or any of the other product components and in nursing mothers because the drug is excreted in milk.

What are the warnings of propylthiouracil?

Rarely, unexpected, severe toxicity (e.g., stomatitis, diarrhea, neutropenia and neurotoxicity) associated with 5-fluorouracil has been attributed to deficiency of dipyrimidine dehydrogenase activity.1 A few patients have been rechallenged with 5-fluorouracil and despite 5-fluorouracil dose lowering, toxicity recurred and progressed with worse morbidity. Absence of this catabolic enzyme appears to result in prolonged clearance of 5-fluorouracil.

Agranulocytosis is potentially the most serious side effect of propylthiouracil therapy. Patients should be instructed to report any symptoms of agranulocytosis, such as fever or sore throat. Leukopenia, thrombocytopenia, and aplastic anemia (pancytopenia) may also occur. The drug should be discontinued in the presence of agranulocytosis, aplastic anemia (pancytopenia), ANCA-positive vasculitis, hepatitis, interstitial pneumonitis, fever or exfoliative dermatitis. The patient’s bone marrow function should be monitored.

Propylthiouracil can cause fetal harm when administered to a pregnant woman. Because the drug readily crosses placental membranes and can induce goiter and even cretinism in the developing fetus, it is important that a sufficient, but not excessive, dose be given. In many pregnant women, the thyroid dysfunction diminishes as the pregnancy proceeds; consequently, a reduction of dosage may be possible. In some instances, propylthiouracil can be withdrawn 2 or 3 weeks before delivery.

If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be warned of the potential hazard to the fetus.

Postpartum patients receiving propylthiouracil should not nurse their babies.

Rare reports exist of severe hepatic reactions including encephalopathy, fulminant hepatic necrosis and death in patients receiving propylthiouracil. Symptoms suggestive of hepatic dysfunction (anorexia, pruritus, right upper quadrant pain, etc.) should prompt evaluation of liver function. Treatment with propylthiouracil should be discontinued promptly in the event of clinically significant evidence of liver abnormality, including hepatic transaminases in excess of 3 times the upper limit of normal.

What are the precautions of propylthiouracil?

General

Patients who receive propylthiouracil should be under close surveillance and should be impressed with the necessity of reporting immediately 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 made to determine whether agranulocytosis has developed. Particular care should be exercised with patients who are receiving additional drugs known to cause agranulocytosis.

Information for Patients

Patients should be advised that if they become pregnant during therapy or intend to become pregnant, they should contact their physician immediately about the desirability of discontinuing the drug. They also should not use propylthiouracil while nursing.

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, pruritus, right upper quadrant pain, etc).

Laboratory Tests

Because propylthiouracil may cause hypoprothrombinemia and bleeding, prothrombin time should be monitored 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 propylthiouracil should be employed.

Drug Interactions

Anticoagulants (Oral): The activity of anticoagulants may be potentiated by anti-vitamin-K activity attributed to propylthiouracil.

β-Adrenergic Blocking Agents: Hyperthyroidism may cause an increased clearance of beta blockers with a high extraction ratio. A dose reduction 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 dosage of digitalis glycosides may be required.

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 propylthiouracil for > 1 year have demonstrated thyroid hyperplasia and carcinoma formation.1 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

Pregnancy- Pregnancy Category D-See :

Nursing Mothers

The drug appears in human milk and is contraindicated in nursing mothers. (See and .)

Pediatric Use

Safety and effectiveness in pediatric patients below the age of 6 have not been established. For pediatric patients 6 years of age and older, see .

What are the side effects of propylthiouracil?

Major adverse reactions (much less common than the minor adverse reactions) include inhibition of myelopoiesis (agranulocytosis, granulopenia, and thrombocytopenia), aplastic anemia, drug fever, a lupus-like syndrome (including splenomegaly and vasculitis), hepatitis, periarteritis and hypoprothrombinemia and bleeding. Nephritis, glomerulonephritis, interstitial pneumonitis, exfoliative dermatitis, and erythema nodosum have been reported. Reports of a vasculitic syndrome associated with the presence of anti-neutrophilic cytoplasmic antibiodies (ANCA) have also been received. Manifestations of ANCA-positive vasculitis may include rapidly progressive glomerulonephritis (crescentic and pauci-immune necrotizing glomerulonephritis) sometimes leading to acute renal failure; fever; pulmonary infiltrates or alveolar hemorrhage; skin ulcers; and leucocytoclastic vasculitis.

Minor adverse reactions include skin rash, urticaria, nausea, vomiting, epigastric distress, arthralgia, paresthesia, loss of taste, taste perversion, abnormal loss of hair, myalgia, headache, pruritus, drowsiness, neuritis, edema, vertigo, skin pigmentation, jaundice, sialadenopathy, and lymphadenopathy.

It should be noted that about 10% of patients with untreated hyperthyroidism have leukopenia (white-blood cell count of less than 4,000/mm), often with relative granulopenia.

What should I look out for while using propylthiouracil?

Propylthiouracil is contraindicated in the presence of hypersensitivity to the drug or any of the other product components and in nursing mothers because the drug is excreted in milk.

Agranulocytosis is potentially the most serious side effect of propylthiouracil therapy. Patients should be instructed to report any symptoms of agranulocytosis, such as fever or sore throat. Leukopenia, thrombocytopenia, and aplastic anemia (pancytopenia) may also occur. The drug should be discontinued in the presence of agranulocytosis, aplastic anemia (pancytopenia), ANCA-positive vasculitis, hepatitis, interstitial pneumonitis, fever or exfoliative dermatitis. The patient’s bone marrow function should be monitored.

Propylthiouracil can cause fetal harm when administered to a pregnant woman. Because the drug readily crosses placental membranes and can induce goiter and even cretinism in the developing fetus, it is important that a sufficient, but not excessive, dose be given. In many pregnant women, the thyroid dysfunction diminishes as the pregnancy proceeds; consequently, a reduction of dosage may be possible. In some instances, propylthiouracil can be withdrawn 2 or 3 weeks before delivery.

If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be warned of the potential hazard to the fetus.

Postpartum patients receiving propylthiouracil should not nurse their babies.

Rare reports exist of severe hepatic reactions including encephalopathy, fulminant hepatic necrosis and death in patients receiving propylthiouracil. Symptoms suggestive of hepatic dysfunction (anorexia, pruritus, right upper quadrant pain, etc.) should prompt evaluation of liver function. Treatment with propylthiouracil should be discontinued promptly in the event of clinically significant evidence of liver abnormality, including hepatic transaminases in excess of 3 times the upper limit of normal.

What might happen if I take too much propylthiouracil?

Signs And Symptoms:

No information is available on the following: LD; 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.

Physicians’ Desk Reference

Protect the patient’s airway and support ventilation and perfusion. Meticulously monitor and maintain, within acceptable limits, the patient’s vital signs, blood gases, serum electrolytes, etc. The patient’s bone marrow function should be monitored. Absorption of drugs from the gastrointestinal tract may be decreased by giving activated charcoal, which, in many cases, is more effective than emesis or lavage; consider charcoal instead of or in addition to gastric emptying. Repeated doses of charcoal over time may hasten elimination of some drugs that have been absorbed. Safeguard the patient’s airway when employing gastric emptying or charcoal.

Forced diuresis, peritoneal dialysis, hemodialysis, or charcoal hemoperfusion have not been established as beneficial for an overdose of propylthiouracil.

How should I store and handle propylthiouracil?

Store at 20°-25°C (68°-77°F) (see USP Controlled Room Temperature). PROTECT FROM LIGHT. KEEP TIGHTLY CLOSED. Sarafem is a registered trademark of Eli Lilly and Company. 50 mg — Each white, round, tablet imprinted with on one side and 348 and partial bisect on the other side contains 50 mg of Propylthiouracil, USP. Tablets are supplied in blisterpacks of 30 (NDC 0615-7583-39).

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Clinical Information

Chemical Structure

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Clinical Pharmacology

Propylthiouracil 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.

Propylthiouracil is readily absorbed from the gastrointestinal tract. It is metabolized rapidly and requires frequent administration. Approximately 35% of the drug is excreted in the urine, in intact and in conjugated forms, within 24 hours.

In laboratory animals, various interventions, including propylthiouracil administration, that continuously suppress thyroid function and thereby increase TSH secretion result in thyroid tissue hypertrophy.

Non-Clinical Toxicology

Propylthiouracil is contraindicated in the presence of hypersensitivity to the drug or any of the other product components and in nursing mothers because the drug is excreted in milk.

Agranulocytosis is potentially the most serious side effect of propylthiouracil therapy. Patients should be instructed to report any symptoms of agranulocytosis, such as fever or sore throat. Leukopenia, thrombocytopenia, and aplastic anemia (pancytopenia) may also occur. The drug should be discontinued in the presence of agranulocytosis, aplastic anemia (pancytopenia), ANCA-positive vasculitis, hepatitis, interstitial pneumonitis, fever or exfoliative dermatitis. The patient’s bone marrow function should be monitored.

Propylthiouracil can cause fetal harm when administered to a pregnant woman. Because the drug readily crosses placental membranes and can induce goiter and even cretinism in the developing fetus, it is important that a sufficient, but not excessive, dose be given. In many pregnant women, the thyroid dysfunction diminishes as the pregnancy proceeds; consequently, a reduction of dosage may be possible. In some instances, propylthiouracil can be withdrawn 2 or 3 weeks before delivery.

If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be warned of the potential hazard to the fetus.

Postpartum patients receiving propylthiouracil should not nurse their babies.

Rare reports exist of severe hepatic reactions including encephalopathy, fulminant hepatic necrosis and death in patients receiving propylthiouracil. Symptoms suggestive of hepatic dysfunction (anorexia, pruritus, right upper quadrant pain, etc.) should prompt evaluation of liver function. Treatment with propylthiouracil should be discontinued promptly in the event of clinically significant evidence of liver abnormality, including hepatic transaminases in excess of 3 times the upper limit of normal.

Anticoagulants (Oral): The activity of anticoagulants may be potentiated by anti-vitamin-K activity attributed to propylthiouracil.

β-Adrenergic Blocking Agents: Hyperthyroidism may cause an increased clearance of beta blockers with a high extraction ratio. A dose reduction 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 dosage of digitalis glycosides may be required.

Theophylline: Theophylline clearance may decrease when hyperthyroid patients on a stable theophylline regimen become euthyroid; a reduced dose of theophylline may be needed.

Patients who receive propylthiouracil should be under close surveillance and should be impressed with the necessity of reporting immediately 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 made to determine whether agranulocytosis has developed. Particular care should be exercised with patients who are receiving additional drugs known to cause agranulocytosis.

Major adverse reactions (much less common than the minor adverse reactions) include inhibition of myelopoiesis (agranulocytosis, granulopenia, and thrombocytopenia), aplastic anemia, drug fever, a lupus-like syndrome (including splenomegaly and vasculitis), hepatitis, periarteritis and hypoprothrombinemia and bleeding. Nephritis, glomerulonephritis, interstitial pneumonitis, exfoliative dermatitis, and erythema nodosum have been reported. Reports of a vasculitic syndrome associated with the presence of anti-neutrophilic cytoplasmic antibiodies (ANCA) have also been received. Manifestations of ANCA-positive vasculitis may include rapidly progressive glomerulonephritis (crescentic and pauci-immune necrotizing glomerulonephritis) sometimes leading to acute renal failure; fever; pulmonary infiltrates or alveolar hemorrhage; skin ulcers; and leucocytoclastic vasculitis.

Minor adverse reactions include skin rash, urticaria, nausea, vomiting, epigastric distress, arthralgia, paresthesia, loss of taste, taste perversion, abnormal loss of hair, myalgia, headache, pruritus, drowsiness, neuritis, edema, vertigo, skin pigmentation, jaundice, sialadenopathy, and lymphadenopathy.

It should be noted that about 10% of patients with untreated hyperthyroidism have leukopenia (white-blood cell count of less than 4,000/mm), often with relative granulopenia.

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Reference

This information is obtained from the National Institute of Health's Standard Packaging Label drug database.
"https://dailymed.nlm.nih.gov/dailymed/"

While we update our database periodically, we cannot guarantee it is always updated to the latest version.

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Professional

Clonazepam Description Each single-scored tablet, for oral administration, contains 0.5 mg, 1 mg, or 2 mg Clonazepam, USP, a benzodiazepine. Each tablet also contains corn starch, lactose monohydrate, magnesium stearate, microcrystalline cellulose, and povidone. Clonazepam tablets USP 0.5 mg contain Yellow D&C No. 10 Aluminum Lake. Clonazepam tablets USP 1 mg contain Yellow D&C No. 10 Aluminum Lake, as well as FD&C Blue No. 1 Aluminum Lake. Chemically, Clonazepam, USP is 5-(o-chlorophenyl)-1,3-dihydro-7-nitro-2H-1,4-benzodiazepin-2-one. It is a light yellow crystalline powder. It has the following structural formula: C15H10ClN3O3 M.W. 315.72

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Interactions

A total of 440 drugs (1549 brand and generic names) are known to interact with Imbruvica (ibrutinib). 228 major drug interactions (854 brand and generic names) 210 moderate drug interactions (691 brand and generic names) 2 minor drug interactions (4 brand and generic names) Show all medications in the database that may interact with Imbruvica (ibrutinib).

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