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|Propylthiouracil |
Drugs search, click the first letter of a drug name: | A | B | C | D | E | F | G | H | I | J | K | L | M | N | O | P | Q | R | S | T | U | V | W | X | Y | Z | 1 | 2 | 3 | 4 | 5 | 6 | 8 | 9 Home Propylthiouracil( PTU ) Pronouncation: (pro-puhl-thigh-oh-YOU-rah-sill)Class: Antithyroid agent Trade Names: Mechanism of ActionPharmacologyInhibits synthesis of thyroid hormones. PharmacokineticsAbsorptionReadily absorbed from the GI tract. Bioavailability is 80% to 95%. T max is 1.99 hr; C max is 7.12 mcg/mL. DistributionProtein binding is 75% to 80%, primarily to albumin. Vd is approximately 0.4 L/kg. MetabolismActively concentrated by the thyroid. Metabolized rapidly in the liver; undergoes glucuronidation. EliminationUrine (35%); less than 1% as unchanged. T 1/2 is 1 to 2 hr. Total body clearance is approximately 7 L/hr. PeakApproximately 17 wk to normalize serum T 3 and T 4 concentrations. Indications and UsageLong-term therapy of hyperthyroidism; amelioration of hyperthyroidism in preparation for subtotal thyroidectomy or radioactive iodine therapy; when thyroidectomy is contraindicated or not advisable. Unlabeled UsesManagement of alcoholic liver disease. ContraindicationsHypersensitivity to antithyroid drugs; lactating women. Dosage and AdministrationAdultsPO The initial dose is 300 mg/day in 3 equal doses q 8 hr. In patients with severe hyperthyroidism or very large goiters, initial dose is usually 400 mg/day, occasionally up to 600 to 900 mg/day. The maintenance dose is 100 to 150 mg/day in divided doses q 8 hr. Children over 10 yrPO The initial dose is 150 to 300 mg/day in divided doses q 8 hr. The maintenance dose is determined by response. Children 6 to 10 yrPO The initial dose is 50 to 150 mg/day in divided doses q 8 hr. Alternate Dosing for ChildrenPO The initial dose is 5 to 7 mg/kg/day in divided doses q 8 hr. The maintenance dose is 1/ 3 to 2/ 3 initial dose, beginning when patient is euthyroid. General AdviceGive with meals to minimize GI irritation. Storage/StabilityStore in tight, light-resistant container at room temperature. Drug InteractionsAnticoagulantsAltered anticoagulant action. Beta blockersIncreased effects of beta blockers. Digitalis glycosidesIncreased digitalis levels, resulting in toxicity. TheophyllineAltered theophylline clearance in hyperthyroid or hypothyroid patients. Laboratory Test InteractionsNone well documented. Adverse ReactionsCNSParesthesias; neuritis; headache; vertigo; drowsiness; neuropathies; CNS stimulation; depression. DermatologicRash; urticaria; pruritus; erythema nodosum; skin pigmentation; exfoliative dermatitis; lupus-like syndrome (splenomegaly, hepatitis, periarteritis; hypoprothrombinemia; bleeding). EENTLoss of taste; sialadenopathy. GINausea; vomiting; epigastric distress. GenitourinaryNephritis. HepaticJaundice; hepatitis. HematologicInhibition of myelopoiesis (eg, agranulocytosis, leukopenia, granulocytopenia, thrombocytopenia); aplastic anemia; hypoprothrombinemia; periarteritis. MiscellaneousAbnormal hair loss; arthralgia; myalgia; edema; lymphadenopathy; drug fever; interstitial pneumonitis; insulin autoimmune syndrome (hypoglycemia). PrecautionsPregnancyCategory D . LactationAvoid nursing. However, if antithyroid drug is essential, PTU is preferred antithyroid agent while nursing. ChildrenHepatotoxicity has occurred in pediatric patients. Discontinue drug immediately if signs and symptoms of hepatic dysfunction develop. AgranulocytosisPotentially most serious side effect. Discontinue drug if agranulocytosis, aplastic anemia, hepatitis, fever, or exfoliative dermatitis occur. Hemorrhagic effectsMay cause hypoprothrombinemia and bleeding. OverdosageSymptomsNausea, vomiting, epigastric distress, headache, fever, arthralgia, pruritus, edema, pancytopenia; most serious effect: agranulocytosis. Patient Information
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