ﺑﺎﺯﮔﺸﺖ ﺑﻪ ﺻﻔﺤﻪ ﻗﺒﻠﯽ
خرید پکیج
تعداد آیتم قابل مشاهده باقیمانده : 3 مورد
نسخه الکترونیک
medimedia.ir

Methimazole: Drug information

Methimazole: Drug information
(For additional information see "Methimazole: Patient drug information" and see "Methimazole: Pediatric drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
Brand Names: US
  • Tapazole [DSC]
Brand Names: Canada
  • JAMP-Methimazole;
  • Mar-Methimazole;
  • Tapazole
Pharmacologic Category
  • Antithyroid Agent;
  • Thioamide
Dosing: Adult
Hyperthyroidism associated with Graves disease, toxic multinodular goiter, toxic adenoma, or iodine-induced thyrotoxicosis

Hyperthyroidism associated with Graves disease, toxic multinodular goiter, toxic adenoma (labeled uses), or iodine-induced thyrotoxicosis (off-label use) :

Note: May use in combination with beta-blockade to manage hyperthyroid symptoms prior to definitive therapy (ie, radioactive iodine therapy or surgery) or as chronic low-dose treatment; for iodine-induced thyrotoxicosis, may be used as an adjunct to beta-blockade for severe or prolonged (eg, >1 month) symptoms or in patients with underlying heart disease (Ref).

Oral: Initial: Individualize initial dose based on clinical status and gland size; free T4 levels may be used to guide initial therapy (Ref):

Free T4 levels 1 to 1.5 times ULN: 5 to 10 mg once daily.

Free T4 levels >1.5 to 2 times ULN (or iodine-induced thyrotoxicosis): 10 to 20 mg once daily.

Free T4 levels >2 times ULN: 20 to 40 mg/day. To achieve euthyroidism more quickly and reduce GI-related adverse effects, may give in 2 to 3 divided doses (especially with doses >30 mg/day) (Ref).

Dose adjustment: Oral: Usual maintenance dose: 5 to 10 mg once daily. Assess free T4 and total T3 at 4- to 6-week intervals; when normal, reduce dose by 30% to 50% and repeat thyroid function tests in 4 to 6 weeks; continue to adjust dose to achieve euthyroidism (Ref).

Duration of therapy: Depends on etiology and plans for definitive therapy:

Patients undergoing definitive therapy: Prior to definitive therapy, continue until euthyroid (typically 4 to 6 weeks); discontinue 2 to 3 days before radioactive iodine therapy or on the day of thyroidectomy (Ref).

Patients not undergoing definitive therapy: For Graves disease, continue for 12 to 18 months, then assess for remission; for toxic multinodular goiter/toxic adenoma, continue indefinitely (Ref).

Iodine-induced thyrotoxicosis: Taper and discontinue therapy as iodine load is cleared (Ref).

Thyroid storm

Thyroid storm (alternative to propylthiouracil) (off-label use): Note: Use in combination with other appropriate agents; if iodine is administered, delay iodine administration by ≥1 hour after methimazole (Ref).

Oral: Initial: 20 mg every 4 to 6 hours (Ref); once clinically stable, dose may be given less frequently (eg, 20 mg once or twice daily) (Ref). In patients who cannot take methimazole by mouth, alternative administration routes (eg, nasogastric, rectal) may be considered (Ref).

Thyrotoxicosis, type I amiodarone-induced

Thyrotoxicosis, type I amiodarone-induced (off-label use):

Oral: Initial: 30 to 40 mg once daily; adjust dose to achieve euthyroidism (eg, free T4, total T3, TSH levels in the normal range); if high doses (eg, >30 mg/day) are required after 3 to 6 months, it may be more effective to administer in 2 to 3 divided doses (Ref). Note: If etiology of amiodarone-induced thyrotoxicosis (eg, type I or type II) cannot be determined or if patient is clinically unstable, use in combination with a glucocorticoid (Ref).

Duration of therapy: Depends on whether amiodarone therapy will be continued:

Continuing amiodarone: Continue methimazole indefinitely (Ref).

Discontinuing amiodarone: Taper methimazole slowly (eg, over months) to avoid recurrence of thyrotoxicosis (Ref).

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Adult

The renal dosing recommendations are based upon the best available evidence and clinical expertise. Senior Editorial Team: Bruce Mueller, PharmD, FCCP, FASN, FNKF; Jason A. Roberts, PhD, BPharm (Hons), B App Sc, FSHP, FISAC; Michael Heung, MD, MS.

Altered kidney function: No dosage adjustment necessary for any degree of kidney impairment (Ref).

Hemodialysis, intermittent (thrice weekly): Dialyzable (~30% to 40%) (Ref): No supplemental dose or dosage adjustment necessary; when scheduled dose falls on a hemodialysis day, administer after hemodialysis (Ref).

Peritoneal dialysis: Likely to be somewhat dialyzable: No dosage adjustment necessary (Ref).

CRRT: No dosage adjustment necessary (Ref).

PIRRT (eg, sustained, low-efficiency diafiltration): No dosage adjustment necessary; when scheduled dose falls on a PIRRT day, administer after PIRRT (Ref).

Dosing: Hepatic Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling.

Dosing: Older Adult

Refer to adult dosing.

Dosing: Pediatric

(For additional information see "Methimazole: Pediatric drug information")

Hyperthyroidism

Hyperthyroidism: Infants, Children, and Adolescents: Oral: Initial: 0.4 mg/kg/day in 3 divided doses (approximately every 8 hours); maintenance 0.2 mg/kg/day in 3 divided doses (50% of initial)

Graves disease

Graves disease (Ref): Note: In severe cases, higher doses may be required (50% to 100% higher); once patient euthyroid, reduce dose by ≥50% to maintain euthyroid; duration of therapy usually 1 to 2 years

Weight-based dosing: Infants, Children, and Adolescents: Oral: Initial: 0.2 to 0.5 mg/kg/dose once daily (range: 0.1 to 1 mg/kg/dose)

Fixed dosing (using 1/4, 1/2, or whole tablets): Oral:

Infants: 1.25 mg/day

Children 1 to 5 years: 2.5 to 5 mg/day

Children 5 to 10 years: 5 to 10 mg/day

Children ≥10 years and Adolescents: 10 to 20 mg/day

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Pediatric

There are no dosage adjustments provided in the manufacturer's labeling.

Dosing: Hepatic Impairment: Pediatric

There are no dosage adjustments provided in the manufacturer's labeling.

Adverse Reactions (Significant): Considerations
Agranulocytosis

Methimazole may cause agranulocytosis, a rare but potentially life-threatening adverse reaction that is reversible upon discontinuation. Patients should report immediately any sign/symptoms of infection (eg, fever, flu-like symptoms, pharyngitis) so a WBC can be assessed (Ref).

Mechanism: May be through direct toxicity, but more recent evidence supports an immune-mediated mechanism (Ref).

Onset: Varied; most cases occur within the first 3 months of treatment (mean 42 days) but can occur later (Ref).

Risk factors:

• Doses >30 mg/day (possible risk factor) (Ref)

• Age >40 years (possible risk factor) (Ref)

• Genetic variants: HLA-B*27:05 (Europeans) (Ref); HLA‐B*38:02 (Han Chinese) (Ref); HLA‐DRB1*08:03 (Han Chinese) (Ref); Nox3 variants (encodes NADPH oxidase) (Ref).

Hepatotoxicity

Methimazole may rarely cause life-threatening hepatotoxicity, including acute hepatic failure and hepatitis (usually cholestatic) (Ref). Hepatotoxicity is reversible with discontinuation. Patients with hepatotoxicity due to methimazole may be at increased risk for hepatotoxicity with propylthiouracil (Ref).

Mechanism: Dose-related; not clearly established. Possible mechanisms include reactive metabolite formation and immune-mediated reaction (Ref).

Onset: Varied; typically within 2 days to 3 months of initiation (Ref).

Risk factors:

• Higher doses (Ref)

• Older age (Ref)

• Polymorphism in SLCO1B1*1a and SLCO1B1*1b (Ref)

• Carriers of the HLA-C*03:02 allele (Ref)

Lupus-like syndrome

Methimazole may cause a lupus-like syndrome, a rare but potentially life-threatening adverse reaction that is reversible with discontinuation and additional treatment (Ref). Manifestations may range from cutaneous involvement to lupus nephritis (Ref).

Mechanism: Not clearly established; hypothesized to be an autoimmune response in genetically predisposed individuals (Ref).

Onset: Varied; typically manifesting weeks to months after initiation (Ref).

Risk factors:

• IgA deficiency (Ref)

Pancreatitis

Acute pancreatitis is a rare, but potentially life-threatening adverse effect of methimazole (Ref). Pancreatitis is typically reversible upon discontinuation but has resulted in death (Ref).

Mechanism: Non–dose-related. While the exact mechanism is unknown, it follows a pattern of a hypersensitivity-type reaction with rechallenge reactions occurring at a shorter latency (Ref).

Onset: Varied; typically occurs within the first 90 days of therapy (Ref).

Risk factors:

• Older age (Ref)

Vasculitis

Although this adverse reaction is more common with propylthiouracil, cases of vasculitis with methimazole have been discussed in the literature (Ref), most notably involving the kidneys, lungs, and skin. Many of these cases involve a positive antineutrophil cytoplasmic antibody (ANCA). ANCA-positive cases involve an inflammatory and necrotic process impacting small vessels. Pulmonary capillaritis and diffuse pulmonary alveolar hemorrhage has been described (Ref). This adverse reaction is potentially life-threatening without intervention but is reversible with discontinuation and supportive care. A review of ANCA-positive vasculitis cases possibly associated with methimazole reported a prevalence range of 0% to 16% with a median prevalence of 6% (Ref).

Onset: Delayed; the median time to vasculitis presentation was 42 months (Ref).

Risk factors:

• Younger age (Ref)

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

Frequency not defined:

Cardiovascular: Edema, periarteritis

Dermatologic: Alopecia, pruritus, skin pigmentation, skin rash

Endocrine & metabolic: Hypothyroidism

Gastrointestinal: Enlargement of salivary glands, epigastric distress, nausea, vomiting

Hematologic & oncologic: Granulocytopenia, lymphadenopathy

Nervous system: Drowsiness, drug fever, headache, paresthesia, vertigo

Neuromuscular & skeletal: Arthralgia, myalgia

Postmarketing:

Cardiovascular: Cerebral vasculitis (Tripodi 2008), hypersensitivity angiitis (Ribeiro 2013), vasculitis (Balavoine 2015)

Dermatologic: Urticaria (Kubota 2016)

Endocrine & metabolic: Insulin autoimmune syndrome (Chen 2018, Gomez 2012)

Gastrointestinal: Acute pancreatitis (Brix 2020), ageusia (Hallman 1953), gastrointestinal hemorrhage (Minkley 2011)

Hematologic & oncologic: Agranulocytosis (Cooper 2005), aplastic anemia (Josol 2010), hypoprothrombinemia (Minkley 2011)

Hepatic: Acute hepatic failure (Wang 2014), hepatitis (Wang 2014), hepatotoxicity (Wang 2014), jaundice (Wang 2014)

Nervous system: Neuritis (Roldan 1972), neuropathy

Neuromuscular & skeletal: Lupus-like syndrome (Beernaert 2020)

Renal: Acute kidney injury (Shell 2020), glomerulonephritis (Hori 1996), nephritis (Reynolds 1979)

Respiratory: Pulmonary alveolar hemorrhage (Arai 2018)

Contraindications

Hypersensitivity to methimazole or any component of the formulation.

Canadian labeling: Additional contraindications (not in US labeling): Breastfeeding, history of acute pancreatitis after administration of methimazole.

Warnings/Precautions

Concerns related to adverse effects:

• Dermatologic effects: Antithyroid agents have been associated with dermatologic reactions. Discontinue in the presence of a severe reaction.

• Fever: Discontinue in the presence of unexplained fever.

• Hypothyroidism: May cause hypothyroidism; routinely monitor TSH and free T4 levels, adjust dose to maintain euthyroid state.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Tablet, Oral:

Tapazole: 5 mg [DSC], 10 mg [DSC]

Generic: 5 mg, 10 mg

Generic Equivalent Available: US

Yes

Pricing: US

Tablets (methIMAzole Oral)

5 mg (per each): $0.44

10 mg (per each): $0.77

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Dosage Forms: Canada

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Tablet, Oral:

Tapazole: 5 mg [contains corn starch]

Tapazole: 10 mg, 20 mg [DSC]

Generic: 5 mg, 10 mg

Administration: Adult

Rectal: In thyroid storm, rectal administration has been described (Ref).

Administration: Pediatric

Oral: May administer without regard to food.

Hazardous Drugs Handling Considerations

Hazardous agent (NIOSH 2016 [group 3]).

Use appropriate precautions for receiving, handling, storage, preparation, dispensing, transporting, administration, and disposal. Follow NIOSH and USP 800 recommendations and institution-specific policies/procedures for appropriate containment strategy (NIOSH 2016; USP-NF 2020).

Note: Facilities may perform risk assessment of some hazardous drugs to determine if appropriate for alternative handling and containment strategies (USP-NF 2020). Refer to institution-specific handling policies/procedures.

Use: Labeled Indications

Hyperthyroidism: Treatment of hyperthyroidism in patients with Graves disease or toxic multinodular goiter for whom surgery or radioactive iodine therapy is not appropriate; amelioration of hyperthyroid symptoms in preparation for thyroidectomy or radioactive iodine therapy.

Use: Off-Label: Adult

Iodine-induced thyrotoxicosis; Thyroid storm; Thyrotoxicosis, type I amiodarone-induced

Medication Safety Issues
Sound-alike/look-alike issues:

MethIMAzole may be confused with methazolAMIDE, metOLazone

Metabolism/Transport Effects

None known.

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.

5-Aminosalicylic Acid Derivatives: May enhance the myelosuppressive effect of Myelosuppressive Agents. Risk C: Monitor therapy

BCG (Intravesical): Myelosuppressive Agents may diminish the therapeutic effect of BCG (Intravesical). Risk X: Avoid combination

Cardiac Glycosides: Antithyroid Agents may increase the serum concentration of Cardiac Glycosides. Risk C: Monitor therapy

Chloramphenicol (Ophthalmic): May enhance the adverse/toxic effect of Myelosuppressive Agents. Risk C: Monitor therapy

Chloramphenicol (Systemic): Myelosuppressive Agents may enhance the myelosuppressive effect of Chloramphenicol (Systemic). Risk X: Avoid combination

Cladribine: May enhance the myelosuppressive effect of Myelosuppressive Agents. Risk X: Avoid combination

CloZAPine: Myelosuppressive Agents may enhance the adverse/toxic effect of CloZAPine. Specifically, the risk for neutropenia may be increased. Risk C: Monitor therapy

Deferiprone: Myelosuppressive Agents may enhance the neutropenic effect of Deferiprone. Management: Avoid the concomitant use of deferiprone and myelosuppressive agents whenever possible. If this combination cannot be avoided, monitor the absolute neutrophil count more closely. Risk D: Consider therapy modification

Dipyrone: May enhance the adverse/toxic effect of Myelosuppressive Agents. Specifically, the risk for agranulocytosis and pancytopenia may be increased Risk X: Avoid combination

Fexinidazole: Myelosuppressive Agents may enhance the myelosuppressive effect of Fexinidazole. Risk X: Avoid combination

MetyraPONE: Antithyroid Agents may diminish the diagnostic effect of MetyraPONE. Management: Consider alternatives to the use of the metyrapone test in patients taking antithyroid agents. Risk D: Consider therapy modification

Olaparib: Myelosuppressive Agents may enhance the myelosuppressive effect of Olaparib. Risk C: Monitor therapy

PrednisoLONE (Systemic): MethIMAzole may decrease the serum concentration of PrednisoLONE (Systemic). Risk C: Monitor therapy

Promazine: May enhance the myelosuppressive effect of Myelosuppressive Agents. Risk C: Monitor therapy

Ropeginterferon Alfa-2b: Myelosuppressive Agents may enhance the myelosuppressive effect of Ropeginterferon Alfa-2b. Management: Avoid coadministration of ropeginterferon alfa-2b and other myelosuppressive agents. If this combination cannot be avoided, monitor patients for excessive myelosuppressive effects. Risk D: Consider therapy modification

Sodium Iodide I131: Antithyroid Agents may diminish the therapeutic effect of Sodium Iodide I131. Management: Discontinue antithyroid medications at least 3 days before sodium iodide I-131 administration, and avoid concurrent use. Risk X: Avoid combination

Theophylline Derivatives: Antithyroid Agents may increase the serum concentration of Theophylline Derivatives. Risk C: Monitor therapy

Vitamin K Antagonists (eg, warfarin): Antithyroid Agents may diminish the anticoagulant effect of Vitamin K Antagonists. Risk C: Monitor therapy

Reproductive Considerations

Patients taking methimazole should use effective contraception and postpone becoming pregnant until a stable euthyroid state is achieved. Patients taking methimazole should notify their health care provider immediately once pregnancy is suspected. The decision to continue antithyroid medications during pregnancy should be individualized (ATA [Alexander 2017]).

Pregnancy Considerations

Methimazole crosses the placenta.

Congenital anomalies have been observed in neonates exposed in utero to methimazole in the first trimester and include anomalies of the upper GI tract (esophageal atresia with or without tracheoesophageal fistula), respiratory tract (choanal atresia), skin (aplasia cutis), and facial dysmorphism. Additional abdominal wall defects (umbilicocele), ventricular septal defects, and defects of the eye and urinary system have also been reported (ATA [Alexander 2017]). Hypothyroidism may occur in the newborn.

Uncontrolled maternal hyperthyroidism may result in adverse neonatal and maternal outcomes. Adverse outcomes associated with poorly controlled thyrotoxicosis include pregnancy loss, pregnancy induced hypertension, maternal congestive heart failure, and thyroid storm, as well as prematurity, low birth weight, intrauterine growth restriction, and stillbirth (ATA [Alexander 2017]).

To avoid potential teratogenic effects, antithyroid drugs may be discontinued as soon as pregnancy is detected in select patients with well-controlled Graves disease at low risk for relapse; close monitoring of maternal and fetal thyroid function recommended (ATA [Alexander 2017]). When treatment is necessary, antithyroid drugs are the treatment of choice for the control of hyperthyroidism during pregnancy, although recommendations for specific agents vary by guideline. Methimazole is generally avoided during the first trimester but may be used later in pregnancy (ACOG 2020; ATA [Alexander 2017]). Dose requirements of methimazole may be decreased as pregnancy progresses. To prevent adverse pregnancy outcomes, the lowest effective dose should be used to keep the maternal TT4/FT4 at or just above the pregnancy specific upper limit of normal (ACOG 2020; ATA [Alexander 2017]).

Breastfeeding Considerations

Methimazole is present in breast milk.

Information related to the presence of methimazole in breast milk is available from 6 lactating women with Graves disease following a single dose of methimazole 15 mg. Peak methimazole concentrations were 0.32 ± 0.10 mcg/mL (breast milk) and 0.31 ± 0.09 mcg/mL (maternal plasma) 2 hours after administration. The half-life of methimazole was calculated to be 4.2 ± 0.8 hours in breast milk. Twelve hours after the dose, breast milk concentrations of methimazole had decreased to 0.03 ± 0.01 mcg/mL (Abe 1995).

Based on available data, thyroid function is normal in infants exposed to lower doses of methimazole via breast milk. In addition, IQ and physical development up to 74 months of age were not impaired in a long-term study of breastfed infants whose mothers were receiving treatment with methimazole. The treatment of hyperthyroidism in breastfeeding patients is the same as non-breastfeeding females. The lowest effective dose should be used; maternal doses of methimazole ≤20 mg/day are advised in breastfeeding patients. Infants exposed to antithyroid medications via breast milk should be monitored for adequate growth and development; routine tests of thyroid function are not recommended (ATA [Alexander 2017]). Taking the dose of methimazole after breastfeeding may help decrease potential infant exposure by providing a 3- to 4-hour interval before the next feed (Amino 2020).

Monitoring Parameters

Signs and symptoms of illness (ie, fever, sore throat, skin eruptions, general malaise).

CBC with differential (baseline and if development of febrile illness or pharyngitis occurs); signs/symptoms of bone marrow suppression; prothrombin time (especially before surgical procedures); LFTs (bilirubin, alkaline phosphatase, ALT, AST) at baseline and if symptoms of liver injury occur (eg, anorexia, pruritus, right upper quadrant pain) (ATA [Ross 2016]).

Thyroid function tests:

Serum free T4 and total T3 at 4- to 6-week intervals during dose titration, then every 2 to 3 months once euthyroid levels are achieved (with long-term therapy [ie, >18 months] may extend interval to every 4 to 6 months); in patients with Graves disease, if thyrotropin receptor antibodies (TRAbs) are negative, thyroid function tests should be monitored every 2 to 3 months for the first 6 months after discontinuing therapy, then at 4- to 6-month intervals for the next 6 months, then every 6 to 12 months thereafter (ATA [Ross 2016]).

Thyroid-stimulating hormone (TSH) periodically throughout treatment; TSH is not an adequate parameter to assess initial response as levels may remain suppressed for several months after starting therapy (ATA [Ross 2016]).

TRAb in patients with Graves disease prior to stopping medication; elevation at the end of therapy decreases likelihood of remission (ATA [Ross 2016]).

Pregnant patients: Free T4 and total T3 every 2 to 4 weeks until stabilized (ACOG 2020). Free T4, total T4, and TSH approximately every 4 weeks throughout pregnancy. TRAb once pregnancy is confirmed, at 18 to 22 weeks' gestation, and 30 to 34 weeks' gestation (ATA [Alexander 2017]).

Mechanism of Action

Inhibits the synthesis of thyroid hormones by blocking the oxidation of iodine in the thyroid gland; blocks synthesis of thyroxine and triiodothyronine (T3); does not inactivate circulating T4 and T3

Pharmacokinetics (Adult Data Unless Noted)

Onset of action: Antithyroid: 12 to 18 hours (Clark 2006).

Duration: 36 to 72 hours (Clark 2006).

Absorption: Almost complete (Clark 2006).

Distribution: Concentrated in thyroid gland, Vd/F: 0.66 L/kg (Jansson 1985).

Protein binding, plasma: None (Cooper 2005).

Metabolism: Hepatic.

Bioavailability: ~93% (Clark 2006).

Half-life elimination: 4 to 6 hours (Clark 2006).

Time to peak, serum: 1 to 2 hours (Clark 2006).

Excretion: Urine (<10% unchanged) (Jansson 1985).

Brand Names: International
International Brand Names by Country
For country code abbreviations (show table)

  • (AE) United Arab Emirates: Favistan;
  • (AR) Argentina: Danantizol;
  • (AT) Austria: Favistan;
  • (BE) Belgium: Strumazol;
  • (BG) Bulgaria: Thyrozol;
  • (BR) Brazil: Tapazol;
  • (CH) Switzerland: Tapazole;
  • (CL) Chile: Tirozol;
  • (CN) China: Methimazole | Tapazole | Thyrozol;
  • (CO) Colombia: Metimazol | Metlina | Tapazol;
  • (CZ) Czech Republic: Favistan | Thyrozol;
  • (DE) Germany: Favistan | Thiamazol | Thiamazol "hennig" | Thiamazol Aristo | Thiamazol hexal | Thyrozol;
  • (DK) Denmark: Tiamazol 1A Farma;
  • (DO) Dominican Republic: Tapazole | Tapel;
  • (EC) Ecuador: Tapazol;
  • (EE) Estonia: Mercazolyl | Thyrozol;
  • (ES) Spain: Tirodril;
  • (FI) Finland: Metimazol;
  • (FR) France: Thyrozol;
  • (GR) Greece: Unimazole;
  • (HK) Hong Kong: Methimazole | Tapazole;
  • (HR) Croatia: Athyrazol;
  • (ID) Indonesia: Thyrozol | Velthrom;
  • (IL) Israel: Mercaptizol;
  • (IN) India: Methimercazole | Methimez;
  • (JP) Japan: Mercazole;
  • (KR) Korea, Republic of: Methimazole | Methimazole bukwang;
  • (LB) Lebanon: Tapazol | Thyrozol;
  • (LT) Lithuania: Mercazolil | Metizol | Tapazole | Thiamazol | Thyrozol;
  • (LU) Luxembourg: Strumazol | Thyrozol;
  • (LV) Latvia: Mercazolil | Thyrozol;
  • (MA) Morocco: Thyrozol;
  • (MX) Mexico: Ganglioside | Tapazol | Tiahexal | Tiamazol | Tiamazol Armstrong | Tiarotec | Tizorol;
  • (MY) Malaysia: Methimazole;
  • (NL) Netherlands: Strumazol;
  • (PE) Peru: Tapazol | Thyrozol | Tiamazol;
  • (PH) Philippines: Methimazole | Strumazol | Tapazole | Tapdin;
  • (PL) Poland: Favistan | Metizol | Thiamazole Merck | Thyrozol;
  • (PR) Puerto Rico: Methimazole | Northyx | Tapazole;
  • (PT) Portugal: Metibasol;
  • (PY) Paraguay: Danantizol;
  • (RU) Russian Federation: Mercazolil | Metizol | Thiamazole philopharm | Thyrozol | Tyrozol;
  • (SA) Saudi Arabia: Favistan;
  • (SE) Sweden: Thacapzol | Thiamazole uni pharma | Tiamazol 2care4 | Tiamazol abacus medicine | Tiamazol ebb | Tiamazol paranova;
  • (SG) Singapore: Thyrozol;
  • (SI) Slovenia: Athyrazol | Favistan;
  • (SK) Slovakia: Favistan | Thyrozol;
  • (TH) Thailand: Methimazole | Tapazole | Timazol;
  • (TN) Tunisia: Thiamazole uni pharma | Thyrozol;
  • (TR) Turkey: Perizol | Thyromazol;
  • (TW) Taiwan: Based | Hontan | Lica | Medazole | Mepazole | Mercazole | Methimazole | Tapazole | Thimazol;
  • (UA) Ukraine: Mercazolil | Methizol | Thyrozol;
  • (UY) Uruguay: Metidazol | Metimazol | Mmi;
  • (VE) Venezuela, Bolivarian Republic of: Tapazol;
  • (VN) Viet Nam: Thysedow
  1. <800> Hazardous Drugs—Handling in Healthcare Settings. United States Pharmacopeia and National Formulary (USP 43-NF 38). Rockville, MD: United States Pharmacopeia Convention; 2020:74-92.
  2. Abe Y, Sato H, Sakai H et al. Antithyroid treatment of maternal hyperthyroidism during lactation. 11th International Thyroid Congress. Toronto, Ontario, Canada, September 10-15, 1995. Abstracts. Thyroid. 1995;5(suppl 1):S1-S275. [PubMed 7580275]
  3. Abdi H, Amouzegar A, Azizi F. Antithyroid drugs. Iran J Pharm Res. 2019;18(suppl 1):1-12. doi:10.22037/ijpr.2020.112892.14005 [PubMed 32802086]
  4. Alexander EK, Pearce EN, Brent GA, et al. 2017 Guidelines of the American Thyroid Association for the Diagnosis and Management of Thyroid Disease During Pregnancy and the Postpartum. Thyroid. 2017;27(3):315-389. [PubMed 28056690]
  5. American College of Obstetricians and Gynecologists (ACOG) Committee on Practice Bulletins—Obstetrics. Practice Bulletin No. 223: Thyroid disease in pregnancy Obstet Gynecol. 2020;135(6):e261-e274. doi:10.1097/AOG.0000000000003893 [PubMed 32443080]
  6. Amino N, Arata N. Thyroid dysfunction following pregnancy and implications for breastfeeding. Best Pract Res Clin Endocrinol Metab. 2020;34(4):101438. doi:10.1016/j.beem.2020.101438 [PubMed 32651061]
  7. Andersohn F, Konzen C, Garbe E. Systematic review: agranulocytosis induced by nonchemotherapy drugs. Ann Intern Med. 2007;146(9):657-665. doi:10.7326/0003-4819-146-9-200705010-00009 [PubMed 17470834]
  8. Anderson PO, Sauberan JB. Modeling drug passage into human milk. Clin Pharmacol Ther. 2016;100(1):42-52. [PubMed 27060684]
  9. Arai N, Nemoto K, Oh-Ishi S, Nonaka M, Hayashihara K, Saito T. Methimazole-induced ANCA-associated vasculitis with diffuse alveolar haemorrhage. Respirol Case Rep. 2018;6(5):e00315. doi:10.1002/rcr2.315 [PubMed 29760925]
  10. Araújo-Fernández S, Ahijón-Lana M, Isenberg DA. Drug-induced lupus: Including anti-tumour necrosis factor and interferon induced. Lupus. 2014;23(6):545-553. doi:10.1177/0961203314523871 [PubMed 24557776]
  11. Balavoine AS, Glinoer D, Dubucquoi S, Wémeau JL. Antineutrophil cytoplasmic antibody-positive small-vessel vasculitis associated with antithyroid drug therapy: how significant is the clinical problem? Thyroid. 2015;25(12):1273-1281. doi:10.1089/thy.2014.0603 [PubMed 26414658]
  12. Bartalena L, Bogazzi F, Martino E. Adverse effects of thyroid hormone preparations and antithyroid drugs. Drug Saf. 1996;15(1):53-63. doi:10.2165/00002018-199615010-00004 [PubMed 8862963]
  13. Bartalena L, Piantanida E, Tanda ML. Methimazole treatment and acute pancreatitis: both caution and reassurance are needed. J Clin Endocrinol Metab. 2020;105(12):dgaa636. doi:10.1210/clinem/dgaa636 [PubMed 32895723]
  14. Beernaert L, Vanderhulst J. Antithyroid drug-induced lupus erythematosus and immunoglobulin A deficiency. Am J Case Rep. 2020;21:e927929. doi:10.12659/AJCR.927929 [PubMed 33349625]
  15. Brix TH, Lund LC, Henriksen DP, et al. Methimazole and risk of acute pancreatitis. Lancet Diabetes Endocrinol. 2020;8(3):187-189. doi:10.1016/S2213-8587(20)30025-5 [PubMed 32035032]
  16. Burch HB, Cooper DS. Management of Graves disease: a review [published correction appears in JAMA. 2016;315(6):614]. JAMA. 2015;314(23):2544-2554. doi:10.1001/jama.2015.16535 [PubMed 26670972]
  17. Chen F, Yang J, Liu Y, et al. Insulin autoimmune syndrome: three case reports. Medicine (Baltimore). 2018;97(51):e13486. doi:10.1097/MD.0000000000013486 [PubMed 30572448]
  18. Chen WT, Chi CC. Associations of HLA genotypes with antithyroid drug-induced agranulocytosis: a systematic review and meta-analysis of pharmacogenomics studies. Br J Clin Pharmacol. 2019;85(9):1878-1887. doi:10.1111/bcp.13989 [PubMed 31108563]
  19. Cheung CL, Sing CW, Tang CS, et al. HLA-B*38:02:01 predicts carbimazole/methimazole-induced agranulocytosis. Clin Pharmacol Ther. 2016;99(5):555-561. doi:10.1002/cpt.309 [PubMed 26599303]
  20. Clark SM, Saade GR, Snodgrass WR, et al. Pharmacokinetics and pharmacotherapy of thionamides in pregnancy. Ther Drug Monit. 2006;28(4):477-483. [PubMed 16885714]
  21. Cooper DS. Antithyroid drugs. N Engl J Med. 2005;352(9):905-917. [PubMed 15745981]
  22. Cooper DS, Goldminz D, Levin AA, et al. Agranulocytosis associated with antithyroid drugs. Effects of patient age and drug dose. Ann Intern Med. 1983;98(1):26-29. doi:10.7326/0003-4819-98-1-26 [PubMed 6687345]
  23. Expert opinion. Senior Renal Editorial Team: Bruce Mueller, PharmD, FCCP, FASN, FNKF; Jason A. Roberts, PhD, BPharm (Hons), B App Sc, FSHP, FISAC; Michael Heung, MD, MS.
  24. Gomez Cruz MJ, Jabbar M, Saini N, et al. Severe hypoglycemia secondary to methimazole-induced insulin autoimmune syndrome in a 16 year old African-American male. Pediatr Diabetes. 2012;13(8):652-655. doi:10.1111/j.1399-5448.2012.00884.x [PubMed 22759245]
  25. Guo JY, Chang CL, Chen CC. Association between thionamides and acute pancreatitis: a case-control study. Thyroid. 2020;30(11):1574-1578. doi:10.1089/thy.2019.0589 [PubMed 32380933]
  26. Hallberg P, Eriksson N, Ibañez L, et al. Genetic variants associated with antithyroid drug-induced agranulocytosis: a genome-wide association study in a European population. Lancet Diabetes Endocrinol. 2016;4(6):507-516. doi:10.1016/S2213-8587(16)00113-3 [PubMed 27157822]
  27. Hallman BL, Hurst JW. Loss of taste as toxic effect of methimazole (tapazole) therapy; report of three cases. J Am Med Assoc. 1953;152(4):322. doi:10.1001/jama.1953.63690040006007d [PubMed 13044528]
  28. Hasegawa J, Hoshino J, Sekine A, et al. Clinical and histological features of antineutrophil cytoplasmic antibody-associated vasculitis related to antithyroid drugs . Clin Nephrol. 2018;89(6):438-444. doi:10.5414/CN109364 [PubMed 29648530]
  29. Hodak SP, Huang C, Clarke D, Burman KD, Jonklaas J, Janicic-Kharic N. Intravenous methimazole in the treatment of refractory hyperthyroidism. Thyroid. 2006;16(7):691-695. doi:10.1089/thy.2006.16.691 [PubMed 16889494]
  30. Hori Y, Arizono K, Hara S, Kawai R, Hara M, Yamada A. Antineutrophil cytoplasmic autoantibody-positive crescentic glomerulonephritis associated with thiamazole therapy. Nephron. 1996;74(4):734-735. doi:10.1159/000189486 [PubMed 8956314]
  31. Ito S. Drug therapy for breast-feeding women. N Engl J Med. 2000;343(2):118-126. [PubMed 10891521]
  32. Jamp Methimazole (methimazole) [product monograph]. Boucherville, Quebec, Canada: Jamp Pharma Corporation; July 2019.
  33. Jansson R, Lindström B, Dahlberg PA. Pharmacokinetic properties and bioavailability of methimazole. Clin Pharmacokinet. 1985;10(5):443-450. doi:10.2165/00003088-198510050-00006 [PubMed 4042519]
  34. Jin S, Li X, Fan Y, et al. Association between genetic polymorphisms of SLCO1B1 and susceptibility to methimazole-induced liver injury. Basic Clin Pharmacol Toxicol. 2019;125(6):508-517. doi:10.1111/bcpt.13284 [PubMed 31240859]
  35. Johnson DG, Campbell S. Hormonal and metabolic agents. In: Bressler R, Katz MD, eds. Geriatric Pharmacology. McGraw-Hill; 1993:427-450.
  36. Josol CV, Buenaluz-Sedurante M, Sandoval MA, Castillo G. Successful treatment of methimazole-induced severe aplastic anaemia in a diabetic patient with other co-morbidities. BMJ Case Rep. 2010;2010:bcr0520102993. doi:10.1136/bcr.05.2010.2993 [PubMed 22802368]
  37. Kawachi Y, Nukaga H, Hoshino M, Iwata M, Otsuka F. ANCA-associated vasculitis and lupus-like syndrome caused by methimazole. Clin Exp Dermatol. 1995;20(4):345-347. doi:10.1111/j.1365-2230.1995.tb01340.x [PubMed 8548997]
  38. Kliegman RM, Stanton BMD, St. Geme J, Schor NF, eds. Nelson' s Textbook of Pediatrics. 20th ed. Saunders Elsevier; 2016.
  39. Komine N, Kaizu K, Uriu K, Matsuoka-Ito A, Takeda Y, Nakamata T. Pharmacokinetics of the antithyroid drug thiamazole in a chronic hemodialysis patient with hyperthyroidism. Clin Exp Nephrol. 2002;6(3):170-174. doi:10.1007/s101570200030 [PubMed 24989959]
  40. Kubota S. Successful re-administration of low-dose of methimazole (MMI) in Graves' disease patients who experienced allergic cutaneous reactions to MMI at initial treatment and had received long-term propylthiouracil (PTU). Intern Med. 2016;55(22):3235-3237. doi:10.2169/internalmedicine.55.7281 [PubMed 27853063]
  41. Li X, Jin S, Fan Y, et al. Association of HLA-C*03:02 with methimazole-induced liver injury in Graves' disease patients. Biomed Pharmacother. 2019;117:109095. doi:10.1016/j.biopha.2019.109095 [PubMed 31202168]
  42. Methimazole tablet [prescribing information]. Congers, NY: Chartwell Pharmaceuticals LLC; December 2021.
  43. Minkley L, Göhring-Frischholz K, Mörike K, Lauer UM, Müssig K. Severe gastrointestinal haemorrhage after methimazole intake. Clin Endocrinol (Oxf). 2011;74(5):657-658. doi:10.1111/j.1365-2265.2010.03945.x [PubMed 21114679]
  44. Nabil N, Miner DJ, Amatruda JM. Methimazole: an alternative route of administration. J Clin Endocrinol Metab. 1982;54(1):180-181. [PubMed 7054215]
  45. Nakamura H, Noh JY, Itoh K, Fukata S, Miyauchi A, Hamada N. Comparison of methimazole and propylthiouracil in patients with hyperthyroidism caused by Graves' disease. J Clin Endocrinol Metab. 2007;92(6):2157-2162. doi:10.1210/jc.2006-2135 [PubMed 17389704]
  46. Nayak B, Burman K. Thyrotoxicosis and thyroid storm. Endocrinol Metab Clin North Am. 2006;35(4):663-686. [PubMed 17127140]
  47. Otsuka F, Noh JY, Chino T, et al. Hepatotoxicity and cutaneous reactions after antithyroid drug administration. Clin Endocrinol (Oxf). 2012;77(2):310-315. doi:10.1111/j.1365-2265.2012.04365.x [PubMed 22332800]
  48. Pecere A, Caputo M, Sarro A, et al. Methimazole treatment and risk of acute pancreatitis: a population-based cohort study. J Clin Endocrinol Metab. 2020;105(12):dgaa544. doi:10.1210/clinem/dgaa544 [PubMed 32813014]
  49. Plantinga TS, Arts P, Knarren GH, et al. Rare NOX3 variants confer susceptibility to agranulocytosis during thyrostatic treatment of Graves' disease. Clin Pharmacol Ther. 2017;102(6):1017-1024. doi:10.1002/cpt.733 [PubMed 28486791]
  50. Reynolds LR, Bhathena D. Nephrotic syndrome associated with methimazole therapy. Arch Intern Med. 1979;139(2):236-237. [PubMed 434980]
  51. Ribeiro Cde O, Magrin PF, Vilar EA, Durães SM, Estrella RR. Cutaneous leukocytoclastic vasculitis in the presence of methimazole therapy. An Bras Dermatol. 2013;88(2):283-286. doi:10.1590/S0365-05962013000200021 [PubMed 23739718]
  52. Roldan EC, Nigrin G. Peripheral neuritis after methimazole therapy. N Y State J Med. 1972;72(23):2898-2900. [PubMed 4508415]
  53. Ross DS. Amiodarone and thyroid dysfunction. Post TW, ed. UpToDate. Waltham, MA: UpToDate Inc. http://www.uptodate.com. Accessed February 25, 2020d.
  54. Ross DS. Thionamides in the treatment of Graves' disease. Post TW, ed. UpToDate. Waltham, MA: UpToDate Inc. http://www.uptodate.com. Accessed August 31, 2022a.
  55. Ross DS. Thyroid storm. Post TW, ed. UpToDate. Waltham, MA: UpToDate Inc. http://www.uptodate.com. Accessed October 12, 2022c.
  56. Ross DS. Treatment of toxic adenoma and toxic multinodular goiter. Post TW, ed. UpToDate. Waltham, MA: UpToDate Inc. http://www.uptodate.com. Accessed January 24, 2022b.
  57. Ross DS, Burch HB, Cooper DS, et al. 2016 American Thyroid Association guidelines for diagnosis and management of hyperthyroidism and other causes of thyrotoxicosis. Thyroid. 2016;26(10):1343-1421. doi:10.1089/thy.2016.0229. [PubMed 27521067]
  58. Shell A, Sullivan JW. Acute kidney injury following methimazole initiation: a case report. J Pharm Pract. 2020;33(1):99-101. doi:10.1177/0897190018789277 [PubMed 30111225]
  59. So E, Arakaki R. Toxic multinodular goiter in a patient with end-stage renal disease and hemodialysis. Hawaii J Med Public Health. 2014;73(7):217-220. [PubMed 25089233]
  60. Sperling MA, ed. Pediatric Endocrinology. 4th ed. Elsevier; 2014.
  61. Surks MI. Iodine-induced thyroid dysfunction. Post TW, ed. UpToDate. Waltham, MA: UpToDate Inc. http://www.uptodate.com. Accessed August 31, 2022.
  62. Tapazole (methimazole) [prescribing information]. Wilmington, NC: Pfizer Inc; December 2019.
  63. Tapazole (methimazole) [product monograph]. Saint-Laurent, Quebec, Canada: Paladin Labs Inc; April 2023.
  64. Tripodi PF, Ruggeri RM, Campennì A, et al. Central nervous system vasculitis after starting methimazole in a woman with Graves' disease. Thyroid. 2008;18(9):1011-1013. doi:10.1089/thy.2008.0121 [PubMed 18788922]
  65. US Department of Health and Human Services; Centers for Disease Control and Prevention; National Institute for Occupational Safety and Health. NIOSH list of antineoplastic and other hazardous drugs in healthcare settings 2016. https://www.cdc.gov/niosh/docs/2016-161/default.html. Updated September 2016. Accessed October 13, 2023.
  66. Vicente N, Cardoso L, Barros L, Carrilho F. Antithyroid drug-induced agranulocytosis: state of the art on diagnosis and management. Drugs R D. 2017;17(1):91-96. doi:10.1007/s40268-017-0172-1 [PubMed 28105610]
  67. Walter MA, Christ-Crain M, Schindler C, Müller-Brand J, Müller B. Outcome of radioiodine therapy without, on or 3 days off carbimazole: a prospective interventional three-group comparison. Eur J Nucl Med Mol Imaging. 2006;33(6):730-737. doi:10.1007/s00259-006-0092-8 [PubMed 16607544]
  68. Wang MT, Lee WJ, Huang TY, Chu CL, Hsieh CH. Antithyroid drug-related hepatotoxicity in hyperthyroidism patients: a population-based cohort study. Br J Clin Pharmacol. 2014;78(3):619-629. doi:10.1111/bcp.12336 [PubMed 25279406]
  69. Woeber KA. Methimazole-induced hepatotoxicity. Endocr Pract. 2002;8(3):222-224. doi:10.4158/EP.8.3.222 [PubMed 12467281]
  70. Zou H, Jin L, Wang LR, Braddock M, Cai WW, Zheng MH. Methimazole-induced cholestatic hepatitis: two cases report and literature review. Oncotarget. 2016;7(4):5088-5091. doi:10.18632/oncotarget.6144 [PubMed 26498145]
Topic 9627 Version 352.0

آیا می خواهید مدیلیب را به صفحه اصلی خود اضافه کنید؟