Thyrotropin Alfa

H01A - Anterior pituitary lobe hormones and analogues ATC H01AB01 Protein approved 1998 Parenteral

JFDA label: Thyrogen

Mechanism of Action

Agonist of Thyrotropin receptor — Thyroid stimulating hormone receptor agonist

Target	Action	Gene / class
Thyrotropin receptor efficacy	AGONIST	TSHR

Indications

Approved

Diagnostic imaging
Thyroid tissue remnant ablation

Contraindications

Source: Lexicomp

Hypersensitivity to thyrotropin alfa or any component of the formulation Absolute
U.S. labeling: There are no contraindications listed in the manufacturer's labeling Absolute

Adverse Reactions

Very Common >10%Common 1–10%Uncommon 0.1–1% Rare 0.01–0.1%Very Rare <0.01%Not Known

Nervous system disorders (3)

Common dizziness · fatigue · Headache

Gastrointestinal disorders (1)

Common Vomiting

Musculoskeletal and connective tissue disorders (1)

Common Weakness

Other (2)

Very Common Gastrointestinal: Nausea

Not Known Endocrine & metabolic: Altered thyroid hormone levels (increased)

Dosing

Source: Lexicomp

Note: Consider pretreatment with glucocorticoids for patients in whom local tumor expansion may compromise vital anatomic structures (such as trachea, CNS, or extensive macroscopic lung metastases). Diagnostic imaging: IM: 0.9 mg, followed 24 hours later by a second 0.9 mg dose; obtain serum Tg sample 72 hours after the second thyrotropin alfa injection Thyroid tissue remnant ablation: IM: 0.9 mg, followed 24 hours later by a second 0.9 mg dose. Radioiodine administration should be given 24 hours following the second thyrotropin alfa injection (for diagnostic scanning and remnant ablation). Perform diagnostic scanning 48 hours after radioiodine administration (72 hours after the second thyrotropin alfa injection). Post-therapy scanning may be delayed (additional days) to allow decline of background activity.

Refer to adult dosing.

There are no dosage adjustments provided in the manufacturer’s labeling; however, elimination is significantly slower in dialysis-dependent end-stage renal impairment and TSH level elevation may be prolonged.

There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).

Warnings & Precautions

Source: Lexicomp

Hyperthyroidism

Thyrotropin alfa use may cause a transient (over 7 to 14 days) and significant rise in serum thyroid hormone concentration in patients with substantial in situ thyroid tissue or with functional thyroid cancer metastases. Thyrotropin alfa–induced hyperthyroidism may result in serious complications in patients with certain risk factors (heart disease, extensive metastatic disease or with underlying serious illness); consider hospitalization for administration and subsequent observation. Deaths within 24 hours of thyrotropin alfa administration have been reported.

Stroke

Postmarketing reports of stroke or symptoms suggestive of stroke (eg, unilateral weakness) have occurred within 3 days of administration in patients without known central nervous system metastases. A majority of these patients had risk factors for stroke (eg, smokers or history of migraine) or were young women taking oral contraceptives. Patients should be well hydrated prior to administration.

Tumor growth

Sudden, rapid, and painful growth of residual thyroid tissue or distant metastases may occur following thyrotropin alfa administration. Symptoms are associated with tissue location and include acute hemiplegia, hemiparesis, and vision loss 1 to 3 days after administration. Laryngeal edema, pain at site of distant metastases, and respiratory distress requiring tracheotomy have also been reported. Consider glucocorticoid premedication in patients where local tumor enlargement may compromise vital structures (trachea, CNS, or extensive macroscopic lung metastases). Disease-related concerns:

Cardiovascular disease

Patients with known history of heart disease in the presence of significant residual thyroid tissue are at increased risk for thyrotropin alfa-induced hyperthyroidism.

Renal impairment

Thyrotropin alfa elimination is significantly reduced in dialysis-dependent end-stage renal impairment, leading to prolonged elevation of TSH levels. Special populations:

Elderly

Elderly patients with residual thyroid tissue are at increased risk for thyrotropin alfa-induced hyperthyroidism

Pregnancy & Lactation

Pregnancy

FDA category C

Animal reproduction studies have not been conducted. Effects on the fetus or pregnant woman are unknown.

Lactation

It is not known if thyrotropin alfa is excreted in breast milk. The manufacturer recommends that caution be exercised when administering thyrotropin alfa to nursing women.

Monitoring

Clinical pearl	Neurologic adverse events (hemiplegia, hemiparesis, stroke, weakness); dyspnea, dysphonia, stridor or other symptoms of local tumor growth

Biology & Pharmacokinetics

Pharmacokinetics

Half-life	10.0 h

Drug–drug interactions (45, DDInter)

Interacting drug	Severity	Management
Acarbose	moderate
Acetohexamide	moderate
Albiglutide	moderate
Alogliptin	moderate
Canagliflozin	moderate
Chlorpropamide	moderate
Dapagliflozin	moderate
Dulaglutide	moderate
Empagliflozin	moderate
Ertugliflozin	moderate
Exenatide	moderate
Glimepiride	moderate
Glipizide	moderate
Glyburide	moderate
Insulin aspart (aspart protamine)	moderate
Insulin aspart (aspart)	moderate
Insulin degludec	moderate
Insulin detemir	moderate
Insulin glargine	moderate
Insulin glulisine	moderate
Insulin human	moderate
Insulin human (inhalation, rapid acting)	moderate
Insulin human (isophane)	moderate
Insulin human (regular)	moderate
Insulin human (zinc extended)	moderate
Insulin human (zinc)	moderate
Insulin lispro	moderate
Insulin lispro (protamine)	moderate
Ketamine	moderate
Linagliptin	moderate
Liraglutide	moderate
Lixisenatide	moderate
Metformin	moderate
Miglitol	moderate
Nateglinide	moderate
Pioglitazone	moderate
Pramlintide	moderate
Repaglinide	moderate
Rosiglitazone	moderate
Saxagliptin	moderate

Showing 40 of 45.

Registered Products (1)

Brand	Form / strength	Pack	Agent	Citizen (JOD)
Thyrogen	Vial 0.9 mg	2 vial	Ulfa Pharma Co.	—