Orotirelin
Also known as: CG-3703, Histalin, Orotic TRH, Orotirelin, TRH analogue
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Summary
Orotirelin is a synthetic TRH analogue developed primarily in Japan as a diagnostic agent for evaluating hypothalamic-pituitary-thyroid axis function. It stimulates TSH and prolactin secretion from the anterior pituitary and has been used to assess spinocerebellar degeneration and thyroid disorders. It has also been investigated for potential neuroprotective and CNS effects.
Mechanism of Action
Synthetic analogue of thyrotropin-releasing hormone (TRH) that binds to TRH receptors in the pituitary gland, stimulating the release of thyroid-stimulating hormone (TSH) and prolactin; used diagnostically to assess pituitary and thyroid function
Routes of Administration
Goals & Uses
- Prolactin stimulation testingEndocrinologyModerate
- Diagnostic evaluation of hypothalamic-pituitary-thyroid axisDiagnosticsHigh
- NeuroprotectionNeurologyLow
- Assessment of spinocerebellar degenerationNeurologyModerate
Contraindications
- HyperthyroidismEndocrineModerate
- PregnancyPopulationModeratePotential fetal risk or insufficient safety data
- Coronary artery diseaseCardiovascularHigh
- Hypersensitivity to orotirelin or TRH analoguesAllergyHigh
Adverse Effects
- Urge to urinateUrologicalCommon
- HeadacheNeurologicUncommonPain in the head or upper neck
- FlushingVascularCommonWarmth and redness of the skin
- NauseaGastrointestinalCommonFeeling of sickness or urge to vomit
- Transient hypotension or hypertensionCardiovascularUncommon
Drug Interactions
- GlucocorticoidsLow
- Thyroid hormones (levothyroxine)Moderate
- Dopamine agonists (bromocriptine, cabergoline)Low
Population Constraints
- Pediatric patientsAgeRelative
- Elderly patientsAgeRelative
- Patients with severe cardiovascular diseaseCardiovascularRelative
Regulatory Status
- European UnionUnapprovedNot approved by the EMA for use in the European Union
- United StatesUnapprovedNot approved by the FDA; not available as a licensed product in the United States
- United KingdomUnapprovedNot approved by the MHRA in the United Kingdom
Approved in Japan as a diagnostic and therapeutic agent. Not approved by the FDA in the United States or by the EMA in Europe.
Evidence & Sources
No sources recorded yet.
Frequently Asked Questions
What is Orotirelin?
Orotirelin is a synthetic TRH analogue developed primarily in Japan as a diagnostic agent for evaluating hypothalamic-pituitary-thyroid axis function. It stimulates TSH and prolactin secretion from the anterior pituitary and has been used to assess spinocerebellar degeneration and thyroid disorders. It has also been investigated for potential neuroprotective and CNS effects.
What is Orotirelin used for?
Orotirelin is educationally associated with: Prolactin stimulation testing, Diagnostic evaluation of hypothalamic-pituitary-thyroid axis, Neuroprotection, Assessment of spinocerebellar degeneration. Educational only — not medical advice.
How is Orotirelin administered?
Recorded routes of administration: Intravenous, Oral.
What are the potential side effects of Orotirelin?
Reported adverse effects include: Urge to urinate, Headache, Flushing, Nausea, Transient hypotension or hypertension. This list is not exhaustive — consult a qualified clinician.
Who should avoid Orotirelin?
Recorded contraindications: Hyperthyroidism, Pregnancy, Coronary artery disease, Hypersensitivity to orotirelin or TRH analogues. Consult a qualified clinician before use.