Pentagastrin
Also known as: AY-6608, Pentagastrin, Pentagastrin stimulation test, Peptavlon, PG, Synthetic gastrin, β-Ala-Trp-Met-Asp-Phe-NH2 (Boc-protected)
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Summary
Pentagastrin is a synthetic pentapeptide analogue of gastrin used primarily as a diagnostic agent to stimulate gastric acid secretion and to provoke calcitonin release in medullary thyroid carcinoma testing.
Mechanism of Action
Activates CCK-B/gastrin receptors on enterochromaffin-like cells, stimulating gastric acid secretion and gastric motility.
Routes of Administration
Goals & Uses
- Provocative test for medullary thyroid carcinomaDiagnostic/OncologyHigh
- Research tool for CCK-B receptor pharmacologyResearchModerate
- Evaluation of pheochromocytoma (historical)Diagnostic/EndocrinologyLow
- Diagnostic stimulation of gastric acid secretionDiagnosticHigh
- Gastric acid secretion stimulation (diagnostic)DiagnosticHigh
- Calcitonin stimulation test for medullary thyroid carcinomaDiagnosticHigh
Contraindications
- Known hypersensitivity to pentagastrinImmuneHigh
- Zollinger‑Ellison syndromeGastrointestinalHigh
- Inflammatory bowel disease (acute)GastrointestinalModerate
- Obstructive jaundice / biliary diseaseHepatobiliaryModerate
- PregnancyPopulationModeratePotential fetal risk or insufficient safety data
- Hypersensitivity to pentagastrin or excipientsAllergy/ImmunologyHigh
- Active gastrointestinal hemorrhageGastrointestinalHigh
- Active peptic ulcer diseaseGastrointestinalHigh
Adverse Effects
- Anaphylaxis / hypersensitivityImmunologicRare
- Dizziness / lightheadednessNeurologicUncommon
- HypotensionCardiovascularRareLow blood pressure
- Abdominal crampsGastrointestinalCommon
- FlushingVascularUncommonWarmth and redness of the skin
- Nausea and vomitingGastrointestinalCommon
- NauseaGastrointestinalCommonFeeling of sickness or urge to vomit
- Abdominal cramping / painGastrointestinalCommon
Drug Interactions
- Proton pump inhibitorsLow
- H2-receptor antagonists (e.g., ranitidine, famotidine)Moderate
- Beta-blockersLow
- Proton pump inhibitors (PPIs)High
- Anticholinergics (e.g., atropine)Moderate
Population Constraints
- PregnancyReproductive SafetyRelative
- Patients with severe hepatic or renal impairmentOrgan ImpairmentRelative
- Pediatric patientsAgeRelative
- Elderly patientsAgeRelative
- PediatricsAgeRelative
Regulatory Status
- European UnionInvestigationalNo marketing authorization; available for research purposes.
- United StatesInvestigationalNot FDA‑approved; used under IND for diagnostic studies.
- United KingdomInvestigationalNot licensed for clinical use; supplied for diagnostic research.
Previously approved in the US (Peptavlon) and other jurisdictions as a diagnostic agent; manufacturing was discontinued in the US and many other markets. No longer commercially available in most countries. Historical use for gastric acid testing and MTC screening.
Evidence & Sources
No sources recorded yet.
Frequently Asked Questions
What is Pentagastrin?
Pentagastrin is a synthetic pentapeptide analogue of gastrin used primarily as a diagnostic agent to stimulate gastric acid secretion and to provoke calcitonin release in medullary thyroid carcinoma testing.
What is Pentagastrin used for?
Pentagastrin is educationally associated with: Provocative test for medullary thyroid carcinoma, Research tool for CCK-B receptor pharmacology, Evaluation of pheochromocytoma (historical), Diagnostic stimulation of gastric acid secretion, Gastric acid secretion stimulation (diagnostic), Calcitonin stimulation test for medullary thyroid carcinoma. Educational only — not medical advice.
How is Pentagastrin administered?
Recorded routes of administration: Intravenous, Subcutaneous.
What are the potential side effects of Pentagastrin?
Reported adverse effects include: Anaphylaxis / hypersensitivity, Dizziness / lightheadedness, Hypotension, Abdominal cramps, Flushing, Nausea and vomiting, Nausea, Abdominal cramping / pain. This list is not exhaustive — consult a qualified clinician.
Who should avoid Pentagastrin?
Recorded contraindications: Known hypersensitivity to pentagastrin, Zollinger‑Ellison syndrome, Inflammatory bowel disease (acute), Obstructive jaundice / biliary disease, Pregnancy, Hypersensitivity to pentagastrin or excipients, Active gastrointestinal hemorrhage, Active peptic ulcer disease. Consult a qualified clinician before use.