Diazoxide
7-chloro-3-methyl-2H-1,2,4-benzothiadiazine 1,1-dioxide
Also known as: Proglycem · Hyperstat IV · Eudemine · Glicemin · Hypertonalum · Proglicem · Sefulken · Tensuril · diazoxidum · NSC-64198 · Sch-6783 · SRG-95213
Reviewed by the VetSheet Veterinary TeamUpdated Apr 5, 2026Evidence-based veterinary reference
Audited v13 dosing evidence
Structured calculator evidenceMedical management of insulinoma after stabilization of hypoglycemic crisis
- q12h
Governing clinical context (1)
- Once hypoglycemic crisis stabilized
Doses are a clinical reference for licensed veterinary professionals. Always confirm against the current label and the individual patient.
Overview
Diazoxide is a non-diuretic thiazide derivative primarily utilized in veterinary medicine for the medical management of insulinomas (insulin-secreting islet cell tumors), particularly in dogs and ferrets.
While it possesses potent direct vasodilatory properties (used intravenously in humans for hypertensive emergencies), its oral use in animals leverages its profound hyperglycemic side effects. By antagonizing insulin release, it helps stabilize blood glucose levels in patients with refractory hypoglycemia.
Clinical Pearls:
- It is often used in conjunction with dietary management (frequent small meals) and glucocorticoids (e.g., prednisone) when those modalities alone fail to control hypoglycemic crises.
- Due to its structural similarity to thiazide diuretics, it can cause sodium and water retention, but it lacks diuretic efficacy.
Mechanism of action
Diazoxide exerts its hyperglycemic and vasodilatory effects via multiple mechanisms:
- K+ ATP Channel Activation: It binds to the sulfonylurea receptor 1 (SUR1) subunit of the ATP-sensitive potassium (K+ ATP) channels on pancreatic beta cells → channel opening → cellular hyperpolarization → decreased intracellular calcium (Ca2+) influx → inhibition of insulin exocytosis from secretory granules.
- Beta-Adrenergic Stimulation: Stimulates the release of epinephrine, which promotes hepatic glycogenolysis and inhibits peripheral cellular glucose uptake.
- Vasodilation: Directly relaxes arteriolar smooth muscle by opening K+ ATP channels in vascular smooth muscle cells → hyperpolarization → vasodilation → decreased peripheral vascular resistance and blood pressure.
Safety & warnings
Contraindications
- Hypoglycemia secondary to insulin overdosage in diabetic patients
- Hypersensitivity to thiazide diuretics (unless benefits outweigh risks)
- Hypersensitivity to thiazides
- Functional hypoglycemia (non-insulinoma)
Adverse effects
- Hypersalivation
- Tachycardia
- Agranulocytosis
- Aplastic anemia
- Thrombocytopenia
- Diabetes mellitus
- Sodium and water retention
- Malaise (ferrets)
- Bone marrow suppression (ferrets)
- Gastrointestinal upset (anorexia, vomiting, diarrhea)
- Hyperglycemia
- Cataracts (rare)
- Bone marrow suppression (rare)
Precautions
Caution: Use with extreme care in patients with congestive heart failure (CHF) or renal disease due to sodium and water retention properties.
- Hepatic Disease: Adverse effects may be more pronounced in dogs with concurrent hepatic disease.
- Pregnancy: FDA Category C; animal studies have shown adverse effects on the fetus. Use only if benefits outweigh risks.
- Laboratory Interference: May cause a false-negative insulin response to the glucagon-stimulation test and displace bilirubin from plasma proteins.
Drug interactions
May decrease the effectiveness of diazoxide in increasing glucose levels
Diazoxide may enhance the hypotensive actions of other hypotensive agents
May enhance the hyperglycemic effects of diazoxide
Diazoxide may increase the metabolism, or decrease the protein binding of phenytoin
May potentiate the hyperglycemic effects of oral diazoxide. Can be used synergistically, but caution is advised as hypotension may occur
Potentiate hyperglycemic and hyperuricemic effects
May potentiate hyperglycemia
May antagonize the effects of diazoxide
Diazoxide is highly protein-bound and may displace or be displaced by other drugs, altering free drug concentrations
Monitoring
- Blood (serum) glucose
- CBC (at least every 3-4 months)
- Physical exam (monitor for clinical signs of adverse effects like edema, cataracts, or tachycardia)
- Blood glucose
- Electrolytes (sodium, potassium)
- Complete blood count (CBC) periodically
- Signs of fluid retention/edema
Pharmacokinetics
Half-life
Absorption
In humans, serum diazoxide levels peak at about 12 hours after dosing with capsules. Blood levels required for hyperglycemic effects are unknown.
Distribution
Highest concentrations are found in the kidneys, with high levels also in the liver and adrenal glands. Approximately 90% is bound to plasma proteins. It crosses the placenta and enters the CNS.
Metabolism
Partially metabolized in the liver.
Elimination
Excreted as both metabolites and unchanged drug by the kidneys. Serum half-life is prolonged in patients with renal impairment.
Overdose
Acute overdosage may result in severe hyperglycemia and ketoacidosis.
- Treatment: Administer insulin, intravenous fluids, and correct electrolyte imbalances.
- Monitoring: Intensive and prolonged monitoring of blood glucose and acid-base status is highly recommended.
Available products
Formulations
- Oral capsules
- Oral suspension
- 15 mg/ml injectable solution (special order)
- 50 mg oral tablet
Veterinary
- None
Human-labeled
- Diazoxide Oral Capsules: 50 mg (Proglycem)
- Diazoxide Oral Suspension: 50 mg/mL with sorbitol in 30 mL calibrated dropper (Proglycem)
- Eudemine 50 mg tablet
- Eudemine 15 mg/ml injectable solution
Regulatory status
POM (Prescription Only Medicine)
POM (Prescription Only Medicine)
No regulatory data for: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
Storage & stability
Store capsules and oral suspensions at 2-30°C and protect from light. Protect solutions/suspensions from freezing. Do not use darkened solutions/suspensions, as they may be subpotent.
Client information
- Purpose: This medication is used to prevent life-threatening drops in blood sugar caused by insulin-secreting tumors (insulinomas).
- Administration: The drug is reportedly very bitter. Administering the medication with meals can help mask the taste and reduce gastrointestinal side effects like vomiting or diarrhea. Compounding pharmacies may be able to formulate a sugar-free flavored liquid.
- Monitoring: Watch your pet closely for signs of hyperglycemia (excessive thirst, increased urination) or returning hypoglycemia (weakness, stumbling, seizures, lethargy).
- Adverse Effects: Contact your veterinarian if you notice abnormal bleeding, severe vomiting/diarrhea, or swelling (fluid retention).
VetSheet drug reference is intended for licensed veterinary professionals as a clinical decision-support aid, not a substitute for professional judgement or the manufacturer’s current label.