RyR1 Structural Alterations Explain Statin-Associated Muscle Dysfunction
December 16, 2025
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Brand Name :
Vykat XR
Synonyms :
Diazoxide choline
Class :
Metabolic, Endocrine
Brand Name :
Vykat XR
Synonyms :
Diazoxide choline
Class :
Metabolic, Endocrine
Dosage forms & Strengths:
Adult
Tablet (extended release)
25 mg
75 mg
150 mg
Administer maximum dose of 5.8 mg/kg daily or 525 mg daily
For 40 to <65 kg:
Weeks 1-2: Take a dose of 75 mg orally daily
Weeks 3-4: Take a dose of 150 mg orally daily
Weeks 5-6: Take a dose of 225 mg orally daily
For 65 to <100 kg:
Weeks 1-2: Take a dose of 150 mg orally daily
Weeks 3-4: Take a dose of 225 mg orally daily
Weeks 5-6: Take a dose of 300 mg orally daily
For 100 to <135 kg:
Weeks 1-2: Take a dose of 150 mg orally daily
Weeks 3-4: Take a dose of 300 mg orally daily
Weeks 5-6: Take a dose of 375 mg orally daily
For ≥135 kg:
Weeks 1-2: Take a dose of 150 mg orally daily
Weeks 3-4: Take a dose of 300 mg orally daily
Weeks 5-6: Take a dose of 455 mg orally daily
Dosage Modifications
Renal or hepatic impairment
Not studied
Coadministration with strong CYP1A2 inhibitors
Administer maximum dose of 3.6 mg/kg daily or 325 mg/daily
Dosing Considerations
Do not replace diazoxide choline with oral suspension.
Laboratory testing before initiation
Test glucose levels and optimize blood sugar in hyperglycemia.
Pediatric
Tablet (extended release)
25 mg
75 mg
150 mg
Administer maximum dose of 5.8 mg/kg daily or 525 mg daily
For 20 to <30 kg:
Weeks 1-2: Take a dose of 25 mg orally daily
Weeks 3-4: Take a dose of 50 mg orally daily
Weeks 5-6: Take a dose of 75 mg orally daily
For 30 to <40 kg:
Weeks 1-2: Take a dose of 75 mg orally daily
Weeks 3-6: Take a dose of 100 mg orally daily
For 40 to <65 kg:
Weeks 1-2: Take a dose of 75 mg orally daily
Weeks 3-4: Take a dose of 150 mg orally daily
Weeks 5-6: Take a dose of 225 mg orally daily
Dosage Modifications
Renal or hepatic impairment
Not studied
Coadministration with strong CYP1A2 inhibitors
Administer maximum dose of 3.6 mg/kg daily or 325 mg/daily
Dosing Considerations
Do not replace diazoxide choline with oral suspension.
Laboratory testing before initiation
Test glucose levels and optimize blood sugar in hyperglycemia.
Geriatrics
Refer as per adult dose
Actions and Spectrum
The mechanism of hyperphagia treatment remains unclear.
It activates potassium channels in hypothalamus, pancreas, and fat to reduce hyperphagia.
Diazoxide treats symptomatic hypoglycemia without diuretic effects.
Diazoxide binds to SUR subunit that promotes potassium efflux from pancreatic beta-cells via KATP channels.
Frequency defined:
>10%
Edema
Hypertrichosis
Hyperglycemia
Rash
1-10%
Arthralgia
Influenza
Pyrexia
Nasopharyngitis
Black Box Warning
None
Contraindication / Caution
Contraindication:
Hypersensitivity to diazoxide
Caution:
Hyperglycemia
Fluid overload
Risk of fluid retention and heart failure
Hypotension & cardiovascular effects
Pregnancy / Lactation
Pregnancy Warnings:
Pregnancy category: N/A
Lactation: Excretion of the drug into the human breast milk is unknown
Pregnancy categories:
Category A: Satisfactory and well-controlled studies show no evidence of risk to the fetus in the first trimester or in the later trimester.
Category B: No evidence of risk to fetus found in animal reproduction studies and there are not enough studies on pregnant women.
Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for an effect in humans, care must be taken for potential risks in pregnant women.
Category D: There is adequate data available with sufficient evidence of human fetal risk from various platforms, but despite potential risks may be used only in emergency cases for potential benefits.
Category X: Drugs listed in this category clearly outweigh risks over benefits. These category drugs should be prohibited for pregnant women.
Category N: There is no data available for the drug under this category.
Pharmacology
It activates ATP-sensitive potassium channels hyperpolarizes membranes to reduce calcium influx and lowers cell excitability.
It inhibits insulin secretion to increase blood glucose levels while direct arterial vasodilation reduces systemic vascular resistance.
Pharmacodynamics
Diazoxide lowers blood pressure by promoting vasodilation in peripheral arterioles’ smooth muscle.
Diazoxide orally increases blood glucose dose-dependently.
In patients with normal renal function, the effect lasts eight hours max.
Pharmacokinetics
Absorption:
It has peak plasma time of 16 hours and reaches steady state after 7 days.
Distribution:
It has high protein binding up to 91-93%.
Volume of distribution: 44.9 L.
Metabolism:
Oxidation or sulfate conjugation produces two inactive metabolites.
Elimination and excretion:
Half-life shows for single dose in healthy volunteers is 28.7-32.4 hours.
It excreted through urine up to 85-92%.
Administration
It is available in tablet form for oral administration.
Swallow whole tablet with water and do not crush or chew the tablet.
Patient information leaflet
Generic Name: Diazoxide choline
Why do we use Diazoxide choline?
Diazoxide choline is indicated to treat hyperphagia with Prader-Willi syndrome.
It is used as first-line therapy in patient with persistent hypoglycemia due to excessive insulin secretion.
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