Version July 2025
Hyperphagia: Oral
|
Weight |
Initial dose (weeks 1 and 2) |
Titration dose (weeks 3 and 4) |
Titration dose (weeks 5 and 6) |
Target maintenance dose |
|---|---|---|---|---|
|
40 to <65 kg |
75 mg once daily |
150 mg once daily |
225 mg once daily |
225 mg once daily |
|
65 to <100 kg |
150 mg once daily |
225 mg once daily |
300 mg once daily |
375 mg once daily |
|
100 to <135 kg |
150 mg once daily |
300 mg once daily |
375 mg once daily |
450 mg once daily |
|
≥135 kg |
150 mg once daily |
300 mg once daily |
450 mg once daily |
525 mg once daily |
Maximum dose: 5.8 mg/kg/day or 525 mg/day.
Missed dose:
<7 days missed: Resume treatment at the previous dosage.
≥7 days missed: Reinitiate treatment with day 1 of the initial titration regimen.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Use is not recommended (has not been studied).
Use is not recommended (has not been studied).
Elevated fasting glucose or HbA1c: Temporarily interrupt diazoxide choline or reduce the dosage until glucose is appropriately managed; consider initiating or adjusting antidiabetic medications. If significant glucose elevations occur during titration, titrate over a longer duration and/or to a lower diazoxide choline dosage. If elevated glucose resolves after a dosage reduction, titrate diazoxide choline dosage in increments of ≤75 mg every 2 weeks or titrate over a longer duration to a maximum dosage of 5.8 mg/kg/day or 525 mg/day.
Fluid overload, significant: Temporarily interrupt diazoxide choline or reduce the dosage. If significant fluid overload occurs during titration, titrate over a longer duration and/or to a lower diazoxide choline dosage. If fluid overload resolves after a dosage reduction, titrate diazoxide choline dosage in increments of ≤75 mg every 2 weeks or titrate over a longer duration to a maximum dosage of 5.8 mg/kg/day or 525 mg/day.
Refer to adult dosing.
(For additional information see "Diazoxide choline: Pediatric drug information")
Dosage guidance:
Dosage form information: Do not substitute diazoxide choline ER tablets for diazoxide oral suspension; the pharmacokinetic profiles are different.
Hyperphagia, treatment:
Children ≥4 years and Adolescents: Oral:
|
Weight |
Initial dose (weeks 1 and 2) |
Titration dose (weeks 3 and 4) |
Titration dose (weeks 5 and 6) |
Target maintenance dose |
|---|---|---|---|---|
|
a Maximum daily dose: 5.8 mg/kg/day not to exceed 525 mg/day. | ||||
|
20 to <30 kg |
25 mg once daily |
50 mg once daily |
75 mg once daily |
100 mg once daily |
|
30 to <40 kg |
75 mg once daily |
150 mg once daily |
150 mg once daily |
150 mg once daily |
|
40 to <65 kg |
75 mg once daily |
150 mg once daily |
225 mg once daily |
225 mg once daily |
|
65 to <100 kg |
150 mg once daily |
225 mg once daily |
300 mg once daily |
375 mg once daily |
|
100 to <135 kg |
150 mg once daily |
300 mg once daily |
375 mg once daily |
450 mg once daily |
|
≥135 kg |
150 mg once daily |
300 mg once daily |
450 mg once daily |
525 mg once daily |
Dosing adjustment for toxicity:
Toxicity occurring during dose titration:
Elevated fasting blood glucose or HbA1c, clinically significant: Titrate over a longer duration and/or to a lower dosage.
Edema or fluid overload, clinically significant: Titrate over a longer duration and/or to a lower target dosage.
Toxicity occurring during treatment:
Elevated fasting blood glucose or HbA1c, clinically significant: Hold or decrease dose of diazoxide choline until glycemic parameters are appropriately managed (eg, initiation or adjustment of antidiabetic therapies).
Edema or fluid overload, clinically significant: May hold or decrease dose of diazoxide choline.
Titration of dose after resolution of toxicity after dosage reduction (elevated blood glucose, HbA1c, or fluid overload):
<30 kg: Titrate dose every 2 weeks (or longer) in increments of ≤25 mg/day; maximum daily dose: 5.8 mg/kg/day.
≥30 kg: Titrate dose every 2 weeks (or longer) in increments of ≤75 mg/day; maximum daily dose: 5.8 mg/kg/day not to exceed 525 mg/day.
Titration of dose after resolution of toxicity after holding diazoxide choline (elevated blood glucose, HbA1c, or fluid overload):
<7 days: Restart at previous dose.
≥7 days: Restart at initial dose and titrate to target maintenance dose as tolerated.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Children ≥4 years and Adolescents: Use is not recommended in patients with kidney impairment (has not been studied).
Children ≥4 years and Adolescents: Use is not recommended in patients with liver impairment (has not been studied).
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Reported adverse reactions are for children, adolescents, and adults.
>10%:
Cardiovascular: Edema (27%; including facial swelling, localized edema, peripheral edema, periorbital edema, pulmonary edema)
Dermatologic: Hypertrichosis (36%), skin rash (12%; including contact dermatitis, erythema multiforme, maculo-papular rash, papular rash, urticaria)
Endocrine & metabolic: Hyperglycemia (17%; including type 2 diabetes mellitus)
1% to 10%:
Endocrine & metabolic: Hirsutism (≥5%), weight gain (≥5%)
Infection: Influenza (5%)
Nervous system: Anxiety (≥5%), emotional lability (≥5%; including anger), obsessive compulsive disorder (compulsive hoarding: ≥5%), suicidal ideation (≥5%)
Neuromuscular & skeletal: Arthralgia (5%)
Respiratory: Nasopharyngitis (5%), streptococcal pharyngitis (≥5%), upper respiratory tract infection (≥5%)
Miscellaneous: Fever (6%)
Frequency not defined:
Endocrine & metabolic: Diabetic ketoacidosis, fluid retention
Nervous system: Aggressive behavior
Respiratory: Lower respiratory tract infection
Hypersensitivity (eg, erythema multiforme) to diazoxide, thiazides, or any component of the formulation.
Concerns related to adverse effects:
• Fluid overload: Edema (eg, general, localized, peripheral), which may lead to pulmonary edema, has been reported with use.
• Hyperglycemia: Elevations in blood glucose, sometimes leading to diabetic ketoacidosis, have occurred. Patients with risk factors for hyperglycemia (eg, concomitant use with growth hormone or systemic corticosteroids, elevated fasting glucose, HbA1c at ULN or above, obesity) may require more frequent monitoring. Consider consultation with health care provider experienced in hyperglycemia in patients who develop hyperglycemia.
Disease-related concerns:
• Cardiovascular disease: Use with caution in patients with compromised cardiac reserve; fluid retention may precipitate heart failure.
Dosage form specific issues:
• Interchangeability: ER tablets are not interchangeable with diazoxide oral suspension (Proglycem); pharmacokinetic profiles differ.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet Extended Release 24 Hour, Oral:
Vykat XR: 25 mg, 75 mg, 150 mg
No
Tablet, 24-hour (Vykat XR Oral)
25 mg (per each): $177.60
75 mg (per each): $532.80
150 mg (per each): $1,065.60
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Oral: Administer with or without food. Swallow tablet whole; do not chew, crush, or split.
Oral: Administer with or without food. Swallow tablet whole; do not split, crush, or chew.
Missed dose:
<7 days: Restart at previous dose.
≥7 days: Restart at initial dose and titrate to target maintenance dose as tolerated.
Hyperphagia: Treatment of hyperphagia in adults and pediatric patients ≥4 years of age with Prader-Willi syndrome.
Diazoxide choline may be confused with diazoxide.
Substrate of BCRP, CYP1A2 (Major with inhibitors), CYP1A2 (Minor with inducers), CYP3A4 (Major with inhibitors), CYP3A4 (Minor with inducers), OAT1/3; Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential;
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.
Antidiabetic Agents: Hyperglycemia-Associated Agents may decrease therapeutic effects of Antidiabetic Agents. Risk C: Monitor
Clofazimine: May increase serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor
CYP1A2 Inhibitors (Moderate): May increase serum concentration of Diazoxide Choline. Risk C: Monitor
CYP1A2 Inhibitors (Strong): May increase serum concentration of Diazoxide Choline. Risk D: Consider Therapy Modification
CYP1A2 Substrates (High risk with Inhibitors): Diazoxide Choline may increase serum concentration of CYP1A2 Substrates (High risk with Inhibitors). Risk X: Avoid
CYP3A4 Inhibitors (Moderate): May increase serum concentration of Diazoxide Choline. Risk C: Monitor
CYP3A4 Inhibitors (Strong): May increase serum concentration of Diazoxide Choline. Risk C: Monitor
Fosphenytoin-Phenytoin: Diazoxide Choline may increase serum concentration of Fosphenytoin-Phenytoin. Diazoxide Choline may decrease serum concentration of Fosphenytoin-Phenytoin. Risk C: Monitor
Fusidic Acid (Systemic): May increase serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Consider avoiding this combination if possible. If required, monitor patients closely for increased adverse effects of the CYP3A4 substrate. Risk D: Consider Therapy Modification
Grapefruit Juice: May increase serum concentration of Diazoxide Choline. Risk C: Monitor
Primaquine: May increase serum concentration of CYP1A2 Substrates (High risk with Inhibitors). Risk C: Monitor
RifAMPin: May decrease serum concentration of Diazoxide Choline. Risk X: Avoid
Thiazide and Thiazide-Like Diuretics: Diazoxide Choline may increase adverse/toxic effects of Thiazide and Thiazide-Like Diuretics. Specifically, the hyperglycemic and hyperuricemic effects may be increased. Risk C: Monitor
Vitamin K Antagonists: Diazoxide Choline may increase serum concentration of Vitamin K Antagonists. Diazoxide Choline may decrease serum concentration of Vitamin K Antagonists. Risk C: Monitor
Diazoxide crosses the placenta.
Outcome data following maternal use of diazoxide during pregnancy are limited. Altered carbohydrate metabolism, hyperbilirubinemia, and thrombocytopenia have been reported in the fetus or neonate. Alopecia and hypertrichosis lanuginosa have also been reported in infants following maternal use of diazoxide during the last 19 to 60 days of pregnancy.
Refer to the diazoxide monograph for additional information.
Diazoxide is present in human milk.
According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and the benefits of treatment to the mother. Refer to the diazoxide monograph for additional information.
Fasting blood/plasma glucose (baseline, then once weekly for the first 2 weeks [more frequently in patients at risk for hyperglycemia], then at least every 4 weeks thereafter and as clinically indicated); in patients treated with antihyperglycemic medications, monitor fasting glucose at least once weekly for 8 weeks and then once every 2 weeks and as clinically needed; HbA1c (baseline, then every 3 months and as clinically indicated); ketones (patients with worsening hyperglycemia); signs and symptoms of fluid overload.
In the treatment of hyperphagia in patients with Prader-Willi syndrome, the mechanism of action is unknown.
Distribution: Vd: ~44.9 L.
Protein binding: 91% to 93%; primarily albumin.
Metabolism: Primarily hepatic via CYP1A2 and to a minor extent by CYP3A4; 2 inactive metabolites are formed via oxidation or sulfate conjugation at the methyl group.
Half-life elimination: 28.7 to 32.4 hours (healthy patients); 106 hours (patients with Prader-Willi syndrome).
Time to peak: 8 hours (fed); 12 hours (fasted).
Excretion: Urine: 85% to 92% (~31% as unchanged drug); feces: ~2%.
