Version July 2025
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).
(For additional information see "Diazoxide choline: Drug information")
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).
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 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.
Oral: Administer with or without food. Swallow tablet whole; do not chew, crush, or split.
Store at 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°F). Protect from humidity. Do not remove desiccant.
Treatment of hyperphagia in patients with Prader-Willi syndrome (FDA approved in ages ≥4 years and adults).
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.
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
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.
Prior to treatment: Fasting blood glucose, HbA1c.
During treatment: Fasting blood glucose (once weekly for first 2 weeks, then at least once every 4 weeks, and as clinically indicated; more frequently in the first few weeks is recommended in patients with risk factors for hyperglycemia), HbA1c (every 3 months and as clinically indicated), signs and symptoms of diabetic ketoacidosis (DKA), fluid status, signs and symptoms of edema and 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%.
