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Vykat XR
diazoxide choline
Adult Dosing .
Dosage forms: ER TAB: 25 mg, 75 mg, 150 mg
hyperphagia, Prader-Willi syndrome-associated
- [40-64 kg]
- Dose: 225 mg PO qd; Start: 75 mg PO qd x2wk, then 150 mg PO qd x2wk; Max: 5.8 mg/kg/day up to 525 mg/day; Info: if elevated fasting glucose, HbA1c or fluid overload, may interrupt tx or decr. dose, then incr. by up to 75 mg/day no more frequently than q2wk; retitrate if tx interrupted >7 days; do not cut/crush/chew tab
- [65-99 kg]
- Dose: 375 mg PO qd; Start: 150 mg PO qd x2wk, then 225 mg PO qd x2wk, then 300 mg PO qd x2wk; Max: 5.8 mg/kg/day up to 525 mg/day; Info: if elevated fasting glucose, HbA1c or fluid overload, may interrupt tx or decr. dose, then incr. by up to 75 mg/day no more frequently than q2wk; retitrate if tx interrupted >7 days; do not cut/crush/chew tab
- [100-134 kg]
- Dose: 450 mg PO qd; Start: 150 mg PO qd x2wk, then 300 mg PO qd x2wk, then 375 mg PO qd x2wk; Max: 5.8 mg/kg/day up to 525 mg/day; Info: if elevated fasting glucose, HbA1c or fluid overload, may interrupt tx or decr. dose, then incr. by up to 75 mg/day no more frequently than q2wk; retitrate if tx interrupted >7 days; do not cut/crush/chew tab
- [>135 kg]
- Dose: 525 mg PO qd; Start: 150 mg PO qd x2wk, then 300 mg PO qd x2wk, then 450 mg PO qd x2wk; Max: 5.8 mg/kg/day up to 525 mg/day; Info: if elevated fasting glucose, HbA1c or fluid overload, may interrupt tx or decr. dose, then incr. by up to 75 mg/day no more frequently than q2wk; retitrate if tx interrupted >7 days; do not cut/crush/chew tab
renal dosing
- [not defined]
- renal impairment: not defined
- HD/PD: not defined
hepatic dosing
- [not defined]
Peds Dosing .
- Dosage forms: ER TAB: 25 mg, 75 mg, 150 mg
hyperphagia, Prader-Willi syndrome-associated
- [4 yo and older, 20-29 kg]
- Dose: 100 mg PO qd; Start: 25 mg PO qd x2wk, then 50 mg PO qd x2wk, then 75 mg PO qd x2wk; Max: 5.8 mg/kg/day up to 525 mg/day; Info: if elevated fasting glucose, HbA1c or fluid overload, may interrupt tx or decr. dose, then incr. by up to 25 mg/day no more frequently than q2wk; retitrate if tx interrupted >7 days; do not cut/crush/chew tab
- [4 yo and older, 30-39 kg]
- Dose: 150 mg PO qd; Start: 75 mg PO qd x2wk; Max: 5.8 mg/kg/day up to 525 mg/day; Info: if elevated fasting glucose, HbA1c or fluid overload, may interrupt tx or decr. dose, then incr. by up to 75 mg/day no more frequently than q2wk; retitrate if tx interrupted >7 days; do not cut/crush/chew tab
- [4 yo and older, 40-64 kg]
- Dose: 225 mg PO qd; Start: 75 mg PO qd x2wk, then 150 mg PO qd x2wk; Max: 5.8 mg/kg/day up to 525 mg/day; Info: if elevated fasting glucose, HbA1c or fluid overload, may interrupt tx or decr. dose, then incr. by up to 75 mg/day no more frequently than q2wk; retitrate if tx interrupted >7 days; do not cut/crush/chew tab
- [4 yo and older, 65-99 kg]
- Dose: 375 mg PO qd; Start: 150 mg PO qd x2wk, then 225 mg PO qd x2wk, then 300 mg PO qd x2wk; Max: 5.8 mg/kg/day up to 525 mg/day; Info: if elevated fasting glucose, HbA1c or fluid overload, may interrupt tx or decr. dose, then incr. by up to 75 mg/day no more frequently than q2wk; retitrate if tx interrupted >7 days; do not cut/crush/chew tab
- [4 yo and older, 100-134 kg]
- Dose: 450 mg PO qd; Start: 150 mg PO qd x2wk, then 300 mg PO qd x2wk, then 375 mg PO qd x2wk; Max: 5.8 mg/kg/day up to 525 mg/day; Info: if elevated fasting glucose, HbA1c or fluid overload, may interrupt tx or decr. dose, then incr. by up to 75 mg/day no more frequently than q2wk; retitrate if tx interrupted >7 days; do not cut/crush/chew tab
- [4 yo and older, >135 kg]
- Dose: 525 mg PO qd; Start: 150 mg PO qd x2wk, then 300 mg PO qd x2wk, then 450 mg PO qd x2wk; Max: 5.8 mg/kg/day up to 525 mg/day; Info: if elevated fasting glucose, HbA1c or fluid overload, may interrupt tx or decr. dose, then incr. by up to 75 mg/day no more frequently than q2wk; retitrate if tx interrupted >7 days; do not cut/crush/chew tab
renal dosing
- [not defined]
- renal impairment: not defined
- HD/PD: not defined
hepatic impairment
- [not defined]
Contraindications / Cautions .
- hypersensitivity to drug or ingredient
- hypersensitivity to thiazides
- caution: hypersensitivity to sulfonamides
- caution: illness
- caution: surgery
- caution: volume depletion
- caution: alcohol abuse
- caution: hyperglycemia risk
- caution: cardiac reserve, compromised
- caution: labor and delivery
Drug Interactions .
Overview
diazoxide
antihypoglycemic agent; nondiuretic benzothiadiazine
- CYP1A2 substrate
- CYP3A4 substrate
- CYP1A2 inhibitor, weak
- hyperglycemic effects
- hypernatremia
- hyperuricemic effects
- hypotensive effects
Contraindicated
- disulfiram
- fezolinetant
Avoid/Use Alternative
- apalutamide
- bosentan
- butalbital
- carbamazepine
- cenobamate
- dabrafenib
- efavirenz
- encorafenib
- enzalutamide
- etravirine
- fexinidazole
- fosphenytoin
- ivosidenib
- leflunomide
- lopinavir/ritonavir
- lorlatinib
- lumacaftor/ivacaftor
- mavacamten
- metronidazole
- mitapivat
- mitotane
- modafinil
- nafcillin
- pacritinib
- pentobarbital
- pexidartinib
- phenobarbital
- phenytoin
- primidone
- repotrectinib
- rifabutin
- rifampin
- rifapentine
- ritonavir
- sotorasib
- St. John's wort
- teriflunomide
- tinidazole
- tizanidine
Monitor/Modify Tx
- acarbose
- acebutolol
- adagrasib
- aliskiren
- allopurinol
- alogliptin
- amiloride
- aminophylline
- amlodipine
- aprocitentan
- atazanavir
- atenolol
- azilsartan medoxomil
- benazepril
- bendamustine
- betaxolol
- bexagliflozin
- bisoprolol
- bromocriptine
- bumetanide
- caffeine citrate
- canagliflozin
- candesartan cilexetil
- captopril
- carvedilol
- ceritinib
- chloramphenicol
- chlorothiazide
- chlorthalidone
- ciprofloxacin
- clarithromycin
- clevidipine
- clozapine
- cobicistat
- colesevelam
- dapagliflozin
- diltiazem
- doxazosin
- dulaglutide
- empagliflozin
- enalapril
- enalaprilat
- enasidenib
- eplerenone
- ertugliflozin
- esmolol
- ethacrynic acid
- exenatide
- febuxostat
- felodipine
- fenoldopam
- fluvoxamine
- fosinopril
- furosemide
- glimepiride
- glipizide
- glyburide
- hydralazine
- hydrochlorothiazide
- idelalisib
- indapamide
- insulin
- irbesartan
- isradipine
- itraconazole
- ketoconazole
- labetalol
- levoketoconazole
- linagliptin
- liraglutide
- lisinopril
- lonafarnib
- losartan
- metformin
- methyldopa
- metolazone
- metoprolol
- mifepristone
- miglitol
- minoxidil
- moexipril
- nadolol
- nateglinide
- nebivolol
- nefazodone
- nelfinavir
- nicardipine
- nifedipine
- nimodipine
- nisoldipine
- olmesartan medoxomil
- pegloticase
- perindopril
- phenoxybenzamine
- phentolamine
- pindolol
- pioglitazone
- posaconazole
- pramlintide
- prazosin
- probenecid
- propranolol
- quinapril
- ramipril
- rasburicase
- repaglinide
- ribociclib
- rosiglitazone
- saxagliptin
- semaglutide
- sitagliptin
- sodium acid phosphate
- spironolactone
- telmisartan
- terazosin
- theophylline
- timolol
- tipranavir
- tirzepatide
- torsemide
- trandolapril
- triamterene
- tucatinib
- valsartan
- verapamil
- viloxazine
- voriconazole
- warfarin
Caution Advised
- alosetron
- pirfenidone
- raloxifene
- roflumilast
- roflumilast topical
- vorasidenib
Adverse Reactions .
Serious Reactions
- hypersensitivity rxn
- erythema multiforme
- hyperglycemia
- diabetic ketoacidosis
- fluid overload
- pulmonary edema
Common Reactions
- hypertrichosis
- edema
- hyperglycemia
- rash
- fever
- arthralgia
- respiratory infection
- weight incr.
- affect lability
- hirsutism
- uric acid incr.
Safety/Monitoring .
Monitoring Parameters
fasting glucose before tx start, then at least qwk x2wk or more frequently if hyperglycemia risk, then at least q4wk; HbA1c before tx start, then q3mo; fluid status; consider ketones if ketoacidosis risk
Look/Sound-Alike Drug Names
diazoxide confused with: Diamox
Pregnancy/Lactation .
Pregnancy
Clinical Summary
weigh risk/benefit during pregnancy, esp. in 3rd trimester; inadequate human data available; no known risk of teratogenicity based on animal data at 0.3-1.2x MRHD, though possible risk of fetal or neonatal hyperbilirubinemia, thrombocytopenia, and altered carbohydrate metabolism based on drug's mechanism of action
Lactation
Clinical Summary
weigh risk/benefit while breastfeeding; inadequate human data available to assess risk of infant harm, though drug excreted into milk; no human data available to assess effects on milk production
Pharmacology .
Metabolism: oxidation, sulfate conjugation; CYP450: 1A2 (primary), 3A4 substrate
Excretion: urine 85-92% (31% unchanged), feces 2%; Half-life: 106h
Subclass: Inherited Metabolic Disorders
Mechanism of Action
exact mechanism of action unknown; decr. neuropeptide Y and Agouti-related protein release, reducing hyperphagia (adenosine triphosphate-sensitive potassium channel activator)
Formulary .
No Formulary Selected
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