Dosing & Uses
Dosage Forms & Strengths
oral suspension
- 50mg/mL
Hypoglycemia
Indicated for hypoglycemia due to hyperinsulinism associated with inoperable islet cell adenoma or carcinoma, or extrapancreatic malignancy
3 mg/kg/day PO divided q8-12hr initially; typical dose range 3-8 mg/kg/day
Patients with refractory hypoglycemia may require higher doses
Prader-Willi Syndrome (Orphan)
Orphan designation for diazoxide choline for treatment of Prader-Willi Syndrome
Sponsor
- Essentialis, Inc; 7915 Corte Cardo; Carlsbad, CA 92009
Dosage Forms & Strengths
oral suspension
- 50mg/mL
Hypoglycemia
Indicated for hypoglycemia due to hyperinsulinism associated with leucine sensitivity, islet cell hyperplasia, nesidioblastosis, extrapancreatic malignancy, islet cell adenoma, or adenomatosis
Newborn/infant: 10 mg/kg/day PO divided q8hr initially; typical dosage range is 8-15 mg/kg/day PO divided q8-12hr (also see Cautions regarding suspected pulmonary hypertension in newborns and infants)
Children: 3 mg/kg/day PO divided q8hr initially; typical dose range is 3-8 mg/kg/day PO divided q8-12hr
Dosing Considerations
May be used preoperatively as a temporary measure, and postoperatively, if hypoglycemia persists
Prader-Willi Syndrome (Orphan)
Orphan designation for diazoxide choline in DDRC (crystalline salt of diazoxide in a controlled-release, once-a-day tablet formulation)
Orphan sponsor
- Essentialis Therapeutics, Inc; 7915 Corte Cardo; Carlsbad, CA 92009
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (0)
Serious - Use Alternative (0)
Monitor Closely (18)
- amifostine
amifostine, diazoxide. Either increases effects of the other by anti-hypertensive channel blocking. Use Caution/Monitor. Monitor blood pressure and adjust dose accordingly.
- atazanavir
atazanavir increases effects of diazoxide by Other (see comment). Use Caution/Monitor. Comment: Reports of hyperglycemia due to insulin resistance with protease inhibitors. .
- benazepril
diazoxide increases effects of benazepril by pharmacodynamic synergism. Use Caution/Monitor. Diazoxide may enhance the hypotensive effect of antihypertensive agents.
- captopril
diazoxide, captopril. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Both drugs lower blood pressure. Monitor blood pressure.
- darunavir
darunavir increases effects of diazoxide by Other (see comment). Use Caution/Monitor. Comment: Reports of hyperglycemia due to insulin resistance with protease inhibitors. .
- fosamprenavir
fosamprenavir increases effects of diazoxide by Other (see comment). Use Caution/Monitor. Comment: Reports of hyperglycemia due to insulin resistance with protease inhibitors. .
- hydrochlorothiazide
hydrochlorothiazide increases toxicity of diazoxide by unspecified interaction mechanism. Use Caution/Monitor. May enhance hyperglycemic effects of diazoxide.
- indinavir
indinavir increases effects of diazoxide by Other (see comment). Use Caution/Monitor. Comment: Reports of hyperglycemia due to insulin resistance with protease inhibitors. .
- insulin degludec
diazoxide decreases effects of insulin degludec by pharmacodynamic antagonism. Use Caution/Monitor. Diazoxide increases blood glucose by inhibiting pancreatic insulin release and stimulating catecholamines release.
- insulin degludec/insulin aspart
diazoxide decreases effects of insulin degludec/insulin aspart by pharmacodynamic antagonism. Use Caution/Monitor. Diazoxide increases blood glucose by inhibiting pancreatic insulin release and stimulating catecholamines release.
- insulin inhaled
diazoxide decreases effects of insulin inhaled by pharmacodynamic antagonism. Use Caution/Monitor. Diazoxide increases blood glucose by inhibiting pancreatic insulin release and stimulating catecholamines release.
- lopinavir
lopinavir increases effects of diazoxide by Other (see comment). Use Caution/Monitor. Comment: Reports of hyperglycemia due to insulin resistance with protease inhibitors. .
- metformin
diazoxide decreases effects of metformin by pharmacodynamic antagonism. Use Caution/Monitor.
- nelfinavir
nelfinavir increases effects of diazoxide by Other (see comment). Use Caution/Monitor. Comment: Reports of hyperglycemia due to insulin resistance with protease inhibitors. .
- ritonavir
ritonavir increases effects of diazoxide by Other (see comment). Use Caution/Monitor. Comment: Reports of hyperglycemia due to insulin resistance with protease inhibitors. .
- saquinavir
saquinavir increases effects of diazoxide by Other (see comment). Use Caution/Monitor. Comment: Reports of hyperglycemia due to insulin resistance with protease inhibitors. .
- tesamorelin
tesamorelin will decrease the level or effect of diazoxide by altering metabolism. Modify Therapy/Monitor Closely. Monitor glucose levels
- tipranavir
tipranavir increases effects of diazoxide by Other (see comment). Use Caution/Monitor. Comment: Reports of hyperglycemia due to insulin resistance with protease inhibitors. .
Minor (12)
- bendroflumethiazide
diazoxide, bendroflumethiazide. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Risk of hyperglycemia.
- chlorothiazide
diazoxide, chlorothiazide. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Risk of hyperglycemia.
- chlorthalidone
diazoxide, chlorthalidone. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Risk of hyperglycemia.
- cyclopenthiazide
diazoxide, cyclopenthiazide. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Risk of hyperglycemia.
- ethotoin
diazoxide decreases levels of ethotoin by increasing metabolism. Minor/Significance Unknown.
- fosphenytoin
diazoxide decreases levels of fosphenytoin by increasing metabolism. Minor/Significance Unknown.
- hydralazine
diazoxide, hydralazine. Either increases effects of the other by pharmacodynamic synergism. Minor/Significance Unknown. Additive hypotensive effects.
- hydrochlorothiazide
diazoxide, hydrochlorothiazide. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Risk of hyperglycemia.
- indapamide
diazoxide, indapamide. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Risk of hyperglycemia.
- methyclothiazide
diazoxide, methyclothiazide. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Risk of hyperglycemia.
- metolazone
diazoxide, metolazone. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Risk of hyperglycemia.
- phenytoin
diazoxide decreases levels of phenytoin by increasing metabolism. Minor/Significance Unknown.
Adverse Effects
Frequency Not Defined
Angina
Cardiac arrest
Anxiety
Fever
Polyneuritis
CHF
Hypotension
Palpitation
Tachycardia
Dizziness
Anorexia
Abdominal pain
Constipation
Diarrhea
Loss of taste
Nausea
Vomiting
Diabetic ketoacidosis
Hirsutism
Scalp hair loss
Hyperglycemia
Sodium and fluid retention
Postmarketing reports
Pulmonary hypertension in neonates and young infants
Warnings
Contraindications
Hypersensitivity to diazoxide, thiazides, or sulfonamide derivatives
Use for functional hypoglycemia
Cautions
Use caution in coronary or cerebral insufficiency, DM, extravasation, heart failure (may increase fluid retention), cardiovascular insufficiency, gout, hypotension, hypokalemia, liver disease, renal dysfunction
Development of abnormal facial features in four children treated chronically (>4 years) with this drug for hypoglycemia hyperinsulinism reported
Treatment with this drug should be initiated under close clinical supervision, with careful monitoring of blood glucose and clinical response until patient’s condition has stabilized; this usually requires several days; if not effective in two to three weeks, the drug should be discontinued
Compensatory HTN (aortic coarctation, arteriovenous shunt)
Ineffective in pheochromocytoma
Nonketotic hyperosmolar coma may occur during treatment; transient cataracts reported
May displace bilirubin from albumin; use caution in newborns with hyperbilirubinemia
The antidiuretic property of diazoxide may lead to significant fluid retention, which in patients with compromised cardiac reserve, may precipitate congestive heart failure; the fluid retention will respond to conventional therapy with diuretics
Concomitantly administered thiazides may potentiate the hyperglycemic and hyperuricemic actions of diazoxide
Ketoacidosis and nonketotic hyperosmolar coma reported in patients treated with recommended doses usually during intercurrent illness; prompt recognition and treatment essential and prolonged surveillance following the acute episode necessary because of long drug half-life of approximately 30 hours; occurrence of these serious events may be reduced by careful education of patients regarding monitoring urine for sugar and ketones and for prompt reporting of abnormal findings and unusual symptoms to healthcare provider
Prolonged treatment requires regular monitoring of urine for sugar and ketones, especially under stress conditions, with prompt reporting of any abnormalities to the physician; additionally, blood sugar levels should be monitored periodically by the physician to determine the need for dose adjustment
Effects of diazoxide on the hematopoietic system and the level of serum uric acid kept in mind; the latter should be considered particularly in patients with hyperuricemia or a history of gout
Antihypertensive effect of other drugs may be enhanced by diazoxide; should keep this in mind when administering it concomitantly with antihypertensive agents
Because of protein binding, administration of diazoxide with coumarin or its derivatives may require reduction in dosage of anticoagulants
In some patients, higher blood levels have been observed with oral suspension than with capsule formulation; dosage should be adjusted as necessary in individual patients if changed from one formulation to the other
Since plasma half-life is prolonged in patients with impaired renal function, a reduced dosage should be considered; serum electrolyte levels should also be evaluated for such patients
Pulmonary hypertension in newborns and infants
- July 16, 2015: FDA warns clinicians to watch for signs of pulmonary hypertension in infants treated for hypoglycemia with diazoxide and discontinue the drug if symptoms appear
- There have been 11 cases identified since the drug was approved (1973) and once diazoxide was discontinued, the symptoms resolved
- Signs of respiratory distress include flaring nostrils, grunting, unusual chest movements, rapid breathing, difficulty feeding, or a bluish tint to the lips or skin
- Monitoring is especially important for infants who have other risk factors for pulmonary hypertension (eg, meconium aspiration syndrome, respiratory distress syndrome, transient tachypnea of the newborn, pneumonia, sepsis, congenital diaphragmatic hernia, and congenital heart disease)
Drug interaction overview
- Since this drug is highly bound to serum proteins, it may displace other substances which are also bound to protein, such as bilirubin or coumarin and its derivatives, resulting in higher blood levels of these substances
- Concomitant administration of oral diazoxide and diphenylhydantoin may result in a loss of seizure control; these potential interactions must be considered when administering therapy; the concomitant administration of thiazides or other commonly used diuretics may potentiate hyperglycemic and hyperuricemic effects of diazoxide
Pregnancy & Lactation
Pregnancy
Safety in pregnancy has not been established; there are no adequate data on fetal effects of this drug when given to pregnant women
When use of this drug is considered, the indications should be limited to those approved for this drug, and the potential benefits to the mother must be weighed against possible harmful effects to the fetus
This drug crosses the placental barrier and appears in cord blood; when given to mother prior to delivery of infant, the drug may produce fetal or neonatal hyperbilirubinemia, thrombocytopenia, altered carbohydrate metabolism, and possibly other side effects have occurred in adults
Alopecia and hypertrichosis lanuginosa reported in infants whose mothers received oral diazoxide during last 19 to 60 days of pregnancy
Labor and delivery
- Since intravenous administration of the drug during labor may cause cessation of uterine contractions, and administration of oxytocic agents may be required to reinstate labor, caution is advised in administering therapy at that time.
Animal data
- Reproduction studies using oral preparation in rats have revealed increased fetal resorptions and delayed parturition, as well as fetal skeletal anomalies; evidence of skeletal and cardiac teratogenic effects in rabbits has been noted with intravenous administration
- The drug has also been demonstrated to cross the placental barrier in animals and to cause degeneration of fetal pancreatic beta cells
Lactation
Information is not available concerning passage of diazoxide in breast milk; because many drugs are excreted in human milk and because of the potential for adverse reactions from diazoxide in nursing infants, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Inhibits pancreatic insulin release resulting increased blood glucose; activates potassium channels
Relaxes smooth muscle to decrease PVR, increases HR & CO; precise mechanism of hypotensive effect not fully elucidated; antagonism of calcium may be involved
Pharmacokinetics
Half-Life: 9-24 hr (children); 24-36 hr (adults), increases in patients with renal impairment
Duration: varies greatly, may last to 3-12 hr
Protein binding: 90%
Metabolism: In liver by oxidation and sulfate conjugation
Renal Clearance: 4-5 mL/min
Excretion: urine by glomerular filtration as unchanged drug and metabolites
Dialyzable: HD: yes, PD: yes; no supplemental dose is required
Excretion: Urine
Images
| BRAND | FORM. | UNIT PRICE | PILL IMAGE |
|---|---|---|---|
| Proglycem oral - | 50 mg/mL suspension |  | |
| diazoxide oral - | 50 mg/mL suspension |  | |
| diazoxide oral - | 50 mg/mL suspension |  |
Copyright © 2010 First DataBank, Inc.
Patient Handout
diazoxide oral
DIAZOXIDE - ORAL
(dye-uh-ZOX-ide)
COMMON BRAND NAME(S): Proglycem
USES: This medication is used to treat very low blood sugar (hypoglycemia). Certain conditions (such as tumor on the pancreas, cancer, leucine sensitivity) can cause the release of too much insulin. Insulin is a natural substance that lowers blood sugar. This drug works by preventing insulin release from the pancreas, helping to return the blood sugar to normal levels. Diazoxide is a thiazide drug, but has no diuretic ("water pill") effects like other thiazides.Diazoxide should not be used to treat low blood sugar from poor nutrition/diet (functional hypoglycemia).
HOW TO USE: Take this medication by mouth as directed by your doctor, usually 2 to 3 times daily (every 8 to 12 hours). Your doctor may direct you to follow a special diet for your condition. Consult your doctor, pharmacist, or dietician for more details.Do not switch between the capsule and suspension form of this medication without talking with your doctor first. Your dose may need to be adjusted. If you are using the suspension, shake the bottle thoroughly before each dose. Carefully measure the dose using a special measuring device/spoon. Do not use a household spoon because you may not get the correct dose. Do not use the suspension if it has turned a dark color. Discard it. (See Storage section.)The dosage is based on your weight, medical condition, and response to treatment. You will need to check your blood sugar and check your urine for sugar and ketones regularly as directed and share the results with your doctor. Your doctor will adjust the dose based on these tests. Your doctor may change your dose often when you first start taking the drug to find the best dose for you. Follow your doctor's directions carefully.Use this medication regularly to get the most benefit from it. To help you remember, take it at the same times each day.Tell your doctor if your condition lasts or gets worse after 2 to 3 weeks.
SIDE EFFECTS: Nausea, loss of appetite, stomach upset, and changes in sense of taste may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.Abnormal growth of body hair, especially on the forehead/back/arms/legs, may occur. This is usually not permanent and will go away when the drug is stopped.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.This medication can cause sodium and water retention which can cause serious heart problems. Tell your doctor right away if any of these serious side effects occur: swelling of arms/legs/hands/feet, unexplained weight gain, shortness of breath, unusual tiredness.This medication may cause your blood sugar to become too high. Checking your blood sugar and urine for sugar/ketones regularly and telling your doctor the results will help prevent this side effect. High blood sugar can be very serious and worsen quickly. Tell your doctor right away if any of these signs of very high blood sugar occur: need to urinate more often, unusual thirst, fruity breath odor, dizziness, unusual weight loss, deep/rapid breathing, bluish color of lips/skin, extreme drowsiness/confusion, weakness.Tell your doctor right away if you have any serious side effects, including: easy bruising/bleeding, fainting, fast/pounding heartbeat, face/muscle twitching, toe/joint pain, unusual restlessness, muscle cramps/stiffness, shaking (tremor).A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.
PRECAUTIONS: Before taking diazoxide, tell your doctor or pharmacist if you are allergic to it; or to other thiazides (such as hydrochlorothiazide); or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: low blood minerals (low potassium blood levels), diabetes, heart disease (such as heart failure, past heart attack), kidney disease, gout, liver disease.The suspension (liquid) form of this medication contains alcohol. Caution is advised if you have diabetes, liver disease, or any other condition that requires you to limit/avoid alcohol in your diet. Ask your doctor or pharmacist about using this product safely.This medication may raise your blood sugar too high under certain conditions. For example, your body may need more insulin while you are under stress due to infection, surgery, or injury. Certain medications (such as corticosteroids like hydrocortisone/prednisone, hormones such as birth control pills) may raise your blood sugar. Your dose may need to be adjusted. Consult your doctor for more details. Tell your doctor right away if any signs of high blood sugar occur (see Side Effects section).Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor. If you become pregnant, think you may be pregnant, or plan to become pregnant, tell your doctor right away.It is unknown if this drug passes into breast milk. Consult your doctor before breast-feeding.
DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.Some products that may interact with this drug include: drugs for high blood pressure (such as enalapril, methyldopa, prazosin), "blood thinners" (such as warfarin), phenytoin.This medication may interfere with certain lab tests (such as a glucagon test), possibly causing false test results. Make sure lab personnel and all your doctors know you use this drug.
OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center. Symptoms of overdose may include: need to urinate more often, unusual thirst, fruity breath odor.
NOTES: Do not share this medication with others.For best results, this medication should be used along with a doctor-approved diet plan. Consult your doctor for more details.Lab and/or medical tests (such as blood sugar, urine sugar/ketones, kidney function, complete blood count, potassium/uric acid levels) should be done while you are taking this medication. Keep all medical and lab appointments. Consult your doctor for more details.
MISSED DOSE: If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.
STORAGE: Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.
Information last revised July 2023. Copyright(c) 2023 First Databank, Inc.
IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.
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