What are the risks of diazoxide treatment in children with congenital hyperinsulinism. How can severe thrombocytopenia be detected and managed as a side effect of diazoxide therapy. Why is monitoring platelet counts crucial during diazoxide treatment in pediatric patients.

Understanding Congenital Hyperinsulinism and Its Treatment

Congenital hyperinsulinism is a rare genetic disorder characterized by excessive insulin secretion, leading to recurrent episodes of hypoglycemia in infants and children. The condition can be life-threatening if left untreated, making proper management crucial.

Diazoxide, often combined with hydrochlorothiazide (HCT), is the first-line treatment for congenital hyperinsulinism. This medication works by inhibiting insulin release from pancreatic beta cells, helping to maintain normal blood glucose levels. However, as with any medication, diazoxide can cause side effects, some of which can be severe and require careful monitoring.

Case Study: A 2.5-Year-Old Boy with Recurrent Hypoglycemia

The case report discusses a 2.5-year-old boy with a history of transient congenital hyperinsulinism who was admitted to the pediatric ward due to recurrent hypoglycemia. Initially treated with diazoxide and HCT as a neonate, the child experienced a relapse of his condition, necessitating the reintroduction of medication.

The treatment regimen began with diazoxide at 5 mg/kg/day and HCT at 2 mg/kg/day. After eight days, the diazoxide dose was increased to 10 mg/kg/day to achieve better glucose control. While this adjustment initially appeared effective, it led to unexpected and severe complications.

Onset of Severe Thrombocytopenia: A Serious Side Effect

Three days after increasing the diazoxide dose, the child developed alarming symptoms:

• Mild rectal bleeding
• Petechiae (small, round, purple spots on the skin)
• Epistaxis (nosebleeds)
• Hematemesis (vomiting blood)

Laboratory investigations revealed severe thrombocytopenia, with platelet counts ranging from 5 to 8×10^9/L on repeated measurements. This dramatic decrease in platelet count posed a significant risk of spontaneous bleeding and other complications.

Can thrombocytopenia be a side effect of diazoxide treatment?

Yes, thrombocytopenia can indeed be a side effect of diazoxide treatment. Although it is not commonly observed, several case reports have documented this serious complication. The mechanism is believed to be drug-induced immune thrombocytopenia, where the medication triggers an immune response against platelets.

Diagnostic Approach and Management of Drug-Induced Thrombocytopenia

Upon suspicion of drug-induced thrombocytopenia, the medical team took the following steps:

1. Immediate discontinuation of diazoxide and HCT
2. Reintroduction of continuous nasogastric tube feeding to maintain glucose levels
3. Close monitoring of platelet counts
4. Consideration of drug rechallenge to confirm the diagnosis

Within seven days of stopping the medications, the child’s platelet count normalized to 236×10^9/L. To definitively identify the cause, a drug rechallenge was performed.

How is drug-induced thrombocytopenia diagnosed?

Drug-induced thrombocytopenia is typically diagnosed through a combination of clinical presentation, laboratory findings, and response to drug withdrawal. A drug rechallenge, while potentially risky, can provide conclusive evidence of the causative agent. In this case, reintroduction of both diazoxide and HCT led to a rapid decline in platelet count within three days, confirming the diagnosis.

Identifying the Culprit: Diazoxide vs. Hydrochlorothiazide

To determine whether diazoxide or HCT was primarily responsible for the thrombocytopenia, the medical team conducted a targeted investigation:

• HCT was discontinued
• Diazoxide was continued in combination with alternative diuretics (furosemide and spironolactone)
• Platelet counts were closely monitored

This approach resulted in a stable but mild thrombocytopenia (83×10^9/L) after four days. Upon discontinuation of all medications, including diazoxide, the platelet count rapidly normalized to 227×10^9/L.

Which medication was primarily responsible for the thrombocytopenia?

The investigation revealed that diazoxide was the primary cause of thrombocytopenia in this case. However, the combination of diazoxide and HCT appeared to have an augmented effect on platelet counts, suggesting a potential interaction between the two medications in inducing this side effect.

Historical Context and Underrecognition of Diazoxide-Induced Thrombocytopenia

Interestingly, severe thrombocytopenia as a side effect of diazoxide was first described in medical literature as early as 1967. Despite this long-standing knowledge, routine monitoring of platelet counts during diazoxide therapy has not been widely adopted in clinical practice.

This case highlights the importance of revisiting and implementing safety measures based on historical data, especially when dealing with potentially life-threatening side effects of commonly used medications.

Implications for Clinical Practice: The Need for Platelet Monitoring

The case report emphasizes the critical need for regular platelet count monitoring in children receiving diazoxide therapy for congenital hyperinsulinism. This practice is not currently part of standard care protocols, which may lead to underdiagnosis of this serious side effect.

How often should platelet counts be monitored during diazoxide treatment?

While there are no universally established guidelines, this case suggests that regular monitoring of platelet counts should be implemented. A reasonable approach might include:

• Baseline platelet count before initiating diazoxide therapy
• Weekly monitoring during the first month of treatment
• Monthly monitoring thereafter
• Immediate testing if any signs of bleeding or bruising occur

The frequency of monitoring may need to be adjusted based on individual patient factors and clinical response.

Balancing Benefits and Risks in Congenital Hyperinsulinism Treatment

Treating congenital hyperinsulinism presents a delicate balance between managing potentially life-threatening hypoglycemia and mitigating the risks of medication side effects. Diazoxide remains a valuable tool in the management of this condition, but its use must be accompanied by vigilant monitoring and patient education.

What alternative treatments are available for congenital hyperinsulinism?

While diazoxide is the first-line treatment, alternative options for managing congenital hyperinsulinism include:

• Octreotide: A somatostatin analog that inhibits insulin secretion
• Glucagon: Used for acute management of hypoglycemia
• Nifedipine: A calcium channel blocker that may help in some cases
• Surgical interventions: Such as partial pancreatectomy in severe cases unresponsive to medical management
• Continuous glucose monitoring and frequent feeding: As supportive measures

The choice of treatment depends on the severity of the condition, genetic factors, and individual patient response.

Future Directions: Improving Safety in Pediatric Pharmacotherapy

This case report serves as a reminder of the importance of post-marketing surveillance and ongoing evaluation of medication safety profiles, particularly in pediatric populations. It highlights several areas for potential improvement in clinical practice and research:

• Development of standardized monitoring protocols for diazoxide therapy
• Investigation into the mechanisms of diazoxide-induced thrombocytopenia
• Exploration of potential genetic factors that may predispose certain patients to this side effect
• Creation of a centralized registry for adverse events related to diazoxide and other treatments for congenital hyperinsulinism

By addressing these areas, healthcare providers can work towards optimizing the safety and efficacy of treatments for children with congenital hyperinsulinism.

How can healthcare systems improve medication safety for pediatric patients?

Enhancing medication safety for pediatric patients requires a multifaceted approach:

1. Implementing robust pharmacovigilance systems specifically designed for pediatric populations
2. Encouraging reporting of adverse events and near-misses through user-friendly platforms
3. Conducting long-term follow-up studies on children receiving chronic medications
4. Developing age-specific dosing guidelines and formulations for pediatric use
5. Providing comprehensive education to healthcare providers on potential drug side effects in children
6. Engaging families and caregivers in medication safety practices and symptom recognition

By adopting these strategies, healthcare systems can work towards minimizing the risks associated with pediatric pharmacotherapy while maximizing treatment benefits.

In conclusion, this case report of severe thrombocytopenia in a child treated with diazoxide for congenital hyperinsulinism underscores the critical importance of vigilant monitoring for medication side effects in pediatric patients. It serves as a call to action for healthcare providers to implement regular platelet count checks during diazoxide therapy and to maintain a high index of suspicion for drug-induced thrombocytopenia. By balancing effective treatment with careful monitoring and prompt recognition of adverse effects, clinicians can optimize outcomes for children with congenital hyperinsulinism and other complex medical conditions requiring long-term pharmacotherapy.

Case report: Thrombocytopaenia: a serious side effect of diazoxide

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• BMJ Case Rep
• PMC6738727

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BMJ Case Rep. 2019; 12(9): e231222.

Published online 2019 Sep 11. doi: 10.1136/bcr-2019-231222

Case report

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A 2.5-year-old boy with a history of (transient) congenital hyperinsulinism was admitted to the paediatric ward with recurrent hypoglycaemia. Diazoxide 5 mg/kg/day and hydrochlorothiazide 2 mg/kg/day were initiated. After increasing the dose of diazoxide to 10 mg/kg/day, the child developed mild rectal bleeding, petechiae, epistaxis and haematemesis. Blood screening showed severe thrombocytopaenia. Diazoxide and hydrochlorothiazide were stopped, and his platelet count normalised. Drug rechallenge was positive. Drug-induced immune thrombocytopaenia was diagnosed.

Keywords: Paediatrics, Pharmacology And Therapeutics, Haematology (incl Blood Transfusion), Endocrinology

Diazoxide and hydrochlorothiazide (HCT) are the first choice of treatment for congenital hyperinsulinism and are used often. Although thrombocytopaenia is a known side effect, it is not standard care to check platelet count before or during diazoxide and/or HCT therapy. This case report will show the need to check platelet count during diazoxide and HCT therapy in every child.

A 2.5-year-old boy was admitted to our paediatric ward because of recurrent hypoglycaemia. His medical history reported neonatal congenital hyperinsulinism. He was treated with diazoxide and HCT for 2 weeks (maximum dose of 10 and 3 mg/kg/day, respectively).

During the present admission, a relapse of his congenital hyperinsulinism was shown (glucose 2.9 mmol/L, C-peptide 0.58 nmol/L (0.18–0.63 nmol/L), insulin 48 pmol/L and ketone bodies 0.1 mmol/L).¹ Laboratory testing did not reveal growth hormone deficiency, hypocortisolism or abnormalities directing towards metabolic causes. DNA analyses did not show any of the currently known gene mutations related to congenital hyperinsulinism (ABCC8, KCJN11, HADH, HNF1A, HNF4A, GCK and GLUT1). Because of the recurrent hypoglycaemia due to the congenital hyperinsulinism, he was started on diazoxide 5 mg/kg/day and HCT 2 mg/kg/day orally. As continuous nasogastric tube feeding remained necessary for maintaining normoglycaemia, the dose of diazoxide was increased to 10 mg/kg/day after 8 days. This appeared effective for his glucose maintenance and the continuous feeding was switched to feeding by frequent portions. However, 3 days after elevating the dose of diazoxide, the child developed mild rectal bleeding, petechiae, epistaxis and haematemesis.

Laboratory investigations showed severe thrombocytopaenia (platelet count on repeated measurements 5–8×10⁹/L) without anaemia and neutropenia. As drug-induced immune thrombocytopaenia had been described after exposure to diazoxide and HCT in some case reports, the possibility of drug-induced immune thrombocytopaenia was considered.^1–4 Diazoxide and HCT were stopped and feeding by nasogastric tube continuously was restarted. His platelet count normalised within 7 days (236×10⁹/L) (). Because rapid testing for platelet reactive antibodies was not available in our hospital, he was re-challenged with both diazoxide and HCT. Both drugs were restarted in the previous dosage and again resulted in thrombocytopaenia within 3 days (78×10⁹/L).

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Platelet count during diazoxide and hydrochlorothiazide therapy.

To investigate whether the thrombocytopaenia was related to either diazoxide or HCT, HCT was stopped, and diazoxide was continued in combination with furosemide and spironolactone. This resulted in stable but mild thrombocytopaenia 4 days later (83×10⁹/L). After discontinuation of diazoxide (as well as furosemide and spironolactone), platelet count rapidly normalised (227×10⁹/L) (). This indicates that there was an augmented effect of the combination of diazoxide and HCT.

Diazoxide is the first choice of treatment for congenital hyperinsulinism.⁵ Known common side effects include hirsutism and fluid retention.⁵ Although severe thrombocytopaenia with increased bleeding tendency was already described as a side effect of diazoxide in 1967, measurement of platelet count after the start of this drug is not part of routine clinical care.² Consequently, in this case, the severe increased bleeding tendency was the presenting symptom of the thrombocytopaenia due to drug-induced immune thrombocytopaenia.

Non-heparin drug-induced thrombocytopaenia is classified as either immune-mediated or non-immune mediated. Immune-mediated reactions lead to platelet destruction due to antibody formation.⁶ This typically occurs approximately 1 or 2 weeks after starting a new drug, and is characterised by a rapid, severe, decrease in platelet count and increased bleeding tendency.⁶ Positive in vitro testing for the presence of platelet reactive antibodies or a relapse of the thrombocytopaenia due to a drug re-challenge after initial recovery of the platelet count when drugs were stopped, confirm the diagnosis drug-induced immune thrombocytopaenia.^{2 6}

One should consider the possibility of an interaction of the combination of drugs and consequently more severe drug-induced immune thrombocytopaenia, in case multiple drugs are used. The treatment is to discontinue the suspected causative drug(s).⁶

In conclusion, this boy suffered from thrombocytopaenia as a rare side effect of the combination of diazoxide and HCT.

The recent publication of Herrera et al showed thrombocytopaenia as an adverse event in using diazoxide as treatment for congenital hyperinsulinism.⁴ This is the first case report that describes that the simultaneous usage of diazoxide and HCT results in more severe thrombocytopaenia in childhood. To prevent thrombocytopaenia, we suggest routine control of platelet count before start and 5 and 10 days after initiation of both drugs and after increasing the dosages of the drugs. This may help to prevent severe thrombocytopaenia and the associated increased bleeding tendency. Besides, it may prevent a lot of investigations for other diseases in the differential diagnosis of increased bleeding tendency of the neonate such as necrotising enterocolitis. Moreover, it prevents that intravenous glucose is needed again when platelet count is too low for the regular nasogastric feeding tube change.

Learning points

• Thrombocytopaenia is a dangerous side effect when using diazoxide and can cause increased bleeding tendency.

• Platelet count should be measured before the start of diazoxide, 5 and 10 days after the start, and after increasing the dosage.

• In the case of drug-induced thrombocytopaenia, withdrawal of diazoxide will normalise thrombocyte levels.

KAT and WJB contributed equally.

Contributors: KAT: selected the patient and contributed to writing the manuscript. WJB contributed to writing the manuscript. JCvdH contributed to patient selection and supervised writing of the manuscript.

Funding: The authors have not declared a specific grant for this research from any funding agency in the public, commercial or not-for-profit sectors.

Competing interests: None declared.

Provenance and peer review: Not commissioned; externally peer reviewed.

Patient consent for publication: Parental/guardian consent obtained.

1.
Combs JT, Grunt JA, Brandt IK.
Hematologic reactions to diazoxide. Pediatrics
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2.
Adachi J, Mimura M, Minami I, et al..
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Wales J, Wolff F.
Hematological side-effects of diazoxide. Lancet
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Herrera A, Vajravelu ME, Givler S, et al..
Prevalence of adverse events in children with congenital hyperinsulinism treated with diazoxide. J Clin Endocrinol Metab
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Arnold DM, Kukaswadia S, Nazi I, et al. .
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Articles from BMJ Case Reports are provided here courtesy of BMJ Publishing Group

Diazoxide and chlorothiazide suspensions | Great Ormond Street Hospital

Diazoxide is used to treat persistently low blood sugar levels (hypoglycaemia) caused by the body producing too much insulin (hyperinsulinism). Chlorothiazide is a diuretic, that is, a medicine that increases the amount of urine produced by the kidneys. This page from Great Ormond Street Hospital (GOSH) describes diazoxide and chlorothiazide, which are usually prescribed together. It explains how they are given and some of their side effects. Each person reacts differently to medicines so your child will not necessarily suffer every side effect mentioned. Diazoxide works by blocking the release of insulin by the body. Chlorothiazide is used in conditions where the body retains too much fluid, causing puffiness (oedema) especially around the eyes or affecting the hands or feet. Chlorothiazide is commonly prescribed alongside diazoxide, as a side effect of this medicine is fluid retention.

How are they given?

Diazoxide is given by mouth two or three times a day. Chlorothiazide is usually given twice a day.

Both are available as a suspension (liquid medicine). For guidance on how to give your child liquid medicines, please read our information sheet or watch our video podcast available on our websiteor the GOSH YouTube™ channel.

Diazoxide and chlorothiazide suspensions are not readily available from your community pharmacy. Neither medicine is available in the UK and so has to be imported from abroad by a licensed pharmaceutical import company. Supplies of these medicines may take longer than usual to obtain, usually several days.

Currently, the Pharmacy department at GOSH obtains diazoxide suspension under the brand name of Proglycem®. The packaging gives the strength of the medicine as 50mg of active ingredient in 1ml of suspension, which is equivalent to 250mg in 5ml. It also contains preservatives, colouring, flavourings and sweetener.

There have been incidents when the wrong strength of other types of medicine have been prescribed so please check the label before giving it your child. If you are given the wrong strength of diazoxide, please inform the team immediately and do not give to your child.

Chlorothiazide suspension is supplied at GOSH in the strength of 250mg of active ingredient in 5ml of suspension. It also contains preservatives, colouring, flavourings and sweetener.

Older children may prefer to take diazoxide and chlorothiazide in tablet or capsule form. Talk to your doctor about this.

Who should not take these medicines?

People with the following conditions should discuss taking these medicines with their doctor.

• Hypersensitivy to diazoxide, chlorothiazide or any of their ingredients
• Pregnant, could be pregnant, trying to become pregnant or breastfeeding
• Existing heart or lung problems, such as pulmonary hypertension, meconium aspiration, respiratory distress, transient tachypnoea, pneumonia, sepsis, congenital diaphragmatic hernia or congenital heart disease.

What are the side effects?

Note: If your child shows any signs of breathing difficulties, such as flaring nostrils, unusual chest movements, rapid breathing, feeding difficulties or a blue tinge to their lips or skin, please see your doctor or take your child to your nearest Accident and Emergency (A&E) department.

If any of the side effects described below are severe or carry on for a long time, please tell your doctor.

Diazoxide

• Loss of appetite, nausea and vomiting
• Raised levels of uric acid in the blood, retention of salts and fluid, puffiness (oedema)
• High blood sugar levels
• Low blood pressure
• Irregular or fast heart rate
• Increased hair growth

Chlorothiazide

• Weakness and low blood pressure
• Mild upset stomach
• Changes in blood count

Interactions with other medicines

Some medicines can react with diazoxide and/or chlorothiazide, altering how well they work. Always check with your doctor or pharmacist before giving your child any other medicines, including herbal or complementary medicines. The following are known to react with diazoxide and/or chlorothiazide so your child will require regular careful monitoring.

Diazoxide

• Anti-hypertension medicines, including ACE inhibitors, angiotensin II receptor agonists, beta blockers, calcium channel blockers and some diuretics
• Alcohol
• Anti-depressants
• Anti-epileptics including phenytoin
• Anti-psychotics

Chlorothiazide

• Anti-diabetic medicines
• Anti-hypertension medicines as above
• Cholestyramine and colestipol resins
• Corticosteroids
• Lithium
• Non-steroidal anti-inflammatory drugs (NSAIDs)

Important

• Keep medicines in a safe place where children cannot reach them
• Keep the suspension, tablets or capsules at room temperature, away from bright light or direct sunlight and away from heat. Do not store in a fridge.
• If you forget to give your child a dose and it is within a few hours of when the dose was due, give it as soon as you remember. Otherwise, do not give this dose but take the next dose when it is due. Do not give a double dose.
• If your child vomits straight after taking the dose, inform your local doctor or nurse, as your child may need to take another one
• If your doctor decides that your child should stop taking these medicines or they pass the expiry date, return any remaining suspension to your pharmacist. Do not flush it down the toilet or throw it away.

Compiled by:

The Pharmacy and Endocrinology departments in collaboration with the Child and Family Information Group Please read this information in conjunction with any patient information leaflet provided by the manufacturer.

Last review date:

July 2020

Ref:

2020F0376

Diazoxide – instructions for use

Diazoxide

Instruction:

• Pharmacological action
• Pharmacokinetics
• Readings
• Contraindications
• With care
• Pregnancy and breastfeeding
• Dosage and Administration
• Side effects
• Overdose
• Interaction
• Special instructions
• Transport Management
• Classification

Pharmacological action

Diazoxide is a peripheral arteriolar vasodilator of myotropic action, has a rapid hypotensive (lowering blood pressure) effect due to peripheral vasodilation (expansion of the lumen of the vessels). Expands predominantly resistive vessels, activates potassium channels, causes the release of K ⁺ and hyperpolarization of the membrane of vascular smooth muscle cells, disrupts the function of voltage-dependent Ca2+ channels and reduces the entry of Ca ²⁺ into cells. When administered intravenously, it causes a rapid decrease in systolic and diastolic blood pressure, which is not accompanied by the phenomena of orthostatic hypotension. Leads to retention of Na ⁺ and water. It has a strong relaxing effect on the gastrointestinal tract and uterus. Reduces glomerular filtration and inhibits the excretion of uric acid in the tubules of the kidneys.

Pharmacokinetics

When administered intravenously, the maximum plasma concentration (C _max ) is reached after 2-5 hours.

Plasma protein binding is 90%.

Metabolized in the liver (up to 60%), excreted by the kidneys. The half-life is 2-28 hours.

Indications

Hypertensive crises, especially those associated with acute encephalopathy, acute glomerulonephritis and eclampsia.

Contraindications

• Hypersensitivity to diazoxide;
• acute cerebrovascular accident;
• acute stage of myocardial infarction;
• functional hypoglycemia;
• period of childbirth;
• lactation.

Precautions

• Ischemic heart disease;
• angina;
• heart failure;
• diabetes mellitus;
• pregnancy.

Pregnancy and breastfeeding

Use in pregnancy

FDA fetal category C.

Adequate and strictly controlled studies on the safety of the use of diazoxide during pregnancy have not been conducted. The potential risk to humans is unknown.

In experimental studies on animals, a decrease in the growth and survival of fetuses, an increase in the duration of labor was revealed.

The use of diazoxide during pregnancy is not recommended, except in cases of emergency, on the advice of a physician and if the potential benefit to the mother outweighs the possible risk to the fetus.

Childbirth

Due to the pronounced relaxing effect, the introduction of diazoxide in the first stage of labor can lead to the termination of independent labor.

Use during breastfeeding

Special studies on the safety of the use of diazoxide during breastfeeding have not been conducted.

It is not known if diazoxide passes into breast milk.

If necessary, breast-feeding should be avoided.

Dosage and Administration

Intravenous bolus, undiluted, 1–3 mg/kg. The maximum single dose is 150 mg. If there is no effect, re-introduction at the same dose after 5-15 minutes.

Side effects

Headache, dizziness, redness of the skin, edema, hyperglycemia, severe arterial hypotension (up to collapse), the appearance of signs of ischemia of the heart or brain, confusion, allergic reactions.

Overdose

Symptoms

Hyperglycemia, which may be combined with ketoacidosis, as well as glucosuria.

Treatment

Insulin administration and fluid and electrolyte rebalancing. Due to the long half-life of the drug (approximately 30 hours), overdose symptoms require long-term observation (up to 7 days) until the blood glucose concentration returns to normal. Successful reduction of blood diazoxide concentrations has been reported with peritoneal dialysis in one patient and hemodialysis in another.

Interactions

• Diuretics (diuretics) – the hyperglycemic and hyperuricemic effects of diazoxide may be enhanced by the simultaneous administration of thiazides or other commonly used diuretics;
• Anticoagulants (drugs that prevent blood clots) coumarin derivatives – the use of diazoxide in patients taking coumarin and its derivatives may lead to increased anticoagulant action and require a reduction in the dose of anticoagulant;
• Diphenylhydantoin (epilepsy medicine) – administration of diazoxide to patients taking diphenylhydantoin may cause loss of control of seizures;
• Chlorpromazine (antipsychotic drug) – the hyperglycemic effect of diazoxide may be enhanced by concomitant use of chlorpromazine;
• Insulin (blood glucose lowering drug) blocks the hyperglycemic action of diazoxide. In addition, diazoxide, by inhibiting glucagon-induced insulin release, may cause a false-negative glucagon test;
• alpha-blockers (expand blood vessels and reduce their tone, most often used in the treatment of arterial hypertension and prostate adenoma) – reduce the severity of the hyperglycemic action of diazoxide;
• Antihypertensive drugs (drugs that lower blood pressure) – Diazoxide may increase the effect of antihypertensive drugs.

Special instructions

Diabetes mellitus requires correction of hypoglycemic therapy.

Influence on the ability to drive vehicles and control mechanisms

It is recommended to refrain from driving and engaging in activities that require increased concentration and speed of psychomotor reactions.

Classification

• ATX

  C02DA01, V03AH01

• Pharmacological group

  Vasodilators

• ICD code 10

  I10 Essential (primary) hypertension

• FDA pregnancy category

  C
  (risk not excluded)

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Find out more about the active substance Diazoxide:

• INN
• Reviews
• Questions
• Latin name
• Chemical formula

Information about the active substance Diazoxide is intended for medical and pharmaceutical professionals, for reference purposes only. The instructions are not intended to replace professional medical advice, diagnosis or treatment. The information contained here may change over time. The most accurate information on the use of drugs containing the active substance Diazoxide is contained in the manufacturer’s instructions attached to the package.

composition, indications, dosage, side effects, analogues, contraindications, MedOboz, latest health news, Health Reviewer

Mainly dilates resistive vessels, stimulates potassium channels, causes K + release and hyperpolarization of the membrane of vascular smooth muscle cells, disrupts the function of voltage-dependent Ca2 + channels and reduces the intake of Ca2+ into cells. When administered intravenously, it quickly reduces systolic and diastolic blood pressure, which is not accompanied by symptoms of orthostatic hypotension. Leads to Na+ water retention. It has a strong relaxing effect on the uterus and organs of the gastrointestinal tract. Reduces the glomerular filtration rate and inhibits the excretion of uric acid in the tubules of the kidneys.

Composition and formulation

Diazoxide is produced as a solution for parenteral administration in ampoules of 20 ml, one package contains one ampoule. The active substance is diazoxide.

Indications

Used in the treatment of hypertensive crises associated with acute encephalopathy, acute glomerulonephritis and eclampsia.

Contraindications

Not prescribed for patients with acute cerebrovascular accident, in the acute period of myocardial infarction and hypersensitivity to diazoxide.

It is recommended to be especially careful when prescribing the drug to patients who suffer from coronary heart disease, heart failure, angina pectoris and diabetes mellitus.

Use in pregnancy and lactation

Diazoxide should only be used in pregnant women for vital signs. In addition, the introduction of the drug is highly undesirable in the first stage of labor, as it can provoke a complete cessation of independent labor in a woman.

If it is impossible to treat a lactating woman without the use of diazoxide, then lactation should be abandoned for the duration of treatment.

Method of administration and doses

Diazoxide is used only in extreme cases, since when it is administered, there is a high probability of developing an uncontrolled decrease in blood pressure.

The drug is intended for intravenous bolus administration in undiluted form at a dosage of 1 to 3 mg per kg of body weight. The highest single dose is 150 mg. If after the first administration of the drug it was not possible to achieve the necessary pharmacological effect, then after 5 or 15 minutes the administration of the drug is repeated at the same dosage.

With repeated administration, it should be remembered that in this case, diazoxide can cause a pronounced retention of sodium and water.