Diakarb, instructions for use, side effects, contraindications

Use of Diacarb for intracranial pressure

The study of disorders at the cellular level in hydrocephalus and increased intracranial pressure showed that the final cause of the pathology are 3 types of swelling of brain tissue:

1. Vasogenic - caused by increased permeability of the inner endothelial layer of capillaries, most often occurs with hemorrhagic or ischemic strokes, space-occupying processes (tumors) in the brain.
2. Cytotoxic - depends on changes in the activity of electrolytes (sodium and potassium) in the enzyme adenosine triphosphatase (ATP), develops with oxygen deficiency of brain cells, impaired myocardial contractility, meningitis, encephalitis.
3. Interstitial - associated with the retention of water and sodium ions in the brain substance surrounding the ventricles, a condition called benign intracranial hypertension (pseudotumor).

The maximum effect of Diacarb occurs with interstitial edema.

Details about the benign form of increased intracranial pressure can be found in this article.

The benign form of the disease with a long course and in order to prevent relapses requires the use of Diacarb three times a day. Neurologists consider it the drug of first choice.

Clinical studies have shown a successful combination of courses of therapy with Diacarb and corticosteroids. A special role is given to the drug in restoring vision by relieving compression from the optic nerve sheaths. This allows patients to be saved from irreversible blindness.

Diacarb (Acetazolamide) is the most used diuretic in the clinical practice of neurologists and doctors of other specialties. The drug was synthesized almost 70 years ago.

It allowed me to get rid of toxic mercury diuretics. Gradually it began to be used in the treatment of cardiac and pulmonary pathologies, glaucoma, and intracranial pressure disorders.

In subsequent years, a large group of diuretics was created and successfully used specifically to lower blood pressure, taking into account potassium conservation. Much attention is paid to combination drugs, including various combinations of antihypertensive and diuretic drugs.

Diacarb remains one of the main drugs in the treatment of hydrocephalus, other pathological disorders of the cerebrospinal fluid circulation, headaches, sleep apnea syndrome (breathing cessation), such a complex disease as familial periodic paralysis (another name for hypo-, normo- and hyperkalemic).

Diacarb for intracranial pressure has been used in neurology for more than 50 years. Thanks to its mild effects, it can be used to treat diseases of the pulmonary and cardiovascular systems not only in adults, but also in children.

The active substance of Diakarba, acetozolamide, has a therapeutic effect in the fight against hydrocephalus, apnea syndrome, increased intracranial pressure and a number of other pathological conditions.

Diacarb (Acetazolamide) has been used for intracranial pressure for about 60 years. The drug has been studied quite well, and doctors are aware of the side effects and contraindications. At the same time, it is quite effective and low-toxic.

The first person a patient with suspected intracranial pressure will meet will, of course, be a therapist. He must listen to complaints and decide on referral for further examination and tests. An ophthalmologist can give a more or less accurate conclusion after examining the fundus. This is where fluid stagnation manifests itself.

Based on the results of magnetic resonance or computed tomography, ultrasound or neurosonography, the neurologist will make a final diagnosis. Next, you will need to consult a surgeon to determine the method of treatment.

Hydrocephalus (dropsy of the brain) is a disease in which a large amount of cerebrospinal fluid accumulates in parts of the brain. The cause of this condition is dysfunction of the production or outflow of cerebrospinal fluid from brain structures. Children and adults are susceptible to the disease. Hydrocephalus of the brain in an adult is more complicated than in a child, since the skull bones fused in the area of ​​the fontanelle do not move apart and the fluid begins to put pressure on nearby brain tissue.

The drug Diacarb or Acetazolamide is quite common in the treatment of disorders of the outflow of fluid from the brain and increased intracranial pressure (ICP) of various origins (genesis). The drug was first used in the West in 1957.

The drug is a weak diuretic (has a diuretic effect) and is a carbonic anhydrase inhibitor. In the nephron tubules, Diacarb blocks the enzyme carbonic anhydrase, and the excretion of K and Na ions increases, while the excretion of Ca does not change. There is a shift in metabolic acidosis.

Diacarb will reduce the production of cerebrospinal fluid, so its use is justified in case of disturbances in the movement of cerebrospinal fluid.

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For glaucoma, Diacarb is used due to the fact that by reducing carbonic anhydrase in the ciliary body of the eyes, less moisture is released and eye pressure decreases.

By reducing the level of carbonic anhydrase activity, the drug has also found use in the treatment of epileptic conditions.

Reviews

We have selected some people's reviews about the drug Diacarb:

1. Christina. From time to time I was bothered by eye pain, a feeling as if the eye was being pressed from the inside out. I tried many medications, and I didn’t even know what was causing this pain. I underwent a medical examination, an MRI, etc., and was prescribed this drug along with a number of others for a month. The course is designed for five years, take the drug once every six months. The pain went away immediately after a month, and it relieves recurring pain within 20-30 minutes. There was no pain after the course for a year. A year later they made themselves felt a little, I took a monthly course again and the worries went away. In general, an excellent remedy, the only one that helped me.
2. Julia. I have been suffering from epilepsy for more than 10 years. Once, when visiting a neurologist, he prescribed Diacarb for me. After reading the instructions for use, to say that I was shocked is to say nothing. After the first tablet, the effect begins in about 30 minutes, so you will not be able to leave the house. It also severely dehydrates the body and removes potassium and is recommended to be taken with asparkam, the doctor did not warn me about this. On the second day I developed headaches, weakness and drowsiness, which was also not encouraging. Therefore, after 5 days I decided to stop using it, since instead of improvement there were only side effects.
3. Nelya. After surgery to remove a brain tumor, Diacarb was prescribed. I took a tablet 3 times a week paired with asparkam. I drank it before bed and in the morning I started having tingling sensations in my fingers, a feeling of numbness in my lips, and drowsiness. I was very scared, but after reading the instructions and the side effects of Diacarb, I calmed down and will continue to take the drug. Apparently all these symptoms are natural when taking Diacarb. Thank you.

Release form and dosage

Acetazolamide tablets are available in blisters in a dosage of 0.25 g. This usually corresponds to the prescribed single dose.

When treating intracranial hypertension, depending on the clinical picture and severity of the condition, it is recommended to take 1 tablet per day or ½ - 1 every 8-12 hours. The maximum therapeutic dose limit is 750–1000 mg per day.

Diacarb is available in the form of tablets with a dose of 250 mg

To date, no overdose has been observed. Theoretically, symptoms of electrolyte imbalance, dehydration, metabolic acidosis, and focal manifestations of the brain are considered possible. There is no special antidote.

When treating intracranial hypertension, depending on the clinical picture and severity of the condition, it is recommended to take 1 tablet per day or ½ - 1 every 8-12 hours. The maximum therapeutic dose limit is 750–1000 mg per day.

Diacarb is available in the form of tablets with a dose of 250 mg

A single dose of Diacarb in adults is 250 mg. It coincides with the dosage of the tablets in the blister.

To normalize ICP (intracranial pressure), doctors prescribe 1 tablet per day. The dose can be divided into two doses, every 12 hours. In severe cases of the disease, the maximum amount of the substance for oral use should not exceed 750–1000 mg per day.

Diacarb for intracranial pressure in adults is also used as part of complex therapy for glaucoma, severe edema of various parts of the body, hydrocele, epilepsy, Meniere's disease, gout, emphysema and bronchial asthma.

If the treatment regimen was followed, no overdose symptoms were observed. However, symptomatically, a shift in electrolyte balance and acidosis may occur. The condition normalizes on its own and does not require special treatment.

Scheme of application of "Diacarb" and "Asparkam"

Complex treatment of hypertension includes combinations of different groups of drugs with diuretics.
Diacarb is one of the most used medications in clinical practice, which belongs to the class of carbonic anhydrase inhibitors with a moderate effect. The drug is widely prescribed by neurologists, cardiologists and ophthalmologists. Accelerated removal of potassium ions from the blood is one of the undesirable consequences of taking the drug.

Replenishment of electrolyte reserves is carried out using anionic-cationic drugs, to which Asparkam belongs.

Acetazolamide (the active ingredient of Diacarba) is a derivative of sulfanilic acid, which blocks carbonic anhydrase, reducing the synthesis of sulfur dioxide and water. Pharmacodynamic effects of the drug:

1. Improving renal blood flow - increases diuresis (diuretic effect) and removes potassium from the body (used to correct moderate hyperkalemia).
2. Regulation of fluid production by the ciliary body reduces intraocular pressure in glaucoma.
3. A decrease in the reabsorption of bicarbonates in the nephron tubules leads to the development of transient (transient) acidosis. The condition returns to normal 1-2 days after discontinuation of the drug.
4. The accumulation of carbon dioxide in brain tissue reduces the excitability of neurons and prevents the development of pathological impulses. The effect is used to prevent epileptic seizures.
5. Controlling the synthesis of cerebrospinal fluid in the ventricles of the brain - normalizes the level of intracranial pressure in intracranial hypertension.

Indications for the use of Diacarb in different areas are presented in the table.

Pathology Clinic

Features of the metabolism of the drug "Diacarba":

• absorbed into the cavity of the small intestine;
• degree of binding to blood proteins 70-90%;
• “target structures” whose tissues are rich in the enzyme carbonic anhydrase: kidneys, eyeball, red blood cells, central nervous system;
• excretion in urine, unchanged;
• 90% of the active substance is eliminated within 24 hours.

Undesirable consequences of taking the drug most often occur in the first stage of therapy (2-3 weeks). The main groups of side effects are presented in the table.

Category Symptoms

The mechanism for the development of most side effects is associated with impaired potassium metabolism in the body. One method of preventing symptoms is to take electrolyte donor medications. For example, use the scheme - “Asparkam” with “Diacarb”.

The composition of Asparkam is aspartate salts of potassium (K+) and magnesium (Mg2+). The medicine is intended to regulate metabolic processes, mainly in the myocardium.

Aspartate transports ions into the cell, where they are involved in the process of muscle contraction at the molecular level.

The drug is prescribed for the correction of electrolyte disturbances (deficiency of potassium and magnesium in the body), the prevention of hypokalemia during treatment with loop diuretics.

Contraindications to the use of Asparkam:

• renal failure;
• hemolytic anemia;
• hyperkalemia;
• myasthenia gravis;
• AV conduction disturbance.

Patients with antacid gastritis experience dyspeptic symptoms, epigastric burning, nausea, and diarrhea.

Dosage regimens for adults

The use of the Diakarba complex with Asparkam implies compliance with the recommendations:

• absorption of the diuretic does not depend on food intake, so it is taken at any time of the day.
• a stable effect is observed when using a therapeutic dose once a day, or every other day.

The regimen for taking Diacarb and Asparkam by adults for various diseases is presented in the table.

Pathology "Diacarb" "Asparkam"

In cardiological practice, Diacarb is not prescribed together with Acetylsalicylic acid (Aspecard, Aspirin) due to the high risk of severe acidosis, lethargy, coma, and death.

Use in childhood

In pediatric practice, Diacarb is prescribed for the treatment of neurological diseases:

• hydrocephalus – accumulation of fluid due to increased synthesis of cerebrospinal fluid or impaired outflow;
• epilepsy with “small” seizures: partial (Jacksonian), myoclonus and absence seizures.

The most sensitive to the drug are disorders of liquor dynamics, which are accompanied by interstitial edema of the brain. This type of intracranial hypertension is caused by an increased content of Na+ ions and water in the periventricular (periventricular) white matter.

Clinical signs of pathology:

1. Headache. Children complain of a feeling of “expansion”, “squeezing of the eyes.” Intensifies when tilting the head and coughing. The pain is most pronounced in the morning, immediately after waking up.
2. Vomiting, after which the intensity of the symptom decreases.
3. Congestion in the fundus is a pathognomonic (most specific) sign.

Conservative treatment of pathology involves:

• diet with limited salt intake;
• drinking regime (reducing the amount of fluid consumed);
• taking diuretics (Diacarba), glucocorticoids (in severe cases).

Surgical treatment is indicated if drug therapy is ineffective for 2 months. "Diacarb" for epilepsy in children is an auxiliary element for basic anticonvulsants.

Neurologists prescribe a combination of Diacarb and Asparkam once before routine vaccination (DPT, CPC, Imovax-Polio) in order to prevent complications in children at risk. Taking medications does not reduce the likelihood of developing seizures.

Parental complaints about prolonged crying, sleep disturbances, and increased excitability are not indications for taking the drug. To reduce nervous excitement in pediatric practice, Cinnarizine or Glycine is used.

How to take Asparkam and Diacarb correctly for children?

Prescription of medications in pediatric practice is carried out taking into account the child’s body weight. Doses and recommendations for taking Asparkam with Diacarb are presented in the table.

Pathologies Dosage calculation Special instructions

Correction of the dose and regimen of anticonvulsants is carried out 2 times a year.

Long-term diuretic therapy requires periodic monitoring of blood pH and water and electrolyte balance. Taking Asparkam with Diacarb is recommended for laboratory-confirmed hypokalemia and hypomagnesemia.

conclusions

"Diacarb" is a drug that has a moderate diuretic effect, which gradually decreases with long-term use. The medication is prescribed as part of complex therapy for neurological and cardiovascular disorders.

In order to prevent water and electrolyte imbalance, it is recommended to use regimens that include Asparkam. The selection of an effective dose, regimen and duration of therapy is carried out by the attending physician. Before you start taking it, you should read the instructions.

Source: https://cardiograf.com/preparaty/prochie/diakarb-i-asparkam-skhema-priema-vzroslym.html

Mechanism of action

Acetazolamide is classified as a weak diuretic. The point of action is the enzyme carbonic anhydrase. With its chemical composition, it blocks the action of sodium and potassium absorption in the most peripheral ends of the tubules of the main functional unit of the kidneys - the nephron.

As a result, the excretion of electrolytes in the urine increases: sodium, potassium, bicarbonate salts, magnesium, calcium, phosphates while maintaining the chlorine content. A side effect is formed - hypokalemia and a decrease in magnesium levels, which can negatively affect the heart rate.

The lack of carbonic acid and bicarbonate salts leads to the fact that the acid-base reaction in the body shifts towards metabolic acidosis (increased acidity). It is this property that is important in the treatment of breathing disorders during sleep.

It should be borne in mind that after three days from the start of treatment, Diakarb loses its diuretic properties. A break of several days is necessary to restore carbonic anhydrase activity. Then the drug begins to “work” again as a diuretic.

Reduced carbonic anhydrase activity in brain tissue contributes to:

• reducing the production of cerebrospinal fluid in the ventricles, which is necessary for chronic intracranial hypertension and other liquorodynamic disorders;
• suppression of foci of excitation in the nuclei that cause epileptic attacks.

In neurological practice, Diacarb is considered a universal drug and is reasonably used to treat adults and children.

Contraindications

Hypersensitivity to the components of the drug and sulfonamides, impaired liver and kidney function, acute renal failure, liver failure, hyponatremia and / or hypokalemia, Addison's disease, adrenal insufficiency, hyperchloremic acidosis. Acetazolamide is contraindicated in patients with cirrhosis as it may increase the risk of hepatic encephalopathy.

Long-term use of acetazolamide is contraindicated in patients with chronic decompensated angle-closure glaucoma, since in the case of complete closure of the angle of the chamber of the eye, the worsening of glaucoma will be masked by reduced intraocular pressure.

Urolithiasis (with hypercalciuria), diabetes mellitus, uremia.

How is intraocular pressure reduced?

Diacarb is used in ophthalmological practice for the treatment of glaucoma. The enzyme carbonic anhydrase is found in the structure of the eye (ciliary body) that produces fluid for the anterior chamber. Suppression of activity causes a decrease in the amount of moisture, which leads to the relief of increased intraocular pressure.

It is important that there is no addiction to Diacarb during long-term treatment. The effect is determined by measuring intraocular pressure. The onset appears within an hour, reaches its maximum effect after 3–5 hours and lasts up to 12 hours. Observations have shown that the initial pressure can be reduced by 50–60%.

Interaction

When Diacarb is combined with antiepileptic osteomalacia may increase . And interaction with diuretics and Theophylline leads to a significant increase in diuretic effect. But this does not apply to acid-forming diuretics . In this case, the diuretic effect, on the contrary, decreases.

In addition, the drug increases the likelihood of the toxic effect of salicylates , carbamazepine , non-depolarizing muscle relaxants , drugs with digitalis, and ephedrine .

Distribution and absorption in the body

After taking two tablets orally and drinking water, they are well absorbed in the intestines. It should take 1 to three hours before the maximum concentration in the blood is reached. Then the drug content drops, but is recorded in the plasma for another day.

In the body, Diacarb “takes” red blood cells, brain tissue, eyeballs, kidneys, and muscles from the blood. Proven ability to penetrate the placenta and breast milk.

This substance does not accumulate in cells. All Acetazolamide is excreted unchanged by the kidneys. Almost 90% of the dose taken is lost in the urine within 24 hours.

The drug is taken with a sufficient amount of water. The maximum concentration of the substance in the blood is observed after 1-3 hours. The complete elimination period is 24 hours.

Diacarb is distributed in red blood cells, brain, eyeballs, kidneys, and muscle tissue. It has the ability to penetrate the blood-brain barrier, so it is not prescribed to pregnant and nursing mothers.

It does not accumulate in the body and is excreted from the body by the kidneys without the formation of metabolites.

Analogues and price of the drug

Full analogue - Acetazolamide.

Analogues of Diacarb in terms of structural biochemical composition are drugs whose active substance is acetazolamide. These drugs are considered synonyms of Diacarb; their dosage and release form are also identical.

1. Fonurit tablets.
2. Acetazolamide Acri tablets.

There are also analogues of Diacarb in terms of therapeutic effect, but with a different chemical composition. These include all drugs based on dichlorphenamide. In our country, such drugs are not officially registered. All of them, like Diacarb, are carbonic anhydrase inhibitors.

Today, the price of a package of Diacarb tablets ranges from 200 to 250 rubles.

Drug Diacarb

In terms of pharmacological action, analogues of Diacarb are

Structural analogues of the active substance (acetazolamide):

• Diuremide
• Acetazolamide
• Anikar
• Glauconox

Important - the indicated instructions for use of Diacarb, its price and reviews do not apply to analogues and cannot be instructions for replacing the drug. If it is necessary to replace Diacarb with an analogue, you must consult a doctor and possible dosage adjustment.

Storage conditions and periods Store in a dry place, protected from light and out of reach of children, in the original packaging, at a temperature not exceeding 25°C. Shelf life – 5 years.

We invite you to read: Increased intraocular pressure in adults: causes, signs and consequences

After oral administration (500 mg), Diacarb is quickly absorbed into the gastrointestinal tract, the maximum content in the blood occurs after 2 hours.

The active component penetrates into the blood plasma, red blood cells, kidneys, and much less into the muscles, liver, central nervous system, and eyes. Does not accumulate in tissues.

Valid for 12 hours.

About 90% of the drug is excreted unchanged by the kidneys (urine) within 24 hours.

Cases of overdose have not been described. Increased side effects are likely.

Treatment: aimed at eliminating symptoms and maintaining the patient’s condition normal, there is no special antidote.

If the patient has acidosis, bicarbonates should be prescribed. Hemodialysis is also indicated (to remove acetazolamide from the body).

Analogues of Diacarb are drugs that also contain acetazolamide.

Diumerid and Acetazolamide are worthy drugs that can replace Diacarb.

Diumerid

Release form: tablets 250 mg.

The drug is digested a little slower and absorbed into the blood.

Indications and contraindications for the use of the medication are the same as for Diacarb.

Price for 20 tablets: 160-200 rubles.

Acetazolamide

Release forms: substance 5 kg, 10 kg.

Due to the virtual absence of auxiliary components, the absorption rate and level of digestibility of this drug will be lower than that of Diacarb.

Schemes and features of treatment with Diacarb

In the treatment of edema of other origins, 1 tablet is prescribed every other day or two. It is important to consider that exceeding the dose by more than 1 g per day does not enhance the result.

In the treatment of glaucoma, Diacarb is part of combination therapy. Depending on the type of disease, it is used 1 tablet every 3-4 days or at the maximum daily dose. For some patients, two tablets a day are enough.

For children, a daily dose of 10–15 mg per kg of body weight is calculated and divided into 3–4 doses. Prescribed over the age of three years. Application regimen: the selected dosage is used for five days, followed by a two-day break. Simultaneous administration of potassium supplements and diet is mandatory.

Before surgery for glaucoma, 2 tablets are prescribed in the evening, and again in the morning up to 500 mg.

In the treatment of epilepsy, adults are prescribed Diacarb once a day, 1–2 tablets for three days, taking a break on the fourth. If necessary, the daily dosage is increased. For children over three years of age, the maximum dose is calculated at 8–30 mg per kg of body weight.

In the treatment of hydrocephalus, Diacarb is used in conjunction with surgical methods.

Asparkam is a source of potassium and magnesium ions

Diacarb is used for hydrocephalus in adults in combination with Asparkam. This is especially true for long-term diseases. The decongestant effect is enhanced with complex therapy; Asparkam replenishes the loss of minerals in the body.

The regimen for adults to take Diacarb and Asparkam for hydrocephalus is to prescribe after one day or two, but in any case, the duration of the course should not exceed more than 10 days.

Hydrocephalus in adults is treated with the combined interaction of Diacarb and surgical treatment.

Another article: What pills to take for hypertension

In the treatment of hydrocephalus, Diacarb is used in conjunction with surgical methods.

Indications for use

Why is Diacarb prescribed? As mentioned above, the drug received its main therapeutic use in the treatment of intracranial pressure and swelling. Indications for the use of Diakarb also include diseases and conditions:

1. Attack of glaucoma (primary and secondary, as well as during an acute attack);
2. In the presence of so-called “mountain” illness in acute form;
3. Edema syndrome (mild to moderate severity, in combination with alkalosis);
4. Epilepsy (as part of combination therapy).

In addition, Diakarb is used for intracranial hypertension in complex treatment.

What are the possible side effects?

In defense of the drug, it should be explained that a side effect is possible if the dosage regimen is violated, the dosage is exceeded, or increased individual sensitivity. Based on the nature of the reactions, one can judge the predominant damage to one of the body systems.

Nervous system disorders cause:

• paresthesia and paralysis;
• tinnitus, decreased hearing;
• increased fatigue;
• dizziness;
• convulsions;
• loss of orientation in the situation.

The effect of drowsiness should be taken into account by persons when driving vehicles.

Digestive disorders manifest themselves:

• nausea and vomiting;
• diarrhea;
• loss of appetite and taste;
• liver necrosis is possible.

In urination there are possible:

• increased urination;
• deposition of salts along the urinary tract.

The hematopoietic system disrupts the bone marrow process of hematopoiesis, resulting in:

• agranulocytosis with a decrease in the total number of leukocytes;
• thrombocytopenia;
• aplastic anemia;
• pancytopenia;
• hemorrhagic diathesis is possible.

Allergic reactions: in the form of skin rash, urticaria, facial swelling, anaphylactic shock, skin erythema.

Vision: possible clinic of transient myopia.

Neurologists recommend caution in using the drug against the background of the patient having emphysema and a tendency to thromboembolism (according to a history).

The effect of drowsiness should be taken into account by persons when driving vehicles.

The drug has a mild effect and, as a rule, does not cause side effects. However, in some cases, dyspeptic disorders and disturbances in the functioning of the nervous system are possible.

Drivers of vehicles should not use Diacarb while working.

The drug is not recommended for use when driving vehicles or during work that requires special attention due to the drowsiness effect.

With long-term use, laboratory monitoring of blood parameters is necessary. Dose adjustment is made when blood sugar increases, a persistent decrease in sodium and potassium, or a change in the acid-base balance.

Analogues of Diacarb include Diuremide, Diamox, Diluran, Glaupax. These are medications with the active ingredient acetazolamide of various brands.

Diuretics with potassium-sparing properties are no less in demand in neurology, which allows reducing the number of medications used during long-term treatment.

Reviews about Diakarb

There are very different opinions about the drug. Some reviews of Diacarb report that the medicine helped, while in others people complain of side effects. In the latter case, they especially often talk about the appearance of cramps and muscle weakness . But in general, positive reviews about Diakarb are still more common.

Some forums also ask whether this remedy can be used during pregnancy. Experts give an unequivocally negative answer to this question. The drug is not prescribed to pregnant women.

Who is the drug contraindicated for?

Given the disturbance of acid-base and electrolyte balance, treatment with Diacarb is not recommended for:

• hypokalemia and hyponatremia (therapy should be accompanied by laboratory monitoring of electrolytes in the blood);
• metabolic acidosis caused by various diseases, including diabetes;
• acute liver and kidney failure;
• chronic liver and kidney failure in case of threat of encephalopathy;
• in the first trimester of pregnancy (in the second and third only for special indications) and during lactation;
• Addison's disease;
• hypersensitivity and allergic manifestations.

The drug is not used in the treatment of children under three years of age. Use requires caution in case of edema due to kidney and liver diseases.

In the acute period after skull injuries with severe headache, Diacarb is prescribed for three days, 0.25 g, up to three times a day.

In the acute period after skull injuries with severe headache, Diacarb is prescribed for three days, 0.25 g, up to three times a day.

Overdose

In case of an overdose of Diakarb, no special cases are described, but the following symptoms are likely:

• water-electrolyte balance disorder;
• metabolic acidosis;
• various CNS disorders.

There is no specific antidote; treatment is symptomatic and supportive. During treatment, it is necessary to control electrolytes in the blood (sodium, potassium), as well as blood pH. Sodium bicarbonate is used for metabolic acidosis. Acetazolamide is removed by hemodialysis.

Drug interactions

Since Acetazolamide is recommended for the combined treatment of various diseases, the instructions for use require taking into account the possible increase and decrease in its effect, and timely adjustment of drug dosages.

The action is enhanced by:

• folic acid antagonists;
• hypoglycemic agents;
• anticoagulants for internal use;
• Cardiac glycosides in the treatment of circulatory failure exhibit toxic properties and cause arrhythmias;
• drugs to increase blood pressure;
• antiepileptic drugs cause bone softening more aggressively;
• Atropine, Amphetamine, Quinidine, Ephedrine dramatically increase undesirable side effects;
• diuresis increases when using Aminophylline;
• β-blockers reduce arterial and intraocular pressure more strongly.

Aspirin and combination drugs including acetylsalicylic acid cause toxic effects on the brain

Combinations with ammonium chloride and diuretics formed during the breakdown of acid lead to a decrease in the diuretic effect.

During anesthesia, anesthesiologists have to take into account the property of Diacarb to increase the concentration of muscle relaxants (drugs for muscle relaxation) in the blood.

"Diacarb" can increase the toxicity of salicylates, various muscle relaxants and ephedrine, therefore the combined use of such drugs is contraindicated, because it is impossible to accurately calculate the required dose. And also you cannot use this remedy together with other diuretics and “Theophylline”, as they enhance the effect of each other. "Asparkam" does not affect the metabolism of other drugs, so it can be used without fear.

Aspirin and combination drugs including acetylsalicylic acid cause toxic effects on the brain

An increase in effect is observed during joint therapy with Diacarb and certain groups of substances:

• folic acid antagonists;
• means to lower blood sugar levels;
• anticoagulants;
• cardiac glycosides;
• hypertensive drugs;
• with Aminophylline (increases the amount of daily urine);
• β-blockers.

Interaction with aspirin is not allowed due to toxic effects on the brain.

Ammonium chloride weakens the effect of the diuretic. Diacarb increases the concentration of muscle relaxants in the blood.

With intracranial pressure, the drug helps stabilize the outflow of cerebrospinal fluid from the brain and improve the patient’s condition. Children with hydrocephalic syndrome often experience dilation of the ventricles of the brain and, as a result, increased intracranial pressure. Diacarb is prescribed for use according to a regimen that cannot be changed to avoid side effects:

• excitability;
• lack of appetite;
• tachycardia.

In pediatric practice, the prescription of Diacarb is justified in the case of the development of not only hydrocephalic syndrome, but also motor disorders, as well as liquor hypertension. Course therapy can reduce the symptoms of high pressure in the cranial cavity and eliminate twitching of the facial muscles.

Treatment of acute conditions associated with increased intracranial pressure is successful if the patient consults a doctor in the early stages of the disease. The appearance of some lethargy and lethargy in the patient in the first days of treatment is associated with a decrease in cerebrospinal fluid secretion. Taking Diacarb is always combined with the prescription of drugs that stabilize the electrolyte balance: Asparkam or Panangin.

pharmachologic effect

Diacarb is widely used as a diuretic for water and sodium retention in the body, as well as in the treatment and prevention of edema of various etiologies.
It has also proven highly effective in treating Meniere's disease and epilepsy. The duration of action of the drug is about 12 hours. Under the influence of this drug, the patient may have an increased risk of developing side effects while taking oral contraceptives and anticoagulants with this drug interaction.

The drug Diacarb is not recommended to be combined with non-steroidal anti-inflammatory drugs, since in this case the patient may develop metabolic acidosis and toxic damage to the central nervous system.

If the patient is already taking cardiac glycosides or drugs that increase blood pressure, adjustment of the daily dose of Diacarb is required.

The therapeutic effects of Diakarb according to the instructions for use are as follows:

1. Diuretic (diuretic) effect.
2. Antiglaucoma effect.
3. Antiepileptic effects.
4. Reduced intracranial pressure.

The diuretic effect of Diacarb is considered weaker in comparison with other diuretics.

When fluid is removed from the body when taking Diacarb, a large amount of potassium ions is also removed. It is for this reason that during a course of taking Diakarb, drugs that enrich the body with potassium and magnesium are prescribed without fail - Asparkam, Panangin, etc.

In smaller quantities compared to potassium ions, phosphates, calcium and magnesium ions are washed out of the body. In order to prevent the development of metabolic disorders, when taken for more than 2 weeks, it is necessary to replenish the loss of the corresponding microelements by the body.

The peculiarities of the mechanism of action are such that it is not advisable to take it for more than three days in a row. That is why there are specially developed instructions for use, according to which it is necessary to take breaks between doses, then its diuretic effect will persist.

In addition to the purely diuretic effect, Diacarb reduces intracranial and intraocular pressure, thus having an antiglaucoma effect. Thanks to the action of Diacarb, the production of fluid in the anterior eye chamber is reduced and thereby the intraocular pressure decreases. Diacarb acts as an inhibitor of carbonic anhydrase of the ciliary body, which makes it possible to successfully use it to relieve an acute attack of glaucoma.

Similar effects of Diakarb are observed in the cavities of the ventricles of the brain and the spinal canal. Thanks to this effect, liquorodynamic parameters are normalized and the level of intracranial pressure is reduced.

Due to the decrease in intracranial pressure, pathological excitability in various structures of the brain is relieved, which leads to a decrease in convulsive readiness and a decrease in the number of epileptiform seizures.

In some cases, a side effect of the drug is also used for therapeutic purposes - its ability to cause metabolic acidosis. This condition helps to effectively eliminate breathing disorders, including sleep apnea.

The duration of action of the drug in the body is about 12 hours.

The diuretic effect is achieved by reducing the amount of electrolytes.

Their quantitative indicator decreases due to a decrease in the activity of the carbanhydrase enzyme (Diacarb inhibits the amount of sodium released from carbonic acid in the nephron tubule), which plays a significant role in the transport of hydrogen ions. A deficiency of these ions contributes to the removal of water and sodium from the body.

Due to the inhibition of carbonic anhydrase in the ciliary body, the amount of aqueous humor produced decreases - this helps reduce pressure in the eyes.

Due to the ability to reduce the level of activity of the substance carbonic anhydrase in the brain, the drug has an antiepileptic effect.

Inhibiting the action of carbonic anhydrase also helps to reduce the amount of cerebrospinal fluid produced in the spinal cord, which reduces intracranial pressure.

Side effects of the drug on body systems:

1. Nervous system: hearing impairment (impaired perception or noise), paresthesia, disorientation, flaccid paralysis, photophobia.
2. Gastrointestinal tract: loss of appetite, vomiting, nausea, diarrhea, diarrhea, polyuria, taste disturbance, hepatic colic, urolithiasis, nephrolithiasis, hematuria, liver necrosis (in case of sensitivity of the body to the components).
3. Metabolism: electrolyte imbalance, metabolic acidosis.
4. Hematopoietic system: leukopenia, agranulocytosis, thrombocytopenia, aplastic anemia, pacytopenia, bone marrow dysfunction.
5. Vision: temporary myopia, sensitivity to light.
6. Allergies: anaphylaxis, urticaria, Lyell's syndrome, Stevens-Johnson syndrome, erythema multiforme.
7. Other: increased body temperature, muscle weakness.
8. Laboratory indicators: glucosuria, hematuria, hyperglycemia, hyponatremia, hypokalemia.

It is worth noting that the medicine:

• Strengthens the severity of the diuretic effect of diuretics.
• When combined with acid-forming diuretics, the diuretic effect of taking Diacarb is reduced.
• Do not take simultaneously with large amounts of acetylsalicylic acid, ephedrine, carbamazepine, or underpolarizing muscle relaxants (the risk of toxic effects increases).
• Diacarb can enhance the effect of hypoglycemic drugs, oral anticoagulants, and folic acid antagonists.
• When taking drugs that increase blood pressure, it is necessary to adjust the dose of Diacarb.
• Increases the absorption of phenytoin, primidone (which is contained in antiepileptic drugs). A severe form of osteomalacia may occur.
• Diacarb enhances the side effects of taking amphetamine, atropine, and quinidine.
• Considering that the drug lowers blood glucose, it is necessary to change the dose of insulin or glycemic tablets when treating diabetes.
• Increases the amount of excreted lithium and weakens its effects.
• Diacarb may increase the level of carbamazepine in the blood.

Are there other drugs with similar properties?

Acetazolamide-based drugs may be sold in pharmacies under other brand names. They are complete analogues of Diacarb and are no different in application. Carbonic anhydrase blockers are:

• Diuremide.
• Diamox,
• Diazomide,
• Diluran,
• Glaupax.

Diacarb has a proven therapeutic effect for various neurological and general diseases. Application requires control using laboratory indicators and knowledge of the characteristics of the action.

Similar drugs:

• Dolobene Gel for external use
• Wobenzym Oral tablets
• Hydrocortisone Substance-powder
• Lipril (Liprilum) Oral tablets
• Soventol Gel
• Feloran Gel for external use
• Lyoton 1000 Gel for external use
• Indovasin Gel for external use
• Indomethacin (Indometacinum) Oral tablets
• Phlogenzym Oral tablets

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DIACARB in neurological practice

•The ability of acetazolamide to reduce the production of cerebrospinal fluid is used in the treatment of liquorodynamic disorders.

•Inhibition of carbonic anhydrase of the ciliary body leads to a decrease in the secretion of aqueous humor and a decrease in intraocular pressure, which explains its use in glaucoma.

•A decrease in the activity of carbonic anhydrase in the brain and suppression of paroxysmal discharges determines the presence of antiepileptic activity in Diacarb.

1) liquorodynamic disorders;

2) chronic intracranial hypertension;

3) sleep apnea syndrome;

5) some types of headaches, as well as for the prevention of attacks in familial hypo- and hyperkalemic periodic paralysis.

Hydrocephalus and increased intracranial pressure

•Vasogenic edema is associated with an increase in the permeability of capillary endothelial cells and, as a rule, occurs with ischemic or hemorrhagic strokes, brain tumors and other pathological conditions.

•Cytotoxic edema is caused by changes in the activity of Na, K dependent ATPase and can develop with hypoxia, myocardial dysfunction, neuroinfections (meningitis, encephalitis), etc.

•Interstitial edema is associated with increased water and sodium in the periventricular white matter; This condition is called pseudotumor cerebri or benign intracranial hypertension.

•Headache. The most typical feature of cephalalgia is an increase in its intensity in the early morning hours or immediately after waking up, which is due to the circadian rhythms of CSF production (40% of cerebrospinal fluid is formed from 4 to 6 am). The headache is bursting in nature with a feeling of squeezing out the eyes from the inside, intensifies when lowering the head down or coughing. Often, as the intensity of the headache increases, repeated vomiting appears.

•Vomiting, as well as headaches, often occurs in the morning. After vomiting, the intensity of cephalgia often decreases or the headache disappears completely.

•Congestion in the fundus is a very pathognomonic sign of intracranial hypertension.

For vasogenic cerebral edema, corticosteroids are most effective - their mechanism of action is associated with the suppression of the activity of Na, K dependent ATPase in the choroidal plexuses. For this purpose, dexamethasone is used at a dosage of 8-12 mg/day. In addition, osmotic diuretics (mannitol 1.5-3 g/kg) are used, which help create a transcranial osmotic gradient.

For interstitial edema (pseudotumor cerebri), the prescription of acetazolamide (diacarb 250 mg/day) and/or the use of shunting is justified.

The main clinical point of use of acetazolamide for respiratory disorders is central sleep apnea syndrome.

•Alveolar hypoventilation disorders;

With strokes, tumors, encephalitis in the area of ​​the brain stem, syringobulbia, as a result of damage to the respiratory center, chemoreceptor zones, and respiratory rhythm generator, severe breathing disorders develop, which can occur both during sleep and while awake. There is no clear opinion about the relationship between cerebral hemispheric strokes and the incidence of respiratory disorders during sleep.

•Slowing of blood flow, which leads to unstable functioning of respiratory control centers;

•Changes in the activity of brain stem structures

Damage to the pathways from peripheral chemoreceptors to the respiratory centers of the medulla oblongata also contributes to the development of SCAS (a similar development mechanism is characteristic of diabetic polyneuropathy).

Respiratory disorders often occur in neuromuscular diseases (myopathy, dystrophic myotonia, myasthenia, etc.). In this case, in the mechanism of development of SCAS, the main role is played by damage to the efferent part of the respiratory system, as a result there is a disruption in the conduction of the stimulus to the respiratory muscles, and the inability of the diaphragm to fully contract during breathing occurs.

Puertas J., et al showed a high prevalence of sleep-disordered breathing in individuals with parkinsonism. However, the relationship between disorders of the autonomic nervous system in parkinsonism and respiratory disorders has not yet been proven. According to T.S. Eligulashvili, sleep apnea in this pathology is associated with incoordination of the respiratory muscles as a result of akinetic-rigid syndrome.

•tumor and paraneoplastic lesions of the central nervous system

•amyotrophic lateral sclerosis

•frequent awakenings at night

•awakenings are accompanied by a feeling of lack of air

• Cheyne-Stokes type breathing, or periodic breathing, is often observed.

Diagnosis of breathing disorders during sleep of central origin is based on clinical characteristics and data from additional examination methods.

1. difficulty breathing or shortness of breath

2. increased physical activity during sleep

3. appearance of cyanosis during sleep

1. Frequent activations during sleep associated with apnea

2. episodes of tachycardia and bradycardia

3. decreased saturation associated with apnea

4. In the multiple sleep latency test results, the average time to fall asleep is less than 10 minutes

Central sleep apnea syndrome, in turn, is divided depending on the severity into mild, moderate and severe, and according to the duration of the disease into acute, subacute and chronic periods.

1.Improving heart function (treatment of concomitant cardiopulmonary pathology)

2.Oxygen inhalation at night

3. Breathing under increased pressure

In a study by White, et al (1982), acetazolamide therapy was administered to 6 men with SCAS. In this case, Diacarb was used at a dosage of 250 mg 4 times a day for 7 days. During therapy, there was a significant decrease in apnea episodes from 54 to 12 per hour.

According to DeBacker, et al. (1995) the administration of acetazolamide (Diacarb) 250 mg, an hour before bedtime for 1 month, can improve the quality and duration of sleep, as well as reduce daytime sleepiness and fatigue, reduce the number of apneas, its index and duration. At the same time, there is an improvement in the frequency of breathing, restoration of the gas composition of the blood, a decrease in the number of awakenings and a decrease in the variability of blood pressure during the REM sleep phase.

According to Surkova N.A. (2006) in the treatment of respiratory disorders during sleep in 40 patients with hypertensive encephalopathy with diacarb at a dose of 250 mg/day, during 3 five-day cycles, there was an improvement in cognitive processes (auditory, visual memory, frontal dysfunction), improved sleep, and daytime activity , as well as reducing the feeling of fatigue.

•should be used with caution in patients with a history of thromboembolic syndrome and in persons with pulmonary emphysema

•simultaneous use of Diacarb and acetisalicylic acid is not recommended

(.) With long-term use, it is necessary to monitor the level of blood electrolytes, the number of platelets and leukocytes, as well as the acid-base status.

Pharmacodynamics and pharmacokinetics

Diacarb tablets are a diuretic . Their diuretic effect is associated with inhibition of carbonic anhydrase , which takes part in the metabolism of carbonic acid. Inhibition of the action of this enzyme occurs in kidney tissue. As a result, the degree of reabsorption into the blood from urine decreases.

This drug also helps with pulmonary heart failure , which can occur with certain lung diseases, for example, with emphysema . In addition, it can be used for excessive intracranial pressure. It inhibits carbonic anhydrase in the brain, which leads to a decrease in the formation of cerebrospinal fluid and intracranial pressure. Accordingly, the associated symptoms, for example, headache, .

Once in the body, this drug also inhibits carbonic anhydrase of the ciliary body, which determines its use in acute attacks of glaucoma . Its action causes a decrease in the secretion of aqueous humor and normalizes its outflow.

In general, tablets are widely used to treat water and sodium retention in the body, as well as to prevent edema of various origins . Thus, they can be used in the treatment of many diseases. Helping to normalize water-salt metabolism, they do not disturb the acid-base balance. Duration of action is up to 12 hours.

After oral administration at a dosage of 500 mg, the maximum concentration of the drug in the blood plasma is reached after 2 hours. Its action is characterized by a high degree of binding to plasma proteins. The active substance penetrates the placental barrier.

The medicine is excreted unchanged through the kidneys, mainly within 24 hours.

Application Features

There have been reports of suicidal ideation and behavior in patients treated with antiepileptic drugs for various indications. A meta-analysis of randomized placebo-controlled trials also showed a small increase in the risk of suicidal ideation and behavior. The mechanism for this risk is unknown, and available data do not exclude the possibility of an increased risk for acetazolamide.

Therefore, signs of suicidal thoughts and behavior should be monitored and appropriate treatment considered. Patients (and caregivers) should be advised to seek immediate medical attention if signs of suicidal thoughts or behavior occur.

Acetazolamide prescribed in doses higher than recommended does not lead to an increase in diuresis, but can cause drowsiness and paresthesia, and can sometimes even lead to a decrease in diuresis. Under certain conditions, however, it is necessary to use very large doses in combination with other diuretics to provide diuresis in completely refractory heart failure.

During treatment with acetazolamide, both a decrease and an increase in plasma glucose levels were noted, this should be taken into account when prescribing the drug for patients with impaired glucose tolerance or diabetes mellitus.

Long-term therapy requires special precautions. The patient should be warned to report all cases of skin changes. It is recommended to periodically monitor the blood picture and the level of electrolytes in the blood serum (especially potassium levels and blood pH), as well as monitoring the peripheral blood picture. Fatalities due to serious reactions to sulfonamides have occurred, although such cases have been rare. In case of a sharp decrease in the number of blood cells or the appearance of toxic changes in the skin, the drug must be immediately discontinued.

Use with caution in pulmonary embolism and pulmonary emphysema, obstruction/obstruction of the lower respiratory tract, in which alveolar ventilation may be reduced, in renal failure, as well as in elderly patients due to the increased risk of developing metabolic acidosis.

In patients with a history of renal stones, the risk/benefit ratio for further stone deposition should be assessed.

The drug alkyrizes urine.

The development of generalized erythema during the use of the drug, accompanied by the appearance of pustules and fever, may be a symptom of acute generalized eczematous pustulosis. If such a condition is diagnosed, treatment with acetazolamide should be discontinued; further use of the drug is contraindicated.

In case of hypersensitivity, symptoms may occur that may threaten the patient's life, for example, Stevens-Johnson syndrome, Lyell's syndrome, fulminant liver necrosis, agranulocytosis, aplastic anemia and bleeding diathesis.

If skin or hematological manifestations develop, the drug should be discontinued immediately.

Acetazolamide should be prescribed with caution to patients taking acetylsalicylic acid (high doses), as there is a possibility of developing anorexia, increased breathing, lethargy, coma and even death.

If you miss a dose, you should not increase the dose at the next dose.

If a patient takes acetazolamide for more than 5 days, there is a risk of developing metabolic acidosis.

Laboratory research

It is recommended to monitor the blood picture and platelet levels at the beginning of treatment and periodically during treatment, and it is also recommended to monitor the level of electrolytes in the blood plasma.

Interaction with other drugs and other types of interactions

• Acetazolamide may enhance the effect of folic acid antagonists, hypoglycemic agents and anticoagulants taken orally.
• Concomitant use of acetazolamide with acetylsalicylic acid can lead to severe acidosis and toxic effects on the central nervous system with the risk of anorexia, tachypnea, lethargia, coma with possible death.
• When using acetazolamide simultaneously with cardiac glycosides or drugs that increase blood pressure, the dose of the former must be changed.
• Acetazolamide disrupts the metabolism of phenytoin, increasing the concentration of the latter in the blood serum. Severe osteomalacia has been observed in patients taking acetazolamide with certain anticonvulsants (phenytoin, primidone).
• Concomitant use of acetazolamide with amphetamines, atropine or quinidine may increase their side effects. The excretion of amphetamine and quinidine is reduced, so it is possible to increase the duration of action of amphetamine and enhance the effect of quinidine by increasing the urine pH level in the renal tubules.
• Acetazolamide may increase or decrease blood glucose concentrations, which should be taken into account when treating diabetes mellitus. A change in the dose of insulin or oral hypoglycemic drugs may be necessary.
• Acetazolamide increases lithium excretion and may decrease plasma lithium levels.
• Acetazolamide may increase plasma concentrations of carbamazepine.
• With simultaneous use, acetazolamide increases the risk of toxic effects of salicylates, digitalis preparations, carbamazepine, ephedrine, and non-depolarizing muscle relaxants.
• The diuretic effect of acetazolamide is enhanced by theophylline and weakened by acid-forming diuretics.
• There have been isolated reports of decreased serum levels of pramidone and increased levels of carbamazepine when used concomitantly with acetazolamide.
• Due to possible additive effects, concomitant use with other carbonic anhydrase inhibitors is not recommended.
• Cyclosporine: Acetazolamide may increase cyclosporine levels.
• Methenamine: Acetazolamide may interfere with the antiseptic effect of methenamine in urine.
• Sodium bicarbonate: Concomitant use of acetozalamide with sodium bicarbonate increases the risk of renal stone formation.