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Diakarb
Last reviewed: 14.06.2024
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Diacarb (acetazolamide) is a carbonic anhydrase inhibitor. This means that it inhibits the action of the enzyme carbonic anhydrase, which normally speeds up the reaction that converts carbon dioxide (CO2) and water into carbonic acid, which results in the formation of bicarbonate in the body.
Here are some important points about carbonic anhydrase inhibitors:
- Action as a diuretic: Blocking carbonic anhydrase with Diacarb results in decreased reabsorption of bicarbonate in the kidneys, which in turn leads to increased excretion of sodium and water in the urine. This makes Diacarb potentially useful as a diuretic.
- Use in the treatment of glaucoma: Carbonic anhydrase inhibitors such as Diacarb can also be used to reduce intraocular pressure in glaucoma. Reducing intraocular pressure can help prevent damage to the optic nerve and preserve vision.
- Prevention of altitude sickness: Diacarb is also used to prevent and treat altitude sickness. Its action is associated with increasing the elimination of carbon dioxide from the body, which helps to adapt to the changed environmental conditions at high altitudes.
- Treatment of other conditions: In some cases, carbonic anhydrase inhibitors can be used to treat other medical conditions, such as neurological disorders or migraines.
It is important to remember that the use of Diacarb and other carbonic anhydrase inhibitors should be carried out under the supervision of a doctor and in compliance with the recommendations for dosage and use.
Indications Diacarba
- Glaucoma: Diacarb may be prescribed to reduce intraocular pressure in glaucoma. It helps reduce the production of intraocular fluid, which can help prevent damage to the optic nerve and preserve vision.
- Altitude sickness: Diacarb is used for the prevention and treatment of altitude sickness. The drug helps the body adapt to the changed environmental conditions at high altitudes, reducing symptoms such as headache, nausea, dizziness and fatigue.
- Epilepsy: Sometimes Diacarb can be used as an additional agent in the treatment of certain forms of epilepsy.
- Acidosis: The drug may be prescribed to correct some forms of acidosis associated with diseases such as urolithiasis or diabetes.
- Prevention of altitude sickness: Diacarb can be used as a prophylactic before traveling to high altitudes to prevent symptoms of altitude sickness.
- Migraine: In some cases, Diacarb may be prescribed to prevent migraines.
Release form
- Tablets: This is the most common form of Diacarb. Tablets can have different dosages, for example, 125 mg, 250 mg or 500 mg.
- Capsules: Some manufacturers may produce Diacarb in capsule form, especially if slow release of the drug is required.
- Powder for the preparation of an injection solution: In rare cases, Diacarb can be presented in the form of a powder for the preparation of an injection solution.
Pharmacodynamics
- Reducing bicarbonate formation: Acetazolamide inhibits bicarbonate formation in the kidneys, resulting in decreased formation of water-soluble bicarbonate and increased urinary excretion of sodium, potassium, and water.
- Diuretic effect: Blocking carbonic anhydrase in the kidneys leads to increased excretion of sodium, potassium and water in the urine. This diuretic action allows acetazolamide to be used to treat edema and increased intracranial pressure.
- Reducing hydrogen secretion: Acetazolamide also reduces hydrogen secretion in the kidneys, which promotes urine acceleration with a higher pH, which may be useful in the treatment of urolithiasis associated with acidic urination.
- Respiratory stimulation: In high doses, acetazolamide may stimulate breathing by increasing the sensitivity of the respiratory centers in the brain to changes in blood carbon dioxide levels.
- Reducing intraocular pressure: Acetazolamide can also be used to lower intraocular pressure, which is useful in the treatment of glaucoma.
Pharmacokinetics
- Absorption: After oral administration of acetazolamide, it is rapidly and completely absorbed from the gastrointestinal tract.
- Maximum concentration (Cmax): The time to reach the maximum concentration of acetazolamide in the blood plasma is usually about 1-4 hours after administration.
- Bioavailability: The oral bioavailability of acetazolamide is generally high, approximately 80-100%.
- Metabolism: Acetazolamide is metabolized in the liver, mainly through hydroxylation.
- Half-life (T½): The elimination half-life of acetazolamide from the body is approximately 8-12 hours.
- Volume of distribution (Vd): Vd of acetazolamide varies, but is usually around 0.7-0.9 L/kg, indicating good distribution of the drug in body tissues.
- Excretion: Acetazolamide is excreted primarily via the kidneys as unchanged drug.
- Metabolism Interactions: Diacarb may interact with other drugs, particularly other diuretics or antiepileptic drugs, which may alter their effectiveness or blood levels.
Dosing and administration
-
Glaucoma:
- The usual starting dose for adults is 250-1000 mg per day, divided into several doses.
- Children can be prescribed a dose of 5 to 10 mg per 1 kg of body weight per day, also divided into several doses.
-
Epilepsy:
- The usual starting dose for adults is 250-1000 mg per day, divided into several doses.
- For children, the dose may vary depending on age and weight, usually the initial dose is 8-30 mg per 1 kg of body weight per day, also divided into several doses.
-
Altitude sickness:
- To prevent mountain sickness, it is usually recommended to start taking the drug 24-48 hours before ascending to altitude.
- The usual dose is 250 mg twice daily.
- The duration of taking Diacarb depends on the duration of stay at altitude.
-
Hypokalemia:
- For the treatment of hypokalemia, Diacarb can be used at a dose of 250-1000 mg per day, divided into several doses.
Use Diacarba during pregnancy
Use of acetazolamide (Diacarb) during pregnancy may be associated with potential risks, although specific data on its safety and effectiveness during this period are limited. Here's what we know based on available research:
- Study in pregnant women with idiopathic intracranial hypertension: In one case study where acetazolamide was used to treat this condition during pregnancy, there were no adverse pregnancy outcomes. A review of the literature also found no convincing evidence of a negative effect of the drug on pregnancy in humans (Lee et al., 2005).
- Other Study: A study of women with intracranial hypertension who were prescribed acetazolamide during pregnancy found no consistent evidence of harmful effects on pregnancy, even if the drug was prescribed before the 13th week of gestation. However, the use of acetazolamide should be avoided during pregnancy unless absolutely necessary (Falardeau et al., 2013).
Due to the potential risks, the use of acetazolamide during pregnancy should only be done under strict medical supervision and only when the benefits outweigh the possible risks.
Contraindications
- Hypersensitivity: People with a known hypersensitivity to acetazolamide or other sulfonamides should avoid its use.
- Severe renal or hepatic impairment: The drug is contraindicated in patients with severe renal or hepatic impairment as it may worsen their condition.
- Hyponatremia: Diacarb should be used with caution in patients with hyponatremia (low blood sodium levels) as it may worsen this condition.
- Hyperkalemia: The drug should also be used with caution in patients with hyperkalemia (high levels of potassium in the blood) as it may worsen this condition.
- Kurolithiasis: If you have urolithiasis, Diacarb may increase the risk of stone formation and is contraindicated.
- Diabetes mellitus: In patients with diabetes mellitus, the drug should be used with caution as it may change blood sugar levels.
- Pregnancy and breastfeeding: The use of Diacarb during pregnancy and breastfeeding should be evaluated by a physician, as data on its safety during these periods are limited.
- Children's age: The use of Diacarb in children requires special caution and should be carried out under the supervision of a physician.
- Use with other medications: Before using Diacarb in combination with other medications, you should consult your doctor to ensure there are no potential interactions.
Side effects Diacarba
- Drowsiness and dizziness: These are some of the most common side effects of Diacarb. Patients may feel drowsy or dizzy, especially at the beginning of treatment or when the dosage is changed.
- Increased sensitivity to light: Some people may experience increased sensitivity to light while taking Diacarb, which may lead to photosensitivity or faster eye fatigue.
- Loss of appetite and diarrhea: Some patients may experience loss of appetite, nausea, or diarrhea while taking Diacarb.
- Electrolyte disorders: The drug can cause changes in electrolyte levels in the body, such as hypokalemia (low potassium) or hyponatremia (low sodium).
- Increased sensitivity to allergens: Some people may experience allergic reactions to Diacarb, such as skin rash, itching, or angioedema.
- Stomach disorders: May include nausea, vomiting, heartburn, or discomfort in the stomach.
- Metallic taste: Some patients may complain of a metallic taste in the mouth.
- Other rare side effects: Include anemia, aplastic anemia, thrombocytopenia, alkalosis, hyperhydration and others.
Overdose
- Electrolyte Imbalance: Excessive excretion of electrolytes (eg, sodium, potassium) in urine can lead to electrolyte imbalance, which may manifest as weakness, abnormal heart rhythms, muscle cramps, and other symptoms.
- Acidosis: Changes in the body's acid-base balance can lead to metabolic acidosis, which can cause rapid and profound respiratory depression, headache, drowsiness and other symptoms.
- Central nervous system symptoms: Overdose of acetazolamide may cause drowsiness, dizziness, seizures, slow breathing, electrolyte shifts, increased intracranial pressure and other central nervous system symptoms.
- Other complications: Possible complications of overdose may also include hypoglycemia, hyperkalemia, deterioration of renal function and other serious complications.
Interactions with other drugs
- Anhydrase Inhibitors: Diacarb is an anhydrase inhibitor and its effect may be enhanced when used concomitantly with other drugs such as acetazolamide, dorzolamide and brinzolamide, which may result in an increased risk of anhydrase inhibitory side effects such as as metabolic acidosis.
- Drugs for the treatment of epilepsy: Diacarb may interact with drugs for the treatment of epilepsy such as phenytoin, carbamazepine and valproic acid, which may increase or decrease their effectiveness and also increase the risk of central nervous system-related side effects.
- Hypertension and Cardiovascular Medicines: Diacarb may potentiate the effects of medications used to treat hypertension, such as diuretics or angiotensin-converting enzyme inhibitors (ACEIs), which may result in severe lowering of blood pressure.
- Diabetes medications: Diacarb may increase the effects of hypoglycemic drugs such as sulfonylureas, which may result in low blood sugar.
- Drugs to treat gout: Diacarb may increase the effects of drugs used to treat gout, such as probenecid, which may increase uric acid levels in the blood and increase side effects.
Attention!
To simplify the perception of information, this instruction for use of the drug "Diakarb " translated and presented in a special form on the basis of the official instructions for medical use of the drug. Before use read the annotation that came directly to medicines.
Description provided for informational purposes and is not a guide to self-healing. The need for this drug, the purpose of the treatment regimen, methods and dose of the drug is determined solely by the attending physician. Self-medication is dangerous for your health.