Diacarb

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:

1. Diuretic action: Blocking carbonic anhydrase by 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.
2. 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.
3. Prevention of mountain sickness: Diacarb is also used for the prevention and treatment of mountain sickness. Its action is associated with an increase in the removal of carbon dioxide from the body, which helps to adapt to the changed environmental conditions at high altitudes.
4. Treating other conditions: In some cases, carbonic anhydrase inhibitors may 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 physician and in compliance with the recommendations for dosage and use.

Indications Diacarb

1. 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.
2. Mountain sickness: Diacarb is used to prevent and treat mountain sickness (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.
3. Epilepsy: Sometimes Diacarb can be used as an additional treatment for some forms of epilepsy.
4. Acidosis: The drug may be prescribed to correct some forms of acidosis associated with diseases such as kidney stones or diabetes.
5. Prevention of altitude sickness: Diacarb can be used as a preventative measure before traveling to high altitudes to prevent symptoms of altitude sickness.
6. Migraine: In some cases, Diacarb may be prescribed for the prevention of migraines.

Release form

1. Tablets: This is the most common form of Diacarb. Tablets can have different dosages, for example, 125 mg, 250 mg or 500 mg.
2. Capsules: Some manufacturers may produce Diacarb in capsule form, especially if a slow release of the drug is required.
3. Powder for preparation of injection solution: In rare cases, Diacarb may be presented in the form of powder for preparation of injection solution.

Pharmacodynamics

1. Decreased bicarbonate formation: Acetazolamide inhibits bicarbonate formation in the kidneys, resulting in decreased formation of water-soluble bicarbonate and increased excretion of sodium, potassium, and water in the urine.
2. Diuretic action: Blocking carbonic anhydrase in the kidneys results in 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.
3. Decreased hydrogen secretion: Acetazolamide also decreases hydrogen secretion in the kidneys, which promotes the production of urine with a higher pH, which may be useful in the treatment of acid-related kidney stones.
4. Stimulation of Respiration: At high doses, acetazolamide may stimulate respiration by increasing the sensitivity of the respiratory centers in the brain to changes in the level of carbon dioxide in the blood.
5. Reducing intraocular pressure: Acetazolamide can also be used to lower intraocular pressure, which is useful in the treatment of glaucoma.

Pharmacokinetics

1. Absorption: After oral administration, acetazolamide is rapidly and completely absorbed from the gastrointestinal tract.
2. Maximum concentration (Cmax): The time to reach the maximum concentration of acetazolamide in the blood plasma is usually about 1-4 hours after administration.
3. Bioavailability: The bioavailability of acetazolamide after oral administration is generally high, approximately 80-100%.
4. Metabolism: Acetazolamide is metabolized in the liver, primarily via hydroxylation.
5. Elimination half-life (T½): The elimination half-life of acetazolamide in the body is approximately 8-12 hours.
6. Volume of distribution (Vd): The Vd of acetazolamide varies, but is typically around 0.7-0.9 L/kg, indicating good distribution of the drug into body tissues.
7. Excretion: Acetazolamide is excreted primarily via the kidneys as unchanged drug.
8. Metabolism interactions: Diacarb may interact with other drugs, in particular with other diuretics or antiepileptic drugs, which may change their effectiveness or blood levels.

Dosing and administration

1. Glaucoma:

   • The usual starting dose for adults is 250-1000 mg per day, divided into several doses.
   • Children may be prescribed a dose of 5 to 10 mg per 1 kg of body weight per day, also divided into several doses.

2. 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.

3. Mountain sickness:

   • To prevent altitude 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.

4. Hypokalemia:

   • For the treatment of hypokalemia, Diacarb can be used in a dose of 250-1000 mg per day, divided into several doses.

Use Diacarb during pregnancy

Using 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 from available research:

1. A study in pregnant women with idiopathic intracranial hypertension: In one study in which acetazolamide was used to treat this condition during pregnancy, no adverse pregnancy outcomes were reported. A review of the literature also found no convincing evidence of adverse effects of the drug on pregnancy in humans (Lee et al., 2005).
2. Another study: In a study of women with intracranial hypertension who were given acetazolamide during pregnancy, there was no convincing evidence of harmful effects on pregnancy, even when the drug was given before the 13th week of gestation. However, acetazolamide should be avoided during pregnancy unless absolutely necessary (Falardeau et al., 2013).

Because of the potential risks, use of acetazolamide during pregnancy should only be done under strict medical supervision and only when the benefits outweigh the possible risks.

Contraindications

1. Hypersensitivity: People with known hypersensitivity to acetazolamide or other sulfonamides should avoid its use.
2. Severe renal or hepatic impairment: The drug is contraindicated in patients with severe renal or hepatic impairment as it may worsen their condition.
3. Hyponatremia: Diacarb should be used with caution in patients with hyponatremia (low sodium levels in the blood) as it may worsen this condition.
4. 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.
5. Urolithiasis: In the presence of urolithiasis, Diacarb may increase the risk of stone formation and is contraindicated.
6. Diabetes mellitus: In patients with diabetes mellitus, the drug should be used with caution, as it may change blood sugar levels.
7. Pregnancy and breastfeeding: The use of Diacarb during pregnancy and breastfeeding should be assessed by a doctor, as data on its safety in these periods is limited.
8. Childhood: The use of Diacarb in children requires special caution and should be carried out under the supervision of a physician.
9. Use with other drugs: Before starting to use Diacarb in combination with other drugs, you should consult a doctor to ensure there are no potential interactions.

Side effects Diacarb

1. 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.
2. Increased sensitivity to light: Some people may experience increased sensitivity to light while taking Diamox, which may lead to photosensitivity or faster eye fatigue.
3. Loss of appetite and diarrhea: Some patients may experience loss of appetite, nausea or diarrhea while taking Diacarb.
4. Electrolyte disturbances: The drug may cause changes in electrolyte levels in the body, such as hypokalemia (low potassium) or hyponatremia (low sodium).
5. Hypersensitivity to allergens: Some people may experience allergic reactions to Diacarb, such as skin rash, itching or angioedema.
6. Stomach disorders: May include nausea, vomiting, heartburn, or abdominal discomfort.
7. Metallic taste: Some patients may complain of a metallic taste in the mouth.
8. Other rare side effects: Include anemia, aplastic anemia, thrombocytopenia, alkalosis, hyperhydration and others.

Overdose

1. Electrolyte imbalance: Excessive loss of electrolytes (eg, sodium, potassium) in the urine can lead to electrolyte imbalance, which can manifest as weakness, abnormal heart rhythms, muscle cramps, and other symptoms.
2. 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.
3. 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.
4. Other complications: Possible complications of overdose may also include hypoglycemia, hyperkalemia, deterioration of renal function and other serious complications.

Interactions with other drugs

1. Anhydrase inhibitors: Diacarb is an anhydrase inhibitor, so its effect may be enhanced when used concomitantly with other drugs such as acetazolamide, dorzolamide and brinzolamide, which may increase the risk of developing side effects associated with anhydrase inhibition, such as metabolic acidosis.
2. Epilepsy medications: Diacarb may interact with epilepsy medications such as phenytoin, carbamazepine and valproic acid, which may increase or decrease their effectiveness and increase the risk of side effects associated with the central nervous system.
3. Medicines for the treatment of hypertension and cardiovascular diseases: Diacarb can enhance the effect of medicines used to treat hypertension, such as diuretics or angiotensin-converting enzyme inhibitors (ACEIs), which can lead to a strong decrease in blood pressure.
4. Medicines for diabetes: Diacarb may enhance the effect of hypoglycemic drugs such as sulfonylurea, which may lead to a decrease in blood sugar levels.
5. Gout medications: Diacarb may enhance the effects of medications used to treat gout, such as probenecid, which may lead to increased uric acid levels in the blood and increased side effects.