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DIAMOX ® Acetazolamide

DIAMOX ® is an acetazolamide based drug

THERAPEUTIC GROUP: Diuretics / Diuretics carbonic anhydrase inhibitors

IndicationsAction mechanismStudies and clinical effectiveness Usage and dosage instructionsWarnings Pregnancy and lactationInteractionsContraindicationsUndesirable effects

Directions DIAMOX ® Acetazolamide

DIAMOX ® is indicated for the treatment of edematous condition due to heart failure, with particular efficacy in improving pulmonary edema and related dyspnea in case of left heart failure. DIAMOX ® has also proved useful in reducing the endocular pressure typical of glaucoma and in assisting antiepileptic therapy, for which particular improvements have been observed especially for younger patients suffering from less aggressive forms.

Mechanism of action DIAMOX ® Acetazolamide

DIAMOX ® is taken orally and rapidly absorbed in the stomach. Maximum levels of its active ingredient, acetazolamide, are observed approximately 2 hours after oral administration, while urinary excretion becomes particularly consistent between the eighth and twelfth hours.

Before being excreted intact in the urine, acetazolamide acts at the level of the proximal convoluted tubule of the nephrons, inhibiting an enzyme expressed by these cells, known as carbonic anhydrase. The aforementioned enzyme catalyzes a very important reversible reaction for maintaining the acid-base balance and for controlling the reabsorption of sodium, which allows hydrating carbon dioxide to carbonic acid (CO2 + H20 → H2CO3). The carbonic acid thus formed can dissociate into bicarbonate and proton ion, which will be exchanged for sodium ions, which can thus be effectively reabsorbed.

The inhibitory action of DIAMOX on carbonic anhydrase, therefore indirectly prevents a reabsorption of bicarbonate and sodium, increasing its urinary excretion and diuresis. As an associated effect we are witnessing an inevitable alkalinization of the urine and a slight blood acidosis.

Studies carried out and clinical efficacy

1 ACETAZOLAMIDE AND MOUNTAIN DISEASES

Acute mountain sickness is a very frequent condition among trekkers, due to a difficult acclimatization dictated by the gradual and constant reduction of oxygen levels, which manifests itself with a complex symptomatology including headache. Acetazolamide at this juncture is particularly important, as inducing a slight haematic acidification stimulates the respiratory system to a more effective gas exchange. This study conducted on 143 trekkers at an altitude of about 4, 000 meters showed that 85mg of acetazolamide could have the same effect on improving headache as 600 mg of ibuprofen, also presenting a protective preventive effect against pulmonary and cerebral edema.

2. ACETAZOLAMIDE AND FUTURE PROSPECTS FOR GLAUCOMA

The administration of acetazolamide is particularly important for the treatment of optical glaucoma, thanks to its ability to reduce intraocular pressure. However, the oral administration of this drug subjects the patient suffering from glaucoma to a series of side effects which significantly reduce the relationship between benefits and costs. For this reason, and given the efficacy of acetazolamide therapy, new administration protocols are being developed that include the typical ocular intake of the aforementioned drug and reduce systemic side effects.

3. ACETAZOLAMIDE IN PEDIATRIC USE

This important study shows one of the most important limitations of acetazolamide treatment in pediatric glaucoma. More precisely - despite the effectiveness of the drug in improving the pathology and the very low invasiveness compared to surgery - the most important limit to its spread in the pediatric environment is given by the delay in induced growth. In fact, during therapy there is a low weight gain probably associated with the acidosis caused by the drug. However, to fully understand the complexity of reactions that develop during this period, it would be necessary to monitor other parameters important for the child's growth.

Method of use and dosage

DIAMOX ® acetazolamide 250 mg tablets / 500 mg capsules there acetazolamide:

  1. To control the edema, we suggest about 1 tablet and a half a day, preferably taken in the morning.
  2. For the treatment of glaucoma we recommend instead 2 to 3 capsules a day, or a tablet taken at 4/6 hour intervals.
  3. For the treatment of epilepsy, in the case of adjuvant therapy generally 1 tablet per day is used; dose that can grow based on the combined therapy and the patient's situation.

In any case the correct dosage should be formulated by the doctor, after a careful evaluation of the patient's physiopathological conditions.

IN ANY CASE, BEFORE TAKING DIAMOX ® Acetazolamide - THE REQUIREMENT AND CHECK OF YOUR DOCTOR IS NECESSARY.

Warnings DIAMOX ® Acetazolamide

The diuretic and saluretic action of DIAMOX ® requires constant monitoring of some blood parameters such as: blood count, sodium, potassium, pH and even glycaemia in patients with diabetes mellitus, both before and during administration. It is also necessary to consider that the treatment with acetazolamide, especially if prolonged or incorrectly dosed, could determine an alteration of the electrolyte and acid-base balance, with possible hyponatremia, hypokalemia and metabolic acidosis.

DIAMOX ® must therefore be used with particular care in the case of patients with chronic obstructive pulmonary disease and emphysema, as a possible acidosis could contribute to the onset of tachypnea, anorexia, drowsiness, lethargy and in more severe cases even to coma.

Acetazolamide, structurally part of the sulfonamides, could be responsible for toxic epidermal necrolysis, aplastic anemia, agranulocytosis and other anaphylactic reactions in patients hypersensitive to these compounds.

The administration of DIAMOX ® could cause drowsiness, confusion or otherwise alter the patient's normal perceptive and reactive qualities, altering driving skills and the use of machinery.

PREGNANCY AND BREASTFEEDING

Experimental data regarding the use of DIAMOX ® and more generally of acetazolamide in pregnancy, suggest to avoid its use during the first trimester, limiting subsequently the assumption only in case of inevitable need. In fact, while human studies do not show embryotoxic or teratogenic effects at doses of 250 mg / day, those conducted on laboratory animals have resulted in animal neonates with serious functional impairment and limb deformity.

Acetazolamide is also, although to a small extent, secreted intact in breast milk; therefore it is recommended to stop breast-feeding during the administration of DIAMOX ®

Interactions

DIAMOX ® may alter the functionality of different drugs such as:

  1. Aspirin and lithium salts, causing an increased elimination, consequently a reduction of the therapeutic effects;
  2. Amphetamines and tricyclic antidepressants, increasing their functionality following reduction of their excretion;
  3. Mercurials and other diuretics, with a consequent increase in diuresis;
  4. Phenytoin (antiepileptic drug), increasing its plasma levels;
  5. Cyclosporine, with increased plasma levels.
  6. Antidiabetic, causing an alteration of the glycemic profile.

Furthermore, acetazolamide can cause an increase in crystals in urine and kidney stones in conjunction with sodium bicarbonate therapy.

Contraindications DIAMOX ® Acetazolamide

Given the biological action of DIAMOX ® its intake is not recommended in the case of acidosis, alteration of the electrolyte balance (hyponatremia and hypopotaxemia), hepatic, renal or adrenal insufficiency, and in case of hypersensitivity to one of its components.

Undesirable effects - Side effects

Most of the side effects of DIAMOX ® are observed in the initial phase of therapy and include:

  1. Paresthesia, tingling, decreased appetite, hearing impairment, nausea, vomiting, diarrhea, polyuria and in more serious cases also drowsiness and confusion.

Prolonged therapy with DIAMOX ® can lead to an alteration of the electrolyte and acid-base balance, which can be remedied by the administration of bicarbonate, which however exposes the patient to a greater risk of kidney stones.

Haematological effects, characterized by agranulocytosis, leukopenia, thrombocytopenia, hypoglycemia, hyponatremia and hypokalemia were also observed.

To the side effects just listed it is then necessary to add all those due to hypersensitivity towards acetazolamide, such as: skin rashes, fever, anaphylactic reactions, erythema, myelosuppression and associated syndromes.

Note

DIAMOX ® is salable only under medical prescription.

The use of DIAMOX ® should always take place after consulting your doctor.

The indiscriminate use of DIAMOX ® between athletes and non-athletes, in the search for the loss of a few pounds, exposes the body to serious side effects. Furthermore, it is always advisable to reiterate that weight loss is dictated by the elimination of liquids and salts and not by a real weight loss effect, understood as a loss of fat mass.

Therefore DIAMOX ® is classified among the substances DOPANTI.

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