Description and composition of Axytex
Table of Contents
Axytex is a diuretic and a carbonic anhydrase inhibitor. It contains acetazolamide as its active ingredient. It also contains inactive ingredients called excipients in sufficient quantities.
It usually comes as tablets and injections. It also come in different strengths expressed in mg.
Axytex is a nonbacteriostatic sulfonamide possessing a chemical structure and pharmacological activity distinctly different from the bacteriostatic sulfonamides.
Acetazolamide is an enzyme inhibitor that acts specifically on carbonic anhydrase, the enzyme that catalyses the reversible reaction involving the hydration of carbon dioxide and the dehydration of carbonic acid.
In the eye, this inhibitory action of acetazolamide decreases the secretion of aqueous humour and results in a drop in intraocular pressure, a reaction considered desirable in cases of glaucoma and even in certain nonglaucomatous conditions.
The diuretic effect of acetazolamide is due to its action in the kidney on the reversible reaction involving hydration of carbon dioxide and dehydration of carbonic acid.
The result is renal loss of HCO3 ions, that carry out sodium, water and potassium. Alkalinization of the urine and promotion of diuresis are thus effected.
Alteration in ammonia metabolism occurs due to increased reabsorption of ammonia by the renal tubules as a result of urinary alkalinisation.
Acetazolamide is readily absorbed following oral administration and binds tightly to plasma proteins as well as to the enzyme carbonic anhydrase.
The drug does not undergo hepatic metabolism. It is renally excreted 100 percent as unchanged drug.
The duration of action is therefore affected directly by creatinine clearance (CrCl). Overall, clearance is dependent also on plasma protein binding.
Uses of Axytex
Axytex is used as an adjunct in the treatment of chronic open-angle glaucoma; secondary glaucoma; as part of pre-operative treatment of acute angleclosure glaucoma.
It is also used for the treatment symptoms of acute altitude sickness, seizures, epilepsy, and drug induced edema.
Safety and effectiveness of acetazolamide in children have not been established.
Dosage of Axytex
Administer Axytex tablets with food to reduce nausea. Note that absorption may be reduced slightly when this is done (administration with food).
1. Chronic open-angle glaucoma, secondary glaucoma:
- By mouth, adult 0.25-1 g daily in divided doses
- Daily dose for the treatment of seizures is 8-30 mg per kg in divided doses.
3. Congestive heart failure
- For the diuretic effect of acetazolamide, it is used in patients with CHF. Here, the starting dose is usually 250 to 375 mg administered once a day in the morning.
- Alternate days adminstration give better diuretic effect to CHF patients.
4. Acute altitude (mountain) sickness
Treatment here should start a day or two days before ascent for optimal result.
The usual recommended dose for the treatment of acute altitude sickness is 500 mg to 1000 mg per day in divided doses.
1000 mg is recommended in cases of rapid ascent.
Patients with creatinine clearance of more 50 ml/min [CrCl) > 50 mL/min]:
- No dosage adjustment required.
Patients with CrCl 10 to 50 mL/min:
- Reduce by half or increase the dosage interval to every 12 hours.
Patients with CrCl <10 mL/min:
- Avoid use. Acetazolamide is contraindicated in severe renal disease.
- Acetazolamide is contraindicated in patients with liver cirrhosis because it decreases ammonia clearance and increases the risk for hepatic encephalopathy.
- In patients with mild liver disease, dose adjustment of the drug is not necessary, since acetazolamide is not metabolized by the liver
Side effects of Axytex
The following are some notable side effects of acetazolamide:
- Taste disturbance
- Lss of appetite
- Reduced libido.
- Metabolic acidosis and electrolyte disturbances on long-term therapy
- Occasionally drowsiness
- Hearing disturbances
- Abnormal liver function
- Renal calculi
- Blood disorders including agranulocytosis and thrombocytopenia
- Rashes including Stevens-Johnson syndrome and toxic epidermal necrolysis
- Transient myopia reported
What to do while using Axytex
- Take tablets acetazolamide with food to reduce nausea and vomiting
- Report numbness or tingling of extremities to your physician
- Ability to perform tasks requiring mental alertness and/ or physical co-ordination may be impaired. Watch out for this and take precautionary measures.
- Drug may cause substantial increase in blood glucose in some diabetic patients. Watch out for this and take precautionary measures.
- Monitor blood count and electrolytes if used for long periods.
- Apply precautionary measure in the following conditions:
- Pulmonary obstruction;
- Diabetes mellitus;
- Hypersensitivity to acetazolamide, sulfonamides, or sulfonamide derivatives, or any of the excipients. Cross sensitivity between acetazolamide, sulfonamides and other sulfonamide derivatives is possible.
- Hyperchloraemic acidosis
- Suprarenal gland failure
- Impairment of renal function, CrCl <10 mL/min
- Marked liver disease or impairment of liver function, including cirrhosis because acetazolamide decreases ammonia clearance and increases the risk for hepatic encephalopathy.
- Long-term administration in patients with chronic non-congestive angle-closure glaucoma since it may permit organic closure of the angle to occur while the worsening glaucoma is masked by lowered intraocular pressure.
Pregnancy and Lactation
Axytex has been shown to be teratogenic (defects of the limbs) in mice, rats, hamsters and rabbits. There are no adequate and well-controlled studies in pregnant women.
Acetazolamide should not be used in pregnancy, especially during the first trimester. Acetazolamide should be used in pregnancy only if the potential benefit justifies the potential risk to the fetus. Consider other available alternatives before using acetazolamide in pregnancy.
Because of the potential for serious adverse reactions in nursing infants from acetazolamide, a decision should be made whether to discontinue nursing or to discontinue the drug taking into account the importance of the drug to the mother
Interactions of Axytex with other
- Aspirin: Increased risk of severe adverse effects including anorexia, tachypnea, lethargy, metabolic acidosis, coma, and death
- Metformin: Increased risk of lactic acidosis.
How to store Axytex
Store in a cool and dry place. Keep away from direct sunlight and the reach of the children.