For the use of a Registered Medical Practitioner, Hospital or Laboratory only.
1. Description
Aplazar contains all amino acids essential for uraemic patients, five out of them are keto or hydroxyanalogue in the form of calcium salts. Therefore it allows reduction in the nitrogen supply and provides calcium. It is a medication for chronic kidney disease patients on conservative management, generally with a glomerular filtration rate (GFR) below 25 mL/min. In combination with very low protein diet / low protein diet, it helps in delaying the progression of kidney disease in the Predialysis period.
2. Composition
One film-coated tablet contains:
- Calcium-3-methyl-2-oxovalerate (α-ketoanalogue of isoleucine, Calcium salt) 67 mg
- Calcium-4-methyl-2-oxovalerate (α-ketoanalogue of leucine, Calcium-salt) 101 mg
- Calcium-2-oxo-3-phenylpropionate (α-ketoanalogue of phenylalanine, Calcium-salt) 68 mg
- Calcium-3-methyl-2-oxobutyrate (α-ketoanalogue of valine, Calcium-salt) 86 mg
- Calcium-DL-2-hydroxy-4-(methylthio)-butyrate (α-hydroxyanalogue of methionine, Calcium salt) 59 mg
- L-lysine 75 mg
- L-threonine 53 mg
- L-tryptophan 23 mg
- L-histidine 38 mg
- L-tyrosine 30 mg
3. Dosage Form
Film-coated Tablet
4. Pharmacology
Pharmacodynamics
Aplazar contains α-ketoanalogues (or hydroxyanalogues) of essential amino acids along with selected essential amino acids. These ketoanalogues are nitrogen-free precursors that are converted into essential amino acids in the body by transamination, utilising nitrogen from non-essential amino acids or other nitrogenous compounds.
Mechanism of action
Supplies precursors of essential amino acids without adding significant nitrogen.
Reduces production and accumulation of nitrogenous waste products such as urea, thereby decreasing uraemic symptoms.
Helps maintain protein synthesis despite dietary protein restriction.
Promotes a positive or improved nitrogen balance.
May slow the progression of CKD when used with a low-protein diet.
Provides calcium because the ketoanalogues are present as calcium salts.
Pharmacokinetics
Absorption: The amino acids and ketoanalogues are absorbed from the gastrointestinal tract. Administration during meals is recommended to optimise absorption and conversion into essential amino acids.
Distribution: After absorption, the ketoanalogues are distributed into body tissues where they participate in amino acid metabolism.
Metabolism: Ketoanalogues undergo transamination to form their corresponding essential amino acids using endogenous amino groups. This process minimises additional nitrogen intake while supporting protein synthesis.
Elimination: The metabolites enter normal amino acid metabolic pathways. Because less nitrogen is introduced than with conventional amino acid supplements, urea generation is reduced, decreasing the nitrogenous waste burden in CKD patients.
5. Indications
Prevention and therapy of damages due to faulty or deficient protein metabolism in chronic renal insufficiency in connection with limited protein in food of 40 g per day (for adults) and less; i.e. generally in patients with a glomerular filtration rate (GFR) below 25 mL/min.
6. Contraindications
Hypercalcaemia, disturbed amino acid metabolism. In case of hereditary phenylketonuria it has to be taken into account that this product contains phenylalanine.
7. Precautions
No experience has been made so far with the application in pregnancy and paediatrics. Aplazar should be taken during meals to allow proper absorption and metabolism into the corresponding amino acids. The serum calcium level should be monitored regularly. An adequate supply of calories should be ensured.
8. Drug Interactions
Simultaneous administration of medicinal products that contain calcium (e.g. acetolyte) may trigger, or worsen, a pathological increase in the serum calcium level.
As the uraemic symptoms improve under therapy with Aplazar tablets, the dose of aluminium hydroxide administered should be reduced, as appropriate. The patient should be monitored for reduced levels of serum phosphate.
In order not to interfere with absorption, an appropriate interval should be observed between administration of Aplazar tablets and medicinal products which form poorly soluble compounds with calcium (e.g. tetracyclines, quinolones such as ciprofloxacin and norfloxacin, preparations that contain iron, fluoride and estramustine). An interval of at least 2 hours should be observed between the intake of Aplazar tablets and such preparations.
If administration of Aplazar tablets leads to increased blood levels of calcium, the sensitivity to medicinal products which increase heart action (cardiac glycosides) and thus also the risk of cardiac arrhythmia is increased.
9. Adverse Effects
Hypercalcaemia may develop. In this case, it is recommended to decrease vitamin D intake. If the hypercalcaemia persists, reduce the dosage of Aplazar as well as any other source of calcium.
10. Dosage & Administration
In general, unless prescribed otherwise, four to eight tablets are swallowed whole three times daily during meals. This dosage applies to adults (70 kg bodyweight) (1 tablet/5 kg body weight/day).
11. Overdosage
No data available.
12. Storage
- Keep out of the reach of children
- Do not store above 25°C
- Protect from moisture
13. Presentation
10 tablets in a strip, 10 strips in a Box.