toxylact: A02ad05 almasilate

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TOXICOLOGY-LACTOLOGY MONOGRAPH — ALMASILATE

ATC Code: A02AD05

CHEMICAL IDENTIFICATION

Almasilate is a buffering antacid consisting of a crystalline polyhydrate of aluminium and magnesium silicate. Its chemical composition comprises 2 atoms of aluminium and 1 atom of magnesium in the molecular structure. The molecular weight of almasilate is approximately 252 kilodaltons. The molecular formula is given as Al₂MgO₈Si₂, with a molecular weight of 262.43 g/mol according to DrugCentral. It is classified under 21 CFR 331.15 as a combination antacid active ingredient for over-the-counter human use.

PHARMACOLOGICAL PROPERTIES

Almasilate acts as an effective antacid by binding hydrogen ions within its polymeric silicate structure, thereby neutralizing excess gastric hydrochloric acid. In addition to its acid-neutralizing capacity, almasilate exhibits the property of binding bile acids in the gastric lumen, which renders it particularly suitable for the treatment of biliary gastritis. It has been used therapeutically for peptic ulcers and dyspepsia, although its efficacy has been noted to be lower than that of other approved antacids.

TOXICOLOGICAL PROFILE

The toxicological profile of almasilate is primarily determined by its aluminium content. Absorbed amounts of aluminium tend to accumulate in adipose tissues, resulting in a more prolonged elimination from the human body. The absorbed fraction of aluminium is eliminated renally; consequently, patients with renal impairment are at particular risk of aluminium accumulation, which may lead to osteomalacia, encephalopathy, microcytic hypochromic anaemia, and adynamic bone disease.

Aluminium absorption from antacid preparations is potentiated when taken concomitantly with certain fruit juices (e.g., grapefruit juice) or when formulated as effervescent tablets. Standard daily doses of aluminium-containing antacids may be associated with absorption of approximately 100 to 500 micrograms of aluminium, which can approximately double plasma concentrations in individuals with normal renal function.

Magnesium, the second cationic component, is minimally absorbed from the gastrointestinal tract. The absorbed fraction is excreted in the urine, and forced diuresis enhances its elimination. No specific systemic toxic effects have been independently attributed to almasilate itself.

USE DURING PREGNANCY

Almasilate is classified as FDA Pregnancy Category C. This classification indicates that animal reproduction studies are either unavailable or have demonstrated an adverse effect on the fetus, and there are no adequate and well-controlled studies in humans. While antacids are generally considered to pose a low risk during pregnancy, heavy or frequent use should be avoided, and the maximum recommended dose should not be exceeded.

USE DURING LACTATION

Toxicological Lactation Category: III — Almasilate is relatively unsuitable for use during the lactation period. It is recommended to await complete elimination of the drug from the maternal plasma before resuming breastfeeding.

This classification is based primarily on the aluminium component. Although aluminium is present naturally in breast milk and does not appear to accumulate in it, the unique pharmacokinetic property of almasilate — namely, the tendency of absorbed aluminium to accumulate in fatty tissues with prolonged elimination — raises concern for the breastfed infant. Infants, particularly those with immature renal function, may be more susceptible to elevated plasma aluminium concentrations.

By contrast, general antacid use during breastfeeding is widely considered acceptable, with extensive clinical experience supporting the safety of aluminium- and magnesium-based antacids in nursing mothers. However, the specific tissue-distribution characteristics of almasilate warrant a more cautious approach.

CONTRAINDICATIONS AND PRECAUTIONS

  • Contraindicated in patients with renal impairment due to risk of aluminium accumulation and toxicity.
  • Avoid concomitant use with fruit juices (especially grapefruit juice) and effervescent formulations, which may increase aluminium absorption.
  • Aluminium-containing antacids may interact with other medications (e.g., quinolone antibiotics such as pefloxacin) by reducing their plasma levels.
  • Excessive doses may lead to phosphate depletion, increased bone resorption, hypercalciuria, and risk of osteomalacia.
  • Prolonged use may cause constipation due to the astringent properties of aluminium salts.

KEY REFERENCES

  • WHO Collaborating Centre for Drug Statistics Methodology. ATC/DDD Index: A02AD05 almasilate.
  • DrugBank. Almasilate (DB13595).
  • FDA National Center for Toxicological Research. ALMASILATE (UNII: OZQ8O62H53).
  • NCBI LactMed. Antacids and Breastfeeding (NBK501322).
  • NHS Specialist Pharmacy Service. Treating heartburn and dyspepsia during breastfeeding.

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