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General Description:

Almasilate, identified by CAS number 71205-22-6, is a notable compound with significant therapeutic applications. Almasilate is a buffering antacid that has been used in peptic ulcers and dyspepsia. It is a crystalline polyhydrate of aluminium/magnesium silicate and mediates its buffering activity by binding hydrogen ions within the polymer. However its therapeutic efficacy is not comparable to other approved antacids, as it is no more effective in neutralizing acid and binding bile salts than other conventional antacids . Given that there are generally more widely available conventional antacids that are just as - if not more - effective than almasilate, almasilate products are only available in certain parts of Europe and/or Asia.

Indications:

This drug is primarily indicated for: Almasilate is indicated for use as an antacid for the neutralization of excess stomach acid . It is subsequently also used for the symptomatic treatment of diseases where it is necessary to neutralize acid in the stomach, for example, for treating stomach and duodenal ulcers or heartburn and stomach conditions caused by excess stomach acid . Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Metabolism:

Almasilate undergoes metabolic processing primarily in: Once aluminum has entered the body, the mechanism by which it is metabolized is still not fully known . Conversely, magnesium balance in the body is predominantly managed via a balance between intestinal absorption, exchange with bone, and renal excretion . This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.

Absorption:

The absorption characteristics of Almasilate are crucial for its therapeutic efficacy: In regards to aluminum-containing antacids like the aluminum-magnesium complex almasilate, it is reported that the bioavailability of ingested aluminum from such antacids is only between 0.01-1% . Additionally, while the optimal absorption of magnesium appears to be in the small intestine and particularly in the ileum and jejunum, with some absorption in the colon, it is believed that the transfer of magnesium from blood to extravascular space is quick and efficient . The drug's ability to rapidly penetrate into cells ensures quick onset of action.

Half-life:

The half-life of Almasilate is an important consideration for its dosing schedule: Readily accessible data regarding the half-life of almasilate is not available. This determines the duration of action and helps in formulating effective dosing regimens.

Protein Binding:

Almasilate exhibits a strong affinity for binding with plasma proteins: Once present in the bloodstream, 60% of aluminum is bound to transferrin proteins, 34% is bound to albumin protein, and the remainder is bound to citrate in the normal human blood serum . Furthermore, 33% of serum magnesium is bound to protein, where approximately 75% of the protein bound fraction of magnesium is bound to albumin and the remaining 25% to globulins . This property plays a key role in the drug's pharmacokinetics and distribution within the body.

Route of Elimination:

The elimination of Almasilate from the body primarily occurs through: The routes of excretion of aluminum in the body are mainly from the kidneys, which account for 95% of the elimination . Magnesium is largely excreted in the urine . Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.

Volume of Distribution:

Almasilate is distributed throughout the body with a volume of distribution of: The distribution of aluminum can occur in the bones, lungs, spleen, liver, kidney, nervous tissues, muscles, the blood itself, and the heart . The highest levels of aluminum in mammalian tissues are found in the skeleton, lungs, kidneys, spleen, thyroid, and parathyroid glands . Conversely, approximately half of the total magnesium in the body is distributed intracellularly in soft tissue and the other half is present in the bones . Less than 1% of the total magnesium content is present in the blood . In pregnant women, apparent volumes of distribution were evidently observed to range from 0.250 to 0.442 L/kg . This metric indicates how extensively the drug permeates into body tissues.

Clearance:

The clearance rate of Almasilate is a critical factor in determining its safe and effective dosage: Readily accessible data regarding the clearance of almasilate is not available. It reflects the efficiency with which the drug is removed from the systemic circulation.

Pharmacodynamics:

Almasilate exerts its therapeutic effects through: Various non-prescription antacid products are available to the general public to purchase and use as a treatment for relieving the occasional, limited, and non-severe sensation of heartburn (or acid indigestion) that may frequently be associated with stomach indigestion (or dyspepsia) or gastroesophageal reflux disease (when stomach contents may rise back up into the esophagus and cause a taste of acid in the back of the mouth, among other symptoms) . Subsequently, when excessive amounts of acids are produced in the stomach (either owing to indigestion or acid reflux, for example), the natural mucous barrier protecting the lining of the stomach can be damaged . Antacids like almasilate consequently contain alkaline ions that chemically neutralize such stomach gastric acids, providing relief to heartburn, relieving pain, and reducing damage in the area . The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Almasilate functions by: Almasilate is a crystalline polyhydrate of aluminum/magnesium silicate and mediates its buffering activity by binding hydrogen ions within the polymer . Specifically, the aluminosilicate minerals dissolve, and in doing so consume acidic hydrogen ions and release moieties like H4SiO4, Al3+, and other cations, including the magnesium associated with the compound . Almasilate consequently contributes to the overall acid-neutralization by consuming acid hydrogen ion in this way . Additionally, aluminum and other metals released from the original compound may also accumulate into secondary aluminum and magnesium based antacid like products that can act as secondary pH buffers . This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Toxicity:

Classification:

Almasilate belongs to the class of inorganic compounds known as post-transition metal silicates. These are inorganic compounds in which the largest oxoanion is silicate, and in which the heaviest atom not in an oxoanion is a post-transition metal, classified under the direct parent group Post-transition metal silicates. This compound is a part of the Inorganic compounds, falling under the Mixed metal/non-metal compounds superclass, and categorized within the Post-transition metal oxoanionic compounds class, specifically within the Post-transition metal silicates subclass.

Categories:

Almasilate is categorized under the following therapeutic classes: Alimentary Tract and Metabolism, Aluminum and magnesium containing antacids, Antacids, Drugs for Acid Related Disorders, Drugs that are Mainly Renally Excreted, Gastric Acid Lowering Agents, Minerals, Pharmaceutic Aids, Silicon Compounds. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.