Tolazamida

A: Tolazamide is a first-generation sulfonylurea drug that primarily acts on pancreatic β-cells by binding to sulfonylurea receptors (SUR1) on the cell membrane. [, , ] This binding blocks ATP-sensitive potassium channels, leading to membrane depolarization and the opening of voltage-gated calcium channels. [, , ] The influx of calcium ions triggers the exocytosis of insulin granules, increasing insulin secretion into the bloodstream. [, , ] This effectively lowers blood glucose levels, particularly in individuals with non-insulin-dependent diabetes mellitus (NIDDM), also known as type 2 diabetes. [, , ]

A:

• Molecular Formula: C₁₄H₂₁N₃O₃S []
• Molecular Weight: 311.4 g/mol []
• Spectroscopic Data: Key spectroscopic features include infrared (IR) and Raman spectra which provide information on functional group vibrations. [] Nuclear magnetic resonance (NMR) spectroscopy would be valuable to determine the structure and conformation. Single-crystal X-ray diffraction studies have been employed to fully elucidate the crystal structures of Tolazamide polymorphs. []

A: Tolazamide exists in different polymorphic forms, which can impact its stability and dissolution rate. [, ] Research suggests that specific amphiphilic block copolymers, like poly(ethylene glycol)-block-poly(lactic acid) (PEG-b-PLA), can act as crystal habit modifiers, influencing the shape of Tolazamide crystals during crystallization. [] This modification may be beneficial in optimizing pharmaceutical formulations.

ANone: Tolazamide is not typically recognized for its catalytic properties. Its primary mode of action revolves around binding to specific biological targets rather than catalyzing chemical reactions.

A: Yes, computational methods, including Density Functional Theory (DFT) calculations, have been used to investigate the potential of Tolazamide and related sulfonylurea compounds as corrosion inhibitors for copper in nitric acid solutions. []

A: While specific SAR studies on Tolazamide modifications are limited in the provided research, it is known that structural differences within the sulfonylurea class of drugs (including Tolazamide) contribute to variations in their pharmacological properties such as duration of action, potency, and metabolism. []

A: Tolazamide stability is influenced by factors such as pH and the presence of excipients. [] Research indicates that the block copolymer PEG-b-PLA can alter Tolazamide's crystal habit, potentially influencing its dissolution rate and bioavailability. [] Formulation approaches would likely focus on controlling crystal form and particle size to optimize drug release and absorption.

ANone: As a pharmaceutical compound, Tolazamide would be subject to stringent SHE regulations during its manufacturing, handling, and disposal. Specific regulations would vary based on geographical location and governing bodies.

A: Tolazamide is well-absorbed after oral administration, with peak serum concentrations reached within 3-4 hours. [] It is extensively metabolized in the liver, primarily via oxidation and conjugation, with metabolites excreted in urine and feces. [] Its elimination half-life is approximately 7 hours. [] Tolazamide's primary pharmacodynamic effect is the stimulation of insulin secretion from pancreatic β-cells, leading to a reduction in blood glucose levels. [, , ]

A: Numerous studies have explored the efficacy of Tolazamide in the treatment of NIDDM. Animal studies using rat models have demonstrated that Tolazamide potentiates insulin action in the liver and adipose tissue. [, , ] Clinical trials have shown its effectiveness in improving glycemic control in NIDDM patients, both as monotherapy and in combination with insulin. [, , , , , , , , ]

A: Secondary failure to sulfonylureas, including Tolazamide, can occur in NIDDM patients, indicating a decline in drug effectiveness over time. [] This could be attributed to several factors, including a progressive decline in β-cell function and reduced insulin sensitivity. []

A: While generally considered safe for its intended use, Tolazamide, like all medications, can cause side effects. [, , ] The most common adverse effects are hypoglycemia, gastrointestinal disturbances, and skin reactions. [, , ] In rare instances, more serious side effects like cholestatic jaundice and hepatic dysfunction have been reported. [, ]

A: Various analytical techniques have been employed to study Tolazamide. High-pressure liquid chromatography (HPLC) is a common method for quantifying Tolazamide levels in biological fluids. [] Gas chromatography (GC) has also been used to determine Tolazamide concentrations in plasma. []

ANone: The provided research does not offer specific details on the environmental impact of Tolazamide. As a pharmaceutical compound, its presence in the environment and potential effects would require further investigation.

A: Research has shown that Tolazamide's dissolution rate varies significantly between different tablet formulations. [] This difference highlights the importance of considering formulation factors when assessing its bioavailability and efficacy.

A: Analytical methods for quantifying Tolazamide, such as HPLC and GC, have established validation procedures. [, ] These procedures ensure the accuracy, precision, and specificity of the methods used for drug analysis.

ANone: As a pharmaceutical product, Tolazamide production is subject to strict quality control and assurance measures throughout its lifecycle, from development and manufacturing to distribution. These measures ensure product consistency, safety, and efficacy.

ANone: The research provided does not focus on the immunogenicity of Tolazamide. Further research would be needed to investigate any potential immune responses associated with its use.

ANone: The provided research does not specifically address drug-transporter interactions involving Tolazamide. Further investigation would be required to understand the role of transporters in its pharmacokinetic profile.

ANone: The research provided does not directly address the biocompatibility or biodegradability of Tolazamide. Further research would be needed to evaluate its long-term effects on biological systems and its environmental fate.

A: Several other sulfonylurea drugs, such as Glibenclamide and Glipizide, are available as alternatives to Tolazamide. [] These drugs share a similar mechanism of action but may differ in their potency, duration of action, and side effect profiles. Biguanides, such as Metformin, represent another class of antidiabetic drugs with a distinct mechanism of action. [] The choice of medication depends on individual patient factors and should be determined by a healthcare professional.

ANone: Specific guidelines for the recycling and waste management of Tolazamide would likely fall under pharmaceutical waste regulations, which vary depending on location. Proper disposal practices are crucial to minimize environmental contamination.

ANone: Research on Tolazamide can benefit from various infrastructure and resources, including:

A: Tolazamide, introduced in the 1960s, belongs to the first generation of sulfonylurea drugs developed for treating type 2 diabetes. [] Its introduction marked a significant advancement in diabetes management by providing an oral alternative to insulin injections. Research on Tolazamide has contributed to a better understanding of pancreatic β-cell function, insulin secretion mechanisms, and the pathogenesis of type 2 diabetes.