What's the difference between amlodipine and amlodipine besylate
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Differences Between Amlodipine and Amlodipine Besylate
Introduction to Amlodipine and Amlodipine Besylate
Amlodipine is a widely used calcium channel blocker prescribed for the treatment of hypertension and angina pectoris. It is often formulated as amlodipine besylate to enhance its solubility and stability. This article explores the differences between amlodipine and its besylate salt form, focusing on their efficacy, tolerability, and pharmacokinetic profiles.
Chemical Composition and Solubility
Amlodipine Besylate
Amlodipine besylate is the most common form of amlodipine used in clinical practice. It is a salt formed by combining amlodipine with benzenesulfonic acid, which increases its water solubility and stability . This formulation ensures that the drug is more easily absorbed in the gastrointestinal tract, leading to consistent therapeutic effects.
Other Amlodipine Salts
Other salt forms of amlodipine, such as amlodipine adipate, camsylate, orotate, and maleate, have been developed to offer alternative formulations. These salts have been studied to compare their efficacy and tolerability with amlodipine besylate. For instance, amlodipine adipate and camsylate have shown similar efficacy and tolerability to amlodipine besylate in reducing blood pressure in patients with mild to moderate hypertension .
Efficacy in Blood Pressure Reduction
Comparative Studies
Several studies have compared the efficacy of different amlodipine salts with amlodipine besylate. For example, an 8-week study found that amlodipine adipate was noninferior to amlodipine besylate in reducing diastolic and systolic blood pressure. Similarly, amlodipine camsylate and orotate have demonstrated comparable efficacy to amlodipine besylate in lowering blood pressure .
Response Rates
The response rates, defined as the proportion of patients achieving target blood pressure levels, were also similar across different amlodipine salt formulations. Studies reported response rates of over 90% for both amlodipine adipate and besylate, indicating that both formulations are effective in managing hypertension .
Tolerability and Adverse Events
General Tolerability
The tolerability profiles of amlodipine besylate and other amlodipine salts are generally similar. Common adverse events include dizziness, headache, and peripheral edema. Studies have shown no significant differences in the incidence of adverse events between amlodipine besylate and other salt forms .
Specific Adverse Events
In a study comparing amlodipine orotate and besylate, the incidence of drug-related adverse events was low and comparable between the two groups. The most common adverse events were peripheral edema and headache, with no severe adverse events reported.
Pharmacokinetics and Bioequivalence
Absorption and Bioavailability
The pharmacokinetic profiles of amlodipine besylate and other amlodipine salts are similar, with no significant differences in absorption, bioavailability, or peak plasma concentrations. Studies have confirmed the bioequivalence of amlodipine besylate with other formulations, such as amlodipine maleate, indicating that they can be used interchangeably in clinical practice .
Food Effects
Food intake does not significantly affect the pharmacokinetics of amlodipine besylate. Studies have shown that the exposure of amlodipine besylate remains consistent whether taken with or without food, ensuring reliable therapeutic effects.
Conclusion
Amlodipine besylate is a well-established formulation of amlodipine, known for its enhanced solubility and stability. Comparative studies have shown that other amlodipine salts, such as adipate, camsylate, orotate, and maleate, offer similar efficacy and tolerability profiles. The pharmacokinetic properties of these formulations are also comparable, making them viable alternatives to amlodipine besylate. Overall, the choice between amlodipine besylate and other salt forms can be based on availability and patient preference, as their clinical outcomes are largely equivalent.
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