Prodrugs in Cardiovascular Medicine

Thijssen, H. H. W.; Drieman, Hans C.

doi:10.1111/j.1527-3466.1990.tb00404.x

Cited by 3 publications

(3 citation statements)

References 91 publications

(73 reference statements)

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“…The phosphate ester is proposed to get activated by the renal alkaline phosphatases [88]. On oral administration to dogs, it has shown selective renal vasodilatory action and is under clinical investigation for the treatment of renal failure and essential hypertension [84].…”

Section: Prodrugs Of Dopamine Receptor Ago-nist (Table 4)mentioning

confidence: 99%

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Prodrug Strategies for Antihypertensives

Dhaneshwar¹,

Sharma²,

Patel³

et al. 2011

CTMC

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There is a great emphasis on research to discover methods aimed at enhancing the efficacy of drugs and reducing their toxicity and unwanted side effects. Prodrugs are biologically inactive compounds that are converted to actual drug molecule, through biotransformation, that combine with the receptors to produce the biological action. Prodrugs can thus be considered as drugs containing specialized nontoxic protective groups utilized in a transient manner to alter or eliminate the undesirable properties of the parent drug molecule. Hypertension is one of the leading risk factors for cardiovascular disease and represents a major health and economic burden. Most of the drugs for cardiovascular diseases have low oral bioavailability, short duration of action, first pass metabolism and variable lipohilicities. Out of the need to overcome these limitations, various prodrugs have been designed for antihypertensive agents. This review extensively focuses on various strategies used for design and development of prodrugs for the various classes of antihypertensives, emphasizing on the details regarding the need for prodrug synthesis for each class, structure, type of modification and goal achieved. It also provides an insight into the major advances in the field of antihypertensive prodrug research.

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Section: Prodrugs Of Dopamine Receptor Ago-nist (Table 4)mentioning

confidence: 99%

“…It is activated by intestinal and hepatic plasma esterases to epinine, an active compound with properties very similar to DA. The isobutyryl carrier protects epinine from extensive first pass metabolism and increases its oral bioavailability three times in plasma than oral epinine [88][89].…”

Section: Prodrugs Of Dopamine Receptor Ago-nist (Table 4)mentioning

confidence: 99%

Prodrug Strategies for Antihypertensives

Dhaneshwar¹,

Sharma²,

Patel³

et al. 2011

CTMC

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“…Although only one review [ 4 ] was found that discusses the role of prodrugs in cardiovascular therapy, it is important to highlight that in the last seven years produgs have affected the cardiovascular field in a very positive way by enhancing oral bioavailability by more than 50 % from the parent drug. Therefore in this review, we will discuss the extensive research efforts that have contributed towards the development of various types of prodrugs to treat cardiovascular diseases such as vascular thrombosis, hypertension, pulmonary hypertension, and atherosclerosis.…”

Section: Introductionmentioning

confidence: 99%

Prodrugs in Cardiovascular Therapy

2008

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Prodrugs are biologically inactive derivatives of an active drug intended to solve certain problems of the parent drug such as toxicity, instability, minimal solubility and non-targeting capabilities. The majority of drugs for cardiovascular diseases undergo first-pass metabolism, resulting in drug inactivation and generation of toxic metabolites, which makes them appealing targets for prodrug design. Since prodrugs undergo a chemical reaction to form the parent drug once inside the body, this makes them very effective in controlling the release of a variety of compounds to the targeted site. This review will provide the reader with an insight on the latest developments of prodrugs that are available for treating a variety of cardiovascular diseases. In addition, we will focus on several drug delivery methodologies that have merged with the prodrug approach to provide enhanced target specificity and controlled drug release with minimal side effects.

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