Strukturní modifikace léčiv ovlivňující biodostupnost a terapeutický účinek = Structure Modification of Drugs or Prodrugs Influencing Their Bioavailability and Therapeutic Effect

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Prodrugs are inactive derivatives of active drug substances which, on undergoing an enzymatic or chemical transformation in vivo, release the active parent drug that can then elicit the desired pharmacodynamic effect. Prodrugs can be classified into carrier prodrugs and bioprecursors. In most cases, carrier prodrugs are simple chemical derivatives of compounds that are only one or two chemical or enzymatic steps away from the active parent drug. Bioprecursors require enzymes of biotransformation phases for their activation; the active species results from a cascade of metabolic reactions involving oxidative/reductive processes. Currently codrugs (mutual prodrugs) become an efficient approach to drug optimization. The soft drug approach is briefly mentioned to clarify the difference between soft drugs and prodrugs. … full description

Bibliographic Details

Main Author

Aneta Černíková

Other Authors

Josef Jampílek

Document Type

Articles

Physical Description

Ilustrace

Published in

Chemické listy. -- ISSN 0009-2770. -- Roč. 108, č. 1 (2014), s. 7-16

Subjects

DRUGS

BIOAVAILABILITY

EFFICIENCY

ENZYMES

Pharmacodynamics

METABOLISM

OXIDATION

REDUCTION

léky

biologická dostupnost

účinnost

enzymy

chemické reakce

farmakodynamika

metabolismus

oxidace

redukce

proléčiva > prekurzory > bioprekurzory > zdvojená léčiva > codrugs > soft drugs

Item Description

11 schémat, 1 tabulka

Bibliography

Literatura na s. 14-15,