The journal has been published since 2004. It was originally published under the title “Clinical Pharmacokinetics”. In 2004–2005, we believed that the most important attention should be paid to clinical pharmacokinetics (PK) studies, both for new pharmacological substances (at the stage of phase I clinical trials) and for drugs widely used in medical practice. As for PK studies within the framework of Phase I studies of a new drug, the main task is to verify and transfer data obtained from preclinical studies of its PK and biotransformation in at least two types of experimental animals. When studying the clinical PK of known drugs, the main goal of research is to identify the PK determinants responsible for the manifestation of their clinical action. In case of a positive result, the parameter correlated with the PK effect can serve as a starting point for the development of optimal regimens for the use of a particular drug in clinical practice under PK control. The same goal is pursued by therapeutic drug monitoring, where optimization of the use of a drug is performed by monitoring its concentrations in the biomaterial. In this case, the concentration of the active substance (and/or its “active” metabolite) must be within the so-called “therapeutic window”, within which the optimal therapeutic effect is manifested with minimal side effects of the drug.

In 2012, there was a need to expand the format of the journal, and it was renamed the journal “Pharmacokinetics and Pharmacodynamics”. This change was dictated by the desire to create a single printed publication for specialists working in the related fields of pharmacokinetics, pharmacodynamics, and biopharmacy. This seems especially important now, when the need for such research has significantly increased because of the natural increase in their role in biomedical research of new and generic drugs, as well as in assessing the quality of finished dosage forms. Currently, it is generally accepted in world practice that preclinical and clinical PK studies when creating new and generic drugs are mandatory, and they help answer several important questions that arise during the study:

• the rate and degree of absorption of the drug from the injection site;
• biotransformation of medicinal substances by identifying “major” metabolites as well as active metabolites that, along with the unchanged medicinal substance, have the same or different pharmacological activity;
• permeability of drugs through histohematic barriers and their delivery to the site of action;
• tissue availability of the drugs;
• the relationship between the pharmacokinetics and pharmacodynamics of the studied medicinal substances, which can play an important role in future data transfer from animals to humans;
• choosing the optimal route of drug administration, considering its “first pass” through the liver and bioavailability;
• pharmacokinetic studies of various dosage forms and selection on the basis of optimal ones with greater bioavailability, allowing them to be recommended for further study and implementation in practice;
• removal of a medicinal substance and its transformation products from the body.

In addition, after receiving approval for phase I clinical trials of PK, studying the new drug being developed, along with safety and tolerability, is mandatory when studying it in volunteers. When conducting phase II and III clinical trials of an innovative drug, its pharmacokinetic study is not mandatory. However, after identifying the clinical effectiveness of the drug being studied and obtaining permission from the Ministry of Health of the Russian Federation for its medical use, PK studies, like PK studies of any drug, including generic ones, are desirable in terms of further development, based on the results obtained, of schemes for rational and optimal use in clinical practice. practice, as mentioned above.

The change in the name of the journal contributed to the appearance of articles related to experimental studies of new and generic drugs and a significant increase in the number of review articles on experimental and clinical PK, drug interactions, bioequivalence, etc.

Since May 25, 2022, the journal "Pharmacokinetics and Pharmacodynamics" has been included in the list of Higher Attestation Commissions, peer-reviewed scientific publications in which the main scientific results of dissertations for the scientific degree of Candidate of Sciences and for the scientific degree of Doctor of Sciences should be published (No. 2456 in the List).

Scientific specialties and corresponding branches of science for which the publication is included in the List of Higher Attestation Commissions:

3.3.6. Pharmacology and clinical pharmacology (medical sciences)

3.3.6. Pharmacology and clinical pharmacology (biological sciences)

3.3.6. Pharmacology and clinical pharmacology (pharmaceutical sciences)