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Файл:Antibiotics. Study aid
.pdf
HIGHER EDUCATION
Federal State Budgetary Educational Institution of Higher Education
“Ivanovo State Medical Academy”
of the Ministry of Healthcare of the Russian Federation
T.R. Grishina, O.A. Gromova,
I.V. Gogoleva, A.G. Kalacheva, T.E. Bogacheva,
N.Yu. Zhidomorov
ANTIBIOTICS
Study aid
© LLC IPR Media Company, 2023
ISBN 978-5-4497-2266-9
Moscow
IPR Media
2023
UDC 577.18
LBC 52.81
А72
Author's team of the Department of Pharmacology
of Ivanovo State Medical Academy:
Grishina T.R. — Doctor of Medical Sciences, Professor, Head of the Department;
Gromova O.A. — Doctor of Medical Sciences, Professor, Professor;
Gogoleva I.V. — Candidate of Medical Sciences, Associate Professor;
Kalacheva A.G. — Candidate of Medical Sciences, Docent, Associate Professor;
Bogacheva T.E. — Candidate of Medical Sciences, Docent, Associate Professor;
Zhidomorov N.Yu. — Candidate of Medical Sciences, Docent, Associate Professor
Reviewers:
Galustyan A.N. — Candidate of Medical Sciences, Associate Professor,
Head of the Department of Clinical Pharmacology and Pharmacoeconomics
of the St. Petersburg State Pediatric Medical University of the Ministry of Health of Russia;
Kuznetsov O.Yu. — Doctor of Medical Sciences, Professor, Head of the Department
of Microbiology and Virology of the Ivanovo State Medical Academy
of the Ministry of Health of Russia
А72 Antibiotics : study aid / T.R. Grishina, O.A. Gromova, I.V. Gogoleva [et al.]. —
Moscow : IPR Media, 2023. — (Higher education). — 1 CD-ROM. — System
requirements: Intel; Microsoft Windows (XP, Vista, Windows 7, etc.); CD-ROM
drive, 512 MB RAM; screen resolution not lower than 1024×768; Adobe Air
software, IPRbooks Reader software, mouse. — Title from the title screen. — Text :
electronic.
ISBN 978-5-4497-2266-9
The study aid concerns basic concepts of chemotherapy and main groups of
antibiotics. The mechanisms of their antibacterial activities as well as
indications and contraindications to the differentiated prescribing of drugs are
discussed in great detail.
The book is intended for studying the discipline of «Antibiotics and
antimicrobial therapy» by students of medical universities.
Educational electronic publication
Minimum system requirements: Standard architecture processor
x86 with a clock frequency of 1.6 GHz or higher; operating system
Microsoft Windows XP, Vista or Windows 7; from 512 MB of RAM;
from 1 GB of free hard disk space; screen resolution not lower than 1024×768
ISBN 978-5-4497-2266-9 © Original layout, design.
LLC IPR Media Company, 2023
Educational publication
Grishina Tatiana Romanovna
Gromova Olga Alekseevna
Gogoleva Irina Viktorovna
Kalacheva Alla Gennadievna
Bogacheva Tatiana Evgenievna
Zhidomorov Nikolai Yurievich
Editor M.V. Polovnikova
Technical editor, computer design A.D. Talmayeva
Cover design Ya.A. Kirsanov, S.S. Siziumova, photo bank Lori
To create an electronic edition, we used:
pdf2swf application from Swftools software, IPRbooks Reader software,
developed on the basis of Adobe Air
Signed for use 02.08.2023. Accounting and publishing lists 3,25.
Data volume 12 Мб. 1 CD-ROM. Edition of 100 copies.
LLC IPR Media Company
8 800 555 22 35 (free call in Russia)
E-mail: sale@iprmedia.ru
4
СONTENT
INTRODUCTION ................................................................................................... 5
1. ROLE OF ANTIBIOTICS IN PHARMACOTHERAPY
OF INFECTIOUS DISEASES ............................................................................... 6
2. ANTIBIOTICS ..................................................................................................... 9
2.1. β-lactam antibiotics ........................................................................................ 9
2.1.1. Penicillins ............................................................................................ 11
2.1.2. Cephalosporins ................................................................................... 16
2.1.3. Carbapenems ....................................................................................... 19
2.1.4. Monobactams ...................................................................................... 20
2.2. Glycopeptides ............................................................................................... 21
2.3. Macrolides .................................................................................................... 23
2.4. Lincosamides ................................................................................................ 27
2.5. Amphenicols ................................................................................................. 29
2.6. Tetracyclines ................................................................................................. 32
2.7. Aminoglycosides .......................................................................................... 35
2.8. Rifamycins .................................................................................................... 38
2.9. Lipopeptides ................................................................................................. 40
2.10. Polymyxins ................................................................................................. 40
2.11. Fusafungin .................................................................................................. 43
2.12. Polyenes ...................................................................................................... 43
2.13. Griseofulvin ................................................................................................ 44
3. UNDESIRABLE EFFECTS OF CHEMOTHERAPY .................................. 46
TEST AND TASKS ................................................................................................ 48
BIBLIOGRAPHY ................................................................................................. 53
5
INTRODUCTION
The study aid gives a complete description of antibiotics as a separate class of
drugs united by a common pharmacodynamics, and also shows fundamental
differences in the effects and use of groups of antibiotics with different chemical
structures. The material contains the definition, classification, spectrum and
mechanism of action with primary pharmacological reaction, effects, indications and
contraindications for use, pharmacokinetics, interaction with other drugs, features of
use in different categories of patients, criteria for efficacy and safety of use,
comparative characteristics of drugs within the group and with other classes, dosing
tactics.
The study aid corresponds to the Federal State Educational Standard in the
main educational program of the specialities “Medical business”, “Pediatrics”,
“Dentistry”, is part of the work program on the discipline “Pharmacology”. The book
contains all the information necessary for mastering the competencies OPK 6,
OPK 7, OPK 8 and is intended for 3rd year students studying in English.
6
1. ROLE OF ANTIBIOTICS IN PHARMACOTHERAPY
OF INFECTIOUS DISEASES
Antimicrobial agent is a natural or synthetic substance that kills or inhibits the
growth of microorganisms.
Chemical compounds and physical agents are classified due to the mode of
their antimicrobial action into:
chemotherapeutic agents affecting the target of clinical interest;
antiseptics and germicides used in medical practice to prevent or combat
bacterial infections of superficial tissues and to sterilize instruments and infected
material.
The latter are not considered here.
Chemical substances produced by a living organism, generally a
microorganism, as well as their derivatives or synthetic analogues are called
antibiotics.
Principles of chemotherapy (antibiotic therapy):
the choice of an antibiotic depends on the clinical and bacteriological
diagnosis and the contraindications of the patient;
the dose, frequency and route of administration of the antibiotic should form
and maintain a therapeutic concentration at the site of localization of the
microorganism throughout the course of treatment;
the early treatment of necessary duration to optimize functioning and reduce
disability in individuals with health conditions;
the combination of different antibiotics or their combination with other drugs
is carried out either to strengthen the antibacterial effect and / or to reduce the risk of
the formation of microorganisms’ resistance; administered antibiotics should not
potentize the side and / or toxic effects of other drugs used;
antibiotic therapy requires predicting and preventing undesirable effects in
time;
boosting of a macroorganism’ s immunity through keeping bed rest, proper
nutrition and vitamin therapy is an obligatory condition for successive chemotherapy.
7
Resistance of the microorganism:
primary antibiotic resistance is the loss of susceptibility of bacteria to the
killing (bacteriocidal) or growth-inhibiting (bacteriostatic) properties of
an antibiotic agent before the treatment; in other words, it is associated with specific
structural and functional features of the given microorganism;
secondary antibiotic resistance is the loss of susceptibility to a
chemotherapeutic agent produced by a strain of microorganisms in the process of
adaptation during chemotherapy.
Methods of antibiotics classification:
chemical structure;
origin;
spectrum of antimicrobial activity;
mode of antimicrobial action;
mechanism of antimicrobial action;
generation;
significance for the treatment of the given disease.
Origin of antibiotics:
biosynthetic (natural) antibiotics are synthesized by a biological object.
Natural antibiotics are most often isolated from the culture medium of microbial
producers;
semi-synthetic antibiotics are obtained chemically from biosynthetic
antibiotics;
synthetic antibiotics (to use this term for semi-synthetic antibiotics or
synthetic chemotherapeutic agents is unreasonable) are designed chemically from
substances being not antibiotics but complete structural analogues of existing
biosynthetic or semi-synthetic antibiotics.
Spectrum of antimicrobial activity is a list of microorganisms without
primary resistance to the given chemotherapeutic agent.
The terms “narrow spectrum of action” and, especially, “broad spectrum of
action” are used often though arbitrarily. Much more reasonable is to use the term to
compare the spectrum breadth of different antibiotics of the same group or antibiotics
of two different groups (‘broader’ or ‘narrower’ indicates specific strains additionally
included or excluded from the spectrum). A number of authors also distinguish the
8
term targeted antibiotic to denote drugs active against only one type of
microorganisms.
With respect to a sensitive strain, the use of a narrow focus drug is usually
more effective and safer than the use of a broad-spectrum drug.
Drugs of choice and reserve:
the drug of choice (first-line antibiotic) is the favored pharmaceutical
treatment for a given pathology;
a reserve drug (second-line antibiotic) is a medication which use in the
given pathology must be proved.
Classification of antibiotics by chemical structure:
β-lactam antibiotics;
Glycopeptides;
Macrolides;
Lincosamides;
Amphenicols;
Tetracyclines;
Aminoglycosides;
Rifamycins;
Lipopeptides;
Polymyxins;
Polyenes;
Steroids.
9
2. ANTIBIOTICS
2.1. β-LACTAM ANTIBIOTICS
β-lactam antibiotics are those that contain β-lactam ring at the core of their
molecule structure (fig. 1).
Fig. 1. Structure оf β-lactam antibiotics
Classification of β-lactam antibiotics by chemical structure:
Penicillins;
Cephalosporins;
Carbapenems*;
Monobactams.
Primary pharmacological reaction (PFR) of the bactericidal effect of
β‑lactam antibiotics
The β‑lactam ring is an analog of the dipeptide D-alanyl-D-alanine involved
in the synthesis of peptidoglycan biopolymer of the microbial cell wall, named
murein.
β‑lactam drugs interact with proteins involved in the construction of murein
called penicillin-binding proteins and block them.
Mechanisms of bactericidal action of β‑lactam antibiotics.
β-lactam antibiotics destroy the following functions of penicillin‑binding
proteins:
synthesis of murein precursors in the cytoplasm;
*
Along with carbapenems, this group also includes penems (pharopenem) and carbapenems and
penams that are not yet used in medicine.
10
transportation of acetylmuramic acid on uridine-5‑phosphate from the
cytoplasm to the cell wall of the microorganism;
cross-linking of peptidoglycan chains into murein by the enzyme
transpeptidase (murein synthase);
inhibition of mureinhydrolase destroying murein.
Mechanism of bactericidal action of β‑lactam antibiotics — blockade of
transpeptidase:
the main mechanism of β‑lactam antibiotics;
PFR — interaction with microbial cell transpeptidase;
the closure of the polypeptide bridge between heteropolymer chains in the
composition of murein is destroyed;
the permeability of the microorganism’ s cell wall of the increases;
the bactericidal effect develops.
Mechanism of bactericidal action of β‑lactam antibiotics — embedding
into murein:
PFR — interaction with enzymes embedding D-alanyl-D-alanine in the Park
nucleotide within the microbial cell cytoplasm;
β-lactam is embedded into the Park nucleotide;
acetylmuramyltripeptid-β-lactam is embedded into the hetero polymer chain
of the murein basis;
the closure of the polypeptide bridge between heteropolymer chains within
the murein is destroyed;
the permeability of the microorganism’s cell wall increases;
the bactericidal effect develops.
Mechanism of bactericidal action of β‑lactam antibiotics — activation of
mureinhydrolase:
PFR — interaction with a mureinhydrolase inhibitor on the cell membrane
of a microorganism;
the inhibitor of mureinhydrolase is blocked;
mureinhydrolase is activated;
the destruction of murein accelerates;
the permeability of the cell wall of the microorganism increases;
the bactericidal effect develops.
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