METHODICAL INSTRUCTIONS TO LESSON № 4 FOR STUDENTS
THEME: CHARACTERISTICS OF ANTIMICROBIAL DRUGS. CLINICAL PHARMACOLOGY OF ANTIBIOTICS. FLUOROQUINOLONES. ANTIVIRAL DRUGS.
Aim: To study clinical pharmacology of antibiotic, sulfanilamides, quinolones, of antiviral and of different antibacterial agents, their clinical usage and complications
Professional motivation :
Antibiotic preparations are the most important chemotherapeutical medicinal preparations. Thanks to theme it became possible to cure the pulmonal form of plague people, sharply decrease death rate in case of such disease as typhus, meningitis, tuberculosis, etc. There are more than six thousand antibiotic preparation described, but in practice only 50-60 of them are widely used.
Excessive use of this highly-active group of chemotherapeutical preparations and underestimating of its potential danger, irrational and non-effective use called the row of undesirable results of antibiotic therapy-increasing of antibiotic resistance and polynatural resistance of microbes and their selection, damaging of separate organs and systems, development of non-specific sensitisation, increasing of frequency of endogenic mixed with super-infections. Above mentioned facts led us to the decision of more careful use of antibiotic preparations an strict observing rational therapy principles.
The modern antimicrobal chemotherapeutic era began in the early 1930 's when Prontosil, a chemical developed by the German dye industry, was to combat Streptococcal infection in mice after metabolism to paraaminobenzene sulfonamide (sulfanilamide) and antibacterial compounds. The sulfonamides were once a mainstay in the treatment of infections disease, but their importance has diminished as bacterial resistance has increased and more effective agents have been developed. Nevertheless, because of their established effectiveness, low cost and the relative lack of the new compounds, sulfonamides are among the drugs which are used in healing of some diseases.
Fundamentally viruses are obligate intracellular parasites. Their replication depends primary on metabolic processes of the host cell Consequently, many chemicals that inhibit viral replication also inhibit some host cell function and possess major toxicity. In order to be clinically effective, chemicals that block viral replication must be administered before the onset of disease, as chemoprophylaxis.
Students’ Independent Study Program
I. Objectives for Students’ Studies
You should prepare for the practical class using exist textbooks and lectures. Special attention should be paid to the following:
1. Biological significance of antibiosis and main mechanism of antibiotics action.
2. Antibiotics of biosynthetic (natural) penicillin group: agents antibacterial spectrum, pharmacokinetics, indications, adverse reactions and precaution.
3. Aminopenicillins, their peculiarities of action and usage, adverse reactions
4. Cephaloosporins: antibacterial spectrum, indications complications
5. Inherence and application of antibiotics macrolide group
6. Antibiotics of tetracyline group: drugs, spectrum of activity, pharmakokinetics, apply and adverse reactions
7. Chloramphemicol (levomycetinum) antibacterial spectrum, use, side effects.
8. Amynoglicosides: antibacterial spectrum, indication, adverse reactions.
9. Peculiarities of action and application of polymyxins
10. Antimicrobal agent of plant origin
11. Principles of rational antibiotic therapy
12. Combine uses of antibiotics.
13. Mechanism and antibacterial spectrum of sulfonamides.
14. Pharmacokinetics of sulfonamides.
15. Period of action and dosage of sulfonamides.
16. Clinical classification and indications of usage of sulfonamide agents.
17. Combine usage of sulfonamides and antibacterial agents of other chemical structure.
18. Adverse reactions and complications of sulfonamides therapy, their prevention and healing.
19. Naftiridinum derivates (acidum nalidixicum), their characteristic and uses.
20. 8-oxychinolinum derivates (enteroseptolum), their characteristic and uses.
21. Nitroforanum derivates as chemiotherapeutic agents.
22. What antiviral agents are used for the fever healing?
Key words: antibiotic, antimycrobal agent, infection, penicillin, cephalosporin, macrolide, tetracycline, amynoglicoside, polymyxin, antibacterial spectrum, sulfonamides, antibacterium spectrum, naftiridinum, 8-oxychinolinum, nitrofuranum.
II. Tests and Assignments for Self-assessment:
A. Rifampicine is used mainly in the treatment of :
2. Typhoid fever
4. Rickettsial diseases
5. Pseudomonas infections
B. Patients having a history of a severe, immediate reaction to penicillin:
1. may be given a cephalosporin without concern
2. have a definite risk of reaction to any cephalosporin
3. have a low risk of having a reaction to a broad spectrum antipseudomonal penicillin
4. have a high risk of hypersensitivity to a broad spectrum antipseudomonal penicillin
1. are bacteriostatic in vitro
2. are bacteriocidal in vitro
3. are effective against rickettsial
4. interfere primary with cell wall synthesis
D. What agents are antiviral:
1. Real-life situation to be solved:
A diabetic patient come to physician with cough and a single shaking chill. His temperature 38,5o C, and a chest X-ray demonstrates lobar pneumonia.
Gram staining reveals gram-positive diplococci. What would the most sensible antibiotic?
I. Answer to the self-assessment:
2.A – 3, B- 2,
Visual Aids and Material Tools: Medical documents, tables, slides.
Students Practical Activities
Student must know:
clinical pharmacology, uses and contraindications of different groups of antibiotics, agents sulfanilamides and antibacterial agents
I. Answer the following questions:
1. What are the antibiotic of the group of choice?
2. What drug belong to the synthetic penicillin?
3. Why can’t be Gentamicinum combined with Furosemidum?
4. Why Benzylpenicillinum-natrium can be injected only parentally?
5. Why Neomicini sulfatis can be injected only parentally ?
6. What side effects are observed after using tetracyclinum ?
7. What antibiotics are not prescribed together ?
Students should be able to: make a choice of the above mentioned drugs in real-life situation, write out the prescription for these drugs in different medicinal forms.
Benzylpenicillinum-natrium, Benzylpenicillinum-kalium, Bicillinum 3,5, Oxacillinum-natrium, Ampicillinum, Cefazolin sodium (kefzol), Cefatoxime sodium (claforan), Ceplalexinum, Gentamycinum sulfas, eruthromycinum, tetracyline, metacycline, levomycetine (chloramphenicolum), Rifampicine, Streptomycinum sulfas, Gramycidinum, Polymixinum sulfas, Nistatinum, Amphotericinum, Griseofulvinum, Novoimanin, Microcid, Chlorphiliptum, Sulfadimezinum, Sulfacilum-natrium, Sulfadimethoxinum, Sulfadiperazinym, Phthalazolum, Biseptolum ( Bactrim ), Acidum nalidixicum, Enteroseptolum, Furasolidonum.
2. Carpenter CF, Chambers HF: Daptomycin: Another novel agent for treating infections due to drug-resistant gram-positive pathogens. Clin Infect Dis 2004;38:994.
3. Mandell LA et al: Update of practice guidelines for the management of community-acquired pneumonia in immunocompetent adults. Clin Infect Dis 2003;37:1405.
4. Scheld WM: Maintaining fluoroquinolone class efficacy: Review of influencing factors. Emerg Infect Dis 2003;9:1.
Prepared by ass. prof. Meretskyy V.M.
Methodical instruction was discussed
and adopted at the Department sitting
Minute № 7
Methodical instruction was adopted
and reviewed at the Department sitting
27.08.2013 Minute № 1