Professional Documents
Culture Documents
that century. Chain and Florey then purified it (penicillin) and clinical use
Definition
agents that are not products of microbes are also termed as antibiotics.
1
Classification
agents, and all are hampered by exceptions and overlaps. Historically, the
2
6 The antimetabolites, i.e. agents that block specific metabolic steps
that are essential to microorganisms.
E.g. trimethoprim, sulfonamides.
7 Nucleic acid analogs – agents that bind to viral enzymes that are
essential for DNA synthesis thus halting viral replication.
E.g. : Zidovudine – Acyclone.
General considerations
3
2) When the patient is
condition.
effect. Therapy should help contain and limit further extension of the
involvement or complications.
debilitation.
3) Trismus.
4
7) Allograph (cardiac, renal, bone marrow, liver and or osseous
implants).
periapical abscess.
vital tooth.
selectively active against the most likely infecting agents and that has the
under treatment.
5
The choice depends on :
a. The patient
b. The infecting organism
c. The drug
A) Patient factors
3) Local factors :
1. Presence of pus and secretions.
2. Presence of necrotic material haematomas, foreign body.
3. Low pH at site of infection.
6
4) Drug allergy : H/O previous exposure to be taken.
5) Impaired host defence.
6) Pregnancy.
7) Genetic factors: Chloramphenicol, sulfonamides are likely to
produce haemolysis in G6PD deficient patient.
C) Drug factors
1) Spectrum of activity : Narrow/broad.
4) Toxicity.
8) Cost.
7
COMBINED USE OF ANTIBIOTICS
Disadvantages of combinations
i) Increased chances of superinfections.
8
2) Hypersensitivity reactions: Unpredictable and unrelated to dose –
3) Drug resistance :
penicillins.
2. Acquired.
preserved and get a chance to proliferate when the sensitive cells are
II] Gene transfer : from one organism to another can occur by:
i) Conjugation : Transfer through sexual contact i.e. bridge
formation, sex pilus.
9
Mechanism of increased bacterial resistance to antibiotics:
ii) Changes in the target sites for the drug in the bacterial cell.
possible.
therapy.
antimicrobial therapy.
10
Use of most antibiotics causes some alteration in the normal
microbial flora of the body. The normal flora contributes to host defense by
organisms. Further, ordinarily the pathogen has to compete with the normal
flora for nutrients etc to establish itself. Lack of competition may allow
in
- Corticosteroid therapy.
- AIDS
- Agranulocytosis.
To minimize superinfections
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b) Do not use antimicrobials to treat self limiting or viral
infections.
sufficient to treat one infection but only briefly suppress another one
Rationale:
cavity.
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enough concentration for a long period of time to affect the organism
areas and may also affect organisms residing within the gingival
periodontal pathogens from the entire may reduce the risk for
antibiotic
1) Gingival fluid concentration (C GCF)
2) Minimum inhibitory concentration (MIC90).
13
CGCF provides information on the peak levels achieved by systemic
and MIC90.
inhibition of growth of an organism appear on the 100% line and those that
do not fall between 0-100%. The most effective antibiotics for treatment of
a particular periodontal pathogen are those that equal or exceed the 100%
value.
enough period.
4) Be substantive.
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5) Not be allergic or toxic.
7) Not be expensive.
diseases.
mm. In the healthy individual this event does not necessitate any
15
therapeutic interaction, but serious systemic infections may develop in
bacteria.
Concluding Remarks:
status, for which reason the patients physician should be consulted before
Individual Drugs
Classification of tetracyclines
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1. Tetracyclines
Description:
Structure:
semisynthetic tetracyclines.
Pharmacological properties:
Absorption:
(93% and 100%) are more extensively protein bound and have more
100mg/day after an initial loading dose of 200 mg and for minocycline 100
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mg x 2 / day, while for tetracycline hydrochloride- 250mg x 4/day. Such
and Al3+ in the G.I. tract (Ericsson et al, 1982). These ions are present in
should be taken either ½ an hour before or after food. Food does not
tetracycline and thus have better ability to pass through the lipid bilayer of
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Pharmacokinetics
All tetracyclines are removed from the circulation by the liver and
excreted into the G.L. tract via the biliary system. There is some
excreted unchanged.
Antibacterial actions:
Spectrum
rapidly multiplying bacteria. They are against all gm+ve bacteria and many
gm-ve species.
Mechanism of Action
minocycline are more lipid soluble and thus pass through the lipid
bilayer of the bacterial cell wall. Once through this layer, an energy
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specifically to the 30s ribosomes. This binding appears to prevent
compounds from the cell (Pato 1977). This action would explain the
Antibiotic resistance
that pumps the drug out of the cell and prevent it from accumulating
resistance gene isolated from the ECO RI Hind III fragment of plasmid
PAT 101 has been shown to confer resistance to approx. 12% of total
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and some bacteroides which are greater than levels attainable in the GCF
by systemic dosing.
approx. 7 time.
concentration of tetracycline.
3. Anticollagenase activity
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including fibroblasts, epithelial cells, macrophages (mature
collagenase harvested from deep pockets appear more resistant to the drugs
the drugs antibacterial properties but to the source of the enzyme and the
inhibition (Burns et al, 1989) because it binds to Zn++ more strongly. Low
et al, 1992).
22
Mechanism of action
relates to the drugs ability to bind with Ca++ and Zn++ ions Ca++ ions
and Zn++ ions are required by the enzyme to maintain its proper
macrophage, elastase).
23
Tetracyclines including chemically modified tetracyclines CMTs
Mechanism of action:
function.
of collagenolytic cathepsins.
Mechanism of action
cytoplasmic calcium.
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5] Antiinflammatory action
Creamer 1991).
Mechanism of action:
25
2. To the release of matrix components from the dentine (i.e. Type I
therapy.
Other uses:
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fried bone allografts have been tried and given encouraging results
(Marby et al).
bullous pemphigoid.
Side effects:
3. Photosensitivity.
4. Skin rashes.
27
Contraindications Possible sequela
Erythomatosis
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II] Erythromycin
Description
penicillin.
Mechanism of action:
Absorption:
(Erythromycin).
Excretion
Clinical use
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III] Clindamycin
Description
lincolnesis.
Mechanism of action
Same as erythromycin
Specturm
Absorption
Excretion
Adverse effects
Clinical use:
tetracycline therapy (Tyler et al, 1998). This agent should considered only
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with medical consultation in penicillin allergic patients when serious
IV] Spiramycin
Description
Spectrum
A.viscous.
Clinical use:
pocket depth and GCF flow (Keyes and Coworkers). In addition it is safe.
Nontoxic drug with few and infrequent side effects and is not in general
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V] Kanamycin
Description:
improve gingival health. Due to its toxicity and marginal results achieved
with kanamycin it would appear to limit. Its use in all but a small number
of individuals who are not able to maintain oral hygiene with routine
1. Penicillin
Description
other.
Structure
Penicillins are all β -lactams and they have the β -lactamic chain
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Mechanism of action
component of the bacterial cell wall. Thus, these antibiotics interfere with
potassium (augmentin) have not been evaluated and their use in periodontal
Side effects : They may induce allergic reaction (10% of patients allergic
Amoxicillin
certain bacteria that opens the lactamic ring and there by renders
penicillin ineffective.
33
5. Clinical use- Broad spectrum penicillin for use against a variety of
they protect the drug against lactamase hydrolysis and increase the
34
III Inhibition of DNA synthesis
Quinolones
Metronidazole
Description
Structure:
Absorption
35
Pharmacokinetics
Spectrum
Mechanism of action
as aerobic and anaerobic bacteria by diffusion. When the nitro group of this
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component is reduced by nitroreductase (a ferrodoxin like electron
Resistance
Clinical use
37
and decreases clinical and histopathological signs of periodontitis
4. Loesche and coworkers found that 250mg tid for 7 days was of
Dosage
Adverse effects
tolerated and result in few side effects which resolve upon cessation of
drug intake.
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2. Minor and rare C.N.S. effects include vertigo, headaches, and with
(Greenstein, 1993).
should be used during pregnancy only when clearly indicated and avoided
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prolonged prothrombin times.
Rationale:
40
3. To lower the dose of individual antibiotics by exploiting possible
Disadvantages
antibiotics.
41
Guidelines for use of antibiotics (Genco, 1981)
antibiotic.
42
in patients taking medication which adversely affect the
For e.g. topical kanamycin applied to teeth and gingiva help reduce
tested and found useful for the treatment of various forms of periodontal
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infections and thus fail to arrest destructive disease activity (Lindhe,
1982).
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6. Ciprofloxacin may be combined with metronidazole or a β -lactam
Why? – When systemic agents are taken orally they are introduced
in pulses that produce peak concentration that differs in time and level for
each body compartment. After the drug reaches a peak blood level there
one must either take frequent doses or have an agent that remain active and
is slowly removed from the body. The latter situation is risky as in may
levels at local sites. Perhaps the greatest concern is that wide use of oral
bacterial strains.
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Such multiple resistance could limit the usefulness of several
subgingival area.
Delivery systems
agent can be delivered to the local site and oral rinses are easy to
use.
Disadvantage : - Requires patient compliance.
- Drug pulses and concentration fluctuations may
limit efficacy.
- Limited to supragingival use.
2) Oral irrigation:
Advantages
1. Easy to use.
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3) Controlled release devices: It refers to delivering active chemicals to
intended effect.
Advantages:
1. Reproducible and prolonged constant rate of delivery.
2. Less frequent administration.
3. Greater patient compliance.
4. Reduced side effects as compared to systemic administration.
has been tetracycline fibers. Although hollow fibers were initially used, the
pocket and the moisture in the area dissolves the drug from the fiber
for 10 days.
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CONTENTS
HISTORY
DEFINITION
CLASSIFICATION
GENERAL CONSIDERATION
b) Indications
c) Contraindications
d) Choice of an antibiotic agent
(i) Patient Factors
1. Age
2. Renal and hepatic function
3. Local factors
4. Drug allergy
5. Impaired host defense
6. Pregnancy
7. Genetic factors
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7. Evidence of clinical efficacy
8. Cost
49