4. From Actinomycetes
The tetracycline's still available in lndia for clinical use are:
Tetracycline
Oxytetracycline
Demeclocycline
Doxycycline
Minocycline
6. Broad-spectrum antibiotic
Promiscuous and often indiscriminate use has
gradually narrowed the field of their usefulness.
1. Cocci
2. Most gram-positive bacilli
3. Gram-negative bacilli
4. Spirochetes, T. Pallidum
5. All rickettsiae (typhus, etc.) And chlamydiae are
highly sensitive.
6. Mycoplasma and actinomyces are moderately
sensitive.
7. Entamoeba histolytica and plasmodia are inhibited
at high concentrations.
7. The older tetracycline's are incompletely
absorbed from GIT; absorption is better if taken
in empty stomach.
Doxycycline and minocycline are completely
absorbed irrespective of food.
Tetracycline's have chelating property-form
insoluble and unabsorbable complexes with
calcium and other metals.
Milk, iron preparations,nonsystemic antacids and
sucralfate reduce their absorption.
8. They are concentrated in liver, spleen and
bind to the connective tissue in bone and
teeth.
Intracellularly, they bind to mitochondria.
Minocycline accumulates in body fat.
9. Most tetracycline's are primarily excreted in
urine by glomerular filtration;
Doxycycline is an exception to this.
10. They are secreted in milk in amounts
sufficient to affect the suckling infant.
11. 1. Tetracycline: ACHROMYCIN,
HOSTACYCLINE,RESTECLIN 250, 500 mg cap, 3%
skin oint, 1% ear/eye drops and oint.
2. Oxytetracycline: TERRAMYCIN 250, 500 mg cap,
50 mg/ml in 10 ml vials inj;3% skin oint, 1%
eye/ear drop and oint.
13. Although tetracycline's are broad-spectrum
antibiotics, they should be employed only for
those infections for which a more selective
and less toxic AMA is not available.
Clinical use declined due to fluoroquinolones
and other efficacious AMAs.
14. The nature and sensitivity of the infecting
organism cannot be reasonably guessed
Initial treatment of mixed infections
16. To Penicillin/Ampicillin
To Ceftriaxone
To Azithromycin For Pneumonia
To Ceftriaxone/Azithromycin For Chancroid.
To Streptomycin For Tularemia.
17. (A) Urinary Tract Infections
(B) Community Acquired pneumonia
(C) Amoebiasis
(D) As Adjuvant To Quinine Or Sulfadoxine
(E) Acne Vulgaris
(F) Chronic Obstructive Lung Disease
20. Esophageal ulceration especially with
doxycycline.
Intramuscular injection of tetracycline's are
very painful; thrombophlebitis of the injected
vein can occur, especially on repeated use
21. 1. Liver damage
Fatty infiltration of liver and jaundice occur
Pregnant women; can precipitate acute
hepatic necrosis which may be fatal.
2. Kidney damage
In the presence of existing kidney disease.
Except doxycycline, accumulate and enhance
renal failure.
A reversible fancony syndrome llke condition
is produced by outdated tetracyclines
3. Phototoxicity
22. 4. Teeth and bones
Brown discoloration, ill-formed teeth, more
susceptible to caries.
Tetracyclines have chelating property
Calcium-tetracycline chelate gets deposited in
developing teeth and bone.
Given from midpregnancy to 5 months of extra
uterine life, deciduous teeth are affected.
3 months and 6 years of age affect the crown of
permanent anterior dentition.
Late pregnancy or childhood, temporary
suppression of bone growth.
Deformities and reduction in height are a
possibility with prolonged use.
23. First, the ‘extrinsic theory’ (Berger et al. , 1989),
Tetracycline attaches to the glycoproteins in acquired pellicles.
This in turn etches the enamel, and demineralization/
remineralization cycles occur.
It oxidizes on exposure to air or as a result of bacterial activity,
and so causes degradation of the aromatic ring, forming
insoluble black quinone.
The second is the ‘intrinsic theory’ (Bowles and Bokmeyer, 1997;
Bowles, 1998),
Where the tetracycline bound to plasma proteins is deposited in
collagen rich tissues, such as teeth.
This complex oxidizes slowly over time with exposure to light.
This deposition in teeth occurs solely within the dentin matrix as
secondary and reparative dentin is formed
24. 5. Antianabolic effect
Reduce protein synthesis and have an overall
catabolic effect.
They induce negative nitrogen balance and can
increase blood urea.
6. Increased intracranial pressure
Noted in some infants.
7. Diabetes insipidus
Demeclocycline antagonizes ADH action and
reduces urine concentrating ability of the kidney.
8. Vestibular toxicity
Minocycline has produced ataxia, vertigo and
nystagmus, which subside when the drug is
discontinued.
25. Resistance to tetracycline develops slowly in a
graded manner.
Tetracycline concentrating mechanism becomes
less efficient or the bacteria acquire capacity to
pump it out.
Plasmid mediated synthesis of a 'protection‘
protein which protects the ribosomal binding site
from tetracycline.
26. Infrequent with tetracycline's.
Skin rashes, urticaria, glossitis, pruritus ani
and vulvae, even exfoliative dermatitis have
been reported.
Angioedema and anaphylaxis are extremely
rare.
27. The tetracycline should be discontinued at the first
sign of superinfection and appropriate therapy
instituted.
Doxycycline and minocycline are less liable to
cause diarrhoea, because only small amounts
reach the lower bowel
28. 1. Not be used during pregnancy, lactation and in
children.
2. Avoided in patients on diuretics: blood urea may rise in
such patients.
3. Used cautiously in renal or hepatic insufficiency.
4. Never be used beyond their expiry date.
5. Do not mix injectable tetracycline's with penicillin-
inactivation occurs.
6. Do not inject tetracycline's intrathecally.
33. Bactericidal - h. Influenzae, strep. Pneumoniae and n.
Meningitidis.
Other organisms e. Coli, k. Pneumoniae, shigella, and certain
strains of brucella, pasteurella, proteus and vibrio comma.
Active against gram positive and negative organisms, rickettsia,
chlamydia , and mycoplasma pneumoniae.
34. Completely absorbed after oral administration,
Bound to plasma protein (approximately 60%) and widely
distributed in body.
Crosses the blood-brain and placental barrier and shows its
presence in csf, bile and milk.
It is conjugated with glucuronic acid in liver and excreted in
urine.
Small amount is excreted in urine in unchanged form.
35. Because of Bone Marrow Toxicity
its use is restricted to the
treatment of infection caused by
S. Typhi And Paratyphi
Other - H. Influenzae
Meningitis, Urinary Tract
Infections, Anaerobic Infections
Caused By Bacteroides Fragilis
And Locally In Eye And External
Ear Infections.
36. Other - Superinfection, Hepatotoxicity And Typhoid Shock.
CNS toxicity - Headache, Mental Confusion, Internal Ophthalmoplegia,
Peripheral Neuritis, Depression, Optical Neuritis
Gray baby syndrome- Gray Cyanosis, Vascular Collapse, Shock And Death.
Bone marrow depression - Aplastic Anaemia,
Leukopenia, Agranulocytosis, Thrombocytopenia.
Allergic Reaction- Skin Rashes, Drug Fever, Dermatitis, Angioneurotic
Edema.
40. Act By Inhibiting Protein Synthesis Of Bacteria By Directly
Combining With Ribosomes.
They Penetrate The Outer Cytoplasmic Membrane And
Inhibit Protein Synthesis.
Streptomycin Combines With The Bacterial 30s
Ribosome's And Interferes With The mRNA-ribosome
Combination.
Other Aminoglycosides Bind To Additional Sites On 50s
Subunit As Well As To 30s-50s Interface.
42. Poorly absorbed after oral administration,
More active in alkaline ph
Excreted unchanged by glomerular filtration
accumulation occurs in renal impairment.
43. All Aminoglycosides produce cochlear and
vestibular damage (Ototoxicity) And
Nephrotoxicity.
Reduce the acetylcholine release from
motor nerve endings and cause
neuromuscular blockade.
45. Used In All Tuberculosis Along With Antitubercular
Drugs.
Other Indications: Tularemia, Plague, Brucellosis,
Bacterial Endocarditis, Enterococcal Endocarditis.
Used concomitantly with Penicillin G for synergistic
effect in the treatment of Enterococcal Endocarditis
when other antibiotics are ineffective or
contraindicated
53. Sulfanilamide exhibits a structural similarity to para-amino
benzoic acid (PABA).
WOODS AND FIELDS proposed theory that sulfonamides, inhibit
bacterial FOLATE SYNTHETASE so folic acid is not formed which
is needed for a number of metabolic reactions.
Causes FOLIC ACID deficiency and ultimately cause injury to
the bacterial cell.
54.
55. Bacteriostatic Antibacterial
Activity Against Gram
Positive And Gram Negative
Organisms , Certain
Species Of Chlamydia
Infections Such As:
Streptococci, Staphylococci,
Pneumococci, Gonococci,
Meningococci,.
Haemophilus Influenzae,
Granulomatis, Vibrio
Comma, Vibrio Cholerae, E.
Coli, Pasteurella Pestis,
Shigella
56. rapidly and
completely absorbed
from GIT mainly in
small intestine
Binding with
plasma proteins
differ
considerably
among different
groups.
The highly
plasma protein
bound
sulfonamides
have longer
action.
57. I. Urinary Tract
Infection
Ii. Acute Bacillary
Dysentery
Iii. Ulcerative
Colitis
Iv. Streptococcal
Pharyngitis, And
Tonsillitis.
V. Trachoma And
Inclusion
Conjunctivitis:
Vi. Chancroid
Vii.
Meningococcal
Meningitis.
Viii. Chloroquine
Resistant Malaria
Ix. Toxoplasmosis
X. Burns
58. Allergic Symptoms Drug Fever, Skin Rash, Urticaria, Eosinophilia,
Photosensitization Reactions, Serum Sickness Like Syndrome.
Stevens- Johnson Syndrome And Exfoliative Dermatitis Are Also
Common With Longer Acting Agents
Uncommon Allergic Reactions Acute Toxic
Hepatitis, Toxic Nephrosis And Acute
Haemolytic Anaemia.
Renal Irritation And May Precipitate Renal
Colic. Crystalluria, Haematuria And
Albuminuria Can Occur May Lead To
Oliguria And Anuria.
Hematopoietic Toxicity
Agranulocytosis, Thrombocytopenia And
Rarely Aplastic Anaemia
Patients With G-6- Pd Deficiency,Cause
Intravascular Haemolysis.
The Other CNS Effects Include Depression,
Confusion, Tinnitus, Fatigue Etc.
59. A combination of trimethoprim and sulfamethoxazole (cotrimoxazole) act
sequentially in the same metabolic pathway in the synthesis of nucleotides.
Sulfonamides act by inhibiting the incorporation of PABA into dihydrofolate by
bacteria.
Pyrimidine derivative related to Antimalarial drug Pyrimethamine,
Selectively inhibits bacterial Dihydrofolate Reductase, necessary for the
conversion of Dihydrofolate to Tetrahydrofolic Acid.
60. Therapeutic uses
Infection caused by salmonella typhi, klebsiella,
enterobacter,pneumocystis carinii etc
And many other sulfonamide resistant strains of s.
Aureus,strep. Pyogenes, shigella, e. Coli, h.
Influenzae, meningococci and gonococci etc.
Effective as a second line agent in penicillin
allergic patients where newer antibiotics are
contraindicated or can’t be used.
61. UT I
Acute Cystitis
Bacterial Diarrhoea
And Dysentery.
Respiratory Tract
Infection - Chronic
Bronchitis And Otitis
Media Etc.
Typhoid.
Nosocomial Infections
Chancroid
Sexually Transmitted
Diseases
Prophylaxis And
Treatment HIV
Associated Infections
Prophylaxis - Organ
Transplantation
Patients Receiving
Immunosuppressants
62.
63. They Are active against a variety of gram positive and
gram negative bacteria.
analogs of nalidixic acid (which was introduced in mid
1960s and had limited use in uti and git infections).
second generation quinolones – the Fluoroquinolones also
effective against gram positive bacteria.
Quinolones, synthetic AMA effective against gram negative
Bacteria.
64. Quinolone Block bacterial DNA
synthesis by inhibiting bacterial
Topoisomerase II (DNA Gyrase)
and Topoisomerase IV
Inhibition of DNA gyrase prevents
the relaxation of positively
supercoiled DNA that is required for
normal transcription and replication.
65. It is 4-QUINOLONE derivative effective against gram negative bacteria mainly E.
Coli and Shigella.
Acts by inhibiting bacterial DNA GYRASE.
Used as urinary antiseptic and in diarrhea caused By E. Coli, Shigella,salmonella.
The side effects are GIT upset, Headache, Drowsiness, Vertigo, Visual
Disturbances and on prolonged use can produce parkinsonism like symptoms.
In Individuals with G-6-PD deficiency can cause haemolysis.
66. Quinolone AMAs having one or more fluorine substitutions, relatively
broad spectrum of action and effective against gram positive And gram
negative organisms.
They are highly effective against E. Coli, Klebsiella, Proteus Mirabilis,
Shigella, Salmonella Species, H. Ducreyi Etc.
67. The presence of a 6-fluoro and 7- piperazine
substitution greatly enhances their
antimicrobial efficacy as compared to nalidixic
acid.
The fluorine atom is responsible for increased
potency against gram negative organisms and
broadens the spectrum of their activity
including gram positive organism.
68. After oral administration, well absorbed
with the bioavailability Of 80 to 95 % and
distributed widely in body fluids and tissues.
The fluoroquinolones are excreted mainly by
tubular secretion and by glomerular
filtration.
69. UTI
Dental Use
Not indicated in acute orofacial infections
Ciprofloxacin may be used in rapidly progressive or refractory
periodontitis
Bacterial
gastroente
ritis.
Typhoid
fever.
Septicemia.
Otitis
media.
Acute
pneumonia
Ocular
infections
70. Fluoroquinolones are well
tolerated.
Tendinitis is rarely reported in adults.
Because of cartilage damage in children it
must be used under close supervision.
Nausea, Vomiting, Diarrhoea, Headache,
Insomnia, Skin Rash , Abnormal Liver
Function Tests (With Trovafloxacin).
Phototoxicity Reported With Pefloxacin,
Lomefloxacin, Sparfloxacin And Ofloxacin.
71. Most potent first generation fluoroquinolone,
Aerobic gram negative bacilli.
Higher concentration in the urine than plasma.
Produces rapid and complete clinical relief in nosocomial
bronchopneumonia
Used prior to cardiac surgery and has attained levels higher
than mics for at least 8 hours.
72. It is more potent than ciprofloxacin for gram positive organisms.
It also inhibits Mycobacterium tuberculosis and mycobacterium leprae and
used as alternative in multidrug resistant therapeutic regimens.
It is also used in the treatment of chronic bronchitis and other ENT infections.
73. It is the levoisomer of ofloxacin and having better activity than
ciprofloxacin and ofloxacin against s. Pneumoniae.
It is also used in chronic bronchitis, sinusitis, pyelonephritis, and
other related infections of soft tissues.
Due to high oral bioavailability, patient can be shifted from Iv to
oral therapy.
It can be administered just once a day regimen as an alternate to
other fluoroquinolones in the treatment of respiratory infections.
74. It is less potent than ciprofloxacin
Primarily used in genitourinary tract
infections.
It is not useful in respiratory and systemic
infections due to gram positive cocci.
75. It is Difluorinated quinolone effective
against gram positive bacteria,
anaerobes and mycobacteria.
It is used in the treatment of
pneumonia, chronic bronchitis,
sinusitis etc.
76. Macrolides, as their name
indicates are characterized by a
large or macrocyclic lactone ring
with attached sugar residue
77. First macrocyclic antibiotic
From streptomyces erythreus.
Widely used antibiotic both in children as well as in adults.
It acts by binding with 50s ribosomal subunit of bacteria and
inhibit protein synthesis.
Narrow spectrum, low concentration are bacteriostatic,
however high concentrations are bactericidal.
79. The spectrum of activity also depends on the
concentration of drug.
It is more active in alkaline medium.
Effective against gram positive and few gram negative
organisms
Also effective against penicillin resistant staphylococci,
mycoplasma, campylobacter, legionella, gardnerella
vaginalis are also highly sensitive.
80. Substitute to penicillin in allergic patients for upper
respiratory tract infections, prophylaxis of rheumatic
fever.
Atypical pneumonia due to mycoplasma
pneumoniae,and whooping cough.
Wound and burn infections and severe impetigo not
responding to topical antibiotics.
82. Gastrointestinal side effects like nausea, epigastric
pain are common.
Diarrhoea occurs occasionally.
Skin rashes, hypersensitivity reaction, hepatotoxicity
Oral candidiasis, thrombophlebitis and fever have
been reported.
83. Azithromycin is an azalide antibiotic, a sub-class of the
macrolides.
Azithromycin differs chemically from erythromycin in that a
methyl substituted nitrogen atom is incorporated into the lactone
ring.
oral administration, rapidly absorbed and widely distributed
throughout the body.
Rapid distribution into tissues and high concentration within
cells result in significantly higher azithromycin concentration is
tissues than in plasma or serum.
84. 1. Lower respiratory tract infections:
2. Ear, nose and throat infections like tonsillitis,
sinusitis, otitis media and pharyngitis.
3. Skin infections
85. Adverse reactions include vomiting, dyspepsia,
flatulence, jaundice, palpitations, chest pain. Allergic
reactions include rash, photosensitivity and angioedema.
CNS side effects are headache, dizziness, vertigo and
fatigue.
86. Nitroimidazoles are imidazole heterocyclic compounds with a
nitro group that have been used to combat anaerobic bacterial
and parasitic infection .
88. After entering the micro-organisms by
diffusion , its nitro group is reduced to
intermediate compounds which cause
cytotoxicity probably by damaging DNA.
Dose: 200,400 mg TDS
93. All dental procedures that involve manipulation of
gingival tissue or the periapical region of teeth or
perforation of the oral mucosa
Suture removal
Extractions
Periodontal procedures (scaling, root planing,
probing, surgery, recall maintenance)
94. Implant placement and reimplantation of avulsed
teeth
Placement of orthodontic bands
95. Bacteremia is anticipated following invasive
dental procedures
Infective endocarditis is an uncommon but
life-threatening complication resulting from
bacteremia
96. 1. Prosthetic cardiac valve or prosthetic material used for
cardiac valve repair
2. Previous IE
3. Congenital heart disease
a. Unrepaired cyanotic CHD
b. Completely repaired defect with prosthetic material for
6months after procedure
c. Repaird CHD with residual defects
4. Cardiac transplant pts who develop cardiac
valvulopathy
97. WHICH PROCEDURES?
All dental procedures that involve
manipulation of gingival tissue
WHICH PROCEDURES DO NOT?
LA through non-infected tissue,
X-rays,
Placement of removable prosthodontic or orthodontic
appliances,
Placement of brackets,
Shedding of deciduous teeth,
Bleeding from trauma to the lips or oral mucosa
98. ABLE TO TAKE ORAL MEDS?
-Amoxicillin 50mg/kg
UNABLE TO TAKE ORAL MEDS?
-Ampicillin or Cefazolin 50mg/kg IV/IM
ALLERGIC TO PCN, ORAL?
-Clindamycin 20mg/kg or
Azithromycin/Clarithromycin 15mg/kg
ALLERGIC TO PCN, NON-ORAL?
-Clindamycin 20mg/kg IV/IM
100. CONCLUSION:
The role of antibiotics in odontogenic infections is of paramount
importance and one that cannot and should not be neglected.
The fact that the microbial flora responsible for odontogenic
infections is a limited one only emphasizes the need for proper
antibiotic selection and administration.
Too often in the look out for curing the infection, we as dental
practitioners tend to adopt a ‘shotgun approach’ and prescribe
unnecessary antibiotics.
101. 1. St. Joseph Literature Review Some good stuff to know about
kids‘ teeth.Wednesday, October 31, 2012 AAPD GUIDELINES
ON ANTIBIOTICS Resident: Elliot Chiu
2. Laurence L. Brunton ,John S.Lazo ,Keith L. Parker; Goodman
and Gilman’s The pharmacological basis of therapeutics; 11th
edi,McGraw Hill,2006
3. KD Tripathi :Essentials of medical pharmacology; Jaypee
brothers, 5th edi,2004
4. Naresh Kumar khanna; Principles of pharmacology for dental
students, CBS publishers, 3rd edi,2010
5. Antibiotic & antimicrobial use in dental practice 2nd ed. by
Michael G. Newman.
6. Tetracycline induced tooth discoloration Venkateswarlu M1
and Naga Sailaja R2
Editor's Notes
Dose has to be reduced in renal failure;
The antimicrobial compounds containing a sulfonamido (SO2 NH2) group are called sulfonamides and a free amino group at the para position is required for its antibacterial Activity
because of bacterial resistance and discovery of many safer and more effective Antibiotics, the utility of sulfonamides is limited to few infections which are of clinical interest.
