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ANALGESICS
CLASSIFICATION OF ANTIBIOTICS
Intracellular Extracellular
Penicillins
Tetracyclins
cephalosporins
chloramphinicol
polymyxin
aminoglycosides
bacitracin
clindamycin
polyenes
1. Inhibitors of Cell Wall
synthesis
Beta-lactams
•Penicillins
•Cephalosporins
•Monobactams
•Carbapenems
Glycopeptides
Fosfomycins
CLASSIFICATION OF PENICILLIN
I) Natural penicillins :
Penicillin G (Benzyl penicillin),procain penicillin-g, benzathine penicillin.
II) Semisynthetic penicillin-
1.Acid resistant penicillins :
Phenoxymethyl penicillin (penicillin V)
2 . Penicillinase – resistant penicillins :
Acid labile : Methicillin, nafillin, cloxacillin, dicloxacillin
Acic resistant: flucloxacillin.
3. Extended spectrum penicillins :
a.Carboxypenicillins : Carbenicillin, ticarcillin,
b. Aminopenicillin : Amipicillin, amoxicilllin.
c. Ureidopenicillin : Mezlocillin, piperacillin.
4. Beta lactamase inhibitors : Clavulanic acid, Sulbactum.
Cephalosporins
First generation- Second generation- Third generation Forth generation
More active
•Aminoglycosides
•MLSK (Macrolides, Lincosamides, Streptogramins,
Ketolides)
•Tetracyclines
•Glycylcyclines
•Phenicols
•Oxazolidinones
•Ansamycins
AMINOGLYCOSIDES
•Broad spectrum of action
•Rapid bactericidal effect
• Inhibitors of Protein Synthesis
• Related in structure and function
• Drugs differ based on location of radical
groups attached to the 3 ring basic
structure
Kanamycin
USES •develops resistance quickly
•Gram-positives, except Streptococus
and Enterococcus.
•Hospital use only
•combine with aminoglycoside • Nephrotoxic and toxic for ears
(Gentamicin or Streptomycin) & •Drug Dosage Adjustment:
penicillin, ampicillin or vancomycin for
severe enterococcal infections •Monitoring mandatory.
(Synergy) •Control the serum level for peak -ensure
• In serious infection, with beta-lactams
or fluoroquinolones the bactericidal effect and avoid side
•Gram-negative nosocomial infections effects
•severe systemic infections
Tetracycline
Broad spectrum antibiotic.
Low absorption through git.
Rapid renal excretion,
Low phototoxic
Marked alteration of intestinal bacteria.
Demiclocycline-
Intermediate potency.
High plasma binding capacity.
Slower renal excretion.
Highest phototoxic.
Doxicycline-
High potency.
Complete absorbtion from intestine.
High plasma binding.
T1/2- 18-24 hr.
Leaast alteration of intestinal flora.
Low toxixcity &metabolised in liver.
Erythromycin (Macrolides )
•anti bacterial spectrum – similar penicillin.
•against penicilin resistant staphylococci.
•small intestine.
•partially destroyed by gastric juice, (enteric coated tablets)
Is a lincosamide
•Natural Resistance
•Enterococcus –poorly expressed
•S. pneumoniae
•Ps. aeruginosa (impermeability)
USES-
•UTI’s
• otitis media in children,
chronic bronchitis in adults,
• enteritis
•Travelers’ Diarrhea.
5. Inhibitors of Nucleic Acid Synthesis
•Quinolines
•Furanes
Quinolones • 1st Generation Quinolones:
Gram-negatives, UTI
high concentrations -infection.
• Fluoroquinolones: Garenoxacin
Gram-negative and Gram-positive ( Anaerobes,
Atypicals, S.pneumoniae and Pseudomonas)
• A. polyenes-
• Amphotricine B, nystatin, hamycin,natamycin
• B. heyerocyclic benzofuran-
• Griseofulvin
Metronidazole
USES-
•Adverse Effectsantibiotic
Nitroimidazole
•anaerobes in intra-abdominal abscess, •Nausea, bacteria
•anerobic diarrhea,and
metallic taste
protozoa
(B.fragilis, spp, Fusobacterium •IV adminstration-
•antibiotic, Thrombophlebitis
amebicide, and antiprotozoal.[
spp, Clostridium spp, Peptostreptococcus
spp, Prevotella spp ) •DOC-mild-to-
•Infrequent adverse effects
moderate Cl.difficle infection
include: Hypersensitivity reactions
• bone and joint infections, septicemia,
(rash, itch, flushing, fever), headache,
•endometritis, or endocarditis. •MOA-taken up by diffusion,
dizziness, vomiting, glossitis,isstomatitis,
selectively
dark urine,absorbed by anerobic
and/or paresthesia.
•Pseudomembranous colitis due
•High doses
bacteria & protoza.
and/or long-term systemic
to Clostridium difficile
•Leukopenia, neutropenia, peripheral
•Helicobacter pylori eradication therapy, •non-enzymatically
neuropathy reduced by reacting
•CNS
with reduced
toxicity.ferredoxin, which is
•MDR -peptic ulcer disease
• National by
generated pyruvate
Toxiology oxido-reductase.
Program (NTP) -
•periapical abscess, periodontal abscess, human carcinogen
acute pericoronitis of impacted or partially •sulfinamides and thioether linkages with
erupted teeth; often used in conjunction cysteine enzymes deactivate these
with Amoxicillin critical enzymes.
MIC-MINIMAL INHIBITORY
CONCENTRATION
Quantitative Measure
• MIC = lowest concentration of antibiotic that inhibits growth
(measured visually)
• Interpretation of quantitative susceptibility tests is based on:
relationship of the MIC to the achievable concentration of
antibiotic in body fluids with the dosage given
•For treatment purposes, the dosage of antibiotic given should
yield a peak body fluid concentration 3-5 times higher than the
MIC
or
MIC x 4 = dosage to obtain peak achievable concentration
MBC – Minimum Bacterial Concentration
Quantitative Measure
• MBC = lowest concentration of antibiotic that
kills bacteria
PRINCIPLES FOR CHOOSING THE APPROPRIATE
ANTIBIOTIC
• Erythromycin estolate
• Tetracyclin
• Ampicillin
• Dose reduction :
– Chloramphinicol
– Metronidazole
– Clindamycin
PREGNANCY AND ANTIBIOTICS
Safe antibiotics
penicillins
cephalosporins
erythromycin
• Adjunctive treatment :
– Endodontic therapy or extraction
– Surgical drainage
– Many chronic dentoalveolar abscesses need
curettage.
Odontogenic infection, oral and
maxillofacial implications
Abscess
Therapeutic uses of antibiotics in maxillofacial
surgery
Pericoronitis :
•Acute pericoronitis, if severe, may require antibiotic therapy.
•Treatment - debridement, drainage of the site,
penicillin 500 mg qid,
amoxacillin 500mg qid,
clindamycin 300mg qid
•patient's mast cells are coated with IgE recognizing that specific allergen.
•then adjacent allergen-specific IgE -cross-linked on the mast cell surface & activated
•Semi synthetic penicillins such as ticarcillin and piperacillin contain the same
nucleus as penicillin G.
•Cephalosporins share a common beta-lactam ring with the penicillins - cross-
reactivity is quite low.
•3-7% of those with penicillin allergy, may have allergic reactions to
cephalosporins as well.
43
PAIN CONTROL STRATEGY
Post-Operative • Analgesic
Prescription
• Opioids 44
• Non-opioids
CLASSIFICATION
ANALGESICS
45
The major analgesic drug class
for treating endodontic pain
46
NSAIDS
Beneficiary actions due to PG synthesis
inhibition
• Analgesia.
• Antipyresis.
• Antiinflammatory.
• Antithrombotic.
48
Toxicities due to PG synthesis inhibition
Pyrazolone derivatives
Phenylbutazone, Oxyphenbutazone
(traditional NSAIDs)
Non selective COX
Indole derivatives
Indomethacin
Oxicam derivatives
Piroxicam, Tenoxicam
Pyrrolo-pyrrole derivative
51
Ketorolac
NON-SELECTIVE COX INHIBITORs
SALICYLATES: History
• In England 18th century- Reverend Freudman first -cure of
agues(Fever)
• willow bark was a bitter glycoside -Salicin, 1st isolated in
1829 by Leroux, -antipyretic effect.
• Sodium salicylate was 1st used for -rheumatic fever
• And as antipyretic in 1875 &
• its utility in the gout soon followed.
• Hoffman -prepared acetyl salicylic acid.
• 1899 introuduced by Dreses under the name aspirin.
ASPIRIN
• Rheumatoid arthritis.
• Osteoarthritis.
PROPIPHENAZONE
• Similar to metamizol.
INDOLE DERIVATIVES
(Indomethacin, Sulindac )
• Potent anti-inflammatory drug, comparable to
phenylbutazone.
58
Propionic acid derivatives
Ibuprofen
• Rated as the safest (SADR reporting system in U.K.)
• Better tolerated than aspirin.
• Anti- inflammatory,analgesic & antipyretic efficacy is
lower than high dose of aspirin.
• Most commonly used NSAID .
Dose: 400-800mg TD, Ibuprofen
250mg BD-TD, Naproxen
• Naproxen : more potent, but inhibits platelet aggregation &
prolong BT.
• 200mg Ibuprofen has same analgesic effect as
acetaminophen 650mg/ codeine 60mg
• 400mg and 600mg doses produced greater levels of
analgesia.
Opioids
CLASSIFICATION
•
64
Morphine
(Prototype)
Pharmacological Action:
CNS: interacts primarily with μ opiod
receptor
• Analgesia: strong analgesic; suppression of
pain is selective, without affecting other
sensations; degree increases with dose.
• Sedation: drowsiness, higher doses induce
sleep and coma.
•Codeine •Pethidine •Methadone •Tramadol
69
Ingle’s endodontics 6th Ed.
Systemic administration
Dexamethasone
• Very potent & highly selective glucocorticoid.
• Long acting.
• Pituitary depression.
• Used in inflammatory & allergic condition.
• Dose: 8mg loading dose,followed by 4 mg every
eight hours (upto max. 5 days).