ANTIBIOTICS AND

ANALGESICS

PRESENTED BY- DR SHRUTIKA

TULASKAR
( JR-I)
Contents

 Introduction
 General pharmacology
 Pediatric dosage formula
 History of antibiotics
 Classification of antibiotics
 Analgesics
 Classification of analgesics
 Conclusion
 references
Introduction

 Most common clinical situations in dentistry amenable to drug

therapy in children are pain and infection
 Antibiotics are one of the most frequently used as well as misused
drugs
 The proper knowledge of antibiotics is need of an hour for
providing good oral health
GENERAL PHARMACOLOGY

 DRUG-
According to WHO (1996)-”Drug is any substance or product that
is intended to be used to modify or explore physiological systems or
pathological states for benefit of recipient “

Essentials of medical pharmacology K D Tripathi 6th edition

 Drug nomenclature-
Chemical name
Nonproprietary name
Proprietary name
 PHARMACOKINETICS
Absorption
Distribution
Metabolism
excretion
 ABSORPTION-
Bioavailability-
It is a fraction of administered dose that reaches the systemic
circulation in unchanged form

Essentials of medical pharmacology K D Tripathi 6 th edition

 Distribution
Lipid solubility
Ionization at physiological pH
Extent of binding to plasma and tissue protein
Differences in regional blood flow
Volume of distribution-the volume that would accommodate all the
drug in body if the concentration throughout was the same as in
plasma
 Metabolism
 Phase 1- Oxidation, Reduction, Hydrolysis, Cyclization,
Decyclization
 Phase 2- Glucoronide conjugation, Acetylation, Methylation,
sulfate conjugation

Essentials of medical pharmacology K D Tripathi 6 th edition

 Excretion
Glomerular filtration
Tubular reabsorption
Tubular secretion
 Kinetics of elimination-
First order-
Zero order-
 Plasma half life-The plasma half life of drug is the time taken for
its plasma concentration to be reduced to half
It is dependent on volume of distribution and clearance of drug
from body
 PHARMACODYNAMICS-
 Enzyme inhibition
 Receptors
 Ion channels
 Transporters
PEDIATRIC DOSAGE FORMULAS-
 Young’s formula-
childs dose= age x adult dose
age +12
 Drillings formula-
childs dose= age x adult dose
20

Textbook of Pedodontics -Shobha Tandon 2 nd edition

 Anders in 1992-
 Doseρ=Doseɑ X wt.pd
wt. pd
Doseɑ =doseρ x wt.pd 0.7

wt. pd
Doseρ=dose of child wt. pd= weight of child
Dosea=dose of adult wt. pd =weight of adult

Textbook of Pedodontics -Shobha Tandon 2 nd edition

ANTIBIOTICS

 Antibiotics are substances produced by microorganisms , which

suppresses the growth or kill other microorganisms at very low
concentration without causing any harm to host
 HISTORY
Antibiosis -Louis Pasteur in 1889
Antibiotic –Selman Waksman in 1942
Sulphonamides- Domagk, Mietsch in 1938
Penicillin –Alexander flaming in 1928
Penicillin was established by Chain, Abraham and Florey in 1941
Classification

According to spectrum of activity-

 Effective against gram positive bacteria-
penicillins, macrolide, lincomycin,vancomycin
 Effective against gram negative bacteria-
streptomycin, aminoglycoside
 Effective against both gram positive and gram negative bacteria-
ampicillin, amoxycillin, carbenecillin, cephalosporin,

Textbook of Pharmocology and Pharmacotherapeutics –R S Sathoskar, S D Bhandarkar, Nirmala N Rege 20th edition
 Effective against acid fast bacilli-
aminoglycosides, quinolones
 Effective against fungi-
Nystatin, Amphotericin B,
 Effective against protozoa-
tetracyclins, poromomycin

Textbook of Pharmocology and Pharmacotherapeutics –R S Sathoskar, S D Bhandarkar, Nirmala N Rege 20 th edition

Based on mechanism of action
 Inhibit cell wall synthesis-
penicillins, cephalosporins, cycloserins
 Cause leakage from cell membranes-
polypeptides-polymyxins, bacitracin
polyenes-amphotericin B,nystatin
 Inhibit protein synthesis-
tetracyclins, chloramphenicol, erythromycin, clindamycin

Essentials of medical pharmacology K D Tripathi 6th edition

 Cause misreading of m-RNA code and affect permeability-
aminoglycoside-streptomycin, gentamycin
 Inhibit DNA gyrase-
fluoroquinolones
 Interfare with DNA function-
Rifampin, metronidazole

Essentials of medical pharmacology K D Tripathi 6th edition

 Interfare with DNA synthesis-
acyclovir
 Interfare with intermediary metabolism-
sulphonamide, trimethoprim, ethambutol

Essentials of medical pharmacology K D Tripathi 6th edition

Beta-lactam antibiotics-

These are antibiotics having beta lactam ring

 Penicillin
 Cephalosporin
 Monobactum
 Carbapenems
Penicillins

 First antibiotic to be used in 1941

 Obtained originally from fungus penicillium notatum
 Presently obtained from p. chrysogenum
 Has wide therapeutic range and is safest drug
 Most widely used penicillin is penicillin G or benzyl penicillin
Mechanism

 Bacterial cell wall consists of peptidoglycan which is cross linked

into a net that strengthens and provides rigidity to bacteria
 Penicillin binding proteins are bacterial enzymes located on cell
membrane and are responsible for biosynthesis of peptidoglycan
 Penicillins bind to these proteins and prevents synthesis and cross
linking of peptidoglycan which weakens the cell wall and makes
the organism vulnerable to rupture by solutes

Textbook of Pharmocology and Pharmacotherapeutics –R S Sathoskar, S D Bhandarkar, Nirmala N Rege 20 th edition

Bacterial resistance-
 The most common mechanism of bacterial resistance to beta
lactam antibiotics is production of beta lactamases that hydrolyses
the beta lactam ring and render the drug inactive
 Penicillin resistant strains of Staphylococci elaborate an enzyme
beta-lactamase(penicillinase)
 Other bacteria that produces penicillinase are E.coli, B.anthracis,
M.tuberculosis

Textbook of Pharmocology and Pharmacotherapeutics –R S Sathoskar, S D Bhandarkar, Nirmala N Rege 20 th edition

 Classification

 Natural - penicillin G
 Semisynthetic-
• penicillinase resistant penicillin – methicillin ,cloxacillin
• acid resisitant penicillin-phenoxymethyl penicillin(penicillin V)
• extended spectrum penicillin-
Aminopenicillin-Ampicillin,amoxicillin,
Carboxypenicillin-Carbenicillin
Ureidopenicillin-piperacillin
 Beta lactamase inhibitors-clavulanic acid , sulbactam
Penicillin G

 It is one of the most potent antimicrobial agents and effective

against gram positive bacterias
 Antibacterial spectrum-
 gram positive and gram negative cocci -Streptococci, Gonococci,
Meningococci,
 gram positive bacilli-Bacillus anthracis, C.diphtheria
Pharmacokinetics-
 It is acid labile and inactivated by gastric acid
 Only 1/3rd of oral dose is absorbed in active form, sc and i.m
absorption is more rapid
 Plasma t1/2 of penicillin G is 30 min and it is prolonged in
neonates and infants due to poor development of renal function
 Preparation and dosage-
 BENZYL PEN 0.5, 1MU inj.
 PROCAINE PENICILLIN G 0.5,1MU
Adverse effects-
 Allergy and anaphylaxis
 Superinfections
 Hyperrkalemia
 acute non allergic reactions
 Jarisch herxheimer reaction
Semisynthetic penicillin

Semisynthetic penicillins were developed to overcome following

drawbacks of benzyl penicillin-
Inactivation by gastric acid
Short duration of action
Poor penetration into csf
Narrow spectrum of activity
Development of resistant organisms
Possibility of anaphylaxis
 Classification-
 Acid resistant alternative to penicillin G- penicillin V
 Penicillinase resistant penicillins-Methicillin, Cloxacillin
 Extended spectrum penicillin-
Aminopenicillin-Ampicillin, bacampicillin, Amoxycillin
Carboxypenicillin-Carbenicillin, Ticarcillin
Ureidopenicillin-piperacillin, mezlocillin
 Beta lactamase inhibitors-Clavulanic acid, Sulbactam, Tazobactam
Penicillinase resistant penicillin

 These congeners have side chains that protect beta lactam ring from
attack by staphylococcal penicillinase
 These drugs are less sensitive to nonpenicillinase producing
bacterias and their only indication is infections caused by
penicillinase producing staphylococci
 Methicillin
 Highly penicillinase resistant but not acid resistant
 The term MRSA is used to refer beta lactam antibiotic resistant
staphylococci
 Most of MRSA strains are resistant to cloxacillin, flucloxacillin and
all beta lactam antibiotic
Dose- 1 g im or slow iv infusion every 4-6 hourly
 Cloxacillin
 Weak antibacterial activity than benzyl penicillin but is 5-10 times
more active than methicillin against resistant staphylococci
 Peak plasma levels are attained in an hour
 Highest drug concentration is seen in kidney and liver
 Dose- 0.5 -1g ,6hourly and maintainance dose is 250 mg
 Nafcillin
 more active than methicillin and cloxacillin but less active than
benzyl penicillin
 87% plasma protein binding
 Dose- 0.5 -1 g im,4-6 hourly and 25 mg per kg twice daily
Acid resistant penicillin

 Penicillin v
 Acid stable, oral absorption is better
 Peak blood level is reached in 1 hr and plasma t1/2 is 30-60 min
 Suitable for nonserious dental infection
 Dose : 125-250 mg 6 hourly
 CRYSTAPEN –V, KAYPEN
Extended spectrum penicillins

 Active against a variety of gram negative bacilli

 They are grouped according to the nature of side chain substitution
and spectrum of activity into amino-carboxy-ureido-penicillin
Aminopenicillins

 This group has an amino substitution in the side chain

 All the drugs have similar antibacterial spectra
Ampicillin
Amoxycillin
Bacampicillin
Ampicillin

 Active against all organisms sensitive to PnG

Many gram negative bacilli e.g. H. influenza, E. Coli, salmonella
Cocci e.g. pneumococci, gonococci, meningococci
 Pharmacokinetics
 Not degraded by gastric acid, oral absorption is incomplete but
adequate, food interferes with absorption
 It is partially excreted in bile and primary channel of excretion is
kidney but tubular secretion is slower than PnG
 plasma t1/2 is 1 hr.
 dose :0.5- 2 grams oral /IV depend on severity of infection, every 6
hrs.
 children 25-50mg/kg/day.
 Uses
 Broad spectrum of action covering both gram-positive and gram-
negative aerobic as well as anaerobic bacteria
 Urinary tract infections, respiratory tract infection, meningitis,
gonorrhea, typhoid fever, bacillary dysentry
 Adverse effect:
 Diarrhoea and rashes
Bacampicillin

 It is ester of ampicillin which is completely absorbed from GIT

 It is a prodrug and is largely hydrolysed during absorption, thus
higher plasma level are attained
 Dose: 400-800mg BD, PENGLOBE 200mg tab
Amoxycillin

 It became available in1972, it is in the WHO list of essential

medicines and it is most commonly prescribed medicine in children

 Oral absorption is better, food does not interfere with absorption,

higher and more sustained blood levels are produced
 More active against penicillin resistance strep. Pneumoniae
 First choice of drug for prophylaxis of local wound infection as
well as distant infection following dental surgery
Dr. Trophimus et al Antibiotics and its use inpediatric dentistry Int journal of applied dental sciences
2018;4(2)
 Dose: 0.25-1g TD oral/IM or slow IV injection
 children 25-50mg/kg/day in 3 divided doses, tab 125,250 mg
Oral suspension 125,250 mg/5ml
AMOXYLIN, NOVAMOX,SYNAMOX
Carbenicillin

 Active against pseudomonas aeruginosa

 It is neither penicillinase resistant nor acid resistant
 It is inactive orally and has to be administered IM or IV
 T1/2 is 1 hr
 Indicated in serious infections caused by pseudomonas or proteus
e.g. burns, urinary tract infection, septicaemia
 High doses have caused bleeding by interfering platelet funtions
 CARBELIN 1g, 5g per vial injection
Piperacillin

 This antipseudomonal penicillin is about 8 times more active than

carbencilllin
 Good activity against Klebsiella and some bacteroids
 Used in serious gram negative infections
 T ½ is 1 hr
 Dose : 100-150 mg/kg/day in 3 divided doses
 PIPRAPEN 1 g, 2g vials.
Beta – lactamase inhibitors

 Beta lactamase are a family of enzymes produced by many gram

positive and gram negative bacteria that inactivate beta lactam
antibiotics by opening the beta lactam ring
 Different beta lactamase differ in their substrate affinities
Clavulanic acid

 Obtained from Streptomyces clavuligerus, it has a beta lactam ring but no

antibacterial activity of its own
 It inhibits a wide variety of beta lactamases produced by both gram
positive and gram negative bacteria
 Clavulanic acid is a progressive inhibitor: inhibition increases with time
so called as suicide inhibitor
 Pharmacokinetics
 Rapid oral absorption and bioavailability of 60%
 Its elimination t ½ is 1 hr and tissue distribution matches
amoxicillin with which it is combined
 It is eliminated mainly by glomerular filtration
uses
 skin and soft tissue infection, dental infections and gonorrhea
 side effects are same as amoxicillin
 AUGMENTIN, ENHANCIN, AMONATE
Sulbactam

 It is semi synthetic beta lactamase inhibitor related chemically as

well as in activity to clavulinic acid
 It is also progressive inhibitor
 Sublactum does not induce chromosomal beta lactamases, while
clavulinic acid can induce
 Oral absorption is inconsistent so it is given parenterally
 It is combined with ampicillin
 this combination is indicated in gonorrhea and mixed aerobic
anerobic infection
 SULBACIN, AMPITUM: ampicillin 1g+sulbactum0.5g per vial
injection
 Adverse effects are pain at the site of infection, thrombophlebitis
of injected vein, rash and diarrhoea
Tazobatam

 it is similar to sulbactum and its pharmacokinetics matches with

that of piperacillin with which it is combined
 Used in severe infection like peritonitis,pelvic/urinary/respiratory
infections
 dose 0.5g combined with piperacillin 4g injected IV over 30 min 8
hourly
 PYBACTUM, TAZACT, TAZOBID
Cephalosporins

 These are group of semisynthetic antibiotics obtained from

cephalosporin-c from fungus cephalosporium
 They are chemically related to penicillins the nucleus of beta
lactam ring fused to dihydrothiazide ring
 Classification-

First
Second
Cephalothin Third Fourth
Cefuroxime
Cefazolin Cefotaxim Cefepime Fifth
Cefoxitine
Cefaclor Ceftrizoxime cefiperome Ceftaoline
Ceftrazone
Cephalexin Cefoperazone cephaloridine ceftobiprole
Cefuroxime
Cephadin
axetal
cephadroxil
 Cefazolin
 More active against klebsiella, e.coli
 Susceptible to staphylococcal beta lactamase
 Preffered for surgical prophylaxis
 T1/2 is 2hrs
 Dose-0.5 g 8 hourly for severe cases
 i.m or i.v for surgical prophylaxis 1 g ½ hr before surgery
 ACCIZON,ORIZOLIN
 Cephalexin
 orally effective first generation cephalosporin
 Used as an alternative to amoxicillin in dentistry
 T1/2 is 1 hr
 Dose-0.25g-1 g 6-8hourly, children 25-100 mg/kg/day in 4 equal
doses , cap 250 and 500 mg, oral suspension 125 and 25 mg/5ml
 CEPHACILLIN250 , SPORIDEX
 Cephadroxyl
 It has good tissue penetration including alveolar bone
 Exerts more sustained action at site of infection and can be given
12 hourly despite t1/2 of 1 hr
 Excreated unchanged in urine
 Frequently selected for dental infections
 Dose-0.5-1 g bd
 DROXYL 0.5, CEFADROX 0.5
 Cefuroximme
 Highly resisitant to beta lactamses (gram negative)
 Well tolerated by i.m route and has been used in some mixed
infection as well as for single dose i.m therapy of gonorrhoea
 Cefuroxime axetil
 Ester of cefuroxime effective orally though absorption is
incomplete
 Activity depend upon hydrolysis and release of cefuroxime
 Dose- 250-500 mg bd Frequently chosen for dental infection
 Ceftum,spizef125,250,500 mg tab and 125 mg /5 ml susp.
 Cefaclor
 Given orally and more active than first generation
 Dose- KEFLOR, VERCEF, DISTACLOR 250mg cap,125mg/5 ml
syrup ,50 mg/ml drops
 Cefprozil
 Oral absorption is good
 Active against strep.pyogenes , strep.pneumonae, H.influenza
 Indicated in bronchitis and skin infection
 Dose-250-500 mg bd child dose is 20 mg/kg /day
 ORPROZIL,ZEMETRIL250,500 mg tab,REFZIL 125mg/5ml and 250
mg/5ml syrup
 Cefotaxime
 Potent action on aerobic gram negative as well as gram positive
bacteria
 Indicated in meningitis ,life threatening hospital acquired
infections, septicaemia and infections in immune compromised
patients
 plasma t1/2 is 1hr
 Dose-1-2 g i.m or i.v 6-12 hourly
 OMNATAX, ORITAXIM,CLAFORAN 0.25,0.5g per vial inj
 Ceftizoxime
 Potent activity on gram negative as well as gram positive bacteria
but not on anaerobes
 T1/2 is 1.5 -2 hr
 Dose- 0.5-1 g i.m/i.v 8-12 hourly
 CEFIZOX, EPOCELIN 0.5 and 1 g per vial inj.
 Ceftriaxone
 Longer duration of action penetration in csf is good and it is
eliminated equally in urine and bile
 Shown high efficacy in a wide range of serious infection including
bacterial meningitis, multiresistant typhoid fever ,abdominal sepsis
and septicaemia
 Hypoprothrombinaemia and bleeding are specific side effects
 Dose-Oframax , Moncef,Montax 0.25 , 0.5 per vial inj, 1-2 g i.v or
i.m /day
 Ceftazidime
 Highly active against pseudomonas and specific indication are
febrile neutropenic patients and burns
 Plasma t1/2 is 1.5-1.8 hr
 Adverse effects are neutropenia ,thrombocytopenia,rise in plasma
transaminases and blood urea
 Dose-0.5-2 g i.m or i.v every 8 hr children30 mg /kg/day
 Fortum,Cefazid,Orzid 0.25,0.5 and 1g per vial inj.
 Cefoperazone
 Indicated in severe urinary ,biliary, respiratory ,skin soft tissue infection
meningitis and septicaemia
 Primarily excreted in bile t1/2 is 2 hr
 If has hypoprothrombinaemic action but does not affect platelet function
 A disulfiram like reaction with alcohol has been reported
 Dose-1-2 gi.m /i.v 12hourly
 Magnamycin 0.25g ,1 g ,2 g inj cefomycin ,negaplus 1 g inj
 Cefixime
 Highly active against enterobacteriacae, H.infiuenzae,
strep.pyogenes
 Longer acting and t1/2 is 3 hr
 Indicated in respiratory infections
 Dose- 8mg/kg/day in2 divided doses,Topcef, Orfix 100,200 mg
tab/cap ,Taxim-o 100mg ,200 mg tabs
 Cefpodoxime proxetil

 Orally active ester prodrug of cefpodoxime

highly active against enterobacteiaceae and streptococci it inhibits
staph. aureus
 Indicated in respiratory ,urinary ,skin and soft tissue infection
 Dose- 200 mg bd
 Cefoprox,cepodem,doxcef 100 ,200 mg tab, 100mg /5 ml dry syrup
 Cefdinir
 Orally active and has good activity against many beta lactamase
producing organisms
Most respiratory pathogens including gram positive cocci are
susceptible
Indicated in pneumonia acute exacerbation of chronic bronchitis and
skin infection
Dose-300 mg
Sefdin,Adcef 300mg cap,125 mg/5ml susp.
 Ceftibuten
 Orally active against gram positive and few gram negative bacteria
but not staph. aureus
 Indicated in respiratory ,ent and orodental infection
 Dose-200 mg bd or400 mg od
 Procadax 400mg cap ,90 mg /5ml powder for oral suspension
 Fourth generation
 This group is characterized by non-susceptibility to inducible
chromosomal beta lactamase while retaining high activity against
enterobacteriacae and spectrum of 3rd generation compounds
 Cefepime
 Developed in 1990
 Has some antibacterial spectrum to that of 3rd generation
compounds but highly resistant to beta lactamase
 Due to high potency and extended spectrum it is effective in many
serious infection like hospital acquired pneumonia ,febrile
neutroprenia ,bacteremia and septicaemia
 Dose-1-2 g i.v 8-12 hourly
 Kefage,Cepime 0.5 mg ,1 g inj
 Toxicology
 Hypersensitivity reaction
 Cross reactivity with penicillin
 Cefamandole, cefoperazone ,cefotetan may cause
hypoprothrombinemia and disulfiram like reaction with alcohol
CHLORAMPHENICOL

 Inhibit protein synthesis by binding to 50 s ribosomal subunits and

cause the inhibition of peptidyl transferase
 Bacteriostatic with broad spectrum of activity
 Resistance develops to this drug due to formation of inactivating
enzyme acetyl transferase
 Drug of choice for typhoid
MACROLIDES

 These are antibiotics having macrocyclic lactone ring with attached

sugars
 Bind to 50s ribosome and block translocation of peptide chain
 Uses-
 Chanchroid, atypical pneumonia ,whooping cough by bordetella
pertusis
 Adverse effects-
 Allergy
 Cholestasis
 Reversible ototoxicity
 ERYTHROMYCIN
 Isolated from Streptomyces erythreus 1952 and employed mainly
as an alternative to penicillin
 Bacteriostatic at low but can be cidal at high concentration depends
on organism and its rate of multiplication
 Partially destroyed by gastric juice
 Plasma t1/2 is 1.5 hr
 Dose-250-500 mg 6 hourly ,children 30-60m mg/kg/day
 Erysef 250 ,erythrocin 250
 AZITHROMYCIN
 This azilide congeners of erythromycin has an expanded spectrum
improved pharmacokinetic better tolerability and drug interaction
profiles
 Acid stable ,rapid oral absorption ,larger tissue distribution and
intracellular penetration
 Indicated in orodental infection,pharyngitis,tonsillitis ,sinusitis
 Side effects are mild gastric upset, abdominal pain ,headache and
dizziness
 Dose-Azithral 250,500 mg tab,100 mg kid tab, 100 mg/5ml susp.
TETRACYCLINS

 Bind to 30 s ribosomal subunit and inhibit the binding of aminoacyl

t-RNA to a site
 All tetracyclins are excreted in urine except doxycycline
 Tetracyclns
 Oxytetracyclin
 Doxycyclin
 Minocyclin
 Uses-
 Ricketssial fever and relapsing fever
 Brucellosis
 Cholera
 Leprosy
 Atypical pneumonia
 Maleria
 Toxicity-
 Kidney failure
 Photosensitivity
 Insipedus diabetes
 Liver toxicity
AMINOGLYCOSIDES

 Bactericidal inhibitors of protein synthesis

 These binds to 30s and 50s ribosomes and freeze initiation interface
with polysome formation and causes misleading of m-RNA code
 Penetration across cell membrane depends on oxygen transport
 Not absorbed orally and don’t cross BBB
 Excreted primarily by glomerular filtration
 Resistance develop due to formation of inactivating enzyme which
acetylate,phosphorylate or adenylate the aminoglycoside
 Systemic aminoglycoside- streptomycin, gentamycin, sisomycin,
amikacin, kanyamycin
 Topical aminoglycoside- neomycin, framycetin
 Uses-
 Gentamycin, tobramycin, amikacin are effective against gram
negative organism
 Streptomycin is first line drug for treatment of tuberculosis, plaque
and tularemia
 Netilmycin is used for serious infection only
 Neomycin can also be used orally for gut sterilization in hepatic
encephalopathy
SULPHONAMIDES

 These drugs are bacteriostatic and act by inhibiting folate synthase

comparatively
 Selective toxicity to bacteria is due to mammalian cells do not
synthesize folic acid and utilize preformed folic acid in diet
 Not effective in presence of pus
 Classification
 Short acting-Sulfisoxazole, Sulfamethiazole, Sulfacytine
 Intermediate acting-Sulfamethoxazole, Sulfadiazine
 Long acting-Sulfadoxine
 Use-
 Sulfacetamide is used for ocular infections where as mafenide and
silver sulfadiazine are used in burn patients
 Sulfadiazine can be used for nocardiosis and sulfisoxazole for uti
 Sulfasalazine and olsalazine are used for treatment of ulcerative
colitis
 Sulfadoxine and pyrimethamine is used for maleria
 Side effects-
 Aplastic anaemia
 Crystalluria
 Rashess
 Hemolysis in G6PD deficiency
 Cotrimoxazole
 fixed drug combination of trimethoprim and sulfamethoxazole in a
ratio of 5:1
 Bactericidal and acts by sequential blockade at two steps in the
DNA synthesis
 Uses-
 Effective in UTI ,respiratory tract infection ,
tonsillitis ,pharyngitis , sinusitis and otitis media
 Drug of choice for pneumocystitis nocardiosis
 Side effects
 Nausea, vomiting, stomatitis, headache
 Blood dyscrasia occurs rarely
 Neonatal hemolysis and methaemoglobinaemia can occur
QUINOLONES

 Synthetic antimicrobial having a quinolone structure

 Nalidixic acid is first derivative which is introduced in mid 1960
 Active against gram negative bacteria
 Acts by inhibiting bacterial DNA gyrase
 Absorbed orally partially metabolised in liver and excreted in urine
 Plasma t1/2 is 8 hrs
 Resistance to nalidixic acid develops rapidly
 Use-
 Primarily used as urinary antiseptic and in diarrhea
 Side effects-
 Gi upset and rashes
 Headache , drowsiness,vertigo
FLUOROQUINOLONES

 These are quinolone antimicrobials having one or more fluorine

substitution
 First generation fluoroquinolone introduced in 1980 having one
fluorine substitution
 In the 1990 compound with additional fluoro and other substitution
have been developed
 Classifacation
First
Norfloxacin, Lomefloxacin
Second-
Ciprofloxacin, Ofloxacin
Third-
Levofloxacin, Pefloxacin
Fourth
Moxifloxacin fleroxacin
 Action- They inhibit enzyme bacterial DNA gyrase which nicks
double standed DNA, introduces negative super coiling of the
strands and then reseals nicked ends.
Lincosamide antibiotics

 Clindamycin-
 It bind to 50s ribosomes , effective against anaerobic Bacteria
 Widely distributed in tissue fluids and tissue including bone
 It is an alternative drug in penicillin resistant anaerobic infection
 Used in osteomyelitis of jaws
 Side effects are rashes , urticaria , abdominal pain but major
problem is diarrhea
 dose- 150-300 mg qid oral, 200-600 mg i.v 8 hourly
 Dalcap 150 mg , Clincin 150 mg
 VANCOMYCIN
 It is glycopeptide antibiotic discovered in 1956 as a penicillin
substitute
 Bactericidal ,acts by inhibiting bacterial cell wall synthesis
 t1/2 is 6 hour
 Systemic use is restricted to serious MRSA infections for which it
is most effective drug
 Vancocin-cp, vancogen 50mg/vial inj.
 Nitroimidazole
 Metroimidazoles- metronidazole the prototype member of this
class was introduced in 1956 for trichommonas vaginitis and later
found to be effective antiprotozoal drug
 Effective against gram negative bacteria only
 Inhibit cell mediated immunity to induce mutagenesis and to cause
radiosensation
 Plasma t1/2 is 8 hrs
 Use –
 Oro-dental infection
 Drug of choice for ANUG
 periodontitis, pericoroniitis, acute apical infection and in some
endodontic infections
 Side effects-
 Anorexia ,nausea, ,metallic taste and abdominal cramps
 Urticaria, flushing, itching
 Prolonged administration may cause peripheral neuropathy
 Dose- flagyl, Metrogyl ,Metron
 Tinidazole
 Equally effective as metronidazole but metabolism is slower t1/2 is
12 hrs
 Dose-Tiniba 300, 500mg tab
Choice of antibiotic-
 Age
 Renal and Hepatic function
 Local factors
 Drug allergy
 Impaired host defence
 Pregnancy
 Genetic factor
Problems that arise with use of antibiotics-
 Toxicity
 Hypersensitivity
 Drug resistance
 Superinfection
 Nutritional deficiencies
 Masking of infection
Add on-
Terminologies

 Pharmacology- pharmacology is the art and science of drugs

 Pharmacognosy- The science of identification of drug from natural source
 Pharmacy- The science of identification, selection, preservation,
standardization, compounding and dispensing of medicinal substance
 Toxicology-The science of poison which includes detection and
measurement of poison as well as treatment of poisoning

Textbook of pharmacology and pharmacotherapeutics ,RS Satoskar, SD Bhandarkar,N Rege 20 th edition

 Pharmacodynamics-(What the drug does to body) the quantitative
study of biological and therapeutic effects of drug and their
pharmacological response
 Pharmacokinetics- (What the body does to the drug) the study of
absorption, distribution, metabolism and excretion of drugs
 Chemotherapy-The effect of drugs upon microorganisms and
parasites,living and multiplying in living organisms

Textbook of pharmacology and pharmacotherapeutics ,RS Satoskar, SD Bhandarkar,N Rege 20 th edition

 Pharmacopoeia- It is an official code containing selected list of
established drugs and medicinal preparations with discriptions of
their properties
 Most commonly used antibiotics in children

Drug Dosage Available forms Side effects contraindications

Oral 20-30 mg/kg/day Cap 250,500mg

in 3 divided dose(8 Tab 125,250 mg Increased
Amoxicillin hourly) Powder for oral thrust,nausea,pruritus Hypersensitivity to
suspension 50 mg/ml and Angioneurotic edema, penicillins
125,250 mg/5ml anaphylaxis
Amoxicillin+ Oral 20-40 mg/kg/day Cap 250 mg,powder for Discoloured Hypersensitivity to
clavulanate in 3 doses (8 hourly) oral suspension125,250 tongue,glossitis,hyperkale penicillins
potassium /5ml mia,anaphylaxis
Amoxicillin+ 50-100 mg/kg in 4 Tab 250,500mg, powder Increased thrust, Hypersensitivity to
cloxacillin doses 6hourly for oral suspension urticaria,hyperkalemia,an penicillin
125,250mg/5ml aphylaxis
Ampicillin 50-100mg/kg/day in 4 Tab 250,500mg Discoloured Hypersensitivity to
doses tongue,glomerulonephriti penicillin
s,anaphylaxis,
edema
Drug dosage Available Side effect contraindications
form
Cephalexin 50-100mg/kg Cap Candidiasis,glossitis,p Hypersensitivity to
in 4 doses 250mg ,125 seudomembranous penicillin,
mg/5ml colitis,nephrotoxicity pregnancy,infants<1
suspension month
500mg
Metronidazole Po 5mg/kg tid 400mg Dry mouth,furry Hypersensitivity,renal
tongue,leukopenia,ab disease,pregnancy,heptic
dominal pain disease
Erythromycin 30-50mg Tab 250- Candidiasis,rash,pruri Hypersensitivityto pre
/kg/day in 500mg,125mg/ tis,pseudomembranou existing hepatic disease
4doses 6 5ml suspension s tinnitus
hourly

Textbook of pedodontics Shobha Tandon 2nd edition

Brand names and manufacturers

Drug brand Manufacturer

Amoxycillin Novamox syrup Cipla pharmaceuticals
125mg/5ml,Cipmoxcap
250,500 mg, Novamox tab
125mg

Acmox tab 250,500 Acme pharmaceuticals

mg ,Acmox 125 mg/5ml
Amoxicillin + Blumox cv kid tab Blue cross pharma.
clavulanic acid
Augmentin tab 250 mg, GSK
Augmentin dry syr
Augpen susp Zuventus
Drug brand manufacturer
Amoxicillin + cloxacillin Novaclox kids tab Cipla
(125 + 125 )
Emoxin kid tab M M lab
Sporigram dry syr 125 Arbro pharma
mg/5ml
Ampicillin Ampisyn cap 125,250,500 cipla
mg
Ampilin syr 125mg/5ml Hetero hc
Cephalexin Phexin kid tab 125 mg, GSK
Phexin dry syr 250mg/5ml
Acfex tab 125 mg,250 mg Acme
Drug brand manufacturer
Erythromycin Arthrox 250 mg tab Apple biotech
Eltocin 125mg, 250 mg IPCA
tab,Eltocin susp 125mg/5ml
Metronidazole Flagyl 200 mg,400 mg tab, AHPL
Flagyl susp 200 mg/5ml
Metrogyl 200 mg,400 mg tab, JB chemicals
Merogyl susp 200 mg/5ml
 Antibiotic prophylaxis for infective endocarditis in children

Drug Oral
Amoxicillin 50 mg/kg 1 hour prior to procedure and
25 mg/kg 6 hours after initial dose
Erythromycin 20 mg/kg 1 hour prior to procedure and
10 mg/kg 6 hour after initial dose
Clindamycin 10 mg/kg 1 hour prior to procedure and 5
mg /kg 6 hour after initial dose

Textbook of pedodontics Shobha Tandon 2nd edition

Pediatric drug dosage formulas

 Clark’s rule- Weight of child in pounds X adult dose = Child’s dose

150 pounds
 Modified weight rule- Weight (kg) X adult dose
50 kg
 Young’s rule- Age of child X Adult dose = child’s dose
Age+12
 Fried’s formula- Age in months X adult dose ( for infants less than 2 years)
150
 Body surface area method-
Body surface area of child(m²) X adult dose
1.73m²
 Penna’s formula- Adult dose X child’s weight
Child’s weight/2+30
 Dilling’s formula- Age in years x adult dose
20
Gracieli P, Crystina A et al, comparative study of rules employed for calculation of pediatric
dose ;Journal of applied oral science ;2005 (13)
 Cowling’s rule- Age at next birthday X adult dose
24
 Bastedo’s rule- Age + 3 X adult dose
30

Gracieli P, Crystina A et al, comparative study of rules employed for calculation of pediatric dose ;Journal of applied oral
science ;2005 (13)
 Ander’s rule- Dose(p) = Dose(a) X wt. pd
wt. ad
 Salisbury formula- child weighing less than 30 kg: weight x 2=% of adult dose
child weighing more than 30 kg:weight + 30=% of adult dose

Gracieli P, Crystina A et al, comparative study of rules employed for calculation of pediatric dose ;Journal of applied oral
science ;2005 (13)
ANALGESICS
Introduction

Algesia(pain)- is a ill defined ,unpleasant sensation, usually evoked by

an external or internal noxious stimulus
Analgesic –A drug that selectively relieves pain by acting in the CNS
or on peripheral pain mechanisms, without significantly altering
consciousness

Textbook of pharmacology and pharmacotherapeutics RS Sathoskar, SD Bhandarkar 20 th edition

Concepts of pain in children-
 Children have higher tolerance to pain
 Pain perception is low because of biologic immaturity
 Little or no memory of painful experience
 More sensitive to side effects of analgesics
 Special risk for addiction to narcotics

Textbook of pedodontics Shobha Tandon 2 nd edition

 Types of pain –
 Acute pain-Short duration , localized
 Chronic pain-Intermittent or constant pain with different intensities,
long duration
 Dental pain – Aδ and c fibres are responsible for dental pain
 Pain is an inflammatory condition resulting from tissue damage ,
infection or invasive treatment
 Terminal nerve endings at site of injury exhibit an enhanced neural
response leading to peripheral sensitization of pain
 Enhanced functional status of pain processing at level of CNS leads
to central sensitization of pain
Pain management in infants, children and adolcents; the reference manual of pediatric dentistry
2019
 Classification of analgesics
 Non-opiods(NSAIDS)
Nonselective COX inhibitors
Preferential COX-2 inhibitors
Selective COX-2 inhibitors
Analgesic-antipyretic with poor anti-inflammatory action
 Opoid analgesics-Natural, semisynthetic, synthetic

Textbook of pharmacology KD Tripathi 6th edition

 OPOID ANALGESICS-
The word opiates refers to products obtained from opium poppy
Opoid drugs produce their effect by binding to opoid receptors which
are widely distributed in the CNS and other tissue
Opoid receptors are-mu, delta, kappa, nociception

Pain management in infants, children and adolcents; the reference manual of pediatric dentistry 2019
 Classification of opoids
Natural opium alkaloid-
morphine, codeine
Semisynthetic opiates-
Diacetylmorphine
Synthetic opiods-
pethidine , methadone, Tramadol
 Complex action opiods and opiod antagonist-
Agonist- antagonist- pentazocine
Partial agonist-antagonist– buprenorphine
Pure antagonist- naloxone, naltrexone

Textbook of Pharmacology KD Tripathi 6 th edition

Morphine-
It is alkaloid of opium and is used as sulfate or hydrochloride
It causes analgesia by acting on mu receptors situated in higher
centers and spinal cord

Textbook of pharmacology and pharmacotherapeutics RS Sathoskar, SD Bhandarkar, N Rege 20th

edition
 Pharmacological actions-
CNS –analgesia, sedation
Respiratory depression
CVS-Vasodilatation
GIT-constipation
 Pharmacokinetics
High first pass metabolism
Plasma protein binding -30 %
Freely crosses placenta and affect foetus more than mother
Primarily metabolized in liver
T1/2 -2-3 hours
 Uses-
Pain relief
Sedation and sleep
Preanaesthetic medication
 Side effects-
Sedation
Apnoea
Acute morphine poisoning
Dependance
 Contraindications-
 Infants and elderly are more susceptible to respiratory depressant
action of morphine
 Bronchial asthma
 Head injury
 Hypotensive state
 Dose- oral-10-50 mg
 parenteral- 10-15 mg im or sc
 Children -0.1 -0.2 mg/kg
 Injection- Morphine Sulphate 10 mg/ml
 Tablet- Morf( cipla) 10,20 ,30 ,100mg
 Codeine-
It is methyl morphine occurs naturally in opium and it is partly converted
to morphine in body
Orally well absorbed , single dose act for 4-6 hours

Textbook of pharmacology and pharmacotherapeutics RS Sathoskar, SD Bhandarkar, N Rege 20 th edition

 Use-
As analgesic
As a antitussive
As a antidiarrhoeal agent
Dose- Adult-10-30 mg , child-0.5-1mg/kg ,Codein Sulphate 15 mg tab
 Fentanyl-
 A pethidine congener 80-100 times more potent than morphine
both in analgesia and respiratory depression
 Due to high lipid solubility it enters brain rapidly and induce
analgesia in 5 min
 Alfentanyl and Remifentanyl-
 These are potent synthetic opoid analgesics with 1/4 to1/10 potency
of fentanyl
 Rapid onset of action 1-1.5 min

Textbook of pedodontics Shobha Tandon 2nd edition

 Uses-
 Short painful procedures requiring analgesia and blunting of stress
reflex
 Longer neurosurgical procedures
Alfenta,ultiva
 Tramadol
Centrally acting analgesic
Good oral availability
T1/2 is 3-5 hrs
It causes less respiratory depression, sedation, constipation and rise in
biliary pressure than morphine
Use-
Mild to moderate intensity short lasting pain due to diagnostic procedures,
injuries
Chronic pain

 Dose- adult- 50 -100 mg

 child-1-2 mg /kg 4-6 hourly
Damadol ,Ultracet( tramadol 37.5 mg+acetaminophen 325 mg)
 Side effects of opiods-
Short term long term
Euphoria constipation
Slow heart rate loss of libido
Loss of cough reflex loss of apetite
Possibility of stroke addiction
 NON OPOID ANALGESICS/NSAIDS-
All drugs in this class have analgesic, antipyretic and anti-
inflammatory actions
They act primarily on peripheral pain mechanism, but also on CNS to
raise pain threshold
 Mechanism of action- During fever, inflammation and pain
Arachidonic acid (AA) is liberated from phospholipid fraction of
cell
 AA is then converted into prostaglandins via cyclooxygenase
pathways( COX 1,COX 2)
 Prostaglandins in CNS lowers the pain threshold of central pain
circuits
 They also sensitizes the chemical receptors of afferent pain endings
to other mediators such as histamines and bradykinins
 NSAIDs act by inhibiting the prostaglandin by acting on COX 1
and COX 2
Classification-
 Nonselective COX inhibitors-
Salicylates- aspirin
Propionic acid derivative- Ibuprofen
Anthranilic acid derivative- Mephenamic acid
Aryl acetic acid derivative- Diclofenac,Aceclofenac
Oxicam derivative- piroxicam
Pyrollo-pirole derivative- Ketorolac

Textbook of pharmacology and pharmacotherapeutics RS Sathoskar,SD Bhandarkar 20 th edition

Indole derivative- Indomethacin
Preferential COX-2 inhibitor- Nimesulide
Selective COX-2 inhibitor- Celecoxib, etoricoxib
Analgesic-antipyretic with poor antiinflammatory action-
Paraminophenol derivative- paracetamol
Pyrazolone derivative- metamizol

Textbook of pharmacology and pharmacotherapeutics RS Sathoskar,SD Bhandarkar 20 th edition

 Salicylates-
Aspirin-
It is acetyl-salicylic acid
It is converted in the body into salicylic acid which is responsible
for its action
 Pharmacological actions-
Antipyretic, analgesic, antiinflammatory action
Respiratory stimulant
Acid base and electrolyte balance
CVS-vasodilatation
Blood-antiplatelet action
 Adverse effect-
Hypersensitivity
Reyes syndrome
Acute salicylate poisoning
 Uses-
As analgesic, antipyretic
Acute rheumatic fever
Rheumatoid arthritis
Osteoarthritis
Postmyocardial infarction
Dose-Aspirin 350 mg tab,Colspirin 100,325,650 mg tab
 Propionic acid derivative-
Ibuprofen was first member of this class to be introduced in 1969 as
alternative to aspirin
It has been rated as safest conventional NSAID by spontaneous
adverse drug reaction reporting system UK

Laskarides C et al,update on analgsics for adult and pediatric dental patients , Dent clin N AM 2016(347-
366)
Uses-analgesic and antipyretic
Rheumatoid arthritis
Soft tissue injuries, dental extraction
 Dose-
 Children-10-15mg/kg/dose
 Brufen, Ibugesic(200 mg,400 mg), Ibuclin jr100,125 mg
Diclofenac sodium-
It inhibit PG synthesis and somewhat COX-2 selective
Neutrophil chemotaxis and superoxide production at inflammatory
site are reduced
Uses-Rheumatoid arthritis, toothache, post traumatic conditions
Adverse effects- Epigastric pain, nausea,dizziness

Textbook of pharmacology and pharmacotherapeutics RS Sathoskar,SD Bhandarkar 20 th edition

 Dose-
Children over 1 year 1-3 mg/kg/day in divided dose
Adult-50 mg tds ,Voveran, Diclonac,Movonac
 Ketorolac-
Potent analgesic and modest antiinflmmatory activity
It inhibits PG synthesis and relieves pain by peripheral mechanism
It is rapidly absorbed after oral and im administration
It is highly plasma protein bound
Adverse effect-abdominal pain,ulceration,headache
Use-postoperative dental and musculoskeletal pain
Dose-10-20 mg 6 hourly ,Ketorol
 Nimesulide-
It is a weak inhibitor of PG synthesis
It is completely absorbed orally and it is 99 % plasma bound and t1/2
is 2-5 hours
Adverse effects-heart burn, rash, pruritus,dizziness
Use-sports injuries, sinusitis,dental surgery,backache
Dose- 100 mg bd,Nimulid,Nimegesic
 Paracetamol-
It is a deacetylated active metabolite of phenacetin
It acts centrally by raising pain threshold but it has weak anti-
inflammatory action
Adverse effect-
Acute paracetamol poisoning-(dose>150 mg /kg)
Abdominal pain
It is not recommended in premature children for fear of hepatotoxicity
 Uses-
Migraine
Musculoskeletal pain
Antipyretic
Dose-0.5-1g tds, infants 50mg, children 1-3 years 80-160 mg, 4-8
years 240-320 mg, 9-12 years 300-600mg
Crocin 0.5,1g tab,Paracin 500mg tab, 125 mg/5ml syrup, 150 mg/ml
paediatric drops,Dicloran A tab (Diclofenac 50 mg + paracetamol 325
mg)
 commonly used drugs and dosages
Drug Dose(mg/kg) Frequency Max dose per
day(mg/kg/day)
Aspirin 10-15 4-6 90
Ibuprofen 5-10 6-8 40
Acetaminophen 10-15 4-6 100
children
Acetaminophen 10 4-6 75
infant
Diclofenac 1-3 4-6 40

Laskarides C et al,update on analgsics for adult and pediatric dental patients , Dent clin N AM 2016(347-
366)
Conclusion

As a dental practitioner proper knowledge of antibiotics and its

prescription is essential as it plays important role in our day to day
clinical practice for treatment of oral and dental infection
References

 Textbook of pharmacology and pharmacotherapeutics- R. S.

SATOSHKAR (12th edition).
 Essentials of medical pharmacology- KD TRIPATHI.(6th edition)
 Textbook of pedodontics- SHOBHA TANDON.( 2nd edition)
 The short textbook of medical microbiology –SATISH GUPTE( 9th
edition)
 Davidson’s principles and practice of medicine( 20th edition)
 Dr. Trophimus G, Dr Vishnu R et al Antibiotics and its use in
pediatric dentistry: A review 2018 ;4(2)
 Christopher D., Nancy et al A new cephalosporin with activity
against Methicillin resistant staph. Aureus journal of clinical
medicine 2012;10(3)
 Laskrides C Update on analgesic medication for adult and pediatric
dental patients Dent clin N Am 2016;347-366
 Pain management in infants,children,adolcents- The reference
manual of pediatric dentistry2018 (331-339)
Thank you