SEMINAR ON ANTIBIOTICS PRESENTED BY Dr. AMIT BYATNAL (POST GRADUATE STUDENT) DEPT. OF ORAL MEDICINE AND RADEIOLOGY, SIBAR INSTITUTE OF DENTAL SCIENCES, TAKKELLAPADU, GUNTUR.
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SEMINAR
ON
ANTIBIOTICS
PRESENTED
BY
Dr. AMIT BYATNAL
(POST GRADUATE STUDENT)
DEPT. OF ORAL MEDICINE AND RADEIOLOGY,
SIBAR INSTITUTE OF DENTAL SCIENCES,
TAKKELLAPADU, GUNTUR.
CERTIFICATE
This is to certify that the Seminar entitled, “ANTIBIOTICS” being
submitted by Dr. Amit Byatnal, under the guidance and supervision and completed
to our full satisfaction.
SIGNATURE OF HEAD OF THE DEPARTMENT
CONTENTSCONTENTSIntroduction.Introduction.
History of AntibioticsHistory of Antibiotics
Classification of antimicrobial drugs Classification of antimicrobial drugs
Problems with AMAProblems with AMA
Choice of AMAChoice of AMA
Principles of administrationPrinciples of administration
Indications for antimicrobial agents used in dentistryIndications for antimicrobial agents used in dentistry
Beta lactam antibioticsBeta lactam antibiotics
Quinolones Quinolones
Tetracyclines Tetracyclines
Macrolides Macrolides
Nitroimidazoles Nitroimidazoles
Antifungal drugs Antifungal drugs
Conclusion Conclusion
References References
INTRODUCTIONINTRODUCTION
Antimicrobial agentsAntimicrobial agents: Substances that will suppress the growth/ : Substances that will suppress the growth/
multiplication of bacteria and prevent their action.multiplication of bacteria and prevent their action.
Antibiotic agentsAntibiotic agents: Chemical substances produced by microorganisms that : Chemical substances produced by microorganisms that
have the capacity, in dilute solutions, to produce antimicrobial action.have the capacity, in dilute solutions, to produce antimicrobial action.
HISTORYOF ANTIBIOTICS HISTORYOF ANTIBIOTICS
1877 Louis Pasteur Inhibition of some microbes by others; anthrax 1877 Louis Pasteur Inhibition of some microbes by others; anthrax
((Bacillus anthracis)Bacillus anthracis)
1908 Gelmo Synthesized sulfanilamide (1st sulfonamide 1908 Gelmo Synthesized sulfanilamide (1st sulfonamide
1928 Fleming…1928 Fleming…
Penicillin notatumPenicillin notatum inhibits growth inhibits growth
‘PENICILLINS’‘PENICILLINS’
1941 Chain n Florey 1941 Chain n Florey
Discovered properties of penicillinDiscovered properties of penicillin
1932 Domagk Prontosil 1932 Domagk Prontosil
Therapeutic value sulfonamidesTherapeutic value sulfonamides
1943, Selman Waksman isolated, 1943, Selman Waksman isolated, Streptomyces griseusStreptomyces griseus …Streptomycin …Streptomycin
ClassificationClassification
Chemical structure:Chemical structure:
Sulfonamides and related drugs.Sulfonamides and related drugs.
Sulfadiazine and others.Sulfadiazine and others.
Sulfones – Dapsone (DDS), Paraaminosalicylic acid (PAS).Sulfones – Dapsone (DDS), Paraaminosalicylic acid (PAS).
Diaminopyrimidines Diaminopyrimidines
TrimethoprimTrimethoprim
PyrimethaminePyrimethamine
QuinolonesQuinolones
Nalidixic acidNalidixic acid
NorfloxacinNorfloxacin
Ciprofloxacin etcCiprofloxacin etc
-lactam antibiotics -lactam antibiotics
PenicillinsPenicillins
CephalosporinsCephalosporins
MonobactamsMonobactams
CarbapenemsCarbapenems
TetracyclinesTetracyclines
OxytetracyclineOxytetracycline
Doxycycline etcDoxycycline etc
Nitrobenzene derivative Nitrobenzene derivative
ChloramphenicolChloramphenicol
AminoglycosidesAminoglycosides
StreptomycinStreptomycin
GentamicinGentamicin
Neomycin etcNeomycin etc
Macrolide antibioticsMacrolide antibiotics
ErythromycinErythromycin
RoxithromycinRoxithromycin
Azithromycin etcAzithromycin etc
Polypeptide antibioticsPolypeptide antibiotics
Polymyxin-BPolymyxin-B
ColistinColistin
BacitracinBacitracin
TyrothricinTyrothricin
GlycopeptidesGlycopeptides
VancomycinVancomycin
Teicoplanin Teicoplanin
OxazolidinoneOxazolidinone
LinezolidLinezolid
Nitrofuran derivativesNitrofuran derivatives
NitrofurantoinNitrofurantoin
FurazolidoneFurazolidone
Nitroimidozoles Nitroimidozoles
MetronidozoleMetronidozole
Tinidazole Tinidazole
Nicotinic acid derivativesNicotinic acid derivatives
IsoniazidIsoniazid
PyrazinamidePyrazinamide
Ethionamide Ethionamide
Polyene antibioticsPolyene antibiotics
NystatinNystatin
Amphotericin-BAmphotericin-B
Hamycin Hamycin
Azole derivatives Azole derivatives
MiconazoleMiconazole
ClotrimazoleClotrimazole
KetoconazoleKetoconazole
FluconazoleFluconazole
Others Others
RifampinRifampin
LincomycinLincomycin
ClindamycinClindamycin
SpectinomycinSpectinomycin
Sod. fusidateSod. fusidate
CycloserineCycloserine
ViomycinViomycin
EthambutolEthambutol
ThiacetazoneThiacetazone
ClofazimineClofazimine
Griseofulvin Griseofulvin
Type of organisms against which primarily activeType of organisms against which primarily active
Antibacterial Antibacterial
PenicillinsPenicillins
AminoglycosidesAminoglycosides
Erythromycin etcErythromycin etc
Antifungal Antifungal
GriseofulvinGriseofulvin
Amphotericin BAmphotericin B
Ketoconazole Ketoconazole
AntiviralAntiviral
IdoxuridineIdoxuridine
AcyclovirAcyclovir
AmantadineAmantadine
Zidovudine etcZidovudine etc
AntiprotozoalAntiprotozoal
ChloroquineChloroquine
PyrimethaminePyrimethamine
MetronidazoleMetronidazole
Diloxanide etcDiloxanide etc
AnthelminticAnthelmintic
MebendazoleMebendazole
PyrantelPyrantel
NiclosamideNiclosamide
Diethyl carbamazine etcDiethyl carbamazine etc
BactericidalBactericidal
AminoglycosidesAminoglycosides
BacitracinBacitracin
CephalosporinsCephalosporins
MetronidiazoleMetronidiazole
VancomycinVancomycin
Penicillins Penicillins
CiprofloxacinCiprofloxacin
Streptomycin Streptomycin
CotrimoxazoleCotrimoxazole
BacteriostaticBacteriostatic
ChloramphenicolChloramphenicol
ClindamycinClindamycin
ErythromycinErythromycin
SulfonamidesSulfonamides
TetracyclineTetracycline
TrimethoprimTrimethoprim
Spectrum of activitySpectrum of activity
Narrow spectrumNarrow spectrum
Broad spectrumBroad spectrum
Mechanism of actionMechanism of action
Problems with use of AMAProblems with use of AMA
ToxicityToxicity
Local irritancy:Local irritancy:
-Systemic toxicity: -Systemic toxicity:
-Therapeutic index- high, low, very low-Therapeutic index- high, low, very low
Hypersensitivity reactions :Hypersensitivity reactions :
Drug resistanceDrug resistance
-- Natural- lack of metabolic process or target siteNatural- lack of metabolic process or target site
-- Acquired – due to use over a period of time, mutations or gene Acquired – due to use over a period of time, mutations or gene
transfertransfer
Preventing Resistance to DrugsPreventing Resistance to Drugs
Limit the use of antimicrobial agents to the treatment of specific pathogens Limit the use of antimicrobial agents to the treatment of specific pathogens
sensitive to the drug being used sensitive to the drug being used
Notorious-Make sure doses are high enough, and the duration of drug Notorious-Make sure doses are high enough, and the duration of drug
therapy long enough , combination therapytherapy long enough , combination therapy
Be cautious about the indiscriminate, inadequate or unduly prolonged use of Be cautious about the indiscriminate, inadequate or unduly prolonged use of
anti-infectives anti-infectives
SuperinfectionSuperinfection
Nutritional deficienciesNutritional deficiencies
Masking of an infectionMasking of an infection
Choice of AMA agent- patient factorsChoice of AMA agent- patient factors
1.Age : affect kinetics of drug. 1.Age : affect kinetics of drug.
Conjugation and excretion of chloremphenicol- gray baby syndromeConjugation and excretion of chloremphenicol- gray baby syndrome
Sulfonamides displace bilirubin from PBS- kernicterusSulfonamides displace bilirubin from PBS- kernicterus
Tetracycline accumulates in bone and teeth Tetracycline accumulates in bone and teeth
2. Renal and hepatic failure: cautious use and dose reduction2. Renal and hepatic failure: cautious use and dose reduction
3. Local factors:3. Local factors:
presence of pus and secretions- AMAs, surgical drainage reduces causative presence of pus and secretions- AMAs, surgical drainage reduces causative
bacteria and suppresses anaerobic bacteriabacteria and suppresses anaerobic bacteria
Presence of necrotic material and infectionPresence of necrotic material and infection
Hematomas – foster growthHematomas – foster growth
4.Drug allergy4.Drug allergy
5.Impaired host defense5.Impaired host defense
6.Pregnancy6.Pregnancy
7.Genetic factors7.Genetic factors
Organism related considerationsOrganism related considerations
Drug factorsDrug factors
Spectrum of activitySpectrum of activity
Type of activityType of activity
Sensitivity of the organismSensitivity of the organism
Relative toxicityRelative toxicity
Pharmacokinetic profilePharmacokinetic profile
Route of administationRoute of administation
Evidence of clinical efficacyEvidence of clinical efficacy
CostCost
Microorganisms isolated from pulpal/periapical infectionsMicroorganisms isolated from pulpal/periapical infections
AerobicAerobic
Gram +Gram +veve cocci cocci
StaphylococciStaphylococci
Gram +Gram +veve Baccili Baccili
LactobacciliLactobaccili
CorynebacteriumCorynebacterium
Eikenella corrodensEikenella corrodens
AnaerobicAnaerobic
Gram +Gram +veve cocci cocci
PeptostreptococcusPeptostreptococcus
Gram –Gram –veve cocci cocci
VeillonellaVeillonella
Gram +Gram +veve baccilli baccilli
ActinomycesActinomyces
EubacteriumEubacterium
ClostridiaClostridia
PropionibacteriumPropionibacterium
Gram -Gram -veve baccilli baccilli
BacteriodesBacteriodes
FusobacteriaFusobacteria
PorphyromonasPorphyromonas
PrevotellaPrevotella
TreponemasTreponemas
Treponema denticolaTreponema denticola
Treponema macrodentiumTreponema macrodentium
Treponema oralisTreponema oralis
Treponema vincentiTreponema vincenti
PRINCIPLES OF ANTIBIOTIC THERAPYPRINCIPLES OF ANTIBIOTIC THERAPY
PRINCIPLE 1: TO DETERMINE THE SEVERITY OF INFECTIONPRINCIPLE 1: TO DETERMINE THE SEVERITY OF INFECTION
PRINCIPLE 2: TO EVALUATE STATE OF PATIENT’S HOST PRINCIPLE 2: TO EVALUATE STATE OF PATIENT’S HOST
DEFENSE MECHANISMSDEFENSE MECHANISMS
PRINCIPLE 3: TO TREAT INFECTION SURGICALLYPRINCIPLE 3: TO TREAT INFECTION SURGICALLY
PRINCIPLE 4: TO SUPPORT THE PATIENT MEDICALLYPRINCIPLE 4: TO SUPPORT THE PATIENT MEDICALLY
PRINCIPLE 5: CHOOSE AND PRESCRIBE APPROPRIATE PRINCIPLE 5: CHOOSE AND PRESCRIBE APPROPRIATE
ANTIBIOTICANTIBIOTIC
PRINCIPLE 6: PROPER ANTIBIOTIC ADMINISTRATIONPRINCIPLE 6: PROPER ANTIBIOTIC ADMINISTRATION
PRINCIPLES OF ANTIBIOTIC ADMINISTRATION PRINCIPLES OF ANTIBIOTIC ADMINISTRATION
Proper dose : Proper dose :
DRUG DOSAGE DRUG DOSAGE
-- ‘Dose’ is the appropriate amount of a drug needed to produce a ‘Dose’ is the appropriate amount of a drug needed to produce a
certain degree of response in a patient.certain degree of response in a patient.
Body size :Body size :
-- Individual dose =Individual dose = BW(kg)/70 x average adult dose BW(kg)/70 x average adult dose
-- Individual dose =Individual dose = BSA(m2BSA(m2 ) /1.7x average adult dose ) /1.7x average adult dose
NEONATES AND INFANTSNEONATES AND INFANTS
Greater percentage of body weight compared with body waterGreater percentage of body weight compared with body water
Greater volume of distributionGreater volume of distribution
Increased serum half livesIncreased serum half lives
Reduced gastric emptyingReduced gastric emptying
Reduced plasma protein bindingReduced plasma protein binding
Reduced GFRReduced GFR
2) Proper time interval :2) Proper time interval :
3) Proper route of administration :3) Proper route of administration :
Parenteral administration will produce the necessary serum level of Parenteral administration will produce the necessary serum level of
antibiotics. antibiotics.
Oral route results in the most variable absorption. Oral route results in the most variable absorption.
For maximum absorption is taken in fasting stage. For maximum absorption is taken in fasting stage.
4) Consistency in regard to route of administration :4) Consistency in regard to route of administration :
When treating a serious, established infections, parenteral antibiotic therapy When treating a serious, established infections, parenteral antibiotic therapy
is frequently the method of choice. is frequently the method of choice.
Combination antibiotic therapy :Combination antibiotic therapy :
The rationale for the use of 2 or more drugs together is to minimize The rationale for the use of 2 or more drugs together is to minimize
the emergence of antibiotic resistant microorganismsthe emergence of antibiotic resistant microorganisms
to increase the certainty of a successful clinical outcome to increase the certainty of a successful clinical outcome
to treat mixed bacterial infections to treat mixed bacterial infections
to prevent superinfectionto prevent superinfection
to treat severe infections of unknown etiology to treat severe infections of unknown etiology
to decrease toxicity without decreasing efficacy to decrease toxicity without decreasing efficacy
-- Examples :Examples :
Isoniazid + ethambutol + streptomycin in treatment of tuberculosis. Isoniazid + ethambutol + streptomycin in treatment of tuberculosis.
Rules :Rules :
2 bactericidal drugs produce, supraadditive effects, not antagonism. (1+1>2)2 bactericidal drugs produce, supraadditive effects, not antagonism. (1+1>2)
The combination of a bacteriostatic and a bactericidal drug generally results The combination of a bacteriostatic and a bactericidal drug generally results
in diminished effects. (1+1<2)in diminished effects. (1+1<2)
2 bacteriostatic drugs are never inhibitory. (1+1=2)2 bacteriostatic drugs are never inhibitory. (1+1=2)
Results :Results :
Indifference when the effect is equal to the single most active drug or equal Indifference when the effect is equal to the single most active drug or equal
to the arithmetic sum of the two, use is not justified. to the arithmetic sum of the two, use is not justified.
Antagonism : when the combined drug effect is less than the algebraic sum Antagonism : when the combined drug effect is less than the algebraic sum
of the effects on the individual drugs in the mixture. of the effects on the individual drugs in the mixture.
Synergism : ability of two antibiotics acting together to markedly increases Synergism : ability of two antibiotics acting together to markedly increases
the rate of bactericidal action compared to either drug alone. the rate of bactericidal action compared to either drug alone.
Disadvantages :Disadvantages :
Adds nothing to therapeutic efficacy and may even reduce it (antagonism). Adds nothing to therapeutic efficacy and may even reduce it (antagonism).
Increase antibiotic toxicity and allergy. Increase antibiotic toxicity and allergy.
Increase the likelihood of superinfection Increase the likelihood of superinfection
Discourages specific etiologic diagnosis and promote false security.Discourages specific etiologic diagnosis and promote false security.
Encourage inadequate doses, particularly with fixed dose combination Encourage inadequate doses, particularly with fixed dose combination
therapy. therapy.
Increased cost Increased cost
Emergence of resistant bacterial strains Emergence of resistant bacterial strains
Increase the environmental spread of antibiotic resistant bacteria. Increase the environmental spread of antibiotic resistant bacteria.
FACTORS INFLUENCING ANTIBIOTIC THERAPYFACTORS INFLUENCING ANTIBIOTIC THERAPY
Minimal Inhibitory ConcentrationMinimal Inhibitory Concentration
Concentration-dependent Vs Time-dependent antibioticsConcentration-dependent Vs Time-dependent antibiotics
Post-antibiotic effectsPost-antibiotic effects
MINIMAL INHIBITORY CONCENTRATIONMINIMAL INHIBITORY CONCENTRATION
Is the lowest antibiotic concentration that prevents growth of microorganismIs the lowest antibiotic concentration that prevents growth of microorganism
after an incubation period of 18 – 24 hours with a standard inoculum of 104 after an incubation period of 18 – 24 hours with a standard inoculum of 104
to 105 cu/mlto 105 cu/ml
MINIMAL BACTERICIDAL CONCENTRATIONMINIMAL BACTERICIDAL CONCENTRATION
Is the lowest concentration of drug that causes the complete destruction of Is the lowest concentration of drug that causes the complete destruction of
the organisms or permits survival of less than 0.1% of the inoculumthe organisms or permits survival of less than 0.1% of the inoculum
RULE OF THUMBRULE OF THUMB
The concentration of the antibiotic in the blood should exceed the MIC by a The concentration of the antibiotic in the blood should exceed the MIC by a
factor of 2-8 times to offset the tissue barriers that restrict access to the factor of 2-8 times to offset the tissue barriers that restrict access to the
infected siteinfected site
CONCENTRATION DEPENDENT CONCENTRATION DEPENDENT
VsVs
TIME DEPENDENT ANTIBIOTICSTIME DEPENDENT ANTIBIOTICS
Aminoglycosides, metronidazole, fluoroquinolonesAminoglycosides, metronidazole, fluoroquinolones
Concentration dependentConcentration dependent
Bactericidal activity depends on the Bactericidal activity depends on the
drug concentrationdrug concentration
Beta-lactams and vancomycinBeta-lactams and vancomycin
Long time of exposure of theLong time of exposure of the
organismsorganisms
Better the bactericidal activityBetter the bactericidal activity
POSTANTIBIOTIC EFFECTSPOSTANTIBIOTIC EFFECTS
Is the persistent supression of microbial growth after short time exposure to Is the persistent supression of microbial growth after short time exposure to
an antimicrobial agent.an antimicrobial agent.
MECHANISM :MECHANISM :
Is the time necessary to recover from sublethal structural and Is the time necessary to recover from sublethal structural and
metabolic alterations that prevents resumption of bacterial metabolic alterations that prevents resumption of bacterial
regrowth.regrowth.
Indications for antimicrobial agents in dentistryIndications for antimicrobial agents in dentistry
Therapeutic indicationsTherapeutic indications
Prophylactic indicationsProphylactic indications
Dental procedure for which antibiotic prophylaxis is recommended to Dental procedure for which antibiotic prophylaxis is recommended to
prevent infective endocardititis prevent infective endocardititis
(AHA recommendation)(AHA recommendation)
Dental extractionsDental extractions
Periodontal proceduresPeriodontal procedures
Replantation procedureReplantation procedure
Implant placementImplant placement
Initial placement of orthodontic bandsInitial placement of orthodontic bands
Intra ligamentary local anesthetic injectionIntra ligamentary local anesthetic injection
Incision and drainageIncision and drainage
Not recommended :Not recommended :
1.Restorative dentistry1.Restorative dentistry
2.LA injections2.LA injections
3.Intracanal endodontic treatment3.Intracanal endodontic treatment
4.Post-op suture removal4.Post-op suture removal
5.Oral radiographs5.Oral radiographs
CLASSIFICATION OF PENICILLINCLASSIFICATION OF PENICILLIN
Natural penicillins : Natural penicillins :
Penicillin G (Benzyl penicillin) Penicillin G (Benzyl penicillin)
Acid resistant penicillins : Acid resistant penicillins :
Phenoxymethyl penicillin (penicillin V)Phenoxymethyl penicillin (penicillin V)
Penicillinase – resistant penicillins : Penicillinase – resistant penicillins :
Acid labile : Methicillin, naficillin, cloxacillin, dicloxacillinAcid labile : Methicillin, naficillin, cloxacillin, dicloxacillin
Extended spectrum penicillins : Extended spectrum penicillins :
Carboxypenicillins : Carbenicillin, ticarcillinCarboxypenicillins : Carbenicillin, ticarcillin
Aminopenicillins : Ampicillin, amoxicillinAminopenicillins : Ampicillin, amoxicillin
Ureidopenicillins Ureidopenicillins
BENZYL PENICILLIN (PENCILLIN G)BENZYL PENICILLIN (PENCILLIN G)
Antibacterial activity Antibacterial activity
Inhibits the growth of susceptible organism.Inhibits the growth of susceptible organism.
Mainly gram +ve, gram –ve cocci and some gram +ve bacilli with exception Mainly gram +ve, gram –ve cocci and some gram +ve bacilli with exception
of enterococci.of enterococci.
Cocci – Highly sensitive – Streptococci, Pneumococci, Staph. aureus, N. Cocci – Highly sensitive – Streptococci, Pneumococci, Staph. aureus, N.
gonorrhoeae, N. meningitis gonorrhoeae, N. meningitis
Bacilli – B. anthracis, Corynebacterium diphtheriae, clostridium tetany and Bacilli – B. anthracis, Corynebacterium diphtheriae, clostridium tetany and
spirochetes spirochetes
Actinomyces israelii is moderately sensitiveActinomyces israelii is moderately sensitive
Preparation and dose :Preparation and dose :
PnG inj 0.5-5 MU i.m or i.v 6-12 hoursPnG inj 0.5-5 MU i.m or i.v 6-12 hours
Procaine pencillin inj 0.5, 1 MU dry powder in vialProcaine pencillin inj 0.5, 1 MU dry powder in vial
ADVERSE REACTIONS :ADVERSE REACTIONS :
Miscellaneous reactions :Miscellaneous reactions :
Nausea and vomiting on oral PnGNausea and vomiting on oral PnG
Sterile inflammatory reaction at the site of IM inj.Sterile inflammatory reaction at the site of IM inj.
Prolonged IV administration may cause thrombophlebitisProlonged IV administration may cause thrombophlebitis
Accidental IV administration of procaine PP cause anxiety, mental Accidental IV administration of procaine PP cause anxiety, mental
disturbances paraesthesia and convulsionsdisturbances paraesthesia and convulsions
Intolerance :Intolerance :
Major problem with PnG includes idiosyncratic, anaphylactic and allergic Major problem with PnG includes idiosyncratic, anaphylactic and allergic
reactionsreactions
Other allergic reactions are Other allergic reactions are
Skin rashes Skin rashes
Serum sicknessSerum sickness
Renal disturbance Renal disturbance
Hemolytic disturbanceHemolytic disturbance
AnaphylaxisAnaphylaxis
Jarisch herxheimer reactionJarisch herxheimer reaction
Super infectionSuper infection
HyperkalemiaHyperkalemia
Uses :Uses :
PnG is the drug of choice for infectionsPnG is the drug of choice for infections
Streptococcal infectionsStreptococcal infections
Pneumococcal infectionsPneumococcal infections
Meningococcal infectionsMeningococcal infections
Gonorrhoea Gonorrhoea
Syphilis Syphilis
Diphtheria Diphtheria
Tetanus and gas gangreneTetanus and gas gangrene
Prophylactic uses Prophylactic uses
The major drawbacks of benzyl penicillin are The major drawbacks of benzyl penicillin are
Inactivation by the gastric hydrochloric acidInactivation by the gastric hydrochloric acid
Short duration of actionShort duration of action
Poor penetration into CSFPoor penetration into CSF
Activity mainly against gram +ve organismActivity mainly against gram +ve organism
Possibility of anaphylaxisPossibility of anaphylaxis
Acid resistant pencillins :Acid resistant pencillins :
1. Potassium phenoxymethyl penicillin (penicillin V)1. Potassium phenoxymethyl penicillin (penicillin V)
Dose : infants 60 mg, children 125-250 mg given 6 hourlyDose : infants 60 mg, children 125-250 mg given 6 hourly
CRYSTAPEN-V, KAYPEN, PENIVORAL 65, 130, 125, 250 mg tablets CRYSTAPEN-V, KAYPEN, PENIVORAL 65, 130, 125, 250 mg tablets
125 mg/5 ml dry ser125 mg/5 ml dry ser
II) Pencillinase resistant pencillins :II) Pencillinase resistant pencillins :
Methicillin Methicillin
Effective in staphylococciEffective in staphylococci
It is given IM or IV (slow) in the dose of 1 gm every 4-6 hours.It is given IM or IV (slow) in the dose of 1 gm every 4-6 hours.
Haematuria, albuminuria and reversible interstitial nephritis are the special Haematuria, albuminuria and reversible interstitial nephritis are the special
adverse effect of methicillin. adverse effect of methicillin.
Cloxacillin Cloxacillin
Weaker antibacterial activity.Weaker antibacterial activity.
Distrubuted throught out the body, but highest concentration in kidney and Distrubuted throught out the body, but highest concentration in kidney and
liver. 30% excreted in urine.liver. 30% excreted in urine.
Oral dose for adults 2-4 gm divided into 4 portions children Oral dose for adults 2-4 gm divided into 4 portions children
50-100mg/kg/day.50-100mg/kg/day.
IM adults 2-12 gm/day, children 100-300 mg/kg/day every 4-6 hours. IM adults 2-12 gm/day, children 100-300 mg/kg/day every 4-6 hours.
BIOCLOX, KLOX, CLOCILIN 0.25, 0.5 gm cap, 0.5 gm/vial.BIOCLOX, KLOX, CLOCILIN 0.25, 0.5 gm cap, 0.5 gm/vial.
III) Extended spectrum pencillins :III) Extended spectrum pencillins :
Amino pencillins Amino pencillins
-- Ampicillin – Ampicillin –
Antibacterial activity is similar to that of PnG that is more effective than Antibacterial activity is similar to that of PnG that is more effective than
PnG against a variety of gram-ve bacteria PnG against a variety of gram-ve bacteria
Drug is effective against H.influenzae strep.viridans, N.gonorrhea, Drug is effective against H.influenzae strep.viridans, N.gonorrhea,
Salmonella, shigellae, Klebsilla and enterococci.Salmonella, shigellae, Klebsilla and enterococci.
-- Absorption, fate and excretion :Absorption, fate and excretion :
Oral absorption is incomplete but adequateOral absorption is incomplete but adequate
Food interferes with absorption Food interferes with absorption
Partly excreted in bile and partly by kidney Partly excreted in bile and partly by kidney
Dose : 0.5-2 gm oral/IM or IV depending on severity of infection every 6 Dose : 0.5-2 gm oral/IM or IV depending on severity of infection every 6
hours hours
-- Children : 25-50 mg/kg/dayChildren : 25-50 mg/kg/day
-- AMPILIN, ROSCILLIAN, BIOCILIN – 250, 500 mg cap 100mg/ml AMPILIN, ROSCILLIAN, BIOCILIN – 250, 500 mg cap 100mg/ml
ped drops, 250 mg/ml dry syr, 1 gm/vial inj. ped drops, 250 mg/ml dry syr, 1 gm/vial inj.
USES :USES :
Urinary tract infectionsUrinary tract infections
Respiratory tract infectionsRespiratory tract infections
Meningitis Meningitis
GonorrhoeaGonorrhoea
Bacillary dysentryBacillary dysentry
SepticaemiasSepticaemias
SABESABE
Adverse effects :Adverse effects :
Diarrhoea is frequent Diarrhoea is frequent
Skin rashes is more commonSkin rashes is more common
Unabsorbed drug irritates lower intestinesUnabsorbed drug irritates lower intestines
Patient with history of hypersensitivity to PnG should not be given Patient with history of hypersensitivity to PnG should not be given
ampicillin.ampicillin.
AMOXICILLIN :AMOXICILLIN :
This is a semisynthetic penicillin.This is a semisynthetic penicillin.
(amino-p-hydroxy-benzylpenicillin)(amino-p-hydroxy-benzylpenicillin)
Antibacterial spectrum is similar to ampicillin. Antibacterial spectrum is similar to ampicillin.
Oral absorption is better; food does not interfere; higher and more sustained Oral absorption is better; food does not interfere; higher and more sustained
blood levels are produced.blood levels are produced.
It is less protein bond and urinary excretion is higher than that of ampicillin.It is less protein bond and urinary excretion is higher than that of ampicillin.
Incidence of diarrhoea is lessIncidence of diarrhoea is less
Dose : 0.25-1 g TDS oral; Dose : 0.25-1 g TDS oral;
AMOXYLIN, NOVAMOX, SYNAMOX, MOX, AMOXIL 250, 500 mg AMOXYLIN, NOVAMOX, SYNAMOX, MOX, AMOXIL 250, 500 mg
cap, 125 mg/5ml dry syr, 500 mg/vial inj.cap, 125 mg/5ml dry syr, 500 mg/vial inj.
USES :USES :
Oro-dental infectionsOro-dental infections
Upper RTIUpper RTI
Bronchitis Bronchitis
Urinary infectionUrinary infection
SBESBE
GonorrhoeaGonorrhoea
BETA LACTAMASE INHIBITORSBETA LACTAMASE INHIBITORS
CLAVULANIC ACID CLAVULANIC ACID
Obtained from STREPTOMYCES CLAVULIGERUSObtained from STREPTOMYCES CLAVULIGERUS
Betalactam ring – no antibacterial activityBetalactam ring – no antibacterial activity
Suicide inhibitor –inactivated after binding to enzymeSuicide inhibitor –inactivated after binding to enzyme
Permeates the outer layers of cell wall of gram-ve bacteriaPermeates the outer layers of cell wall of gram-ve bacteria
Adverse effects :Adverse effects :
Pain-thrombophebitisPain-thrombophebitis
Rashes and diarrhoeaRashes and diarrhoea
Uses :Uses :
Mixed aerobic-anaerobic infectionsMixed aerobic-anaerobic infections
Dental infections caused by beta lactamase producing bacteriaDental infections caused by beta lactamase producing bacteria
GonorrhoeaGonorrhoea
Skin/soft tissue infectionsSkin/soft tissue infections
SULBACTAMSULBACTAM
CEPHALOSPORINSCEPHALOSPORINS
Cephalosporium acremonium was the first source.Cephalosporium acremonium was the first source.
They contain 7 amino cephalosporonic acid nucleus. They contain 7 amino cephalosporonic acid nucleus.
Structurally they contain betalactam and dihydro thiazine rings. Structurally they contain betalactam and dihydro thiazine rings.
Mechanism of action : Mechanism of action :
Act by inhibiting bacterial cell was synthesis and are bactericidal. Act by inhibiting bacterial cell was synthesis and are bactericidal.
Classification Classification
Classified according to its antibacterial activity. Classified according to its antibacterial activity.
First generation cephalosporin First generation cephalosporin
Good activity against gram +ve bacteria. (except enterococci). Good activity against gram +ve bacteria. (except enterococci).
Most oral cavity anaerobes are sensitive.Most oral cavity anaerobes are sensitive.
Parental Parental Oral Oral
CEPHALOTHIN CEPHALOTHIN CEPHALEXINCEPHALEXIN
CEFAZOLINCEFAZOLIN CEPHRADINE CEPHRADINE
CEFADROXIL CEFADROXIL
Cephalaxin and Cephadroxil : Cephalaxin and Cephadroxil :
Useful in treating community acquired, respiratory and urinary tract Useful in treating community acquired, respiratory and urinary tract
infections and in surgical prophylaxis. infections and in surgical prophylaxis.
Infections of head and neck region. Infections of head and neck region.
Dose: Oral 0.25 - 1g 6-8 hrly Dose: Oral 0.25 - 1g 6-8 hrly
Children : 25-100mg/kg/dayChildren : 25-100mg/kg/day
IM – 0.25g 8 hrly (mild cases) 1g 6 hrly (severe cases). IM – 0.25g 8 hrly (mild cases) 1g 6 hrly (severe cases).
Drops – cephaxin 125mg/5ml syrup. Drops – cephaxin 125mg/5ml syrup.
100mg /ml ped. drops.100mg /ml ped. drops.
SPORIDEX, CEPHAXIN, CEPHACILLIN, CEFADROX, DROXYLSPORIDEX, CEPHAXIN, CEPHACILLIN, CEFADROX, DROXYL
Second generation cephalosporins : Second generation cephalosporins :
Increased activity against gram –ve organism. Increased activity against gram –ve organism.
More active against anaerobes. More active against anaerobes.
-- Parenteral Parenteral Oral Oral
CEFUROXIME CEFUROXIME CEFACLOR CEFACLOR
CEFOXITIN CEFOXITIN CEFUROXIME AXETIL CEFUROXIME AXETIL
More active against H. influenzae, E coli.More active against H. influenzae, E coli.
Dose : 250mg, 125mg, 125mg/5ml syr. and Dose : 250mg, 125mg, 125mg/5ml syr. and
50 mg /ml ped. drops. 50 mg /ml ped. drops.
KEFLOR, CEFTUM, CEFOGEN, FUROXIL. KEFLOR, CEFTUM, CEFOGEN, FUROXIL.
Third Generation CephalosporinsThird Generation Cephalosporins
High activity against gram –ve entrobacteriaceae, some inhibit High activity against gram –ve entrobacteriaceae, some inhibit
Pseudomonas as well.Pseudomonas as well.
Parenteral OralParenteral Oral
Cefataxime CefiximeCefataxime Cefixime
Ceftizoxime Cefpodoxime proxetilCeftizoxime Cefpodoxime proxetil
Ceftriaxone CefdinirCeftriaxone Cefdinir
Ceftazidime CeftibutenCeftazidime Ceftibuten
CefoperazoneCefoperazone
Dose: 250mg, 500mg, 1000mg per vial injDose: 250mg, 500mg, 1000mg per vial inj
CLAFORAN, CEFIZOX,MONOCEF,CEFAZID.CLAFORAN, CEFIZOX,MONOCEF,CEFAZID.
Fourth Generation CephalosporinsFourth Generation Cephalosporins
Similar to 3Similar to 3rdrd generation ,but is highly resistant to beta- lactamases. generation ,but is highly resistant to beta- lactamases.
Due to high potency and extended spectrum, it is effective in many serious Due to high potency and extended spectrum, it is effective in many serious
infections like hospital acquired pneumonia, bacteremia, septicaemia.infections like hospital acquired pneumonia, bacteremia, septicaemia.
ParentralParentral
CefepimeCefepime
CefpiromeCefpirome
Dose: 1-2 g i.m/i.v 12hrlyDose: 1-2 g i.m/i.v 12hrly
CEFROM, CEFROTH, KEFAGECEFROM, CEFROTH, KEFAGE
Adverse reactions : Adverse reactions :
Local reactions – cause pain (IM) and cause thrombophlebitis (IV) Local reactions – cause pain (IM) and cause thrombophlebitis (IV)
Allergy – skin rashes Allergy – skin rashes
Nephrotoxicity Nephrotoxicity
Bleeding disordersBleeding disorders
Intolerance to alcohol Intolerance to alcohol
Uses : Uses :
Alternatives to penicillins. Alternatives to penicillins.
RTI, UTI and soft tissue infection RTI, UTI and soft tissue infection
Penicillinase producing staph infection. Penicillinase producing staph infection.
Septicaemias. Septicaemias.
Surgical prophylaxis Surgical prophylaxis
Meningitis, gonorrhoea Meningitis, gonorrhoea
Typhoid Typhoid
Mixed aerobic and anaerobic infections Mixed aerobic and anaerobic infections
Infection by odd organism or hospital infections Infection by odd organism or hospital infections
Prophylactic treatment in neutropenic patients. Prophylactic treatment in neutropenic patients.
Dental infectionsDental infections
Alternative to pencillins- hypersensitivity and resistanceAlternative to pencillins- hypersensitivity and resistance
Oral – 1Oral – 1stst and 2 and 2ndnd generation generation
SulfonamidesSulfonamides
Short acting(4-8hr)- SulfadiazineShort acting(4-8hr)- Sulfadiazine
Intermediate acting (8-12hr)- Sulfamethoxazole, Intermediate acting (8-12hr)- Sulfamethoxazole,
SulfamoxoleSulfamoxole
Long acting(7 days)- Sulfadoxine, SulfamethopyrazineLong acting(7 days)- Sulfadoxine, Sulfamethopyrazine
Special purpose Sulfonamides – Sulfacetamide sod,Special purpose Sulfonamides – Sulfacetamide sod,
Sulfasalazine,Sulfasalazine,
Mafenide,Mafenide,
Silver sulfadiazineSilver sulfadiazine
Mechanism of actionMechanism of action
In In bacteriabacteria, antibacterial sulfonamides act as , antibacterial sulfonamides act as competitive inhibitorscompetitive inhibitors of the of the
enzyme enzyme dihydropteroate synthetasedihydropteroate synthetase, DHPS. DHPS catalyses the conversion , DHPS. DHPS catalyses the conversion
of PABA (of PABA (parapara -aminobenzoate-aminobenzoate ) to ) to dihydropteroatedihydropteroate, a key step in , a key step in folatefolate
synthesis. Folate is necessary for the cell to synthesize synthesis. Folate is necessary for the cell to synthesize nucleic acidsnucleic acids (nucleic (nucleic
acids are essential building blocks of acids are essential building blocks of DNADNA and and RNARNA), and in its absence ), and in its absence
cells will be unable to divide. Hence the sulfonamide antibacterials exhibit a cells will be unable to divide. Hence the sulfonamide antibacterials exhibit a
bacteriostaticbacteriostatic rather than rather than bactericidalbactericidal effect. effect.
Side effectsSide effects
Sulfonamides have the potential to cause a variety of untoward reactions, Sulfonamides have the potential to cause a variety of untoward reactions,
including urinary tract disorders, haemopoietic disorders, including urinary tract disorders, haemopoietic disorders, porphyriaporphyria and and
hypersensitivity reactions. When used in large dose, it may develop a strong hypersensitivity reactions. When used in large dose, it may develop a strong
allergic reaction. One of the most serious is allergic reaction. One of the most serious is Stevens Johnson syndromeStevens Johnson syndrome(or (or
toxic epidermal necrolysis).toxic epidermal necrolysis).
QUINOLONESQUINOLONES
Entirely synthetic antimicrobials are active primarily against gram –ve Entirely synthetic antimicrobials are active primarily against gram –ve
bacteria.bacteria.
Nalidixic acid- low potency, modest blood and tissue levels, limited Nalidixic acid- low potency, modest blood and tissue levels, limited
spectrum, high resistancespectrum, high resistance
Fluoroquinolones – high potency, expanded spectrum, better tissue Fluoroquinolones – high potency, expanded spectrum, better tissue
penetrance, slow resistance.penetrance, slow resistance.
CIPROFLOXACINCIPROFLOXACIN
First generation FQ active against a broad range of bacteria especially First generation FQ active against a broad range of bacteria especially
gram –ve aerobic bacilli.gram –ve aerobic bacilli.
Microbiological features :Microbiological features :
Rapid bactericidal activity and high potency.Rapid bactericidal activity and high potency.
Relatively long post antibiotic effect Relatively long post antibiotic effect
Low frequency of mutational resistance.Low frequency of mutational resistance.
Protective intestinal streptococci and anaerobes are spared.Protective intestinal streptococci and anaerobes are spared.
Less active at acidic pH.Less active at acidic pH.
Adverse effect :Adverse effect :
GIT – Nausea, vomiting, bad taste, anorexia, diarrhoea is infrequent.GIT – Nausea, vomiting, bad taste, anorexia, diarrhoea is infrequent.
CNS- Dizziness, headache, restlessness, anxiety, insomnia and seizures are CNS- Dizziness, headache, restlessness, anxiety, insomnia and seizures are
rare.rare.
Skin/hypersensitivity – rashes, pruritis, urticaria.Skin/hypersensitivity – rashes, pruritis, urticaria.
Tendonitis and tendon ruptureTendonitis and tendon rupture
Uses :Uses :
Broad range of infectionsBroad range of infections
Minor cases, orodental -not indicatedMinor cases, orodental -not indicated
UTIUTI
Bacterial gastroenteritisBacterial gastroenteritis
Prophylaxis -TyphoidProphylaxis -Typhoid
Bone, soft tissue, wound infection.Bone, soft tissue, wound infection.
Combinations- gram –ve septicaemiasCombinations- gram –ve septicaemias
TuberculosisTuberculosis
CIFRAN, CIPLOX, CIPROBID, CIPROLET CIFRAN, CIPLOX, CIPROBID, CIPROLET
250, 500,750 mg tab, 200mg/100 ml IV infusion 3mg/ml eye drops.250, 500,750 mg tab, 200mg/100 ml IV infusion 3mg/ml eye drops.
NorfloxacinNorfloxacin
-- Less potent than Ciprofloxacin.Less potent than Ciprofloxacin.
-- Used for Pseudomonas, Urinary and genital tract infections.Used for Pseudomonas, Urinary and genital tract infections.
NORFLOX -200,400mgNORFLOX -200,400mg
OfloxacinOfloxacin
-- Activity against gram –ve bacteria Activity against gram –ve bacteria
-- Chlamydia and MycoplasmaChlamydia and Mycoplasma
-- Alternative drug for TuberculosisAlternative drug for Tuberculosis
-- Used mainly for GonorrheaUsed mainly for Gonorrhea
ZANOCIN -200,400mgZANOCIN -200,400mg
LevofloxacinLevofloxacin
-- Sinusitis, Pylonephritis, soft tissue infections.Sinusitis, Pylonephritis, soft tissue infections.
LOMEF- 400mgLOMEF- 400mg
GatifloxacinGatifloxacin
-- Excellent activity against Streptococci pneumoniae Excellent activity against Streptococci pneumoniae
-- Indicated in community acquired pneumonia, exacerbation of chronicIndicated in community acquired pneumonia, exacerbation of chronic
bronchitis, and other respiratory tract infections. bronchitis, and other respiratory tract infections.
-- Used in urinary tract infectons and gonorrhhoea.Used in urinary tract infectons and gonorrhhoea.
GATIQIN – 200,400 mg tabGATIQIN – 200,400 mg tab
SparfloxacinSparfloxacin
-Enhanced activity against gram –ve bacteria, Bacteroides -Enhanced activity against gram –ve bacteria, Bacteroides
fragilis, anaerobes and mycobacteria.fragilis, anaerobes and mycobacteria.
-- Indicated in Pneumonias, chronic bronchitis, sinusitis and other ENT Indicated in Pneumonias, chronic bronchitis, sinusitis and other ENT
infections.infections.
-- Good efficacy in Mycobacterium avium infection in AIDS patients Good efficacy in Mycobacterium avium infection in AIDS patients
and Leprosy.and Leprosy.
-- Higher incidence of phototoxic reactions.Higher incidence of phototoxic reactions.
SPARTA, SPARDAC -100,200 mg tabSPARTA, SPARDAC -100,200 mg tab
NITROIMIDAZOLESNITROIMIDAZOLES
METRONIDAZOLE :METRONIDAZOLE :
Introduced in 1959Introduced in 1959
Broad spectrum- e.histolytica, giardia lambliaBroad spectrum- e.histolytica, giardia lamblia
Anaerobic infections- chance discoveryAnaerobic infections- chance discovery
Tinidazole, secnidazole, ornidazole, satranidazole Tinidazole, secnidazole, ornidazole, satranidazole
Cidal activity against protozoa and anaerobic bacteria such as B fragilis, Cidal activity against protozoa and anaerobic bacteria such as B fragilis,
Fusobacterium, h.pyroli, spirochetesFusobacterium, h.pyroli, spirochetes
Metronidazole is selectively toxic to anaerobic microorganisms. Metronidazole is selectively toxic to anaerobic microorganisms.
Pharmacokinetics :Pharmacokinetics :
Completely absorbed from the small intestine. Completely absorbed from the small intestine.
Widely distributed in the body Widely distributed in the body
It is metabolized in liver It is metabolized in liver
Excreted in urine. 8hrExcreted in urine. 8hr
Adverse effects :Adverse effects :
Anorexia, nausea, metallic taste and abdominal cramps Anorexia, nausea, metallic taste and abdominal cramps
Looseness of stool is occasional,Looseness of stool is occasional,
Headache, glossitis, dryness of mouth, dizziness, rashes and transient Headache, glossitis, dryness of mouth, dizziness, rashes and transient
neutropenia.neutropenia.
Prolonged administration may cause peripheral neuropathy and CNS effectsProlonged administration may cause peripheral neuropathy and CNS effects
Thrombophlebitis Thrombophlebitis
Contraindications :Contraindications :
In neurological disease, blood dyscrasias, chronic alcoholismIn neurological disease, blood dyscrasias, chronic alcoholism
First trimister of pregnancyFirst trimister of pregnancy
OrnidazoleOrnidazole
Activity similar to Metronidazole but it is slowly metabolised .Activity similar to Metronidazole but it is slowly metabolised .
Used in anaerobic infections, Amoebiasis, Giardiasis, Trichomonasis, and Used in anaerobic infections, Amoebiasis, Giardiasis, Trichomonasis, and
bacterial vaginosis.bacterial vaginosis.
DAZOLIC -500mg tab, 500mg/100ml vial for i.v. infusion.DAZOLIC -500mg tab, 500mg/100ml vial for i.v. infusion.
Uses- Orodental infectionsUses- Orodental infections
MZ 200-400mg TDS(15-30mg/kg/day) – anaerobes not inhibited by MZ 200-400mg TDS(15-30mg/kg/day) – anaerobes not inhibited by
pencillinpencillin
ANUG- MZ+Amox - 5daysANUG- MZ+Amox - 5days
Periodontitis, pericoronitis, acute apical infections, endodontic infections- 5-Periodontitis, pericoronitis, acute apical infections, endodontic infections- 5-
7 days7 days
Aerobic and facultative bacteria- MZ+pencillin/cephalosporin/macrolidesAerobic and facultative bacteria- MZ+pencillin/cephalosporin/macrolides
FLAGYL, METROGYL, METRON, ALDEZOLE 200, 400 mg tab, 200 FLAGYL, METROGYL, METRON, ALDEZOLE 200, 400 mg tab, 200
mg/5ml susp.mg/5ml susp.
TINIDAZOLE TINIDAZOLE
It is an equally efficacious congener of metronidazole It is an equally efficacious congener of metronidazole
Metabolism is slower and duration of action is longerMetabolism is slower and duration of action is longer
Incidence of side effects is lower-Metallic taste, nausea, rashes Incidence of side effects is lower-Metallic taste, nausea, rashes
TINIBA, TRIDAZOLE, 300, 500, 1000 mg tab, 800 mg/400 ml ivTINIBA, TRIDAZOLE, 300, 500, 1000 mg tab, 800 mg/400 ml iv
Dental infections: 0.5g(10mg/kg) BD for 5 daysDental infections: 0.5g(10mg/kg) BD for 5 days
2g orally followed 0.5g BD for 5days2g orally followed 0.5g BD for 5days
800mg iv until oral therapy800mg iv until oral therapy
TETRACYCLINESTETRACYCLINES
Napthacene derivatives made up by fusion of 4 partially unsaturated Napthacene derivatives made up by fusion of 4 partially unsaturated
cyclohexane radicals cyclohexane radicals
Tetracyclines are bacteriostatic.Tetracyclines are bacteriostatic.
ClassificationClassification
Antimicrobial activity :Antimicrobial activity :
Gram+ve and –ve cocci are sensitive-R Gram+ve and –ve cocci are sensitive-R
Gram+ve bacilli are inhibitedGram+ve bacilli are inhibited
Entero bacteriaceae are highly resistantEntero bacteriaceae are highly resistant
Spirochetes are quite sensitive Spirochetes are quite sensitive
All rickettsiae and chlamydiae are highly sensitive All rickettsiae and chlamydiae are highly sensitive
Mechanism of actionMechanism of action
Tetracycline antibiotics inhibit Tetracycline antibiotics inhibit protein synthesisprotein synthesis by inhibiting the binding of by inhibiting the binding of
aminoacyl-tRNAaminoacyl-tRNA to the to the mRNA-ribosomemRNA-ribosome complex. They do so mainly by complex. They do so mainly by
binding to the binding to the 30S ribosomal subunit30S ribosomal subunit in the in the mRNA translationmRNA translation complex. complex.[[
Tetracyclines are widely used in treatment of periodontal diseases.Tetracyclines are widely used in treatment of periodontal diseases.
Used in the treatment of Localised aggressive periodontitis. Used in the treatment of Localised aggressive periodontitis.
Adverse effects :Adverse effects :
GIT-epigastric burning, nausea, vomiting, diarrheaGIT-epigastric burning, nausea, vomiting, diarrhea
Liver damageLiver damage
Renal failureRenal failure
Phototoxicity Phototoxicity
Effects on teeth & bones- Ca tetracycline chelate Effects on teeth & bones- Ca tetracycline chelate
Hypersensitivity Reactions Hypersensitivity Reactions
Superinfection; Antianabolic effectSuperinfection; Antianabolic effect
DOSEDOSE
Tetracycline – 1-2g per day in adultsTetracycline – 1-2g per day in adults
Children over 8yrs -25 to 50mg /kg daily in 2 to4 divided dose Children over 8yrs -25 to 50mg /kg daily in 2 to4 divided dose
TERRAMYCIN,RESTECLIN-250,500mgcap,50mg/ml in10ml vial injTERRAMYCIN,RESTECLIN-250,500mgcap,50mg/ml in10ml vial inj
Ledermycin 150,300mg cap/tabLedermycin 150,300mg cap/tab
DOXT, NOVADOX, TETRADOX-100mg cap.DOXT, NOVADOX, TETRADOX-100mg cap.
Cyanomycin 50,100 mg capCyanomycin 50,100 mg cap
Precaution :Precaution :
Not to be used in pregnancy, lactation and in childrenNot to be used in pregnancy, lactation and in children
Avoided in patients on diureticsAvoided in patients on diuretics
Used cautiously in renal and hepatic insufficiencyUsed cautiously in renal and hepatic insufficiency
Beyond expiry date should not be usedBeyond expiry date should not be used
Do not mix injectable Tc with Pn- inactivation occursDo not mix injectable Tc with Pn- inactivation occurs
Local Drug Delivery SystemsLocal Drug Delivery Systems
Subgingival DoxycyclineSubgingival Doxycycline
-FDA approved 10% of Doxycycline in gel system using a syringe -FDA approved 10% of Doxycycline in gel system using a syringe
Atridox.Atridox.
Reduction in oral microbes. No overgrowth of foreign pathogens.Reduction in oral microbes. No overgrowth of foreign pathogens.
Subgingival MinocyclineSubgingival Minocycline
-- Sustained release form of Minocycline microspheres(Arestin) for Sustained release form of Minocycline microspheres(Arestin) for
subgingival placement as an adjuvant to scaling and root planing.subgingival placement as an adjuvant to scaling and root planing.
-2% Encapsulated into bioresorbable microspheres is used.-2% Encapsulated into bioresorbable microspheres is used.
ORODENTAL CONDITIONSORODENTAL CONDITIONS
Limited use- acute dental infectionsLimited use- acute dental infections
Periodontal diseases – collagenasePeriodontal diseases – collagenase
Refractory periodontal disease – 2week tetracycline(1g/day) or Refractory periodontal disease – 2week tetracycline(1g/day) or
doxycycline(0.1-0.2g/day)doxycycline(0.1-0.2g/day)
Juvenile periodontitis – 2-4 week Juvenile periodontitis – 2-4 week
MACROLIDESMACROLIDES
Macrocyclic lactone ring with attached sugarsMacrocyclic lactone ring with attached sugars
ERYTHROMYCIN-Streptomyces erythreus ERYTHROMYCIN-Streptomyces erythreus
Alternative to pencillin Alternative to pencillin
Water solubility is limited-stable in coldWater solubility is limited-stable in cold
Antibacterial activity : static- cidalAntibacterial activity : static- cidal
Narrow spectrum antibioticNarrow spectrum antibiotic
against penicillin resistant staphylococci against penicillin resistant staphylococci
Active against more gram+ve Active against more gram+ve
Mechanism of action :Mechanism of action :
Dose :Dose :
Adults 250 - 500mg 6hrlyAdults 250 - 500mg 6hrly
Children 30 – 60mg/kg/dayChildren 30 – 60mg/kg/day
Erythromycin (base) - ERYSAFE 250 mg tabErythromycin (base) - ERYSAFE 250 mg tab
Erythromycin stearate -ERYTHROCIN – 250,500mg tabErythromycin stearate -ERYTHROCIN – 250,500mg tab
100mg/5ml susp;100mg/ml ped drops100mg/5ml susp;100mg/ml ped drops
E estolate- ALTHROCIN 125mg kid tab E estolate- ALTHROCIN 125mg kid tab
E ethylsuccinate- ERYNATE E ethylsuccinate- ERYNATE
Adverse effects :Adverse effects :
GIT – epigastric pain GIT – epigastric pain
On high doses – hearing impairmentOn high doses – hearing impairment
Hypersensitivity reactions – rareHypersensitivity reactions – rare
Uses :Uses :
Substitute for penicillin, pencillin resistant infectionsSubstitute for penicillin, pencillin resistant infections
Oral adm, safe and effectiveOral adm, safe and effective
Perio/periapical/NUG/extractionPerio/periapical/NUG/extraction
Prophylactic useProphylactic use
ROXITHROMYCINROXITHROMYCIN
Semisynthetic - long acting, stable macrolide Semisynthetic - long acting, stable macrolide
Antibacterial spectrum similar to erythromycinAntibacterial spectrum similar to erythromycin
DoseDose - 150-300mg BD 30min before food - 150-300mg BD 30min before food
Children - 2.5-5mg/kg BDChildren - 2.5-5mg/kg BD
ROXID, ROXIBID 150,300mg tab ROXID, ROXIBID 150,300mg tab
50mg kid tab,150 mg tab50mg kid tab,150 mg tab
Clarithromycin – CLARIMAC 250,500mg tabClarithromycin – CLARIMAC 250,500mg tab
CLINDAMYCINCLINDAMYCIN
It is lincosamide antibiotic having similar action (macrolide 50s)It is lincosamide antibiotic having similar action (macrolide 50s)
Bacteriostatic – low conc;Bacteriocidal – high conc Bacteriostatic – low conc;Bacteriocidal – high conc
Most active against gram+ve cocci, C.diphtheriae, Actinomyces Most active against gram+ve cocci, C.diphtheriae, Actinomyces
Highly active against – anaerobes (B fragilis)Highly active against – anaerobes (B fragilis)
Pharmacokinetics :Pharmacokinetics :
Oral absorption – goodOral absorption – good
Distribution – skeletal and soft tissuesDistribution – skeletal and soft tissues
Excreted in urineExcreted in urine
Adverse effects :Adverse effects :
Rashes ,UrticariaRashes ,Urticaria
Abdominal pain Abdominal pain
Superinfection -Enterocolitis &DiarrhoeaSuperinfection -Enterocolitis &Diarrhoea
Uses :Uses :
Anaerobic and mixed infections- alternative to Pn & macroAnaerobic and mixed infections- alternative to Pn & macro
Abscess and bone infections-staphy and bacteroidsAbscess and bone infections-staphy and bacteroids
Infective endocarditisInfective endocarditis
Doses : 150-300 mg QID oral ; 200-600mg I.v. 8 hourlyDoses : 150-300 mg QID oral ; 200-600mg I.v. 8 hourly
DALCAP, CLINCIN, DALCIN, 150, 300 mg cap, 300mg/2ml and 600 DALCAP, CLINCIN, DALCIN, 150, 300 mg cap, 300mg/2ml and 600
mg/4ml inj. mg/4ml inj.
Anti fungal drugsAnti fungal drugs
FungusFungus
Composed of a rigid cell wall made up of chitin and various Composed of a rigid cell wall made up of chitin and various
polysaccharides, and a cell membrane containing ergosterolpolysaccharides, and a cell membrane containing ergosterol
Protective layers of the fungal cell make the organism resistant to antibioticsProtective layers of the fungal cell make the organism resistant to antibiotics
Related groups of anti fungal agentsRelated groups of anti fungal agents
1.Antibiotics 1.Antibiotics
A. Polyenes A. Polyenes
B. Heterocyclic benzofuramB. Heterocyclic benzofuram
2.Antimetabolites 2.Antimetabolites
3. Azoles 3. Azoles
A.ImidazolesA.Imidazoles
B.Triazoles B.Triazoles
4.Allylamine 4.Allylamine
5.Topical agents5.Topical agents
NystatinNystatin
A polyene derived from A polyene derived from Streptomyces nourseiStreptomyces noursei
Binds to sterols of fungal cell membraneBinds to sterols of fungal cell membrane
Topical antifungal agentTopical antifungal agent- fungicidal- fungicidal
22ndnd choice to clotrimazole choice to clotrimazole
1 lac units-4 times a day, 10-14 days1 lac units-4 times a day, 10-14 days
Suspended with glycerine Suspended with glycerine
CLOTRIMAZOLE CLOTRIMAZOLE
Effective in the topical treatment. Esp, athletes foot, otomycosis and oral, Effective in the topical treatment. Esp, athletes foot, otomycosis and oral,
cutaneous candidiasis. cutaneous candidiasis.
10mg -3-4times a day. Gel or lotion-denture stomatitis10mg -3-4times a day. Gel or lotion-denture stomatitis
Angular chelitisAngular chelitis
well tolerated although Local irritation and burning well tolerated although Local irritation and burning
No systemic toxicity is seen after topical use.No systemic toxicity is seen after topical use.
SURFAZ, CLOTRIN, CLODERM, 1% lotion, cream, powder 100mg tab.SURFAZ, CLOTRIN, CLODERM, 1% lotion, cream, powder 100mg tab.
ANTIVIRAL DRUGSANTIVIRAL DRUGS
Anti-herpes virusAnti-herpes virus
Idoxuridine,acylovir,famiclovirIdoxuridine,acylovir,famiclovir
Anti-retrovirusAnti-retrovirus
NRTINRTI
ZidovudineZidovudine
LamivudineLamivudine
NNRTINNRTI
nevirapinenevirapine
PIPI
RitonavirRitonavir
IndinavirIndinavir
Antiinnfluenza virusAntiinnfluenza virus
AmantadineAmantadine
Nonselective antiviral drugs-ribavirinNonselective antiviral drugs-ribavirin
AcyclovirAcyclovir
Indications:Indications: Herpes simplex virus (HSV) 1 and 2 infections; HSV Herpes simplex virus (HSV) 1 and 2 infections; HSV
encephalitis; shingles and chickenpox; ointment for herpes infections; creamencephalitis; shingles and chickenpox; ointment for herpes infections; cream
for cold sores for cold sores
Actions:Actions: Inhibits viral DNA replication Inhibits viral DNA replication
SymptomsSymptoms
Rapid progressing- facial cellulitis-HI/SPRapid progressing- facial cellulitis-HI/SP
Chronic/ slowly progressing-odontogenic- staphylococcal/mixedChronic/ slowly progressing-odontogenic- staphylococcal/mixed
>101 F –nonodontogenic- hospitalization>101 F –nonodontogenic- hospitalization
Colour:red/ violeciousColour:red/ violecious
Swelling: indurated, non fluctuant or erythematous – cellulitisSwelling: indurated, non fluctuant or erythematous – cellulitis
Pointed, fluctuant or productive- abscessPointed, fluctuant or productive- abscess
ManagementManagement
Upper faceUpper face
Outpatient: amoxicillin clavulanate or cefaclor orallyOutpatient: amoxicillin clavulanate or cefaclor orally
Ceftriaxone- 1 day ivCeftriaxone- 1 day iv
Inpatient : cefuroxime/ ampicillin+ sulbactam 7-10 daysInpatient : cefuroxime/ ampicillin+ sulbactam 7-10 days
Odontogenic –pencillin/ clindamycin, surgical interventionOdontogenic –pencillin/ clindamycin, surgical intervention
Lower faceLower face
Outpatient: cephalexin, amoxicillin clavuanate, erythromycinOutpatient: cephalexin, amoxicillin clavuanate, erythromycin
Inpatient : iv cefazolin, clindamycinInpatient : iv cefazolin, clindamycin
Some of the commonly used drugsSome of the commonly used drugs
Amox-250,500mg-tidAmox-250,500mg-tid
250mg-Rs 67.50250mg-Rs 67.50
500mg-Rs120.80500mg-Rs120.80
Children20-40mg/kg body weight-tidChildren20-40mg/kg body weight-tid
-125,250mg-125,250mg
Cephalexin(sporidex)Cephalexin(sporidex)
250,500mg250,500mg
250mg-10tab-Rs66.50250mg-10tab-Rs66.50
500mg-10tab-Rs120.50500mg-10tab-Rs120.50
125mg,250mg/5ml125mg,250mg/5ml
125mg;30ml-Rs34.50125mg;30ml-Rs34.50
250mg;30ml-Rs52.60250mg;30ml-Rs52.60
Sporidex dispersible tabsSporidex dispersible tabs
125mg-10tabs-Rs32.25125mg-10tabs-Rs32.25
250mg-10tabs-Rs69.95250mg-10tabs-Rs69.95
Paed drops-100mg/mlPaed drops-100mg/ml
10ml-Rs3310ml-Rs33
MetrogylMetrogyl
200mg;tab 10-Rs3.64200mg;tab 10-Rs3.64
400mg;tab 10-6.31- given tid for 5-10 days400mg;tab 10-6.31- given tid for 5-10 days
Suspension; 200mg /5ml-30ml-Rs8.09Suspension; 200mg /5ml-30ml-Rs8.09
60ml-Rs-12.2760ml-Rs-12.27
List of referencesList of references
Essentials of medical pharmacology :Essentials of medical pharmacology :
KD TRIPATHI; 5th edi.KD TRIPATHI; 5th edi.
Clinical pharmacology – Bennet & Brown 9Clinical pharmacology – Bennet & Brown 9thth ed ed
Oral & maxillofacial infections – Topazian 4Oral & maxillofacial infections – Topazian 4thth ed ed
.Text book of pediatric dentistry – Damle 3.Text book of pediatric dentistry – Damle 3rdrd ed ed
Caranza Text book of periodontology 10Caranza Text book of periodontology 10thth
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