Antibiotics

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

CONTENTSCONTENTS

Introduction.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

•• ββ-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 50-Oral dose for adults 2-4 gm divided into 4 portions children 50-

100mg/kg/day.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