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ANTIBACTERIAL

DRUGSPresented by Ruth Galvez Gutierrez

JDB Ltd. Continuing Education

ProgramJune 13, 2008


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ANTIMICROBIALS

Antibiotics

definition

substances produced bymicroorganism to suppress the growth of othermicroorganisms.

Antimicrobial agentsdefinition

-Agents synthesized in thelaboratory

- Natural antibiotics produced bymicroorganism

- Semi-synthetic agents : key portionof the compound is producednaturally; other portion issynthetic.


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ANTIBACTERIAL THERAPY

Antibacterials areprescribed for to treatinfections caused bybacteria. These

Pathogens can infect:

Gastrointestinal System

Cardiovascular System

Respiratory System

Central Nervous System

Genital System

Urinary Tract

Blood

Musculoskeletal System

Eye

Ear, Nose, Throat

Skin


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CLASSIFICATION

Mechanism of Action

1) Inhibition of synthesis or

damage to cell wall

2) Inhibition of synthesis ordamage to cell

membrane

3) Modification of

synthesis or metabolism

of nucleic acids

Agent

1) Penicillins,

Cephalosporins,

Monobactams,

Bacitracin, Vancomycin

2) Polymyxins

3) Quinolones, Rifampicin,

Nitrofurantoins,

Nitroimidazoles


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CLASSIFICATION

Mechanism ofAction

4) Inhibition or

modification ofprotein synthesis

5) Modification ofenergymetabolism

Agent

4)Aminogylcosides,Tetracyclines,

Chloramphenicol,Erythromycin,Clindamycin,Spectinomycin,Mupirocin

5)Sulphonamides,Trimethoprim,Isoniazid


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CATEGORY 1

Category 1 Inhibition of synthesis or

damage to cell wall. This leads to death of the

bacteria. The cells burst and die. These drugs

are referred to as Bactericidal.Included:The Beta-Lactam Agents -

Penicillins, Cephalosporins,Carbapenems,

Monobactams, Beta-Lactamase Inhibitors.


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Beta-Lactamase Agents

Penicillins- chemical structure has a beta-

lactam ring and a second ring attached.

Penicillins Treatment of throat infections, otitis

media, endocarditis, meningitis, pneumonia,prophylaxis in limb amputation, tonsilitis,

erysipelas, rheumatic heart fever.


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Penicillins

Drug

Generic nameBenzylpenicillin

Brand name Crystapen

Contra-indications

history of allergy causesanaphylactic shock

Side effects- fever, jointpain, rashes,

angioedema, kidneyproblems, nausea,anaphylaxis, diarrhea.

Presentation & Dosage

Presentation -Injectableonly

Dosage Adult

intramuscular, slowintravenous injection or byinfusion. Given 1.2g daily in4 divided doses max- 2.4g

Child 1mo to 12 yrs-100mg/kg daily in 4 divideddoses


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Penicillins

Drug

Generic name -1)Procaine Penicillin

2) Benzathine penicillin

Brand name

various Contra-indications

sames as benzylpenicillin

Side effects same asbenzylpenicillin


1) & 2) Presentations -Injectables intramuscularonly

1) Dose

Combinationform of Procaine 300mgand Benzyl 60mg every12-24hours IM

2) Combination form ofBenzathine and Benzyl1.2

2.4

4 m.u. IM

long acting


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Penicillins

Drug

Generic name-

1) Amoxicillin

2) Ampicillin Brand name various

Contra-indication- penicillin

allergy

Side effects- same asbenzylpenicillin


1) & 2) Presentation- Oral

capsule/tablet & suspension

i.e liquid forms

1) Adult Dose 250mg

500mg every 8hours. Child

125mg-250mg every 8hours

( 5-14 days)

2) Adult & Child Dose

same but every 6 hours


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Penicillins

Drug

Beta-Lactamase Inhibitors orPenicillinase(enzyme)Resistant

Generic names

1)Cloxacillin, Dicloxacillin2)Flucloxacillin,3)Clavulanate

4)Sulbactam

Brand names

various for1)&2) 3)Augmentin

Contra-indications & Sideeffectssame asbenzylpenicillin


1) & 2) PresentationsOral capsules/tablets &suspensions i.e. liquidforms; IM & IV injections

Adult Dose

Oral

250mg-500mg very 6hoursbefore food

IM 250mg every 6h; IV250mg-1g every 6h

Child Dose

any route - adult dose.


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Cephalosporins

Drug

First Generation

Cephalosporins

Cephalothin

Cefazolin

Cephalexin

Cephradine Cefadroxil

Cefaclor

Cefprozil

Presentation

First Generation

Cephalosporins

1) IV

2) IV

3) Oral

4) Oral & IV5) Oral

6) Oral

7) Oral


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CephalosporinsDrug

Second Generation

1) Cephamandole

2) Cefuroxime3) Cefonicid

4) Cefoxitin

5)Cefotetan6) Cefmetazole

7) Cefprozil

Presentation

Second Generation

1) IV

2) Oral & IV & IM3) IV

4) IV

5)IV6) IV

7) Oral


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Cephalosporins

Drug

Third Generation

1) Cefotaxime

2) Ceftizoxime

3) Ceftriaxone

4) Cefixime

5) Ceftazidime

6) Cefoperazone

7) Cefpodoxime

8) Ceftibuten

Presentation

Third Generation

1) IV

2) IV

3) IV / IM

4) Oral

5) IV / IM

6) IV

7) Oral

8) Oral


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CephalosporinsDrug

Fourth Generation

1) Cefepime

2) Cefirome

Presentation

Fourth Generation

1) IV

2) IV


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Cephalosporins

Drug

First, Second, Third &Fourth GenerationCephalosporins

Contra-indications & SideEffects

Contra-indicationCephalosporin Sensitivity(Allergy) Approx 20%Cross Sensitivity withPenicillin Allergy

Side Effects- Diarrhea, n/v,rash, fever, headache,abdominal discomfort,

dizziness, jaundice (liver),blood disorders , nephritis(kidney)


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CephalosporinsDrug

First Generation

1)Oral

2) IV

Dosage

First Generation

Adult 250mg -500mg

every 6 to 8 hours; orevery 12 hours

Child 125mg- 250mgevery 6-8hours; or

12hourly2) 0.5 -1g every 6

12hours


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Cephalosporins

Drug

Second Generation

1) Oral

2) IV

Dosage

Second Generation

1) Adult Dose 500mg -1g

every 12 hours. Child Dose-125mg 250mg every 12

hours

2) Adult Dose- 1g-2g every 6-

8hours. Child Dose- 20-

40mg/kg every 6-8 or 12

hours


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Cephalosporins

Drug

Third Generation

1) Oral

2) IV

Dosage

Third Generation

1) Adult Dose- 200mg -400mg once daily or

divided every 12 hours.Child 8mg/kg oncedaily or divided every 12hours.

2) Adults- 1g-2g once dailyor divided every 12h.Child- 20,50, or 80mg/kgdaily. Doses by slow IVinfusion or IM


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Cephalosporins

Drug

Fourth Generation

1)IV

Dosage

Fourth Generation

1) Adult dose- 1-2g or

up to 4g once daily or2 divided doses.Severe infections 6g daily. Child dose

50mg/kg in 2 divideddoses or IM


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Other Beta-Lactam Drugs

Include CARBAPENEMS &

MONOBACTAMS

Carbapenems

1) Imipenem - IV

2) Meropenem IV

Monobactam1) Aztreonam IV & IM (


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Vancomycin & Bacitracin

Drug

1) Vancomycin

Generic name

Vancomycin .

Brand Name - Various

2)Bacitracin

Presentation & Dose

1) Capsules & IV Inj

Adult Dose- Oral- 125mg

every 6 hours. Child-5mg/kg every 6hours

IV 500mg-1g every

12hours. Child-10mg/kg

every 6hours2) Topical Use only - Ointment


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ANY

QUESTIONS

??????????


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LESSON 2

ANTIBACTERIAL

DRUGS

Presented by Ruth Galvez GutierrezJDB. Ltd. Continuing Education Program

June 21, 2008


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CATEGORY 2

Category 2 Inhibition of synthesis

or damage to cyto-plasmic

membrane. This drug penetrates

the cell wall then produces holes inthe cell membrane through which

intracellular constituents leak out

of the bacteria and causes it to die.This drug isBactericidal.

This categoryincludes Polymixins.


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POYMYXINS

Polymyxins are used topically in the

treatment of eye, ear, skin infections.

Polymyxins are used orally,

intramuscularly, or intravenously forthe treatment of oro-pharyngeal

infections (oral & throat cavity) and for

the suppression of the intestinal flora

in immuno-compromised patient(intensive care).


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POLYMYXINS

Drug

Generic name:

Colistin

Brand name:

Colomycin

Containdications:

Pregnancy,

breastfeeding; kidney

failure; Myastheniagravis

Side effects:

neurotoxic &

nephrotoxic


Presentation:oral

capsule; injectable

im or iv; nebulised

solution

Dosage:1-3m.i.u

every 8hours

Rarely used:mainly in

Immunocompromisedpatients and under

most vigilant patient

care (Intensive Care)


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POLYMYXINSDrug

Generic name:Polymyxin B Sulphate

Brand name: various;usually combinationforms for topical use.

Contraindications:same as Colistin

Side effects:neurotoxic in systemicuse: dizziness,confusion, visualdisturbances,respiratory paralysis,rash, fever.Nephrotoxic Kidney

complications

Presentations & DosagePresentation

Topical Skin Ointment0.1% in combinationwith Neomycin & Eye

Ointments 0.1% incombination withTetracycline orGramicidin.

Dosage:applied 2-3xdaily

Oral

IV & IM

Dosage:1.5-2mg/kgdaily


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CATEGORY 3

Category 3Modification of

synthesis or metabolism of

nucleic acids

This category includes

Quinolones, Rifampicin,

Nitrofurantoin and

Nitroimidazoles.


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QUINOLONES

DrugQuinolones include :

Naldixic Acid,

Oxolinic Acid,

Cinoxacin,Ciprofloxacin,

Norfloxacin,

Ofloxacin,

Lomefloxacin,Enoxacin,

Pefloxacin,

Levofloxain,

Sparfloxacin,

Presentation

Oral

Oral

OralOral, IV

Oral

Oral, IV

OralOral

Oral, IV

Oral, IV

Oral


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Clinical Uses of QuinolonesRespiratory Tract Infections- Necrotizing

Otitis, Sinusitis, Bacterial Bronchitis,

Pneumonia.

Urinary Tract Infections- Cystitis,

Pyelonephritis, Prostatitis.Skin Structure Infections- Cellulitis (not

first line treatment)

Osteomyelitis bone tissue

Bacterial Diarrheal Diseases

Sexually Transmitted Diseases

Gonorrhea, Chlamydia, Chancroid,

Syphylis.


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Clinical Problems of

Quinolones

Gastrointestinal effects

nausea,vomiting, abdominal pain, rarelydiarrhea

Central Nervous System effects

dizziness, headache, restlessness,depression, insomnia, disturbances invision, taste and smell, ( rarelyseizures).

Damage to growing cartilage ( notrecommended for use in children)

Theophylline interaction (w/Ciprofloxacin & Enoxacin)

Allergic reaction- rashes, itching, fever


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QUINOLONES

Drug

Generic name:Nalidixic acid

Brand names:Urogesic, Negram

Indicated :UrinaryTract Infections

Contra-indications& Side effects :same as for allQuinolones

Presentation &Dosage

Presentation -Oral tablets500mg

Dose- 500mg -1gevery 6 hours for7 days; Child 50mg/kg daily individed doses


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QUINOLONES

Drug

Generic name:

Ciprofloxacin

Brand name:Cipro,

Ciproxina

Contra-indications &

Side-effects:same

as for all Quinolones

Exception: in child

when benefit

outweighs risk


Oral:tablets 250mg;

500mg; 1g

Dose Oral:250-500mg

2xdaily for UTIs; 250-

500mg stat for

Gonorrhea; other

infections: 500-

750mg2xdaily Dose IV:200-400mg

2xdaily

Child: 7.5-15mg/kg


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QUINOLONES

Drug

Generic name:

Norfloxacin

Brand name:Noroxin

Indications:UTI

Contra-indications& Side-effects:

same as for

Quinolones

Presentation

&Dosage

Oral:tablets 400mg

Dosage:400mg2xdaily for 7-

10days; Chronic

UTIs : treatment up

to 12 weeks.


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QUINOLONES

Drug

Generic name:Ofloxacin

Brand name:Floxin

Contra-idications &Side-effects:sameas for Quinolonesincluding :tachycardia,hypotension,psychotic reactions.


Oral:tablets 200mg &400mg; IV infusion-2mg/ml (50ml bot)

Dose:UTIs 200-400mgdaily in the morning;chronic UTIs-400mg2xdaily; Skin & LowerRespiratory-tract

infections-400mgdailyor 2xdaily; Gonorrhea -400mg stat

IV :200mg-400mg onceor 2xdaily dependingon severity of infection


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QUINOLONES

Drug

Generic name:Levofloxacin

Brand name:Levaquin,

Tavanic Contra-indications &

Side-effects:same asfor all Quinolones,including: tremor,

tachycardia,hypotension


Oral:tablets 250mg

Dose:Sinusitis-500mgdaily for 10-14days;

Chronic Bronchitis-250-500mg daily for 7-10days; Pneumonia-500mg 1-2xdaily for 7-10days; UITs-250mg

daily for 7-10days;Skin & Softtissue infection-250-500mg 1-2xdaily for 7-10days

IV:500mg 1-2Xdaily


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NITROFURANS

NITROFURANS -3 Drugs used

clinically include:

1)Nitrofurantoin:used to treat

Urinary Tract Infections (UTIs)

2)Furazolidine : used to treat

intestinal infections antiprotozoal

and antibacterial

3)Nitrofurazone :used only for

topical applications


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NITROFURANTOINDrug

Generic name:

Nitrofurantoin

Brand name:

Macrobid; Furadantin

Contra-indications:

Impaired Kidney

Function, Child under

3mo old ,Pregnancy,

Breastfeeding.

Side-effects:

anorexia,n/v,

diarrhea, peripheral

neuropathy


Oral :tablets or

capsules - 50mg &

100mg

Dose:50mg-100mg

every 6 hours for7days. Child over 3

mo: 3mg/kg daily in 4

divided doses.


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FURAZOLIDINE

DRUG

Generic name:

Furazolidine

Brand name:Diafren,

Enterocetin

Contra-indications:

Infants under 1 mo of

age

Side effects:n/v;

headache,dizziness,

drowsiness; Allergic

skin reactions-rashes


Oral:Suspension

25mg/5mls; tablets

50mg

Dose:Adults- 100mg

4xdaily for 2-5days up

to 7 days. Child

1.25mg/kg 4xdaily;

10days treatment forGiardiasis.


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NITROFUAZONEDRUG

Generic name:Nitrofurazone

Brand name:FuratopCream, Furasep

Cream Indications:bacterial

infections of wounds,burns, ulcers, cuts,before skin grafting

Caution:Knownallergic reaction

Side effects:Allergicreactions-skin

rashes, itching


Topical :Cream andSolution both 0.2%concentration

Dose:Apply directly

on lesions or on gauzefirst; 2-3 times dailyor as advised bydoctor


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RIFAMPICIN

Rifampicinis used in combinationwith other drugs mainly to treatTubercolosis

Treatmentsneed to be fullysupervised- Public Health aspect considered a communicabledisease. The population must be

protected. Vaccination Programstarted in infancy.


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Rifampicin

Drug Generic name:Rifampicin

Brand name:Rimactane

Conta-indications:Jaundice (liverfunction)

Side-effects:anorexia, n/v,

diarrhea, chills, fever,dizziness, bone pain,shortness of breath,collapse and shock,jaundice, rashes,muscular weakness


Oral:Capsules 150mg;Syrup 100m/5ml

IV:300mg vial & 600mgvial

Dose:0.6-1.2g daily Combination with otherdrugs


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ANY

QUESTIONS

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