 That is capable of destroying or weakening certain

microorganisms, especially bacteria or fungi, that cause

infections or infectious diseases.

 Antibiotics are usually produced by or synthesized from other

microorganisms, such as molds.

 These are used to treat infections caused by bacteria.

 Antibacterial agents or antibiotics fall into several major

categories.
 Aminoglycosides
 Carbapenes
 Cephalosporin's
 Erythromycins
 Penicillin's (including various sub groups)
 Sulfonamides
 Tetracycline's
 Fluoroquinolones
 Metranidazole
 Miscellaneous agents
 These drugs containing amino sugars, are used primarily in
infections caused by gram negative enterobacteria and
suspected sepsis.

 The toxic potential of these drugs limit their use.

 MOA: These are bactericidal, they inhibit the bacterial

protein synthesis by binding the function of 30 S ribosomal
sub unit.

 Their MOA is not fully known.

 Major amino glycosides include:

AGENT HALF ADMINISTRATION COMMON DOSAGE

LIFE RANGE(A)
15MG/KG/DAY(once daily
Amikacin 2-3 hrs IV, IM dose)
3mg/ kg/day(standard)
Gentamycin 2 hrs IV, IM 6-7mg/kg/day(once daily)

Kanomycin 2-4 hrs Oral, IV 15mg/kg every 8-12hrs

50-100mg/kg/day(oral)
Neomycin 2-3hrs Oral, Topical 10-15mg/day (topical)

Netilmicin 2-7 hrs IV, IM 3-6mg/kg/day

Streptomycin 2-3 hrs IM 15mg/kg/day

3mg/ kg/day(standard)
Tobramycin 2-5 hrs IV, IM 6-7mg/kg/day(once daily)
 Streptomycin :
 It is active against both gram positive and gram negative
bacteria.
 This drug has restricted its use to organisms that cause plague,
tularemia, gram positive streptococci and mycobacterium
tuberculosis.
 Amikacin, kanomycin, gentamycin, tobramycin, neomycin
netilmicin are active against many gram negitive bacteria.
 Gentamycin active against some staphylococcus strains. it is
more active than Tobramycin against Serratia organisims
 Amikacin is broadest spectrum aminoglycoside with activity
against most aerobic gram negative bacilli as well as many
anaerobic gram negative strains that resist gentamycin and
tobramycin.
 It is also active against M. tuberculosis and M. avium-
intracellulare.
 Tobramycin may be more active against pseudomonas
aeruginosa than gentamycin.
 Netilmicin may be active against gentamycin- resistant
organisms it appears to be less ototoxic than other
aminoglycosides.
 Neomycin in addition to its activity against such gram negative
organisms as Escherichia coli and klebsiella pneumoniae, is
active against several gram positive organisms.
 Therapeutic uses:
 Streptomycin is used to treat plague, tularemia, acute
brucellosis(given in combination with tetracycline) and
tuberculosis( given in combination with other anti tubercular
agents).
 Gentamycin, tobramycin, amikacin and netilmicin are used for
gram negitive bacillary infections( those caused by
enterobacter, serratia, klebsiella and p. aeruginosa),
 Bacterial endocarditis caused by streptococcus viridians (given in
combination with pencillin), pneumonia (given in combination with
cephalosporin's or penicillin), meningitis, complicated uti,
osteomylelitis and peritonitis.

 Neomycin is used for preoperative bowel sterilization; hepatic coma

and in topical form for skin and mucous membrane
infections(burns).

 PRECAUTIONS & MONITERING EFFECTS:

 Amino glycosides cause serious adverse effects to prevent or

minimize such problems blood drug concentrations, BUN and serum
creatinine levels should be monitored during the therapy.
 A) OTOTOXICITY:
 Amino glycosides causes vestibular or auditory damage.
 Gentamycin and streptomycin can cause primarily vestibular
damage. (tinnitus, vertigo and ataxia)
 Amikacin, kannamycin, and neomycin cause mainly auditory
damage. (hearing loss).
 Tobramycin can result in both vestibular and auditory damage.
 B) NEPHROTOXICITY:
 Because amino glycosides accumulate in the proximal
convoluted tubule, mild renal dysfunction develops in up to
25% of patients receiving these drugs for several days.
 Neomycin is the most nephrotoxic amino glycoside,
streptomycin is the least nephrotoxic.

 Gentamycin and tobramycin are nephrotoxic to approximately

same degree.

 Risk factors for increased nephrotoxic effects include:

 Preexisting renal disease

 Previous or prolonged amino glycoside therapy

 Concurrent administration of another nephrotoxic drug.

 NEUROMUSCULAR BLOCKADE:

 This problem may arise in patients receiving high dose amino

glycoside therapy:

 Risk factors for neuromuscular blockade include :

 Concurrent administration of neuromuscular agents or an

anesthetic

 Preexisting hypocalcaemia or myasthenia gravis.

 Intraperitonial or rapid IV administration.

 Hypersensitivity and local reactions are rare adverse effects of

amino glycosides.
 These agents are ß Lactams that contain a fused ß lactam ring and a five
membered ring system that differs from penicillin's in being unsaturated and
containing a carbon atom instead of sulfur atom.

 The class has a broader spectrum of activity than do most ß lactam .

 Imipenem was first carbapenam compound introduced in United states

followed by Meropenam and most recently Ertapenam and Doripenam
came into existence.

 Imipenam is combined by Cilastanin sodium as it is inhibited by the renal

dipeptidases.
 Major carbapenems include:

Agent Elimination Half life ROA Dosage

route

Doripenam Renal 1 hr IV 500mg every 8 hrs

Imipenam Renal 1 hr IV 250 mg every 6 hrs

Ertapenam Renal 4 hrs IV, IM 1g/day

Meropenam Renal 1.5 hrs IV, IM 0.5-2g every 8 hrs

 Mechanism of Action:

 Carbapenems are bactericidal, inhibiting bacterial cell wall

synthesis.

 Spectrum of activity:

 These drugs have the broadest spectrum of all ß lactam

antibiotics.

 The group is active against most gram positive cocci, gram

negative rods and anaerobes.

 This class has good activity against many bacterial strains

that resist other antibiotics.
 Ertapenam has narrower spectrum of activity than other
carbapenams.
 It has little or no activity against P. aeruginosa and
Acinetobacter.
 Therapeutic uses:
 These are effective against urinary tract and lower respiratory
infections, intra abdominal and gynecological infections and
skin, soft tissue and joint infections.
 Precautions and monitoring effects:
 Carbapenems may cause nausea, vomiting, diarrhea and
pseudomembraneous colitis.
 Seizures, dizziness and hypotension may develop; seizures
appear less frequently with meropenam or ertapenem.

 Patients who are allergic to penicillin or cephalosporin's may

suffer cross- sensitivity reactions during carbapenams therapy.
 These agents are known as ß lactam antibiotics because
their chemical structure consists of ß lactam ring adjoined
to a thiazolidine ring.

 Cephalosporin's generally are classified in major groups

based on mainly on their spectrum activity.

 Mechanism of action:

 These are bactericidal they inhibit bacterial cell wall

synthesis, reducing cell wall stability and thus causing
membrane lysis.
 Spectrum of activity:
 First generation: These cephalosporin's are active against most
gram positive cocci (except enterococci) as well as enteric aerobic
gram negative bacilli.

 Second generation: Cephalosporin's are active against the

organisms covered by first generation cephalosporin's and have
extended gram negative coverage, including ß lactamse producing
strains of Haemophilus influenzae.

 Third generation: Cephalosporin's have wider activity against

more gram negative bacteria, for example Enterobacter, citrobacter,
serratia, providencia, neisseria and haemophilus
 Fourth generation cephalosporin's include cefepime and
ceftaroline.

 These shows evidence of greater activity versus gram positive

cocci, enterobacteriaceae and pseudomonas than third
generation.

 It has poor activity against anaerobes, stenonotrophonomas and

pseudomonas species.
 First generation cephalosporin's:
Agent Elimination Half life ROA Dosage
route

Cefadroxil Renal 1-5 hrs Oral 1-2G/DAY

Cefazolin Renal 1.4-2.2 hrs IV 250mg-1g/day

Cefalexin Renal 0.9-1.3 hrs Oral 250-500mg every

6hrs

Cephapirin Renal 0.6-0.8 hrs IV, IM 500mg-2gm every

4-6 hrs

cephradine Renal 1.3 hrs Oral , IV 250-500mg every

6hrs
 Second generation Cephalosporins:
Agent Elimination Half life ROA Dosage
route

Cefaclor Renal 0.8 hr Oral 250-500MG

Cefmetazol Renal 72 mins IV 2g every 6- 12 hrs

e

Cefotetan Renal 2.8-4.6hrs IV, IM 1-2g every 12 hrs

Cefoxitin Renal 0.8 hrs IV 1-2g every 6-8 hrs

Cefprozil Renal 78 mins Oral 250-500 mg every

12-24 hrs

Cefuroxime Renal 1.5-2.2 hrs IV, IM 750mg-1.5g every

8hrs
 Third generation:
Agent Elimination Half life ROA Dosage
route
Cefixime Renal 3-4 hrs Oral 400mg/day
Cefdinir Renal 1.7-1.8hrs Oral 300mg every 12
hrs
Cefditoren Renal 1.6hrs Oral 400mg every 12
hrs
Cefoperazo Renal 1.6-2.4hrs IV 2-4g every 12 hrs
ne
Cefotaxime Renal 1.5hrs IV 1-2g every 6-8 hrs

Cefpodoxim Renal 2.5hrs Oral 100-400mg every

e 12 hrs
Ceftazidime Renal 1.8hrs IV,IM 1-2g every 8-12
hrs
Ceftibuten Renal 2.5hrs Oral 400mg/day

Ceftizoxime Renal 1.7hrs IV 1-2g every 8-12

hrs
 Fourth generation:

Agent Elimination Half life ROA Dosage

route

Cefepime Renal 2-2.3hrs IV,IM 1-2g every

8-12hrs

Ceftaroline Renal 2.6hrs IV 600mg every

12hrs
 First Generation: these are commonly administered to
treat serious Klebsiella infections and gram positive
and some gram negative infections in patients with
mild penicillin allergy.ono
 Second generation: these are valuable in treatment of
UTI resulting from E.coli organisms acute otitis media,
sinusitis and gonococcus diseases.
 Cefaclor (ceclor): it is useful in otitis media and
sinusitis in the patients who are allergic to ampicillin
and amoxicillin.
 Cefuroxime(Zinacef): it is commonly administered for
outpatient community acquired pneumonia.

 Third generation : these can penetrate into cerebrospinal

fluid and thus are valuable in treatment of meningitis caused
by meningococci, pneumococci, H. influenza etc.,

 These are also used to treat sepsis and fever.

 Fourth generation agent cefepime is approved for treatment

of UTI’s, skin infections, pneumonia.
 Precautions and monitoring
 Because all cephalosporin's are eliminated renally doses must
be adjusted for patients with renal impairment.

 Other adverse effects include nausea, vomiting, diarrhea,

nephrotoxicity.

 Cephalosporin's may cause false positive glycosuria results on

test using the copper reduction method's

 Ceftriaxome is now contraindicated in new borns in

concomitant with calcium containing solutions due to the risk
of precipitation in lungs and kidneys.
 MOA: these may be bactericidal or bacteriostatic they bind
to the 50S ribosomal subunit , inhibiting bacterial protein
synthesis.
 Spectrum Of Activity: these are active against many gram
positive organisms including streptococci ,
corynaebacterium, neisseria species as well as some strains
of mycoplasma, legionella and treponema.
 Therapeutic uses:
 These are drugs used for treatment of mycoplasma
pneumoniae, campylobacter infections, legionnaries
disease, chlamidial infections and diphtheria.
 In patients with penicillin allergies erythromycins are most
commonly used especially in treatment of pneumococcal
pneumonia, s.aureus infections, syphilis and gonorrhea.
 These may be given prophylactic ally before dental procedures
to prevent bacterial endocarditis.
 Precautions & monitoring parameters:
 Gastrointestinal distress(GI) (nausea, vomiting, diarrhea,
epigastric discomfort) may occur with all erythromycin forms
and are most common adverse effect.
 Allergic reactions may present as skin eruptions, fever and
eosinophilia.
 Cholestatic hepatitis may arise in patients treated for 1 week or
longer with erythromycin estolate , symptoms usually disappear
within few days as drug therapy ends.

 IM injections for more than 100mg produce severe pain

persisting for hours.

 Transient hearing impairment may develop with high dose

erythromycin therapy.
Agent Elimination route Half life ROA DOSAGE

AZITHROMYCIN HEPATIC 68HRS ORAL 250mg/day

Clarithromycin Renal 3-7 hrs Oral 250-500mg every

12 hrs

Erythromycin Heaptic 1.2-3.6hrs Oral 250-500mg every 6

based estolate, hrs
ethyl succinate
and stereate

Erythromycin IV 0.5-2.0g every 6

gluceptate and hrs
lactobionate
 I. Natural penicillin's:

 Among most important antibiotics natural penicillin's are

preferred drugs in treatment of many infectious diseases.

 Available agents:

 Penicillin G: sodium and potassium salts are administered

orally, intravenously and intramuscularly,

 Penicillin V: it is a soluble drug form administered orally.

 Penicillin G procaine and Penicillin G benzthine are

repository drug forms and administered IM.
 MOA:
 Penicillin's are bactericidal, they inhibit bacterial cell wall
synthesis in a manner similar to cephalosporin's.
 Spectrum of activity:
 Natural penicillin's are highly active against gram positive
cocci and some gram negative cocci.
 Penicillin G is 5 to 10 times more active than penicillin V
against gram negative organisms and some aerobic organisms.
 As natural penicillin are already hydrolyzed by penicillinases
they ineffective against S. aureus and other organisms that
resist penicillin
 Therapeutic uses:
 Penicillin G is preferred agent for all the infections
caused by penicillin susceptible s. pneumoniae organisms
including:
 Pneumonia
 Arthritis
 Meningitis
 Peritonitis
 Pericarditis
 Osteomyelitis
 Mastoiditis
 Penicillin's G and V are highly effective against other
streptococcal infections such as pharyngitis, otitis media
 Sinusitis and bacteremia.

 Penicillin G preferred agent in gonococcal infections, syphilis,

anthrax, actinomycosis, gas gangrene and listeria infections.

 Penicillin V is most useful in skin, soft tissue and mild

respiratory infections.

 Penicillin G procaine is effective against syphilis and

uncomplicated gonorrhea.

 Penicillin G and V are used prophylactic ally to prevent

streptococcal infections, rheumatic fever and neonatal
opthalmia.
 Precautions and monitoring:

 Hypersensitivity reactions:

 The rash may be urticarial, vesicular, bullous, scarlantiform or

maculopapular.

 Anaphylaxis is a life-threatening reaction that most commonly

occurs with parenteral administration. Signs and symptoms
include severe hypotension, bronchoconstriction, nausea,
vomiting, abdominal pain and extreme weakness.

 Other manifestations of hypersensitivity reactions include

fever, eosinophilia, angioedema and serum sickness.
 Other adverse effects of natural penicillin's include GI distress,
bone marrow suppression (impaired platelet aggregation,
agranulocytosis).

 With high dose therapy seizures may occur particularly in

patients with renal impairment.
 Agent Elimination Half-life ROA Dosage
route

Penicillin G Renal 0.5hrs Oral, IV, IM 200,000-

500,000U
every 6-8 hrs

Penicillin V Renal 1 hr Oral 500mg-2g per

day

Penicillin G Renal 24-60hrs IM 300,000-

Procaine 600,000u/day

Penicillin G Renal 24-60hrs IM 300,000-

benzathine 600,000u/day
 Penicillinase resistant penicillin's:

 These penicillin's are not hydrolyzed and the agents include

methicillin, nafcillin and isoxazolyl penicillin's- dicloxacillin and
oxacillin.

 MOA: same as natural penicillin's.

 Spectrum of activity:

 Because these penicillin's resist pencillinases these are active against

staphylococci.

 Therapeutic uses:

 These are used in staphylococcal infections resulting from organisms

that resist natural penicillins.
 These agents are less potent than natural penicillin's .

 Nafcillin is excreted through liver and thus may be useful in

treating staphylococcal infections in patients with renal
impairment.

 Oxacillin and dicloxacillin are most valuable in long term

therapy of serious staphylococcal infections (endocarditis,
osteomyelitis) and in treatment of staphylococcal infections of
skin and soft tissues.

 Precautions and monitoring effects:

 Like natural penicillins hypersenitivity reactions including

 Methicillin may cause nephrotoxicity and interstitial nephritis.

 Oxacillin may be hepatotoxic.

Agent Elimination Half- ROA Dosage

route life
Dicloxacillin Renal 0.5- Oral 500mg-1g/day
9.5hr
Methicillin Renal 0.5-1hr IV,IM 1-2g every 4-
6hrs
Nafcillin Hepatic 0.5hrs Oral, 0.25-2g every
IV,IM 4-6hrs
Oxacillin Renal 0.5hrs Oral, 500mg-2g
IV,IM every 4-6hrs
 Aminopenicillins :this group includes the semi synthetic
agents ampicillin and amoxicillin. Because of their wider
antibacterial spectrum these drugs are also known as broad
spectrum penicillin's.

 MOA: same as natural penicillin's

 Spectrum of activity:

 These has a spectrum that is similar to but broader than that

of natural and penicillinase resistant penicillins.

 Aminopenicliins are ineffective against most staphylococcal

organisms.
 Therapeutic uses:

 These are used to treat gonococcal infections, upper respiratory

infections, uncomplicated urinary tract infections and otitis
media.

 For the infections resulting from penicillin resistant organisms

ampicillin may be given in combination with salbactum.

 Amoxicillin is less effective than ampicillin in shigellosis

 Amoxicillin is more effective against S.aureus and klebsiella

infections when administered in combination with clavulanic
acid.
 Precautions and monitoring:

 Hypersensitivity reactions may occur.

 Diarrhea is most common with ampicillin.

 Ampicillin and amoxicillin cause generalized erythomatous,

maculopapular rash.
 Agent Elimination Half-life ROA Dosage
route

Amoxicillin Renal 0.8-1.4hr Oral 250-500mg

every 8 hrs

Amoxicillin/ Renal 1hr Oral 250-500mg

clavulanic acid every 8 hrs

Ampicillin Renal 0.8-1.5hrs Oral, 250-2g every

IV,IM 4-6hrs

Ampicillin / Renal 1-1.8hrs IV,IM 1.5-3g every 6

salbactum hrs
 Extended spectrum penicillin:
 These agents have widest antibacterial spectrum similar to that of
aminopenicillins but also are effective against klebsiella and
enterobacter species.

 These are called as antipseudomonal penicillin's this group

includes the carboxypenicillins(tircacillin) and ureidopencillins
(pipercillin).

 MOA: same as natural penicillin's

 Spectrum of activity:

 These drugs have spectrum similar to that of aminopenicillins but

also are effective against klebsiella and enterobacter species.
 Tircacillin is active against P. aeruginosa combined with
clavulanic acid(timentin).

 Pipercillin is more active than tircacillin against Pseudomonas

organisms.

 Pipercillin and tazobactum it is a β-lactamase inhibitor that

expands the spectrum of activity to include staphylococci,
haemophylus, bacterioids.

 Generally tazobactam does not enhance activity against

pseudomonas.
 Therapeutic uses:
 These are mainly used to treat serious infections caused by
gram negative organisms (sepsis, pneumonia, infections in
abdomen, bone and soft tissues).
 Tazobactum/pipercillin is effective in treatment of nocosomal
pneumonia.
 Precautions and monitoring:
 Hypersensitivity reactions may occur.
 Tircacillin may cause hypokalemia.
 High dose content of tircacillin may pose a danger to patients
with heart failure.
 All inhibit platelet aggregation which may result in bleeding.

Agent Elimination Half-life ROA Dosage

route

Pipercillin Renal 0.8-1.4hrs IV,IM 1.0-1.5mg/kg

every 6-12 hrs

Pipercillin/t Renal 0.7-1.2hrs IV 3.3g every 6hrs

azobactum

Ticarcillin/ Renal 1-1.5hrs IV 3.1g every 4-

clavulanic 6hrs
acid
 Sulfonamides

 Derivatives of sulfanilamide, these agents were the first drugs

to prevent and cure human bacterial infections successfully.

 Sulfonamides remain drug of choice for certain infections.

 The major sulfonamides are sulfadiazine, sulfamethoxazole,

sulfisoxazole and sulfamethizole.

 MOA: sulfonamides are bacteriostatic, they suppress bacterial

growth by triggering a mechanism that blocks folic acid
synthesis, there by forcing bacteria to synthesize their own
folic acid.
 Spectrum of activity:

 Sulfonamides are broad spectrum agents with activity against

many gram positive organisms (s. pyogenes, s.pneumoniae)
and certain gram negative organisms (H. influenzae, E.coli).

 They are also effective against certain strains of Chlamydia

trachomatis, nocardia, actinomyces and Bacillus anthracis.

 Therapeutic uses:

 Sulfonamides most often are used to treat urinary tract

infections caused by E.coli including acute and chronic cystitis
and chronic upper respiratory tract infections.
 These agents are also used in nocardiasis, trachoma,
conjunctivitis and dermatitis.

 Sulfadiazine may be administered in combination with

pyrimethamine to treat toxoplasmosis.

 Sulfamethoxazole may be given in combination with

trymethoprim to treat pneumonia, enteritis, sepsis, UTI,
respiratory infections and gonococcal urethritis.

 Sulfisoxazole is sometimes used in combination with

erythromycin ethylsuccinate to treat acute otitis media caused
by H. influenzae organisms.
 Prophylactic sulfonamide therapy has been used
successfully to prevent streptococcal infections and
rheumatic fever recurrences.

 Precautions and monitoring effects:

 Sulfonamides may cause blood dyscrasias(hemolytic

anemia- particularly in patients with G6PD deficiency,
a plastic anemia, thrombocytopenia, agranulocytosis
and eosinophilia).

 Hypersensitivity reactions include mostly in skin and

mucous membranes.
 Manifestations include various types of skin rashes, exfoliate
dermatitis and photosensitivity.

 Crystalluria and hematuria may occur possibly leading to UTI

obstruction, sulfonamides should be used cautionly in patients
with renal impairment.

 AIDS patients have increased frequency of cutaneous

hypersensitivity reactions to sulfamethoxyzole.
 Agent Elimination Half-life ROA Dosage
route

Sulfacytine Renal 4-4.5hrs Oral 250mg every

6hrs

Sulfadiazine Renal 6hrs Oral, IV 2-4g/day

Sulfamethoxazole Hepatic 9-11hrs Oral 1-3g/day

Sulfisoxazole Renal 3-7hrs Oral, IV 2-8g/day

Sulfamethizole Renal Oral 0.5-1g every

6-8hrs
 Tetracycline's

 These broad spectrum agents are effective against certain

bacterial strains that resist other antibiotics.

 These drugs are preferred only in few situations.

 The major drugs are democlocycline(declomycin),

doxycycline (vibramycin), minocycline (minocin), and
oxytetracyclin (terramycin).

 MOA: these are bacteriostatic they inhibit bacterial protein

synthesis by binding to 30 S ribosomal subunits.
 Spectrum of activity:

 These are active against gram positive and gram negative

organisms spirochetes, rickettsial species and certain
protozoa.

 Therapeutic uses:

 These are agents of choice in rickettsial (rocky mountain

spotted fever), chlamidial and mycoplasmal infections,
amebiasis and bacillary infections.

 Tetracycline's are useful alternatives of penicillin's in

treatment of anthrax, syphilis, gonorrhea, Lyme disease and
 H.influenzae respiratory infections.
 Oral or topical tetracycline's may be administered as a
treatment of acne.
 Doxycycline is highly effective in prophylaxis of traveler’s
diarrhea.
 Demeclocycline is used commonly as an adjunctive agent to
treat the syndrome of inappropriate antidiuretic hormone
secretion (SIADH).
 GI distress is common in adverse effects of tetracyclines. This
problem can be minimized by administering the drug with
food or temporarily reducing the dose.
 Phototoxic reactions may develop with exposure to sunlight.
This reaction is common with demoxycycline and
doxycycline.

 Tetracycline's may cause hepatotoxicity particularly in

pregnant women.

 Renally impaired patients may experience increased BUN

levels.

 Tetracycline's may induce permanent tooth discoloration, tooth

enamel effects and retarded bone growth in infants and
children.
 IV tetracyclines are irritating and may cause phlebitis.

Agent Eliminatio Half-life ROA Dosage

n route

Demeclocyclin Renal 10-17hrs Oral 300mg-1g/day

e

Doxycycline Hepatic 14-25hrs Oral,IV 100-200mg

every 12 hrs

Minocycline Heptic 12-15hrs Oral, IV 100-200mg

every 12 hrs

Oxytetracycline Renal 6-12 hrs Oral, 200-500mg

IM every 6hrs
 Fluoroquinolines
 These agents include ciprofloxacin, norfloxicin, ofloxicin,
moxifloxicin, levofloxicin and gemifloxicin.
 MOA: these inhibit DNA gyrase.
 Spectrum of activity: these are highly active against enteric
gram negative bacilli, salmonella, shigella, campylobacter,
haemophilus and neisseria.
 Ciprofloxacin has an activity against P. aeruginosa and
some anaerobes.
 It has moderate activity against M.tuberculosis
 Gram positive organisms are less susceptible than gram
negative but usually are sensitive.

 Therapeutic uses:

 Norfloxicin is indicated for the oral treatment of UTI,

uncomplicated gonococcal infections and prostatitis.

 Ciprofloxacin, ofloxicin and levofloxicin are available orally

and intravenously.

 Ciprofloxacin is approved in use of UTI, LRTI, sinusitis,

bone, joint and skin structure infections, typhoid fever,
urethral and cervical gonococcal infections and diarrhea.
 Ofloxicin approved for use in LRTI, uncomplicated
gonococcal and chlamydial cervicitis and urethritis,
prostatitis and UTI.
 Levofloxicin is approved for treatment for UTI,
gemifloxicin, moxifloxicin and levofloxicin are also used in
lower respiratory tract infections and available orally.
 Moxifloxicin is approved for treatment of complicated intra
abdominal infections but should not be used for UTI’s.
 Precautions and monitoring:
 Occasional adverse effects include nausea, dyspepsia,
headache, dizziness, insomnia, photosensitivity.
 Infrequent adverse effects include rash, urticaria, leucopenia
and elevated liver enzymes, crystalluria occurs with high doses
at alkaline PH.
Agent Eliminatio Half-life ROA Dosage
n route
Ciprofloxicin Renal 5-6hrs IV 200-600mg
every 12hrs

Gemifloxicin Fecal 4-12hrs Oral 320mg once

daily

Levofloxicin Renal 8hrs IV, Oral 250-500mg

every 24hrs

Moxiflyg/doxi Hepatic 12hrs Oral 400mg

 Miscellaneous agents

1. Aztreonam:

• This agent was the first commercially available monobactam.

• It resembles the amino glycosides in its efficacy against

many gram negative organisms but does not cause
nephrotoxicity or ototoxicity.

• MOA: Aztreonam is bactericidal, it inhibits bacterial cell

wall synthesis.

• Spectrum of activity: This drug is active against many gram

negative organisms, including Enterobacter
 Therapeutic uses:

 It is used for UTI infections, septicemia, skin infections, lower

respiratory infections.

 Precautions and monitoring:

 It sometimes causes, nausea, vomiting and diarrhea.

 This drug may include skin rash.

Agent Elimination Half- ROA Dosage

route life
Aztreonam Renal 1.7hrs Oral, IV 50-100mg/kg/day
 Chloram phenicol:

 It is a nitrobenzene derivative, this drug has broad activity

against rickettsia as well as many gram negative organisms.

 It is also effective against many ampicillin-resistant strains of

H. inluenzae.

 MOA: it is bacterial bacteriostatic, sometimes it may be

bactericidal against a few bacterial strains.

 Spectrum of activity: it is active against rickettsia and wide

range of bacteria, including H. influenza, salmonella typhi,
neisseria meningitis.
 Therapeutic uses:

 It can be used only to suppress infections that cannot be

treated effectively with other antibiotics.

 It is used for typhoid, meningococcal infections in

cephalosporin allergic patients and anaerobic infections.

 Rickettesial infections in pregnant patients, tetracycline

allergic patients and renally impaired patients.

 Precautions and monitoring:

 It can cause bone marrow suppression with resulting

pancytopenia rarely the drug leads to a plastic anemia.
 Hypersensitivity reactions may occur.
 This drug therapy may leads to grey baby syndrome.
 Clindamycin
 This agent has essentially replaced lincomycin, the drug from
which it is derived.
 MOA: it is bacteriostatic. It binds to ribosomal subunit.
 Spectrum of activity: this agent is active against most gram
positive and many anaerobic agents.
 Therapeutic uses: it is used for abdominal and female
genitourinary tract infections.
 Precautions and monitoring effects:

 Clindamycin may cause rash, nausea, vomiting, diarrhea,

fever, abdominal pain and bloody stools. Blood dyscrasias
may occur.

Agent Elimination Half-life ROA Dosage

route
Clindamycin Hepatic 2-4hrs Oral, 300-900mg
IV,IM every 6-8hrs
 Dapsone:

 A member of sulfone class this drug is primary agent in

treatment of all forms of leprosy.

 MOA: it is bateriostatic for mycobacterium leprae, its

mechanism is resembles the sulfonamides.

 Spectrum of activity: this drug is active against M.leprae.

 It also has same activity against Pneumocystis.carinil organisms

and malarial parasite plasmodium.

 Therapeutic uses:

 It is a drug of choice for treating leprosy.

 This agent is also used in dermatitis herpetiformis (skin disorder).

 Precautions and monitoring:

 Hemolytic anemia may occur with daily doses> 200mg.

 Nausea, vomiting and anorexia may develop.

 Adverse CNS effects include headache, dizziness, nervousness, lethargy

and psychosis.

 Other adverse effects includes skin rash, peripheral neuropathy, blurred

vision, hepatitis etc.,

Agent Elimination Half-life ROA Dosage

route
Dapsone Hepatic 28hrs Oral 50-100mg/day
 Clofazimine:

 It is a phenazine dye with antimicrobial and anti inflammatory

activity.

 MOA: it appears to bind preferentially to mycobacterial DNA,

inhibiting replication and growth.

 It is bactericidal against M.leprae.

 It is active against various mycobacteria, M.leprae,

M.tuberculosis.

 Clofazimine is used to treat leprosy and variety of

mycobacterium infections.
 Pigmentation may occur in 75%to 100% patients within few
weeks.. This skin discoloration may lead to severe
depression(suicide).

 Urine sweat and other body fluids may be discolored.

Agent Elimination Half-life ROA Dosage

route
Clofazimine Hepatic 70 days Oral 50-100mg/day
 Rifaximin :
 It is semi synthetic antibiotic structurally related to rifamycin.
 MOA: it inhibits bacterial RNA synthesis by binding to the
β subunit of bacterial DNA dependent RNA polymerase.
 This is non systematically absorbed drug has activity against
both enterotoxigenic strains of E.coli.
 Therapeutic uses: it is used in treatment of travelers diarrhea
and noninvasive strains of E.coli and prophylaxis of hepatic
encephalopathy.
 High resistant rates have been reported after 5 days of
treatment.
 Precautions and monitoring:

 Because of its limited systemic absorption adverse effects are

few but include constipation vomiting and headache.

Agent Eliminati Half-life ROA Dosage

on route
Rifaximin Fecal 6hrs Oral 200mg
t.i.d
 Trimethroprim:

 A substituted pyrimidine trimetroprim is most commonly

combined with sulfamethaxazole in preparation called co-
trimoxazole.

 MOA: it inhibits the dihydrofoliate reductase thus blocking

bacterial synthesis of folic acid.

 Spectrum of activity:

 It is active against most gram negative and gram positive

organisms

 Trimethroprim-sulfamethaxazole are active against a variety of

 Organisms like S. pneumoniae, N. meningitis and
cornybacterium diptheriae.
 Therapeutic uses:
 It may be used alone or in combination with
sulfamethaxazole to treat UTI, klebsiella and enterobacter
organisms.
 The combination therapy is effective for gonococcal urethritis,
chronic bronchitis and salmonella infections.
 Precautions and Monitoring:
 Most adverse effects involve the skin like rash, pruritis and
exfoliate dermatitis.
 The combination therapy causes blood dyscrasias.

 Adverse GI effects nausea, vomiting and epigastric distress.

 Patients with AIDS may suffer with fever, rash, malaise and
pancytopenia.

Agent Elimination Half-life ROA Dosage

route
Trimethoprim Renal 8-15hrs Oral 100-
200mg/day
 Metronidazole:
 It is used in treatment of amebiasis, giardiasis and
trichomoniasis.
 MOA: it is a synthetic compound with amebicidal and
trichomonacidal action. its mechanism of action involves
disruption of helical structure of DNA.
 Spectrum of activity& therapeutic uses:
 This is prefered drug in amebic dysentary, giardiasis and
trichomoniasis.
 These are also active against all anaerobic cocci and gram
negative anaerobic bacilli.
 Precautions and monitoring:

 The most common adverse effect of this drug is

nausea, epigastric distress.

 It is carcinogenic in mice and should not be used

unnecessarily.

 Headache, vomiting, metallic taste and stomatitis have

been reported.

Agent Elimination Half-life ROA Dosage

route
Metronidazol Hepatic 1-1.6hrs Oral, IV 250-500mg every 6-
e 8hrs