Vancomycin, Quinolones,

Tetracyclines, Aminoglycosides,
Macrolides, Chloramphenicol,
Clindamycin
Jillianne Pardo, M.D.

Objectives
To

discuss
the
mechanism
of
action,
indications, dosing, pharmacokinetics and,
pharmacodynamics of the following antimicrobial
drug classes:
Vancomycin
Quinolones
Tetracycline
Aminoglycosides
Macrolides
Chloramphenicol

Vancomycin
GLYCOPEPTIDE ANTIBIOTICS

Vancomycin
Tricyclic glycopeptide
Produced by Streptococcus orientalis

and Amycolatopsis orientalis

Mechanism of
Action

Pharmacokinetics
Absorption

Distribution

Metabolism

Poorly absorbed Widely

Minimal
from
the
distributed in the
metabolism
intestinal tract
body
CSF levels: 7-30%
with meningeal
irritation

Excretion

Mostly excreted in
the urine (90%)

Pharmacokinetics
Drug

Half-Life (h) Bioavailability Peak Serum

(%)

Concentration

Dose (g)

(mcg/mL)

Vancomycin

5-11 adults Negligible

2-4 children oral
bioavailability

15-30

Primary

Route of

Excretion

~1-2

Renal

Antibacterial Activity
Drug
Vancomycin

Spectrum of Activity
Bactericidal.
Active against most
gram positive
pathogens
No activity against
gram negatives except
flavobacterium

Staphylococcus
(MRSA)
Streptococcus
pneumoniae
Listeria
Enterococcus
Bacillus
Corynebacterium
Clostridium difficile

Resistance
Modification of D-Ala-A-Ala binding

site of peptidoglycan
Altered cell wall metabolism in VRSA

thickened cell wall w/ increased

number of D-Ala-D-Ala residues

Clinical Uses:
Vancomycin
Preparation

Neonate

0.5, 0.75, 1, 5, 10 gram IV

preparations
Postmenstrual Age
<29
30-36
37-44

Bacteremia: 10 mkdose
Meningitis: 15 mkdose

Postnatal Age

Dosage Interval (hr)

0-14

18

>14

12

0-14

12

>14

0-7

12

>7

Clinical Uses:
Vancomycin
Age

General Dosage CNS Infections,

Endocarditis,
Ostemyelitis, Pneumonia,
MRSA bacteremia

1mo 12
yrs

15mg/kg Q6

20 mg/kg Q6 hr

Adolescent 15mg/kg Q6Q8

20 mg/kg Q6-8 hr

Adult

20 mg/kg Q8-12 hr

15mg/kg Q8-

Clinical Uses:
Vancomycin
Indication

Pediatric Dose Adult Dose

Endocarditis prophylaxis
for GU or GI procedures
Moderate-risk patients
allergic to ampicillin or
amoxicillin:

20 mg/kg/dose
IV over 1-2 hrs

1 g/dose IV over
1-2 hrs

High risk patients allergic Same as above + gentamicin

to ampicillin or amoxicillin 1.5mkdose for high-risk patients

Clinical Uses:
Vancomycin
Preparation

Pseudomembranous colitis

25mg/ml oral
solution
125, 250 mg
capsule

Child: 40-50 mkD q6 PO x 7-10 days (Max:

500mg/24h to 2g/24hr)
Adult: 125mg/dose q6 PO x 7-10

Adverse Drug
Reactions
Fever, chills, phlebitis at IV site
Flushing (red man syndrome) and shock

due to histamine release due to rapid

infusion
Dose-related hearing loss
Ototoxicity, nephrotoxicity when used with

drugs which cause the same reactions

Drug Interactions
Synergistic

with gentamicin and

streptomycin against E. faecium and
E. faecalis

Quinolones

Classification of
Quinolones
Classified

by
generation
based
antimicrobial spectrum of activity

on

1st generation (quinolones): Nalidixic acid

Fluoroquinolones
2nd gen: Norfloxacin, Ciprofloxacin, Ofloxacin
3rd gen: Levofloxacin, Moxifloxacin, Gemifloxacin,

Gatifloxacin, Spafloxacin
4th gen: Trovafloxacin

Mechanism of Action

Inhibits bacterial DNA replication

by binding to the topoisomerases
of the target pathogen, inhibiting
bacterial enzyme DNA gyrase

Pharmacokinetics
Absorption

Distribution

Metabolism

Excretion

Good
oral Widely distributed Converted to active Mostly renal (active
bioavailability (80in body fluids and
and
inactive
tubular secretion)
95%)
tissues (including in
metabolites
Moxifloxacin

CSF
and
bile)
Impaired by di- and
partly
hepatic
trivalent
cations Crosses
placenta,
metabolism
and
(e.g. antacids)
and enters breast
biliary excretion
milk

Pharmacokinetics
Drug

Half-Life (h)

Oral

Peak Serum

Oral Dose (mg) Primary Route

Bioavailability Concentration
(%)

(mcg/mL)

of Excretion

Ciprofloxacin

35

70

2.4

500

Renal

Gatifloxacin

98

3.4

400

Renal

Gemifloxacin

70

1.6

320

Renal &
nonrenal

Levofloxacin

57

95

5.7

500

Renal

Moxifloxacin

910

> 85

3.1

400

Nonrenal

Norfloxacin

3.55

80

1.5

400

Renal

Ofloxacin

57

95

2.9

400

Renal

Antibacterial Activity
1st gen
Nalidixic acid

Spectrum of Activity
Gram negative except
pseudomans

2nd gen
Norfloxacin

Least active against both

gram (+) and gram (-)
among fluorquinolones

Antibacterial Activity
2nd gen
Ciprofloxacin,
Enoxacin,
Ofloxacin
Lomefloxacin,
Pefloxacin

Spectrum of Activity
Excellent gram (-)
activity
Moderate to good
gram (+) coverage
Covers some
atypical
organisms

Enterobacter
Pseudomonas
Neisseria
Haemophilus
Camplyobacter
Methicillin-susceptible
S.aureus
Mycoplasma pneumonia
Ciprofloxacin: Most active against gram negative among fluoroquinolones (esp.
Chlamydia pneumoniae
Pseudomonas aeruginosa)

Antibacterial Activity
3rd gen

Spectrum of Activity

Levofloxacin
Gatifloxacin
Gemifloxacin
Moxifloxacin

Excellent gram (-)

activity
Improved activity
against gram (+)
organisms
Coverage of atypical
organixms

Gram negative
organisms
S. Pneumonia
Staphylococci

Mycoplasma
chlamydia
Legionella
species
Moxifloxacin modest activity against anaerobes;
poor
activity
Mycobacteria
against Pseudomonas

Antibacterial Activity
4th gen
Trovafloxacin

Spectrum of Activity
Excellent gram (-)
activity
Improved activity
against gram (+)
organisms
Coverage of atypical
organisms
Broad anaerobic
coverage

Gram negative
organisms
Anaerobes
S. Pneumonia
Staphylococci
Mycoplasma
chlamydia
Legionella species

Summary of Antibacterial Activity

Resistance
Resistant organisms emerge about once in 10 7 to 109

(esp. among
serratia)

staphylococci,

pseudomonas

and

May be due to:

One or more point mutations in the quinolone

binding region of the target enzyme

Change in the permeability of the organism
Due to efflux pump production or changes in porin structure
Seen in M. tuberculosis, S. aureus, and S. pneumonia

Resistance
Plasmid-mediated resistance:
Utilizes Qnr proteins, which protect DNA gyrase from

the fluoroquinolones
Variant of an aminoglycoside acetyltransferase

capable of modifying ciprofloxacin

Confer low-level resistance that may facilitate the

point mutations that confer high-level resistance.

Resistance to one fluoroquinolone, particularly if

it is of high level, generally confers crossresistance to all other members of this class.

Clinical Uses:
Ciprofloxacin
Preparation
Immediate-release
tablets: 100, 250,
500, 750mg

Pediatric Dosage

Adult Dosage

Urogenital tract infections (E.coli, Klebsiella, Pseudomonas)

Bacterial diarrhea
(shigella, salmonella, ETEC, campylobacter), Soft tissue, bone, joint
infections, Respiratory tract infections

Extended-release
tables: 500, 1000mg
Oral suspension:
250mg/5ml,
500mg/5ml
Injection: 10mg/ml
Premixed injection:
200mg/100ml,

PO: 20-30 mg/kg/day x q12

Max: 1.5g/24h
IV: 20-30 mg/kg/day x q12
Max: 800mg/24h

PO: Immediate- release: 250750mg/dose q12

Extended-release:
500mg/dose q24
IV: 200 400mg/dose q12

Clinical Uses:
Ciprofloxacin
Preparation
Immediate-release
tablets: 100, 250, 500,
750mg
Extended-release tables:
500, 1000mg
Oral suspension:
250mg/5ml, 500mg/5ml
Injection: 10mg/ml
Premixed injection:

Pediatric Dosage

Adult Dosage

Complicated UTI or pyelonephritis

PO: 20-40 mg/kg/day

PO: 1000 mg/dose q24h
x q12 Max: 1.5g/24h

IV: 18-30 mg/kg/day

x q8 Max:1.2g/24h
Treat for 10-21 days

IV: 400mg/dose q8 for

severe infections

Clinical Uses:
Ciprofloxacin
Indication

Pediatric Dosage

Adult Dosage

Acute otitis externa

(Ciprofloxacin otic drops)

2-3 drops to affected ear BID x 7 days

Acute otitis media

(Ciprofloxacin +
dexamethasone otic
drops)

4 drops to affected ear BID x 7 days

Bacterial conjunctivitis
(Ciprofloxaxin ophthalmic
drops 3.5mg/ml
and ointment 3.3mg/g)

Drops: 1-2 drops q2 while awake for 2 days then 1-2

drops q4 while awake for 5 days
Ointment: Apply 0.5 in ribbon TID 2 days then BID
x 5 days

Clinical Uses:
Levofloxacin
Preparation
Tablets: 250, 500,
750mg
Oral solution:
25mg/ml
Injection: 25mg/ml

Pediatric Dosage

Adult Dosage

Recurrent AOM, CAP, complicated and uncomplicated UTI,

uncomplicated skin infection

<5 yrs: 8-10mkdose IV/PO

q12 Max: 500mg/24h
>5 yrs: 8-1010mkdose IV/PO
q24 Max: 500mg/24h
In recurrent AOM, treat for 10
days
For CAP, max dose:
750mg/24h

CAP: 500 mg PO/IV Q24 hr 714

days; or 750 mg PO/IV Q24 hr 5
days
Complicated UTI/acute
pyelonephritis: 250 PO/IV Q24 hr
10 days; or 750 mg PO/IV Q24 hr 5
days
Uncomplicated UTI: 250 mg PO/IV
Q24 hr 3 days
Uncomplicated skin/skin structure
infection: 500 mg PO/IV Q24 hr 7
10 days
Acute bacterial sinusitis: 500 mg

Adverse Drug
Reactions
GI upset, headache , restlessness, rash, dizzines
Peripheral neuropathy
Renal failure, seizures
QTc interval prolongation gatifloxacin,

levofloxacin, gemifloxacin, moxifloxacin

Reversible arthropathy, damage to growing

cartilage (caution I < 18 yrs age)

Tendon rupture

Drug Interactions
CYP 450 1A2 inhibitor
Increase effects of caffeine, MTX, theophylline,

warfarin, cyclosporine

Levels increased by probenecid

Decreased absorption when taken with

antacids or other divalent salts

TETRACYCLINE

Tetracyclines
Closely related compounds consisting

of four fused ring with a system of

conjugated double bonds
Substitutions

are
responsible
for
individual variations in pharmacokinetics

Mechanism of Action

Pharmacokinetics
Absorption

Distribution

Metabolism

Excretion

Adequately
Converted
but Widely
to Mostly excreted bile
incompletely
distributed except
active metabolites (10-50% in feces )
and urine (10-40%)
absorbed orally
to CSF
in the liver
Except Doxycycline
Dairy
food Penetrates
and tigecycline
decrease
abscesses
absorption
through chelation

Antibacterial Activity
Drug

Spectrum of Activity

Tetracyclines Broad-spectrum

bacteriostatic
Gram positive and
gram
negative
bacteria
Anaerobes, rickettsiae,
chlamydiae,
mycoplasmas, protozoa

Clinical Uses of Tetracyclines

Resistance
Impaired influx or increased efflux by an active

transport protein
Mg2+-dependent)

pump

(plasmid

encoded,

Enzymatic inactivation
Production of bacterial proteins that prevent

tetracyclines from binding to the ribosome

Any organism resistant to one tetracycline is

resistant to all

Clinical Uses:
Doxycycline
Preparation
capsule
50, 75, 100, 150 mg
Powder for
injection
100mg
Syrup
50mg/5mL

Neonate
<8 years: Not
recommended;
may cause tooth
discoloration and
enamel hypoplasia
during tooth
development

Child
>8 years, <45 Kg
Load: 4.4 mg/kg/day PO/IV
divided q12hr day 1
Maintenance: 2.2-4.4
mg/kg/day IV/PO qDay (may
divide BID for higher doses)
>8 years, >45 kg
100 mg PO q12hr or 50 mg
PO q6hr on day 1, followed by
maintenance dose of 100
mg/day as single dose or as 50

Clinical Uses:
Doxycycline
Preparation

Adult

50, 75, 100, 150 mg

Initial: 200 mg/day divided twice daily

PO/IV on first day (IV may be given OD)

Powder for injection

THEN

capsule

100mg

Maintenance: 100-200 mg/day qDay or

divided q12hr PO/IV (IV may be given
qDay)

Adverse Drug
Reactions
GI effects: Nausea, vomiting, and diarrhea are the

most common
Dental: can be deposited in the fetal teeth, leading

to fluorescence, discoloration, and enamel dysplasia

Hepatic and renal injury
Deposits in bone causing temporary stunting
Phototoxicity, pseudotumor cerebri

Drug Interactions
Aluminum, calcium, magnesium,

zinc, iron containing products

decrease absorption through
chelation
Carbamazepine, rifampin,

barbiturates decrease half-life

AMINOGLYCOSIDES

Aminoglycosides
Derived from Streptomyces (-mycin)

or Micromonospora (-micin)
Polycationic precludes easy

passage across tissue membranes

Mechanism of Action

Pharmacokinetics
Absorption
Absorbed
very
poorly from the
GIT
Usually
administered TIV
as a 30- to 60minute infusion

Distribution

Do not enter cells

readily
Excluded from the
central nervous
system and the eye
In active
inflammation, CSF
levels reach 20% of
plasma levels

Metabolism

Excretion

Cleared
by
the
Excreted
unchanged in the kidney
excretion is directly
urine

proportional
to
creatinine clearance

Resistance
Impaired entry of aminoglycoside into the cell
Plasmid-associated

production
of
a
transferase enzyme or enzymes inactivates
the aminoglycoside

Receptor

protein on the 30S ribosomal

subunit may be deleted or altered as a result
of a mutation.

Antibacterial Activity
Drug

Spectrum of Activity

Aminoglycoside Active against aerobic E. coli, Klebsiella,

gram negative bacilli Proteus sp.
with synergistic actions
with beta lactamase
no
activity
anaerobes

against

Clinical Uses:
Gentamicin
Preparation
Injectable solution
10mg/ml
40mg/ml
80mg/2ml

Neonate
<30 weeks gestation
0-28 days: 2.5 mg/kg/day
IV/IM
>28 days: 3 mg/kg/day
IV/IM
30-36 weeks gestation
0-14 days: 3 mg/kg/day
IV/IM
>14 days: 5 mg/kg/day
IV/IM divided q12hr
>36 weeks gestation
0-7 days: 5 mg/kg/day IV/IM

Child
5 years: 2-2.5
mg/kg/dose IV/IM q8hr
<5 years: 2.5 mg/kg/dose
IV/IM q8hr

Clinical Uses:
Gentamicin
Preparation
Injectable solution
10mg/ml
40mg/ml

Adult
Conventional dosing
3-5 mg/kg/day IV/IM divided q8hr
Extended dosing interval (q24h+)
Initial: 4-7 mg/kg/dose IV qDay

Clinical Uses: Amikacin

Preparation
Injectable solution
50mg/mL
250mg/mL
100mg/2ml
250mg/2ml
500mg/2ml

Neonate
Aged 7 days
29 weeks gestational age: 18 mg/kg IV/IM q48hr
30-33 weeks gestational age: 18 mg/kg IV/IM q36hr
34 weeks gestational age: 15 mg/kg IV/IM q24hr
Aged >7 days
30-33 weeks gestational age: 15 mg/kg IV/IM q24hr
34 weeks gestational age: 15 mg/kg IV/IM q1218hr
Aged 8-28 days old & <29 weeks gestational

Clinical Uses: Amikacin

Preparation
Injectable solution
50mg/mL
250mg/mL
100mg/2ml
250mg/2ml
500mg/2ml

Child

Adult

15-22.5 mg/kg/day 15 mg/kg/day divided

IV/IM divided q8hr IV/IM q8-12hr

Clinical Uses:
Streptomycin
Preparation

Child

Adult

Injectable solution

Tuberculosis: Daily
therapy: 20-40 mg/kg IM
qDay; no more than 1 g/day
Twice weekly therapy: 2040 mg/kg IM 2 times/week;
no more than 1.5 g/day

Tuberculosis: Daily therapy: 15

mg/kg IM qDay; no more than 1
g/day
Twice weekly therapy: 25-30
mg/kg IM 2 times/week; no more
than 1.5 g/day

powder for injection

1g
injectable solution
400mg/mL

Adverse Drug
Reactions
Ototoxicity
irreversible, manifests itself mainly as

vestibular dysfunction

Nephrotoxicity (5-25%)
usually reversible and mild
patients receiving gentamicin for longer than

35 days

Drug Interactions
Synergize with B-lactams since these

drugs act on cell wall synthesis

thereby
enhancing
diffusion
of
aminoglycosides into the bacterium
Additional nephrotoxicity with other

nephrotoxic drugs

Chloramphenicol

Mechanism of Action

Pharmacokinetics
Absorption

Distribution

Metabolism

Excretion

Good
oral Widely distributed Inactivated
by Mostly excreted in
bioavailability
in
the
body
conjugation
w/
the urine (15%) and
(80%); Lipophilic
including the CNS
glucoronic acid
feces (4%)
and CSF
Rapidly
Reduction
and
to
completely absorbed Concentration
in
inactive aryl amines
brain tissue may be
equal to serum

Pharmacokinetics
Drug

Half-Life (h) Bioavailability Peak Serum

(%)

Dose (mg)

Concentration

Primary Route
of Excretion

(mcg/mL)

Chloramphenicol 1.5-3

80

10-15

10-50
mg/kg/day

Renal and Bile

Antibacterial Activity
Drug
Chloramphenicol

Spectrum of Activity
Broad spectrum
Active against both
aerobic and
anaerobic grampositive and gram
negative
organisms

Salmonella
Streptococcus
Hemophilus
Neisseria
Bacteroides
Mycoplasma
Rickettsia

Resistance
Plasmid mediated resistance:

chloramphenicol acetyltransferase
inactivates chloramphenicol
Changes in permeability of organism

Clinical Uses: Chloramphenicol

Preparation

Neonate Dosage

Infant/Child/Adult
Dosage

1g vial

Susceptible infections including meningitis

IV: LD: 20mg/kg;
MD:
< 7 days: 25 mkD q24
> 7 days:
<2 kg: 25mkD q24
> 2kg:50mkD q12

IV: 50-75 mkD q6

Meningitic dose: 75100mkD q6
Max dose: 4g/24h

Adverse Drug
Reactions
GI upset, Candida overgrowth, bone marrow

suppression, aplastic anemia

Hemolytic anemia in patients w/ G6PD

deficiency
Gray baby syndrome
Low capacity of neonates to glucoronylate the

antibiotic
Underdeveloped renal function

Drug Interactions
CYP P450 inhibitor
Increases the concentrations of drugs such as

warfarin, tolbutamide, phenytoin,

chlorpropramide

Bacteriostatic inhibitor of microbial

protein synthesis antagonizes

bactericidal drugs

Macrolides

Macrolides
Prototype Dug: Erythromycin
Other macrolides:
Azithromycin, Clarithromycin

Mechanism of Action

Pharmacokinetics
Absorption

Distribution

Metabolism

Excretion

Generally
well- Widely distributed Converted to active Mostly excreted in
tolerated
and
except to the brain
metabolite
(except
the bile and lost in
absorbed orally
and CSF
erythromycin)
feces, and only 5% is
Food interferes with Erythromycin is
excreted in the urine
absorption
noted to traverse the
Clarithromycin

placenta and reach

renal excretion
the fetus

Pharmacokinetics
Drug

Oral

Peak Serum Oral Dose

Primary

ty (%)

n (mcg/mL)

Excretion

35

0.4

250-500

Fecal and
Renal (5%)

Clarithromycin 6

50

2-3

250-500

Renal

Erythromycin

1.5

30-40

250-500

Fecal and
Renal (5%)

Telithromycin
(Ketolide)

10

57

800

Fecal and
Renal

Azithromycin

Half-Life
(h)

70

Bioavailabili Concentratio (mg)

Route of

Antibacterial Activity
Drug
Azithromycin
Clarithromycin
Erythromycin
(Telithromycin)

Spectrum of Activity
S. aureus, streptococcus
Corynebacteria
aerobic
Gram
Clarithromycin more active against
Mycobacterium
aviumand
complexH. influenzae
positive cocci
Mycoplasma,
Legionella,
Also has activity against M. leprae
and Toxplasma
bacilli and
gondii
C.trachomatis
C. Psittaci
Azithromycin
again M. avium complex and T.
Some gramactive
negative
Neisseria, Bordetella
gondii, less active than clarithromycin and
organisms
pertussis,
Bartonella
erythromycin against staphylococci
and streptococci
henselae, and B
Slight more active against H. influenza
Highly active against chlamydia
quintana some

Active against

Resistance
Plasmid-mediated
Reduced permeability of the cell membrane or active

efflux
Production of esterases that hydrolyze macrolides

(Enterobacteriaceae)
modification of the ribosomal binding site (ribosomal

protection) by chromosomal mutation or

macrolide-inducible or constitutive methylase

Cross-resistance between macrolides

by

Clinical Uses:
Clarithromycin
Indication

Infant/Child

Adolescent/adult

Acute Otitis media,

pharyngitis,
pneumonia, acute
maxillary sinusitis,
uncomplicated skin
infections

15mkD q12 PO
(Max 1g/24h)

250-500 mg/dose
q12 PO

H. Pylori infection

XR: 1000 mg q24

PO
250 mg q12 to 500
mg q8 w/ other
meds

Clinical Uses:
Erythromycin
Preparation

Neonate

Child

Adolescent/adult

Erythromycin
base: Tab: 250,
500

(EES prep)
<1.2 kg 20mkD q12

(Base or EES
prep)

Pertussis: 1-4 g/24

hr q6

Erythromycin
succinate (EES):
100mg/2.5 ml
200mg/5 ml
400mg/5 ml
Erythromycin
stearate tab 250

> 1.2 kg
30-50 mkD q60-7 days: 20mkD q12
q8
>7 d: 30-40 mkD q6q8
Pertussis: 40-50
mkD q6 PO x 14
Chlamydial
days
conjunctivitis or
pneumonia:
50mkD q6 x 14 days

Clinical Uses:
Erythromycin
Preparation

Child

Adolescent/adult

RF prophylaxis: 500 mg/24hrs q12 PO

Erythromycin
lactobionate

20-50 mkD q6 TIV

500, 1000mg
Ophthalmic

0.5 in ribbon to
affected eye BID-QID

15-20 mkD q6 TIV

Clinical Uses:
Azithromycin
Preparation

Tablet:
250, 500, 600 mg
Oral suspension:
100mg/5ml,
200mg/5ml
Inj:
500mg

Infant

Child

Otitis media/CAP/Pertussis
5 day regimen: 10mkD PO OD on Day
1 then 5 mkD PO OD on D2-5

Adolescent/adult

5 day regimen:
500 mg OD Day 1
then 250 mg OD
Day 2-5

3 day regimen: 10mkD PO OD x 3 days

1 day regimen:
30mkD PO single dose (Max 1500mg)

3 day regimen:
500 mg OD x 3
days

Adverse Drug
Reactions
GI intolerance
Acute

cholestatic
erythromycin estolate

hepatitis

Fever, eosinophilia, rashes

QT

prolongation,
arrythmias

ventricular

Drug Interactions
Erythromycin CYP 450 inhibitor
Increases concentration of several drugs

(theophylline, warfarin, cyclosporine,

methylprednisolone)
Increases serum concentration of digoxin by

increasing bioavailability

Antacids delay absorption and reduce peak

absorption

CLINDAMYCIN
LINCOSAMIDE

Clindamycin
Chlorine-substituted

derivative of
lincomycin, which is elaborated by
Streptomyces lincolnensis

Mechanism of Action

Pharmacokinetics
Absorption

Distribution

Metabolism

Excretion

Good
oral Widely
distributed Converted to active Mostly excreted in
bioavailability (90%)
except to the brain
metabolites in the
the urine (10%) as
and CSF
liver
active drug bile and
Penetrates abscesses
feces (4%)
Actively taken up and
concentrated by
phagocytic cells

Pharmacokinetics
Drug

Half-Life (h)

Oral

Peak Serum

Oral Dose (mg) Primary Route

Bioavailability Concentration

Clindamycin

2-3

(%)

(mcg/mL)

90

2-3

of Excretion

150-300

Fecal and
Renal (5%)

Antibacterial Activity
Drug
Clindamycin

Spectrum of Activity
Active against
aerobic and
anaerobic gram
positive cocci,
Some anaerobic
gram negative
bacilli and
protozoans

Staphylococcus
Streptococcus
Pneumococcus
Chlamydia
Bacteroides, other
anaerobes
Gardnerella

Clinical Uses:
Clindamycin
Preparation
75, 150, 300 mg
capsule
75mg/5ml oral
solution
150mg/ml
injection

Neonate

Child

5 mg/kg/dose
< 7 days:
< 2kg: Q12 hr
> 2 kg: Q8

PO: 10-30 mkD q6-q8

> 7 days:
< 1.2 kg: q12hr
1.2-2 kg: q8hr
>2 kg q6hr

Bacterial endocarditis:
20mg/kg (Max: 600 mg)
1 hr before procedure
(PO)

(Max: 1.8g/24 hr)

IM/IV: 25-40 mkD q6-q8
(Max: 4.8g/24hr)

Clinical Uses:
Clindamycin
Preparation

Adult

75, 150, 300 mg capsule

75mg/5ml oral solution
150mg/ml injection

PO: 150-450 mg/dose q6-8 hr (Max:

1.8g/24h)
IM/IV: 1200-1800 mg/24hr IM/IV q6-q12
(Max: 4.8g/24h)
Bacterial endocarditis: 600 mg PO/IV
1 hr prior to procedure (PO)
30 mins prior to procedure (IV)

Topical cream, gel

Apply to affected area BID

Adverse Drug
Reactions
Diarrhea, nausea, skin rashes
Impaired liver function and

neutropenia
Clostridum difficile

pseudomembranous colitis

THANK YOU!