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DRUGS used to

TREAT/PREVENT
Infection - is the successful
establishment and growth of
microorganism in the tissues of the
host
> treated by:
A. surgical procedures
B. dressing changes
C. ANTIMICROBIAL DRUGS
Classification of Microorganisms:
group of microorganisms, invade
the human host through many routes (respi,
GI, skin…)
:aerobic - require oxygen
:anaerobic - cannot live in the presence of oxygen
: Gram POSITIVE- those whose cell wall

with alcohol during culture and sensitivity


testing.
:Gram-positive bacteria will retain the
crystal violet dye when washed in a 
decolorizing solution. 
Gram NEGATIVE- whose cell wall loose a
stain or are decolorized by alcohol
Gram-negative bacteria are bacteria that do 
not retain crystal violet dye, when  a 
counterstain (safranin) is added after the crystal 
violet, coloring all Gram-negative bacteria with a 
red or pink color - outer membrane preventing 
the penetration of the stain. 
Compared with Gram-positive bacteria, Gram-negative
bacteria are more resistant against antibodies, because
of their impenetrable wall.
- intracellular parasites
that survive only in living tissues.
Eg. adenoviruses, herpesviruses, and
retroviruses
- plant-like organisms that
live as parasites on living tissue or
as saprophytes on decaying organic
matter.
Normal flora -protects the
human host by occupying
space and consuming nutrients.
This interferes with the ability
of potential pathogens to
establish residence and
proliferate.
: bacteria is
sensitive – inhibited or Resistant
destroyed by antibacterials
: bacteria is
microorganisms - grow
resistant – continue to and multiply when
grow instead ======
susceptible organisms (eg,
RESISTANCE TO normal flora) are
ANTIBACTERIALS
suppressed by
antimicrobial drugs or
CROSS RESISTANCE-
occurs between drugs that
when normal body
has similar actions (eg. defenses are impaired by
penicillins and
cephalosporins). immunosuppressive
disorders or drugs.
CONTRIBUTING FACTORS ARE:

1. Widespread use of antimicrobial drugs,


especially broad-spectrum agents.
2. Interrupted or inadequate
antimicrobial treatment of infections.
3. Type of bacteria
4. Type of infection
5. Condition of the host
6. Location or setting
Factors which impair the host defense mechanisms and predispose to
infection by disease-producing microorganisms:

•Breaks in the skin and mucous membranes


related to trauma, inflammation, open
lesions, or insertion of prosthetic devices,
tubes, and catheters for diagnostic or
therapeutic purposes
• Impaired blood supply
• Neutropenia and other blood disorders
• Malnutrition
• Poor personal hygiene
• Suppression of normal bacterial flora by
antimicrobial drugs
Suppression of the immune system and the
inflammatory response by
immunosuppressive drugs, cytotoxic
antineoplastic drugs, and adrenal
corticosteroids
• Diabetes mellitus and other chronic diseases
• Advanced age
ANTIBACTERIALS
• : broad spectrum – effective against 
gram (-) and gram (+)
• : narrow spectrum – effective against 
one type of bacteria
• : bactericidal – directly kill the bacteria
• : bacteriostatic – prevent the growth of 
     bacteria
MECHANISMS OF ANTIBACTERIAL
ACTIONS:
1. Inhibition of bacterial cell wall synthesis or
activation of enzymes that disrupt bacterial cell
walls. (bactericidal)
Eg. penicillins,
cephalosporins
vancomycin

2. Inhibition of protein synthesis by bacteria or


production of abnormal bacterial proteins. (both)
Eg. aminoglycosides
tetracyclines
macrolides
3. Disruption of microbial cell
membranes
eg, antifungals / antiprotozoal

4. Inhibition of organism reproduction by


interfering with nucleic acid synthesis
eg, fluoroquinolones

5. Inhibition of cell metabolism and


growth
eg, sulfonamides
GENERAL ADVERSE REACTIONS

1. Hypersensitivity / allergic reaction


( rash, pruritus, shortness of breathe,
shock)
2. Superinfection ( vaginal and GiT
yeast infection, Proteus and
pseudomonas)
3. Organ toxicity – damage organs
involved in metabolism and excretion.
GENERAL RESPONSIBILITIES:
M – monitor superinfections
E – valuate renal (BUN/ serum creatinine/ creatinine
clearance)/ liver impairment ( SGPT/ ALT ; SGOT/ AST)

D – iarrhea – Take yogurt


I – nform provider prior to taking other medicines
C – ulture prior to initial dose
A – lcohol is out, ask about allergy
T – take full course of pills
E – valuate cultures, WBC, temperature, blood
• Penicillins
• Vancomycin
• Cephalosporins
• Chloramphenicols
• Macrolides and 
• Fluoroquinolones
Lincosamides
• Sulfonamides
• Tetracyclines
• Peptides
• Aminoglycosides
• I. Basic Penicillins
• II. Broad Spectrum penicillin {BSP}
(Aminopenicillins)
• III. Penicillinase – Resistant Penicillins
{PRP} (Antistaphylococcal Penicillins)
• IV. Extended – Spectrum Penicillins {ESP}
• (Antipseudomonal Penicillins)
• V. Beta- Lactamase Inhibitors
History: 
Alexander Fleming (1928), British bacteriologist
- “mold” – penicillium notatum (contaminating 
bacterial cultures)
Howard Florey (1939) purified penicillin
- used during World War II, marketed in 1945

PENICILLIN (beta- lactam antibiotics)


1. A natural antibacterial agent obtained from 
the mold genus Penicillium
- its beta lactam structure is called Beta- 
lactam ring.
BETA- LACTAM RING- 
interferes bacterial cell wall 
synthesis by inhibiting the 
bacterial enzyme necessary for 
cell division and cellular synthesis 
leading to cell lysis (breakdown)
- Can be both bacteriostatic and 
bactericidal

BETA-LACTAMASES –
enzymes produced by bacteria, 
inactivate penicillin 
(PENICILLINASES)
I. BASIC PENICILLINS
A. Penicillin G
C/I:
• Primarily
*allergy to penicillin
bactericidal
*severe renal 
• First penicillin 
disorder
administered
– Not stable in an 
acid environment;  S/E & A/E
given by *hypersensitivity
injection (rash-shock)
– Excreted in bile  *superinfection
and urine *N/V & diarrhea
B. Penicillin V
• Less potent than Pen G
• Effective against mild to moderate 
infection
• 2/3 is absorbed by GIT
• Taken with full glass of water 1 hour 
before food intake or two hours after meal 
(food decreases absorption)
II BROAD SPECTRUM PENICILLINS
(BSP)
(Aminopenicillins)
• Broad spectrum Penicillins
• Costlier than basic penicillin
• NOT penicillinase resistant (easily inactivated
 by beta lactamases thus becoming ineffective 
against S. Aureus)
• Eg : ampicillin (Ampicillin)
: amoxicillin (Amoxin) -- (most prescribed in                                        
adults & children)
: amoxicillin-clauvanate (Amoxyclav,Augmentin)

INDICATIONS: ( gram + & -)
: E. coli
: H. influenzae
: Shigella dysenteriae
: Proteus Mirabilis
: Salmonella
III. PENICILLINASE – RESISTANT
PENICILLINS
(PRP)
(Antistaphylococcal Penicillins)
• Used to treat penicillinase-
producing S. Aureus (gram +)
• Eg:  [O] : cloxacillin
: dicloxacillin
  [IM/IV] : methicillin
: nafcillin
: oxacillin
NOT effective against gram(-)organism
Less effective than Pen G against 
gram (+) organisms
MRSA-methicillin-resistant staphylococcus aureus
Amoxicillin (BSP) & Cloxacillin (PRP)
• Therapeutic effects/ uses:
• Staphylococcus aureus infection
• Most gram + & - cocci & bacilli: RTI, 
UTI, syphilis, gonorrhea, meningitis, 
skin infection, some bone & joint 
infections  and catheter infections

MOA: 
inhibition of enzyme in cell wall
synthesis; bactericidal effect
• C/I: hypersensitivity to penicillin & 
cephalosporins
: caution: renal failure, bleeding d/o, or 
hepatic d/o
S/E & A/E:
1. N,V, D, stomatitis  {Mgt: SFF)
2. Hypersensitivity (rash, urticaria, shock, 
wheezing)
3. Superinfections ( black furry tongue, thrush 
& vaginal discharge
4. Hematologic & neurotoxic effects
Other Specific Information:
*DRUG: decrease effect with tetracycline &  
erythromycin; increase effect with ASPIRIN,
PROBENECID
*FOOD: DECREASED effect with ACIDIC or
JUICES
*Education: call ASAP with undesirable effects, 
take 1-2 h AC or 2-3h PC. May take with 
food. Inc OFI.
*Evaluation: (-) cultures, body temp, CBC esp 
WBC, monitor elevation of AST,ALT
IV. EXTENDED – SPECTRUM
PENICILLINS
(Antipseudomonal Penicillins)
• Effective against
Eg:
Pseudomonas
Aeroginosa [gm (-)] * carbenicillin 
• broad spectrum (IV)
indanyl
• NOT penicillinase resistant * mezlocillin sodium
• similar action but less toxic  * piperacillin – 
than aminoglycosides tazobactam
• INDICATIONS: * ticarcillin - 
* Proteus clavulanate
*Serratia
*Klebsiella pneumoniae
*Enterobacter
*Acinotabacter
V. Beta-lactamase
inhibitors
Penicillinase sensitive penicillin +
Beta Lactamase inhibitors

Amoxicilin (BSP) + clavulanic acid= 
Augmentin, Amoxyclav
Ampicillin (BSP) + sulbactam = 
Unasyn
  Piperacillin (ESP) + tazobactam = 
Tazocin
• Cephalosporium Acremonium              
(a fungus)
• In 1948, was discovered from 
seawater
• Active against gram (+) and (-)
bacteria
• Resistant to beta- lactamase
• 1960 used with clinical 
effectiveness--- semi-synthetic
• MOA:
inhibition of
cell wall
synthesis

:Bactericidal effect
FIRST GENERATION BACTERIA SUSCEPTIBLE

“fa”/ “pha” Can be destroyed by  Proteus mirabilis


beta- lactamases Escherichia coli
Cefadroxil,  Klebsiella    
Cefazolin,  Effective against Gm (+)        pneumoniae
Cephalexin & moderate activity
Gm (-)

SECOND GENERATION BACTERIA SUSCEPTIBLE

“fo”/ “fu” BROADER SPECTRUM  PEK +  HEN


–gram (-); NOT affected  Haemophilus 
Cefuroxime,  by B-lactamases        influenzae
Cefofetan,  Enterobacter    
Cefonicid         aerogenes
Neisseria gonorrhea
           meningitidis
CLASSIFICATIONS:
THIRD GENERATION BACTERIA
SUSCEPTIBLE

“ft” resistant to beta- HENPEK +


lactamases; broader Serratia  
Ceftriaxone,  gram (-) activity
Ceftazidime,C Less effective against Gram      marcesncens
efixime,  (+) pseudomonas    
Cefdinir      aeruginosa
FOURTH GENERATION BACTERIA
SUSCEPTIBLE

“fe” Greater action against gram PEK +  


(-) and minimal action 
Cefepime against gram (+) 
organisms
Staphylococci & 
Resistant to most B- Streptococci
lactamases
Pseudomonas 
aeruginosa
S/E & A/D:
•  GI disturbances: (NAVDA) {best with 
food/milk}

• increased blood clotting time (large 
doses),
•  CNS symptoms: headache,vertigo
• IV/IM – prolonged/high doses = 
PHLEBITIS or THROMBOPHLEBITIS
• HYPERSENSITIVITY RXN
•  Nephrotoxicity
Drug Interactions:
• ROH + cefamandole, cefoperazone or 
moxalactam = (Antabuse/ Disulfiram
like reaction)= flushing, N/V, dizziness,
HA, muscular cramps
• with uricosoric/probenecid= decrease 
excretion of cephalosporins (TOXICITY)
• + anticoagulants/
thrombolytics/NSAIDS=                           
increase risk bleeding
Other Specific information
• Administer on an empty stomach for
better results; may be taken with food if 
GI irritation develops
• Yogurt or buttermilk prevents 
superinfection of the intestinal flora with 
long term use of cephlosporins
• Use glucose enzymatic test (use of
blood sample not urine sample) to 
decrease false positive results.
–refrigerate oral suspensions
–Administer IV (50-100 mL 
diluent) cephalosporins over 
30-45 mins 2-4 times/day 

• Evaluation:
(-) culture, normal temp, normal WBC 
count 
GI: N/V, diarrhea
I : increase glucose 
values
A: anaphylaxis, alcohol 
may cause vomiting
N:  nephrotoxicity
T:  thrombocytopenia
CEF the Giant is a powerful 
antibiotic that can destroy several 
types of bacteria but he can also 
produce undesirable GIANT effects. 
CEF THE GIANT
MACROLIDE
 MOA: inhibits bacterial CHON
synthesis
 EXAMPLE:
– Erythromycin  broad
– Azithromycin spectrum
– Clarithromycin

ALTERNATIVE for patients allergic to


PCN
ERYTHROMYCIN
 Derived from fungus- 
like bacterium                                        
PREPARATIONS:
( Streptomyces   IM – too painful
erythreus)  PO
 First macrolide – + ethylsuccinate
developed, good  – + striate
alternative for patients  – + stolate
allergic to penicillin _________________
= readily absorbed (GI)
 Bacteriostatic @ R: gastric acid destroys therefore 
acid resistant salts are added 
lower doses to decrease dissolution in the 
stomach allowing the drug to 
 Bactericidal @ higher be absorbed in the duodenum 
doses
– Metabolized in the 
liver INDICATIONS:
– Excretion in the   Most active gram (+) ; 
bile to feces
moderate gram (-)
– Cross the 
breastmilk and   DOC:
placenta – Mycoplasma
 IV COMPOUNDS: pneumonias
– + lactobimate – Legionnaires disease
– + gluceptate – STDs, GI infection,
skin & soft tissue
________________
= increase 
absorption
 SIDE/ ADVERSE EFFECTS:

–N/V, diarrhea, 
abdominal cramps
–Hepatotoxicity
EXTENDED MACROLIDE GROUP
1.  azithromycin (ZITHROMAX)
 Indications: mild-moderate streptococci infection, RTI, 
gonorrhea, chancroid {STD}, H. influenzae, Strep. PNA, 
S. aureus
 PC :C (can’t be ruled out)
 A :PO – once a day x 5 days – incompletely 
absorbed in the   GIT
 D: t ½ : 40-50 hrs; only 37% reaches in the systemic 
circulation
 E : bile, feces & urine (less)
 Side Effects:
NAVDA is uncommon, give AC./ 1 hr ac or 2
hr pc + 1 glass of water not FRUIT JUICE
 IV PREP – must be diluted in NSS or D5W – to prevent phlebitis
EXTENDED MACROLIDE GROUP

2. Clarithromycin (KLARICID) – 2nd


developed
Indications:  RTI, MAC, gram (-) & (+), tissue 
infections, H. pylori
PC : C
A : PO 
D : t ½ : 3-6 hrs    ==== 2 x a day
M : PB = 65-75%
E : bile
Side Effects:
NAVDA is common, TAKE with MILK/MEAL
EXTENDED MACROLIDE GROUP
3. dirithromycin (DYNABAC)
 Indications:  CHRONIC BRONCHITIS, URTI, 
CAP, Skin Infections, H. pylori, Legionnaire’s 
disease, Chlamydia
 PC : C
A : PO x 5 days
D : t ½ : 20-50 hrs
M : PB = uk
E : bile, feces
Side Effects:
NAVDA is common, TAKE with FOOD,
or within 1 hr of eating
THE MACROLIDE GIRL

G- GI disturbances                             
( undesirable  NS
effects) D5W

I- IV site ( check 
irritation)
R- reduces activity 
of med if 
given with 
acids (fruit 
juices) or food
L- liver function 
test

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