Antibacterial Agents

Antimicrobial
Antibiotic
LEILANI O. ESTACIO, MAN RN
ANTIBACTERIALS

ANTIBACTERIAL/ANTIMICROBIAL/ANTIBIOTIC are frequently used

interchangeably

ANTIBACTERIAL and ANTIMICROBIALS are substances that INHIBIT

bacterial growth or kill bacteria and other microorganisms

ANTIBIOTIC refers to chemicals produced by one kind of microorganism that

INHIBITs the growth of or kills another at very low concentration
Antimicrobial can be group according to:

1. According to microorganism they act primarily against

2. According to their function -microbicidal (disinfectant)

- biostatics
ANTIBACTERIAL DRUGS

ANTIBACTERIAL DRUGS obtained from natural sources or manufactured

ALEXANDER FLEMMING (British bacteriologist)

◦ Mold contaminating bacterial cultures INHIBITING bacterial growth
◦ Penicillium notatum

Howard Florey
◦ Purified penicillin
◦ Expanded Flemings' findings
ANTIBACTERIAL DRUGS

BACTERIOSTATIC inhibit the GROWTH of bacteria

BACTERICIDAL KILL bacteria

MECHANISM of ANTIBACTERIAL ACTION

◦ Inhibition of bacterial cell-wall synthesis
◦ Alteration of membrane permeability
◦ Inhibition of protein synthesis
◦ Inhibition of the synthesis of bacterial ribonucleic acid (RNA)
◦ Interference with metabolism within the cell
ANTIBACTERIAL DRUGS
FACTORS AFFECTING ANTIBACTERIAL USE

◦ Body defenses

◦ Resistance to antibacterial
◦ Inherent resistance
◦ Acquired resistance
◦ Cross-resistance

◦ Adverse reactions to Antibacterial Drugs

◦ Allergy or Hypersensitivity
◦ Superinfection
◦ Organ toxicity
ANTIBACTERIAL DRUGS

Narrow-Spectrum
◦ Primarily effective against one type of organism

Broad-Spectrum
◦ Effective against both gram-positive and gram-negative
Problems that arise w/ the use of
antimicrobial agent
1.TOXICITY – reached the toxic level
2. HYPERSENSITIVITY REACTIONS – undesirable reactions
produce by normal immune system
3. DRUG RESISTANCE – reduction of effectiveness of a
medication such as antimicrobial in treating disease
4.SUPER INFECTION – infection occurring after or on top of
an earlier infection
5. NUTRITIONAL DEFICIENCY
Penicillin
◦ A natural antibacterial agent obtained from the mold genus
Penicillium
◦ Beta-lactam antibiotics
◦ Beta-lactam structure (beta-lactam ring)
◦ Interferes with bacterial cell-wall synthesis by inhibiting bacterial enzyme for cell-
division and cellular synthesis
◦ Beta-lactamases (penicillinase)
◦ Inactivate beta-lactam antibiotics by attacking penicillin
 Penicillin
Broad-Spectrum Penicillin (Aminopenicillins)
◦ Used to treat both gram-positive and gram-negative bacteria
◦ Readily inactivated by beta-lactamases
◦ Ampicillin
◦ Amoxicillin (most prescribed penicillin) AMOXIL
◦ Bacampicillin
Penicillinase-Resistant Penicillin
(anti-staphylococcal penicillin)
◦ Used to treat penicillinase-producing S.Aureus
◦ Cloxacillin
◦ Dicloxacillin
◦ Nafcillin sodium
◦ Oxacillin
 Penicillin

Extended-Spectrum Penicillin
(anti-pseudomonal penicillin)
◦ Not penicillinase-resistant but has the same mechanism of action with
aminoglycoside but is less toxic
 Penicillin
Beta-Lactamase Inhibitors
◦ Broad-spectrum antibiotic combined with beta-lactamase inhibitors
◦ Clavulanic acid
◦ Sulbactam
◦ Tazobactam
◦ Combined with a penicillinase-sensitive penicillin:
◦ Amoxicillin-clavulanic acid (Augmentin)
◦ Piperacillin-tazobactam (PipTaz)
◦ Ampicillin-sulbactam (Unasyn)
◦ Ticarcillin-clavulanic acid (Timentin)
Most Penicillin should be given on empty stomach (1 hour before or 2 hours after meal) to enhance absorption.
Penicillin that can be given without regards to meals include amoxicillin, penicillin V and amoxicillin-clavulanate
potassium.

EXIT ROUTE: penicillin are metabolized to a limited extent in the liver to inactive
metabolites.
Nafcillin and Oxacillin are excreted in bile.
PHARMACODYNAMICS : Bactericidal in action.
They bind reversibly to several enzymes outside the bacterial cytoplasmic
membrane ( Penicillin Binding Protein)
 Cephalosporin
Cephalosporium acremonium
◦ Fungus found to be active against gram-positive and gram-negative bacteria
resistant to beta-lactamase

◦ Contain beta-lactam structure

◦ Inhibits cell wall synthesis and subsequent lysis of cell wall

◦ Not all are affected by beta-lactamases

 Cephalospirin
First-Generation
◦ Destroyed by beta-lactamase
◦ Cefazolin
◦ Cephalexin
◦ Cefadroxil
◦ Cephradine
Second-Generation
◦ Not all are affected by beta-lactamase
◦ Cefaclor
◦ Cefoxitin
◦ Cefuroxime
◦ Cefmetazole
◦ Cefonicid
 Cephalospirin

Third-Generation
◦ Resistant to beta-lactamases
◦ Cefotaxime
◦ Cefpodoxime
◦ Ceftriaxone
◦ Ceftazidime

Fourth-Generation
◦ Resistant to beta-lactamases
◦ Cefepime
 Client Teaching
WOF signs of superinfection
◦ Mouth ulcers
◦ Anal/vaginal discharge
Advise ingestion of buttermilk or yogurt to prevent
superinfection of the intestinal flora with long term
use of a cephalosporin
Compliance and adherance to treatment regimen
Infuse all IV cephalosporins over 30-minute period to
prevent pain and irritation
Observe for HYPERSENSITIVITY reaction
DRUG INTERACTION:
Patient receiving Cephalosporin's who drink alcoholic
beverages with or up to 72 hours after taking a dose may
experience acute alcohol intolerance
S/symptoms: headache, flushing, dizziness, nausea,
vomiting, abdominal cramps within 30 minutes of alcohol
ingestion. This reaction can occur up to 3 days after
discontinuing the antibiotic.
 Chloramphenicol

 Is an antibiotic useful for the treatment of a number of

bacterial infections.
 This includes use as an eye ointment to treat conjunctivitis,
By mouth or by injection into a vein
it is used to treat meningitis, plague, cholera, and typhoid
fever
 Macrolides,
Tetracyclines,
Aminoglycosides,
and Fluoroquinolones
 Macrolides
Azithromycin (Zithromax)
Clarithromycin (Clariget)
Erythromycin
◦ First macrolide derived from fungus-like bacteria Streptomyces
erythreus
◦ Destroyed by gastric acid, prevented by adding acid-resistant salts
(ethylsuccinate, stearate, estolate)
Used to treat mild to moderate infections of the respiratory tract,
sinuses, GI tract, skin and soft tissues, STIs
AE: Hepatotoxicity (check liver function)
MACROLIDES
1. Erythromycin
2. Azithromycin
3. Clarithromycin
4. Fidaxomicin
5. Telithromycin
Considerations
◦ C/S before starting therapy
◦ Liver function test:
◦ Alkaline phosphatase
◦ Alanine aminotransferase (ALT)
◦ Aspartate aminotransferase (AST)
◦ Bilirubin
◦ Check for jaundice
◦ Administer 1 hour before or 2 hours after meals
◦ (+) GI upset: take with meals
 Lincosamides
Inhibits bacterial protein synthesis
Bacteriostatic and bactericidal
◦Clindamycin
◦More prescribed and is active against most gram-
positive including staphylococcus aureus and anaerobic
microorganisms
 Vancomycin

Glycopeptide bactericidal antibiotic

◦ Used against drug-resistant S. Aureus
◦ Levels should be monitored
◦ Nephrotoxic and Ototoxic
◦ Can cause temporary/permanent hearing loss
◦ Rapid infusion:
◦ Red man syndrome or Red neck syndrome
◦ Red blotching of face, neck, and chest
 Tetracycline
Isolated from Streptomyces aureofaciens
Used against mycoplasma pneumonia
Helicobacter pylori infection
Acne vulgaris
◦ Should not be taken with MAGNESIUM and ALUMINUM antacids
preparations, milk products containing CALCIUM, IRON-containing drugs
----PREVENTS ABSORPTION
◦ Tetracycline Hydrochloride (ACHROMYCIN)
◦ Doxycycline Hyclate(VIBRAMYCIN)
◦ Minocycline Hydrochloride (MINOCIN)
◦ Demeclocycline Hydrochloride (DECLOMYCIN)
Tetracycline in low dosages effectively treat acne because
they decrease fatty acid content of sebum.
Tetracycline can reduce the effectiveness of hormonal contraceptives,
which may result in breakthrough bleeding or ineffective contraception.
Tetracycline can reduce also the bactericidal action of penicillin.
Give water with the oral drug and the patient takes to promote passage to
the stomach. Incomplete swallowing can cause severe esophageal
irritation.
Don’t give drug within 1 hour of bedtime to prevent esophageal reflux.
IV administration ay cause phlebitis.
 Tetracycline
Side effects and adverse effects:
◦ GI disturbances
◦ PHOTOSENSITIVITY
◦ Teratogenic effect (1st trimester)
◦ Do not give in <8 y/o (permanently DISCOLORS teeth)

◦ Ototoxicity
◦ Nephrotoxicity
◦ Superinfection
 Tetracycline
Considerations
◦ Light-sensitive and heat-sensitive
◦ Decomposes in toxic form
◦ Check expiration date
◦ Sun block and protective clothing
◦ Lessens effectiveness of oral contraceptives
◦ Dietary considerations
 Aminoglycosides
Act by inhibiting bacterial protein synthesis
Used for gram negative bacteria
◦ Streptomycin
◦ Derived from Streptomyces griseus
◦ Used for treatment of Tuberculosis
Cannot be absorbed in GI tract and cannot cross into CSF
Crosses BBB in children but not in adult
Primarily administered IM or IV
◦ NEOMYCIN (given orally as preoperative bowel antiseptic)
◦ GENTAMYCIN (Tx of Pseudomonas Aeruginosa)
◦ AMIKACIN
◦ TOBRAMYCIN
 Aminoglycosides

Considerations:
◦ Nephrotoxicity (check UO and kidney function)
◦ Ototoxicity (check for hearing loss and
◦ Check for superinfections
Pharmacotherapeutics of
AMINOGLYCOSIDES
MOST USEFUL IN TREATING OF:
1. infections caused by gram – bacilli
2. serious nosocomial (hospital acquired) infections, such as gram – bacteremia , peritonitis and
pneumonia
3. UTI caused by enteric bacilli that are resistant to less toxic antibacterial drugs such as
penicillin
4. Infection of the CNS
 Fluoroquinolones

Interferes with enzyme DNA gyrase needed to synthesize bacterial DNA

Effective in both gram-positive and gram-negative
Used in urinary tract, bone, and joint infections; bronchitis, pneumonia,
gastroenteritis; and gonorrhea
◦ Ciprofloxacin
◦ Norfloxacin
◦ Levofloxacin
◦ moxifloxacin
Sulfonamides
 Sulfonamides
One of the oldest antibacterial agents used to combat infection
Isolated from coal tar derivative compound
Not classified as ANTIBIOTIC (not obtained from biologic substances)
Bacteriostatic (inhibits folic acid)
◦ Sulfisoxazole
◦ Sulfadiazine
◦ Sulfamethoxazole
 Cotrimoxazole (Combined with Trimethoprim for synergistic effect (1:5
ratio).Useful in treating urinary, intestinal, and lower respiratory tract infection, otitis
media, gonorrhea
 Sulfonamides

Topical Sulfonamides:
◦ Mafenide acetate (Sulfamylon)
◦ Prescribed in second and third degree burns
◦ Silver sulfadiazine (Silvadene)
◦ Used also for Treatment of burns
 Sulfonamides
Considerations:
◦ Increase OFI to prevent crystalluria
◦ Avoid in 3rd trimester of pregnancy
◦ Avoid antacids (decreases absorption)
◦ Taken 1 hr before or 2 hrs after meals
◦ Photosensitivity precaution
Antifungal Antibiotics
An antifungal medication, also known as an
antimycotic (Fungus) medication.

is a pharmaceutical fungicide or fungistatic used to

treat and prevent mycosis such as athlete's foot,
ringworm, candidiasis (thrush), serious systemic
infections such as cryptococcal meningitis
 DRUGS ACTING ON IMMUNE SYSTEM (Immunologic Agents)
  are Immunologic agents?
What
Immunologic agents are drugs that can modify the immune response, either by
enhancing or suppressing the immune system. They are used to fight infections,
prevent and treat certain diseases.
Immunologic agents include drugs used for immunosuppression to prevent graft
rejection. They can be used as cancer chemotherapy agents.
Some immunologic agents can down-regulate the inflammatory process and can be
used to treat inflammatory conditions such as rheumatoid arthritis, autoimmune
conditions.
Types of Immunologic agents
●Immune globulins
●Immunostimulants
bacterial vaccines
colony stimulating factors
interferons
interleukins
therapeutic vaccines
viral vaccines
Types of Immunologic Agents
● Immunosuppressive agents
calcineurin inhibitors
interleukin inhibitors