CIRILO ALBERT HICBAN RN, RM

Lecturer
Antimicrobials- chemicals that eliminate living
microorganisms that are pathogenic to the
patient.

The antimicrobial agents are subdivided by

chemical families into drug classes.
Antibiotics – Chemicals produced by one kind of
microorganism that inhibits the growth of or kills
another

Antibacterials:
Natural
Manufactured

Bacteriostatic- Inhibit the growth of bacteria

Bactericidal- Kills bacteria
 Inhibition of bacterial cell wall synthesis
 Alteration of membrane permeability
 Inhibition of protein synthesis
 Inhibition of Protein Synthesis of bacterial RNA
and DNA
 Interference with the metabolism within the cell
Resistance to Use of Antibiotic
Antibacterials Combinations
 Natural or Inherent  Additive Effect
Resistance  Potentiative Effect
 Acquired Resistance
 Nausea, Vomiting and Diarrhea
 Secondary Infection-
 Allergies and Anaphylaxis
 Nephrotoxicity
 Hepatotoxicity
 Ototoxicity
 Blood Dyscrasias
 Natural antibacterial agent obtained from mold
genus Penicillium
 World War II
 “Miracle Drug”
 Discovered by Fleming
 SE: hypersensitivity and
superinfection
Action: Penicillin’s beta-lactam structure interferes with
bacterial cell wall synthesis

 Can be bactericidal or bacteriostatic

 Should be taken with full glass of water 1 hr before food
intake or 2 hours after mealtime

penicillin G
 First to be administered orally and by injection
 Painful to be administered IM and has short duration
procaine Penicillin (longer duration of action and less painful)
penicillin V
 Effective against mild to moderate infections (anthrax)
 Treat both gram positive and gram negative bacteria
 Costlier than penicillin
 Effective against E.Coli, Haemophilus Influenzae, Shigella
Dysenteriae and Salmonella
 Not penicillinase resistant

Example:
ampicillin
amoxicillin – not affected by food
bacampicillin – not affected by food
 Antistaphylococcal Penicillins
 Not effective against gram negative organisms and they are
less effective than Pen G against gram positive
microorganisms

Example:
cloxacillin
natillin
oxacillin
 Anti-pesudomonal penicillins
 Effective against Pseudomonas Aeruginosa
 Gram-negative
 Similar action to Aminoglycosides but less toxic
 Not Penicillinase Resistant

 piperacillin sodium
 piperacillin-tazobactam
 carbenicillin indanyl
When a broad spectrum antibiotic is combined with
beta-lactamase inhibitor, the resulting antibiotic
inhibits the bacterial beta-lactamases, thus
making the antibiotic effective and extending its
antimicrobial effect.

clavulanic acid, sulbactam, tazobactam

Broad Spectrum Antibiotic + Beta-Lactamase Inhibitors
= ANTIBIOTIC

Amoxicillin + Clavalunic Acid = Augmentin

Ampicillin + Sulbactam = Unasyn

Piperacillin + Tazobactam = Zosyn

Ticarcillin + Clavalunic Acid = Timentin

 
Action: same as Penicillin
Fungus Cephalosporium Acremonium
Active against gram positive and gram negative and
resistant to beta-lactamase

SE: nephrotoxicity
- Efective against gram-positive bacteria
Streptococci and mostly staphylococci

- Effective against most gram-negative bacteria

cephalexin, cefazolin sodium

Same effectiveness as first generation.
Possess a broader spectrum against other gram-negative
bacteria:

cefaclor (Ceclor), cefoxitin sodium, (Mefoxitin),

cefuroxime(Zinacef)
Same effectiveness as the first and second generations
Also effective against gram-negative bacteria

Less effective against gram-positive bacteria

cefixime, ceftazidime, ceftriaxone (Rocephin)

Similar to the third generation
Resistant to most beta-lactamase bacteria
Has a broader gram-positive coverage than the third
generations.

cefepime
 Staphylococcal infections
 Cardiac surgical prophylaxis for patient with
penicillin allergies
 It’s use was almost abandoned because of
nephrotoxicity and ototoxicty

vancomycin HCl
 Similar spectrums of antibiotic effectiveness to
penicillin
 Penicillin substitutes
Action: Inhibit Bacterial protein synthesis

 Broad spectrum antibiotics; longer half-life

 bacteriostatic and bactericidal effect
 Orally and Intravenously but not IM
 Active against most gram positive bacteria
 Mild to moderate infections of the Respiratory Tract, sinuses, GI,
skin and soft tissue, diphtheria, impetigo and STD’s
 SE: hepatoxicity

 erythromycin is the drug of choice for mycoplasmal pneumonia and

Legionairre’s disease
 clarithromycin, azithromycin
 
Action: Same as macrolides
 Active against gram positive organisms

clindamycin, lincomycin
Action: Prevents bacterial ribosomes from translating its
RNA, preventing the synthesis of new proteins
 New classification of antibiotics, structurally related to
macrolides
 for adults 18 years old and above
 acute chronic bronchitis, acute bacterial sinusitis and
community acquired pneumonia

telithromycin
 1st broad spectrum antibiotic effective against gram
positive and gram negative bacteria

 used against Mycoplasma Pneumonia

 useful in treating Helicobacter Pylori when combine w/

metronidazole and bismuth subsalicylate

 Acne Vulgaris
 IM form causes severe pain and tissue irritation
 Should be taken on empty stomach (except doxycyline
and minocycline)
 Avoid magnesium, aluminum, iron and milk
 SE: photosensitivity, possible teratogenic effect (1st
trimester), teeth discoloration (last trimester and
chilidren less than 8yrs old), ear damage, nephrotoxicity
and superinfection

doxycyclines, minocycline, methacycline

Actions: Kill bacteria primarily by inhibiting protein
synthesis.
 Used against gram negative and gram positive bacteria
 Drug of choice to treat Tularemia and Bubonic
Pneumonic forms of Plague
 Cannot be absorbed in the GI and cannot cross the CSF

streptomycin - first Aminoglycoside

neomycin-preoperative bowel antiseptic
paromycin - intestinal amoebiasis and tapeworm infestation

gentamicin
tobramycin
netilmicin
amikacin – may be use if resistant to gentamycin and
tobramycin

SE: ototoxicity, nephrotoxicity

Action: interfere with the enzyme DNA gyrase which is
needed to synthesize bacterial DNA.
 Antibacterial spectrums includes both gram positive and
gram negative organisms
 Treat primarily UTI, bone, joint infections, bronchitis,
pneumonia

ciprofloxacin (Ciprobay), norfloxacin, levofloxacin,

moxifloxacin (Avelox)
Unclassified Antibacterial Drugs

 chloramphenicol – used to treat serious infections

(H. influenzae, Mycoplasmas)

 spectinomycin – Neisseria Gonorrhea, used also for

patients with allergy to penicillins, cephalosporins,
tetracyclines

 quinupristin – for Vancomycin-Resistant

Enterococcus faecium (VREF)
 Action: Inhibit bacterial synthesis of folic acid essential
for bacterial growth (bacteriostatic)
 Isolated from coal tar derivative compound
 Used if allergic to penicillin
 UTI, ear infections and newborn eye prophylaxis,
meningococcal meningitis and against organisms
Chlamydia and Toxoplasma Gondii

sulfisoxazole, sulfamethoxazole, sulfadiazine

(Silvadene)
trimethroprim-sulfamethoxazole cotrimoxazole
(Bactrim)
 Ethambutol
Inhibits bacterial tuberculosis growth by altering
cellular RNA synthesis and Phosphate
metabolism.
Bacteriostatic
It must be used in combination with other anti-
tubercular agents.
Side Effect: Blurred vision, Red-Green vision
changes
 Isoniazid – first oral preparation
 Bactericidal and bacteriostatic
 appears to disrupt the M. Tuberculosis cell wall and
inhbit replication. Blocks vitamin B6 (pyridoxine)
 Used as prophylaxis for (+) HIV, in contact with PTB
patient (6 mos. To 1 year)
 1 hr before or 2 hours after meal

 Side Effect: Peripheral Neuritis, hepatotoxicity

 Rifampicin
Action: prevents RNA synthesis in mycobacterium
inhibiting DNA-dependeny RNA polymerase.
Side Effect: Reddish-orange secretions, hepatotoxic

 Pyrazinamide - bacteriostatic and bactericidal

Side Effect: arthralgia, hepatotoxic
 Antimycotic Drugs
2 Types of Fungal Infections:
1. Superficial Fungal Infections
2. Systemic Fungal Infections
Anti-fungal Drugs are classified into the following groups:

*Polyenes
*Azoles
*Antimetabolites
*Antiprotozoals
*Echinocandins
Polyenes
*amphotericin B
Drug of choice for treating severe systemic fungal
infections.
Highly toxic can cause nephrotoxicity and electrolyte
imbalance (hypokalemia and hypomagnesemia)

*nystatin (Mycostatin)
Used for candidal infection
Available in suspension, cream ointment, oral/vaginal
tablet
Azoles
Effective against candidiasis

Examples:
Ketoconazole –first effective anti fungal
Fluconazole
Itraconazole
Antimetabolites
Is used in combination with other antifungal drugs such as
Amphoterecin B.
Example: Flucytosine

Antiprotozoal
Is used to treat mild to moderate Pneumocytis Carinii
Pneumonia
Example: Atovaquone (Mepron)
Echinocandins
Is used to treat Candida and Aspergillosis
infections. Given thru IV.

Adverse effects: increased AST and ALT

Example: caspofungin ( Cancidas)

Action: Interfere with bacterial cell membrane function. Derived
from Bacillus Subtilis.
Given slow IV push
2 two groups:
1. Polymxins - gram-negative bacteria
2. Bacitracin - gram-positive bacteria and some gram-
negative bacteria, Can be used to treat meningitis

Side Effect: nephrotoxicity (BUN and creatinine is increased),

neurotoxicity (numbness and tingling of the extremeties,
paresthesias and dizziness)
 metronidazole (Flagyl)
 Used to treat various disorders in the GI tract
 Intestinal amebiasis, trichomoniasis,
Inflammatory bowel disorders
 Used with other agents to treat Helicobacter
pylori
 Antiviral drugs are used to prevent or delay the spread of
a viral infection.
Action: inhibit the viral replication by interfering with viral
nucleic acid synthesis in the cell.

*Non-classified antivirals
*Topical antivirals
*Neuroaminidase Inhibitors
*Gammaglobulin (Immune Globulin)
*Purine Nucleosides
 Non-classified antivirals
Used to treat Influenza A:
1. amantadine HCl (Symmetrel)
2. rimantadine HCl (Flumadine)
cidofovir- CMV retinitis
foscarnet (Foscavir)- HIV retinitis and herpes simplex
infection in clients with AIDS
vidarabine- HSV-1, herpes zoster, varicella zoster CMV,
HSV encephalitis

Side Effect: insomia, depression,anxiety,confusion, ataxia,

hypotension, neurologic problems
 Topical Antivirals
These are used to treat Herpes Simplex Virus
Example:
idoxuridine ( Herplex Liquifilm)
penciclovir ( Denavir)
 Neuramidase Inhibitors
Decreases viral spread and shortening the duration
of flu symptoms.
Should be taken 48hrs of flu

Example:
Zanamivir (Relenza)
Oseltamavir Phosphate (Tamiflu)
Gamma Globulin (Immune Globulin)
 Administered intramuscularly, at early infectious stage
 Provides passive form of immunity by blocking the
penetration of virus into the host cell

Example:
immune globulin (Gamimune N)
Purine Nucleosides
 Interferes with the steps of viral nucleic acid synthesis

These are effective in combating Herpes Simplex viruses,

Herpes Zoster, Varicella Zoster Virus, and CMV.
Example:
ribavirin (Virazole)
acyclovir (Zovirax)
Antiviral HIV Drugs
inhibits viral replication

 Reverse Transcriptase Inhibitors

delavirdine, lamivudine

 Protease Inhibitors
indinavir, ritonavir

* *When used in combination helps to decrease HIV drug resistance

 Given orally
 When drug-resistant malaria occurs, combinations of
anti-malarials are used to facilitate effective treatment.
Example:
Choloroquine HCl – commonly prescribe
Mefloquine
Primaquine Phosphate
Quinine Sulfate
Side Effect: GI upset, CN VIII involvement