7/12/201

ANTIBIOTICS
• ANTIBACTERIALS
• ANTIPROTOZOALS
• ANTI FUNGAL
• ANTI HELMINTHICS

Jemwel Sico RN MAN

ANTIBACTERIALS TERMS TO REMEMBER

• 1. PENICILLINS • Bacteriostatic drugs – inhibit
the growth of bacteria (inhibit
• 2. CEPHALOSPHORINS
growth to prevent
• 3. MACROLIDES multiplication)
• 4. TETRACYCLINES • Bactericidal drugs – kill
• 5. AMINOGLYCOSIDES bacteria
• Culture and Sensitivity test
• 6. FLOUROQUINOLONES (C&S) – can detect the
infective microorganism
present in a sample and what
drug can kill it.
• Antibiotic resistance -

TERMS TO REMEMBER TERMS TO REMEMBER

• Additive – equal to the sum of the effects of the • Narrow-spectrum – primarily effective
two antibiotics against one type of organism
• Potentiative – occurs when one antibiotic • Broad-spectrum – can be effective against
potentiates the effects of the second antibiotic,
both gram-positive and gram-negative
increasing the effectiveness
organisms
• Anatagonistic – is a combination of a drug that is
bactericidal and a drug that is bacteriostatic. When
these two drugs are used together, the desired
effect may be greatly reduced.
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Mechanisms of Antibacterial Action ANTIBIOTIC RESISTANCE

• (1) Inhibition of bacterial cell-wall synthesis(prevent bacterial cell
wall to build up)
• (2) alteration of membrane permeability(when taking antibiotics,
the cell wall will allow fluids to enter and it will swell, it will rupture and
the cell will die)
• (3) inhibition of protein synthesis(when taking some antibiotics it
will prevent the cell of the bacteria to produce protein and if no protein,
the cell will die) Ribosomes = protein (Rough ER)
• (4) inhibition of the synthesis of bacterial ribonucleic acid (RNA)
and deoxyribonucleic acid (DNA)(A cell cannot live without DNA, it
will not multiply. No DNA = dead cell)
• (5)
• 1. Self-Medicating (DO NOT SELF MEDICATE!!)
• 2. Don’t stop taking medications even to symptoms subsided
• 3. Repeated exposures
• 4. Do not argue with the doctor’s order (do not demand a drug you
don’t need)
• 5. Follow orders, take prescribed drugs religiously
• 6. Do not take antibiotics if it is a viral infection (Antibiotics are
ineffective against viruses)
• 7. Do not give left over/expired antibiotics
• 8. Give it round the clock

General Adverse Reactions to Antibacterials PENICILLINS

• 1. Allergic (hypersensitivity) reactions, most common side
effect = skin test!!
• 2. Superinfection (kills normal flora or the body)
– *E. coli – large colon, helps produces Vitamin K
– *Bile – large intestine that produces colon bacili that produces brown
color in stool
– *Lactobacillus – vagina, helps keep acidic environment
– *Improve normal flora: Drink yakult to increase colon bacili, yogurt,
probiotics, kimchi
• 3. Organ toxicity
Penicillin
• Penicillin’s beta lactam structure (beta lactam ring)
interferes with bacterial-cell wall synthesis by inhibiting
the bacterial enzyme that is necessary for cell division
and cellular synthesis.
• Can be both bacteriostatic and bactericidal
• Mainly referred to as beta-lactam antibiotics
• Beta lactamase - enzyme produced by
microorganisms, the penicillin cannot penetrate/activate,
so that penicillin cannot kill the bacteria

Pharmacokinetics - Penicillin Pharmacodynamics - Penicillin

• Bactericidal in
• After oral administration, action
penicillin are absorbed
mainly in the duodenum and
upper jejunum of the small
intestine.
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Antibiotics: Penicillins
Penicillin: Mechanism of Action
• Natural penicillins
Penicillins enter the bacteria via the cell wall. • Aminopenicillins
• Penicillinase-resistant penicillins
Inside the cell, they bind to penicillin-binding protein.
• Extended-spectrum penicillins
Once bound, normal cell wall synthesis is disrupted.
• Beta – lactamase inhibitors
Result: bacteria cells die from cell lysis.
Penicillins do not kill other cells in the body.

Antibiotics: Penicillins
Penicillin: Mechanism of Action

Natural penicillins Penicillins enter the bacteria via the cell wall.
penicillin G (Pentids, Pfizerpen, Celinex) Inside the cell, they bind to penicillin-binding
 penicillin V (V-Cillin, Betapen-VK) protein.
Once bound, normal cell wall synthesis is
Aminopenicillins disrupted.
Amoxicillin (Amoxin) Result: bacteria cells die from cell lysis.
Ampicillin Penicillins do not kill other cells in the body.

Antibiotics: Penicillins Antibiotics: Penicillins

• Penicillin-beta-lactamase inhibitor combination
Penicillinase-resistant penicillins
drugs:
Cloxacillin (Ciclox)
Dicloxacillin (Dynapen) – ampicillin + sulbactam = Unasyn
Nafcillin (Nafcil)
Extended-spectrum penicillins – amoxicillin + clavulanic acid = Augmentin
piperacillin, ticarcillin, carbenicillin, – ticarcillin + clavulanic acid = Timentin
mezlocillin
– piperacillin + tazobactam = Zosyn

Beta-Lactamase Inhibitors
• inhibits the bacterial beta-lactamases, making
the antibiotic effective and extending its
antimicrobial effect
• Oral use: Clavulanic acid (Augmentin, TImentin)
• Parenteral use: Sulbactam (Unasyn) and
Tazobactam (Zosyn)
Cephalosphorins
Pharmacokinetics
• Adminitered orally
• Food decreases absorption
• Administered parenterally.
– Not Absorbed in the GI tract.
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Side effects and Adverse Reactions
• Nausea, vomiting and diarrhea are common
GI disturbances
• Severe allergic reaction leads to
anaphylactic shock. Clinical manifestations
of a severe allergic reaction include laryngeal
edema, severe bronchoconstriction with
stridor, and hypotension.
Cephalosporins
• administered when patient is sensitive to penicillin
• have a beta lactam structure and act byinhibiting the
bacterial enzyme necessary forcell wall synthesis
• Only a few cephalosporins are administered orally.
These include Cephalexin (Keflex), Cefadroxil (Duricef),
Cefaclor (Ceclor), Cefuroxime Axetil (Ceftin), Cefuroxime
sodium (Zinacef), Cefdinir (Omnicef), and Cef-tibuten
(Cedax). The rest of the cephalosphorins are
administered IM and IV.
Pharmacodynamics
• Inhibit cell wall
synthesis
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Indications: CEPHALOSPHORIN GENERATIONS

• Pharyngitis • First Generation of Cephalosporins– effective against

• Tonsillitis gram postivie bacteria and most gram negative bacteria)
• Second Generation of Cephalosporins– same
• Lower resp tract infections effectiveness as first generation. Possess a broader
• Septicemia spectrum against other gram negative bacteria
• Meningitis • *First and second generation of Cephalosporins are
• Perioperative prophylaxis usually localized

CEPHALOSPHORIN GENERATIONS Cephalosporins: First Generation

• Third Generation of Cephalosporins– same • Cefadroxil
effectiveness of second and first generations. Also
effective against gram negative bacteria, less effective
• Cephalexin (Keflex, Cefalin, Ceporex)
against gram positive bacteria • cephradine
• Fourth Generation of Cephalosporins– is similar to • Cefazolin Na (Ancef and Kefzol)
third generation. It is resistant to most beta-lactamase –Good gram-positive coverage
bacteria. Has broader gram positive coverage than third –Poor gram-negative coverage
generation. –used for surgical prophylaxis, URIs, otitis media
• * Third and fourth generation of Cephalosporins can cross
the blood-brain barrier

Cephalosporins: Second Generation

Cephalosporins: Third Generation
• Cefaclor (Ceclor)
Ceftizoxime (Tergecin, Ceftizox)
• Cefoxitine (Mefoxin) Ceftazidime (Fortaz, Fortum)
• Cefuroxime (Kefurox and Ceftin) Cefotaxime (Claforan)
Cefixime (Suprax)
– Good gram-positive coverage Ceftriaxone (Rocephin)

– Better gram-negative coverage than first Most potent group against gram-negative
generation Less active against gram-positive
– Used prophylactically for abdominal or colorectal Used for difficult-to-treat organisms such as
surgeries Pseudomonas
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SIDE EFFECTS AND ADVERSE REACTIONS

Cephalosporin: Fourth Generation
• GI distrubances (nausea, vomiting, diarrhea),
cefepime (Maxipime) alteration in blood clotting time (increased bleeding), with
Newest cephalosporin agents. administration of large doses, andnephrotoxicity
Broader spectrum of antibacterial activity than (toxicity of the kidneys)
third generation, especially against gram-positive
bacteria.