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Pharm205 Unit6
Pharm205 Unit6
ANTIBIOTICS 101
Week II - FINALS
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ANTIBIOTICS ANTIBIOTICS
Antibiotics are medicines that fight bacterial infections in people TYPES
and animals. They work by killing the bacteria or by making it • ANTIBACTERIALS
hard for the bacteria to grow and multiply. • ANTIFUNGALS
• ANTI-PARASITICS
• ANTIVIRALS
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CELL WALLS
BACTERIA
• Made up of PEPTIDOGLYCAN; that contains peptides and
amino sugars mainly named NAM (NAcetylmuramic acid) &
NAG (N-Acetylglucosamine)
FUNGI
CELL WALL INHIBITORS
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• Made up of CHITIN; which is composed of NAcetylglucosamine
(NAG’S)
PLANTS
• Made up of CELLULOSE; which is composed of
monosaccharide units called glucose
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PENICILLINS PENICILLINS
2 rings: • Contains Beta Lactam Thiazolidine
Beta-Lactam Ring – cyclic amide; most Ring; called 6-APA (6-Amino
important chemical nucleus of Penicillanic Acid) or the PENAM RING
penicillin’s • Naturally occurring and Semi-
Thiozolidine Ring – sulfur containing synthethic can also be called
ring antibiotics
• “Antibiotics” produced from microbes
(fungi, bacteria)
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PENICILLINS PENICILLIN G
• Came from the fungus named • Aka PEN G chemically known as
Penicillin notatum produces Pen G Benzyl Penicillin
then they improve by adding amino • Considered Drug of Choice (DOC) for
group called Amoxicillin Gram positive bacterial infections and
• Discovered by Alexander Fleming sexually-transmitted diseases such as
• Successfully isolate the chemical were “Syphilis”
Florey and Chain; used a very • It has mild adverse effects
important technique called freeze
drying or Lyophilization
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PENICILLIN G PENICILLIN G
PROBLEMS AND REMEDIES PROBLEMS AND REMEDIES
• Acid-labile or acid sensitive; if drug is taken • Water insoluble; replace the hydrogen with Sodium and Potassium
orally it starts to degrade; only taken which is the salt forms of Penicillin making it water soluble already
intravenously or intramuscularly • Degraded by Beta-lactamase or Penicillinase; produced by
• Easily excreted; therefore they form Staphylococcus aureus which is resistant to Pen G
Depository (Depot) form of Pen G namely Pen
G Benzathine and Pen G Procaine; they also
combine Pen G & ‘Probenicid’ which is a
uricosuric acid (gout) that competes with the
active tubular secretion of Pen G
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PENICILLIN V
MECHANISM OF ACTION
• Aka PEN V chemically known as • Inhibition of the synthesis of peptidoglycan
Phenoxymethyl Penicillin GRAM (+) Bacteria
• It has an electron withdrawing group • Has a thick peptidoglycan; composed of 40 peptidoglycan layers cell
making it ‘acid stable’; it can be taken wall of bacteria
orally • If the cell wall is destroyed cell contains will be leak out that leads to
bacterial death
• Cell wall inhibitors are bactericidal
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CARBOCYPENICILLINS
• Carbenicillin – 1 st antipseudomonal PCN; caused by pseudomonas
aeruginosa (drug resistant)
• Carbenicillin Indanyl Sodium – derivative and given orally for UTIs
• Ticarcillin – same activity with Carbenicilllin
EXTENDED SPECTRUM
PENICILLINS
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UREIDOPENICILLINS ANTI-PSEUDOMONAL
• Derivative of Urea
•C – Carbenicillin
• Mezlocillin, Azlocillin, Piperacillin (most potent)
• All active against Gram negative bacilli such as Klebsiella pneumoniae •T – Ticarcillin
• Also active against Pseudomonas aeruginosa
• Also degraded by beta-lactamase; thus they added beta-lactamase
•M – Mezlocillin
inhibitors; examples: Piperacillin (antibiotic) + Tazobactam (BLI) = •A – Azlocillin
Piptaz® ,Tazocin® & Piper-Tazo®
•P – Piperacillin (most potent)
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NOTE
• Oxacillin, Cloxacilllin & Dicloxicillin are called Isoxazolyl Penicillins
(Halogens); can be orally administered
• 4 GROUPS OF PCNS
BACTERIAL RESISTANCE TO
1. Natural – Pen g & Pen V
PENICILLINS
2. Amino – Amox & Ampi Week II - FINALS
3. Anti-pseudonomal – CT MAP
4. Anti-Staph – MN OCDE
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BETA LACTAMASE
• Enzyme that catalyzes opening of the beta lactam ring to produce
peniicilloic acid
• Several strains are resistance due to altered penicillin binding proteins;
MOA – inhibits transpeptidation
• Some strains are resistant decreased entry or active efflux of antibiotic
BETA LACTAMASE INHIBITORS
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TAZOBACTAM
• More potent than sulbactam and slightly broader activity than
clavulanic acid
• Piperacillin + Tazobactam (Zosyn®, Piptaz®, PiperTazo® &
Tazocin®)
CEPHALOSPORINS
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MONOBACTAMS AZTREONAM
• Binds with PBP3 in gram-negative bacteria only
• Only has the beta-lactam • Even called “Magic Bullet for Pseudonomas”
ring and only effective • E.g: E. coli, Klebsiella, Proteus, Serratia,
against gram-negative Citrobacter and Pseudonomas
bacteria • Treats:
• UTI
• LRTI
• Intra-abdominal infection
• Gynaecological infection
• Septicimia
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TIGEMONAM CARBAPENEM
• Administered Orally (PO) • Olivanic acids, Thienamycin, Imipenem, Meropenem,
• Resistant to beta-lactamases Ertapenem
• Treats • Comprise a family of fused beta-lactam rings
• UTI • Has broadest antimicrobial spectrum of any antibiotic
• Non-life threatening infections by Mos without beta- • Analogues of penicillins or clavams, the sulphur or oxygen
lactamase
being replaced with carbon
• Considered as the last line of agents against bacterial
infections.
• Reserved agents that are resistant to other antimicrobial
agents
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IMIPENEMS MEROPENEM
• N – Formimidoyl derivative of thienamycin that is very • Dimethylcarbomoyl pyrolidinyl derivative of thienamycin
resistant to beta-lactamase • More stable against dehydropeptidase enzyme
• From Streptomyces cattleya • Meropenem (Merrem IV®)
• Readily hydrolysed by renal dehydropeptidase (DHP)
• Highly nephrotoxic
• Imipinem + Cilastatin (DHP-inhibitor) (Primaxin®), Tienam®
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