Intro To Antimicrobial Pharm

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A substance produced by a microorganism that suppresses the growth of other microorganisms

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Antibiotic

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Chemotherapeutic Drugs

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Antimicrobial drugs
Antiparasitic drugs
Antineoplastic drugs

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Antimicrobial drugs can be subclassified into the following:

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Antibacterial
Antifungal
Antiviral

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Any chemical used in the treatment, relief, or prophylaxis of a disease

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Chemotherapeutic drug

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Use of a drug to prevent imminent infection of a person at risk

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Prophylaxis

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Refers to the range of microorganisms that an antimicrobial agent can kill or inhibit

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Spectrum of activity

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Narrow spectrum agent or activity

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Antimicrobials effective against a limited array of microbial types. Targets a specific cell component found only in certain microbes
ex. drug effective mainly against gram-positive bacteria

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Broad spectrum agent or activity

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Antimicrobials effective against a wide variety of microbial types. Targets cell components common to most pathoges
ex. drug effective against both gram-positive and gram-negative

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Antimicrobial activity of a drug can be generally characterized in three ways:

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-bactericidal versus bacteriostatic effect
-may have a concentration-dependent or time-dependent killing effect
-its spectrum of activity against different microbes

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These antibiotics inhibit/stop the growth and reproduction of bacteria but do not kill them

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Bacteriostatic agents

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Works with the immune system to remove microorganisms from the body

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Bacteriostatic agents

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T/F: Most bacteriostatic agents are protein synthesis inhibitors

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True

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Tetracycline

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Bacteriostatic

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Macolides

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Bacteriostatic

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Kills bacteria

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Bactericidal agents

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Use of this type of drug is critical when the immune system is weak or depressed

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Bactericidal agents

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These types of drugs can have a concentration dependent or time dependent killing effect

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Bactericidal

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T/F: Drugs that target the cell wall are bacteriostatic

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False

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MIC

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minimum inhibitory concentration; the lowest concentration of a drug that inhibits bacterial growth

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Example of time-dependent, bactericidal agents

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Beta-lactam antibiotics

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T/F: Greater drug concentrations result in greater killing of bacteria with time-dependent bactericidal agents

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False

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Concentration-dependent killing

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Bacterial kill increases with increasing levels of drug

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Examples of concentration-dependent drugs

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aminoglycosides and fluoroquinolones

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T/F: Bacteriostatic drugs should be used in patients with impaired immune defense

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False; bactericidal drugs should be used

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Drug required for use in Endocarditis and Meningitis

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Bactericidal drugs

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Drugs required for use in infections in neutropenic cancer patients

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Bactericidal drugs; b/c anti-cancer drugs suppress the immune system

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To adversely affect one type of cell and spare normal human cells:

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Selective toxicity

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What does penicillin target?

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bacterial cell wall

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How are antimicrobials classified?

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What they target or mechanism of action

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Common target of agents that inhibit synthesis of bacterial cell walls:

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peptidoglycan in bacterial cell wall

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Beta-lactam antibiotics

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inhibit synthesis of bacterial cell walls

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Beta-lactam antibiotics

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inhibit insertion of peptidoglycan into cell wall

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largest and most widely prescribed antibiotic class

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Beta-lactam antibiotics

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Vancomycin

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cell wall inhibitor

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Bacitracin

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cell wall inhibitor

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Key to beta-lactam mechanism of action

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beta-lactam ring

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What does beta-lactam ring bind to?

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penicillin binding proteins; key bacterial enzymes in cell wall synthesis

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Penicillin

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beta-lactam

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cephalosporin

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beta-lactam

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monobactam

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beta-lactam

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carbapenems

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beta-lactam

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Enzyme that cleaves beta-lactam bond

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beta-lactamase; breaks beta-lactam ring; drug is inactive

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what determines spectrum of antibacterial activity?

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R side chains

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Enzyme that breaks beta-lactam bond in penicillin

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penicillinase

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Enzyme that breaks beta-lactam bond in cephalosporin

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cephalosporinase

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MRSA

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methicillin-resistant Staphylococcus aureus

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T/F: beta-lactam antibiotics work against MRSA

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False

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T/F: PBP is altered in MRSA

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True; that's why beta-lactam drugs are ineffective because they can't dint to the pencillin binding protein

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4 groups of beta-lactams

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1) Natural penicillins
2) Cephalosporins
3) Carbapenems
4) Monobactams

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T/F: beta-lactams are bactericidal

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True

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T/F: beta-lactams are concentration-dependent killers

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False; beta-lactams are time-dependent killers

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penicillin G

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natural penicillin

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nafcillin

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Penicillinase-resistant penicillin

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amoxicillin

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Extended-spectrum penicillins

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ticarcillin

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Antipseudomonal penicillins

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Methicillin-like antibiotic

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nafcillin

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penicillin G

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narrow spectrum antibiotic; gram-positive bacteria

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Largest and most widely used class of antibiotics

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Cephalosporins

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First generation Cephalosporins

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Cephalexin

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Second generation Cephalosporins

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Cefoxitin

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Third generation Cephalosporins

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Ceftriaxone

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Fourth generation Cephalosporin

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Cefepime

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2nd, 3rd, and 4th generation cephalosporins:

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increased activity against gram-negative, increased resistance to beta-lactamases, increased ability to cross BBB

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Imipenem

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Carbapenems

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Aztreonam

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Monobactams

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Other cell wall inhibitors

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Vancomycin and Bacitracin

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Vancomycin

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does not cross lipid membrane of gram-negative bacteria

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Acquired antibiotic resistance to Vancomycin due to:

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amino acid alterations in side chain peptidoglycan building blocks; drug binding site is mutated

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Bacitracin

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interferes with transport of peptidoglycan precursors across cytoplasmic membrane; cell wall synthesis is inhibited; toxicity limits use to topical applications

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Polymyxin and daptomycin

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act directly on the bacterial cell membrane; disrupt the integrity of the cell membrane; increase permeability leading to leakage of intracellular components

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daptomycin

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binds to bacterial membranes causing rapid depolarization and loss of membrane potential leading to cell death

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polymyxin and daptomycin

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bactericidal with concentration-dependent killing

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Drugs that are generally bacteriostatic agents:

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agents that inhibit bacterial protein synthesis; shutting down protein synthesis does not kill bacteria

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Doxycycline

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Tetracyclines
Inhibit protein synthesis

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Erythromycin

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Macrolides
Inhibit protein synthesis

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Gentamycin

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Aminoglycosides
Inhibit protein synthesis

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Drugs that irreversibly inhibit protein synthesis

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Aminoglycosides

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T/F: Drugs that inhibit protein synthesis are irreversible

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False

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Tetracycline resistance

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Efflux pump and ribosome protection

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Aminoglycoside resistance

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microbial enzymes and aminoglycoside modifying enzymes

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Macrolide resistance

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Efflux pump and ribosome modification

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Rifampin

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Inhibition of RNA polymerase
Interferes with nucleic acid synthesis

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Fluoroquinolones

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Inhibition of DNA replication
Interferes with nucleic acid synthesis

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Ciproflaxin

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Inhibition of DNA replication
Interferes with nucleic acid synthesis

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T/F: Drugs that interfere with nucleic acid synthesis are bactericidal

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True

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Trimethoprim

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Metabolic inhibitor

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Sulfonamides

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Metabolic inhibitor

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Sulfamethoxazole

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Metabolic inhibitor

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Drugs that target the folic acid synthesis pathway:

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Drugs that inhibit synthesis of essential metabolites

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Cofactor needed for synthesizing the building blocks of DNA

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Folic acid

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Describes the atomic or molecular structure of drug

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Chemical name

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Official name of the drug

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Generic name

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Name that is public property

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Generic name

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Brand name

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Trade name