Antibacterial Drugs Ct64

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Gram Positive Bacteria

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Streptococcus
Staphylococcus
Listeria

Thick cell wall

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Gram Negative

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E.Coli
Salmonella
Pseudomonas

Thinner cell wall, outer membrane dipopolysaccharide protein developed to compensate for thin cell wall.

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Superinfection

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Appearance of a new infection during the treatment of the primary infection, as a result of tx. Superinfections often drug resistant to antibiotic in given for infection #1.

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Cell Wall Inhibitors (B-Lactams)
Penicillins
Cephalosporins
Ampicillins

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Attach to penicillin binding proteins (PBP's) membrane. Results in inhibition of enzymes that form crosslinks in cell wall

The consequence is to weaken the cel wall so it cannot withstand osmotic pressure, resulting in cell lysis and death

Bacteriocidal

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Penicillin binding proteins or PBP's

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The final step in the synthesis of the cell wall is the cross linking of the peptidoglycans via enzymatic reactions that bind a cell wall substrate, PBP's. PBP's are involved in assembly, maintenance, and regulation of baterial cell walls.

B-lactams resemble this cell wall substrate

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Cephalosporins

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B-lactam antibiotic
40 different variations
Classified by generations
Difference between generations is predominately spectrum
3rd Gen-hospital acquired infections
4th Pseudamonas and meningitis (cross BBB)

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Adverse Reactions

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Penicillins
Toxic reactions in massive doses
CNS irritation causing convulsions
Allergic reactions- greatest danger assoc. with use is anaphylactic shock, rash, oral lesion

Cephalosporins
Superinfections

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4 Mechanisms of B-lactam Resistance

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Inactivation of the B-lactam ring
Alterations of PBP's
Reduction of antibiotic access to PBP's
Elaboration of efflux mechanisms-

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B-lactam Resistance

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Tools to fight resistance
Penicillins (group 2) and cephalosporins that are resistant to B-lactamase
B-lactamase inhibitor (clavulcanic acid) blocks B lactamase , Augmentin

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Cell Metabolism Inhibitors
(Protein Synthesis)

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Macrolides & Clindamysin Bacteriostatic
Tetracyclines Bacteriostatic
Aminoglycosides Bacteriostatic

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Tetracyclines

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Stored in the dentine and enamel of unerupted teeth-stains

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Cell Metabolism Inhibitors

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Bacteria must synthesize folic acid for use

sulfonamides- Bacteriostatic
Trimethoprim- Bacteriostatic

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Adverse Effects Cell Metabolism Inhibitors

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Sulfonamides-high concentrations can cause crystal formation, kidney obstruction
Trimethoprim-Adverse effects rare except in AIDS

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Cell Replication Inhibitors

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Nitrofurans
Bacteriostatic but can become bacteriocidal
DNA gyrase-promotes unwinding of DNA

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Nitrofurans

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Bacteriostatic and bacteriocidal dependent of the dose

Interfere with red blood cell enzyme systems in babies

Contraindicated in pregnant women near term

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First line of Anti Tuberculosis Drugs

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Isoniazid
Only works on dividing cells

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Antifungals

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Yeast and Molds
Groupings for fungal infections: Skin and Deep Mycoses

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Structural classes of antifungals

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Membrane Disrupting Agents- Polyenes
Ergosterol synthesis inhibitors-Azoles

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Polyenes
Membrane disrupting Agents
M of A

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Binds sterols (preferentially ergosterol) and disrupts osmotic integrity of cell membrane
Fungicidal

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Polyenes complications and drug interactions

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Nephrotoxicity
Major limitation of Amphotericin B

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Azoles
Two Broad Classes
structurally similar to cholesterol

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Imidazoles-Older
Triazoles-Newer

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Azole M of A

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Inhibits lanosterol demethylase (a cytochrome P450, CYP enzyme) and impair the synthesis of ergosterol
Fungistatic

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Azoles drug interactions

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Numerous and dangerous
Interacts with co admininstered drugs that induce CYP P450 metabolism are a concern

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Echinocandins
Glucan Synthase Inhibitors

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Echinocandin Mechanism: Block cell wall synthesis via B-1,3 glucan synthesis inhibition
Fungicidal

Indicated for salvage therapy for invasive aspergillosis

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Antimetabolites of Echinocandins

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Flucytosie-Nucleic acid inhibitor antimetabolite
Griseofulvin- Anti-mitotic

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Antimetabolite Mechanism

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Block fungal DNA and protein synthesis (Flucytosine)
fungal mitosis (Griseofulvin)
Fungistatic

Complications: bone marrow suppression, hallucinations

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Antivirals

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Obligate intracellular parasite

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Replication of DNA viruses

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Inhibition of viral DNA polymerase
Every anti-viral works here

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Enfuvirtide (T-20)

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Derived from the HIV envelope

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Ion Channel Blockers

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Amantadine
Rimantadine

ASA and acetaminophen decrease rimantadine plasma levels

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Acyclovir and Valcyclovir

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Specificity
Viral TK: HSV & VZV infected cells

Valacyclovir is a prodrug for acyclovir and is completely converted to acyclovir by first pass metabolism
Bioavailability of acyclovir is 3-5 times higher

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Ganciclovir

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Specificity-CMV
Clinical Uses: Tx of CMV retinitis in immunocompromised; prophylaxis

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Trifluridine

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Inhibitor of viral DNA polymerase AND cellular DNA polymerase

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Cidofovir

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Active against mutant viruses

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Nucleoside analogs-Anti HIV agents

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Competitive inhibitor of reverse transcriptase
Specifity: Blocks HIV replication and the infection of new cells, but they have little effect on cells that are already infected.

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Non-Nucleoside Analogs
NNRTI's

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Inhibit viral reverse transcriptase by inducing a conformational change in enzyme that causes enzyme inactivation
Active against HIV reverse transcriptase only

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Protease Inhibitor
Inhibit viral maturation

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HIV