Ketoconazole
- antifungal
- first oral antifungal drug
- toxic to liver so now usually replaced with itraconazole or fluconazole
- best absorbed at highly acidic levels, so antacids or other causes of decreased stomach acid levels will lower the drugs absorption when taken orally
- the side-effects are sometimes used to treat non-fungal problems. The decrease in testosterone caused by the drug makes it useful for treating prostate cancer and for preventing post operative erections following penile surgery
Mefloquine
- Anti-protozoan drug
- used for malaria
- used to treat resistant cases
- semi-synthetic
Praziquantel
-Anti-helminthic drug
used for flukes + tapeworms
Niclosamide
- Anti-helminthic drug
- used for tapeworms
- destroys scolex and adjoining proglottids of tapeworms
Polymyxins
- Drug that acts on Cell Membrane
- Cause loss of selective permeability in cell membrane
- Gram (-)
- Topical only
Rifampin
- drug that affects Nucleic Acid Sythesis
- Inhibits RNA polymerase
- used to treat TB and leprosy
Quinolones (ciprofloxacin)
(DNA)
- inhibits replication and transcription
- inhibits gyrase (unwinding enzyme)
Protein Synthesis Inhibitors acting on Ribosomes: Site of Action 50S subunit
- Chloramphenicol
- Erythromycin
- Clindamycin
- Streptogramin (Synercid)
Protein Synthesis Inhibitors acting on Ribosomes: Site of action 30S subunit
- Aminoglycosides
- Gentamicin (treat pseudomonas)
- Streptomycin
- Tetracyclines
Protein Synthesis Inhibitors acting on Ribosomes: Both 30S and 50S subunits
blocks initiation of protein synthesis
-Linezolid (zyvox)
Linezolid (Zyvox)
blocks initiation of protein synthesis on ribosomes
What drugs block pathways and inhibit metabolism on Ribosomes?
- Sulfonamides (sulfa drugs)
- Trinethoprim
Sulfonamides and Trinethoprim do what on ribosomes?
block pathways and inhibit metabolism on ribosomes
Penicillins
-Drugs that act on cell wall
-Organic chemical structure includes beta-lactam ring
-Originally isolated from mold Penicillium chrysogenum
-Bactericidal
-Narrow Spectrum
-Problems: allergic reactions and development of bacterial resistance to drug through beta-lactamase (penicillinase)
-Natural:
>Penicillin G (gram +)(requires injection)
>Penicillin V (gram +)(oral administration)
-Semisynthetic:
>Methicillin (used until MRSA)
>Ampicillin (Broad spectrum)
>Amoxicillin (Broad spectrum; combined with inhibitor of penicillinase)
Penicillin G
- Natural Penicillin drug
- Gram (+)
- requires injection
- Narrow Spectrum
- Best drug of choice when bacteria are sensitive; low cost; low toxicity
- Disadvantages: can be hydrolyzed by penicillinase; allergies occur; requires injection
Penicillin V
- Natural Penicillin drug
- Gram (+)
- Oral administration
- Narrow spectrum
- Good absorption from intestine; otherwise, similar to penicillin G
- Disadvantages: hydrolysis by penicillinase; allergies
Methicillin
- Semi-synthetic Penicillin drug
- used until MRSA
- Narrow spectrum
- not usually susceptible to penicillinase
- Disadvantages: poor absorption, allergies; growing resistance
Ampicillin
- Semi-synthetic Penicillin drug
- Broad Spectrum
- works on gram (-) bacilli
- Disadvantages: can be hydrolyzed by penicillinase; allergies; only fair absorption
Amoxicillin
- Semi-synthetic Penicillin drug
- Broad spectrum; combined with inhibitor of penicillinase
- For gram (-) infections; good absorption
- Disadvantages: hydrolysis by penicillinase; allergies
Cephalosporins
-Drugs that act on Cell Wall
-Originally isolated from the mold cephalosporium
-Bactericidal
-Broader spectrum than penicillin
>Cephalothin (first generation; requires injection)
>Cefixime (third generation; oral administration)
Cephalosporins: Cephalothin
- first generation of cephalosporins
- requires injection
Cephalosporins: Cefixime
- third generation of cephalosporins
- oral administration
Vancomycin
- Drug that act on Cell Wall
- used for life-threatening, methicillin-resistant staphylococcal infections (MRSA) and Enterococcus; except VRE
Isoniazid (INH)
inhibits synthesis of mycolic acid in cell wall of Mycobacterium
Bacitracin
- Topical
- Produced by B. subtilis
- Component of triple antibiotic ointments
Rifampin
- Drug that affects Nucleic Acid Synthesis
- inhibits synthesis of mRNA
- used to treat TB and leprosy
Aminoglycosides
-Drugs that inhibit Protein Synthesis
-produced by Streptomyces
-act on 30S subunit in ribosomes
>Streptomycin:
-narrow spectrum; including Mycobacterium
-hearing loss
>Gentamicin:
-narrow spectrum
-including pseudomonas
>Neomycin:
-broad spectrum
-topical use
Aminoglycosides: Streptomycin
- drug that inhibits Protein Synthesis
- produced by streptomyces
- narrow spectrum
- including Mycobacterium
- hearing loss
- act on 30S subunit in ribosomes
Aminoglycosides: Gentamicin
- drug that inhibits Protein Synthesis
- produced by streptomyces
- narrow spectrum
- including pseudomonas
- act on 30S subunit in ribosomes
Aminoglycosides: Neomycin
- drug that inhibits Protein Synthesis
- produced by streptomyces
- broad spectrum
- topical use
Tetracyclines
- Drugs that inhibit Protein Synthesis
- produced by streptomyces
- very broad spectrum
- Drug of choice for Rickettsias, Chlamydia, Propionibacterium
- Harms microbiota
- Animal feed additive
- Harms teeth of children
- Photosensitive
- act on 30S subunit in ribosomes
Chloramphenicol
- Drug that inhibits Protein Synthesis
- produced by streptomyces
- very broad spectrum
- possibly toxic
- Act on 50S subunit in Ribosomes
Erythromycin
- Drug that inhibits Protein Synthesis
- broad spectrum
- alternative to Penicillin for penicillin-resistant bacterium and in case of penicillin allergy in patient
- Act on 50S subunit in ribosomes
Azithromycin (Z pack)
- Drug that inhibits Protein Synthesis
- semi-synthetic
- broader spectrum
- better tissue penetration than Erythromycin
Telithromycin (Ketek)
- Drug that inhibits Protein Synthesis
- semi-synthetic
Clindamycin
- Drug that inhibits Protein Synthesis
- used primarily for intestinal infection by anaerobes
- Acts on 50S subunit in ribosomes
Drugs that Interfere with Metabolism/ Enzyme Activity
- Sulfonamides
- Trimethoprim
Amphotericin B
- Antifungal Drug
- systemic
- topical
- Nystatin (topical)
Azoles
-Antifungal drugs >Ketoconazole (Nizoral) >Fluconazole (Diflucan) >Miconazole (Monistat) >Itraconazole (Sporanox)
Flucytosine
- Antifungal drug
- many fungi resistant so combined with amphotericin
Echinocandins
- Antifungal drug
- capsofungin inhibits fungal cell wall (chitin)
Allylamines
- Antifungal Drug
- Terbinafine (Lamisil)
- Systemic
- Topical
- inhibits ergosterol
Chloroquine
- Anti-protozoan drug
- prophylaxis
- suppression of acute cases of malaria
- affect nucleic acid synthesis
Primaquine
- Anti-protozoan drug
- relapsing cases of malaria
Metronidazole (Flagyl)
- Anti-protozoan drug
- Amobeasis, Giardiasis, Trichomoniasis
- also used for anaerobic bacteria
Mebendazole
- Anti-helminthic drug
- broad spectrum
- intestinal roundworms
- work locally in intestines to inhibit microtubule of worms, eggs and larvae
Pyrantel, piperazine
- Anti-helminthic drug
- paralyze muscles of intestinal round worms
Ivermectin
- Anti-helminthic drug
- veterinary treatment for tapeworms and flukes
- used for humans for Strongyloidiosis
Antiviral Drugs
-most antiviral drugs have limited spectrum activity
-most are designed to block a step in viral multiplication
>barring penetration into host cell
>blocking replication, transcription, and/or translation of viral genetic material
>preventing the normal maturation of viral particles
Influenza Drugs
-Antiviral Drugs
>Amantadine (block entry of influenza virus by interfering with fusion of virus with cell membrane)
>Relenza
>Tamiflu
(Relenza + Tamiflu both stop the actions of influenza neuraminidase, required for entry of virus into cell)
Herpes Drugs
- Antiviral Drugs
- Acyclovir (Zovirax)(both terminates DNA replication in herpes virus); Valacyclovir (Valtrex); Famciclovir (Famvir)
- Ganciclovir (Cytovene) for CMV; an analog of guanine
- Valtrex and Famvir only active in virus infected cells
Analog
antiviral agents mimic structure of nucleotides
HIV drugs
- Antiviral drugs
- interfere with action of reverse transcriptase enzyme
Maravoc
- Antiviral Drug
- covers up receptors
Fuzeon
- Antiviral Drug
- prevents viral envelope from fusing with host
- prevents binding of viral receptors to cell receptor which blocks fusion of virus with cell
Interferons
- Antiviral Drugs
- Glycoproteins produced by viral infected cells
- (Fibroblasts, Leukocytes)
Cell Wall Inhibitors
- Penicillins
- Vancomycin
- Bacitracin
- Isoniazid
Drugs that Act on Cell Wall
- Penicillins
- Cephalosporins
- Vancomycin
- Isoniazid (INH)
- Bacitracin
Drugs that Affect Nucleic Acid Synthesis
- Fluoroquinolones (Ciprofloxacin)
- Rifampin
- Chloroquine
Drugs that inhibit Protein Synthesis
- Aminoglycosides
- Tetracyclines
- Chloramphenicol
- Erythromycin
- Azithromycin (Z pack)
- Telithromycin (Ketek)
- Clindamycin
Antifungal Drugs List
- Amphotericin B
- Azoles
- Flucytosine
- Echinocandins
- Allylamines
Anti-protozoan Drugs List
- Quinine
- Chloroquine
- Mefloquine
- Primaquine
- Metronidazole (Flagyl)
Anti-helminthic Drug List
- Mebendazole
- Pyrantel, piperazine
- Niclosamide
- Praziquantel
- Ivermectin
Anti-viral Drugs List
- Influenza drugs
- Herpes drugs
- HIV drugs
- AZT
- Maravoc
- Fuzeon
- Interferons