Professional Documents
Culture Documents
Microbiology Pharmacology
Shan Nanji
+ Aminoglycosides 2
“amI-NOt-glycosides”
MOA: Bacteriocidal
n Block _____________________
n Inhibit Formation Of Initiation Complex
And Cause _____________________
n Of mRNA
n _____________________
“amI-NOt-glycosides”
n RESISTANCE:
n Transferase Enzymes
Inactivate the Drug by:
1) Acetylation
2) Phosphorylation
3) Adenylation
Aminoglycosides
“amI-NOt-glycosides”
S/E:
n _____________________ Especially with
Cephalosporins
n Ototoxicty– Especially when used with
_____________________
n Teratogen
Clinical Use:
n SevereGram (-) Rod Infections
n Synergistic with B-lactam Antibiotics
Aminoglycosides
“amI-NOt-glycosides”
n Tularemia
Tetracyclines “+-etracyclins”
MOA: Bacteriostatic
n Bind to 30s
n _____________________
n Limited CNS Penetration
n DO NOT take with Milk, Antacids, or an Iron Containing Prep
n RESISTANCE:
n Decrease Uptake Into Cells or
n Increased Efflux Out of Cells by
Plasmid Encoded Transport Pumps
Tetracyclines “+-etracyclins”
MOA: Bacteriostatic
Tetracyclines “+-etracyclins”
n RESISTANCE:
Tetracyclines “+-etracyclins”
Clinical Use:
n _____________________
n Accumulates_____________________
n Rickettsia
n Chlamydia
Tetracyclines “+-etracyclins”
S/E:
n GI Distress
n Discoloration of Teeth
n Inhibition of Bone Growth in Children
n Photosensitivity
Tetracyclines “+-etracyclins”
n _____________________
n _____________________
Tetracyclines “+-etracyclins”
n Doxycycline
n Hepatic Excretion
n _____________________
n ADH Antagonist
n Can be Used a Diuretic in SIADH
n Minocycline
n Effective against acne
n “Mi–NO like acne on my woman!”
Penicillin
MOA:
1. Bind Penicillin-Binding Proteins
2. Block Transpeptidase Cross Linking of Peptidoglycan
3. Activate Autolytic Enzymes
n RESISTANCE:
n Beta Lactamases Cleave Beta Lactam Ring
Penicillin
Clinical Use:
n Mostly for Gram (+) organisms
n S.Pneumo
n S.Pyogenes
n Actinomyces
Syphilis
n
n Bacteriocidal for:
n Gram (+) Cocci
n Gram (+) Rods
n Gram (–) Cocci
n Sphirocetes
Penicillin
S/E:
n Hypersensitivity reactions
n Hemolytic anemia
Penicillin
n Penicillin G
n IV Form
n Penicillin V
n Oral
MOA:
n Same As Penicillins
n But Narrow Spectrum
n Penicillinase Resistant
n Due To Bulkier R-group
1. Bind Penicillin-Binding Proteins
2. Block Transpeptidase Cross Linking of Peptidoglycan
3. Activate Autolytic Enzymes
Clinical Use:
n S.Aureus
n Except MRSA
n Resistance Due To Altered Penicillin
Binding Protein Target Site
S/E:
n Hypersensitivity Reactions
n Methicillin – Interstitial Nephritis
Penicillinase-Resistant Penicillins
n Methicillin
n Interstitial Nephritis
n Nafcillin
n Dicloxacillin
Aminopenicillins
MOA:
n SAME AS PENICILLINS
n BUT WIDER SPECTRUM
Aminopenicillins
Clinical Use:
n Extended Spectrum Penicillins
n H-Influenza
n E.Coli
n Salmonella
n Shigella
n Enterococci
Aminopenicillins
S/E:
n Hypersensitivity Reactions
n Ampicillin – Rash
Aminopenicillins
n Ampicillin
n Amoxicillin
n amOxicillin = greater O-ral bioavailability
Anti-Pseudomonals
MOA:
n Same as Penicillins but Extended Spectrum
1. Bind Penicillin Binding Proteins
2. Block Transpeptidase Cross Linking of Peptidoglycan
3. Activate Autolytic Enzymes
Anti-Pseudomonals
Clinical Use:
n Pseudomonas And Gram (-) Rods
n Susceptible To Penicillinase
S/E:
n Hypersensitivity Reactions
Anti-Pseudomonals
n Ticarcillin
n Carbenicillin
n Piperacillin
n _____________________
n Methicillin – Interstitial Nephritis
n Nafcillin
n Dicloxacillin
n Anti-Pseudomonals
n Ticarcillin
n Carbenicillin
n Piperacillin
Beta-Lactamase Inhibitors
n Sul_____________________
n Tazo_____________________
Cephalosporins
MOA:
Cephalosporins
S/E:
n Hypersensitivity Reactions
n _____________________
n Cross Hypersensitivity with _____________________
n in 5-10% of Patients
n Increase ____________________ of Aminoglycosides
Cepaholosporins
n Cefazo_____
n Cepha_____in
Cepaholosporins
Cepaholosporins
n Ce____lor – “CeFAKlor”
n Ce____itin
n Ce____oxime
Cephalosporins
n Third Generation
n Serious Gram (-) infections resistant to other B-lactams
n Cef___axone
n Meningitis
n Gonorrhea
n Cefo___ime
n Cef___idime
n Pseudomonas
Cephalosporins
n Fourth Generation
n Increase activity against Pseudomonas and
Gram (+) Organisms
n Cefepime
Chloramphenicol
n MOA:
n Resistance:
n Plasma Encoded Acetyltransferase that
Inactivates Drug
Chloramphenicol
n Clinical Use:
n MENingitis
n ChloraMphENicol
n S/E:
n Dose Dependent ______________
n Dose Independent ______________
n ______________
Clindamycin
n MOA:
Clindamycin
n Clinical Use:
n Anaerobic infections
n S/E:
n ______________
n Fever
n Diarrhea
Macrolides “mac-RO-SLIDES”
MOA: Bacteriostatic
RESISTANCE:
n Methylation of the rRNA Binding Site
n At the 23s of the 50s Subunit
Macrolides “mac-RO-SLIDES”
Clinical Use:
n Atypical Pneumonias
n Mycoplasma
n Chlamydia
n Legionella
n URI
n STDs
n Gram + Cocci
n Streptococcal Infections In Patients Allergic To Penicillin
n Also Neisseria
Macrolides “mac-RO-SLIDES”
S/E:
n Prolonged ____________(Erythromycin)
n GI Discomfort
n ______________
n Eosinophilia
n Theophyllines
Flouroquinolones
MOA: Bacteriocidal
RESISTANCE:
n Chromosome encoded mutation in DNA Gyrase
Flouroquinolones
n Ciprofloxacin
n Norfloxacin
n Levofloxacin
n Ofloxacin
n Sparfloxacin
n Moxifloxacin
n Gatifloxacin
n Enoxacin
n Nalididixic Acid (quinolone)
Flouroquinolones
Clinical Use:
n Gram (-) Rods Of Urinary And GI Tracts (Pseudomonas),
Neisseria
n Some Gram + Organisms
Flouroquinolones
S/E:
n GI Upset
n Superinfections
n Skin Rashes
n Headache
n Dizziness
n C/I In Pregnant And Children
Causes Cartilage Damage
n
Metronidazole
MOA: Bacteriocidal and Anti-protozoal
Metronidazole
Clinical Use:
n GET GAP on the Metro!
Metronidazole
S/E:
n Metallic Taste
n Disulfiram Reaction With Alcohol
n Flushing
n Sweating
n Nausea
Aztreonam
MOA:
n Binds to PBP3, Preventing Peptidoglycan Crosslinking
Imipenem+Cilastatin, Meropenem
MOA:
n Β-Lactamase Resistant Carbapenem
n Cilastatin
n ____________________________
Imipenem+Cilastatin, Meropenam
S/E:
n CNS Toxicity
n Seizures
n GI Distress
n Skin Rash
Vancomycin
MOA:
n Inhibits Cell Wall Peptidoglycan Formation
n Enterococci
Shan Nanji - NanjiMD@gmail.com
+ 55
Vancomycin
n S/E:
n Nephrotoxicity
n Ototoxicity
n Thrombophlebitis
n “Red Man Syndrome”
n Flushing
Sulfonamides
- Sulfamethoxazole(SMX), Sulfisoxazole, Sulfadiazine
MOA:
n Bacteriostatic
n Inhibit Dihydropteroate Synthase
n Through PABA Antimetabolites
Sulfonamides
- Sulfamethoxazole(SMX), Sulfisoxazole, Sulfadiazine
n S/E:
n Hypersensitivity Reactions
n Nephrotoxicity
n Photosensitivity
n Kernicterus
n Infants
n Hemolysis
n If G6PD Deficient
n Resistance:
n Altered Enzyme
n Decreased Uptake
n Increased PABA Synthesis
Trimethoprim
- TMP
MOA:
n Bacteriostatic
Trimethoprim
- TMP
n S/E:
n Megaloblastic Anemia
n Leukopenia
n Granulocytopenia
n Possible use of ______________ to Alleviate
Rifampin
MOA:
n Inhibits ______________
n Rapid Resistance if Used By Itself
n Leprosy
n Meningococcal Prophylaxis
Rifampin
n S/E:
n ORANGE, orange, ORANGE Body Fluids!
n Hepatotoxicity
Isoniazid (INH)
MOA:
n Decrease Synthesis of Mycolic Acids
n KatG (Bacterial Catalase-Peroxidase)
Needed to Activate Isoniazid
n Clinical Use:
n Mycobacterium Tuberculosis
n As Prophylaxis
Isoniazid (INH)
n S/E:
n Neurotoxicity
Pyrazinamide
MOA:
n Unknown
n Clinical Use:
n Mycobacterium Tuberculosis
n S/E:
n Hyperuricemia
n Hepatotoxicity
Ethambutol
MOA:
n Blocks Arabinosyltransferase
n Decreases Carbohydrate Polymerization of Cell Wall
n Clinical Use:
n Mycobacterium Tuberculosis
n S/E:
n Optic Neuropathy
n Red/Green Color Blindness
Mycobacterium Tuberculosis
n Treatment Regimen:
n Rifampin
n Isoniazid
n Pyrazinamide
n Ethambutol
Amphotericin B (Antifungal)
MOA:
n Binds ______________
n Forms ______________
n Clinical Use:
n Cryptococcus
n Blastomyces
n Coccidioides
n Histoplasma
n Candida
n Mucor
n S/E:
n Optic Neuropathy
n ______________ Color Blindness
Amphotericin B (Antifungal)
n S/E:
n Fever
n Chills
n HypOtension
n Nephrotoxicity
n Arrhythmias
n Anemia
n IV Phlebitis
Nystatin (Antifungal)
MOA:
n Binds Ergosterol
n Forms Leaky Membrane Pores
n Clinical Use:
n Oral Candidiasis
n Topical:
n Diaper Rash
Azoles (Antifungal)
MOA:
n Inhibit Fungal Sterol Synthesis
n By Inhibition of P-450
n Clinical Use:
n Cryptococcal Meningitis in AIDS
n Blastomyces
n Coccidioides
n Histoplasma
n Candida
n S/E:
n Inhibition of Testosterone Synthesis (Gynecomastia)
n Liver Dysfunction (Inhibits P-450)
Flucytosine (Antifungal)
MOA:
n Inhibits DNA and RNA Synthesis
n Converted to ______________ by ______________
n Clinical Use:
n Cryptococcal Meningitis
n Combined with Amphotericin B
n S/E:
n Bone Marrow Suppression
Caspofungin, Micafungin
(Antifungals)
MOA:
n Inhibit Cell Wall Synthesis
n By Inhibition of β-glucan
n Clinical Use:
n Invasive Aspergillosis
n Candida
n S/E:
n GI Upset
n Flushing
Terbinafine (Antifungals)
MOA:
n Inhibits Fungal Squalene Epoxidase
n Clinical Use:
n Dermatophyte Infections
n S/E:
n Abnormal Liver Function Tests (LFT’s)
n Visual Disturbances
Griseofulvin (Antifungals)
MOA:
n Interferes with Microtubule Function during Mitosis
n Clinical Use:
n Superficial
Infections (Oral Treatment)
n Dermatophyte Infections
n S/E:
n Carcinogenic
n Teratogenic
n Confusion
n Headaches
n Induce P-450
Chloroquine (Antiprotozoan)
MOA:
n Blocks Detoxification of Heme
n Heme Accumulates
n Clinical Use:
n Plasmodial Infections
n EXCEPT P. Falciparum
n S/E:
n Retinopathy
Antiprotozoan Therapy
n Pyrimethamine
n Toxoplasmosis
Antihelminthic Therapy
n Pyrimethamine
n PyrantelPamoate
n Ivermectin
n Diethylcarbamazine
n Praziquantel
n Treats Flukes
n Schistosoma
Zanamivir, Oseltamivir
(AntiVirals)
MOA:
n Inhibit Influenza Neuraminidase
n Decreased Viral Release
n Clinical Use:
n Influenza A and B
n Prevention and/or Treatment
n S/E:
n Retinopathy
Ribavirin (AntiVirals)
MOA:
n Inhibit Synthesis of Guanine Nucleotides
n Through Competitively Inhibiting IMP Dehydrogenase
n Clinical Use:
n RSV
n Chronic Hepatitis C
n S/E:
n Hemolytic Anemia
n Extremely Teratogenic
n Clinical Use:
n _____ (Most Infections)
n _____
n Resistance
n Viral Thymidine Kinase Mutation
Ganciclovir (AntiVirals)
MOA:
n Inhibits Viral DNA Polymerase
n ______________ causes Phosphorylation
n Cellular Kinases Add Additional Phosphates
n Clinical Use:
n CMV
n S/E:
n Leukopenia
n Neutropenia
n Thrombocytopenia
n Nephrotoxicity
n Resistance
n CMV DNA Polymerase Mutation
n Absent Viral Kinase
Shan Nanji - NanjiMD@gmail.com
+ 82
Foscarnet (AntiVirals)
MOA:
n Inhibits Viral DNA Polymerase
n Binds to Pyrophosphate Binding Site of Enzyme
n ______________
n Clinical Use:
n CMV Retinitis If Ganciclovir Fails
n S/E:
n Nephrotoxicity
n Resistance
n DNA Polymerase Mutation
Cidofovir (AntiVirals)
MOA:
n Inhibits Viral DNA Polymerase
n No Viral Kinase Phosphorylation Required
n ______________
n Clinical Use:
n CMV Retinitis If Ganciclovir Fails
n Acyclovir-Resistant HSV
n S/E:
n Nephrotoxicity
n To Reduce Nephrotoxicity:
n Coadminister Probenecid and IV Saline
Shan Nanji - NanjiMD@gmail.com
+ 84
AIDS - NRTI
MOA :
n Comp/Rev. Inhibit nucleotide binding to reverse
transcriptase
n Needs Thymidine Kinase to be active.
n S/E :
n Bone Marrow Suppression
(reversed with G-CSF and EPO)
n Peripheral Neuropathy
n Lactic Acidosis (nucleosides)
n Rash (non-nucleosides)
n Megaloblastic Anemia (ZDV)
AIDS - NRTI
n Abacavir
n Tenofovir – Does NOT need to be phosphorylation
n Zalcita_____
n Emtricita___
n Lamivu___
n Zidovu___ – Used for general prophylaxis and
during pregnancy to reduce transmission risk.
n Decreases vertical transmission. Blasts your BM
n Stavu___
n Didano___
n Painful neuropathy and pancreatitis
Protease Inhibitors
“-navir”
MOA:
n Inhibit pol gene
-> prevents maturation
n S/E:
n Hyperglycemia
n GI Intolerance
n Lipodystrophy
Protease Inhibitors
n LopiNAVIR
n AtzaNAVIR
n FosampreNAVIR
n SaquiNAVIR
n ______
n Can cause crystillization in the urine
n ______
n Liver disease
NNRTI
MOA:
n Bind to Reverse Transcriptase at a Different Site
n Do Not Need Thymidine Kinase to be Activated.
n S/E :
n Bone Marrow Suppression
(reversed with G-CSF and EPO)
n Peripheral Neuropathy
NNRTI
n Ne___apine
n Efa___enz
n Dela___dine
Integrase Inhibitor
n _________
MOA:
n Inhibits HIV Genome Integration
into Host Cell Chromosome by
Reversibly Inhibiting HIV Integrase
n S/E:
n Hypercholesterolemia