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72 Cards in this Set
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antimicrobial drugs
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antibacterial, antifungal, and antiviral drugs
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antibiotic
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a substance that is produced by one microbe and inhibits the growth or viability of other microbes
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bactericidal
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Kills sensitive pathogens, number of viable pathogens drops rapidly
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bacteriostatic
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Inhibits the growth of bacteria and allows the immune system to eliminate the pathogen
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narrow spectrum drugs
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active against a single species or a limited group of pathogens
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extended spectrum drugs
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intermediate range of activity
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broad spectrum drugs
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active against a wide range of pathogen
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minimum inhibitory concentration
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lowest concentration of a drug that inhibits its bacterial growth
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concentration dependent killing rate
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concentration goes up the rate of killing goes up
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post antibiotic affect
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after an antibacterial drug is removed there is a persistent effect on bacterial growth
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mutation
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microbes can spontaneously mutate to a form that is resistant to a particular antimicrobial drug
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transferable resistance
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donation of genes that encode proteins responsible for resistance during bacterial conjugation
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resistance factors
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the genes that encode resistance proteins
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Laboratory Tests for Microbial Sensitivity
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culture and sensitivity
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General rule: Microbial sensitivity
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The peak serum concentration of a drug should be 4-10 times greater than the MIC in order for a pathogen to be susceptible to a drug
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Mechanisms of resistance
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Inactivation of the drug by microbial enzymes, decreased accumulation of the drug by the microbe, and Reduced affinity of the target macromolecule for the drug
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Pseudomonas Aeruginosa
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2 drug bug
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combination drug therapy
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Antagonistic, Additive, Indifferent and Synergistic
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Prophylactic Therapy
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Sterilization of diagnostic and surgical instruments, use of disinfectants, disinfection of skin and mucous membranes before invasive procedures
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Beta Lactam Drugs
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Penicillins and Cephalosporins and Carbapenems
MOA: Bind to and inhibit penicillin binding proteins (PBPs), enzymes that are responsible for cell wall synthesis |
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Penicillin Resistance
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1.Inactivation of the drugs by Beta-Lactamase
2.Reduced affinity of PBPs for the antibiotics 3.Decreased entry of the drugs into the bacteria through porins |
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Clostridium difficile
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Anaerobic, gram-positive, spore-forming, bacillus
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Beta-Lactamase Inhibitors
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Clavulanate, Augmentin
Inhibit Class A Beta-Lactamase MOA: surrogate substrates for Beta Lactamase |
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Methacillin Resistant Staphylococcus Aureus
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Staph- Gram Positive
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Cephalosporins
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Beta-Lactam ring + 2 or more R groups
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Vancomycin
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–Staphylococcus(including MRSA), Enterococci, Streptococci
–Serious infections or any susceptible MRSA-IV –C. difficile diarrhea: ORAL ONLY |
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Vancomycin Resistance Enterococci
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Two main types: E. Facecium or E. Faecalis
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Aminoglycosides
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Pharmacokinetics
–IV due to poor oral absorption –Excreted by Kidneys –Concentration dependent killing Spectrum: highly active against wide range of gram negative bacilli Resistance: Enzyme inactivation, decreased binding, decreased uptake |
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Tetracycline
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Pharmacokinetics: binds with divalent and trivalent cations
Spectrum: broad spectrum, bacteriostatic (gram + and gram neg) –USE: genital infections, Lyme disease, acne, cholera Resistance: has been used in animal feed around the world to induce weight gain which has contributed to some resistance |
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Macrolides
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Erythromycin, Azithromycin (Zithromax)
USE: gram –and gram + bacteria that cause upper respiratory infections and pneumonia, sinusitis, otitis media and bronchitis Resistance: decreased binding to 50S portion of the ribosome, enzymatic inactivation, and increased bacterial efflux |
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Zyvox
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MOA: binds to 50S and prevents the formation of the 70S initiation complex required for bacterial protein synthesis
Spectrum: •Bactericidal: streptococci •Bacteriostatic: enterococci and staphylococci |
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Cleocin
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Higher incidence of C. Difficile diarrhea
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Leprosy
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Infection of skin and peripheral nervous system
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Isoniazid
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Pharmacokinetics: Slow Acetylators
MOA: inhibits the synthesis of mycolic acid a mycobacterial cell wall component Spectrum: bactericidalto M. Tuberculosis USE: active and latentTB infections |
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Ethambutol
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Bacteriostatic
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Pyrazinamide
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Bactericidal
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Rifampin
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Broad spectrum antibiotic
MOA: prevents bacterial RNA and DNA synthesis USE: active TB, latent TB alternative to isoniazid, prophylaxis for several other bacterial diseases Resistance: higher tendency for resistance |
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Nucleoside Analogs
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Acyclovir (Zovirax), Valacyclovir (Valtrex)
MOA: prodrugs, inhibition of DNA polymerase, blocks DNA synthesis, blocks viral replication Resistance: not common USE: Herpes and shingles |
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Reverse Transcriptase Inhibitors
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NRTIs: converted to active metabolites (nucleotides) by host cell enzymes then incorporated into DNA, leads to DNA chain termination
NNRTIs: bind directly to and inhibits reverse transcriptase |
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NRTI
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Zidovudine (AZT)
Spectrum and Indications: HIV –AZT: reduces in utero transmission, needlestick prophylaxis Resistance: most likely when receiving single-drug therapy for 6 months or longer |
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NNRTI
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Efavirenz (Sustiva)
Resistance: never used alone or resistance develops |
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Protease Inhibitors
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Atazanavir (Reyataz)
MOA: bind the active site of protease enzyme and inhibit its proteolytic activity –Ritonavir: also inhibits the metabolism of other Pis |
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Drugs for Influenza
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Amantadine
MOA: block the M2 proton-selective ion channel and viral uncoatingin host cell, and therefore viral RNA transcription Spectrum/Use: prevention and treatment of influenza A Resistance: Significant resistance present, last line drugs |
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Drugs for Influenza: Neuraminidase Inhibitors
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Oseltamivir (Tamiflu)
MOA: Inhibition of the enzyme neuraminidase and prevents release of intact virions from host cell Spectrum: Influenza A & B |
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Proto-oncogenes
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stimulate cell division
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3 classes of genes
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1.Oncogenes
2.Tumor Suppressor Genes 3.DNA repair genes |
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Metastasis
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invasion of previously unaffected organs
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Angiogenesis
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formation of new blood vessels to support metastatic invasion and growth
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Antineoplastics
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MOAs: destroy malignant cells by
–Inhibiting cyclins, CDKs and growth factors (interference with cell replication) –Increase cancer cell apoptosis –Interference with supply and uptake of nutrients –Interfere with DNA and RNA inside the nucleus |
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Induction therapy
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produce a rapid reduction in the tumor cell burden
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consolidation therapy
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seeks to extend the initial remission
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maintenance therapy
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aims to sustain the remission
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Intermittent therapy
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allows the bone marrow and other normal host cells to recover between treatment courses, reduces toxicity levels
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Cytotoxic Agents: Antimetabolites
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Methotrexate
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Cytotoxic Agents: Alkylating agents
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Cisplatin
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Cytotoxic Agents: Antibiotic antineoplastic agents
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Doxorubicin
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Cytotoxic Agents: Mitotic inhibitors
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Vincristine
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Targeted drugs: Monoclonal Antibodies
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Rituximab
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Targeted drugs: Interferons
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Interferon-alpha-2b
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Targeted drugs: antineoplastic agents affecting hormonal balance
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Tamoxifen and Proscar
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Amphotericin B
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USE:
–systemic and subcutaneous fungal infections –Yeasts (not dermatophytes) Resistance: few reports of fungal resistance |
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Diflucan
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USES:
–topically to treat superficial fungal infections –Orally for more stubborn fungal infections (onychomycosis) –Systemic infections Spectrum and indications: –fungistatic or fungicidal –work on dermatophytes and yeasts |
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Lamisil
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Primarily for superficial dermatophyte infections
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Cancidas
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MOA: Inhibition of Beta-1,3-D-glucan
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Flagyl
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Spectrum : many protozoa and some bacteria
MOA: formation of free nitro-radicals that attack DNA and proteins |
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Quinine
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Indication: Malaria
Prevents replication |
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Ivermectin (Stromectol)
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MOA:
1.Binds to and increases permeability of chloride channels in nerve and muscle cells of invertebrates 2.Hyperpolarization of nerve or muscle cells 3.Paralysis and death USE: various worms, scabies, lice |
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Mebendazole (Vermox)
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MOA: alters the parasites ability to uptake glucose
USE: pinworms |
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Permethrin (Nix, Elimite)
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MOA: Disrupts Na+ channels in nerve cell membrane
USE: Lice and scabies |
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Malathion
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MOA: Cholinesterase inhibitor
USE: Lice |
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Antifolate Drugs
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Sulfamethoxazole
Pharmacokinetics: metabolites of sulfamethoxazole are less water soluble and they can accumulate in thekidneys and crystalize (crystalluria) Use: 1.UrinaryTract Infections 2.Ocular infections 3.Sulfadiazine-Burn cream to prevent skin infections |
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Fluoroquinolones
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Ciprofloxacin (Cipro), Moxifloxacin (Avelox)
Broadspectrum bactericidal activity, concentration dependent killing MOA: inhibit DNA gyrase and Topoisomerase IV Pharmacokinetics: bind with divalent and trivalent cations Spectrum: gram negative USES: UTI –retain gram negative activity and add gram positive |