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72 Cards in this Set

  • Front
  • Back
antimicrobial drugs
antibacterial, antifungal, and antiviral drugs
antibiotic
a substance that is produced by one microbe and inhibits the growth or viability of other microbes
bactericidal
Kills sensitive pathogens, number of viable pathogens drops rapidly
bacteriostatic
Inhibits the growth of bacteria and allows the immune system to eliminate the pathogen
narrow spectrum drugs
active against a single species or a limited group of pathogens
extended spectrum drugs
intermediate range of activity
broad spectrum drugs
active against a wide range of pathogen
minimum inhibitory concentration
lowest concentration of a drug that inhibits its bacterial growth
concentration dependent killing rate
concentration goes up the rate of killing goes up
post antibiotic affect
after an antibacterial drug is removed there is a persistent effect on bacterial growth
mutation
microbes can spontaneously mutate to a form that is resistant to a particular antimicrobial drug
transferable resistance
donation of genes that encode proteins responsible for resistance during bacterial conjugation
resistance factors
the genes that encode resistance proteins
Laboratory Tests for Microbial Sensitivity
culture and sensitivity
General rule: Microbial sensitivity
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
Mechanisms of resistance
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
Pseudomonas Aeruginosa
2 drug bug
combination drug therapy
Antagonistic, Additive, Indifferent and Synergistic
Prophylactic Therapy
Sterilization of diagnostic and surgical instruments, use of disinfectants, disinfection of skin and mucous membranes before invasive procedures
Beta Lactam Drugs
Penicillins and Cephalosporins and Carbapenems

MOA: Bind to and inhibit penicillin binding proteins (PBPs), enzymes that are responsible for cell wall synthesis
Penicillin Resistance
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
Clostridium difficile
Anaerobic, gram-positive, spore-forming, bacillus
Beta-Lactamase Inhibitors
Clavulanate, Augmentin
Inhibit Class A Beta-Lactamase

MOA: surrogate substrates for Beta Lactamase
Methacillin Resistant Staphylococcus Aureus
Staph- Gram Positive
Cephalosporins
Beta-Lactam ring + 2 or more R groups
Vancomycin
–Staphylococcus(including MRSA), Enterococci, Streptococci
–Serious infections or any susceptible MRSA-IV
–C. difficile diarrhea: ORAL ONLY
Vancomycin Resistance Enterococci
Two main types: E. Facecium or E. Faecalis
Aminoglycosides
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
Tetracycline
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
Macrolides
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
Zyvox
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
Cleocin
Higher incidence of C. Difficile diarrhea
Leprosy
Infection of skin and peripheral nervous system
Isoniazid
Pharmacokinetics: Slow Acetylators

MOA: inhibits the synthesis of mycolic acid a mycobacterial cell wall component

Spectrum: bactericidalto M. Tuberculosis

USE: active and latentTB infections
Ethambutol
Bacteriostatic
Pyrazinamide
Bactericidal
Rifampin
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
Nucleoside Analogs
Acyclovir (Zovirax), Valacyclovir (Valtrex)

MOA: prodrugs, inhibition of DNA polymerase, blocks DNA synthesis, blocks viral replication

Resistance: not common

USE: Herpes and shingles
Reverse Transcriptase Inhibitors
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
NRTI
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
NNRTI
Efavirenz (Sustiva)

Resistance: never used alone or resistance develops
Protease Inhibitors
Atazanavir (Reyataz)

MOA: bind the active site of protease enzyme and inhibit its proteolytic activity
–Ritonavir: also inhibits the metabolism of other Pis
Drugs for Influenza
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
Drugs for Influenza: Neuraminidase Inhibitors
Oseltamivir (Tamiflu)

MOA: Inhibition of the enzyme neuraminidase and prevents release of intact virions from host cell

Spectrum: Influenza A & B
Proto-oncogenes
stimulate cell division
3 classes of genes
1.Oncogenes
2.Tumor Suppressor Genes
3.DNA repair genes
Metastasis
invasion of previously unaffected organs
Angiogenesis
formation of new blood vessels to support metastatic invasion and growth
Antineoplastics
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
Induction therapy
produce a rapid reduction in the tumor cell burden
consolidation therapy
seeks to extend the initial remission
maintenance therapy
aims to sustain the remission
Intermittent therapy
allows the bone marrow and other normal host cells to recover between treatment courses, reduces toxicity levels
Cytotoxic Agents: Antimetabolites
Methotrexate
Cytotoxic Agents: Alkylating agents
Cisplatin
Cytotoxic Agents: Antibiotic antineoplastic agents
Doxorubicin
Cytotoxic Agents: Mitotic inhibitors
Vincristine
Targeted drugs: Monoclonal Antibodies
Rituximab
Targeted drugs: Interferons
Interferon-alpha-2b
Targeted drugs: antineoplastic agents affecting hormonal balance
Tamoxifen and Proscar
Amphotericin B
USE:
–systemic and subcutaneous fungal infections
–Yeasts (not dermatophytes)

Resistance: few reports of fungal resistance
Diflucan
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
Lamisil
Primarily for superficial dermatophyte infections
Cancidas
MOA: Inhibition of Beta-1,3-D-glucan
Flagyl
Spectrum : many protozoa and some bacteria

MOA: formation of free nitro-radicals that attack DNA and proteins
Quinine
Indication: Malaria

Prevents replication
Ivermectin (Stromectol)
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
Mebendazole (Vermox)
MOA: alters the parasites ability to uptake glucose

USE: pinworms
Permethrin (Nix, Elimite)
MOA: Disrupts Na+ channels in nerve cell membrane

USE: Lice and scabies
Malathion
MOA: Cholinesterase inhibitor

USE: Lice
Antifolate Drugs
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
Fluoroquinolones
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