Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
180 Cards in this Set
- Front
- Back
What is a chemical selective destruction of invading organisms?
|
Chemotherapy
|
|
What is the ratio of toxic dose:effective dose?
|
Therapeutic Index
|
|
What type of chemotherapy stems from the concept that substances derived from one living thing may serve to kill other living things?
|
Antibiotic Chemotherapy
|
|
What drug was discovered in 1936 and began the modern era of chemotherapy?
|
Sulfanilamide
|
|
How are chemotherapeutic agents classified?
|
According to their Mechanism of Action
|
|
What type of chemotherapeutic agents inhibit bacterial cell wall synthesis?
|
Penicillin
Cephalosporins Vancomycin Bacitracin Cycloserine |
|
What type of chemotherapeutic agents act directly on the cell membrane?
|
Polyeene Antifungal Agents:
Nystatin Amphotericin B |
|
What types of antibacterial agents affect the function of bacterial ribosomes to inhibit protein synthesis, and are bacteriostatic?
|
Chloramphenicol
Tetracyclines |
|
What types of antibacterial agents affect the function of bacterial ribosomes to inhibit protein synthesis, and are bacteriocidal?
|
Streptomycin
|
|
What types of chemotherapeutic agents affect nucleic acid metabolism?
|
Rifampin (DNA dependent RNA polymerase)
Fluoroquinolones - Ciprofloxacin |
|
What types of chemotherapeutic agents block metabolic steps essential to a microorganism?
|
<u>Antimetabolites</u>:
Sulfonamides Trimethoprin |
|
What chemotherapeutic agent can be either bacteriocidal or bacteriostatic depending on the environment?
|
Sulfonamides
|
|
What generally happens when you combine two bacteriostatic agents?
|
Produce an Additive effect
|
|
What generally happens when you combine 1 bacteriocidal and 1 bacteriostatic agent?
|
Generally results in antagonism
|
|
What generally happens when you add two bacteriocidal agents?
|
Generally results in a synergistic effect.
|
|
When is a microorganism said to be resistant?
|
When the concentration of the drug required to weaken or kill the microorganism is greater than can be tolerated by the host.
|
|
What type of resistance occurs in the absence of selective pressure?
|
De Novo (Intrinsic) Resistance
|
|
What are six mechanisms of resistance from chemotherapeutic agents?
|
1) Absence of Target (Ergosterol's absent)
2) Alterations in Target (Pen. Binding Protein Alterations) 3) Low concentration at target (Interference with membrane passage) 4) Lack of metabolic activation (Antifungal Flucytosine -> Fluorouracil) 5) Inactivation (Penicillinases) 6) Escape from Effect (Alternate Metabolic Pathways) |
|
What condition must be considered when prescribing sulfonamides and chloramphenicol?
|
Glucose-6-Phosphate Dehydrogenase Deficiency (May produce Hemolysis)
|
|
What antibiotic produces hearing loss in newborn when taken during pregnancy?
|
Streptomycin
|
|
What log cell kill is required to cure microbial infections?
|
2 (99% of population is killed)
|
|
What was the first effective chemotherapeutic agent employed systemically?
|
Sulfonamides
|
|
What types of bacteria do sulfonamides target?
|
Broad-Spectrum - Gram + and Gram -
|
|
What is the mechanism of action of sulfonamides?
|
They are structural analogs and competitive antagonists of PABA (Para-Aminobenzoic Acid)
|
|
What are sulfonamides often used in combination with?
|
Trimethoprin
|
|
How do sulfonamides not interfere with host metabolism?
|
Mammalian cells use preformed folic acid.
|
|
Which drug inhibits dihydrofolate reductase and prevents the transformation of dihydrofolate to tetrahydrofolate?
|
Trimethoprim
|
|
How is resistance to sulfonamides presented?
|
Increased synthesis of PABA
Alterations in enzyme that utilizes PABA Increased capacity to destroy or inactive the drug Development of an alternative metabolic pathway for synthesis of essential metabolites |
|
Where are sulfonamides absorbed?
|
Gut
|
|
Is the level of sulfonamides in urine higher or lower than serum levels?
|
10-25 (?) higher
|
|
Should you use sulfonamides on a patient with 6-glucose phosphate dehydrogenase deficiency?
|
No, it could produce acute hemolytic anemia
|
|
Sulfadiazine
Sulfamerazine Sulfamethazine Trisulfapyrimidines Sulfisoxazole and Sulfamethoxazole are what types of drugs? |
Sulfonamides
|
|
What sulfonamide is used routinely for urinary tract infection?
|
Sulfisoxazole
|
|
Why are long-acting sulfonamides not available in the US any longer?
|
Due to the high incidence of Stevens-Johnson syndrome
|
|
What is the mechanism of Trimethoprim?
|
It is a selective inhibitor of Dihydrofolate reductase
|
|
What must be absent with the use of trimethoprim in order to make it bacteriocidal?
|
Thymine
|
|
Which types of bacteria are targeted by Trimethoprim?
|
Both Gram - and Gram +
Its Broad Spectrum |
|
Which chemotherapeutic agents are inhibitors of cell wall synthesis?
|
Penicillin
Cephalosporin Vancomycin Bacitracin Cycloserine |
|
Which type of bacteria is most affected by penicillins?
|
Gram +
|
|
What drug inhibits the first stage of the cell wall synthesis? (Production of Cell Wall Building Blocks)
|
Cycloserine
|
|
What drug(s) inhibit the second stage of the cell wall synthesis? (Precursor transported from inside cell membrane to outside)
|
Vancomycin and Bacitracin
|
|
What drug(s) inhibit the third stage of the cell wall synthesis? (Cross linking of the cell wall)
|
Penicillin and Cephalosporin
|
|
What does Cell Death require?
|
Action of Autolysin
|
|
What are three mechanisms of resistance to Penicillin?
|
Lack of accessibility to target (Gram Negative)
Production of Penicillinases (Beta-Lactamase) Alterations in Penicillin Binding Proteins |
|
About what percent of penicillin is protein bound?
|
33-50%
|
|
What is the standard reference of Penicillin?
|
Penicillin G
|
|
Is oral use of Penicillin G indicated?
|
Not, it is inactivated at low pH
|
|
Which type of Pen G is used for syphyllis and rheumatic fever prophylaxis?
|
Benzathine Pen G
|
|
Which type of Pen G is used for the treatment of ghonorrea?
|
Procaine Pen G
|
|
Which type of penicillin is acid stable?
|
Penicillin V
|
|
Which drugs are penicillinase resistant penicillins?
|
Methicillin
Cloxacillin Nafcillin Dicloxacillin |
|
Which drugs are broad spectrum penicillins?
|
Ampicillin
Amoxicillin Carbenicillin |
|
Which drug is one of the last lines of defense in threatment of Methicillin-resistant S. aureus?
|
Vancomycin
|
|
Which antibiotic inhibits the intermediate stage of cell wall synthesis and is used as a topical treatment because it is too toxic for systemic use?
|
Bacitracin
|
|
Which 1st Gen drug of the cephalosporins is beta-lactamase resistant?
|
Cephalothin
|
|
Which drug of the cephalosporins is acid stable?
|
Cephalexin
|
|
Which drug of the cephalosporins is effective against otitis caused by H. influenza?
|
Cefaclor
|
|
What are the third generation drugs of the cephalosporin group?
|
Cefotaxime
Ceftizoxine |
|
What drugs are considered protein synthesis inhibitors?
|
Tetracyclines
Chloramphenicol Aminoglycosides Macrolides Clindamycin |
|
What do tetracyclines target?
|
Broad Spectrum (G+ , G-, Atypical)
Bacteriostatic |
|
What reduces the Oral F of Tetracyclines?
|
Divalent and Trivalent metal containing products. (Milk, cheese, yogurt, kaopectate, pepto-bismol, vitamins w/iron, and calcium supplements)
|
|
Can nursing mothers take tetracyclines?
|
No, it is excreted in milk
|
|
Which tetracyclines are short acting?
|
Chlortetracycline
Tetracycline Oxytetracycline |
|
Which tetracyclines are intermediate acting?
|
Demeclocycline
Methacycline |
|
Which tetracyclines are long acting?
|
Doxycycline
Minocycline |
|
What are some common adverse side effects of tetracyclines?
|
GI Irritation
Photosensitivity Reactions Permanent Discoloration of Teeth |
|
What is the drug of choice for cholera, rickettsiae, Lyme's disease, Chlamydial pneumonias, and vaginitis?
|
Tetracyclines
|
|
What common drug could be given for acne, or ulcers associated with H. pylori?
|
Tetracyclines
|
|
What tetracycline drug is often used systemically for periodontal disease?
|
Periostat (Doxycycline)
|
|
What tetracycline drug is often used topically for periodontal disease?
|
Arrestin (Minocycline)
Atridox (Doxycycline) |
|
What antibacterial protein synthesis inhibitor can be associated with aplastic anemia?
|
Chloramphenicol
|
|
What organisms does Chloramphenicol target?
|
Gram +, Gram - Aerobes
Anaerobes (Excellent Activity) Atypical Bacteria Bacteriostatic |
|
Which part of protein synthesis does chloramphenicol affect?
|
Blocks the peptidyltransferase activity on the 23S RNA of the 50S subunit
|
|
What drug is associated with Gray baby syndrome?
|
Chloramphenicol
|
|
What drug has been used for Typhoid Fever, Severe Meningitis, and Severe Pneumona?
|
Chloramphenicol
|
|
Which type of protein synthesis inhibitor chemotherapeutic agent is bacteriocidal?
|
Aminoglycosides
|
|
Which organisms do aminoglycosides target?
|
Gram - (Enteric) and some Gram + (Staph and Strep)
|
|
What are the three effects of aminoglycosides associated with binding to the 30S ribosomal subunit?
|
Inhibit initiation
Premature termination Misincorporation |
|
What is the method of use for aminoglycosides?
|
IV, or IM
|
|
What are the toxic effects of aminoglycosides?
|
Low therapeutic index
Nephrotoxicity Ototoxicity |
|
Gentamicin
Tobramycin Amikacin Netilmicin Neomycin Streptomycin and Spectinomycin Are all drugs that belong to which type of antibacterial? |
Aminoglycosides
|
|
Which aminoglycoside is used for Pseudomonal pneumonia?
|
Tobramycin
|
|
Which aminoglycoside is used for aminoglycoside-resistant infections?
|
Amikacin and Netilmicin
|
|
Which aminoglycoside is used for TB?
|
Streptomycin
|
|
Which aminoglycoside is used for N. gonorrhea?
|
Spectinomycin
|
|
What are three types of macrolides?
|
Erythromycin
Azithromycin Clarithromycin |
|
Which organism is mainly targeted by macrolides?
|
Aerobic Gram + cocci and bacilli
|
|
Which macrolide has an increased activity towards H. influenzae?
|
Azithromycin
|
|
What is the mechanism of macrolides?
|
Bind to 50S ribosomal subunit to block translocase activity of ribosome
|
|
Why is erythromycin enteric-coated or ester derivatives?
|
In order to avoid gastric inactivation (it is inactivated by stomach acid)
|
|
Which macrolide is excreted unchanged in the bile?
|
Azithromycin
|
|
Which macrolide has a high potential for drug interactions?
|
Erythromycin
|
|
What are two mechanisms of resistance to macrolides?
|
Acquisition of met gene (erythromycin efflux transporter)
Acquisition of erm gene (methylates a base residue in 23S RNA of ribosome) |
|
How does Clindamycin differ from Erythromycin?
|
Has a high activity for anaerobes
|
|
What is the drug of choice for lung abscess, anaerobic lung and pleural space infections?
|
Clindamycin
|
|
Which antibacterial is used in certain parasitic or fungal infections of T. gondii, and P. carinii?
|
Clindamycin
|
|
What is the prototype drug of the fluoroquinolones?
|
Ciprofloxacin
|
|
What is the mechanism of fluoroquinolones?
|
Inhibitor of bacterial DNA synthesis
|
|
What are common adverse effects of fluoroquinolones?
|
GI disturbances
Nausea Vomiting |
|
How is Vancomycin administered?
|
Parenteral
|
|
What does Metronidazole mainly target?
|
Anaerobic gram -
Clostridium species Bactericidal |
|
Which drug has neurologic effects attributed to seizures?
|
Metronidazole
|
|
What topical antibacterial is used for gram + bacteria in combination with polymixin and neomycin?
|
Bacitracin
|
|
What antibiotic is a hospital grade antibiotic that is broad spectrum restricted use as a drug of last resort?
|
Imipenem-cilastatin
|
|
What is Aztreonam used for?
|
Pseudomonas, Klebsiella, and Serratia
|
|
What is the transformation of normal tissue into cancer cells?
|
Carcinogenesis
|
|
How long must a person not have recurrance after cancer-therapy before they are considered disease-free?
|
5 Years
|
|
If the tumor shrunk after therapy, how would the result be classified?
|
Partial Response/Remission
|
|
What would a tumor be classified as if it was neither growing nor shrinking after therapy?
|
Stable Disease
|
|
Which phase of chemotherapy regimen seeks rapid reduction in tumor cell burden?
|
Induction Therapy
|
|
Which phase of chemotherapy regimen seeks to complete or extend initial remission?
|
Consolidation Therapy
|
|
Which phase of chemotherapy regimen seeks to sustain the remission for as long as possible?
|
Maintenance Therapy
|
|
Which tumors would you take the watch and wait approach? (No Therapy)
|
Slow growing cancers (Lymphoma and some Prostate Tumors)
|
|
What log kill would destroy the total cell population?
|
9
|
|
What may serve to recruit cells into active growth and increase sensitivity to chemotherapy?
|
Surgery and Radiation
|
|
What is an example of enhanced drug inactivation in a chemotherapeutic regimen?
|
Gluthathione Redox Pathway
|
|
What are examples of Cytotoxic Drugs?
|
Alkylating agents
Antimetabolites Antitumor antibiotics Mitotic inhibitors Topoisomerase inhibitors |
|
Which tissues are most affected by chemotherapy drugs?
|
Those with high growth fraction -
Bone Marrow Skin Hair Follicles Gastrointestinal Tract Developing Sperm |
|
When would you want to start chemotherapy treatment?
|
When tumor burden is low and growth fraction is high
|
|
How should chemotherapy drugs be administered?
|
Near max individual doses
As frequently as possible |
|
What cancer chemotherapeutic agent requires metabolic activation with one exception?
|
Antimetabolites (the exception being Methotrexate)
|
|
What cell cycle are antimetabolites specific to?
|
S Phase
|
|
What is the mechanism of antimetabolites?
|
They interfere with metabolic steps leading to DNA synthesis
|
|
Which type of chemotherapeutic drugs are chemically synthesized?
|
Alkylating Agents
|
|
Which type of cancer chemotherapuetic drug is not highly cell cycle specific, but is cell cycle active?
|
Topoisomerase Poisons
|
|
Which types of cancer chemotherapeutic drugs do not require metabolic activation?
|
Microtubule Poisons
Topoisomerase Poisons |
|
What type of cancer chemotherapeutic drug promotes DNA strand breaks?
|
Topoisomerase Poisons
|
|
Which cell cycle are Microtubule Poisons specific to?
|
M phase
|
|
What do monofunctional alkylating agents do?
|
Cause DNA damage as the cell attemps to repair alkylation
|
|
What do bifunctional alkylating agents do?
|
Cross link DNA
|
|
What are the difficulties in treating fungal infections?
|
Cell structure is closely related to mammalian cells
Slow growth rate Infections can often occur in poorly vascularized tissues |
|
What are four classes of drugs used to treat systemic fungal drug infections?
|
Polyenes
Azoles DNA/RNA synthesis inhibitors Mitotic spindle inhibitors |
|
What is the broadest spectrum of all antifungals?
|
Amphotericin B (Polyene antifungal)
|
|
What is the mechanism of polyenes?
|
Binds ergosterol to create leaky membranes (pores)
|
|
Which type of polyene has activity towards Candida, and is too toxic for systemic use?
|
Nystatin
|
|
What is the first line drug for OPC and vaginal candidaisis?
|
Nystatin
|
|
Which drug is the Azole prototype?
|
Ketoconazole
|
|
What is the mechanism of Ketoconazole?
|
An Ergosterol synthesis inhibitor
|
|
Which Azole antifungal is a strong inhibitor of CYP3A4 which leads to many drug interactions?
|
Ketoconazole
|
|
Which azole antifungal inhibits testosterone and glucocorticoid synthesis which can lead to gynecomastia in males?
|
Ketoconazole
|
|
Fluconazole is a drug of which class?
|
Azole
|
|
Which Azole antifungal is a topical use only because it is too toxic for systemic use?
|
Clotrimazole
|
|
What is the mechanism of Flucytosine?
|
Inhibits DNA synthesis
|
|
What organisms are targeted by Flucytosine?
|
Narrow Spectrum (Cryptococcus and Candida)
|
|
What is the mechanism of Griseofulvin?
|
It is a mitotic spindle inhibitor which interferes with yeast cell division
|
|
Which antifungal drug does not work when used topically and is taken orally for dermatophytic infections of hair, nails, and scalp?
|
Griseofulvin (Mitotic Spindle Inhibitor)
|
|
What was the first orally available drug for treating symptoms of HSV infection?
|
Acyclovir
|
|
What is the mechanism of Acyclovir?
|
It acts as a DNA chain terminator after being converted into acyclovir triphosphate by both cellular and viral molecules
|
|
What are two other derivatives of the anti-viral Acyclovir?
|
Valavyclovir
Penciclovir |
|
Which antiviral used for HSV infections attains higher concentrations for longer times?
|
Penciclovir
|
|
Which antiviral drug used for HSV infections gives higher bioavailability?
|
Valacyclovir
|
|
Which antiviral medication is a 22-carbon saturated primary alcohol that inhibits fusion of human host cell with the envelope of HSV?
|
Docosanol
|
|
What drug is used for CMV Retinitis in immunocompromised hosts and as a prophylaxis in transplant patients?
|
Ganciclovir
|
|
What are two anti-influenza A only drugs? (Have no effect on Influenza B)
|
Amantadine
Rimantidine |
|
What is the mechanism of Amantadine and Rimantidine?
|
It blocks the uncoating of virus after it enters the cell (M2 Protein interference)
|
|
What type of drugs are Zanamivir, and Oseltmavir?
|
Neuraminidase Inhibitors
|
|
Which drugs inhibit both Influenzae A and Influenzae B?
|
Zanamivir
Oseltmavir |
|
What is a normal CD4+ T cell count?
|
1 x 10^6 /mL
|
|
What CD4+ T cell count indicates the first AIDS symptoms?
|
<200,000 /mL
|
|
When do you initiate drug therapy for HIV?
|
When CD4+ count <200,000 cells/mL
|
|
What are 5 classes of drugs for HIV?
|
NRTI (Nucleoside reverse transcriptase Inhibitors)
Non-NRTI Protease Inhibitors Entry fusion Inhibitors Integrase strand transfer Inhibitors |
|
What is the mechanism of Nucleoside Reverse Transcriptase Inhibitors?
|
They are nucleoside analogues that selectively inhibit HIV Reverse Transcriptase
|
|
How are NRTI's selective but not specific?
|
They can also be incorporated into host cell DNA. Mitochondrial form of DNA Polymerase is more affected than Cellular DNA Polymerase
|
|
What is HAART?
|
Highly Active Antiretroviral Therapy: A combination of 3 HIV drugs simultaneously
|
|
Which drugs used with HAART are chosen first?
|
NRTI:
Zidovudine Abacavir Stavudine Tenofovir |
|
Which drugs used with HAART are chosen second?
|
Emtricitabine
Lamivudine |
|
What class of drugs are Nevirapine, Delavirdine, and Efavirenz?
|
Non-Nucleoside Reverse Transcriptase Inhibitors
|
|
What class of drugs are Nevirapine, Delavirdine, and Efavirenz?
|
First Generation Non-Nucleoside Reverse Transcriptase Inhibitors
|
|
What class of drug is Etravirine?
|
Second Generation Non-Nucleoside Reverse Transcriptase Inhibitors
|
|
Which class of HIV drug is most susceptible to rapid development of drug resistance?
|
NNRTIs
|
|
What is the preferred NNRTI for starting therapy?
|
Efavirenz
|
|
What drug class do the following drugs belong to:
Saquinavir Ritonavir Indinavir Lopinavir |
HIV Protease Inhibitors, First Gen
|
|
Which PI is often included in HAART regimens with another protease inhibitor because it increases the concentration of lopinavir?
|
Ritonavir
|
|
What second generation PI derivative is reserved as a backup for highly resistance HIV (which is also administered with ritonavir)?
|
Tipranavir
|
|
What are two general concerns with PI's?
|
They inhibit and/or induce two major families of drug metabolizing enzymes: Cytochrome P450 3A4 and UGT1A1 - Causes drug interactions
They elevate blood LDL |
|
What newer derivative of PI lacks a hypercholesterolemic effect?
|
Atazanavir
|
|
What is the only AIDS drug that must be administered parenterally?
|
Enfuvirtide
|
|
What is Enfuvirtide?
|
An amino acid peptide that inhibits viral entry by preventing fusion
|
|
What entry fusion inhibitor prevents fusion by antagonizing the chemokine coreceptor 5?
|
Maraviroc
|
|
What HIV Integrase Inhibitor is reserved for HAART regimens in patients who are resistant to at least one antiretroviral agent from each conventional class?
|
Raltegravir
|