Term
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Definition
| Class-antibacterial/antiprotozoal/drug for amebiasis (diarrhea)
Mechanism-addition of N-groups allowing easy diffusion into bacteria/organisms for DNA disruption
Target-intestinal and extraintestinal organisms such as: anaerobic bacteria ("ABC's" like C.diff); used for H.pylori to txt acid reflux; protozoans living in low oxygen environments (Entamoeba histolytica, Giardia lamblia, Trichomonas vaginalis)
Cidal/Static-Cidal
Special-avoid alcohol ingestion; may cause metallic taste and furring of the tongue; Similar drug is Tinidazole; may get nausea due to increased penetration (CNS based, not gut irritation) |
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Term
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Definition
| Class-antibacterial/antiprotozoal/drug for amebiasis (diarrhea)
Mechanism-addition of N-groups allowing easy diffusion into bacteria/organisms
Target-intestinal and extraintestinal organisms such as: anaerobic bacteria ("ABC's" like C.diff) and H.pylori; protozoans living in low oxygen environments (Entamoeba histolytica, Giardia lamblia, Trichomonas vaginalis)
Cidal/Static-Cidal
Special-Similar to metronidazole, with shorter txt duration and fewer side effects |
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Term
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Definition
| Class-antifungal
Mechanism-bind to ergosterol to create disruption in fungal cell membrane
Target-broad spectrum
Special-used for systemic infection; given by slow IV, starting with low dose and work up; can produce chills, fever, headache; often combined with sedative (phenothiazine) or corticosteriod to diminish adverse effects |
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Term
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Definition
| Class-antifungal
Mechanism-complexes with ergosterol in the cell membrane (creating disruptions)
Target-Topical fungal infections (athlete's foot) or vaginal candidiasis
Special-works same way as amphotericin B (but given for isolated infections) |
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Term
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Definition
| Class-antifungal (Imidazoles)
Mechanism-affect ergosterol synthesis
Target-chronic fungal infections*
Special-can be given orally; side effects include blocking synthesis of androgens so men may have increased female sex characterisitics* |
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Term
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Definition
| Class-antifungal (triazoles)
Mechanism-interfers with fungal sterols (ergosterol) in cell membrane
Target-broad spectrum of fungal infections
Special-more toxic than itraconazole; inhibits testosterone synthesis; given oral or IV |
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Term
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Definition
| Class-antifungal (allylamines)
Mechanism-blocks synthesis of ergosterol
Target-cutaneous mycotic infections like ringworm, nail infections, dermatophytic infections*
Special- |
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Term
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Definition
| Class-antifungals
Mechanism-inhibits fungal cell wall synthesis
Target-Candida; Aspergillus
Special-none. |
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Term
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Definition
| Class-antifungal
Mechanism-specific transport into fungal cell which is then converted to active form 5FdUMP
Target-
Special-prodrug; used orally and in combination with other antifungals |
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Term
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Definition
| Class-antifungal
Mechanism-interfers with polymerized microtubules and disrupts mitotic spindle
Target-
Special-none. |
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Term
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Definition
| Class-antimalarial/antiamebiasis
Mechanism-complexes with DNA and prevents replication and transcription* (For Crone: accumulates in food vacuole of parasite and shuts down heme polymerase, leading to toxic accumulation)
Target-Plasmodium species (malaria) in the erythrocytic stage; especially used for species Central America, Middle East (NOT sensitive to species in S. America, Africa, Asia). Therapeutic goal by giving this is to txt symptoms.
Special-given orally; active against amebas in the liver; in low doses it is not very toxic, but high does or for long duration can cause toxicity of the skin, blood and eyes |
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Term
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Definition
| Class-antimalarial
Mechanism-mechanism not clear* For Crone: interfers with mitochondrial activity of the parasite
Target-Plasmodium species (malaria)
Special-kills the LIVER form (exoerythrocytic) of malaria but not the erythrocytic stage (use Chloroquine for that); often used as a prophylaxis |
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Term
| Atovaquone (taken as combination form Malarone) |
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Definition
| Class-antimalarial/parasitic
Mechanism-interferes with electron transport chain in malarial mitochondria
Target-Plasmodium species (malaria) in SE Asia, sub-Saharan Africa and S. America (different species)
Special-taken with proguanil (Malarone) |
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Term
| Proguanil (taken as combination form Malarone) |
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Definition
| Class-antimalarial/parasitic
Mechanism-dihydrofolate reductase inhibitor
Target-Plasmodium species (malaria) in SE Asia, sub-Saharan Africa and S. America (different species)
Special-this drug is combined with Atovaquone (known as Malarone). Proguanil enhances the atovaquone effec on mitochondrial membranes |
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Term
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Definition
| Class-antimalarial
Mechanism-dihydrofolate reductase inhibitor which inhibits reduction of folic acid, therefore malaria cannot make their own DNA and cannot divide and grow
Target-Plasmodium (malaria)
Special-bad bacterial/cancer drug*; Folic acid is needed for 1 carbon transfer reaction to make pyramadine/purines to make DNA, without folic acid can't make DNA*; attacks the erythrocytic stage of malaria
Comparisons-types of inhibitors of folic acid reductase include Bactrim (Trimethaprim + sulfamethoxazole) for bacteria, Methotrexate for cancer |
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Term
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Definition
| Class-antihelminthic
Mechanism-increases calcium influx to alter parasite muscle function
Target-Flatworms (fluke and tapeworm); used to txt schistomiasis (blood fluke)
Special-none. |
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Term
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Definition
- Vector-female mosquito (Anopheles); mosquito bite injects sporozoites from saliva into blood stream
- Sporozoites penetrate liver cells and undergo schizogeny (asexual cleavage multiplication) and produce merozoites
- Merozoites head to RBC; form trophozoites (ring stage) and multiply by fission to create more merozoites
- Eventually malaria cells mature and sexual gametocytes can be picked up from mosquito for next round
- Sexual fusion in gut of mosquito; those cells travel to salivary gland of mosquito until infects human
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Term
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Definition
| Class-antihelminthic
Mechanism-inhibits fumarate reductase which interferes with ATP production. Also inhibits microtuble synthesis-->lack attachment and cant move as well. Organism becomes "tired," and loses grip from intestintal tract, dies.
Target-roundworms
Special-same as Mebendazole and Thiabendazole |
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Term
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Definition
| Class-antihelminthic
Mechanism-inhibits fumarate reductase which interferes with ATP production. Also inhibits microtuble synthesis-->lack attachment and cant move as well. Organism becomes "tired," and loses grip from intestintal tract, dies.
Target-roundworms
Special-same as Albendazole and Thiabendazole |
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Term
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Definition
| Class-antihelminthic
Mechanism-inhibits fumarate reductase which interferes with ATP production. Also inhibits microtuble synthesis-->lack attachment and cant move as well. Organism becomes "tired," and loses grip from intestintal tract, dies.
Target-roundworms
Special-same as Mebendazole and Albendazole |
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Term
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Definition
- Class-antihelminthic
- Mechanism-neuromuscular paralysis in the helminth
- Target-pinworm (enterobiasis) and roundworm (ascariasis)
- Special-none
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Term
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Definition
- Class-antiprotozoal/antiamebiasis (diarrhea)
- Mechanism-unknown
- Target-this is a very potent antiprotozoal; attacks extraintestinal
- Special-causes nausea (because its derived from ipecac root)
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Term
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Definition
- Class-antiprotozoal/antiamebiasis (diarrhea)
- Mechanism-unknown
- Target-attacks intestinal (Entamoeba histolytica)
- Special-none.
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Term
| Halogenated hydroxyquinolines |
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Definition
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Term
| Antiseptics and Disinfectants |
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Definition
These include:
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Phenol
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Iodine
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Hydrogen Peroxide
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Ethyl Alcohol 70%
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Zephiran
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Mercurochrome
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Silver Nitrate
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Nitrofurazone
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Term
| Reasons why a drug may not work |
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Definition
- Patient compliance
- Drug interaction ex) excess presence of another drug in the blood that binds up the active form of the drug you want to give
- Resistance-intrinsic resistance is when the organism is already resistant; acquired resistance is when you put pressure on an organism population and it adapts to survive in the presence of the drug
- Toxicity-you can't use the full dose to txt because of toxicty, so the drug is not therapeutic
- Drug may not be slective and doesn't kill the organism ex) choosing the wrong drug
- Infection is in a place in the body where the drug cant get to ex) deep seated wound without blood supply; brain
- Superinfection-drug kills 1 organism, but doesn't kill the other that is not proliferating (think of normal flora infections)
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Term
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Definition
- LD50 is the lethal dose to kill 50% of the pathogen or inhibit growth by 50%
- ED50 is the effective dose to produce the therapeutic effect
- Index = LD50/ED50
- High index indicates that the drug has a "large therapeutic window," meaning a large dose is needed to produce toxic effects. We want a high index to protect the patient
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Term
| Sites of Selective Toxicity |
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Definition
- Cell Wall-inactivate transpeptidase to inhibit crosslinking within peptidoglycan layer. ie) penicillins; cephalosporins
- Cell Membrane-disruption of lipid bilayer. ie) polymyxins; most antifungals
- Essential Nutrient-interference with biosynthetic pathway (folic acid). ie) sulfonamides; antifolates
- Protein Synthesis-different composition of ribosomes. ie) aminoglycosides (30s); tetracyclines (30s); macrolides (50s)
- DNA Synthesis-different DNA polymerases. ie) quinolones; antineoplastics
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Term
| Rating of Selective Toxicity |
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Definition
- Excellent-penicillins; cephalosporins; sulfonamides
- Fair-aminoglycosides; tetracyclines
- Poor-alkylating agents; pyrimidine analogues; purine analogues
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Term
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Definition
| Class-antifungal (triazoles)
Mechanism-interfers with fungal sterols (ergosterol) in cell membrane
Target-broad spectrum of fungal infections
Special-less toxicity than ketoconazole and no endocrine side effects; inhibits testosterone synthesis; given oral or IV* |
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