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Pharmacology II Exam III MOAs
Pharmacology II Exam III MOAs
53
Pharmacology
Professional
03/06/2012

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Term
Isoniazid
Definition
Inhibits synthesis of mycolic acid;
Prodrug converted to active metabolite by mycobacterial peroxidase
Term
Rifampin
Definition
Inhibits bacterial RNA synthesis by binding to the beta subunit of DNA-dependent RNA polymerase, blocking RNA transcription
Term
Rifabutin
Definition
Inhibits bacterial RNA synthesis by binding to the beta subunit of DNA-dependent RNA polymerase, blocking RNA transcription
Term
Rifapentine
Definition
Inhibits bacterial RNA synthesis by binding to the beta subunit of DNA-dependent RNA polymerase, blocking RNA transcription
Term
Ethambutol
Definition
Inhibits arabinosyl transferase resulting in impaired mycobacterial cell wall synthesis
Term
Streptomycin
Definition
Inhibits bacterial protein synthesis by binding directly to the 30S ribosomal subunits causing faulty peptide sequence to form in the protein chain
Term
Pyrazinamide
Definition
Targets mycobacterial fatty acid synthase I gene involved in mycolic acid synthesis
Term
Ethionamide
Definition
Inhibits peptide synthesis imparing cell wall formation; bacteriostatic; Prodrug activated by a mycobacterial redux system
Term
Aminosalicylic Acid
Definition
A competitive antagonist with PABA (like sulfonamides); baceriostatic
Term
Cycloserine
Definition
Inhibits bacterial cell wall synthesis by competing with amino acid (D-alanine) for incorporation into the bacterial cell wall
Term
Gatifloxacin, Moxifloxacin
Definition
Anti-TB quinolones; DNA gyrase and topoisomerase IV inhibitor which are both necessary for DNA replication and transcription, DNA repair, recombination, and transposition
Term
Interferon-γ
Definition
Participates in immunoregulation by enhancing the oxidative metabolism of macrophages; activates macrophages
Term
Dapsone
Definition
Competitive antagonist of para-aminobenzoic acid (PABA) and prevents normal bacterial utilization of PABA for the synthesis of folic acid
Term
Amphotericin B
Definition
Binds to ergosterol altering cell membrane permeability in susceptible fungi via pore formation and causes leakage of cell components with subsequent cell death.
Term
Flucytosine
Definition
Penetrates fungal cells and is converted to fluorouracil which competes with uracil interfering with fungal RNA and protein synthesis
Term
Azoles
Definition
Interferes with cytochrome P450 activity, decreasing ergosterol synthesis (principal sterol in fungal cell membrane) and inhibiting cell membrane formation
Term
Caspofungin
Definition
Inhibits synthesis of β(1,3)-D-glucan, an essential component of the cell wall of susceptible fungi.
Term
Micafungin
Definition
Inhibits synthesis of β(1,3)-D-glucan, an essential component of the cell wall of susceptible fungi.
Term
Andiulafungin
Definition
Inhibits synthesis of β(1,3)-D-glucan, an essential component of the cell wall of susceptible fungi.
Term
Griseofulvin
Definition
Inhibits fungal cell mitosis at metaphase; binds to human keratin making it resistant to fungal invasion
Term
Terbinafine
Definition
Synthetic allylamine derivative which inhibits squalene epoxidase, a key enzyme in sterol biosynthesis in fungi. This results in a deficiency in ergosterol within the fungal cell wall and results in fungal cell death. Binds to keratin.
Term
Chloroquine
Definition
May act by concentrating in the parasite food vacuoles and preventing the polymerization of heme into hemozoin; concentrates within parasite acid vesicles and raises internal pH resulting in inhibition of parasite growth; interferes with metabolism and hemoglobin utilization by parasites
Term
Amodiaquine
Definition
May act by concentrating in the parasite food vacuoles and preventing the polymerization of heme into hemozoin; concentrates within parasite acid vesicles and raises internal pH resulting in inhibition of parasite growth; interferes with metabolism and hemoglobin utilization by parasites
Term
Tinidazole
Definition
Reduction of nitro group to reactive product; After diffusing into the organism, it is proposed that tinidazole causes cytotoxicity by damaging DNA and preventing further DNA synthesis.
Term
Albendazole
Definition
Causes selective degeneration of Cytoplasmic microtubules in intestinal and tegmental cells of intestinal helminths and larvae.
Term
Nitazoxanide
Definition
Activity may be due to interference with the pyruvate:ferredoxin oxidoreductase (PFOR) enzyme-dependent electron transfer reaction which is essential to anaerobic metabolism.
Term
Ivermectin
Definition
Paralyzes nematodes and arthropods by increasing GABA signaling
Term
Mebendazole
Definition
Inhibits the formation of helminth microtubules
Term
Piperazine
Definition
Blocks acetylcholine at the neuromuscular junction causing paralysis of the worm.
Term
Praziquantel
Definition
Increases the cell permeability to calcium in schistosomes, causing strong contractions and paralysis of worm musculature leading to detachment of suckers from the blood vessel walls and to dislodgment
Term
Pyrantel Pamoate
Definition
Causes the release of acetylcholine and inhibits cholinesterase; acts as a depolarizing neuromuscular blocker, paralyzing the helminths
Term
Thiabendazole
Definition
Affects microtubule synthesis
Term
Mupirocin
Definition
Binds to bacterial isoleucyl transfer-RNA synthetase resulting in the inhibition of protein synthesis
Term
Polymyxin B and E
Definition
act as cationic detergents damaging the bacterial cytoplasmic membrane of gram-negative organisms causing leakage of intracellular substances and cell death
Term
Methenamine
Definition
Hydrolyzed to formaldehyde and ammonia in acidic urine.
Term
Acyclovir
Definition
Converted to monophosphate by virus-specific thymidine kinase then further converted to triphosphate by other cellular enzymes. Triphosphate inhibits DNA synthesis and viral replication by competing with deoxyguanosine triphosphate for viral DNA polymerase and being incorporated into viral DNA.
Term
NRTIs
Definition
Act by competitively inhibiting HIV-1 reverse transcriptase thereby blocking viral DNA synthesis and suppressing HIV replication. They can be incorporated into the forming DNA chain and cause chain termination.
Term
NNRTIs
Definition
Bind directly to HIV-1 reverse transcriptase and cause conformational change blocking RNA and DNA-dependent DNA polymerase thereby inhibiting DNA synthesis.
Term
Protease Inhibitors
Definition
Binds to the site of HIV-1 protease activity and inhibits cleavage of viral Gag-Pol polyprotein precursors into individual functional proteins required for infectious HIV. This results in the formation of immature, noninfectious viral particles.
Term
Enfuvirtide
Definition
Blocks viral entry into a healthy cell by binding to the gp41 glycoprotein on the viral envelope and preventing the fusion of the virus with the plasma membrane.
Term
Raltegravir
Definition
Inhibits the catalytic activity of integrase, thus preventing integration of the proviral gene into human DNA.
Term
Interferon Alpha
Definition
Inhibits viral penetration, translation, transcription, protein processing, maturation, and release; Also increases expression of MHC class I and II molecules, enhances phagocytic activity of macrophages, increases proliferation and survival of CTLs
Term
Amantadine
Definition
Blocks the M2 proton ion channel of the virus thereby stopping the uncoating of influenza A virus preventing penetration of virus into host
Term
Rimantadine
Definition
Exerts its inhibitory effect early in the viral replicative cycle, possibly inhibiting the uncoating process.
Term
Zanamivir
Definition
Neuraminidase inhibitors that interfere with the release of progeny virus from infected cells to new host cells.
Term
Oseltamivir
Definition
Neuraminidase inhibitors that interfere with the release of progeny virus from infected cells to new host cells.
Term
Ribavirin
Definition
Inhibits replication of RNA and DNA viruses; inhibits influenza virus RNA polymerase activity and inhibits the initiation and elongation of RNA fragments resulting in inhibition of viral protein synthesis.
Term
Palivizumab
Definition
Exhibits neutralizing and fusion-inhibitory activity against RSV; these activities inhibit RSV replication in laboratory and clinical studies
Term
Polymyxins
Definition
Binds to the LPS in the membranes of Gm- bacteria disrupting the structure of both the outer and inner cell membranes
Term
Daptomycin
Definition
Uses Ca to insert tail into the plasma membrane, aggregating and forming pores. This opens the plasma membrane allowing k+ to move out of the cell, resulting in depolarization and loss of excitibility of membrane and prevention of action potential. This causes all of the metabolic activity inside the bacteria to halt, resulting in death (bactericidal).
Term
Sulfonamides
Definition
Structural analogs of PABA; they inhibit dihydropteroate synthase (which produces dihydrofolic acid) ultimately inhibiting bacterial DNA synthesis.
Term
Trimethoprim
Definition
Inhibits dihydrofolate reductase (DHFR) preventing the production of tetrahydrofolic acid and preventing bacterial DNA synthesis.
Term
Fluoroquinolones
Definition
Inhibit bacterial topoisomerase II (DNA gyrase) and topoisomerase IV which are responsible for DNA unwinding and separation respectively. They prevent DNA synthesis.
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