Biochemistry Drugs

  1. Pravastin (use)
    Treat high cholesterol and prevent Vascular Disease
  2. Pravastatin (mechanism)
    • HMG-CoA reductase is enzyme that catalyzes the rate limiting step in cholesterol synthesis.
    • It is a competitive inhibitor of this enzyme
    • Lowers cholesterol synthesis 
  3. DFP (di-isopropyl flourophosphate) (use)
    • Insectide but can be poisonous
    • used in neuroscience research
    • used in treatment of some glaucomas
  4. DFP (di-isopropyl flourophosphate) (mechanism)
    • Acetylcholinesterase (enzyme the cleaves Acetylcholine at neuronal synapse) is irreversibly inhibited by it by covalent bonding
    • potent neurotoxin 
    • cousin to Sarin nerve gas
  5. Aspirin (use)
    • Treatment of pain
    • anti-coagulant
  6. Aspirin (mechanism)
    Irreversible inhibitor of cyclooxygenase 1 and 2 (COX 1 and 2), which is required for blood clotting
  7. Azidothymidine (AZT) (use)
    • Anti-viral nucleoside
    • Prolongs life of HIV patients
    • Diminishes HIV dementia
    • Reduce mother-child transmission by >20%
  8. Azidothymidine (AZT) (mechanism)
    • Analog of nucleoside, deoxythymidine 
    • Azide group in place of 3'OH group required for nucleic acid polymerization 
    • Host cell converts drug to AZT-triphosphate via host cell kinase
    • Viral reverse transcriptase tries to utilize AZT-triphosphate but the polymerization is interrupted and virus can't procreate
  9. Didanosine (ddI) (use)
    • Anti viral nucleside 
    • Treatment of HIV
    • in combination with other drugs
  10. Didanosine (ddI) (mechanism)
    • Analog of nucleoside, deoxyadenosine
    • Missing 3'OH group
    • In host, converts to ddI-triphosphate
    • ddI has >100 fold affinity for reverse transcriptase than eukaryotic DNA polymerase 
  11. Acyclovir (use)
    • Anti-viral nucleoside
    • Used in Herpes simplex and varicella zoster treatment 
    • High specificity for infected cells 
  12. Acyclovir (mechanism)
    • Analog of nucleoside, deoxyguanosine 
    • missing 3'OH 
    • Converted to acyclovir-triphosphate via VIRAL kinase (making it have the high specificity for infected cells)
  13. Tenofovir (use)
    • Anti-viral nucleotide 
    • HIV treatment
  14. Tenofovir (mechanism)
    • Analog of nucleoTIDE, deoxyadenosine monophosphate 
    • Missing 3'OH
    • Convers to tenofovir diphosphate via host kinases 
    • Competes with deoxyadenosine triphosphate for incorportation into viral DNA strand
  15. Cytosine Arbinoside (Cytarabine) (use)
    • Anti-cancer drug
    • Specifically leukemia, esp acute myeloid leukemia and lymphoma 
  16. Cytosine Arbinoside (Cytarabine) (mechanism)
    • Cytosine nucleoside analog
    • In cells, converts to araC-triphosphate
    • Has extra OH at position 2, sterically hindering the next base 
  17. Adenosine Arabinoside (Vidarabine) (use)
    • Anti-cancer drug
    • Used to treat herpes simplex 
    • anti-neoplastic agent in Relapsed Childhood Acute Lymphoblastic Leukemia
  18. Adenosine Arabinoside (Vidarabine) (mechanism) 
    • Analog of nucleoside, deoxyadenosine
    • In host cell, converted to ara-A triphosphate
    • It gets incorporated into newly replication strand 
    • Due to the planar shape of the analog, next base cannot incorporate 
  19. 5-Azacytidine and 5-aza-2'-Deoxycytidine (Decitabine) (use)
    • DNA Hypomethylation agents
    • Used in myelodysplastic syndrome and acute myeloid leukemia
  20. 5-Azacytidine and 5-aza-2'-Deoxycytidine (Decitabine) (mechanism)
    • In cancer cells, key cell cycle regulatory genes become methylated. (methylation turns genes OFF)
    • Cytidine analogs possesses nitrogen atom in place of 5'Carbon of base where it would normally methylated. 
  21. Ciprofloxacin (Quinolone) (use)
    • DNA gyrase inhibitor 
    • antibiotic in UTL, prostatis, gastroenteritis, nosocomial infection, STI's 
  22. Ciprofloxacin (Quinolone) (mechanism)
    • Prevents re-ligation action of gyrase (only in bacteria) on DNA strand
    • Double stranded breaks become permanent
    • Cells can either repair the breaks or die (apoptosis)
    • Extremely effective at destroying gram- bacteria
    • Slightly with gram+
    • Kills only aerobic bacteria 
  23. Actinomycin D (use)
    • DNA replication inhibitor 
    • Used in treatment of cancers
    • Wilm tumor, rhabdomyosacrcoma, Kapost's Sarcome, gestational trophoblastic tumors, testicular cancers
  24. Actinomycin D (mechanisms) 
    • Phenoxazone ring of drug intercalates with adjacent guanine and cytosine residues
    • Meanwhile 2 peptide side chains on the drug extend along the minor groove this stabilizing the drug-DNA compound
    • Prevents DNA replication
  25. Campothectin (use)
    • Topoisomerase I inhibitor
    • Single agent in treatment of cancers including: Ovarian, lung cancers, acutre myelocytic lekemia, and myelodysplastic 
  26. Campothectin (mechanisms)
    • Irreversibly binds to and inhibits Topoisomerase I completely, thus inhibits replication 
    • Isolated from an exotic plant 
  27. Etoposide (use)
    • Topoisomerase 2 inhibitor
    • ANTI-CANCER DRUG: leukemia, lung, testis and ovary
  28. Etoposide (mechanism)
    • Binds to topoisomerase 2 and stabilizes the cleavage complex 
    • so topoisomerase 2 cannot proceed with its function 
    • inhibits replication 
  29. Rifampin (use)
    • Prokaryotic transcription inhibitor 
    • Antibiotic
    • Used in gram+ infections and tuberculosis 
  30. Rifampin (mechanisms)
    • Bind to prokaryotic polymerase 
    • Causes conformational change that prevents formation of 1st phosphodieater bond of RNA polymer 
    • Inhibits transcription 
  31. alpha-Amantin (definition)
    • Death cap mushroom poison 
    • treated by GI decontamination via charcoal, high dose penecillin, liver transplant 
  32. alpha-Amantin (mechanism)
    • Forms 1:1 complex with eukaryote RNA polymerase II
    • inhibits transcription 
    • 4 Phases:
    • 1. asymptomatic
    • 2. gastrointestinal 
    • 3. apparent recovery
    • 4. finally hepatic and renal failure 
  33. Streptomycin (use)
    • Antibiotic 
    • Inhibitor of intiation during translation in prokaryotes 
  34. Streptomycin (mechanism)
    • Aminoglycoside structure
    • Binds to 30s subunit and prevents assemble of translation machinery
  35. Tetracycline (use)
    • Antibiotic
    • Inhibitor of elongation during protein synthesis in prokaryotes
  36. Tetracycline (mechanism)
    • Four ring structure
    • Blocks elongation protein synthesis by preventing aminoacyl-tRNA access to the A site 
  37. Erthromycin (use)
    • Antibiotic
    • Inhibitor of elongation during protein synthesis in prokarytoes
  38. Erthromycin (mechanism)
    • Macrolide structure
    • Binds to 50s of the complete ribosomal complex
    • Blocks ribosome translocation 
  39. Chloramphenicol (use)
    • Antibiotic
    • Inhibitor of elongation during protein synthesis in prokaryotes
  40. Chloramphenicol (mechanism)
    • Inhibits peptidyl transferase activity of ribosome
    • May inhibit mitochondrial translation as well (so used moreso in third world countries)
    • Important for some meningitis treatment
  41. Cycloheximide (use)
    • Research agent 
    • Inhibitor of elongation during protein synthesis in prokaryotes
  42. Cycloheximide (mechanism)
    • Inhibits peptidyl transferase activity of ribosome
    • Important experimental tool 
  43. Puromycin (definition)
    • Toxin
    • Inhibitor of elongation during protein synthesis in ALL organism 
  44. Puromycin (mechanism)
    • Prevents elongation by causing premature termination 
    • Toxic to both prokaryotes and eukaryotes 
  45. Caffeine and Theophylline (definition)
    • Stimulants
    • Found in many soft drinks and coffee
  46. Caffeine and Theophylline (mechanism)
    • Inhibits phosphodiesterase
    • so prolonged signaling by cAMP
    • Prolonged stimulatory effects 
  47. Cholera and E.Coli Toxin (definition)
    Toxins of Cholera and E. Coli bacteria
  48. Cholera and E.Coli Toxin (mechanisms)
    • Produce their effects by ADP-ribosylating (permanently inactivating), G-stimulatory proteins in cAMP second messenger system. 
    • Producing profuse diarrhea 
  49. Pertussis Toxin (definition)
    • Toxin of pertussis bacteria. 
    • Caused Whooping cough 
  50. Pertussis Toxin (mechanism)
    • Toxin ADP-ribosylates the G-inhibitory proteins of the cAMP second messenger system. 
    • Produces drying mucus membranes of respiratory tractand a dry whooping cough persisting over weeks 
  51. Nitroglycerin and Nitroprusside (use)
    Vasodilators used in treatment of high blood pressure
  52. Nitroglycerin and Nitroprusside (mechanism)
    • Metabolizes to Nitric Oxide in cells
    • NO activates cGMP that causes relaxation in smooth muscle by decreasing phosphorylation of myosin chains
  53. Arsenate (definition)
    Deadly toxin
  54. Arsenate (mechanism)
    • Bypasses Glyceraldehyde 3 phosphate dehydrogenase step in glycolysis, 
    • thus decreasing amount of energy produced per glucose
    • bings to lipoic acid and inhibits pyruvate dehydrogenase 
  55. Fluoride (use)
    Used in blood glucose test to inhibit glycolysis to the accurate glucose levels are obtained 
  56. Fluoride (mechanism)
    Inhibits enolase (step 9) in glycolysis, prevents formation of second ATP and pyruvate
  57. Malonate (definition)
    Toxin produced by some plant and bacteria
  58. Malonate (mechanism)
    • Inhibits Succinate Dehydrogenase of TCA 
    • Can deadly
  59. Rotenone (use)
    • Commonly used insectide
    • Linked to development of parkinsons disease
  60. Rotenone (mechanism)
    Inhibits NADH Dehydrogenase (Complex 1) of ETC
  61. Piericidin A (use)
    Bacterial Antibiotic 
  62. Piericidin A (mechanism)
    Inhibits NADH Dehydrogenase (Complex 1) of ETC
  63. Amystal (definition)
    • Barbituate 
    • Psychoactive sedative hypnotic 
  64. Amystal (mechanism)
    Inhibits NADH Dehydrogenase (Complex 1) of ETC
  65. Antimycin A (use)
    Bacterial Antibiotic
  66. Antimycin A (mechanism)
    Inhibits Cytochrome b of cytochrome reductase complex (complex 3) of ETC
  67. CO, Azide, Hydrogen Sulfide, and Cyanide (definition)
    • Toxins
    • Cyanide is highly acutely toxic
  68. CO, Azide, Hydrogen Sulfide, and Cyanide (mechanism)
    Inhibit Cytochrome Oxidase (Complex 4) of ETC
  69. Oligomycin (definition)
    Streptomyces toxin 
  70. Oligomycin (mechanism)
    • Toxin produced by streptomyces bacteria
    • Inhibits F0 subunit of ATP synthase 
  71. Atractyloside (definition)
    Toxin produced by thistle plant 
  72. Atractyloside (mechanism)
    • Binds outward facing side of ADP/ATP transporter
    • Effects similiar to Oligomycin 
    • so it inhibits the transporter 
  73. Bongkrekic Acid (definition)
    Respiratory toxin produced in coconuts infected with Burkholderia toxin 
  74. Bongkrekic Acid (mechanism)
    • Binds inward facing side of ADP/ATP transporter
    • Effects similiar to Oligomycin 
    • so inhibits the transporter
  75. Dinitrophenol (DNP) (use)
    Research agent
  76. Dinitrophenol (DNP) (mechanism)
    • Electron transport chain uncoupler
    • Destroy proton gradient across inner mitochondrial membrane by allowing H+ to leak through without generating ATP
    • Energy is lost through generation of heat 
  77. Gramicidin (use)
    Antibiotic produced by Bacillus brevis
  78. Gramicidin (mechanism)
    • Channel forming ionophore
    • Non specific ion gradient destruction 
    • disrupts ETC
  79. Valinomycin (use)
    Antibiotic produced by streptomyces
  80. Valinomycin (mechanism)
    • Carrier Ionphore
    • Disrupts ion gradient across inner mitochondrial membrane by carrying K+ into matrix
    • Disrupts ETC
Card Set
Biochemistry Drugs
Pre midterm