Exam 1 Drugs Flashcards
What are the type, mechanism and target of Azidthymine (Zidovudine or AZT)?
Type: anti-viral Nucleoside Analogue of deoxythymidine
No 3’ OH Group due to N=N=N group at 3’ position
Mechanism: phosphorylated by host cellular kinase and utilized by viral reverse transcriptase and incorporated into dsDNA leading to chain termination
Target: viral reverse transcriptase
Inhibitor of viral replication
(Treats HIV)
What are the type, mechanism and target of Didanosine (DDI)?
Type: Anti-viral nucleoside analogue of deoxyadenosine
Type: No 3’ OH group (completely absent)
Mechanism: phosphorylated by host cellular kinase and utilized by viral reverse transcriptase and incorporated into dsDNA leading to chain termination
Target: viral reverse transcriptase
Inhibitor of viral replication
(Treats HIV)
What are the type, mechanism and target of tenofovir?
Type: Antiviral nucleotide base
- Analogue of deoxyadenosine monophosphate
- No 3’ OH group (broken ring); only 2 phosphate groups
Mechanism: phosphorylated once by host cellular kinase
-competes with deoxy-ATP (it’s natural nucleotide base) for incorporation. Causes chain termination of DNA
Target:
viral reverse transcriptase
Inhibitor of viral replication
(Treats HIV)
What are the type, mechanism and target of acyclovir ?
Type: antiviral nucleoside analogue of deoxyguanosine
No 3’ OH Group due to broken ring structure of pentose sugar
Mechanism: first phosphorylation by viral thymidine kinase (specificity b/c only infected cells possess viral kinase ), last two phosphorylation by host cellular kinase. Cause chain termination once incorporated to DNA
Target: viral DNA polymerase
Inhibitor of viral replication
Treats: herpes simplex and varicella zoster
What are the type, mechanism and target of Adenosine arabinoside (Vidarabine)?
Type: anti-viral nucleoside analogue for deoxyadenosine
3’ OH group sterically hindered
Ribose sugar replaced by arabinose (2’OH sterically hinders 3’ OH)
Mechanism: phosphorylated by host cell kinases
-Sterically hindered 3’ OH prevents DNA polymerase from adding next dNTP leading to chain termination
Target: viral DNA polymerase, inhibits viral DNA polymerase
Used to treat: relapsed childhood Acute lymphoblastic leukemia and herpes simplex infections
What are the type, mechanism and target of cytosine arabinoside (araC or Cytarabine)?
Type: Nucleoside analogue for cytosine
3’ OH group sterically hindered
Ribose sugar replaced by arabinose (2’ OH sterically hinders 3’ OH )
Mechanism: Rapidly converted to its phosphorylated form without the use of a kinase.
Sterically hindered 3’ OH prevents DNA polymerase from adding next dNTP leading to chain termination
Target: human DNA polymerase, inhibitor of DNA Replication
Use: leukemia, in particular acute myeloid leukemia
What are the type, mechanism and target of 5-aza- 2’-deoxycytidine (Decitabine)- 5-azacytidine
(Deficient of methylation)?
Type: cytidine analogue
Nitrogen at position 5 of base instead of carbon causes hypomethylation
Mechanism: methyl group cannot be added to nitrogen at position 5 methyltransferase causing MORE transcription (DEregulation) p53 gene
Target: DNA methyl-transferase
Inhibits methylation once incorporated into DNA and RNA
Use: myelodysplastic syndrome and acute myeloid leukemia
What are the type, mechanism and target of Ciprofloxacin and Nalidixic acid (Quinolone family) ?
Type: antibiotic
Mechanism: inhibits bacterial DNA Gyrase (topoisomerase II), which leads to positive coil build up and chain termination
Target: inhibitor of bacterial DNA Gyrase (bacterial topoisomerase II)
Disrupts DNA replication and transcription
Use: respiratory infections, UTIs, Anthrax
What are the type, mechanism and target of Novobiocin (Courmarin family)?
Type: antibiotic
Mechanism: Inhibits bacterial DNA Gyrase (topoisomerase II), which leads to positive coil build up and chain termination
Target: Inhibitor of bacterial DNA Gyrase (bacterial topoisomerase II)
Disrupts DNA Replication and transcription
Use: staph infections, MRSA
What are the type, mechanism and target of 5-fluorouracil?
Type: anti-cancer
Mechanism: in cells, it is converted to FdUMP which inhibits thymidine kinase, and thus inhibiting synthesis of thymine nucleotides that are required for DNA synthesis
Target: thymidine kinase
Use: cancer
What are the type, mechanism and target of antimyocin D (Dactinomycin) (Dactin….) D intercalates forming one word (like dsDNA)?
Type: anti-cancer
Mechanism: intercalates between adjacent G-C bases preventing DNA from unwinding. The polypeptide chains extend along the minor groove of the helix, thereby stabilizing the drug- DNA complex
Target: inhibitor of DNA replication and transcription (RNA synthesis)
Uses: cancer, chemotherapy
What are the type, mechanism and target of Camptothecin?
Type: Anti-cancer
Mechanism: inhibits eukaryotic enzyme topoisomerase I, resulting in DNA breaking (tangling)
Target: eukaryotic topoisomerase I
Use: cancer, chemotherapy
What are the type, mechanism and target of Etoposide?
Type: anti-cancer
Mechanism: inhibits eukaryotic enzyme topoisomerase II, resulting in DNA breakage (tangling)
Target: eukaryotic topoisomerase II
Use: cancer, chemotherapy
What are the type, mechanism and target of Rifamycin(rifampin)?
“I don’t want to get my fam in my TB”
Type: antibiotic
Mechanism: blocks formation of the first phosphodiester bond by binding to prokaryote RNA polymerase resulting in a conformational change in the RNA polymerase and inhibiting initiation of transcription
Target: RNA polymerase (prokaryotes)
Use: tuberculosis
What are the type, mechanism and target of Alpha-Amantin toxin (from Amanita phalloides death cap mushroom) ?
Type: toxin
Mechanism: mushroom produces the toxin alpha-amanitin which is a potent inhibitor of RNA polymerase II (Eukaryotic) causing no mRNA to be formed and thus no proteins
Four phases:Asymptomatic, GI, Appearent recovery, hepatic phase
Target: RNA Polymerase II (Eukaryote)
Use: GI decontamination, penicillin, liver transplant
What are the type, mechanism and target of streptomycin (strep distorts)?
Type: aminoglycoside antibiotic
Mechanism: Binds 30s ribosomal subunit of prokaryotes and distorts structure, preventing initiation of translation via preventing the assembly of the complete ribosome
Target: 30s ribosomal subunit- separated(prokaryotes)
Use: bacterial infection
What are the type, mechanism and target of tetracycline?
Type: antibiotic (4 ring structure)
Mechanism: interacts with 30s subunit of complete 70s ribosome and blocks access of A site, preventing elongation of translation
Target: 30s subunit to complete 70S ribosome(prokaryotes)
Use: bacterial infection
What are the type, mechanism and target of erythromycin (erythrocytes “trans locate “ O2 throughout body)?
Type:antibiotic -marcolide structure
Mechanism: binds 50s subunit of complete 70s ribosome and blocks access of A site, preventing elongation of translation
Target: 50s subunit of complete 70s ribosome (prokaryotes)
Uses: bacterial infection
What are the type, mechanism and target of Chloramphenicol?
-like chloroplasts… prokaryotic.
Ramp prevents peptidyltransferase.
Type: antibiotic
Mechanism: inhibits peptidyltransferase (peptide bond formation ), preventing elongation of translation
Target: peptidyltransferase(prokaryotes)
Use: not widely used due to inhibition of mitochondrial inhibition
What are the type, mechanism and target of Cycloheimide? Cyclops is eukaryotic…. And probably has peptyltransferase
Type: antibiotic
Mechanism: inhibits eukaryotic peptidyl-transferase (peptide bond formation), preventing elongation of translation
Target: peptidyltransferase
Used in laboratories
What are the type, mechanism and target of Puromycin?
When you’re pure, you are growing and… tend to premature …. And fall out of (P) sight.
Type: antibiotic-structural analogue to part of aminoacyl-tRNA
Mechanism: Blocks elongation after it forms peptide bond with growing protein chain, causing peptide to fall out of P site and premature translation termination
Target: growing protein chain
-prokaryotes and eukaryotes
Use: no clinical use
What are the type, mechanism and target of Diphtheria?
“Your IP address determines your location”
Type: toxin
Mechanism: Inactivates eukaryotic EF-2, preventing translocation
Target : EF-2 (elongation factor-2) - eukaryotes
What are the type, mechanism and target of Azathioprine?
“ Aza captain, you have to suppress any rejection or fights “
Type: purine analogue- immunosuppressive drug
Mechanism: metabolized to 6-mercaptopurine, which suppresses rejection during organ transplantation
Target: inhibits an enzyme required for DNA synthesis
Uses: organ transplantation
What are the type, mechanism and target of Allopurinol?
Type: purine analogue
Mechanism: inhibits xanthine oxidase, thus lowering the conversion of purine bases to Uric acid end products. The purines are excreted as xanthine and hypoxanthine which are more soluble than uric acid.
Target: xanthine oxidase
Uses: gout
What are the type, mechanism and target of adenosine (adenocard)?
Type: purine nucleoside
Mechanism: plays a role in energy transfer and can act as an inhibitory neurotransmitter. It slows the heart rate, and plays a role in sleep regulation
Use: supraventricular tachycardia
