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med school pre Rough Review > Exam 1 Drugs > Flashcards

Exam 1 Drugs Flashcards

1
Q

What are the type, mechanism and target of Azidthymine (Zidovudine or AZT)?

A

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)

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2
Q

What are the type, mechanism and target of Didanosine (DDI)?

A

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)

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3
Q

What are the type, mechanism and target of tenofovir?

A

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)

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4
Q

What are the type, mechanism and target of acyclovir ?

A

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

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5
Q

What are the type, mechanism and target of Adenosine arabinoside (Vidarabine)?

A

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

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6
Q

What are the type, mechanism and target of cytosine arabinoside (araC or Cytarabine)?

A

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

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7
Q

What are the type, mechanism and target of 5-aza- 2’-deoxycytidine (Decitabine)- 5-azacytidine
(Deficient of methylation)?

A

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

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8
Q

What are the type, mechanism and target of Ciprofloxacin and Nalidixic acid (Quinolone family) ?

A

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

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9
Q

What are the type, mechanism and target of Novobiocin (Courmarin family)?

A

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

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10
Q

What are the type, mechanism and target of 5-fluorouracil?

A

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

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11
Q

What are the type, mechanism and target of antimyocin D (Dactinomycin) (Dactin….) D intercalates forming one word (like dsDNA)?

A

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

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12
Q

What are the type, mechanism and target of Camptothecin?

A

Type: Anti-cancer

Mechanism: inhibits eukaryotic enzyme topoisomerase I, resulting in DNA breaking (tangling)

Target: eukaryotic topoisomerase I

Use: cancer, chemotherapy

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13
Q

What are the type, mechanism and target of Etoposide?

A

Type: anti-cancer

Mechanism: inhibits eukaryotic enzyme topoisomerase II, resulting in DNA breakage (tangling)

Target: eukaryotic topoisomerase II

Use: cancer, chemotherapy

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14
Q

What are the type, mechanism and target of Rifamycin(rifampin)?

A

“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

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15
Q

What are the type, mechanism and target of Alpha-Amantin toxin (from Amanita phalloides death cap mushroom) ?

A

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

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16
Q

What are the type, mechanism and target of streptomycin (strep distorts)?

A

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

17
Q

What are the type, mechanism and target of tetracycline?

A

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

18
Q

What are the type, mechanism and target of erythromycin (erythrocytes “trans locate “ O2 throughout body)?

A

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

19
Q

What are the type, mechanism and target of Chloramphenicol?

-like chloroplasts… prokaryotic.
Ramp prevents peptidyltransferase.

A

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

20
Q

What are the type, mechanism and target of Cycloheimide? Cyclops is eukaryotic…. And probably has peptyltransferase

A

Type: antibiotic

Mechanism: inhibits eukaryotic peptidyl-transferase (peptide bond formation), preventing elongation of translation

Target: peptidyltransferase

Used in laboratories

21
Q

What are the type, mechanism and target of Puromycin?

A

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

22
Q

What are the type, mechanism and target of Diphtheria?

A

“Your IP address determines your location”

Type: toxin

Mechanism: Inactivates eukaryotic EF-2, preventing translocation

Target : EF-2 (elongation factor-2) - eukaryotes

23
Q

What are the type, mechanism and target of Azathioprine?

A

“ 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

24
Q

What are the type, mechanism and target of Allopurinol?

A

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

25
Q

What are the type, mechanism and target of adenosine (adenocard)?

A

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

med school pre Rough Review (7 decks)

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