Brainscape's Knowledge GenomeTM


Top Flashcards (Certified)
All Flashcards

MODA List 1 > 2-2 Van Veen > Flashcards

2-2 Van Veen Flashcards

1
Q

Aciclovir

A

Antiviral Purine analogue (guanine)
Prodrug - only monophosphorylated by
viral thymidine kinase in infected cells
Cellular enzymes convert to acyclovir-TP
Preferentially interacts with viral DNA
polymerase (30 x)
Competitive substrate, and is incorporated in viral DNA, causing termination of DNA replication (no 3’OH)
Resistance in Herpes virus due to change in specificity of viral thymidine kinase

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Amantadine

A

Antiviral for Influenza A
Early - Acts on M2 proton channel involved in nucleocaspid uncoating
High affinity binding site at low pH where it blocks proton conduction
Late - interfere with hemagglutinin processing
Acidification of interior of virion is required for hemagglutinin-mediated membrane fusion and release into cytosol

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Amoxicillin

A

B-lactam Antibiotic
Blocks cell wall peptidoglycan-crosslinking transpeptidase by covalent and irreversible binding as a pseudo-substrate
Forms a slowly hydrolysing covalent acyl enzyme intermediate

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Amphotericin B

A

Polyene antibiotic - antifungal and antiparasitic
Low degree of selective toxicity and low therapeutic index, little selectivity and quite toxic
Target ergosterol in fungal (and leishmania protozoa) cell membranes, forming pores

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Artemisinin

A

Antimalarial
Prodrug of dihydroartemisinin
Generates highly reactive organic free radicals
Short but rapid action
Also prevent development of oocyst in mosquito

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Bacitracin

A

Cyclic peptide antibiotic
Forms a very tight complex with Mg2+ and bactoprenol pyrophosphate, inhibits dephosphorylation to bactoprenol phosphate so inhibits regeneration of the lipid carrier (for NAM-NAG unit), and hence, the biosynthesis of PG
It is active against Gram-positive bacteria.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Bevacizumab

A

A humanised monoclonal antibody that binds and inhibits the human VEGF
Anti-angiogenic - can interfere with wound healing
anti-VEGF

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Cephalosporin

A

B-lactam antibiotic with B-lactam and thiazolidine ring
B-lactamases result in hydrolytic ring opening and deactivation
Rotating use of antibiotics improves efficacy and reduces emergence of resistance

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Chloramphenicol

A

Bacteriostatic broad spectrum antibiotic
Interfere with protein biosynthesis
Target 50S ribosomal subunit
Blocks amino-acyl tRNA interaction with A site of peptidyl transferase centre
Resistance by inactivating acetyltransferases
Can cause bone marrow suppression

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Chloroquine

A

Antimalarial
Accumulates inside food vacuole
(Plasmodium use hemaglobin as N source. Toxic heme polymerised to non-toxic hemozoin in food vacuole. )
Inhibit heme polymerization reaction in plasmodium
Drug resistance by exclusion of drug from site of action
Efflux by CRT (chloroquine resistance transporter)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Ciprofloxacin

A

Synthetic fluoroquinolone antibiotic
Activity against gram +ve and -ve bacteria
inhibits type II DNA topoisomerases (DNA gyrase and topo IV)
Inhibits changes in supercoiling in replication and gene expression
Used against Bacillus anthracis in anthrax and Pseudomonas infections - oral therapy preferred

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Cisplatin

A

Anti-cancer
Platinum compound that binds directly to DNA to prevent replication and expression
Only active in cis form
Cross-linking agent in DNA
React at N7 of guanine and adenine
Intrastrand cross-link of 2 neighbouring guanines pGpG
Major bending of duplex to major groove
Inhibit DNA polymerase and DNA replication
Resistance - cells have higher levels of DNA repair enzymes
Used IV
Renal toxicity and bone marrow suppression

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Clavulanate

A

Suicide substrate for lactamase

Forms a slowly hydrolysing acyl enzyme intermediate

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Augmentin

A

Amoxicillin + Clavulanate

B-lactam antibiotic + B-lactamase inhibitor

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Co-trimoxazole

A

Antibiotic acting as anti-metabolite
Trimethoprim + sulfamethoxazole
Both block a step in biosynthesis of folic acid
Work together synergistically

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Cyclophosphamide

A

Anti-cancer
Nitrogen mustard - covalently link alkyl group to chemical moieties in nucleic acids and proteins
Broad application in cancer chemotherapy
Absorbed well orally and do not accumulate in a particular tissue
Metabolised by cytochrome P450 in liver to active phosphoramide mustard

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Doxorubicin

A

Anti-cancer
Anthracycline, bind non-covalently to DNA
Prevent replication and expression
Generate free radicals due to hydroxyquinone moiety –> DNA cleavage and lipid peroxidation
Inhibitor of type 2 topoisomerase
Antibiotic - intercalates into DNA (local injection)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Erlotinib

A

Orally active
Small molecule ligand that inhibits EGFR tyrosine kinase
(Lung cancer)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Erythromycin

A

14-membered Macrolide antibiotic
Targets 23S rRNA in 50S ribosomal subunit
Bind 23S rRNA at entrance to polypeptide export tunnel
Allow 6-8 oligopeptidyl tRNA build up before terminating
Competitive with lincosamide antibiotics
Can be bacteriostatic or bactericidal
Resistance - inactivation by enzymatic hydrolysis
Second choice for penicillin allergies
Gram +ve
Short elimination half life

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Etoposide

A

Inhibitor of human type 2 topoisomerase
Resistance can be due to modified topoisomerases
Cancer

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Fansidar

A

A combination of sulfadoxin and pyrimethamine
Against Plasmodium falciparum malaria
Used when chloroquine resistance is suspected and oral treatment is
appropriate

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Fluconazole

A

Antifungal synthetic triazole
Inhibits enzymes in ergosterol biosynthesis
Affects membrane permeability and activity of membrane associated enzymes
Resistance due to active azole efflux and alterations in activity and amount of enzymes
Athletes foot and vaginal cadidiasis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

Flutamide

A

Oral anti-androgen
Prostate cancer
Competes with testosterone and powerful metabolite, dihydrotestosterone
Prevents stimulation of growth of prostate cancer cells

24
Q

Fosfomycin

A

Inhibits cell wall biosynthesis

Inhibits pyruvyl transferase (transfers PEP to UDP-NAG in production of UDP-NAM-tripeptide)

25
Fusidic acid
Affects protein synthesis Binds and inhibits elongation factor G, preventing movement of 30S subunit along mRNA, blocking translocation Narrow spectrum, for staphylococcal infections
26
Goseraline
Decapeptide analogue of GnRH that binds tightly and disrupts endogenous hormonal feedback, causing down-regulation of testosterone and estrogen production Biochemical castration
27
Imatinib
Specific inhibitor of a number of tyrosine kinase enzymes (c-kit , which is over-expressed in gastro-intestinal stromal tumours GISTs) Inhibits BCR-ACL protein kinase activity, active in CML
28
Isoniazid
Prevention and treatment of M Tuberculosis | Inhibits biosynthesis of Mycolic acid in cell envelope
29
Leucovorin
Adjuvant in canver chemotherapy involving methotrexate Used in combination with 5-fluorouracil Salvage normal tissues from folate depletion Readily converted to reduced folic acid derivatives Does not require action of dihydrofolate reductase, so function as vitamin unaffected by inhibition of these enzymes
30
Methicillin
ß-lactam antibiotic Inhibit peptidoglycan-crosslinking transpeptidase enzymes by covalent and irreversible binding as a pseudosubstrate Resistance with mecA gene, and fem which adds pentaglycyl crossbridge to PG, making it a better MecA substrate
31
Methotrexate
Antimetabolite and antifolate Inhibits folic acid metabolism Folic acid antagonist Inhibits dihydrofolate reductase Similar to trimethoprim (bacterial) and pyrimethamine (protazoal) Competes with folic acid for active transport into mammalian cells Toxicity to normal tissues, so used with Leucovorin Resistance based on enhanced expression of DHFR or reduced uptake from mutations in folate carrier
32
Miconazole
Antifungal synthetic imidazole Inhibits enzymes in ergosterol biosynthesis Also active against Leishmania, due to ergosterol membrane
33
Mitomycin C
Aziridine containing antibiotic that alkylates and cross-links DNA Cross-linking of 2 G bases, preventing separation of strands Selectively inhibits DNA synthesis in bacteria and tumour cells Activated by reduction of the quinone group
34
Mitoxantrone
Anthracycline Anti-cancer Modified structure so lack quinone type free radical generation Resistance by drug efflux by transporters
35
Nevirapine
Anti-HIV Non nucleoside reverse transcriptase inhibitor Used in HAART therapy Bind and denature catalytic site of enzyme
36
Penicillin
Bactericidal B-lactam antibiotic Selective toxicity and large therapeutic index Inhibit PG cross-linking transpeptidases by forming a slowly hydrolysing covalent acyl enzyme intermediate Contains B-lactam and thiazolidine ring Resistance by B-lactamases and penicillin-binding proteins
37
Prednisone
Synthetic corticosteroid prodrug, converted by liver to prednisolone Inhibits growth of lymphocytes in leukemias
38
Pyrimethamine
Inhibits dihydrofolate reductase in plasmodium falciparum | Anti-protazoa
39
Rifampin
Bactericidal, inhibit RNA synthesis Binds B-subunit of DNA dependent RNA polymerase (tight but non-covalent) Directly blocks elongating RNA chain - prevents initiation of RNA synthesis Synthesis in progress at time of exposure is unaffected Intrinsic resistance by fungi, because drug does not readily enter envelope, so concentration is low Used to treat mycobacterium infections
40
Saquinavir
Inhibit HIV protease, essential for viral replication and release of virus particles Used in HAART therapy
41
Streptomycin
Aminoglycoside, affects protein synthesis, acts on 30S subunit Binds the 30S subunit near the A site for aminoacyl-tRNA binding Cause disruption in decoding and translational accuracy, decrease in the fidelity of translation Nephrotoxicity and ototoxicity Gram negative rods
42
Sulfadoxin
Sulfa drug, competitively inhibits dihydropteroate synthase in plasmodium
43
Sulfamethoxazole
Antimetabolite antibiotic A sulfa drug; p-aminobenzoate analogue Competitively inhibits dihydropteroate synthase in the biosynthesis of tetrahydrofolate (methyl carrier required for synthesis of dTMP).
44
Suramin
Used for human trypanosomiasis Does not contain toxic metal, so high therapeutic index inhibits glycerol-3-phosphate oxidase and NAD+-dependent glycerol-3-phosphate dehydrogenase Interferes with the reoxidation of NADH, and inhibits ATP synthesis
45
Tamoxifen
Orally-active oestrogen receptor antagonist used in the treatment of breast cancer Signal transduction inhibitor Attenuates transcription of estrogen responsive genes involved in breast cancer Exerts estrogen agonist effects in other tissues such as bone and uterus
46
Taxol
Causes assembly of microtubules from tubulin dimers Causes stabilization of ordinary cytoplasmic microtubules and the formation of abnormal bundles of microtubules Taxane, mitotic inhibitor
47
Tetracycline
Bacteriostatic antibiotic Polyketide antibiotic; binds to 16 rRNA in 30S subunit of ribosome and inhibits the movement of aminoacyl-tRNA into the A site Effective against a wide range of bacteria, and are first-line drugs against mycoplasma and cholera Drug toxicity associated with binding of calcium in bones and teeth. Resistance - specific tetracycline efflux transporters
48
Topotecan
Inhibit human type 1 topoisomerase | Ovarian and lung cancer
49
Trastuzumab
A humanised monoclonal antibody against the human epidermal growth factor receptor 2 (HER2) in breast cancer IV once a week Can cause cardiac dysfunction
50
Trimethoprim
Antimetabolite antibiotic | Inhibits dihydrofolate reductase in folic acid biosynthesis (tetrahydrofolate)
51
Valinomycin
Antibiotic acting on cytoplasmic membrane Ionophoretic capacity Electroneutral, but carries single +ve charge of K+ A cyclic peptide antibiotic that binds K+, and facilitates K+ diffusion across the membrane
52
Vancomycin
Glycopeptide antibiotic Binds pentapeptidyl tails in PG repeating unit terminating in D-Ala-D-Ala Prevents transpeptidation Effective against Clostridium Difficile and used IV for Gram +ve cocci
53
Vinblastine
Vinca alkaloid Antimitotic drug Anti-cancer
54
Zanamivir
Inhibits neuraminidase, a glycoprotein enzyme, of Influenza A and maybe B Enhance viral aggregation and inhibit release from the host cells
55
Zidovudine AZT
Nucleoside reverse transcriptase inhibitor Thymidine analogue Used in HAART treatment

MODA List 1 (8 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2025 Bold Learning Solutions. Terms and Conditions