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MODA Drug Flashcards > Chemotherapy > Flashcards

Chemotherapy Flashcards

1
Q

Aciclovir

A

Purine analogue

Upon activation by viral thymidine kinase, phosphorylated compound competitively inhibits viral DNA polymerase.

Also acts as chain terminator.

Is present in Zovirax creams against herpes simplex infections of the skin and mucous membranes.

Aciclovir is 30 times more potent against the viral DNA polymerase that the host enzyme.

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2
Q

Amantadine

A

Blocks the function of M2 ion channel protein involved in nucleocapsid uncoating of influenza virus.

At a later stage, it interferes with hemagglutinin processing

Is used predominantly in prophylaxis and treatment of infections by Influenza A virus.

Not effective against Influenza B virus

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3
Q

Amoxicillin

A

ß-lactam antibiotic

Inhibits peptidoglycan-crosslinking transpeptidase enzymes by covalent and irreversible binding as a pseudosubstrate.

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4
Q

Amphotericin B

A

Polyene antifungal and antiparasitic drug

Forms pores in the membrane by an ergosterol-dependent mechanism.

Is currently the drug of choice for most systemic mycoses: active against Cryptococcus, Candida, and Aspergillus.

Low degree of selective toxicity and a low therapeutic index

Can be administered systemically

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5
Q

Anastrozole

A

Aromatase inhibitor

Prevents conversion of androgen precursors to estradiol

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6
Q

Artemisinin

A

Antimalarial

Prodrug of the biologically active metabolite dihydroartemisinin.

Active during the stage when the parasite is located inside red blood cells.

Mode of action through generation of highly reactive organic free radicals

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7
Q

Bevacizumab

A

Anti-VEGF monoclonal antibody

Humanised mAb

Bevacizumab is administered in combination with 5-fluoro-uracil for the treatment of metastatic colorectal cancer.

Anti-angiogenic so can interfere with wound healing

Can cause hypertension and proteinuria

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8
Q

Cephalosporin

A

Class of β-lactam antibiotics

Inhibits the transpeptidation reaction by which cross-links are formed between PG strands

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9
Q

Cetuximab

A

Anti-EGFR monoclonal antibody

Human/mouse chimeric monoclonal antibody that binds to the extracellular domain of EGFR

Reverses the resistance of colorectal cancer to the topoisomerase inhibitor irinotecan, and is used in combination with irinotecan in the treatment of EGFR over-expressing metastatic colorectal cancer in patients who are refractory to irinotecan

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10
Q

Chloramphenicol

A

Blocks aminoacyl tRNA binding to P site 50S subunit of ribosome.

Prevents peptide bond formation

Very effective broad-spectrum antibiotic but use is restricted because of bone marrow suppression in some cases.

Drug is indicated in life-threatening infections such as meningitis

Bacteriostatic

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11
Q

Chloroquine

A

Antimalarial 4-aminoquinoline drug

Accumulates inside food vacuole of intraerythrocytic parasite and inhibits haem polymerisation reaction

Inhibits antigen presentation in dendritic cells - used in rheumatoid arthritis

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12
Q

Ciprofloxacin

A

Fluoroquinolone antibiotic

Inhibits type II DNA topoisomerases (DNA gyrase and topo IV)

Inhibits changes in supercoiling required for replication and gene expression.

FDA- approved drug for killing Bacillus anthracis in anthrax infections.

Particularly useful for Pseudomonas infections where oral therapy is preferred, such as respiratory tract infections in patients with cystic fibrosis

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13
Q

Cisplatin

A

Platinum-based drug used to treat various types of cancers, including sarcomas, some carcinomas (e.g. small cell lung cancer, and ovarian cancer), lymphomas and germ cell tumours.

Binds covalently to DNA

Intra-strand cross-linking agent principally at N7 sites of guanine and adenine

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14
Q

Clavulunate

A

ß-lactamase inhibitor

Forms a slowly hydrolysing acyl enzyme intermediate

Cannot inhibit class B ß-lactamase

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15
Q

Co-amoxiclav

A

It is a combination antibiotic consisting of amoxicillin trihydrate, a β-lactam antibiotic, and potassium clavulanate, a β-lactamase inhibitor

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16
Q

Co-trimoxazole

A

Combination of sulfamethoxazole and trimethoprim.

Sulfamethoxazole and trimethoprim each block a step in biosynthesis of folic acid

Sulfamethoxazole blocks the enzyme dihydropteroate synthase (DHPS)

Trimethoprim inhibits dihydrofolate reductase (DHFR)

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17
Q

Cyclophosphamide

A

Nitrogen mustard alkylating agent

Prodrug

Converted in the liver to active forms that have chemotherapeutic activity.

Used treatment of lymphomas, some forms of leukemia and some solid tumours.

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18
Q

Daunomycin

A

Anthracyclin

Rigid planar polycyclic antibiotic

Intercalate into DNA

Prevents normal replication and transcription of DNA

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19
Q

D-cycloserine

A

Structural analogue of D-Ala

Blocks the early stages of cell wall synthesis within the cytoplasm

Prevents the synthesis of pentapeptide by inhibiting L-Ala racemase, D-Ala-D-Ala synthetase and D-Ala-D- Ala/ muramyl tripeptide ligase.

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20
Q

Erlotinib

A

Small molecule ligand that inhibits EGFR tyrosine kinase

Orally active, potent, and selective quinazoline derivative

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21
Q

Erythromycin

A

14-membered macrolide antibiotic

Binds to 23S rRNA in 50S subunit to block chain elongation in protein synthesis

Blocks the polypeptide exit tunnel.

Similar antibacterial spectrum as penicillin

Suitable second-line drug for patients allergic to penicillin.

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22
Q

Etoposide

A

Inhibitor of the human enzyme topoisomerase II.

It is used in the treatment of lung cancer, testicular cancer, lymphoma, and non-lymphocytic leukaemia.

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23
Q

Fansidar

A

Combination of sulfadoxin and pyrimethamine

Analogous to antibacterial co-trimoxazole

Used in the treatment of patients with P. falciparum malaria when chloroquine resistance is suspected and oral treatment is appropriate.

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24
Q

Fluconazole

A

Triazole antifungal drug

Inhibits ergosterol biosynthesis.

Fluconazole is often used in the treatment of athlete’s foot and vaginal candidiasis.

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25
Q

5-Fluorouracil

A

Belongs to the family of antimetabolites

Pyrimidine analogue.

It is typically administered with leucovorin.

Some of its principal use is in colorectal cancer and pancreatic cancer

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26
Q

Flutamide

A

Oral anti-androgen drug primarily used to treat prostate cancer.

Competes with testosterone and its powerful metabolite, dihydrotestosterone (DHT) for binding to androgen receptors in the prostate gland.

Prevents their stimulation of growth of prostate cancer cells.

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27
Q

Foscarnet

A

Organic analogue of pyrophosphate

Inhibits DNA polymerase of cytomegalovirus and herpes virus.

Prevents the cleavage of pyrophosphate from nucleoside triphosphate during DNA polymerization

28
Q

Fosfomycin

A

Antibiotic that inhibits cell wall peptidoglycan biosynthesis

Inhibits pyruvyl transferase, the enzyme that catalyzes the transfer of the phosphoenolpyruvate group to UDP N-acetylglucosamine in the production of UDP N-acetyl muramyl-tripeptide.

29
Q

Fusidic acid

A

Inhibits elongation factor G

Inhibits the movement of the 30S subunit by one codon along the mRNA.

Narrow spectrum

Used against staphylococcal infections.

30
Q

Goseraline

A

Decapeptide analogue of gonadotropin-releasing hormone

Disrupts endogenous hormonal feedback systems

Causes down-regulation of testosterone and estrogen production.

31
Q

Imatinib

A

2-phenylaminopyrimidine derivative

Inhibitor of tyrosine kinase enzymes, eg. BCR-ABL

Is used in treating chronic myeloid leukemia, and gastrointestinal stromal tumours.

Gleevec.

32
Q

Isoniazid

A

First-line medication used in the prevention and treatment of tuberculosis.

Inhibits the biosynthesis of mycolic acids in the cell envelope of Mycobacterium tuberculosis.

33
Q

Leucovorin

A

Has vitamin activity that is equivalent to folic acid

Used to salvage normal tissues from folate depletion

Adjuvant used in cancer chemotherapy involving the drug methotrexate.

It is also used in synergistic combination with the chemotherapy agent 5-fluorouracil.

34
Q

Lomustine

A

Nitrosurea

Cross-links DNA to OTHER DNA strands or protein

Prevents DNA replication

Used against lymphoma (particularly cutaneous (skin) lymphoma) and melanoma, and tumours in kidney and lung.

Penetrates the blood/brain barrier so can be used to treat brain cancer

35
Q

Melarsoprol

A

Generates melarsen oxide

Contains arsenite

Preferentially toxic for Trypanosoma species

36
Q

Melphalan

A

Nitrogen mustard alkylating agents

Phenylalanine derivative

Used to treat chronic myeloid leukaemia.

Preferentially accumulates in melanomas

37
Q

Methicillin

A

ß-lactam antibiotics

Inhibits peptidoglycan-crosslinking transpeptidase enzymes by covalent and irreversible binding as a pseudosubstrate.

38
Q

Methotrexate

A

Antimetabolite and antifolate drug.

Inhibits the metabolism of folic acid.

Replaced the more powerful and toxic antifolate aminopterin.

39
Q

Miconazole

A

Imidazole antifungal and antiprotozoal drug.

Inhibits ergosterol biosynthesis.

40
Q

Mitomycin C

A

Aziridine-containing antibiotic

Alkylates and cross-links DNA

Prevents strand separation during DNA replication and transcription.

41
Q

Mitoxantrone

A

Anthracycline agent - intercalates into DNA

Does not show quinone-type free radical formation.

Used in the treatment of metastatic breast cancer, acute myeloid leukemia, and non- Hodgkin’s lymphoma.

42
Q

Oseltamivir

A

Inhibits neuraminidase

Prevents release of the virion progeny from infected cells

Hinders movement of the virus particles through the upper respiratory tract.

43
Q

Nevirapine

A

Anti-HIV drug

Non-nucleoside reverse transcriptase inhibitor.

Binds to the enzyme near the catalytic site and denatures it.

44
Q

Penicillin

A

ß-lactam antibiotics

Bacteriocidal

Inhibits peptidoglycan-crosslinking transpeptidase enzymes by covalent and irreversible binding as a pseudosubstrate.

Acts at the outside surface of the cytoplasmic membrane

45
Q

Prednisone

A

Synthetic corticosteroid prodrug

Converted by the liver into prednisolone,

Inhibits growth of lymphocytes in leukemias.

46
Q

Pyrimethamine

A

Analogue of the antibiotic trimethoprim

Inhibits dihydrofolate reductase in Plasmodium.

47
Q

Rifampin

A

Binds to β subunit of the DNA-dependent RNA polymerase

Binds at the exit tunnel

Inhibits initiation of RNA synthesis.

Often used to treat infections by Mycobacterium.

Cannot cross fungal cell envelope

48
Q

Saquinavir

A

HIV protease inhibitor

Protease vital for both viral replication within the cell and release of mature viral particles from an infected cell

49
Q

Streptomycin

A

Aminoglycoside antibiotic

Targets 30S subunit of ribosome and decrease fidelity of mRNA translation.

Streptomycin exhibits nephrotoxicity and ototoxicity, can cause seizures at toxic levels

Used against Gram-negative rods including Pseudomonas and Proteus and TB - narrow spectrum

Bactericidal

Shows synergy with beta-lactam antibiotics

50
Q

Sulfadoxin

A

Sulfa drug

Inhibits dihydropteroate synthase in Plasmodium.

Analogue of the antibiotic sulfamethoxazole

51
Q

Sulfamethoxazole

A

Sulfa drug

Blocks the enzyme dihydropteroate synthase (DHPS)

p-aminobenzoate analogue that competitively inhibits dihydropteroate synthase in the biosynthesis of tetrahydrofolate (methyl carrier required for synthesis of dTMP).

52
Q

Suramin

A

Trypanocidal (kills trypanosomes)

Does not contain toxic metal, hence, its therapeutic index is much higher than that of melarsen.

Molecular mechanism still unknown;

Might act on glycolytic enzymes.

53
Q

Tamoxifen

A

Orally-active oestrogen receptor antagonist

Used against breast cancer

Has oestrogen agonist effects in bone and uterus

54
Q

Taxol

A

Taxane

Disrupts the equilibrium between free tubulin dimers and microtubules by shifting it in the direction of assembly rather than disassembly

Causes formation of abnormal bundles of microtubules

Mitotic inhibitor used to treat patients with lung, ovarian, breast cancer, head and neck cancer, and advanced forms of Kaposi’s sarcoma.

55
Q

Tetracycline

A

Broad spectrum polyketide antibiotic

Binds to 16 rRNA in 30S subunit of ribosome

Inhibits the movement of aminoacyl-tRNA into the A site.

First-line drugs against mycoplasma and cholera.

Drug toxicity is associated with binding of calcium in bones and teeth.

Some activity against protozoa, including Plasmodium

56
Q

Topotecan

A

Topoisomerase I inhibitor.

Used to treat ovarian cancer and lung cancer.

57
Q

Trastuzumab

A

Humanised monoclonal antibody against the human epidermal growth factor receptor 2 (HER2)

IV administration

Can cause cardiac dysfunction, especially if administered with anthracyclines.

58
Q

Trimethoprim

A

Inhibits dihydrofolate reductase in the biosynthesis of tetrahydrofolate.

59
Q

Valinomycin

A

Cyclic peptide antibiotic

Binds K+, and facilitates K+ diffusion across the membrane

Electroneutral

60
Q

Vancomycin

A

Glycopeptide antibiotic

Binds to D-Ala-D-Ala termini of the pentapeptide in peptidoglycan

Prevents its cross-linking to a neighbouring pentapeptide in another peptidoglycan strand.

Effective against Clostridium difficile

Used intravenously against Gram-positive cocci, such as Enterococcus and Staphylococcus.

61
Q

Vinblastine

A

Vinca alkaloid

Interactions with the tubulin dimer prevent microtubule assembly, and hence, result in the disappearance of microtubules

Anti-mitotic drug used to treat Hodgkin’s lymphoma, non-small cell lung cancer, breast cancer and testicular cancer.

62
Q

Vinca alkaloids

A

Including colchicine and podophyllotoxin

Bind to free tubulin dimers

Interactions with the tubulin dimer prevent microtubule assembly, and hence, result in the disappearance of microtubules

63
Q

Zanamivir

A

Inhibits neuraminidase

Prevents budding and release of virion progeny from infected cells

Hinders movement of the virus particles through the upper respiratory tract.

64
Q

Zidovudine (azidothymidine, AZT)

A

Anti-HIV drug

Nucleoside reverse transcriptase inhibitor

Thymidine analogue.

Must be phosphorylated by host cell enzymes before becoming active

Chain terminator as lacks 3’ OH group

65
Q

Anthracyclines

A

Intercalate into DNA

66
Q

HAART

A

Combination of nevirapine, zidovudine and saquinavir

Used during serious manifestations in AIDS patients

MODA Drug Flashcards (7 decks)

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