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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
5-Fluorouracil
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
26
Flutamide
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.
27
Foscarnet
Organic analogue of pyrophosphate Inhibits DNA polymerase of cytomegalovirus and herpes virus. Prevents the cleavage of pyrophosphate from nucleoside triphosphate during DNA polymerization
28
Fosfomycin
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
Fusidic acid
Inhibits elongation factor G Inhibits the movement of the 30S subunit by one codon along the mRNA. Narrow spectrum Used against staphylococcal infections.
30
Goseraline
Decapeptide analogue of gonadotropin-releasing hormone Disrupts endogenous hormonal feedback systems Causes down-regulation of testosterone and estrogen production.
31
Imatinib
2-phenylaminopyrimidine derivative Inhibitor of tyrosine kinase enzymes, eg. BCR-ABL Is used in treating chronic myeloid leukemia, and gastrointestinal stromal tumours. Gleevec.
32
Isoniazid
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
Leucovorin
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
Lomustine
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
Melarsoprol
Generates melarsen oxide Contains arsenite Preferentially toxic for Trypanosoma species
36
Melphalan
Nitrogen mustard alkylating agents Phenylalanine derivative Used to treat chronic myeloid leukaemia. Preferentially accumulates in melanomas
37
Methicillin
ß-lactam antibiotics Inhibits peptidoglycan-crosslinking transpeptidase enzymes by covalent and irreversible binding as a pseudosubstrate.
38
Methotrexate
Antimetabolite and antifolate drug. Inhibits the metabolism of folic acid. Replaced the more powerful and toxic antifolate aminopterin.
39
Miconazole
Imidazole antifungal and antiprotozoal drug. Inhibits ergosterol biosynthesis.
40
Mitomycin C
Aziridine-containing antibiotic Alkylates and cross-links DNA Prevents strand separation during DNA replication and transcription.
41
Mitoxantrone
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
Oseltamivir
Inhibits neuraminidase Prevents release of the virion progeny from infected cells Hinders movement of the virus particles through the upper respiratory tract.
43
Nevirapine
Anti-HIV drug Non-nucleoside reverse transcriptase inhibitor. Binds to the enzyme near the catalytic site and denatures it.
44
Penicillin
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
Prednisone
Synthetic corticosteroid prodrug Converted by the liver into prednisolone, Inhibits growth of lymphocytes in leukemias.
46
Pyrimethamine
Analogue of the antibiotic trimethoprim Inhibits dihydrofolate reductase in Plasmodium.
47
Rifampin
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
Saquinavir
HIV protease inhibitor Protease vital for both viral replication within the cell and release of mature viral particles from an infected cell
49
Streptomycin
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
Sulfadoxin
Sulfa drug Inhibits dihydropteroate synthase in Plasmodium. Analogue of the antibiotic sulfamethoxazole
51
Sulfamethoxazole
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
Suramin
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
Tamoxifen
Orally-active oestrogen receptor antagonist Used against breast cancer Has oestrogen agonist effects in bone and uterus
54
Taxol
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
Tetracycline
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
Topotecan
Topoisomerase I inhibitor. Used to treat ovarian cancer and lung cancer.
57
Trastuzumab
Humanised monoclonal antibody against the human epidermal growth factor receptor 2 (HER2) IV administration Can cause cardiac dysfunction, especially if administered with anthracyclines.
58
Trimethoprim
Inhibits dihydrofolate reductase in the biosynthesis of tetrahydrofolate.
59
Valinomycin
Cyclic peptide antibiotic Binds K+, and facilitates K+ diffusion across the membrane Electroneutral
60
Vancomycin
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
Vinblastine
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
Vinca alkaloids
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
Zanamivir
Inhibits neuraminidase Prevents budding and release of virion progeny from infected cells Hinders movement of the virus particles through the upper respiratory tract.
64
Zidovudine (azidothymidine, AZT)
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
Anthracyclines
Intercalate into DNA
66
HAART
Combination of nevirapine, zidovudine and saquinavir Used during serious manifestations in AIDS patients

MODA Drug Flashcards (7 decks)

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