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Exam Questions > Drugs > Flashcards

Drugs Flashcards

1
Q

Rosiglitazone

A

Glitazone - PPAR agonist, increase gene transcription - improve insulin resistance

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2
Q

Metformin

A

Multiple MOA, for diabetes, PCOS

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3
Q

Sitagliptin

A

DPP-4 inhibitor - blocks DPP-4 enzyme which then increases insulin production, blocks glucose release from liver

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4
Q

Exenatide

A

GLP-1 agonist - blocks glucose release from liver, slows glucose absorption from the gut, increases insulin secretion, gives sensation of fullness.

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5
Q

Methotrexate

A

Folate antagonist - DHFR inhibitor this prevents formation of active tetrahydrofolate. Folate required to DNA and RNA formation

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6
Q

Doxorubicin, Idarubicin, Daunorubicin

A

Anthracycline - cytotoxic agent, intercalation of DNA base pairs and prevent DNA repair by inhibiting topoisomerase 1 & 2

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7
Q

Flurouracil

A

Pyrimidine analogue. Thymidylate synthase inhibitor, this blocks the pathway leading to a lack of of dTMP. dTMP is required for DNA.

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8
Q

Mercaptopurine

A

Purine analogue - competes with purine derivities for HGPRT enzyme. It is converted TIMP then incorporated into DNA leading to base pair mismatch and strand breaks.

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9
Q

Paclitaxel

A

Taxane - stabilises microtubules by binding to b tubulin inside microtubules. This freezes cell in mitosis and activates apoptosis.

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10
Q

Cyclophosphamide

A

Nitrogen mustard - intrastand linking and cross-linking resulting in DNA strand breaks.
Anklyating agent

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11
Q

Thiotepa

A

Ethyleneimines - intrastand linking and cross-linking resulting in DNA strand breaks.
Anklyating agent

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12
Q

Busulfan

A

alkyl sulfonates - intrastand linking and cross-linking resulting in DNA strand breaks.
Anklyating agent

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13
Q

Carmustine

A

Nitrosoureas - intrastand linking and cross-linking resulting in DNA strand breaks.
Anklyating agent

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14
Q

Dacarbazine

A

Triazenes - intrastand linking and cross-linking resulting in DNA strand breaks.
Anklyating agent

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15
Q

Oxaliplatin

A

Platinum compound - Displaces chloride ions leaving positively charged ions in the cell to act against DNA eventually leading to apoptosis

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16
Q

Irinotecan

A

Topoisomerase 1 inhibitor - unzips the DNA exposing bases, prevents binding of base pairs and closure of DNA. Able to complete protein synthesis.

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17
Q

Etoposide

A

Topoisomerase 2 inhibitor - breaks DNA strand and reattaches stand at another location

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18
Q

Vincristine

A

Vinca Alkaloid - binds to tubulin and inhibits polymerisation and microtubule formation. This then prevents spindle formation in mitosis.

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19
Q

Mensa

A

Protects bladder and kidneys. Attaches to oxidative metabolities of chemotherapy agents to detoxify acrolein.

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20
Q

Carbimazole

A

used to treat hyperthyroidism. pro-drug converted to methimazole. This prevents thyroid peroxidase enzyme from iodinating tyrosine residues hence decreasing production of T3 and T4

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21
Q

Ulipristal , Levongesterol

A

SPRM. Partial agonist as well as antagonist properties at the progesterone receptor., also weak antiglucocorticoid. Used for emergency contraception

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22
Q

Human chorionic gonadotrophin (HCG)

A

Extracted from urine - induces ovulation

23
Q

choriogonadotrophin alfa (rHCG)

A

recombinate form - induces ovulation

24
Q

Follitropin

A

Recombinate form of FSH - stimulates follicular development and controlled ovulation

25
Q

Corifollitropin alfa

A

modified FSH - stimulates follicular developed and controlled ovulation

26
Q

Lutropin alfa

A

recombinate LH - stimulates follicular development

27
Q

Triptorelin

A

GnRH agonist - initially stimulates gonadrotrophin release but this ultimately causes negative feedback and inhibits secretion. Used to prevent premature release of oocytes and used in endometriosis

28
Q

Goserelin

A

GnRH agonist - initially stimulates gonadrotrophin release but this ultimately causes negative feedback and inhibits secretion. Used to prevent premature release of oocytes and used in endometriosis

29
Q

Clomiphene

A

Estrogen modulator - partial agonist at ovary antagoinst at hypothalamus and pituitary. Fools thalamus into believing there is a lack of estrogen so increases FSH release stimulating ovulation.

30
Q

Lapatinib

A

Tyrosine kinase inhibitor. Blocks TK activity in various ECFR families including HER2. Binds to ATP-binding pocket preventing self phosphorylation

31
Q

Trastuzumab

A

Monoclonal antibody that binds to HER2. Causes inhibition of pathway and flags cell for destruction

32
Q

Trastuzumab emtansine

A

Monoclonal antibody against HER2 + cytotoxic agent

33
Q

Pertuzumab

A

A monoclonal antibody which binds to HER2 preventing dimerization and disrupts signaling

34
Q

Bevacizumab

A

A monoclonal antibody blocks angiogenesis by inhibiting VEGF A. This inhibits cell growth by disrupting blood flow.

35
Q

Rituximab

A

Monoclonal antibody against CD20 on b-cells. Encourages apoptosis, antibody-dependant cell death (NK cells) and complement medicated cell death

36
Q

Tositumomab

A

Murine IgG2a lambda monoclonal antibody against CD20 on b-cells. It is combined with radioisotope iodine 131 to provide targeted radiation

37
Q

What is the Philadelphia chromosome?

A

A traslocation of genetic material between Chromosomes 9 and 22. On chromosome 22 the BCR-ABL1 gene is formed which produces a tyrosine kinase that is ‘always on’. Seen in leukaemia esp. CML.

38
Q

Imatinib

A

Tyrosine kinase inhibitor - works by occupy the TK site reducing activity. In CML it targets the TK produced by the Philadelphia chromosome. It binds close to the ATP binding site locking the receptor.

39
Q

Bortezomib

A

Binds to a subunit of the 20s of the 26s proteasome. This prevents degradation of proteins leading to cell apoptosis from protein build up.

40
Q

L-asparagine (colaspase)

A

Leukaemic cells do not ahve the ability to produce asparagine (a non-essential amino acid which maintains DNA and RNA). L-asparagine depletes plasma levels of asparagine in leukaemic cells by converting to ammonia. This leads to less DNA, RNA and protein production and leads to apoptosis. Normal cells able to produce asparagine so not affected.

41
Q

Tamoxifen

A

SERM- Partial oestrogen antagonist in breast and agonist in bone

42
Q

Fulvestrant

A

SERD- Fulvestrant is a antiestrogen which acts as an antagonist of the estrogen receptor (ER) and additionally as a selective estrogen receptor degrader (SERD).

43
Q

Anastrazole

A

Aromatase inhibitor- blocks conversion of androgen to oestrogen.

44
Q

Temazepam

A

Benzo- enhances GABA-A receptor causing sedation and muscle relaxation.

45
Q

Abiraterone

A

inhibits CYP17A1 an enzyme that catalyzes the biosynthesis of androgens. decrease serum levels of testosterone and other androgens.

46
Q

Leuprorelin

A

GnRH agonist. Leads to increase at start but then leads to gradual decrease over several weeks. Use to treat prostate cancer.

47
Q

Rasburicase

A

Helps clear uric acid from the urine that builds up from increased cell death. Also use allopurinal. catalyses the enzymatic oxidation of uric acid into a more soluble metabolite. Urate oxidase

48
Q

neostigmine

A

Interfers with the breakdown of Ach. Blocks the active site AchE preventing the breakdown of Ach.

49
Q

Sugammadex

A

Forms a complex with rocuronium or vecuronium.

50
Q

gemcitabine

A

Enters the cell and is phosphorylation 3 times into an active form gemcitabine triphosphate. It then incorporates itself into DNA

51
Q

Nifidipine

A

Tocolytic- Supress labour by causing relaxation of uterine smooth muscle. Usually given with corticosteroids for surfactant in premature babies.

52
Q

bromocriptine

A

Dopamine agonist- Acts on D2 receptor for laction in pituitary lactinomas.

53
Q

Dutasteride

A

5α-reductase inhibitors, which block the action of the 5α-reductase enzymes that convert testosterone into DHT

Exam Questions (5 decks)

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