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Pharmacology > Anticancer drugs > Flashcards

Anticancer drugs Flashcards

1
Q

Non cell cycle specific

A

Alk agents
Platinum compounds
Antitumor antibiotics

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2
Q

Cell cycle specific

S phase inhibitors

A

Antimetabolites
Hydroxyurea
Topoisomerase inhibitors
Histone deacetylase inhibitors

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3
Q

M cycle specific

A 
Vinca alkaloids
Taxanes
Epothilones
Estramustine
Eribulin
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4
Q

Mucositis

A

Alk agents
5fu
cytarabine
Mtx

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5
Q

Maximum Alopecia

A

Alk agents
Anthracyclines
Topoisomerase inhibitors

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6
Q

Dose limiting toxicity

A

Bone marrow suppresion

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7
Q

Maximum emesis

A

Cysplatin>carmustine>anthracyclines>high dose cyclophosphamide>dacarbazine>mechlorethamine

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8
Q

Minimum emesis

A

Chlorambucil
busulfan
bleomycin

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9
Q

Early onset nausea

late onste nausea

A

Ondansetrron

late onset-palonosetron
aprepitant fosaprepitant-nk1 antagonists

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10
Q

Alkylating agents

Moa

A

Alkyl group of AA-Binds to H atom of dna at N 7 position-mispairing of guanine-thymine->cytotoxicity

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11
Q

Alkylating agents most specific for which phase

A

G1-S phase

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12
Q

Mc leukemia seen in Alk agents
Mechanism of action
Duration

A

AML due to chromosomal deletien at 5 7

4years

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13
Q

Mc leukemia seen with Cisplatin
Moa
duration

A

AML

Duration 2-3 yrs

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14
Q

Topoisomerase inhibitors

Mc leukemia MOA duration

A

AML

translocation of mixed lineage leukemia gene 11q23

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15
Q

Alkylating agents Classification

A

Nitrogen mustards
Nitrosoureas
Methylation
Misc

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16
Q

Meaning of bifunctional alk agents

A

Two reactive groups-cause Dna cross linking-high cytotoxicity

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17
Q

Alk agents with one reactive group

A

Drugs acting via meth

  1. procarbazine
  2. dacarbazine
  3. temozolomide
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18
Q

Drugs causing crosslinking dna

A

Cisplatin

mitomycin c

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19
Q

Nitrogen mustards classification

A 
Cyclophosphamide
Ifosfamide
mechlorethamine
melphalan
chlorambucil
bendamustine
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20
Q

Cyclophosphamide Metaboism and MOA

A

Metabolised by CYP2B6- 4hydroxycyclophosphamide-aldophosphamide and chloracetaldehyde
aldophosphamide-phospharamide mustard-anticancer effect
chloroacetaldehyde-neurotoxicity

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21
Q

hemmorhagic cystitis

A

acrolein

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22
Q

Neoplastic uses of cyclo

A

Breast and ovarian cancer
solid tumors in children
non hodgkins lymphoma

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23
Q

non neoplastic effect of cyclo

A

wegwners granulomatosis
RA
Steroid dependent NS

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24
Q

Hemmorhagic cystitis

A

Ifosfamide>cyclophosphamide
Treated by
Vigorous hydration
mesna

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25
Q

SE of cyclophosphamide

A

Hemmorhagic cystitis,neurotoxicity SIADH followed by hyponatremia
Bone marrow suppresion with relative sparing of platelets

Safe in renal dysfunction

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26
Q

Ifosfamide

uses

A

CYP450
Slowly metabolised therefore toxicity is much higher

Testicular cancer-BEP regimen add on
osteosarcoma

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27
Q

chloroacetaldehyde causes

A

Neurotox-GTCS,Ataxia,coma

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28
Q

Most neurotoxic

A

Ifosfamide>cyclophosphamude

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29
Q

Neurotox treatment

A

Methylene blue

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30
Q

which causes vesication

A

Mechlorethamine

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31
Q

Properies of melphalan

A

High plasma protein binding to both albumin and alpha 1 acid glycoprotein

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32
Q

Multiple myeloma treatment

A

Induction-Lenalidomide
Bortezomib
dexamethasone ->STem cell transplantation if age <70yrs(Melphalan is contraindicated due to cytotoxicity)

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33
Q

MAintenance of multiple myeloma

A

High risk-lenalidomide+bortezomib

low risk-lenalidmide

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34
Q

Uses of Chlorambucil and bendamustine

A

CLL and hodgkins lymphoma

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35
Q

Classification Nitrosoureas

A

Carmustine
Lomustine
Somustine
Stretpozocin

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36
Q

Uses of caarmustine and lomustine

A

HIghly lipid soluble-tt of brain cancers

37
Q

SE of Nitosoureas

A

SustINED NEUTROPENIA

38
Q

Streptozocin uses and properties

A

Precipitated in pancreatic b islet cells

used in pancreatic ca and carcinoid tumor

39
Q

AA by methylation drugs

A

Procarbaxine
dacarbazine
temozolomide

40
Q

Uses of dacarbazine

A

ABVD regmen of HL
malihnant melanoma
Sarcoma

41
Q

Procarbazine SE

A

Disulfiram like reacton

Cheese reaction

42
Q

uses of TEmozolomide

A

DOC-malignant brain tumors

Glioma,Astrocytoma

43
Q

Anticancer drug causing cataract

A

Busulfan also causes pulmonary fibrosis

44
Q

platinum compounds MOA

A

Free electrons of PC-Bind to N7 position of guanine in dna-formation of platinum based crosslinks-anticacncer effect and secondary leukemia AML

45
Q

Bivalent and Quadrivalent compounds

A

Cisplatina and carboplatin

oxiplatin

46
Q

Cisplatin mechanism of action

A

IV-combines with chloride ions becomes inactive-enters cells by copper transporter-chloride replaced by water group-becomes active

47
Q

inactivation of cisplatin

A

aluminium

48
Q

Dose of cisplatin

A

20mg/sq m/day

49
Q

cisplatin uses

A

Lung ca-Alongwith etoposide,gemcitabine,premetrexed
double platin therapy with carboplatin

GIT ca-DOC for esophageal and gastric ca alongwith taxanes and 5FU

Urogenital ca
Ovarian ca-cisplatin+paclitaxel 
Bladder ca-Gemcitabine+cisplatin
Testicular ca-Bleomycin+etoposide+cisplatn
CErvical ca-DOC

HEad and neck ca-cisplatin+5fu

Osteosarcoma

50
Q

Rx of small cell lung ca

A

Cisplatin,etoposide

51
Q

Rx of small cell lung cap

A

Cis,eto,vinorelbine->squamous variety-add gemcitabine

non squamous-premetrexed

52
Q

SE of Cisplatin

A

Nephrotoxicity,Ototoxicity-Bilateral high frequency irreversible hearing loss,Neurtotoxicity-Stock and glove peripheral sensorimotor neuropathy,Ememsis,Raynauds phenomenon

53
Q

NEphrotoxicity of cisplatin prevention

A

Forced diuresis by mannitol

Administration of 1-2L of Nacl-Inactivation of cisplatin by chloride compunds

54
Q

Protective uses of Nacl

A

with cisplatin and amphotericin b

55
Q

Uses of oxaliplatin

A

Colorectal ca,

Inhibits thymidilate synthetase therefore causes synergism with 5FU

56
Q

Carboplatin dose limiting toxicity

A

Thrombocytopenia

57
Q

Oxaliplatin dose limiting tox

A

peripheral neuropathy

58
Q

types of antitumor antibiotics

A

Anthracyclines and others

59
Q

Classification of anthracyclines

A

Derived from a fungus streptomyces peucetius

DOxorubicin,Danurubicin,Epirubicin,Valrubicin,Mitoxantrone

60
Q

other drugs under antitumor antibiotics

A

Actinomycin d
mitomycin c
Bleomycin

61
Q

Anthracycline toxicity

A

Requires Fe for free radical production therefore iron chelating agent dexrazoxane is used to prevent toxicity

62
Q

Topoisomerase inhibition

A

S phase inhibition

63
Q

free radical formation

A

G2 phase inhibition

64
Q

Doxorubicin uses

A

ovarian ca,osteosarcoma,lymphoma and multiple myeloma

65
Q

Danurubicin uses

A

used with doxo for tt of kaposi sarcoma

used alonwith cytrabine for tt of AML

66
Q

Epirubicin and valrubicin uses

A

breast and bladder ca

67
Q

SE of anthracyclines

A

Cardiotoxicity-maximum with doxo/dano
Acute-Pericarditis and myocarditis followed by arrhytmia
Chronic use-COngestive heart failure and dilated cardiomyopathy
Vacuolar myofibril degeneration in heart with chronic use

Vesication-doxo

Red discolouration of urine is seen with doxo/danorubicin

Radiation recall syndrome-Doxo/Dano/Actinomycin d

68
Q

lymphoma tt regimen

A 
NHL
low risk-FCR
1.Fludarabine
2.Cyclophosphamide
3.Rituximab

Intermediate risk/High risk CHOP-R

  1. Cyclophosphamide
  2. Hydroxydanorubicin
  3. Oncovin
  4. Prednisolone
  5. Rituximab
Hodgkins lymphoma
ABVD regimen
1.Adriamycin aka doxo
2Bleomycin
3.vincristine
4.Dacabazine
69
Q

bleomycin metabolism and SE

A

Metabolised by bleomycin hydrolase.
BH deficient in lungs and skin

Lungs-causes type 1 pneumocyte damage and type 2 compensatory hyperplasia-pulmonary fibrosis
Skin-flagellate dermatitis
Raynauds phenomena
acute hypertension

70
Q

Mitomycin c MOA and uses`andSE

A

MOA
inhibts topoisomerase2
alkylates DNA

uses-Anal and bladder cancer used topically
in post nasal surgery for synechia prevention and also ito prevent laryngoesophageal stensosi

SE
HUS
TTP
PF

71
Q

Dactinomycin MOA uses SE

A

Actinomycin d
Inhibits RNA polymerase

uses

  1. Choriocarcinoma
  2. wilms tumor
  3. Sarcoma

SE radiation recall syndrome

72
Q

Antimetabolites SE

A

Antifolate
purine analog
pyrimidine analog

Mucositis,diarrhoea,secondary leukemia not seen

73
Q

DNA SYNTHESIS

A

Dump-tmp by enzyme thymidylate synthase
TMP is required for Dna synthesis

Thymidylate synthase requires cofactor methyl group donated by THF (DHF-THF by enzyme DHFR)

Inhibition of DHFR inhibits DNA synthesis

74
Q

Methotrexate MOA

A

Inhibits DHFR and TS

MTX inhibits de novo purine synthesis which affects lymphocytes whivh have no salvage pathway

75
Q

Uses of MTX

A 
Metotrecat
Multiple sclerosis
Ectopic prego
Transplant rejection GVHD
Osteosarcoma
topically for psoriasis
rheumatoid arthritis it is DMARD of choice
Wegeners granulomatosis
All
Trophoblastic disease Chorioca
76
Q

SE of MTX

A

Myelosuppresion
To minimise Leucovorin is given
Mucositis

Renal toxicity-To use in patients with Renal failure given alongwith Glucarpidase which metabolises MTX into inactivr metabolites which are excreted in liver
Glucarpidase also breaks down leucovorin,therefore not given 2hr before or after intake of Leycoborin/folinic acid

Hepatotoxicity and Cirrhosis seen in prolonged tt

Crystalliuria-To prevent bicarbonate is given which alkalinzes the urine,MTX becomes more watet soluble as it is acidic drug

Intrathecal administration can cause meningismus,arachnoiditis and seizures

77
Q

RESISTANCE TO MTX

A

1.Dhfr enzyme induction(Acute resistance)<24hrs
2.chronic resistance
GENE MUTATION OR AMPLIFICATION >24HRS
3.Pgp pumps

78
Q

Pemetrexed uses and SE

A

Non small cell non squamous lung ca with xisplatin and in mesothelioma

SE
Less as compared to MTX,less potent inhibitor of DHFR also blocks TS,also block GART
low dose folinic or folic acid given to ameliorate toxicity
Inj B 12 also required

79
Q

pyrimidine analogs
5FU
MOA

A

5fu-metabolised in tumor cells into fluorodeoxyuridylmonophosphate fdump-competively inhibits Thymidylate synthase,
Leucovorin increases sensitivity of TS to fdump by forming ternary complex with fdump and TS

80
Q

Hand foot mouth syndrome causes

A

Palmar and plantar desquamation and erythema caused by 5FU,capecitabine,gemcitabine,doxorubicin and VEGFR and TK inhibitors

81
Q

5FU uses and SE

A

Uses
1.colorectal ca-FOLINIC ACID+5FU+OXALIPLATIN
FOLFIRI-FOLINIC ACID+5FU+IRINOTECAN
FOLFIRINOX-FOLINIC ACID +5FU+IRINOTECAN+OXALIPLATIN
2.Head and neck ca alongwith cisplatin
3.Anal carcinoma with mitomycin c as topical agent

SE

  1. Hand foot mouth syndrome
  2. pulmonary toxicity
  3. Acute coronary vasospasm
  4. In patients with deficient dihydropyrimidinedehydrogenase toxicity can develop
82
Q

Cytarabine MOA and SE

A

Inhibits DNA polymerase

Uses:
alongwith daunorubicin or idarubicin in AML
CML
High grade lymphoma
Lymphomatous meningitis

Myelosuppresion Drug limiting toxicity
high doses-cerbellar symptoms-dysarthhia,ataxia
cerebral tox-seizures and dementia

NON CARDIOGENIC PULMONARY EDEMA

83
Q

Gemcitabine uses and SE

A

Pancreatic ca
non small cell lung ca

HUS,interstital pneumonitis,posterior leukoencephalopathy

84
Q

Azacytadine and decitabine MOA uses

A

Cause demethylation of DNA

used in myelodysplasia

85
Q

Myelodysplasia with 5q syndrome tt

A

lenalidomide

86
Q

Treatment of Aml

A

V VINCRISTINE
P PREDNISOLONE
A ASPARAGINASE
D DAUNORUBICIN

87
Q

ALL TT

A

Cytarabine+Daunorubicin or idarubicin

88
Q

CLL TT

A

F Fludarabine
C Cyclophosphamide
R Rituximab

89
Q

CML TT

A

Imatinib

Pharmacology (2 decks)

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