Anticancer Drugs Flashcards

1
Q

Adjuvant chemo is used for what stage of cancer

Cancer where neoadjuvant is not given

A

Stage 1 and above

Thyroid cancer

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2
Q

Neoadjuvants are done for : (6)

A
  1. Breast cancer
  2. Bladder cancer
  3. CRC
  4. Esophageal cancer
  5. NSCLC
  6. Gastric Adenocarcinoma
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3
Q

Define langerhans histiocytosis
Rx.

A

Infiltration and accumulation of monocytes,macrophages, dendritic cells in affected tissues.
Can spontaneously regress.

Rx: corticosteroid + arabinoside-cytarabine + vincristine

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4
Q

Rx for osteosarcoma (5)

A

Rx of choice : surgery
Drugs :
1. High dose MTX
2. Cyclophosphamide
3. Cisplatin
4. Etoposide
5. Doxorubicin

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5
Q

Bone marrow sparing anticancer drugs (3)

A
  1. Vincristine
  2. Bleomycin
  3. Fludarabine
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6
Q

Rx for prostate cancer (3)

A

Leuprolide
Goserelin
GNRH antagonist : Degarelix

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7
Q

S/e of mechlorethane. S/e can be reversed by …….

A

BMS
GM-CSF

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8
Q

Classification of alkylating agents (5)

A
  1. Classic nitrogen mustards
  2. Nitrosureas
  3. Platinum compounds
  4. Triazines
  5. Others
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9
Q

Egs of nitrogen mustards (3)

A

Mechlorethamine- mustard HCL
Cyclophosphamide
Ifosamide (analogue of cyclophosphamide)

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10
Q

PK of nitrosureas (2)
Eg of nitroureas.

A

Excellent CNS penetrators. Used for Rx Glioblastoma multiformae

-mustine.

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11
Q

Nitrosurea causing renal damage
S/e of estramustine (2)

A

Semustine.

Gynecomastia, Thromboembolism

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12
Q

Egs of platinum drugs
Eg of triazines (3)

A

-platins

-Dacarbazine
-procarbazine
-temozolomide

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13
Q

Busulfan, chlorambucil are ……drugs

MOA of alkylating agents (3)

A

Alkylating drugs

Produce carbonium ions.
Results in DNA cross linking
abnormal base pairing
breakage of DNA strand.

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14
Q

First nitrogen mustard
Can be given as only ….
What happens if given topical

A

Mechlorethamine
Iv-local severe vesicant
If topical-cutaneous T cell lymphoma

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15
Q

Prodrug in nitrogen mustard
S/e of cyclophosphamide is due to ….

A

Cyclophosphamide —> phosphor amide mustard+ acrolein.

Haemorrhagic cystitis is due to Acrolein; protected by mesna.

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16
Q

Very high doses of cyclophosphamide causes ……(3)

A

Acute myocardial necrosis
Alopecia
SIADH

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17
Q

Ifosfamide S/e

A

Also a prodrug.
Ifosfamide—>
chloracetaldehyde + acrolein.
Chloracetaldehyde causes Nephro toxicity
Acrolein—> hge cystitis

More harmful than cyclophosphamide.
Increased neurotoxicity,nephrotoxicity,hge cystitis, platelet suppression.

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18
Q

Nitrogen mustards are called ….
Nephrotoxicity of cisplatin seen with in …..part of kidney.
S/e of cisplatin (3)

A

Radiomimetics - action ~ ionising radiation

PCT,DCT

Nephro toxicity
Ototoxicity- high frequency hearing loss
Neurotoxicity- sensory neuropathy

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19
Q

S/e of carboplatin-

S/e of oxaliplatin (2)

A

similar to cisplatin but milder, more myelosuppression.

Acute and chronic neurotoxicity
Reversible laryngopharyngeal spasm

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20
Q

Primary action of dacarbazine is on …..
Procarbazine acts mainly on…. S/e

A

RNA and protein synthesis

MAOI
Disulfiram like reaction with alcohol.

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21
Q

Action of temozolomide.
S/e (2)

A

Cross BBB - useful for GBM
They have increased bioavailability

Headache, constipation

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22
Q

Busulfan is specific for ….

Adrenal insufficiency can be seen with …..
Other s/e (4)

A

Myeloid tissue- granulocyte precursors

Busulfan
Hyperpigmentation
Hyperuricemia
Sterility
Pulmonary fibrosis

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23
Q

Busulfan active on ……. Tissue
Chlorambucil active on …….tissue

A

Myeloid
Lymphoid

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24
Q

Radiosensitizer for head and neck cancer is ….
Role of amifostine

A

Cisplatin

To decrease cisplatin induced nephrotoxicity

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25
Q

S/e of cytarabine
How does amifostine protect in head and neck cancer

A

Cerebellar ataxia

Protects against parotid gland atrophy due to radiation of H&N

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26
Q

Amifostine protects against

Gemcitabine is effective against …

A

Salivary glands
Skin
GIT
not CNS

Pancreatic cancer

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27
Q

Cisplatin induced N&V drug….

A

Palosetron

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28
Q

How is MTX DOC for choriocarcinoma?
Another drug added for rx of chorizo carcinoma is …..

A

Reduced folate carrier - transport MTX into cells. In choriocarcinoma; there is increased expression of RFC.

Actinomycin D

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29
Q

Uses of methotrexate

A
  1. Increased dose
    a. Osteosarcoma
    b. ALL
    c. Burkitts lymphoma
    d. CNS lymphoma ,choriocarcinoma.
  2. Low- moderate dose:
    Rheumatoid arthritis
    Psoriasis
    Ankylosing spondylitis
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30
Q

Low to moderate dose of MTX is …

MTX inhibits …..enzymes and thus decrease …..

Folinic acid is aka……

A

7.5-25 mg/week
DHFR
DNA & protein synthesis

Leucovorin
Citrovorum factor

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31
Q

When to give folinic acid ? (7)

A

Doses >100mg/m2
BMS
Mucositis
Acute renal failure
Idiosyncratic pneumonitis
Hepatotoxic
Rash

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32
Q

Hepatotoxic histopathology seen with MTX
MTX toxicity increase when….present

A

Macrovesicular fatty change

Effusion- pleural effusion, ascites present.

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33
Q

………is seen in extreme MTX toxicity
MTX use in Rheumatoid arthritis. How?

A

Reversible transient Oligospermia

Increase in extra cellular adenosine by MTX

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34
Q

MTX cleaving enzyme

Resistance to MTX is by ….(2)

A

Glucarpidase.

Increase in DHFR - gene amplification

Increase in P-gp - throws away any drug that comes into the cell. Responsible for MDR.

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35
Q

Verapamil can be used in anti cancer rx for property of …..

MTX toxicities include: (5)

A

Inhibit Pgp and increase anti cancer drug action.

  1. Myelosuppression
  2. Nephro, hepatotoxic
  3. Neuro- intrathecal and high dose
  4. Phototoxicity
  5. Pulmonary toxicity.
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36
Q

Drugs which increase toxicity of MTX (5)

A

Aspirin
Penicillin
NSAID
Omeprazole
TMP-SMZ

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37
Q

Methotrexate toxicity Rx. (3)

A
  1. Urine alkalisation -increase elimination of acidic drugs
  2. When MTX- with renal failure: glucarpidase
  3. Leucovirin may be used.
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38
Q

Drugs that are poor substrates of Pgp. (3)

A

Cabazitaxel
Eribulin
Ixabepilone

Good substrate for pgp.
Paclitaxel

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39
Q

MOA of pemetrexed.
S/e
…….is used

A

Thymidylate synthase
Hand foot syndrome
Folic acid/vit b12.

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40
Q

Eggs of folate antagonists

A
  1. Methotrexate
  2. Pemetrexed
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41
Q

Egs of purine antagonists (6)

A
  1. 6 MP
  2. Thioguanine- 6TG
  3. Azathioprine
  4. Fludarabine
  5. Cladribine
  6. Pentostatin
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42
Q

MOA of pentostatin.
Rx.

A

Irreversible inhibitor of ADA.
Hairy cell leukaemia

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43
Q

MOA of cladribine
Use: ….

A

Inhibits DNA polymerase and DNA replication

DOC for hairy cell leukaemia

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44
Q

Fludarabine is ……
MOA

A

Antiviral-vidarabine
Incorporated into DNA—> inhibit DNA synthesis

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45
Q

Precursor of 6MP
Toxic to ….
Toxic effects increase by ….

A

Azathioprine

Proliferating lymphocytes
Allopurinol

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46
Q

Drugs that block de novo purine synthesis (2)

Require activation by ……

A

Mercaptopurine
Thioguanine

HGPRT

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47
Q

S/e of 6MP
Toxicity of 6MP happens when given with ….

A

Reversible cholestatic jaundice

Allopurinol.

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48
Q

S/e of azathioprine

MOA & S/e of MMF

A

BMS

Inhibit IMPDH—> decrease purine syn.
S/e: N,V,D

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49
Q

Use of MMF

A

For prevention of graft rejection.
Triple therapy :
Calcineurin inhibitor + MMF+ steroid

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50
Q

S/e of vincristine (4)

S/e of bleomycin (2)

A

Peripheral neuropathy
SIADH
Alopecia
Areflexia

Pulmonary fibrosis
Flagellate pigmentation

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51
Q

Difference between vinca alkaloids and taxanes

A

Vinca: inhibit polymerisation
Taxanes: enhance polymerisation

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52
Q

Vincristine blocks polymerisation in ……phase. It’s called….

A

Metaphase
Spindle poisons

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53
Q

Taxanes are aka….
Block microtubules in ……phase

A

Taxols
Anaphase
Prevent disassembly

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54
Q

Glove and stocking pattern peripheral neuropathy seen with …..

What are the epothilones? Use: s/e

A

Taxanes

Ixabepilone
Use: breast cancer resistance to tax Ames and anthrocyclines

BMS, peripheral neuropathy

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55
Q

Pk of thalidomide

Thalidomide acts via inhibiting …..
S/e of thalidomide (3)

A

Spontaneous dissociation in blood. No renal or liver metabolism.

Angiogenesis

Sedation
Constipation
P. Neuropathy

56
Q

S enantiomer of thalidomide is …. It is ….

A

Lenalidomide. It is more potent, non teratogenic

57
Q

Uses of thalidomide (6)

A
  1. Multiple myeloma
  2. Kaposi sarcoma
  3. HIV ass ulcer
  4. Behcet syndrome
  5. ENL
  6. GVHD
58
Q

Vinca alkaloid derived from ….plant

Topotecan,iridothecan derieved from….
S/e

A

Periwinkle plant-catharantha alkaloids

Camptotheca acuminata
Cholinergic s/e

59
Q

Paclitaxel obtained from ….
Indication of paclitaxel (6)

A

Bark of western yew tree

  1. Ovarian cancer
  2. Breast cancer
  3. H&N cancer
  4. Small cell lung cancer
  5. Esophageal cancer
  6. Prostrate cancer
60
Q

Histopathology of DCMP in doxorubicin

MOA of anthracyclines

A

Vacuolated degeneration of myofibrils

Free radicals -interfere with dna intercalation( breaks in DNA to decrease replication)

61
Q

S/e…..prevented by ……
Anthracyclines are not preferred in radiotherapy. Why?

A

Cardio toxicity
Dexrazoxane

Radiation recall.-dose reduction to prevent radiation toxicity.

62
Q

Actinomycin D is aka…..
Bleomycin is a …..drug

Mitoxantrone is ……

A

Dactinomycin

Antitumor antibiotic drug.
Analogue of doxorubicin

63
Q

Antitumor antibiotic that causes DNA unwinding

Bleomycin. Moa (5)

A

Dactinomycin

Chelates copper and iron
Produce superoxide ion, free radical.
Intercalates between DNA strands
Causes chain scissors
Inhibit DNA repair

64
Q

Bleomycin damages ……pneumocytes
Test for bleomycin toxicity.
Bleonycin toxicity is enhanced by ……

A

Type 1.
Causes hyperplasia of type 2 pneumocytes.

Decreased DLCO.

Oxygen.

65
Q

Flagellate hyperpigmentation is also known as …..

Uses of daunorubicin and doxorubicin

Topical rx for psoriasis

A

Scratch dermatitis

Daunorubicin: haematological malignancy
Acute leukemia

Doxorubicin: solid tumor,
soft tissue sarcoma

Tazarotene.

66
Q

What is levamisole?

MOA.

A

Immumodulator antihelminthic
Low dose: immunostimulant
High dose: immunosuppressant

Depolarization by stimulating nicotine receptors

67
Q

Use of levamisole

Mitomycin C is active at sites of …..
MOA

S/e of mitomycinC

A

CRC with 5FU

Low oxygen tension
DNA cross links

HUS

68
Q

Uses of mitomycin C (3)

A
  1. SCC of anal canal
  2. Topical uses: laryngeal stenosis
  3. Intravitreal bladder cancer
69
Q

MOA of procarbazine

Drug acts via hypomethylation of DNA

A

Class of trizene
Acts via methylation of DNA—> dna damage

Decitabine

70
Q

Drugs that inhibit dna methyl transferase (2)
Use.

A

Decitabine
Azacytidine

Use: myelodysplastic syndrome

71
Q

L-asparaginase is obtained from ……
Use.

Moa of hydroxyurea

A

E coli

ALL

Inhibit ribonucleotide reductase
Decrease dna synthesis

72
Q

When to stop tamoxifen when conceiving?

SERMS do not inhibit….

A

3 months before

Vasomotor symptoms of menopause : hot flashes.

73
Q

Imatinib is ……
DOC for ….

S/e of imatinib (3)

A

Tk inhibitor . Given oral

CML( BCR-ABL) , GIST (c-kit)

S/e:
1. N/v/d
2 Edema- periorbital, pleural effusion
3. Myalgia

74
Q

How does resistance to imatinib occur?
Drugs to be given at that time?

A

Mutation to bcr-abl kinase
Dasatinib> bosutinib>nilotinib

75
Q

Main c-kit inhibitor
Others (2)

A

Imatinib
Sunitinib
Regorafenib

76
Q

EGFR TK inhibitors
ALK Inhibitors (2) use.
BRAF kinase inhibitor

A

Erlotinib, gefetinib

Crizotinib
Ceritinib.
NSCLC

Vemurafenib

77
Q

Diseases with EGFR mutation? (4)

A
  1. CRC
  2. NSCLC
  3. Pancreatic cancer
  4. H&N cancer
78
Q

Drugs against EGFR (2)

A

Cetuximab
Panitumumab

79
Q

Difference between sunitinib and sorafenib

A

Sunitinib:
MultiTK inhibitor.
Against : VEGF-RCC
C-kit and PDGFR- GIST

Sorafenib:
VEGFR kit
RAF kinase

Use: RCC.

Other uses of sunitinib:
GIST, pancreatic cancer (SuGiPa)

Other uses of sorafenib:
HCC
Thyroid cancer

80
Q

Tk given for medullary thyroid cancer (2)

A

Cabzantinib
Vandetanib

81
Q

Drug given for myelofibrosis

TK Drugs given for NSCLC (4)

A

Ruxolitinib

Erlotinib
Gefetinib
Crizotinib
Afatinib

82
Q

Drugs blocking Her2neu (3)

A

Ab against her2neu: trastuzumab
Prevent dimerization: pertuzumab
Inhibit intracellular TK: lapatinib, neratinib

83
Q

Use of bevacizumab(3)

A

DR
CRC
NSCLC

84
Q

MAB for CRC
Anti-VEGF (1)
Anti-EGFR (2)

A

Anti-VEGF: bevacizumab
Anti-EGFR: cetuximab, panituzumab

85
Q

What are the anti-VEGF drugs ?

A

Ramu ki Bibi Rani
Ramucirumab: stomach, AdenoCA, NSCLC
Bevazicumab: CRC,NSCLC.

Ranibizumab: decrease bv proliferation in retina
Age related macular edema-wet AMD
Dm macular edema.

86
Q

Drugs for CA breast (3)

A

Doxorubicin —s/e CMP

Trastuzumab —s/e CMP
Pertuzumab

Paclitaxel —s/e peripheral neuropathy

87
Q

Drug for her2neu positive breast cancer refractory to trastuzumab

A

Lapatinib + capecitabine

88
Q

Anti CD antagonists (6)

A

Ritu Is T O O Much
Rituximab
Ibrintumumab
Tositumumab
Ofatimumab
Obintuzumab
MS- Ocrelizumab

89
Q

Uses of rituximab (6)

A

NHL
CLL
RA
MS
SLE
TTP

90
Q

Drug for PNH

Mab for refractory AML in patients >60years

A

Eculizumab : C5 convertase

Gemtuzumab +ozagamicin - CD33 ab

91
Q

Differentiation syndrome
Rx

A

Those Rx for. aml m3 with retinoic acid- fever, pleural and pericardial effusion, chest pain.

Dexamethasone ASAP.

92
Q

Retinoid to rx mycosis fungoides

Another drug causing differentiation syndrome

A

Bexarotene- activating RXR.

Isocitrate DH

93
Q

AML Rx for different subtype

Cytarabine not given in M3. Why?

A

M0-M7: cytarabine +daunorubicin
M3: ATRA+
arsenic trioxide

Can cause DIC

94
Q

HDAC inhibitor for mycosis fungoides
(Histone deacetylase inhibitor)

A

Vorinostat
Romidepsin

95
Q

Mtor inhibitor for Rx advanced Tcell cancer

Use of everolimus

A

Temsirolimus

RCC
Breast cancer

96
Q

what is denileukin difitox?
Use:

A

Aa+ diphtheria toxin

Mycosis fungoides

97
Q

S/e of denileukin difitox

A

Immediate : hypersensitivity
Delayed:
vascular leak syndrome -pulmonary and peripheral edema

98
Q

MOA and use of aldesleukin
Toxicity of aldesleukin

A

MOA: IL-2 recombinant
Use: malignant melanoma
Metastatic renal cell cancer

Capillary leak syndrome

99
Q

Egs of serine threonine kinase inhibitor. Use.

A

Vemurafenib, dabrafenib- BRAF
Trametinib- MET

Use: malignant melanoma

100
Q

MOA of bortezomib

Use.
S/e

A

Proteosome inhibitor -prevent NF kB from preventing apoptosis

Multiple myeloma

Neuropathy

101
Q

Purified antigen presenting cells used in hormone dependent prostate cancer

Drug inhibiting hedgehog pathway
Use.

A

Sipuleucel-T

Vismodegib
Metastatic Basal cell cancer

102
Q

S/e of bevacizumab (4)

A

Thromboembolism
Gi perforation
Wound dehiscence
Tracheoesophageal fistula

103
Q

Drugs against M phase
Drugs against G2 phase

A

METV
Estramustine
Taxanes
Vinca

BED
Bleomycin
Etoposide
Daunorubicin

104
Q

Drug inhibiting G1 phase

A

Vinblastine

105
Q

Action of mesna is …..
Amifostine

A

Preventing ifosamide bladder toxicity
Against radiation toxicity

106
Q

MOA of palifermin

Drug given to decrease dry mouth from radiation.

A

Keratinocyte growth factor inhibitor

Pilocarpine

107
Q

Use of strontium

L-asparaginase is bone marrow …..

A

Reduce bone pain from bone mets

Sparing

108
Q

Drugs for neutropenia

Drug for TCP

A

Filgistim- G-CSF
Sargramostim- GMCSF

IL-11: Oprelvekin

109
Q

Drug for ifosamide induced neurotoxicity
Drug for paclitaxel induced hyperuricemia.

A

Methylene blue

Replace with protein bound paclitaxel

110
Q

Mc drugs causing mucositis (3)

A

Cytarabine
5FU
Methotrexate

111
Q

Prevention of oral mucositis

Diarrhoea is associated with …..

A

Palifermin

5FU
Capecitabine
Irinotecan

Tk inhibitors :
saorafenib, Sunitinib, imatinib, dasatinib.

EGFR:
Cetuximab, panitumumab, erlotinib.

112
Q

Drugs causing hyperpigmentation (3)

A

Busulfan
Hydroxyurea
Liposomal doxorubicin

113
Q

Hand foot syndrome mx ass with ….(5)

A

5FU
Capecitabine
Liposomal doxorubicin
Sunitinib, sorafenib
Pemetrexed

114
Q

Define hand foot syndrome

A

Tingling , burning of palms and soles
Progress to
severe pain, tenderness,edema and plaque formation

Spread to dorsum of hands and feet

115
Q

Rx had and foot syndrome by

A

Cessation of offending agent- pyridoxine

116
Q

Uses of TNF alpha inhibitors (3)

A

RA
IBD
Psoriatic arthritis

117
Q

DOC for SLE

A

Belimumab-B-lymphocyte stimulator

118
Q

C/F of TNF alpha inhibitor (3)

A
  1. TB: active,
    latent: INH for 1mo.
  2. HBV+
  3. Grade 3,4 CHF
119
Q

Use of IL-2 receptor blockers

A

Basiliximab: prevent graft rejection
Docolizumab: M.S

120
Q

S/e of calcineurin inhibitors (4)

A

Nephrotoxicity +
1. Hirsuitism
2. Hyperplasia of gums
3. HTN
4. Hyperuricemia

121
Q

S/e of tacrolimus

A

Nephrotoxic
D- DM
N- Neurotoxic
D: diarrhea
A: alopecia

122
Q

Drug which inhibit both EGFR and her2neu

Brentuzumab used for …..
works on …..

A

Lapatinib

CD30
Hogkins ,anaplastic large cell lymphoma

123
Q

Daratumumab is against …..
Use:

Alemtuzumab against
Use

A

CD38
MM

CD 52
CLL

124
Q

Iblizumab is against …… use

A

CD6
Psoriasis

125
Q

MAB against asthma (3)

A
  1. Omalizumab -against IgE
  2. IL-5: mepolizumab, benralizumab
    reslizumab-iv
  3. Dupilumab- IL-4,IL-13
126
Q

Mab used in IBD (3)

A

Moderate to severe UC &CD
1. Ustekinumab- only CD
2. TNF alpha inhibitors -UC&CD
3. Anti-integrins :
Natalizumab- alpha 4 integrin
Vedolizumab- a4B7
Block B cell migration

127
Q

Biologicals for psoriasis (3)

A
  1. Ustekinumab: IL-12/23
  2. Guselkinumab: IL-23
  3. IL-17 inhibitors : SBI
    Secukinumab
    Brodalumab
    Ixekizumab
128
Q

Biologicals in MS (5)

A
  1. Natalizumab
  2. Alemtuzumab
  3. Daclizumab
  4. Basiliximab
  5. Ocrelizumab- CD20.
129
Q

What are integrins?
Ab against integrins (2)

A

Proteins present on T lymphocytes, on adhesion with VCAM, lymphocytes come out I.e, egress lymphocytes from bv.

Natalizumab: a4B1
Vedolizumab: a4B7

130
Q

Anti IL-1 antibodies

A

CAR
Canikinumab: CAPS
Anakinra: RA,CAPS
Rilonacept : fusion protein against IL-1
Acute gout: NSAID, colchicine,steroid resistant

131
Q

IL-6 antibodies

Siltuximab use.

A

Tocilizumab
Sarilumab

Castle man’s disease

132
Q

Drugs acting on IL-2 (4)

A
  1. Aldesleukin
  2. Denileukin difitox
  3. Basilizimab
  4. Daclizumab
133
Q

World’s costliest medicine use

A

Onasemnogene abeparvovec
Spinal muscular dystrophy <2yrs age with SMN1 mutation

134
Q

What is epigenomics?

A

Alteration in histone, chromatin, and methylation of DNA sequences

135
Q

Proteomics

Microbiomics

A

Study of proteins

Study of bacterial flora of a person

136
Q

Metagenomics

A

Study of environmental species which can influence human biology directly or indirectly.

137
Q

Metabolomics

A

Study of range of metabolites in cells or organs and ways they are altered in disease states.