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Repro/heme Pharm > Repro > Flashcards

Repro Flashcards

0
Q

Trimix

A 
Phentolamine: alpha-blocker
Papaverine: vasorelaxer --> PDE1
PGE1: inc cAMP
Ind: erectile dysf(x)
Admin: injection
--admin at dec [ ] to dec penile fibrosis
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1
Q

Alprostadil

A 
PGE-1 analogue
Inc cAMP
Ind: erectile dysf(x)
Admin: injection
SE: pain @ injection site
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2
Q

Sildenafil

A 
PDE-5 inhib in corpus cavernosum
T1/2 = 4-6hrs
Metab = p450
Ind: erectile dysf(x)
Admin: oral --> avoid heavy meals / 1hr before sex
SE: headache / blue aura / NAION
CI: pt on alpha-blockers
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3
Q

Vardenafil

A

PDE-5 inhib
Ind: erectile dysf(x)
Similar to sildenafil

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4
Q

Tadalafil

A 
PDE-inhib
T1/2= 18hrs
Metab= p450 (sim to sildenafil)
--not affected by food
DoA= 36hrs
Ind: erectile dysf(x)
SE: PDE5 > PDE3A --> less cardiac side effects
      PDE5 > PDE6 --> less visual effects
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5
Q

Apomorphine

A

D1/D2 agonist
Ind: erectile dysf(x) –> works within 20min
Admin: sublingual
–half as effective as PDE inhibitors
SE: nausea / headache / yawning /dizziness

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6
Q

Gonorrhea resistance

A 
B-lactamase
Altered affinity of PCN-binding proteins
Tet-m (for tetracycline)
Homo men
California
Hawaii
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7
Q

Ceftriaxone

A 
Uncomplicated gonorrhea --> single dose
3rd gen cephalosporin --> resist to cephalosporinases
     Binds xspeptidase
SE: hypersensitivity
Seizures at high conc
C diff inf
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8
Q

Azithromycin

A 
Chlamydia --> single dose
Macrolide
Prevents xslocation @ P site
SE: GI upset
Unusually long t1/2
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9
Q

Doxycycline

A

Chlamydia –> 2x/d for 7d
Tetracycline –> blocks amino-acyl t-RNA @ A
SE: GI upset / photo sensitivity / ion chelator
CI: pt discoloration

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10
Q

Lenprolide

A

GnRH agonist
Pulsatile = LH/FSH release
Continuous = downreg of pituitary receptors/shuts down HP axis
Tx: prostate cancer
Endometriosis
Prev premature LH surges in ovarian hyperstimulation

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11
Q

Ganirelix

A 
GnRH antag
Absence of flare response
Does NOT cause receptor downreg 
Almost immed inhib LH/FSH release
Dose proportionality
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12
Q

Bromocriptine

A

Dopamine agonist
Tx: Parkinson’s
Hyperprolactinemia

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13
Q

Oxytocin

A

Stimulates uterine contractions

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14
Q

Methyltestosterone

A

Androgen
Ind for androgen replacement therapy
Has anabolic activity

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15
Q

Oxandrolone

A

Androgen
Hormone replacement therapy
Higher anabolic activity

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16
Q

Nandrolone

A

Androgen
Hormone replacement therapy
Higher anabolic activity

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17
Q

SE of anabolic steroids

A 
Masculinization
Acne
Sleep apnea
Erythrocytosis
Gynecomastia
Azoospermia
Dec HDL
Inc aggressiveness
Psychotic Sx
Hepatic dysf(x) --> peliosos or cholestatic jaundice
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18
Q

Finesteride

A

Type II alpha-reductive inhib
Inhib testosterone –> dihydrotest
Tx: BPH
Male pattern baldness

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19
Q

Flutamide

A 
Non-steroidal antiandrogen
Tx: prostate cancer
Treat flare response 
Hirsutism
SE: hepatic failure
Hot flashes
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20
Q

Spironolactone

A 
Aldosterone antag
Testosterone receptor antag
Tx: PCOS
Hirsutism
SE: gynecomastia
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21
Q

Ketoconazole

A

Antifungal
Broad spectrum antimycotic
Tx: Can be used orally to inhib test –> prostate cancer
Cushings

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22
Q

Tamoxifen

A 
antag = breast tissue
partial agonist = endometrium
Tx: breast cancer (+ER)
prevent redevl of cancer after surgery
red instance of cancer in contralat breast
SE: DVT / hot flashes / lb gain
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23
Q

Toremifene

A 
Estrogen antag = breast tissue
Estrogen partial agonist = endometrium
Tx: breast cancer (+ER)
prevent redevl of cancer after surgery
red instance of cancer in contralat breast
SE: DVT / hot flashes / lb gain
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24
Q

Raloxifene

A 
Estrogen agonist = bone
Estrogen antag = breast and endometrial
Tx: osteoperosis
invasive breast cancer
SE sim to Tamoxifen
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25
Q

Clomiphene

A

Estrogen antag = hypothal and pituitary
Estrogen agonist = ovary
Tx: stim ovulation (inc GnRH pulse freq)
may cause ovarian enlargement but mild

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26
Q

Danazol

A 
weak partial agonist = progestin, androgen, glucocort receptors
inhib steroid synth
SE: sim to some testosterone dx/dy
Tx: endometriosis
fibrocystic disease of the breast
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27
Q

Anastrozole

A

aromatase inhib
block estrogen synth
Tx: metastatic breast cancer (resist to ER antag)

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28
Q

Letrozole

A

aromatase inhib
block estrogen synth
Tx: metastatic breast cancer (resist to ER antag)

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29
Q

Fulvestrant

A

selective estrogen receptor downregulator (SERD)
potent antiestrogen
immobilizes ERalpha
interacts with cytokeratins 8 and 18

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30
Q

Mifeprestone

A

competitive progesterone antag
Tx: induce abortion
used in conj with misoprostol
Complication: excessive vaginal bleeding

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31
Q

Diethylstilbestrol (DES)

A

non-steroidal estrogen
injection
used to be used to treat habitual abortion
fetal exposure causes cervicovaginal structural abnormalities
Tx: palliative treat for advanced breast cancer and prostatic Ca

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32
Q

IL-2

A

inc lymphocyte diff and inc NKs –> use in renal cell cancer and metastatic melanoma

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33
Q

IL-11

A

inc platelet formation –> used in thrombocytopenia

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34
Q

Filgrastim (G-CSF)

A

inc granulocytes –> used for marrow recovery

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35
Q

Sargramostim (GM-CSF)

A

inc granulocytes and macrophages -> used for marrow recovery

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36
Q

Erythropoietin

A

anemias, especially assoc with renal failure

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37
Q

Thrombopoietin

A

thrombocytopenia

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38
Q

Props affecting MoA of antineoplastic drugs

A

inc nucleic acid repair mech
insens to apoptosis
prod of chemicals that inhib drugs
alterations in drug targets

39
Q

Props affecting intracell conc of antineoplastic drugs

A

dec prod of prodrugs
inc inactivation of drugs
dec accumulation

40
Q

MOPP

A

Mechlorethamine
Oncovin
Procarbazine
Prednisone

41
Q

ABVD

A

Adriamycin
Bleomicin
Vinblastine
Darcarbazine

42
Q

Methotrexate

A 
antimetabolite 
folate antagonist
Tx: ALL
breast cancer
SE: reversible BM suppression 
(treat with Leucovorin Rescue)
43
Q

Pemetrexed

A 
antimetabolite
folate antagonist
Tx: Lung cancer
SE: reversible BM suppression 
(treat with Leucovorin Rescue)
44
Q

5-FU

A 
thymidylate synthase inhibitor
Tx: GI Ca
breast cancer
SE: coronary atherosclerosis
alopecia
thrombophlebitis
45
Q

Capecitabine

A 
thymidylate synthase inhibitor
Tx: metastatic colorectal Ca
SE: coronary atherosclerosis
alopecia
thrombophlebitis
46
Q

Leucovorin Rescue

A

active form of B vitamin complex folate
activity does not req DHFR
administer before 42hrs have lapsed
cannot enter cancer cells

47
Q

6-mercaptopurine

A 
purine analog
Tx: acute leukemia
CML
Non-Hodgkin Lymphoma
SE: myelosuppression
48
Q

Cytarabine

A 
pyrimidine analog
Tx: acute leukemia
CML
Non-Hodgkin Lymphoma
SE: myelosuppression
49
Q

Cyclophosphamide

A 
nitrogen mustard --> alkylating agent
Tx: NHL
Ovarian and breast cancer
SE: BM suppression
hemorrhagic cystitis
50
Q

Busulfan

A

nitrogen mustard –> alkylating agent
Tx: CML
SE: Pulmonary fibrosis
hyperpigmentation

51
Q

Chlorambucil (NCCS)

A

nitrogen mustard –> alkylating agent
Tx: CML
SE: BM suppression
hepatotoxicity

52
Q

Carmustine

A

Nitrosoureas –> alkylating agent
Tx: glioblastoma multiforme
SE: ataxia
dizziness

53
Q

Lomustine

A

Nitrosoureas –> alkylating agent
Tx: glioblastoma multiforme
SE: ataxia
dizziness

54
Q

Semustine

A

Nitrosoureas –> alkylating agent
Tx: glioblastoma multiforme
SE: ataxia
dizziness

55
Q

Resistance to alkylating agents

A

O-6 Methylguanine-DNA methylxsferase
removed alkyl group
solution: administer Streptozotocin before giving the alkylating agent
Strepto is an alkyl group donator

56
Q

Nitrogen mustard and nitrosourea toxicity

A

hematopoietic –> dose-limiting (granulocytes and platelets)
GI
Gonadal damage –> serious; sertoli cells preserved; germ cells disappear
Alopecia

57
Q

Cisplatinum

A

Platinum compound –> alkylating agent
Tx: testicular cancer
bladder cancer
ovarian cancer
SE: focal acute tubular necrosis –> most serious; dose limiting
ototoxicity
severe N/V–> control with metoclopramide

58
Q

Carboplatinum

A

Platinum compound –> alkylating agent
Tx: testicular cancer
bladder cancer
ovarian cancer
SE: focal acute tubular necrosis –> most serious; dose limiting
ototoxicity
severe N/V–> control with metoclopramide

59
Q

Oxaliplatin

A

Platinum compound –> alkylating agent
Tx: testicular cancer
bladder cancer
ovarian cancer
SE: focal acute tubular necrosis –> most serious; dose limiting
ototoxicity
severe N/V–> control with metoclopramide

60
Q

Tetraplatin

A

Platinum compound –> alkylating agent
Tx: testicular cancer
bladder cancer
ovarian cancer
SE: focal acute tubular necrosis –> most serious; dose limiting
ototoxicity
severe N/V–> control with metoclopramide

61
Q

Procarbazine

A 
Triazene --> alkylating agent
prodrug --> methyl-diazonium --> methylates DNA
Tx: Hodgkin Lymphoma
SE: BM suppression
sterility
immunosuppression
62
Q

Dacarbazine

A 
Trizene --> alkylating agent
prodrug --> methyl-diazonium --> methylates DNA
Tx: Melanoma
SE: BM suppression
sterility
immunosuppression
63
Q

DNA Topoisomerase Class I

A

grasps one DNA strand

essential role in DNA replication and xscription

64
Q

DNA Topoisomerase Class II

A

grasps both DNA strands

important role in cell division

65
Q

Doxorubicin (Adriamycin)

A

anthracycline–> topoisomerase II inhib
intercalates DNA
prod free radicals
try to avoid extravasaction
Tx: Hodgkin lymphoma / breast / endometrial / lung / ovarian
SE: CARDIOTOXIC / BM suppression / Alopecia

66
Q

Etoposide

A

Epipodophyllotoxin –> topoisomerase II inhib
blocks complex
Tx: lung / testicular / leukemia
SE: BM suppression

67
Q

Bleomycin

A 
Streptomyces produced glycopeptides
binds DNA --> generates free radicals
chelates iron
inhib G2 phase
Tx: Hodgkin Lymphoma
testicular cancer
SE: Pulmonary fibrosis
hyperpigmentation
moderate myelosuppression
68
Q

Prednisone

A 
Glucocorticoid
triggers apoptosis 
may work on non-dividing cells
Tx: CLL
Hodgkin lymphoma
SE: Cushing
immunosupp
cataract
69
Q

Vincristine

A 
Vinca alkaloid
binds tubulin
blocks polymerization of microtubules
M-phase specific
Tx: Hodgkin lymph
SE: BM suppression
potent vesicant
70
Q

Vinblastine

A 
Vinca alkaloid
binds tubulin
blocks polymerization of microtubules
M-phase specific
Tx: Hodgkin lymph / Wilms / ChorioCa / neuroblastoma
SE: neurotox
paralytic ileus
potent vesicant
71
Q

Paclitaxel

A

Taxane
binds polymerized beta-tubulin –> stabalizes and disrupts mitosis
Tx: ovarian / local breast / metastatic breast / non-small cell lung / prostate
SE: BM suppression

72
Q

Imatinib

A

inhib tyrosine kinase d/t 9-22 xslocation (bcr-abl)
Tx: CML
inhib PDGFR-alpha and c-Kit
Tx: gastric Ca

73
Q

Dasatinib

A 
inhib: bcr-abl
c-Kit
PDGFR-alpha
SRC
Tx: CML
74
Q

Nilotinib

A

inhib: bcr-abl / c-Kit / PDGFR-alpha / SRC
Tx: CML

75
Q

Gefitinib

A

inhib: EGFR / ERB-B2
Tx: non-small cell lung

76
Q

Erlotinib

A

inhib: EGFR / ERB-B2
Tx: non-small cell lung

77
Q

Lapatinib

A

inhib: HER2/neu and EGFR
Tx: breast

78
Q

Sorafenib

A

inhib: VEGFR / EGFR / PDGFR
Tx: renal cell / hepatocellular

79
Q

Naked monoclonal Ab

A

induce/potentiate immune response
block growth signals
block blood vessels

80
Q

Conjugated/radiolabeled monoclonal Ab

A

deliver radioisotopes to cancer cells

81
Q

Rituximab

A

naked
CD20 target
Tx: NHL

82
Q

Cetuximab

A

naked
EGFR target
Tx: metastatic colorectal Ca
head and neck cancers

83
Q

Panitumumab

A

naked
EGFR target
Tx: colorectal Ca

84
Q

Bevacizumab

A 
naked
VEGF target
Tx: metastatic colorectal cA
Non small cell lung cancer
recurrent-metastatic breast
85
Q

Trastuzumab

A

naked
HER2 target
Tx: breast cancer

86
Q

Ibritumomab Tiuxetan

Indium-111 or Yttrium-90

A 
radiolabeled Ab
CD20 antigen target
Tx: NHL
SE: thromboctypenia
neutropenia
87
Q

Tositumomab

Iodide-131

A

radiolabeled Ab
CD20 antigen target
Tx: NHL
SE: severe cutaneous and mucocutaneous reactions

88
Q

Chloroquine

A

blood schizontocide
attacks in erythrocyte stage
weak base –> accumulation in the lysosome
prevents metal of Hb –> inhib heme polymerase
PK: high GI absorption
absorption disrupted by antacids
Ind: acute attack or prevention / prego pt
SE (high doses): pruritus
retinopathies
hypoTN or arrhythmias

89
Q

Hydroxychloroquine

A

blood schizontocide
attacks in erythrocyte stage
weak base –> accumulation in the lysosome
prevents metal of Hb –> inhib heme polymerase
PK: high GI absorption
absorption disrupted by antacids
Ind: acute attack or prevention / prego pt
SE (high doses): pruritus
retinopathies
hypoTN or arrhythmias

90
Q

Quinine

A

blood schizontocide
effective against all erythrocyte forms
H-bonded complex w/ DNA –> inhib xscription
PK: oral –> vivax and falciparium
antacids inhib absorption
SE: arrhythmias / N / V / cinchonism / hypoglycemia /
prolonged use: blackwater fever –> acute hemolytic anemia and renal failure

91
Q

Quinine + clindamycin

A

use in chloroquine-resistant P. Falciparium in prego pt

93
Q

Mefloquine

A

blood schizontocide
prophylaxis in chloroquine-resistant falciparium
Category B
may disrupt polymerization hemozoin
do not combine with cardiac conduction drugs
SE: vivid dreams
CI: hx of epilepsy or psychiatric disorders

94
Q

Pyrimethamine + sulfadoxine

A 
blood schizontocide
prophylaxis against erythrocytic forms
--also active against primary plasmodium inf in the liver
inhib DHFR (sim to trimethoprim)
used in combo with sulfonamides
SE: blood dyscrasias
folic acid def
Steven-Johnson syndrome
95
Q

Aretemether + lumefantrine

A 
blood schizontocide
antimalarial
free radical mechanism...sim to chloroquine
chloroquine resistant P. falciparium
not effective for prophylaxis
SE: usually well tolerated; some GI
96
Q

Atovaquone/proguanil (Malarone)

A

blood schizontocide
inhib cyto bc1 complex (complex III)
is prodrug to lower the effective concentration
Tx: uncomplicated chloroquine or multi drug resistant malaria
not recommended for prophylaxis
SE: severe renal impairment
CI: PREGO

97
Q

Primaquine

A 
tissue schizontocide
effective against exoerythrocytic stage
radical cure of P. vivax and oval
terminal prophylaxis
CI: PREGO
PK: PO / t1/2 3-6h
SE: issues seen in pt with G6PDH polymorphisms

Repro/heme Pharm (1 decks)

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