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Flashcards in Repro Deck (97):
0

Alprostadil

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

1

Trimix

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

2

Sildenafil

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

3

Vardenafil

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

4

Tadalafil

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

5

Apomorphine

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

6

Gonorrhea resistance

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

7

Ceftriaxone

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

8

Azithromycin

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

9

Doxycycline

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

10

Lenprolide

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

11

Ganirelix

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

12

Bromocriptine

Dopamine agonist
Tx: Parkinson's
Hyperprolactinemia

13

Oxytocin

Stimulates uterine contractions

14

Methyltestosterone

Androgen
Ind for androgen replacement therapy
Has anabolic activity

15

Oxandrolone

Androgen
Hormone replacement therapy
Higher anabolic activity

16

Nandrolone

Androgen
Hormone replacement therapy
Higher anabolic activity

17

SE of anabolic steroids

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

18

Finesteride

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

19

Flutamide

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

20

Spironolactone

Aldosterone antag
Testosterone receptor antag
Tx: PCOS
Hirsutism
SE: gynecomastia

21

Ketoconazole

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

22

Tamoxifen

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

23

Toremifene

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

24

Raloxifene

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

25

Clomiphene

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

26

Danazol

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

27

Anastrozole

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

28

Letrozole

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

29

Fulvestrant

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

30

Mifeprestone

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

31

Diethylstilbestrol (DES)

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

32

IL-2

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

33

IL-11

inc platelet formation --> used in thrombocytopenia

34

Filgrastim (G-CSF)

inc granulocytes --> used for marrow recovery

35

Sargramostim (GM-CSF)

inc granulocytes and macrophages -> used for marrow recovery

36

Erythropoietin

anemias, especially assoc with renal failure

37

Thrombopoietin

thrombocytopenia

38

Props affecting MoA of antineoplastic drugs

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

39

Props affecting intracell conc of antineoplastic drugs

dec prod of prodrugs
inc inactivation of drugs
dec accumulation

40

MOPP

Mechlorethamine
Oncovin
Procarbazine
Prednisone

41

ABVD

Adriamycin
Bleomicin
Vinblastine
Darcarbazine

42

Methotrexate

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

43

Pemetrexed

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

44

5-FU

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

45

Capecitabine

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

46

Leucovorin Rescue

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

47

6-mercaptopurine

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

48

Cytarabine

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

49

Cyclophosphamide

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

50

Busulfan

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

51

Chlorambucil (NCCS)

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

52

Carmustine

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

53

Lomustine

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

54

Semustine

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

55

Resistance to alkylating agents

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

56

Nitrogen mustard and nitrosourea toxicity

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

57

Cisplatinum

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

Carboplatinum

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

Oxaliplatin

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

Tetraplatin

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

Procarbazine

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

62

Dacarbazine

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

63

DNA Topoisomerase Class I

grasps one DNA strand
essential role in DNA replication and xscription

64

DNA Topoisomerase Class II

grasps both DNA strands
important role in cell division

65

Doxorubicin (Adriamycin)

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

Etoposide

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

67

Bleomycin

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

Prednisone

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

69

Vincristine

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

70

Vinblastine

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

71

Paclitaxel

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

72

Imatinib

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

73

Dasatinib

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

74

Nilotinib

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

75

Gefitinib

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

76

Erlotinib

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

77

Lapatinib

inhib: HER2/neu and EGFR
Tx: breast

78

Sorafenib

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

79

Naked monoclonal Ab

induce/potentiate immune response
block growth signals
block blood vessels

80

Conjugated/radiolabeled monoclonal Ab

deliver radioisotopes to cancer cells

81

Rituximab

naked
CD20 target
Tx: NHL

82

Cetuximab

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

83

Panitumumab

naked
EGFR target
Tx: colorectal Ca

84

Bevacizumab

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

85

Trastuzumab

naked
HER2 target
Tx: breast cancer

86

Ibritumomab Tiuxetan
Indium-111 or Yttrium-90

radiolabeled Ab
CD20 antigen target
Tx: NHL
SE: thromboctypenia
neutropenia

87

Tositumomab
Iodide-131

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

88

Chloroquine

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

Hydroxychloroquine

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

Quinine

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

Quinine + clindamycin

use in chloroquine-resistant P. Falciparium in prego pt

93

Mefloquine

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

Pyrimethamine + sulfadoxine

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

Aretemether + lumefantrine

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

96

Atovaquone/proguanil (Malarone)

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

Primaquine

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