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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
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 ```

Pharm (14 decks)

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