Drug MOA/SE/Use Flashcards
(259 cards)
1
Q
Zidovudine MOA
A
thymidine analogue (w/ 3’-azido) prevents phosphodiester linkage, inhibiting RT & viral replication
2
Q
Zidovudine Resistance
A
common in newly infected pts & those previously Tx w/ this drug
3
Q
Zidovudine S/E
A
Extreme ANEMIA & NEUTROPENIA in compromised bone marrow function pts;
GI (n/v, diarrhea, hepatitis)
HEMA (anemia, granulocytopenia, thrombocytopenia, bone marrow toxicity)
4
Q
Zidovudine can be used w/ all other NRTIs except?
A
Stavudine
5
Q
Which pt condition warrants extreme caution when using Zidovudine?
A
Bone marrow compromised pts
6
Q
HIV+ pregnant females using which drug during wks 14-34 along + infants until 6 wks, can reduce transmission rates to 8%
A
Zidovudine
7
Q
Didanosine MOA
A
ideoxyinosine, w/ a 3’-H instead of a 3’-OH; Activation to ddATP, competitive inhibition of RT enzyme
8
Q
Didanosine S/E
A
Peripheral neuropathy, potentially fatal pancreatitis, GI disturbances
9
Q
What limits Didanosine?
A
Lowered absorption d/t gastric pH or food
10
Q
Lamivudine MOA
A
3’-Carbon replaced by 3’-Sulfur; Competitive inhibition of RT
11
Q
Lamivudine S/E
A
Less cellular toxicity - but less potent than Zidovudine; Related to Didanosine, but NO risk for peripheral neuropathy
12
Q
What limits Lamivudine?
A
Rapid RESISTANCE if on monotherapy!
13
Q
Which NRTIs have action against HBV?
A
Lamivudine & Emtricitabine & Tenofovir
14
Q
Emtricitabine MOA
A
5’-Fluorinated derivative of Lamivudine (3’-Sulfur); Competitive inhibition of RT
15
Q
Emtricitabine S/E
A
BEST TOLERATED! Hyperpigmentation of palms & soles
16
Q
Abacavir MOA
A
Nucleoside Analog - Competitive inhibition of RT
17
Q
Abacavir S/E
A
3-9% Severe HSN rxn - rash, fever, malaise
Respiratory or GI Sx
18
Q
Preferred Tx for Tx-naive patients
A
Epzicom & Truvada combination drugs
19
Q
Epzicom
A
Abacavir/Lamivudine combination pill
20
Q
Truvada
A
Emtricitabine/Tenofovir combination pill
21
Q
Tenofovir MOA
A
NucleoTide analog - Competitive inhibition of RT
22
Q
Tenofovir S/E
A
n/v, diarrhea, renal toxicity
23
Q
Tenofovir Use
A
Active against HBV & NRTI-RESISTANT strains
24
Q
Limitations of Efavirenz
A
contraindicated during pregnancy - neural tube defects
25
Efavirenz MOA
binds directly to RT to alter enzyme's catalytic site
26
Efavirenz S/E
CNS Sx: Dizziness, HA, insomnia, inability to concentrate & rash
27
Atripla
Efavirenz/Emtricitabine combination pill
28
Ritonavir S/E
Common: n/v, weakness, diarrhea
Circumoral & peripheral parethesia (tingling/numbness)
Elevated liver enzymes
inhibits p450 -> drug toxicity
29
Ritonavir MOA
Peptidomimetic inhibitor of HIV protease
30
Ritonavir Uses
w/ other NRTIs or at low doses to "BOOST" serum concentrations of other PIs
31
Most commonly used PI
Nelfinavir
32
Nelfinavir S/E
well tolerated - nausea, diarrhea
33
Indinavir S/E
Nephrolithiasis, Dermatologic changes (alopecia, dry skin & mucous membranes)
Asymptomatic hyperbilirubinemia, HA, blurred vision, dizziness
34
Atazanavir S/E
GI disturbance, ABNORMAL FAT DISTRIBUTION, Elevated liver enzymes
35
Chloroquine/Hydrochloroquine MOA
Interferes w/ Hgb digestion -> heme accumulation & toxicity to Plasmodium
36
Chloroquine/Hydrochloroquine S/E
(Less than Quinine)
Retinal & Corneal toxicity (visual dysfunction);
CNS - HA, dizzy, tinnitus; GI: take w/ food
Immunologic: rash, blood dyscrasia, lupus-like
37
Chloroquine/Hydrochloroquine should be used w/ caution in pts w/
liver disease
38
Chloroquine/Hydrochloroquine should not be used in pts w/
psoriasis & porphyria
39
Chloroquine/Hydrochloroquine is used to Tx
Clinical cure for ALL forms
Radical care for P. falciparum & P. malariae
Prophylaxis for sensitive forms
40
At high doses Chloroquine/Hydrochloroquine may be used for
Anti-inflammatory action @ HIGH doses - for RA & Lupus Erythematosus
41
Resistance to Chloroquine/Hydrochloroquine via
P. falciparum - involves a transport pump that removes the drug
42
Quinine/Quinidine S/E
```
Cinchonism: HA, nausea, dizziness, blurred vision, tinnitus, deafness
GI irritation (n/v), Depressant effect on heart & mild neuromuscular blockade
```
43
Quinine/Quinidine Contraindications
Pregnancy - birth defects & abortion
44
Quinine/Quinidine at low doses is used for
Muscle relaxant @ LOW doses - for nocturnal leg cramps
45
Quinine/Quinidine is used to Tx
Clinical cure for ALL forms
Gametocytocidal for P. vivax & P. malariae
Tx of Chloroquine-resistant P. falciparum
Analgesic & Antipyretic effects
46
Mefloquine S/E
Less toxic than Chloroquine
| GI upset, Myocardium depression, Seizures, Aggrevation of latent psychoses
47
Mefloquine should be used w/ caution in pts w/
Caution w/ pt Hx of mental illness, epilepsy, CV disorders
48
Mefloquine is used to Tx
Tx & Prophylaxis of Chloroquine-resistant strains of P. falciparum
49
Pyrimethamine/Proguanil MOA
dihydrofolate reductase inhibitor in erythrocytic forms & some effect on sporozoites & pre-erythrocytic forms
50
Pyrimethamine/Proguanil Use
Px of Chloroquine-resistant strains of P. falciparum & Presumptive Tx when used w/ Sulfonamides
51
Atovaquone + Proguanil MOA
depolarizes mitochondria to inhibit ETC
52
Atovaquone + Proguanil Use
Alternative to Mefloquine & Doxycycline fp Px of Chloroquine-resistant P. falciparum
53
Which drug is rapidly becoming the PRIMARY Tx for most forms of Malaria?
Coartem: combination of Artemisinin/Artemether + Lumefantrine
54
Atovaquone + Proguanil S/E
RARE: HA, abd pain, unknown safety during pregnancy
55
Which antibiotic class can be used as a Tx & Px alternative for malaria?
Tetracycline (Doxycycline)
56
Primaquine action
Active against tissue forms of all species, gametocytocidal, little effect on the erythrocytic forms & will not suppress active disease
57
Primaquine S/E
Acute - Mild; Chronic - Increasing severity
| GI upset, CNS (HA, dizzy), Hemolytic anemia (in G6PD deficient ind)
58
Contraindications for Primaquine
pregnancy - teratogenic
59
Primaquine Uses
Radical cure for P. vivax & P. ovale by eradicating the tissue forms
Causal Prophylaxis - but it is not used d/t toxicity
60
Tetracycline (Doxycycline) MOA
Inhibition of plasmodial protein synthesis
61
Tetracycline (Doxycycline) S/E
Phototoxicity, Permanent discoloration of teeth in children
62
Tetracycline (Doxycycline) Contraindication
pregnancy & children < 8
63
Most common helminthic infection in the US
Enterobius vermicularis (pinworm)
64
Enterobius vermicularis (pinworm) Sx
Perianal irritation & pruritus, anorexia, restlessness, insomnia
65
Ascaris lumbricoides (roundworm) Sx
"Light" infections are aSx, while "Heavy" infections cause abd pain, allergic responses to metabolites (rash, asthma), insomnia, restlessness, appendicitis, bile duct occlusion, intestinal perforation
66
Necator americanus (hookworm) Sx
Iron-deficient anemia (mental dullness)
67
T. solium & T. saginata Sx
GI upset, loss of appetite, T. solium larvae can penetrate the GIT & migrate to produce cysticercosis (encyst in visceral organs, muscle, CNS); Neurocysticercosis may cause Neurogenic & Psychiatric Sx, increased ICP, severe HA, intellectual deterioration, decreased visual acuity & seizures
68
Entamoeba histolytica Sx
Inflammation, severe bloody diarrhea, possible spread to liver (hepatic abscess)
69
Giardia lamblia Sx
profuse, watery, foul-smelling diarrhea, abd distention, cramping, anorexia, nausea
70
Trichomonas vaginalis Sx
greenish, malodorous discharge, vulvar pruritus, dyspareunia, dysuria, friable cervix
71
Cryptosporidium parvum Sx
large amt of watery diarrhea w/ vomiting, cramping, flatulence
72
Enterobius vermicularis Tx
Albendazole or Pyrantel
73
Mild Ascaris lumbricoides Tx
Albendazole
74
Heavy Ascaris lumbricoides Tx
Pyrantel
75
Necator americanus Tx
Albendazole
76
T. solium & T. saginata Tx
Praziquantel
77
aSx Entamoeba histolytica Tx
Iodoquinol or Paromomycin
78
Sx Entamoeba histolytica Tx
Metronidazole followed by Iodoquinol or Paromomycin
79
Giardia lamblia Tx
Metronidazole or Nitazoxanide
80
Trichomonas vaginalis Tx
Metronidazole
81
Cryptosporidium parvum in AIDS pt Tx
Paromomycin
82
Cryptosporidium parvum in immunocompromised pt Tx
Nitazoxanide
83
Albendazole MOA
Binds to free b-tubulin of the parasite to inhibit MT polymerization & MT-dependent glucose uptake
84
Albendazole S/E
GI: n/v, diarrhea, abd pain
Teratogenic potential - use only if benefits > risks; Increase liver enzymes & hepatotoxicity
Leukopenia (<1%)
85
Albendazole Uses
1. Enterobius Vermicularis (Pinworm),
2. Mild/aSx Ascaris lumbricoides (roundworm),
3. Necator americanus (hookworm)
86
Pyrantel MOA
Activation of cholinergic nicotinic receptors, resulting in a depolarizing neuromuscular blockade & paralysis
87
Pyrantel S/E
GI: n/v, cramps; HA, dizziness, drowsiness
88
Pyrantel Uses
1. Enterobius Vermicularis (Pinworm)
| 2. Heavy Ascaris lumbricoides (roundworm) infection
89
Pyrantel should be used w/ caution in
pts w/ liver disease, pregnancy, & children <2
90
Praziquantel MOA
Induces muscle contraction then spastic paralysis by causing an increase in Ca2+ influx
91
Praziquantel S/E
Dizziness, drowsiness, HA, decreased mental alertness; GI: abd pain, n/v
Increase liver enzymes
Urticaria, rash, low-grade fever, arthralgia, myalgia
92
Praziquantel Uses
Taenia solium, Taenia saginata, Neuroschistosomiasis, used as Tx & Px
93
Praziquantel should be used w/ caution in
avoid w/ pregnancy if possible
94
Metronidazole MOA
reduced & binds to intracellular macromolecules (DNA), inhibition of DNA synthesis, etc
95
Metronidazole S/E
Drug Interactions - disulfiram-like rxn w/ EtOH, increases oral anticoagulant activity
Nausea, HA, dry-mouth/metallic taste
Infrequent - Vomiting, diarrhea, insomnia, dark urine, weakness, dizziness, seizures, peripheral neuropathies
Carcinogenic potential
96
Metronidazole Uses
1. Sx Entamoeba histolytica
2. Giardia lamblia
3. Trichomonas vaginalis
4. Anaerobic bacteria - GNR, Bacteroides fragilis, & GPC, C. difficile
97
Metronidazole should not be used in
1st trimester - carcinogenic
98
Iodoquinol S/E
Neurotoxicity - optic neuritis & loss of vision
| Mild GI upset
99
Iodoquinol Uses
Alone in aSx Entamboeba histolytica or following Metronidazole for Sx E. histolytica
100
Paromomycin MOA
Aminoglycoside & inhibits protein synthesis by binding to the 30S ribosomal subunit
101
Paromomycin S/E
GI: anorexia, n/v, epigastric burning, increased GI motility, abd cramps, diarrhea
Potential nephrotoxicity, ototoxicity, & neuromuscular blocking effects
102
Paromomycin Uses
1. Alone in aSx Entamboeba histolytica or following Metronidazole for Sx E. histolytica
2. Drug of choice for C. parvum infection in AIDS pts
103
Nitazoxanide MOA
Interferes w/ anaerobic energy metabolism by inhibiting pyruvate:ferredoxin 2-oxidoreductase enzyme depependent electron transfer rxn
104
Nitazoxanide S/E
displaces highly-bound drugs (Warfarin)
Common - abd pain, diarrhea, nausea, HA
Unlike Metronidazole - free of carcinogenic potential
105
Nitazoxanide Uses
1. C. parvum in immunocompetent children (1-11), adolescents, & adults
2. G. lamblia in children >1, adolescents, & adults
106
Mechlorethamine MOA
7-N of guanine alkylation, producing an alkylated purine (multiple sites of alkylation cause cross-linking of DNA strands); Results in miscoding of DNA strands, incomplete repair of alkylated segment -> DNA strand breaks, depurination, abnormal base pairing
107
Mechlorethamine S/E
Toxicity - bone marrow, spermatogenesis, GIT, hair follicles
Acute toxicity - n/v, phlebitis
Delayed toxicity - bone marrow depression (leukopenia, thrombocytopenia, anemia; immunosuppression, alopecia, *Secondary neoplasia
108
Mechlorethamine Uses
Hodgkin's Disease
109
Mechlorethamine, CCS or CCNS?
CCNS - although primarily M & G1
110
Cyclophosphamide MOA
activated by p450; alkylation cause cross-linking of DNA strands; Results in miscoding of DNA strands, incomplete repair of alkylated segment -> DNA strand breaks, depurination, abnormal base pairing
111
Cyclophosphamide S/E
Toxicity - bone marrow, spermatogenesis, GIT, hair follicles
Acute toxicity - n/v, phlebitis
Delayed toxicity - bone marrow depression (leukopenia, thrombocytopenia, anemia; immunosuppression, alopecia, *Secondary neoplasia
112
Cyclophosphamide Uses
Immunosuppressive agent: Wegener's granulomatosis, RA, Organ transplantation
Acute & Chronic Leukemia: Hodgkin's & Non-Hodgkin's, Burkitt's lymphoma, Multiple myelomas, testicular cancer, breast cancer, lung cancer, ovarian/endometrial/cervical carcinoma
113
Cyclophosphamide, CCS or CCNS?
CCNS
114
Carmustine MOA
activation -> alkylation cause cross-linking of DNA strands; Results in miscoding of DNA strands, incomplete repair of alkylated segment -> DNA strand breaks, depurination, abnormal base pairing
115
Carmustine S/E
Toxicity - bone marrow, spermatogenesis, GIT, hair follicles
Acute toxicity - n/v, phlebitis
Delayed toxicity - bone marrow depression (leukopenia, thrombocytopenia, anemia; immunosuppression, alopecia, *Secondary neoplasia
116
Carmustine Uses
Brain tumors, Hodgkin's & Non-Hodgkin's lymphomas, Multiple Myeloma
117
Carmustine, CCS or CCNS?
CCNS
118
Cisplatin MOA
Bifunctional alkylator that causes inter-intrastand DNA cross-linking & disruption of DNA double helix which interferes w/ DNA synthesis
119
Cisplatin S/E
nephrotoxicity + ototoxicity;
Toxicity - bone marrow, spermatogenesis, GIT, hair follicles
Acute toxicity - n/v, phlebitis
Delayed toxicity - bone marrow depression (leukopenia, thrombocytopenia, anemia; immunosuppression, alopecia, *Secondary neoplasia
120
Cisplatin Uses
Testicular, ovarian, bladder, gastric, esophageal, pancreatic, lung, head/neck tumors
121
Cisplatin, CCS or CCNS?
CCNS, but G1 most sensitive
122
Methotrexate MOA
Dihydrofolate reductase inhibitor prevents the conversion of Folic acid to Tetrahydrofolate -> inability to convert deoxyuridylate to thymidylate blocks DNA, RNA, & protein synthesis
123
Methotrexate S/E
Acute - n/v, diarrhea
| Delyaed - GI/oral ulcers, bone marrow suppression, alopecia, hepatotoxicity, pulmonary infiltrates, fever
124
Methotrexate Uses
Psoriasis & RA;
| Acute lymphocytic leukemia, Non-Hodgkin's lymphomas, leukemia, breast, pancreatic & bladder carcinoma
125
Methotrexate, CCS or CCNS?
CCS in S phase
126
Which protein allows normal cells to bypass the block caused by Methotrexate?
Leucovorin
127
Resistance to Methotrexate is via
decreased uptake by tumor cells & increased concentration of target enzyme
128
Mercaptopurine MOA
Converted by HGPRT to a nucleotide, which inhibits enzymes of purine interconversion. Results in inhibition of purine nucleotide synthesis & metabolism, and alters the synthesis & function of RNA & DNA
129
Mercaptopurine S/E
Acute: infrequent n/v, diarrhea
Delayed: gradual bone marrow depression
130
Mercaptopurine Uses
Immunosuppressant
| Maintenance of remission of acute lymphocytic, acute myelogenous & CNS leukemia
131
Mercaptopurine, CCS or CCNS?
CCS - S phase
132
Mercaptopurine is metabolized by
xanthine oxidase to 6-thiouric acid
133
The metabolism of Mercaptopurine can be blocked by what drug?
Allopurinol
134
Fluorouracil MOA
Activated to 5-deoxyuridine
binds thymidylate synthetase covalently to block the conversion of deoxyuridylate to thymidylate (rate-limiting step in DNA synthesis)
135
Fluorouracil S/E
Delayed: n/v, oral/GIT ulcerations, bone marrow depression
136
Fluorouracil Uses
Carcinoma of breast, colon, pancreatic, ovarian, head, gastric, esophageal, head/neck
137
Fluorouracil, CCS or CCNS?
CCS - S phase
138
Fluorouracil resistance occurs via
decreased activation & increased inactivation
139
Cytarabine MOA
Active Cytarabine triphosphate competes w/ Deoxycitidine triphosphate to cause DNA pol inhibition
140
Cytarabine S/E
Delayed: n/v, bone marrow depression, megaloblastosis, leukopenia, thrombocytopenia
141
Cytarabine Uses
Remission induction in acute non-lymphocytic leukemia; Acute lymphocytic leukemia; Chronic myelocytic leukemia; Meningeal leukemia
142
Cytarabine, CCS or CCNS?
CCS - S phase
143
Daunorubicin Hydrochloride MOA
Intercalate & bind to DNA b/w base pairs on adjacent strands, resulting in uncoiling of DNA & destroy the DNA template to inhibit DNA-directed RNA & DNA pols
144
Daunorubicin Hydrochloride S/E
Acute - n/v, red urine, tissue necrosis, arrhythmias
| Delayed - bone-marrow depression, alopecia, GI upset, & CARDIOMYOPATHY
145
Daunorubicin Hydrochloride Uses
Acute Non-Lymphocytic Leukemia of adults
146
Daunorubicin Hydrochloride, CCS or CCNS?
CCNS but most effective in S phase
147
Doxorubicin Hydrochloride MOA
Intercalate & bind to DNA b/w base pairs on adjacent strands, resulting in uncoiling of DNA & destroy the DNA template to inhibit DNA-directed RNA & DNA pols
148
Doxorubicin Hydrochloride S/E
Acute - n/v, red urine, tissue necrosis, arrhythmias
| Delayed - bone-marrow depression, alopecia, GI upset, & CARDIOMYOPATHY
149
Doxorubicin Hydrochloride Use
Synergistic in combination; Lymphoma, Leukemia, Hodgkin's disease, ovarian, lung, bladder, neuroblastoma
150
Doxorubicin Hydrochloride, CCS or CCNS?
CCNS but most effective in S phase
151
Daunorubicin Hydrochloride & Doxorubicin Hydrochloride resistance occurs via
diminished drug uptake
152
Vinblastine Sulfate MOA
Bind tubulin & disrupt the mitotic spindle apparatus, preventing segregation of chromosomes -> Metaphase arrest
153
Vinblastine Sulfate S/E
Acute - local reactivity
| Delayed - neurological, constipation, alopecia, mild bone depression
154
Vinblastine Sulfate Use
Breast carcinoma, acute leukemia, Hodgkin's & Non-Hodgkin's lymphoma
155
Vinblastine Sulfate, CCS or CCNS?
CCS for M phase
156
Vincristine Sulfate MOA
Bind tubulin & disrupt the mitotic spindle apparatus, preventing segregation of chromosomes -> Metaphase arrest
157
Vincristine Sulfate S/E
Acute - mild n/v, phlebitis
| Delayed - neurological, bone-marrow depression
158
Vincristine Sulfate Use
Hodgkin's disease, Kaposi's sarcoma, Testicular, bladder, lung carcinoma
159
Vincristine Sulfate, CCS or CCNS?
CCS for M phase
160
Etoposide MOA
Complexes w/ topoisomerase II & DNA, resulting in DNA breaks, no resealing of the breaks -> cell death
161
Etoposide S/E
Acute - n/v, diarrhea (IV - 15%, oral - 55%)
| Delayed - leukopenia 10-14d & recovery by 3wks; Alopecia in 66%
162
Etoposide Uses
```
Testicular cancer (w/ bleomycin + cisplatin)
Small Cell Carcinoma of lung (w/ cisplatin)
```
163
Etoposide, CCS or CCNS?
CCS for G2
164
Paclitaxel MOA
Anti-MT agent; promotes MT assembly by enhancing tubulin polymerization
165
Paclitaxel S/E
Acute - n/v (52%)
Delayed - bone marrow suppression: neutropenia, leukopenia, thrombocytopenia, anemia; HSN; peripheral neuropathy (60%)
Alopecia (~100%)
166
Paclitaxel Uses
Metastatic Ovarian or Breast Cancer
| Non-Small Cell Carcinoma of lung
167
Paclitaxel, CCS or CCNS?
CCS for G2 & M phases
168
Prednisone or Dexamethasone MOA
Inhibits phospholipase A2 & COX-2;
| Suppresses mitosis in lymphocytes
169
Prednisone or Dexamethasone S/E
Iatrogenic Cushing's Syndrome, osteoporosis, infections; Psychiatric disturbances, peptic ulcer, HTN, edema, adrenal suppresion, obesity, dyslipidemia
170
Prednisone or Dexamethasone Uses
Palliative management of Leukemia & Lymphoma in adults,
Acute Leukemia of childhood,
Breast Cancer
171
Tamoxifen MOA
competitively binds to estrogen receptors -> inhibits the expression of estrogen-related genes
172
Tamoxifen S/E
Extremely well tolerated,
Most common - Menopausal Sx
Short-term: hot flashes, HA, fatigue, n/v, vaginal dryness, skin rashes
Long-term: visual disturbances, vaginal bleeding, ocular toxicity, thromboembolic events, thrombocytopenia & leukopenia
Most serious - potential tumor-promoting activity -> inceased incidence of endometrial cancer
173
Tamoxifen Use
Estrogen-receptor (+) Invasive breast cancer,
Adjuvant therapy of breast cancer to reduce risk of recurrence & development of new cancers
Used frequently in men w/ breast cancer
174
Tamoxifen, CCS or CCNS?
CCS blocks G1 phase
175
Imatinib Mesylate MOA
inhibits Bcr-Abl tyrosine kinase, preventing phosphorylation of the kinase substrate by ATP, which inhibits cell proliferation & induces apoptosis in Bcr-Abl (+)
176
Imatinib Mesylate S/E
Acute - abdominal pain, n/v, diarrhea
| Delayed - fatigue, joint pain, muscle cramps, fluid retention, superficial edema & rash
177
Imatinib Mesylate Uses
Ph(+) Chronic Myeloid Leukemia in blast crisis,
Acute Lymphocytic Leukemia,
Dermatofibrosarcoma, Hypereosinophilic syndrome & Chronic eosinophilic leukemia
178
Imatinib Mesylate, CCS or CCNS?
CCS - G1
179
Bcr-Abl Fusion Protein
a constitutively abnormal tyrosine kinase created by t(9:22) Philadelphia chromosomal translocation seen w/ CML
180
Trastuzumab MOA
IgG1 mAb that binds HER-2 receptors (EGF), blocks EGF binding & down-regulates tyrosine kinase signaling activity
181
Trastuzumab S/E
Acute - n/v, diarrhea
| Delayed - anemia, neutropenia, infections, fatigue, fever, HA, infusion rxn, rash, & cardiomyopathy
182
Trastuzumab Use
Adjuvant for Breast Cancer: 30% are EGF-2 overexpressing, give w/ Doxorubicin, Cyclophosphamide + Paclitaxel
HER-2 Overexpressing Metastatic Breast Cancer: give w/ Paclitaxel (1st line Tx)
183
Trastuzumab, CCS or CCNS?
CCS for G1 arrest
184
Breast Cancer Tx:
CMF: Cyclophosphamide + Methotrexate + Fluorouracil & Tamoxifen
185
Bladder Cancer:
M-VAC: Methotrexate + Vinblastine + Adriamycin + Cisplatin
186
Cervical Cancer Tx:
BIP: Bleomycin + Ifosfamide + Cisplatin
187
Lung Cancer Tx:
CAE: Cyclophosphamide + Doxorubicin (Adryamicin) + Etoposide
188
Which Chemotherapeutic drug is lipid soluble & can be used for brain cancer Tx?
Carmustine
189
Which Chemotherapeutic drug causes ototoxicity & nephrotoxicity S/Es?
Cisplatin
190
Which Chemotherapeutic drug causes Cardiotoxicity S/Es?
Daunorubicin Hydrochloride & Doxorubicin Hydrochloride
191
Which Chemotherapeutic drug causes Neurological toxicity S/Es?
Vinblastine Sulfate & Vincristine Sulfate
192
Ph(+) Chronic Myeloid Leukemia in blast crisis may be treated using
Imatinib Mesylate
193
c-kit receptor (+)- GI Stromal tumor may be treated using
Imatinib Mesylate
194
Antipsychotic drug used as an antiemetic?
Prochlorperazine
195
Which drugs are more potent than Chlorpromazine
Trifluoperazine & Fluphenazine
196
Trifluoperazine & Fluphenazine S/E
less sedation & less anticholinergic (CV effects), but MORE EPS
197
Chlorpromazine S/E
More sedation & more anticholinergic (CV effects, but LESS EPS
198
Potent Phenothiazine that comes in long-acting forms
Fluphenazine
199
Phenothiazine MOA
D2-antagonist
200
Potent antipsychotic w/ the greatest risk of EPS
Haloperidol
201
Clozapine MOA
Blocks D4 & 5-HT2 receptors
202
Clozapine Uses
May work in pts unresponsive to other meds, effective against + & - Sx
203
Clozapine S/E
agranulocytosis, seizures, weight gain, hyperglycemia, type II DM
204
Olanzapine
Clozapine w/o agranulocytosis risk
205
Risperidone MOA
Blocks both DA2 & 5-HT2 receptors
206
Risperidone S/E
Weight gain, hyperglycemia
207
Olanzapine Uses
Scizophrenia & Mania
208
Aripiprazole MOA
Partial agonist/antagonist at D2 & 5-HT1a receptors
209
Aripiprazole S/E
Less likely to cause weight gain & hyperglycemia; Little tendency to cause EP S/E
210
Imipramine MOA
Inhibit the synaptic reuptake of NE & 5-HT
211
Amitriptyline MOA
Inhibit the synaptic reuptake of NE & 5-HT
212
Fluoxetine
Selectively inhibit the reuptake of 5-HT
213
Amitriptyline S/E
GREATEST Anticholinergic S/E (dry mouth, constipation, urine retention, loss of accomodation), More sedation, Weight gain
214
Drug used for the Tx of Enuresis & Urinary Incontinence
Imipramine
215
Fluvoxamine MOA
Selectively inhibit the reuptake of 5-HT
216
Sertraline MOA
Selectively inhibit the reuptake of 5-HT
217
Paroxetine MOA
Selectively inhibit the reuptake of 5-HT
218
Citalopram MOA
Selectively inhibit the reuptake of 5-HT
219
Escitalopram MOA
Selectively inhibit the reuptake of 5-HT
220
Venlafaxine & Desvenlafaxine MOA
Inhibits both NE, 5-HT, & DA reuptake; Mild Stimulant Activity
221
Duloxetine MOA
Inhibits both NE, 5-HT, & DA reuptake; Mild Stimulant Activity
222
Trazodone MOA
Inhibit the reuptake of 5-HT & block 5-HT-2 receptors
223
Nefazodone MOA
Inhibit the reuptake of 5-HT & block 5-HT-2 receptors
224
Bupropion MOA
Selectively inhibits DA reuptake; Mild Stimulant Activity "Psychic Energizer"
225
Mirtazepine MOA
Blocks presynaptic alpha-2-adrenergic receptors; Enhances the synaptic release of NE & 5-HT; Also blocks some 5-HT receptor subtypes
226
Atomoxetine MOA
Selective NE reuptake inhibitor
227
Phenelzine MOA
Prevent the metabolic breakdown of NE, 5-HT, & DA, by inhibiting MAO-A & MAO-B
228
Tranylcypromine MOA
Prevent the metabolic breakdown of NE, 5-HT, & DA, by inhibiting MAO-A & MAO-B
229
Selegiline MOA
Selective inhibitor of MAO-B, prevents the metabolic breakdown of DA only
230
Lithium Carbonate Use
Most Effective drug for Manic-Depressive Disorder
231
Valproic Acid Analogs
Anti-epileptic Agent; Mania
232
Carbamazepine Use
Anti-epileptic Agent; Mania
233
Clonazepam Use
Mania
234
Cannabinoids
specific canabinoid receptors in CNS
| Endogenous compounds: analog of archidonic acid, arachidonylethanolamide
235
Salvia MOA
Active compound is Salvinorin A
| Agonist at kappa opioid & D2 receptors
236
Kratom MOA
Agonist activity at mu-opioid receptor
237
Cannabinoids Uses
Adjunct to Cancer Chemotherapy (antiemetic)
| Prevention of wasting in AIDS pts
238
Lithium Carbonate MOA Theory - Ionic
alters neuronal distribution of effect of Na+, K+, or Ca2+ in CNS
239
Lithium Carbonate MOA Theory - Biogenic Amine
alters release, reuptake, or metabolism of NT amine
240
Lithium Carbonate MOA Theory - Phospholipid
alters phopholipid metabolism involved in the phosphoinositide signaling pathway
241
Duloxetine Use
Neuropathic Pain
242
Fluoxetine S/E
Least Anticholinergic effects, Causes less weight gain, less sedation, less CV effects
HA, anxiety, tremor, agitation, nausea, sexual dysfunction in Males
243
Fluvoxamine Use
OCD
244
Paroxetine S/E
Higher drug interaction potential; More weight gain than other SSRIs
245
Which SSRI has the greatest potential for withdrawal syndrome?
Paroxetine (rapid acting)
246
Tx for Bulemia, Anorexia, Related Eating Disorders
SSRIs
247
Venlafaxine & Desvenlafaxine S/E
nausea, nervousness, anxiety, sweating
| Fewer CV effects, but may cause HTN, tachycardia, palpitations, & sexual dysfunction
248
Venlafaxine & Desvenlafaxine Use
Depression, GAD
| May work in pts refractory to SSRIs
249
Which drug is recommended for nighttime Tx of depression
Trazodone or Nefazodone
250
Trazodone S/E
Lower incidence of Anticholinergic & CV S/E
| May cause: priapism, sexual dysfunction in Males, VERY sedating
251
Bupropion Use
Nicotine, Cocaine, Amphetamine Dependence
252
Which drug is recommended for pts w/ depression & anxiety?
Mirtazepine
253
Drug for the Tx of ADHD in children & adults
Atomoxetine
254
Which drug causes potentially fatal Tyramine interactions & interactions w/ many drugs?
Phenelzine & Tranylcypromine
255
Serotonin Syndrome
switching b/w MAO-I & other classes may cause severe fever, convulsions, death if 3-4wks isn't provided b/w switch
256
Which drug is offered as a transdermal patch for depression?
Selegiline
257
Which drug is used to tx Parkinson's Disease?
Selegiline
258
Contraindications for Lithium Carbonate
pts w/ impaired renal function, CV or thyroid Ds, or during pregnancy
259
Drug interactions for Lithium Carbonate
NSAIDs, Diuretics, any drug altering renal function; Carbamazepine, methyldopa, anti-depressants/psychotics enhance neurotoxicity
