Drug Table - Complete Flashcards
(328 cards)
1
Q
Alkylating Agents Mechanism
A
Produce strong electrophiles throughcarbonium or ethyleneimonium ionintermediates, which covalently bond viaalkylation of nucleophilic moieties in DNA(mostly N7 position of guanine); Cell CycleNon-Specific (CCNS)
2
Q
Alkylating Agents Important Side Effects
A
Bone marrow, mucosal toxicity,nausea and vomiting, toxic effectson reproductive systems,increased leukemia risk
3
Q
Alkylating Agents Miscellaneous
A
Resistance may occur due to:decreased permeability or uptake;increased rates of catabolism;enhanced DNA repair; increasedglutathione production (inactivatesvia conjugation)
4
Q
List 11 Alkylating Agents
A
Mechlorethamine (Mustargen)Cyclophosphamide (Cytoxan)Ifosfamide (Ifex)Carmustine (Gliadel)Lomustine (Ceenu)Dacarbazine (DTIC)Procarbazine (Matulane)Temozolomide (Temodar)Cisplatin (Platinol)Carboplatin (Paraplatin)Oxaliplatin (Eloxatin)
5
Q
Mechlorethamine class
A
(Mustargen)Nitrogen mustard
6
Q
Mechlorethamine mechanism
A
Alkylating agent; spontaneous conversion to active metabolites in body fluids orenzymatically converted in liver
7
Q
Mechlorethamine Therapeutics
A
Hodgkin’s disease, topically for treatment of cutaneous T-cell lymphoma
8
Q
Mechlorethamine “Other” side effects
A
Severe nausea and vomiting,myelosuppression (leucopenia,thrombocytopenia)
9
Q
Mechlorethamine Misc
A
Don’t use much anymore due to sterility
10
Q
Cyclophosphamide(Cytoxan)Class
A
Nitrogen mustard
11
Q
Cyclophosphamide(Cytoxan)Mechanism
A
Alkylating agent; conversion by hepatic cytochrome P450 to active metabolite phosphoramide mustard
12
Q
Cyclophosphamide(Cytoxan)Therapeutics
A
Most widely used alkylating agent (broad clinical spectrum); singly or incombination for ALL, CLL, non-Hodgkin’s lymphoma, and breast, lung, and ovarian cancer
13
Q
Cyclophosphamide(Cytoxan)Important Side Effects
A
Hemorrhagic cystitis (bladderirritation) due to acrolein (toxicdrug metabolite); adequatehydration and administration ofMESNA (2-mercaptoethanesulfonate) minimizes problem
14
Q
Cyclophosphamide(Cytoxan)”Other” Side Effects
A
Nausea, vomiting,myelosuppression
15
Q
Cyclophosphamide(Cytoxan)Miscellaneous
A
Relatively long plasma half-life (7-15 hrs); taken orally
16
Q
Difference between Ifosfamide and Cyclophosphamide
A
TherapeuticsIfos is used for Sarcoma and testicular cancerCyclophosphamide is the most widely used
17
Q
Carmustine (Gliadel)Lomustine (Ceenu)Class
A
Nitrosoureas
18
Q
Carmustine (Gliadel)Lomustine (Ceenu)Mechanism
A
Alkylating agent
19
Q
Carmustine (Gliadel)Lomustine (Ceenu)Therapeutics
A
Brain tumors (cross blood-brain barrier)
20
Q
Carmustine (Gliadel)Lomustine (Ceenu)Imp Side Effects
A
Renal toxicity, pulmonary fibrosis
21
Q
Carmustine (Gliadel)Lomustine (Ceenu)Other side effects
A
Profound myelosuppression,severe nausea and vomiting
22
Q
Dacarbazine (DTIC)class
A
Triazenes
23
Q
Dacarbazine (DTIC)Mechanism
A
Alkylating agent; prodrug activated by livercytochromes
24
Q
Dacarbazine (DTIC)Therapeutics
A
Part of ABVD for Hodgkin’s disease; also, malignant melanoma
25
Dacarbazine (DTIC)"Other" Side Effects
Nausea and vomiting,myelosuppression (neutropenia, thrombocytopenia), flu-likesymptoms (fever, fatigue)
26
Dacarbazine (DTIC)Miscellaneous
IV administration
27
Procarbazine(Matulane)class
Triazenes
28
Procarbazine(Matulane)Mechanism
Alkylating agent; forms free radicals
29
Procarbazine(Matulane)Therapeutics
Hodgkin's lymphoma
30
Procarbazine(Matulane)Important side effects
May cause leukemia
31
Temozolomide(Temodar)class
Triazenes
32
Temozolomide(Temodar)Mechanism
Alkylating agent; nonenzymatic conversionto methylhydrazine at physiologic pH
33
Temozolomide(Temodar)Therapeutics
Malignant gliomas
34
Temozolomide(Temodar)"Other" Side Effects
Nausea and vomiting,myelosuppression (neutropenia,thrombocytopenia), flu-likesymptoms (fever, fatigue)
35
Temozolomide(Temodar)Miscellaneous
Taken orally
36
Cisplatin (Platinol)class
Platinum analogs
37
Cisplatin (Platinol)Mechanism
Alkylating agents that do not formcarbonium ion intermediates or formallyalkylate DNA; covalently bind nucleophilicsites on DNA (e.g., guanine N7); convertedto active cytotoxic forms by reacting withwater to form (+)charged, hydratedintermediates that react with DNA guanine,forming inter- and intrastand cross-links
38
Cisplatin (Platinol)Therapeutics
Testicular, ovarian, cervical, andbladder cancers; also useful intreatment of head and neck cancer,and lung carcinoma
39
Cisplatin (Platinol)Imp Side Effects
Nephrotoxicity, ototoxicity,peripheral motor and sensoryneuropathy at high doses
40
Cisplatin (Platinol)Other side effects
Severe nausea and vomiting,mild to moderatemyelosuppression
41
Carboplatin(Paraplatin)Class
Platinum analogs
42
Carboplatin(Paraplatin)Mechanism
Alkylating agents that do not formcarbonium ion intermediates or formallyalkylate DNA; covalently bind nucleophilicsites on DNA (e.g., guanine N7); convertedto active cytotoxic forms by reacting withwater to form (+)charged, hydratedintermediates that react with DNA guanine,forming inter- and intrastand cross-links
43
Carboplatin(Paraplatin)Therapeutics
Ovarian cancer
44
Carboplatin(Paraplatin)Other side effects
Myelosuppression(thrombocytopenia)
45
Oxaliplatin (Eloxatin)class
Platinum analogs
46
Oxaliplatin (Eloxatin)Mechanism
Alkylating agents that do not formcarbonium ion intermediates or formallyalkylate DNA; covalently bind nucleophilicsites on DNA (e.g., guanine N7); convertedto active cytotoxic forms by reacting withwater to form (+)charged, hydratedintermediates that react with DNA guanine,forming inter- and intrastand cross-links
47
Oxaliplatin (Eloxatin)Therapeutics
Gastric and colorectal cancer
48
Oxaliplatin (Eloxatin)Imp Side effects
Peripheral sensory neuropathy(cold-induced)
49
Oxaliplatin (Eloxatin)Other side effects
Neutropenia
50
Antimetabolites in general
Structural analogs of folic acid or of thepurine/pyramidine bases found in DNA; actin S-phase (cell cycle specific)
51
Antimetabolites list
Methotrexate (Trexall)Pemetrexed (Alimta)5-Fluorouracil (5-FU, Carac)Cytarabine (AraC, Depocyt)Gemcitabine (dFdC, Gemzar)6-Mercaptopurine (Purinethol)
52
Methotrexate (Trexall) class
Folate analogs
53
Methotrexate (Trexall) mech
Inhibits dihydrofolate reductase (DHFR),which converts dietary folate totetrahydrofolate (THF) needed for thymidineand purine synthesis; given orally orintrathecally
54
Methotrexate (Trexall) Therapeutics
Childhood ALL and choriocarcinoma;combination therapy for Burkitt'slymphoma and carcinomas of breast,ovary, head and neck, and bladder;administered intrathecally formeningeal leukemia and meningealmetastases of tumors (can't crossBBB); high-dose for osteosarcoma
55
Methotrexate (Trexall) Imp Side effects
Renal toxicity (crystallization inurine at high doses), hepatotoxicity(long-term, fibrosis/cirrhosis),reproductive (defective oogenesisor spermatogenesis, abortion)
56
Methotrexate (Trexall) Other side effects
Bone marrow(myelosuppression,spontaneous hemorrhage); GItoxicity (oral ulceration,stomatitis)
57
Methotrexate (Trexall) Misc
Can use leucovorin to prevent toxiceffects of MTX, as healthy cells cantake it up a lot better than tumor cells
58
Pemetrexed (Alimta) class
Folate analogs
59
Pemetrexed (Alimta) Mech
Polyglutamate forms that inhibit THFdependentenzymes (e.g., DHFR, TS);metabolized to polyglutamate forms thatinhibit THF-dependent enzymes (e.g.,DHFR, thymidylate synthase (TS))
60
Pemetrexed (Alimta) Therapeutics
Colon cancer, mesothelioma, non-smallcell lung cancer, pancreatic cancer
61
5-Fluorouracil (5-FU, Carac) class
Pyramidine analogs
62
5-Fluorouracil (5-FU, Carac) Mech
5-FU is converted to active metabolites: 5-FdUMP inhibits TS; 5-FdUTP incorporatesinto RNA & interferes with RNA function;prodrug [capesitabine] ribosylated and phophosrylated into5-FdUMP
63
5-Fluorouracil (5-FU, Carac) Therapeutics
Combination therapy for breast,colorectal, gastric, head and neck,cervical and pancreatic cancer;topically for basal cell carcinoma
64
5-Fluorouracil (5-FU, Carac) Imp Side Effects
Hand-foot syndrome (erythema,sensitivity of palms and soles),cardiac toxicity (acute chest pains)
65
5-Fluorouracil (5-FU, Carac) Other side effects
Anorexia and nausea; mucosalulcerations, stomatitis, diarrhea;thrombocytopenia and anemia
66
5-Fluorouracil (5-FU, Carac) Misc
Leucovorin can potentiate effects of5-FU; must be given IV (GI toxicityand rapid degradation + metabolismin gut and liver)
67
Cytarabine (AraC, Depocyt) Class
Pyramidineanalogs
68
Cytarabine (AraC, Depocyt) Mech
Ara-C converted by deoxycytidine kinase toAra-CMP --> Ara-CTP; terminates DNAsynthesis as Ara-CTP
69
Cytarabine (AraC, Depocyt) Therapeutics
AML (most effective treatment), ALLand blast phase CML
70
Cytarabine (AraC, Depocyt) Other side effects
Severe myelosuppression(leucopenia, thrombocytopenia,anemia), GI tract toxicity(ulceration, stomatitis, diarrhea)
71
Gemcitabine (dFdC, Gemzar) class
Pyramidineanalogs
72
Gemcitabine (dFdC, Gemzar) Mech
Converted to active metabolites: dFdCDPinhibits ribonucleotide reductase (lowersdeoxyribonucleotide); dFdCTP incorporatesinto DNA, terminating DNA synthesis
73
Gemcitabine (dFdC, Gemzar) Therapeutics
Pancreatic cancer; effective againstnon-small cell lung cancer, ovarian,bladder, esophageal, and head andneck cancer
74
Gemcitabine (dFdC, Gemzar) Other side effects
Myelosuppression (leucopenia,thrombocytopenia, anemia), flulike
75
Gemcitabine (dFdC, Gemzar) Misc
More effective against solid tumorsthan cytarabine
76
6-Mercaptopurine (Purinethol) Class
Purine analogs(antimetabolites)
77
6-Mercaptopurine (Purinethol) Mech
Prodrug metabolized by hypoxanthineguaninephosphoribosyl transferase(HGPRT) to 6-thioinosinic acid (TIMP);TIMP inhibits first step of de novo purinebase synthesis and the formation of AMPand xanthinylic acid from inosinic acid,reducing purine levels. As well, TIMP isconverted to thio-guanine ribonucleotides,inhibiting DNA and RNA synthesis
78
6-Mercaptopurine (Purinethol) Therapeutics
Maintain remission in acute ALL
79
6-Mercaptopurine (Purinethol) Imp side effects
Hepatotoxicity in prolonged use
80
6-Mercaptopurine (Purinethol) Other side effects
Bone marrow suppression
81
6-Mercaptopurine (Purinethol) Misc
Drug interaction with allopurinol (forgout), which inhibits xanthineoxidase; decrease 6-MP dose toavoid drug accumulation andtoxicities
82
DNA Intercalating Agents General Mechanism
Bind DNA through intercalation betweenspecific bases, blocking DNA, RNA or bothsynthesis; cause DNA strands to break andinterfere with cell replication; CCNS
83
Dactinomycin (Actinomycin D, Cosmegen) Mech
Intercalates G-C base pairs of DNA,interfering with DNA-dependant RNApolymerase; also causes ssDNA breaks
84
Dactinomycin (Actinomycin D, Cosmegen) Therapeutics
Pediatric tumors (Wilms' tumor,rhabdomyosarcoma Ewing's sarcoma);choriocarcinoma in women
85
Dactinomycin (Actinomycin D, Cosmegen) Imp Side effects
Hematopoietic suppression withpancytopenia
86
Dactinomycin (Actinomycin D, Cosmegen) Other side effects
Anorexia, nausea, vomiting
87
Daunorubicin (Cerubidine) Class
Anthracyclines
88
Daunorubicin (Cerubidine) Mech
Intercalate between DNA base pairs anddonate electrons to O2 to form superoxide;superoxide reacts with itself to form H2O2 --> cleaved in the presence of Fe to form OHradical, which cleaves DNA
89
Daunorubicin (Cerubidine) Therapeutics
AML
90
Daunorubicin (Cerubidine) Imp Side effects
Irreversible dose-dependentcardiotoxicity; alopecia
91
Daunorubicin (Cerubidine) Other side effects
Myelosuppression(neutropenia), stomatitis, GIdisturbances
92
Daunorubicin (Cerubidine) Misc
Dexrazoxane is cardio-protective
93
Idarubicin (Idamycin) Class
Anthracyclines
94
Idarubicin (Idamycin) Mech
Intercalate between DNA base pairs anddonate electrons to O2 to form superoxide;superoxide reacts with itself to form H2O2 --> cleaved in the presence of Fe to form OHradical, which cleaves DNA
95
Idarubicin (Idamycin) Therapeutics
AML
96
Idarubicin (Idamycin) Imp Side effects
Irreversible dose-dependentcardiotoxicity; alopecia
97
Idarubicin (Idamycin) Other side effects
Myelosuppression(neutropenia), stomatitis, GIdisturbances
98
Idarubicin (Idamycin) Misc
Dexrazoxane is cardio-protective
99
Doxorubicin (Adriamicin, Doxil) class
Anthracyclines
100
Doxorubicin (Adriamicin, Doxil) Mech
Intercalate between DNA base pairs anddonate electrons to O2 to form superoxide;superoxide reacts with itself to form H2O2 --> cleaved in the presence of Fe to form OHradical, which cleaves DNA
101
Doxorubicin (Adriamicin, Doxil) Therapeutics
Sarcomas, breast and lung carcinomas,malignant lymphomas
102
Doxorubicin (Adriamicin, Doxil) Imp side effects
Irreversible dose-dependentcardiotoxicity; alopecia
103
Doxorubicin (Adriamicin, Doxil) Other side effects
Myelosuppression(neutropenia), stomatitis, GIdisturbances
104
Doxorubicin (Adriamicin, Doxil) Misc
Dexrazoxane can be used to preventcardiotoxic effects
105
Epirubicin (Ellence) Class
Anthracyclines
106
Epirubicin (Ellence) Mech
Intercalate between DNA base pairs anddonate electrons to O2 to form superoxide;superoxide reacts with itself to form H2O2 --> cleaved in the presence of Fe to form OHradical, which cleaves DNA
107
Epirubicin (Ellence) Therapeutics
Metastatic breast cancer, gastriccancer
108
Epirubicin (Ellence) Imp side effects
Irreversible dose-dependentcardiotoxicity; alopecia
109
Epirubicin (Ellence) Other side effects
Myelosuppression(neutropenia), stomatitis, GIdisturbances
110
Epirubicin (Ellence) Misc
Dexrazoxane can be used to preventcardiotoxic effects
111
Bleomycin (Blenoxane) Mech
Acts in G2 phase of cell cycle. Binds toDNA, producing ss- and dsDNA breaks
112
Bleomycin (Blenoxane) Therapeutics
Combination therapy for testiculartumors or Hodgkin's disease;squamous cell carcinomas andlymphomas
113
Bleomycin (Blenoxane) Imp side effects
Pulmonary toxicity (pulmonaryfibrosis); cutaneous toxicity(hyperpigmentation,hyperkeratosis, erythema);hyperthermia
114
Bleomycin (Blenoxane) Other side effects
Minimally myelo- andimmunosuppressive (often usedin combo therapy); headache,nausea, vomiting
115
Bleomycin (Blenoxane) Misc
Dexrazoxane can be used to preventcardiotoxic effects
116
Microtubule Inhibitors
Inhibit mitosis and cause metaphase arrestby interfering with microtubule function(tubulin (de)polymerization); CCS
117
Vinblastine (Velban) Class
Vinca alkaloids
118
Vinblastine (Velban) Mech
Block tubulin polymerization intomicrotubules
119
Vinblastine (Velban) Therapeutics
Metastatic testicular tumors (withbleomycin, cisplatin); component ofABVD used for Hodgkin's disease
120
Vinblastine (Velban) Other side effects
Myelosuppression, nausea,vomiting
121
Vincristine (Oncovin) Class
Vinca alkaloids
122
Vincristine (Oncovin) Mech
Block tubulin polymerization intomicrotubules
123
Vincristine (Oncovin) Therapeutics
Childhood ALL (with glucocorticoids);Hodgkin's and non-Hodgkin'slymphomas
124
Vincristine (Oncovin) Important side effects
Dose-limiting neurotoxicity(peripheral neuropathy)
125
Vincristine (Oncovin) Other side effects
Relatively low bone marrowtoxicity
126
Paclitaxel (Taxol, Abraxane) Class
Taxanes
127
Paclitaxel (Taxol, Abraxane) Mech
Block microtubule depolymerization intotubulin
128
Paclitaxel (Taxol, Abraxane) Therapeutics
Metastatic breast, ovarian, lung, andhead and neck cancers
129
Paclitaxel (Taxol, Abraxane) Imp side effects
Peripheral neuropathy
130
Paclitaxel (Taxol, Abraxane) other side effects
Neutropenia; hypersensitivityreactions
131
Docetaxel (Taxotere) class
Taxanes
132
Docetaxel (Taxotere) Mech
Block microtubule depolymerization intotubulin
133
Docetaxel (Taxotere) Therapeutics
Metastatic breast, ovarian, lung, andhead and neck cancers; hormonerefractory prostate cancer
134
Docetaxel (Taxotere) Important side effects
Peripheral neuropathy
135
Docetaxel (Taxotere) Other side effects
Neutropenia; hypersensitivityreactions
136
Etoposide (Etopophos) class
Epipodophyllotoxins
137
Etoposide (Etopophos) mechanism
Inhibits topoisomerase II
138
Etoposide (Etopophos) Therapeutics
Testicular carcinoma, lung cancer, andnon-Hodgkin's lymphoma
139
Etoposide (Etopophos) other side effects
Dose-limiting myelosuppression(neutropenia), oral mucositis
140
Teniposide (Vumon) Class
Epipodophyllotoxins
141
Teniposide (Vumon) Mechanism
Inhibits topoisomerase II
142
Teniposide (Vumon) Therapeutics
ALL
143
Teniposide (Vumon) Other side effects
Dose-limiting myelosuppression(neutropenia), oral mucositis
144
Irinotecan (Camptosar) Class
Camptothecinanalogs
145
Irinotecan (Camptosar) Mechanism
Inhibits topoisomerase I
146
Irinotecan (Camptosar) Therapeutics
Advanced colorectal cancer; lung,ovarian, cervical and brain tumors
147
Irinotecan (Camptosar) Other side effects
Severe neutropenia, severediarrhea
148
Topotecan (Hycamtin) Class
Camptothecinanalogs
149
Topotecan (Hycamtin) Mechanism
Inhibits topoisomerase I
150
Topotecan (Hycamtin) Therapeutics
Ovarian and small cell lung cancer
151
Topotecan (Hycamtin) Other side effects
Severe neutropenia, severediarrhea
152
Prednisone (Meticorten) Class
Glucocorticoids
153
Prednisone (Meticorten) Mechanism
Inhibit mitosis in lymphocytes
154
Prednisone (Meticorten) Therapeutics
ALL; combination for Hodgkin's, non-Hodkin's, multiple myeloma, and CLL
155
Dexamethasone (Decadron) Class
Glucocorticoids
156
Dexamethasone (Decadron) Mechanism
Inhibit mitosis in lymphocytes
157
Dexamethasone (Decadron) Therapeutics
Reduces edema in brain and spinalcord tumors with radiation therapy
158
Tamoxifen (Soltamox) Class
Selectiveestrogen-receptormodulators(SERMs)
159
Tamoxifen (Soltamox) Mechanism
Competes with estradiol for binding toestrogen receptor
160
Tamoxifen (Soltamox) Therapeutics
ER-positive breast cancer, or asadjuvant therapy following primarybreast tumor excision; prevention ofbreast cancer in high-risk patients
161
Tamoxifen (Soltamox) Important side effects
Hot flushes, hair loss; increasedrisk of endometrial cancer;increased risk of thromboembolicevents
162
Tamoxifen (Soltamox) Other side effects
Nausea and vomiting
163
Fulvestrant (Faslodex) Class
Selectiveestrogen-receptordownregulators(SERDs)
164
Fulvestrant (Faslodex) Mechanism
Binds with much higher affinity (>100-fold)to estrogen receptor than tamoxifen,inhibiting dimerization, increasingdegradation, and reducing overall ER levels
165
Fulvestrant (Faslodex) Therapeutics
Posmenopausal women with ERpositivemetastatic breast cancer
166
Aminoglutethamide (Cytadren) Class
Aromataseinhibitors
167
Aminoglutethamide (Cytadren) Mechanism
Inhibits function of aromatase
168
Aminoglutethamide (Cytadren) Therapeutics
Relatively weak, used against breastcancer
169
Aminoglutethamide (Cytadren) Imp side effects
Significant
170
Anastrozole (Arimidex) Class
Aromataseinhibitors
171
Anastrozole (Arimidex) Mechanism
Inhibits function of aromatase
172
Anastrozole (Arimidex) Therapeutics
First-line for ER-positive breast cancerin postmenopausal women
173
Letrozole (Femara) class
Aromataseinhibitors
174
Letrozole (Femara) Mechanism
Inhibits function of aromatase
175
Letrozole (Femara) Therapeutics
ER-positive breast cancer inpostmenopausal women
176
Exemestane (Aromasin) class
Aromataseinhibitors
177
Exemestane (Aromasin) Mechanism
Steroidal inhibitor of aromatase
178
Exemestane (Aromasin) Therapeutics
ER-positive breast cancer inpostmenopausal women
179
Leuprolide (Lupron) class
GnRH analogs
180
Leuprolide (Lupron) Mechanism
Binds GnRH receptor; inhibits release ofFSH & LH
181
Leuprolide (Lupron) Therapeutics
Androgen ablation therapy, along withAR blockers
182
Goserelin (Zoladex) Class
GnRH analogs
183
Goserelin (Zoladex) Mechanism
Binds GnRH receptor; inhibits release ofFSH & LH
184
Goserelin (Zoladex) Therapeutics
Androgen ablation therapy, along withAR blockers
185
Flutamide (Eulexin) Class
Nonsteroidalandrogen-receptorblockers
186
Flutamide (Eulexin) Mechanism
Competes with androgen for AR binding
187
Flutamide (Eulexin) Therapeutics
Androgen ablation therapy, along withGnRH analogs
188
Bicalutamide (Casodex) Class
Nonsteroidalandrogen-receptorblockers
189
Bicalutamide (Casodex) Mechanism
Competes with androgen for AR binding
190
Bicalutamide (Casodex) Therapeutics
Androgen ablation therapy, along withGnRH analogs
191
Imatinib (Gleevac) Class
Tyrosine Kinaseinhibitor
192
Imatinib (Gleevac) Mechanism
Inhibits Abl kinase by binding where ATPshould go; also inhibits PDGFR and c-kit;metabolized by cytochrome P450
193
Imatinib (Gleevac) Therapeutics
First line therapy for CML; also,gastrointestinal tumor (GIST)
194
Imatinib (Gleevac) Imp Side effects
Nausea and vomiting, fluidretention, muscle cramps,arthralgia
195
Imatinib (Gleevac) Other side effects
Myelosuppression
196
Imatinib (Gleevac) Misc
Oral (1/day)
197
Gefitinib (Iressa) Class
Tyrosine Kinaseinhibitor
198
Gefitinib (Iressa) Mechanism
Inhibit epidermal growth factor receptor(EGFR) tyrosine kinase
199
Gefitinib (Iressa) Therapeutics
Non-small lung cancer
200
Erlotinib (Tarceva) Class
Tyrosine Kinaseinhibitor
201
Erlotinib (Tarceva) Mechanism
Inhibit epidermal growth factor receptor(EGFR) tyrosine kinase
202
Erlotinib (Tarceva) Therapeutics
Non-small lung cancer
203
Nilotinib (Tasigna) class
Tyrosine Kinaseinhibitor
204
Nilotinib (Tasigna) Mechanism
Inhibits Abl kinase
205
Nilotinib (Tasigna) Therapeutics
Imatinib-resistant CML
206
Nilotinib (Tasigna) Imp side effects
Myelosuppression
207
Nilotinib (Tasigna) other side effects
QT prolongation, hepatotoxicity,electrolyte abnormalities
208
Nilotinib (Tasigna) misc
Oral (2/day)
209
Dasatinib (Sprycel) class
Tyrosine Kinaseinhibitor
210
Dasatinib (Sprycel) mechanism
Inhibits Abl & Src kinases
211
Dasatinib (Sprycel) therapeutics
Imatinib-resistant CML
212
Dasatinib (Sprycel) Imp side effects
Myelosuppression, bleeding, fluidretention, pulmonary arterialhypertension
213
Dasatinib (Sprycel) other side effects
Diarrhea, nausea and vomiting,weakness, infections
214
Dasatinib (Sprycel) misc
Oral (1/day)
215
Rituximab (Rituxan) class
Monoclonalantibody
216
Rituximab (Rituxan) mechanism
CD20 B-cell antibody that can directlyactivate apoptosis, activate complement, oractivate cell-mediated cytotoxicity (e.g., Tcells, NK cells)
217
Rituximab (Rituxan) therapeutics
Non-Hodgkin's lymphomas
218
Rituximab (Rituxan) imp side effects
Infusion reactions, tumor lysissyndrome (TLS), severemucocutaneous reactions,progressive multifocalleukoencephalopathy (PML)
219
Rituximab (Rituxan) other side effects
Skin reactions, irregularheartbeat, muscle or joint pain
220
Rituximab (Rituxan) misc
Patients need careful monitoring
221
Trastuzumab (Herceptin) class
Monoclonalantibody
222
Trastuzumab (Herceptin) mechanism
Unknown HER2/neu (ErbB2) receptorantibody mechanism (enhanced receptorendocytosis or blocking homo- orheterodimerization)
223
Trastuzumab (Herceptin) therapeutics
HER2/neu-overexpressing metastaticbreast cancer
224
Trastuzumab (Herceptin) Imp side effects
Hypersentivity reaction; ventriculardysfunction
225
Trastuzumab (Herceptin) misc
Usually combined with taxanes;enhances doxorubicin cardiotoxicity
226
Cetuximab (Erbitux) class
Monoclonalantibody
227
Cetuximab (Erbitux) mechanism
EGFR1 (ErbB1)
228
Cetuximab (Erbitux) therapeutics
EGFR-positive metastatic colorectalcancer
229
Cetuximab (Erbitux) imp side effects
Allergic reactions, sudden cardiacdeath, dermatologic problems,infections, renal failure, electrolyteabnormalities
230
Cetuximab (Erbitux) other side effects
Asthenia/malaise, fever,nausea, constipation, interstitialpneumonitis
231
Cetuximab (Erbitux) misc
Clinical trials, probably combine withcisplatin
232
Cetuximab (Erbitux) class
Monoclonalantibody
233
Cetuximab (Erbitux) mechanism
EGFR1 (ErbB1)
234
Cetuximab (Erbitux) therapeutics
EGFR-positive metastatic colorectalcancer
235
Cetuximab (Erbitux) imp side effects
Allergic reactions, sudden cardiacdeath, dermatologic problems,infections, renal failure, electrolyteabnormalities
236
Cetuximab (Erbitux) other side effects
Asthenia/malaise, fever,nausea, constipation, interstitialpneumonitis
237
Cetuximab (Erbitux) misc
Clinical trials, probably combine withcisplatin
238
Ipilimumab (Yervoy) class
Humanmonoclonalantibody
239
Ipilimumab (Yervoy) mechanism
Cytotoxic T-Lymphocyte Antigen 4 inhibitor;stimulates immune system
240
Ipilimumab (Yervoy) therapeutics
Melanoma
241
Vemurafenib (Zelboraf) class
Serine/threoninekinase inhibitor
242
Vemurafenib (Zelboraf) mechanism
Inhibits oncogenic BRAF kinase
243
Vemurafenib (Zelboraf) therapeutics
Unresectable Stage III and IV ormetastatic melanomas w/BRAFmutations
244
Vemurafenib (Zelboraf) imp side effects
Arthralgia, fatigue, photosensitivity,nausea, alopecia, diarrhea, QTprolongation
245
Vemurafenib (Zelboraf) other side effects
Cutaneous squamous cellcarcinoma, keratoacanthoma,new primary cutaneousmelanoma
246
Vemurafenib (Zelboraf) misc
Superior to dacarbazine in Phase IIItrials
247
Dabrafenib (Tafinlar) class
Serine/threoninekinase inhibitor
248
Dabrafenib (Tafinlar) mechanism
Inhibits oncogenic BRAF kinase
249
Dabrafenib (Tafinlar) therapeutics
Unresectable Stage III and IV ormetastatic melanomas w/BRAFmutations
250
Dabrafenib (Tafinlar) imp side effects
Serious febrile drug reactions,uveitis and iritis, hyperglycemia,hyperkeratosis
251
Dabrafenib (Tafinlar) other side effects
Higher risk of developing above
252
Dabrafenib (Tafinlar) misc
May cause male infertility
253
Trametinib (Mekinist) mechanism
Inhibits MEK
254
Trametinib (Mekinist) therapeutics
Unresectable Stage III and IV ormetastatic melanomas w/BRAFmutations
255
Trametinib (Mekinist) imp side effects
Cardiomyopathy, retinal disorders,interstitial lung disease, seriousskin toxicities
256
Trametinib (Mekinist) other side effects
Rash, diarrhea, stomatitis,hypertension, pruritis
257
Trametinib (Mekinist) misc
May cause female infertility
258
Hydroxyurea (Hydrea) mechanism
Inhibits ribonucleoside diphosphatereductase
259
Hydroxyurea (Hydrea) therapeutics
CML (replaced by Imatinib),polycythemia vera, essentialthrombocythemia; treatment for sicklecell disease (increases Hb-F)
260
Retinoids Mechanism
ATRA induces terminal differentiation inmalignant immature promyelocytes, whichsubsequently apoptose
261
Retinoids Therapeutics
APL
262
Retinoids imp side effects
"Leukocyte Activation Syndrome"(LAS), an increase in WBCs (fever,weight gain, respiratory distress,serosal effusion, renal failure)
263
Retinoids misc
Combined w/anthracyclines;corticosteroids used to block "LAS"
264
Arsenic Trioxide (Trisenox) Therapeutics
Relapsed APL
265
Thalidomide (Thalomid) Therapeutics
Multiple myeloma and myelodysplasticsyndromes
266
Interferons
Hairy-cell leukemia, CML, and AIDSrelatedKaposi's sarcoma
267
ABVD
Doxorubicin (adriamycin), bleomycin,vinblastine, dacarbazine
268
CHOP
Cyclophosphamide, hydroxydoxorubicin,vincristine (oncovine), prednisone
269
MOPP
Mechlorethamine, vincristine (oncovine),procarbazine, prednisone
270
CMF
Cyclophosphamide, methotrexate, 5-fluorouracil
271
FEC
5-fluorouracil, epirubicin, cyclophosphamide
272
Class for:Estradiol (valerate & cypionate)Estrone sulfateEquilin sulfateQuinestrol
Estradiol esters(steroidal)
273
Class for:Ethinyl estradiolMestranol
Alkyl estrogen
274
Mechanism for:Estradiol (valerate & cypionate)Estrone sulfateEquilin sulfateQuinestrolEthinyl estradiolMestranol
Absorbed through skin, mucus membranes,GI Tract; body-wide distribution via sexhormonebinding globulin
275
Therapeutics for:Estradiol (valerate & cypionate)Estrone sulfateEquilin sulfateQuinestrolEthinyl estradiolMestranol
Contraception, primary hypogonadism,postmenopausal hormone therapy
276
Imp side effects for:Estradiol (valerate & cypionate)Estrone sulfateEquilin sulfateQuinestrolEthinyl estradiolMestranol
Weight gain, HTN; less commonly,may cause breast cancer, DVT,cervical and endometrial cancer
277
Other side effects for:Estradiol (valerate & cypionate)Estrone sulfateEquilin sulfateQuinestrolEthinyl estradiolMestranol
Nausea, breast tension/pain,vaginal bleeding, headache
278
Misc for:Estradiol (valerate & cypionate)Estrone sulfateEquilin sulfateQuinestrolEthinyl estradiolMestranol
Strongly contraindicated in breast orendometrial cancers, endometriosis,undiagnosed vaginal bleeds;relatively contradinicated inpregnancy, thromboembolic disease,HTN, hepatic disease, family historyof breast or uterine cancer
279
Diethylstilbestrol class
Non-steroidalsynthetic estrogen
280
Diethylstilbestrol Imp side effect
Increased risk of clear celladenocarcinoma of vagina & cervix
281
Tamoxifen citrate (Nolvadex) class
Non-steroidal antiestrogen;selectiveestrogen receptormodifier
282
Tamoxifen citrate (Nolvadex) mechanism
Blocks estrogen from binding ER andcausing growth in ER(+) breast cancer
283
Tamoxifen citrate (Nolvadex) therapeutics
ER(+) breast cancer
284
Tamoxifen citrate (Nolvadex) imp side effects
Pro-estrogenic effect on uterineepithelium (increase risk ofendometrial cancer); partialestrogen agonist in bone andendometrium
285
Tamoxifen citrate (Nolvadex) misc
Anti-estrogenic effect on mammaryepithelium; must be used in veryhigh doses
286
Clomiphene citrate (Clomid) class
Non-steroidal antiestrogen
287
Clomiphene citrate (Clomid) mechanism
Blocks estrogen binding to hypothalamicreceptors (no estradiol negative feedbackon gonadotropins) --> increased secretionof gonadotropins & LH --> ovulation
288
Clomiphene citrate (Clomid) therapeutics
Stimulate ovulation in patients whowant to get pregnant
289
Clomiphene citrate (Clomid) imp side effects
Hot flashes, multiple pregnancy
290
Clomiphene citrate (Clomid) other side effects
Stomach pain, headache, upsetstomach, vomit
291
Clomiphene citrate (Clomid) misc
Cis-isomer (zuclomiphene) is a weakestrogen agonist; trans-isomer(enclomiphene) is a potent estrogenantagonist
292
ClassMicronized progesteroneTransvaginal progesterone
Naturalprogesterone
293
Therapeutics forMicronized progesteroneTransvaginal progesterone
Contraception, hormone replacementtherapy
294
Imp side effects forMicronized progesteroneTransvaginal progesterone
Fatigue, drowsiness
295
Misc forMicronized progesteroneTransvaginal progesterone
Contraindicated in thromboembolicdisorders or patients with such ahistory, liver disease (metabolised inthe liver), undiagnosed vaginalbleeding, pregnancy (atrophy ofendometrium leading to birthdefects)
296
Class for:MedroxyprogesteroneNorethindroneNorgestrelMegestrol
Syntheticprogesterone
297
Therapeutics for:MedroxyprogesteroneNorethindroneNorgestrelMegestrol
Contraception, hormone replacementtherapy
298
Imp side effects for:MedroxyprogesteroneNorethindroneNorgestrelMegestrol
Edema, abdominal bloating; lesscommonly: strong androgeniceffects (hirsutism, acne)
299
Other side effects for:MedroxyprogesteroneNorethindroneNorgestrelMegestrol
Anxiety, irritability, depression,muscular pain; increased risk ofthrombus and PE
300
Misc for:MedroxyprogesteroneNorethindroneNorgestrelMegestrol
Contraindicated in thromboembolicdisorders or patients with such ahistory, liver disease (metabolised inthe liver), undiagnosed vaginalbleeding, pregnancy (atrophy ofendometrium leading to birthdefects)
301
Class for:Monophasic Ortho-NovumBiphasic Ortho-NovumTriphasic Ortho-Novum
Combination pill
302
Mechanism for:Monophasic Ortho-NovumBiphasic Ortho-NovumTriphasic Ortho-Novum
Constant level of estrogen suppresses FSH,LH surge; progesterone suppresses LHsurge, thickens cervical mucus, leads toendometrial atrophy
303
Therapeutics for:Monophasic Ortho-NovumBiphasic Ortho-NovumTriphasic Ortho-Novum
Contraception
304
Imp side effects for:Monophasic Ortho-NovumBiphasic Ortho-NovumTriphasic Ortho-Novum
As with synthetic estrogen andprogesterones
305
Monophasic Ortho-Novum Misc
Consistent dose of estrogen andprogestin (only take 21 days)
306
Biphasic Ortho-Novum Misc
Fixed estrogen, progestin increasedfor days 11-21
307
Triphasic Ortho-Novum Misc
Fixed or variable estrogen, whileprogestin increases in 3 phases (1-7,8-14, 15-21)
308
Mini-pill class
Progestin only
309
Mini-pill mechanism
As progestin
310
Mini-pill Therapeutics
Less effective than combination pill forcontraception; use when patient hasestrogen contraindication; good inlactating women (estrogen reduces milkproduction)
311
Mini-pill imp side effect
More likely to produce irregularmenstrual cycle (estrogen requiredto provide stability to endometrium)
312
Mini-pill other side effect
Suppresses endometrial cancer
313
Levonorgestrel (Plan B) class
Syntheticprogestogen
314
Levonorgestrel (Plan B) Mechanism
Not known
315
Levonorgestrel (Plan B) Therapeutics
Prevent implantation
316
Levonorgestrel (Plan B) Imp side effect
Likely the same as combinationoral contraceptives
317
Levonorgestrel (Plan B) misc
Must be taken within 72 hours ofcoitus
318
Mifepristone (RU-486, Korlym) class
Anti-progestin;glucocorticoidreceptorantagonist
319
Mifepristone (RU-486, Korlym) Mechanism
Competitively binds to progesteronereceptor (leading to detachment of fetus);glucocorticoid recepter antagonist
320
Mifepristone (RU-486, Korlym) Therapeutics
Abortion; Cushing's Syndrome
321
Mifepristone (RU-486, Korlym) Misc
Must take early in pregnancy (by day49); oral administration; must begiven by doctor in medical facilityprepared for surgery if abortionincomplete
322
Class for:Sildenafil citrate (Viagra)Vardenafil HCl (Levitra)Tadalafil (Cialis)
PDE5 inhibitor
323
Mechanism for:Sildenafil citrate (Viagra)Vardenafil HCl (Levitra)Tadalafil (Cialis)
Bind catalytic site of PDE5; inhibits PDE5breakdown of cGMP --> decreased Ca -->smooth muscle relaxation --> erection
324
Therapeutics for:Sildenafil citrate (Viagra)Vardenafil HCl (Levitra)Tadalafil (Cialis)
Erectile dysfunction; does not trigger anautomatic erection, but improvesresponse to sexual stimulation
325
Imp side effects for:Sildenafil citrate (Viagra)Vardenafil HCl (Levitra)Tadalafil (Cialis)
Headache, dizziness, change invision (NAION)
326
Other side effects for:Sildenafil citrate (Viagra)Vardenafil HCl (Levitra)Tadalafil (Cialis)
Flushing, upset stomach, stuffyor runny nose, UTI, diarrhea
327
Misc for:Sildenafil citrate (Viagra)Vardenafil HCl (Levitra)
Oral (once/day max); half-life of 4hours, peak plasma concentration in1-2 hours; contraindicated if onnitrates or α-blockers (unsafe drop inBP)
328
Misc for:Tadalafil (Cialis)
Oral (once/day max); half-life of 17.5hours, peak plasma concentration in1-2 hours; contraindicate if onnitrates or α-blockers (unsafe drop inBP)
