Unit 1-Cancer, arthritis, gout, reproductive pharm Flashcards
1
Q
Mechanism of alkylating agents
A
Produce electrophiles via carbonium or ethyleneimonium ions which akylate to nucleophilic moieties on DNA bases eg guanine;
Cell cycle nonspecific
2
Q
Side effects of alkylating agents
A
- bone marrow toxicity
- mucosal toxicity
- nausea and vomiting
- reproductive effects
- increased risk of leukemia
3
Q
How may resistance to alkylating agents occur?
A
- decreased permeability or uptake
- increased catabolism
- enhanced DNA repair
- increased glutathione productive which inactivates drug by conjugation
4
Q
Mechlorethamine
Drug class
A
nitrogen mustard
5
Q
Mechlorethamine
Mechanism
A
- alkylating agent
- spontaneous conversion to active metabolites in body fluids or enzymatically converted in liver
6
Q
Mechlorethamine
Uses
A
- Hodgkin’s lymphoma as part of MOPP combo therapy
- topically used for cutaneous T-cell lymphomas
7
Q
Mechlorethamine
Side effects
A
- Severe nausea and vomiting
- Myelosuppression (leukopenia and thrombocytopenia
8
Q
Cyclophosphamide
Drug Class
A
Nitrogen Mustard
9
Q
Cyclophosphamide
Mechanism
A
- Alkylating agent
- Conversion by liver CYP50 to active form phosphoramide mustard
- relatively long half life
- taken orally
10
Q
Cyclophosphamide
Uses
A
- broad spectrum uses
- most widely uses alkylating agent
- ALL, CLL, non-hodgkin’s lymphoma, breast, lung, and ovarian cancers
11
Q
Cyclophosphamide
Important side effects
A
- Hemorrhagic cystitis (bladder irritation) due to acrolein which is a toxic drug metabolite
- Minimize this side effect with adequate hydration and MESNA (2-mercaptoethane sulfonate)
- Also nausea, vomiting, and myelosuppression
12
Q
Ifosfamide
Drug class
A
Nitrogen mustard
13
Q
Ifosfamide
Mechanism
A
Alkylating agent; converted by liver CYP450 to active metabolite phosphoramide mustard (just like cyclophosphamide)
Long plasma half life
Taken orally
14
Q
Ifosfamide
Uses
A
Sarcoma and testicular cancer
15
Q
Ifosfamide
Side effects
A
- Hemorrhagic cytitis due to acrolein which is a toxic drug metabolite
- minimize problem with adequate hydration and MESNA (2-mercaptoethane sulfonate)
- same problem as in cyclophosphamide
- also nausea, vomiting, myelosuppression
16
Q
Carmustine
Drug Class
A
Nitrosurea
17
Q
Carmustine
Mechanism of Action
A
Alkylating Agent
18
Q
Carmustine
Uses
A
Brain tumors
(can cross BBB)
19
Q
Carmustine
Side effects
A
- CNS toxicity (dizziness)
- Pulmonary fibrosis
- Also nausea, vomiting, profound myelosuppression
20
Q
Lomustine
Drug class
A
Nitrosurea
21
Q
Lomustine
Mechanism of action
A
Alkylating agent
22
Q
Lomustine
Uses
A
Brain tumors (can cross BBB)
23
Q
Lomustine
Side effects
A
- CNS toxicity (dizziness)
- pulmonary fibrosis
- Also profound myelosuppression, severe nausea and vomiting
24
Q
Dacarbazine
Drug class
A
Triazene
25
Dacarbazine
Mechanism of action
* alkylating agent
* prodrug converted by liver to active form
* IV administration
26
Dacarbazine
Uses
* part of AVBD protocol for Hodgkin's disease
* also malignant melanoma
27
Dacarbazine
Side effects
* nausea, vomiting
* myelosuppression (thrombocytopenia, neutropenia)
* flu-like symptoms (fever, fatigue)
28
Procarbazine
Drug class
Triazene
29
Procarbazine
Mechanism of action
Alkylating agent; forms free radicals
30
Procarbazine
Uses
Hodgkin's lymphoma
31
Procarbazine
Side effects
May cause leukemia
32
Temozolomide
Drug class
Triazene
33
Temozolomide
Mechanism of action
* alkylating agent
* non-enzymatic conversion to methylhydrazine at physiologic pH
* taken orally
34
Temozolomide
Uses
Malignant gliomas
35
Temozolomide
Side effects
* Nausea and vomiting, myelosuppression (neutropenia, thrombocytopenia), flu-like symptoms (fever, fatigue)
36
Cisplatin
Drug class
Platinum analog
37
Cisplatin
Mechanism of action
* Alkylating agent but does not form carbonium intermediate
* instead it reacts with water to form a +charged intermediate that reacts with guanine to crosslink DNA
38
Cisplatin
Uses
* ovarian, testiclular, cervical, bladder cancers
* also head, neck, lung cancers
39
Cisplatin
Side effects
* nephrotoxicity, ototoxicity
* peripheral motor and sensory neuropathy at high doses
* also severe nausea and vomiting; mild to moderate myelosuppression
40
Carboplatin
Drug class
Platinum analog
41
Carboplatin
Mechanism of action
* Alkylating agent but does not form carbonium intermediate
* instead it reacts with water to form a +charged intermediate that reacts with guanine to crosslink DNA
42
Carboplatin
Uses
Ovarian cancer
43
Carboplatin
Side effects
Myelosuppression (thrombocytopenia)
44
Oxaliplatin
Drug class
Platinum analog
45
Oxaliplatin
Mechanism of action
* Alkylating agent but does not form carbonium intermediate
* instead it reacts with water to form a +charged intermediate that reacts with guanine to crosslink DNA
46
Oxaliplatin
Uses
Gastric and colorectal cancers
47
Oxaliplatin
Side effects
* peripheral sensory neuropathy (cold-induced)
* also neutropenia
48
Mechanism of action of antimetabolite drugs
Structural analogs of folic acid or purine/pyrimidine bases of DNA;
Act in S-phase ie are cell-cycle specific
49
Methotrexate
Drug Class
Folate analog
50
Methotrexate
Mechanism of action
* Inhibits dihydrofolate reductase which catalyzes conversion of folate to tetrahydrofolate, which is needed for purine and thymidine synthesis
* given orally or intrathecally
51
Methotrexate
Uses
* Childhood ALL and choriocarcinoma
* combination therapy for Burkitt's lymphoma and carcinomas of breast, ovary, head and neck, and bladder;
* administered intrathecally for meningeal leukemia and meningeal metastases of tumors (can't cross BBB);
* high-dose for osteosarcoma
52
Methotrexate
Side effects
* Renal toxicity (crystallization in urine at high doses)
* hepatotoxicity (longterm, fibrosis/cirrhosis)
* reproductive (defective oogenesis, spermatogenesis, abortion)
* also bone marrow (myelosuppression, spontaneous hemorrhage); GI toxicity (oral ulceration, stomatitis)
* can use leucovorin to prevent toxic side effects, as healthy cells take it up better than tumor cells
53
Permetrexed
Drug Class
Folate analog
54
Permetrexed
Mechanism of action
metabolized to polyglutamate forms that inhibit THF-dependent enzymes (e.g., DHFR, thymidylate synthase (TS))
55
Permetrexed
Uses
* colon cancer
* mesothelioma
* non-small cell lung cancer
* pancreatic cancer
56
5-Fluorouracil
Drug Class
Pyrimidine analog
57
5-Fluorouracil
Mechanism of action
* 5-FU is converted to active metabolites: 5-FdUMP inhibits TS; 5-FdUTP incorporates into RNA & interferes with RNA function; prodrug ribosylated and phophorylated into 5-FdUMP
58
5-Fluorouracil
Uses
* Combination therapy for breast, colorectal, gastric, head and neck, cervical and pancreatic cancer;
* topically for basal cell carcinoma
59
5-Fluorouracil
Side effects
* Hand-foot syndrome (erythema, sensitivity of palms and soles)
* cardiac toxicity (acute chest pains)
* Anorexia and nausea; mucosal ulcerations, stomatitis, diarrhea; thrombocytopenia and anemia
* Leucovorin can potentiate effects of 5-FU; must be given IV (GI toxicity and rapid degradation + metabolism in gut and liver)
60
Cytarabine
Drug Class
Pyrimidine analog
61
Cytarabine
Mechanism of action
Ara-C converted by deoxycytidine kinase to Ara-CMP --\> Ara-CTP; terminates DNA synthesis as Ara-CTP
62
Cytarabine
Uses
* AML (most effective treatment)
* ALL
* blast phase CML
63
Cytarabine
Side effects
* Severe myelosuppression (leucopenia, thrombocytopenia, anemia)
* GI tract toxicity (ulceration, stomatitis, diarrhea)
64
Gemcitabine
Drug Class
Pyrimidine analog
65
Gemcitabine
Mechanism of action
Converted to active metabolites: dFdCDP inhibits ribonucleotide reductase (lowers deoxyribonucleotide); dFdCTP incorporates into DNA, terminating DNA synthesis
66
Gemcitabine
Uses
* Pancreatic cancer
* effective against non-small cell lung cancer, ovarian, bladder, esophageal, and head and neck cancer
* More effective against solid tumors than cytarabine
67
Gemcitabine
Side effects
Myelosuppression (leucopenia, thrombocytopenia, anemia), flu-like symptoms
68
6-Mercaptopurine
Drug Class
Purine analog
69
6-Mercaptopurine
Mechanism of action
* Prodrug metabolized by hypoxanthine-guanine phosphoribosyl transferase (HGPRT) to 6-thioinosinic acid (TIMP);
* TIMP inhibits first step of de novo purine base synthesis and the formation of AMP and xanthinylic acid from inosinic acid, reducing purine levels.
* As well, TIMP is converted to thio-guanine ribonucleotides, inhibiting DNA and RNA synthesis
70
6-Mercaptopurine
Uses
Maintain remission in acute ALL
71
6-Mercaptopurine
Side effects
* Hepatotoxicity in prolonged use
* Bone marrow suppression
* Drug interaction with allopurinol (for gout), which inhibits xanthine oxidase; decrease 6-MP dose to avoid drug accumulation and toxicities
72
Mechanism of action of DNA Intercalating Agents
* Bind DNA through intercalation between specific bases, blocking DNA, RNA or both synthesis; cause DNA strands to break and interfere with cell replication;
* Cell Cycle non-specific
73
Dactinomycin
Mechanism of Action
* intercalates between G-C pairs of DNA, interfering with DNA-dependent RNA polymerase therefore disrupting transcription
* also causes ssDNA breaks
74
Dactinomycin
Uses
* Pediatric tumors (Wilm's tumor, rhabdomyosarcoma, Ewing's sarcoma)
* choriocarcinoma in women
75
Dactinomycin
Side effects
* Hematopoietic suppression with pancytopenia
* also anorexia, nausea, vomiting
76
Mechanism of action of Anthracylines
* Intercalate between DNA base pairs and donate electrons to O2 to form superoxide;
* superoxide reacts with itself to form H2O2 --\> cleaved in the presence of Fe to form OH radical, which cleaves DNA
77
Daunorubicin
Drug Class
Anthracylines
78
Daunorubicin
Mechanism of action
* Intercalate between DNA base pairs and donate electrons to O2 to form superoxide;
* superoxide reacts with itself to form H2O2 --\> cleaved in the presence of Fe to form OH radical, which cleaves DNA
79
Daunorubicin
Uses
AML
80
Daunorubicin
Side Effects
* Irreversible, dose-dependent cardiotoxicity
* alopecia
* also myelosuppression (neutropenia), stomatitis, GI disturbances
* Dexrazoxane is cardio-protective
81
Idarubicin
Drug Class
Anthracylines
82
Idarubicin
Mechanism of action
* Intercalate between DNA base pairs and donate electrons to O2 to form superoxide;
* superoxide reacts with itself to form H2O2 --\> cleaved in the presence of Fe to form OH radical, which cleaves DNA
83
Idarubicin
Uses
AML
84
Idarubicin
Side effects
* Irreversible dose-dependent cardiotoxicity
* alopecia
* also myelosuppression (neutropenia), stomatitis, GI disturbances
* Dexrazoxane is cardio-protective
85
What drug is given with anthracylines to protect against cardiac side effects?
Dexrazoxane
86
Doxorubicin
Drug Class
Anthracylines
87
Doxorubicin
Mechanism of Action
* Intercalate between DNA base pairs and donate electrons to O2 to form superoxide;
* superoxide reacts with itself to form H2O2 --\> cleaved in the presence of Fe to form OH radical, which cleaves DNA
88
Doxorubicin
Uses
* Sarcoma, breast, lung carcinomas
* Malignant lymphomas
89
Doxorubicin
Side effects
* Irreversible dose-dependent cardiotoxicity;
* alopecia
* also myelosuppression (neutropenia), stomatitis, GI disturbances
* Dexrazoxane can be used to prevent cardiotoxic effects
90
Epirubicin
Drug Class
Anthracyclines
91
Epirubicin
Mechanism of action
* Intercalate between DNA base pairs and donate electrons to O2 to form superoxide;
* superoxide reacts with itself to form H2O2 --\> cleaved in the presence of Fe to form OH radical, which cleaves DNA
92
Epirubicin
Uses
* Metastatic breast cancer
* gastric cancer
93
Epirubicin
Side effects
* Irreversible dose-dependent cardiotoxicity;
* alopecia
* Myelosuppression (neutropenia), stomatitis, GI disturbances
* Dexrazoxane can be used to prevent cardiotoxic effects
94
Bleomycin
Mechanism of action
Acts in G2 phase of cell cycle. Binds to DNA, producing ss- and dsDNA breaks
95
Bleomycin
Uses
* Combination therapy for testicular tumors or Hodgkin's disease;
* squamous cell carcinomas and lymphomas
96
Bleomycin
Side effects
* Pulmonary toxicity (pulmonary fibrosis);
* cutaneous toxicity (hyperpigmentation, hyperkeratosis, erythema);
* hyperthermia
* also minimally myelo- and immunosuppressive (often used in combo therapy); headache, nausea, vomiting
97
Mechanism of action of microtubule inhibitors
* Inhibit mitosis and cause metaphase arrest by interfering with microtubule function (tubulin (de)polymerization);
* Cell-cycle specific
98
Vinblastine
Drug Class
Vinca alkaloids
99
Vinblastine
Mechanism of action
Block tubulin polymerization into microtubules
100
Vinblastine
Uses
* Metastatic testicular tumors (with bleomycin, cisplatin);
* component of ABVD used for Hodgkin's disease
101
Vinblastine
Side effects
Myelosuppression, nausea, vomiting
102
Vincristine
Drug Class
Vinca alkaloids
103
Vincristine
Mechanism of Action
Block tubulin polymerization into microtubules
104
Vincristine
Uses
Childhood ALL (with glucocorticoids); Hodgkin's and non-Hodgkin's lymphomas
105
Vincristine
Side effects
* Dose-limiting neurotoxicity (peripheral neuropathy)
* Relatively low bone marrow toxicity
106
Paclitaxel
Drug Class
Taxanes
107
Paclitaxel
Mechanism of action
Block microtubule depolymerization into tubulin
108
Paclitaxel
Uses
Metastatic breast, ovarian, lung, and head and neck cancers
109
Paclitaxel
Side effects
* Peripheral neuropathy
* Neutropenia
* hypersensitivity reactions
110
Docetaxel
Drug Class
Taxanes
111
Docetaxel
Uses
* Metastatic breast, ovarian, lung, and head and neck cancers;
* hormone refractory prostate cancer
112
Docetaxel
Side effects
* peripheral neuropathy
* Neutropenia
* hypersensitivity reactions
113
Mechanism of Topoisomerase Inhibitors
* Prevent the resealing of topo I (ssDNA) and topo II (dsDNA);
* Cell-cycle specific
114
Etoposide
Drug Class
Epipodophyllotoxins
115
Etoposide
Mechanism of action
Inhibits topoisomerase II
116
Etoposide
Uses
Testicular carcinoma, lung cancer, and non-Hodgkin's lymphoma
117
Etoposide
Side effects
* Dose-limiting myelosuppression (neutropenia)
* oral mucositis
118
Teniposide
Drug Class
Epipodophyllotoxins
119
Teniposide
Mechanism of action
Inhibits topoisomerase II
120
Teniposide
Uses
ALL
121
Teniposide
Side effects
Dose-limiting myelosuppression (neutropenia), oral mucositis
122
Irinotecan
Drug Class
Camptothecin analogs
123
Irinotecan
Mechanism of action
Inhibits Topoisomerase I
124
Irinotecan
Uses
* Advanced colorectal cancer;
* lung, ovarian, cervical and brain tumors
125
Irinotecan
Side effects
Severe neutropenia, severe diarrhea
126
Topotecan
Drug Class
Camptothecin analogs
127
Topotecan
Mechanism of action
Inhibits topoisomerase I
128
Topotecan
Uses
Ovarian and small cell lung cancer
129
Topotecan
Side effects
Severe neutropenia, severe diarrhea
130
Docetaxel
Mechanism of action
Block microtubule depolymerization into tubulin
131
Glucocorticoid Use and mechanism in cancer
* Particularly useful for tx of lymphocytic leukemias and lymphomas
* inhibit mitosis in lymphocytes
* do not induce myelosuppression
132
Prednisone
Drug Class
Glucocorticoids
133
Prednisone
Mechanism of action
* inhibit mitosis in lymphocytes
134
Prednisone
Uses
* ALL
* MOPP and CHOP combination for Hodgkin's, non-Hodkin's
* multiple myeloma, and CLL
135
Dexamethasone
Drug Class
Glucocorticoids
136
Dexamethasone
Mechanism of action
inhibit mitosis in lymphocytes
137
Dexamethasone
Uses
Reduces edema in brain and spinal cord tumors in conjunction with radiation therapy
138
Tamoxifen
Drug Class
Selective estrogen-receptor modulators (SERMs)
139
Tamoxifen
Mechanism of action
Competes with estradiol for binding to estrogen receptor
140
Tamoxifen
Uses
* ER-positive breast cancer
* or as adjuvant therapy following primary breast tumor excision
* prevention of breast cancer in high-risk patients
141
Tamoxifen
Side effects
* Hot flushes, hair loss; increased risk of endometrial cancer; increased risk of thromboembolic events
* also nausea and vomiting
142
Mechanism of action of Selected Estrogen Receptor Downregulators (SERDS)
* completely anti-estrogenic
* ie have no estrogen agonist activity
143
Fulvestrant
Drug Class
Selective Estrogen-Receptor Downregulator
144
Fulvestrant
Mechanism of action
Binds with much higher affinity (\>100-fold) to estrogen receptor than tamoxifen, inhibiting dimerization, increasing degradation, and reducing overall ER levels
145
Fulvestrant
Uses
Posmenopausal women with ER-positive metastatic breast cancer
146
List of aromatase inhibitors
* Aminoglutethamide
* Anastrozole
* Letrozole
* Exemestane
147
Aminoglutethamide
Drug Class
Aromatase inhibitors
148
Aminoglutethamide
Mechanism of action
Inhibits function of aromatase
149
Aminoglutethamide
Uses
Relatively weak, used against breast cancer
150
Anastrozole
Drug Class
* Aromatase inhibitor
* 3rd generation
* nonsteroidal
151
Anastrozole
Uses
First-line for ER-positive breast cancer in postmenopausal women
152
Letrozole
Drug Class
* aromatase inhibitor
* 3rd generation
* nonsteroidal
153
Letrozole
Uses
ER-positive breast cancer in postmenopausal women
154
Exemestane
Drug class
* aromatase inhibitor
* 3rd generation
* steroidal
155
Exemestane
Mechanism of action
Steroidal inhibitor of aromatase
156
Anastrozole
Mechanism of action
Inhibits function of aromatase
157
Letrozole
Mechanism of action
Inhibits function of aromatase
158
Leuprolide
Drug Class
GnRH analog
159
Leuprolide
Mechanism of action
Binds GnRH receptor; inhibits release of FSH & LH
160
Leuprolide
Uses
* Androgen ablation therapy, along with AR blockers
* for prostate cancer
161
Goserelin
Drug Class
GnRH analogs
162
Goserelin
Mechanism of action
Binds GnRH receptor; inhibits release of FSH & LH
163
Goserelin
Uses
* Androgen ablation therapy, along with AR blockers
* for prostate cancer
164
Flutamide
Drug class
Nonsteroidal androgen-receptor blockers
165
Flutamide
Mechanism of action
Competes with androgen for AR binding and prevent receptor translocation to nucleus
166
Flutamide
Uses
* Androgen ablation therapy, along with GnRH analogs
* for prostate cancer
167
Bicalutamide
Drug Class
Nonsteroidal androgen-receptor blockers
168
Bicalutamide
Mechanism of action
Competes with androgen for AR binding and prevent receptor translocation to nucleus
169
Bicalutamide
Uses
* Androgen ablation therapy, along with GnRH analogs
* for prostate cancer
170
Hydroxyurea
Mechanism of action
Inhibits ribonucleoside diphosphate reductase so cannot convert ribonucleotides to deoxyribonucleotides --\> inhibit DNA synthesis
171
Hydroxyurea
Uses
* CML (replaced by Imatinib),
* polycythemia vera, essential thrombocythemia
* treatment for sickle cell disease (increases Hb-F)
172
Retinoids
Mechanism of action
All trans retinoic acid (ATRA) induces terminal differentiation in malignant immature promyelocytes, which subsequently apoptose
173
Retinoids
Uses
APL
174
Arsenic Trioxide
Uses
heavy metal toxin used for tx of relapsed APL
175
Thalidomide
Uses
Multiple myeloma and myelodysplastic syndromes
176
Interferons
Hairy-cell leukemia, CML, and AIDS-related Kaposi's sarcoma (interferon alpha)
177
Imatinib
Drug class
Tyrosine Kinase Inhibitor
178
Imatinib
Mechanism of action
Inhibits Abl kinase by binding where ATP should go; also inhibits PDGFR and c-kit; metabolized by cytochrome P450
179
Imatinib
Uses
* First line therapy for CML
* also, gastrointestinal tumor (GIST)
180
Imatinib
Side effects
* Nausea and vomiting, fluid retention, muscle cramps, arthralgia
* Myelosuppression
181
Gefitinib
Drug Class
Tyrosine Kinase inhibitor
182
Gefitinib
Uses
Non-small lung cancer
183
Gefitinib
Side effects
* Interstitial lung disease, liver damage, GI perforation, severe diarrhea, ocular disorders Skin reactions (rash, acne, pruritis, dry skin)
* Skin reactions (rash, acne, pruritis, dry skin)
184
Erlotinib
Drug Class
Tyrosine Kinase inhibitor
185
Erlotinib
Mechanism of action
Inhibit epidermal growth factor receptor (EGFR) tyrosine kinase
186
Erlotinib
Uses
Non-small lung cancer; pancreatic cancer
187
Erlotinib
Side effects
* Rash, diarrhea, appetite loss, N & V, stomach pain, fatigue, shortness of breath, mouth sores, dry skin, itching, cough
* Liver or renal failure, interstitial lung disease, increased bleeding or clot formation, GI perforation, corneal ulceration or perforation
188
Rituximab
Drug class
Monoclonal antibody
189
Rituximab
Mechanism of action
CD20 B-cell antibody that can directly activate apoptosis, activate complement, or activate cell-mediated cytotoxicity (e.g., T cells, NK cells)
190
Rituximab
Uses
Non-Hodgkin's lymphomas
191
Rituximab
side effects
* Infusion reactions, tumor lysis syndrome (TLS), severe mucocutaneous reactions, progressive multifocal leukoencephalopathy (PML)
* Skin reactions, irregular heartbeat, muscle or joint pain
192
Trastuzumab
Drug Class
Monoclonal antibody
193
Trastuzumab
Mechanism of action
Unknown HER2/neu (ErbB2) receptor antibody mechanism (enhanced receptor endocytosis or blocking homo- or heterodimerization)
194
Trastuzumab
Uses
* HER2/neu-overexpressing metastatic breast cancer
* Usually combined with paclitaxel or doxorubicin;
195
Trastuzumab
Side effects
* Hypersentivity reaction; ventricular dysfunction
* enhances doxorubicin cardiotoxicity
196
Indomethacin
Drug Class
non-selective NSAID
197
Indomethacin
Mechanism of action
Eliminate pain; reduce inflammation (but does not slow disease progression)
198
Indomethacin
Uses
* Rheumatoid arthritis
* acute gouty arthritis
199
Indomethacin
Side effects
Gastric and duodenal ulcers
200
Naproxen
Drug Class
non-selective NSAID
201
Naproxen
Mechanism of action
Eliminate pain; reduce inflammation (but does not slow disease progression)
202
Naproxen
Uses
* Rheumatoid arthritis
* acute gouty arthritis
203
Naproxen
Side effects
Gastric and duodenal ulcers
204
COX-2 inhibitors
Drug class
Selective NSAID
205
COX-2 inhibitor
Mechanism
Eliminate pain; reduce inflammation (but does not slow disease progression)
206
COX-2 inhibitor
Uses
Superseding conventional NSAIDs for rheumatoid arthritis
207
COX-2 inhibitor
Side effects
50% fewer gastric and duodenal ulcers than traditional NSAIDs
208
Disease modifying anti-rheumatic drugs (DMARD)
Mechanism
drugs that retard or halt the progression of the disease
209
Quinolones (chloroquine and hydroxychloroquine)
Drug class
DMARD (antimalarial)
210
Quinolones (chloroquine and hydroxychloroquine)
Mechanism
Reduces T-cell activation & chemotaxis
211
Quinolones (chloroquine and hydroxychloroquine)
Uses
* Rheumatoid arthritis, SLE
* Used for patients who no longer respond to NSAIDS or can't tolerate other DMARDs
212
Quinolones (chloroquine and hydroxychloroquine)
Side effects
Retinal damage (chloroquine)
213
Glucocorticoids
Drug class
DMARD
214
Glucocorticoids
Mechanism of action
1. Inhibits phospholipase A2 (inhibiting release of arachidonic acid and, thus, formation of prostaglandins)
2. Inhibits cytokine production (which prevents induction of COX-2)
215
Glucocorticoids
Uses
* Rheumatoid arthritis; acute gouty arthritis (intraarticular injection for relief of acute monoarticular gout)
* Started initially (fast acting) before other drugs become effective
Can give orally or intra-articularly
216
Glucocorticoids
Side effects
Cushingoid symptoms
217
Sulfasalazine
Drug class
DMARD
218
Sulfazalazine
Mechanism of action
* Likely inhibition of IL-1 & TNF-alpha release
* Acts more quickly than other drugs
219
Sulfasalazine
Uses
Rheumatoid arthritis
220
Sulfasalazine
Side effects
N/V, skin rashes, neutropenia (30% of patient discontinue drug)
Headaches
221
Methotrexate
Drug class (RA)
DMARD (immunosuppressant)
222
Methotrexate (RA)
Mechanism of action
1. Inhibition of aminoimidazolecarboxamide (AICAR) transformylase and
thymidylate synthetase, with secondary effects on PMN chemotaxis
2. Causes adenosine accumulation, which inhibits inflammation
* Takes several weeks to start working; "gold standard" of therapy
223
Methotrexate (RA)
Uses
Rheumatoid Arthritis
224
Methotrexate (RA)
Side effects
Nausea, stomatitis, hepatotoxicity (rare)
225
Leflunomide
Drug Class
DMARD
| (Immunosuppressive)
226
Leflunomide
Mechanism
* Inhibits dihydroorotate dehydrogenase (DHODH), which inhibits T-lymphocyte response to stimuli
* Takes several weeks to start working; oral prodrug
227
Leflunomide
Uses
Rheumatoid arthritis
228
Leflunomide
Side effects
Diarrhea, hepatotoxity
229
Biological Response Modifiers
Mechanism
interfere with cytokine signalling in inflammation
230
Etanercept
Drug Class
Biologic Response Modifiers
231
Etanercept
Mechanism of action
Blocks binding of TNF to TNF receptors
232
Etanercept
Uses
Rheumatoid arthritis
233
Infliximab
Drug class
biological response modifiers
234
Infliximab
Mechanism of action
Blocks binding of TNF to TNF receptors
235
Infliximab
Uses
Rheumatoid arthritis
236
Infliximab
Side effects
Antigenic response to murine monoclonal Ab
237
Adalimumab
Drug Class
biological response modifiers
238
Adalimumab
Mechanism of action
Blocks binding of TNF to TNF receptors
239
Adalimumab
Uses
Rheumatoid arthritis
240
Golimumab
Drug class
Biological response modifiers
241
Golimumab
Mechanism of action
Blocks binding of TNF to TNF receptors
242
Golimumab
Uses
Rheumatoid arthritis
243
Golimumab
Side effects
Risk of serious infections
244
Certolizumab
Drug class
Biologic Response Modifiers
245
Certolizumab
Mechanism of action
* Blocks binding of TNF to TNF receptors
* Conjugated to PEG for stabilization
246
Certolizumab
Uses
Rheumatoid arthritis
247
Certolizumab
Side effects
risk of serious infections
248
Anakinra
Drug class
Biologic Response Modifiers
249
Anakinra
Mechanism of action
* IL-1 Receptor Antagonist
* Short (6 hr) plasma half-life; daily treatment with high doses
250
Anakinra
Uses
Rheumatoid arthritis
251
Tocilizumab
Drug Class
Biologic Response Modifiers
252
Tocilizumab
Mechanism of action
IL-6 Receptor Antagonist
253
Tocilizumab
Uses
Rheumatoid Arthritis
254
Tocilizumab
Side effects
serious infections eg Tb, fungal, viral, other opportunistic
255
Abatacept
Drug class
Biologic Response Modifiers
256
Abatacept
Mechanism of action
Inhibits T-cell activation and induces T-cell apoptosis
257
Abatacept
Uses
Rheumatoid arthritis
258
Abatacept
Side effects
Headaches; infections
259
Rituximab
Drug class
Biological response modifiers
260
Rituximab
Mechanism of action
Anti-CD20 mAb, reduces circulating B cells
261
Rituximab
Uses
* Rheumatoid arthritis
* Used for RA refractory to TNF-alpha inhibitors
262
Rituximab
Side effects
Infections; hypersensitivity reactions
263
Tofacitinib
Drug class
biological response modifiers
264
Tofacitinib
Mechanism of action
Inhibition of JAK 1 & 3 which inhibits production of inflammatory mediators
265
Tofacitinib
Uses
Rheumatoid arthritis
266
Tofacitinib
Side effects
Upper respiratory tract infections; headaches, diarrhea
Malignancies
267
Treatment of acute gout: drug and mechanism
NSAIDs
eicosanoid mediated pain and inflammation
for initial tx of acute gout
268
Colchicine
Mechanism
* Prevents tubulin polymerization & leads to inibition of leukocyte migration, phagocytosis, and release of cytokines
* Works in 12-24 hours!
269
Colchicine
Uses
Acute gouty arthritis
270
Colchicine
Side Effects
* Low Therapeutic index
* Long-term use causes peripheral neuropathy & neutropenia
* Nausea, vomiting, abdominal pain, troublesome diarrhea
271
Probenecid
Drug class
Uricosuric agents
272
Probenecid
Mechanism
Compete with urate at the anionic transport site of the renal tubule and inhibit urate reabsorption
273
Probenecid
Uses
Chronic tophaceous gout
274
Probenecid
Side effects
Urate crystal mobilization and acute gouty arthritis
Gastrointestinal irritation
Secretion of some weak acids (e.g., penicillin) is reduced
275
Allopurinol
Mechanism
1. Reduces uric acid synthesis by inhibiting xanthine oxidase (competitive inhibition) --\> alloxanthine
2. Alloxanthine is a non-competitive inhibitor of xanthine oxidase
276
Allopurinol
Uses
Chronic tophaceous gout
277
Allopurinol
Side effects
Acute attacks of gouty arthritis early in treatment due to mobilization of urate crystals
278
Febuxostat
Mechanism
Non-purine, non-competitive antagonist of xanthine oxidase
279
Febuxostat
Uses
Chronic tophaceous gout
280
Febuxostat
Side effects
Nausea, rash, arthralgias
| (also expensive)
281
Pegloticase
Drug Class
Recombinant, stabilized uricase
282
Pegloticase
Mechanism
Converts uric acid to allantoin
283
Pegloticase
Uses
Chronic tophaceous gout
use when refractory to other therapies
284
Estradiol (valerate & cypionate)
Drug class
Estradiol esters (steroidal)
285
Estradiol (valerate & cypionate)
Mechanism
Absorbed through skin, mucus membranes, GI Tract; body-wide distribution via sex-hormone binding globulin
286
Estradiol (valerate & cypionate)
Uses
Contraception, primary hypogonadism, postmenopausal hormone therapy, osteoporosis
287
Estradiol (valerate & cypionate)
Side effects
* Weight gain, HTN; less commonly, may cause breast cancer, increased risk of heart attack & stroke, DVT, cervical and endometrial cancer
* Nausea, breast tension/pain, vaginal bleeding, headache
* Strongly contraindicated in breast or endometrial cancers, endometriosis, undiagnosed vaginal bleeds; relatively contradinicated in pregnancy, thromboembolic disease, HTN, hepatic disease, family history of breast or uterine cancer
288
Estrone sulfate
Drug class
Estradiol esters (steroidal)
conjugated
289
Estrone sulfate
Mechanism
Absorbed through skin, mucus membranes, GI Tract; body-wide distribution via sex-hormone binding globulin
290
Estrone sulfate
Uses
Contraception, primary hypogonadism, postmenopausal hormone therapy, osteopososis
291
Estrone sulfate
Side effects
* Weight gain, HTN; less commonly, may cause breast cancer, increased risk of heart attack & stroke, DVT, cervical and endometrial cancer
* Nausea, breast tension/pain, vaginal bleeding, headache
* Strongly contraindicated in breast or endometrial cancers, endometriosis, undiagnosed vaginal bleeds; relatively contradinicated in pregnancy, thromboembolic disease, HTN, hepatic disease, family history of breast or uterine cancer
292
Equilin sulfate
drug class
Estradiol esters (steroidal)
conjugated
293
Equilin sulfate
Mechanism
Absorbed through skin, mucus membranes, GI Tract; body-wide distribution via sex-hormone binding globulin
294
Equilin sulfate
Uses
Contraception, primary hypogonadism, postmenopausal hormone therapy, osteoporosis
295
Equilin sulfate
Side effects
* Weight gain, HTN; less commonly, may cause breast cancer, increased risk of hear attack & stroke, DVT, cervical and endometrial cancer
* Nausea, breast tension/pain, vaginal bleeding, headache
* Strongly contraindicated in breast or endometrial cancers, endometriosis, undiagnosed vaginal bleeds; relatively contradinicated in pregnancy, thromboembolic disease, HTN, hepatic disease, family history of breast or uterine cancer
296
Ethinyl estradiol
Drug class
alkyl estrogen
297
Ethinyl estradiol
Mechanism
Absorbed through skin, mucus membranes, GI Tract; body-wide distribution via sex-hormone binding globulin
298
Ethinyl estradiol
Uses
Contraception, primary hypogonadism, postmenopausal hormone therapy, osteoporosis
299
Ethinyl Estradiol
Side effects
* Weight gain, HTN; less commonly, may cause breast cancer, increased risk of heart attack & strokeDVT, cervical and endometrial cancer
* Nausea, breast tension/pain, vaginal bleeding, headache
* Strongly contraindicated in breast or endometrial cancers, endometriosis, undiagnosed vaginal bleeds; relatively contradinicated in pregnancy, thromboembolic disease, HTN, hepatic disease, family history of breast or uterine cancer
300
Mestranol
Drug class
Alkyl estrogen
301
Mestranol
Mechanism
Absorbed through skin, mucus membranes, GI Tract; body-wide distribution via sex-hormone binding globulin
302
Mestranol
Uses
Contraception, primary hypogonadism, postmenopausal hormone therapy
303
Mestranol
Side effects
* Weight gain, HTN; less commonly, may cause breast cancer, DVT, cervical and endometrial cancer
* Nausea, breast tension/pain, vaginal bleeding, headache
* Strongly contraindicated in breast or endometrial cancers, endometriosis, undiagnosed vaginal bleeds; relatively contradinicated in pregnancy, thromboembolic disease, HTN, hepatic disease, family history of breast or uterine cancer
304
Quinestrol
Drug Class
Estradiol esters (steroidal)
305
Quinestrol
Mechanism
Absorbed through skin, mucus membranes, GI Tract; body-wide distribution via sex-hormone binding globulin
306
Quinestrol
Uses
Contraception, primary hypogonadism, postmenopausal hormone therapy, osteoporosis
307
Quinestrol
Side effects
* Weight gain, HTN; less commonly, may cause breast cancer, increased risk of heart attack & stroke, DVT, cervical and endometrial cancer
* Nausea, breast tension/pain, vaginal bleeding, headache
* Strongly contraindicated in breast or endometrial cancers, endometriosis, undiagnosed vaginal bleeds; relatively contradinicated in pregnancy, thromboembolic disease, HTN, hepatic disease, family history of breast or uterine cancer
308
Diethylstilbestrol
Drug Class
Non-steroidal synthetic estrogen
309
Diethylstilbestrol
Side effects
Increased risk of clear cell adenocarcinoma of vagina & cervix
310
Tamoxifen citrate
Drug Class
Non-steroidal anti-estrogen; selective estrogen receptor modifier
311
Tamoxifen citrate
Mechanism
Blocks estrogen from binding ER and causing growth in ER(+) breast cancer
312
Tamoxifen citrate
Uses
ER(+) breast cancer
313
Tamoxifen citrate
side effects
* Pro-estrogenic effect on uterine epithelium (increase risk of endometrial cancer); partial estrogen agonist in bone and endometrium
* Anti-estrogenic effect on mammary epithelium; must be used in very high doses
314
Clomiphene citrate
Drug class
Non-steroidal anti-estrogen
315
Clomiphene citrate
Mechanism
* Blocks estrogen binding to hypothalamic receptors (no estradiol negative feedback on gonadotropins) --\> increased secretion of gonadotropins & LH --\> ovulation
* Cis-isomer (zuclomiphene) is a weak estrogen agonist; trans-isomer (enclomiphene) is a potent estrogen antagonist
316
Clomiphene citrate
Uses
Stimulate ovulation in patients who want to get pregnant
317
Clomiphene citrate
Side effects
* Stomach pain, headache, upset stomach, vomit
318
Micronized progesterone
Drug class
Natural progesterone
319
Micronized progesterone
Mechanism
Binds to PR; decreased first-pass metabolism & enhanced dissolution due to micronization
320
Micronized progesterone
Uses
Contraception, hormone replacement therapy
321
Micronized progesterone
Side effects
* Fatigue, drowsiness
* Contraindicated in thromboembolic disorders or patients with such a history, liver disease (metabolised in the liver), undiagnosed vaginal bleeding, pregnancy (atrophy of endometrium leading to birth defects)
322
Transvaginal progesterone
Drug Class
Natural progesterone
323
Transvaginal progesterone
Mechanism
Binds to PR; vaginal gel (uterine effects without first pass metabolism and minimal systemic side effects)
324
Transvaginal progesterone
Uses
Contraception, hormone replacement therapy
325
Transvaginal progesterone
Side effects
* Fatigue, drowsiness
* Contraindicated in thromboembolic disorders or patients with such a history, liver disease (metabolised in the liver), undiagnosed vaginal bleeding, pregnancy (atrophy of endometrium leading to birth defects)
326
Medroxyprogesterone
Drug class
Synthetic progesterone
327
Medroxyprogesterone
Uses
Contraception, hormone replacement therapy
328
Medroxyprogesterone
Side effects
* Edema, abdominal bloating; less commonly: strong androgenic effects (hirsutism, acne)
* Anxiety, irritability, depression, muscular pain; increased risk of thrombus and PE
* Contraindicated in thromboembolic disorders or patients with such a history, liver disease (metabolised in the liver), undiagnosed vaginal bleeding, pregnancy (atrophy of endometrium leading to birth defects)
329
Norethindrone
Drug class
Synthetic progesterone
330
Norethindrone
Uses
Contraception, hormone replacement therapy
331
Norethindrone
Side effects
* Edema, abdominal bloating; less commonly: strong androgenic effects (hirsutism, acne)
* Anxiety, irritability, depression, muscular pain; increased risk of thrombus and PE
* Contraindicated in thromboembolic disorders or patients with such a history, liver disease (metabolised in the liver), undiagnosed vaginal bleeding, pregnancy (atrophy of endometrium leading to birth defects)
332
Norgestrol
Drug class
Synthetic progesterone
333
Norgestrol
Uses
Contraception, hormone replacement therapy
334
Norgestrol
Side effects
* Edema, abdominal bloating; less commonly: strong androgenic effects (hirsutism, acne)
* Anxiety, irritability, depression, muscular pain; increased risk of thrombus and PE
* Contraindicated in thromboembolic disorders or patients with such a history, liver disease (metabolised in the liver), undiagnosed vaginal bleeding, pregnancy (atrophy of endometrium leading to birth defects)
335
Megestrol
Drug Class
Synthetic progesterone
336
Megestrol
Uses
Contraception, hormone replacement therapy
337
Megestrol
Side effects
* Edema, abdominal bloating; less commonly: strong androgenic effects (hirsutism, acne)
* Anxiety, irritability, depression, muscular pain; increased risk of thrombus and PE
* Contraindicated in thromboembolic disorders or patients with such a history, liver disease (metabolised in the liver), undiagnosed vaginal bleeding, pregnancy (atrophy of endometrium leading to birth defects)
338
Monophasic Ortho-Novum
Drug class
Combination pill
339
Monophasic Ortho-Novum
Mechanism
* Constant level of estrogen suppresses FSH, LH surge; progesterone suppresses LH surge, thickens cervical mucus, leads to endometrial atrophy, counters estrogenic effect on endometrium (reduces risk of endometrial cancer)
* Consistent dose of estrogen and progestin (only take 21 days)
340
Monophasic Ortho-Novum
Use
Contraception
341
Monophasic Ortho-Novum
Side effects
* Edema, abdominal bloating; less commonly: strong androgenic effects (hirsutism, acne)
* Anxiety, irritability, depression, muscular pain; increased risk of thrombus and PE
* Contraindicated in thromboembolic disorders or patients with such a history, liver disease (metabolised in the liver), undiagnosed vaginal bleeding, pregnancy (atrophy of endometrium leading to birth defects)
342
Biphasic Ortho-Novum
Drug class
* Combination pill
* Fixed estrogen, progestin increased for days 11-21
343
Biphasic Ortho-Novum
Mechanism
Constant level of estrogen suppresses FSH, LH surge; progesterone suppresses LH surge, thickens cervical mucus, leads to endometrial atrophy, counters estrogenic effect on endometrium (reduces risk of endometrial cancer)
344
Biphasic Ortho-Novum
Uses
Contraception
345
Biphasic Ortho-Novum
Side effects
* Edema, abdominal bloating; less commonly: strong androgenic effects (hirsutism, acne)
* Anxiety, irritability, depression, muscular pain; increased risk of thrombus and PE
* Contraindicated in thromboembolic disorders or patients with such a history, liver disease (metabolised in the liver), undiagnosed vaginal bleeding, pregnancy (atrophy of endometrium leading to birth defects)
346
Triphasic Ortho-Novum
Class
* Combination pill
* Fixed or variable estrogen, while progestin increases in 3 phases (1-7, 8-14, 15-21)
347
Triphasic Ortho-Novum
Mechanism
Constant level of estrogen suppresses FSH, LH surge; progesterone suppresses LH surge, thickens cervical mucus, leads to endometrial atrophy, counters estrogenic effect on endometrium (reduces risk of endometrial cancer)
348
Triphasic Ortho-Novum
Uses
Contraception
349
Triphasic Ortho-Novum
Side effects
* Edema, abdominal bloating; less commonly: strong androgenic effects (hirsutism, acne)
* Anxiety, irritability, depression, muscular pain; increased risk of thrombus and PE
* Contraindicated in thromboembolic disorders or patients with such a history, liver disease (metabolised in the liver), undiagnosed vaginal bleeding, pregnancy (atrophy of endometrium leading to birth defects)
350
Mini-pill
Drug class
Progestin only
351
Mini-pill
Uses
Less effective than combination pill for contraception; use when patient has estrogen contraindication; good in lactating women (estrogen reduces milk production)
352
Mini-pill
Side effects
* More likely to produce irregular menstrual cycle (estrogen required to provide stability to endometrium)
* also suppresses endometrial cancer
353
Levonorgestrel (Plan B)
Drug class
Synthetic progestogen
354
Levonorgestrel (Plan B)
Mechanism
* Unknown
* but must be taken within 72 hours of coitus
355
Levonorgestrel (Plan B)
Uses
Prevent implantation
356
Levonorgestrel (Plan B)
Side effects
Likely the same as combination oral contraceptives
357
Mifepristone
Drug class
Anti-progestin; glucocorticoid receptor antagonist
358
Mifepristone (RU-486, Korlym)
Mechanism
Competitively binds to progesterone receptor (leading to detachment of fetus); glucocorticoid recepter antagonist
359
Mifepristone (RU-486, Korlym)
Uses
* Abortion; Cushing's Syndrome
* Must take early in pregnancy (by day 49); oral administration; must be given by doctor in medical facility prepared for surgery if abortion incomplete
360
Sildenafil citrate (Viagra)
Drug class
PDE5 inhibitor
361
Sildenafil citrate (Viagra)
Mechanism
Bind catalytic site of PDE5; inhibits PDE5 breakdown of cGMP --\> decreased Ca++ --\> smooth muscle relaxation --\> erection
362
Sildenafil citrate (Viagra)
Uses
Erectile dysfunction; does not trigger an automatic erection, but improves response to sexual stimulation;
363
Sildenafil citrate (Viagra)
Side effects
* Headache, dizziness, change in vision (NAION)
* Flushing, upset stomach, stuffy or runny nose, UTI, diarrhea
* Oral (once/day max); half-life of 4 hours, peak plasma concentration in 1-2 hours; contraindicated if on nitrates or α-blockers (unsafe drop in BP)
364
Vardenafil HCl (Levitra)
Drug class
PDE5 inhibitor
365
Vardenafil HCl (Levitra)
Mechanism
Bind catalytic site of PDE5; inhibits PDE5 breakdown of cGMP --\> decreased Ca++ --\> smooth muscle relaxation --\> erection
366
Vardenafil HCl (Levitra)
Uses
Erectile dysfunction; does not trigger an automatic erection, but improves response to sexual stimulation;
367
Vardenafil HCl (Levitra)
Side effects
* Headache, dizziness, change in vision (NAION)
* Flushing, upset stomach, stuffy or runny nose, UTI, diarrhea
* Oral (once/day max); half-life of 4 hours, peak plasma concentration in 1-2 hours; contraindicated if on nitrates or α-blockers (unsafe drop in BP)
368
Tadalafil (Cialis)
Drug class
PDE5 inhibitor
369
Tadalafil (Cialis)
Mechanism
Bind catalytic site of PDE5; inhibits PDE5 breakdown of cGMP --\> decreased Ca++ --\> smooth muscle relaxation --\> erection
370
Tadalafil (Cialis)
Uses
Erectile dysfunction; does not trigger an automatic erection, but improves response to sexual stimulation;
371
Tadalafil (Cialis)
Side effects
* Headache, dizziness, change in vision (NAION)
* Flushing, upset stomach, stuffy or runny nose, UTI, diarrhea
* Oral (once/day max); half-life of 17.5 hours, peak plasma concentration in 1-2 hours; contraindicate if on nitrates or α-blockers (unsafe drop in BP)
372
Nilotinib
Drug Class
Tyrosine kinase inhibitor
373
Nilotinib
Mechanism
Inhibits Abl kinase
374
Nilotinib
Uses
Imatinib-resistant CML
375
Nilotinib
Side effects
* Myelosuppression
* also QT prolongation, hepatotoxicity, electrolyte abnormalities
376
Dasatinib
Drug Class
Tyrosine Kinase Inhibitor
377
Dasatinib
Mechanism
inhibits Abl and Src kinases
378
Dasatinib
Uses
Imatinib-resistant CML
379
Dasatinib
Side effects
* Myelosuppression, bleeding, fluid retention, pulmonary arterial hypertension
* also diarrhea, nausea and vomiting, weakness, infections
380
Vemurafinib
Drug Class
Serine/threonine kinase inhibitor
381
Vemurafinib
Mechanism
Inhibits oncogenic BRAF kinase
382
Vemurafinib
Uses
* Unresectable Stage III and IV or metastatic melanomas w/BRAF mutations
* trial found it works better than dacarbazine
383
Vemurafinib
Side effects
* Arthralgia, fatigue, photosensitivity, nausea, alopecia, diarrhea, QT prolongation (increased risk of ventricular arrythmias)
* new primary cutaneous melanoma
384
Dabrafenib
Drug Class
Serine/threonine kinase inhibitor
385
Dabrafenib
Mechanism
Inhibits oncogenic BRAF kinase
386
Dafrabenib
Uses
Unresectable Stage III and IV or metastatic melanomas w/BRAF mutations
387
Dabrafenib
Side effects
* Serious febrile drug reactions, uveitis and iritis, hyperglycemia, hyperkeratosis
* High risk of cutaneous squamous cell carcinoma, keratoacanthoma, new primary cutaneous melanoma
* May cause male infertility
388
Trametinib
Drug class
Dual specificity kinase
389
Trametinib
Uses
Unresectable Stage III and IV or metastatic melanomas w/BRAF mutations
390
Trametinib
Side effects
* Cardiomyopathy, retinal disorders, interstitial lung disease, serious skin toxicities
* Rash, diarrhea, stomatitis, hypertension, pruritis
* May cause female infertility
391
Ipilimumab
Drug class
Human monoclonal antibody
392
Ipilimumab
Mechanism
Cytotoxic T-Lymphocyte Antigen 4 inhibitor; stimulates immune system
393
Ipilimumab
Uses
Melanoma
394
Interleukin-2 use in chemotherapy
binds IL-2 receptor on lymphocytes and modulates immune system;
used in immunotherapy for melanoma
395
Gefitinib
Mechanism
Inhibit epidermal growth factor receptor (EGFR) tyrosine kinase
396
Afatinib
Drug Class
Tyrosine Kinase inhibitor
397
Afatinib
Mechanism
Inhibit EGFR tyrosine kinase
398
Afatinib
Uses
Non-small cell lung cancer
399
Afatinib
Side effects
* Diarrhea, vomiting, rash/dermatitis acneiform, stomatitis, paronichia, dry skin, pruritis, decreased appetite
* Dyspnea, fatigue, pulmonary toxicity, pneumonia, sepsis
400
Lapatinib
Drug class
Tyrosine kinase inhibitor
401
Lapatinib
Mechanism
Inhibits EGFR and ErbB2 (HER2) tyrosine kinase
402
Lapatinib
Uses
Advanced or metastatic breast cancer over-expressing HER2; hormone (+) metastatic breast cancer over expressing HER2 receptor in post menopausal women
403
Lapatinib
Side effects
* Hepatotoxicity, nausea, diarrhea, fatigue, rashes, QT-prolongation
* Decreased left ventricular function when combined with capecitabine, hypokalemia, hypomagnesemia
404
Ado-trastuzumab emtansine
Drug class
Antibody-drug conjugate
405
Ado-trastuzumab emtansine
Mechanism
Conjugate undergoes receptor-dependent internalization & drug released inside cell
406
Ado-trastuzumab emtansine
Uses
ErbB2 (HER2) positive metastatic breast cancer patients with prior treatment history of trastuzumab and/or taxane
407
Ado-trastuzumab emtansine
Side effects
Fatigue, nausea, musculoskeletal pain, thrombocytopenia, headache, hypokalemia, peripheral neuropathy, _ventricular dysfunction_, interstitial lung disease
Interstitial lung disease, infusion-associated reactions, _hepatotoxicity_, birth defects
408
Cetuximab
Drug class
monoclonal antibody
409
Cetuximab
Mechanism
competitively inhibits EGFR (ERB1) tyrosine kinase
410
Cetuximab
Uses
* EGFR-positive metastatic colorectal cancer (in combination with irinotecan, 5-FU, and leu ovarian [FOLFIRI]); squamous cell carcinoma of the head and neck (combined with radiation therapy)
* Clinical trials, probably combine with cisplatin
411
Cetuximab
Side effects
* Allergic reactions, sudden cardiac death, dermatologic problems, infections, renal failure, electrolyte abnormalities
* Asthenia/malaise, fever, nausea, constipation, interstitial pneumonitis
412
Panitumumab
Drug class
fully human monoclonal antibody
413
Panitumumab
Mechanism
EGFR (ErbB1) inhibitor
414
Panitumumab
Uses
EGFR-expressing metastatic colorectal cancers resistant to fluoropyrimidine, oxaliplatin, and irinotecan regimens
415
Panitumumab
Side effects
Skin toxicities, paronychia, hypomagnesemia, fatigue, abdominal pain, nausea, diarrhea, constipation
416
Nivolumab
Drug class
Human monoclonal antibody
417
Nivolumab
Mechanism
Inhibits programmed cell death protein 1 (PD-1) so immune system can attack melanoma cells
418
Nivolumab
Uses
Melanoma patients previously treated with ipilimumab, or those harboring the BRAF V600 mutation previously treated with ipilimumab and a BRAF inhibitor; metastatic squamous NSCLC that has progressed after platinum-based chemotherapy
419
Nivolumab
Side effects
* Rash, itching, cough, upper respiratory tract infections, edema, fatigue, shortness of breath, musculoskeletal pain, decreased appetite, nausea, constipation
* Severe immune-mediated side effects on healthy organs (lung, colon, liver, kidneys, hormone-producing glands
