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Pharmacology > Unit 1-Cancer, arthritis, gout, reproductive pharm > Flashcards

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

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2
Q

Side effects of alkylating agents

A
  • bone marrow toxicity
  • mucosal toxicity
  • nausea and vomiting
  • reproductive effects
  • increased risk of leukemia
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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
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4
Q

Mechlorethamine

Drug class

A

nitrogen mustard

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5
Q

Mechlorethamine

Mechanism

A
  • alkylating agent
  • spontaneous conversion to active metabolites in body fluids or enzymatically converted in liver
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6
Q

Mechlorethamine

Uses

A
  • Hodgkin’s lymphoma as part of MOPP combo therapy
  • topically used for cutaneous T-cell lymphomas
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7
Q

Mechlorethamine

Side effects

A
  • Severe nausea and vomiting
  • Myelosuppression (leukopenia and thrombocytopenia
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8
Q

Cyclophosphamide

Drug Class

A

Nitrogen Mustard

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9
Q

Cyclophosphamide

Mechanism

A
  • Alkylating agent
  • Conversion by liver CYP50 to active form phosphoramide mustard
  • relatively long half life
  • taken orally
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10
Q

Cyclophosphamide

Uses

A
  • broad spectrum uses
  • most widely uses alkylating agent
  • ALL, CLL, non-hodgkin’s lymphoma, breast, lung, and ovarian cancers
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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
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12
Q

Ifosfamide

Drug class

A

Nitrogen mustard

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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

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14
Q

Ifosfamide

Uses

A

Sarcoma and testicular cancer

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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
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16
Q

Carmustine

Drug Class

A

Nitrosurea

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17
Q

Carmustine

Mechanism of Action

A

Alkylating Agent

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18
Q

Carmustine

Uses

A

Brain tumors

(can cross BBB)

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19
Q

Carmustine

Side effects

A
  • CNS toxicity (dizziness)
  • Pulmonary fibrosis
  • Also nausea, vomiting, profound myelosuppression
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20
Q

Lomustine

Drug class

A

Nitrosurea

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21
Q

Lomustine

Mechanism of action

A

Alkylating agent

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22
Q

Lomustine

Uses

A

Brain tumors (can cross BBB)

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23
Q

Lomustine

Side effects

A
  • CNS toxicity (dizziness)
  • pulmonary fibrosis
  • Also profound myelosuppression, severe nausea and vomiting
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24
Q

Dacarbazine

Drug class

A

Triazene

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25
Q

Dacarbazine

Mechanism of action

A
  • alkylating agent
  • prodrug converted by liver to active form
  • IV administration
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26
Q

Dacarbazine

Uses

A
  • part of AVBD protocol for Hodgkin’s disease
  • also malignant melanoma
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27
Q

Dacarbazine

Side effects

A
  • nausea, vomiting
  • myelosuppression (thrombocytopenia, neutropenia)
  • flu-like symptoms (fever, fatigue)
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28
Q

Procarbazine

Drug class

A

Triazene

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29
Q

Procarbazine

Mechanism of action

A

Alkylating agent; forms free radicals

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30
Q

Procarbazine

Uses

A

Hodgkin’s lymphoma

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31
Q

Procarbazine

Side effects

A

May cause leukemia

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32
Q

Temozolomide

Drug class

A

Triazene

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33
Q

Temozolomide

Mechanism of action

A
  • alkylating agent
  • non-enzymatic conversion to methylhydrazine at physiologic pH
  • taken orally
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34
Q

Temozolomide

Uses

A

Malignant gliomas

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35
Q

Temozolomide

Side effects

A
  • Nausea and vomiting, myelosuppression (neutropenia, thrombocytopenia), flu-like symptoms (fever, fatigue)
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36
Q

Cisplatin

Drug class

A

Platinum analog

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37
Q

Cisplatin

Mechanism of action

A
  • 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
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38
Q

Cisplatin

Uses

A
  • ovarian, testiclular, cervical, bladder cancers
  • also head, neck, lung cancers
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39
Q

Cisplatin

Side effects

A
  • nephrotoxicity, ototoxicity
  • peripheral motor and sensory neuropathy at high doses
  • also severe nausea and vomiting; mild to moderate myelosuppression
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40
Q

Carboplatin

Drug class

A

Platinum analog

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41
Q

Carboplatin

Mechanism of action

A
  • 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
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42
Q

Carboplatin

Uses

A

Ovarian cancer

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43
Q

Carboplatin

Side effects

A

Myelosuppression (thrombocytopenia)

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44
Q

Oxaliplatin

Drug class

A

Platinum analog

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45
Q

Oxaliplatin

Mechanism of action

A
  • 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
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46
Q

Oxaliplatin

Uses

A

Gastric and colorectal cancers

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47
Q

Oxaliplatin

Side effects

A
  • peripheral sensory neuropathy (cold-induced)
  • also neutropenia
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48
Q

Mechanism of action of antimetabolite drugs

A

Structural analogs of folic acid or purine/pyrimidine bases of DNA;

Act in S-phase ie are cell-cycle specific

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49
Q

Methotrexate

Drug Class

A

Folate analog

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50
Q

Methotrexate

Mechanism of action

A
  • Inhibits dihydrofolate reductase which catalyzes conversion of folate to tetrahydrofolate, which is needed for purine and thymidine synthesis
  • given orally or intrathecally
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51
Q

Methotrexate

Uses

A
  • 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
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52
Q

Methotrexate

Side effects

A
  • 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
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53
Q

Permetrexed

Drug Class

A

Folate analog

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54
Q

Permetrexed

Mechanism of action

A

metabolized to polyglutamate forms that inhibit THF-dependent enzymes (e.g., DHFR, thymidylate synthase (TS))

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55
Q

Permetrexed

Uses

A
  • colon cancer
  • mesothelioma
  • non-small cell lung cancer
  • pancreatic cancer
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56
Q

5-Fluorouracil

Drug Class

A

Pyrimidine analog

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57
Q

5-Fluorouracil

Mechanism of action

A
  • 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
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58
Q

5-Fluorouracil

Uses

A
  • Combination therapy for breast, colorectal, gastric, head and neck, cervical and pancreatic cancer;
  • topically for basal cell carcinoma
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59
Q

5-Fluorouracil

Side effects

A
  • 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)
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60
Q

Cytarabine

Drug Class

A

Pyrimidine analog

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61
Q

Cytarabine

Mechanism of action

A

Ara-C converted by deoxycytidine kinase to Ara-CMP –> Ara-CTP; terminates DNA synthesis as Ara-CTP

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62
Q

Cytarabine

Uses

A
  • AML (most effective treatment)
  • ALL
  • blast phase CML
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63
Q

Cytarabine

Side effects

A
  • Severe myelosuppression (leucopenia, thrombocytopenia, anemia)
  • GI tract toxicity (ulceration, stomatitis, diarrhea)
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64
Q

Gemcitabine

Drug Class

A

Pyrimidine analog

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65
Q

Gemcitabine

Mechanism of action

A

Converted to active metabolites: dFdCDP inhibits ribonucleotide reductase (lowers deoxyribonucleotide); dFdCTP incorporates into DNA, terminating DNA synthesis

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66
Q

Gemcitabine

Uses

A
  • Pancreatic cancer
  • effective against non-small cell lung cancer, ovarian, bladder, esophageal, and head and neck cancer
  • More effective against solid tumors than cytarabine
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67
Q

Gemcitabine

Side effects

A

Myelosuppression (leucopenia, thrombocytopenia, anemia), flu-like symptoms

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68
Q

6-Mercaptopurine

Drug Class

A

Purine analog

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69
Q

6-Mercaptopurine

Mechanism of action

A
  • 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
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70
Q

6-Mercaptopurine

Uses

A

Maintain remission in acute ALL

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71
Q

6-Mercaptopurine

Side effects

A
  • 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
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72
Q

Mechanism of action of DNA Intercalating Agents

A
  • 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
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73
Q

Dactinomycin

Mechanism of Action

A
  • intercalates between G-C pairs of DNA, interfering with DNA-dependent RNA polymerase therefore disrupting transcription
  • also causes ssDNA breaks
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74
Q

Dactinomycin

Uses

A
  • Pediatric tumors (Wilm’s tumor, rhabdomyosarcoma, Ewing’s sarcoma)
  • choriocarcinoma in women
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75
Q

Dactinomycin

Side effects

A
  • Hematopoietic suppression with pancytopenia
  • also anorexia, nausea, vomiting
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76
Q

Mechanism of action of Anthracylines

A
  • 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
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77
Q

Daunorubicin

Drug Class

A

Anthracylines

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78
Q

Daunorubicin

Mechanism of action

A
  • 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
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79
Q

Daunorubicin

Uses

A

AML

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80
Q

Daunorubicin

Side Effects

A
  • Irreversible, dose-dependent cardiotoxicity
  • alopecia
  • also myelosuppression (neutropenia), stomatitis, GI disturbances
  • Dexrazoxane is cardio-protective
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81
Q

Idarubicin

Drug Class

A

Anthracylines

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82
Q

Idarubicin

Mechanism of action

A
  • 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
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83
Q

Idarubicin

Uses

A

AML

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84
Q

Idarubicin

Side effects

A
  • Irreversible dose-dependent cardiotoxicity
  • alopecia
  • also myelosuppression (neutropenia), stomatitis, GI disturbances
  • Dexrazoxane is cardio-protective
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85
Q

What drug is given with anthracylines to protect against cardiac side effects?

A

Dexrazoxane

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86
Q

Doxorubicin

Drug Class

A

Anthracylines

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87
Q

Doxorubicin

Mechanism of Action

A
  • 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
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88
Q

Doxorubicin

Uses

A
  • Sarcoma, breast, lung carcinomas
  • Malignant lymphomas
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89
Q

Doxorubicin

Side effects

A
  • Irreversible dose-dependent cardiotoxicity;
  • alopecia
  • also myelosuppression (neutropenia), stomatitis, GI disturbances
  • Dexrazoxane can be used to prevent cardiotoxic effects
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90
Q

Epirubicin

Drug Class

A

Anthracyclines

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91
Q

Epirubicin

Mechanism of action

A
  • 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
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92
Q

Epirubicin

Uses

A
  • Metastatic breast cancer
  • gastric cancer
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93
Q

Epirubicin

Side effects

A
  • Irreversible dose-dependent cardiotoxicity;
  • alopecia
  • Myelosuppression (neutropenia), stomatitis, GI disturbances
  • Dexrazoxane can be used to prevent cardiotoxic effects
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94
Q

Bleomycin

Mechanism of action

A

Acts in G2 phase of cell cycle. Binds to DNA, producing ss- and dsDNA breaks

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95
Q

Bleomycin

Uses

A
  • Combination therapy for testicular tumors or Hodgkin’s disease;
  • squamous cell carcinomas and lymphomas
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96
Q

Bleomycin

Side effects

A
  • Pulmonary toxicity (pulmonary fibrosis);
  • cutaneous toxicity (hyperpigmentation, hyperkeratosis, erythema);
  • hyperthermia
  • also minimally myelo- and immunosuppressive (often used in combo therapy); headache, nausea, vomiting
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97
Q

Mechanism of action of microtubule inhibitors

A
  • Inhibit mitosis and cause metaphase arrest by interfering with microtubule function (tubulin (de)polymerization);
  • Cell-cycle specific
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98
Q

Vinblastine

Drug Class

A

Vinca alkaloids

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99
Q

Vinblastine

Mechanism of action

A

Block tubulin polymerization into microtubules

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100
Q

Vinblastine

Uses

A
  • Metastatic testicular tumors (with bleomycin, cisplatin);
  • component of ABVD used for Hodgkin’s disease
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101
Q

Vinblastine

Side effects

A

Myelosuppression, nausea, vomiting

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102
Q

Vincristine

Drug Class

A

Vinca alkaloids

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103
Q

Vincristine

Mechanism of Action

A

Block tubulin polymerization into microtubules

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104
Q

Vincristine

Uses

A

Childhood ALL (with glucocorticoids); Hodgkin’s and non-Hodgkin’s lymphomas

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105
Q

Vincristine

Side effects

A
  • Dose-limiting neurotoxicity (peripheral neuropathy)
  • Relatively low bone marrow toxicity
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106
Q

Paclitaxel

Drug Class

A

Taxanes

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107
Q

Paclitaxel

Mechanism of action

A

Block microtubule depolymerization into tubulin

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108
Q

Paclitaxel

Uses

A

Metastatic breast, ovarian, lung, and head and neck cancers

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109
Q

Paclitaxel

Side effects

A
  • Peripheral neuropathy
  • Neutropenia
  • hypersensitivity reactions
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110
Q

Docetaxel

Drug Class

A

Taxanes

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111
Q

Docetaxel

Uses

A
  • Metastatic breast, ovarian, lung, and head and neck cancers;
  • hormone refractory prostate cancer
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112
Q

Docetaxel

Side effects

A
  • peripheral neuropathy
  • Neutropenia
  • hypersensitivity reactions
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113
Q

Mechanism of Topoisomerase Inhibitors

A
  • Prevent the resealing of topo I (ssDNA) and topo II (dsDNA);
  • Cell-cycle specific
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114
Q

Etoposide

Drug Class

A

Epipodophyllotoxins

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115
Q

Etoposide

Mechanism of action

A

Inhibits topoisomerase II

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116
Q

Etoposide

Uses

A

Testicular carcinoma, lung cancer, and non-Hodgkin’s lymphoma

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117
Q

Etoposide

Side effects

A
  • Dose-limiting myelosuppression (neutropenia)
  • oral mucositis
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118
Q

Teniposide

Drug Class

A

Epipodophyllotoxins

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119
Q

Teniposide

Mechanism of action

A

Inhibits topoisomerase II

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120
Q

Teniposide

Uses

A

ALL

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121
Q

Teniposide

Side effects

A

Dose-limiting myelosuppression (neutropenia), oral mucositis

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122
Q

Irinotecan

Drug Class

A

Camptothecin analogs

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123
Q

Irinotecan

Mechanism of action

A

Inhibits Topoisomerase I

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124
Q

Irinotecan

Uses

A
  • Advanced colorectal cancer;
  • lung, ovarian, cervical and brain tumors
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125
Q

Irinotecan

Side effects

A

Severe neutropenia, severe diarrhea

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126
Q

Topotecan

Drug Class

A

Camptothecin analogs

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127
Q

Topotecan

Mechanism of action

A

Inhibits topoisomerase I

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128
Q

Topotecan

Uses

A

Ovarian and small cell lung cancer

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129
Q

Topotecan

Side effects

A

Severe neutropenia, severe diarrhea

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130
Q

Docetaxel

Mechanism of action

A

Block microtubule depolymerization into tubulin

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131
Q

Glucocorticoid Use and mechanism in cancer

A
  • Particularly useful for tx of lymphocytic leukemias and lymphomas
  • inhibit mitosis in lymphocytes
  • do not induce myelosuppression
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132
Q

Prednisone

Drug Class

A

Glucocorticoids

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133
Q

Prednisone

Mechanism of action

A
  • inhibit mitosis in lymphocytes
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134
Q

Prednisone

Uses

A
  • ALL
  • MOPP and CHOP combination for Hodgkin’s, non-Hodkin’s
  • multiple myeloma, and CLL
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135
Q

Dexamethasone

Drug Class

A

Glucocorticoids

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136
Q

Dexamethasone

Mechanism of action

A

inhibit mitosis in lymphocytes

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137
Q

Dexamethasone

Uses

A

Reduces edema in brain and spinal cord tumors in conjunction with radiation therapy

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138
Q

Tamoxifen

Drug Class

A

Selective estrogen-receptor modulators (SERMs)

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139
Q

Tamoxifen

Mechanism of action

A

Competes with estradiol for binding to estrogen receptor

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140
Q

Tamoxifen

Uses

A
  • ER-positive breast cancer
  • or as adjuvant therapy following primary breast tumor excision
  • prevention of breast cancer in high-risk patients
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141
Q

Tamoxifen

Side effects

A
  • Hot flushes, hair loss; increased risk of endometrial cancer; increased risk of thromboembolic events
  • also nausea and vomiting
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142
Q

Mechanism of action of Selected Estrogen Receptor Downregulators (SERDS)

A
  • completely anti-estrogenic
  • ie have no estrogen agonist activity
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143
Q

Fulvestrant

Drug Class

A

Selective Estrogen-Receptor Downregulator

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144
Q

Fulvestrant

Mechanism of action

A

Binds with much higher affinity (>100-fold) to estrogen receptor than tamoxifen, inhibiting dimerization, increasing degradation, and reducing overall ER levels

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145
Q

Fulvestrant

Uses

A

Posmenopausal women with ER-positive metastatic breast cancer

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146
Q

List of aromatase inhibitors

A
  • Aminoglutethamide
  • Anastrozole
  • Letrozole
  • Exemestane
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147
Q

Aminoglutethamide

Drug Class

A

Aromatase inhibitors

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148
Q

Aminoglutethamide

Mechanism of action

A

Inhibits function of aromatase

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149
Q

Aminoglutethamide

Uses

A

Relatively weak, used against breast cancer

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150
Q

Anastrozole

Drug Class

A
  • Aromatase inhibitor
  • 3rd generation
  • nonsteroidal
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151
Q

Anastrozole

Uses

A

First-line for ER-positive breast cancer in postmenopausal women

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152
Q

Letrozole

Drug Class

A
  • aromatase inhibitor
  • 3rd generation
  • nonsteroidal
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153
Q

Letrozole

Uses

A

ER-positive breast cancer in postmenopausal women

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154
Q

Exemestane

Drug class

A
  • aromatase inhibitor
  • 3rd generation
  • steroidal
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155
Q

Exemestane

Mechanism of action

A

Steroidal inhibitor of aromatase

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156
Q

Anastrozole

Mechanism of action

A

Inhibits function of aromatase

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157
Q

Letrozole

Mechanism of action

A

Inhibits function of aromatase

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158
Q

Leuprolide

Drug Class

A

GnRH analog

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159
Q

Leuprolide

Mechanism of action

A

Binds GnRH receptor; inhibits release of FSH & LH

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160
Q

Leuprolide

Uses

A
  • Androgen ablation therapy, along with AR blockers
  • for prostate cancer
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161
Q

Goserelin

Drug Class

A

GnRH analogs

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162
Q

Goserelin

Mechanism of action

A

Binds GnRH receptor; inhibits release of FSH & LH

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163
Q

Goserelin

Uses

A
  • Androgen ablation therapy, along with AR blockers
  • for prostate cancer
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164
Q

Flutamide

Drug class

A

Nonsteroidal androgen-receptor blockers

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165
Q

Flutamide

Mechanism of action

A

Competes with androgen for AR binding and prevent receptor translocation to nucleus

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166
Q

Flutamide

Uses

A
  • Androgen ablation therapy, along with GnRH analogs
  • for prostate cancer
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167
Q

Bicalutamide

Drug Class

A

Nonsteroidal androgen-receptor blockers

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168
Q

Bicalutamide

Mechanism of action

A

Competes with androgen for AR binding and prevent receptor translocation to nucleus

169
Q

Bicalutamide

Uses

A
  • Androgen ablation therapy, along with GnRH analogs
  • for prostate cancer
170
Q

Hydroxyurea

Mechanism of action

A

Inhibits ribonucleoside diphosphate reductase so cannot convert ribonucleotides to deoxyribonucleotides –> inhibit DNA synthesis

171
Q

Hydroxyurea

Uses

A
  • CML (replaced by Imatinib),
  • polycythemia vera, essential thrombocythemia
  • treatment for sickle cell disease (increases Hb-F)
172
Q

Retinoids

Mechanism of action

A

All trans retinoic acid (ATRA) induces terminal differentiation in malignant immature promyelocytes, which subsequently apoptose

173
Q

Retinoids

Uses

A

APL

174
Q

Arsenic Trioxide

Uses

A

heavy metal toxin used for tx of relapsed APL

175
Q

Thalidomide

Uses

A

Multiple myeloma and myelodysplastic syndromes

176
Q

Interferons

A

Hairy-cell leukemia, CML, and AIDS-related Kaposi’s sarcoma (interferon alpha)

177
Q

Imatinib

Drug class

A

Tyrosine Kinase Inhibitor

178
Q

Imatinib

Mechanism of action

A

Inhibits Abl kinase by binding where ATP should go; also inhibits PDGFR and c-kit; metabolized by cytochrome P450

179
Q

Imatinib

Uses

A
  • First line therapy for CML
  • also, gastrointestinal tumor (GIST)
180
Q

Imatinib

Side effects

A
  • Nausea and vomiting, fluid retention, muscle cramps, arthralgia
  • Myelosuppression
181
Q

Gefitinib

Drug Class

A

Tyrosine Kinase inhibitor

182
Q

Gefitinib

Uses

A

Non-small lung cancer

183
Q

Gefitinib

Side effects

A
  • 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
Q

Erlotinib

Drug Class

A

Tyrosine Kinase inhibitor

185
Q

Erlotinib

Mechanism of action

A

Inhibit epidermal growth factor receptor (EGFR) tyrosine kinase

186
Q

Erlotinib

Uses

A

Non-small lung cancer; pancreatic cancer

187
Q

Erlotinib

Side effects

A
  • 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
Q

Rituximab

Drug class

A

Monoclonal antibody

189
Q

Rituximab

Mechanism of action

A

CD20 B-cell antibody that can directly activate apoptosis, activate complement, or activate cell-mediated cytotoxicity (e.g., T cells, NK cells)

190
Q

Rituximab

Uses

A

Non-Hodgkin’s lymphomas

191
Q

Rituximab

side effects

A
  • Infusion reactions, tumor lysis syndrome (TLS), severe mucocutaneous reactions, progressive multifocal leukoencephalopathy (PML)
  • Skin reactions, irregular heartbeat, muscle or joint pain
192
Q

Trastuzumab

Drug Class

A

Monoclonal antibody

193
Q

Trastuzumab

Mechanism of action

A

Unknown HER2/neu (ErbB2) receptor antibody mechanism (enhanced receptor endocytosis or blocking homo- or heterodimerization)

194
Q

Trastuzumab

Uses

A
  • HER2/neu-overexpressing metastatic breast cancer
  • Usually combined with paclitaxel or doxorubicin;
195
Q

Trastuzumab

Side effects

A
  • Hypersentivity reaction; ventricular dysfunction
  • enhances doxorubicin cardiotoxicity
196
Q

Indomethacin

Drug Class

A

non-selective NSAID

197
Q

Indomethacin

Mechanism of action

A

Eliminate pain; reduce inflammation (but does not slow disease progression)

198
Q

Indomethacin

Uses

A
  • Rheumatoid arthritis
  • acute gouty arthritis
199
Q

Indomethacin

Side effects

A

Gastric and duodenal ulcers

200
Q

Naproxen

Drug Class

A

non-selective NSAID

201
Q

Naproxen

Mechanism of action

A

Eliminate pain; reduce inflammation (but does not slow disease progression)

202
Q

Naproxen

Uses

A
  • Rheumatoid arthritis
  • acute gouty arthritis
203
Q

Naproxen

Side effects

A

Gastric and duodenal ulcers

204
Q

COX-2 inhibitors

Drug class

A

Selective NSAID

205
Q

COX-2 inhibitor

Mechanism

A

Eliminate pain; reduce inflammation (but does not slow disease progression)

206
Q

COX-2 inhibitor

Uses

A

Superseding conventional NSAIDs for rheumatoid arthritis

207
Q

COX-2 inhibitor

Side effects

A

50% fewer gastric and duodenal ulcers than traditional NSAIDs

208
Q

Disease modifying anti-rheumatic drugs (DMARD)

Mechanism

A

drugs that retard or halt the progression of the disease

209
Q

Quinolones (chloroquine and hydroxychloroquine)

Drug class

A

DMARD (antimalarial)

210
Q

Quinolones (chloroquine and hydroxychloroquine)

Mechanism

A

Reduces T-cell activation & chemotaxis

211
Q

Quinolones (chloroquine and hydroxychloroquine)

Uses

A
  • Rheumatoid arthritis, SLE
  • Used for patients who no longer respond to NSAIDS or can’t tolerate other DMARDs
212
Q

Quinolones (chloroquine and hydroxychloroquine)

Side effects

A

Retinal damage (chloroquine)

213
Q

Glucocorticoids

Drug class

A

DMARD

214
Q

Glucocorticoids

Mechanism of action

A
  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
Q

Glucocorticoids

Uses

A
  • 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
Q

Glucocorticoids

Side effects

A

Cushingoid symptoms

217
Q

Sulfasalazine

Drug class

A

DMARD

218
Q

Sulfazalazine

Mechanism of action

A
  • Likely inhibition of IL-1 & TNF-alpha release
  • Acts more quickly than other drugs
219
Q

Sulfasalazine

Uses

A

Rheumatoid arthritis

220
Q

Sulfasalazine

Side effects

A

N/V, skin rashes, neutropenia (30% of patient discontinue drug)

Headaches

221
Q

Methotrexate

Drug class (RA)

A

DMARD (immunosuppressant)

222
Q

Methotrexate (RA)

Mechanism of action

A
  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
Q

Methotrexate (RA)

Uses

A

Rheumatoid Arthritis

224
Q

Methotrexate (RA)

Side effects

A

Nausea, stomatitis, hepatotoxicity (rare)

225
Q

Leflunomide

Drug Class

A

DMARD

(Immunosuppressive)

226
Q

Leflunomide

Mechanism

A
  • Inhibits dihydroorotate dehydrogenase (DHODH), which inhibits T-lymphocyte response to stimuli
  • Takes several weeks to start working; oral prodrug
227
Q

Leflunomide

Uses

A

Rheumatoid arthritis

228
Q

Leflunomide

Side effects

A

Diarrhea, hepatotoxity

229
Q

Biological Response Modifiers

Mechanism

A

interfere with cytokine signalling in inflammation

230
Q

Etanercept

Drug Class

A

Biologic Response Modifiers

231
Q

Etanercept

Mechanism of action

A

Blocks binding of TNF to TNF receptors

232
Q

Etanercept

Uses

A

Rheumatoid arthritis

233
Q

Infliximab

Drug class

A

biological response modifiers

234
Q

Infliximab

Mechanism of action

A

Blocks binding of TNF to TNF receptors

235
Q

Infliximab

Uses

A

Rheumatoid arthritis

236
Q

Infliximab

Side effects

A

Antigenic response to murine monoclonal Ab

237
Q

Adalimumab

Drug Class

A

biological response modifiers

238
Q

Adalimumab

Mechanism of action

A

Blocks binding of TNF to TNF receptors

239
Q

Adalimumab

Uses

A

Rheumatoid arthritis

240
Q

Golimumab

Drug class

A

Biological response modifiers

241
Q

Golimumab

Mechanism of action

A

Blocks binding of TNF to TNF receptors

242
Q

Golimumab

Uses

A

Rheumatoid arthritis

243
Q

Golimumab

Side effects

A

Risk of serious infections

244
Q

Certolizumab

Drug class

A

Biologic Response Modifiers

245
Q

Certolizumab

Mechanism of action

A
  • Blocks binding of TNF to TNF receptors
  • Conjugated to PEG for stabilization
246
Q

Certolizumab

Uses

A

Rheumatoid arthritis

247
Q

Certolizumab

Side effects

A

risk of serious infections

248
Q

Anakinra

Drug class

A

Biologic Response Modifiers

249
Q

Anakinra

Mechanism of action

A
  • IL-1 Receptor Antagonist
  • Short (6 hr) plasma half-life; daily treatment with high doses
250
Q

Anakinra

Uses

A

Rheumatoid arthritis

251
Q

Tocilizumab

Drug Class

A

Biologic Response Modifiers

252
Q

Tocilizumab

Mechanism of action

A

IL-6 Receptor Antagonist

253
Q

Tocilizumab

Uses

A

Rheumatoid Arthritis

254
Q

Tocilizumab

Side effects

A

serious infections eg Tb, fungal, viral, other opportunistic

255
Q

Abatacept

Drug class

A

Biologic Response Modifiers

256
Q

Abatacept

Mechanism of action

A

Inhibits T-cell activation and induces T-cell apoptosis

257
Q

Abatacept

Uses

A

Rheumatoid arthritis

258
Q

Abatacept

Side effects

A

Headaches; infections

259
Q

Rituximab

Drug class

A

Biological response modifiers

260
Q

Rituximab

Mechanism of action

A

Anti-CD20 mAb, reduces circulating B cells

261
Q

Rituximab

Uses

A
  • Rheumatoid arthritis
  • Used for RA refractory to TNF-alpha inhibitors
262
Q

Rituximab

Side effects

A

Infections; hypersensitivity reactions

263
Q

Tofacitinib

Drug class

A

biological response modifiers

264
Q

Tofacitinib

Mechanism of action

A

Inhibition of JAK 1 & 3 which inhibits production of inflammatory mediators

265
Q

Tofacitinib

Uses

A

Rheumatoid arthritis

266
Q

Tofacitinib

Side effects

A

Upper respiratory tract infections; headaches, diarrhea

Malignancies

267
Q

Treatment of acute gout: drug and mechanism

A

NSAIDs

eicosanoid mediated pain and inflammation

for initial tx of acute gout

268
Q

Colchicine

Mechanism

A
  • Prevents tubulin polymerization & leads to inibition of leukocyte migration, phagocytosis, and release of cytokines
  • Works in 12-24 hours!
269
Q

Colchicine

Uses

A

Acute gouty arthritis

270
Q

Colchicine

Side Effects

A
  • Low Therapeutic index
  • Long-term use causes peripheral neuropathy & neutropenia
  • Nausea, vomiting, abdominal pain, troublesome diarrhea
271
Q

Probenecid

Drug class

A

Uricosuric agents

272
Q

Probenecid

Mechanism

A

Compete with urate at the anionic transport site of the renal tubule and inhibit urate reabsorption

273
Q

Probenecid

Uses

A

Chronic tophaceous gout

274
Q

Probenecid

Side effects

A

Urate crystal mobilization and acute gouty arthritis

Gastrointestinal irritation

Secretion of some weak acids (e.g., penicillin) is reduced

275
Q

Allopurinol

Mechanism

A
  1. Reduces uric acid synthesis by inhibiting xanthine oxidase (competitive inhibition) –> alloxanthine
  2. Alloxanthine is a non-competitive inhibitor of xanthine oxidase
276
Q

Allopurinol

Uses

A

Chronic tophaceous gout

277
Q

Allopurinol

Side effects

A

Acute attacks of gouty arthritis early in treatment due to mobilization of urate crystals

278
Q

Febuxostat

Mechanism

A

Non-purine, non-competitive antagonist of xanthine oxidase

279
Q

Febuxostat

Uses

A

Chronic tophaceous gout

280
Q

Febuxostat

Side effects

A

Nausea, rash, arthralgias

(also expensive)

281
Q

Pegloticase

Drug Class

A

Recombinant, stabilized uricase

282
Q

Pegloticase

Mechanism

A

Converts uric acid to allantoin

283
Q

Pegloticase

Uses

A

Chronic tophaceous gout

use when refractory to other therapies

284
Q

Estradiol (valerate & cypionate)

Drug class

A

Estradiol esters (steroidal)

285
Q

Estradiol (valerate & cypionate)

Mechanism

A

Absorbed through skin, mucus membranes, GI Tract; body-wide distribution via sex-hormone binding globulin

286
Q

Estradiol (valerate & cypionate)

Uses

A

Contraception, primary hypogonadism, postmenopausal hormone therapy, osteoporosis

287
Q

Estradiol (valerate & cypionate)

Side effects

A
  • 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
Q

Estrone sulfate

Drug class

A

Estradiol esters (steroidal)

conjugated

289
Q

Estrone sulfate

Mechanism

A

Absorbed through skin, mucus membranes, GI Tract; body-wide distribution via sex-hormone binding globulin

290
Q

Estrone sulfate

Uses

A

Contraception, primary hypogonadism, postmenopausal hormone therapy, osteopososis

291
Q

Estrone sulfate

Side effects

A
  • 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
Q

Equilin sulfate

drug class

A

Estradiol esters (steroidal)

conjugated

293
Q

Equilin sulfate

Mechanism

A

Absorbed through skin, mucus membranes, GI Tract; body-wide distribution via sex-hormone binding globulin

294
Q

Equilin sulfate

Uses

A

Contraception, primary hypogonadism, postmenopausal hormone therapy, osteoporosis

295
Q

Equilin sulfate

Side effects

A
  • 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
Q

Ethinyl estradiol

Drug class

A

alkyl estrogen

297
Q

Ethinyl estradiol

Mechanism

A

Absorbed through skin, mucus membranes, GI Tract; body-wide distribution via sex-hormone binding globulin

298
Q

Ethinyl estradiol

Uses

A

Contraception, primary hypogonadism, postmenopausal hormone therapy, osteoporosis

299
Q

Ethinyl Estradiol

Side effects

A
  • 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
Q

Mestranol

Drug class

A

Alkyl estrogen

301
Q

Mestranol

Mechanism

A

Absorbed through skin, mucus membranes, GI Tract; body-wide distribution via sex-hormone binding globulin

302
Q

Mestranol

Uses

A

Contraception, primary hypogonadism, postmenopausal hormone therapy

303
Q

Mestranol

Side effects

A
  • 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
Q

Quinestrol

Drug Class

A

Estradiol esters (steroidal)

305
Q

Quinestrol

Mechanism

A

Absorbed through skin, mucus membranes, GI Tract; body-wide distribution via sex-hormone binding globulin

306
Q

Quinestrol

Uses

A

Contraception, primary hypogonadism, postmenopausal hormone therapy, osteoporosis

307
Q

Quinestrol

Side effects

A
  • 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
Q

Diethylstilbestrol

Drug Class

A

Non-steroidal synthetic estrogen

309
Q

Diethylstilbestrol

Side effects

A

Increased risk of clear cell adenocarcinoma of vagina & cervix

310
Q

Tamoxifen citrate

Drug Class

A

Non-steroidal anti-estrogen; selective estrogen receptor modifier

311
Q

Tamoxifen citrate

Mechanism

A

Blocks estrogen from binding ER and causing growth in ER(+) breast cancer

312
Q

Tamoxifen citrate

Uses

A

ER(+) breast cancer

313
Q

Tamoxifen citrate

side effects

A
  • 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
Q

Clomiphene citrate

Drug class

A

Non-steroidal anti-estrogen

315
Q

Clomiphene citrate

Mechanism

A
  • 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
Q

Clomiphene citrate

Uses

A

Stimulate ovulation in patients who want to get pregnant

317
Q

Clomiphene citrate

Side effects

A
  • Stomach pain, headache, upset stomach, vomit
318
Q

Micronized progesterone

Drug class

A

Natural progesterone

319
Q

Micronized progesterone

Mechanism

A

Binds to PR; decreased first-pass metabolism & enhanced dissolution due to micronization

320
Q

Micronized progesterone

Uses

A

Contraception, hormone replacement therapy

321
Q

Micronized progesterone

Side effects

A
  • 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
Q

Transvaginal progesterone

Drug Class

A

Natural progesterone

323
Q

Transvaginal progesterone

Mechanism

A

Binds to PR; vaginal gel (uterine effects without first pass metabolism and minimal systemic side effects)

324
Q

Transvaginal progesterone

Uses

A

Contraception, hormone replacement therapy

325
Q

Transvaginal progesterone

Side effects

A
  • 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
Q

Medroxyprogesterone

Drug class

A

Synthetic progesterone

327
Q

Medroxyprogesterone

Uses

A

Contraception, hormone replacement therapy

328
Q

Medroxyprogesterone

Side effects

A
  • 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
Q

Norethindrone

Drug class

A

Synthetic progesterone

330
Q

Norethindrone

Uses

A

Contraception, hormone replacement therapy

331
Q

Norethindrone

Side effects

A
  • 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
Q

Norgestrol

Drug class

A

Synthetic progesterone

333
Q

Norgestrol

Uses

A

Contraception, hormone replacement therapy

334
Q

Norgestrol

Side effects

A
  • 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
Q

Megestrol

Drug Class

A

Synthetic progesterone

336
Q

Megestrol

Uses

A

Contraception, hormone replacement therapy

337
Q

Megestrol

Side effects

A
  • 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
Q

Monophasic Ortho-Novum

Drug class

A

Combination pill

339
Q

Monophasic Ortho-Novum

Mechanism

A
  • 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
Q

Monophasic Ortho-Novum

Use

A

Contraception

341
Q

Monophasic Ortho-Novum

Side effects

A
  • 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
Q

Biphasic Ortho-Novum

Drug class

A
  • Combination pill
  • Fixed estrogen, progestin increased for days 11-21
343
Q

Biphasic Ortho-Novum

Mechanism

A

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
Q

Biphasic Ortho-Novum

Uses

A

Contraception

345
Q

Biphasic Ortho-Novum

Side effects

A
  • 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
Q

Triphasic Ortho-Novum

Class

A
  • Combination pill
  • Fixed or variable estrogen, while progestin increases in 3 phases (1-7, 8-14, 15-21)
347
Q

Triphasic Ortho-Novum

Mechanism

A

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
Q

Triphasic Ortho-Novum

Uses

A

Contraception

349
Q

Triphasic Ortho-Novum

Side effects

A
  • 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
Q

Mini-pill

Drug class

A

Progestin only

351
Q

Mini-pill

Uses

A

Less effective than combination pill for contraception; use when patient has estrogen contraindication; good in lactating women (estrogen reduces milk production)

352
Q

Mini-pill

Side effects

A
  • More likely to produce irregular menstrual cycle (estrogen required to provide stability to endometrium)
  • also suppresses endometrial cancer
353
Q

Levonorgestrel (Plan B)

Drug class

A

Synthetic progestogen

354
Q

Levonorgestrel (Plan B)

Mechanism

A
  • Unknown
  • but must be taken within 72 hours of coitus
355
Q

Levonorgestrel (Plan B)

Uses

A

Prevent implantation

356
Q

Levonorgestrel (Plan B)

Side effects

A

Likely the same as combination oral contraceptives

357
Q

Mifepristone

Drug class

A

Anti-progestin; glucocorticoid receptor antagonist

358
Q

Mifepristone (RU-486, Korlym)

Mechanism

A

Competitively binds to progesterone receptor (leading to detachment of fetus); glucocorticoid recepter antagonist

359
Q

Mifepristone (RU-486, Korlym)

Uses

A
  • 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
Q

Sildenafil citrate (Viagra)

Drug class

A

PDE5 inhibitor

361
Q

Sildenafil citrate (Viagra)

Mechanism

A

Bind catalytic site of PDE5; inhibits PDE5 breakdown of cGMP –> decreased Ca++ –> smooth muscle relaxation –> erection

362
Q

Sildenafil citrate (Viagra)

Uses

A

Erectile dysfunction; does not trigger an automatic erection, but improves response to sexual stimulation;

363
Q

Sildenafil citrate (Viagra)

Side effects

A
  • 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
Q

Vardenafil HCl (Levitra)

Drug class

A

PDE5 inhibitor

365
Q

Vardenafil HCl (Levitra)

Mechanism

A

Bind catalytic site of PDE5; inhibits PDE5 breakdown of cGMP –> decreased Ca++ –> smooth muscle relaxation –> erection

366
Q

Vardenafil HCl (Levitra)

Uses

A

Erectile dysfunction; does not trigger an automatic erection, but improves response to sexual stimulation;

367
Q

Vardenafil HCl (Levitra)

Side effects

A
  • 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
Q

Tadalafil (Cialis)

Drug class

A

PDE5 inhibitor

369
Q

Tadalafil (Cialis)

Mechanism

A

Bind catalytic site of PDE5; inhibits PDE5 breakdown of cGMP –> decreased Ca++ –> smooth muscle relaxation –> erection

370
Q

Tadalafil (Cialis)

Uses

A

Erectile dysfunction; does not trigger an automatic erection, but improves response to sexual stimulation;

371
Q

Tadalafil (Cialis)

Side effects

A
  • 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
Q

Nilotinib

Drug Class

A

Tyrosine kinase inhibitor

373
Q

Nilotinib

Mechanism

A

Inhibits Abl kinase

374
Q

Nilotinib

Uses

A

Imatinib-resistant CML

375
Q

Nilotinib

Side effects

A
  • Myelosuppression
  • also QT prolongation, hepatotoxicity, electrolyte abnormalities
376
Q

Dasatinib

Drug Class

A

Tyrosine Kinase Inhibitor

377
Q

Dasatinib

Mechanism

A

inhibits Abl and Src kinases

378
Q

Dasatinib

Uses

A

Imatinib-resistant CML

379
Q

Dasatinib

Side effects

A
  • Myelosuppression, bleeding, fluid retention, pulmonary arterial hypertension
  • also diarrhea, nausea and vomiting, weakness, infections
380
Q

Vemurafinib

Drug Class

A

Serine/threonine kinase inhibitor

381
Q

Vemurafinib

Mechanism

A

Inhibits oncogenic BRAF kinase

382
Q

Vemurafinib

Uses

A
  • Unresectable Stage III and IV or metastatic melanomas w/BRAF mutations
  • trial found it works better than dacarbazine
383
Q

Vemurafinib

Side effects

A
  • Arthralgia, fatigue, photosensitivity, nausea, alopecia, diarrhea, QT prolongation (increased risk of ventricular arrythmias)
  • new primary cutaneous melanoma
384
Q

Dabrafenib

Drug Class

A

Serine/threonine kinase inhibitor

385
Q

Dabrafenib

Mechanism

A

Inhibits oncogenic BRAF kinase

386
Q

Dafrabenib

Uses

A

Unresectable Stage III and IV or metastatic melanomas w/BRAF mutations

387
Q

Dabrafenib

Side effects

A
  • 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
Q

Trametinib

Drug class

A

Dual specificity kinase

389
Q

Trametinib

Uses

A

Unresectable Stage III and IV or metastatic melanomas w/BRAF mutations

390
Q

Trametinib

Side effects

A
  • Cardiomyopathy, retinal disorders, interstitial lung disease, serious skin toxicities
  • Rash, diarrhea, stomatitis, hypertension, pruritis
  • May cause female infertility
391
Q

Ipilimumab

Drug class

A

Human monoclonal antibody

392
Q

Ipilimumab

Mechanism

A

Cytotoxic T-Lymphocyte Antigen 4 inhibitor; stimulates immune system

393
Q

Ipilimumab

Uses

A

Melanoma

394
Q

Interleukin-2 use in chemotherapy

A

binds IL-2 receptor on lymphocytes and modulates immune system;

used in immunotherapy for melanoma

395
Q

Gefitinib

Mechanism

A

Inhibit epidermal growth factor receptor (EGFR) tyrosine kinase

396
Q

Afatinib

Drug Class

A

Tyrosine Kinase inhibitor

397
Q

Afatinib

Mechanism

A

Inhibit EGFR tyrosine kinase

398
Q

Afatinib

Uses

A

Non-small cell lung cancer

399
Q

Afatinib

Side effects

A
  • Diarrhea, vomiting, rash/dermatitis acneiform, stomatitis, paronichia, dry skin, pruritis, decreased appetite
  • Dyspnea, fatigue, pulmonary toxicity, pneumonia, sepsis
400
Q

Lapatinib

Drug class

A

Tyrosine kinase inhibitor

401
Q

Lapatinib

Mechanism

A

Inhibits EGFR and ErbB2 (HER2) tyrosine kinase

402
Q

Lapatinib

Uses

A

Advanced or metastatic breast cancer over-expressing HER2; hormone (+) metastatic breast cancer over expressing HER2 receptor in post menopausal women

403
Q

Lapatinib

Side effects

A
  • Hepatotoxicity, nausea, diarrhea, fatigue, rashes, QT-prolongation
  • Decreased left ventricular function when combined with capecitabine, hypokalemia, hypomagnesemia
404
Q

Ado-trastuzumab emtansine

Drug class

A

Antibody-drug conjugate

405
Q

Ado-trastuzumab emtansine

Mechanism

A

Conjugate undergoes receptor-dependent internalization & drug released inside cell

406
Q

Ado-trastuzumab emtansine

Uses

A

ErbB2 (HER2) positive metastatic breast cancer patients with prior treatment history of trastuzumab and/or taxane

407
Q

Ado-trastuzumab emtansine

Side effects

A

Fatigue, nausea, musculoskeletal pain, thrombocytopenia, headache, hypokalemia, peripheral neuropathy, ventricular dysfunction, interstitial lung disease

Interstitial lung disease, infusion-associated reactions, hepatotoxicity, birth defects

408
Q

Cetuximab

Drug class

A

monoclonal antibody

409
Q

Cetuximab

Mechanism

A

competitively inhibits EGFR (ERB1) tyrosine kinase

410
Q

Cetuximab

Uses

A
  • 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
Q

Cetuximab

Side effects

A
  • Allergic reactions, sudden cardiac death, dermatologic problems, infections, renal failure, electrolyte abnormalities
  • Asthenia/malaise, fever, nausea, constipation, interstitial pneumonitis
412
Q

Panitumumab

Drug class

A

fully human monoclonal antibody

413
Q

Panitumumab

Mechanism

A

EGFR (ErbB1) inhibitor

414
Q

Panitumumab

Uses

A

EGFR-expressing metastatic colorectal cancers resistant to fluoropyrimidine, oxaliplatin, and irinotecan regimens

415
Q

Panitumumab

Side effects

A

Skin toxicities, paronychia, hypomagnesemia, fatigue, abdominal pain, nausea, diarrhea, constipation

416
Q

Nivolumab

Drug class

A

Human monoclonal antibody

417
Q

Nivolumab

Mechanism

A

Inhibits programmed cell death protein 1 (PD-1) so immune system can attack melanoma cells

418
Q

Nivolumab

Uses

A

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
Q

Nivolumab

Side effects

A
  • 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

Pharmacology (26 decks)

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