Brainscape's Knowledge GenomeTM


Top Flashcards (Certified)
All Flashcards

GER Pharm Unit 1 > UPDATED Unit 1 Deck > Flashcards

UPDATED Unit 1 Deck Flashcards

1
Q

alkalating agents

A
  • produce strong electrophiles through carbonium or ethyleneimonium intermediates, which covalently bond via alkylation of nucleophilic moieties in DNA (mostly N7 position of guanine); Cell Cycle Non-Specific (CCNS)
  • side effects: bone marrow, mucosal toxicity, nausea and vomiting, toxic effects on reproductive systems, increased leukemia risk
  • resistance may occur due to decreased permeability or uptake; increased rates of catabolism; enhanced DNA repair; increased glutathione production (inactivates via conjugation)
  • classes: nitrogen mustards, nitrosoureas, triazenes, platinum analogs
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Mechlorethamine (Mustargen)

A
  • alkalating agent; class: nitrogen mustard
  • mechanism: spontaneous conversion to active metabolites in body fluids or enzymatically converted in liver
  • treats: hodgkin’s disease, topically for treatment of cutaneous T-cell lymphoma
  • other side effects: severe nausea and vomiting, myelosuppression (leucopenia, thrombocytopenia)
  • don’t use much anymore due to sterility
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Cyclophosphamide (Cytoxan)

A
  • alkalatin agent; class: nitrogen mustard
  • mechanism: conversion by hepatic cytochrome P450 to active metabolite phosphoramide mustard
  • treats: most widely used alkylating agent (broad clinical spectrum); singly or in combination for ALL, CLL, non-Hodgkin’s lymphoma, and breast, lung, and ovarian cancer
  • important side effects: hemorrhagic cystitis (bladder irritation) due to acrolein (toxic drug metabolite); adequate hydration and administration of MESNA (2-mercaptoethane sulfonate) minimizes problem
  • other side effects: nausea, vomiting, myelosuppression
  • relatively long plasma half-life (7-15 hrs); PO
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Ifosfamide (Ifex)

A
  • alkylating agent; class: nitrogen mustard
  • mechanism: conversion by hepatic cytochrome P450 to active metabolite phosphoramide mustard
  • treats: sarcoma and testicular cancer
  • important side effects: hemorrhagic cystitis (bladder irritation) due to acrolein (toxic drug metabolite); adequate hydration and administration of MESNA (2-mercaptoethane sulfonate) minimizes problem
  • other side effects: nausea, vomiting, myelosuppression
  • relatively long plasma half-life (7-15 hrs); PO
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Carmustine (Gliadel)

Lomustine (Ceenu)

A
  • alkylating agent; class: nitrosureas
  • mechanism: alkylating agent
  • treats: brain tumors (cross blood-brain barrier)
  • important side effects: renal toxicity, pulmonary fibrosis
  • other side effects: profound myelosuppression, severe nausea and vomiting
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Dacarbazine (DTIC)

A
  • alkylating agent; class: triazenes
  • mechanism: prodrug activated by liver cytochromes
  • treats: part of ABVD for Hodgkin’s disease; also, malignant melanoma
  • other side effects: nausea and vomiting, myelosuppression (neutropenia, thrombocytopenia), flu-like symptoms (fever, fatigue)
  • IV administration
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Procarbazine (Matulane)

A
  • alkylating agent; class: triazenes
  • mechanism: forms free radicals
  • treats: hodgkin’s lymphoma
  • important side effects: may cause leukemia
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Temozolomide (Temodar)

A
  • alkylatin agent; class: triazenes
  • mechanism: nonenzymatic conversion to methylhydrazine at physiologic pH
  • treats: malignant gliomas
  • other side effects: nausea and vomiting, myelosuppression (neutropenia, thrombocytopenia), flu-like symptoms (fever, fatigue)
  • PO
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Cisplatin (Platinol)

A
  • alkylating agent; class: platinum analog
  • mechanism: doesn’t form carbonium intermediate or formally alkylate DNA; covalently bind nucleophilic sites on DNA (e.g., guanine N7) and is converted to active cytotoxic forms by reacting with water to form (+)charged, hydrated intermediates that react with DNA guanine, forming inter- and intrastand cross-links
  • treats: testicular, ovarian, cervical, and bladder cancers; also useful in treatment of head and neck cancer, and lung carcinoma
  • important side effects: nephrotoxicity, ototoxicity, peripheral motor and sensory neuropathy at high doses
  • other side effects: severe nausea and vomiting, mild to moderate myelosuppression
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Carboplatin (Paraplatin)

A
  • alkylating agent; class: platinum analog
  • mechanism: doesn’t form carbonium intermediate or formally alkylate DNA; covalently bind nucleophilic sites on DNA (e.g., guanine N7) and is converted to active cytotoxic forms by reacting with water to form (+)charged, hydrated intermediates that react with DNA guanine, forming inter- and intrastand cross-links
  • treats: ovarian cancer
  • other side effects: myelosuppression (thrombocytopenia)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Oxaliplatin (Eloxatin)

A
  • alkylating agent; class: platinum analog
  • mechanism: doesn’t form carbonium intermediate or formally alkylate DNA; covalently bind nucleophilic sites on DNA (e.g., guanine N7) and is converted to active cytotoxic forms by reacting with water to form (+)charged, hydrated intermediates that react with DNA guanine, forming inter- and intrastand cross-links
  • treats: gastric and colorectal cancer
  • important: peripheral sensory neuropathy (cold-induced)
  • other side effects: neutropenia
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Methotrexate (Trexall)

A
  • antimetabolite; class: folate analog
  • mechanism: inhibits DHFR (converts dietary folate to THF; needed for thymidine and purine synthesis); given orally or intrathecally
  • treats: 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
  • important side effects: renal toxicity (crystallization in urine at high doses), hepatotoxicity (long-term, fibrosis/cirrhosis), reproductive (defective oogenesis or spermatogenesis, abortion)
  • other side effects: bone marrow (myelosuppression, spontaneous hemorrhage); GI toxicity (oral ulceration, stomatitis)
  • notes: can use leucovorin to prevent toxic effects of MTX, as healthy cells can take it up a lot better than tumor cells
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Pemetrexed (Alimta)

A
  • antimetabolite; class: folate analog
  • mechanism: polyglutamate forms that inhibit THF-dependent enzymes (e.g., DHFR, TS); metabolized to polyglutamate forms that inhibit THF-dependent enzymes (e.g., DHFR, thymidylate synthase (TS)
  • treats: colon cancer, mesothelioma, non-small cell lung cancer, pancreatic cancer
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

5-Fluorouracil (5-FU, Carac)

A
  • antimetabolite; class: pyramidine analog
  • mechanism: 5-FU→active metabolites: 5-FdUMP inhibits TS; 5-FdUTP incorporates into RNA & interferes with RNA function; prodrug ribosylated and phophosrylated into 5-FdUMP
  • treats: combination therapy for breast, colorectal, gastric, head and neck, cervical and pancreatic cancer; topically for basal cell carcinoma
  • important side effects: hand-foot syndrome (erythema, sensitivity of palms and soles), cardiac toxicity (acute chest pains)
  • other side effects: anorexia and nausea; mucosal ulcerations, stomatitis, diarrhea; thrombocytopenia and anemia
  • notes: leucovorin can potentiate effects of 5-FU; must be given IV (GI toxicity and rapid degradation + metabolism in gut and liver)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Cytarabine (AraC, Depocyt)

A
  • antimetabolite; class: pyramidine analog
  • mechanism: Ara-C converted by deoxycytidine kinase to Ara-CMP→Ara-CTP; terminates DNA synthesis as Ara-CTP
  • treats: AML (most effective treatment), ALL and blast phase CMLother side effects:
  • other side effects: severe myelosuppression (leucopenia, thrombocytopenia, anemia), GI tract toxicity (ulceration, stomatitis, diarrhea)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Gemcitabine (dFdC, Gemzar)

A
  • antimetabolite; class: pyramidine analog
  • mechanism: converted to active metabolites: dFdCDP inhibits ribonucleotide reductase (lowers deoxyribonucleotide); dFdCTP incorporates into DNA, terminating DNA synthesis
  • treats: pancreatic cancer; effective against non-small cell lung cancer, ovarian, bladder, esophageal, and head and neck cancer
  • other side effects: myelosuppression (leucopenia, thrombocytopenia, anemia), flu-like
  • notes: more effective against solid tumors than cytarabine
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

antimetabolites

A
  • structural analogs of folic acid or of the purine/pyramidine bases found in DNA; act in S-phase (cell cycle specific)
  • classes: folate, pyramidine, and purine analogs
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

6-Mercaptopurine (Purinethol)

A
  • antimetabolite; class: purine analog
  • mechanism: prodrug metabolized by (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
  • treats: maintain remission in acute ALL
  • important side effects: hepatotoxicity in prolonged use
  • other side effects: bone marrow suppression
  • notes: drug interaction with allopurinol (for gout), which inhibits xanthine oxidase; decrease 6-MP dose to avoid drug accumulation and toxicities
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Dactinomycin (Actinomycin D, Cosmegen)

A
  • DNA intercalating agent
  • mechanism: intercalates G-C base pairs of DNA, interfering with DNA-dependant RNA polymerase; also causes ssDNA breaks
  • treats: pediatric tumors (Wilms’ tumor, rhabdomyosarcoma Ewing’s sarcoma); choriocarcinoma in women
  • important side effects: hematopoietic suppression with pancytopenia
  • other side effects: anorexia, nausea, vomiting
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Daunorubicin (Cerubidine)

Idarubicin (Idamycin)

A
  • DNA intercalating agent; class: anthracyclines
  • mechanism: 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→ OH radical, which cleaves DNA
  • treats: AML
  • important side effects: irreversible dose-dependent cardiotoxicity; alopecia
  • other side effects: myelosuppression (neutropenia), stomatitis, GI disturbances
  • notes: dexrazoxane is cardio-protective
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Doxorubicin (Adriamicin, Doxil)

A
  • DNA intercalating; class: anthracycline
  • mechanism: 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→ OH radical, which cleaves DNA
  • treats: sarcomas, breast and lung carcinomas, malignant lymphomas
  • important side effects: irreversible dose-dependent cardiotoxicity; alopecia
  • other side effects: myelosuppression (neutropenia), stomatitis, GI disturbances
  • notes: dexrazoxane is cardio-protective
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Epirubicin (Ellence)

A
  • DNA intercalating; class: anthracycline
  • mechanism: 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→ OH radical, which cleaves DNA
  • treats: metastatic breast cancer, gastric cancer
  • important side effects: irreversible dose-dependent cardiotoxicity; alopecia
  • other side effects: myelosuppression (neutropenia), stomatitis, GI disturbances
  • notes: dexrazoxane is cardio-protective
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

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; CCNS
  • “cins”
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

Bleomycin (Blenoxane)

A
  • DNA intercalating
  • mechanism: acts in G2 phase of cell cycle (binds to DNA, producing ss- and dsDNA breaks)
  • treats: combination therapy for testicular tumors or Hodgkin’s disease; squamous cell carcinomas and lymphomas
  • important side effects: pulmonary toxicity (pulmonary fibrosis); cutaneous toxicity (hyperpigmentation, hyperkeratosis, erythema); hyperthermia
  • other side effects: minimally myelo- and immunosuppressive (often used in combo therapy); headache, nausea, vomiting
  • notes: dexrazoxane is cardio-protective
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
microtubule inhibitors
* Inhibit mitosis and cause metaphase arrest by interfering with microtubule function (tubulin (de)polymerization); CCS * classes: vinca alkaloids, taxanes,
26
Vinbla**stine** (Velban)
* MT inhibitor; class: vinca alkaloid * mechanism: blocks tubulin polymerization into MTs * treats: metastatic testicular tumors (with bleomycin, cisplatin); component of ABVD used for Hodgkin's disease * other side effects: myelosuppression, nausea, vomiting
27
Vincri**stine** (Oncovin)
* MT inhibitor; class: vinca alkaloid * mechanism: blocks tubulin polymerization into MTs * treats: Childhood ALL (with glucocorticoids); Hodgkin's and non-Hodgkin's lymphomas * important side effects: dose-limiting neurotoxicity (peripheral neuropathy) * other side effects: relatively low bone marrow toxicity
28
Pacli**taxel** (Taxol, Abraxane)
* MT inhibitor; class: taxane * mechanism: block MT depolymerization into tubulin * treats: metastatic breast, ovarian, lung, and head and neck cancers * important side effects: peripheral neuropathy * other side effects: neutropenia; hypersensitivity reactions
29
Doce**taxel** (Taxotere)
* MT inhibitor; class: taxane * mechanism: block MT depolymerization into tubulin * treats: metastatic breast, ovarian, lung, and head and neck cancers * important side effects: peripheral neuropathy * other side effects: neutropenia; hypersensitivity reactions
30
topoisomerase inhibitors
* prevent the resealing of topo I (ssDNA) and topo II (dsDNA); CCS * classes: epipodophyllotoxins, camptothecin analogs
31
Eto**poside** (Etopophos)
* topoisomerase inhibitor; class: epipodophyllotoxin * mechanism: inhibits topoisomerase II * treats: testicular carcinoma, lung cancer, and non-Hodgkin's lymphoma * other side effects: dose-limiting myelosuppression (neutropenia), oral mucositis
32
Teni**poside** (Vumon)
* topoisomerase inhibitor; class: epipodophyllotoxin * mechanism: inhibits topoisomerase II * treats: ALL * other side effects: dose-limiting myelosuppression (neutropenia), oral mucositis
33
Irin**otecan** (Camptosar)
* topoisomerase inhibitor; class: camptothecin analog * mechanism: inhibits topoisomerase I * treats: advanced colorectal cancer; lung, ovarian, cervical and brain tumors * other side effects: severe neutropenia, severe diarrhea
34
Top**otecan** (Hycamtin)
* topoisomerase inhibitor; class: camptothecin analog * mechanism: inhibits topoisomerase I * treats: ovarian and small cell lung cancer * other side effects: severe neutropenia, severe diarrhea
35
hormone therapy
* used in the treatment of hormone-dependent neoplasms * classes: glucocorticoids, SERMs, SERDs, aromatase inhibitors, GnRH blockers, nonsteroidal androgen receptor blockers
36
Predni**sone** (Meticorten)
* hormone therapy; class: glucocorticoid * mechanism: inhibit mitosis in lymphocytes * treats: ALL; combination for Hodgkin's, non-Hodkin's, multiple myeloma, and CLL
37
Dexametha**sone** (Decadron)
* hormone therapy; class: glucocorticoid * mechanism: inhibit mitosis in lymphocytes * treats: reduces edema in brain and spinal cord tumors with radiation therapy
38
Tamoxifen (Soltamox)
* hormone therapy; class: SERM * mechanism: competes with estradiol for binding to estrogen receptor * treats: ER+breast cancer, or as adjuvant therapy following primary breast tumor excision; prevention of breast cancer in high-risk patients * important side effects: hot flushes, hair loss; increased risk of endometrial cancer; increased risk of thromboembolic events * other side effects: nausea and vomiting
39
Fulvestrant (Faslodex)
* hormone therapy; class: SERD * mechanism: binds with much higher affinity (\>100-fold) to estrogen receptor than tamoxifen, inhibiting dimerization, increasing degradation, and reducing overall ER levels * treats: posmenopausal women with ER+ metastatic breast cancer
40
Aminoglutethamide (Cytadren)
* hormone therapy; class: aromatase inhibitor * mechanism: inhibits function of aromatase * treats: relatively weak, used against breast cancer * important side effects: significant
41
Anastrozole (Arimidex)
* hormone therapy; class: aromatase inhibitor * mechanism: inhibits function of aromatase * treats: First-line for ER+ breast cancer in postmenopausal women
42
Letrozole (Femara)
* hormone therapy; class: aromatase inhibitor * mechanism: inhibits function of aromatase * treats: ER+ breast cancer in postmenopausal women
43
Exemestane (Aromasin)
* hormone therapy; class: aromatase inhibitor * mechanism: **Steroidal** inhibitor of aromatase * treats: ER+ breast cancer in postmenopausal women
44
Leuprolide (Lupron) Goserelin (Zoladex)
* hormone therapy; class: GnRH analog * mechanism: binds GnRH receptor; inhibits release of FSH & LH * treats: androgen ablation therapy, along with AR blockers
45
Flutamide (Eulexin) Bicalutamide (Casodex)
* hormone therapy; class: nonsteroidal androgen-receptor blockers * mechanism: competes with androgen for AR binding * treats: androgen ablation therapy, along with GnRH blockers
46
Ima**tinib** (Gleevac)
* tyrosine kinase inhibitor * mechanism: inhibits Abl kinase by binding where ATP should go; also inhibits PDGFR and c-kit; **metabolized by cyt P450** * treats: first line therapy for CML; also, gastrointestinal tumor (GIST) * important side effects: nausea and vomiting, fluid retention, muscle cramps, arthralgia * other side effects: * notes: myelosuppression; 1 PO QDay
47
Gefi**tinib** (Iressa) Erlo**tinib** (Tarceva)
* tyrosine kinase inhibitor * mechanism: inhibit epidermal growth factor receptor (EGFR) tyrosine kinase * treats: non-small cell lung cancer
48
Nilo**tinib** (Tasigna)
* tyrosine kinase inhibitor * mechanism: inhibits Abl kinase * treats: imatinib-resistant CML * important side effects: myelosuppression * other side effects: QT prolongation, hepatotoxicity, electrolyte abnormalities * notes: 2 PO QDay
49
Dasa**tinib** (Sprycel)
* tyrosine kinase inhibitor * mechanism: inhibits Abl & Src kinases * treats: imatinib-resistant CML * important side effects: myelosuppression, bleeding, fluid retention, pulmonary arterial hypertension * other side effects: diarrhea, nausea and vomiting, weakness, infections * notes: 1 PO QDay
50
Rituxi**mab** (Rituxan)
* monoclonal antibody * mechanism: CD20 B-cell antibody that can directly activate apoptosis, activate complement, or activate cell-mediated cytotoxicity (e.g., T cells, NK cells) * treats: non-Hodgkin's lymphomas * important side effects: infusion reactions, tumor lysis syndrome (TLS), severe mucocutaneous reactions, progressive multifocal leukoencephalopathy (PML) * other side effects: skin reactions, irregular heartbeat, muscle or joint pain * notes: patients need careful monitoring
51
Trastuzu**mab** (Herceptin)
* monoclonal antibody * mechanism: unknown HER2/neu (ErbB2) receptor antibody mechanism (enhanced receptor endocytosis or blocking homo- or heterodimerization) * treats: **HER2/neu-overexpressing metastatic breast cancer** * important side effects: hypersentivity reaction; ventricular dysfunction * notes: usually combined with taxanes; enhances doxorubicin cardiotoxicity
52
Cetuxi**mab** (Erbitux)
* monoclonal antibody * mechanism: EGFR1 (ErbB1) * treats: EGFR+ metastatic colorectal cancer * important side effects: allergic reactions, sudden cardiac death, dermatologic problems, infections, renal failure, electrolyte abnormalities * other side effects: asthenia/malaise, fever, nausea, constipation, interstitial pneumonitis * notes: clinical trials, probably combine with cisplatin
53
Ipilimu**mab** (Yervoy)
* human monoclonal antibody * mechanism: Cytotoxic T-Lymphocyte Antigen 4 inhibitor; stimulates immune system * treats: melanoma
54
Vemura**fenib** (Zelboraf)
* serine/threonine kinase inhibitor * mechanism: inhibits oncogenic BRAF kinase * treats: unresectable Stage III and IV or metastatic melanomas w/BRAF mutations * important side effects: arthralgia, fatigue, photosensitivity, nausea, alopecia, diarrhea, QT prolongation * other side effects: cutaneous SCC, keratoacanthoma, new primary cutaneous melanoma * notes: superior to dacarbazine in Phase III trials
55
Dabra**fenib** (Tafinlar)
* serine/threonine kinase inhibitor * mechanism: inhibits oncogenic BRAF kinase * treats: unresectable Stage III and IV or metastatic melanomas w/BRAF mutations * important side effects: serious febrile drug reactions, uveitis and iritis, hyperglycemia, hyperkeratosis * other side effects: higher risk of developing cutaneous SCC, keratoacanthoma, new primary cutaneous melanoma vs. vemurafenib * notes: may cause male infertility
56
Trametinib (Mekinist)
* mechanism: Inhibits MEK * treats: unresectable Stage III and IV or metastatic melanomas w/BRAF mutations * important side effects: cardiomyopathy, retinal disorders, interstitial lung disease, serious skin toxicities * other side effects: rash, diarrhea, stomatitis, hypertension, pruritis * notes: may cause female infertility
57
Hydroxyurea (Hydrea)
* mechanism: inhibits ribonucleoside diphosphate reductase * treats: CML (replaced by Imatinib), polycythemia vera, essential thrombocythemia; treatment for sickle cell disease (increases Hb-F)
58
Retinoids
* mechanism: ATRA induces terminal differentiation in malignant immature promyelocytes, which subsequently apoptose * treats: APL * important side effects: "Leukocyte Activation Syndrome" (LAS), an increase in WBCs (fever, weight gain, respiratory distress, serosal effusion, renal failure) * notes: combined w/anthracyclines; corticosteroids used to block "LAS"
59
Arsenic Trioxide (Trisenox)
treats relapsed APL
60
Thalidomide (Thalomid)
treats multiple myeloma and myelodysplastic syndromes
61
Interferons
treats hairy-cell leukemia, CML, and AIDS-related Kaposi's sarcoma
62
ABVD
combination therapy of doxorubicin (adriamycin), bleomycin, vinblastine, dacarbazine
63
CHOP
combination therapy of cyclophosphamide, hydroxydoxorubicin, vincristine (oncovine), prednisone
64
MOPP
combination therapy of mechlorethamine, vincristine (oncovine), procarbazine, prednisone
65
CMF
combination therapy of cyclophosphamide, methotrexate, 5-fluorouracil
66
FEC
combination therapy of 5-fluorouracil, epirubicin, cyclophosphamide
67
Estradiol (valerate & cypionate) Estrone sulfate Equilin sulfate
* estradiol esters (steroidal) * mechanism: absorbed through skin, mucus membranes, GI Tract; body-wide distribution via sex-hormone binding globulin * treats: contraception, primary hypogonadism, postmenopausal hormone therapy * important side effects: weight gain, HTN; less commonly, may cause breast cancer, DVT, cervical and endometrial cancer * other side effects: nausea, breast tension/pain, vaginal bleeding, headache * notes: 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
68
Ethinyl estradiol Mestranol Quinestrol
* alkyl estrogen * mechanism: absorbed through skin, mucus membranes, GI Tract; body-wide distribution via sex-hormone binding globulin * used for contraception, primary hypogonadism, postmenopausal hormone therapy * important side effects: weight gain, HTN; less commonly, may cause breast cancer, DVT, cervical and endometrial cancer * other side effects: nausea, breast tension/pain, vaginal bleeding, headache * notes: 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
69
Diethylstilbestrol (DES)
* non-steroidal synthetic estrogen * important side effects: increased risk of clear cell adenocarcinoma of vagina & cervix
70
Tamoxifen citrate (Nolvadex)
* non-steroidal anti-estrogen; selective estrogen receptor modifier * mechanism: blocks estrogen from binding ER and causing growth in ER+ breast cancer * treats: ER+ breast cancer * important side effects: pro-estrogenic effect on uterine epithelium (increase risk of endometrial cancer); partial estrogen agonist in bone and endometrium * notes: anti-estrogenic effect on mammary epithelium; must be used in very high doses
71
Clomiphene citrate (Clomid)
* **non-steroidal anti-estrogen** * mechanism: blocks estrogen binding to hypothalamic receptors (no estradiol negative feedback on gonadotropins)→ increased secretion of gonadotropins & LH→ovulation * used to stimulate ovulation in patients who want to get pregnant * important side effects: hot flashes, multiple pregnancy * other side effects: stomach pain, headache, upset stomach, vomit * notes: sis-isomer (zuclomiphene) is a weak estrogen agonist; trans-isomer (enclomiphene) is a potent estrogen antagonist
72
Micronized progesterone
* natural progesterone * mechanism: binds to PR; decreased first-pass metabolism & enhanced dissolution due to micronization * contraception, hormone replacement therapy * important side effects: fatigue, drowsiness * notes: 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)
73
Transvaginal progesterone
* **natural progesterone** * mechanism: binds to PR; vaginal gel (uterine effects without first pass metabolism and minimal systemic side effects) * used for contraception, hormone replacement therapy * important side effects: fatigue, drowsiness * notes: 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)
74
Medroxyprogesterone Norethindrone Norgestrel Megestrol
* **synthetic progesterone** * used for contraception, hormone replacement therapy * important side effects: Edema, abdominal bloating; less commonly: strong androgenic effects (hirsutism, acne) * other side effects: Anxiety, irritability, depression, muscular pain; increased risk of thrombus and PE * notes: 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)
75
Monophasic Ortho-Novum
* combination OCP * mechanism: constant level of estrogen suppresses FSH, LH surge; progesterone suppresses LH surge, thickens cervical mucus, leads to endometrial atrophy * same side effects as estrogen and progesterone * notes: consistent dose of estrogen and progestin (only take 21 days)
76
Biphasic Ortho-Novum
* combination OCP * mechanism: constant level of estrogen suppresses FSH, LH surge; progesterone suppresses LH surge, thickens cervical mucus, leads to endometrial atrophy * same side effects as estrogen and progesterone * notes: fixed estrogen, progestin increased for days 11-21
77
Triphasic Ortho-Novum
* combination OCP * mechanism: constant level of estrogen suppresses FSH, LH surge; progesterone suppresses LH surge, thickens cervical mucus, leads to endometrial atrophy * same side effects as estrogen and progesterone * notes: fixed or variable estrogen, while progestin increases in 3 phases (1-7, 8-14, 15-21)
78
mini-pill
* progestin only OCP * mechanism is the same as progesterone * less effective than combination pill for contraception; use when patient has estrogen contraindication; good in lactating women (estrogen reduces milk production) * important side effects: more likely to produce irregular menstrual cycle (estrogen required to provide stability to endometrium) * other side effects: suppresses endometrial cancer
79
Levonorgestrel (Plan B)
* synthetic progestogen * mechanism of action is unknown * prevents implantation (must be taken within 72 hours of coitus) * side effects are likely the same as OCPs
80
Mifepristone (RU-486, Korlym)
* anti-progestin; glucocorticoid receptor antagonist * mechanism: competitively binds to PR (leading to detachment of fetus); glucocorticoid receptor antagonist * used for abortion; cushing's syndrome * notes: must take early in pregnancy (by day 49); PO; must be given by doctor in medical facility prepared for surgery if abortion incomplete
81
Silden**afil** citrate (Viagra) Varden**afil** HCl (Levitra) Tadal**afil** (Cialis)
* PDE5 inhibitor * Bind catalytic site of PDE5; inhibits PDE5 breakdown of cGMP→ decreased Ca→ smooth muscle relaxation→ erection * treats: ED (does not trigger an automatic erection, but improves response to sexual stimulation) * important side effects: headache, dizziness, change in vision (NAION) * other side effects: flushing, upset stomach, stuffy or runny nose, UTI, diarrhea * notes: PO (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)
82
Indomethacin (Indocin) Naproxen (Aleve)
* non-selective NSAID * mechanism: eliminate pain; reduce inflammation (does not slow disease progression) * treats RA and acute gouty arthritis * important side effects: gastric and uodenal ulcers
83
COX-2 inhibitors
* selective NSAID * mechanism: elimates pain; reduce inflammation (does not slow disease progression) * Superseding conventional NSAIDs for RA * important side effects: 50% fewer gastric and duodenal ulcers than traditional NSAIDs
84
quinolones
* DMARD (antimalarial) * mechanism: reduces T-cell activation and chemotaxis * treats: RA, SLE * important side effects: retinal damage (chloroquine) * used for patients who no longer respond to NSAIDS or can't tolerate other DMARDs
85
glucocorticoids (corticosteroids)
* DMARD * mechanism: inhibits phospholipase A2 (inhibiting release of arachidonic acid and, thus, formation of prostaglandins) and inhibits cytokine production (which prevents induction of COX-2) * treats RA; acute gouty arthritis (intraarticular injection for relief of acute monoarticular gout) * important side effects: cushingoid syndrome * Started initially (fast acting) before other drugs become effective Can give orally or intra-articularly
86
Sulfasalazine (Azulfidine)
* DMARD * mechanism: likely inhibition of IL-1 & TNF-alpha release * treats RA * important side effects: N/V, skin rashes, neutropenia (30% of patient discontinue drug) * other side effects: headaches * acts quicker than other drugs
87
Methotrexate (Trexall)
* DMARD (immunosuppressive) * mechanism: inhibition of aminoimidazolecarboxamide (AICAR) transformylase and thymidylate synthetase, with secondary effects on PMN chemotaxis; causes adenosine accumulation, which inhibits inflammation * treats: RA (gold standard) * important side effects: nausea, stomatitis, hepatotoxicity (rare) * takes several weeks to start working
88
Leflunomide (Arava)
* DMARD (immunosuppressive) * mechanism: inhibits dihydroorotate dehydrogenase (DHODH), which inhibits T-lymphocyte response to stimuli * treats RA * important side effects: diarrhea, hepatotoxity * takes several weeks to start working; oral prodrug
89
Etanercept (Enbrel)
* biological response modifier * mechanism: blocks binding of TNF to TNF receptors * treats RA * 2x weekly subQ injections
90
Infliximab (Remicade)
* biological response modifier * mechanism: blocks binding of TNF to TNF receptors * treats RA * important side effects: antigenic response to murine monoclonal Ab
91
Adalimumab (Humira)
* biological response modifier * mechanism: blocks binding of TNF to TNF receptors * treats RA * 2x monthly injections; fully human so no antigenic response
92
Golimumab Certolizumab
* biological response modifier * mechanism: blocks binding of TNF to TNF receptors * treats RA * important side effects: risk of serious infection * certolizumab is conjugated to PEG for stabilization
93
Anakinra (Kineret)
* biological response modifier * mechanism: IL-1 receptor antagonist * treats RA * short (6 hr) plasma half-life; daily treatment with high doses
94
Tocilizumab (Actemra)
* biological response modifier * mechanism: IL-6 receptor antagonist * treats RA
95
Rituximab (Rituxan)
* biological response modifier * mechanism: anti-CD20 mAb, reduces circulating B cells * treats RA * important side effects: infections, hypersensitivity reactions * used for RA refractory to TNF-alpha inhibitors
96
Abatacept (Orencia)
* biologic response modifier * mechanism: inhibits T-cell activation and induces T-cell apoptosis * treats: RA * important side effects: headaches, infections * used in patients for RA refractory to MTX or TNF-alpha inhibitors
97
Tofacitinib
* biologic response modifier * mechanism: inhibition of JAK 1 & 3 which inhibits production of inflammatory mediators * treats: RA * important side effects: Upper respiratory tract infections; headaches, diarrhea * other side effects: malignancies
98
cochicine (Colcrys)
* mechanism: prevents tubulin polymerization→ inibition of leukocyte migration, phagocytosis, and release of cytokines * treats: acute gouty arthritis * important side effects: long-term use causes peripheral neuropathy & neutropenia * other side effects: nausea, vomiting, abdominal pain, troublesome diarrhea * works in 12-24 hours
99
Probenecid (Benemid)
* uricosuric agent * mechanism: compete with urate at anionic transport site of renal tubule and inhibit urate reabsorption * treats: chronic tophaceous gout * important side effects: urate crystal mobilization and acute gouty arthritis * other side effects: GI irritation * secretion of some weak acids (e.g., penicillin) is reduced
100
Allopurinol (Zyloprim)
* mechanism: reduces uric acid synthesis by inhibiting xanthine oxidase (competitive inhibition)→ alloxanthine (non-competitive inhibitor of xanthine oxidase) * treats: chronic tophaceous gout * important side effects: acute attacks of gouty arthritis early in treatment due to mobilization of urate crystals
101
Febuxostat (Uloric)
* mechanism: non-purine, non-competitive antagonist of xanthine oxidase * treats: chronic tophaceous gout * important side effects: nausea, rash, arthralgias * $$$
102
Pegloticase (Krystexxa)
* recombinant, stabilized uricase * mechanism: converts uric acid to allantoin * treats: chronic tophaceous gout
103
Afatinib (Gilotrif)
* tyrosine kinase inhibitor * mechanism: inhibits EGFR tyrosine kinase * treats non-small cell lung cancer * important side effects: diarrhea, vomiting, rash/dermatitis acneiform, stomatitis, paronichia, dry skin, pruritis, decreased appetite * other side effects: Dyspnea, fatigue, pulmonary toxicity, pneumonia, sepsis * 1 PO QDay
104
Lapatinib (Tykerb)
* tyrosine kinase inhibitor * mechanism: inhibits EGFR and ErbB2 (HER2) tyrosine kinase * treats: HER2+ advanced or metastatic breast cancer; hormone+/HER2+ metastatic breast cancer in post menopausal women * important side effects: hepatotoxicity, nausea, diarrhea, fatigue, rashes, QT-prolongation * other side effects: decreased LV function when combined with capecitabine, hypokalemia, hypomagnesemia * 1 PO QDay
105
Ado-trastuzumab emtansine (Kadcyla)
* Ab-drug conjugate * mechanism: conjugate undergoes receptor-dependent internalization & drug released inside cel * treats: HER+ metastatic breast cancer patients with prior treatment history of trastuzumab and/or taxanel * important side effects: fatigue, nausea, musculoskeletal pain, thrombocytopenia, headache, hypokalemia, peripheral neuropathy, ventricular dysfunction, interstitial lung disease * other side effects: interstitial lung disease, infusion-associated reactions, hepatotoxicity, birth defects
106
Panitumumab (Vectibix)
* fully human monoclonal antibody * mechanism: EGFR (ErbB1) * treats: EGFR-expressing metastatic colorectal cancers resistant to fluoropyrimidine, oxaliplatin, and irinotecan regimens * important side effects: skin toxicities, paronychia, hypomagnesemia, fatigue, abdominal pain, nausea, diarrhea, constipation
107
Nivolumab (Opdivo)
* human monoclona Ab * mechanism: inhibits programmed cell death protein 1 (PD-1) * treats: 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 * important side effects: rash, itching, cough, upper respiratory tract infections, edema, fatigue, shortness of breath, musculoskeletal pain, decreased appetite, nausea, constipation * other side effects: severe immune-mediated side effects on healthy organs (lung, colon, liver, kidneys, hormone-producing glands

GER Pharm Unit 1 (1 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2025 Bold Learning Solutions. Terms and Conditions