PHARM CANCER.ENDOCRINE Flashcards

1
Q

Constant proportion of cell population killed rather than a constant number

A

Log-kill hypothesis

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2
Q

Treatment with cancer chemotherapy at high doses every 3-4 weeks, too toxic to be used continuously

A

Pulse therapy

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3
Q

Toxic effect of anticancer drug can be lessened by rescue agents

A

Rescue therapy

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4
Q

Drug used concurrently with toxic anticancer agents to reduce renal precipitation of urates

A

Allopurinol

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5
Q

Pyrimidine analog that causes “Thiamine-less death” given with leucovorin rescue

A

5-flouracil (5-FU)

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6
Q

Drug used in cancer therapy causes Cushing-like symptoms

A

Prednisone

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7
Q

Side effect of Mitomycin

A

SEVERE myelosuppression

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8
Q

MOA of cisplatin

A

Alkylating agent

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9
Q

Common toxicities of cisplatin

A

Nephro and ototoxicity

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10
Q

Analog of hypoxanthine, needs HGPRTase for activation

A

6-mercaptopurine (6-MP)

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11
Q

Interaction with this drug requires dose reduction of 6-MP

A

Allopurinol

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12
Q

May protect against doxorubicin cardio-toxicity by chelating iron

A

Dexrazoxane

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13
Q

Blows DNA (breaks DNA strands), limiting SE in pulmonary fibrosis

A

Bleomycin

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14
Q

MOPP regimen used in Hodgkin’s disease (HD)

A

Mechlorethamine + oncovorin (vincristine) + procarbazine, and prednisone

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15
Q

Regimen used for non-Hodgkin’s lymphoma

A

CHOP (cyclophosphamide, oncovin(vincristine), doxorubicin and prednisone), rituximab (rituxan)

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16
Q

Regimen used for breast cancer

A

CMF (cyclophosphamide, methotrexate, and fluorouracil) and tamoxifen if ER+

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17
Q

Alkylating agent, vesicant that causes tissue damage with extravasation

A

Mechlorethamine

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18
Q

Anticancer drug also used in RA, produces acrolein in urine that leads to hemorrhagic cystitis

A

Cyclophosphamide

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19
Q

Prevention of cyclophosphamide induced hemorrhagic cystitis

A

Hydration and mercaptoethanesulfonate (MESNA)

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20
Q

Microtubule inhibitor that causes peripheral neuropathy, foot drop (eg. ataxia), and “pins and needles” sensation

A

Vincristine

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21
Q

Binds tubulin and prevents the disassembly of microtubules during the M phase of the cell cycle inducing mitotic arrest

A

Paclitaxel (taxol)

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22
Q

Toxicities include nephrotoxicity and ototoxicity, leading to a severe interaction with aminoglycosides

A

Cisplatin

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23
Q

Agent similar to cisplatin, less nephrotoxic, but greater myelosuppression

A

Carboplatin

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24
Q

Converts asparagine to aspartate and ammonia, denies cancer cells of essential AA (asparagine)

A

L-asparaginase

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25
Q

Used for hairy cell leukemia; it stimulates NK cells

A

Interferon alpha

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26
Q

Anti-androgen used for prostate cancer

A

Flutamide (Eulexin)

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27
Q

Anti-estrogen used for estrogen receptor + breast cancer

A

Tamoxifen

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28
Q

Some cell cycle specific anti-cancer drugs

A

Bleomycin, vinca alkaloids, antimetabolites (eg., 5-FU, 6-MP, methotrexate, etoposide)

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29
Q

Some cell cycle non-specific drugs

A

Alkylating agents (eg., mechlorethamine, cyclophosphamide), antibiotics (doxorubicin, daunorubicin), cisplatin, nitrosourea

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30
Q

Anti-emetics used in association with anti-cancer drugs that are 5-HT3 (serotonin receptor subtype ) antagonist

A

Odansetron, granisetron, dolasetron, palonosetron

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31
Q

Nitrosoureas with high lipophilicity, used for brain tumors

A

Carmustine (BCNU) and lomustine (CCNU)

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32
Q

Alkylating agent that produces disulfiram-like reaction with ethanol

A

Procarbazine

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33
Q

Somatostatin (SRIF) analog used for acromegaly, carcinoid, glucagonoma and other GH producing pituitary tumors

A

Octreotide

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34
Q

Somatotropin (GH) analog used in GH deficiency (dwarfism)

A

Somatrem

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35
Q

GHRH analog used as diagnostic agent

A

Sermorelin

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36
Q

GnRH agonist used for infertility or different types of CA depending on pulsatile or steady usage respectively

A

Leuprolide

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37
Q

GnRH antagonist with more immediate effects, used for infertility

A

Ganirelix

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38
Q

Hormone inhibiting prolactin release

A

Dopamine

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39
Q

ACTH analog used for diagnosis of patients with corticosteroid abnormality

A

Cosyntropin

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40
Q

Synthetic analog of ADH hormone used for diabetes insipidus and nocturnal enuresis

A

Desmopressin (DDAVP)

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41
Q

Agent of choice for the treatment of hypothyroidism

A

Levothyroxine (T4)

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42
Q

An isomer of T3 which may be used in myxedema coma

A

Liothyronine (T3)

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43
Q

Anti-thyroid drugs

A

Thioamides (methimazole, propylthiouracil), potassium iodide, radioactive iodine (131I)

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44
Q

Thioamide agents used in hyperthyroidism

A

Methimazole and propylthiouracil (PTU)

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45
Q

Thioamide less likely to cross placenta, inhibits peripheral conversion of T4 to T3 in high doses, and indicated for pregnant women in 1st trimester

A

Propylthiouracil (PTU)

46
Q

Propylthiouracil (PTU) mechanism of action

A

Inhibits thyroid peroxidase

47
Q

Can be effective for short term therapy of thyroid storm, but after several weeks of therapy causes an exacerbation of hyperthyroidism

A

Iodide salts (potassium iodide)

48
Q

Permanently cures thyrotoxicosis, patients will need thyroid replacement therapy thereafter. Contraindicated in pregnancy

A

Radioactive iodine

49
Q

Used for the symptomatic treatment of thyrotoxicosis by blocking cardiac adverse effects

A

Beta-blockers such as propranolol and esmolol

50
Q

3 zones of adrenal cortex and their products

A

Glomerulosa (mineralocorticoids), fasciculata (glucocorticoid=GC), and reticularis (adrenal androgens)

51
Q

Pneumonic for 3 zones of adrenal cortex

A

GFR

52
Q

Used for Addison’s disease, Congenital Adrenal Hyperplasia (CAH), inflammation, allergies, and asthma (as a local inhalation)

A

Glucocorticoids

53
Q

Short acting GC’s

A

Cortisone and hydrocortisone (equivalent to cortisol)

54
Q

Intermediate acting GC’s

A

Prednisone, methylprednisolone, prednisolone, oaramethasone, fluprednisone and triamcinolone

55
Q

Long acting GC’s

A

Betamethasone, dexamethasone, and paramethasone

56
Q

Mineralocorticoids

A

Fludrocortisone and deoxycorticosterone

57
Q

Some side effects of corticosteroids

A

Hyperglycemia, Osteopenia, impaired wound healing, inc. risk of infection, inc. appetite, HTN, edema, PUD, euphoria, psychosis

58
Q

Period of time of therapy after which GC therapy will need to be tapered

A

5-7 days

59
Q

Used for Cushing’s syndrome (increased corticosteroid) and sometimes for adrenal function test

A

Metyrapone

60
Q

Inhibits conversion of cholesterol to pregnenolone therefore inhibiting corticosteroid synthesis

A

Aminoglutethimide

61
Q

Antifungal agent used for inhibition of all gonadal and adrenal steroids

A

Ketoconazole

62
Q

Antiprogestin used as potent antagonist of GC receptor

A

Mifepristone

63
Q

Diuretic used to antagonize aldosterone receptors

A

Spironolactone

64
Q

Common SE of spironolactone

A

Gynecomastia and hyperkalemia

65
Q

Slightly increased risk of breast cancer, endometrial cancer, heart disease (questionable), has beneficial effects on bone loss

A

Estrogen

66
Q

Antiestrogen drugs used for fertility and breast cancer respectively

A

Clomiphene and tamoxifen

67
Q

Common SE of tamoxifen and raloxifene

A

Hot flashes

68
Q

Selective estrogen receptor modulator (SERM) used for prevention of osteoporosis and currently being tested for treatment of breast cancer (Stars study)

A

Raloxifene

69
Q

Non-steroidal estrogen agonist causes clear cell adenocarcinoma of the vagina in daughters of women who used it during pregnancy

A

Diethylstilbestrol (DES)

70
Q

Estrogen mostly used in oral contraceptives (OC)

A

Ethinyl estradiol and mestranol

71
Q

Anti-progesterone used as abortifacient

A

Mifepristone (RU-486)

72
Q

Constant low dose of estrogen and increasing dose of progestin for 21 days (last 5 days are sugar pills or iron prep)

A

Combination oral contraceptives (OC)

73
Q

Oral contraceptive available in a transdermal patch

A

Ortho-Evra

74
Q

Converted to more active form DHT by 5 alpha-reductase

A

Testosterone

75
Q

5 alpha-reductase inhibitor used for benign prostatic hyperplasia (BPH) and male pattern baldness

A

Finasteride (Proscar and Propecia respectively)

76
Q

Anabolic steroid that has potential for abuse

A

Nandrolone and stanozolol

77
Q

Anti-androgen used for hirsutism in females

A

Cyproterone acetate

78
Q

Alpha cells in the pancreas produce

A

Produce glucagon

79
Q

Beta cells in the pancreas produce

A

Produce insulin

80
Q

Beta cells are found

A

Islets of Langerhans

81
Q

Delta cells in the pancreas produce

A

Produce Somatostatin

82
Q

Product of proinsulin cleavage used to assess insulin production

A

C-peptide

83
Q

Endogenous insulin

A

Normal C-peptide

84
Q

Very rapid acting insulin, having fastest onset and shortest duration of action

A

Lispro (Humalog)/Apidra (glulisine)

85
Q

Rapid acting, crystalline zinc insulin used to reverse acute hyperglycemia

A

Regular (Humulin R)

86
Q

Long acting insulin

A

NPH insulin

87
Q

Ultra long acting insulin, has over a day duration of action

A

Glargine (Lantus)

88
Q

Major side effect of insulin

A

Hypoglycemia

89
Q

Important in synthesis of glucose to glycogen in the liver

A

GLUT 2

90
Q

Important in muscle and adipose tissue for glucose transport across muscles and TG storage by lipoprotein lipase activation

A

GLUT 4

91
Q

Examples of alpha-glucosidase inhibitors (AGI)

A

Acarbose, miglitol

92
Q

MOA of AGI’s

A

Act on intestine, delay absorption of glucose

93
Q

SE of AGI’s

A

Flatulence (do not use beano to tx), diarrhea, abdominal cramps

94
Q

Alpha-glucosidase inhibitor associated with elevation of LFT’s

A

Acarbose

95
Q

Amino acid derivative for treatment of Type II diabetes

A

Nateglinide

96
Q

MOA of nateglinide

A

Stimulates rapid and transient release of insulin through closure of the ATP-sensitive K+ channel

97
Q

Biguanide

A

Metformin

98
Q

Drugs available in combination with metformin

A

Acroplus Met progutazone and metformin, Janumet and Janumet XR Sitagliptin and Metformin, Glyburide, glipizide, and rosiglitazone

99
Q

MOA of metformin

A

Decreases hepatic glucose production and intestinal glucose absorption; increase insulin sensitivity

100
Q

Most important potential SE of metformin

A

Lactic acidosis

101
Q

Meglitinide

A

Repaglinide

102
Q

MOA of repaglinide

A

Insulin release from pancreas; faster and shorter acting than sulfonylurea

103
Q

First generation sulfonylurea

A

Chlorpropamide, tolbutamide, tolazamide, etc.

104
Q

Second generation sulfonylurea

A

Glyburide, glipizide, glimepiride, etc.

105
Q

MOA of both generations

A

Insulin release from pancreas by modifying K+ channels

106
Q

Common SE of sulfonylureas, repaglinide, and nateglinide

A

Hypoglycemia

107
Q

Sulfonylurea NOT recommended for elderly because of very long half life

A

Chlorpropamide

108
Q

Thiazolidinediones

A

Pioglitazone, Rosiglitazone, Troglitazone (withdrawn/d from market)

109
Q

Reason troglitazone was withdrawn from market

A

Hepatic toxicity

110
Q

MOA of thiazolindinediones

A

Stimulate PPAR-gamma receptor to regulate CHO and lipid metabolism

111
Q

SE of Thiazolindinediones

A

Edema, mild anemia; interaction with drugs that undergo CytP450 3A4 metabolism; if used over one year, bladder Cancer; with CHF, may cause new or worsening CHF

112
Q

Hyperglycemic agent that increases cAMP and results in glycogenolysis, gluconeogenesis, reverses hypoglycemia, also used to reverse severe beta-blocker overdose and smooth muscle relaxation

A

Glucagon