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Flashcards in PHARM CANCER.ENDOCRINE Deck (112):
1

Constant proportion of cell population killed rather than a constant number

Log-kill hypothesis

2

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

Pulse therapy

3

Toxic effect of anticancer drug can be lessened by rescue agents

Rescue therapy

4

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

Allopurinol

5

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

5-flouracil (5-FU)

6

Drug used in cancer therapy causes Cushing-like symptoms

Prednisone

7

Side effect of Mitomycin

SEVERE myelosuppression

8

MOA of cisplatin

Alkylating agent

9

Common toxicities of cisplatin

Nephro and ototoxicity

10

Analog of hypoxanthine, needs HGPRTase for activation

6-mercaptopurine (6-MP)

11

Interaction with this drug requires dose reduction of 6-MP

Allopurinol

12

May protect against doxorubicin cardio-toxicity by chelating iron

Dexrazoxane

13

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

Bleomycin

14

MOPP regimen used in Hodgkin's disease (HD)

Mechlorethamine + oncovorin (vincristine) + procarbazine, and prednisone

15

Regimen used for non-Hodgkin's lymphoma

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

16

Regimen used for breast cancer

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

17

Alkylating agent, vesicant that causes tissue damage with extravasation

Mechlorethamine

18

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

Cyclophosphamide

19

Prevention of cyclophosphamide induced hemorrhagic cystitis

Hydration and mercaptoethanesulfonate (MESNA)

20

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

Vincristine

21

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

Paclitaxel (taxol)

22

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

Cisplatin

23

Agent similar to cisplatin, less nephrotoxic, but greater myelosuppression

Carboplatin

24

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

L-asparaginase

25

Used for hairy cell leukemia; it stimulates NK cells

Interferon alpha

26

Anti-androgen used for prostate cancer

Flutamide (Eulexin)

27

Anti-estrogen used for estrogen receptor + breast cancer

Tamoxifen

28

Some cell cycle specific anti-cancer drugs

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

29

Some cell cycle non-specific drugs

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

30

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

Odansetron, granisetron, dolasetron, palonosetron

31

Nitrosoureas with high lipophilicity, used for brain tumors

Carmustine (BCNU) and lomustine (CCNU)

32

Alkylating agent that produces disulfiram-like reaction with ethanol

Procarbazine

33

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

Octreotide

34

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

Somatrem

35

GHRH analog used as diagnostic agent

Sermorelin

36

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

Leuprolide

37

GnRH antagonist with more immediate effects, used for infertility

Ganirelix

38

Hormone inhibiting prolactin release

Dopamine

39

ACTH analog used for diagnosis of patients with corticosteroid abnormality

Cosyntropin

40

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

Desmopressin (DDAVP)

41

Agent of choice for the treatment of hypothyroidism

Levothyroxine (T4)

42

An isomer of T3 which may be used in myxedema coma

Liothyronine (T3)

43

Anti-thyroid drugs

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

44

Thioamide agents used in hyperthyroidism

Methimazole and propylthiouracil (PTU)

45

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

Propylthiouracil (PTU)

46

Propylthiouracil (PTU) mechanism of action

Inhibits thyroid peroxidase

47

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

Iodide salts (potassium iodide)

48

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

Radioactive iodine

49

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

Beta-blockers such as propranolol and esmolol

50

3 zones of adrenal cortex and their products

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

51

Pneumonic for 3 zones of adrenal cortex

GFR

52

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

Glucocorticoids

53

Short acting GC's

Cortisone and hydrocortisone (equivalent to cortisol)

54

Intermediate acting GC's

Prednisone, methylprednisolone, prednisolone, oaramethasone, fluprednisone and triamcinolone

55

Long acting GC's

Betamethasone, dexamethasone, and paramethasone

56

Mineralocorticoids

Fludrocortisone and deoxycorticosterone

57

Some side effects of corticosteroids

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

58

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

5-7 days

59

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

Metyrapone

60

Inhibits conversion of cholesterol to pregnenolone therefore inhibiting corticosteroid synthesis

Aminoglutethimide

61

Antifungal agent used for inhibition of all gonadal and adrenal steroids

Ketoconazole

62

Antiprogestin used as potent antagonist of GC receptor

Mifepristone

63

Diuretic used to antagonize aldosterone receptors

Spironolactone

64

Common SE of spironolactone

Gynecomastia and hyperkalemia

65

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

Estrogen

66

Antiestrogen drugs used for fertility and breast cancer respectively

Clomiphene and tamoxifen

67

Common SE of tamoxifen and raloxifene

Hot flashes

68

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

Raloxifene

69

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

Diethylstilbestrol (DES)

70

Estrogen mostly used in oral contraceptives (OC)

Ethinyl estradiol and mestranol

71

Anti-progesterone used as abortifacient

Mifepristone (RU-486)

72

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

Combination oral contraceptives (OC)

73

Oral contraceptive available in a transdermal patch

Ortho-Evra

74

Converted to more active form DHT by 5 alpha-reductase

Testosterone

75

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

Finasteride (Proscar and Propecia respectively)

76

Anabolic steroid that has potential for abuse

Nandrolone and stanozolol

77

Anti-androgen used for hirsutism in females

Cyproterone acetate

78

Alpha cells in the pancreas produce

Produce glucagon

79

Beta cells in the pancreas produce

Produce insulin

80

Beta cells are found

Islets of Langerhans

81

Delta cells in the pancreas produce

Produce Somatostatin

82

Product of proinsulin cleavage used to assess insulin production

C-peptide

83

Endogenous insulin

Normal C-peptide

84

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

Lispro (Humalog)/Apidra (glulisine)

85

Rapid acting, crystalline zinc insulin used to reverse acute hyperglycemia

Regular (Humulin R)

86

Long acting insulin

NPH insulin

87

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

Glargine (Lantus)

88

Major side effect of insulin

Hypoglycemia

89

Important in synthesis of glucose to glycogen in the liver

GLUT 2

90

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

GLUT 4

91

Examples of alpha-glucosidase inhibitors (AGI)

Acarbose, miglitol

92

MOA of AGI's

Act on intestine, delay absorption of glucose

93

SE of AGI's

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

94

Alpha-glucosidase inhibitor associated with elevation of LFT's

Acarbose

95

Amino acid derivative for treatment of Type II diabetes

Nateglinide

96

MOA of nateglinide

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

97

Biguanide

Metformin

98

Drugs available in combination with metformin

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

99

MOA of metformin

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

100

Most important potential SE of metformin

Lactic acidosis

101

Meglitinide

Repaglinide

102

MOA of repaglinide

Insulin release from pancreas; faster and shorter acting than sulfonylurea

103

First generation sulfonylurea

Chlorpropamide, tolbutamide, tolazamide, etc.

104

Second generation sulfonylurea

Glyburide, glipizide, glimepiride, etc.

105

MOA of both generations

Insulin release from pancreas by modifying K+ channels

106

Common SE of sulfonylureas, repaglinide, and nateglinide

Hypoglycemia

107

Sulfonylurea NOT recommended for elderly because of very long half life

Chlorpropamide

108

Thiazolidinediones

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

109

Reason troglitazone was withdrawn from market

Hepatic toxicity

110

MOA of thiazolindinediones

Stimulate PPAR-gamma receptor to regulate CHO and lipid metabolism

111

SE of Thiazolindinediones

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

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

Glucagon