PHARM CANCER.ENDOCRINE Flashcards by Anna Miller

Constant proportion of cell population killed rather than a constant number

Log-kill hypothesis

How well did you know this?

Not at all

Perfectly

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

Pulse therapy

How well did you know this?

Not at all

Perfectly

Toxic effect of anticancer drug can be lessened by rescue agents

Rescue therapy

How well did you know this?

Not at all

Perfectly

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

Allopurinol

How well did you know this?

Not at all

Perfectly

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

5-flouracil (5-FU)

How well did you know this?

Not at all

Perfectly

Drug used in cancer therapy causes Cushing-like symptoms

Prednisone

How well did you know this?

Not at all

Perfectly

Side effect of Mitomycin

SEVERE myelosuppression

How well did you know this?

Not at all

Perfectly

MOA of cisplatin

Alkylating agent

How well did you know this?

Not at all

Perfectly

Common toxicities of cisplatin

Nephro and ototoxicity

How well did you know this?

Not at all

Perfectly

Analog of hypoxanthine, needs HGPRTase for activation

6-mercaptopurine (6-MP)

How well did you know this?

Not at all

Perfectly

Interaction with this drug requires dose reduction of 6-MP

Allopurinol

How well did you know this?

Not at all

Perfectly

May protect against doxorubicin cardio-toxicity by chelating iron

Dexrazoxane

How well did you know this?

Not at all

Perfectly

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

Bleomycin

How well did you know this?

Not at all

Perfectly

MOPP regimen used in Hodgkin’s disease (HD)

Mechlorethamine + oncovorin (vincristine) + procarbazine, and prednisone

How well did you know this?

Not at all

Perfectly

Regimen used for non-Hodgkin’s lymphoma

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

How well did you know this?

Not at all

Perfectly

Regimen used for breast cancer

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

How well did you know this?

Not at all

Perfectly

Alkylating agent, vesicant that causes tissue damage with extravasation

Mechlorethamine

How well did you know this?

Not at all

Perfectly

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

Cyclophosphamide

How well did you know this?

Not at all

Perfectly

Prevention of cyclophosphamide induced hemorrhagic cystitis

Hydration and mercaptoethanesulfonate (MESNA)

How well did you know this?

Not at all

Perfectly

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

Vincristine

How well did you know this?

Not at all

Perfectly

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

Paclitaxel (taxol)

How well did you know this?

Not at all

Perfectly

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

Cisplatin

How well did you know this?

Not at all

Perfectly

Agent similar to cisplatin, less nephrotoxic, but greater myelosuppression

Carboplatin

How well did you know this?

Not at all

Perfectly

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

L-asparaginase

How well did you know this?

Not at all

Perfectly

Used for hairy cell leukemia; it stimulates NK cells

Interferon alpha

Anti-androgen used for prostate cancer

Flutamide (Eulexin)

Anti-estrogen used for estrogen receptor + breast cancer

Tamoxifen

Some cell cycle specific anti-cancer drugs

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

Some cell cycle non-specific drugs

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

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

Odansetron, granisetron, dolasetron, palonosetron

Nitrosoureas with high lipophilicity, used for brain tumors

Carmustine (BCNU) and lomustine (CCNU)

Alkylating agent that produces disulfiram-like reaction with ethanol

Procarbazine

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

Octreotide

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

Somatrem

GHRH analog used as diagnostic agent

Sermorelin

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

Leuprolide

GnRH antagonist with more immediate effects, used for infertility

Ganirelix

Hormone inhibiting prolactin release

Dopamine

ACTH analog used for diagnosis of patients with corticosteroid abnormality

Cosyntropin

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

Desmopressin (DDAVP)

Agent of choice for the treatment of hypothyroidism

Levothyroxine (T4)

An isomer of T3 which may be used in myxedema coma

Liothyronine (T3)

Anti-thyroid drugs

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

Thioamide agents used in hyperthyroidism

Methimazole and propylthiouracil (PTU)

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)

Propylthiouracil (PTU) mechanism of action

Inhibits thyroid peroxidase

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)

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

Radioactive iodine

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

Beta-blockers such as propranolol and esmolol

3 zones of adrenal cortex and their products

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

Pneumonic for 3 zones of adrenal cortex

GFR

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

Glucocorticoids

Short acting GC's

Cortisone and hydrocortisone (equivalent to cortisol)

Intermediate acting GC's

Prednisone, methylprednisolone, prednisolone, oaramethasone, fluprednisone and triamcinolone

Long acting GC's

Betamethasone, dexamethasone, and paramethasone

Mineralocorticoids

Fludrocortisone and deoxycorticosterone

Some side effects of corticosteroids

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

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

5-7 days

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

Metyrapone

Inhibits conversion of cholesterol to pregnenolone therefore inhibiting corticosteroid synthesis

Aminoglutethimide

Antifungal agent used for inhibition of all gonadal and adrenal steroids

Ketoconazole

Antiprogestin used as potent antagonist of GC receptor

Mifepristone

Diuretic used to antagonize aldosterone receptors

Spironolactone

Common SE of spironolactone

Gynecomastia and hyperkalemia

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

Estrogen

Antiestrogen drugs used for fertility and breast cancer respectively

Clomiphene and tamoxifen

Common SE of tamoxifen and raloxifene

Hot flashes

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

Raloxifene

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

Diethylstilbestrol (DES)

Estrogen mostly used in oral contraceptives (OC)

Ethinyl estradiol and mestranol

Anti-progesterone used as abortifacient

Mifepristone (RU-486)

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)

Oral contraceptive available in a transdermal patch

Ortho-Evra

Converted to more active form DHT by 5 alpha-reductase

Testosterone

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

Finasteride (Proscar and Propecia respectively)

Anabolic steroid that has potential for abuse

Nandrolone and stanozolol

Anti-androgen used for hirsutism in females

Cyproterone acetate

Alpha cells in the pancreas produce

Produce glucagon

Beta cells in the pancreas produce

Produce insulin

Beta cells are found

Islets of Langerhans

Delta cells in the pancreas produce

Produce Somatostatin

Product of proinsulin cleavage used to assess insulin production

C-peptide

Endogenous insulin

Normal C-peptide

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

Lispro (Humalog)/Apidra (glulisine)

Rapid acting, crystalline zinc insulin used to reverse acute hyperglycemia

Regular (Humulin R)

Long acting insulin

NPH insulin

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

Glargine (Lantus)

Major side effect of insulin

Hypoglycemia

Important in synthesis of glucose to glycogen in the liver

GLUT 2

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

GLUT 4

Examples of alpha-glucosidase inhibitors (AGI)

Acarbose, miglitol

MOA of AGI's

Act on intestine, delay absorption of glucose

SE of AGI's

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

Alpha-glucosidase inhibitor associated with elevation of LFT's

Acarbose

Amino acid derivative for treatment of Type II diabetes

Nateglinide

MOA of nateglinide

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

Biguanide

Metformin

Drugs available in combination with metformin

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

MOA of metformin

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

Most important potential SE of metformin

Lactic acidosis

Meglitinide

Repaglinide

MOA of repaglinide

Insulin release from pancreas; faster and shorter acting than sulfonylurea

First generation sulfonylurea

Chlorpropamide, tolbutamide, tolazamide, etc.

Second generation sulfonylurea

Glyburide, glipizide, glimepiride, etc.

MOA of both generations

Insulin release from pancreas by modifying K+ channels

Common SE of sulfonylureas, repaglinide, and nateglinide

Hypoglycemia

Sulfonylurea NOT recommended for elderly because of very long half life

Chlorpropamide

Thiazolidinediones

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

Reason troglitazone was withdrawn from market

Hepatic toxicity

MOA of thiazolindinediones

Stimulate PPAR-gamma receptor to regulate CHO and lipid metabolism

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

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