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Chemotherapy
Chemotherapeutic agents, targets, and toxicities
32
Pharmacology
Professional
10/06/2011

Additional Pharmacology Flashcards

 


 

Cards

Term

Alkylating Agents

-names

Definition

Mechlorethamine

Cyclophosphamide

Ifosfamide

Carmustine

Lomustine

Busulfan

Cisplatin

Carboplatin

Term

Antimetabolites

-names

Definition

Methotrexate

Fluorouracil (5-FU)

Capecitabine

6-mercaptopurine

cytarabine

Term

Antibiotics

- names

Definition

Doxorubicin

Epirubicin

Dactinomycin

Bleomycin

Term

Drugs from plants

-names

Definition

Vincristine

Vinblastine

Vinorelbine

Paclitaxel

Docetaxel

Etoposide

Term

Differentiating agents

- names

Definition

Tretinoin

Arsenic trioxide (ATO)

 

Term

Hormone/Receptor inhibitors

-names

Definition

Aromatase inhibitors

Tamoxifen

Imatinib

Trastubzumab

Cetuximab

Bevacizumab

Term

Mechlorethamine

-mechanism

-type of agent

-administration

Definition

Mechanism:

- cause formation of crosslinked DNA (cell cycle nonspecific)

 

Type:

- Alkylating agent, nitrogen mustard

 

Administration:

- IV only

Term

Cyclophosphamide

-Mechanism

-Type

-Toxicity

-Other

Definition

Mechanism:

- crosslinks DNA, cell cycle nonspecific

 

Type:

- Alkylating agents, nitrogen mustards

 

Toxicity:

- cardiotoxicity

- bladder burn

- renal toxicity

 

Other:

- MESNA used to treat bladder burn side effects

 

Term

Ifosfamide

-mechanism

-type

-toxicity

-other

Definition

Mechanism:

- crosslink DNA, cell cycle non-specific

 

Type:

- alkylating agent, nitrogen mustard

 

Toxicity:

- Renal toxicity

- CNS (confusion)

- bladder burn

 

Other:

-IV admin

- Cyt P450 activates drug

Term

Carmustine

Lomustine

-type

-mechanism

-clinical use

-toxicity

-other

Definition

Type:

-alkylating agent, nitrosourea

 

Mechanism:

- inhibit DNA, RNA, and protein synthesis

- lipid soluble so crosses BBB

 

Clinical use:

- glioblastoma

 

Toxicity:

- bone marrow depression

- pulmonary fibrosis

 

Other:

- Carmustine: IV fusion

- Lomustine: taken orally

Term

Busulfan

-type

-mechanism

-clinical use

-toxicity

-other

Definition

Type:

- alkylating agents, alkyl sulfonates

 

Mechanism:

- crosslinks DNA, cell cycle nonspecific

 

Toxicity:

- bone marrow suppression

 

Other:

- given orally

Term

Cisplatin

Carbaplatin

-type

-mechanism

-toxicity

-other

Definition

Type:

- alkylating agent, platinum complex

 

Mechanism:

- crosslinks w/ GG pairs (bends DNA)

 

Toxicity:

- peripheral neuropathy

- renal toxicity

 

Other:

- concentrates in liver, kidney, intestine, and ovaries

- hydration helps renal toxicity

- Carbaplatin is milder and dose dependent in its bone marrow suppression

 

Term

Methotrexate

-type

-mechanism

-clinical use

-toxicity

-other

Definition

Type:

- antimetabolites, cell cycle dependent

 

Mechanism:

- purine antimetabolite

- folic acid analogue, competitive inhibitor of DHF reductase

- inhibits folate-dependent enzymes of de novo purine and thymidylate synthesis

 

Toxicity:

- hepatic necrosis

- bone marrow depression

 

Other:

- used in higher dose for chemo than in RA

- can accumulate if you have renal disease

- leucovorin can rescue from toxicity

Term

Fluorouracil (5-FU)

-type

-mechanism

-clinical use

-toxicity

-other

Definition

Type:

- antimetabolite, cell cycle dependent

 

Mechanism:

- fraudulent nucleotide that inhibits DNA synthesis (T analogue)

 

Toxicity:

- severe ulceration of GI mucosa


Other:

- leucovorin potentiates action

Term

Capecitabine

-type

-mechanism

-clinical use

-toxicity

-other

Definition

Type:

- antimetabolite, cell cycle dependent

 

Mechanism:

- prodrug of fluorouracil (thymine analogue)

 

Toxicity:

- bone marrow suppression

- pain

- sensitivity to touch of the palms and sole

 

Other:

- severe interaction w/ coumadin derived drugs

Term

6-mercaptopurine

-type

-mechanism

-clinical use

-toxicity

-other

Definition

Type:

- antimetabolites, cell cycle dependent

 

Mechanism:

- inhibits purine (guanine) synthesis


Clinical use:

- leukemia in children

 

Toxicity:

- bone marrow depression

 

Other:

- people with TPMT mutation should not receive b/c it can kill

Term

Cytarabine

-type

-mechanism

-toxicity

-other

Definition

Type:

- antimetabolites, cell cycle dependent

 

Mechanism:

- inhibits DNA chain elongation by being a fraudulent nucleotide (cytosine)

 

Toxicity:

- bone marrow depression

 

Other:

- S phase specific

Term

Doxorubicin

-type

-mechanism

-clinical use

-toxicity

-other

Definition

Type:

- antibiotics, anthracycline

 

Mechanism:

- blocks DNA topoisomerase II thus inhibiting resealing of DNA nicks

 

Toxicity:

- cardiac toxicity (acute and chronic) due to generation of free oxygen radicals

Term

Epirubicin

-type

-mechanism

-clinical use

-toxicity

-other

Definition

Type:

- antibiotic

 

Mechanism:

- blocks DNA topoisomerase II preventing DNA nick sealing

 

Toxicity:

- cardiac toxicity

- bone marrow depression

 

Other:

- drug interacts with cimetidine (H2 antagonist for ulcers)

Term

Dactinomycin

-type

-mechanism

-toxicity

-other

Definition

Type:

- antibiotics

 

Mechanism:

- intercalates b/w GC base pairs;

- inhibits RNA pol

- interferes w/ DNA topo II

 

Toxicity:

- severe local tissue damage

- necrosis w/ extravasation

- bone marrow depression

 

Other:

- does not cross BBB

Term

Bleomycin

-type

-mechanism

-clinical use

-toxicity

-other

Definition

Type:

- antibiotic

 

Mechanism:

- DNA-[drug]-Fe complex causes DNA fragmentation through formation of free radicals 


Toxicity:

- mild bone marrow toxicity

- pulmonary fibrosis in 5-10% of patients

Term

Vincristine

Vinblastine

Vinorelbine

-type

-mechanism

-clinical use

-toxicity

-other

Definition

Type:

- Plant drugs

 

Mechanism:

- binds tubulin and inhibits tubulin polymerization 

- metaphase arrests and leads to cellular apoptosis

 

Toxicity:

- neurotoxic (sensory neuropathy)

- bone marrow toxicity

- Neurotoxicity: Vincristine > Vinblastine

- BM toxicity: vinblastine > vincristine

 

Other:

- vincristine and bleomycin are 2 chemo

- drugs that cause mild bone marrow depression

Term

Paclitaxel

Docetaxel

-type

-mechanism

-clinical use

-toxicity

-other

Definition

Type:

- plant drug

 

Mechanism:

- freezes polymerized microtubules leading to metaphase arrest

 

Toxicity:

- peripheral sensory neuropathy

Term

Etoposide

-type

-mechanism

-toxicity

Definition

Type:

- plant drugs

 

Mechanism:

- causes DNA breaks by blocking DNA topo II

 

Toxicity:

- bone marrow depression

Term

Tretinoin (all trans retinoic acid- ATRA)

-type

-mechanism

-clinical use

-toxicity

-other

Definition

Type:

- Differentiating agent

 

Mechanism:

- binds retinoid X receptor RARα dimer to displace repressor of differentiation

 

Clinical use:

- acute promyelocytic leukemia (APL) - high rate of complete remission

 

Toxicity:

- retinoic acid syndrome = fever, weight gain, dyspnea, pulmonary infiltrates

Term

Arsenic trioxide (ATO)

-type

-mechanism

-clinical use

-toxicity

-other

Definition

Type:

- differentiating agent

 

Mechanism:

- uncouples mitochondrial oxidative phosphorylation

- generates free radicals

- causes differentiation of APL cells and inhibits angiogenesis 

 

Clinical use:

- APL

 

Toxicity:

- atrial or ventricular arrhythmias

Term

Exemestane

Letrozole

Anastrozole

-type

-mechanism

-clinical use

-toxicity

-other

Definition

Type:

- aromatase inhibitors, hormone/receptor inhibitors

 

Mechanism:

- block conversion of androgens to estrogens

 

Clinical use:

- breast cancer

 

Toxicity:

- musculoskeletal pain

 

Other:

- tumor must be estrogen responsive/sensitive

 

Term

Tamoxifen

-type

-mechanism

-clinical use

-toxicity


Definition

Type:

- hormone/receptor inhibitors

 

Mechanism:

- binds estradiol and is competitive inhibitor of the estrogen receptor

 

Clinical use:

- estrogen-dependent breast cancer

 

Toxicity:

- hot flashes

- can reduce serum cholesterol

Term

Imatinib

-type

-mechanism

-clinical use

-other

Definition

Type:

- receptor tyrosine kinase inhibitor

 

Mechanism:

- inhibits BCR-ABL tyrosine kinase and PDGF receptor

 

Clinical use:

- chronic myelogenous leukemia

- philadelphia chromosome cancers

 

Other:

- BCR-ABL is detected by FISH

Term

Trastubzumab

-type

-mechanism

-clinical use

-toxicity

-other

Definition

aka Herceptin

Type:

- hormone/receptor inhibitor

- receptor tyrosine kinase inhibitor

 

Mechanism:

- monoclonal antibody recognizes HER2 and prevents the cellular growth, division, and amplification

 

Clinical use:

- Breast cancer (25% are HER2+)

 

Toxicity:

- cardiomyopathy

- CHF

Term

Cetuximab

-type

-mechanism

-clinical use

-toxicity

-other

Definition

Type:

- monoclonal antibody 

- tyrosine kinase inhibitors

 

Mechanism:

- binds, blocks function of EGFR (HER1)

- inhibits growth and induces apoptosis

 

Clinical use:

- colorectal cancer

 

Toxicity:

- rapid onset of airway obstruction and hypotension

- S/e are infusion related

Term

Bevacizumab

-type

-mechanism

-clinical use

-toxicity

-other

Definition

Type:

- monoclonal antibody

- tyrosine kinase inhibitor

 

Mechanism:

- binds VEGF thus inhibiting angiogenesis

 

Clinical use:

- colorectal cancer

 

Toxicity:

- hypertension

- GI perforation

- CHF

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