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Applied Pharmacology > Chemotherapy Drugs > Flashcards

Chemotherapy Drugs Flashcards

1
Q

What are the different classes of chemotherapy drugs?

A
  • Cytotoxic drugs ( alkylating agents, antimetabolites, cytotoxic antibiotics, plant derivatives)
  • Hormones
  • Monoclonal antibodies
  • Protein Kinase Inhibitors
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2
Q

What are the different classes of alkylating agents? (cytotoxic drugs)

A
  • Nitrogen mustards - cyclophosphamide
  • Nitrosoureas - lomustine (CCNU), carmustine (BCNU)
  • Busulphan
  • Platinum compounds - cisplatin, carboplatin
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3
Q

What are the different classes of antimetabolites? (cytotoxic drugs)

A
  • Folate antagonists - eg. methotrexate
  • Pyrimidine analogues - eg. fluorouracil
  • Purine analogues - eg. fludarabine
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4
Q

What are examples of cytotoxic antibiotics? (cytotoxic drugs)

A
  • Doxorubicin
  • Bleomycin
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5
Q

What are examples of plant derivatives? (cytotoxic drugs)

A
  • Vincristine
  • Vinblastine
  • Vindesine
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6
Q

What are the different classes of hormones?

A
  • Glucocorticoids (eg prednisolone, dexamethasone) -
  • Oestrogens (eg. diethylstilebestrol)
  • Progestogens (eg. megesterol)
  • Gonadotropin-releasing hormone analogues (eg goserelin)
  • Anti-oestrogens (eg tamoxifen)
  • Anti-androgens (eg. flutamide)
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7
Q

How do cytotoxic drugs work?

A
  • They block DNA synthesis/prevent cell division
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8
Q

How do hormones (and their antagonists) work?

A
  • They suppress opposing hormone secretion or inhibit their actions.
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9
Q

How do monoclonal antibodies work?

A
  • They target specific cancer cells
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10
Q

How do protein kinase inhibitors work?

A
  • They block cell signalling pathways in rapidly diving cells.
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11
Q

How do alkylating agents work? (cytotoxic drugs)

A
  • Target cells in DNA synthesis phase (S-phase)
  • Form covalent bonds with DNA (cross -linking) to prevent uncoiling (inhibits replication)
  • SIDE EFFECTS - sterility (in men) ad increased risk of non-lymphocytic leukaemia (AML)
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12
Q

Explain nitrogen mustards (alkylating agents, CYTOTOXIC DRUGS)

A
  • Have cytotoxic effects in rapidly growing cells - very reactive, given IV.
  • Mechlorethamine
  • Cyclophosphamide
  • Melphalan
  • Chlorambucil
  • Bendamustine
  • Estramustine
  • SIDE EFFECTS - can cause cystitis (cyclophosphamide)
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13
Q

Explain nitrosoureas (alkylating agents, CYTOTOXIC DRUGS)

A
  • Highly lipophilic - cross the BBB to treat CNS tumours.
  • Carmustine (IV) - multiple myeloma, non-Hodgkins lymphoma and brain tumours
  • Lomustine (oral) - Hodkins disease, malignant melanoma and certain solid tumours.
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14
Q

Explain platinum compounds (alkylating agents, CYTOTOXIC DRUGS)

A
  • Cisplatin - testicular, lung, cervical, bladder etc
  • Potent alkylator - binds to RNA>DNA>protein
  • Binds to purine bases (G,A,U).
  • Resistance may develop - DNA repair by DNA polymerase.
  • SIDE EFFECTS - very nephrotoxic (requires hydration), severe N+V, risk of tinnitus, peripheral neuropathy, hyperuricaemia (gout) and anaphylaxis.
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15
Q

Explain other platinum compounds (platinum compounds > alkylating agents, CYTOTOXIC DRUGS)

A
  • Carboplatin - derivative of cisplatin (ovarian and lung cancer).
  • Less side effects- can be outpatient.
  • Oxaliplatin - used to treat colorectal cancer (with fluorouracil and folinic acid).
  • SIDE EFFECTS - bone marrow suppression (myelotoxic).
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16
Q

What other alkylating agents are there? (cytotoxic drugs)

A
  • Busulfan - selective for bone marrow, leukaemia treatment.
  • Procarbazine - used to treat Hodgkins disease but causes hypersensitivity rash and inhibits MAOIs :( -
  • Trabecteolin - soft tissue sarcoma/advanced ovarian cancer but is hepatotoxic :(
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17
Q

Explain folate antagonists (antimetabolites, CYTOXIC DRUGS)

A
  • Folate essential for DNA synthesis/cell division
  • Methotrexate - inhibits dihydrofolate reductase (oral, IM, IV).
  • Low lipid solubility (doesn’t cross BBB). Childhood acute lymphoblastic leukaemia, chariocarcinoma, non-Hodgkins and solid tumours
  • Cautions - Mostly excreted in the urine - lower doses for patients with renal impairment, NSAIDs reduce excretion = increased toxicity
  • Tumour cells may develop resistance.
  • Given with folinic acid to ‘rescue’ normal cells.
  • Also used to suppress immune system (arthritis)
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18
Q

Explain Pyrimidine Analogues (antimetabolites, CYTOTOXIC DRUGS)

A
  • Compete with C and T bases which make up DNA and RNA - inhibits DNA synthesis.
  • Fluorouracil (solid tumours, GI cancers and breast cancers)
  • Capecitaine (colon/colorectal cancer, breast cancer)
  • Cytarabine (acute myeloblastic leukaemia) -
  • Gemcitabine (pancreatic/bladder/ovarian/breast cancer)
19
Q

Explain purine analogues (antimetabolites, CYTOTOXIC DRUGS)

A
  • Compete with A and C - inhibit purine metabolism
  • Mercaptopurine
  • Tioguanine
  • Pentostatin
  • Fludaraine
20
Q

Explain doxorubicin (cytotoxic antibiotics, CYTOTOXIC DRUGS)

A
  • Binds to RNA and inhibits DNA/RNA synthesis (IV) - acute myeloblastic leukaemia.
  • Inhibit topoisomerase II (swivels DNA and introduces double strand breaks to prevent tangling and unwinds DNA for replication).
  • SIDE EFFECTS - local necrosis if it touches skin, cardiac dysrhythmias/head failure in high doses
21
Q

Explain bleomycin (cytotoxic antibiotics, CYTOTOXIC DRUGS)

A
  • Degrades pre-formed DNA
  • Active against non-dividing cells (Go phase) -
  • Metastatic germ cell cancer/non-hodgkins
  • SIDE EFFECTS - pulmonary fibrosis (10% patients), 50% develop mucocutaeneous reactions (mouth sores, hair loss, fungal infections) and pyrexia
22
Q

What other cytotoxic antibiotics are there? (cytotoxic drugs)

A
  • Dactinomycin - paediactric cancers
  • Mitomycin - IV - upper GI and breast cancers.
23
Q

Explain Vincristine, Vinblastine and Vindesine (Plant derivatives, cytotoxic drugs)

A
  • Madagascar periwinkle
  • Prevents polymerisation of tubulin (microtubules), prevents spindle formation ‘vinca alkaloids’
  • Effects only occur during mitosis
  • Relatively non-toxic (except vincristine - neuromuscular effects)
  • All used to treat leukaemias, lymphomas and some solid tumours (breast and lung)
24
Q

Explain Paclitaxel and Docetaxel (Plant derivatives, cytotoxic drugs)

A
  • ‘Taxanes’ - yew tree
  • similar mechanisms to vinca alkaloids
  • Used to treat breast cancer and ovarian cancer (except docetaxel)
25
Q

Explain etoposide (Plant derivatives, cytotoxic drugs)

A
  • Mandrake root - testicular cancer/lymphomas -
  • Avoid skin contact -
  • Small cell carcinoma of bronchus
  • SIDE EFFECTS - rapid fall in blood pressure
26
Q

How are hormones used to treat cancer?

A
  • Used in the treatment of cancers in hormone-sensitive tumours (breast, prostate, ovarian)
  • Tumour growth inhibited by receptor antagonists, hormones with opposing actions, or drugs, which block synthesis of endogenous hormones.
  • Rarely cure diseases but reduce symptoms
27
Q

How are oestrogens used to treat cancers (Hormones)

A
  • Ethinyloestradiol & Diethylstilbestrol
  • Antagonists of androgen - dependant prostate cancer.
  • Stimulates resting mammary cells to proliferate as proliferating cells are more susceptible to drugs.
  • SIDE EFFECTS - nausea, fluid retention, thrombosis, impotence and gynaecomastia.
28
Q

How are progestogens used to treat cancers? (hormones)

A
  • Megestrol
  • Medroxyprogesterone
  • Norethisterone - Used to treat endometrial cancer.
29
Q

How are GnRH analogues used to treat cancers? (Hormones)

A
  • Goserelin
  • Buserelin
  • Leuprorelin
  • Triptorelin
  • Inhibit GnRH research to decrease LH/FSH to decrease testosterone.
  • Used to treat prostate/breast cancer.
30
Q

How are Somatostatin analogues used to treat cancer? (hormones)

A
  • Octreotide
  • Lanreotide
  • Inhibit cell proliferation/hormone (CCK/Gastrin) secretion.
  • Used to treat hormone-secreting tumours of GI tract.
31
Q

How is tamoxifen used to treat cancers? (hormone antagonists, HORMONES)

A
  • Competitive antagonists of oestrogen receptors to inhibit transcription of oestrogen-responsive genes> breast cancer treatment.
  • SIDE EFFECTS - menopausal effects, endometrial cancer and increased risk of blood clots
32
Q

How is Letrozole and Exemastine used to treat cancers? (hormone antagonists, HORMONES)

A
  • Inhibit aromatase (enzyme involved in oestrogen synthesis).
  • This blocks the conversion of adrogens to oestrogens in peripheral tissue but does not inhibit ovulation.
33
Q

How is flutamide, cyproterone and bicalutamide used to treat cancers? (hormone antagonists, HORMONES)

A
  • Androgens antagonists - prostate cancer treatment.
34
Q

How is prednisolone and dexamethasone used to treat cancer? (glucocorticoids, HORMONES)

A
  • Inhibit lymphocyte proliferation - treatment of lymphomas/leukaemias.
  • Counter some side effects of other anti-cancer drugs (N+V)
35
Q

How are monoclonal antibodies used to treat cancer?

A
  • Produced by cultured-hybridoma cells (formed by fusing anti-body producing b-cells with b-cell cancer (myeloma)).
  • React with specific target proteins expressed on cancer cells - activates immune system - lysis of cancer cells.
  • Some mAbs activate GF-receptors on cancer cells - inhibit survival/promote apoptosis.
  • Targeted therapy - less side effects
  • expensive, must be given in combination with other drug.
36
Q

How is Rituximab used to treat cancer (Monoclonal antibodies)

A
  • Binds to CD20 protein, expressed on certain lymphoma cells - lysis of b-lymphocytes
  • 40-50% effective when used with chemotherapy.
  • Used to treat Non-Hodgkins lymphoma expressing CD20.
  • SIDE EFFECTS - hypotension, chills and fever, hypersensitivity.
37
Q

How is Trastuzumab used to treat cancer? (monoclonal antibodies)

A
  • Binds to HER2 (a GF-receptor)
  • Induces immune response and cell cycle inhibitors
  • HER2 overexpressed in ~25% breast cancer = rapid proliferation (aggressive form)
  • Given with standard drugs to increase survival rate.
  • SIDE EFFECTS - tremor, flu-like symptoms, itchy eyes, BP changes, palpitations.
38
Q

How is Bevacizumab used to treat cancer? (monoclonal antibodies)

A
  • Treatment of colorectal cancer.
  • Neutralises VEGF (overexpressed in tumours) prevents angiogenesis (IV)
39
Q

How are Imatinib, Dasatinib** and **Nilotinib used to treat cancer? (Protein Kinase Inhibitors)

A
  • Blocks tyrosine kinases involved in GF signalling pathways (oral)
  • Used to treat chronic myeloid leukaemia (CML)
  • Problems with drug resistant.
40
Q

Control of Side effects of cancer drugs

A
  • N+V - Ondansetron, Granisetron, Metaclopramide
  • Anxiety - Lorazepam
  • Myelosuppression - Stem cell transplant, Lenagrastim.
41
Q

Side effects of cancer chemo:

A

Are minimised by treatment with anti-emetics and good nursing care.

42
Q

What is the mechanism of action for the majority of anti-cancer drugs?

A

Prevention of cell division.

43
Q

Bulsafan is an alkylating agent which is selective for bone marrow. It is therefore used in the treatment of:

A

Leukaemia.

44
Q

As a treatment for cancer, monoclonal antibodies are different from other drugs because they;

A

Selectively improve host immunity.

Applied Pharmacology (12 decks)

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