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PHARMACOLOGY

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Used for the palliative treatment of advanced breast cancer. ANDROGENS. Drug interactions: ... the treatment of advanced prostate cancer. Include: Goserelin ... – PowerPoint PPT presentation

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Title: PHARMACOLOGY


1
PHARMACOLOGY
  • Cancer drugs

2
OBJECTIVES
  • Identify the classes of drugs used to treat
    cancer.
  • Identify the uses and varying actions of these
    drugs.
  • Identify how these drugs are absorbed,
    distributed, metabolized, and excreted.
  • Identify drug interactions and adverse reactions
    of these drugs.

3
DRUGS AND CANCER
  • The following are classifications of
    antineoplastic (chemotherapeutic) drugs
  • Alkylating drugs
  • Antimetabolite drugs
  • Antibiotic antineoplastic drugs
  • Hormonal antineoplastic drugs
  • Natural antineoplastic drugs
  • Unclassifiable antineoplastic drugs

4
ALKYLATING DRUGS
  • Effective against various malignant neoplasms.
  • Produce their effects by deactivating DNA.
  • Six classes nitrogen mustards, alkyl sulfonates,
    nitrosoureas, triazenes, ethylenimines, and
    alkylating-like drugs.

5
NITROGEN MUSTARDS
  • Largest group of alkylating drugs that include
    chlorambucil, cyclophosphamide, estramustine,
    ifosfamide, mechlorethamine hydrochloride (the
    first introduced and the most rapid-acting),
    melphalan, and uracil mustard.

6
NITROGEN MUSTARDS
  • Pharmacokinetics
  • Vary widely metabolized in the liver excreted
    by the kidneys mechlorethamine is metabolized
    almost immediately.
  • Pharmacodynamics
  • Form covalent bonds with DNA molecules in a
    chemical reaction called alkylation resulting in
    cell death.

7
NITROGEN MUSTARDS
  • Pharmacotherapeutics
  • Because they produce leukopenia, they are
    effective against malignant neoplasms such as
    Hodgkins disease, leukemia, malignant lymphoma,
    multiple myeloma, melanoma, and cancers of the
    breast, ovaries, uterus, lung, brain, testes,
    bladder, prostate, and stomach.

8
NITROGEN MUSTARDS
  • Drug interactions
  • Interact with a wide variety of other drugs.
  • Adverse reactions
  • Fatigue

9
ALKYL SULFONATES
  • Busulfan is commonly used to treat chronic
    myelogenous leukemia and less commonly to treat
    polycythemia vera.
  • Pharmacokinetics
  • Absorbed rapidly and well from the GI tract
    little known about distribution metabolized
    extensively in the liver excreted in the urine.

10
ALKYL SULFONATES
  • Pharmacodynamics
  • Forms covalent bonds with DNA molecules in
    alkylation.
  • Pharmacotherapeutics
  • Primarily affects granulocytes and platelets
    resulting in being the drug of choice for chronic
    myelogenous leukemia.

11
ALKYL SULFONATES
  • Drug interactions
  • Increased risk of bleeding when taken with
    anticoagulants or aspirin.
  • Adverse reactions
  • Bone marrow suppression

12
NITROSOUREAS
  • Include carmustine, lomustine, and streptozocin.
  • Pharmacokinetics
  • When administered topically to treat mycosis
    fungoides, is 5-28 systemically absorbed when
    administered orally, is absorbed adequately but
    incompletely streptozocin is administered IV and
    is not absorbed.

13
NITROSOUREAS
  • Distribute to fatty tissues and CSF metabolized
    extensively in the liver excreted in the urine.
  • Pharmacodynamics
  • Interfere with amino acids, purines, and DNA
    halting their reproduction.

14
NITROSOUREAS
  • Pharmacotherapeutics
  • Easily cross the blood-brain barrier, therefore
    are used to treat brain tumors and meningeal
    leukemias.
  • Drug interactions
  • Each has its own interactions.
  • Adverse reactions
  • Severe nausea and vomiting.

15
TRIAZENES
  • Dacarbazine functions as an alkylating drug after
    it has been activated by the liver.
  • Pharmacokinetics
  • After IV Injection is distributed throughout the
    body metabolized in the liver excreted by the
    kidneys (half is excreted unchanged and half is
    excreted as one of the metabolites).

16
TRIAZENES
  • Pharmacodynamics
  • First must be metabolized by the liver and then
    seems to inhibit RNA and protein synthesis.
  • Pharmacotherapeutics
  • Used primarily to treat patients with malignant
    melanoma and Hodgkins disease.

17
TRIAZENES
  • Drug interactions
  • No significant interactions.
  • Adverse reactions
  • Leukopenia

18
ETHYLENIMINES
  • Thiotepa is a multifunctional alkylating drug.
  • Pharmacokinetics
  • After IV administration, is 100 bioavailable
    crosses the blood-brain barrier and is
    metabolized extensively by the liver excreted in
    the urine.

19
ETHYLENIMINES
  • Pharmacodynamics
  • Interferes with DNA replication and RNA
    transcription.
  • Pharmacotherapeutics
  • Primarily used to treat bladder cancer and may
    also be useful in other cancers.

20
ETHYLENIMINES
  • Drug interactions
  • Use with anticoagulants and aspirin may increase
    the risk of bleeding.
  • Adverse reactions
  • Blood-related including leukopenia,
    thrombocytopenia, and pancytopenia.

21
ALKYLATING-LIKE DRUGS
  • Carboplatin and cisplatin are heavy metal
    complexes that contain platinum and resemble
    bifunctional alkylating drugs.
  • Pharmacokinetics
  • Distribution and metabolism of carboplatin arent
    clear eliminated by the kidneys
  • When cisplatin is administered interpleurally or
    intraperitoneally, may be systemically absorbed.

22
ALKYLATING-LIKE DRUGS
  • Pharmacodynamics
  • Cell non-specific and inhibit DNA synthesis by
    cross-linking strands of DNA and inhibiting DNA
    synthesis.
  • Pharmacotherapeutics
  • Carboplatin is used to treat ovarian and lung
    cancer.
  • Cisplatin is used to treat bladder, ovarian, and
    metastatic testicular cancers.

23
ALKYLATING-LIKE DRUGS
  • Drug interactions
  • When administered with an aminoglycoside, the
    risk of toxicity to the kidney increases.
  • Adverse reactions
  • Bone marrow depression

24
ANTIMETABOLITE DRUGS
  • Resemble natural metabolites and become involved
    in their process of nucleic acid and protein
    synthesis.
  • Are cell cycle-specific and primarily affect
    cells that actively synthesize DNA (S
    phase-specific).

25
ANTIMETABOLITE DRUGS
  • Classified according to the metabolite affected
  • folic acid analogues
  • pyrimidine analogues
  • purine analogues

26
FOLIC ACID ANALOGUES
  • Methotrexate is the most commonly used.
  • Pharmacokinetics
  • Absorbed well and distributed throughout the
    body metabolized partially excreted primarily
    unchanged in the urine.
  • Pharmacodynamics
  • Reversibly inhibits the action of the enzyme
    dihydrofolate reductase blocking normal
    biochemical reactions.

27
FOLIC ACID ANALOGUES
  • Pharmacotherapeutics
  • Useful in treating acute lymphoblastic leukemia,
    choriocarcinoma, osteogenic sarcoma, malignant
    lymphomas, and carcinomas of the head, neck,
    bladder, testis, and breast.
  • Also prescribed for psoriasis and rheumatoid
    arthritis.

28
FOLIC ACID ANALOGUES
  • Drug interactions
  • Interact with several drugs.
  • Salicylates and NSAIDS increase toxicity.
  • Concurrent use of alcohol increases the risk of
    liver toxicity.
  • Adverse reactions
  • Bone marrow suppression

29
PYRIMIDINE ANALOGUES
  • A diverse group of drugs that inhibit production
    of pyrimidine nucleotides necessary for DNA
    synthesis.
  • Includes
  • Cytarabine
  • Floxuridine
  • Flourouracil
  • Gemcitabine

30
PYRIMIDINE ANALOGUES
  • Pharmacokinetics
  • Because of poor oral absorption, are given by
    other routes for the most part are distributed
    well throughout the body including the CSF
    metabolized extensively in the liver excreted in
    the urine.

31
PYRIMIDINE ANALOGUES
  • Pharmacodynamics
  • Kill cancer cells by interfering with the natural
    function of pyrimidine nucleotides.
  • Pharmacotherapeutics
  • Used to treat many tumors as well as acute
    leukemias, GI tract adenocarcinomas, carcinomas
    of the breast and ovaries, and malignant
    lymphomas.

32
PYRIMIDINE ANALOGUES
  • Drug interactions
  • No significant interactions.
  • Adverse reactions
  • fatigue and lack of energy
  • inflammation of the mouth, esophagus, and throat,
    bone marrow suppression, nausea, and anorexia.

33
PURINE ANALOGUES
  • Incorporated into DNA and RNA interfering with
    nucleic acid synthesis and replication.
  • Include
  • Fludarabine phosphate
  • Cladribine
  • Mercaptopurine
  • Thioguanine

34
PURINE ANALOGUES
  • Pharmacokinetics
  • Not clearly defined largely metabolized in the
    liver excreted in the urine.
  • Pharmacodynamics
  • First must undergo conversion to the nucleotide
    level to be active and the resulting nucleotides
    are then incorporated into DNA (similar to
    pyrimidine analogues).

35
PURINE ANALOGUES
  • Pharmacotherapeutics
  • Used to treat acute and chronic leukemias and
    lymphomas.
  • Drug interactions
  • No significant interactions.
  • Adverse reactions
  • Bone marrow suppression, nausea, vomiting,
    anorexia, diarrhea, stomatitis.

36
ANTIBIOTIC NEOPLASTICS
  • Are antimicrobial products that produce
    tumoricidal effects by binding with DNA and
    inhibiting processes of normal and malignant
    cells.
  • Include bleomycin sulfate, dactinomycin,
    daunorubicin, doxorubicin hydrochloride,
    idarubicin hydrochloride, mitomycin, mitoxantrone
    hydrochloride, pentostatin, and plicamycin.

37
ANTIBIOTIC NEOPLASTICS
  • Pharmacokinetics
  • Because usually administered IV, no absorption
    occurs distribution, metabolism, and elimination
    vary.
  • Pharmacodynamics
  • Intercalate or insert themselves between adjacent
    base pairs of a DNA molecule physically
    separating them.

38
ANTIBIOTIC NEOPLASTICS
  • Pharmacotherapeutics
  • Act against many cancers.
  • Drug interactions
  • Interact with many other drugs.
  • Adverse reactions
  • bone marrow suppression.

39
HORMONAL ANTINEOPLASTIC DRUGS
  • Prescribed to alter the growth of malignant
    neoplasms or to manage or treat their
    physiological effects.
  • Effective against hormone-dependent tumors.
  • Include antiestrogens, androgens, antiandrogens,
    progestins, and gonadotropin-releasing hormone
    analogues.

40
ANTIESTROGENS
  • Tamoxifen citrate is the drug of choice for
    advanced breast cancer involving
    estrogen-receptor-positive tumors in
    postmenopausal women.
  • Also used as an adjunct treatment for breast CA
    and to reduce its incidence in high risk women.

41
ANTIESTROGENS
  • Pharmacokinetics
  • After oral administration is absorbed well
    extensively metabolized in the liver excreted in
    the feces.
  • Pharmacodynamics
  • Binds to the estrogen receptors and inhibits
    estrogen-mediated tumor growth.

42
ANTIESTROGENS
  • Pharmacotherapeutics
  • Used in the palliative treatment of metastatic
    breast cancer that is estrogen-receptor-positive.
  • Drug interactions
  • Few interactions reported.
  • Adverse reactions
  • Relatively nontoxic.

43
ANTIESTROGENS
  • Drug interactions
  • Antacids may affect absorption when taken in
    enteric-coated form.
  • Adverse reactions
  • Hot flashes, fluid retention, N, V, D.

44
ANDROGENS
  • Are synthetic forms of testosterone
    (fluoxymesterone, testolactone, testosterone
    enanthate and testosterone propionate).
  • Pharmacokinetics
  • Oral agents are absorbed well parenteral agents
    are absorbed slowly distributed well
    metabolized extensively in the liver excreted in
    the urine.

45
ANDROGENS
  • Pharmacodynamics
  • Inhibit estrogen synthesis or competitively bind
    at estrogen receptors preventing estrogen from
    affecting estrogen-sensitive tumors.
  • Pharmacotherapeutics
  • Used for the palliative treatment of advanced
    breast cancer.

46
ANDROGENS
  • Drug interactions
  • May alter dose requirements of insulin, oral
    antidiabetic drugs, or oral anticoagulants.
  • Adverse reactions
  • Nausea and vomiting.

47
ANTIANDROGENS
  • Used as adjunct therapy with gonadotropin-releasin
    g hormone analogues in treating advanced prostate
    cancer.
  • Includes
  • Flutamide
  • Nilutamide
  • Bicalutamide

48
ANTIANDROGENS
  • Pharmacokinetics
  • Absorbed rapidly and completely metabolized
    rapidly and extensively excreted primarily in
    the urine.
  • Pharmacodynamics
  • Inhibit androgen uptake or prevent androgen
    binding in cell nuclei in target tissues.

49
ANTIANDROGENS
  • Pharmacotherapeutics
  • Used along with gonadotropin-releasing hormone
    analogue to treat metastatic prostate cancer.
  • Drug interactions
  • No significant interactions.
  • Adverse reactions
  • Hot flashes and impotence.

50
PROGESTINS
  • Hormones used to treat various forms of cancer
    including
  • Hydroprogesterone caproate
  • Medroxyprogesterone acetate
  • Megastrol acetate

51
PROGESTINS
  • Pharmacokinetics
  • Absorbed well orally and slowly parenterally
    distributed well throughout the body metabolized
    in the liver excreted as metabolites in the
    urine.
  • Pharmacodynamics
  • Possibly bind to a specific receptor to act on
    hormonally sensitive cells (cytostatic).

52
PROGESTINS
  • Pharmacotherapeutics
  • Used for the palliative treatment of advanced
    endometrial, breast, and renal cancers.
  • Megestrol is used most often.
  • Drug interactions None with megastrol.
  • Adverse reactions Mild fluid retention.

53
GONADOTROPIN-RELEASING HORMONE ANALOGUES
  • Used for the treatment of advanced prostate
    cancer.
  • Include
  • Goserelin acetate
  • Leuprolide acetate

54
GONADOTROPIN-RELEASING HORMONE ANALOGUES
  • Pharmacokinetics
  • Goserelin is absorbed slowly the first 8 days and
    then quickly thereafter leuprolide is absorbed
    well subcutaneously distribution, metabolism,
    and excretion not known.
  • Pharmacodynamics
  • Act on the pituitary gland increasing luteinizing
    hormone secretion stimulating testosterone
    production.

55
GONADOTROPIN-RELEASING HORMONE ANALOGUES
  • Eventually the reverse occurs inhibiting the
    testicular release of testosterone which, in
    turn, inhibits tumor growth.
  • Pharmacotherapeutics
  • Used for the palliative treatment of metastatic
    prostate cancer.
  • Drug interactions None.
  • Adverse reactions Hot flashes impotence.

56
NATURAL ANTINEOPLASTIC DRUGS
  • Include vinca alkaloids and podophyllotoxins.
  • Vinca alkaloids are nitrogenous bases derived
    from the periwinkle plant and include
    vinblastine, vincristine, and vinorelbine.
  • Are cell-cycle specific and are effective during
    the phase of mitosis and cell division.

57
NATURAL ANTINEOPLASTIC DRUGS
  • Used to treat many types of cancer.
  • Podophyllotoxins are also cell cycle-specific and
    include etoposide and teniposide.
  • Used to treat testicular cancer, small-cell lung
    cancer, and acute lymphoblastic leukemia.
  • Most common adverse reaction is hair loss.

58
UNCLASSIFIABLE ANTINEOPLASTIC DRUGS
  • Include asparaginase, procarbazine, hydroxyurea,
    interferon, aldesleukin, altretamine, paclitaxel,
    and docetaxel.
  • Asparaginase deprives cancer cells of asparagine
    causing cell death.
  • Used to induce remission in acute lymphocytic
    leukemia.

59
UNCLASSIFIABLE ANTINEOPLASTIC DRUGS
  • Procarbazine is used to treat Hodgkins disease
    (MOPP regimen) and primary and metastatic brain
    tumors.
  • Because it has MAO inhibiting properties,
    tyramine-rich foods should be avoided.
  • Hydroxyurea is used to treat chronic myelogenous
    leukemia, head and neck cancers, and solid tumors.

60
UNCLASSIFIABLE ANTINEOPLASTIC DRUGS
  • Interferons inhibit viral replication, suppress
    cell proliferation, enhance macrophage activity,
    and increase cytotoxicity of lymphocytes for
    target cells.
  • Used to treat hairy cell leukemia, AIDS-related
    Kaposis sarcoma, and condylomata acuminata.

61
UNCLASSIFIABLE ANTINEOPLASTIC DRUGS
  • Aldesleukin is a human recombinant interleukin-2
    derivative which is used to treat metastatic
    renal cell carcinoma.
  • Altretamine is a synthetic cytotoxic
    antineoplastic drug that is used as palliative
    treatment of ovarian cancer.

62
UNCLASSIFIABLE ANTINEOPLASTIC DRUGS
  • Taxines are used to treat metastatic ovarian and
    breast carcinoma after chemotherapy has failed.
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