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Antidiabetic Drugs

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Lecture 14 Chapter 46 Antidiabetic Drugs Antidiabetic Drugs Drugs used to control diabetes mellitus - a chronic disease that affects carbohydrate metabolism 2 groups ... – PowerPoint PPT presentation

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Title: Antidiabetic Drugs


1
Lecture 14
  • Chapter 46
  • Antidiabetic Drugs

2
Antidiabetic Drugs
  • Drugs used to control diabetes mellitus - a
    chronic disease that affects carbohydrate
    metabolism
  • 2 groups of antidiabetic agents Insulin oral
    hypoglycemic agents
  • - Oral hypoglycemic agents synthetic
    preparations that stimulate insulin release or
    alter metabolic response to hyperglycemia
  • - Insulin a protein secreted from the beta
    cells of the pancreas - necessary for carbo
    metabolism an important role in protein fat
    metabolism

3
Antidiabetic Agents
  • Diabetes Mellitus - A chronic disease resulting
    from deficient glucose metabolism, caused by
    insufficient insulin secretion from the beta
    cells high blood sugar (hyperglycemia). 3
    Ps
  • 1. Polyuria - inc. urine output
  • 2. Polydipsia - inc. thirst
  • 3. Polyphagia - inc. hunger
  • 2 forms of diabetes
  • 1. Insulin-dependent diabetes mellitus (IDDM)
    or type I - was refereed to as juvenile-onset w/
    no insulin secretion

4
Antidiabetic Agents
  • 2. Non-insulin-dependent diabetes mellitus
    (NIDDM) or type II - was referred to as
    maturity-onset or adult-onset diabetes w/ some
    insulin secretion
  • Unknown how lack of insulin causes diabetes -
    poss. infection, heredity
  • Insulin - Released from the beta cells of the
    islets of Langerhans in the pancreas in response
    to an increase in bld. glucose
  • - Promotes the uptake of glucose, amino acids,
    fatty acids converts them to substances
    stored in body cells

5
Antidiabetic Agents
  • - Glucose is converted to glycogen for future
    glucose needs in the liver muscle lowers bld.
    glucose level (range for bld. glucose is 70 - 110
    mg/dl)
  • bld. glucose gt 180 sugar in urine
    diuretic effects polyuria
  • - Insulin can be animal (pork or beef), or
    human (using DNA technology)
  • - Concentration of insulin is 100 U/ml,
    insulin packaged in a 10 ml vial. For accurate
    dosing, insulin can be given in insulin syringes
    ONLY.

6
Antidiabetic Agents
  • - Before using insulin, need to ensure well
    mixed - always roll between hands - Do NOT Shake
    Vial bubbles inaccurate dose
  • - insulin CANNOT be administered orally - GI
    tract secretions destroy insulin structure
  • - Given subcutaneous at a 45 to 90 degree
    angle
  • - Regular insulin ONLY can be given IV
  • - Insulin sites need to be rotated to prevent
    lipodystrophy (tissue atrophy or hypertrophy)
    interferes w/ insulin absorption

7
Antidiabetic Agents Insulin
  • Types of Insulin's - 3 standard types
  • 1. Rapid-acting - Regular insulin - clear soln
    w/o added substances to prolong insulin action
  • Onset 1/2 to 1 h Peak 2 to 4 h Duration
    6 to 8 h
  • 2. Intermediate-acting - NPH, Lente - contain
    protamine (a protein that prolongs the action of
    the insulin)
  • Onset 1 to 2 h Peak 6 to 12 h Duration
    18 to 24 h
  • 3. Long-Acting - Ultralente - contain lg.
    crystals which dissolve slowly to prolong
    duration
  • Onset 4 to 8 h, Peak 14 to 20 h Duration
    24 to 36 h

8
Antidiabetic Agents Insulin
  • Lispro Insulin (Humalog) - a new rapid acting
    insulin approved in 1996
  • Action 5 min. Duration 2 to 4 h - can be
    administered 5 min. before meal time
  • Combination Insulin's - commercially premixed
  • Humulin 70/30, Novolin 70/30, Humulin 50/50
  • (70/30 70 NPH and 30 Reg)
  • Reg can be mixed w/ NPH or Lente - Reg goes in
    first in the syringe Clear to Cloudy

9
Antidiabetic Agents Insulin
  • SE adverse RXNS
  • -Hypoglycemic - when more insulin is
    administered than needed for glucose metabolism
  • - S S nervous, trembling, uncoordinated,
    cold clammy, incoherent (drunk)
  • - Rx giving sugar orally or IV
  • - Ketoacidosis - An inadequate amt. of insulin
    inability to metabolize sugar fat catabolism
    use of fatty acids (ketones) for energy
  • - S S Extreme thirst, polyria, fruity
    breath odor
  • - Rx Insulin

10
Antidiabetic Agents Oral Agents
  • Used by persons w/ NIDDM - should NOT be used by
    persons w/ IDDM
  • NIDDM has some degree of insulin secretion by
    pancreas
  • Several classes of oral hypoglycemic agents
  • Sulfonylureas - First Second generation
  • - Chemically related to sulfonamides, but lack
    antibacterial activity - stimulate the beta cells
    to secrete more insulin
  • - 1st generation divided into short,
    intermediate long acting antidiabetics

11
Antidiabetic Agents Oral Agents
  • - tolbutamide (Orinase) - short Tolazamide
    (Tolinase) - intermediate Chlorpropamide
    (Diabinese) - long
  • - Action - Stimulate beta cells to secrete
    insulin
  • - Use NIDDM
  • - SE - similar to insulin - hypoglycemic rxn
    w/o adequate food intake
  • - DI - ASA, anticoagulant, anticonvulsants,
    sulfonamides, some NSAIDs can inc. action of
    sulfonylureas an insulin rxn

12
Antidiabetic Agents Oral Agents
  • Nonsulfonylurease Newer drugs
  • Biguanides Metformin (Glucophage)
  • - Decreases hepatic production of glucose from
    stored glycogen diminishes the inc. in serum
    glucose after a meal
  • - Dec. the absorption of glucose from the
    small intestine
  • - Evidence it inc. insulin receptor
    sensitivity
  • - Does not produce hypo or hyperglycemia
  • - SE - N V, anorexia, abd cramping, gas
  • - Can be combined w/ a sulfonylurea insulin

13
Antidiabetic Agents Oral Agents
  • Alpha-Glucosidase Inhibitor Acarbose (Precose)
  • - Action - inhibits the digestive enzyme in
    sm. intestine responsible for release of glucose
    from the complex carbohydrates (CHO) in the diet
  • - By inhibiting alpha glucosidase (enzyme) -
    the CHO cannot be absorbed they pass into the
    lg. intestine
  • - does not cause a hypoglycemic rxn
  • - Use - for clients who do not achieve results
    on diet alone

14
Antidiabetic Agents Oral Agents
  • Thiazolidinediones Troglitazone (Rezulin) -
    unrelated to other antidiabetic drugs
  • - Action - Decrease insulin resistance, helps
    muscle cells respond to insulin use glucose
    more effectively
  • - May be used w/ sulfonylurea, metformin, or
    insulin
  • - May cause serious hepatic toxicity - Not
    used in England
  • Rapaglinide (Prandin) - classification unknown -
    Newest
  • - For use alone or w/ metfromin - short acting
  • - Action - similar to sulfonylureas, but does
    not cause hypoglycemia

15
Antidiabetic Agents Oral Agents
  • Hyperglycemic Drugs - Glucagon
  • - Action - A hyperglycemic hormone secreted by
    the alpha cells of the islets of Langerhans -
    Inc. bld sugar by stimulating glycogenolysis
    (breakdown of glycogen to glucose) in the liver -
    protects body cells
  • - Use - Insulin-induced hypoglycemia when
    other methods not available or not working
  • - Clients prone to hypoglycemia should keep in
    home family members taught how to use
  • - Begins to work in 5 to 20 min.

16
Antidiabetic Agents Oral Agents
  • Diazoxide (Proglycem) - chemically related to
    thiazide diuretics
  • - Action - Inc. bld sugar by inhibiting
    insulin release from the beta cells stimulating
    release of epi (adrenalin from the adrenal
    medulla
  • - Use - Chronic hypoglycemia caused by
    hyperinsulinism d/t islet cell Ca or hyperplasia
  • - Not used to Rx hypoglycemic rxns
  • - Parenteral form (Hyperstat) used for
    malignant HTN
  • - Oral diazoxide usually does not cause
    hypotension

17
Chapter 33
  • Anticancer Drugs

18
Anticancer Drugs
  • In the US, cancer is the 2nd cause of death
    (heart dx - 1st)
  • Results from the alterations in DNA w/in the cell
  • Use of anticancer drugs include - cure, control,
    palliative
  • Chemo may be used as sole Rx of Ca or in
    conjunction w/ radiation surgery
  • Cell-Cycle Nonspecific Specific - Anticancer
    drugs cause Ca cell death by interfering w/ Ca
    cell replication
  • - Interferes w/ either all phases or a specific
    phase of the cell cycle (pg. 575, fig. VII-I)

19
Anticancer Drugs
  • - Cell-cycle nonspecific (CCNS) act on any
    phase during the cell cycle
  • - kill the cell during the dividing resting
    phase of cell cycle alkylating drugs, antitumor
    antibiotics, hormones
  • - Cell-cycle specific (CCS) act on a specific
    phase of the cell cycle
  • - effective against rapidly growing Ca cells
    antimetabolites, vica alkaloids, antitumor
    antibiotics
  • Growth fraction doubling time are two factors
    that play a major role in the Ca cell response to
    the anticancer drug

20
Anticancer Drugs
  • - Anticancer drugs are more effective against
    the Ca cells having a high growth fraction -
    leukemias some lymphomas
  • - Ca of the breast colon melanomas low
    growth fraction poor response to
    antineoplastics
  • - small early forming Ca cells fast-growing
    tumors respond well to anticancer drugs
  • Drug Rx for early dx higher cure rate than late
    stages
  • Solid tumors low growth fraction less
    sensitive to drugs

21
Anticancer Drugs
  • Higher doses of drugs result in better
    tumoricidal (killing) effects
  • Ca growth usually faster in earlier stages. As
    tumor grows bld supply dec growth rate dec.
    drugs more effective against sm. tumors w/
    sufficient bld supply
  • Cancer Chemotherapy - tumor cells are similar to
    normal cells in that it is difficult for antiCa
    drugs to be selective in killing tumor cells
    not normal cells
  • - Drug protocol therapy too long doses too
    high toxic
  • - Eliminating every Ca cell difficult (1
    mill. cells could remain w/o symptoms - ??? on
    continuing Ca therapy

22
Anticancer Drugs
  • Drug Resistance - tumor resistance can develop
    against an antiCa drug d/t drug used infrequently
    or the tumors location limits the effectiveness
  • - Brain tumors respond poorly (BBB)
  • Combination Chemotherapy - Single-agent drug
    therapy seldom used
  • - Combo of drugs to enhance tumoricidal
    effects
  • - CCS CCNS are often combined to max. cell
    deaths
  • - dec. drug resistance, shorten intensify
    drug effect
  • - inc. destruction of Ca cells, dec. drug
    toxicity - several drugs lower doses less
    injury to normal cells

23
Anticancer Drugs
  • Alkylating Drugs - one of the largest groups of
    Ca drugs
  • - Kill cells by forming cross-links on DNA
    strands
  • - Belong to the CCNS category affect all
    phases of the cell cycle - effective against many
    types of cancers acute chronic leukemias,
    lymphomas, mult. myeloma, solid tumors (breast,
    ovaries, uterus, lungs)
  • - Classified into 4 groups Nitrogen mustards
    (Cyclophosphamide), nitrosoureas (Carmustine),
    alkyl sulfonates (Busulfan), alkylating-like
    drugs (Cisplatin)

24
Anticancer Drugs
  • Cyclophosphamide (Cytoxan) - Nitrogen mustard
  • - Action - Inhibition of protein synthesis
    through interference w/ DNA replication by
    alkylation of DNA
  • - Use - Hodgkins dx, solid tumors
  • - SE - bone marrow suppression , alopecia, N
    V, diarrhea, wt. loss, hematuria (maintain
    adequate hydration), impotence, sterility
  • - An early antiCa drugs, can be administered PO

25
Anticancer Drugs
  • Antimetabolites - Oldest group
  • - Resemble natural metabolites - disrupt the
    metabolic processes some of the agents inhibit
    enzyme synthesis
  • - CCS (5-FU, floxuridine - also CCNS)
  • - Subdivided into folic acid (folate)
    antagonists (Methotrexate) - also used as an
    immunosuppressant following organ transplant -
    substitutes for folic acid, needed for the
    synthesis of proteins DNA pyrimidine analogues
    (5-fluorouracil) purine analogues
    (6-mercaptopurine)

26
Anticancer Drugs
  • Flurouracil (Adrucil, 5-FU, Efudex) - IV
  • - Action - CCS, blocks the enzyme action
    necessary for DNA RNA synthesis
  • - low therapeutic index
  • - alone or w/ other drugs, can cross BBB
  • - Use - Ca of breast, cervix, colon, ovary,
    stomach, pancreas
  • - SE - N, V, diarrhea, alopecia, rash, bone
    marrow suppression, stomatitis (inflammation of
    oral mucosa)

27
Anticancer Drugs
  • Antitumor Antibiotics - (Bleomycin, dactinomycin,
    daunorubicin, doxorubicin) - inhibit protein
    RNA synthesis bind DNA causing fragmentation
  • - Classified as CCNS (except for bleomycin)
  • - Drugs differ from each other are used for
    diff. Cas
  • Doxorubicin (Adriamycin) - IV
  • - Action - Inhibits DNA RNA synthesis
  • - Use - W/ other agents for Ca of breast,
    ovaries, lung, bladder, leukemias, lymphomas
  • - SE - Similar to general adverse rxns to
    antineoplastics

28
Anticancer Drugs
  • - Capable of causing vesication - blistering of
    tissue if drug leaks out into surrounding
    interstitial tissue - rxn ranges from painful,
    reddened swelling to deep necrotic lesion needing
    debridement skin grafts
  • - Drug is a deep red color - urine will be red
    1 - 2 days after administration
  • - Can cause cardiotoxicity
  • Mitotic Inhibitors (Vinca Alkaloids) - block cell
    division at M phase of cell cycle (Vincristine,
    Vinblastine, Vinorelbine tartrate) - CCS

29
Anticancer Drugs
  • - Single drugs or in combo therapy
  • - SE - leukopenia, alopecia, stomatitis, N,V,
    neurotoxicity
  • Hormones Hormone Antagonisits - Used in combo
    therapy for Rx of various Ca.
  • - 2 major actions 1) Agonists that inhibit
    tumor cell growth - estrogen, progestins,
    androgens, adrenocorticosteroids 2) Antagonists
    that compete w/ endogenous hormone -
    aminoglutethimide, tamoxifen
  • Corticosteroids (glucocorticoids) classified as
    antiinflammatory agents - suppressing the
    inflammatory process that occurs w/ tissue
    involvement

30
Anticancer Drugs
  • - Hormones also suppress leukicytes is
    effective in controlling leukemia lymphoma
  • - Used w/ other drugs as part of an
    antineoplastic regimen - MOPP (oncovin,
    procarbazine prednisone) - Hodgkins disease
  • - Prednisone frequently prescribed -
    inexpensive cortisone derivative
  • - Dexamethasone hydrocortisone - IM or IV -
    can decrease cerebral edema caused by a brain
    tumor

31
Anticancer Drugs
  • Tamoxifen (Nolvadex) -
  • - Action - exact neoplastic action unknown,
    acts as an estrogen antagonist
  • - Use - Breast cancer in women and men
  • - SE - Adverse rxns usually minor well
    tolerated
  • Miscellaneous Agents - antineoplastic drugs whose
    MOA does not place them in a category. Used in
    combo w/ other Ca drugs to Rx a variety of solid
    tumors hematologic malignancies - pactitaxel
    (Taxol), docetaxel (Taxotere), pentostatin
    (Nipent), etoposide (VP-16)

32
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