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    2020 Respiratory Drugs Dentistry

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    Visayan Alliah Gail
    The document discusses pharmacological therapies for bronchial asthma, including bronchodilators like beta agonists, methylxanthines, and muscarinic antagonists; anti-inflammatory drugs like corticosteroids and leukotriene antagonists; and targeted monoclonal antibodies like omalizumab. It describes the pharmacodynamics, pharmacokinetics, routes of administration, and side effects of these various respiratory drugs used to treat conditions like asthma and COPD. The goal of treatment is to provide bronchodilation and reduce airway inflammation through these pharmacological classes of respiratory medications.

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    2020 Respiratory Drugs Dentistry

    Uploaded by

    Visayan Alliah Gail
    18 views27 pages
    The document discusses pharmacological therapies for bronchial asthma, including bronchodilators like beta agonists, methylxanthines, and muscarinic antagonists; anti-inflammatory drugs like corticosteroids and leukotriene antagonists; and targeted monoclonal antibodies like omalizumab. It describes the pharmacodynamics, pharmacokinetics, routes of administration, and side effects of these various respiratory drugs used to treat conditions like asthma and COPD. The goal of treatment is to provide bronchodilation and reduce airway inflammation through these pharmacological classes of respiratory medications.

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    The document discusses pharmacological therapies for bronchial asthma, including bronchodilators like beta agonists, methylxanthines, and muscarinic antagonists; anti-inflammatory drugs like corticosteroids and leukotriene antagonists; and targeted monoclonal antibodies like omalizumab. It describes the pharmacodynamics, pharmacokinetics, routes of administration, and side effects of these various respiratory drugs used to treat conditions like asthma and COPD. The goal of treatment is to provide bronchodilation and reduce airway inflammation through these pharmacological classes of respiratory medications.

    Copyright:

    © All Rights Reserved
    Download as PPTX, PDF, TXT or read online from Scribd
    Download as pptx, pdf, or txt
    18 views27 pages

    2020 Respiratory Drugs Dentistry

    Uploaded by

    Visayan Alliah Gail
    The document discusses pharmacological therapies for bronchial asthma, including bronchodilators like beta agonists, methylxanthines, and muscarinic antagonists; anti-inflammatory drugs like corticosteroids and leukotriene antagonists; and targeted monoclonal antibodies like omalizumab. It describes the pharmacodynamics, pharmacokinetics, routes of administration, and side effects of these various respiratory drugs used to treat conditions like asthma and COPD. The goal of treatment is to provide bronchodilation and reduce airway inflammation through these pharmacological classes of respiratory medications.

    Copyright:

    © All Rights Reserved
    Download as PPTX, PDF, TXT or read online from Scribd
    Download as pptx, pdf, or txt
    of 27

    Respiratory Drugs

    Florencia D. Munsayac, MD, MBA, FPSECP, RMT


    Our Lady of Fatima University-College of Dentistry
    Objective:
    • Discuss the pharmacological therapy of
    bronchial asthma as to its
    pharmacodynamics/effects/pharmacokinetics/
    side effects/drug interactions
    Bronchial asthma
    Drugs Used in Bronchial Asthma
    • Bronchodilators
    • Sympathomimetic Agents/Beta agonists
    • Non-selective beta agonists: Epinephrine, Isoproterenol, Ephedrine
    • Selective Beta2 agonists
    • Short-acting: Albuterol, Terbutaline, Metaproterenol, Levalbuterol, Pirbuterol
    • Long-acting: Salmeterol, Formoterol
    • Ultra-long-acting: Indacaterol, Olodaterol, Vilanterol and Bambuterol
    • Methyxanthines: Theophylline, Theobromide, Caffeine
    • Muscarinic antagonists: Ipratropium bromide, Tiotropium, Aclidinium, Umeclidinium
    • Anti-inflammatory Agents
    • Corticosteroids: Prednisone, Hydrocortisone, Methyprednisolone, Triamcinolone acetonide, Beclomethasone,
    Budesonide, Ciclesonide, Fluticasone, Flunisolide, Mometasone, Triamcinolone
    • Release inhibitors: Cromolyn sodium/Nedocromil
    • Leukotriene antagonists: Zeliuton, Montelukast, Zafirlukast
    • Targeted Monoclonal Antibodies
    • IgE Antibody: Omalizumab
    • Anti-IL-5 Therapy: Mepolizumab, Reslizumab, Benralizumab
    I. Bronchodilator Therapies

    1. Sympathomimetic Agents/Adrenoceptor Agonists


    - Directly relax airway smooth muscle by activating Gs
    adenylyl cyclase-cAMP bronchodilatation

    - ↑ conductance of large Ca+2-sensitive K+ channels in


    airway smooth muscle hyperpolarization &
    relaxation

    - Inhibit release of inflammatory mediators & cytokines


    from the mast cells, basophils, eosinophils, neutrophils,
    & lymphocytes

    - ↑ mucociliary transport
    I. Bronchodilator Therapies

    1. Sympathomimetic Agents/Adrenoceptor Agonists

    a. Selective B2- agonists

    - Short-acting: terbutaline, albuterol, levalbuterol, metaproterenol, pirbuterol

    - Long acting: salmeterol, formoterol

    - Ultra-long-acting: indacaterol, olodaterol, vilanterol, bambuterol

    b. Non-selective Beta-Agonists

    - Epinephrine

    - Ephedrine

    - Isoproterenol
    I. Bronchodilator Therapies

    1. Sympathomimetic Agents/Adrenoceptor Agonists


    a. Non-Selective Beta-Agonists
    Epinephrine Ephedrine Isoproterenol
    SC – 0.4ml of 1:1000 Oral Inhalation – 80-120mcg
    Inhalation – 320mcg/puff
    Onset 15 minutes 5 minutes

    Duration of 60-90 minutes longer 60-90 minutes


    action

    Side effects Tachycardia, arrhythmias, Pronounced Arrhythmias


    worsening of angina pectoris central
    effects
    I. Bronchodilator Therapies
    1. Sympathomimetic Agents/Adrenoceptor Agonists
    b. Selective B2- agonists – Short-acting
    Route/s Terbutaline Albuterol Metaproterenol Pirbuterol

    Metered-dose inhaler
    - Maximal effect: 15-30 minutes
    - DOA: 3-4 hours
    Hand-held nebulizer
    - Reserved for patients unable to
    coordinate from MDI

    Oral: tablet
    -Side effects: skeletal muscle tremor,
    nervousness, weakness

    Subcutaneous injection
    (0.25mg)
    - Cumulative effects may be seen
    after repeated injections
    I. Bronchodilator Therapies

    1. Sympathomimetic Agents
    b. Selective B2- agonists - Long acting:
    - Salmeterol (a partial agonist)
    - Formoterol (a full agonist)

    - Long duration of action – 12 hours  high lipid solubility


    - No anti-inflammatory action

    - Indacaterol, Olodaterol, Vilanterol, bambuterol (Ultra-long-


    acting Beta agonists)  as monotherapy for the treatment of
    COPD
    I. Bronchodilator Therapies
    2. Methylxanthine drugs
    a. theophylline (1,3-dimethylxanthine)
    - most commonly used
    - derivatives:
    - aminophylline
    - dyphylline
    - oxtriptylline

    b. theobromide (3,7-dimethylxanthene)

    c. caffeine (1,3,7-trimethyxanthine)
    I. Bronchodilator Therapies
    2. Methylxanthine drugs
    Mechanisms of action
    - Inhibit cyclic nucleotide phosphodiesterases ↑ IC cAMP &
    cGMP smooth muscle relaxation, reduction in immune &
    inflammatory activity of specific cells

    = Roflumilast: selective inhibitor of PDE4

    - Inhibition of cell surface receptors for adenosine


    = Enprofylline: Xanthine derivative, more potent bronchodilator,
    devoid of adenosine antagonism
    - Histone deacetylase activation
    I. Bronchodilator Therapies
    2. Methylxanthine drugs
    • Pharmacodynamics
    –CNS
    • mild cortical arousal w/ increased alertness & deferral of fatigue
    • nervousness; insomnia
    • in very high doses: medullary stimulation, convulsions and death
    • primary SE: nervousness and tremor
    –CVS
    • have positive inotropic and chronotropic effects
    • arrhythmia
    • sinus tachycardia and increased cardiac output
    • rises the PVR and BP slightly
    • decrease blood viscosity and may improve blood flow – pentoxifylline

    -
    I. Bronchodilator Therapies
    2. Methylxanthine drugs
    • Pharmacodynamics

    – GIT
    • stimulate secretion of gastric acid and digestive enzymes

    – Kidneys
    • weak diuretics

    – Skeletal muscles
    • have potent effects in improving contractility and in reversing fatigue of diaphragm in
    patient with COPD

    – Smooth muscle
    • inhibit antigen-induced release of histamine from lung tissue
    I. Bronchodilator Therapies
    2. Methylxanthine drugs
    • Pharmacokinetics
    • Metabolized by CYP1A2 and CYP3A4  involve in large number of disease
    and drug interactions

    • Target serum concentrations: 5 – 15mg/L (28 – 83 umol/L)


    • > 15 mg/L (>83 umol/L): increased risk of adverse effects
    • < 20 mg/L (111 umol/L): HA, nausea, vomiting, and insomnia
    • Higher concentrations: cardiac arrhythmias, seizures and death
    I. Bronchodilator Therapies
    3. Anti-Muscarinic/Anticholinergic Agents
    – Competitively inhibits the effect of acetylcholine at muscarinic receptors
    (M3) → effectively block the contraction of the airway smooth muscle
    and increase in secretion of mucus
    – Ipratropium bromide – a quarternary ammonium derivative of atropine
    – Tiotropium – structural analog of ipratropium
    – Delivered by inhalation (metered dose inhaler/nebulizer)
    – Slightly less effective than beta agonist

    – Adverse effects: blurred vision, dry mouth and urinary retention


    – Effective in COPD
    II. Controller Therapies
    • Corticosteroids
    – Reducing the inflammatory cells and their activation in the airways

    – Minimize sputum production and secretion

    – Reduce numbers of activated T lymphocytes and surface mast cells in the


    airway mucosa ↓ AHR

    – Improve the response to beta2-agonists

    – Available in inhaled, oral and injectable dosage forms


    II. Controller Therapies
    • Inhaled Corticosteroids
    – Beclometasone, budesonide, ciclesonide, fluticasone, flunisolide, mometasone,
    triamcinolone

    – Preferred therapy for all forms of persistent asthma in all age groups

    – The most effective way to avoid systemic adverse effects of corticosteroid


    therapy

    – SE: hoarseness, oropharyngeal candidiasis  topical clotrimazole


    II. Controller Therapies
    • Systemic Corticosteroids
    – Methyprednisolone, prednisone, Prednisolone

    – ROA: oral, IV

    – SE: truncal obesity, bruising, osteoporosis, diabetes, hypertension, gastric


    ulceration, proximal myopathy, depression, cataracts
    II. Controller Therapies

    • Anti-leukotrienes
    – Zileuton
    • Selectively and reversibly inhibits the 5-lipoxygenase pathway

    – Montelukast and Zafirlukast


    • Blocks the cysteinyl leukotrienes LTD4 and LTE4 at the CsyLT1
    receptor
    II. Controller Therapies
    Anti-leukotrienes
    Zileuton Zafirlukast Montelukast

    Absorption Rapid Rapid Rapid

    Metabolism extensively by CYPs & by Metabolized Metabolized


    UDP- extensively by hepatic extensively by
    glucoronosyltransferase CYP2C9 CYP3A4 & CYP2C9

    Bioavailability 90% 60-70%

    Protein Binding 93% 99% 99%

    Half-life 2.5 hours 10 hours 3-6 hours


    II. Controller Therapies
    • Antileukotrienes
    – Other effects:
    • Have demonstrated an important role in aspirin-induced asthma

    • Effect on symptoms, airway caliber, bronchial reactivity and airway inflammation: less
    marked than inhaled corticosteroids, almost equally effective in reducing the frequency of
    exacerbations
    II. Controller Therapies
    • Cromolyn Sodium & Nedocromil
    • Act by inhibiting mast cell degranulation

    • Have no direct bronchodilator action

    • Main indication: reducing symptoms of allergic rhinoconjunctivitis


    Targeted (Monoclonal Antibody) Therapy
    1. Anti-IgE Antibodies
    - drugs that reduce the amount of IgE that binds to its receptors (Fcε-R1 and Fcε-R2) on
    mast cells, dendritic cells, basophils and other inflammatory cells

    - Omalizumab (anti-IgE MAb)


    = indications: - severe asthma exacerbations
    - evidence of allergic sensitization
    - chronic recurrent urticaria
    - peanut allergy
    = administered as a single SC injection q 2 – 4 weeks
    = 60% bioavailability
    = peak serum levels: 7 – 8 days
    = half-life: 26 days
    = elimination: liver reticuloendothelial system, bile
    = important effect: reduction in frequency and severity of asthma exacerbations
    Targeted (Monoclonal Antibody) Therapy
    2. Anti-IL-5 Therapy
    – approval as add-on, maintenance therapy of severe asthma in
    patients with eosinophilic phenotype
    - Mepolizumab
    - carries a small (0.3%) risk of anaphylaxis
    - reactivation of herpes zoster
    - Reslizumab
    - associated with hypersensitivity reactions
    - Benralizumab
    - recently been developed for the treatment of eosinophilic
    asthma
    Other Respiratory Agents
    A. Mucolytic Agents
    1. Acetylcysteine (mucomyst)
    - reduce the thickness and stickiness of purulent and non-purulent pulmonary
    secretions
    - antidote for paracetamol poisoning

    2. Carbocysteine (SCMC)
    - act by regulating and normalizing the viscosity of secretion from the mucus cell of
    respiratory tract
    - decrease the size and number of mucus producing cells

    3. Bromhexine
    - depolymerization of mucopolysaccharides, direct effect on bronchial glands
    - liberation of lysosomal enzymes producing cells which digest mucopolysaccharide
    fibers
    B. Mucokinetic & Secretolytic
    1. Ambroxol
    - increase respiratory tract secretions
    - enhance pulmonary surfactant production
    - stimulates cilia activity

    C. Expectorant
    1. Vagal stimulants: glyceryl guiacolate, salt solution
    2. Direct stimulants: KISS, bromhexine, SCMC, ambroxol

    D. Antitussives
    1. Narcotic antitussives: heroin, codeine, morphine
    2. Non-narcotic antitussive: Dextromethorphan

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