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    Asthma 017

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    Mariam Alavidze
    The document discusses the pharmacology of cough and asthma, outlining various classes of drugs used to treat these conditions including antitussives, expectorants, mucolytics, bronchodilators, and anti-inflammatory agents. It provides details on specific medications within each class, their mechanisms of action, therapeutic uses, side effects, contraindications, and drug interactions. Guidelines for stepwise management of asthma are also presented.

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    © All Rights Reserved
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    Asthma 017

    Uploaded by

    Mariam Alavidze
    47 views46 pages
    The document discusses the pharmacology of cough and asthma, outlining various classes of drugs used to treat these conditions including antitussives, expectorants, mucolytics, bronchodilators, and anti-inflammatory agents. It provides details on specific medications within each class, their mechanisms of action, therapeutic uses, side effects, contraindications, and drug interactions. Guidelines for stepwise management of asthma are also presented.

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    asthma_017

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    The document discusses the pharmacology of cough and asthma, outlining various classes of drugs used to treat these conditions including antitussives, expectorants, mucolytics, bronchodilators, and anti-inflammatory agents. It provides details on specific medications within each class, their mechanisms of action, therapeutic uses, side effects, contraindications, and drug interactions. Guidelines for stepwise management of asthma are also presented.

    Copyright:

    © All Rights Reserved
    Download as PDF, TXT or read online from Scribd
    Download as pdf or txt
    47 views46 pages

    Asthma 017

    Uploaded by

    Mariam Alavidze
    The document discusses the pharmacology of cough and asthma, outlining various classes of drugs used to treat these conditions including antitussives, expectorants, mucolytics, bronchodilators, and anti-inflammatory agents. It provides details on specific medications within each class, their mechanisms of action, therapeutic uses, side effects, contraindications, and drug interactions. Guidelines for stepwise management of asthma are also presented.

    Copyright:

    © All Rights Reserved
    Download as PDF, TXT or read online from Scribd
    Download as pdf or txt
    of 46

    Pharmacology of cough

    According to the type of coughing

    productive improductive
    (with sputum) (dry, racking)

    colourful clear tracheitis


    pleuritis
    bacteria viral inf, allergy

    antibiotics, antihistamines, humidity 


    mucolytics candies
    antitussives
    Antitussives

    Centrally acting antitussives


    1. Opioids
     morphine: only in oedema of the lungs
     codeine
    - elevates the threshold of coughing centre in CNS
    - μ-receptor agonist
    - causes respiratory depression
    - analgesic effect (in higher doses)

    Side effects:
    - nausea
    - constipation
    - somnolence
    - addiction!, withdrawal symptoms
    Avoid in case of:
    - respiratory depression
    - chronic constipation
    - cough with sputum
    Interaction:
    - NSAID, TCA, MAOI, CNS depressants, expectorants, alcohol

     dihydrocodeine tablet
    - more effective than codeine
    - hemi synthetic
    - addiction
    Therapeutic use:
    - improductive cough
    - pain
    Side effects, contraindication: see codeine
     dextrometorphane
    OTC: MEDDEX WICK syrup, candy
    RHINATHIOL syrup (children/adults)
    ROBITUSSIN Antitussicum and Junior syrup
    TUSSOPRONT solution (children/adults)
    - morphine derivate, but no opioid effect, no analgesic effect
    - no effect on the μ-receptor
    - no respiratory depression, no addiction, no withdrawal symptoms
    in therapeutic dose
    Mechanism of action:
    - elevates the threshold of coughing centre in CNS
    - NMDA receptor antagonist
    Side effects:
    - drowsiness, vertigo
    - GI symptoms
    Avoid in case of:
    - liver failure
    - cough with sputum
    - asthma bronchiale
    1. Non-opioids
     butamirate (drops, tablet, syrup)
    - exact mechanism is unknown
    - mild bronchospasmolytic effect, respiratory function improves
    - no addiction
    Avoid in case of:
    - productive cough
    - under 3years of age, 1. trimester of pregnancy
    Side effects:
    - not significant (nausea, vomiting)
    Peripherally acting antitussives
     prenoxdiazine
    OTC: LIBEXIN, RHINATHIOL TUSSO tablet
    Effects:
    - inhibits stretch-receptors in the lung
    - significant bronchodilator effect
    - weak local anesthetic effect
    - also acts on coughing centre in CNS
    Administration:
    - 3-4X daily, for adults, children: ¼- ½ tablet
    Side effects:
    - dry mouth
     levodropropisine OTC: LEVOPRONT drops, syrup
    - acts in the tracheobronchial system
    Contraindicated:
    - under 2 years of age
    - severe liver failure, pregnancy
    Side effects:
    - GI problems
    Interaction: effects of sedatives ↑ (drops contain 30% alcohol)
    Expectorants
    - secretolytics and mucolytics
    Contraindicated: antitussive drugs
    Side effects: GI problems

    Secretolytics
    - increase the ecxretion of mucous
     Ipecacuanha, emetin: stimulate the mucous memrane of the
    stomach (vagus reflex)
     sapononines: Primulae radix, Saponariae albae radix,
    Ipecacuanhae radix (vagus reflex)
     ammonium-chlorid
    - local stimulatory effect
     volatile oils in inhalation: chamomile, thyme, eucalyptus,
    peppermint:
    - increase secretion in the bronchi, also liquefy mucus
    - inhalation, do not use under the age of 3
    Side effects:
    - Mucous membrane: burning sensation
    - skin: inflammation, hyperaemia
    - GI: diarrhoea
    - pregnant uterus: contraction
    OTC:
    • BRONCHIPRET syrup, drops
    • EUKALIPTUSZ SCHERER capsule
    • MIXTURA PECTORALIS FonoVII
    Expectorants
    Mechanism of action:
    - mediated (at least in part) by a vagal reflex initiated by stimulation
    of the gastric mucosa following oral administration

     guaifenesin
    OTC: ROBITUSSIN Expectorans syrup
    GUAIFENOMED WICK syrup
    Mechanism of action:
    - decrease the viscosity and adhesion of mucous
    - stimulate gastric muscosa
    Administration:
    - For adults and above 12 years of age: 10 ml/every 4 hours
    - 6-12 years: 5 ml every 4 hours
    - 2-6 years: 2,5 ml every 4 hours
    Side effects: GI (nausea, vomiting)
    It contains alcohol.
    Mucolytics
    - drugs that liquefy mucus, decrease viscosity of the mucous
    - effective in case of productive coughing, helps to get rid of mucus
    in the airways.
    - very important for patients with cystic fibrosis

     acetylcysteine (injection, infusion)


    OTC: ACC 100, 200 granules, ACC 200, 600 effervescent
    FLUIMUCIL effervescent, syrup
    SOLMUCOL candy
    - cause depolimerisation of the nucleic acids
    - antioxidant activity (free -SH)
    - it breaks disulfide bonds in mucus and liquefies it, making it easier
    to cough up
    Therapeutic use:
    - mucolytic agent
    - paracetamol poisoning
    Side effects:
    - Allergy
    - GI symptoms
    Interaction:
    - antibiotics (2hour break) (increased secretion)
    N-acetyl-benzoquinone
     carbocisteine
    OTC: FENORIN syrup
    MUCOPRONT capsule, syrup
    RHINATHIOL syrup for children and for adults

    - no free –SH group


     bromhexine (inj.)
    OTC: PAXIRASOL solution, tablet
    - increase the activity of hydrolytic enzymes → break the
    polysaccharides
    - increase surfactant
    - breaks down to an active metabolite: ambroxol
     ambroxol (inj.)
    OTC: AMBROBENE solution, capsule, syrup, tablet
    AMBROXOL-TEVA syrup, tablet
    HALIXOL syrup, tablet
    MUCOANGIN tablet
    - active metabolite of bromhexine
    - Inj: to stimulate surfactant in neonates
     dornase-alpha (inhalational solution)
    - genetically engineered, human enzyme
    Mechanism of action:
    - liquefy the mucus in the alveoli
    and airways (degradated white blood
    cells, debris, broken DNA)

    Therapeutic use:
    - mainly for CF patients
    Side effects:
    - pharingitis
    - hoarseness
    - laryngitis
    - rash
    Pharmacotherapy of
    asthma
    Allergic inflammation in the airways
    Pharmacotherapy of asthma

    1. Bronchodilators
     β2-receptor agonists
     xanthenes derivates
     muscarinerg antagonists

    2. Anti-inflammatory agents
     glucocorticoids
     leukotriene inhibitors
     omalizumab
     chromones
    Guidelines for the management of asthma

    1. step: Occasional use of relief bronchodilators


    inhaled short acting -agonists „as required”
    if needed more than once daily  2.
    2. step_ 1 + regular inhaled antiinflammatory agents
    inhaled short acting -agonists „as required”
    + low dose inh steroids twice daily
    3. step: 2 + long acting -agonists twice daily
    or
    inhaled short acting -agonists „as required”
    + high dose inh steroids twice daily
    4. step: high dose inh steroids twice daily + regular
    bronchodilators: inh long acting -agonists/
    p.os SR theophyllin /inh ipratropium/
    p.os long acting -agonists
    5. step: 4 + addition of regular steroid tablets
    inhaled short acting -agonists „as required”
    + high dose inh steroids twice daily
    + long acting bronchodilators
    + p.os steroids in single daily dose
    1. LOCALLY ACTING AGENTS
    - use of aerosols
    - produce a high local concentration in the lungs with a low
    systemic delivery → minimal systemic side effects
    A) Bronchodilators:
    β2-agonists: salbutamol, terbutalin, fenoterol (short-acting)
    salmeterol, formoterol (long-acting)
    Anticholinergic agents: ipratropium-bromide, thiotropium-bromide

    B) Anti-inflammatory agents
    Inhalational glucocorticoids: beclomethasone, budesonide,
    fluticasone, ciklesonide

    C) Inhibition of histamine release: cromolyn sodium (not


    anymore in the therapy)
    2. SYSTEMICALLY USED AGENTS
    A) Bronchodilators
    β2-agonists: salbutamol, terbutalin, clenbuterol
    Xhantines: theophylline, aminophylline

    B) Glucocorticoids
    metilprednisolon, prednisolon, triamcinolon, hidrocortison,
    betametasone

    C) Leukotriene-receptor antagonists: montelucast, zafirlucast

    D) Anti-IgE therapy: omalizumab

    E) IL-5 antibody: mepolizumab


    1. β2-adrenerg receptor agonists
    Effects:
    • most potent bronchodilator effect
    • they are able to relax bronchi in severe asthmatic attacks
    (spontaneous or triggered)
    • may have short or long effect
    • relax smooth muscle via β2-adrenergic receptors, by elevating
    cAMP level
    • improve mucociliar clearance
    • decrease bronchial secretion
    • decrease the permeability of microvessels
    • decrease the mediator secretion from mastocytes
    Side effects:
    - common: tremor, flush, tachycardia, anxiety, restlessness
    - rare: arrhythmia, angina pectoris, pulmonary oedema
    - in case of high doses: headache, sweating, vertigo, hypokalaemia

    Contraindication:
    - hyperthyroidism
    - diabetes
    - heart failure
    - hypertension

    - pregnancy, breastfeeding!
    Interaction:
    - β-blockers
    - MAOI, TCA
    - cardiotonic agents
    - oral antidiabetics, insulin
    - diuretics (K+↓)

    Inhalational agents
    Short-acting, inhalational drugs:
    4-6 hours
     salbutamol
     terbutaline
     fenoterol
    For symptomatic relief of asthma!
    Side effects: local irritation
    Long-acting, inhalational drugs: 12 hours
     salmeterol
     formoterol
    Use: prophylactic treatment

    Inhales betamimetics in combination:


     fenoterol + ipratropium bromide
     formoterol + bechlometasone
     salmeterol + fluticasone
     formoterol + budesonide

    Systematically used agents


     salbutamol
     terbutaline
     clenbuterol
    2. Xanthines derivates

     theophylline capsule, injection, tablet, suppository


     aminophylline tablet, injection
    - inj: iv or infusion
    - methylated xanthines
    Mechanism of action:
    - PDEI (non-selective) → cAMP ↑ ⇒ bronchodilator effect
    - adenosine receptor antagonist
    Side effects:
    • stimulate CNS: anxiety, sleep disorders, tremor, seizure
    • CV: heart rate ↑, tachycardia, arrhythmia
    • mild diuretic effect
    • tremor of the skeletal muscles
    • GI: increase secretion
    • nausea, vomiting, stomach problems, headache
    Pharmacokinetics:
    - good absorption
    - tight therapeutic effect→ TDM!
    - liver metabolism
    Interaction:
    - enzyme inhibitors and inducers
    3. Anticholinergic agents
     ipratropium-bromide
     tiotropium-bromide
    Combination: fenoterol + ipratropium bromide
    Mechanism of action:
    - inhibit broncho-constriction and mucous secretion caused by ACh
    - competitive muscarinic receptor antagonist
    Side effects:
    - inhalation: dry mouth
    - mild anticholinergic side effects
    4. Glucocorticoids
    Inhaled glucocorticoids :

     budesonide
     flutikasone
     ciklesonide

    Use: prophylactically

    Combination:
     formoterol + bechlometasone
     salmeterol + fluticasone
     formoterol + budesonide

    Side effects:
    - huskiness
    - oral candidates (mouth wash)
    Systemic glucocorticoids:
    Therapeutic use:
    - chronic severe asthma
    - acute asthma exacerbations

     methylprednisolone injection, tablet


     triamcinolone tablet
     hydrocortisone tablet
     prednisolone tablet

    Administration: iv, im, or infusion


    Side effects:
    • adrenal cortex suppression
    • osteoporosis
    • impaired growing in children
    • thinning of the skin
    • cataract
    Interaction:
    - Agents reducing blood pressure
    - antidiabetics
    - oral anticoncipients
    5. Leukotriene-receptor antagonists
     zafirlukast tablet
     montelukast tablet

    Mechanism of action:
    - competitive antagonists of leukotriene receptors
    - Inhibit the effects of leukotrienes: smooth muscle contraction,
    oedema of airway and mucous production
    Therapeutic use:
    - asthma prevention, long-lasting treatment
    Side effects:
    - headache, GI-symptoms
    - allergy
    - liver failure
    Avoid in case of:
    - under 12 years of age (zafirlukast)
    - pregnancy, breastfeeding
    - liver failure

    - montelukast can be given to children

    Interaction:
    - inhibit CYP-enzymes
    6. Monoclonal antibody
     omalizumab injection
    - recombinant humanized monoclonal antibody
    - sc injection every 2 to 4 weeks
    Mechanism of action:
    - bounds selectively to IgE → IgE cannot bind to IgE receptors on
    mast cells and basophiles → prevent the allergic reactions
    Use:
    - moderate to severe asthma
    Side effects:
    - injection-site reactions: redness, stinging, bruising
    - headache
    Contraindicated: pregnancy, breastfeeding
    7. Indirect sympatomimetics
     ephedrin tablet
    Effects:
    - α és β receptors
    - direct stimulatory effect on CNS and respiratory system
    - bronchodilator, GI and uterus smooth muscle dilator
    Side effects:
    - tremor, sleepiness, psychosis
    - GI: nausea, vomiting
    - Hypertension, tachycardia, arrhythmia
    - headache
    - sweating
    Contraindicated:
    - hypertension
    - hyperthyroidism
    - heart failure, arrhythmia, glaucoma

    8. Cromolyn sodium nasal spray, eye drops


    Use: allergic rhinitis, conjuctivitis
    Mechanism of action:
    - inhibits mediator release from bronchial mast cells
    9. Interleukin-5 antagonist
     mebolizumab

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