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DRUGS AFFECTING

THE RESPIRATORY
ORGANS FUNCTION
Drugs affecting the respiratory organs
function

anticough drugs;
expectorants;
breathing stimulants;
drugs used for bronchial asthma;
drugs used for lungs edema
COUGH

with presence of secretion in


dry
bronchi

PRODUCTIVE
Sputum with significant viscous-elastic
properties:
- muco- and proteolytic drugs
Sputum with significant adhesive properties: NONPRODUCTIVE
- drugs which stimulate production of surfactant Cataral inflammation (usually viral),
Decreasing of speed of mucociliar transport with reflector and central cough:
unchanged properties of sputum:
- anticough drugs
- drugs which stimulate ciliar function
Signs of allergic reaction:
Significant disorders of bronchial permeability,
morphological changes of bronchi (atrophy of - antihistamine drugs
mucous membrane, bronchial stenosis), Bronchospasm:
excessive production of mucus: - broncholytics
- alkali inhalations
Signs of allergic reaction with increased
histamine activity:
- antihistamine drugs

REHYDRANTS IN ALL CASES


Anticough drugs
Drugs of central action (depress central links
of cough reflex):
а) narcotic: codein, dextromethorphan
б) nonnarcotic: glaucin hydrochloride (glauvent),
oxeladin citrate (tussuprex)
Drugs of peripheral action (block sensitive
receptors of cough reflexogenic zones): libexin
Oxeladin citrate, Tussuprex
Glaucin hydrochloride (glauvent) + ephedrine + Sage
oil
Libexin
Expectorants
Secrete-motor drugs (stimulate expectoration):
а) drugs of reflex action: drugs of medical plants, sodium
benzoate, bronchicum elixir, mucaltin
б) drugs of resorbtive and local action: bromide -sodium
and potassium, ammonium chloride, sodium
hydrocarbonate, ether oils
Bronchosecretolytic drugs (mucolytics):
а) proteolytic enzymes: tripsin, chimopsin, chimotripsin,
desoxyribonuclease
б) mucolytics: acetylcystein, carbocystein
в) drugs which influence surfactant production or
surfactants: bromhexin, ambroxol, “Alveofakt”, “Ekzosurf”
Althea officinalis Thermopsis Viola

Drugs of medical plants


Combined remedy “Bronchicum”
Mucaltin (Mucaltinum)
Ledum palustrae Origanum vulgaris

Drugs of medical plants


Crystal tripsin (Trуpsinum crystallisatum)
Ampoules - 0,005 g and 0,01 g
Acetylcystein (Acetylcysteinum)
Forms of production: tablets - 0,1, 0,2 and 0,6, 20 % solution for inhalation in ampoules –
5 and 10 ml; 10 % solution for injection in ampoules - 2 ml and 5 % solution in ampoules – 10ml.
Bromhexin (Bromhexinum)
Аmbroxol (Lasolvan)
Forms of production: tablets - 0,03 and syrup.
COUGH
Dry
With presence of sputum in bronchi
 PRODUCTIVE
Sputum with significant viscous-elastic properties - muco- and proteolytic drugs
Sputum with significant adhesive properties - drugs which stimulate production of
surfactant
Decreasing of speed of mucociliar transport with unchanged
properties of sputum - drugs which stimulate cilia function
Significant disorders of bronchial permeability, morphological changes of bronchi (atrophy
of mucous membrane, bronchial stenosis), excessive production of mucus - alkali
inhalations
Signs of allergic reaction with increased histamine activity - antihistamine drugs
 NONPRODUCTIVE
Cataral inflammation (usually viral), reflector and central cough - anticough drugs
Signs of allergic reaction - antihistamine drugs
Bronchospasm - broncholytics

REHYDRANTS IN ALL CASES


Stimulants of breathing (analeptics)

Analeptics of direct action: bemegrid,


ethymisol, caffeine
Analeptics of mixed action: cordiamin,
camphor, carbon acid (carbogen – mixture
of O2 and CO2)
Analeptics of reflex action:
lobelin, cytiton
Aethimizol (Aethimizolum)
Sodium caffeine-benzoate (Coffeinum-natrii benzoas)
Bemegrid (Bemegridum)
Cordiamin (Cordiaminum)
Camphor (Camphora)
DRUGS FOR BRONCHIAL
ASTHMA
Introduction
 Chronic inflammatory disease of the airways
 Most common childhood chronic disease
 Affects ~4.8 million (CDC, 1995)
 >100 million days of restricted activity
 470,000 hospitalizations/yr
Introduction
 >5000 deaths annually
 Highest in blacks ages 15-24
 Hospitalizations highest in blacks & children
Pathogenesis and Definition
 Key points
 Chronic inflammatory disorder of the airways
 Immunohistopathologic features
 denudation of airway epithelium
 collagen deposition beneath basement membrane

 edema

 mast cell activation


 Working definition of asthma (1995, NHLBI)
 Asthma is a chronic inflammatory disorder of the
airways in which many cells & cellular elements
play a role (mast cells, eosinophils, T lymphocytes,
macrophages, neutrophils, & epithelial cells).
 Airflow limitation
 Acute bronchoconstriction
 stress - mechanisms ??
 Airway edema

 mediators
 increase microvascular permeability/ leakage
 mucosal thickening & airway swelling
 airway rigidity
To remove attack of bronchial asthma

Broncholytic drugs:
Adrenomimetics (α, β-adremonimetics, β-adrenomimetics, β2-
adrenomimetics)
Methylxantines
Cholinoblockers (M-cholinoblockers, ganglionblockers)

Antiallergics and drugs that reduce


airway hyperresponsiveness
Expectorants
Beta-adrenomimetics
Salbutamol, Ventolin, Berotek, Asthmopent
Asthma Treatment/Quick Relief
 Short-acting beta2 agonists
 Relax airway smooth muscle and increase in airflow
in <30 minutes
 Drug of choice for treating symptoms and
exacerbations and EIB
 Use of >1 canister/mo indicates inadequate control
and indicates need to intensify anti-inflammatory tx
 Regularly scheduled use NOT recommended
 Long-acting beta-2 agonists
 Relax airway smooth muscle
 Duration of action >12 hrs

 Not used in acute exacerbations

 Adjunct to anti-inflammatory tx for long-term


symptom control especially nocturnal symptoms
Methylxanthines
Theophyllin (of prolonged action)
 Methylxanthines
 Provides mild-moderate bronchodilation
 Low dose has mild anti-inflammatory action

 Sustained release form used as alternative but not


preferred to long-acting beta2 agonists to control
nocturnal symptoms
 Use may be necessary because of cost or patient
compliance
M-cholinoblockers
Atropine sulfate, Solutan, Ipratropii bromidum
(Atrovent)
 Anticholinergics
 Cholinergic innervation important in regulation of
airway smooth muscle tone
 Ipratropium bromide (quaternary derivative of
atropine without its’ side effects)
 Additive benefit with inhaled beta 2-agonists in
severe asthma exacerbations
 Effectiveness in long-term management not
demonstrated
Inhibitors of mast cells degranulation

 Cromolyn, Ketotifen and Nedocromil


antagonize antigen-induced (IgE-mediated) mast
cell degranulation
 they prevent the release of histamine and slow-
reacting substance of anaphylaxis (SRS-A) -
mediators of type I allergic reactions
 their beneficial effects in the treatment of
asthma are largely prophylactic
 Cromolyn & nedocromil
 Have distinctive properties
 Similar anti-inflammatory reactions
 blocks Cl - channels
 modulate mast cell mediator release

 modulate eosinophilic recruitment

 inhibits early and late asthmatic response to antigen


challenge
 Cromolyn & nedocromil
 Similar anti-inflammatory reactions
 inhibits bronchospasm (exercise, cold dry air, bradykinin
aerosol)
 nedocromil more potent in inhibiting bronchospasm in
the above situations
 Both reduce asthma symptoms
 improve PF
 reduce need for short acting beta2 agonists
 Cromolyn & nedocromil
 Dosing requirements
 recommended for both 4 X/day
 nedocromil effective at 2 X/day

 Clinical response for both is less predictable than


steroids
 Both have strong safety profile
Ketotifen
Tilade (sodium nedocromil)
Corticosteroid hormones in the management of
asthma

 In 1991- guidelines for the diagnosis and


management of asthma were published by the
National Asthma Education Program (USA).
This report described the patho-physiology of
asthma including airway obstruction, airway
inflammation, and airway hyperresponsiveness.
 Since then, corticosteroids have moved to the
forefront in the treatment of asthma.
 Corticosteroids
 Dose dependent on product and delivery device
 2 X/day use is common in moderate-to-severe
persistent asthma
 1 or 2 X/day may be used in mild persistent asthma
Inhaled corticosteroids
 Beclomethasone
 Budesonide
 Dexamethasone
 Flunisolide
 Fluticasone
 Triamcinolone

Administration corticosteroids by inhalation limits


the systemic adverse reactions associated with oral
or parenteral therapy
Administration of inhaled corticosteroids

 by the use of chambers or spacers


 these devices help decrease systemic absorption
and subsequent adverse reactions of the
corticosteroids
 most inhaled therapy is delivered via metered
dose inhalers
 other method - the breath-actuated dry powder
inhaler devices (Rotahaler, Diskhaler,
Turbuhaler)
Prednisolon, Hydrocortizone, Dexamethazone.
 Leukotriene modifiers
 Leukotrienes are potent biochemical mediators
released from mast cells, eosinophils, and basophils
that:
 contract bronchial smooth muscle
 increase vascular permeability

 increase mucus secretions

 attract & activate inflammatory cells in airways


Potential role in the treatment of asthma

 Zileuton
- a 5-lipoxygenase inhibitor
 Zafirlukast
- a leukotriene-receptor antagonist

Leukotrienes attract cellular infiltrates producing epithelial


injury, abnormalities in neural mechanisms, increases in
airway smooth muscle responsiveness, and airway
obstruction
 Leukotriene modifiers
 Zafirlukast & zileuton (oral tabs)
 improves lung fx and diminishes symptoms & need for
short-acting beta2 agonists
 Studies in mild-moderate asthma showing modest
improvements
 Alternative to low-dose inhaled steroids for pts. with
mild persistent asthma
 Further study in of other groups needed
 Leukotriene modifiers
 Zafirlukast - leuktriene receptor antagonist
 attenuates late response to inhaled allergen and post-
allergen induced bronchospasm
 modest improvement in FEV1 (11% > placebo)

 improved symptoms

 reduced albuterol use

 Warning - increases warfarin half-life and PT & PTT


must be monitored with dose adjustment when
indicated