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ANTI-INFLAMMATORY AGENTS
  USED IN ASTHMA AND COUGH
  SUPPRESSANTS




ANKIT GILANI
DEPT OF PHARMACOLOGY AND TOXICOLOGY
NIPERA1113PC03 (sem-1)
SUBJECT – PC-620
ASTHMA

 An inflammatory condition in which there is
  recurrent reversible airways obstruction in
  response to irritant stimuli that are too weak to
  affect non-asthmatic subjects.

                       symptoms




                        shortness of
       wheezing     breath ( especially   cough.
                     in breathing out)
PATHOGENESIS
characterised by:




 inflammation of the airways
 bronchial hyper-reactivity
 reversible airways obstruction
TREATMENT



BRONCHODILATORS
                             ANTI-INFLAMMATORY
   β-Adrenoceptor
      agonists,                    AGENTS
  Xanthine drugs ,                 Glucocorticoids ,
 Muscarinic receptor               Cromoglicate and
   antagonists,                      nedocromil ,
Cysteinyl leukotriene          Anti-IgE treatment .
receptor antagonists,
Histamine H1-receptor
     antagonists.
ANTI-INFLAMMATORY AGENTS

 Mainly glucocorticoids
 Cromoglicate and nedocromil (weak anti-
  inflammatory and short duration , now
  hardly used for asthma)
 Omalizumab
  (humanised monoclonal anti-IgE antibody)
Mechanism of glucocorticoids
 decrease formation of cytokines, in particular the
  Th2 cytokines that recruit and activate eosinophils
  and are responsible for promoting the production of
  IgE and the expression of IgE receptors.

 Glucocorticoids also inhibit the generation of the
  vasodilators PGE2 and PGI2, by inhibiting induction of
  COX-2

 By inducing annexin 1, they could inhibit production
  of leukotrienes and platelet- activating factor.
 Corticosteroids inhibit the allergen-induced
  influx of eosinophils into the lung.

 Glucocorticoids up-regulate β2
  adrenoceptors, decrease microvascular
  permeability, and indirectly reduce
  mediator release from eosinophils by
  inhibiting the production of cytokines (e.g.
  IL-5 and granulocyte-macrophage colony-
  stimulating factor) that activate
  eosinophils.
EXAMPLES :
1) Systemic ( given orally) :
 Prednisone
 Prednisolone
 Methylprednisolone


2) Inhaled :
 Beclometasone
 Budenoside
 Fluticasone
 Mometasone
 Ciclesonide
Unwanted effects

Systemic :

 Thinning of the skin, Tendency to bruise,
Osteoporosis, Muscle Weakness, Infections
,Hypertension, etc.
inhaled :
Oropharyngeal candidiasis (thrush)
sore throat and croaky voice
  [ use of 'spacing' devices, reduces these
problems ]
DRUGS FOR COUGH
COUGH : a protective reflex that removes foreign
  material and secretions from the bronchi and
  bronchioles.

 It can be triggered by inflammation in the
  respiratory tract, for example by undiagnosed
  asthma or chronic reflux with aspiration, or by
  neoplasia.

 In these cases, cough suppressant (antitussant)
  drugs are useful.
DRUGS FOR COUGH

  Pharyngeal demulcents


  Expectorants (mucokinetics)


  Antitussives (cough centre suppressants)


  Adjuvant antitussives (bronchodilators)
MECHANISM OF COUGH SUPPRESSION

 Antitussive drugs act by an ill-defined effect in
  the brain stem, depressing the 'cough centre'.
 All opioid narcotic analgesics have antitussive
  actions in doses below those required for pain
  relief.
 Those used as cough suppressants are members
  of the group with minimal analgesic actions and
  addictive properties.
 New opioid analogues that suppress cough by
  inhibiting release of excitatory neuropeptides
  through an action on ÎĽ receptors on sensory
  nerves in the bronchi are being assessed.
EXAMPLES

 Codeine (methylmorphine) is a weak opioid
  with considerably less addiction liability than
  the main opioids, and is a mild cough
  suppressant.
 It decreases secretions in the
  bronchioles, which thickens sputum, and
  inhibits ciliary activity. Constipation is
  common.

 Dextromethorphan and pholcodine are
  believed to have fewer adverse effects.
Anti inflammatory agents used in asthma and cough suppressants

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Anti inflammatory agents used in asthma and cough suppressants

  • 1. ANTI-INFLAMMATORY AGENTS USED IN ASTHMA AND COUGH SUPPRESSANTS ANKIT GILANI DEPT OF PHARMACOLOGY AND TOXICOLOGY NIPERA1113PC03 (sem-1) SUBJECT – PC-620
  • 2. ASTHMA  An inflammatory condition in which there is recurrent reversible airways obstruction in response to irritant stimuli that are too weak to affect non-asthmatic subjects. symptoms shortness of wheezing breath ( especially cough. in breathing out)
  • 4. characterised by:  inflammation of the airways  bronchial hyper-reactivity  reversible airways obstruction
  • 5. TREATMENT BRONCHODILATORS ANTI-INFLAMMATORY β-Adrenoceptor agonists, AGENTS Xanthine drugs , Glucocorticoids , Muscarinic receptor Cromoglicate and antagonists, nedocromil , Cysteinyl leukotriene Anti-IgE treatment . receptor antagonists, Histamine H1-receptor antagonists.
  • 6. ANTI-INFLAMMATORY AGENTS  Mainly glucocorticoids  Cromoglicate and nedocromil (weak anti- inflammatory and short duration , now hardly used for asthma)  Omalizumab (humanised monoclonal anti-IgE antibody)
  • 8.  decrease formation of cytokines, in particular the Th2 cytokines that recruit and activate eosinophils and are responsible for promoting the production of IgE and the expression of IgE receptors.  Glucocorticoids also inhibit the generation of the vasodilators PGE2 and PGI2, by inhibiting induction of COX-2  By inducing annexin 1, they could inhibit production of leukotrienes and platelet- activating factor.
  • 9.  Corticosteroids inhibit the allergen-induced influx of eosinophils into the lung.  Glucocorticoids up-regulate β2 adrenoceptors, decrease microvascular permeability, and indirectly reduce mediator release from eosinophils by inhibiting the production of cytokines (e.g. IL-5 and granulocyte-macrophage colony- stimulating factor) that activate eosinophils.
  • 10. EXAMPLES : 1) Systemic ( given orally) :  Prednisone  Prednisolone  Methylprednisolone 2) Inhaled :  Beclometasone  Budenoside  Fluticasone  Mometasone  Ciclesonide
  • 11. Unwanted effects Systemic : Thinning of the skin, Tendency to bruise, Osteoporosis, Muscle Weakness, Infections ,Hypertension, etc. inhaled : Oropharyngeal candidiasis (thrush) sore throat and croaky voice [ use of 'spacing' devices, reduces these problems ]
  • 12.
  • 13. DRUGS FOR COUGH COUGH : a protective reflex that removes foreign material and secretions from the bronchi and bronchioles. It can be triggered by inflammation in the respiratory tract, for example by undiagnosed asthma or chronic reflux with aspiration, or by neoplasia. In these cases, cough suppressant (antitussant) drugs are useful.
  • 14. DRUGS FOR COUGH Pharyngeal demulcents Expectorants (mucokinetics) Antitussives (cough centre suppressants) Adjuvant antitussives (bronchodilators)
  • 15. MECHANISM OF COUGH SUPPRESSION  Antitussive drugs act by an ill-defined effect in the brain stem, depressing the 'cough centre'.  All opioid narcotic analgesics have antitussive actions in doses below those required for pain relief.  Those used as cough suppressants are members of the group with minimal analgesic actions and addictive properties.  New opioid analogues that suppress cough by inhibiting release of excitatory neuropeptides through an action on ÎĽ receptors on sensory nerves in the bronchi are being assessed.
  • 16. EXAMPLES  Codeine (methylmorphine) is a weak opioid with considerably less addiction liability than the main opioids, and is a mild cough suppressant.  It decreases secretions in the bronchioles, which thickens sputum, and inhibits ciliary activity. Constipation is common.  Dextromethorphan and pholcodine are believed to have fewer adverse effects.