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b. Respiratory depressant
d. Nasal decongestants
RESPIRATORY DRUGS (cont’d)
a. Bronchodilators
b. Anti-inflammatory drugs
c. Others
RESPIRATORY STIMULANTS
(ANALEPTICS)
Stimulates respiration by increasing activity of
carotid chemoreceptors (PO2) or respiratory
centre (PCO2) or both
No longer in popular use. Only occasionally
used, in ventilatory failure due to chronic
obstructive disease, but not in ventilatory
failure due to severe asthma or overdose of
CNS depressants
Largely replaced by mechanical ventilation
RESPIRATORY STIMULANTS
(ANALEPTICS)
a. No inhibition of ciliary
activity
b.
c. No
Noinhibition of secretions
constipation
d. No liability to addiction
:Nasal Congestion
• Results from oedema of nasal mucosa
• Occurs mainly in
- Flu (URTI)
- Rhinitis
(allergic or non-allergic)
RHINITIS
(The inside story)
NASAL DECONGESTANTS
Mechanisms of Action
Vasoconstriction (α 1(receptor activation •
.)e.g., phenylephrine(
Bronchodilation
Bronchoconstriction
Histamine Adrenaline
Leukotrienes PGE2
Acetylcholine EpDRF
PGD2 NO
Neuropeptides
Adenosine
Etc
CONTROL OF AIRWAY CALIBRE
Bronchoconstriction Bronchodilation
Ach *** Catecholamines ***
(adrenaline)
PGF2α PGD NANC (VIP? NO?)
Substance P? PGE2
Neurokinins?
ANTIGEN-INDUCED DEGRANULATION OF MAST CELL
AND THE RELEASE OF ALLERGIC MEDIATORS
allergen
IgE antibody
Mediator release
-histamine
Mast Cell
-PAF
-leukotrienes
-PGD2
Bronchoconstriction
Bronchial hyper-reactivity
Anti-inflammatory Agents
- Corticosteroids
- Anti-rheumatics
- Immunosupressors
Others
- DSCG, Nedocromil, etc.
BRONCHODILATORS
4 Groups
d. Anti-Leukotriene Drugs
• Cyst-LT receptor antagonists (eg, Zafirlukast)
• LT synthesis inhibitors (eg, Zileutin)
BETA ADRENOCEPTOR AGONISTS
Drugs Receptor Specificity
α, ß 1, ß2
Adrenaline +++ +++ +++
Nor-adrenaline +++ + +
Isoprenaline - +++ +++
Salbutamol - + +++
Terbutaline - + +++
Remiterol - + +++
Fenoterol - + +++
Salmeterol Long- - + +++
formoterol acting
Mechanism of Action ofβ 2-receptor agonists
β 2-receptor
G-protein
Adenylate cyclase
MUSCLE REAXATION
CLINICAL USE OF ß2 AGONISTS
Most widely used antiasthma drugs
Drug of choice for acute attack
Salbutamol and terbutaline most used
Given by inhalation, but also orally
Instant effect (lasts 3-5h; 12h for some)
Also used in chronic bronchitis
ADVERSE EFFECTS OF ß2 AGONISTS
Muscle tremor
ß1 -mediated tachycardia
May mask deterioration of asthma
XANTHINE DERIVATIVES
Theophylline (aminophylline)-prototype
Enprofylline
Proxifylline
Actions of Xanthine Derivatives
Bronchodilators
Stimulate heart & CNS (use is beverage)
Has anti-inflammatory effect
Mechanisms of Action
Inhibition of phosphodiesterases?
Antagonism of adenosine receptors?
Release of adrenaline?
Mechanism of Action ofβ 2-agonists
and PDE Inhibitors
β 2-receptor
PDE
Inhibitors
G-protein
Adenylate cyclase
PDE AMP-’5
ATP cAMP
Myosin-P Myosin
MUSCLE REAXATION
MUSCLE CONTRACTION
CLINICAL USE OF XANTHINE DERIVATIVES
IN ASTHMA
- Corticosteroids
- Immunosupressors
- Others
STEROIDS (GLUCOCORTICOIDS)
IN ASTHMA
Powerful anti-inflammatory and
immunosuppressive actions
No bronchodilator effect
- Beclomethasone (aerosol)
- Budesonide (aerosol)
- Prednisolone (systemic, oral)
- Hyrocortisone (systemic, IV)
Mechanism of Action of Steroids
in Asthma
Steroid
Cytokine Annexins
s(IL-1, TNFa, IL-5, IL-4, GM-CSF) (lipocortins)
Caution in children
ADVERSE EFFECTS OF STEROIDS
Aerosol:
Oropharyngeal candidiasis
Dysphonia
Systemic:
Adrenal insufficiency (if withdrawn rapidly)
Osteoporosis
Lowered resistance to infection
Cushing’s syndrome
Hyperglycemia
DISODIUM CROMOGLYCATE IN
ASTHMA
Prophylactic anti-asthma drug
No bronchodilator effect
Affects all forms of asthma
More effective in children than adults
Drug of choice in children
Effective against both early & late phases
DISODIUM CROMOGLYCATE IN
ASTHMA (cont’d)
Poorly absorbed, given by inhalation
Has some anti-inflammatory effect
May also act by inhibiting neuronal reflex and
stabilization of mast cells
No side effects except cough by particle
irritation
OTHER ANTI-ASTHMA DRUGS
KETOTIFENHT antagonist.
• Effect due mainly to anti-inflammatory action.
• Effective orally.
• Effect develops after 2-3 weeks
NEDOCROMIL SODIUM
• Similar to DSCG in many respects.
METHOTHREXATE/CYCLOSPORIN-A
OXYGEN
Learning Objectives
Classify bronchodilators and describe the mechanism of .1
.action of each group
Muscle relaxation
(Similar mechanism on mast cells inhibit mediator release)