pharmacology of respiratory drugs
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PHARMACOLOGY OF RESPIRATORY DRUGS. Susanne Young May 04’. content. Physiology/ sites of action Review drugs in use Main considerations in anaesthesia. Control of bronchial tone+++. ß2. Muscarinic ACh. Ad Cyclase. G.Cyclase. +. _. GTP. ATP. cAMP. Kinases. cGMP. PDE. 5’AMP.

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pharmacology of respiratory drugs

PHARMACOLOGY OF RESPIRATORY DRUGS

Susanne Young

May 04’

content
content
  • Physiology/ sites of action
  • Review drugs in use
  • Main considerations in anaesthesia
control of bronchial tone
Control of bronchial tone+++

ß2

Muscarinic ACh

Ad Cyclase

G.Cyclase

+

_

GTP

ATP

cAMP

Kinases

cGMP

PDE

5’AMP

prostaglandin synthesis
Prostaglandin Synthesis

Phospholipids

PLA2

Arachidonic Acid

Lipoxygenase

COX

PGG2

5HPETE

Leukotrienes

IgE

TXA2

PGI2

common respiratory drugs
Common Respiratory Drugs
  • ß2 agonists
  • Long acting ß2 agonists
  • Anti-cholinergics
  • Inhaled steroids
less common
Less common
  • Leukotriene receptor antagonist
  • Methylxanthines
  • Sodium cromoglycate
2 agonists
ß2 AGONISTS
  • Salbutuamol, Bricanyl, Terbutaline
  • Less selective in hi dose- get ß1effect
  • 100mcg per puff lasts 4hrs or so.
  • Salmeterol, Eformoterol
  • Last 12 hrs or so
  • 15x more potent at ß2 than Salbutamol
side effects
Side Effects
  • ß2 Muscle tremor
  • Hypokalaemia (Na+/K+ ATPase)
  • ß1 Anxiety
  • Nausea and vomitting
  • Hypertension
  • Tachyarryhthmias
  • Dizziness/ Headache
anticholinergics
Anticholinergics
  • 200 yrs ago Datura plants were smoked!
  • Atropine later
  • Then more selective agents
  • Ipatropium
  • Peak effect 30-60 mins
  • Lasts 6hrs or so
  • Spireva= Tiotropium- longer acting o.d egg
inhaled steroids
Inhaled steroids
  • Becotide/ Flixotide/ Pulmicort
  • Dose range 100 mcg to 1g per day
  • Peak effect 6-12hrs
  • Anti- inflammatory
  • Sensitise ß2 receptors
  • Prevent tachyphlaxis
methylxanthines
Methylxanthines
  • Caffeine related!
  • In use since 1930
  • Very alkaline- never give im
  • Therapeutic range 10-20mg/l
  • Half life increased in: CCF, elderly
  • Decreased in smokers, enzyme induction
  • Side Effects incl:
  • Inc HR, FOC, arrythmias.
  • Inc GORD. Hypokalaemia, seizures
methylxanthines cont
Methylxanthines (cont)
  • Proposed mechanisms:
  • PDE Inhibition
  • Adenosine (causes mast cell degranulation) Receptor Antagonism
  • Prostaglandin Inhibition
  • Endogenous CA release
leukotriene receptor antagonists
Leukotriene Receptor Antagonists
  • Good in rhinitis
  • Not better than but additive to steroids
  • Steroid sparing
  • Preventer
sodium cromoglycate
Sodium Cromoglycate
  • Mast cell stabiliser, closes Ca++ channels
  • May be of use in allergic asthma in kids
  • Preventer, but
  • Not as effective as inhaled steroid
considerations conclusions
Considerations/ Conclusions
  • ? Avoid Histamine releasing drugs
  • ? Avoid NSAID’s
  • ß2 agonists, corticosteroids, Theophylline (and Sux) all cause Hypokalaemia
  • Arrythmias are potentiated by hypoxia
ad