Pulmonary Pharmacology Flashcards
Cholinergic Input
Stim. muscarinic receptor ^ activity of guanyl cyclase > conversion of GTP to cyclic GMP.
Cyclic GMP > BRONCHOCONSTRICTION.
Cyclic GMP broken down by phosphodiesterase
SNS Beta2 input
Stim. Beta2 receptor ^ activity of adenyl cyclase > conversion of ATP to cyclic AMP. Cyclic AMP (second messenger) ^ activity of protein kinase > inhibits smooth muscle contraction > BRONCHODILATION. Cyclic AMP broken down by phosphodiesterase
SNS Alpha input
Stim. Alpha1 receptor > decrease cyclic AMP > BRONCHOCONSTRICTION (in diseased lungs only)
Histamine
Heparin
Tryplase
Allergen induced Mediators of BRONCHOCONSTRICTION
Immediate to 5 min. response
Arachidonic Acid producing Leukotriente-D4 and Prodstaglandin-D2
Allergen induced Mediators of BRONCHOCONSTRICTION
5-30 min. response
TNF-alpha and IL-4
Allergen induced Mediators of BRONCHOCONSTRICTION
Hours to respond
Albuterol (Salbutamol (INN), Proventil, Ventolin)
Bronchodilator
Sympathomimetic (Beta2 agonist)
Selective
Fast acting - “rescue drug”
Terbutaline (Brethine, Brethine tablet)
Bronchodilator
Sympathomimetic (Beta2 agonist)
Selective
Short acting
Salmeterol (Serevent)
Bronchodilator
Sympathomimetic (Beta2 agonist)
Selective
Long acting
Formoterol (Oxeze, Foradil)
Bronchodilator
Sympathomimetic (Beta2 agonist)
Selective
Long acting
Itolterol (Tornalate)
Bronchodilator
Sympathomimetic (Beta2 agonist)
Selective
Long acting
Metaproterenol (Alupent)
Bronchodilator
Sympathomimetic (Beta2 agonist)
Selective
Long acting
Pirbuterol (Maxair)
Bronchodilator
Sympathomimetic (Beta2 agonist)
Selective
Long acting
Ephedrine (alpha-mild activity, beta1-mod. activity, beta2- more activity)
Bronchodilator
Sympathomimetic (Beta2 agonist)
NON-selective
Epinephrine or Adrenaline (alpha-mod. activity, beta1-storng activity, beat2-mod. activity)
Bronchodilator
Sympathomimetic (Beta2 agonist)
NON-selective
Isoproterenol (Isuprel) - beta1, beta2
Bronchodilator
Sympathomimetic (Beta2 agonist)
NON-selective
Ethylnorepinephrine - beat1, beta2
Bronchodilator
Sympathomimetic (Beta2 agonist)
NON-selective
Side effects of selective drugs
Nervousness
Headaches
Tremors
Side effects of NON-selective drugs
Nervousness, Headaches, Tremors
Results of beta stim.: tachycardia, angina, cardiac dysrhythmias
Results of alpha stim.: peripheral vasoconstriction
Phentolamine
Bronchodilator
Sympatholytic (Alpha agonist)
Bronchconstriction by blocking alpha receptors
Ipratropium (Atrovent)
Bronchodilator
Parasympatholytic (anti-cholingergics)
Blocks cholinergic receptor - causes BRONCHODILATION
Aiminophylline
Bronchodilator
Methylxanthine
BRONCHODILATION
Theophylline (Theo-dur)
Bronchodilator
Methylxanthine
BRONCHODILATION
Side effects of Methylxanthines
Can be serious or life threatening
Therapeutic levels: 10-20mg/ml
Toxic level: 15-20mg/ml
Plasma levels are monitored closely