Asthma Drugs (listed with MOA) Flashcards
**Albuterol
MOA
Adverse Effects
SHORT ACTING - ß2 specific agonist
MOA:
SMOOTH MUSCLE RELAXATION
• Increased bronchodilation by stimulating ß2 GCPR Gs receptors which cause cAMP production leading to relaxation
MAST CELL INHIBITION
• via ß2 receptor on mast cells, but this effect is only short term
INCREASED BEATING OF CILIA
• via cAMP
Adverse effects:
• TACHYCARDIA and TREMOR
• Hypokalemia is RARE
**Salmeterol
MOA
Adverse Effects
LONG-ACTING ß2 agonist:
• binds to the beta receptor for longer
Works like normal beta agonist in that it increases cAMP leading to increased ciliary beating, decreased histamine release by mast cells, and reduces bronchial smooth muscle tone.
- *BUT it MUST BE ADMINISTERED with corticosteroids because constant Beta Agonism leads to binding of Beta Arrestin and fewer functional Beta Receptors.
- *Interestingly Beta2 receptor binding may also up regulate corticosteroid receptors for a synergistic effect
**Formoterol
MOA
Adverse Effects
LONG-ACTING ß2 agonist:
• binds to the beta receptor for longer
Works like normal beta agonist in that it increases cAMP leading to increased ciliary beating, decreased histamine release by mast cells, and reduces bronchial smooth muscle tone.
- *BUT it MUST BE ADMINISTERED with corticosteroids because constant Beta Agonism leads to binding of Beta Arrestin and fewer functional Beta Receptors.
- *Interestingly Beta2 receptor binding may also up regulate corticosteroid receptors for a synergistic effect
*Atropine
MOA
Adverse Effects
ANTIMUSCARINIC AGENT
MOA:
Competitive inhibition of M1, M2, and M3 receptors
(remember M2 blockade can be bad b/c its a heteroreceptor that tells the post ganglionic neuron to stop releasing Ach)
3 main effects:
• Reduced airway smooth muscle constriction (M3 mostly, some M2)
• Decreased mucous secretion (M1 mostly, some M3)
• Enhanced ß2-mediated bronchodilation
ADVERSE EFFECTS and Contraindications:
• Pupillar dilation and increased intraocular pressure - DONT give it to people with glaucoma
**Ipratropium
MOA
Adverse Effects
ANTIMUSCARINIC AGENT
MOA:
Competitive inhibition of M1, M2, and M3 receptors
(remember M2 blockade can be bad b/c its a heteroreceptor that tells the post ganglionic neuron to stop releasing Ach)
3 main effects:
• Reduced airway smooth muscle constriction (M3 mostly, some M2)
• Decreased mucous secretion (M1 mostly, some M3)
• Enhanced ß2-mediated bronchodilation
ADVERSE EFFECTS and Contraindications:
• Pupillar dilation and increased intraocular pressure - DONT give it to people with glaucoma
*Tiotropium
MOA
Adverse Effects
ANTIMUSCARINIC AGENT
MOA:
Competitive inhibition of M3 receptors MOSTLY (while there is some stimulation of M1 and even less of M2, this is negligible)
4 main effects
Added effect = reduced airways smooth muscle constriction
• Reduced airway smooth muscle constriction (M3 mostly, some M2)
• Decreased mucous secretion (M1 mostly, some M3)
• Enhanced ß2-mediated bronchodilation
ADVERSE EFFECTS and Contraindications:
• Urinary Retention
*Theophylline
MOA
Adverse Effects
Type of Caffeine
MOA:
Fast:
• inhibits phosphodiesterase that breaks cAMP down and increased cAMP levels cause smooth muscle relaxation
Long term:
• causes histone deacetylation which down regulates gene expression of inflammatory genes
Adverse Effects;
• Nevousness, Siezures in extremely high serum levels
Aminophylline
MOA
Adverse Effects
Type of Caffeine
MOA:
Fast:
• inhibits phosphodiesterase that breaks cAMP down and increased cAMP levels cause smooth muscle relaxation
Long term:
• causes histone deacetylation which down regulates gene expression of inflammatory genes
Adverse Effects;
• Nevousness, Siezures in extremely high serum levels
Cromolyn sodium
MOA
Adverse Effects
MOA:
• Inhibits degranulation of mast cells in the lung and Inhibits the inflammatory response on eosinophils
• REDUCES BRONCHIAL HYPERACTIVITY WITH EXERCIDSE and ANTIGEN inhaled asthma
Adverse Effects:
• Adverse effects are rare
**Fluticasone
MOA
Adverse Effects
MOA:
Downregulates cytokine and chemokine production by inhibiting Histone Deacetylase
Also, decreases mRNA stability for genes like TNF-alpha, IL-6, GM-CSF, and COX-2
May also prevent GATA-3 and MAPK from entering the nucleus to produce TH2 cytokines like IL-5, IL-4, and IL-13
- Decreases the production of inflammatory cytokines and activates anti-inflammatory genes
- Reduces mucous secretion
- ENHANCES the EFFECT OF ß2-agonists
Adverse Effects:
• Oropharyngeal Candidiasis and Osteopenia (very rarely)
**Budesonide
MOA
Adverse Effects
MOA:
Downregulates cytokine and chemokine production by inhibiting Histone Deacetylase
Also, decreases mRNA stability for genes like TNF-alpha, IL-6, GM-CSF, and COX-2
May also prevent GATA-3 and MAPK from entering the nucleus to produce TH2 cytokines like IL-5, IL-4, and IL-13
- Decreases the production of inflammatory cytokines and activates anti-inflammatory genes
- Reduces mucous secretion
- ENHANCES the EFFECT OF ß2-agonists
Adverse Effects:
• Oropharyngeal Candidiasis and Osteopenia (very rarely)
**Levalbuterol
MOA
Adverse Effects
SHORT ACTING - ß2 specific agonist
R-isomer of albuterol, given to reduce the adverse effects
MOA:
SMOOTH MUSCLE RELAXATION
• Increased bronchodilation by stimulating ß2 GCPR Gs receptors which cause cAMP production leading to relaxation
MAST CELL INHIBITION
• via ß2 receptor on mast cells, but this effect is only short term
INCREASED BEATING OF CILIA
• via cAMP
**Monteleukast
MOA
Adverse Effects
MOA:
Block LTD4 receptors - b/c LTC4 and LTD4 are responsible for many of the symptoms of asthma (bronchial hyperreactivity, bronchoconstriction, and mucosal edema)
IDEAL FOR ASPRIN INDUCED ASTHMA
Adverse Effects:
• just typical shit
**Zafirlukast
MOA
Adverse Effects
MOA:
Block LTD4 receptors - b/c LTC4 and LTD4 are responsible for many of the symptoms of asthma (bronchial hyperreactivity, bronchoconstriction, and mucosal edema)
IDEAL FOR ASPRIN INDUCED ASTHMA
Adverse Effects:
• maybe elevated liver enzymes in some ppl
**Zileuton
MOA
Adverse Effects
MOA:
• Inhibits ALL leukotriene formation by BLOCKING 5-LIPOOXIGENASE (preventing it from acting on arachiodonic acid)
Adverse Effects:
• Causes Hepatic Enzyme Elevation***
