Term
| Most potent drug for long-term control of asthma |
|
Definition
|
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Term
| Effect of Glucocorticoids on Macrophage, Monocytes, Lymphocytes |
|
Definition
| Interleukins(1,2,3,6), TNF(alpha) and INF(gamma) are reduced or inhibited |
|
|
Term
| Effects of Glucocorticoids on Endothelial Cells |
|
Definition
| Endothelial leukocyte adhesion molecule-1 (ELAM-1), intracellular adhesion molecule-1 (ICAM-1), Vascular adhesion molecule (VCAM-1) reduced |
|
|
Term
| Therapeutic effects in asthma |
|
Definition
- Inhibition of eosinophilic airway inflammation
- increase in the number o beta-2 receptors and responsiveness
- Decrease in mucus production and hypersecretion
- decrease in vascular permeability
|
|
|
Term
| Goals for Inhaled Cortico Steriods |
|
Definition
- High pulmonary deposition
- Low oropharyngeal absorption and adverse effects
- Low systemic bioavailability
- High pulmonary deposition
|
|
|
Term
|
Definition
- Frequent local adverse events include oral candidiasis and dysphonia
- Inhaled steroids may cause reflex cough
- Concern of growth retardation in children
|
|
|
Term
| Combination of ICS with LABA |
|
Definition
Most effective combination therapy for asthma control
indicated for patients with inadequately controlled by low dose inhaled corticosteroids |
|
|
Term
|
Definition
- Cromolyn (Intal)
- Nedocromil (Tilade)
|
|
|
Term
| Characteristics of Mast Cell stabilzer |
|
Definition
Only good when prophylactically.
Chronic use may reduce overall bronchial reactivity
No effect on airway smooth muscle tone
Only administered by inhalation |
|
|
Term
| Leukotriene Receptor antagonist (Drugs) |
|
Definition
Zafirlukast (Accolate) - oral 20mg BID. Decreased w/ meals
Montelukast (Singulair) - 10mg each night |
|
|
Term
| 5-Lipoxygenase Inhibitors |
|
Definition
Effect the rate limiting step of luekotrienes synthesis
Zileuton 600 mg extended release
ADE: increase liver enzymes, reversible hepitis and hyperbilirubinemia.
PK interactions: 3A4 substrate. |
|
|
Term
|
Definition
Novel Drugs
Omalizumab (Xolair) Offered to severe allergic asthma not well controlled by standard medication
SubQ injection every 2-4 weeks
MOA: Anti-IgE antibody - antibody against IGE antibodies
|
|
|
Term
| Steroids SAR: C1-C2 double bond |
|
Definition
| Reduce Mineralocorticoid activity |
|
|
Term
| Steroids SAR: Halogenation at C6 and or C9 |
|
Definition
| Increases GR and MR affinity |
|
|
Term
| Steroids SAR: Esterification at C17 or C21 |
|
Definition
| More lipophilic molcule with increased permeability and metabolic activity. |
|
|
Term
| Inactive Prodrug forms of Glucocorticosteroids |
|
Definition
| Beclomethasone dipropionate and Ciclesonide |
|
|
Term
| Low Systemic bioavailable Glucocorticoids |
|
Definition
| Mometasone Furoate, Ciclesonide, Fluticasone propionate |
|
|
Term
| Intracellular fatty acid conjugation |
|
Definition
| Budesonide and Des-Ciclesonide |
|
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