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Asthma Drugs 2
a
18
Pharmacology
Graduate
08/30/2012

Additional Pharmacology Flashcards

 


 

Cards

Term
Most potent drug for long-term control of asthma
Definition
Glucocorticoids
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
Adverse drug effects
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
Mast Cell Stabilizers
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
Immune Modulators
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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