Anti-Asthma Drugs Flashcards
Responsible for processing the oxygen into the blood system and exhaling carbon dioxide
Respiratory System
Episodic narrowing and inflammation of the airway caused by stimuli
Asthma
What are the possible causes of asthma?
Allergens, exercise, stress
Two types of COPD (Chronic Obstructive Pulmonary Disorder)
Chronic bronchitis and Emphysema
COPD characterized by problems with mucous secretion that leads to bronchoconstriction
Chronic bronchitis (aka “Blue Bloaters”)
COPD characterized by elasticity of the alveoli which results into difficulty of inhaling air
Emphysema (aka “Pink Puffers”)
Thick mucous secretion excreted into the lungs; these mucous are stuck in the lungs
Cystic Fibrosis
Infection caused by Mycobacterium tuberculosis
Tuberculosis
Asthma is referred to as the inflammation of airways, what could be a possible result?
Cascade of inflammatory mechanisms, resulting to bronchoconstriction -> no passage of air
Treatment of Asthma
- Dilation of airway
- Reduction of inflammation
Class of drugs that binds to the beta receptors, stimulating cAMP in the smooth muscles causing relaxation
Sympathomimetic agents
Sympathomimetic agents are similar to ____ and ____?
Epinephrine and Norepinephrine
Sympathomimetic agents are best delivered how?
Through inhalation -> concentrated in the lungs
Rapid acting bronchodilator when injected subQ or inhaled
Epinephrine
Epinephrine’s maximal bronchodilation is achieved _____ and lasts for _____?
15 minutes after inhalation, lasts for 60-90 minutes
T or F: Epinephrine causes adverse reactions when inhaled?
False, when injected subQ
Adverse effects of Epinephrine when injected subQ
Tachycardia, Arrhythmia, Worsening of angina pectoris
Indications of Epinephrine
- Acute vasodilation
- Shock
- Bronchospasm of anaphylactic shock
Has a more pronounced central activity and much lower potency; longer duration of action than Epinephrine
Ephedrine
T or F: Ephedrine is frequently used in the management of asthma
False
Potential non-selective B1 and B2 bronchodilator
Isoproterenol
T or F: Isoproterenol is rarely used in the management of asthma
True, due to its non-specificity (B1 and B2)
Drugs that are commonly used for asthma and is a part of maintenance drugs
Beta-selective Drugs
T or F: Beta-selective drugs are effective after ingestion and have a longer duration of action than Epinephrine and Isoproterenol
True
Can long-acting and ultra long-acting beta-selective drugs be combined?
Yes
Sympathomimetic agents that given as “relievers” because it can only be given if the patient/s already know the cause of asthma
Short Acting Beta-2 Agonists (SABA)
SABA drugs
Terbutaline, Albuterol, Metaproterenol, Pirbuterol (PAMT)
Route of Admin of Albuterol (SABA)
Inhaled or Oral
Route of Admin of Terbutaline
Inhaled, Oral, SubQ
Route of Admin of Metaproterenol and Pirubterol
Inhaled
Possible effect of Terbutaline when given large doses
Inhibition of uterine contraction for premature labor
Sympathomimetic agents that are given as “controllers” because they can be given even without asthma attacks
Long Acting Beta-2 Agonists (LABA)
LABA that is a partial agonist
Salmeterol
LABA that is a full agonist
Formeterol
Why does LABA drugs have a duration of action of 12 or more hours?
Due to their high lipid solubility
Beta-blocker agonist that is used for the treatment of COPD
Ultra Long-Acting Beta-2 Agonist
Ultra Long-Acting Beta-2 Agonists are taken ____ daily?
Once daily
Purine derivates who’s MOA is the inhibition of phosphodiesterase to increase cAMP levels
Methylxanthines
Methylxanthine drugs
Caffeine, Theophylline, Theobromine
Stimulates cardiac function, relaxation of smooth muscles, and reduction in immune and inflammatory activity
cAMP
T or F: Theophylline is absorbed well in the GI and is metabolized by the liver
True
Side-effects of Theophylline
GI distress, Tremor, Insomnia
Toxicities of Theophylline
Arrhythmia, Hypotension, Vomiting
Antidote for Methylxanthine overdose
Beta-blockers
Class of drugs that competitively inhibits the action of acetylcholine at the muscarinic receptor
Antimuscarinic agents
T or F: Antimuscarinic agents blocks the contraction of the airway smooth muscles and decreases secretion of mucus
False, increases secretion of mucus
Prototypic muscarinic antagonist
Atropine
T or F: Muscarinic antagonists can be given for asthma without Beta-agonists
False, cannot be given (MA and BA comes hand in hand)
Short-acting Muscarinic Antagonist (SAMA)
Ipratropium
Selective quaternary ammonium derivative of atropine
Ipratropium
T or F: Ipratropium can be delivered into the circulation and does not readily enter the CNS
True
Ipratropium is effective in patients with ______ just like _____
COPD, Albuterol
Long-acting Muscarinic Antagonists (LAMA)
Tiotropium, Aclidinium
Binds to the M1, M2, and M3 receptors with equal affinity but dissociates most rapidly from M2 receptors
LAMA (Tiotropium, Aclidinium)
LAMA are taken in by _____
Inhalation
T or F: LAMA are part of the maintenance medications for patients with Asthma
False, they are only given as add ons
Class of drugs that inhibit phospholipase A2 and COX-2 expression -> reducing inflammatory cytokines and reduced thickness on the respiratory mucosa
Corticosteroids
T or F: Corticosteroids has an effect on dilation
False
What kind of corticosteroids are commonly used?
Inhaled
Corticosteroids are routinely used in combination with what?
Beta-agonists
Are oral and parenteral corticosteroids used on a normal basis?
No, they are reserved for patients requiring urgent treatment
Corticosteroids given for urgent treatment
Prednisolone (oral)
Methylprednisolone (IV)
Inhalational corticosteroids
Beclomethasone, Budesonide, Ciclesonide, Flunisolide, Fluticasone, Mometasone, Triamcinolone
T or F: Inhalation Corticosteroids (ICS) are delivered with minimal system absorption
True, hence, more concentrated in the lungs
Side effect of ICS
Oropharyngeal candidiasis - fungal infection around oral cavity that can be combatted with oral hygiene
Class of drugs that has no effect on the airway’s smooth muscle tone
Anti-inflammatory drugs; Release inhibitors
Drugs that are effective in inhibiting both antigen and exercise-induced asthma
Release inhibitors
Release inhibitors drugs
Cromolyn, Nedocromil
T or F: Release inhibitors have low solubility and are poorly absorbed from the GI tract
True, hence should be inhaled
Alters the function of delayed chloride channel in cell membrane -> inhibiting its activation
Release inhibitors
Release inhibitors acts on _____ and _____ both containing _____ that leads to inflammatory cascade
Mast cells and Eosinophils, collectively known as Histamine
Release inhibitors are useful for reducing __________
Allergic Rhinoconjunctivitis
Side effects of Release inhibitors include:
Throat irritation, cough, mouth dryness, wheezing, chest tightness
T or F: To prevent release inhibitors symptoms, B2 agonist is needed to be administered beforehand
True
Results from the action of 5-lipoxygenase on arachidonic acid, synthesized by various inflammatory cells in the airways
Leukotrienes
Potent neutrophil chemoattractant
LTB4
Exerts many effects known to occur in asthma such as bronchoconstriction, increased bronchial activity, mucosal edema, and mucus hypersecretion
LTC4 and LTD4
Class of drugs whose MOA is to either inhibit 5-lipoxygenase or inhibit binding of LTD4 to its receptor
Leukotriene Pathway inhibitors
Drugs classified as LT Pathway inhibitors
Zileuton, Zafrilukast, Montelukast
5-lipoxygenase inhibitor
Zileuton
LTD4 receptor antagonists
Zafrilukast and Montelukast
Route of admin of LTD4 receptor antagonists
Oral
Most prescribed Leukotriene Receptor Antagonist which is approved for children and is taken once daily
Montelukast
T or F: Montelukast should be taken with meals
False, it has no regard to meals
Least prescribed Leukotriene Receptor Antagonist due to its liver toxicity
Zileuton
T or F: Leukotriene Receptor Antagonists are as effective as inhaled steroids
False
T or F: Leukotriene Receptor Antagonist are recommended for acute asthma
False
Leukotriene Receptor Antagonist are effective in:
- Exercise-induced bronchospasm
- Antigen 2-induced bronchospasm and aspirin allergy
- Aspirin-induced bronchospasm
Humanized murine monoclonal antibody
Omalizumab
Prevents the activation by asthma trigger antigens
Omalizumab
Class of drug that inhibits the binding of IgE but does not activate IgE already bound to mast cells
Anti-IgE Monoclonal Antibodies
Route of administration of Anti-IgE
Subcutaneous
T or F: Omalizumab is given as last line treatment
True