Respiratory Drugs and Autacoids Flashcards
Formoterol is also used as a reliever due to its short onset of action and longer duration of ___ hours
12 hours
R-isomer of albuterol used in children with asthma
Levalbuterol
Beta-agonist that inhibits uterine contractions to prevent premature labor
Terbutaline
Which of the following ultra-LABA may be used as monotherapy for treatment if COPD?
A. Indacaterol
B. Olodaterol
C. Vilanterol
D. Bambuterol
E. AOTA
E. AOTA
-may be used as monotherapy with COPD but needs to be in combi with ICS for Asthma
Which of the following cannot be used in acute exacerbation?
A. Salbutamol
B. Metaproterenol
C. Salmeterol
D. Pirbuterol
E. Levalbuterol
C. Salmeterol
- LABA with 20 min duration
This is a unique LABA that has a longer duration of action but same onset as SABA; hence, it may be used as a controller and a reliever medication.
Formoterol
This is used largely for treatment of the acute vasodilation and bronchospasm of anaphylaxis, but it can cause tachycardia, arrhythmia, and worsening of angina pectoris as it is an alpha and beta agonist
Epinephrine
This sympathomimetic has an oral activity and more pronounced central effects and lower potency compared to EPI
Ephedrine (longer duration rin)
T/F:
Tolerance does not develop with Methylxanthines, but it elicits adverse CNS effects; hence, it’s an add-on treatment only
True
T/F:
Theophylline is commonly used in pediatrics and not with COPD
False:
- not in pediatrics since it has narrow Therapeutic Index, but it is seen more on COPD
Which of the following is FALSE of Theophylline?
A. Slowest rates of clearance occur in infants and neonates
B. Blood levels need to be monitored when used
C. Aminophylline is the commonly used preparation for therapeutic purposes
D. Superior effects than corticosteroids
D. its inferior to corticosteroids
This xanthine-derived drug is used in intermittent claudication as it decreases the blood viscosity
Pentoxifylline
Which of the following is not an MOA of Theophylline?
A. Inhibits PDE3 for the relaxation of airway
B. Inhibits histone deacetylation
C. Inhibits receptors for adenosine
D. Inhibits PDE4 to prevent release of cytokines and chemokines
B. should be enhanced histone deacetylation for activation of inflammatory gene transcription
Which of the following is not a sign of Theophylline toxicity?
A. Hypertension
B. GI Distress
C. Insomnia
D. Tremors
E. Arrhythmia
A. should be hypotension
Which of the following is a low concentration CV effect of Theophylline?
A. Increased catecholamine release
B. Enhanced histone deacetylation
C. Inhibits receptors for adenosine in SNS nerves
D. Inhibits PDE decreasing calcium influx
E. Both A and C
E. Both A and C
What is the GI effect of Theophylline?
Stimulate Gastric acid and digestive enzyme secretion
Which of the following is an effect of Theophylline?
A. Increased tubular sodium reabsorption and decreased GRF
B. Inhibit antigen-induced release of histamine from lung tissue
C. Decreased GI secretion
D. Negative chronotropy and inotropy
B. inhibits Histamine, weak diuretic, stimulates GI secretions and positive chronotropy and inotropy
Earliest sign of Theophylline toxicity is
Nausea and vomiting
The selective quaternary ammonium derivative of atropine used as an add-on therapy for patients having severe asthma attacks
Ipratropium bromide
Which of the following are not true of Ipratropium bromide?
A. Minimally crosses the nasal and gastrointestinal membranes and the blood-brain barrier
B. Results to greater bronchoconstriction with less toxicity
C. Useful in COPD patients who are unresponsive to beta-2 agonists
D. Not used in long-term asthma treatment
E. Given throughout and after duration of asthma attack
E. Ipratropium bromide is only given is severe asthmatic patients about 48-72 hours, and bronchodilation and anti-inflammatory effects suggest discontinuation
Which of the following is NOT true of Tiotropium bromide?
A. It’s a long-acting muscarinic antagonist
B. it’s taken by inhalation
C. May be used by asthma only patients
D. Maintenance therapy for patients with COPD and overlapping asthma
E. NOTA
C. it is NOT recommended for patients with asthma only
These are the inhibitory proteins synthesized as corticosteroids block all pathways of eicosanoid synthesis
annoxins or lipocortins
Which of the following is the most important action of corticosteroids in asthma?
A. Contraction of engorged vessels in the bronchial mucosa
B. Potentiation of the effects of beta-receptor agonists
C. Inhibition of infiltration of airways by lymphocytes, eosinophils, and mast cells
D. Reduce bronchial hyperactivity
C.
all are effects of Corticosteroids
Which of the following surface-active corticosteroids are for local aerosol administration, considered safe and for long-term use?
A. Beclomethasone
B. Budesonide
C. Fluticasone
D. AOTA
D. AOTA
Which of the following are given via IV for Status asthmaticus patients?
A. Methylprednisolone
B. Prednisone
C. Prednisolone
D. Fluticasone
A. Methylprednisolone and Hydrocortisone
Which inhaled corticosteroid is associated with less frequent oral candidiasis?
A. Flunisolide
B. Ciclesonide
C. Triamcinolone
D. Mometasone
E. NOTA
B. Ciclesonide
- prodrug activated by bronchial esterases
Drug for Biologic therapy that binds to IgE on sensitized mast cells and prevents activation by asthma triggers and subsequent release of inflammatory mediators
Omalizumab
Medications used for the prophylaxis of mild to moderate persistent asthma
Mast cell stabilizers or chromones
A prototype drug used to reduce symptoms of allergic rhino-conjunctivitis
Cromolyn (Disodium Cromoglycans)
Which of the following is not a feature of Cromolyn?
A. used for Systemic mastocytosis
B. for management of Hay Fever
C. readily absorbed in the systemic circulation
D. requires 4-6 weeks trial to determine efficacy
C. Cromolyn (Disodium Cromoglycate) is poorly absorbed into the systemic circulation and havelittle toxicity mild adverse effect
What is the most important clinical effect of Omalizumab?
Reduction in the frequency and severity of asthma exacerbations, while enabling a reduction in cortocosteroid requirements.
Which asthma medication has been proven effective as a treatment for chronic recurrent urticaria and for peanut allergy
Omalizumab
True or False:
The first injection of Omalizumab can be done at home
False: it should be done in a hospital setting
There can be anaphylaxis or severe form of allergy despite being an anti-allergy medication.
Remember: This is a monoclonal antibody. It can elicit an immune response.
True or False:
A 12 year-olf girl may be prescribed with Omalizumab if she has IgE levels of 250 IU and is able to afford treatment
False: should be around 400 IU
Which of the following is NOT a side effect of Omalizumab?
A. Malignancy
B. URTI
C. Viral infections
D. Sinusitis
E. Hypotension
E. Hypotension
There is a need for screening for chronic infections the hepatitis B and TB in patients being prescribed with:
A. Cromolyn
B. Theophylline
C. Omalizumab
D. Zileuton
E. Ipatropium bromide
C. Omalizumab
Anti-thymic stromal lymphopoietin drug for non-eosiniphilic type of asthma
Tezepelumab
Add-on Anti-Interleukin-4 Receptor a drug for severe eosinophilic or Type 2 asthma
Dupilumab
Which among the Anti-IL-5 monoclonal antibody works on Isotype humanized IgG4?
Reslizumab
Which drugs are no longer part of the management for asthmatic patients based on 2022 GINA Guidelines?
A. Mast cell stabilizers
B. Lipoxygenase inhibitors
C. COX inhibitors
D. Leukotriene antagonists
E. Inhaled corticosteroids
B. Mast cell stabilizers
True or False:
Using two or more canisters of an inhaler is a marker for
increased risk of asthma fatality.
True
True or False:
For patients with severe asthma attacks, inhalation of a β-receptor agonist is as effective as subcutaneous injection of epinephrine.
False: that’s for mild
Severe attacks require treatment with oxygen, frequent or continuous administration of aerosolized albuterol, and systemic treatment with prednisone or methylprednisolone (0.5 mg/kg every 6–12 hours).
Which is NOT true of COPD?
A. COPD may involve both airways and alveoli
B. It has better response to ICS therapy than Asthma
C. Like asthma, it results to reduction in maximum expiratory flow
D. Manifests neutriphilic infiltration
E. Preventable disease, and cannot be fully reversed with treatment once developed
B. should be “it has poor response to ICS therapy”
Which drug combination is used for the relief of COPD symptoms?
SABA inhalation (especially for acute exacerbation) and Anticholinergic
Which type of antimuscarinic drug may potentially cause vagal-induced bronchoconstrition?
Short-acting Muscarinic Antagonists
Which of the following is not a Long-acting antimuscarinic used for COPD?
A. Oxitropium
B. Tiotropium
C. Glycopyrollate
D. Umeclinidinium
E. Aclidinium
A. Oxitropium is a SAMA
True or False: The use of Theophylline require frequent monitoring of levels paticularly in adult COPD patients as clearance decrease with age.
True
Salmeterol, when combined with this drug, produces a greater improvement in FEV1 and breathlessness than when taken alone.
Theophylline
These are anti-inflammatory agents for COPD that were found to reduce exacerbations over 1 year when administered
Antibiotics (azithromycin and erythromycin)
These drugs were recently included in the Global Initiative for Chronic Obstructive Lung Disease (GOLD) 2021 as its principal action is to reduce inflammation by inhibiting the breakdown of intracellular cyclic AMP
PDE4 inhibitors
Which of the following is not true of Rofumilast?
A. It’s a PDE4 inhibitor
B. It’s a once daily oral medication with direct bronchodilator activity
C. It reduces moderate and severe exacerbations treated with systemic corticosteroids in patients with Chronic Bronchitis
D. It has greater beneficial effects in patients with a prior history of hospitalization for an acute exacerbation
E. It requires precautions in patients with depression
B. it induces indirect activity
The drug of choice in acute asthmatic brochospasm
Albuterol
This is a drug similar to albuterol and is also available as oral drug
Terbutaline
Which of the following may manifest cardiac effects when administered for asthma?
A. Epinephrine
B. Isoproterenol
C. Formeterol
D. Both A and B
D.
Isoproterenol = powerful
Which of the following is a management for Hay fever?
A. Cromolyn
B. Fluticasone
C. Theophylline
D. Both A and B
D. Both A and B
Leukotriene Antagonists effective in preventing exercise-induced asthma and aspirin-induced bronchospastic attack
Zafirlukast
Montelukast
An asthma patient reducing predisone dosage and taking LTD4 antagonist manifested systemic vasculitis accompanied by worsening asthma, pulmonary infiltrates, and eosinophilia. What is this drug?
A. Montelukast
B. Theophylline
C. Cromolyn
D. Omalizumab
E. Dupilumab
A. Montelukast (LTD4 antagonist like Zafirlukast)
- Churg-Strauss syndrome isa disorder marked by blood vessel inflammation. This inflammation can restrict blood flow to organs and tissues, sometimes permanently damaging them. This condition is also known as eosinophilic granulomatosis with polyangiitis (EGPA)
A patient had a history of Nedocromil medications. Which of the following is not true of this drug?
A. It’s a prophylactic anti-inflammatory agent via INHALATION
B. Administered shortly BEFORE exercise or inevitable exposure to allergens
C. Effect is mediated by inhibition of various SODIUM channels reponsible for secretion and cellular activation of MAST Cells
D. Has NO DIRECT bronchodilator action but inhibits bronchospasm via mast cell degranulation
C. Inhibition of various DELAYED CHLORIDE CHANNELS
A patient had a history of Nedocromil medications. Which of the following is not true of this drug?
A. It’s a prophylactic anti-inflammatory agent via INHALATION
B. Administered shortly BEFORE exercise or inevitable exposure to allergens
C. Effect is mediated by inhibition of various SODIUM channels reponsible for secretion and cellular activation of MAST Cells
D. Has NO DIRECT bronchodilator action but inhibits bronchospasm via mast cell degranulation
C. Inhibition of various DELAYED CHLORIDE CHANNELS
Which of the following is known to increase skeletal muscle strength helpful for the diaphragms of COPD patients?
A. Cromolyn
B. LAMA
C. Theophylline
D. PD4 inhibitors
E. Roflumilast
C. Theophylline
Drug that inhibits 5-lipoxygenase decreasing the biosynthesis of leukotrienes but has been associated with LFT abnormalities
Zileuton
- inhibits lipozygenase
- orally active
- prevents exercise- and antigen-induced bronchospasm
- associated with liver toxicities (Liver function test abnormalities)
- for adult patients only
Route of administration of Omalizumab
Parenteral (subQ injections)
Interleukins blocked by Dupilumab
IL-4 and IL-13
This is known as “anti-inflammatory reliever” for asthma that reduces the risk of severe exacerbation for adults and adolescents
low dose ICS-formeterol
- reduces the risk of severe exacerbation compared with SABA relievers
Storage cells of histamine
→ Mast cells, mainly in lungs, skin & GIT mucosa as an inactive complex
→ Platelets & basophilic leukocytes in CNS
→ Enterochromaffin-like (ECL) cells of the stomach
Firstline of treatment for allergic rhinitis
Antihistamine
Most important receptor for histamine for in lines the smooth muscles and is also present in the endothelial tract
H1
- used for allergic rhinitis and skin conditions
H receptors found in myenteric plexus
H3: presynaptic autoreceptors and heteroreceptors
H receptors for Eosinophils, Neutrophils and CD4 T cells
H4
True or False:
In humans, mast cells in skin and basophils have a negative feedback control mechanism mediated by H2 receptors, but lungs mast cells do not
True
Which is not true of histamine?
A. It inhibits the release of lysosome contents
B. It inhibits T- and B-lymphocyte function via H1 and H3 receptors
C. Causes leakage of plasma-containing mediators of acute
inflammation and antibodies
D. Causes local vasodilation
B. These actions are mediated by H2 or H4 receptors
Structures of the H1 and H2 receptors differ significantly; Each appear to be more closely related to: _______ and _______ respectively
H1 - Muscarinic
H2 - 5-HT1
Which drug is an agonist at H4 and an antagonist or inverse agonist at H3 receptors
Clobenpropit
Activation of which Gs H receptor may couple to Gq?
H2 receptor
Activation of which H receptor is very important chemotactic effects on eosinophils and mast cells?
H4 receptors
- found mainly in leukocytes
Interaction of mast cells with ______ antibodies and allergens will bring about the release of inflammatory mediators such as histamine which causes wheal formation
IgG
True or False?
Manifestations of wheal and flare reaction is also seen in the lining of the respiratory tract
True
Manifestations of wheal and flare reaction is also seen in the lining of the respiratory tract particularly, the nose
Bronchoconstriction via Histamine is mediated by which receptor?
H1
- Smooth muscle
- Endothelium
- Brain
Diarrhea due to Histamine stimulation is mediated by which receptors?
H2
- in gastric parietal cells
- contraction of intestinal smooth muscle
- secretion of gastric pepsin and intrinsic factor
Which H2-blocking drug (H3 antagonist also) has ab analgesic effects comparable to that produced by opioids?
Burimamide
DOC: Anaphylactic Shock
Epinephrine
Which of the following is not a Beta receptor activity of Epi?
A. Pulmonary bronchodilation
B. Increased Myocardial contractility
C. Suppress release of leukotrienes
D. Decrease mucosal edema
D. is for alpha receptor activity
Alpha receptor activity
▪ Decrease mucosal edema (like laryngeal edema)
▪ Decrease peripheral vasodilation and vascular permeability
These are known as Selectively Acting H1 receptor antagonists
2nd generation drugs
Which newer generation of anti-histamine has a less sedating property compared to others?
Bilastine
Anti-histamine that has significant acute suppressant effect on antipsychotic drugs-associated extrapyramidal symptoms
Diphenhydramine
Many first-generation agents, especially those of the ethanolamine have significant _______-like effect on peripheral muscarinic receptors
Atropine-like
Antihistamines especially those in the _______ subgroup may cause orthostatic hypotension to susceptible individuals
phenothiazine
A first-generation potent H1-blocking agent that notably blocks serotinin and resembles phenothiazine AH
Cyproheptadine
These are first-gen H1-antagonist that are actually more potent than procaine as local anesthetics
Diphenhydramine and promethazine
Which of the following are not a quality of of 2nd generation antihistamines?
A. Anti-inflammatory action
B. P-glycoprotein transporter inhibitor
C. Anti-muscarinic effect
D. Less-lipid soluble
E. Less sedation
C. exhibited especially by ethanolamines
Which of the following is not an effect of first-gen H1-antagonist?
A. Serotonin-blocking action
B. Anti-nausea
C. Benefit for non-allergic rhinorrhea
D. Anti-inflammatory
E. Local anesthesia
D. Anti-inflammatory
These are the second-line drugs after glucocorticoids for Hay fever or allergic rhinitis
H1 antagonist nasal spray
Drug of choice for urticaria
H1 antagonists
This may be precipitated by histamine release maintained by peptide kinins that are not affected by antihistaminic agents
Angioedema
Which among the drugs below reduces awareness of itching in atopic dermatitis?
A. Diphenhydramine
B. Cyproheptadine
C. Roflumilast
D. Fluticasone
A. Diphenhydramine
True or False?
With the used of antihhistamines in atopic dermatitis, clinical effectiveness of one group may diminish with continued use and switching to another group may restore drug effectiveness.
True
Which of the following is effective in preventing motion sickness?
A. Scopolamine
B. Diphenhydramine
C. Promethazine
D. Piperazine
E. AOTA
AOTA
Greatest: diphenhydramine and promethazine
Significant activity and less sedating: piperazines (meclizine and cyclizine)
Buclizine, hydroxyzine and meclizine are indicated less for
allergies rather are used for motion sickness
Both scopolamine and the H1 antagonists are more effective in preventing motion sickness when combined with:
ephedrine or amphetamine
Several large prospective studies disclosed NO increase in the incidence of birth defects with the use of Doxylamine, thereby justifying the reintroduction of a similar product:
Diclegis
These constitute the most common undesirable actions of H1-antagonists
Sedation and anticholinergic action
These antihistamines are no longer marketed as they are cardiotoxic and may induce cardiac arrhythmia or lethal ventricular arrhythmias
Astemizole and Terfenadine
(occurs in combination with ketoconazole, itraconazole, or macrolide antibiotics)
A patient underwent V. arrhythmia upon taking doses of an antibiotic. History determined that patient was also taking one of the following antihistamines:
A. Fexofenadine
B. Cetirizine
C. Astemizole
D. Desloratadine
E. Promethazine
C. Astemizole
and Terfenadine when used with drugs that are inhibit its metabolism by CYP3A4 such as ketoconazole, itraconazole, or macrolide antibiotics may be cardiotoxic
The mechanism of toxicity of Terfenasine as Astemizole involves:
blockade of the HERG (IKr) potassium channels in the heart
Which of the following is not a second generation H1-antagonist?
A. Azelastine
B. Olopatadine
C. Acrivastine
D. Azatadine
E. Fexofenadine
D. Azatadine
This first-generation alkylamine is a common component of OTC “cold” medication
Chlorpheniramine
What is the cardiotoxic effects of first-generation anti-histamine
prolongs QTC
Duration of action of first-gen H1 antagonist
4-8 hours
True or False:
Second-generation H1-antagonists exhbits no tolerance
True
Which histamine-selective ligands are of value in sleep disorders, narcolepsy, obesity, and cognitive and psychiatric disorders.
H3
This is an inverse H3-receptor agonist, has been shown to reduce sleep cycles in mutant mice and in humans with narcolepsy
Tiprolisant