Quiz 7

  1. MoA: Inhibitor of mast cell mediators such as histamine and leukotrienes
    beta agonist
    ONLY for long term treatment of COPD, chronic bronchitis, emphysema
    Delivered by nebulizer every 12 hours
    Not for acute rescue
    Sympathomimetic Bronchodilator
    Long acting agents, comes with warnings
    Diasteroemeric pure drug (R,R) of Foradil, two times as potent
    50-65% plasma protein bound
    Metabolism: primary--clucuronidation, secondary--)-demethylation, no CYP inhibition
    Excretion: 67% urinary, 22% feces--Renal failure not an issue caution in heaptic failure
    No apparent effect on QT elongation
    • Arformeterol tartrate or (R,R)-formoterol L-tartrate
    • Brovana Inhalation Solution (15mcg/2mL)
  2. MoA: Long-acting beta2-adrenergic agonist
    LABA increases risk of asthma-related death
    COPD, chronic bronchitis and/or emphysema
    Sympathomimetic Bronchodilator
    Use capsules with neoinhaler only
    Once daily dosing increases compliance
    New in 2011
    • Indacaterol maleate
    • Arcapta Neohaler
  3. Xanthine Bronchodilator
    MOA: direct relaxation of the smooth muscle of the bronchi and pulmonary blodo vessels by possible inhibition of phosphodiesterase leading to increase cAMP, inhibtion of extracellular adenosine (a bronchoconstictor) and stimulation of endogenous catecholamines
    For symptomatic relief or prevention of bronchial asthma and reversible bronchospasm associated with chronic bronchitis and emphysema
    Unlabeled: treatment of apnea and bradycardia of prematurity, essential tremor, COPD
    Contraindicated: Peptic ulcer, seizure disorders if no medication to treat seizures, Xanthine hypersensitivity
    Precaution: hepatic diseases, hypertension, CHF
    Metabolized in liver
    Many drug interactions
    Low theraputic index
    Remember: Do not brand interchange without consulting, take dosage same time every day, avoid caffeine, do not crush or chew, tell dr. if changing dosage, Somoking will alter and lower blood levels
    • Theophylline
    • Aminophenylline
    • Dyphylline
    • Oxtriphylline
  4. Xanthine Bronchodilator
    Tablets, capsules, syrup, elixer, solution, extended release tablets and capsules, timed-rlease tablets and capsules, injection containing dextrose
    Prolonged release products 12-24 hours
    • Theophylline
    • Slo-Phyllin, Theolair, Bronkodyl, Elixophyllin, Quibron-T, Theobid, Respid, Sustaire, Theo-Dur, Uni-Dur
  5. Xanthine Bronchodilator
    79% Theophylline
    Tablets, controlled-rlease tablets, oral liquid, injection, suppositories
    IV loading doses: after determining current serum levels
    Many protein binding sites
    • Aminophylline
    • Generics, Phyllocontin, Truphylline
  6. Xanthine Bronchodilator
    Tablets, elixer, injection
    NOT METABOLIZED TO THEOPHYLLINE so monitor its own levels
    • Dyphylline
    • Generics, Dilor, Lufyllin
  7. Xanthine Bronchodilator
    Tablets sustained-action tablets, pediatric syrup, elixir
    64% Theophylline
    • Oxitriphylline
    • Generics, Choledyl SA
  8. MoA: drug and its N-oxid metabolite are selective inhibitors of phosphosdiesterase 4, leads to an accumulation of intracellular cyclic AMP leads to bronchial smooth muscle relaxation
    80% Bioavailable with or without food, 97-99% plasma protein bound
    Metabolized by CYP 1A2 and 3A4 to N-oxide, no significant CYP induction
    Indications: reduction of the risk of COPD exacerbations in patients with severe COPD assocated with a history of chronic bronchitis
    Psychiatric events, suicidality, weight decrease and excreted in mother's milk
    • Roflumilast
    • Daliresp
  9. Anti-cholinergic Bronchodilators
    MoA: Synthetic quaternary anticholinergic parasympatholytic ammonium compound chemically rleated to atropine which antagonizes the effects of acetlycholine to decrease the intracellular concentrations of cGMP
    Solutions and aerosols for maintenance treatment of bronchospasm of COPD, chronic bronchitis, and emphysema
    Contraindicated in food allergy to soy bean or peanut prodcuts
    Nasal sprays for hay fever and commom coald
    • Ipratropium Bromide
    • Tiotropium Bromide
  10. Anti-Cholinergic Bronchodilator
    Solution for inhalation, aerosol, nasal spary
    Combination aerosol product available with albuterol sulfate available (Combivent)
    • Ipratropium Bromide
    • Atrovent, generics
  11. Combination of ipratropium bromide and albuterol sulfate
  12. Anti-Cholinergic Bronchodilator
    New in 2004
    an inhalation powder using the HandiHaler device
    Long-acting agent use one daily
    • Tiotropium Bromide
    • Spiriva
  13. Leukotriene Receptor Antagonists
    • Zafirlukast
    • Montelukast Sodium
    • Zileuton
  14. Leuoktriene Receptor Antagonist
    Propylaxis and chronic treatment of asthma in people 12 and older
    MoA: selective and competitive leukotrience receptor antagonist of leukotriene D4 and E4 which are components of slow-reacting substance of anaphylaxis preventing bronchoconstriction
    Metabolized by CYP2C9 yet inhbits CYP3A4 and CYP2C9
    • Zafirlukast
    • Accolate
  15. Leukotrience Receptor Antagonists
    Prophylaxis and chronic treatment of asthma in adults and children older than one
    MoA: selective and competitive CysLT1 receptor antagonist of leukotrience C3, D4 and E4 which are components of SRSA prevent bronchonstriction
    Metabolized by CYP2A9 and CYP3A4
    Tablets, chewable tablets, oral granules
    • Montelukast Sodium
    • Singulair
  16. Leuoktriene Receptor Antagonist
    Prophylaxis and chronic treatment of adults and children 12 and older
    Extended-release tablets
    MoA: orally active inhibitor of 5-lipoxygenase, the enzyme that catalyzes the formation of leukotriences from arachidonic
    both r and s enantiomers are pharmacologically active
    Metabolized by CYP1A2, CYP2C9, CYP3A4
    not in patients with active liver disease of elevated ALT
    Drug interactis with Theophylline and warfarin
    • Zileuton
    • Zyflo CR
  17. Repiratory Corticosteroid Inhalation Products
    MoA: Adrenal corticosteroids with basic glucocorticoid activity and actions, ecact mechanism on lung tissue unknown
    Halogen incorporation increases lipid solubility
    Treatment inducluding maintenance and prophylaxis of chronic asthma patients including those that require systemic corticosteroids or those that could benefit from systemic dose reduction/elimination
    Metabolism in liver, all highly protein bound
    • Beclomethasone dipropionate
    • Budesonide
    • Fluticasone propionate
    • Flunisolide
    • Triamcinolone Acetonide
    • Mometasone furoate
  18. Respiratory corticosteroid inhalation product
    Patient sould remember to rinse mouth after using
    Suppresses immune response
    1 Cl
    • Beclomethasone dipropionate
    • Beclovent, Vanceril
  19. Respiratory corticosteroid inhalation product
    No halogens, rapid first pass effect
    long acting B2
    used in combination with formoterol to make Symbicort
    • Budesonide
    • Pulmicort
  20. Respiratory corticosteroid inhalation product
    Activates CP450 3A5 a predominant lung enzyme
    combination product with salmeterol is Advair Discus
    3 F's
    • Fluticasone propionate
    • Flovent
  21. Respiratory corticosteroid inhalation product
    1 F
    Two similar products
    • Fluisolide (aerobid, Aerobid-M)
    • Triamcinolone Acetonide (Azmacort)
  22. Respiratory corticosteroid inhalation product
    New for 2005
    Cap activated inhalation drivent multi-dose dry powder inhaler
    Combinations with Formoterol id Dulera
    2 Cl
    • Mometasone furoate
    • Asmanex Twisthaler
  23. Respiratory Corticosteroid Intranasal Products
    MoA: Adrenal corticosteroids with basic glucocorticoid activity and actions exact mechanism in nasal tissue is unknown
    Metabolized in liver, hightly protein bound
    Local infections form Candiada albicans rarely occur
    Seasonal rhinitis and prevention of reoccurrence of nasal polyps following surgical removal
    Use in children is NOT indicated for all products
    Warning: Use caution in patients on systemic alternate-day corticosteroid treatment since HPA suppression likelihood may increase local delivery can reduce the systmeic glucocorticoid activity
    Can irritate and dry out nasal mucosa, do not use if exposed to chicken pox or measles
    • Flunisolide
    • Beclomethasone dipropionate
    • Triamcinolone Acetonide
    • Fluticasone propionate
    • Mometasone furoate
    • Budesonide
    • Ciclesonide
  24. Nasalide and Nasarel brand name for Flunisolide
    Not Bioequivaent, Not interchangable
  25. Respiratory Corticosteroid Intranasal Products
    Flunisolide brand names
    Nasolide, Nasarel
  26. Respiratory Corticosteroid Intranasal Products
    Beclomethasone dipropionate brand names
    Beconase, Beconase AQ, Vancenase
  27. Respiratory Corticosteroid Intranasal Products
    Fluticasone propionate brand name
  28. Respiratory Corticosteroid Intranasal Products
    Memetasone furoate brand name
  29. Respiratory Corticosteroid Intranasal Products
    Budesonide brand name
  30. Respiratory Corticosteroid Intranasal Products
    New for 2006
    Low gastrointestinal absorption and high first pass metabolism
    Can also use twice per day for treatment of asthma as Alvesco
    • Ciclesonide
    • Omnaris
  31. Mucolytic respiratory products
    MoA: thiol group disrups the disulfide linkages in mucoproteins causing depolymerization and drop in viscosity NO EFFECT ON DNA
    Solution for inhalation
    adjunctive therapy for abnormal, viscid, or inspissate mucus secretions in chronic bronchopulmonary disease, COPD, asthma, cystic fibrosis, posttraumatic chest conditions, anesthesia, tracheostomay care
    Antidote to hepatoxins, acetaminophen overdosage
    • Acetylcysteine
    • Mycomyst, Mucosil
  32. Mucolytic Respiratory Product
    Recombinant Human Deoxyribosenuclease
    For Cystic Fibrosis
    MoA: Enzyme is delivered by inhalation to assist in the clearance of bronchial secrations due to the death of leukocytes, bacteria, and tissue large amounts of DNA acculate leading to sputum. No effect on intracellular DNA
    Do not use same nebulizer for other inhalation medications
    Not for breast-feeding mothers, children under 5, people with hamster allergies
    Must be stored in fridge, cold and dark
    • Dornase Alfa
    • Pulmozyme
  33. Inhaled Antibiotic
    MoA: Monobactam inhibits cell wall crosslinking
    Treatment of cystic fibrosis patients to improve pulmonary function
    Useful in resistant strains
    Solution for inhalation
    • Aztreonam
    • Cayston
  34. Respiratory Inhalation Products, Mast cell stabilizers?
    • Nedocromil sodium
    • Cromolyn sodium
  35. Inhalation Product, Mast cell stabilizer
    Prophylactic treatment of bronchila asthma, prevention of exercise-induced bronchospasm, allergic rhinitis, food allergies
    MoA: anti-inflammatory agent that has NO intresnic bronchodilatory, antihistamin, anticholinergic, vasoconstrictive, or glucocorticoid activity. Inhibits degrandulation of mast cells
    ne ulizer for inhalation, aerosol sprays, nasal solutions, oral concentrate
    Cannot be used for acute attack, prophylactic may take up to four weeks
    • Cromolyn Sodium
    • Crolom, Cromoptic, Gastrocrom, Intal, Intal Inhaler, Nasalcrom, Opticrom
  36. Inhalation Product, Mast Cell Stabilizer
    Prophylactice maintenance therapy in the management of mild to moderate asthma
    MoA: anti-inflammatory agent that has NO intrensic brchodilator, antihistaminic, anticholinergic, vasoconstrictive or glucocorticoid activity it inhibits the degranulation of mast cells
    Cannot be used for acute attack, during attack free periods
    Do not stop abrupty!
    Aerosol spray
    • Nedocromil Sodium
    • Tilade
  37. Brand name of mast cell stabilizer Nedocromil Sodium for ophthalmic use?
  38. Recombinant humaized monoclonal anti-IgE antibody
    MoA: Bids free the Fc region of circulating IgE and blocks attachment to mast cells to prevent response, drown regulates the production of allergen specific high affinity receptors
    Treatment of unresponsive asthma
    Subcutaneous injections
    Black box warning
    cancer risks and hard to clear parasite infections
    Severe asthma unresponsive to conventional therapies
    • Omalizumab
    • Xolair
  39. Nasal Decongestants different chemical classes?
    • Arylalkylamines
    • Imidazolines
    • Alkylamines
  40. Arylalkylamine
    No longer available as a product due to recent opinion of FDA that an increased likelihood of cerebral vascular accident exists (Stroke)
  41. Arylalkylamine
    No longer OTC
    Used to make methamphetamine
    comes in extended release, tablets, capsules, liquid and drops
    Can be given to babies as young as 3 months
  42. Arylalkylamine
    Available as a spray or jelly
    Effects blood pressure
    • d-(-)-ephedrine
    • Pretz-D, Kondon's Nasal
  43. Arylalkylamine
    Used for children 6 or older COMT mechanism of clearance
    Epinephrine, Adrenalin solution 0.1%
  44. Arylalkylamine
    Duration only four hours
    Replaced pseudoephedrine as OTC agent
    Abuse potential due to stimulant include aromatics (menthol, camphor, eucalyptol) only metabolized by MAO
    • Phenylephrine HCl
    • Neo-Synephrine
  45. Imidazolines
    Limited CNS access since at physiolical pH it exists in the ionized form
    Duration 4-6 hours
    Partial agonist of alpha1 and alpha 2 adrenergic receptors
    • Tetrahydrozoline
    • Tyzine
  46. Imidazoline
    duration of action 8-10 hours
    • Xylometzoline
    • Otrivin 0.05% and 0.1% solution
  47. Imidazoline
    Drops and spray
    duration 6 hours
    Not for children under 12 without MD guidance
    • Naphazoline
    • Privine
  48. Alkylamines
    2 hours duration of action
    High abuse potential (put in IV)
    Abuse leads to cardiomyopathy, pulmonary hypertension, emboil, dyspnea, and sudden death
    • Propylhexidrine
    • Benzedrex Inhaler
  49. Repiratory Enzymes
    Purified from large pools of human plasma
    For congenital alpha 1 antitrypsin deficiency expressing as panacinar emphysema
    MoA Replacement of naturally deficient inhbitor
    • Human alpha1 proteinase inhbitor
    • Prolastin injection
  50. Lung surfactants
    **Overdosage with any of the lung sufactants can result in acute airway obstruction, watch for rales and moist breath sounds
    modify alveolar surface tension, restoring lung surface activity and stabilizing alveoli function
    • Colfosceril Palmitate
    • Beractant
    • Calfactant
    • Poractant alfa
  51. Synthetic lung surfactant, dipalmitoylphosphatidylcholine, DPC
    Prophylactic or rescue use in premature infants with less thatn 1350 g or at risk of ARDS
    MoA: substituion of natural deficiency of pulmonary sufactant missin in ARDS, suspension is milky white
    • Colfosceril Palmitate
    • Exosurf Neonatal
  52. Lung surfactant
    Isolated from bovine lung extract
    DPPC and palmitic acid are added to standardized the product
    Prophylactic or rescue use in premature infants with or at risk of ARDS
    MoA: substitution of natural deficiency of pulmonary sufactant missing in ARDS, suspension product is milky white
    • Beractant
    • Survanta
  53. Lung surfactant
    ARDS in infants under 29 weeks within 30 minutes of birth
    Isolated from calf lung extract
    • Calfactant
    • Infrasurf
  54. Lung surfactant
    mixture of phospholipids delivered via intratracheal use
    Prophylactic or rescue use in premature infants with or at risk of ARDS, ARDS in adults due to viral pneumonia or near drowning, HIV-infected infants
    MoA: substitiution of natural deficiency of pulmonary surfactant missing in ARDS suspension prduct that is milky white
    Known to suppress secectoions of TNF alpha via human monocytes
    • Poractant alfa
    • Curosurf
  55. Antihistamines
    MoA: reversible, competitive H1 receptor antagonists that reduce or prevent most of the physiological effects of histamine mediate by H1 receptor.
    Varying degrees of anticholinergic, antihistaminic, and antimuscarinic activity that makes them useful sedatives, antiemetics, antitussives, antiparkinsonism or adjunctives or pre- or post- surgical analgesic therapy and motion sickness
    First generation agents- non-selective agents that bind central and peripheral receptors and can result in CNS stimulation or depression (high dose)
    Chemical Classes
    • Alkylamines
    • Ethanolamines
    • Phenothiazines
    • Piperazines
    • Piperidines
    • Phthalazoinone
  56. Antihistamines MoA: reversible, competitive H1 receptor antagonists that reduce or prevent most of the physiological effects of histamine mediate by H1 receptor. Varying degrees of anticholinergic, antihistaminic, and antimuscarinic activity that makes them useful sedatives, antiemetics, antitussives, antiparkinsonism or adjunctives or pre- or post- surgical analgesic therapy and motion sickness
    Second generation agents- selective agents that bind only peripheral receptors and as a group are less sedating
    Chemical Classe
    Piperazine peripheral selective
  57. Alkylamines
    • Brompheniramine maleate
    • Chlorpheniramine maleate
    • Dexchlorpheniramine
  58. Ethanolamines
    • Clemastine Fumarate
    • Diphenhydramine HCl
    • Tripelennamine HCl
  59. Phenothiazine
    Promethazine HCl
  60. Piperazines
  61. Piperidines
    • Azatadine maleate
    • Cyproheptadine
    • Phenindamine tartrate
  62. Phthalazinone
    Azelastine HCl

    • Chloropheniramine maleate
    • Chlor-Trimenton
  63. 1st Generation Antihistamine, Alkylamines
    Tablets, time released tablets, syrup
    Half dosage because not racemic
    Typer I hypersensitivity reactions
    • Dexchlorpheniramine
    • Polaramine
  64. 1st Generation Antihistamine, Alkylamines
    Allergic rhinitis (oral)
    Type I hypersensitivity (Parenteral)
    • Brompheniramine maleate
    • Dimetapp
  65. 1st Generation Antihistamine, Ethanolamines
    Allergic rhinitis, Urticardia, and angioedema
    Tablets, Syrup (only for children)
    • Clemastine Fumarate
    • Tavist Antihist-1
  66. 1st Generation Antihistamine, Ethanolamines
    Immediate type I hypersensitivy reactions, motionsickness, antiparkinsonism, sleep disorders, antitussive
    Soft gell capsules, capsules, tablets, chewable tablets, liquid, solution, elixir syrup, injection
    • Diphenhydramine HCl
    • Benadryl
  67. 1st Generation Antihistamine, Ethanolamines
    Tablets, extended release tablets
    Type I hypersensitivy reactions
    No extended release in children
    • Tripelennamine Citrate of HCl
    • PBZ
  68. 1st Generation Antihistamine, Phenothiazines
    Type I hypersensitivity reactions, motion sickness, sedation, anti-emetic (best!), analgesia post-op
    Tablets, syup, suppositiories, injection
    IM injection only!
    • Promethazine HCl
    • PPhenergan
  69. 1st Generation Antihistamine, Piperazines
    Pruitis, sedation, anti-anxiety, adjuncitive analgesia, anti-emetic
    Very High anticholinergic
    Tablets, capsules, syrup, oral suspension, injection (DEEP IM ONLY)
    • Hydroxyzine
    • Atarax, Vistaril, Vistazine
  70. 1st Generation Antihistamine, Piperidines
    Allergic rhinitis, chronic uticaria
    Not for children under 12
    Highly sedating
    • Azatadine maleate
    • Optimine tablets
  71. 1st Generation Antihistamine, Piperidines
    Type I hypersensitivity reactions, appetite stimulant in anorexia nervosa and cancer related cachexia
    Tablets, syrup
    • Cyproheptadine HCl
    • Cyproheptadine
  72. 1st Generation Antihistamine, Piperidines
    Allergic rhinitis
    Reduce dose in children 6-11
    Phenindamine tartrate
  73. 1st Generation Antihistamine, Phthalazinone
    Allergic rhinitis
    Nasal spray needs 4 spays to prime
    Do not get in eyes
    Metered-dose nasal spray
    • Azelastine HCl
    • Asteline
  74. 1st Generation Antihistamine, Phthalazinone
    Azelastine HCl better tasting formula
  75. 1st Generation Antihistamine, Phthalazinone Azelastine Brand of Azelastine HCl for Opthalmic use
  76. 2nd Generation Antihistamines, Piperazine peripheral selective agents
    • Cetirizine
    • Levocetrizine
    • Loratadine
    • Fexofenadine HCl
    • Olopatadine HCl
  77. 2nd Generation Antihistamines, Piperazine peripheral selective agents
    Tablets, Syrup
    Allergic rhinitis, chronic idiopathic urticardia
    Dosage in patients have renal and hepatic failure must be reduced
    93% protein bound
    Racemic Mixture
    • Cetirizine
    • Zyrtec
  78. 2nd Generation Antihistamines, Piperazine peripheral selective agents
    Single enantiomer, Unknown advantage
    okay in children 6-11 with reduced dose
    • Levocetirizine
    • Xyzal
  79. 2nd Generation Antihistamines, Piperazine peripheral selective agents
    Allergic rhinitis, urticaria
    Reditabs expire after 6 months
    tablets, reditabs, syrup
    97% protein bound
    • Loratadine
    • Claritin
  80. 2nd Generation Antihistamines, Piperazine peripheral selective agents
    Seasonal allergic rhinitis chronic idiopathic urticaria
    70% protein bound
    Tablets and capsules
    Children over six can use
    Don't drink with fruit juice
    • Fexofenadine HCl
    • Allegra
  81. 2nd Generation Antihistamines, Nasal spray
    Seasonal allergic rhinitis, prevents itching
    MoA: relatively selective dual H1-receptor antagonists and inhbitor of histamine and other mediator release from mast cells by acting as a mast cell stabilizer, dual mechanism
    No alpha-adrenergic, dopaminergic or muscurinic type 1/2 receptor effects
    • Olopatadine HCl
    • Patanase
  82. Antitussive Agents
    • Codine Sulfate
    • Dextromethophran HBr
    • Diphenhydramine HCl
    • Benzonate
  83. Expectorants
    • Guaifenesiin
    • Terpin hydrate
    • Iodinated glycerol
    • Potasium Iodine
  84. Antitussive Agent
    Narcotic, Schedule 2
    Not for children under 2
    Pain relief and suppression of cough induced by chemical of mechanical respiratory tract irritation
    MoA: Inhbition of the CNS medulla mediated cough reflex
    Hepatic metabolism
    Take with food and milk if GI upset occurs
    Codeine (Sulfate)
  85. Antitussive Agents
    Capsules, lozenges, liquid, syup
    OTC agent
    Control nonproductive cough
    MoA Inhbition of the CNS medulla mediated cough reflex, no analgesic or addictive properties
    Tenage abuse
    • Dextromethorphan HBr
    • Benylin DM, Robutussin
  86. Antitussive Agent
    Control of cough due to colds or allergy
    MoA: anticholinergic activity results in a blockade of vagal nerve mediated cough reflex
    • Diphenhydramine HCl
    • Tusstat
  87. Antitussive Agents
    Looks like candy so children overdose
    MoA: Structurally related to tetracaine- anesthetizes stretch receptors in the respiratory areas dampening their activity reducing cough reflex at its source
    activity 15-20 minutes
    Duration 3-8 hours
    Swallow whole!
    • Benzonatate
    • Tessalon
  88. Expectorant
    Syrup, liquid, capsules, tablets, extended oral and sustaine release tablets, capsules
    Symptomatic relief of respiratory conditions characterized by a dry, nonproductive cough in the presence of mucus
    MoA: enhancement of respiratory tract fluid output by reducing adhesiveness and surface tension of phlegm
    Take with lots of fluid
    • Guaifenesin
    • Humibid, Mucinex
  89. Expectorant
    ymptomatic relief of dry, non-productive cough
    MoA: direct stimulation of repiratory tract secetory glands
    May cause drowsiness, drink with plenty of water
    Terpin hydrate
  90. Expectorant
    Tablets, elixir, solution
    Children take half dose based on wight
    Thin out mucous and make cough easier
    • Iodinated glycerol
    • Iophen
  91. Expectorant
    Symptomatic treatment of chonic pulmonary disease, used in prevention of iodine uptake in radiation emergency
    MoA: enhances release of repiratory secretion and fluids decreasing phlegm viscosity
    Discontinue use and notify MD if epigastric pain, skin rash, metallic taste or N/V occurs
    • Potassium iodine
    • SSKI, Pima
Card Set
Quiz 7