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Respiratory II > Drugs for Treatment of Ear, Eye, Nose, and Throat Problems > Flashcards

Drugs for Treatment of Ear, Eye, Nose, and Throat Problems Flashcards

1
Q

Allergic Rhinitis Drugs delivered locally as nasal spray

A

Drugs delivered locally as nasal spray

  • Antihistamines
  • Antimuscarinics
  • Cromolyn compounds
  • Topical corticosteroids
  • Nasal decongestants
  • Sympathomimetic Agents
  • alpha-adrenergic agonists
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2
Q

Antihistamine Action

A
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3
Q

Antihistamines:
H1 Receptor Antagonists

A

Several structural classes

Pharmacokinetics

  • rapidly absorbed
  • large Vd
  • 2nd generation drugs do not cross BBB
  • metabolized in the liver
  • t1/2 most drugs = 4-6 hours
  • sustained release preparations t1/2= 12-24 hrs
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4
Q

Histamine H1 antagonists

A
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5
Q

Histamine H1 - Receptor Blockers

A
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6
Q

Clinical Indications 1

A
  • Acute and Chronic Allergic Rhinitis
  • Vasomotor rhinitis
    • antimuscarinic effects help
  • Eosinophilic nonallergic rhinitis
  • Viral Upper Respiratory Infection
    • antimuscarinic effects help
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7
Q

Clinical Indications 2

A
  • Urticaria
  • Allergic conjunctivitis
  • Anaphylactic reactions
    • adjunct to epinephrine
  • Motion sickness and nausea
  • Insomnia
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8
Q

Key Drugs - 1st Generation

A
  • Diphenhydramine (Benadryl)
  • Chlorpheniramine (Chlor-Trimeton)
  • Others
    • Dimenhydrinate (Dramamine)
    • Cyclizine (Marezine)
    • Hydroxyzine (Atarax)
    • Meclizine (Bonine)
    • Promethazine (Phenergan)
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9
Q

Key Drugs - 2nd generation

A
  • Cetirizine (Zyrtec)
    • $63.29 (2003 price for 30 day supply)
  • Fexofenadine (Allegra)
    • $84.62
  • Loratadine (generic, Claritin, Alavert)
    • $21.30, $27.30, $16.50
  • Desloratadine (Clarinex)
    • $69.74
  • Azelastine (Astelin) Intranasal spray
    • $71.48
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10
Q

Key Points - 2nd generation

A
  • Less complete distribution to CNS
    • little drug crosses BBB –therefore, much less sedation compared to 1st generation drugs
  • Have longer elimination t1/2 than 1st generation
    • therefore, longer duration of action
  • Lower incidence of antimuscarinic side effects, e.g. dry mouth, dysuria, etc.
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11
Q

Clinical Effects

A
  • All antihistamines are effective for relieving:
    • sneezing
    • nasal itching
    • nasal discharge (rhinorrhea)
  • Not very effective for relieving:
    • congestion
    • add decongestant
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12
Q

Side Effects 1

A
  • 1st generation agents
    • sleepiness
    • interfere with learning
    • decrease work productivity
    • impair psychomotor performance
    • increases risk of injury
  • Patient may be unaware of these effects
  • Side effects may persist morning after taking drug at bedtime
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13
Q

Side Effects 2

A
  • Sedation - antimuscarinic effect
    • 1st generation only
  • CNS
    • dizziness, tinnitus, nervousness, insomnia, fatigue, blurred vision
    • 1st generation only
  • GI
    • nausea, vomiting, loss of appetite
  • Dry mouth – (antimuscarinic effect)
    • 1st generation only
  • Urinary retention –
    • (antimuscarinic effect) 1st generation only
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14
Q

Decongestants

A
  • alpha-adrenergic agonists
  • cause vasoconstriction, reduce edema
  • available as nasal spray or oral tablets
    • Pseudoephedrine
      • prescription, or behind the counter restrictions
    • Phenylephrine
    • Naphazoline
    • Oxymetazoline
    • Tetrahydrozoline
    • Xylometazoline
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15
Q

Decongestants

alpha-adrenergic agonists

A
  • alpha-adrenergic agonists
    • Effective only for relief of nasal congestion and not sneezing, itching, or discharge
    • Often given in combination with an H1-antihistamine
    • Adverse effects include insomnia, excitability, headache, nervousness, palpitations, tachycardia, arrhythmia, hypertension, nausea, vomiting, and urinary retention.
    • Should not be used more than 3 days in order to avoid rebound congestion and rhinitis medicamentosa
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16
Q

Antitussives

A
  • Opioids: central suppression of cough reflex
    • Codeine
    • Dextromethorphan
  • Non-opioids:
    • Benoxinate - local anesthetic
    • Diphenhydramine - antihistamine
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17
Q

Expectorants

A
  • Facilitate secretion or decrease viscosity of mucus to facilitate clearance of mucus secretions in airways.
  • N-acetyl-cysteine breaks sulfhydryl bonds in mucus proteins; makes mucus less sticky
  • Guaifenesin: claimed to facilitate removal of viscous mucus.
  • Potassium iodide: claimed to decrease viscosity of mucus.
  • Recombinant DNAse (Dornase alpha)
      • useful in cystic fibrosis.
18
Q

Other Therapy for Rhinitis

A
  • Ipratropium bromide
    • vasomotor rhinitis
  • Intranasal cromolyn sodium, nedocromil
  • Intranasal corticosteroids
    • beclomethasone dipropionate
    • budesonide
    • flunisolide
    • fluticasone propionate
    • triamcinolone acetonide
19
Q

Antimuscarinics:
Ipratropium bromide

A
  • A quaternary muscarinic receptor antagonist
    • If given parenterally, effects are like atropine
    • But, only given as inhaled aerosol to treat COPD
      • few side effects, even when swallowed because is poorly absorbed from GI and does not cross into brain
      • quaternary amine- poor diffusion across membranes
    • Parasympathetic - mediated bronchospasm is a significant component of airway resistance in some asthmatics and COPD patients, especially psychogenic exacerbations
20
Q

Ipratropium bromide

Therapeutic Use:

A
  • Therapeutic Use:
    • Bronchodilation develops more slowly and is usually less intense than that produced by b-agonists.
    • Useful bronchodilation lasts up to 6 hours.
    • Principal use of ipratropium is in COPD.
    • Combined with albuterol = COMBIVENT
    • Also used intranasally (Roxane) to reduce secretions in the upper and lower respiratory tract in allergic rhinitis and chronic postnasal drip syndrome.
21
Q

Cromolyn Compounds

A
  • Cromolyn sodium nasal spray (Nasalcrom)
  • Cromolyn sodium (Intal)
22
Q

Antihistamines Partially Block

A
23
Q

Cromolyn Compounds

MOA

A
  • Cromolyn compounds are anti-inflammatory agents that indirectly inhibit antigen-induced bronchospasm and directly inhibit the release of histamine and other autocoids from sensitized mast cells.
  • May suppress the activating effects of chemoattractant peptides on eosinophils, neutrophils, and monocytes.
24
Q

Cromolyn Compounds:
Therapeutic Use

A
  • Cromolyn compounds do not directly relax smooth muscle, therefore they are not useful for control of acute bronchospasm.
  • Cromolyn compounds are primarily prophylactic. When inhaled several times daily, they inhibit both the immediate and late asthmatic responses to antigenic challenge or exercise.
25
Q

Cromolyn Compounds:
Therapeutic Use Continued

A
  • Nedocromil is a newer compound, somewhat more potent than cromolyn sodium.
  • Nedocromil is approved for use is asthmatic patients > 12 years old; cromolyn is approved for all ages.
  • Adverse effects: are infrequent and generally mild.
  • Used mostly in mild to moderate asthma as an added therapy or as a prophylactic alternative to inhaled steroids or oral methylxanthines.
26
Q

Intranasal corticosteroids

A
  • Intranasal corticosteroids
    • beclomethasone dipropionate (Beconase AQ)
    • budesonide (Rhinocort Aqua)
    • flunisolide (generic, Nasarel)
    • fluticasone propionate (Flonase)
    • mometasone furoate (Nasonex)
    • triamcinolone acetonide (Nasacort AQ)
27
Q

Molecular Mechanism of Action

A
28
Q

Summary of immunosuppression Actions of Glucocorticoids

A
29
Q

Intranasal Corticosteroids

A
  • Most effective drugs available for relief of symptoms of allergic rhinitis
  • Available in aqueous solution/pump spray formulations
  • They all reduce sneezing, itching, discharge, and congestion
  • Most are effective when given once daily
  • Take at least one week to be maximally effective.
30
Q

Intranasal Corticosteroids

Side Effects

A
  • Side Effects – usually mild
  • Dryness & irritation or burning of nasal mucosa
  • Sore throat
  • Epistaxis
  • Headache
31
Q

Leukotriene Modifier

A
  • Montelukast (Singulair)
    • Cysteinyl leukotrienes (cousins of prostaglandins) released in nasal mucosa during allergic inflammation.
    • Oral montelukast blocks leukotriene receptor
    • Modestly beneficial for relief of sneezing, itching, discharge, and congestion
    • One study showed montelukast to be as effective as loratadine, but not as effective, alone or in combination with loratadine, as an intranasal corticosteroid
    • Safe and with few side effects
32
Q

Allergic Conjunctivitis

Overview

A
  • The most common form of ocular allergy
  • Usually associated with allergic rhinitis
    • May be seasonal or perennial
  • Main symptom is itching
  • Oral antihistamines (2nd generation) usually effective
  • Topical antihistamine eye drops
    • also effective
    • may be more rapid acting
    • also antiinflammatory
33
Q

Allergic Conjunctivitis

A
  • Antihistamine/decongestant combinations
    • pheniramine/naphazoline (Visine A)
    • antazoline/naphazoline (Vasocon-A)
  • Available over-the-counter may be more effective than either agent alone but are short acting and can cause rebound vasodilation with continued use
34
Q

Topical Ocular
H1 - Antihistamines

A
  • Azelastine (Optivar)
  • Emedastine difumarate (Emadine)
  • Levocabastine HCl (Livostin)
35
Q

Topical Ocular
Mast Cell Stabilizers

A
  • Cromolyn sodium (generic, Crolom)
  • Lodoxamide tromethamine (Alomide)
  • Nedocromil sodium (Alocril)
  • Pemirolast potassium (Alamast)
36
Q

H1 Antihistamine
+ Mast Cell Stabilizers

A
  • Ketotifen fumarate (Zaditor)
  • Olopatadine HCl (Patanol)
    • These drugs are primarily antihistamines but are marketed as also having mast cell stabilizing activity. Probably all H1 antihistamines have mast cell stabilizing activity.
37
Q

Antivirals

A
38
Q

Virus Anatomy

A
39
Q

Viral Infectious Process

A
40
Q

Viral Infection

A
41
Q

Antiviral Agents 1

A
  • Amantadine & Rimantadine
    • RNA viruses
    • Inhibit uncoating of viral nucleic acids
    • Inhibit viral replication
    • Prophylaxis of type A influenza
    • Treatment initiated within 48 hours after initial appearance of symptoms is effective
42
Q

Antiviral Agents 2

A
  • Oseltamivir (Tamiflu), oral
    • Inhibits neuraminidase of influenza A or B
    • Hemagglutinin on viral surface binds to host cell receptors allows virus entry
    • Neuraminidase on viral surface sugar from receptor. This step required for release of progeny viral particles
    • Also inhibits viral spread
    • Bird flu = H5N1 strain
  • Zanamivir (Relenza)
    • same as above, but inhaler device

Respiratory II (14 decks)

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