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

1
Q

Decongestants overview

A

alpha-adrenergic agonists

cause vasoconstriction, reduce edema

available as nasal spray or oral tablets

can act on imidazaline receptros

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2
Q

alpha adrenergic agonists drug list

A

Pseudoephedrine
prescription, or behind the counter restrictions
Phenylephrine
Naphazoline
Oxymetazoline
Tetrahydrozoline (used for eyes to get red out)
Xylometazoline

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3
Q

alpha adrenergic agonists overview

A

Effective only for relief of nasal congestion and not sneezing, itching, or discharge

Often given in combination with an H1-antihistamine

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4
Q

alpha adrenergic agonists

AE

A

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 (drug induced rebound congestion)

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5
Q

Antitussives

Opioids

A

central suppression of cough reflex
Codeine
Dextromethorphan

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6
Q

Antitussives

non-Opioids

A

Benoxinate -local anesthetic

Diphenhydramine -antihistamine

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7
Q

Expectorants

overview

A

used in copd

Facilitate secretion or decrease viscosity of mucus to facilitate clearance of mucus secretions in airways.

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8
Q

N-acetyl-cysteine*

A

Expectorants

breaks sulfhydryl bonds in mucus proteins; makes mucus less sticky

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9
Q

Guaifenesin*

A

Expectorants

claimed to facilitate removal of viscous mucus.

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10
Q

Potassium iodide:

A

Expectorants

claimed to decrease viscosity of mucus.

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11
Q

Recombinant DNAse (Dornase alpha)

A

Expectorants

-useful in cystic fibrosis.

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12
Q

Other Therapy for Rhinitis

A

Ipratropium bromide
vasomotor rhinitis

Intranasal cromolyn sodium, nedocromil

Intranasal corticosteroids

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13
Q

Intranasal corticosteroids

A
beclomethasone dipropionate (Beconase AQ)
budesonide (Rhinocort Aqua)
flunisolide (generic, Nasarel)
fluticasone propionate (Flonase)
mometasone furoate (Nasonex)
triamcinolone acetonide (Nasacort AQ)
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14
Q

Allergic Rhinitis

Drugs delivered locally as nasal spray

A
Antihistamines
Antimuscarinics
Cromolyn compounds
Topical corticosteroids
Nasal decongestants
Sympathomimetic Agents
-adrenergic agonists
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15
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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16
Q

What drugs act on the cholinergic muscarinic receptor

A

Diphenhydramine

clemastine

promethazine

they have a sedative effect in brain

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17
Q

what drugs act on the alpha drenergic recetpros

A

promthezine

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18
Q

what receptors act at serotonin receptors

A

cyproheptadine

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19
Q

Clinical Indications oh H1 antagonists

A

Acute and Chronic Allergic Rhinitis

Vasomotor rhinitis
antimuscarinic effects help

Eosinophilic nonallergic rhinitis

Viral Upper Respiratory Infection
antimuscarinic effects help

Urticaria

Allergic conjunctivitis

Anaphylactic reactions
adjunct to epinephrine

Motion sickness and nausea

Insomnia

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20
Q

Key Drugs -1st Generation H1 antagonists

A
  • Diphenhydramine (Benadryl)
  • Chlorpheniramine (Chlor-Trimeton)
Others
Dimenhydrinate (Dramamine)
Cyclizine (Marezine)
Hydroxyzine (Atarax)
Meclizine (Bonine)
*Promethazine (Phenergan)
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21
Q

Key Drugs -2nd generation H1 antagonists

A
Cetirizine (Zyrtec)

Fexofenadine (Allegra)

Loratadine (generic, Claritin, Alavert)

Desloratadine (Clarinex)

Azelastine (Astelin) Intranasal spray

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22
Q

Key Points -2nd generation H1 antagonists

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 1stgeneration
therefore, longer duration of action

Lower incidence of antimuscarinic side effects, e.g. dry mouth, dysuria, etc.

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23
Q

Clinical Effects

antihistamines

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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24
Q

Side Effects
1stgeneration agents

h1 antagonists

A

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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25
Q

Side Effects
1stgeneration agents

Sedation

A

antimuscarinic effect

1stgeneration only

26
Q

Side Effects
1stgeneration agents

CNS

A

dizziness, tinnitus, nervousness, insomnia, fatigue, blurred vision
1stgeneration only

27
Q

Side Effects
1stgeneration agents

GI

A

nausea, vomiting, loss of appetite

28
Q

Side Effects
1stgeneration agents

Dry mouth

A

–(antimuscarinic effect)

1stgeneration only

29
Q

Side Effects
1stgeneration agents

urinary retention

A

(antimuscarinic effect)1stgeneration only

30
Q

Other Therapy for Rhinitis

A

Ipratropium bromide
vasomotor rhinitis

Intranasal cromolyn sodium, nedocromil

Intranasal corticosteroids
beclomethasone dipropionate
budesonide
flunisolide
fluticasone propionate
triamcinolone acetonide
31
Q

Antimuscarinics: Ipratropium bromide

A

A quaternary muscarinic receptor antagonist

32
Q

Ipratropium bromide If given parenterally

A

effects are like atropine

33
Q

Ipratropium bromide if given as an aerosol

A

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

34
Q

Ipratropium bromide parasympathetic

A

mediated bronchospasm is a significant component of airway resistance in some asthmatics and COPD patients, especially psychogenic exacerbations

35
Q

Ipratropium bromide

Therapeutic Use:

A

Bronchodilation develops more slowly and is usually less intense than that produced by -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 rhinitisand chronic postnasal drip syndrome.

36
Q

Cromolyn Compounds

drugs

A

Cromolyn sodium nasal spray (Nasalcrom)

Cromolyn sodium (Intal)

37
Q

Cromolyn Compounds

A

Cromolyn compounds are *anti-inflammatoryagents 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.

38
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.

Used mostly in mild to moderate asthma as an added therapy or as a prophylactic alternative to inhaled steroids or oral methylxanthines.

39
Q

cromolyn compounds

adverse effects

A

are infrequent and generally mild

40
Q

Intranasal Corticosteroids

overview

A

*Most effective drugsavailable 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.

41
Q

Intranasal Corticosteroids

A

Side Effects –usually mild

Dryness & irritation or burning of nasal mucosa

Sore throat

Epistaxis

Headache

42
Q

Leukotriene Modifier overview

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
Safe and with few side effects

43
Q

Leukotriene Modifier

One study showed montelukast to be as effective

A

as loratadine, but not as effective, alone or in combination with loratadine, as an intranasal corticosteroid

44
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

45
Q

Allergic Conjunctivitis

Treatment

A

Oral antihistamines (2ndgeneration) usually effective

Topical antihistamine eye drops
also effective
may be more rapid acting
also antiinflammatory

46
Q

Allergic Conjunctivitis

*Antihistamine/decongestant combinations

A

pheniramine/naphazoline (Visine A)

antazoline/naphazoline (Vasocon-A)

Available over-the-countermay be more effective than either agent alone but are short actingand can cause rebound vasodilation with continued use

47
Q

Topical Ocular H1 -Antihistamines

A

Azelastine (Optivar)
Emedastine difumarate (Emadine)
Levocabastine HCl (Livostin)

48
Q

Topical Ocular Mast Cell Stabilizers

A

Cromolyn sodium (generic, Crolom)
Lodoxamide tromethamine (Alomide)
Nedocromil sodium (Alocril)
Pemirolast potassium (Alamast)

49
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.

50
Q

Antiviral Agents

*Amantadine& Rimantadine

A

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

51
Q

Oseltamivir (*Tamiflu), oral

A

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

52
Q

Zanamivir (*Relenza)

A

same as Tamiflu but with an inhaler

53
Q

side effects of antihistamine are just

A

if taken chronically and at high doses

54
Q

tetrhydrozoline

A

visine

55
Q

Ipratropium bromide blockes

A

muscarinic decreases secretion so used for nasal drip

56
Q

A quaternary muscarinic receptor antagonist

A

permanently charged doesnt cross membranes

57
Q

young kids dont want to put on

A

steroids

58
Q

Intranasal corticosteroids control

A

symptoms then stop taking

59
Q

antihistamines Molecular Mechanism of Action

A

slow hours at the soonest

steroids

heat shock proteins

turning on and off packets of genes

60
Q

glucocorticoids summary of action

A

inhibits migration and activation of cells in immune resposne

poor wound healing

61
Q

Inhibits neuraminidase of influenza A or B

A

prevents entry into cell