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Respiratory: Pharmacology > Drugs for Rhinitis and Rhinorrhoea > Flashcards

Drugs for Rhinitis and Rhinorrhoea Flashcards

1
Q

What is rhinitis?

A

A common and often debilitating disease involving acute or chronic inflammation of the nasal mucosa

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2
Q

What are the characteristic symptoms of rhinitis?

A
  • rhinorrohea (‘runny nose’ - watery mucus accumulation in nasal cavity)
  • sneezing
  • itching
  • nasal congestion and obstruction (swelling of nasal mucosa largely due to dilated blood vessels - particularly in cavernous sinusoids)
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3
Q

What is nasal congestion?

A

Does NOT refer to mucous - refers to dilated blood vessels in respiratory or nasal mucosa
* These dilated blood vessels contribute to swelling of mucosa and lead to obstruction of airflow through nasal cavity

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4
Q

What are the different types of rhinitis?

A
  • Allergic
  • Non-allergic
  • Mixed
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5
Q

What are the classifications of allergic rhinitis?

A
  • Seasonal (SAR)
  • Perennial (PAR)
  • Episodic (EAR)
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6
Q

What condition is allergic rhinitis often linked to?

A

Asthma

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7
Q

What is the mechanism of allergic rhinitis?

A
  • Inhalation of allergen increases specific IgE levels
  • IgE binds to receptors on mast cells and basophils
  • Re-exposure to allergen causes mast cell and basophil degranulation
  • Release of mediators including histamine, cysLTs, tryptase, prostaglandins
  • Causes acute itching, sneezing, rhinorrhoea and nasal congestion
  • Delayed response caused by recruitment of lymphocytes and eosinophils to nasal mucosa causes congestion and obstruction
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8
Q

What is non-allergic rhinitis?

A

Any rhinitis, acute, or chronic, that does not involve IgE-dependent events

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9
Q

What are causes of non-allergic rhinitis?

A
  • Infection – infectious rhinitis (largely viral)
  • hormonal imbalance – hormonal rhinitis (e.g. pregnancy)
  • vasomotor disturbances – vasomotor rhinitis (cause unknown, i.e. idiopathic)
  • Nonallergic rhinitis with eosinophilia syndrome (NARES)
  • Medications – drug induced rhinitis (e.g. aspirin)
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10
Q

What is occupational rhinitis?

A

May involve both allergic and non-allergic components

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11
Q

What do both rhinitis and rhinorrhoea?

A
  • Involve increased mucosal blood flow
  • Increased blood vessel permeability
  • These effects increase the volume of the nasal mucosa and cause difficulty breathing in
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12
Q

What is used to target inflammation in rhinitis?

A

Glucocorticoids (anti-inflammatory) - will treat allergic rhinitis

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13
Q

What drugs are used to block mediator receptors in rhinitis and rhinorrhoea?

A
  • H1 (histamine) receptor antagonists

* CysLT1 receptor antagonists

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14
Q

What drugs are used to decrease nasal blood flow?

A

Vasoconstrictors (act on a1 adrenoceptors)

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15
Q

What drugs are anti-allergic in the treatment of rhinitis?

A

Sodium cromoglicate (immunosuppressant effect)

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16
Q

What is the purpose of a decongestant?

A

Does not get rid of mucous in the nose, restricts blood flow to vasal mucosa

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17
Q

What is the mechanism of glucocorticoids?

A

Reduce vascular permeability, recruitment and activity of inflammatory cells and the release of cytokines and mediators

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18
Q

What are glucocorticoids used to treat?

A
  • Mainstay therapy for SAR and PAR

* Also used in NARES and vasomotor rhinitis

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19
Q

How are glucocorticoids administered in rhinitis?

A

Applies topically as a spray to the nasal mucosa e.g. intranasal administration once daily

20
Q

How are glucocorticoids used to treat moderate-to-severe and severe intractable rhinitis?

A
  • Moderate-to-severe - may be combined with anti-histamines

* Severe - may be given orally (short term)

21
Q

What are examples of glucocorticoids?

A
  • beclometasone
  • fluticasone
  • prednisolone (oral)
22
Q

What are anti-histamines?

A

H1 receptor antagonists

23
Q

What is the mechanism of H1 receptor antagonists?

A
  • Competitive antagonists that reduce effects of mast cell derived histamine
  • Less effect on congestion than other symptoms
24
Q

What effects does histamine normally have?

A
  • vasodilatation and increased capillary permeability
  • activation of sensory nerves
  • mucus secretion from submucosal glands
25
Q

What are H1 receptor antagonists effective in treating?

A

Effective in SAR, PAR and EAR, less so in non-allergic rhinitis

26
Q

How are H1 receptor antagonists administered?

A

Administered orally, or as an intranasal spray (azelastine)

27
Q

Are H1 receptor antagonists used in combination with other therapies?

A

Effective as monotherapy

28
Q

What generation of H1 receptor antagonists are preferred?

A

Available as first and second generation agents
* Second generation agents preferred due to reduced sedation (do not cross blood brain barrier) and lack of anti-cholinergic effects

29
Q

What are examples of H1 receptor antagonists (anti-histamines)?

A
  • loratidine
  • fexofenadine
  • cetirizine (also has mild anti-inflammatory action)
30
Q

What are anti-cholinergic drugs?

A

Muscarinic receptor antagonists

31
Q

What are the mechanisms of anti-cholinergic drugs?

A

ACh released from post-ganglionic parasympathetic fibres activates muscarinic receptors on nasal glands causing a watery secretion that contributes to rhinorrhoea – blocked by muscarinic antagonists

32
Q

What are the effects of muscarinic receptor antagonists?

A

Reduce rhinorrhoea in PAR and SAR but have no influence upon itching, sneezing and congestion (note the anti-cholinergic activity of first generation H1 blockers may contribute to their ability to suppress rhinorrhoea)

33
Q

How are anti-cholinergic drugs administered?

A

Administered intranasally

34
Q

What are side effects of muscarinic receptor antagonists?

A

May cause dryness of nasal membranes, but no other adverse effects

35
Q

What is the only muscarinic receptor antagonist used in treatment of rhinitis?

A

Ipratropium is the sole agent used in this class

36
Q

What is the mechanism of sodium cromoglicate?

A

Mast cell stabilisation

37
Q

What is sodium cromoglicate used for in the treatment of rhinitis?

A

Used for maintenance treatment of allergic rhinitis with an onset of action of 4 to 7 days, but weeks may be required for full effect

38
Q

How is sodium cromoglicate administered?

A

Nasal administration - less effective than nasal corticosteroids

39
Q

What is the mechanism of Cysteinyl Leukotriene receptor antagonists?

A

CysLT1 receptor antagonists reduce the effects of CysLTs upon the nasal mucosa

40
Q

What are the effects of CysLT1 receptor antagonists?

A

Equi-effective with H1 receptor antagonists in treating PAR and SAR, with which their effect may be addictive

41
Q

How are CysLT1 receptor antagonists administered?

A

Via oral route

42
Q

What are CysLT1 receptor antagonists used to treat?

A

Allergic rhinitis and asthma

43
Q

What is an example of a CysLT1 receptor antagonist?

A

Montelukast is the sole agent used in this class

44
Q

What are the mechanisms of vasoconstrictors?

A

Act as directly, or indirectly, to mimic the effect of noradrenaline. Produce vasoconstriction via activation of 1-adrenoceptors to decrease swelling in vascular mucosa

45
Q

What is an example of a vasoconstrictor?

A

Oxymetazoline, a selective 1-adrenoceptor agonist (given intranasally), is effective, short term, in reducing congestion in allergic rhinitis

46
Q

Why is nasal administration of oxymetazoline for more than a few days not recommended?

A

Due to the development of a rebound increase in nasal congestion upon discontinuation - rhinitis medicamentosa

47
Q

Why does rhinitis medicamentosa occur with oxymetazoline?

A

Due to a1 receptor desensitisation and down regulation

Respiratory: Pharmacology (4 decks)

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