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Respiratory > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

How does the parasympathetic division control bronchial smooth muscles

A

Postganglionic cholinergic fibres cause bronchial smooth muscle contraction mediated my M3 muscarinic ACh receptors on airway smooth muscle cells and increase mucus production via M3 muscarinic ACh receptors on goblet cells
Postganglionic noncholinergic fibres cause bronchial smooth muscle relaxation by Nitric Oxide (NO) and Vasoactive Intestinal Peptide (VIP)

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2
Q

Is there sympathetic innervation of bronchial smooth muscle in humans

A

No but post-ganglionic fibres supply submucosal glands and smooth muscle of blood vessels

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3
Q

How does sympathetic nervous system cause bronchodilation

A

Sympathetic innervation of vascular smooth muscle. Adrenaline from Chromaffin cells of adrenal medulla cause bronchodilation via B2-adrenoceptors

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4
Q

What cause contraction in smooth muscle cells

A

Depolarization opens Ca channels causing an inflow of Calcium. Hormones activates GPCR which eventually leads to the opening of IP3 receptor causing Ca influx. Increased intracellular Ca leads to contraction

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5
Q

How does increase Ca cause contraction

A

Ca binds to Calmodulin which forms a Ca-Calmodulin complex. This combines myosin light chain kinase (MLCK) to activate it. This kinase phosphorylates inactive myosin cross bridge to phosphorylated myosin cross bridge (binds actin). This allows sliding of Actin and Myosin filaments.

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6
Q

What brings about relaxation in smooth muscle

A

Dephosphorylation of myosin light chain by myosin phosphatase. This requires return of intracellular Ca concentration to basal level

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7
Q

How does protein kinase A inhibit contraction or facilitate relaxation

A

Adrenaline from sympathetic nervous system activates GPCR which activates protein kinase A. This inhibits contraction by inhibiting myosin light chain kinase. It also facilitates relaxation by stimulating myosin phosphatase

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8
Q

What is Asthma

A

Intermittent attacks of bronchoconstriction causing tight chest, wheezing, difficulty in breathing and cough

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9
Q

What can chronic asthma cause

A

Increase mass of smooth muscle
Accumulation of interstitial fluid (oedema)
Increased secretion of mucus
Epithelial damage (exposing nerve fibres)
Sub-epithelial fibrosis

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10
Q

What causes bronchial hyper-responsiveness in asthma

A

Exposure of sensory nerve endings contributes to increased sensitivity of the airways by bronchoconstrictor influences

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11
Q

Hypersensitivity vs hyperreactivity

A

Hypersensitivity is how much concentration of bronchoconstrictor is needed to induce a fall in FEV1 whereas hyperreactivity is the opposite

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12
Q

Phases of asthma attack

A

In two phases, immediate phase (bronchospasm) and delayed phase (inflammatory reaction)

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13
Q

Response to allergens in nonatopic individuals

A

Low level Th1 response, cell-mediated involving IgG and macrophage
Strong Th2 response, antibody-mediated involving IgE

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14
Q

How does allergic asthma develop

A

Induction phase - Antigen presenting cells present to CD4+ T cells which cause preferential differentiation into Th2 cells that activate B cells via IL-4. These B cells mature to IgE secreting plasma cells.
Effector phase - Th2 also secrete IL-5 and activate Eosinophils. IL-3 and IL-4 from Th2 cells cause expression of Fc receptors for IgE on mast cells

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15
Q

What happens on subsequent encounter to antigen in allergic asthma

A

Antigen cross links with IgE receptors. This stimulates Ca2+ entry into mast cells and release of Ca2+ from intracellular stores. This causes release of preformed Histamine from mast cells and production and release of other agents such as leukotrienes that cause airway smooth muscle contraction. They also release pro-inflammatory factors: platelet-activating factor, prostaglandins that attract cells: macrophage and eosinophils causing local inflammation

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16
Q

Why can corticosteroids cause pneumonia

A

Due to immune suppression and impaired ciliary clearance. Especially with fluticasone, retainted in lung for long periods

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17
Q

Why are oral steroids used for acute exacerbations and not maintenance

A

Ex: Prednisolone, has a low therapeutic ratio. Inhaled steroids such as Beclomethasone have a high therapeutic ratio and is used as maintenance monotherapy in asthma

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18
Q

Combination therapy for COPD

A

Inhaled corticosteroid (ICS) + LABA

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19
Q

How can lung delivery be optimised

A

Using extra fine solution inhaler with a spacer

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20
Q

Function of spacer device

A

Acts as a holding chamber for the aerosol, improve lung deposition, reduce particle size and velocity

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21
Q

When are cromones such as cromoglycate used

A

In asthma only. They are mast cell stabilizers. Not used much due to poor efficacy

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22
Q

How can leukotrienes cause asthma

A

Leukotrienes cause oedema in blood vessels, increase mucus secretion, decrease mucus transport, eosinophillic influx, contraction and proliferation of airway smooth muscle

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23
Q

How can eosinophil influx cause cause epithelial cell damage

A

Increase numbers of eosinophils in the airway causes release of inflammatory mediators such as cationic proteins. These damage epithelial cells and expose sensory fibres. This stimulates cough and other bronchial reflexes

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24
Q

Leukotriene receptor antagonists can be used in?

A

Asthma only, exercise induced asthma and allergic rhinitis (with histamine)

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25
Q

Most potent anti-inflammatory drug

A

Inhaled corticosteroids

26
Q

When are anti-IgE monoclonal antibodies used

A

Omalizumab; used in severe persistent allergic asthma . Given as an injection every 2-4 weeks.

27
Q

When are anti-IL5 injections given to patients every 4 weeks

A

Mepolizumab, reslizumab; severe refractory eosinophilic asthma despite max therapy

28
Q

What medication has little effect on pulmonary function but reduces exacerbations and oral steroid sparring effect

A

Anti-IgE and anti-IL5. Both given as injection and very expensive.

29
Q

What is severe refractory eosinophilic asthma

A

Severe asthma that can’t be adequately controlled despite available treatment possibilites

30
Q

Physiological effects of B2 agonists

A

Mast cell stabilization, increased muco-ciliary clearance, decreased extravasation of proteins, smooth muscle relaxation,

31
Q

Examples of long acting B2 agonists

A

BID - Salmeterol/formoterol

OD - Indacaterol/ vilanterol/olodaterol

32
Q

What is in a SMART combination inhaler

A

Beclamethasone (ICS) + Formoterol (LABA)

33
Q

B2 agonists in asthma and COPD

A

ICS + LABA dual in asthma

ICS + LABA or LAMA/LAMA dual or ICS/LABA/LAMA triple in COPD

34
Q

What do M1 cholinergic receptors do

A

Enhance cholinergic reflex

35
Q

What do M2 cholinergic receptors do

A

Inhibit acetylcholine release

36
Q

What do M3 cholinergic receptors do

A

Mediate bronchoconstriction and mucus secretion

37
Q

What do muscarinic antagonist drugs work on

A

Post junctional end plate M3 receptors

38
Q

Short acting muscarinic antagonist

A

Ipatropium QID - Inhaled 4 times daily

39
Q

Long acting muscarinic antagonist

A

Tiotropium (OD), Umeclidinium (OD), Aclidinium (BID) and Glycopyrronium (OD/BID)

40
Q

Muscarinic antagonists in COPD

A

LAMA/LABA dual - Glycopyrronium + Indacaterol or Tiotropium + Olodaterol
ICS/LAMA/LABA triple - Beclometasone + Formoterol + Glycopyrronium

41
Q

Muscarinic antagonist in asthma

A

Triple therapy with Tiotropium only

ICS/LABA/LAMA

42
Q

What is used with inhaled corticosteroids as non steroidal anti-inflammatory

A

Methylxanthines
Theophylline (Oral) for maintenance therapy
Aminophylline (IV) for acute attacks

43
Q

What are used in addition to LABA/LAMA in COPD to reduce exacerbations

A

PDE4 inhibitors such as Roflumilast (oral tablet OD)

44
Q

What can be used to reduce sputum viscosity and aide sputum expectoration in COPD

A

Mucolytics such as carbocisteine and erdosteine (oral)

45
Q

Are respiratory stimulants such as doxapram hydrochloride indicated for acute asthma

A

Doxapram stimulates increase in tidal volume and respiratory rate. These are NOT indicated acute asthma

46
Q

Pathology of COPD

A

Irritants cause stimulation of resident alveolar macrophage. Cytokine production activates neutrophils and CD8+ T cells that increase macrophage numbers. They release matrix metalloproteinase that cause chronic bronchitis and emphysema

47
Q

What receptors cause bronchoconstriction

A

M3 muscarinic receptors via parasympathetic efferents

48
Q

Where are M1 muscarinic acetylcholine receptors present

A

Ganglia, facilitate fast neurotransmission mediated by ACh acting on nicotine receptors.

49
Q

Where are M2 muscarinic acetylcholine receptors present

A

Postganglionic neurone terminals where they act as inhibitory autoreceptors reducing release of ACh

50
Q

Where are M3 muscarinic acetylcholine receptors present

A

Airway smooth muscle that mediate contraction to ACh

Also on mucus secreting cells mediating mucus secretion

51
Q

Why prefer selective muscarinic acetylcholien receptor antagonist over Atropine (not selective)

A

Reduces systemic exposure avoiding multiple potential adverse effects of generalised parasympathetic block

52
Q

Why do muscarinic receptor antagonists have little systemic absorption

A

Due to quarternary ammonium group

53
Q

Do muscarinic receptor antagonists have an effect of COPD progression

A

No, use is mainly palliative to reduce bronchospasms and decrease mucus secretion

54
Q

What does Ipratropium block

A

M1, M2 and M3 receptors

55
Q

What drugs block M3 receptors

A

Tiotropium, glycopyrronium, aclidinium, umeclidinium

56
Q

What is block of M2 receptors in COPD not wanted

A

M2 is an inhibitory autoreceptor present on post-ganglionic neurones. Antagonism of this will increase amount of ACh released from post-ganglionic neurone

57
Q

Examples of ultra-LABA

A

Indacaterol and olodaterol, not recommended for acute relief of bronchospasms. Once daily dosing

58
Q

Is LABA or SAMA more effective in increased FEV1

A

Combination of both, B2 agonists and M antagonists

59
Q

How do PDE4 drugs work

A

Phosphodiesterase-4 (PDE4) is the prominent PDE present on macrophage, neutrophils and T cells. Inhibition of PDE4 may have inhibitory effects of inflammation and immune cells

60
Q

Example of PDE4 drug

A

Rofumilast. Oral treatment for severe COPD but limiting adverse GI effects

61
Q

Are COPD patients generally responsive to glucocorticoids

A

No due to oxidative/nitrative stress associated with chronic inhalation of tobacco smoke

62
Q

When are glucocorticoids generally administered to COPD patients

A

Patients with frequent and severe exacerbations when given with a LABA

Respiratory (26 decks)

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