Antiasthmatic Drugs

1. ANTI
ASTHMATICS
PREPARED BY:
USHA RANI KANDULA,
ASSISTANT PROFESSOR,
DEPARTMENT OF ADULT HEALTH NURSING,
ARSI UNIVERSITY,ASELLA,ETHIOPIA,
SOUTH EAST AFRICA.

2. DEFINITION
 Asthma is characterized by
increased responsiveness of
trachea and bronchi to various
stimuli and by narrowing of the
airways.
 Antiasthmatic are drugs used to
treat asthmatic conditions.

3. CLASSIFICATION
OF
ANTI ASTHMATICS

4. CLASSIFICATION OF ANTI
ASTHMATICS
 Bronchodilators
 Leukotriene antagonists
 Mast cell stabilizers
 Anti-inflammatory agents
 Anti-IgE antibody

5. BRONCHODILATORS

6. Bronchodilators
 These are the drugs used in
bronchial asthma and relax the
spasm of bronchi by sympathetic
nervous system stimulation.

7. Bronchodilators
 Classified as –
 Beta 2 sympathomimetics
 Methylxanthines
 Anticholinergics

8. Beta 2 Symapathomimetics
 The Symapathomimetic drugs,
whose mimic that of sympathetic
stimulation.
 The Symapathomimetic agents or
beta - adrenergic receptor agonists
are widely used for treatment of
asthma.

9.  There are two type of receptors-
beta 1 and beta 2.
 The beta 1 adrenergic receptors
are present in the heart and beta 2
receptors are present in lungs.

10.  By stimulation of beta 2
adrenergic receptors these agents
; relax bronchial muscles, inhibit
the release of mediators from
mast cells, enhance mucociliary
activity and effect composition of
mucus.

11.  So when beta- adrenergic
receptor agonists are
administered, adverse effects are
caused by stimulation of beta-1
receptors in heart, which cause
cardiac stimulation.

12.  Thus, now drugs having greater
affinity to beta 2 adrenergic
receptors has been developed.

13.  Adenergic that effect the primarily
beta 2 adrenergic receptors are
called selective beta 2 adrenergic
agonists.
 But selectivity is lost at
sufficiently high concentration of
these drugs.

14. BETA 2
SYMPATHOMIMETICS
DRUGS

15. Beta 2 sympathomimetics
 Terbutaline
 Salbutamol
 salmetrol

16. Beta 2 sympathomimetics
 Beta 2 sympathomimetic agents
are classified under 2 broad
categories.
 i.e.
 1.catecholamines
 2. noncatecholamines

17.  For the purpose of simplify the
understanding , the important beta 2
sympathomimetic drugs are
discussed under
 1.selective beta 2 receptor agonist
and
 2.non-selective beta 2 receptor
agonist categories.

18. CLASSIFICATION
OF SYMPATHOMIMETICS
1. SELECTIVELY BETA 2
RECEPTOR AGONIST
2. NON-SELECTIVELY
BETA 2 RECEPTOR
AGONIST

19. SELECTIVELY BETA 2
RECEPTOR AGONIST

20. Selectively beta 2 receptor
agonist
 Salbutamol ( albuterol ) :
 It is a short acting beta 2
adrenergic receptor agonist used
for the relief of bronchospasm in
conditions such as asthma and
COPD.

21. Salbutamol MOA
 Airway smooth muscle has little
sympathetic nervous supply but
contain lots of beta 2
adrenoreceptors that respond to
circulating adrenaline.

22. Con-------------
 The stimulation of beta 2
receptors leads to rise in
intracellular cyclic adenine
monophosphate (cAMP) levels
and the subsequent bronchial
smooth muscle relaxation.

23. Dose
 Oral ( children )
 2-6 years: 0.1-0.2 mg/kg/dose
three times / day , maximum does
not exceed 12 mg/day ( divided
doses)

24.  6-12 years : 2mg/dose 3-4
times/day; maximum does not
exceed 24 mg/day (divided doses)
 Extended release : 4 mg every 12
hours ; maximum dose not to
exceed 24 mg/day ( divided
doses).

25. Above 12 years and adults
 2-4 mg 3-4 times /day, not to
exceed 32 mg/day
 Extended release : 8 mg every 12
hours , not to exceed 32 mg /day
 Elderly : 2 mg 3-4 times/day,
maximum 8 mg 4 times/day.

26. Nebulization
 Children: > 2-12 years : 0.63-1.25
mg every 4-6 hours .
 Children 4 years :
 - quick relief : 0.63-2.5 mg every 4-
6 hours.
 Exacerbation of asthma : 0.15
mg/kg every 20 min for 3 doses.

27. Children 5-11 years
 Quick relief: 1.25-5mg every 4-8
hours
 Exacerbation of asthma :
0.15mg/kg every 20 min 3 times.

28. Above 12 years and adults
 Quick relief : 1.25-5mg every 20
min for 3 doses
 Continuous infusion :
 Adults : severe bronchospasm
and status asthmaticus .

29. Indications
 Asthma
 COPD
 Exercise induced bronchospasm

30. II. NON-SELECTIVE BETA 2
RECEPTOR AGONIST

31. II. NON-selective beta 2 receptor
agonist
 Ephedrine
 Ephedrine (EPH) is a
sympathomimetic amine used as
a stimulant, decongestant,
treating allergic asthma and
bronchodilator.

32. Ephedrine MOA
 Ephedrine releases tissue stores
of norepinephrine and there by
produces an alpha and beta
adrenergic stimulation , longer
acting and less potent than
epinephrine.

33. Dose
 Children : oral, 3mg /kg/day
 IM , slow IV push : 0.2-0.3 mg/kg
 Adults : oral : 25-50 mg every 3-4
hours
 Sc:25-50 mg
 IV: 5-25mg/dose slow IV push

34. Indications
 Treatment of bronchial asthma
and bronchospasm

35. METHYLXANTHINES

36. Methylxanthines
 Theophylline
 Aminophylline
 Hydroxyethyl theophylline

37. Theophylline
 Theophylline , known as
dimethylxanthine drug used for
COPD or asthma.

38. Theophylline MOA
 It causes bronchodilatation, which
increase tissue concentrations of
cAMP, (cyclic adenine
monophosphate (cAMP) which in
turn promotes catecholamine of
lipolysis, glycogenolysis and
gluconeogenesis and induces
release of epinephrine from adrenal
medulla cells.

39. Dosage
 Adult minimum / maximum dose :
6.0 mg/kg /24.0 mg/kg
 Paediatric minimum / maximum
dose : 2.0mg/kg/24.0mg/kg

40. ANTICHOLINERGICS
(MUSCARINIC
ANTAGONIST)

41. An anticholinergic agent
is a substance that blocks
the neurotransmitter acetylcholine in
the central and the peripheral nervous
system.

42. Anticholinergic drugs
 Ipratropium bromide
 Tiotropium bromide

43. Ipratropium bromide
 - Ipratropium bromide is an
anticholinergic drug,
 - chemically related to atropine.

44. Ipratropium bromide MOA
 It blocks muscarinic cholinergic
receptors,
 Resulting in a decrease in the
formation of cyclic guanosine
monophosphate (cGMP).
 This results in decreased
contractility of smooth muscle.

45. Dosage
 1.Aerosol / inhalation two
inhalations four times daily . Do
not exceed 12 inhalations in 24
hours.
 Spray 0.03 formulation :2 sprays
per nostril 3 or 4 times daily.

46. Indications
 In the treatment of obstructive
lung diseases.
 The management of COPD and
asthma.
 To reduce rhinorrhea .

47. LEUKOTRIENE
ANTAGONISTS

48. Leukotrienes
 Leukotrienes are inflammatory
chemicals the body releases after
coming in contact with an allergen or
allergy trigger.

49. Leukotriene antagonists
 Montelukast
 Zafirlukast

50. Montelukast
 A leukotriene antagonist is a drug
that inhibits leukotrienes.

51. Montelukast MOA
 That inhibits the cysteinyl
leukotrine receptor .

52. Dosage
 Oral ( children )
 6-11 months : Asthma : 4mg once
daily
 6-23 months : allergic rhinitis :
4mg once daily
 12-23 months : Asthma : 4 mg
once daily.

53.  6-14 years : Asthma, allergic rhinitis
: 5mg , once daily
 Above 15 and adults : Asthma or
allergic rhinitis : 10 mg/day
 Asthma, acute : 10 mg a single dose
 Bronchoconstriction, exercise
induced asthma : 10 mg at least 2
hours prior.

54. MAST CELL STABILIZERS

55. MAST CELL
 A mast cell is a type of white
blood cell and part of
immune and neuroimmune syste
mcontains histamine .

56. Mast cell stabilizers
 Mast cell stabilizers are used to
prevent or control allergic
disorders.
 They block a calcium channel
essential for mast cell
degranulation, stabilizing the cell .

57.  So prevent the release of
histamine and related mediators.

58. Mast cell stabilizers
 Sodium cromoglycate
 Ketotifen

59. Sodium cromoglycate
 Cromoglicic acid is a mast cell
stabilizer.
 This drug prevent the release of
inflammatory chemicals as
histamine from mast cells.

60. Sodium cromoglycate MOA
 It prevents the release of
mediators that attract
inflammatory cells
 And because it stabilizes the
inflammatory cells.

61. Dosage
 One sterule 4 times daily at 4-6
hourly intervals.

62. Indications
 To treat allergic rhinitis
 Asthma
 Allergic conjunctivitis
 Food allergies

63. ANTI-INFLAMMATORY
AGENTS

64. Anti-inflammatory agents
Classified as –
Systemic corticosteroids
Inhalational corticosteroids

65. CORTICOSTEROIDS

66. corticosteroids
 Corticosteroids are one of the
type of steroids.
 It is used in the treatment of the
asthma is called
glucocorticosteroid .

67.  They work by suppressing the
inflammatory reaction that causes
swelling and narrowing of the
bronchi.

68. Systemic corticosteroids
 Hydrocortisone
 Prednisolone

69. Hydrocortisone
 Hydrocortisone is a
natural corticosteroid produced
by the adrenal glands located
adjacent to the kidneys.

70. Hydrocortisone MOA
 Hydrocortisone decreases
inflammation by migration of
leukocytes and reversal of
increased capillary permeability.

71. Dosage
 Anti-inflammatory or
immunosuppressive (infants and
children):
 Oral : 2.5-10mg/kg/day
 IM, IV : 1-5 mg/kg/day
 Adolescents and adults : oral,
IM,IV:15-240 mg every 12 hours.

72.  Status asthmaticus ( children and
adults ) : IV : 1-2 mg/kg/dose
every 6 hours for 24 hours,
 Then maintenance of 0.5-1 mg/kg
every 6 hours.

73. Indications
 Adrenocortical insufficiency
 Diseases of allergic, inflammatory
or autoimmune origin.

74. Inhalational corticosteroids
Beclomethasone dipropionate
Fluticasone propionate

75. Beclomethasone ( inhaled )
 Inhaled corticosteroids are the
preferred treatment for long-term
control of mild, moderate, severe
asthma symptoms in children,
teen and adults.

76.  They help control narrowing and
inflammation in the bronchial
tubes.
 Beclomethasone dipropionate ,
also referred to as
beclomethasone, is a potent
glucocorticoid steroid.

77.  In the form of an inhaler , it is
used for the prophylaxis of
asthma.
 As a nasal spray , it is used for
the treatment of rhinitis and
sinusitis.

78. Beclomethasone MOA
 Controls the rate of protein
synthesis and depresses the
migration of
leukocytes,fibroblasts.

79.  It also reverses capillary
permeability and lysosomal
stabilization at the cellular level to
prevent or control inflammation.

80. Dose
 Inhalation, nasal
 Rhinitis, nasal polyps
 Children > 6 yrs and adults : 1-2
inhalations each nostril twice
daily.

81. Indications
 Oral inhalation : Asthma
 Nasal aerosol : rhinitis and nasal
polyps following surgery.

82. Anti-IgE antibody
 Omalizumab : is a monoclonal
antibody targeting the high –
affinity receptor binding site on
human immunoglobulin IgE.

83.  It reduces the severity of
exacerbations (increase in the
severity of a disease)
 -and reduce medication use and
improve rhinitis related quality of
life.

84. Omalizumab MOA
Omalizumab is an IgG
monoclonal antibody , which
inhibits IgE binding to the high
affinity IgE receptor on mast
cells and basophils.

85.  By decreasing bound IgE, the
activation and release of
mediators in the allergic response
is limited.

86. Idications
 Allergic asthma .

87. NURSES
RESPONSIBILITIES

88. NURSES RESPONSIBILITIES
 Assess the patient --------
 Proper method of drug intake
 Relieveing of symptoms
 Effectiveness of drugs
 Hypersensitivity of the drugs

89. PATIENT EDUCATION

90. Patient education
 Use drugs exactly as directed
 Do not take more than
recommended dosage
 Instruct patient on proper use of
inhaler
 How to insert drug into the inhaler

91. Con-------
 Inhalational devices require
regular cleaning.
 Do not stop other asthma
medications unless adviced by
the prescriber.
 Inform the complications.

92. THANKING
YOU