Hello members...this is my 39th powerpoint...
It deals with LABA & SABA...The brochodilators used in the treatment of Pulmonary diseases like Asthma & COPD.
It gives a short insight into the drugs used, their indications with dosages, ADRs, interactions, etc.
Worthwhile for a precise information on the same!!
Happy reading!!!
:) :)
3. - BETA-2 AGONISTS ( Also known as Beta-2 adrenergic receptor agonists)
represent drugs that come under the class of “BRONCHODILATORS”
- Drugs relax & enlarge (dilate) airways in lungs makes breathing easier
- Primarily used to treat asthma & other pulmonary disorders like COPD
- Classified into:
1. SABA(Short-Acting Beta-2 Agonists)
2. LABA(Long-Acting Beta-2-Agonists).
5. - Beta-2-agonists bind to beta-2-receptors (coupled with stimulatory
G-protein of adenyl cyclase enzyme) of bronchial smooth muscle of
lung enzyme increases concentration of Cyclic-AMP levels in lung
leads to reduction of Ca++ concentration within cells activation
of protein kinase A leads to increased membrane potassium
conductance causes smooth muscle relaxation & bronchodilation.
- Activation of beta-adrenergic receptors causes relaxation of
smooth muscle in the lung causes dilation & opening of airways.
9. Also known as “Quick-acting”, “Reliever” / “Rescue” medications
These drugs relieve acute asthma symptoms/ attacks very quickly, by opening
the airways
Rescue medications are considered best for treating sudden asthma symptoms
Action of inhaled bronchodilators starts within minutes(post-inhalation)
lasts for 2-4 hours
SABA also used before exercise, to prevent exercise-induced asthma.
11. Short-acting, selective beta-2 receptor agonist, used in the treatment of Asthma
& COPD
DRUG-INTERACTIONS:
a. Salbutamol + Saquinavir Both increase toxicity of each other by
Pharmacodynamic synergism high risk of hypokalemia, QT prolongation &
cardiac arrhythmias
b. Salbutamol + arformoterol Pharmacodynamic synergism insomnia may
occur.
• CONTRAINDICATIONS:
a. Hypersensitivity to salbutamol
b. Severe hypersensitivity to milk proteins
12. DOSE:
a. FOR BRONCHOSPASM:
- As nebulizer solution : 2.5 mg BID/TID PRN; 1.25-5 mg Q4-8 hr PRN, for quick
relief
- As aerosol MDI : 180 mcg(2 puffs), inhaled PO Q4-6 hr(Not to exceed 12
inhalations/24 hour)
- As powder MDI: 180 mcg (2 puffs) inhaled PO q4-6hr; not to exceed 12
inhalations/24 hr.
- As tablet and syrup: 2-4 mg PO q6-8hr; not to exceed 32 mg/day
13. Levosalbutamol has similar therapeutic effects as that of salbutamol in acute
exacerbation of asthma but has no side-effects, such as tachycardia &
hypokalemia.
DRUG INTERACTION:
a. Levosalbutamol + Arformoterol reduced serum potassium & sedation.
• DOSE:
a. FOR BRONCHOSPASM:
- Nebulizer solution: 0.63-1.25 mg 3 times daily q6-8hr
- Aerosol: 90 mcg (2 actuations of metered-dose inhaler) q4-6hr
b. FOR ASTHMA EXACERBATION:
- As nebulizer solution: 1.25-2.5 mg q20min for 3 doses, then 1.25-5 mg q1-4hr PRN
Aerosol: 180-360 mcg (4-8 actuations of metered-dose inhaler) q20min for ≤4 hr, then q1-4hr PRN
14. Synthetic amine
Structurally & pharmacologically similar to ISOPROTERENOL
Used as bronchodilator in treatment of asthma
DRUG INTERACTIONS:
a. METAPROTERENOL + SALBUTAMOL Increased adrenergic effects
chances of raised blood pressure & HR
• DOSE:
a. FOR REVERSIBLE BRONCHOSPASM:
- 20 mg PO three/four times daily
15. Beta-agonist bronchodilator, used in asthma treatment for reversal of acute
bronchospasm, & also as maintenance medication to prevent future attacks.
DOSE:
For Asthma Maintenance :
- 1-2 actuations q4-6hr PRN; not to exceed 12 actuations/day
16. Non-selective beta-adrenergic receptor agonist
Also known as ISOPRENALINE
Used in management of shock, heart block/cardiac arrest & bronchospasm
DOSE:
a. For Bronchospasm during anesthesia:
0.01-0.02 mg IV, repeat PRN
17. Resorcinol , is a SABA, used as bronchodilator
DOSE:
a. For Bronchospasm:
i. As PO:
Initiate at 2.5 mg three/four times daily PO
Maintenance: 5 mg three times daily PO q6hr while patient is awake; reduce dose to 2.5 mg q6hr
Not to exceed 15 mg/day
ii. As s.c:
0.25 mg q15-30min x 3 doses PRN in lateral deltoid
Not to exceed 0.5 mg/4 hr
19. - The long-acting bronchodilators are used to provide control ( NOT QUICK
RELIEF ) of asthma.
- They should only be used in conjunction with INHALED STEROIDS for long-
term control of asthma symptoms.
- Used twice a day.
- Long-acting beta-agonist bronchodilators increase the risk of death from asthma
and should only be used as additional treatment for people who are also using an
inhaled steroid.
20. Examples of LABA include:
1. Formoterol
2. Arformoterol
3. Salmeterol
4. Indacaterol
5. Vilanterol
6. Olodaterol .
21. Inhaled LABA, used in the management of asthma, COPD & exercise-induced
bronchospasm.
DRUG INTERACTION:
a. Formoterol + CPZ Prolongation of QTc interval
b. Formoterol + Amiodarone/Dronedarone Prolongation of QTc interval
• DOSE:
a. 20 mcg, inhaled via nebulizer, q12hr(For long-term maintenance treatment of
COPD)
22. R-enantiomer of formoterol
Potent, highly specific, nebulized, LABA
Approved by US-FDA for long-term maintenance treatment of
bronchoconstriction in patients with COPD
DRUG INTERACTION:
a. Arformoterol + Linezolid increased effects of former, by pharmacodynamic
synergism high risk of acute hypertensive episode
• DOSE:
- 15 mcg inhaled via nebulization twice daily (AM & PM)
- Not to exceed 30 mcg/day
23. Inhalational LABA
Can be used in combination with FLUTICASONE
DRUG INTERACTION:
a. Salmeterol + indinavir increased levels of salmeterol increased toxicity.
DOSES:
a. For asthma prevention & maintenance:
- 1 inhalation (50 mcg) twice daily; not to exceed twice daily administration
b. For COPD maintenance:
- 1 inhalation (50 mcg) twice daily; not to exceed twice daily administration.
24. - LABA, used in COPD as bronchodilator
- Can also be used in combination with GLYCOPYRROLATE(Utibron Neohaler)
- ADRs:
a. Post-inhalational cough(>10%)
b. Nasopharyngitis (6.5%)
c. Headache (5.1%).
- DRUG INTERACTION:
a. Indacaterol + Umeclidinium bromide / Vilanterol increased toxicity of each
other increased HR & B.P
25. DOSE:
IN COPD:
- Long-acting beta2-agonist indicated for long-term, once-daily maintenance
bronchodilator treatment of airflow obstruction in patients with chronic
obstructive pulmonary disease (COPD), including chronic bronchitis and/or
emphysema
- 75 mcg inhaled orally qDay; not to exceed once daily
- Limitations of use:
1. Not indicated for acute deteriorations of COPD
1. Not indicated for asthma
26. Selective LABA, with inherent 24-hour activity for once-daily asthma treatment
Used in combination as:
a. Vilanterol + Fluticasone propionate
b. Vilanterol + Fluticasone + Umeclidinium bromide
• ADRs:
a. Nasopharyngitis (9%)
b. URTI (7%)
c. Anticholinergic effects (with umeclidinium)
d. Headache (7%)
e. Oropharyngeal candidiasis(6%)
27. DOSE:
a. With FLUTICASONE:
- For COPD: 25 mcg/100 mcg (1 actuation), inhaled PO qDay
- For asthma : (25 mcg/100 mcg or 25 mcg/200 mcg per actuation) once daily via
oral inhalation
b. WITH UMECLIDINIUM BROMIDE:
- For COPD: 62.5 mcg/25 mcg (1 actuation), inhaled PO qDay
c. VILANTEROL + FLUTICASONE + UMECLIDINIUM COMBINATION:
- For COPD: 1 inhalation PO qDay(100 mcg/62.5 mcg/25 mcg).
28. LABA, that activates specific BETA-2-ADRENERGIC receptors on the surface of
smooth muscle cells, increasing the levels of intracellular CYCLIC-AMP, thereby
causing smooth muscle relaxation.
Has been reported to cause nasopharyngitis more compared to other LABAs
DRUG INTERACTIONS:
a. Olodaterol + Amitriptyline prolongation of QTc interval increased risk of
ventricular arrhythmias
• Indicated for maintenance bronchodilator treatment in patients with
COPD(including chronic bronchitis &/ emphysema), with airflow obstruction
• DOSE:
- 5 mcg(2 actuations), inhaled PO, qDay, at the same time of the day
- Not to exceed 2 inhalations every 24 hours.