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‘‘Salbutamol’’
Direct/Short-Acting,
Selective Beta2-Adrenergic
Receptor Agonist
Adrenergic
Receptor
Agonists
Alpha
Adrenergic
Agonists
Selective
Selective
Alpha 1
Selective
Alpha 2
Non-Selective
Beta
Adrenergic
Agonists
Selective
Selective
Beta 1
Selective
Beta 2
Non-
Selective
Short
Acting
Symptomatic
Use
Salbutamol
Metaproterenol
Terbutaline
Long Acting
Prophylactic
Use
Salmeterol
Formoterol
Selective Beta 2-Adrenergic Receptor
Agonists:
INTRODUCTION
(selective beta 2 agonist : duration 3-5hrs)
It belongs to
adrenergic
class
Beta 2
agonist
Causes
bronchodilation
Mechanism of
Action
• Act directly on B2-receptors that are
located on:
o Peripheral Blood Vessels,
o Bronchi,
o GIT,
o Skeletal Muscle,
o Liver,
o Mast cell.
1
Actions
• Activation results in:
o Bronchodilation,
o Relaxation of the GIT,
o Glycogenolysis in the liver,
o Inhibition of histamine release from mast cells.
Indications
• Bronchial Asthma
• Bronchospasm
• COPD
•Pre-mature Labor
In Sports, used by
runners, cyclists,
swimmers, etc. to
increase oxygen
uptake and cardiac
function.
Dosage Forms
Oral (tablets, syrup)
Inhalational/Nebulizer
Intravenous
a
Pharmacokinetics
Onset of Action
Oral: 20 min;
Inhalation: 5-15 min.
IV: Immediate Onset
Duration
Oral: 8 hr;
Inhalation: 3-6 hr;
Modified-release
preparation: 12 hr.
Plasma Half life:
3 to 5 hours
Absorption:
Readily absorbed from the GI tract.
Metabolism
Hepatic and in the gut wall.
Excretion
Via the urine as metabolites and unchanged
drug.
Some excretion in the faeces.
Dose
 Oral; 2,4 mg tablets ( 3-4 PRN)
; 2mg/5ml syrup
 Inhalant; Inhaler formulation (it uses spacer devices(which
improves drug delivery) 200-400 mg 4 times a day
 IV infusion; 3-20 mcg/min
 Subcutaneous; 500 mcg (repeated over 4 hrs if necessary)
[Reduced doses for pediatrics]
Generic Name: Albuterol / Salbutamol
Brand Names:
o Ventolin®,
o Proventil®,
o Proventil HFA®,
oNovo-Salbutamol®.
a Side
Effects
Common (1 in 100 people)
Shaking, usually of the hands (tremor).
Headache.
Faster than normal heartbeat (tachycardia).
Uncommon (1 in 1000 people)
Heart palpitations
Muscle cramps
Mouth and throat irritation
Rare (1 in 10,000 people)
Low level of potassium in your blood (Hypokalemia).
Very rare (1 in 10,000 people)
Irregular heartbeat (Arrhythmia).
Unexpected narrowing of the airways (Paradoxical
Bronchospasm).
Contraindications
Contraindications
Hypersensitivity to the active substance salbutamol or to the
excipients.
Although some forms of salbutamol sulphate have been used in
the management of premature labor, Salbutamol Nebuliser
Solution should not be used for this purpose.
DRUG INTERACTIONS
 Salbutamol will enhance the activity of other β2 sympathomimetics.
 β receptor blocking agents such as propranolol inhibit the activity of
salbutamol.
 The effects of salbutamol may be enhanced by concomitant administration
of aminophylline or other xanthines.
 Corticosteroids may increase the risk of hyperglycaemia.
Over Dose
Over Dose
• Tachycardia,
• Arrhythmia,
• Restlessness,
• Chest pain
• Vigorous tremor,
• Hyperglycemia
• Increased systolic BP
• Decreased diastolic BP
• Psychotic reactions
INTERVENTIONS &
ASSESMENTS
 Monitor potassium levels to detect possible hypokalemia.
 Monitor blood glucose levels to detect possible
hyperglycaemia.
Pregnancy and Lactation
Pregnancy Category : C
Lactation: Considered only when benefits over
weigh risks.
Patient Care Considerations
 Administration / storage.
 Patients with severe attack of asthma should have oxygen.
 Inform the patient that Albuterol may cause an unusual
dryness or bad taste.
 Dose and frequency of inhalation adjustment.
 Warn about over dependence.
Wisdom words
Selective Beta2 Agonist Salbutamol

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Selective Beta2 Agonist Salbutamol