Ventolin
Ventolin
PREGNANCY CLASS: C
CHEMICAL STRUCTURE:
MECHANISM OF ACTION:
Salbutamol is a selective B2 adrenoceptor agonist. At therapeutic doses it
acts on the B2 adrenoceptors of bronchial muscle, with little or no action on
the B1 adrenoceptors of cardiac muscle. It stimulates B2 receptors of
bronchioles by increasing levels of cAMP which relaxes smooth muscles to
produce bronchodilatation. Also causes CNS stimulation, cardiac stimulation,
increased diuresis, skeletal muscle tremors, and increased gastric acid
secretion.
Guaifenesin can make the viscous mucus of the respiratory pathway more
fluid and therefore expectoration and reduces cough.
PHARMACOKINETICS:
Absorption:
After oral administration, salbutamol is absorbed from the gastrointestinal
tract and undergoes considerable first-pass metabolism to the phenolic
sulfate (inactive 4-O-sulfate).
Guaifenesin is well-absorbed after oral administration. After the
administration of guaifenesin 600 mg in healthy adult volunteers the
maximum peak plasma concentration (Cmax) was approx 1.4 mcg/mL
with Tmax about 15 minutes after drug administration.
Distribution:
The bioavailability of orally administered salbutamol is about 50%.
Salbutamol is bound to plasma proteins to the extent of 10%.
Metabolism:
Salbutamol administered IV has a half-life (t1/2) of 4-6 hrs and is cleared
partly renally and partly by metabolism to the inactive 4'-O-sulfate
(phenolic sulfate) which is also excreted primarily in the urine.
Guaifenesin has a plasma t1/2 of approximately 1 hr and was not
detectable in the blood after 8 hrs. Guaifenesin appears to undergo both
oxidation and demethylation.
Elimination:
The majority of a dose of salbutamol given IV, orally or by inhalation is
excreted within 72 hrs primarily via urine. The feces are a minor route of
excretion.
Guaifenesin is excreted in urine.
INDICATIONS:
Relief of bronchospasm in bronchial asthma, chronic bronchitis, emphysema
and other reversible, obstructive pulmonary diseases. Also useful for treating
bronchospasm in patients with co-existing heart disease of hypertension.
DOSAGE AND ADMINISTRATION:
Capsule
Adults & Children over 12 years: 1-2 capsules two or three times a day.
Children 6-12 years: 1 capsule two or three times a day.
Below 6 years: Not recommended.
Syrup
Adults: 10 to 20mL of expectorant syrup (2-4 mg salbutamol) two or three
times a day.
Children: 2-6 years: 5 to 10mL of expectorant syrup (1-2 mg salbutamol)
two or three times daily.
7-12 years: 10mL of expectorant syrup (2 mg salbutamol) two or three
times daily.
Over 12 years: 10 to 20mL of expectorant syrup (2-4mg salbutamol) two
or three times daily.