Salbutamol

Presented By: Ameer hamza shaheedBPD-01093126

Submitted to: Sir Irfan

Clinical pharmacology

SalbutamolDrug name (generic):

SalbutabolTherapeutic class:

Bronchodilator Agent Adrenergic beta-Agonists Tocolytic agent

Pharmacological class: Sympathomimetic (beta2-adrenergic agonist)

Chemical name (IUPAC):

4-[2-(tert-butylamino)-1-hydroxyethyl]-2-(hydroxymethyl)phenol

Chemical structure:

Empirical formula:

C13H21NO3

Pregnancy category: C

Physical properties:

Odour : Odourless

Solubilty: Sparingly soluble in water; soluble in ethanol (96%); slightly soluble in ether.

Colour: A white or almost white, crystalline powder

Pharmacodynamic

Salbutamol is a short-acting, selective beta2-adrenergic receptor agonist used in the treatment of asthma and COPD.

Salbutamol is formulated as a racemic mixture of the R- and S-isomers.

S-isomer:

R-isomer:

Mechanism of Action

Salbutamol is a beta(2)-adrenergic agonist and thus it stimulates beta(2)-adrenergic receptors.

Salbutamol increases cAMP production by activating adenylate cyclase.

Increased intracellular cyclic AMP increases the activity of cAMP-dependent protein kinase A, which inhibits the phosphorylation of myosin and lowers intracellular calcium concentrations.

Mechanism of Action

A lowered intracellular calcium concentration leads to a smooth muscle relaxation and bronchodilation.

Increased cyclic AMP concentrations are also inhibits the release of bronchoconstrictor mediators such as histamine, leukotreine from the mast cells in the airway.

Pharmacokinetics

Pharmacokinetics Bioavailability :oral bioavailability 50%Half life : half life is 4 hours (Taken from rang & dell page 168)

Onset of Action:oral: 30 minutes, Inhalation : 5-15 minutes

Duration of action :

8 to 12 hours(page 361 R&D)

Metabolism : It is subject to first pass metabolism in the liver

Pharmacokinetics

Exretion : Readily excreated in the urine as metabolite and unchanged drug Some excreate in faeces.

Reference Martindale 35th edition page 1016

Clinical uses and Side Effects

f55555555555555555fffffffffffffffffffffff1fffffffffff5Female reproductive

system Relaxation of uterus (during pregnancy)

Reference From nurses drug hand book page 37

Drug Intrections

Contraindication& precaution

Doses

Acute bronchospasm:1 or 2 inhalation of salbutamol i.e 100 microgram 3 or 4 time dailySevere attack of bronchospasm:250 microgram i.v insolution form 10 microgram/mlPremature labour.I.V infusion 200 microgram with 5% gluse used for dilution.

Products for Salbutamol available in market

Brand name Manufacturer Name

Dosage Forms

Ventoline GSK Injection: 0.5 mg Syrupe: 60 mlTablet : 8 mg

Respoline Munawar pharma Tablet : 2 mg

Aeroline Ankaz Syrupe : 60 , 450 MLTablet : 2 , 4 MG

Salbutamol Nawab sons Syrupe : 60 ML

Asmatol Siza Injection : 0.5 MGTablets : 4 MG

Ventomol Venus Tablets : 2 & 3 MG

Reference

Taken from martindale 35th edition page 1016

Reference Pharmaguid page # 1159

Thank you