Salmeterol

Question 1

What are some other drugs in the same class as Salmeterol?

Answer 1

Salbutamol
Terbutaline (SABA)
Formoterol (LABA)

Question 2

What is salmeterol used for?

Answer 2

It is a bronchodilator for the long term regular treatment of asthma in adults and children receiving ICS or OCS

Question 3

What is the mechanism of action of Salmeterol?

Answer 3

Salmeterol is a selective LABA with a long side chain binding to the exo site of the receptor.
It stimulates adenyl cyclase causing an increase in intracellular cAMP levels.
This triggers bronchial smooth muscle relaxation.

Salmeterol also inhibits the release of mediators for immediate hypersensitivty.

Question 4

What are the main pharmacokinetic/pharmacodynamic characteristics regarding Salmeterol?

Answer 4

Effective within 10-20minutes
Lasts up to 12 hours
Extensively metabolised by CYP3A4
Mainly excreted in faeces
Elimination half life is 5.5 hours

Question 5

What are some precautions regarding salmeterol use?

Answer 5

DO NOT USE for patients with unstable or acutely deteriorating asthma
USE WITH CAUTION for patients with hyperthyroidism, CV disease, arrhythmias, hypertension, diabetes

May change in composition and production of breast milk.
May have potential risk when used during breastfeeding.

Question 6

What are the contraindications of salmeterol?

Answer 6

Hypersensitivity to any ingredient in the preparation

Use for asthma without long term asthma preventors

Question 7

What are some adverse effects associated with salmeterol?

Answer 7

Fine tremors, headache, muscle cramps, palpitation, peripheral vasodilation

High doses associated with hyperkalaemia

Question 8

What are some interactions regarding use of Salmeterol?

Answer 8

Ketoconazole and other CYP3A4 inhibitors can significantly increase plasma salmeterol concentrations, prolonging the QT interval

Avoid non selective and selective beta blockers in patients with reversible obstructive airways disease

Concurrent use with beta 2 agonists and MOAIs may increase risk of CVD adverse effects

Question 9

What are the alarm bells associated with Salmeterol use?

Answer 9

Must only be administered in combination with anti inflam. therapy (e.g. ICS) for treatment of asthma

Dosages and frequency of administration only to be adjusted based on medical advice

Monitor Potassium levels