Drugs

Question 1

Where are beta2- receptors found?

Answer 1

in smooth muscle of the bronchi, GI tract, uterus and blood vessels.

Question 2

How do beta2- agonists reduce breathlessness?

Answer 2

stimulation of beta2-receptor activates a signalling cascade (by increase in cAMP) that leads to smooth muscle relaxation –> improves airflow in contracted airways

Question 3

What type of receptor is a beta2-receptor

Answer 3

a G protein-coupled receptor

Question 4

name a short acting beta agonist

Answer 4

salbutamol, terbutaline

Question 5

name a long acting beta agonist

Answer 5

salmeterol, formoterol

Question 6

what makes a LABA long acting?

Answer 6

increased lipophilicity

Salmeterol is salbutamol with a long lipophilic chain attached to it

Question 7

where are beta-1-adrenoceptors found?

Answer 7

the heart

Question 8

where are beta-3 adrenoceptors found?

Answer 8

brown adipose tissue

Question 9

Side effects of beta-agonists

Answer 9

Common fight/flight adverse effects: tachycardia, palpitations, anxiety + tremor.

also promote glycogenolysis

? tolerance

Question 10

types of bronchodilators (3)

Answer 10

beta-agonists, muscarinic antagonists & methylxanthines

Question 11

Another name for muscarinic antagonists

Answer 11

antimuscarinics

Question 12

short acting muscarinic antagonist

Answer 12

ipratropium

Question 13

long acting muscarininc antagonist

Answer 13

tiotropium

Question 14

Mechanism of muscarinic antagonist for COPD

Answer 14

block ACh binding to muscarinic receptors (M3) –> blocks affects of ACh —> stopping excessive bronchocontriction

Question 15

At what step in chronic asthma treatment do you potentially use a long acting antimuscarinic?

Answer 15

step 4, in addition to a LABA and high-dose inhaled corticosteroid

Question 16

What do methylxanthines inhibit?

Answer 16

phosphodiesterase. Which is needed for the conversion of cAMP to 5’AMP.

So indirectly leads to elevations in cAMP –> increased smooth muscle relaxation

Question 17

What is theophylline?

Answer 17

a non-selective PDE inhibitor

Has wide ranging SEs: GI, CVS, CNS

Question 18

classes of steroid

Answer 18

sex (testes, ovaries)

corticosteroids (adrenal cortex)

Question 19

types of corticosteroid

Answer 19

mineralocorticoids: aldosterone - Na+ retention
glucocorticoids: hydrocortisone - metabolic, anti-inflammatory

Question 20

name some semi-synthetic glucocorticoids

Answer 20

prednisolone, budesoinde

Question 21

corticosteroid mechanism of action

Answer 21

pass through plasma membrane + interact with receptors in the cytoplasm.

activated receptor then passes into nucleus to modify transcription of a number of genes

pro-inflammatory cytokines, interleukins and chemokines are down regulated whilst anti-inflammatory proteins are up.

this reduces mucosal inflammation, widens the airways and reduces mucus secretion, improving symptoms and receding exacerbations in asthma & COPD

Question 22

AE’s of corticosteroids

Answer 22

immunosuppressive: oral candidiasis (thrush), hoarse voice, ?pneumonia in COPD
metabolic: osteoporosis + muscle wasting

Question 23

What does GRE stand for?

Answer 23

glucocorticosteroid response element

they can increase transcription (+GRE) or decrease it (-GRE)

Question 24

why are NSAIDs detrimental in asthma?

Answer 24

they inhibit COX, so there’s a build up of arachidonic acid, and then an increase in cos-leukotrines, which are very potent bronchoconstrictors!

Question 25

stage 1 - 4 of asthma management

Answer 25

1: SABA
2: SABA + ICS
3: SABA + ICS + LABA
4: add prednisolone? long acting antimuscarinic?

Question 26

How is COPD managed differently to asthma?

Answer 26

asthma = beta agonists + steroids
COPD = beta agonists/muscarinic antagonists + steroids