pharmacology Flashcards
How many muscarinic receptors
5
Where are M1
Ganglia
What do M1 do
Facilitate ACh transmission
What do M2 do
Inhibitory
What does stimulation of vagus nerve cause
Bronchoconstriction
What do NANC do
Regulates the airways
What do NANC release
Bronchodilators
- VIP
- NO
Sympathetic innervate the airways
true or false
False
They innervate submucosal glands
What do b agonist do
Relax bronchial smooth muscle
What does irritation of C fibers cause
- cough
- mucus
What does parasympathetic work through
M3
What do amiodarone and methotrexate do to the lung
Damage it
What does heart failure lead to
Pulmonary oedema
What is commonest disease in children
Asthma
What is asthma
Recurrent reversible obstructive disease in response to irritant stimuli
What does asthma cause
Wheeze
Is COPD reversible
No
Symptoms of asthma
- wheeze
- SOB
Underlying pathology of asthma
Chronic asthma
- inflammation
- bronchial hyper-reactivity
- reversible obstruction
What is bronchial hyper-reactivity
Abnormal sensitivity to a wide range of stimuli
What are the phases of asthma
- immediate
- delayed
What does Th2 do In asthma
- attracts eosinophils
- IL-5 attracts eosinophils
- eosinophils attract CySTL1 receptors
- promote IgE
What does IL-4 and IL-13 do
Switch B cells to IgE
What is omalizumab
Anti IgE antibody
What does allergen interaction with IgE cause release of
- histamine
- leukotriene
- prostaglandin
What can delayed phase cause
Nocturnal asthma
What does Th0 give rise to
Th1 and Th2
What do glucocorticoid do
Inhibit action of IL-4 …
What are type of asthmatic drugs
- bronchodilators
- anti-inflammatory agents
How is asthma treatment monitored
FEV1
What drug can precipitate asthma
NSAID (aspirin)
What do bronchodilators reverse
Bronchospasm
SABA example
Salbutamol
When is glucocorticoid added
When SABA used more than 3 times a week
What is step 3
Add LABA to glucocorticoid
Example of LABA
Salmeterol
Leukotriene example
Monteleukast
What is oral glucocorticoid
Prednisone
How are B2 adrenoreceptor agonist administered
Inhaled
Example of methylxanthine
Aminophylline
What do methylxanthine
Inhibits PDE4
How is methylxanthine given
IV or oral as add on therapy
How is methylxanthine metabolized
In liver by P450
Example of leukotriene
Montelukast
How is leukotriene given
Add on therapy
Side effect of SABA
- tremor
- tachycardia
What does theophylline activate
Histone deacetylase (HDAC)
Side effect of methylxanthine
- arrhythmia
- seizure
Example of SAMA
Ipratropium
Example of LAMA
Tiotropium
What limits side effects in muscarinic antagonist
Quaternary ammonium group
What is LAMA selective for
M3
What is LAMA used with for COPD
LABA
What is the role of glucocorticoids
Anti-inflammatory
What does IL-3 do
Regulate mast cell production
Example of glucocorticoid
- beclometasone
- fluticasone
When are oral glucocorticoid given
Severe disease
Side effect of glucocorticoid
- thrush (oral candidiasis)
- sore throat
- hoarse voice
What is cromoglicate
Mast cell stabilizer
What does cromoglicate prevent
Histamine release from mast cells
What is mepolizumab
IL-5 inhibitor
Treatment of severe acute asthma
- O2
- inhaled SABA + ipatropium
= IV hydrocortisone - oral prednisolone
- IV magnesium
Treatment of IPF
- pirfenidone
- nintedanib
What is pirfenidone
Immunosuppressant that reduces fibroblast proliferation
What is nintedanib
Tyrosine kinase inhibitor
what are the 4 stages of drug disposition
ADME
- absorption
- distribution
- metabolism
- excretion
what does rate of diffusion depend on
- molecular size
- diffusion coefficient
what size of molecule diffuses more easily
smaller
what are pericytes
impermeable layer of periendothelial cells
where can cells not go
- across BBB
- across placenta (to foetus)
what are the 4 ways small molecules can cross cell membrane
- diffusion through lipid
- combination with solute carrier
- diffusion through aquaporins
- pinocytosis
can polar or non-polar diffuse easily across the membrane
non-polar
what are most drugs strong or weak acids and bases
weak acids or bases
what is used to calculate dissociation constant (pKa)
Henderson-Hasselbach equation
does the ionised or unionised form cross the membrane
unionised
what drugs are lipid soluble
- antibiotics
- aminoglycoside
example of weak acid
aspirin
example of weak base drug
pethidine
can ionised species cross the cell membrane
no
does ionised species travel equally to all compartments
no
what increases surface area in small intestine
villi and microvilli
how do drugs mainly exist
in bound form
what is most important protein drugs are bound to
albumin
example of drugs bound to albumin
- acidic drugs (warfarin, NSAID)
- basic drugs (antidepressants)
what are the 3 factors that determine the amount of drug bound to a protein
- concentration of free drug
- affinity for binding site
- concentration of protein
how many sites is there on albumin
2
what does albumin mainly bind
acidic drugs
what drug can be absorbed in the mouth
GTN
how do most drugs leave the body
urine
where are drugs metabolised
liver
what is used in drug metabolism
CYP450
what are xenobiotics
foreign chemicals
how many phases of drug metabolism
2
what is phase 1
oxidation
reduction
hydrolysis
is phase 1 catabolic or anabolic
catabolic
in phase 1 does it make drugs more or less active
more
where are CYP enzymes
in smooth endoplasmic reticulum
what are CYP450
haemorrhoids proteins
what are the most important CYP enzymes
1-3
can grapefruit juice inhibit drug metabolism
yes
affect of Brussel sprouts and cigarette smoke on P450 enzymes
induce them
how is ethanol metabolised
alcohol dehydrogenase
is phase 2 catabolic or anabolic
anabolic
what happens in phase 2
conjugation
does phase 2 make them more active or inactive
inactive
where does phase 2 occur
liver
