Reading...
Play button
Play button
Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
69 Cards in this Set
- Front
- Back
|
spesific immunotherapy used in asthma
|
SCIT = subcutaneus immunotherapy
SLIT = sublingual immunotherapy |
|
|
group of drugs used in treatment of asthma
|
sympatomimetics
anticholinergics corticosteroides methylxantines antileukotriens antihistamines |
|
|
antiasthmatics with rapid effect
|
beta-mimetics
parasympatolyics |
|
|
asthma - nonselective beta-mimetics
|
adrenaline, isoproterenol, orciprenaline, ephedrine
|
|
|
asthma - selective beta-mimetics
|
metaproterenol, albuterol, salbutamol, terbutalin, fenoterol
|
|
|
asthma - parasympatolyics
|
ipratropium
|
|
|
most common short-actng beta agonist
|
albuterol
|
|
|
action of beta-mimetics
|
increase cAMP
|
|
|
beta2 mimetics with long term effect + their mode of application
|
salmeterol >> via inhalation
klenbuterol, prokaterol >> per os (table, sirup) formoterol |
|
|
rapid & short-term acting beta2-sympatomimetics (RABA)
1) onset of action: inhalation & p.o 2) duration of action 3) used in what treatment |
1) onset of action in 5-10 min (inhal.), 15-90 min (p.o.)
2) duration of action 4-6 hrs 3) acute treatment |
|
|
rapid & short-term acting beta2-sympatomimetics (RABA) - drugs
|
salbutamol /Ventolin/
fenoterol (Berotec) terbutalin (Bricanyl) |
|
|
Long-term acting beta2- sympatomimetics (LABA) - drugs
|
salmeterol /Serevent/
formoterol /Oxis/ procaterol /Lontermin/ klenbuterol |
|
|
Long-term acting beta2- sympatomimetics (LABA)
1) duration of action 2) commonly used in combination with 3) preferred route of apllication |
1) bronchodilation > 12 hrs
2) ICS (corticosteroids) 3) preference inhalation (20x higher effect that p.o) |
|
|
ADRs of beta2-mimetics (5)
|
1) muscle tremor (higher doses)
2) palpitation, tachycardia, arrhythmia, sudden death 3) headache 4) paradox bronchospasm (after inhalation) 5) rarely allergy |
|
|
action of beta-mimetics on smooth muscle receptors
|
bronchodilation
|
|
|
action of beta-mimetics on other receptors (epithelium, masticates etc)
|
1) mastocytes stabilization
2) inhibition of release mediators from eo, macro, T-cells or neu 3) decreased plasma exsudation to airways |
|
|
corticosteroids used in treatment of asthma
|
beclometasone
budesonide flunisolide fluticasone triamcinolone |
|
|
corticosteroid used in treatment of asthma - their effect
|
- potent antiinflammatory effect
- decrease of number of inflammatory potent cells - inhibition of bronchoconstrictory mechanisms - direct relaxation of smooth muscle cells |
|
|
synergism of ICS and beta mimetics
|
CS recover bronchial responsivity to beta-2 mimetics
|
|
|
synergism of ICS and beta mimetics - mechanism
|
- increased affinity of agonists to receptors
- decreased degradation of receptors - decreased activity of COMT - decreased up-take of mediators to presynaptic button |
|
|
local ADRs of ICS
|
oropharyngel candidosis
dysphonia cough |
|
|
local ADRs of ICS - prevention
|
mouth washing after admin.
use of prodrugs (activation in lungs: ciclesonide >> C21-des-methylpropionyl-ciclesonide) |
|
|
frequently discussed systemic ADRs of ICSs
|
suprarenal supression
decreased BMD glaukoma & cataracta |
|
|
methylxantines - drugs
|
theophylline
aminophylline |
|
|
aminophylline =
|
theophylline + ethylendiaminde
|
|
|
action of methylxantines
|
- myotropic influence via inhibition of phosphodiesterase and via antagonism on the adenosine receptors A2
>> bronchodilatation >> prevention from bronchoconstriction caused by histamine, cholinergic agonists (metacholine) or exertion. |
|
|
aminoglutethimide =
|
inhibitor of GC synthesis
|
|
|
mifepristone =
|
clucocorticoid receptor antagonist
|
|
|
theophylline - synergism with ICS
|
both in vitro & in vivo higher activity of HDAC (histon deacetylases) in epit. cells & macrophages => higher eff. of ICS on genes with antiinflammatory properties
|
|
|
anticholinergics - drugs
|
ipratropium /Atrovent, in comb. with 2 mimet. Berodual/
tiotropium /Spiriva/ |
|
|
ipratropium /Atrovent, in comb. with 2 mimet. Berodual/
1) similar structure to 2) duration, onset 3) use |
1) similar structure to atropine
2) shorter eff. 4-8 hrs, rapid onset: 5‒15 min 3) for acute use with RABA for long-term therapy with LABA |
|
|
tiotropium /Spiriva/
1) duration, onset 2) use |
1) longer eff. up to 48 hrs, slower onset
2) for long-term therapy of BA or COPD |
|
|
cromones - drugs
|
cromoglycate sodium
nedocromil |
|
|
cromoglycate sodium
1) action 2) reached full effect |
1) inhibition of degranulation of mastocytes after exposition to specific agents
2) full effect after 4-6 weeks |
|
|
nedocromil - action
|
similar to cromoglycate in mechanism of action: inhibition of degranulation of mastocytes after exposition to specific agents
|
|
|
antileukotriens & leukotriene receptor antagonistis (LTRAs)
|
zafirlukast
montelukast zileuton |
|
|
zileuton - action
|
inhib. of 5-lipooxygenase
|
|
|
location of histamine receptors H1
|
smooth muscles, endothelium, dendritic cells, neu, mono, eo,
T a B ly, hepato, chondrocytes, CNS |
|
|
location of histamine receptors H2
|
gastric parietal cells, myocardium, uterus, CNS
|
|
|
location of histamine receptors H3
|
CNS, airways, GIT
|
|
|
location of histamine receptors H4
|
mast cells
|
|
|
antihistamines - 1st generation - features
|
- = sedative antihistamines
- inverse agonists of H1 receptor - low selectivity = influence of other receptors - short interaction with the receptor => a need of more frequent administration (b.i.d. or t.i.d.) |
|
|
antihistamines - 1st generation - common ADRs (5)
|
(1) antimuscarine eff.
(2) arrhythmia (3) sedation (cross via HEB) (4) potentiation of alcohol (5) adrenolytic & antiserotonergic eff. |
|
|
antihistamines - 1st generation - topical drugs
|
Bisulepine
Bilastine Dimetinden Clemastine Promethazin Ketotifen |
|
|
antihistamines - 1st generation - oral drugs
|
Dimetinden
Ketotifen |
|
|
antihistamines - 1st generation - parenteral drugs
|
Bisulepin
Promethazin Clemastin |
|
|
antihistamines - 1st generation - combined preparations: local
|
Spersallerg – eye
Sanorin-Analergin – eye, nose Vibrocil – nose |
|
|
antihistamines 2nd generations - compared to 1st generation
|
higher selectivity = better safety profile
|
|
|
antihistamines 2nd generations - substances for systemic administration
|
acrivastine, cetirizine, loratadine, mizolastine
|
|
|
antihistamines 2nd generations - substances for local administration
|
azelastine, emedastine, epinastine, levocabastine, olopatadine
|
|
|
antihistamines 3nd generations - for systemic administration
|
levocetirizine, desloratadine, fexofenadine
|
|
|
antihistamines 3nd generations
1) types 2) features |
1) = active enantiomers (levocetirizine) or metabolites (desloratadine or fexofenadine)
2) higher selectivity => better tolerability & safety profile |
|
|
inhibitors of calcium channels used in treatment of asthma
|
verapamile
nifedipine |
|
|
asthma vs glaucoma - drugs of choice
|
in glaucoma – BB = drug of choice (CI: in AB)
in AB – CS = drug of choice (CI: in glaucoma) |
|
|
„ULABA“
|
ultra-long acting beta-2 agonists“ - arformoterol, carmoterol, indacaterol, GSK-159797 …in clinical praxis from 2010 for AB & COPD (once daily)
|
|
|
omalizumab
|
anti IgE – effective in all. rhinitis as well
|
|
|
bimosiamos
|
inhalatory pan-selectine anta => inhibition of rolling & extravasation of infl. cells
|
|
|
antitussics - classes (5)
|
1) peripheral sensors inhibition
2) afferent signals modulation 3) cough centre inhibition 4) efferent signals modulation 5) effector modulation |
|
|
antitussics - peripheral sensors inhibition
|
benzonatate, dropropizine
|
|
|
antitussics - afferent signals modulation
|
prenoxdiazine
|
|
|
antitussics - cough centre inhibition
|
- a) opioid – codein, dextromethorphan
- b) non-opioid - butamirate, pipazetate - clobutinol – RC stimulation + cough centre inhibition |
|
|
antitussics - efferent signals modulation
|
myorelaxants
|
|
|
antitussics - effector modulation
|
penthoxyverine - bronchodilation
|
|
|
expectorants - classes (3)
|
1) secretolytics
2) mucolytics 3) secretomotorics |
|
|
expectorants - secretolytics
|
saponines & alcaloids - ipekakuana, primula, NaI, KI, NH4Cl
|
|
|
expectorants - mucolytics
|
acetylcystein, carbocystein, mesna, bromhexin, ambroxol
|
|
|
expectorants - secretomotorics
|
plant etheric oils - ol. menthae piperitae
|
|
|
location of muscarininc receptors
|
M1: parasymp. ganglion, exocrine glands, CNS
M2: heart M3: smooth muscle cells of blood vessels, lungs >> - mediated increase in IC calcium & bronchoconstriction in lungs - trigger release of NO in vessels >> dilation |
|
|
tiotropium
|
Tiotropium is a muscarinic receptor antagonist, often referred to as an antimuscarinic or anticholinergic agent. Although it does not display selectivity for specific muscarinic receptors, on topical application it acts mainly on M3 muscarinic receptors[6] located on smooth muscle cells and submucosal glands leading to a reduction in smooth muscle contraction and mucus secretion, thus producing a bronchodilatory effect
|
