Pharmacology Flashcards
epinephrine
B > alpha agonist
ephedrine
indirect adrenergic agonist, release stored catecholamines (stimulate B for lung effects)
isoproterenol
B1 and B2 agonist
albuterol
B2 agonist
short acting
terbutaline
B2 agonist
short acting
salmeterol
B2 agonist
long acting
used with steroids
formeterol
B2 agonist
long acting
used with steroids
atropine
M antagonist
Tx: asthma/COPD
ipratropium
M antagonist
poorly absorbed with no significant systemic effects
Tx: COPD
tiotropium
M antagonist
long acting
poorly absorbed with no significant systemic effects
Tx: COPD
Umeclidinium
M3 antagonist
Tx: COPD
theophylline
methylxanthine
aminophylline
methylxanthine
cromolyn sodium
Mast cell stabilizer: inhibits mast cell degranulation
alter chloride channel activity, inhibit eosinophilic inflammatory response, inhibit cough, reduces bronchial hyperactivity
AE: (no systemic toxicity) tracheal irritation (cough, bronchospasm), bad taste
RARE: chest pain, restlessness, hypotension, arrhythmia, N/V, CNS depression, seizure, anorexia
PROPHYLAXIS: asthma/COPD
methylxanthines
related to CAFFEINE
PDE inhibition (decrease cAMP degradation)
adenosine antagonist (strengthens diaphragm, inhibits bronchoconstriction)
decrease release of histamine
AE:
5-10 ug/mL serum: N/V, nervous, headache, insomnia
>20 ug/mL: vomit, HYPOKALEMIA, hyperglycemia, tachycardia, arrhythmia, tremor, neuromuscular irritability, seizures
Tx: asthma/COPD
CI: caffeine, CV
B agonist
bronchodilator: increase cAMP
inhibitory effect on release of mediators from mast cell, inhibit microvascular permeability, stimulate mucociliary clearance
Tx: asthma/COPD
AE: N/V, headache
decrease BP, increase HR and cardiac arrhythmias, HYPOKALEMIA-QT prolongation, PaO2 decrease, CNS toxic effects (agitation, convulsions, coma, respiratory and vasomotor collapse), HYPERGLYCEMIA
M antagonist
reduces bronchoconstriction, decreases mucus, enhances B2 bronchodilation
AE: pupillary dilation, cycloplegia
budesonide
corticosteroid
give with FORMOTEROL
fluticasone
corticosteroid
give with SALMETEROL
mometasone
corticosteroid
beclomethasone
corticosteroid
ciclesonide
corticosteroid
oral inhalation
prodrug of des-ciclesonide
prednisone
corticosteroid
oral
prednisolone
corticosteroid
methyprednisolone
corticosteroid
dexamathasone
corticosteroid
oral or IV
corticosteroids
anti-inflammatory
MoA: decrease inflammatory cytokines (NFkB, HDAC2), reduce mucus secretion, reduces bronchial hyperactivity, enhance B2 agonist effect), reduce GATA into nucleus (suppress TH2 cell activity), inhibits PLA2
inhaled AE: oral candidiasis, hoarse, dry mouth, decrease growth (children), decrease bone density (premenopausal women)
oral AE: glucose intolerence, HTN, weight gain, bone demineralization, cataracts, immunosuppression, retarded growth (children), cushingoid syndrome
AE: HYPERGLYCEMIA
Tx: ASTHMA, wegners granulomatosis
not as much COPD
leukotriene receptor blocker
block LTD4: decrease bronchial reactivity and bronchoconstriction, decrease mucosal hyper secretion and mucosal edema, decrease inflammation
AE: GI
PROPHYLAXIS: asthma/COPD
monteleukast
leukotriene receptor blocker
AE: laryngitis, pharyngitis, nausea, otitis, sinusitis, viral infections
CI: possible suicide ideation
zafirlukast
leukotriene receptor blocker
AE: headache, elevated liver enzymes
zileuton
leukotriene synthesis inhibitor (LTB4, LTC4, LTD4, LTE4): decrease sm. muscle contraction and vessel permeability, reduce leukocyte migration
AE: elevated hepatic enzymes
CI: CYP1A2 (interacts with theophylline)
PROPHYLAXIS: asthma/COPD
omalizumab
anti-IgE Ab (use with steroid)
AE: allergic rxn, injection reaction, sore throat/cold sym.
CI: cardiac complications, avoid concurrent agents
Tx: asthma/COPD
B2 receptor
Gs
stimulate AC - cAMP - PKA - increase EPAC and decrease MLCK
first generation antihistamines
short lived
SEDATION
anticholinergic side effects: DON’T give to asthmatics (thickening/drying of mucosa)
mild effect of GI peristalsis
AE: serotonergic: increase appetite
adrenergic: hypotension, tachycardia
antimuscarinic: dry mouth, urinary retention, tachycardia, constipation, blurred vision
minor not clinically important: QT prolongation, ventricular arrhythmia
other AE: resp. distress, potentiation of nasal congestion
Tx: allergy, nausea, insomnia, allergic rhinitis
CI: MAOI, COPD, asthma, peptic ulcer, BPH
second generation antihistamines
longer action
no sedation or anticholinergic SE
Tx: urticaria, seasonal allergic rhinitis
diphenhydramine
1st gen: H1 antagonist
suppresses cough reflex by acting directly on cough center
Tx: cough, anaphylaxis, parkinsonism (not sure if just this one or all H1 antagonists)
HIGHLY sedating
dimenhydrinate
1st gen: H1 antagonist
Tx: anaphylaxis
HIGHLY sedating
clemastine
1st gen: H1 antagonist
HIGHLY sedating
chlorpheniramine
1st gen: H1 antagonist
brompheniramine
1st gen: H1 antagonist
Tx: urticaria
triprolidine
1st gen: H1 antagonist
promethazine
1st gen: H1 antagonist
AE: IV use gangrene, breathing problems in children
HIGHLY sedating
cyclizine
1st gen: H1 antagonist
meclizine
1st gen: H1 antagonist
hydroxyzine
1st gen: H1 antagonist
Tx: N/V, pruritis
tripelennamine
1st gen: H1 antagonist
loratadine
2nd gen: H1 antagonist
terfenadine
2nd gen: H1 antagonist
ANTIFUNGALS: fatal arrhythmia
astemizole
2nd gen: H1 antagonist ANTIFUNGALS: fatal arrhythmia
acrivastine
2nd gen: H1 antagonist
cetirizine
2nd gen: H1 antagonist
telemastine
2nd gen: H1 antagonist
3rd generation antihistamines
greater binding to H1
early gen drugs modified
non sedating, fewer antimuscarinic effects
Tx: allergic conjunctivitis, saesonal allergic rhinits
desloratadine
2nd gen H1 antagonist
long half life
olopatadine
3rd gen: H1 antagonist
inhibits histamine, PGD2, and tryptase release from mast cell
Tx: OCULAR rhinitis
levocabastine
3rd gen: H1 antagonist
most potent and specific
azelastine
3rd gen: H1 antagonist
inhibits histamine and leukotriene receptors
blocks Ca mobilization and 5-lipoxygenase pathway
inhibits PAF receptor
emedastine
3rd gen: H1 antagonist
asthmatic use
mizolastine
3rd gen: H1 antagonist
anti PAF and LTD4
ebastine
3rd gen: H1 antagonist
anti leukotriene and antibradykinin