Anti-Histamines and Prostaglandin/Leukotriene Agonist/Antagonist Flashcards
Classic antihistamines work by
H1 receptor antagonist
Classic antihistamines treat
seasonal allergies
Classic antihistamine side effects
sedation, local anesthetic action, anticholinergic activity, anti-motion sickness activity, can cause an allergic reaction in sunburned skin
classic antihistamine’s unique properties
increases effects of other sedatives ethanol and barbiturates
classical antihistamines are
Diphenhydramine (benadryl) and Chlorpheniramine
Diphenhydramine is an
ethanolamine
Chlorpheniramine is a
alkylamine
Fexofenadine (allegra) MOA
second gen H1 receptor antagonist
fexofenadine treats
seasonal allergies
fexofenadine side effects
less sedation inducing than benadryl
Cimetidine MOA
H2 receptor antagonist
cimetidine treats
peptic ulcer and heart burn (gastro-esophageal reflux disease (GERD))
cimetidine side effects
supra-high doses as in zollinger-elison will cause gynecormastia
cimetidine unique properties
P450 inhibitor
Famotidine MOA
H2 receptor antagonist
famotidine treats
peptic ulcer and GERD
famotidine side effects
don’t use in pts with renal failure, newer gen H2 blocker doesn’t have P450 interaction
Cromolyn sodium MOA
stabilizes mast cell plasma membrane, reduces calcium entry blocking histamine release
cromolyn sodium treats
anti-allergen prophylactic therapy
cromolyn side effects
side effects are rare, some pts may show hypersensitivity
cromolyn unique properties
prophylactic, must be used prior to allergen exposure
omalizumab MOA
blocks IgE binding to mast cells
omalizumab treatment
prophylactic treatment of asthma
omalizumab side effects
injection site reaction, viral infections, upper resp infections, sinusitis, headache, sore throat
synthetic Prostaglandin E1 drug is
Alprostadil
Alprostadil MOA
smooth muscle relaxation/vasodialation
Alprostadil treats
maintenance of dustus arteriosus patency and erectile dysfunction
alprostadil side effects
pain at injection sites, could cause hypotension but rare
misoprostol MOA
PGE1 analog, cytoprotective, activates apical
misoprostol treats
prevention of peptic ulcer disease, in combo with RU-486 terminate early pregnancies
misoprostol side effects
diarrhea, abdominal pain, uterine contraction, not for use in pregnant women
misoprostol unique properties
given with an NSAID for arthritis pain management.
Dinoprostone MOA
PGE2 analog
dinoprostone treats
induces labor
Lubiprostone MOA
activates apical type II Cl- channels; EP receptor independent action
Lubiprostone treats
treatment of chronic constipation and IBS
lubiprostone side effects
minimal: decreases gastric emptying, n/d. don’t use in pats with mechanic GI obstruction
lubiprostone unique properties
receptor independent action
Carboprost is a synthetic
15-methyl prostaglandin PGF2alpha
carboprost MOA
contracts uterus, decreases blood flow and bleeding
carboprost treats
induces labor or controls post partum hemorrhage
carboprost side effects
n/v/d, bronchoconstriction, may induce asthma attack
carboprost unique properties
administered intra-amniotically to avoid systemic effects and modification delays its metabolism
latanoprost is synthetic
stable analog PGF2alpha
latanoprost MOA
FP receptor agonist; promotes outflow of aqueous humor and lowers intraocular pressure
latanoprost treats
ophthalmic preparation, open angle glaucoma
latanoprost side effects
causes drying of eyes, conjuntivitis,
latanoprost unique properties
irreversible pigmentation of the iris and eyelashes
what drugs works similar to latanoprost
travoprost
synthetic PGI2 (prostacyclin) is
epoprostenol
Epoprostenol MOA
vascular smooth muscle relaxation via increased camp, IP3/calcium
epoprostenol treats
anti-thrombotic, vasodilator, anti-aggregatory, blocks plate activation, pulmonary and portopulmonary HTN
epoprostenol side effects
flushing, headache, hypotension, n/d
epoprostenol unique properties
product of COX-2, cox2 inhibition eliminates PGI2 while maintaining TXA2
Iloprost MOA
vasodilator; decreases pulmonary arterial pressure
Iloprost treats
pulmonary arterial hypertension
Iloprost side effects
flushing, headache, hypotension, n/d
Iloprost unique properties
used in primary or secondary pulmonary hypertension, delays or prevents need for lung/lung-heart transplantation
-lukast
CysLTR1 and CysLTR2 antagonist
-lukast MOA
relaxes bronchial smooth muscle in asthma; antagonizes LTC4, LTD4, LTE4
-lukast treats
mild asthma
-lukast drugs
Zafirlukast and Monelukast
Zafirlukast unique properties
P450 interaction; affects warfarin metabolism, can be used in children of 6yo and older
Montelukast unique properties
no P450, can be used in children 12yo and older
zileuton MOA
lipoxygenase (LOX) inhibitor; blocks leukotriene production reducing bronchoconstricition
Zileuton treats
asthma where interleukins contribute to symptoms
Zileuton side effects
increases serum levels of theophyline and warfarin, maybe hepatotoxic, not for children under 12