Pcol 2 exam 5 leukotrine, antihistamines, drugs for emesis, Flashcards
Xolair
Monoclonal antibody against IGE
it will prevent IGE molecules from binding to the mast cells so prevent IGE from sensitizing the mast cells
Cromolyn (Intal)
Nedocromil
Mast cell stabalizers Cro- or -cro-
MOA:
-They will bind to the mast cell and stabilize it.
-The IGE is still able to bind and the allergen is still able to bind and cross link . But there is reduce release of inflammatory mediators because the mast cells are stabaliaze
Montelukast (S-)
Zafirlukast (A-)
Montelukast (Singulair)
Zafirlukast (Accolate)
Leukotriene receptor antagonist (-lukast)
MOA:
-They will block the cysteinyl leukotriene receptor on the bronchial smooth muscle so block Leukotriene C4,D4,E4 from binding–> therefore reduces the bronchioconstriction
Thera:
-For allergy and for asthma associated with allergy
AE:
-HA
-Increase incidence of upper respiratory infections
-Suicide thoughts –> montelukast (singulair)
Zileuton (Zy-)
5-lipooxygenase inhibitor
MOA:
-inhibits 5-lipooxygenase so no conversion of arachidonic acid into leukotriene.
-But 5-lipooxygenase is very polymorphic and the levels vary in between pt so some pt will not respond well because they are not wild type
AE:
-significant diarrhea
Zyflo
Diphenhydramine
First gen antihistamine
-First gen is more lipophilic can cross the BBB and block H1 in the CNS –> get sedation and gain weight
Aromatic rings - spacer- 3 nitrogen –> same feature as anticholinergic so they can block muscarinic receptors and get drying effect:
Drying effect: reduce secretion in nose, airway, eye
MOA:
-bind reversible to the H1 receptor and will block histamine from binding.
-Reduces the histamine effects
-poor selectivity can block H1, a1 and muscarinic
-Thera:
-pt should take it chronically because if they take it when they have the symptoms it wont block.
Aromatic rings - spacer- 3 nitrogen –> same feature as anticholinergic so they can block muscarinic receptors and get drying effect:
Drying effect: reduce secretion in nose, airway, eye
-Blocking muscarinic receptor in the ear can treat motion sickness
AE:
-sedation, gain weight –> block H1 in CNS
-Constipation, tachycardia, mydriasis-_. block muscarinic
Benadryl
Clemastine
tra-
Clemastine (travist)
1st gen antihistamine H1 receptor antagonist
MOA:
-reversible block H1 receptors and prevents histamine from binding so reduces the effects of histamine in the
bronchial smooth muscle ,–> so reduces bronchioconstriction
large blood vessel, –> reduces vasodilation reduces risk of shock
nerve endings –> reduces itching
-Pt need to take it chronically because if they take it when they ge the symptoms it wont work
-aromatic ring - spacer - 3 amine –> same feature of anticholinergic so they can block muscarinic receptors and get the drying effect:
-Reduces secretion in airway, nose, eye–> beneficial in treating hypersensitive rxn
-they are very lipophilic and can cross the BBB and get to the CNS and block H1 receptors in the CNS so get sedation, gain weight
AE:
-sedation, gain weight
-Constipation, xerostomia, tachycardia, mydriasis
Travist
Dimenhydramine
Drama-
H1 receptor antagonist
1st gen
MOA:
-reversible block H1 receptor and reduces the effect of histamine
-But can cross BBB and block H1 in the CNS -_> get sedation, gain weight
-Can block muscarinic receptor –> good for drying effect –> decrease secretion in eyes, airway, nose
-Can block A1
Thera:
-pt need to take it chronically
-Can also treat motion sickness by blocking muscarinic in the ear
AE:
-xerostomia, constipation, mydriasis, tachycardia –> block musca
-Sedation, gain weight –> block H1 in CNS
dramamine
Chlorpheniramine
Chlor-tri
H1 receptor antagonist
-1st generation
MOA:
-Reversible blocks H1 receptor and reduces the histamine effects
-But can block muscarinic receptors —> get drying effect is good in hypersensitive rxn –> reduce mucus in nose, airway, eye
-has less sedative effect but still high anticholinergic
-pt need to take it chronically because if they take it when they have symptoms it wont work
Chlor-trimeton
Bromopheniramine
H1 receptor antagonist
First gen
MOA:
-reversible blocks H1 receptor so reduces the activity of histamine
-Can block muscarinic receptors so get dryging effect
-has less sedative effect
AE:
-xerostomia, tachycardia, constipation, mydriasis
-gain weight, some sedation
Hydroxyzine
atarax-, virsta-
Hydroxyzine (atarax, vistaril)
First gen antihistamine
MOA:
-Reversible H1 receptor antagonist. It will block H1 receptor and reduces the histamine effects .
Pt should take it chronically because if take it when they have symptoms –> it wont work
-Can also block muscarinic receptors -_> get dryng effect of decrease secretion in the nose, airway and eye
AE:
-Sedation, gain weight –> can cross BBB and block H1 in CNS
-Xerostomia, tachycardia, mydriasis –> block muscarinic
Atarax, vistaril
Ceclizine
1st gen antihistamine
reversible block H1 receptors
Meclizine
antiv-
Meclizine (antivert)
1st gen antihistamine
MOA:
-Reversible block H1 receptors –> so reduces the effect of histamine
-Pt need to take it chronically because if they take it when they have the symptoms –> it wont work
-Can block muscarinic receptors –> drying effect –> decrease secretion in nose, eye and airway –> good during hypersensitive rxn
AE:
-Sedation, gain weight
-Xerostiomia, mydriasis, tachycardia
Promethazine
phene-
Promethazine (Phenergan)
Reversible H1 receptor blocker
Reduces the effect of histamine
-has severe anticholenergic effects and can cross the BBB and block H1 and causes severe sedation
-Use as antiemtici –> treat motion sickness
Cyproheptadine
First gen antihistamine
Reversible H1 receptor antagonist
Doxepin
Sile-
TCA
-can use topically use as antihistamine to treat itching
Itching is due to activation of H1 receptors in the nerve endings
Silenor
Loratidine
Second gen antihistamine
MOA:
-reversible blocks H1 receptor
-Is more selective, cannot cross BBB because is amphotetic molecule so no sedation no gain weight
Thera:
-for allergies, need to take it chronically because if take it when have symptoms it wont work
Claritin
Desloratadine
Clari
Desloratadine (Clarinex)
Second gen antihistamine
MOA:
-Reversible blocks H1 receptor and reduces the activity of histamine
-Is more hydrophilic and does not cross the BBB so no sedation no gain weight
-Has more selectivity so wont block muscarinic receptors –> ni drying effect
Thera:
-Need to take it chronically for allergy and cannot wait until the symptoms start because it wont work
Clarinex
Cetrizine
Zyr-
Second generation antihistamine
MOA:
-Reversible blocks H1 receptor and will prevent histamine from binding. decreases histamine activity
-is more selective, doesnt cross BBB so no sedation
-no anticholinergic
-no dry effect
-pt need to take it chronically
Zyrtec
Azelastine
Aste-
Second generationa antihistamine
MOA:
-reversible blocks H1 receptor so decreases histamine activity because histamine wont be able to bind
-More selective
-doesnt cross BBB - so no sedation no gain weight
-Doesnt block muscarinic receptors-so no drying effect
Astelin
Fexofenadine
alle-
Second gen antihistamine
allegra
