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44 Cards in this Set

  • Front
  • Back
What are the main cells that contain histamine?
Mast Cells

Basophil Cells

Certain Neurons in CNS

Enterchromaffin-like cells in GI
Where are there high concentrations of histamine containing mast cells and basophil cells?
Lungs

Skin

GI tract
What stimulates histamine release? (2)
Mechanical Stimulation

Chemical Stimulation
-bacterial toxins
-certain drugs
Where are H1 receptors located?
Smooth Muscle

Vascular Endothelium

Sensory Neurons

Heart
What effect does histamine have on bronchial smooth muscle?
bronchoconstriction
Are H1 receptor blockers effective in treating/preventing bonchoconstriction in pt's with asthma?
Not alone
What effect does histamine have on arterioles?
Vasodilation ---> Leaky
How does histamine cause edema?
Increases vascular permeability

Makes vessels leaky
What effect may histamine have on BP?
↓BP
What effect does histamine have on mucocutaneous nerve endings?
Depolarizes --> Itching/irritation
Why were 2nd generation H1 receptor blockers developed?
2nd generation developed to reduce the side effects caused by 1st generation H1 receptor blockers
1st generation H1 Blockers
Diphenhydramine

Meclizine
2nd generation H1 Blockers
Fexofenadine

Loratadine
Diphenhydramine

Meclizine
1st generation H1 Blockers
Fexofenadine

Loratadine
2nd generation H1 Blockers
What is the role of histamine in allergic rhinitis?
NO induced vasodilation and Increased vascular permeability

Nasal Congestion
What is the main histamine receptor involved in allergic rhinitis?
H1 receptor
What types of effects does histamine have on the skin?
NO induced VD--> red spot

Vessel leakage--> Wheal

Axon reflex - vasodilation --> Flare
What is the main receptor involved in acute uticaria?
H1 receptor
Will H1 blockers treat the hypotension and bronchoconstriction involved with anaphylaxis?
NO, USE EPI

Antihistamines can be used w/ EPI but NEVER ALONE
How do antihistamines act as sedatives?
CNS depression

sedation
What receptors in the vestibular apparatus activate the vomit center?
H1 , Muscarinic
What receptors do antihistamines block to stop motion sickness/vomiting?
H1, Muscarinic
Can 1st generation antihistamines cross the BBB?
YES

this is why they have so many side effects (sedative, antiemetic, antimuscarinic)
Why do 2nd generation antihistamines have so few side effects?
CAN'T CROSS BBB
What other drug should antihistamines be given with treat angioedema?
EPI
"Antihistamines ____ better than reverse symptoms"
prevent symptoms
What drug can be used topically for temporary relief of puritis and pain associated with sunburn, minor cuts and scrapes, insect bites, etc..?
Diphenyhydramine
Which antihistamines can be used for sedation/hyposis ----> sleep aids
1st generation antihistamines
Which antihistamines can be used for motion sickness and the common cold?
1st Generation Antihistamines

**Anticholinergic Effects**
Which antihistamines have adverse effects such as sedation, dizziness and fatigue?
mainly 1st generation antihistamines
which antihistamine should be avoided while driving becuase it produces an effect similar to driving with a BAC of 0.05 - 0.1%?
Diphenhydramine
Which antihistamines cause Atropine-like effects?

(dry mouth, blurred vision, dry eyes, urinary retention/hesitancy)
1st generation antihistamines
Which antihistamine has teratogenicity?
Meclizine
When used topically, a side effect of antihistamine creams is _______
contact dermatitis
Acute antihistamine poisoning looks like _______ poisoning
Atropine poisoning

(convulsions, hallucinations, excitment, Ataxia, fixed dilated pupils, flushed face, dry-mouth, urinary retention, fever)
A patient who you have recently prescribed an antihistamine to complains of falling and convulsions. Upon examination they have fixed dilated pupils, dry-mouth, a flushed face and state they haven;t peed in two days. What are you thinking
Antihistamine poisoning --> mimics atropine poisoning
What drugs can you give to treat symptoms of atropine poisoning?
for convulsions --> diazepam

for anticholinergic effects --> physostigmine
What is physostigmine's MOA in treating antihistamine poisoning?
Acetocholinesterase Inhibitor (AChEI)

(inhibits breakdown of ACh from muscarinic receptor)
This is given as a nasal spray or opthalmic ointment (allergic conjunctivitis) to treat or prevent seasonal rhinitis. It inhibits mast cell release of histamine
Cromolyn
How do α-blockers help treat rhinitis?
Vasocontrict nasal passages --> ↓congestion
What are 2 α-blockers that help treat rhinitis?
pseudoephederine

phenylepherine
These agents are used to treat seasonal rhinitis. They are effective, but expensive. Improves itching, rhinorrhea and congestion. Not much help for allergic conjunctivitis. Work best if started before allergy season.
Intranasal corticosteroids (INC)
Leukotriene inhibitor used for seasonal rhinitis
Montelukast