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11 Cards in this Set

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  • Back
What role does histamine have in the body?

CNS - Excitatory neurotransmitter, regulates sleep wake cycle




Periphery - Bronchoconstriction, vasodilation




GIT - increased gastric acid secretion

What is the difference between H1 and H2 histamine receptors?

H1 - CNS and periphery


CNS and peripheral effects


H2 - parietal cells


GIT effects

What are H1-antihistamines and what are they used for?

Antagonise H1-histamine receptors leading to decrease in H1 effects.




Used for histamine-mediated inflammatory reactions (ie allergies)

What are H2-antihistamines and what are they used for?

Antagonise H2-hitamine receptors leading to decreased H2 effects.




Used for histamine-mediated gastric acid disorders (gastric ulcers)

What property of the different H1 antihistamines effects their capacity to alter the sleep-wake cycle?

Lipophilicity - More lipophilic drugs more readily cross BBB leading to depression of CNS




-Older antihistamine generally are more lipophilic

Why are H1-antihistamines not used in the treatment of anaphylaxis? What is used?

- Not fast enough


- Other mediators involved other than just histamine so simply blocking that will not have great enough effect




ADRENALINE (symptomatic treatment)

What side effects are associated with H1-antihistamines?

CNS


Sedation (Although can cause seizures after extremely high doses)




Antimuscarinic effects


Dry mouth, pupil dilation, tachycardia

What must not be done when administering H1-antihistamines?

Must not be given IV (may cause CNS excitatory side effects such as seizures)

What are the 1st generation H1 antihistamines? (3)

Promethazine


Dimenhydrinate


Chlorpheniramine

What are the 2nd generation antihistamines? (3)

Loratidine


Cetirizine


Fexofenadine

How do the 1st and 2nd generation antihistamines differ?

Lipophilicity and thus capacity to cross the blood brain barrier.




1st gen more lipophilic


2nd gen less lipophilic