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Pharm I - Test # 3 - Histamines
Fall Semester - 2010 - Pharm Test #3
30
Medical
Graduate
12/14/2010

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Term
Where are H1 receptors located?
Definition
Smooth Muscle
Endothelium
Brain
Term
Where are H2 receptors located?
Definition
Gastric Mucosa, Cardiac Muscle, Mast Cells, Brain
Term
Where are H3 receptors located?
Definition
Presynaptic Brain, Myenteric Plexus
Term
Where are H4 receptors located?
Definition
Eosinophils, Neutrophils, CD4 Tcells
Term
What is the triple response that an Intradermal injection of histamine can cause?
Definition
Redness
Inflammation
Flare Response
Term
In which types of patients is histamine contraindicated in?
Definition
Pts with asthma, active ulcer disease or GI bleeding
Term
What are some adverse effects of histamine?
Definition
Flushing
Hypotension
Tachycardia
HA
Wheals
Bronchoconstriction
GI Upset
Term
Describe the relationship between a physiologic antagonist and histamine. Give an example of a physiologic antagonist.
Definition
Smooth m. actions opposite those of histamine, but work through different receptors
Example = Epinephrine
Term
Describe the relationship between a release inhibitor and histamine. Give an example of a release inhibitor.
Definition
Reduce degradation of mast cells resulting from antigen-IgE interaction
Examples = Cromolyn and Nedocromil
Term
Describe the relationship between a receptor antagonist and histamine.
Definition
Competitively antagonize the actions of histamine
Term
What are anti-histamines used for? What receptor do they work on?
Definition
Anti-histamines are used for allergies.
They block the H1 receptors
Term
What are H2 Blockers used to treat?
Definition
Reduce the amount of stomach acid, so reduce GERD and Heart burn
Term
Which anti-histamine generation has more sedative effects?
Definition
1st Generation
Term
Which anti-histamine generation is more likely to block autonomic receptors?
Definition
1st Generation
Term
Which anti-histamine generation is rapidly absorbed? When is its peak onset?
Definition
Both 1st and 2nd; Peak onset in 1 to 2 h
Term
Which anti-histamine generation has a shorter duration of action?
Definition
1st generation
Term
Which anti-histamine generation is more lipid soluble? What does this allow the drug to do?
Definition
1st generation; Allows it to cross the BBB
Term
Which anti-histamine generation is metabolized by the CYP-450 system in the liver and therefore has a higher possibility of drug interactions? Which drugs is it likely to interact with?
Definition
2nd Generation
Interacts with -azoles, macrolides (erythromycin), and sedating agents
Term
Which anti-histamine generation generally has a less sedating action?
Definition
2nd Generation
Term
Which anti-histamine generation is used in N/V associated with pregnancy?
Definition
2nd Generation
Term
Which anti-histamine generation has anti-parkinson's effects?
Definition
1st generation
Term
Which anti-histamine generation is used in motion sickness and vestibular disturbances?
Definition
2nd generation
Term
Which generation of anti-histamines has serotonin blocking actions?
Definition
1st generation
Term
What effect do H2 Blockers have on H1 receptors?
Definition
Thought to have NO effect on H1 receptors
Term
Is there a low toxicity or high toxicity with H2 blockers?
Definition
Low toxicity
Term
Which two 2nd generation anti-histamines are no longer on the US market due to their potential to cause arrhythmias?
Definition
Terfenadine (Seldane) and Astemizole (Hismanal)
Term
What 3 drugs are 2nd generation H1 anti-histamines?
Definition
Cetirizine (Zyrtec)
Fexofenadine (Allegra)
Lortadine (Claritin)
Term
What do anti-histamine drugs end in?
Definition
-zine
-dine
-mine
-nate [Dimenhydrinate (Dramamine) - only one ending in -nate]
Term
What 11 drugs are 1st generation H1 anti-histamines?
Definition
5 - mines
Brompheniramine
Diphenhydramine
Chlorpheniramine
Carbinoxamine
Tripelennamine
4 - zines =
Hydroxyzine
Cyclizine
Meclizine
Promethazine
1 - dine
Cyproheptadine
1 -nate
Dimenhydrinate
Term
What 4 drugs are H2 anti-histamines?
Definition
Cimetidine
Rantidine
Famotidine
Nizatidine
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