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Block 1: Pharmacology > Lecture 7 > Flashcards

Lecture 7 Flashcards

1
Q

Allergy?

A

Disorder of the immune system resulting in excessive histamine release

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2
Q

Allergic reactions can occur to?

A

Normally harmless environmental substances (allergens)

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3
Q

Common allergic reactions include?

A

-Eczema
-Hives
-Hay Fever
-Asthma

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4
Q

Allergic Reaction can occur to?

A

-Food Allergens
-Drug Allergens
-Venom (of stinging insects such as wasps and bees)

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5
Q

First-Generation Antihistamine?

A

(CROSS BBB)
-Chlorpheniramine
-Diphenhydramine (Benadryl)
-Hydroxyzine

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6
Q

“Hi Drowsy Children” or “Call Dat Hoe”?

A

(First-Generation Antihistamine)
-Chlorpheniramine
-Diphenhydramine (Benadryl)
-Hydroxyzine

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7
Q

Second-Generation Antihistamine?

A

(DO NOT CROSS BBB)
-Cetirizine
-Azelastine (intranasal)
-Loratadine
-Fexofenadine

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8
Q

“CALF”?

A

(Second-Generation Antihistamine)
-Cetirizine
-Azelastine (intranasal)
-Loratadine
-Fexofenadine

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9
Q

First-Generation and Second-Generation Antihistamine are all?

A

Inverse Agonists for mainly H1 Receptor

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10
Q

Autacoids are produced by?

A

Neural and Non-Neural tissues

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11
Q

Monoamines such as?

A

-Histamines
-Serotonin
-Prostaglandins
-Leukotrienes

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12
Q

Histamine can be released?

A

-Locally in response to injury or a local hormone (also prostaglandins and leukotrienes)
-In response to an allergic reaction

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13
Q

High concentrations of Histamine may lead to?

A

Anaphylactic Shock

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14
Q

Drugs that inhibit the synthesis or block the receptor for autacoids?

A

Alleviate allergic reactions

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15
Q

Drugs that activate the receptors are helpful for?

A

Inducing labor, fighting migraines, and headaches

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16
Q

Histamines are made from?

A

Amino Acid Histidine by the enzyme L-histidine decarboxylase

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17
Q

Histamines are stored in?

A

Granules (vesicles)

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18
Q

Histamine is metabolized by?

A

N-methyltransferase enzymes within GI tract and liver

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19
Q

1) Antigen (allergen, venom, etc.) binds to?

A

Immunoglobin E (IgE)

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20
Q

2) Antibody-antigen complex interacts with?

A

G-protein coupled receptors on mast cells and basophils (abundant in the GI tract, skin, and respiratory tract), resulting in release of histamines

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21
Q

Stimuli that Increase cGMP?

A

Increase Histamine release

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22
Q

Increase cAMP will make?

A

Decrease Histamine release

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23
Q

Histamine Pathway?

A

Ag –> IgE –> GPCR of Mast cells and basophils –> Histamine release –> H1 Receptors

24
Q

Histamine is an?

A

Agonist for G protein-coupled receptors

25
Activation of histamine (H) receptors results in?
Increase cGMP
26
Different Isoforms of Histamine Receptors?
-H1 -H2
27
H1?
Localized on smooth muscle, neurons
28
H2?
Gastric mucosa, heart, mast cells, neurons (Don't get H2 receptors on mast cells confused with IgE/Ag complex binding to mast cells)
29
Activation of H1 Receptors?
Involved in allergic reactions causing dermatitis (inflammation of skin), rhinitis (stuffy nose), conjunctivitis (pink eye)
30
Activation of H1 results in?
1) Vasodilation (decrease in BP) (edema) 2) Nerve ending causing pruritus/cough reflex 3) Bronchoconstriciton and contraction of most GI smooth muscles
31
Activation of H2 Receptor?
1) Increases Gastric Acid Secretion 2) Involves in Allergic Reaction 3) Increases Hear Rate and Contractility
31
Histamine Pathway?
Ag binds to IgE --> Ab/Ag complex interacts with GPCR on basophils/Mast cell --> Increases cGMP --> increase Ca --> Histamine release from vesicle -->histamine
32
H1 Pathway?
Histamine Activates H1 --> increase cGMP on smooth muscle cells and Neurons --> Bronchoconstriction/Cough/Pruritus/Vascular permeability/Vasodilation
33
H2 Pathway?
Histamine Activates H2 --> increase HR and contractility/Allergic Rxn/Increase gastric secretion
34
Histamine can either bind to?
H1 or H2
35
Where in the pathway do Antihistamines block?
Will block these receptors (will still release Histamine just won't have an effect on receptors)
36
Antihistamines are?
Inverse Agonists for H1 receptor
37
Antihistamine drugs are divided into 2 main categories?
-First-Generation -Second-Generation
38
Cross BBB and cause sedation?
(Very lipid soluble) (First-Generation) -Hydroxyzine -Diphenhydramine -Chloraphenoiramine
39
Do NOT cross BBB (not sedative)?
(Second-Generation) -Cetirizine -Azelastine (nasal spray) -Loratadine -Fexofenadine
40
What do Inverse Agonists do?
Stabilize Inactive Receptors
41
Azelastine?
Nasal Spray
42
Absorption (Antihistamine Drugs)?
When administered orally, they are absorbed rapidly
43
Distribution (Antihistamine Drugs)?
(Widely distributed) First-Generation cross BBB (but not Second-Generation)
44
First-Generation cross BBB but not Second-Generation because of?
Higher Lipid Solubility
45
Elimination (Antihistamine Drugs)?
Metabolized in the Liver by N-methyltransferase (Phase II) (Some antihistamines can be excreted into urine unchanged)
46
What does N-methyltransferase do?
(Phase II) Metabolizes Antihistamine Drugs in the Liver
47
What blocks the production of cGMP?
Antihistamines
48
Clinical Use (Antihistamines)?
More effective before onset of allergy (if you have allergies take medicine on a regular basis)
49
Clinical Use of First-Generation Antihistamines?
1) Sedation (pre-operative) CNS depressant so can decrease amount of anesthesia needed 2) Treat nausea and vomiting 3) To prevent motion sickness and vertigo
50
Clinical Use of Second-Generation Antihistamines?
Mainly used to ONLY treat Allergies
51
What does Diphenhydramine do?
(First-Generation) Can block muscarinic receptors causing dry mouth, blurred vision, tachycardia, and urinary retention
52
Azelastine can cause?
(Nasal Spray) Dizziness, Headache, Nasal Irritation, Dry-Mouth, and Weight Gain
52
What's the enzyme that breaks down Histamines?
N-methyltransferase
53
How do you make Histamines?
Histidine (Carboxylase)
54
Which can cross BBB?
First-Generation

Block 1: Pharmacology (9 decks)

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