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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
Q

Activation of histamine (H) receptors results in?

A

Increase cGMP

26
Q

Different Isoforms of Histamine Receptors?

A

-H1
-H2

27
Q

H1?

A

Localized on smooth muscle, neurons

28
Q

H2?

A

Gastric mucosa, heart, mast cells, neurons
(Don’t get H2 receptors on mast cells confused with IgE/Ag complex binding to mast cells)

29
Q

Activation of H1 Receptors?

A

Involved in allergic reactions causing dermatitis (inflammation of skin), rhinitis (stuffy nose), conjunctivitis (pink eye)

30
Q

Activation of H1 results in?

A

1) Vasodilation (decrease in BP) (edema)
2) Nerve ending causing pruritus/cough reflex
3) Bronchoconstriciton and contraction of most GI smooth muscles

31
Q

Activation of H2 Receptor?

A

1) Increases Gastric Acid Secretion
2) Involves in Allergic Reaction
3) Increases Hear Rate and Contractility

31
Q

Histamine Pathway?

A

Ag binds to IgE –> Ab/Ag complex interacts with GPCR on basophils/Mast cell –> Increases cGMP –> increase Ca –> Histamine release from vesicle –>histamine

32
Q

H1 Pathway?

A

Histamine Activates H1 –> increase cGMP on smooth muscle cells and Neurons –> Bronchoconstriction/Cough/Pruritus/Vascular permeability/Vasodilation

33
Q

H2 Pathway?

A

Histamine Activates H2 –> increase HR and contractility/Allergic Rxn/Increase gastric secretion

34
Q

Histamine can either bind to?

A

H1 or H2

35
Q

Where in the pathway do Antihistamines block?

A

Will block these receptors (will still release Histamine just won’t have an effect on receptors)

36
Q

Antihistamines are?

A

Inverse Agonists for H1 receptor

37
Q

Antihistamine drugs are divided into 2 main categories?

A

-First-Generation
-Second-Generation

38
Q

Cross BBB and cause sedation?

A

(Very lipid soluble)
(First-Generation)
-Hydroxyzine
-Diphenhydramine
-Chloraphenoiramine

39
Q

Do NOT cross BBB (not sedative)?

A

(Second-Generation)
-Cetirizine
-Azelastine (nasal spray)
-Loratadine
-Fexofenadine

40
Q

What do Inverse Agonists do?

A

Stabilize Inactive Receptors

41
Q

Azelastine?

A

Nasal Spray

42
Q

Absorption (Antihistamine Drugs)?

A

When administered orally, they are absorbed rapidly

43
Q

Distribution (Antihistamine Drugs)?

A

(Widely distributed)
First-Generation cross BBB (but not Second-Generation)

44
Q

First-Generation cross BBB but not Second-Generation because of?

A

Higher Lipid Solubility

45
Q

Elimination (Antihistamine Drugs)?

A

Metabolized in the Liver by N-methyltransferase (Phase II) (Some antihistamines can be excreted into urine unchanged)

46
Q

What does N-methyltransferase do?

A

(Phase II)
Metabolizes Antihistamine Drugs in the Liver

47
Q

What blocks the production of cGMP?

A

Antihistamines

48
Q

Clinical Use (Antihistamines)?

A

More effective before onset of allergy (if you have allergies take medicine on a regular basis)

49
Q

Clinical Use of First-Generation Antihistamines?

A

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
Q

Clinical Use of Second-Generation Antihistamines?

A

Mainly used to ONLY treat Allergies

51
Q

What does Diphenhydramine do?

A

(First-Generation)
Can block muscarinic receptors causing dry mouth, blurred vision, tachycardia, and urinary retention

52
Q

Azelastine can cause?

A

(Nasal Spray)
Dizziness, Headache, Nasal Irritation, Dry-Mouth, and Weight Gain

52
Q

What’s the enzyme that breaks down Histamines?

A

N-methyltransferase

53
Q

How do you make Histamines?

A

Histidine (Carboxylase)

54
Q

Which can cross BBB?

A

First-Generation

Block 1: Pharmacology (9 decks)

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