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PHARMACOLOGY - Pulmonary > Histamine Antagonists > Flashcards

Histamine Antagonists Flashcards

1
Q 
Brompheniramine
Drug Class
MOA
Metabolism
Administration
Adverse Effects
Contraindications
Other
A

Drug Class
1st Generation Antihistamine

MOA
Works to block ALL histamine receptors and on come Ach (muscarinic) receptors, does not inhibit the release of histamine
Crosses the BBB

Metabolism
4-6 hours Duration of Action

Adverse Effects
Sedative, Inhibition of GI peristalsis (via anti-Cholinergic effects)

Contraindications
Patients with asthma (dries out mucosa, Local anti-Ach effects like Reduced Ciliary movement and systemic anti-Ach effects)

Other

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2
Q 
Chorpheniramine
Drug Class
MOA
Metabolism
Administration
Adverse Effects
Contraindications
Other
A

Drug Class
1st Generation Antihistamine

MOA
Works to block ALL histamine receptors and on come Ach (muscarinic) receptors, does not inhibit the release of histamine
Crosses the BBB

Metabolism
4-6 hours Duration of Action

Adverse Effects
Sedative, Inhibition of GI peristalsis (via anti-Cholinergic effects)

Contraindications
Patients with asthma (dries out mucosa, Local anti-Ach effects like Reduced Ciliary movement and systemic anti-Ach effects)

Other

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3
Q 
Clemastine
Drug Class
MOA
Metabolism
Administration
Adverse Effects
Contraindications
Other
A

Drug Class
1st Generation Antihistamine

MOA
Works to block ALL histamine receptors and on come Ach (muscarinic) receptors, does not inhibit the release of histamine
Crosses the BBB

Metabolism
4-6 hours Duration of Action

Adverse Effects
Sedative, Inhibition of GI peristalsis (via anti-Cholinergic effects)

Contraindications
Patients with asthma (dries out mucosa, Local anti-Ach effects like Reduced Ciliary movement and systemic anti-Ach effects)

Other

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4
Q 
Cyclizine
Drug Class
MOA
Metabolism
Administration
Adverse Effects
Contraindications
Other
A

Drug Class
1st Generation Antihistamine

MOA
Works to block ALL histamine receptors and on come Ach (muscarinic) receptors, does not inhibit the release of histamine
Crosses the BBB

Metabolism
4-24* hours Duration of Action

Adverse Effects
Sedative, Inhibition of GI peristalsis (via anti-Cholinergic effects)

Contraindications
Patients with asthma (dries out mucosa, Local anti-Ach effects like Reduced Ciliary movement and systemic anti-Ach effects)

Other

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5
Q 
Dimenhydrinate
Drug Class
MOA
Metabolism
Administration
Adverse Effects
Contraindications
Other
A

Drug Class
1st Generation Antihistamine

MOA
Works to block ALL histamine receptors and on come Ach (muscarinic) receptors, does not inhibit the release of histamine
Crosses the BBB

Metabolism
4-6 hours Duration of Action

Adverse Effects
Sedative, Inhibition of GI peristalsis (via anti-Cholinergic effects)

Contraindications
Patients with asthma (dries out mucosa, Local anti-Ach effects like Reduced Ciliary movement and systemic anti-Ach effects)

Other

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6
Q 
Diphenhydramine
Drug Class
MOA
Metabolism
Administration
Adverse Effects
Contraindications
Other
A

Drug Class
1st Generation Antihistamine

MOA
Works to block ALL histamine receptors and on come Ach (muscarinic) receptors, does not inhibit the release of histamine
Crosses the BBB

Metabolism
4-6 hours Duration of Action

Adverse Effects
Sedative, Inhibition of GI peristalsis (via anti-Cholinergic effects)

Contraindications
Patients with asthma (dries out mucosa, Local anti-Ach effects like Reduced Ciliary movement and systemic anti-Ach effects)

Other

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7
Q 
Hydroxyzine
Drug Class
MOA
Metabolism
Administration
Adverse Effects
Contraindications
Other
A

Drug Class
1st Generation Antihistamine

MOA
Works to block ALL histamine receptors and on come Ach (muscarinic) receptors, does not inhibit the release of histamine
Crosses the BBB

Metabolism
4-24* hours Duration of Action

Adverse Effects
Sedative, Inhibition of GI peristalsis (via anti-Cholinergic effects)

Contraindications
Patients with asthma (dries out mucosa, Local anti-Ach effects like Reduced Ciliary movement and systemic anti-Ach effects)

Other

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8
Q 
Meclizine
Drug Class
MOA
Metabolism
Administration
Adverse Effects
Contraindications
Other
A

Drug Class
1st Generation Antihistamine

MOA
Works to block ALL histamine receptors and on come Ach (muscarinic) receptors, does not inhibit the release of histamine
Crosses the BBB

Metabolism
4-24* hours Duration of Action

Adverse Effects
Sedative, Inhibition of GI peristalsis (via anti-Cholinergic effects)

Contraindications
Patients with asthma (dries out mucosa, Local anti-Ach effects like Reduced Ciliary movement and systemic anti-Ach effects)

Other

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9
Q 
Promethazine
Drug Class
MOA
Metabolism
Administration
Adverse Effects
Contraindications
Other
A

Drug Class
1st Generation Antihistamine

MOA
Works to block ALL histamine receptors and on come Ach (muscarinic) receptors, does not inhibit the release of histamine
Crosses the BBB

Metabolism
4-6 hours Duration of Action

Administration
Deep IM injection (subcutaneous injection contraindicated)

Adverse Effects
Sedative, Inhibition of GI peristalsis (via anti-Cholinergic effects), DIRECT IV INJECTION MAY CAUSE SEVERE TISSUE INJURY (including gangrene), SEVERE BREATHING PROBLEMS in some children under 2.

Contraindications
Patients with asthma (dries out mucosa, Local anti-Ach effects like Reduced Ciliary movement and systemic anti-Ach effects)

Other

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10
Q 
Tripolidine
Drug Class
MOA
Metabolism
Administration
Adverse Effects
Contraindications
Other
A

Drug Class
1st Generation Antihistamine

MOA
Works to block ALL histamine receptors and on come Ach (muscarinic) receptors, does not inhibit the release of histamine
Crosses the BBB

Metabolism
4-6 hours Duration of Action

Adverse Effects
Sedative, Inhibition of GI peristalsis (via anti-Cholinergic effects)

Contraindications
Patients with asthma (dries out mucosa, Local anti-Ach effects like Reduced Ciliary movement and systemic anti-Ach effects)

Other

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11
Q 
Acrivastine
Drug Class
MOA
Metabolism
Administration
Adverse Effects
Contraindications
Other
A

Drug Class
2nd Generation Anti-histamine

MOA
Blockage of Mainly H1 receptors
Does NOT significantly cross the BBB

Administration
Oral

Adverse Effects
Mild Cognitive Disturbance

Contraindications
Safer to use with asthmatics

Other

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12
Q 
Cetirizine
Drug Class
MOA
Metabolism
Administration
Adverse Effects
Contraindications
Other
A

Drug Class
2nd Generation Anti-histamine

MOA
Blockage of Mainly H1 receptors
Does NOT significantly cross the BBB

Metabolism
12 hour duration

Administration
Oral

Adverse Effects
*Mild Sedative effect (unique among 2nd generation drugs), Mild Cognitive Disturbance

Contraindications
Safer to use with asthmatics

Other

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13
Q 
Fexofenadine
Drug Class
MOA
Metabolism
Administration
Adverse Effects
Contraindications
Other
A

Drug Class
2nd Generation Anti-histamine

MOA
Blockage of Mainly H1 receptors
Does NOT significantly cross the BBB

Metabolism
8-24 hour duration

Administration
Oral

Adverse Effects
Mild Cognitive Disturbance

Contraindications
Safer to use with asthmatics

Other

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14
Q 
Loratadine
Drug Class
MOA
Metabolism
Administration
Adverse Effects
Contraindications
Other
A

Drug Class
2nd Generation Anti-histamine

MOA
Blockage of Mainly H1 receptors
Does NOT significantly cross the BBB

Metabolism
24 hours

Administration
Oral

Adverse Effects
Mild Cognitive Disturbance

Contraindications
Safer to use with asthmatics

Other

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15
Q 
Azelastine
Drug Class
MOA
Metabolism
Administration
Adverse Effects
Contraindications
Other
A

Drug Class
3rd Generation Anti-histamine

MOA
INHIBITS BOTH HISTAMINE AND LEUKOTRIENE ACTIVITY by Blocking Ca2+ mobilization in mast cells and blocking the 5-Lipoxygenase pathway
• Also antagonizes PAF receptor

Metabolism
Administration
Adverse Effects
Contraindications
Other
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16
Q 
Desloratidine
Drug Class
MOA
Metabolism
Administration
Adverse Effects
Contraindications
Other
A

Drug Class
3rd Generation Anti-histamine

MOA
GREATER specificity for H1 receptors (17x as specific as loratidine), LOWER affinity for Muscarinic receptors

Metabolism
27 hour half life

Administration
Adverse Effects
Contraindications
Other

17
Q 
Emedastine
Drug Class
MOA
Metabolism
Administration
Adverse Effects
Contraindications
Other
A

Drug Class
3rd Generation Anti-histamine

MOA
H1 antagonism and prevention of LTC4 from leukocytes

Metabolism
Administration
Adverse Effects
Contraindications
Other
18
Q 
Levocabastine
Drug Class
MOA
Metabolism
Administration
Adverse Effects
Contraindications
Other
A

Drug Class
3rd generation Anti-histamine

MOA
Rapid acting antihistamine used in nasal and ocular rhinitis

Metabolism
Administration
Adverse Effects
VERY FEW SIDE EFFECTS

Other
Piperidine derivative 1250 more times potent than chlorpheniramine.

19
Q 
Mizolastine
Drug Class
MOA
Metabolism
Administration
Adverse Effects
Contraindications
Other
A

NO APPROVED for US use

Antagonizes PAF and LTD4 induced bronchoconstriction

Non-sedative

20
Q 
Olopatadine
Drug Class
MOA
Metabolism
Administration
Adverse Effects
Contraindications
Other
A

Drug Class
3rd Generation Antihistamine

MOA
• H1 receptor specificity is greater than that of other ocular antihistamines
• Inhibits Tryptase release and PGD2 from opthalmic inflammatory cells
• INHIBITS HISTAMINE RELEASE FROM MAST CELLS

Metabolism
Administration
Adverse Effects
Contraindications
Other
21
Q

Why is adherence a bigger problem for 1st generation Antihistamines than 2nd generation?

A

1st Generation Antihistamines have more side effects and require multiple dosing

22
Q

What are the 3 goals of 3rd generation anti-histamines to improve on the 2nd generation?

A
  • Increase H1 receptor specificity
  • Block Histamine Release
  • Combine multiple target receptor types to give both anti-histamine and anti-asthmatic function
23
Q

What are the 3 goals of 3rd generation anti-histamines to improve on the 2nd generation?

A
  • Increase H1 receptor specificity
  • Block Histamine Release
  • Combine multiple target receptor types to give both anti-histamine and anti-asthmatic function
24
Q 
Eblastine
Drug Class
MOA
Metabolism
Administration
Adverse Effects
Contraindications
Other
A

NOT APPROVED FOR U.S. USE

Hybrid of 1st generation and 2nd generation Antihistamines

Antileukotriene, antibradykinin, less asthmatic activity

Similar adverse effects as loratidine

25
Q 
Eblastine
Drug Class
MOA
Metabolism
Administration
Adverse Effects
Contraindications
Other
A

NOT APPROVED FOR U.S. USE

Hybrid of 1st generation and 2nd generation Antihistamines

Antileukotriene, antibradykinin, less asthmatic activity

Similar adverse effects as loratidine

26
Q

How does efficacy of drug compare between 1st and 2nd/3rd generation drugs when it comes to:
• Allergic Rhinitis
• Urticaria
• Atopic Dermatitis

A

Equal efficacy but compliance is better in the 2nd and 3rd generations because dosing is less frequent

27
Q

What can 1st generation Antihistamines be used for that 2nd/3rd generation drugs can’t be used for?

A 
1st generation can do: 
• anti-motion sickness
• Antiemetic
• Appetite Stimulant 
• Increased sleepiness
28
Q

Name the 10 first generation antihistamines.

A
  • Bromopheniramine
  • Chlorpheniramine
  • Clemastine
  • Dimenhydrinate
  • Diphenhydramine
  • Hydroxyzine
  • Meclizine
  • Promethazine (IV injection causes tissue damage, breathing suppression in children under 2)
  • Tripolidine
29
Q

Name the 4 second generation antihistamines.

A
  • Acrivastine
  • Cetirazine (only one that is a mild sedative)
  • Fexfenadine
  • Loratadine
30
Q

What are the 3rd Generation antihistamines?

A
  • Azelastine (inhibits histamine, LOX, and prevents Ca2+ mobilization)
  • Desloratidine (H1 specificity higher than Loratadine, Lower muscarinic binding, 27 hour half-life)
  • Emedastine (H1 antagonist + LTC4 inhibition from WBCs)
  • Levobastine (ocular and nasal use, very very potent)
  • Mizolastine (Antagonizes PAF and LTD4 induced bronchoconstriction)
  • Olopatadine (Ocular use, H1 specific, Tryptase and PD2 inhibition)
31
Q

Name the 10 first generation antihistamines.

A
  • Bromopheniramine
  • Chlorpheniramine
  • Clemastine
  • Dimenhydrinate
  • Diphenhydramine
  • Hydroxyzine
  • Meclizine
  • Promethazine (IV injection causes tissue damage, breathing suppression in children under 2)
  • Tripolidine
32
Q

Name the 4 second generation antihistamines.

A
  • Acrivastine
  • Cetirazine (only one that is a mild sedative)
  • Fexfenadine
  • Loratadine
33
Q

What are the 3rd Generation antihistamines?

A
  • Azelastine
  • Desloratidine (H1 specificity higher than Loratadine, Lower muscarinic binding, 27 hour half-life)
  • Emedastine
  • Levobastine
  • Mizolastine
  • Olopatadine

PHARMACOLOGY - Pulmonary (30 decks)

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