Histamine Antagonists Flashcards
Brompheniramine Drug Class MOA Metabolism Administration Adverse Effects Contraindications Other
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
Chorpheniramine Drug Class MOA Metabolism Administration Adverse Effects Contraindications Other
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
Clemastine Drug Class MOA Metabolism Administration Adverse Effects Contraindications Other
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
Cyclizine Drug Class MOA Metabolism Administration Adverse Effects Contraindications Other
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
Dimenhydrinate Drug Class MOA Metabolism Administration Adverse Effects Contraindications Other
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
Diphenhydramine Drug Class MOA Metabolism Administration Adverse Effects Contraindications Other
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
Hydroxyzine Drug Class MOA Metabolism Administration Adverse Effects Contraindications Other
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
Meclizine Drug Class MOA Metabolism Administration Adverse Effects Contraindications Other
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
Promethazine Drug Class MOA Metabolism Administration Adverse Effects Contraindications Other
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
Tripolidine Drug Class MOA Metabolism Administration Adverse Effects Contraindications Other
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
Acrivastine Drug Class MOA Metabolism Administration Adverse Effects Contraindications Other
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
Cetirizine Drug Class MOA Metabolism Administration Adverse Effects Contraindications Other
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
Fexofenadine Drug Class MOA Metabolism Administration Adverse Effects Contraindications Other
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
Loratadine Drug Class MOA Metabolism Administration Adverse Effects Contraindications Other
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
Azelastine Drug Class MOA Metabolism Administration Adverse Effects Contraindications Other
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
Desloratidine Drug Class MOA Metabolism Administration Adverse Effects Contraindications Other
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
Emedastine Drug Class MOA Metabolism Administration Adverse Effects Contraindications Other
Drug Class
3rd Generation Anti-histamine
MOA
H1 antagonism and prevention of LTC4 from leukocytes
Metabolism Administration Adverse Effects Contraindications Other
Levocabastine Drug Class MOA Metabolism Administration Adverse Effects Contraindications Other
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.
Mizolastine Drug Class MOA Metabolism Administration Adverse Effects Contraindications Other
NO APPROVED for US use
Antagonizes PAF and LTD4 induced bronchoconstriction
Non-sedative
Olopatadine Drug Class MOA Metabolism Administration Adverse Effects Contraindications Other
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
Why is adherence a bigger problem for 1st generation Antihistamines than 2nd generation?
1st Generation Antihistamines have more side effects and require multiple dosing
What are the 3 goals of 3rd generation anti-histamines to improve on the 2nd generation?
- Increase H1 receptor specificity
- Block Histamine Release
- Combine multiple target receptor types to give both anti-histamine and anti-asthmatic function
What are the 3 goals of 3rd generation anti-histamines to improve on the 2nd generation?
- Increase H1 receptor specificity
- Block Histamine Release
- Combine multiple target receptor types to give both anti-histamine and anti-asthmatic function
Eblastine Drug Class MOA Metabolism Administration Adverse Effects Contraindications Other
NOT APPROVED FOR U.S. USE
Hybrid of 1st generation and 2nd generation Antihistamines
Antileukotriene, antibradykinin, less asthmatic activity
Similar adverse effects as loratidine
Eblastine Drug Class MOA Metabolism Administration Adverse Effects Contraindications Other
NOT APPROVED FOR U.S. USE
Hybrid of 1st generation and 2nd generation Antihistamines
Antileukotriene, antibradykinin, less asthmatic activity
Similar adverse effects as loratidine
How does efficacy of drug compare between 1st and 2nd/3rd generation drugs when it comes to:
• Allergic Rhinitis
• Urticaria
• Atopic Dermatitis
Equal efficacy but compliance is better in the 2nd and 3rd generations because dosing is less frequent
What can 1st generation Antihistamines be used for that 2nd/3rd generation drugs can’t be used for?
1st generation can do: • anti-motion sickness • Antiemetic • Appetite Stimulant • Increased sleepiness
Name the 10 first generation antihistamines.
- Bromopheniramine
- Chlorpheniramine
- Clemastine
- Dimenhydrinate
- Diphenhydramine
- Hydroxyzine
- Meclizine
- Promethazine (IV injection causes tissue damage, breathing suppression in children under 2)
- Tripolidine
Name the 4 second generation antihistamines.
- Acrivastine
- Cetirazine (only one that is a mild sedative)
- Fexfenadine
- Loratadine
What are the 3rd Generation antihistamines?
- 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)
Name the 10 first generation antihistamines.
- Bromopheniramine
- Chlorpheniramine
- Clemastine
- Dimenhydrinate
- Diphenhydramine
- Hydroxyzine
- Meclizine
- Promethazine (IV injection causes tissue damage, breathing suppression in children under 2)
- Tripolidine
Name the 4 second generation antihistamines.
- Acrivastine
- Cetirazine (only one that is a mild sedative)
- Fexfenadine
- Loratadine
What are the 3rd Generation antihistamines?
- Azelastine
- Desloratidine (H1 specificity higher than Loratadine, Lower muscarinic binding, 27 hour half-life)
- Emedastine
- Levobastine
- Mizolastine
- Olopatadine
