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Pharmacology > Antihistamine > Flashcards

Antihistamine Flashcards

1
Q

Describe Histamine

A

biogenic amine. central role in the immediate hypersensitivity and allergic responses. Rapidly inactivated after release into blood and tissues.
stored in secretory granules in Mast cells, ECL cells of fundus and stomach.

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2
Q

What is Histamine’s Effect on the Nervous System?

A

Nerve bodies in hypothalamus to all areas of brain. Regulates Wakefulness, Pit Hormones, appetite, itch
H1 - Peripheral neurons - Epidermis - Itch; Dermis-Pain

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3
Q

What is Histamine’s Effect on the Cardiovascular System?

A

Vasodilation, fall in B/P. Both H1 and H2
Vasoconstriction in some venous beds - edema
Increased vascular permeability - H1 (cont endothelium disrupts tight junctions, leak)
H2 - Inc Ca2+ leads to inc contraction, SA node inc HR

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4
Q

What is Histamine’s Effect on the Pulmonary System?

A

H1 in Lung smooth muscle - inc secretion, bronchoconstriction

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5
Q

What is Histamine’s Effect on the Immune System?

A

Increases Vasc permeability, adhesion molecules, CHemotaxis, Inflammatory cytokines, antigen presentation of apc’s
Helps immune function.

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6
Q

What are the characteristics, effects, side effects and uses of H1-antihistamines?
Examples?

A

Reversibly bind to Receptors and stabilize the Inactive form.
Treat: allergiic rhinitis, conjunctivitis, Urticaria; N/V;Motion sickness; Sedatives; Sleep aid; cough; cold

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7
Q

What drugs have the strongest anticholinergic actions?

A

Promethazine

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8
Q

What are the characteristics, effects, side effects and uses of H1-antihistamines?
Examples?

A

Reversibly bind to Receptors and stabilize the Inactive form.
Treat: allergiic rhinitis, conjunctivitis, Urticaria; N/V;Motion sickness; Sedatives; Sleep aid; cough; cold
At high doses has anticholinergic effects

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9
Q

Which Histamines are first and second generations?

A

1st: Chlorpheniramine, Diphenhydramine, Pyrilamine, Hydroxyzine, Meclizine, Promethazine, Cyproheptadine
2nd: Azelastine, Fexofenadine, Loratadine, Desloratadine, Levocetirizine, Cetirizine

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10
Q

What is the difference between first and second generation H1 antihistamines?

A

H1: reversible receptor inhibitor, nonselective, Higher lipophilicity
H2: bind non competitively to H1 receptor, lower lipophilicity means doesn’t cross BBB (less sedating), higher selectivity toward H1 receptor.

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11
Q

What drugs have the strongest anticholinergic actions?

A

H1 antihistamines: diphenhydramine, promethazine

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12
Q

What drugs have the strongest sedative actions?

A

H1 antihistamines: Diphenhydramine, Hydroxyzine, Promethazine

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13
Q

What drugs have the strongest antiemetic/antimotion sickness actions?

A

H1 antihistamines: Diphenhydramine, Promethazine, Hydroxyzine, Meclazine

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14
Q

What drugs have the weakest anticholinergic actions?

A

H1 antihistamine 2nd gen

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15
Q

What drugs have the weakest sedative actions?

A

H1 antihistamine 2nd gen: Loratadine, Fexofenadine

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16
Q

What drugs have the weakest antiemetic/antimotion sickness actions?

A

H1 antihistamine 2nd Gen

17
Q

What drugs are the strongest inhibitors of serotonin receptors?

A

H1 antihistamines; cyproheptadine, wt gain, inc appetite

18
Q

What drugs are the strongest inhibitors of alpha-adrenergic receptors?

A

H1 antihistamine: promethazine, dizziness, postural hypotension

19
Q

MOA: Chlorpheniramine

A

1st gen. Moderate sedating, Moderate antimuscarinic activity, little anti-emetic function.

allergic rhinitis mostly

20
Q

MOA: Diphenhydramine

A

1st gen. benadryl
Signif sedation, signif antimuscarinic, signif antiemetic

cough, motion sickness, extrapyramidal symptoms from antipsychotic drugs

blocks Na channels in excitable membranes

21
Q

MOA: Pyrilamine

A

1st gen
Low to moderate sedative action, Little muscarinic, no anti emetic activity

Weak sleep aid

22
Q

MOA: Hydroxyzine

A

1st gen. marked sedation/antimuscarinic.

primarily an antiemetic/sedative

23
Q

MOA: Meclizine

A

1st gen. Minimal antimuscarinic. less sedation than hydroxine

Motion sickness in vertigo

24
Q

MOA: Promethazine

A

1st gen. Strong antiemetic/motion sickness.

blocks Na channels. inhib alpha 1 adrenergic receptors.
can block dopamine receptors

25
Q

MOA: Cyproheptadine

A

1st gen. Low sedation/antimuscarinic. Serotonin receptor antagonist

SE: inc wt gain, appetite. Tx serotonin syndrome

26
Q

MOA: Loratadine

A

2nd gen

27
Q

MOA: Desloratadine

A

2nd gen

28
Q

MOA: Levocetirizine

A

2nd gen

29
Q

MOA: Cetirizine

A

2nd gen

30
Q

MOA: Cetirizine

A

2nd gen. out of this generation, this has the most sedation.

31
Q

MOA: Azelastine

A

2nd gen. inverse agonist. Reduce Mast Cell release.

Intranasally or in eyes

32
Q

MOA: Cromolyn

A

Mast cell stabilizer. Prophylactic tx of allergy. inhib chloride channels

33
Q

MOA: Nedocromil

A

Mast cell stabilizer. prophylactic tx of allergy. Inhib chloride channels

34
Q

MOA: Doxepin

A

antidepressant. inhib H1 and H2 receptors.

Urticaria

35
Q

MOA: Ketotifen

A

Stabilize mast cells. eye drops

36
Q

MOA: Omalizumab

A

Monoclonal IgE antibody. Prophylactic tx of allergy, asthma, chronic urticaria.
Binds to free IgE ab and prevents binding of FcE3b on mast cells. reduce cytokines released from mast cells

Pharmacology (10 decks)

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