Final Exam - Histamine & Antihistamine Flashcards

1
Q

What is the primary effect of histamine stimulation of H1 receptors on smooth muscle?

A

smooth muscle contraction.

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2
Q

How does histamine binding to H1 receptors lead to vasodilation?

A

stimulates the release of nitric oxide, which is a vasodilator. This relaxation of vascular smooth muscles causes vasodilation.

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2
Q

What is the consequence of histamine increasing the permeability of post-capillary venules?

A

allows fluids and cells to pass through the vessel walls, contributing to swelling and inflammation.

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3
Q

What sensation is induced by histamine binding to H1 receptors?

A

induce itch, leading to the sensation of itching.

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4
Q

What are the three components of the histamine triple response?

A

triple response consists of the reddening of the skin, the appearance of surrounding flare (swelling), and the presence of a weal, which is a raised, red, itchy area of skin.

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5
Q

Name two sedating antihistamines.

A

Doxylamine and Promethazine

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6
Q

Name three non-sedating antihistamines.

A

Fexofenadine, Loratadine, and Cetirizine

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7
Q

What is a characteristic of sedating antihistamines regarding their ability to cross the blood-brain barrier (BBB)?

A

can cross the BBB and cause central effects such as sedation and drowsiness

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8
Q

What prevents non-sedating antihistamines from crossing the BBB?

A

their high affinity for P-glycoprotein (P-gP) and their effects on other receptors.

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9
Q

What is the primary specificity of non-sedating antihistamines?

A

are specific for histamine at H1 receptors

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10
Q

How do the durations of action differ between sedating and non-sedating antihistamines?

A

shorter for sedating antihistamines (8-30 hours) and longer for non-sedating antihistamines (24 hours).

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11
Q

What potential drug interactions are associated with sedating antihistamines due to their ability to cross the BBB?

A

may interact with other medications or agents that cause sedation or central nervous system (CNS) depression, such as benzodiazepines, opioid analgesics, and alcohol

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12
Q

What distinguishes non-sedating antihistamines in terms of cardiac safety?

A

are considered cardiac safe

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13
Q

In addition to the treatment of allergies, what other uses are associated with sedating antihistamines?

A

short-term insomnia, as analgesics in combination with paracetamol and codeine, in cough preparations, and for the treatment of motion sickness.

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14
Q

What is the primary use of non-sedating antihistamines?

A

treatment of allergies

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15
Q

What are the common therapeutic uses of sedating antihistamines?

A

treatment of allergies, including allergic rhinitis and hives (skin rashes). They can also be used for prophylactic purposes.

16
Q

In addition to treating allergy, what specific condition is short-term insomnia treated with a sedating antihistamine like doxylamine?

A

Short-term insomnia can be treated with doxylamine, a sedating antihistamine.

16
Q

How can sedating antihistamines enhance the effects of analgesics like paracetamol and codeine?

A

Sedating antihistamines, when used in combination with paracetamol and codeine, can enhance the effects of these analgesic medications.

17
Q

What is a common inclusion for sedating antihistamines in cough preparations?

A

Sedating antihistamines are often included in cough preparations.

18
Q

What therapeutic uses are common for non-sedating antihistamines, particularly in the treatment of allergies?

A

treatment of allergies, including allergic rhinitis and hives (skin rashes). They can also be used for prophylactic purposes.