Pharm 2 Flashcards

1
Q

Histamine

A

Biogenic amine
smooth muscle stim, intense vasodepressor, mimics allergic and hypersensitivity reactions.
physiological - gastric acid secretion, neuromodulation and neurotransmission

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2
Q

histamine synthesis

A

histidine decarboxylase takes histidine (AA) to histamine

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3
Q

histamine degredation

A

2 steps - histamine methyltransferase and MAO

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4
Q

Cells which produce histamine

A

Mast cell pool - slowly sun largest supply of histamine
-mast cells and basophils
released in shock or allergic reaction.
GI, Skin, CNS - rapidly syn and works as a neurotransmitter

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5
Q

H-1 receptors

A

classical smooth muscle, vascular effects

  • constriction of bronchi, gut, smooth muscle and large blood vessels
  • largest effect at microvasculature&raquo_space; dilation of arterioles and drop in BP and increase cap perm&raquo_space; edema
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6
Q

H-2 receptors

A

found in GI tract - mediate gastric secretion of HCL

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7
Q

H-3 receptors

A

inhibition of adenyl cyclase through Gi protein

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8
Q

CNS H receptors

A

H-3 and H-1

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9
Q

HIstamine in rodents

A

arteriole CONSTRICTION

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10
Q

histamine in rabbits

A

pronounced vessel constriction, increased BP

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11
Q

Cromolyn

A

blocks mast cell degranulation - used as prophylaxis for bronchial asthma in people

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12
Q

H-1 antihistamines

A

orally absorbed in mono gastric animals, can give IM

competitive inhibitors - most effective as a prophylactic

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13
Q

H-1 antihistamines side effects

A

CNS - sedation
Anti-cholinergic - dry mouth, blurred vision, tachycardia
contraindications - glaucoma, ileus, cardiac arrythmias

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14
Q

anaphylactic reaction treatments

A
  1. systemic epinephrine - physiological antagonism - bronchial dilation and vasoconstriction
  2. Fluids
  3. adjunctive - H-1 antihist > Benadryl, Corticosteroids
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15
Q

Treatment of dermal conditions

-uticaria, hypersensitivity reactions, insect stings, pruritus

A

H-1 antihistamines - systemically or topically

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16
Q

Anti-emetic/motion sickness effects of antihistamines

A

due to anti-cholinergic action of some antihistamines - ex. dramamine

17
Q

Cimetidine, Ranitidine, and Famotidine

A

H-2 receptor blocker

18
Q

Serotonin degradation

A

monoamine oxidase

19
Q

Serotonin synthesis

A

2 steps. Tryptophan&raquo_space;tryptophan hydroylase&raquo_space; 5-hydroxytryptophan» amino acid decarboxylase&raquo_space; 5-hydroxytryptamine

20
Q

endogenous serotonin

A

enterochromaffin cells - 90%
CNS
mast cells
concentrated in platelets

21
Q

Triphasic response

A

Serotonin > 1. decreased BP and HR, 2. increased BP > direct effect, 3. prolonged decrease in BP

22
Q

Dextran in rats

A

mast cell degranulation&raquo_space; large amount of serotonin leads to triphasic response

23
Q

serotonin effects on vasculature

A

homeostasis > local vasoconstriction

24
Q

serotonin effects on CNS

A

important for maintenance of normal mood

25
Q

amitriptyline

A

tricyclic anti depressant

26
Q

metoclopramide

A

blocks 5-HT3 receptors in the brain

27
Q

carcinoid syndrome

A

5-HT producing tumors in GI tract > flushing, diarrhea, bronchoconstriction, sudden decrease in BP, edema and ascites.

28
Q

kinin

A

endogenous vasodilator > increase vascular permeability of microcirculation, increase contraction of nonvascular smooth muscle, evoke pain

29
Q

Converting Enzyme (Kinases)

A

degrade bardykinin and kalllidin as well as convert angiotensinogen to angiotensin

30
Q

Kinins, cardio effects

A

dilation of arterioles, contraction of large vessels, increased capillary permeability

31
Q

kinins, renal

A

diuretic, natriuretic

32
Q

allermyl

A

topical - blocks the synthesis TNFa

33
Q

Thalidomide

A

topical - blocks formation of TNFa