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
amitriptyline
tricyclic anti depressant
26
metoclopramide
blocks 5-HT3 receptors in the brain
27
carcinoid syndrome
5-HT producing tumors in GI tract > flushing, diarrhea, bronchoconstriction, sudden decrease in BP, edema and ascites.
28
kinin
endogenous vasodilator > increase vascular permeability of microcirculation, increase contraction of nonvascular smooth muscle, evoke pain
29
Converting Enzyme (Kinases)
degrade bardykinin and kalllidin as well as convert angiotensinogen to angiotensin
30
Kinins, cardio effects
dilation of arterioles, contraction of large vessels, increased capillary permeability
31
kinins, renal
diuretic, natriuretic
32
allermyl
topical - blocks the synthesis TNFa
33
Thalidomide
topical - blocks formation of TNFa