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Pharm Test 3 > Histamine + Anti-Histamine > Flashcards

Histamine + Anti-Histamine Flashcards

1
Q

H1 blockers

1st gen
Rx

A

Chorpheniramine
Diphenydramine
Dimehydrinate

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2
Q

H1 Blockers

2nd gen
Rx

A

Loratadine
Certirizine
Fexofenadine

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3
Q

Other Drugs

Rx

A

Cromolyn Sodium

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4
Q

Histidine made from

A

L-histidine

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5
Q

Histamine metabolism

A

Released from mast cell/basophils, stored w/ heparin/acidic proteins

RAPIDLY broken down to inactive metabolites (MAO-B)

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6
Q

Autocoid

A

Released and act locally

Histamine

ALSO: serotonin, inflammatory modulators

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7
Q

Histamine roles

A

Immune
NT

In periphery widespread: skin/lungs

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8
Q

Histamine activates

A
  • Inflammation
  • activates acid-producing parietal cells
  • NT central/peripheral
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9
Q

HIstamine

Reaction type?

A

Type 1 hypersensitivity IgE

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10
Q

H1

A

Smooth muscle, CNS = up Ca2+

Endothelium = Up NO, cGMP

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11
Q

H2

A

Vascular smooth muscle

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12
Q

Why histamine released?

A

Immunologic (type 1, inflammation)

Mechanical (injury)

Drug effects (opiods, meds)

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13
Q

Cromolyn

A

Blocks histamine release

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14
Q

Histamine

Why smooth muscle contraction but vasodilation?

A

On H1/h2 smooth muscle, Up Ca2+ constrict

On H1 endothelial cell = releases NO, trumps any contraction

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15
Q

HIstamine

Peripheral effects

A
  • stimulate primary afferent nerve endigns : itch Pain (h1)

* CNS = NT. (Wakefullness, appetite, body temp)

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16
Q

Where can histamine be eaten?

A

Spoiled scombroid fish

High in histidine –> histamine (bacteria)

S/s: N/V, headache, flushing, sweating
GIVE H1 BLOCKER

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17
Q

Anaphylaxis vs Local allergic

cause?

A

Systemic = most NOT by histamine (other mediators)

*local = histamine (urticaria, allergic rhitinitis)

18
Q

Allergy

*subacute, preventative
*Mast cel stabilizer
Tx?

A

*Subacute, preventative
Inhaled fluticasone

  • Mast cell stabilizer - cromolyn sodium
  • stop mast cell degranualtion
  • nasal spray

*H1 antihistimines

19
Q

H1 antihistimines

S.E. wakefullness

A

Some make you awake! (CNS opposite)

20
Q

H1 antihistimines

Work against other inflammatory mediators?

A

NO

Asthma- leukotrienes

21
Q

Motion sickness?

A
  • **dimenhydrinate
  • Diphenhydramine

PROPHYLAXIS

22
Q

1st gen

More anti-chol?

A

Dyphenhydramine
Dimenhydrinate

LESS chlorpheniramien

23
Q

1st gen h1 blocker

Little specificity = S.E.
(Blocking what?)

OD?

A
  • chol blocker
  • dryness, urinary retention, sinus tach
  • a-adrenergic blocker/cardiac
    • hypoTN/reflex tach, dizziness
  • serotonin
  • hungry
  • H1
  • less inflame/itch/sneeze/rhinorrhea
  • less CNS neurotransmission/cognitive
  • Sedation
  • hungry

NO in GLAUCOMA, PROSTATIC HYPERTROPHY

Toxicity after OD = CNS over cardio S.E. – death w/in hours

24
Q

H1 blockers

uses

A
  • *Allergic rhinitis/conjunctivitis (2nd GEN)
  • *itching/urticaria (2nd GEN)
  • atopic derm (some)
  • Drug rxns (NO ANAPHYLAXIS)
  • Motion sickness/antiemetic
  • NO w/ COLD
  • local anesthetic (if allergic to others)
  • *Sleep aid (1st GEN)
25
Q

2nd gen H1 blocker

Uses

A

Allergic rhinitis
Allergic conjunctivitis
Urticaria

26
Q

1st gen h1 blocker

Uses

A

Insomnia

Motion sickness

27
Q

H1 blockers

Absorbtion

A

*rapid, lipid soluble
*2nd gen ionized at phys pH, up affinity for PGP (p-glycoprotein = pumps right out of cell)
SO METAB IN PERIPHERY, NOT REACHING CNS

28
Q

Histamines effective for sinus congestion?

A

NO

29
Q

H1 blockers

T 1/2?

A

2nd gen longer

30
Q

H1 blocker

Metab

A

Liver to urine

Fexofenadine = liver to bile

31
Q

H1 Blocker

Clearance

A

Renal

fexofenadine = bile

32
Q

H1 blocker

Pregger?

A

Cross placenta (no risk in preg)

Eliminated in breast milk

33
Q

Fexofenadine transported by

A

intestinal OATP1A2 = fruit juice inhibition

34
Q

Adverse patient population

A

Elderly - NO 1st GEN

  • falls
  • incontinence
  • altered consciousness/delirium

Infants - NO 1st GEN
*adverse effect, fatalities

35
Q

H1 1st gen

Daytime use

A

NOPE

Also no w/ alcohol

Some children get energy

Ex. Benadryl/Sominex (same rx)

36
Q

Antiemetic

A

Promethazine

37
Q

2nd gen antihistimine w/ possible anti-chol + sedation

A

Cetirizine

38
Q

H1 blocker

Mech

A

Inverse agonist

39
Q

1st gen, which is sleep aid?

A

Dyphenhydramine

40
Q

Dyphenhydramine/Dimenhydrinate VS. Chlorpheniramine

A

D’s = more ANTI-CHOL (and more sedation)

Chlorpheniramine = OTC cold meds

41
Q

OTC cold meds

Rx?

A

Chlorpheniramine

1st gen

42
Q

2nd gen antihistimines

Themes?

A

Fexophenadine
Loratidine
Cetirizine

  • NO ANTICHOL
  • NO SEDATION
  • LITTLE BBB PENETRATION

Pharm Test 3 (11 decks)

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