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Pharm 4 > Biogenic Amines > Flashcards

Biogenic Amines Flashcards

(30 cards)

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1
Q

Synth of histamine

A

Histidine→(histadine decarboxylase)→Histamine

*Histamine found in almost all tissues

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2
Q

Normal physiology of histamine

A
  • Growth and regeneration
  • Neuromodulator
  • Regulator of microcirculation
  • Defense mechanism
    • Histamine stored in mast cells in skin and lungs
    • Immune fxn and inflam process
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3
Q

When are histamines released

A
  • After tissue injury
    • Inflammation response
    • Mech, thermal, radiant injuries
  • After chemical exposure
    • Drugs and insect venom
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4
Q

Histamine

Mechanism and effects

A

Mech: bind to specific receptors

Effects:

  • Vascular
    • Constricts large vessels, dilates smaller
      • Cooling of blood @ injury site
    • Endothelial cell leakage-local edema-“wheal”
    • Triple response ton injected histamine
      • Central red spot-vasodilation
      • Flare-surrounding lighter red
      • Wheal-swelling-edema
  • Neuronal
    • Stim sens neurons→itching, pain
    • CNS-probably increased alertness and wakefulness
  • Smooth m
    • Bronchoconstriction
    • Constrics intestinal mm→diarrhea
  • Exocrine secretion
    • Stim. bronchiole, salivary, and digestive secretions

Diarrhea

Itching

Alertness

Pain

Edema

Restriction (broncho and large vessels)

Secretions (bronchiole, salivary, adn digestive)

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5
Q

H1 Blockers

Mech and effects

A

Mech: Block histamine receptor

Effects:

  • CNS
    • Sedative effect
      • Some can be excitatory in children and elderly
    • Anti-nausea and anti-emetic
  • Drys mucous membranes
    • Blockade of H1 receptor
  • Peripheral nervous system
    • Local anesthetic-(may be in sunburn tx)
  • Smooth muscle dilator
    • Bronchial smooth m dilation
    • Can inh. secretion of ILs and other inflammation mediators
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6
Q

H2 Blockers

Mech and effects

A

Mech: Block histamine receptor

Effects:

  • Blocks gastric secretion
    • Histamine required to stim. acid secretion from parietal cells
  • Blockade of H2 receptors→Decrease H secretion
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7
Q

Indications for first gen H1 antihistamines

A

Alleric response

  • Dermatoses
  • Urticarias
  • Insect stings and bites

Allergic rhinitis-decrease congestion and sneezing

  • Allergic conjunctivitis

Not of value in treating asthma

Antiemetic/nauseant

Sedative

  • Contain diphenhydramine
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8
Q

First Generation H1 blockers

A

Diphenhydramine

Clemastine

Chloropheniramine

Hydroxyzine

Promethazine

Tripelennamine

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9
Q

Diphenhydramine

A

First gen H1 blocker

Tx: Sedative, motion sickness

Pharmacokinetics: Slightly lipid soluble, not ionized→Gets into CNS

Toxicity:

  • High TI
    • But suicide attempts b/c readily available
  • Interactions w/ other CNS depressants
  • Anti-muscarinic effects
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10
Q

Clemastine

A

First gen H1 blocker

Tx: Motion sickness, sedative

Pharmacokinetics: Slightly lipid soluble, not ionized→Gets into CNS

Toxicity:

  • High TI
    • But suicide attempts b/c readily available
  • Interactions w/ other CNS depressants
  • Anti-muscarinic effects
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11
Q

Chlorpheniramine

A

First gen H1 blocker

Tx: Does not cause as much sedation

Pharmacokinetics: Slightly lipid soluble, not ionized→Gets into CNS

Toxicity:

  • High TI
    • But suicide attempts b/c readily available
  • Interactions w/ other CNS depressants
  • Anti-muscarinic effects
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12
Q

Hydroxyzine

A

First gen H1 blocker

Tx: Sedative, anti-itch

Pharmacokinetics: Slightly lipid soluble, not ionized→Gets into CNS

Toxicity:

  • High TI
    • But suicide attempts b/c readily available
  • Interactions w/ other CNS depressants
  • Anti-muscarinic effects
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13
Q

Promethazine

A

First gen H1 blocker

Tx: Strong sedative, strong anti-emetic

Related to anti-psychotic drugs

Pharmacokinetics: Slightly lipid soluble, not ionized→Gets into CNS

Toxicity:

  • High TI
    • But suicide attempts b/c readily available
  • Interactions w/ other CNS depressants
  • Anti-muscarinic effects
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14
Q

Tripelennamine

A

First gen H1 blocker

Tx: Sedative, local anesthetic effect

Pharmacokinetics: Slightly lipid soluble, not ionized→Gets into CNS

Toxicity:

  • High TI
    • But suicide attempts b/c readily available
  • Interactions w/ other CNS depressants
  • Anti-muscarinic effects
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15
Q

Second generation H1 blockers

A

Loratadine

Fexofenadine

Desloratadine

Cetirizine

Don’t cause drowsiness

Fewer CNS effects

Ionized in blood

Not metab. by P450

  • What does the fox say?*
  • What des the fex ce?*

_Des_loratadine (+ loratadine) _fex_ofenadine _ce_tirizine

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16
Q

Loratadine

Study These Flashcards
A

Second gen H1 blocker

Pharmacokinetics: Ionized in blood so fewer CNS effects

Don’t cause drowsiness

Not metab by P450

Toxicity:

  • High TI
    • But suicide attempts b/c readily available
  • Anti-muscarinic effects
17
Q

Fexofenadine

Study These Flashcards
A

Second gen H1 blocker

Pharmacokinetics: Ionized in blood so fewer CNS effects

Don’t cause drowsiness

Not metab by P450

Toxicity:

  • High TI
    • But suicide attempts b/c readily available
  • Anti-muscarinic effects
18
Q

Desloratadine

Study These Flashcards
A

Second gen H1 blocker

Pharmacokinetics: Ionized in blood so fewer CNS effects

Don’t cause drowsiness

Not metab by P450

Toxicity:

  • High TI
    • But suicide attempts b/c readily available
  • Anti-muscarinic effects
19
Q

Cetirizine

Study These Flashcards
A

Second gen H1 blocker

Pharmacokinetics: Ionized in blood so fewer CNS effects

Don’t cause drowsiness

Not metab by P450

Toxicity:

  • High TI
    • But suicide attempts b/c readily available
  • Anti-muscarinic effects
20
Q

H2 blockers

Names

Study These Flashcards
A

“-tidine”s

Cimetidine

Ranitidine

Famotidine

Nizatidine

*Only diff amongst all is that cimetidine has anti-androgenic effects

21
Q

Cimetidine

Study These Flashcards
A

H2 blocker

Does not cross BB barrier

Effects:

  • Blockade of H2 receptors→Decrease H secretion
    • Histamine required to stim. acid secretion from parietal cells

SE:

  • Anti-androgenic effect
    • Males: gynecomastia and reduced sperm count
    • Females: Lactation
22
Q

Ranitidine

Study These Flashcards
A

H2 blocker

Does not cross BB barrier

Effects:

  • Blockade of H2 receptors→Decrease H secretion
  • Histamine required to stim. acid secretion from parietal cells
23
Q

Famotidine

Study These Flashcards
A

H2 blocker

Does not cross BB barrier

Effects:

  • Blockade of H2 receptors→Decrease H secretion
  • Histamine required to stim. acid secretion from parietal cells
24
Q

Nizatidine

Study These Flashcards
A

H2 blocker

Does not cross BB barrier

Effects:

  • Blockade of H2 receptors→Decrease H secretion
  • Histamine required to stim. acid secretion from parietal cells
25
Serotonin synth
Tryptophan→→5-hydroxytryptamine (5HT) Found in enterochromaffin cells of gut
26
Physiologic effects of 5HT
* Smooth mm constriction * *Sero=serum* * *Tonin=tone (mm constriction)* * Itching, pain * Neurotransmission * Nausea
27
Carcinoid syndrome
Tumor of enterochromaffin cells→Increase 5HT Bronchospasm Skin flushing Diarrhea Fibrosis of heart valves No CNS effects--doesn't get into CNS when produced peripherally ***C**utaneous flushing* ***A**sthmatic bronchospasm* ***R**ight valve fibrosis* ***P**ellegra* ***E**nterochrommafin cells* ***D**iarrhea* ***N**o CNS effects*
28
Migraine headaches
Migrane=hemi-crania=one side of head Dilation of blood vessels in dura and pia mater Inflam., swelling, throbbing pain Associated w/ aura Genetic component--3x more likely in women Role of 5HT is inferred
29
Sumatriptan and other "-triptan"s
Rizatriptan Zolmitriptan Naratriptan Almotriptan Eletriptan Frovatriptan Tx: Migraine Mech: 5HT _receptor agonist_ Route: Orally as spray Not to be used w/ SSRIs or MAO inh--will lead to synergistic effect→_5HT syndrome_→malignant hyperthermia like syndrome
30
"-ergotamine"s
Ergotamine Dihydroergotamine Tx: Migrane Mech: _Partial_ 5HT receptor agonist Can affect adrenergic and dopaminergic receptors Useful in initial stages SE: * Ergotism=excess of ergot alkaloids→St. Anthony's Fire * Hallucinations (these are the source of LSD) * Uterine contractions-_preg. category X_ * Severe vasospasm→gangrene (loss of O2 to periphery * ​Not as safe as triptans

Pharm 4 (9 decks)

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