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Pharm 4 > Biogenic Amines > Flashcards

Biogenic Amines Flashcards

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

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

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

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

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

A

“-tidine”s

Cimetidine

Ranitidine

Famotidine

Nizatidine

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

21
Q

Cimetidine

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

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

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

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
Q

Serotonin synth

A

Tryptophan→→5-hydroxytryptamine (5HT)

Found in enterochromaffin cells of gut

26
Q

Physiologic effects of 5HT

A
  • Smooth mm constriction
    • Sero=serum
    • Tonin=tone (mm constriction)
  • Itching, pain
  • Neurotransmission
  • Nausea
27
Q

Carcinoid syndrome

A

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

Cutaneous flushing

Asthmatic bronchospasm

Right valve fibrosis

Pellegra

Enterochrommafin cells

Diarrhea

No CNS effects

28
Q

Migraine headaches

A

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
Q

Sumatriptan

and other “-triptan”s

A

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
Q

“-ergotamine”s

A

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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