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Pharmacology Test 3 > Antihistamines and Autocoids (Londono) > Flashcards

Antihistamines and Autocoids (Londono) Flashcards

1
Q

Autocoids

A

Biological factors

Act like hormones, but act locally

Short duratio of action

Not carried in blood

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2
Q

How are autocoids released

A

Response to

  • Trauma
  • Dust mites
  • Fungus
  • Mold
  • Sunlight
  • Chemicals
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3
Q

Autacoid classes

A
  1. Eicosanoids: mediate inflammatory processes
  • Prostaglandins
  • Leukotrienes
  • Thromboxane
  1. Polypeptides
  • Angiotensin
  • Kinins
  • Substance P (modulate inflamm in human medicine)
  1. Decarboxylated Amino Acids
  • Histamine
  • Serotonin
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4
Q

Histamine:

Synthesis

Metabolism

Effects

A

Synthesized in

  • Mast cells
  • Basophils
  • ECL cells
  • CNS: neurotransmitter

​Metabolized in Liver by oxidation

Mediates

  • inflammation
  • anaphylaxis
  • gastric acid secretion
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5
Q

H1 receptors mostly responsible for

A

Vasodilation

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6
Q

Tissue: Vascular smooth muscle

Effect:

Clinical Signs:

Receptor:

A

Effect:

  • venule/arteriole dilation
  • venoconstriction

Clinical signs:

  • Erythema

Receptor:

  • H1
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7
Q

Tissue: Airway

Effect:

Clinical Signs:

Receptor:

A

Effect:

  • Bronchoconstriction
  • Increased secretion
  • Mucosal edema

Clinical Signs:

  • Asthma
  • Reflex irritation
  • Coughing/sneezing

Receptor:

  • H1
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8
Q

Tissue: Vascular endothelium

Effect:

Clinical Signs:

Receptor:

A

Effect:

  • Contraction and separation

Clinical Signs:

  • Edema
  • Wheel response

Receptor:

  • H1
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9
Q

Tissue: Peripheral nerves

Effect:

Clinical Signs:

Receptor:

A

Effect:

  • Sensitization

Clinical Signs:

  • Itch
  • Pain

Receptor

  • H1
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10
Q

Tissue: Heart

Effect:

Clnical signs:

Receptor:

* not well described don’t pay much attention

A

Effect:

  • Inc in heart rate and contractility

Clinical Signs:

  • Tacycardia

Receptor:

  • H2
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11
Q

Tissue: Stomach

Effect:

Clinical Signs:

Receptor:

A

Effect:

  • Inc acid secretion

Clinical signs:

  • Ulceration

Receptor:

  • H2
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12
Q

Tissue: CNS

Effect:

Clinical Signs:

Receptor:

A

Effect:

  • Neurotransmitter

Clinical signs:

  • Circadian rhythm

Receptor

  • H3
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13
Q

H1 Antihistamines

!st and 2nd gen

A

1st

  • Allergy meds that cause drowsiness: cross the BBB
  • Lipophilic

2nd

  • Allergy meds that don’t cross the BBB
  • Not lipophilic

Use

  • Allergy
  • dermatitis
  • nausea: CRTZ

Limited role

  • asthma: don’t reach brochial tree?
  • anaphylaxis: no great effect
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14
Q

Diphenhydramine

A

1st gen H1 Antihistamine

use

  • acute allergic reaction
  • antipruritic
  • prevent reactions (vaccines, chemo)
  • motion sickness
  • mast cell tumor

crosses blood brain barrier

Adverse effects

  • CNS
  • anticholinergic
    • dry mouth
    • retention of urine
    • inc secretion in gut
    • inc secretion in lungs
  • Cants can be hyper
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15
Q

Cyproheptadine

A

H1-Antihistamine

Acts on

  • Serotonin
    • appetite stimulant
  • Alpha-receptors
  • histamine

1st generation

NOT VERY ANTIHISTAMINIC: not for itchy dogs

Horses

  • head shaking
  • cushings (not first choice)

Adverse effects

  • CNS
  • Anticholinergic
  • Cats may get excited
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16
Q

Meclizine (antivert)

A

1st genereation H1 Antihistamine

Motion sickness

Vestibular dz: helps with the motion sickness, not dz

MOA:partially understood, CTZ

17
Q

Other H1-blockers

A

1st generation

  • Promethazine: pruritic patient
  • Hydroxyzine (Atarax)

Second generation

  • Cetirizine (Zyrtec)
18
Q

H2-Antihistamines

A

Reversible competitive antagonists

Gastric Parietal Cells

Reduce gastric acid secretion

  • Famotidine
  • Ranitidine
  • Cimetidine
  • Nizatidine
19
Q

Famotidine (Pepcid)

A

Most potent and longest half-life

First pass hepatic metabolism

No prokinetic or antiemetic activity

Side effects uncommon

No prokinetic or antiemetic effect

20
Q

H3 and H4 Antihistamines

A

Not approved for clinical use

Experimental models

Improve attention and wakefulness

21
Q

Serotonin (5-HT)

A

Synthesized from Tyrptophan

Found in

  • GI (ECL cells)
  • CNS
  • Platelets

Serotonergic projections

  • Spinal cord
    • pain
    • inflammation
    • motor function
  • Forebrain
    • mood
    • state of alertness
22
Q

Serotonin Overdose

A

Neuro signs

  • seizures
  • depression
  • tremors
  • hyperesthesia
  • ataxia

GI signs

  • vomiting
  • diarrhea
  • abdominal pain
  • hypersalivation

Other

  • hyperthermia
  • blindness
23
Q

Pharmacology

A

MAOIs

Amphetamines

  • make vesicles less likely to store serotonin

SSRIs

  • decrease reuptake of serotonin into presynaptic cleft

TCAs

  • decreases degradation of serotonin
24
Q

Amphetamines

A

Inhibitors of serotonin storage

Displaces 5-HT, domapine and norepinephrine from storage vesicles

In humans used for depression and ADHD

*No application in vet med

25
Q

Monoamine Oxidase Inhibitors

A

Inhibitors of serotonin degradation

Two types

  • MAOI-a
  • MAOI-b

Reversible vs irreversible

26
Q

Selegiline (anypril)

A

Selective MAOI-b, MAOI-a at high doses

TX of canine cognitive dysfunction

Inc dopamine activity

Cushings dz +/- 20%

Adverse effects

  • GI signs
  • CNS
27
Q

Cushings

A

Inc ACTH

28
Q

Reuptake Inhibitors

A

Net inc in extracellular 5-HT

Used for TX of anxiety, depression and OCD

Four main classes

  • TCAs
  • SSRIs
  • SNRIs
  • NRIs
29
Q

Clomipramine (Clomicalm)

A

Tricyclic antidepressant

Only FDA approved drug (dogs)

TX

  • OCD
  • Anxiety
  • Dominance
  • Aggression

Side effects

  • change in behavior
30
Q

Fluoxetine (prozac)

A

Selective-serotonin reuptake inhibitor

FDA approved in dogs for TX of separation anxiety in conjuction with behavior modification plan

Adverse effects

  • anorexia
  • seizures
31
Q

Mirtazapine

A

Atypical antidepressant

5-HT2 and 5-HT3 inhibitor

Central alpha-2 receptor inhibitor (net inc NE)

Appetite stimulant

Antiemetic

Adverse effects

  • drowsiness/sedation
  • voalization
  • tachycardia
32
Q

Trazadone

A

5-HT2 inhibitor and SSRI

Adjuctive anxiolytic

TX of hospitalization-related anxiety and post-op recovery

Adverse effects:

  • GI signs
  • ataxia
  • hypotension

Less cardiovascular effects

33
Q

Cisapride

A

5-HT4 agonist

Enhances acetylcholine release

Prokinetic

TX of

  • GI stasis
  • reflux esophagitis
  • constipation/megacolon (cats)

Adverse effects: well tolerated

34
Q

Ondansetron (zofran)

A

Serotonin receptor agonist

Potent antiemetic

Receptors in vagal nerve terminals and CTZ

Controversial use in cats

Well tolerated in dogs

Pharmacology Test 3 (12 decks)

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