Autacoids Flashcards

1
Q

What are the 4 autacoids

A

Histamine
Serotonin
Prostaglandins
Peptides

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2
Q

What drugs inhibit histamine release

A

Cromolyn sodium
Catecholamines
Phosphodiesterase inhibitors
Glucocorticoids

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3
Q

Major H1 Mediated Effects on Vessels and Smooth Muscle

A

Contraction of smooth muscles of: GI, bronchioles, uterus, Large blood vessels
Vasodilation followed by contraction leading to increased permeability, edema, hypotension and hypovolemic shock

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4
Q

Other H1 Mediated Effects

A

Stimulation of exocrine secretion
Positive inotropic effect
CNS stimulation, inhibition of appetite

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5
Q

Major H2 Mediated Effects

A

Gastric acid secretion

Positive inotropic effect and increased heart rate

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6
Q

H1 antagonists are __

A

Antihistamines

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7
Q

H1 Antagonists - First Generation Characteristics

A

Crosses BBB

Sedating

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8
Q

H1 Antagonists First Generation Drugs

A
Diphenydramine
Promethazine
Cyproheptadine
Terfenadine
Meclizine
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9
Q

H1 Antagonists Second Generation Characteristics

A

Non-sedating
Does not cross BBB
More receptor selectivity

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10
Q

What do some second generation antagonists exhibit

A

non-competitive antagonism

anti-inflammatory effects by stabilizing mast cells

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11
Q

Second generation drugs

A

Piperidines (Terfenadine, astemizole, loratadine)

Ketotifen (noncompetitive H1 agntagonist)

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12
Q

Do first or second generation drugs have a longer duration of action

A

Second generation (12-24 hrs)

**First generation is 3-12 hrs

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13
Q

H1 Antagonists are readily absorbed ___

A

Orally

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14
Q

H1 Antagonists are metabolized by ___ and excreted by ___

A

Metabolized by the liver and excreted in the urine

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15
Q

Which H1 drug is used as an antiemetic, antitussive and sedative

A

Diphenhydramine

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16
Q

Which H1 drug is available as opthalmic for treatment of allergic conjunctivitis and orally as adjunctive for asthma prevention

A

Ketotifen

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17
Q

Side effects of H1 Antagonists

A

Anticholinergic effect
GI irritation
Alpha adrenergic block (phenothiazines)

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18
Q

Which two H1 Antagonists are associated with Cardiac Arrhythmias

A

Terfenadine and Astemizole

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19
Q

What are the H2 Antagonist drugs

A

Cimetidine
Ranitidine
Famotidine
Nizatidine

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20
Q

Do H2 Antagonists cross the BBB

A

NO

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21
Q

Cimetidine effects

A

Immunomodulatory
Inhibits suppressor T cells
Enhances cell mediated immunity

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22
Q

Ranitidine and Nizatidine effects

A

Cholinergic activity by inhibiting acetyl cholinesterase –> stimulates GI motility

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23
Q

Uses for H2 Antagonists

A

Peptic Ulcer
Gastric erosive disease
Gastroesophageal reflux disease
Duodenal ulcer

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24
Q

Cimetidine is used in the treatment of equine ____

A

Melanoma

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25
Ranitidine or Nizatidine can be used as a ___
Prokinetic
26
Cisapride Mechanism of Action
5-HT4 receptor agonist in enteric neurons
27
Cisapride is a ___ and acts on ___
Prokinetic | Small and Large intestine
28
Fluoxetine Mechanism of Action
Selective Serotonin reuptake inhibitor - antidepressant | Increases serotonin levels in the brain
29
Fluoxetine Clinical Uses
Canine separation anxiety Behavioral disorders in dogs and cats Inappropriate elimination in cats
30
Side effects of Fluoxetine
Nausea Anorexia Irritability Sleeping disturbances
31
Cyproheptadine Mechanism of Action
Blocks H1 Receptors, serotonin receptors | Inhibition of serotonin inhibits ACTH
32
Uses for cyproheptadine
Antihistamine Appetite stimulant in small animals Serotonin Syndrome in dogs and cats
33
Ondansetron Mechanism of Action
5-HT3 Receptor Antagonist (central and peripheral)
34
Use for Ondansetron
Prevention and treatment of anticancer chemotherapy induced nausea and vomiting
35
Metoclopramide Mechanism of Action
5-HT3 Receptor Antagonist | D1 and D2 receptor antagonist
36
Uses of Metoclopramide
Antiemetic | Prokinetic
37
Mirtazapine Mechanism of Action
Enhances noradrenergic and serotonergic activity by antagonizing central presynaptic alpha2 adrenergic inhibitory autoreceptors and heteroceptors Potent antagonist of 5-HT2 and 5-HT3 receptors
38
Mirtazapine uses
Antidepressant | Antiemetic
39
Serotonin Antagonists
Cyproheptadine Ondansetron Metoclopramide Mirtazapine
40
Neurokinin Antagonist
Maropitant Citrate
41
Maropitant Citrate Mechanism of Action
Blocks Neurokinin 1 receptors preventing substance P from binding --> antiemetic (pain, stress, anxiety, psychologic stress/vomiting)
42
Maropitant Citrate Uses
Only used in dogs over 16 wks | Tablet or injection for prevention of acute vomiting due to motion sickness
43
Where is renin secreted from and what does it do
Juxtaglomerular apparatus | Converts angiotensinogen to angiotensin 1
44
What stimulates the release of renin
Hypotension, decreased renal blood flow, low Na or Cl, sympathetic stimulation (B1 adrenergic)
45
What inhibits renin secretion
Angiotensin 2, ADH, Hypertension, Increased Na reabsorption, B1 Adrenergic blockers
46
What does Angiotensin 2 do
Potent Vasocontrictor, Stimulates aldosterone secretion, inhibits renin
47
Angiotensin 2 Antagonists
ACE Inhibitors | Angiotensin 2 Receptor Antagonists - Losartan
48
Prostaglandins
Misoprostol Fluprostenol Bimatoprost
49
Misoprostol Mechanism of Action
Causes GI cytoprotection and decreases acid secretion
50
Misoprostol use
Given orally as an anti ulcer drug
51
Fluprostenol Mechanism of Action
Causes luteolysis | Stimulates motility of the smooth muscles of repro. tract
52
Fluprostenol use
Reproduction
53
Bimatoprost Mechanism of Action
PG agonist - increases uveoscleral outflow by stimulating FP receptors in the eye
54
Bimatoprost use
Topically on eye in treatment of open-angle glaucoma or ocular hypertension
55
Prostaglandin Inhibitors
Cyclooxygenase Inhibitors - NSAIDS | Phospholipase A2 Inhibitors - Corticosteroids
56
Leukotrienes Inhibitors
Zafirlukast, Zileuton
57
Zafirlukast Mechanism of Action
Leukotriene receptor antagonists
58
Zafirlukast use
Prevention of bronchoconstriction in bronchial asthma in cats
59
Zileuton Mechanism of Action
5-Lipoxygenase inhibitor (leukotriene formation inhibition)
60
Zileuton use
Prevention of bronchoconstriction in bronchial asthma
61
What is Oclacitinib
Janus Kinase Inhibitor
62
Oclacitinib Mechanism of Action
Inhibits pruritogenic and pro-inflammatory cytokines by inhibiting JAK1 and JAK3 without inhibiting cytokines involved with hematopoiesis (JAK2)
63
Oclacitinib use
Control of pruritis associated with allergic dermatitis and atopic dermatitis (dogs over 12 months)