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
Q

Ranitidine or Nizatidine can be used as a ___

A

Prokinetic

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26
Q

Cisapride Mechanism of Action

A

5-HT4 receptor agonist in enteric neurons

27
Q

Cisapride is a ___ and acts on ___

A

Prokinetic

Small and Large intestine

28
Q

Fluoxetine Mechanism of Action

A

Selective Serotonin reuptake inhibitor - antidepressant

Increases serotonin levels in the brain

29
Q

Fluoxetine Clinical Uses

A

Canine separation anxiety
Behavioral disorders in dogs and cats
Inappropriate elimination in cats

30
Q

Side effects of Fluoxetine

A

Nausea
Anorexia
Irritability
Sleeping disturbances

31
Q

Cyproheptadine Mechanism of Action

A

Blocks H1 Receptors, serotonin receptors

Inhibition of serotonin inhibits ACTH

32
Q

Uses for cyproheptadine

A

Antihistamine
Appetite stimulant in small animals
Serotonin Syndrome in dogs and cats

33
Q

Ondansetron Mechanism of Action

A

5-HT3 Receptor Antagonist (central and peripheral)

34
Q

Use for Ondansetron

A

Prevention and treatment of anticancer chemotherapy induced nausea and vomiting

35
Q

Metoclopramide Mechanism of Action

A

5-HT3 Receptor Antagonist

D1 and D2 receptor antagonist

36
Q

Uses of Metoclopramide

A

Antiemetic

Prokinetic

37
Q

Mirtazapine Mechanism of Action

A

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
Q

Mirtazapine uses

A

Antidepressant

Antiemetic

39
Q

Serotonin Antagonists

A

Cyproheptadine
Ondansetron
Metoclopramide
Mirtazapine

40
Q

Neurokinin Antagonist

A

Maropitant Citrate

41
Q

Maropitant Citrate Mechanism of Action

A

Blocks Neurokinin 1 receptors preventing substance P from binding –> antiemetic (pain, stress, anxiety, psychologic stress/vomiting)

42
Q

Maropitant Citrate Uses

A

Only used in dogs over 16 wks

Tablet or injection for prevention of acute vomiting due to motion sickness

43
Q

Where is renin secreted from and what does it do

A

Juxtaglomerular apparatus

Converts angiotensinogen to angiotensin 1

44
Q

What stimulates the release of renin

A

Hypotension, decreased renal blood flow, low Na or Cl, sympathetic stimulation (B1 adrenergic)

45
Q

What inhibits renin secretion

A

Angiotensin 2, ADH, Hypertension, Increased Na reabsorption, B1 Adrenergic blockers

46
Q

What does Angiotensin 2 do

A

Potent Vasocontrictor, Stimulates aldosterone secretion, inhibits renin

47
Q

Angiotensin 2 Antagonists

A

ACE Inhibitors

Angiotensin 2 Receptor Antagonists - Losartan

48
Q

Prostaglandins

A

Misoprostol
Fluprostenol
Bimatoprost

49
Q

Misoprostol Mechanism of Action

A

Causes GI cytoprotection and decreases acid secretion

50
Q

Misoprostol use

A

Given orally as an anti ulcer drug

51
Q

Fluprostenol Mechanism of Action

A

Causes luteolysis

Stimulates motility of the smooth muscles of repro. tract

52
Q

Fluprostenol use

A

Reproduction

53
Q

Bimatoprost Mechanism of Action

A

PG agonist - increases uveoscleral outflow by stimulating FP receptors in the eye

54
Q

Bimatoprost use

A

Topically on eye in treatment of open-angle glaucoma or ocular hypertension

55
Q

Prostaglandin Inhibitors

A

Cyclooxygenase Inhibitors - NSAIDS

Phospholipase A2 Inhibitors - Corticosteroids

56
Q

Leukotrienes Inhibitors

A

Zafirlukast, Zileuton

57
Q

Zafirlukast Mechanism of Action

A

Leukotriene receptor antagonists

58
Q

Zafirlukast use

A

Prevention of bronchoconstriction in bronchial asthma in cats

59
Q

Zileuton Mechanism of Action

A

5-Lipoxygenase inhibitor (leukotriene formation inhibition)

60
Q

Zileuton use

A

Prevention of bronchoconstriction in bronchial asthma

61
Q

What is Oclacitinib

A

Janus Kinase Inhibitor

62
Q

Oclacitinib Mechanism of Action

A

Inhibits pruritogenic and pro-inflammatory cytokines by inhibiting JAK1 and JAK3 without inhibiting cytokines involved with hematopoiesis (JAK2)

63
Q

Oclacitinib use

A

Control of pruritis associated with allergic dermatitis and atopic dermatitis (dogs over 12 months)