Autocoids (Ex2) Flashcards

1
Q

What are four autocoids?

A

Histamine
Serotonin
Prostaglandins
Peptides

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2
Q

What induces histamine release?

A
  • physical injury
  • insect stings and reptile venom
  • allergy and anaphylaxis
  • disease
  • drugs and chemicals
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3
Q

What are four drugs that inhibit histamine release?

A
  • Cromolyn sodium
  • Catecholamines
  • Phosphodiesterase inhibitors
  • Glucocorticoids
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4
Q

Major H1-Mediated Effects

A
  • contraction of smooth muscles of GI, bronchioles, uterus, and large blood vessels
  • vasodilation of vessels, then contraction, leading to increased permeability, edema, hypotension, and hypovolemic shock
  • 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

Major H3-Mediated Effects

A
  • inhibiting release of histamine, serotonin, norepinephrine, and acetylcholine
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7
Q

First Generation H1-Antagonists

effects, examples

A
  • cross blood-brain barrier, so cause sedation
  • anti-cholinergic effects
  • Ehylenediamines, Ethanolamines, Alkylamines, Piperazines, Phenothiazines, Methyl piperidines
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8
Q

Second Generation H1-Antagonists

features, effects, examples

A
  • non-sedating, do not cross BBB
  • more receptor selectivity
  • anti-inflammatory effects by stabilizing mast cells
  • less anti-cholinergic
  • piperidines, ketotifen
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9
Q

Pharmacokinetics of H1-Antagonists

A
  • readily absorbed orally
  • wide distribution
  • duration is 3-12 hours
  • metabolized by liver
  • excreted in urine
  • most are enzyme inducers
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10
Q

Therapeutic uses of H1-Antagonists

A
  • allergy and anaphylaxis (not effective if histamine is already released, more preventative)
  • anti-motion sickness (only 1st gen)
  • Ketotifen used to treat allergic conjunctivitis, and prevention of asthma
  • Not effective in bronchial asthma (must use beta-2 agonist)
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11
Q

Side Effects of H1-Antagonists

A
  • first gen causes sedation
  • anticholinergic effect (atropine-like)
  • GI irritation
  • alpha adrenergic blocking effect
  • cardiac arrhythmias
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12
Q

What are 4 H2-Antagonist Drugs?

A
  • Cimetidine
  • Ranitidine
  • Famotidine
  • Nizatidine
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13
Q

H2-Antagonist MOA

A
  • competitive antagonist to H2 receptors (reduces gastric acid output)
  • Cimetidine has immunomodulatory effects: inhibits suppressor T cells and enhances cell-mediated immunity
  • Ranitidine and Nizatidine inhibit acetyl cholinesterase, stimulating GI motility
  • do not cross BBB
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14
Q

Therapeutic uses of H2-Antagonists

A
  • peptic or duodenal ulcer
  • gastric erosive disease
  • gastroesophageal relfux disease
  • Cimetidine: equine melanoma
  • Ran or Niz: use as prokinetic (stimulate GI motility)
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15
Q

Cisapride

classification, uses

A
  • 5-HT4 receptor agonist in enteric neurons
  • stimulates GI motility and secretions
  • used as a prokinetic
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16
Q

Fluoxetine

classification, MOA, uses, side effects

A
  • selective serotonin re-uptake inhibitor
  • acts by increasing serotonin levels in the brain
  • trtmt of canine separation anxiety
  • in dogs and cats for other behavioral disorders
  • trtmt in cats with inappropriate elimination and marking
  • side effects: nausea, anorexia, anxiety, irritability, sleeping disturbances
17
Q

Cyproheptadine

classification, MOA, uses

A
  • serotonin antagonist
  • blocks H1-receptors and serotonin receptors
  • inhibition of serotonin inhibits ACTH
  • anti-histamine
  • stimulate appetite in small animals
  • trtmt of serotonin syndrome in dogs and cats
18
Q

Ondansetron (Zofran)

classification, use

A
  • 5-HT3 receptor antagonist

- prevention and trtmt of anti-cancer chemotherapy-induced nausea and vomiting

19
Q

Metoclopramide

classification, uses

A
  • 5-HT3 receptor antagonist
  • D1 and D2 receptor antagonist
  • antiemetic
  • prokinetic
20
Q

Mirtazapine

classification, MOA, uses

A
  • tricyclic antidepressant
  • antagonist of 5-HT2 and 5-HT3 receptors
  • enhances noradrenergic and serotonergic activity by antagonizing central presynaptic alpha 2 inhibitory autoreceptors and heteroreceptors
  • antidepressant, antiemetic
21
Q

Trazodone

classification, MOA, uses

A
  • antidepressant in humans
  • serotonin antagonist re-uptake inhibitor
  • blocks 5-HT2a and alpha1 receptors
  • inhibits re-uptake of serotonin by blocking SERTt
  • increases serotonin levels in the brain
  • extra-label in dogs/cats to treat behavioral disorders (anxiety)
22
Q

Trazodone Side Effects

A
  • vomiting, diarrhea, lethargy, sedation, hyperactivity, shaking, and agitation
  • can cause priapism in humans, so used with caution in male breeding dogs
  • large doses may cause seizures
23
Q
Maropitant Citrate (Cerenia)
(classification, MOA, use)
A
  • neurokinin antagonist
  • blocks neurokinin 1 receptors, preventing substance P from binding, resulting in antiemetic effect
  • only in dogs as tablets or injection for prevention of acute vomiting due to motion sickness
  • possible in treating vomiting due to viral infections or chemo
24
Q

What stimulates Renin secretion?

A
  • hypotension
  • decreased renal blood flow
  • low Na or Cl in blood
  • sympathetic stimulation (B1 receptors)
25
Q

What inhibits Renin secretion?

A
  • angiotensin 2
  • ADH
  • hypertension
  • increased reabsorption of sodium
  • B1 blockers
26
Q

Describe the synthesis of prostaglandins

A
  • membrane phospholipids converted to arachidonic acid by phospholipase A2
  • arachidonic acid converted to leukotrienes by lipooxygenase, or to prostaglandins by COX-1 and COX-1
27
Q

Misoprostol

MOA and use

A
  • a synthetic prostaglandin E1 that causes GI cytoprotection and decreases acid secretion
  • given orally as an anti-ulcer drug
28
Q

Fluprostenol

MOA, use

A
  • prostaglandin F2alpha
  • causes luteolysis
  • stimulates motility of repro tract
  • used in reproduction
29
Q

Bimatoprost

MOA, use

A
  • prostaglandin agonist that increases uveoscleral outflow by stimulating FP receptors in the eye
  • topically on the eye in trtmt of open angle glaucoma or ocular hypertension
30
Q

What are NSAIDs?

What are corticosteroids?

A

NSAIDs: COX inhibitors
Cort: phospholipase A2 inhibitors (also COX2)

31
Q

Galliprant

classification, MOA, use

A
  • non-COX inhibiting NSAID in the piprant family
  • selective PGE2 EP4 receptor antagonist
  • osteoarthritis pain and inflammation in dogs
32
Q

Oclacitinib (Apoquel)

classification, MOA, use

A
  • Janus kinase inhibitor
  • inhibits pruritogenic and pro-inflammatoru cytokines by inhibiting JAK1 and JAK3
  • for control of pruritis associated with allergic dermatitis and atopic dermatitis in dogs