Autocoids (Ex2) Flashcards
1
Q
What are four autocoids?
A
Histamine
Serotonin
Prostaglandins
Peptides
2
Q
What induces histamine release?
A
- physical injury
- insect stings and reptile venom
- allergy and anaphylaxis
- disease
- drugs and chemicals
3
Q
What are four drugs that inhibit histamine release?
A
- Cromolyn sodium
- Catecholamines
- Phosphodiesterase inhibitors
- Glucocorticoids
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
5
Q
Major H2-Mediated Effects
A
- gastric acid secretion
- positive inotropic effect and increased heart rate
6
Q
Major H3-Mediated Effects
A
- inhibiting release of histamine, serotonin, norepinephrine, and acetylcholine
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
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
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
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)
11
Q
Side Effects of H1-Antagonists
A
- first gen causes sedation
- anticholinergic effect (atropine-like)
- GI irritation
- alpha adrenergic blocking effect
- cardiac arrhythmias
12
Q
What are 4 H2-Antagonist Drugs?
A
- Cimetidine
- Ranitidine
- Famotidine
- Nizatidine
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
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)
15
Q
Cisapride
classification, uses
A
- 5-HT4 receptor agonist in enteric neurons
- stimulates GI motility and secretions
- used as a prokinetic
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
What inhibits Renin secretion?
- angiotensin 2
- ADH
- hypertension
- increased reabsorption of sodium
- B1 blockers
26
Describe the synthesis of prostaglandins
- 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
Misoprostol
| MOA and use
- a synthetic prostaglandin E1 that causes GI cytoprotection and decreases acid secretion
- given orally as an anti-ulcer drug
28
Fluprostenol
| MOA, use
- prostaglandin F2alpha
- causes luteolysis
- stimulates motility of repro tract
- used in reproduction
29
Bimatoprost
| MOA, use
- 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
What are NSAIDs?
| What are corticosteroids?
NSAIDs: COX inhibitors
Cort: phospholipase A2 inhibitors (also COX2)
31
Galliprant
| classification, MOA, use
- non-COX inhibiting NSAID in the piprant family
- selective PGE2 EP4 receptor antagonist
- osteoarthritis pain and inflammation in dogs
32
Oclacitinib (Apoquel)
| classification, MOA, use
- 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
