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Flashcards in Autacoids Deck (42):
1

H1-mediated effects

Contraction of the smooth muscles of the GI, bronchioles, uterus, and large blood vessels
Vasodilation of capillaries, arterioles, and venules then contraction leading to increased permeability, edema, hypotension, and hypovolemic shock
Positive inotropic effect
Stimulation of exocrine secretion

2

H2-mediated effects

Gastric acid secretion
Positive inotropic effect and increased heart rate

3

H3-mediated effects

Inhibiting release of histamine, serotonin, norepinephrine, and acetylcholine

4

H1 antagonists 1st generation

Ehylenediamines
Ethanolamines
Alkylamines
Piperazines
Phenothiazines
Methyl piperidines

5

H1 antagonists 2nd generation

Non-sedating, more receptor selectivity, some exhibit non-competivtive antagonism, antiinflammatory effects by stabilizing mast cells
Piperidines
Ketotifen

6

Pharmacokinetics of H1 antagonists

Readily absorbed orally
Wide distribution including the brain, except the 2nd generation
Metabolized by liver and excreted in urine
Most are enzyme inducers

7

Therapeutic uses of H1 antagonists

Allergy and anaphylaxis
Antimotion sickness
Ketotifen is available as ophthalmic for treatment of allergic conjunctivitis, and orally as adjunctive for prevention of asthma

8

Side effects of H1 antagonists

1st generation causes sedation
Anticholinergic effect
Gastrointestinal irritation
Alpha-adrenergic blocking effect

9

H2 antagonist drugs

Cimetidine
Ranitidine
Famotidine
Nizatidine

10

MOA of H2 antagonists

Competitive antagonists to H2 receptors
Cimedtidine has immunomodulatory effects including inhibiting suppressor T cells and enhancing cell-mediated immunity
Ranitidine and Nizatidie, not Cimetidine or Famotidine, have cholinergic activity by inhibiting acetyl cholinesterase, stimulating gastrointestinal motility

11

Uses of H2 antagonists

Peptic ulcer
Gastric erosive disease
Gastroesophageal reflux disease
Duodenal ulcer
Cimetidine is used in the treatment of equine melanoma (as immunomodulator)
Ranitidine and Nizatidine can be used as prokinetic

12

Serotonin (5-HT) Agonist drugs

Cisapride
Fluoxetine
Cyproheptadine
Ondansetron
Metoclopramide
Mirtazapine
Trazodone

13

Cisapride
-MOA
-Use

5-HT Agonist
MOA = 5-HT4 recptor agonist in enteric neurons
Use = prokinetic (stimulates GI motility)

14

Fluoxetine
-MOA

5-HT Agonist
Selective serotonin reuptake inhibitor (SSRI) antidepresant
Acts by increasing serotonin levels in the brain
Increasing serotonin levels improves signs of depression in humans

15

Fluoxetine
-Clinical use

5-HT Agonist
Approved for treatment of canine separation anxiety in conjunction with a behavior modification plan
Used in dogs and cats to treat behavioral disorders (aggression, obsessive compulsive, anxiety)
Used in treatment of cats with inappropriate elimination and urine marking

16

Fluoxetine
-Side effects

5-HT Agonist
Nausea, anorexia, irritability, and sleeping disturbances

17

Cyproheptadine
-MOA

5-HT Agonist
Blocks H1 receptors
Blocks serotonin receptros
Inhibition of serotonin inhibits ACTh

18

Cyproheptadine
-Uses

5-HT Agonist
Antihistamine
Stimulate appetite in small animals
Treatment of "serotonin syndrome" in dogs and cats

19

Ondansetron
-MOA
-Use

5-HT Agonist
MOA = 5-HT3 receptor antagonist (central and peripheral)
Use = Prevention and treatment of anticancer chemotherapy-induced nausea and vomiting

20

Metoclopramide
-MOA
-Use

5-HT Agonist
MOA = 5-HT3 receptor antagonist; D1 and D2 receptor antagonist
Use = Antimetic (effective against vomiting and nausea)

21

Mirtazapine
-MOA

5-HT Agonist
A TCA that enhances noradrenergic and serotonergic activity by antagonizing central presynaptic alpha2-adrenergic inhibitory autoreceptors and heteroreceptors
A potent antagonist of 5-HT2 and 5-HT3 receptors

22

Mirtazapine
-Use

5-HT Agonist
Antidepressant
Antimetic

23

Trazadone
-MOA

5-HT Agonist
Serotonin antagonist reuptake inhibitor (SARI)
Blocks 5-HT2A and alpha-adrenergic receptors
Inhibits reuptake of serotonin by blocking SERT (serotonin transporter)
Increases serotonin levels in the brain

24

Trazadone
-Uses

5-HT Agonist
Extra label in dogs and cats for treatment of behavior disorders such as separation anxiety and other anxiety, such as fear of fireworks, and post-surgical cage confinement

25

Trazadone
-Side effects

5-HT Agonist
Vomiting, diarrhea, lethargy, sedation, hyperactivity shaking, and agitation
Used with caution in male breeding dogs because it can cause priapism (prolong erection) in humans
Large doses may cause seizures

26

Neuokinins Antagonists

Maropitant citrate

27

Maropitant citrate
-MOA

Neuokinin Antagonist
The neuropeptide (tachykinin) substance P (SP) is involved in integration of pain, stress, anxiety, psychologic stress, and vomiting
Maropitant blocks neuokinin 1 (NK1) receptors preventing substance P from binding resulting in antiemetic effect

28

Maropitant citrate
-Use

Neuokinin Antagonist
Used only in dogs (over 16 weeks of age) as tablets or injection for the prevention of acute vomiting due to motion sickness and may be effective in treating vomiting due to viral infections and anticancer chemotherapy

29

Renin activity

A proteolytic enzyme
Converts angiotensinogen to angiotensin I

30

Stimulation of renin secretion

Hypotension
Decreased renal blood flow
Low Na of Cl in the blood
Sympathetic stimulation (B1-adrenergic receptors)

31

Inhibition of renin secretion

Angiotensin II
ADH
Hypertension
Increased reabsorption of sodium
B1-adrenergic blockers

32

Angiotensin II activity

A potent vasoconstrictor
Stimulates aldosterone secretion
Inhibits renin release

33

Angiotenisn II Antagonists

ACE Inhibitors = Captopril, Enalapril, Lisinopril, Benazepril
Angiotensin II-receptor antagonists = Losartan (blocks Angiotensin II type 1 receptors)

34

Prostaglandins

Misoprostol
Dinoprost tromethamine
Cloprostenol
Fenprostalen
Fluprostenol
Latanoprost
Travoprost
Bimatoprost

35

Misoprostol
-MOA
-Use

MOA = A synthetic prostaglandin E1 that causes GI cytoprotection and decreases acid secretion
Use = Given orally as an anti-ulcer drug

36

Fluprostenol
-MOA
-Use

Prostaglandin
MOA = cause leuteolysis; stimulate motility of the smooth muscles of the reproductive tract
Use = in reproduction

37

Latanoprost, Travoprost, Bimatoprost
-MOA
-Use

Prostaglandins
MOA = PG agonists that increase uveoscleral outflow by stimulating FP receptors in the eye
Use = used topically on the eye in the treatment of open-angle glaucoma or ocular hypertension

38

Prostaglandin Inhibitors

Cyclooxygenase Inhibitors - NSAIDs
Phospholipase A2 Inhibitors - Corticosteroids (also inhibit COX-2)

39

Prostaglandin Antagonist
-Class

Galliprant
Non-cyclooxygenase (COX) inhibiting, NSAID in the piprant family (prostaglandin receptor antagonist, PRA)

40

Galliprant
-MOA
-Use

Prostaglandin Inhibitor
MOA = Selective PGE2 EP4 receptor antagonist
Use = Osteoarthritis pain and inflammation in dogs

41

Janus Kinase (JAK) Inhibitor
-Drug
-MOA

Oclacitinib
Inhibits pruritogenic and pro-inflammatory cytokines by inhibiting JAK1 and JAK3 without inhibitin cytokines involved in hematopoiesis that are dependent on JAK2

42

Oclacitinib
-Use

Used for the control of pruritus associated with allergic dermatitis and atrophic dermatitis in dogs over 12 months