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Pharm exam 2 > Autacoids > Flashcards

Autacoids Flashcards

1
Q

H1-mediated effects

A

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

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2
Q

H2-mediated effects

A

Gastric acid secretion

Positive inotropic effect and increased heart rate

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3
Q

H3-mediated effects

A

Inhibiting release of histamine, serotonin, norepinephrine, and acetylcholine

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4
Q

H1 antagonists 1st generation

A 
Ehylenediamines
Ethanolamines
Alkylamines
Piperazines
Phenothiazines
Methyl piperidines
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5
Q

H1 antagonists 2nd generation

A

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

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6
Q

Pharmacokinetics of H1 antagonists

A

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

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7
Q

Therapeutic uses of H1 antagonists

A

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

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8
Q

Side effects of H1 antagonists

A

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

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9
Q

H2 antagonist drugs

A

Cimetidine
Ranitidine
Famotidine
Nizatidine

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10
Q

MOA of H2 antagonists

A

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

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11
Q

Uses of H2 antagonists

A

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

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12
Q

Serotonin (5-HT) Agonist drugs

A 
Cisapride
Fluoxetine
Cyproheptadine
Ondansetron
Metoclopramide
Mirtazapine
Trazodone
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13
Q

Cisapride

  • MOA
  • Use
A

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

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14
Q

Fluoxetine

-MOA

A

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

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15
Q

Fluoxetine

-Clinical use

A

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

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16
Q

Fluoxetine

-Side effects

A

5-HT Agonist

Nausea, anorexia, irritability, and sleeping disturbances

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17
Q

Cyproheptadine

-MOA

A

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

18
Q

Cyproheptadine

-Uses

A

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

19
Q

Ondansetron

  • MOA
  • Use
A

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

20
Q

Metoclopramide

  • MOA
  • Use
A

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

21
Q

Mirtazapine

-MOA

A

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
Q

Mirtazapine

-Use

A

5-HT Agonist
Antidepressant
Antimetic

23
Q

Trazadone

-MOA

A

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
Q

Trazadone

-Uses

A

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
Q

Trazadone

-Side effects

A

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
Q

Neuokinins Antagonists

A

Maropitant citrate

27
Q

Maropitant citrate

-MOA

A

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
Q

Maropitant citrate

-Use

A

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
Q

Renin activity

A

A proteolytic enzyme

Converts angiotensinogen to angiotensin I

30
Q

Stimulation of renin secretion

A

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

31
Q

Inhibition of renin secretion

A 
Angiotensin II
ADH 
Hypertension
Increased reabsorption of sodium
B1-adrenergic blockers
32
Q

Angiotensin II activity

A

A potent vasoconstrictor
Stimulates aldosterone secretion
Inhibits renin release

33
Q

Angiotenisn II Antagonists

A

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

34
Q

Prostaglandins

A 
Misoprostol
Dinoprost tromethamine
Cloprostenol
Fenprostalen
Fluprostenol
Latanoprost
Travoprost
Bimatoprost
35
Q

Misoprostol

  • MOA
  • Use
A 
MOA = A synthetic prostaglandin E1 that causes GI cytoprotection and decreases acid secretion
Use = Given orally as an anti-ulcer drug
36
Q

Fluprostenol

  • MOA
  • Use
A

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

37
Q

Latanoprost, Travoprost, Bimatoprost

  • MOA
  • Use
A

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
Q

Prostaglandin Inhibitors

A

Cyclooxygenase Inhibitors - NSAIDs

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

39
Q

Prostaglandin Antagonist

-Class

A

Galliprant

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

40
Q

Galliprant

  • MOA
  • Use
A

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

41
Q

Janus Kinase (JAK) Inhibitor

  • Drug
  • MOA
A

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

42
Q

Oclacitinib

-Use

A

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

Pharm exam 2 (12 decks)

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