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Pharm 2 > E2. Autacoids > Flashcards

E2. Autacoids Flashcards

1
Q

What are the 4 groups that are classified as autacoids?

A
  • Histamine
  • Serotonin (5‐HT)
  • Prostaglandins (PGs)
  • Peptides
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2
Q 
Select the drugs that are  serotonin (5 –HT) agonists?(can be more than one)
A. Fluoxetine
B. Ranitidine
C. Ondansetron
D. Cisapride
E. Metoclopramide
A

D. Cisapride
A. Fluoxetine
C and E are antagonists

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3
Q

What does Cisapride act on (MOA), and what is its use?

A

– Mechanism of action
• 5‐HT4 receptor agonist in enteric neurons
– Use
• Prokinetic

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4
Q

How does Fluoxetine work?

A

Acts by increasing serotonin levels in the brain. Increasing those levels improves signs of depression in humans.

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5
Q

What is the clinical use for Fluoxetine?

A

-Approved for treatment of canine separation anxiety in conjunction with a behavior modification plan
• Used in dogs and cats to treat other behavioral disorders such as
aggression, obsessive compulsive behaviors and anxiety
• Used in treatment of cats with inappropriate elimination and urine marking

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6
Q

What are some side effects you will see from Fluoxetine use? (5)

A

Nausea, anorexia, anxiety, irritability, and sleeping disturbances. (More information look at page 267)

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7
Q

What drugs are serotonin (5 – HT) antagonist? (3)

A

Cyproheptadine, Onidasetron, Metroclopramide.

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8
Q

What is the mechanism of action for Cyproheptadine?(3)

A
  • Blocks H1‐receptors
  • Blocks serotonin receptors
  • Inhibition of serotonin inhibits ACTH
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9
Q

What are the three uses for Cyproheptadine?

A
  • Antihistamine
  • To stimulate appetite in small animals
  • In the treatment of “serotonin syndrome” in dogs and cats
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10
Q

What is the mechanism of action for Onidasetron and Metroclopramide?

A

Onidasetron:
• 5‐HT3 receptor antagonist (central and peripheral)

Metroclopramide:
• 5‐HT3 receptor antagonist
• D1 and D2 receptor antagonist

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11
Q

What are the clinical uses for Onidasetron and Metroclopramide?

A

Onidasetron:
• Prevention and treatment of anticancer chemotherapy‐ induced nausea and vomiting

Metroclopramide:
• Antiemetic
• Prokinetic

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12
Q

Look at the slides 1-3/6 for histamine information

A

.

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13
Q

What are the four drugs/groups that generally inhibit histamine release? (4/6)

A

– catecholamines (epinephrine)
– cromolyn sodium
– phosphodiesterases (aminophylline)
– glucocorticoids

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14
Q 
When you inhibit H1 receptors you are blocking which of the following?
A. Inflammation
B. Anaphylaxis
C. Allergies
D. Drug reactions
E. All of the above
A

E. All of the above

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15
Q

What are the H2 receptors required for?

A

Gastric acid secretion

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16
Q

What are the major H1 mediated effects? (4) (slide6-7/6)

A
  • Contraction of smooth muscles (esp. GI, bronchioles, uterus and large vessels classically resulting in bronchoconstriction).
  • Vasodilation and then contraction of small vessels – capillaries, arterioles and venules - which leads to increased permeability (shock, hypotension, edema).
  • Positive inotropic effect.
  • Other effects such as CNS stimulation/alterations in sleep/wake cycles, itching, vomiting and
    inappetence, and local reflex vasodilation.
17
Q

What is the major H2 mediated effect?

A

Gastric acid secretion

18
Q

Look at slides 9 – 10/6. More important just to know that they are H3 and H4 receptors

A

.

19
Q

What drugs are your H1 agonists (first generation)? (10)

A

Pyrilamine(Equiphed®)
Diphenydramine(Benadryl®),
Dimenhydrinate (Dramamine, Gravol®),
Chlorpheniramine(Chlor-trimetron®)

20
Q

Of the 10 first-generation H1 blockers how many are primarily used for something else?

A

3

21
Q 
Which of these drugs are used as appetite  stimulants in cats?
A. Dimenhydrinate (Dramamine, Gravol®)
B. Cyproheptadine(Periactin®)
C. Meclizine(Antivert®)
D. Any of the above can work
E. None of the above work
A

B. Cyproheptadine(Periactin®)

22
Q 
Which of these drugs are used to treat vestibular nausea?
A. Dimenhydrinate (Dramamine, Gravol®)
B. Cyproheptadine(Periactin®)
C. Meclizine(Antivert®)
D. Any of the above can work
E. None of the above work
A

A. Dimenhydrinate (Dramamine, Gravol®)

23
Q 
Which of these drugs are used to treat for "old dog" vestibular disease in canines?
A. Dimenhydrinate (Dramamine, Gravol®)
B. Cyproheptadine(Periactin®)
C. Meclizine(Antivert®)
D. Any of the above can work
E. None of the above work
A

C. Meclizine(Antivert®)

24
Q

What are the three drugs that are second-generation H1 blockers?

A
  • Terfenadine (Seldane®)
  • Loratadine (Claritin®)
  • Fexofenadine (Allegra®)
    
25
Q

True or false:
H1 antagonists have a wide distribution (including the CNS (first and second generation)) and are poorly absorbed orally.

A

False. Are readily absorbed orally and only the first generation goes to the CNS.

26
Q

Which generation of H1 antagonists has the longer duration of action?

A 
Second generation (12 to 24 hours)
*first generation 3 to 12 hours.
27
Q

How are the H1 antagonists metabolized, and in what are they excreted in?

A

Metabolized by the liver, and excreted in the urine.

28
Q

What are the therapeutic uses for H1 antagonist? (4) (slide 16/6)

A

– Allergy
– Anaphylaxis
– Anti-motion sickness
– Mild sedative

29
Q

Look at slide 17/6 for side effects of H1 antagonist

A

.

30
Q

What are the 4 H2 drugs?

A

– cimetidine
– ranitidine
– famotidine
– nizatidine

31
Q

How can you tell the difference between your H2 blockers and your H1 blockers?

A

All the H2 blockers end in “tidine”

32
Q

What type of antagonists are the H2 receptor antagonist?

A

Competitive antagonists

33
Q 
Which of the following drugs has immunomodulating activity?
A. Famotidine
B. Nizatidine
C. Cimetidine
D. Ranitidine
A 
C. Cimetidine
*Hepaticmicrosomalenzymeinhibitor(numerousdrug-druginteractions). Used to reduce gastric acid and also in treatment of equine melanoma (because of
immunomodulating activity (alteration of T-cell function and cell-mediated immunity).
34
Q 
What drug should you use if you want to control gastric acid only?
A. Famotidine
B. Nizatidine
C. Cimetidine
D. Ranitidine
A

A. Famotidine

35
Q 
What drug can be used for gastric acid and also for the G.I. prokinetic activity? 
A. Famotidine
B. Nizatidine
C. Cimetidine
D. Ranitidine
A

B. Nizatidine

D. Ranitidine

36
Q

What system is responsible for metabolizing Cimetidine, ranitidine and famotidine?

A

Cytochrome p450 system

37
Q

True or false:

H2 blockers have good oral bioavailability, and are less lipid soluble so they don’t cross the blood brain barrier.

A

True

38
Q

What is an issue with cimetidine involving the cytochrome p450 system and other drugs that use that system for metabolization?

A

Cimetidine will inhibit that system reducing the clearance of other drugs.

Pharm 2 (17 decks)

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