Miscellaneous Drugs & Ganglionic Blockers Flashcards

1
Q

What are the Alpha-2 Agonists?

A
  1. Clonidine
  2. GuanaBenz
  3. Guanfacine
  4. Methyldopa but its a prodrug
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2
Q

What happens with chronic activation of Alpha-2 and Beta-2 receptors?

A

Down regulation and loss of sensitivity to the Alpha-2 Agonist.

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3
Q

What complex/compund blocks the GRKs receptor complex formation?

A

Spinophilin

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4
Q

What happens when Beta-arrestins bind to phosphorylated Alpha-2 adrenoceptors?

A

This activates B-arr dependent signaling, these processes desensitize G protein signaling

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5
Q

What is the end result of B-arr binding?

A

The initiation of Alpha-2 adrenoceptor endocytosis

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6
Q

What are the Alpha-2 herteroreceptors?

A

Expression of the Alpha-2 receptor on Non-cholinergic tissue (Also presynaptic)

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7
Q

Where do Alpha agonist have most of their activity (Bradycardia, hypotension, sedation etc)

A

Alpha-2 heteroreceptors

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8
Q

How are the Bradycardia and hypotension achieved by the Alpha-2 agonists?

A

By activation of the parasympathetics especially the Vagal nerve system

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9
Q

What are the 2 functions of Alpha-2 Autoreceptors?

A
  1. Limit release of Norepi from sypathetic nerves

2. Limit release of Epi from Adrenal Chromaffin cells at rest

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10
Q

What is a requirement for an Alpha-2 agonist to be able to clinically lower BP?

A

Must cross the Blood Brain Barrier

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11
Q

What are the clinical effects of Alpha-2 Agonists?

A
  1. Parelled and Balanced drop in PVR and Systolic and Diastolic BP
  2. Withdrawal of SNS tone
  3. NO REFLEX TACHYCARDIA
  4. Decrease in Plasma renin activity
  5. Regression of Left Ventricular Hypertrophy
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12
Q

What are some of the Benefits of Alpha-2 agonists?

A
  1. Useful in Blocking reflex Tachycardia

2. No meaningful effect upon blood glucose or Lung function

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13
Q

Which two Alpha-Agonists are available by IV?

A

Clonidine and Methyldopa

Clonidine transdermal Patch

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14
Q

Which Alpha-2 Agonist has the Longes Half life?

A

Methyldopa Longest & Guanfacine Shortest

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15
Q

What spplement would chelate alphamethyldopa?

A

Iron supplements, suggested 2 hour gap between consumptions

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16
Q

What is indicated as a hazard in Methyldopa use?

A

Dose dependent renal Failure

17
Q

Why is Alphamethyldopa contraindicated in Pheochromocytoma?

A

It interfers with catecholamine quantitation

18
Q

What are the most complained about side effects of the Alpha-2 Agonists

A
  1. Somnolence

2. Dry mouth which increases likelyhood of caries, periodontal disease, and oral candidiasis

19
Q

Which two Alpha-Agonist have the best profiles for use in pregnancy?

A

Methyldopa and Guanfacine

20
Q

Which transporter does Reserpine inhibit?

A

VMAT2

21
Q

What are the contraindications for Reserpine?

A
  1. Depression, increases suicidal tendencies
  2. Peptic ulcer dis or Ulcerative Colitis
  3. Pregnancy
  4. Breast feeding
22
Q

What are the nicotinic postsynaptic receptors?

A

Ligand gated ion channels in the postsynaptic membrane