GCPR (alpha, beta, muscarinic, dopamine, histamine, vasopressin) Flashcards

1
Q

Alpha 1
Agonist: phenylephrine, NE
Antagonist: Doxazosin, tamsulosin

A

Increases:

  • vasoconstriction
  • pupil dilation
  • intestinal & bladder sphincter muscle contraction
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2
Q

Alpha2
Agonist: methyldopa
Antagonist: Mirtazapine

A
Decreases:
- sympathetic outflow
- insulin release
- lipolysis
Increases:
- platelet aggregation
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3
Q

Beta1
Agonist: dobutamine
Antagonist: ABEAM (atenolol, metoprolol)

A

Increases:

  • heart rate
  • contractility
  • renin release
  • lipolysis
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4
Q

Beta2
Agonist: albuterol, salmeterol
Antagonist: non-selective beta blockers

A
Increases:
- vasodilation
- bronchodilation
- HR
- contractility
- lipolysis
- insulin release
- aqueous humor production 
- ciliary muscle relaxation (accommodation)
Decreases:
- uterine tone (tocolysis)
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5
Q

M1 (PS, muscarinic)
Agonist: bethanechol
Antagonist: benztropine, scopalamine

A

CNS, enteric nervous system

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6
Q

M2 (PS, muscarinic)
Agonist:
Antagonist: Atropine

A

Decreases:

  • HR
  • contractility of atria
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7
Q

M3 (PS, muscarinic) - no pure M3 drugs
Agonist: Carbachol, pilocarpine, methacholine
Antagonist:
- Eyes: Atropine, hematropine, tropicamide
- Resp: Ipratropium, tiotropium,
- GU: Oxybutynin, darifenacin, solifenacin
- GI/resp: Glycopyrrolate

A

Increases:

  • exocrine gland secretion (lacrimal, salivary, gastric acid)
  • gut peristalsis
  • bladder contraction
  • bronchoconstriction
  • pupillary sphincter muscle contraction (miosis)
  • ciliary muscle contraction
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8
Q

D1
Agonist: dopamine (D1 = D2), fenolopam (selective)
Antagonist: not on purpose

A

Relaxes renal vascular smooth muscle (increases renal perfusion)

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9
Q

D2
Agonist: dopamine, bromocriptine, cabergoline
Antagonist: metoclopromide, antipsychotics

A

Modulates transmitter release, especially in the brain

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10
Q

H1
Agonist: none
Antagonist: diphenhydramine, loratadine

A

Increases:

  • nasal and bronchial mucus production
  • vascular permeability
  • bronchoconstriction
  • pruritis
  • pain
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11
Q

H2
Agonist: none
Antagonist: cimetidine, ranitidine, famotidine, nizatidine

A

Increases gastric acid secretion

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12
Q

V1

A

Vasoconstriction

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13
Q

V2
Agonist: desmopressin (DDAVP)
Antagonist: maybe demeclocycline

A

Increases water permeability and reabsorption in the collecting tubules of the kidneys; stimulates release of vWF from endothelial cells

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14
Q

Gq pathway

A

Gq –> phospholipase C –> IP3 –> increased [Ca2+]

Also phospholipase C –> DAG –> Protein Kinase C

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15
Q

Gs pathway

A

Gs –> adenylate cyclase –> cAMP –> PKA –> increased [Ca2+] in heart and decreased myosin light chain kinase (results in smooth muscle dilation)

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16
Q

Gi pathway

A

Gi inhibits adenylate cyclase –> decreased cAMP –> decreased PKA —> decreased [Ca2+] in heart and increased myosin light chain kinase (smooth muscle contraction)