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

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

Flashcards in GCPR (alpha, beta, muscarinic, dopamine, histamine, vasopressin) Deck (16):
1

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

Increases:
- vasoconstriction
- pupil dilation
- intestinal & bladder sphincter muscle contraction

2

Alpha2
Agonist: methyldopa
Antagonist: Mirtazapine

Decreases:
- sympathetic outflow
- insulin release
- lipolysis
Increases:
- platelet aggregation

3

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

Increases:
- heart rate
- contractility
- renin release
- lipolysis

4

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

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

5

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

CNS, enteric nervous system

6

M2 (PS, muscarinic)
Agonist:
Antagonist: Atropine

Decreases:
- HR
- contractility of atria

7

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

Increases:
- exocrine gland secretion (lacrimal, salivary, gastric acid)
- gut peristalsis
- bladder contraction
- bronchoconstriction
- pupillary sphincter muscle contraction (miosis)
- ciliary muscle contraction

8

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

Relaxes renal vascular smooth muscle (increases renal perfusion)

9

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

Modulates transmitter release, especially in the brain

10

H1
Agonist: none
Antagonist: diphenhydramine, loratadine

Increases:
- nasal and bronchial mucus production
- vascular permeability
- bronchoconstriction
- pruritis
- pain

11

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

Increases gastric acid secretion

12

V1

Vasoconstriction

13

V2
Agonist: desmopressin (DDAVP)
Antagonist: maybe demeclocycline

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

14

Gq pathway

Gq --> phospholipase C --> IP3 --> increased [Ca2+]
Also phospholipase C --> DAG --> Protein Kinase C

15

Gs pathway

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

16

Gi pathway

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