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MCW - Pharmacology > Block 2_6 - Smooth Muscle > Flashcards

Block 2_6 - Smooth Muscle Flashcards

1
Q

Nitrates - Mechanism of Action

A
  1. Nitric Oxide Donors
  2. Intracellular Signaling - Cyclic GMP/Protein Kinase G
  3. Arterial and venous circulation (venous dominant)
    - dilations decreases venous return to the heart and decreases preload mostly
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2
Q

Nitroglycerin / Nitroprusside

  1. Physiological Effect
  2. Use
  3. Toxicitiy
A
  1. Relaation of arterial and venous smooth muscle (nitroglycerin)

Relaxation of arterial and venous circulations (nitroprusside)

Venous dominant

  1. Heart Failure
  2. Hypotension
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3
Q

Name 2 direct vasodilatiors

A

Hydralazine

Minoxidil

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4
Q

Hydralazine

  1. Site of Action
  2. Use
  3. Toxicitiy
A
  1. Arterial circulation (increases cGMP)
  2. Heart Failure
  3. Hypotension
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5
Q

Name 2 nitrate vasodilators

A

Nitroglycerin

Nitroprusside

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6
Q

Minoxidil (rogaine)

  1. Site of Action
  2. Mechanism
  3. Use
  4. Side Effect
A
  1. Arterial Circulation (has effect on afterload - decreases total peripheral resistance - therefore, it is a better antihypertensive agent)
  2. Vasodilation due to smooth muscle hyperpolarization from K+ potassium channel opening
  3. Heart Failure, Hypertension, male pattern baldness
  4. reflex tachycardia, headache, hair growth
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7
Q

Diazoxide

  1. Effects
  2. Use
A
  1. Membrane channel dilator

Cell membrane actions (K+ channel opener/Activator)

  1. Hypertension
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8
Q

Name 2 Calcium channel blockers (non-dihydropyridines)

  • selectivity
  • circulation
  • use
A

Phenylalkylamine - Verapamil

Benzothiazapine - Diltiazem

  • non-selective
  • arterial circulation
  • antihypertensive
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9
Q

Name 3 Phosphodiesterase 3 (PDE3) inhibitors

  • mechanism (5)
  • use
A

Milrinone, Inamrinone, Cilostazol

  • intracellular signagling: inhibit PDE3 breakdown of cAMP into AMP to increase contraction (in heart)

Heart Muscle - contraction

  1. Phosphorylation of Ca2+ channels - inotropic
  2. Phosphorylates Myofilaments - inotropic
  3. Phosphorylates K+ channels - chronotropic (decreases repolarization time = ↑ HR = ↑CO)

Smooth Muscle - relaxation

  1. ↑cAMP inhibits myosin light chain kinase, the enzyme that is responsible for phosphorylating smooth muscle myosin and causing contraction, and reduces sensitivity to Ca2+
  2. ↑cGMP activates protein kinase G - Phosphorylates K+ channels - hyperpolarization
    - heart failure (positive inotropic effect) - decrease afterload and pumping ability of the heart
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10
Q

Name 2 Phosphodiesterase 5 (PDE5) inhibitors

  • Mechanism
  • Use
A

Sildenafil, Tadalafil

  • ↑cGMP levels by preventing its breakdown by PDE5 –> increased smooth muscle relaxation
  • erectile dysfunction
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11
Q

Renin-Angiotensin Inhibitors

  1. 3 Types - Mechanism
  2. Circulation
  3. Use
A
  1. Renin Inhibitors - prevent Renin from converting angiotensinogen to angiotensin I

Angiotensin converting enzyme (ACE) Inhibitors - prevents conversion of Angiotensin I to Angiotensin II

Angiotensin Receptor Blockers (ARB) - block ability of angiotensin II to act on AT1 receptors to cause contraction

  1. Arterial and Venous Circulation
  2. Hypertension
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12
Q

Bradykinin

  1. mechanism
  2. circulation
A
  1. vasodilator - ACE inactivates bradykinin. Therefore, inhibit ACE to ↑bradykinin levels
    - generate Endothelial-derived factors / B2 receptor (vascular endothelium)
    - EDF: PGI2, EDHF, NO - cause vasodilation
  2. arterial and venous circulation
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13
Q

Fenoldopam

    • Mechanism
    • circulation
    • use
A
  1. Dopamine A1 Receptor Agonist (direct and indirect pathway) - ↑cAMP
  2. Arterial and Venous Circulation
  3. Hypertensive Crisis - strong vasodilator effect –> lowers BP quickly
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14
Q

Prazosin

- Mechanism
 - circulation
 - use
A
  1. Alpha-Adrenergic blocker
  2. Arterial and venous circulation
  3. vasodilation in arterial and venous vascular beds
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15
Q

Bronchodilators that act as beta 2 agonists

  1. mechanism
  2. toxicity
A

Albulterol, pirbuterol, terbutaline, salmeterol, formoterol

1. Intracellular Signaling - ↑cAMP activates protein kinase A to cause relaxation

  1. cardiotoxicity due to ↑cAMP unlikely since albuterol given through airways
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16
Q

Bronchodilators that act as Anti-cholinergics

  1. mechanism
  2. side effects
  3. use
A

ipratropium, tiotropium

  1. muscarinic receptor antagonist (antimuscarinic) - inhibits ability of Ach to cause contraction
  2. decreased mucous secretion
  3. bronchildator in asthma
17
Q

Bronchildators - Methylxanthine

Mechanism of action (2)

A

theophylline, aminophylline

  1. phosphodiesterase inhibition to increase cAMP levels and enhance bronchildation
    - adenosine receptor antagonism inhibits bronchoconstriction

MCW - Pharmacology (8 decks)

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