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FIU - NO donors & enhancers
NO donors & enhancers
10
Pharmacology
Professional
12/21/2011

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Cards

Term
How does NO act to relax smooth muscle?
Definition
activates guanylate cyclase, which produces cGMP (which is broken down by PDE). cGMP activates protein kinase that prevents release of Ca from ER, leading to muscle relaxation.
Term
NO function in body
Definition
main vasodilator
Term
Nitroglycerin mode of action, effect/use
Definition
NO donor, for acute angina, also reduces bp (dose dependent), requires sulfhydryl-containing cysteine -> depletion of cysteine = nitrate tolerance.
Term
Amyl nitrate use
Definition
Treatment of angina and cyanide poisoning (by creating methemoglobin which sequesters cyanide as non-toxic cyanomethemoglobin. Methemoglobin converted back to hemoglobin by methylene blue). Also illegal inhalant that produces euphoria (poppers).
Term
isosorbide mononitrate and dinitrate
Definition
NO donor with longer t1/2's (5 hrs/1 hr) than nitroglycerin (minutes, need expensive patches)
Term
nicorandil, effect, arrhythmias? side effects?
Definition
NO donor (increases cGMP) and K-channel opener (hyperpolarizes cell), arterial and venous relaxation/dilation; doesn't cause arrhythmias because is selective of vascular potassium channels (no opening of cardiac or pancreatic channels); mouth ulcers
Term
Ranolazine mode of action, effect
Definition
indirectly reduces available Ca in cardiac muscle by altering the transcellular late Na current which affects sodium dependent calcium channels, relaxes heart muscle and reduces cardiac ischemia (lack of O2)
Term
Trimetazidine mode of action, effect
Definition
shifts cardiac metabolism from fatty acid beta oxidation toward glucose oxidation reducing O2 consuption, relaxes cardiac muscle/cardioprotective
Term
Ivabradine mode of action, effect
Definition
Inhibits sinus node pacemaking current (enhanced PNS effect), slows heart rate without side effects of beta-1 blockers (reduced contractility) and beta-2 blockage (prevention of bronchodilation)
Term
DON'T use NO donors with these drugs
Definition
PDE 5 inhibitors like sildenafil (also relax smooth muscle, take off nitrates for the day), alpha-1 blockers (block constriction of blood vessels and reduce bp like NO donors)
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