| Indication |
For the prevention of angina |
| Pharmacodynamics |
Nitroglycerin, an organic nitrate, is available in many forms as
a vasodilator. Nitroglycerin is used in the treatement of angina
pectoris and perioperative hypertension, to produce controlled
hypotension during surgical procedures, to treat hypertensive
emergencies, and to treat congestive heart failure associated with
myocardial infarction. |
| Mechanism of action |
Similar to other nitrites and organic nitrates, nitroglycerin is
converted to nitric oxide (NO), an active intermediate compound which
activates the enzyme guanylate cyclase. This stimulates the synthesis of
cyclic guanosine 3',5'-monophosphate (cGMP) which then activates a
series of protein kinase-dependent phosphorylations in the smooth muscle
cells, eventually resulting in the dephosphorylation of the myosin
light chain of the smooth muscle fiber. The subsequent release of
calcium ions results in the relaxation of the smooth muscle cells and
vasodilation. |
| Absorption |
Not Available |
| Volume of distribution |
|
| Protein binding |
Not Available |
| Metabolism |
Hepatic, cytochrome P450 (P450) is a key enzyme of organic nitrate biotransformation |
| Route of elimination |
Not Available |
| Half life |
3 minutes |
| Clearance |
|
| Toxicity |
Increased intracranial pressure, with any or all of persistent
throbbing headache, confusion, and moderate fever; Vertigo;
Palpitations; Visual disturbances; Nausea and vomiting (possibly with
colic and even bloody diarrhea); Syncope (especially in the upright
posture); Air hunger and dyspnea, later followed by reduced ventilatory
effort; Diaphoresis, with the skin either flushed or cold and clammy;
Heart block and bradycardia; Paralysis; Coma; Seizures; Death. |
