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Erythrityl Tetranitrate: Indication

Erythrityl tetranitrate is a vasodilator used to prevent angina. It works similarly to nitroglycerin by being converted to an active intermediate that stimulates the enzyme guanylate cyclase, increasing cyclic GMP levels. This causes smooth muscle relaxation and vasodilation. Research shows that the potency of organic nitrates at activating guanylate cyclase depends mainly on the number of nitrate groups, possibly due to varying nitric oxide release. Overdose symptoms include increased intracranial pressure, syncope, respiratory issues, and potentially death. It should be taken on an empty stomach and avoided with alcohol.

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101 views3 pages

Erythrityl Tetranitrate: Indication

Erythrityl tetranitrate is a vasodilator used to prevent angina. It works similarly to nitroglycerin by being converted to an active intermediate that stimulates the enzyme guanylate cyclase, increasing cyclic GMP levels. This causes smooth muscle relaxation and vasodilation. Research shows that the potency of organic nitrates at activating guanylate cyclase depends mainly on the number of nitrate groups, possibly due to varying nitric oxide release. Overdose symptoms include increased intracranial pressure, syncope, respiratory issues, and potentially death. It should be taken on an empty stomach and avoided with alcohol.

Uploaded by

Abeer
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© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
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Erythrityl

Tetranitrate
This compound belongs to
the class of organic
compounds known as nitrate
esters. These are
compounds containing a
nitrate ester functional
group, with the general
structure RON+(=O)O, (R
cannot be a hydrogen). Erythrityl Tetranitrate is a
vasodilator with general properties similar to
nitroglycerin.

INDICATION:
For the prevention of angina.

MECHANISM OF ACTION:
It is similar to other nitrites and organic nitrates,
erythrityl tetranitrate is converted to 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.

STRUCTURE ACTIVITY RELATIONSHIP OF


ORGANIC NITRATES:
The SAR of organic nitrates is still under study and has
not yet been established. However Researches show us
that when the effect of different organic nitrates on the
activity of soluble guanylate cyclase prepared from rat
liver was investigated, we found a close correlation
between the number of nitrate ester groups and the
potency of guanylate cyclase activation.
The effect of sterical factors and lipophilicity on
organic nitrate-inducedactivation of guanylate
cyclase was small.
Isosorbide-2-nitrate was found to be more potent
than the stereoisomeric isosorbide-5-nitrate.
Similarly, the cyclic dinitrates isomannide
dinitrate , isoidide dinitrate and isosorbide dinitrate
exhibited small but significant differences in their
guanylate cyclase stimulatory potency.
Two lipophilic ester derivatives of isosorbide-5nitrate showed a 2-fold potency difference for
vasodilation but were equipotent for activation of
guanylate cyclase.
Also, the increase in lipophilicity due to
esterification of the free hydroxylic group had no
major influence on guanylate cyclase activation by
isosorbide-5-nitrate.
These results demonstrate that in a cell-free system,
the potency of organic nitrates for guanylate
cyclase activation is mainly determined by the number
of nitrate groups. Since organic nitrate-

induced activation of guanylate cyclase may involve


the formation of nitric oxide free radicals, it is
conceivable that the differences in potency reflect a
varying degree of nitric oxide release from each
compound tested.

TOXICITY:
Symptoms of overdose include 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.

FOOD INTERACTION:
Avoid alcohol.
Take on empty stomach: 1 hour before or 2 hours
after meals.

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