Penthrite
Penthrite Uses, Dosage, Side Effects, Food Interaction and all others data.
Penthrite is the nitrate ester of pentaerythritol that possesses explosive properties. When mixed with a plasticizer, this chemical forms a plastic explosive. It is recognized by the FDA to be a coronary vasodilator in the treatment of heart conditions such as angina .
It is a pentaerythritol nitrate in which all four hydroxy groups of pentaerythritol have been converted to the corresponding nitrate ester. It is a vasodilator with properties that are quite similar to those of glyceryl trinitrate, however, with a more prolonged duration of action. It is also one of the most powerful high explosives known and is a component of the plastic explosive known as Semtex .
PETN has the chemical formula C5H8N4O12. It is formed by reacting pentaerythritol (C5H12O4), an alcohol commonly used in paints and varnishes, with nitric acid (HNO2). The reacting solution is chilled to precipitate the PETN. It is then filtered out, washed, dried, and recrystallized to produce a colorless crystalline material that is stored and shipped as a mixture with water and alcohol .
| Trade Name | Penthrite |
| Generic | Pentaerythritol tetranitrate |
| Pentaerythritol tetranitrate Other Names | Corpent, PENT, PENTA, Pentaerithrityl tetranitrate, pentaerithrityli tetranitras, Pentaerythritol tetranitrate, Penthrite, Tetranitrate de pentaerithrityle, Tetranitrato de pentaeritritilo |
| Type | |
| Formula | C5H8N4O12 |
| Weight | Average: 316.1366 Monoisotopic: 316.01387174 |
| Groups | Approved |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Used for the treatment of angina pectoris .
How Penthrite works
Penthrite is the lipid soluble polyol ester of nitric acid belonging to the family of nitro-vasodilators. Penthrite releases free nitric oxide (NO) after the denitration reaction, which triggers NO-dependent signaling transduction involving soluble guanylate cyclase (sGC). Nitric oxide binds reversibly to the ferrous-heme center of sGC, causing conformational change and activating the enzyme. This enzyme activation results in increased cellular concentrations of _cyclic guanosine monophosphate _(cGMP) within the vascular smooth muscle, resulting in vasodilation mediated by cGMP-dependent protein kinases. Additionally, this agent causes dose-dependent arterial and venous bed .
Toxicity
The toxicity of nitrate drugs are the result of nitrate conversion to nitrite in the body. Nitrite leads to the autocatalytic oxidation of oxyhemoglobin to both hydrogen peroxide and methemoglobin. This increase in methemoglobin levels is a condition known as methemoglobinemia and is manifested by tissue hypoxia, as methemoglobin is unable to bind oxygen .
Dizziness, redness of the skin (due to vasodilatation), skin irritation and headache are common adverse effects of this drug. Postural hypotension can also occur, especially if this drug is taken at higher doses or while standing .
PETN - Oral LD50 (mouse) = 25,000 mg/kg
Food Interaction
- Take with or without food. Food delays drug absorption, but not to a significant extent.
Volume of Distribution
The steady-state volume of distribution was 4.2 +/- 1.1 L/kg (n = 6) in rats given this drug by the intra-arterial route .
Half Life
The elimination half-life in plasma from male volunteers given an oral 100-mg dose of the tetranitrate was reported to be 4-5 hours .
Clearance
In a pharmacokinetic study of rats after intra-arterial administration of this drug, the clearance was measured to be 0.61 +/- 0.16 L/min/kg .
Elimination Route
Mainly the urine .
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