Peritrate

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Peritrate

Method of action: Antianginal

Treatment option: Seizure Prophylaxis

Medically reviewed

Laura Arias

Last updated on 22/12/2025

This page provides general, reference-level information compiled from official medical sources. It is not a substitute for professional medical advice, diagnosis, or treatment. For decisions about your health, please consult a qualified healthcare professional.

Overview of Peritrate

Property Description
Active Ingredient Pentaerithrityl Tetranitrate (PETN)
Form Oral Tablet (Standard and Sustained-Action)
Pharmacological Class Organic Nitrate / Nitro-vasodilator
General Purpose Prophylactic (Preventative) Treatment of Angina
Origin Synthetic Compound (Nitric Acid Ester)

The Identity and Class of Peritrate

Peritrate is a specialized medication whose active component is Pentaerithrityl Tetranitrate (PETN), classified as a nitro-vasodilator. It belongs to the broader pharmacological class of organic nitrates, a category of drugs used to induce the relaxation of blood vessel walls. This compound is a synthetic chemical entity derived from a nitric acid ester.

The drug's primary function is the prophylactic treatment of angina pectoris, meaning it is specifically utilized to prevent the painful episodes of angina rather than treating an acute attack once it has begun. This preventative application is clinically recognized for managing the underlying symptoms of coronary artery disease. Long-acting organic nitrates are standardly used for maintenance therapy in patients with chronic stable angina. Consequently, the medication is primarily a preventative agent, intended for sustained, long-term management of adult patients.


Composition, Form, and General Purpose

The medication's composition is focused on its single active ingredient, Pentaerithrityl Tetranitrate, which is taken orally. Peritrate is supplied as an oral tablet and is notably available in both standard and sustained-action tablet (SA) variants. The sustained-action design is a differentiating factor because it ensures the necessary long-acting therapeutic coverage, which is vital for continuous, day-to-day prevention.

By acting as a systemic vasodilator, Peritrate reduces the workload on the heart. Its action causes the walls of arteries and veins to relax and widen; this relaxation reduces the pressure and volume of blood returning to the heart, which effectively lowers the heart's pumping effort. The overall benefit is the stabilization of blood flow and oxygen supply to the heart muscle, thereby decreasing the likelihood of chest pain associated with coronary artery disease.

Regulatory References

  1. National Library of Medicine

What side effects are possible with Peritrate?

Possible Side Effects and Safety Information

The safety profile of Peritrate (Pentaerithrityl Tetranitrate) is officially classified based on the drug's potent action as a nitro-vasodilator, with documented effects primarily affecting the vascular and nervous systems. This information is derived exclusively from government-approved regulatory documents.

Adverse Reaction Scope

Classification Scope Officially Documented Reactions/Notes
Common / Very Common Headache, Nausea, Vomiting, Dizziness, and Flushing. Headache is often transient, being most common at the start of treatment or following a dose increase.
Uncommon Hypotension (low blood pressure), Postural Hypotension, and Syncope (loss of consciousness).
System-Organ Classes Vascular Disorders (e.g., Hypotension, Flushing) and Nervous System Disorders (e.g., Headache, Dizziness, Syncope).
Serious Reactions Severe Hypotension and Syncope are listed as potential serious concerns related to rapid changes in systemic blood pressure.

Specific Safety Constraints

The regulatory label includes specific limitations and constraints regarding use. Drug Tolerance (diminished effect) is a documented pattern that may develop with continuous, uninterrupted long-term exposure. Safety documents specify that Older Adults and individuals with pre-existing low blood pressure have an increased susceptibility to severe hypotensive effects.

Use is absolutely contraindicated with Phosphodiesterase type 5 (PDE5) inhibitors (e.g., sildenafil, tadalafil) due to the risk of life-threatening profound hypotension. The drug is also contraindicated in individuals with Severe Anemia and Closed-Angle Glaucoma.

Overdose and Emergency Response

Overdose and When to Seek Help

Overdose of Pentaerithrityl Tetranitrate is characterized by manifestations affecting the cardiovascular and hematologic systems, as formally documented in regulatory labeling. Initial presentations reflect profound systemic vasodilation, including sustained and severe hypotension (low blood pressure), intense throbbing headache, dizziness, weakness, syncope, nausea, and vomiting.

Severe Outcomes

A critical, life-threatening outcome documented for this organic nitrate class is Methemoglobinemia. This condition impairs the blood’s capacity to transport oxygen, leading to severe tissue hypoxia. Clinical signs of this serious complication may include generalized cyanosis (bluish-gray skin), confusion, seizures, and in extreme cases, coma. Infants and patients with specific congenital enzyme deficiencies, such as G6PD deficiency, are documented as having an increased risk for severe Methemoglobinemia.

Required Emergency Action

It is formally stated that immediate medical attention or emergency help must be sought in all cases of suspected overdose, particularly if signs of severe hypotension, cyanosis, or central nervous system involvement are present. Management for severe Methemoglobinemia requires the specific antidote Methylene Blue, which is administered alongside crucial supportive measures. These measures include fluid administration to manage hypotension, and continuous monitoring of vital signs and methemoglobin levels is required in a hospital setting.

Therapeutic Uses of Peritrate

Peritrate (Pentaerithrityl Tetranitrate) is commonly used to help with the prophylactic management of symptomatic episodes associated with chronic stable angina pectoris. This long-term, preventative therapy is relevant in clinical settings marked by increased discomfort or tension, generally supporting the ongoing management of coronary artery disease.

This medication is applied in addressing symptom clusters that may become intense or disruptive, including those related to the frequency, severity, and duration of anginal episodes. Used as a maintenance agent for adult patients, it may assist with maintaining functional stability by managing symptoms that interfere with daily functioning.

“The continuous preventative effect helps maintain a sense of stability when symptoms are more noticeable and assists with maintaining functional stability for day-to-day comfort.”

Applied in a continuous, preventative context, Peritrate is commonly used for managing conditions characterized by symptoms that interfere with daily functioning, such as recurrent episodes of chest pain and chest tightness that contribute to functional strain.


Quick Fact: Relief for Chronic Stable Angina

Eligibility and Restrictions for Use

The eligibility profile for Peritrate (Pentaerythritol Tetranitrate) is primarily defined by mandatory exclusions (contraindications) outlined in previous regulatory documents, as the drug's use is not supported by current, active labeling from major agencies like the FDA. The following groups are explicitly prohibited from using this medicine:


Populations For Whom Use is Contraindicated

  • Known Hypersensitivity: Individuals with a history of allergy or sensitivity to Pentaerythritol Tetranitrate or any components of the specific formulation.
  • Co-administration with PDE5 Inhibitors: Patients who have recently used or are currently using Phosphodiesterase Type 5 (PDE5) inhibitors (such as sildenafil), due to the risk of severe, life-threatening hypotension.
  • Severe Blood Conditions: Patients diagnosed with Severe Anemia.
  • Specific Acute Heart Conditions: Patients who have experienced a recent Myocardial Infarction (heart attack).

Other Eligibility Considerations

The most critical restriction is the absolute prohibition against concurrent use with PDE5 inhibitors, a standard constraint for all nitrate-class medicines. Data regarding specific restrictions for use during pregnancy or lactation were not uniformly documented as formal eligibility statuses across the available contraindication sections.

What should I know about interactions with other medicines?

Official Regulatory Interaction Profile

The official interaction profile for Pentaerithrityl Tetranitrate (Peritrate) is defined by its significant pharmacodynamic interactions documented in government regulatory sources. The most critical interaction is the formal prohibition on co-administration with Phosphodiesterase Type 5 (PDE5) Inhibitors, which include active ingredients such as Sildenafil, Tadalafil, and Vardenafil.

This is classified as a Contraindicated Combination due to the enhanced additive pharmacodynamic effect, which augments the blood pressure-lowering action. This synergy creates a high risk of severe, life-threatening hypotension, as specified in official labeling.

A mandatory timing restriction is part of this prohibition, requiring a defined separation period (e.g., 24 hours after Sildenafil use) before Peritrate can be administered. This constraint is officially documented to mitigate hypotensive risk.

Beyond the formal contraindication, regulatory documents note that co-administration with other antihypertensive drugs and vasodilators may result in additive hypotensive effects. This category includes product classes such as Beta-blockers, Calcium Channel Blockers, and Diuretics. The antiarrhythmic agent Amiodarone is also specifically noted as a medicine that may increase Peritrate’s vasodilatory activity. No specific pharmacokinetic interactions, such as those involving CYP enzymes or transporters, are explicitly documented in the official prescribing information.

Mechanism of Action

How Peritrate Works

Peritrate, which contains pentaerythritol tetranitrate (PETN), functions as a prodrug and begins its action in systems involving enzyme-mediated signaling. It is metabolized within vascular smooth muscle cells by specific enzymes, such as mitochondrial aldehyde dehydrogenase (mALDH2), releasing free nitric oxide (NO).

The released NO initiates a critical mechanistic cascade by diffusing into the smooth muscle cell where it binds to and activates soluble guanylate cyclase (sGC). This enzyme activation subsequently elevates the intracellular concentration of the second messenger, cyclic guanosine monophosphate (cGMP).

The increase in cGMP modulates key intracellular pathways by activating cGMP-dependent protein kinases. This action ultimately facilitates the dephosphorylation of the myosin light chain and a reduction in intracellular calcium levels. The resulting physiological consequence is the relaxation of vascular smooth muscle cells (vasodilation) and a subsequent decrease in vascular resistance, thereby regulating the diameter of the blood vessel lumen.

Dosage and Administration Information

How to Use Peritrate

The general usage of Peritrate (Pentaerithrityl Tetranitrate) is defined by guidelines that govern its administration route, dosing schedule, and required frequency patterns. It is administered orally and is intended for use as a long-term, prophylactic treatment.


Official Administration Guidelines

The protocol for use is differentiated by the formulation: the standard tablet and the sustained-action (SA) form.

Category Instruction
Route of Administration Oral administration only.
Dosing Schedule Standard Tablets: Dosing ranges up to 40 mg per dose. Sustained-Action Forms: Typically administered as an 80 mg dose.
Timing & Meals Standard Tablets are administered around mealtimes, taken one-half hour before or one hour after meals and at bedtime (QID). Sustained-Action Forms should be taken on an empty stomach.
Age-Group Rules The medication is not approved for use in pediatric patients.

Procedural Constraints

A core principle of therapy involves maintaining a consistent schedule that incorporates a daily nitrate-free interval of approximately 10 to 12 hours. This procedural step is necessary to mitigate the development of pharmacological tolerance.

The standard form is taken four times daily (QID), while the sustained-action form allows for a twice-daily (BID) schedule. Sustained-action tablets must be swallowed whole to ensure the controlled release mechanism functions as intended. Additionally, when discontinuing long-term use, the dose must be gradually decreased rather than stopped abruptly.

These protocols establish the standardized approach to using the medicine, focusing solely on administration parameters.

Recent Clinical Evidence

Evidence for Prophylactic Management of Chronic Angina

Peritrate (Pentaerithrityl Tetranitrate) was studied for its use in research exploring how symptoms change over time for individuals with chronic stable angina. The research base includes short-term randomized controlled trials (RCTs). These trials focused on measures of physical capacity, such as the time participants could exercise before experiencing symptoms, and on monitoring the frequency of anginal episodes. Research contributes to the broader evidence landscape for long-acting nitrates, but findings were mixed across some evidence, and results apply only to the populations studied.

Status of Long-Term Evidence and Durability of Effect

Research provides insight into short-term changes but has limited information for long-term outcomes that go beyond a few months of observation. A key challenge research has explored is that the body may develop a reduced response, known as tolerance, with continuous use. The evidence is also limited regarding the medication’s influence on more serious clinical events, such as the risk of heart attack or overall mortality. The research does not determine whether an individual will respond similarly over long periods.

Evidence in Select Subgroups and Regulatory Findings

The available evidence is limited for many specific subgroups, meaning data for certain groups remain insufficient. Research has explored investigational studies in high-risk pregnant women, examining outcomes related to systemic or functional imbalance. However, the findings were mixed, and the regulatory evidence for these subgroups varies. Some official regulatory findings indicated that effectiveness was not established by substantial evidence from adequate and well-controlled studies. This highlights that certainty remains low for definitive claims of effectiveness, and more research is needed in these areas.

Frequently Asked Questions (FAQ)

Common questions about Peritrate (FAQ)

Q: How long does Peritrate usually stay in your system?

Studies examining the drug's activity indicate that its active component is broken down into metabolites. The plasma elimination half-life of one active metabolite is approximately 4–5 hours, while a secondary metabolite has a half-life of 10–11 hours. The half-life refers to the time it takes for half of the substance to be cleared from the plasma.

Q: How quickly does Peritrate usually start working?

Peritrate is described in official documents as a long-term, preventative treatment for the management of angina. Research shows that mean peak levels of the active metabolite in the body are typically reached around 3 hours after a dose of the tablet formulation is administered.

Q: Is it possible to develop a tolerance to Peritrate over time?

Yes, official regulatory documents state that tolerance, which is a diminished response to the drug, may occur with its continuous, uninterrupted use. The potential for tolerance is why official administration guidelines incorporate a daily 'nitrate-free interval'.

Q: What happens if I stop taking Peritrate suddenly?

According to official documentation, the drug's dose must be gradually decreased upon discontinuation rather than stopped abruptly. This procedural step is included in the official label to avoid a potential withdrawal reaction.

Q: Are there any foods or drinks that interact with Peritrate?

Official administration instructions for the sustained-release form may specify that it should be taken on an empty stomach. However, specific warnings against mixing the drug with particular foods are generally not detailed in official patient information.

Q: Does Peritrate interact with alcohol?

Official warnings note that combining Peritrate with alcohol may enhance its blood pressure-lowering effect (hypotensive effect). For this reason, official patient information may state that alcohol should be avoided while using this medicine.

Q: Can Peritrate cause drowsiness or affect driving?

The official adverse reaction profile notes that the drug may cause dizziness or lightheadedness, which can occur due to low blood pressure. Official label information indicates that if these effects develop, activities that require concentration, such as driving a car or operating machinery, are generally restricted.

Q: Can Peritrate be taken with blood pressure medicine?

Peritrate, as a vasodilator, can cause an additive blood pressure-lowering effect when combined with other antihypertensive agents, such as beta-blockers. Clinical studies have described the use of this drug in conjunction with other anti-anginal therapies, including beta-blockers.

Q: Is Peritrate a type of beta-blocker?

No, Peritrate is classified as an organic nitrate/nitro-vasodilator. This is a distinct pharmacological class from beta-blockers, which work by a different mechanism. Both drug classes are sometimes used together in treatment.

Q: Can Peritrate cause changes in vision?

Blurred vision has been reported as a side effect in official adverse reaction profiles. Official reports classify blurred vision as a side effect that requires a doctor's attention.

Q: Can Peritrate be used during pregnancy or breastfeeding?

Official patient warnings state that the use of this medicine during pregnancy or breastfeeding must be discussed with a healthcare provider. The safety profile requires professional assessment in these circumstances.

Q: Is it normal to experience stomach upset when first taking Peritrate?

Gastrointestinal distress, which includes symptoms like nausea and vomiting, has been reported as a common adverse reaction in official documents. This effect is often described as mild and transient, meaning it may subside with continued use.

Q: Does Peritrate change my heart rate?

Yes, a fast heart rate (tachycardia) has been reported as a possible adverse effect. This change can sometimes occur as a compensatory sympathetic reflex in response to the drug's blood pressure-lowering action.

Q: How is Peritrate related to other drugs that prevent angina?

Peritrate is classified as a long-acting nitrate vasodilator, and it is primarily used for the prophylactic management of chronic stable angina. This distinguishes it from other drug classes used for preventative heart treatment, such as beta-blockers, calcium channel blockers, and ACE inhibitors.

How should Peritrate be stored and disposed of?

How to Store and Dispose of Peritrate

Peritrate (Pentaerithrityl Tetranitrate) must be stored under specific environmental conditions to maintain its stability, as defined by regulatory standards.

Storage Requirements

Condition Requirement
Temperature Store at Controlled Room Temperature, typically 20 C to 25 C (68 F to 77 F).
Protection The product must be protected from light, moisture, and excessive heat. Do not freeze the tablets.
Container Keep the medication in its original container and ensure the container is tightly closed.
Child Safety Store all medication out of the sight and reach of children.

Disposal Instructions

Disposal of unused or expired Peritrate must be handled correctly to comply with environmental regulations. Do not dispose of the medication in household trash or pour it down a sink or toilet. Unused product must be discarded through a medicine take-back program or according to local pharmaceutical waste regulations.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

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