What is Penselin (Persantine)?
Penselin helps to prevent platelets in your blood from sticking together and forming a blood clot on or around an artificial heart valve.
Penselin is used to prevent blood clots after heart valve replacement surgery.
Penselin may also be used for other purposes not listed in this medication guide.
Dipyr >It is believed that platelet reactivity and interaction with prosthetic cardiac valve surfaces, resulting in abnormally shortened platelet survival time, is a significant factor in thromboembolic complications occurring in connection with prosthetic heart valve replacement.
Penselin tablets have been found to lengthen abnormally shortened platelet survival time in a dose-dependent manner.
In three randomized controlled clinical trials involving 854 patients who had undergone surgical placement of a prosthetic heart valve, Penselin tablets, in combination with warfarin, decreased the incidence of postoperative thromboembolic events by 62 to 91% compared to warfarin treatment alone. The incidence of thromboembolic events in patients receiving the combination of Penselin tablets and warfarin ranged from 1.2 to 1.8%. In three additional studies involving 392 patients taking Penselin tablets and coumarin-like anticoagulants, the incidence of thromboembolic events ranged from 2.3 to 6.9%.
In these trials, the coumarin anticoagulant was begun between 24 hours and 4 days postoperatively, and the Penselin tablets were begun between 24 hours and 10 days postoperatively. The length of follow-up in these trials varied from 1 to 2 years.
Penselin tablets do not influence prothrombin time or activity measurements when administered with warfarin.
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Persantine (Penselin) is a platelet inhibitor used to prevent blood clots after heart valve replacement surgery. Persantine is available in generic form. Common side effects of Persantine include:
- stomach upset,
- headache, and
- flushing (warmth, redness, or tingly feeling under your skin), particularly at first as your body adjusts to the medication.
Other side effects of Persantine include:
Tell your doctor if you have serious side effects of Persantine including:
- stomach pain,
- yellowing eyes or skin,
- dark urine, or
- unusual bleeding or bruising.
The recommended dose of Persantine is 75-100 mg four times daily as an adjunct to the usual warfarin therapy. Persantine may interact with nonsteroidal anti-inflammatory drugs (NSAIDs) or other blood thinners such as warfarin (Coumadin). Tell your doctor about all the prescription and over-the-counter medications you use. This includes vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start using a new medication without telling your doctor. During pregnancy, Persantine should be used only when prescribed. This medication passes into breast milk. Consult your doctor before breastfeeding.
Our Persantine (Penselin USP) Side Effects Drug Center provides a comprehensive view of available drug information on the potential side effects when taking this medication.
This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
1.5 Uses and applications
Penselin is an adenosine reuptake inhibitor and a phosphodiesterase inhibitor with antiplatelet and vasodilating activity. As a result, the compound is therefore used in thrombo-imbolic disorders. Orally administered Penselin is used in association with orally administered anticoagulants for the prophylactic treatment of thromboimbolism following cardiac valve replacement. It is also used as a coronary vasodilator .
Penselin exerts its antiplatelet action by several mechanisms . One of these is through the inhibition of phosphodiesterase enzyme in platelets, resulting in an increase in intraplatelet cyclic AMP and the consequent potentiation of the platelet inhibiting actions of prostacyclin. Another is the direct stimulation of the release of this eicosanoid by vascular endothelium, and the third is the inhibition of cellular uptake and metabolism of adenosine (thereby increasing its concentration at the platelet vascular interface).
The antiplatelet/antithrombotic activity of Penselin has been demonstrated in laboratory and in animal models, and has been shown to inhibit platelet aggregation and vessel-wall thrombogenesis . Penselin has been given either alone or with aspirin in the management of myocardial infarction and stroke. For the secondary prevention of stroke or transient ischemic attack, the drug may be given as a modified-release preparation in a dose of 200 mg twice daily. Penselin administered intravenously results in a marked coronary vasodilation and is used in stress testing in patients with ischemic heart disease .
What Is Aggrenox (Aspirin Dipyr >
Aggrenox is the brand name for a combination medicine that contains the drugs aspirin and Penselin.
This prescription medication is used to reduce the risk of stroke in people who have already had a transient ischemic attack (TIA or "mini-stroke") or a stroke due to a blood clot.
According to the Centers for Disease Control and Prevention (CDC), stroke is the third leading cause of death in the United States. More than 140,000 people die each year from a stroke.
Aggrenox is in a class of drugs known as antiplatelet agents. It works by preventing blood from clotting.
The Food and Drug Administration (FDA) approved Aggrenox in 1999. It's manufactured by Boehringer Ingelheim Pharmaceuticals, Inc.
No pharmacokinetic drug-drug interaction studies were conducted with Persantine (Penselin USP) Tablets. The following information was obtained from the literature.
Adenosine: Penselin has been reported to increase the plasma levels and cardiovascular effects of adenosine. Adjustment of adenosine dosage may be necessary.
Cholinesterase Inhibitors: Penselin may counteract the anticholinesterase effect of cholinesterase inhibitors, thereby potentially aggravating myasthenia gravis.
Penselin Stress Test
The Penselin nuclear test is a means of testing the response of the heart to increase blood circulation caused by the intravenous introduction of a radioactive chemical into the bloodstream. An appropriate amount of the dipridamole in injected into the vein to stimulate the heart in just the same way as physical exercise does, thereby making it possible to assess the functioning of the blood vessels and valves of the heart under controlled conditions in a pathological laboratory.
Penselin has a vasodilatory effect and should be used with caution in patients with severe coronary artery disease (e.g., unstable angina or recently sustained myocardial infarction). Chest pain may be aggravated in patients with underlying coronary artery disease who are receiving Penselin.
Elevations of hepatic enzymes and hepatic failure have been reported in association with Penselin administration.
Penselin should be used with caution in patients with hypotension since it can produce peripheral vasodilation.
No pharmacokinetic drug-drug interaction studies were conducted with Penselin tablets. The following information was obtained from the literature.
Penselin has been reported to increase the plasma levels and cardiovascular effects of adenosine. Adjustment of adenosine dosage may be necessary.
Penselin may counteract the anticholinesterase effect of cholinesterase inhibitors, thereby potentially aggravating myasthenia gravis.
Penselin is a pyrimidopyrimidine derivative with vasodilator and antiplatelet properties. The mechanism of action of Penselin as an antiplatelet agent involves increased intracellular cyclic adenosine monophosphate (cAMP), which inhibits the platelet shape change. Increased cAMP concentration is due to one or both of two mechanisms: inhibition of phosphodiesterase and blockade of uptake of adenosine (which acts at adenosine A 2 receptors to stimulate platelet adenylyl cyclase and thus increase cAMP).
Pregnancy Category B
Reproduction studies have been performed in mice, rabbits and rats at oral Dipyr >2 basis) and have revealed no evidence of harm to the fetus due to Penselin. There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, Penselin should be used during pregnancy only if clearly needed.
Penselin is metabolised in the liver and has a half-life of 12 hours. A modified-release formulation is better tolerated than the standard formulation.
Penselin is a pyramidopyrimidine compound that, acting as a phosphodiesterase inhibitor, modestly reduces platelet function.428,429