Dipyridamole
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Clinical Pharmacology
Pharmacotherapeutic group: vasodilating agent
Pharmacological action: Dipyridamole has a inhibitory effect on platelet aggregation, improves microcirculation. It has a vasodilating effect.
As a pyrimidine derivative, dipyridamole is an interferon inducer and has a modulating effect on the functional activity of the interferon system, increases the decreased production of interferon alpha (a) and gamma (g) by white blood cells in vitro.
Dipyridamol increases non-specific antiviral resistance to viral infections.
Pharmacokinetics: The maximum plasma concentration of dipyridamole is achieved within 1 hour after ingestion. Dipyridamole is almost completely bound to blood proteins. The accumulation of dipyridamole occurs in myocardiocytes and in erythrocytes. Dipyridamole is metabolized in the liver by binding to glucuronic acid. The half-life is 20-30 minutes in the first phase, in the second phase - about 10 hours. Cumulation is possible (mainly in patients with impaired liver function). Excreted in the bile as monoglucuronide.
Indications
Treatment and prevention of cerebral circulatory disorders of ischemic type, dyscirculatory encephalopathy.
Prevention of arterial and venous thrombosis and their complications, prevention of thromboembolism after the operation of prosthetic heart valves.
Prevention of placental insufficiency in complicated pregnancy.
As part of complex therapy for any violations of microcirculation.
As an interferon inducer and immunomodulator for the prevention and treatment of influenza, ARVI.
Composition
1 coated tablet contains:
active substance: dipyridamole 25, 50 or 75 mg; Auxiliary components: milk sugar (lactose), Kollidon VA64 (copolyvidone), magnesium stearate, microcrystalline cellulose, sodium croscarmelose (primelloza), hydroxypropylmethylcellulose (hypromellose), talc (colloidal silicon dioxide), titanium dioxide, 80-ti-80, titan-80; yellow E104.
Dipyridamole is marketed under different brands and generic names, and comes in different dosage forms:
Brand name | Manufacturer | Country | Dosage form |
---|---|---|---|
Dipyridamole-FPO | Obolensky OP | Russia | pills |
Curantyl® | Berlin-Chemie/Menarini | Germany | pills |
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Dosage and Administration
Unless otherwise prescribed by a doctor, the following dosing regimens are recommended:
To reduce platelet aggregation, it is recommended to use Dipiridimol in a dose of 75-225 mg / day in several doses. In severe cases, the dose may be increased to 600 mg / day.
For the prevention of thromboembolic syndrome, stent thrombosis and coronary artery bypass grafts - 50 mg along with ASA on the first day, then 100 mg, followed by 4 times a day (canceled 7 days after the operation, subject to continued administration of ASK 325 mg / day) or 100 mg 4 times a day for 2 days before surgery and 100 mg 1 hour after surgery (if necessary in combination with warfarin).
For the prevention of influenza and other acute respiratory diseases, especially during epidemics, take the following scheme: 50 mg / day 1 time in 7 days for 4-5 weeks.
For the prevention of relapses in patients with frequent respiratory viral infections, Dipyridamole is recommended to be taken as follows: 100 mg / day (2 times 50 mg with an interval of 2 hours) once a week for 8-10 weeks.
Dipyridamole is recommended to take on an empty stomach, without chewing the pills, coated, washing down with a small amount of liquid.
Adverse reactions
Palpitations, bradycardia, thrombocytopenia, changes in the functional properties of platelets, bleeding, feeling of ear congestion, noise in the head, arthritis. Vomiting, diarrhea, epigastric pain, as well as such symptoms as weakness, dizziness, nausea, headache, myalgia, rhinitis may occur. Usually these side effects disappear with long-term use of dipyridamole.
As a result of the potential vasodilating action, high-dose dipyridamole may cause arterial hypotension, hot flashes and tachycardia, coronary robbery (at doses of more than 225 mg per day).
Hypersensitivity reactions of rash or urticaria are possible.
If you experience side effects, you must inform your doctor.
Contraindications
· Acute myocardial infarction, unstable angina, common stenosing atherosclerosis of the coronary arteries.
· Subaortic aortic stenosis
· Decompensated heart failure
· Hypertrophic obstructive cardiomyopathy
· Arterial hypotension and hypertension
· Severe heart rhythm disturbances
· Hemorrhagic diathesis
· Diseases with a tendency to bleed (gastric ulcer and duodenal ulcer, etc.)
· Chronic obstructive pulmonary disease
· Hepatic and / or renal failure
· Hypersensitivity to the drug.
With care Lactation period, children age (up to 12 years old - lack of sufficient experience).
Drug interactions
Xanthine derivatives (coffee, tea) can weaken the vasodilator and antithrombotic action of dipyridamole. The use of Dipyridamole with both direct and indirect anticoagulants (heparin) and thrombolytic agents or acetylsalicylic acid increases the risk of hemorrhagic complications, which must be considered when sharing.
Dipyridamole may enhance the effect of antihypertensive drugs.
Dipyridamole may impair the anticholinergic properties of cholinesterase inhibitors.
The antiaggregative effect is enhanced when taking antibiotics of cephalosporins (cefemandol, cefeperazone, cephatetan), penicillin antibiotics, tetracyclines, chloramphenicol, beta lactams, nicotinic acid.
Antacids reduce the maximum concentration due to decreased absorption.
Special instructions
To reduce dyspeptic phenomena taken with milk.
During treatment, you should avoid the use of natural coffee and tea, weakening the effect of dipyri-damola.
In coronary robbery syndrome, aminophylline is indicated to improve intracardiac blood flow.
Overdosage
Symptoms: short-term hypotension.
Treatment: symptomatic (incl.management of vasopressor agents).
- Brand name: Dipyridamole-FPO
- Active ingredient: Dipyridamole
- Dosage form: Coated pills.
- Manufacturer: Obolensky OP
- Country of Origin: Russia
Studies and clinical trials of Dipyridamole (Click to expand)
- Inhibition of herpes simplex virus reactivation by dipyridamole in a mouse model
- Prevention of human pancreatic cancer cell-induced hepatic metastasis in nude mice by dipyridamole and its analog RA-233
- Performance of a polyurethane vascular prosthesis carrying a dipyridamole (Persantin®) coating on its lumenal surface
- Dipyridamole enhancement of drug sensitivity in acute lymphoblastic leukemia cells
- Flow cytometric evaluation of platelet activation in blood collected into EDTA vs. Diatube-H, a sodium citrate solution supplemented with theophylline, adenosine, and dipyridamole
- Molecularly imprinted polymer microspheres with nanopore cavities prepared by precipitation polymerization as new carriers for the sustained release of dipyridamole
- Trial of platelet-inhibiting drug in scleroderma double-blind study with dipyridamole and aspirin
- Reduced red blood cell deformability in patients with rheumatoid vasculitis improvement after in vitro treatment with dipyridamole
- Determination of dipyridamole using TCPO–H2O2 chemiluminescence in the presence of silver nanoparticles
- The effect of dipyridamole on tissue perfusion following freezing injury in the rat
- Random control trial of a short course of aspirin and dipyridamole (Persantin) for femorodistal grafts
- Methodology of internal standard selection. Comment on the work of Wang and co-workers: simultaneous determination of dipyridamole and salicylic acid in human plasma by high-performance liquid chromatograph-mass spectrometry
- Quantitative determination of dipyridamole in human plasma by high-performance liquid chromatography–tandem mass spectrometry and its application to a pharmacokinetic study
- Simultaneous determination of dipyridamole and salicylic acid in human plasma by high performance liquid chromatography-mass spectrometry
- Dipyridamole versus intracoronary injection of contrast medium for the evaluation of coronary reserve in man: A comparative study
- Quantitative demonstration of dipyridamole-induced coronary steal and alteration by angioplasty in man: Analysis by simultaneous, continuous dual doppler spectral flow velocity
- Effects of caffeine and theophylline on coronary hyperemia induced by adenosine or dipyridamole
- Dipyridamole versus verapamil for treatment of no-reflow during primary angioplasty
- Ethylenediaminetetraacetic acid plus citrate-theophylline-adenosine-dipyridamole (EDTA-CTAD): A novel anticoagulant for the flow cytometric assessment of platelet and neutrophil activation ex vivo in whole blood
- Dipyridamole plastic membrane electrodes based on individual and mixed ion-exchangers of dipyridamolium phosphotungstate and tetraphenylborate
- Effect of Dipyridamole on Kidney Function in Cirrhosis
- Hepatic sinusoidal fibrosis induced by cholesterol and stilbestrol in the rabbit: 1. Morphology and inhibition of fibrogenesis by dipyridamole
- Enhancement of an anti-tumor effect of interferon by dipyridamole in established human malignant melanoma cell lines
- Dipyridamole enhancement of doxorubicin-induced translocation of nucleophosmin and inhibition of cell growth in HL-60 cells