Instructions for Pentoxifylline
Composition Pentoxifylline:
One retard tablet contains: Pentoxifylline 400 mg. Excipients: Ethyl cellulose, calcium phosphate dibasic, magnesium stearate, talc; Shell composition: titanium dioxide, hydroxypropyl methylcellulose, diethyl phthalate, carmoisine varnish.
Pharmacodynamics Pentoxifylline:
pentoxifylline improves microcirculation and rheological properties of blood.
The mechanism of action of pentoxifylline is associated with inhibition of phosphodiesterase and the accumulation of cAMP in the smooth muscle cells of blood vessels and blood cells. Pentoxifylline inhibits platelet and erythrocyte aggregation, increases their elasticity, reduces plasma fibrinogen level and enhances fibrinolysis, which reduces blood viscosity and improves its rheological properties.
Having a weak myotropic vasodilating effect, somewhat reduces the total peripheral resistance and slightly dilates the coronary vessels. In general, improves microcirculation and oxygen supply to tissues in the central nervous system and limbs, and to a lesser extent in the kidneys.
Pharmacokinetics Pentoxifylline:
After oral administration, is rapidly and almost completely absorbed from the gastrointestinal tract. The drug almost does not bind to proteins. Most pentoxifylline is metabolized in the liver and excreted by the kidneys in the form of water-soluble metabolites (more than 90%).
The half-life of is 1.6 hours. In patients with severe renal impairment, the excretion of metabolites is slowed down. The maximum concentration of in blood plasma after a single oral administration is observed after 1 hour. By the 8th hour, the concentration is significantly reduced (up to 10% of the initial).
Side effects Pentoxifylline:
Most often, when taking pentoxifylline, adverse effects from the gastrointestinal tract may appear (nausea, feeling of fullness in the abdomen, stomach cramps, vomiting, diarrhea).
Sometimes dizziness and headache may occur. Occasionally, you can observe a decrease in blood pressure, angina pectoris, heart rhythm disturbance, a feeling of high tide. In rare cases, hypersensitivity reactions observed redness of the skin, itching, urticaria.
In some cases, jaundice (intrahepatic cholestasis) and an increase in the level of liver enzymes (transaminases, alkaline phosphatase) may appear. In isolated cases, the occurrence of very severe hypersensitivity reactions was described - angioedema, developing within a few minutes after taking pentoxifylline, convulsive spasms of the muscles of the bronchi, anaphylactic shock.
At the first signs of a hypersensitivity reaction, it is urgent to stop taking the drug and consult a doctor. There are separate reports of the possibility of bleeding (in the gastrointestinal tract, in the skin, in the mucous membranes), thrombocytopenia and aplastic anemia. In this regard, in the treatment with, regular monitoring of the blood picture is necessary.
Indications Pentoxifylline:
Pentoxifylline is used for peripheral circulation disorders caused by atherosclerosis, diabetes mellitus (diabetic angiopathy), inflammation; acute and chronic cerebrovascular disorders of the ischemic type; atherosclerotic and discirculatory encephalopathies; angioneuropathies (paresthesia, Raynaud's disease); trophic tissue disorders due to a violation of arterial or venous microcirculation (trophic ulcers, post-thrombophlebic syndrome, frostbite, gangrene); obliterating endarteritis; acute, subacute and chronic circulatory failure in the retina or choroid; hearing impairment of vascular origin.
Contraindications Pentoxifylline:
Pentoxifylline is contraindicated in the following cases: Increased sensitivity to , other methylxanthines or other components of the finished dosage form;
acute myocardial infarction;
Massive bleeding
acute hemorrhagic stroke;
-expressed coronary or cerebral atherosclerosis; severe cardiac arrhythmias;
retinal hemorrhage; -pregnancy and lactation, Pentoxifylline
- age up to 18 years.
Precautions: Caution should be exercised when prescribing Pentoxifylline to patients with peptic ulcer of the stomach and duodenum, patients who have recently undergone surgery (risk of bleeding).
For patients with labile blood pressure and with a tendency to hypotension and patients with severe renal impairment, the dose is gradually increased and individually selected.
Pregnancy and lactation: contraindicated
Drug Interactions Pentoxifylline:
is able to enhance the action of antihypertensive drugs and anticoagulants. In patients with diabetes who are being treated with insulin or taking antidiabetic drugs, can enhance the hypoglycemic effect of antidiabetic drugs, up to the occurrence of hypoglycemic reactions.
Dosage Pentoxifylline:
The duration of treatment and the dosage regimen of are determined individually by the attending physician, depending on the clinical picture of the disease and the resulting therapeutic effect.
The drug is taken orally immediately after a meal, without chewing, with a sufficient amount of liquid.
For adults, is prescribed starting with 0.2 g 3 times a day. Prolonged dosage forms are prescribed 2 times a day. The course of treatment is 2-3 weeks or more.
Overdose Pentoxifylline:
Clinical picture: dizziness
vomiting
drop in blood pressure
tachycardia,
redness of the skin,
loss of consciousness, fever (chills), agitation,
areflexia,
tonic-clonic convulsions,
vomiting "coffee grounds",
arrhythmias.
Overdose treatment is symptomatic.
Particular attention should be directed to maintaining blood pressure and respiratory function. Convulsive seizures are relieved by the administration of diazepam.
Urgent measures in case of severe anaphylactic reactions (shock):
when the first signs appear (sweating, nausea, cyanosis), stop taking the drug immediately;
In addition to other necessary measures, provide a lower position of the head and upper body and provide freedom for breathing;
urgent medical measures: injected into / in epinephrine (adrenaline).
If necessary, the administration of epinephrine can be repeated.