Universal reference book for medicines
Product name: AGAPURIN (AGAPURIN)

Active substance: pentoxifylline

Type: A drug that improves microcirculation.
Angioprotector
Manufacturer: ZENTIVA (Slovak Republic)
Composition, form of production and packaging
Solution for injections is
transparent, colorless.

1 ml of 1 amp.

pentoxifylline 20 mg 100 mg

Excipients: sodium chloride, water d / and.

5 ml - ampoules (5) - packs of cardboard.

INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2008.

PHARMACHOLOGIC EFFECT

Spasmolytic agent from the group of purines.
Improves microcirculation and rheological properties of blood. The mechanism of action is associated with inhibition of phosphodiesterase and an increase in cAMP content in platelets and ATP in erythrocytes with a simultaneous saturation of the energy potential, which in turn leads to vasodilation, a decrease in total peripheral vascular resistance, an increase in the impact and minute blood volume without significant changes in heart rate.
Expanding the coronary arteries, increases the delivery of oxygen to the myocardium (antianginal effect), the vessels of the lungs - improves oxygenation of the blood.Increases the tone of the respiratory musculature (intercostal muscles and diaphragm).
With intravenous administration leads to an increase in collateral circulation, an increase in the volume of flowing blood through a unit of section. It leads to an increase in the content of ATP in the brain, favorably affects the bioelectric activity of the central nervous system. Reduces the viscosity of the blood, increases the elasticity of the erythrocyte membrane (due to the effect on the pathologically altered erythrocyte deformability). Improves microcirculation in areas of impaired blood circulation.
In the occlusal lesion of peripheral arteries ("intermittent" lameness), leads to an elongation of the distance of walking, elimination of night cramps of gastrocnemius muscles and pain at rest.

PHARMACOKINETICS

The drug is rapidly metabolized in the liver.
In the process of metabolism, several active metabolites are formed, the main ones being metabolite 1 and metabolite 5. Their concentrations in the blood plasma are 5 and 8 times (respectively) higher than the concentration of the starting substance.
It is excreted in the form of metabolites (94%) and through the intestine (4%), in the first 4 hours up to 90% of the dose is excreted.
Unchanged, 2% of the drug is withdrawn.Pentoxifylline and its metabolites do not bind to blood plasma proteins.
With severe renal dysfunction, excretion of metabolites is slowed down.
When liver function is disrupted, the half-life is prolonged and bioavailability is increased.
INDICATIONS

- violation of peripheral blood circulation against atherosclerotic, diabetic and inflammatory processes (including "intermittent" lameness caused by atherosclerosis, diabetic angiopathy, obliterating endarteritis);

- trophic tissue disorders due to violation of arterial or venous microcirculation (varicose ulcers, gangrene, frostbites);

- angioneuropathy (paresthesia, acrocyanosis, Raynaud's disease);

- Acute and chronic disorder of cerebral circulation of ischemic origin (including cerebral atherosclerosis);

- conditions after hemorrhagic or ischemic stroke;

- Disturbances of blood circulation in the vessels of the eye (acute and chronic circulatory insufficiency of the mesh and vascular membranes of the eye);

- Dysfunction of the middle ear of vascular genesis, accompanied by deafness.

DOSING MODE

The drug can be administered iv, in / a, / m.
When carrying out infusions, the patient should be in a prone position.
Intravenous: 100 mg (1 amp.) In 250-500 ml of a 0.9% solution of sodium chloride or in a 5% solution of dextrose (glucose) drip for 1.5-3 hours. With good tolerability, the dose can be increased by 100 mg per day.
The maximum daily dose is 300 mg.
Intraarterial: first 100 mg of the drug in 20-50 ml of 0.9% sodium chloride solution, in the following days - 200-300 mg in 30-50 ml of the solvent.
Enter with the speed of 100 mg (5 ml of 2% solution of the drug) for 10 minutes. When expressed atherosclerosis of the cerebral vessels can not be introduced into the carotid artery.
Patients with chronic renal failure (CC less than 10 ml / min) are administered 50-70% of the usual dose.

Intramuscularly: 1-2 times / day for 100 mg (1 amp.).

SIDE EFFECT

From the side of the central nervous system: headache, dizziness;
anxiety, sleep disorders, convulsions.
From the cardiovascular system: tachycardia, arrhythmia, cardialgia, rarely - the progression of symptoms of angina pectoris, lowering blood pressure.

From the skin: hyperemia of the skin of the face, "tides" of blood to the skin of the face and upper chest, swelling, increased brittleness of the nails.

On the part of the digestive system: nausea, vomiting, a feeling of heaviness in the stomach, a decrease in appetite, intestinal atony, exacerbation of cholecystitis, cholestatic hepatitis, bleeding from the mucous membranes of the stomach, intestines.

From the senses: a visual impairment, scotoma.

On the part of the hemostasis system and hemopoiesis: thrombocytopenia, leukopenia, pancytopenia, hypofibrinogenemia;
bleeding from the vessels of the skin.
Allergic reactions: rarely - itching, skin hyperemia, urticaria, angioedema, anaphylactic shock.

On the part of laboratory indicators: an increase in the activity of hepatic transaminases: ALT, ACT, LDG and APF.

CONTRAINDICATIONS

- severe coronary or cerebral atherosclerosis;

acute myocardial infarction;

- marked violations of the rhythm of the heart;

uncontrolled arterial hypotension;

- porphyria;

- massive bleeding;

- hemorrhage in the retina of the eye;

- acute hemorrhagic stroke;

- pregnancy, lactation;

- age under 18 years (effectiveness and safety not established);

- Hypersensitivity to pentoxifylline and substances from the group of xanthine derivatives.

With caution: patients with labile arterial pressure, a tendency to arterial hypotension, chronic heart failure, a penchant for hemorrhages, a condition after recent surgery, liver and / or kidney failure.

PREGNANCY AND LACTATION

Contraindicated in pregnancy and lactation.

APPLICATION FOR FUNCTIONS OF THE LIVER

With insufficient renal function with a creatinine level above 400 mmol / l, doses are reduced by 30-50%.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

With caution: liver failure.

APPLICATION FOR CHILDREN

Contraindication: age under 18 years (efficacy and safety not established).

APPLICATION IN ELDERLY PATIENTS

In elderly people, a dose reduction (reduction in the rate of excretion) may be required.

SPECIAL INSTRUCTIONS

Treatment should be carried out under the control of blood pressure.
Patients with chronic heart failure should be compensated for blood circulation.
In patients with diabetes mellitus, who take hypoglycemic drugs, the use of large doses can cause severe hypoglycemia (dose adjustment is required).

When used concomitantly with anticoagulants, care should be taken to closely monitor blood coagulation system performance.

In patients who have recently undergone surgery, systematic monitoring of hemoglobin and hematocrit concentration is necessary.

The administered dose should be reduced in patients with low and unstable blood pressure.

In elderly people, a dose reduction (reduction in the rate of excretion) may be required.

Smoking can reduce the therapeutic effectiveness of the drug.

The compatibility of a solution of pentoxifylline with another infusion solution should be checked in each case.

OVERDOSE

Symptoms: weakness, dizziness, marked decrease in blood pressure, syncope, tachycardia, drowsiness, loss of consciousness, tonic-clonic convulsions, increased nervous excitability, hyperthermia, areflexia, signs of gastrointestinal bleeding (vomiting "coffee grounds").

Treatment: symptomatic, aimed at maintaining the function of breathing and blood pressure.

DRUG INTERACTION

Pentoxifylline may enhance the effect of drugs affecting the blood coagulation system (indirect and direct anticoagulants, thrombolytics), anitibiotics (including cephalosporins: cefamandol, cefoperazone, cefotetana), valproic acid.

Increases the effectiveness of antihypertensive drugs, insulin and oral hypoglycemic agents.

Cimetidine increases the concentration of pentoxifylline in the blood plasma (risk of side effects).

Joint application with other xanthines can lead to excessive nervous excitation.

TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

Store at a temperature of 10-25 ° C in a dry and inaccessible place for children.

Shelf life -
3 years.

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