Alprostadil (When ATH C01EA01)

When ATH:
C01EA01

Characteristic.

A synthetic analog of a natural prostaglandin E₁ (PGE₁). White or almost white crystalline powder with a melting point between 115 and 116 °C, solubility at 35 °C — 8000 g / 100 ml of bidistilled water. Molecular weight - 354,49.

Pharmacological action.
Vasodilator, antiagregatine.

Application.

Concentrate / lyophilisates for solution for infusion: chronic obliterating peripheral arterial disease stage III-IV (Fontaine classification), accompanied by pain at rest or trophic changes. Occlusive disease with severe intermittent claudication (if not shown surgery), limb artery atherosclerosis, diabetic angiopathy, thromboangiitis obliterans (Buerger's disease), Raynaud's syndrome with trophic disorders, vasculitis, systemic scleroderma, leg cramps, peripheral circulatory disorders as a result of the damaging effects of physical factors, especially vibration superlimiting. Ductus-dependent congenital heart defects in newborns (to temporarily maintain the functioning of the ductus arteriosus until the reconstructive cardiac surgery), incl. mitral atresia, pulmonary atresia, tricuspid valve, tetrada Fallo.

Lyophilisate for solution for injection intracavernosal: neurogenic erectile dysfunction, Vascular, psychogenic or mixed aetiology; carrying out pharmacological tests in the diagnosis of erectile dysfunction.

Contraindications.

Concentrate / lyophilisates for solution for infusion: hypersensitivity, pregnancy, lactation. In neonatology: depression of respiratory function, respiratory distress syndrome, state-of spontaneous staunchly ductus arteriosus.

Lyophilisate for solution for injection intracavernosal: hypersensitivity, predisposition to prolonged erections (drepanocytemia, incl. if you suspect, mnozhestvennaya myeloma, leukemia and others.), anatomical deformation of the penis (angulation, kavyernoznyi fibrosis, Peyronie's disease), urethrostenosis, gipospadiя, Age to 18 and older 75 years (no experience in the use of these groups of patients); men, which is contraindicated or not recommended sexuality; the presence of penile implant.

Restrictions apply.

Concentrate / lyophilisates for solution for infusion: acute and subacute myocardial infarction, incl. transferred over the last 6 Months; severe or unstable angina form, decompensated chronic heart failure, hypotension, cardiovascular failure (special attention should be paid to monitoring the load capacity of the carrier solution), swelling or infiltrative changes in the lungs, severe bronchial obstruction with signs of respiratory distress, hepatic failure (incl. history), states, characterized by an increased risk of bleeding (gastric ulcer and duodenal ulcer, severe vascular disease of the brain, proliferative retinopathy with a propensity to bleed, extensive trauma and others.), hemodialysis (treatment should be carried out in the period postdializnom), diabetes mellitus type 1, especially when extensive vascular lesions (in elderly patients), concomitant therapy with vasodilating or anticoagulant drugs. In neonatology: bradipnoé, hypotension, tachycardia or hyperthermia.

Lyophilisate for solution for injection intracavernosal: thrombocytopenia, polycythemia, venoznыy thrombosis (incl. predisposition), increased blood viscosity, ʙalanit, uretrit.

Side effects.

During infusion,

From the nervous system and sensory organs: headache, dizziness, paraesthesia, convulsions, fatigue, feeling of uneasiness, violation of the sensitivity of the skin and mucous membranes; rarely - confusion, psychosis.

Cardio-vascular system and blood (hematopoiesis, hemostasis): low blood pressure, tachycardia, kardialgija, abnormal heart rhythm, OF блокада, redness of the skin; rarely - the development and deepening of heart failure, leukopenia or leukocytosis.

From the respiratory system: breathlessness; rare - respiratory distress syndrome, acute pulmonary edema.

From the digestive tract: discomfort in the epigastric region, nausea, vomiting, diarrhea, increase in liver transaminases; rarely - hyperbilirubinemia.

With the genitourinary system: rarely - renal failure, hematuria.

On the part of the musculoskeletal system: arthralgia; with prolonged continuous use (more 4 Sun) - Reversible hyperostosis of tubular bones.

Allergic reactions: skin rashes, hives, itch.

Other: increased perspiration, hyperthermia, chills, swelling of the limbs, into a vein which conducts infusion; rare - increase in titer of C-reactive protein; injection site reactions - pain, edema, эritema, violation of the sensitivity, phlebitis proximal space on / in the (to 40% patients).

Rarely (to 1% cases): shock, acute heart failure, giperʙiliruʙinemija, bleeding, drowsiness, bradipnoé, decrease in respiratory function, tachypnea, anurija, impairment of renal function, gipoglikemiâ, ventricular fibrillation, AV блокада II степени, supraventricular arrhythmia, tension of the neck muscles, irritability, gipotermiя, giperkapniя, flushing of the skin, hematuria, peritoneal signs, taxifilaksija, hyperkalemia, thrombocytopenia, anemia.

Newborns: apnea (rate 10-12%), elevated temperature (14%), flushing of the skin (about 10%, especially when a / introduction and), bradikadiâ (7%), decrease in blood pressure (4%), convulsions (4%), tachycardia (3%); about 2% - Diarrhea, sepsis; about 1% - Cardiac arrest, swelling, DIC, kaliopenia; ≤1% - bleeding in the brain, Excessive extension of the neck, gipotermiя, jitters, slackness, congestive heart failure, AV блокада II степени, supraventricular tachycardia, ventricular fibrillation, bradipnoé, stridor, giperkapniя, respiratory depression, tachypnea, regurgitation of gastric contents, giperʙiliruʙinemija, anemia, bleeding, thrombocytopenia, anurija, hematuria, peritoneal signs, gipoglikemiâ, hyperkalemia; during the course of treatment (within a few weeks) reported hyperostosis in the bone of the lower extremities (cm. and "Safety Precautions").

If intracavernous administration

Local reactions: penile pain (37%), unduly prolonged erection (to 04.06 am - 4%), hematoma (3%) and ecchymosis (2%) at the injection site (associated with improper administration technique), the formation of fibrotic nodules and Peyronie's disease (3–8%), swelling of the penis (1%), rash on the penis (1%); less 1% - Priapism (0,4%), ʙalanit, hemorrhage at the injection site; inflammation, itching and swelling at the injection site, bleeding from the urethra, Penile Disorders, incl. heat sensation in the penis, numbness, fungal infection, irritation, hypersensitivity, fimoz, rash, эritema, venous shunt, painful erection, abnormal ejaculation.

Systemic effects (rarely): pain and swelling of the scrotum and testes, increased urination, urinary incontinence, fluctuations in blood pressure (increase or decrease), tachycardia, supraventricular beats, the peripheral blood circulation, fatigue, headache, gipesteziya, swelling of the feet, hyperhidrosis, nausea, dry mouth, increase in serum creatinine, leg cramps, weakness in the buttocks, topoalgia (chest, in the buttocks, pelvic, in the legs, genitals, stomach), midriaz, flu-like symptoms.

Cooperation.

Pharmaceutical incompatible with solutions of other drugs.

When the infusion method of administration: may potentiate the effect of antihypertensive drugs, vasodilators and antianginal drugs; the simultaneous use of alprostadil in patients, taking drugs, anti-clotting (antykoahulyantы, antiagregantы) It may increase the chance of bleeding; in combination with cefamandole, cefoperazone, tsefotetanom and thrombolytic - increases the risk of bleeding; sympathomimetic (epinephrine, norepinephrine) - Reduce the vasodilator effect; must be considered, that interaction is possible even in the case, If these drugs were used long before, It was begun therapy with alprostadil.

If intracavernous introduction joint appointment with antihypertensive drugs, Diuretics, NSAIDs, insulin and oral hypoglycemic drugs does not affect the efficacy and safety of alprostadil.

Overdose.

Concentrate / lyophilisates for solution for infusion

Symptoms: decrease in blood pressure, flushing of the skin, weakness; in newborn (Besides) - Apnea, bradycardia.

Treatment: slowing or stopping the infusion, simptomaticheskaya therapy; when the signs of depression of the respiratory center in the newborn is a ventilator.

Lyophilisate for solution for injection intracavernosal

Symptoms: penile pain, prolonged erection and / or priapism, irreversible deterioration of erectile function.

Treatment: If an erection lasts for less 6 no, necessary medical supervision, tk. often spontaneous regression; if more 6 h - Carrying intracavernous injection agonists (such as ephedrine, epinephrine, Phenylephrine), perform aspiration of blood from the corpora cavernosa or, if necessary, surgery.

Dosing and Administration.

B / A, I /, intrakavernoznye. Dosage regimen individual, depending on the indication and the dosage form.

Precautions.

Alprostadil infusion may be used only doctors, with experience in Angiology, familiar with modern methods of continuous monitoring of the state of the cardiovascular system and to have the appropriate equipment. During treatment requires monitoring of blood pressure, Heart Rate, biochemical parameters and blood clotting (in disorders of blood coagulation or simultaneous therapy drugs, that affect clotting).

Patients with coronary artery disease, and patients with peripheral edema and renal dysfunction (sыvorotochnыy creatinine >1,5 mg / dL) must be supervised in the hospital during treatment with alprostadil and within days after its termination. To prevent symptoms of fluid overload in patients with renal insufficiency, the volume of a fluid as possible should not exceed 50-100 ml / day. Always a dynamic monitoring of the patient: control of blood pressure and heart rate, if necessary - the control of body weight, fluid balance, measurement of central venous pressure or echocardiographic examination conducting.

Phlebitis (proximal to the site of administration), usually, It is not a cause for discontinuation of therapy, signs of inflammation disappear after a few hours after cessation of the infusion, or change the injection site; specific treatment in such cases does not require. CVC to reduce the frequency of symptoms of the side effects of the drug.

Due to the risk of sleep apnea in newborns should be applied alprostadil institutions, with qualified personnel and equipment, necessary to provide intensive care for children, under the constant control of blood pressure, if the conditions for immediate mechanical ventilation.

Apnea (cm. Side effects) most often observed in infants with a birth weight of less than 2 kg and typically occurs within the first hour of infusion. Appointment alprostadil newborns can lead to obstruction of the hole pylorus. This effect, apparently, It depends on the duration of therapy and cumulative dose of drug. Newborns, receiving alprostadil at recommended doses more 120 no, You should be carefully monitored.

In the treatment of erectile dysfunction before treatment with alprostadil should be held diagnostics treatable causes of erectile dysfunction. Dose selection should be carried out in each patient individually, under the supervision of a physician, the control of the cardiovascular system and the duration of erections. To reduce the risk of prolonged erections or priapism when selecting the dose necessary to raise it slowly, until the minimum effective dose (the appearance of an erection lasting no more than 1 h and sufficient for sexual intercourse). During the selection of the dose the patient should be under medical supervision until the disappearance of erection. With the ineffectiveness of the first dose of the second, higher, It may be introduced no earlier than 1 no. If there is a response interval between doses should be at least 1 day. Self-injection, patients may be prescribed only after a detailed briefing of the patient and the development of self-injection technology. Treatment is initiated with a dose of, chosen doctor. Patients are encouraged to visit the doctor every 3 months to evaluate the efficacy and safety of the treatment and, if necessary, to adjust the dose.

The patient should be warned, that in the course of treatment he should tell your doctor about all the cases, an erection lasting more than 4 no. Untimely correction of priapism can lead to permanent damage to the tissues of the penis and permanent loss of potency.

Alprostadil is not designed for simultaneous use with other drugs to treat erectile dysfunction.

Cautions.

It should strictly observe the relevant dosage form alprostadil specific indications for its use.

You can not mix with the solutions of other drugs.

Cooperation