Composition, form of production and packaging
Lyophilizate for the preparation of solution for intracavitary injection 1 vial.
alprostadil 10 Ојg
- "- 20 mcg
Vials (1) complete with a solvent in a syringe, needles (2 pcs.) And napkins (2 pcs.) - plastic boxes.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2005.
PHARMACHOLOGIC EFFECT
The drug prostaglandin E 1 , used for erectile dysfunction. With intracavernous injection (into the penis) alprostadil inhibits? 1- adrenoreceptors of the tissues of the penis, relaxes the musculature of the cavernous bodies, increases blood flow and improves microcirculation. Alprostadil causes an erection by relaxation of the trabecular smooth muscles of the cavernous bodies and dilatation of the cavernous arteries, which leads to the expansion of the lacunar spaces and the closure of the blood flow by pressing the venules against the protein membrane (occlusion of the penis veins).
Alprostadil suppresses the aggregation of platelets.
The onset of action of the drug 5-10 minutes after the administration, the duration of the action is 1-3 hours.
INDICATIONS
- erectile dysfunction of neurogenic, vascular, psychogenic or mixed etiology;
-diagnosis of erectile dysfunction (as an additional means to other diagnostic tests).
DOSING MODE
The first injections of the drug should be carried out in the doctor's office by specially trained medical personnel. Self-injection can only begin after a detailed briefing of the patient and mastering the technique of self-injection.
The doctor should carefully evaluate the patient's skills and his ability to perform this procedure. Intracavernous administration should be carried out in accordance with the rules of asepsis.
The drug is used by direct intracavernous administration using needles of size 27-30 G, length 13 mm. The drug is introduced into the dorso-lateral part of the proximal third of the penis.
Selection of initial dose
The dose is selected individually by careful titration under the supervision of a physician. It is necessary to adhere to the resulted scheme (see table 1) of introduction of a preparation in view of the erectile answer until the dose causing an erection the duration sufficient for the sexual certificate or act, but no more than 60 minutes will be reached. If there is no specific dose, the next higher dose can be administered after 1 hour. If there is a response, the interval between doses should be at least 1 day. The patient should be in the doctor's office until the full detemtsentsiya comes (stopping the erection, reducing the size of the penis).
Table 1
Dose for erectile dysfunction of neurogenic etiology (with spinal cord injuries) Dose for erectile dysfunction of vascular, psychogenic and mixed etiology
Initial injection 1.25 Ојg 2.5 Ојg
Second injection 2.5 mcg With partial response to the first injection - 5 mcg; in the absence of response - 7.5 mcg
The third injection of 5 Ојg-
The value of incremental increase in the dose until the optimal dose is 5 Ојg 5-10 Ојg
Supportive therapy
The dose chosen for self-injection should cause the patient to have an erection sufficient for a sexual intercourse, with a duration of no more than 1 hour. If the duration of the erection exceeds 1 hour, the dose should be reduced. Self-administration of the drug at home should begin with a dose set in the doctor's office. If necessary, the dose should be changed only after consultation with the doctor and in accordance with the instructions for the selection of a dose. The lowest effective dose should be given. The recommended frequency of injections is no more than 3 times a week, but not more than 1 time / day. The erection usually comes in 5-20 minutes after the injection.
The average dose of alprostadil at the end of 6 months of therapy is 20.7 Ојg. In most patients, the maintenance dose was 5-20 Ојg. Doses over 60 Ојg are not recommended.
As an additional tool for the diagnosis of erectile dysfunction , a single dose of the drug is used, which causes a normal erection. The drug is used in pharmacological tests, as an additional tool for performing duplex or Doppler ultrasound, in a sample for washing out xenon-133, radioisotope phallography and arteriography of the penis, which allows you to visualize and assess the condition of the vessels of the penis.
Terms of use
Preparation of solution for intracavernous administration
For dilution, use only the supplied solvent or water for injection with benzyl alcohol 0.9%. After dilution in 1 ml of solvent, the volume of the resulting solution is 1.13 ml. In 1 ml of this solution contains 10.5 Ојg or 20.5 Ојg of alprostadil, however, after injection, 10 Ојg or 20 Ојg of alprostadil, respectively, occurs because 0.5 Ојg is lost due to adsorption on the walls of the syringe and vial. After dilution of the drug should not be added to the bottle any substances.
Before administration, the solution must be visually checked for particles or discoloration.
Self-injection procedure (for the patient)
1. Wash your hands with soap and water.
2. Remove the plastic protective cap from the bottle.
3. Using one of the supplied alcohol-impregnated napkins, wipe the rubber stopper of the vial (the second napkin will be needed later). The used tissue should be discarded.
4. Unpack the large 22G11 / 2 needle without removing the plastic protective cap from it. Connect the needle to the syringe by putting the needle base on the syringe and firmly pressing.
5. Carefully remove the protective cap from the needle.
6. Holding the syringe with the needle up, move the plunger of the syringe to the "1 ml" mark (to remove excess solvent from the syringe.)
7. Push the rubber stopper of the vial into the center of the bottle and press the piston down to insert the solvent into the vial.
8. Gently holding the syringe and the vial as one unit, with gentle circular motions, achieve complete dissolution of the powder. Do not use the drug if the resulting solution is cloudy, or has become stained, or contains any particles.
9. Turn the bottle upside down without removing the syringe. After making sure that the needle tip is below the liquid level, slowly pull the syringe piston toward yourself until the level of the solution reaches the desired mark on the syringe.
10. To remove air bubbles, tap the syringe lightly, or put the solution back into the vial, and then slowly re-dial it into the syringe.
11. Remove the needle from the vial and gently place the protective cap on it.
12. Open the package with a smaller needle (27G1 / 2), but do not remove the needle, but put the package aside.
13. Remove the larger needle from the syringe with the protective cap and set aside to discard.
14. While holding a syringe in one hand, take a smaller sized needle from the opened package without removing the plastic protective cap from it, and connect it to the syringe, as a larger needle was connected.
Chart A
The transverse section of the penis shows the injection site.
Veins, arteries, nerves
Cavernous bodies (two)
Places of injection:
insertion of a needle into one of the cavernous bodies
Urethra
Chart B
Sexual penis, top view; the injection sites are shaded.
Places of injection
The drug should be injected into one of the two areas of the penis, which are called cavernous bodies.
15. Carry out the procedure for self-administration of the drug should be in a sitting, standing or reclining position.
16. Injections should be performed only at the locations indicated on diagrams A and B. Avoid contact with visible veins. Repeated injections should be performed alternately on one side of the penis. Each time, you should choose a new point on the corresponding side for injection.
17. Take the head of the penis with your thumb and forefinger. Pull out the penis and hold it firmly with your fingers so that during the procedure it does not slip out. Men who have not undergone circumcision should take out the foreskin in order to pinpoint the location of the injection.
18. Thoroughly treat the skin at the injection site with an unused cloth impregnated with alcohol. Put this napkin aside.
19. Take the syringe with your thumb and forefinger, without placing your thumb on the piston. With a firm movement, insert the needle at an angle of 90 В° into the injection site indicated by the doctor (Fig. 1).
Figure 1: Insertion of the needle into the injection site
20. Use your thumb or forefinger to press the plunger. With slow confident movement, enter the entire contents of the syringe.
21. Remove the needle from the penis. While holding the penis from both sides, press the napkin impregnated with alcohol to the place of injection and hold it for about 3 minutes. If there is blood, then you should press the napkin until the bleeding stops.
22. After using the contents of this package, all materials should be discarded, adhering to the relevant safety rules. You can use the plastic wrapping of the drug Kaverdjekt as follows: place the used syringe, needle and bottle in a plastic container. Remove the red plastic locking device from the container and set it aside. Then close the container tightly, and a click should be heard. Remove the notched center of the label (where the red lock is drawn) to reveal the notch. To lock the container, completely push the red locking device into the groove. When the locking device is in its place, the container is securely locked and can be discarded. A container containing the used syringe, needles and vial can not be included in the recycling process.
SIDE EFFECT
Local reactions: pain and burning in the penis; in 4% of patients there was a prolonged erection (duration 4-6 hours); in 3-4% of patients - penile fibrosis, including penile angulation, formation of fibrous nodules and Peyronie's disease; 3% of patients had a hematoma at the injection site and 2% had ecchymosis at the injection site (these side effects are usually associated with injection technique rather than with alprostadil).
Less than 1% is priapism (duration of erection is more than 6 hours, frequency is 0.4%, in most cases spontaneous relaxation of the penis was observed), balanitis, hemorrhages at the injection site, inflammation, itching and swelling at the injection site, bleeding from the urethra, sensation of heat in the penis, numbness, fungal infection, irritation, hyperesthesia of the skin, phimosis, erythema, "venous discharge" from the cavernous bodies, painful erection, ejaculatory impairment.
Systemic reactions: most often - increased blood pressure, dizziness, headache, back pain, upper respiratory tract infection, flu-like syndrome, sinusitis, nasal congestion, cough, prostatitis, pain syndrome.
Less than 1% is testicular pain, testicular swelling, a feeling of heat in the testicles, a thickening of the testicles, reddening of the scrotum, pain in the scrotum, spermatoceles, swelling of the scrotum, hematuria, impaired urination, increased urination, mandatory urination, pelvic pain, AD, tachycardia, vasodilation, peripheral vascular disorders, supraventricular extrasystole, vasovagal reactions, hypoesthesia, muscle weakness, hyperhidrosis, rash, itching, nausea, dry mouth, increased serum creatinine, seizures and crooked muscles, dilated pupils.
Decrease in blood pressure and increased heart rate were observed when the drug was used at doses greater than 20 Ојg and 30 Ојg, respectively, and, apparently, were dose-dependent. However, these changes were not clinically significant; Only 3 patients discontinued treatment because of symptomatic hypotension.
CONTRAINDICATIONS
- diseases predisposing to the occurrence of priapism (sickle cell anemia, myeloma, leukemia);
- anatomical deformations of the penis (angulation of the penis, cavernous fibrosis, Peyronie's disease);
- presence of an implant of the penis;
- established hypersensitivity to the components of the drug.
The drug is not used in men who are contraindicated or not recommended sex life.
In persons under 18 years of age, the safety and efficacy of the drug have not been studied.
SPECIAL INSTRUCTIONS
Before starting treatment with the drug Kaverdzhekt, diagnosis of the causes of erectile dysfunction should be performed.
Continuous monitoring of the patient's self-administered condition should be carried out, especially in the initial period, when a dose change may be required. Every 3 months the patient is recommended to visit a doctor to assess the effectiveness and safety of treatment and dose adjustment (if necessary).
It is known that after intra-cavernous introduction of vasoactive drugs, including Kaverdzhekt, priapism may develop. To reduce the risk of priapism, the lowest effective dose should be given. The patient should immediately inform the doctor about all cases of erection lasting more than 4 hours. Treatment of priapism is conducted in accordance with established medical practice.
After intracavernous administration of the drug, penile fibrosis can develop, including penile angulation, formation of fibrous nodules and Peyronie's disease. The incidence of fibrosis may increase with increasing duration of drug use. To identify signs of fibrosis of the penis or Peyronie's disease, a regular examination of patients with a close examination of the penis is recommended. In patients with development of penile angulation, cavernous fibrosis or Peyronie's disease, treatment with the drug should be discontinued.
Since intracavernous administration may cause minor bleeding, patients using Cavageject should be informed of protective measures against infections transmitted by sexual and hematogenous pathways, including human immunodeficiency virus (HIV).
Patients receiving treatment with anticoagulants such as warfarin or heparin have an increased tendency to bleed after intra-cavernous injection.
In patients receiving MAO inhibitors and alpha-adrenomimetics, in the case of prolonged erection, a hypertensive crisis may develop.
In patients with IHD, chronic heart failure or lung diseases, sexual stimulation and sexual intercourse can lead to an exacerbation of the disease.
Alprostadil should be kept in compliance with the specific indications for its use.
There was no clinically significant effect of Kaverdzhekt on the results of a laboratory study of blood and urine.
The bottle with the diluted preparation is intended for single use and is discarded after use. The patient should be instructed on the rules for the destruction of the needle, syringe and vial.
OVERDOSE
Symptoms: pain in the penis, prolonged erection and / or priapism, irreversible deterioration of erectile function.
Treatment: if the erection lasts less than 6 hours, medical supervision is necessary, because often there is a spontaneous detumescence; if the erection persists for more than 6 hours, an intracavernous injection of alpha-adrenomimetics (ephedrine, epinephrine, phenylephrine, ethylhelin), or aspirate blood from cavernous bodies, or perform surgical treatment should be done. The patient should be under medical supervision until the disappearance of systemic phenomena and / or before the full detemntsentsii penis.
DRUG INTERACTION
Kaverdzhekt is not intended for mixing or simultaneous administration with other drugs, as well as for joint use with other drugs for the treatment of erectile dysfunction.
The possibility of pharmacokinetic interactions with other drugs has not been investigated.
Joint use with antihypertensive drugs, diuretics, hypoglycemic drugs (including insulin) or non-steroidal anti-inflammatory drugs does not have any effect on the safety or efficacy of the drug Kaverdzhekt.
The safety and efficacy of the joint use of the drug Kaverdzhekt with other vasoactive drugs has not been studied.
The presence of benzyl alcohol in the solvent reduces the degree of binding to the walls of the vial. In this regard, when using water for injection containing benzyl alcohol, a more stable solution is obtained and a more complete administration of the preparation is provided.
TERMS AND CONDITIONS OF STORAGE
List B. The drug should be stored out of reach of children at a temperature of no higher than 25 В° C. The undiluted solution should be stored in the original vial at a temperature of no higher than 25 В° C not more than 24 hours. Do not freeze or cool!
Conditions of leave from pharmacies
The drug is released by prescription.
