Каверджект

Каверджект – the drug of a wide range of pharmacological action used for therapy of disturbances of erectile function.

Form of release and structure

Каверджект release in the form of lyophilisate for preparation of solution for intra cavernous introduction: the lyophilized porous weight or powder from almost white till white color; solvent – colourless transparent (in bottles, on 1 bottle in a plastic box complete with solvent (in the one-time syringe on 1 ml), 2 injection cannulas and 2 napkins).

Is a part of 1 bottle:

• Active ingredient: alprostadit – 10 or 20 mkg;
• Auxiliary components: lactose, sodium citrate.

Solvent: benzyl alcohol – 9000 mkg, water for injections – to 1 ml.

Indications to use

• Treatment of disturbances of erectile function of the psychogenic, neurogenic, vascular or mixed etiology;
• Diagnosis of erectile dysfunction in a complex with other diagnostic tests.

Contraindications

Absolute:

• The multiple myeloma, drepanocytic anemia, leukosis and other diseases contributing to emergence of a priapism;
• Anatomic defects of a penis (cavernous fibrosis, penis angulation, Peyroni's disease);
• Penis implant;
• The diagnosed hypersensitivity to Kaverdzhekt's components.

Also it is not necessary to use drug at men to whom sex life is not recommended or is contraindicated.

It is necessary to use with care of Kaverdzhekt to persons under 18 as efficiency and safety of its use in this age group is not studied.

Route of administration and dosage

The solution prepared from lyophilisate is intended for direct intra cavernous introduction to a dorsolateral part of a proximal third of a penis, with use of syringe needles of 27-30 G in size and 13 mm long.

The initial dose is selected the attending physician individually for each patient, by means of careful titration.

Depending on the reasons of erectile dysfunction it is necessary to adhere to the following schemes (taking into account erectile reaction) before achievement of a dose, duration, causing an erection sufficient for full sexual intercourse (but no more than 1 hour). Calculation of a dose in case of disturbances of an erection of a neurogenic etiology (injury of a spinal cord):

• The I (initial) injection – 1,25 mkg;
• The II injection – 2,5 mkg;
• The III injection – 5 mkg.

The size of step-by-step increase in a dose of drug up to achievement of optimum – 5 mkg.

Calculation of a dose in case of disturbances of an erection of the psychogenic, vascular and mixed etiology:

• The I (initial) injection – 2,5 mkg;
• The II injection – in case of the partial answer to the first injection – 5 mkg; in the absence of the answer – 7,5 mkg;
• The III injection – does not become.

The size of step-by-step increase in a dose of drug up to achievement of optimum – 5-10 mkg.

In case of lack of reaction to the next injection, the following, higher dose, it is necessary to enter 1 hour later. In the presence of the answer the interval between injections has to be not less days.

The patient has to be under observation of the doctor until there comes complete cessation of an erection – detumescence.

At a maintenance therapy the dose chosen for a self-injection has to provide the erection sufficient for sexual intercourse lasting no more than 1 hour. In case of exceeding of this time the dose needs to be lowered.

Independent therapy in house conditions begins with the dose defined in an office of the doctor if it needs to be changed, then it is necessary to consult with the doctor and according to his instructions to pick up a dose (the smallest effective). It is recommended to carry out introduction of injections no more than 3 weekly and not more often than 1 time a day. The standard time necessary for emergence of a steady erection – 5-20 min. from the beginning of administration of drug.

Later half a year from an initiation of treatment the required average dose of an alprostadil makes 20,7 mkg. For most of patients a maintenance dose – 5-20 mkg; the most admissible – 60 mkg.

When using Kaverdzhekt's as an additional tool it is necessary to apply the single dose causing a normal erection to diagnosis of erectile dysfunction. In pharmacological tests the drug is administered as additional (for conducting Doppler or duplex ultrasonic testing, in test on xenon-133 washing away, arteriography of a penis or a radio isotope fallografiya) to visualize and make assessment of a condition of vessels of a penis.

For preparation of solution from lyophilisate as solvent for cultivation it is necessary to use the ready structure which is applied in the syringe or water for injections with benzyl alcohol of 0,9%. The volume of the received solution after cultivation in 1 ml of solvent – 1,13 ml, with the maintenance of an alprostadil – 10,5 mkg or 20,5 mkg in 1 ml. As a result of an injection respectively 10 mkg or 20 mkg of an alprostadil as 0,5 mkg are lost because of adsorption on walls of a bottle and the syringe get to an organism. After drug is divorced, it is not necessary to add any substances to a bottle.

Before introduction solution should be investigated visually on discoloration or existence of particles.

For holding a procedure of a self-injection of Kaverdzhekt follows the patient:

1. To carefully wash hands water with soap;
2. To remove a protective plastic lid from a bottle;
3. To wipe a rubber bung of a bottle of one of the enclosed napkins impregnated with alcohol (the used napkin needs to be thrown out);
4. To unpack the big needle marked "22 G11/2"; without removing a plastic protective cap from a needle, to connect it to the syringe, having put on the basis a neck of the syringe and having strong pressed;
5. To remove a protective cap from a needle;
6. To remove excess of water from the syringe: to bring the piston to the mark "1 ml", holding the syringe vertically, a needle tip up;
7. To pierce a needle in the central part a rubber bung of a bottle, to press on the piston down, to enter water into a bottle;
8. Holding a bottle and the syringe as a single whole, accurately, easy roundabouts completely to dissolve powder; not to use solution if it muddy, got coloring, or contains any inclusions;
9. Without taking out the syringe to turn a bottle upside down, to be convinced that the tip of a needle is lower than the level of solution, to slowly pull the piston on itself until the level of solution reaches a required point in the syringe;
10. It is easy to knock on the syringe to remove vials of air, or again to enter solution into a bottle then slowly to take him back in the syringe;
11. To take a needle from a bottle and to accurately put on it a protective cap;
12. To open packaging with the smaller needle marked "27G 1/2" without getting a needle to put packaging aside;
13. To remove from the syringe a big needle together with a protective cap, to put aside afterwards to throw out;
14. To take a smaller needle from the opened packaging (holding the syringe in one hand) and, without removing a protective plastic cap from a needle, to connect it to the syringe as earlier connected a big needle;
15. The procedure of self-administration of drug should be carried out in situation reclining, sitting or standing;
16. Injections should be entered only into one of two areas of a penis which are called cavernous bodies, avoiding hit of a needle in visible veins; the subsequent injections need to be carried out alternately to one and to other side of a penis, choosing every time a new point for introduction of a needle on the relevant party;
17. Big and index fingers to take a penis for a head and to delay it, strong holding fingers that during the procedure it did not slip out; men to whom circumcision (trimming) was not carried out should take away a prepuce to define the exact venue of an injection;
18. To carefully process leather in the place of a prick the second napkin from a set impregnated with alcohol then to put it aside;
19. To take the syringe big and index fingers (without placing a thumb on the piston) and confident movement to enter a needle into the place for an injection specified by the doctor, at an angle 90 °;
20. Big or index finger to press the piston and slow confident movement to enter all contents of the syringe;
21. Holding a penis from two parties to take from it a needle; to press the napkin impregnated with alcohol to the place of an injection and to take about 3 min.; at emergence of blood the napkin needs to be pressed until bleeding does not stop;
22. Having used contents of a plastic container it it is necessary to throw out, following the corresponding safety rules: to place the used needles, a bottle and the syringe back in a plastic container from which previously to take the plastic locking device of red color and to put aside; to densely close a container before click, to remove the made an incision central part of the label (with the drawn red lock), baring a groove; to completely push the red locking device in a groove to lock a container (when it rises on the place, the container will be reliably locked, therefore, it can be thrown out). The container containing a bottle, needles and the used syringe, cannot be included in process of recirculation of waste.

Side effects

Local reactions:

• More than 1%: burning and a phallodynia, the prolonged erection lasting 4-6 h (4%), penis fibrosis (including an angulation, Peyroni's disease, formation of fibrous small knots (3-4%)), a hematoma (3%) and an ecchymoma (2%) in the place of an injection (as a rule, these side effects are connected with the injection equipment, but not with action of an alprostadil);
• Less than 1%: a priapism lasting erection more than 6 h (0,4%) (spontaneous relaxation of a penis was in most cases observed), hemorrhages, a balanitis, an itch, an inflammation and hypostasis in the place of an injection, a caumesthesia in a penis, urethrorrhagias, a fungal infection, numbness, irritation, a skin hyperesthesia, an erythema, a phymosis, "venous dumping" from cavernous bodies, disturbance of an ejaculation, a painful erection.

System reactions:

• More than 1%: dizziness, headache, increase in the arterial pressure (AP), dorsodynia, grippopodobny syndrome, upper respiratory tract infections, sinusitis, cough, nose congestion, prostatitis, pain syndrome;
• Less than 1%: pain in the field of a basin; testicles – a thickening, hypostasis, pain, a caumesthesia; a scrotum – reddening, pain, hypostasis; an urination – disturbance, increase, imperative desires; to a spermatotsela, a hamaturia, tachycardia, decrease in the ABP, a vazodilatation, peripheral vascular disorders, supraventricular premature ventricular contraction, vazovagalny reactions, a hypesthesia, muscular weakness, a hyperhidrosis, rash, a skin itch, nausea, dryness in a mouth, spasms of gastrocnemius muscles, increase in level of creatinine in blood serum, expansion of pupils.

Increase of pulse and decrease in the ABP were registered when using Kaverdzhekt's in doses more than 20 mkg and 30 mkg, most likely they were dozozavisimy, but were not clinically significant; therapy because of symptomatic hypotonia was interrupted only by 3 patients.

The priapism and/or long erection, irreversible deterioration in erectile function, phallodynia can be symptoms of overdose of an alprostadil. At continuation of an erection less than 6 h monitoring as the termination of an erection is frequent is necessary, reduction of the sizes of generative organs owing to outflow of blood (detumescence) happens spontaneously. If the effect lasts more than 6 h – it is necessary to make an intrakavernozny injection of α-adrenomimetik (ephedrine, Phenylephrinum, Epinephrinum, Etilefrinum), to execute aspiration of blood from cavernous bodies or to carry out surgical intervention. The patient is recommended to be kept under medical control before disappearance of the system phenomena and/or before full detumescence.

Special instructions

It is necessary to carry out diagnosis of the erection causes of infringement which are giving in to treatment prior to therapy alprostadily.

Specially prepared health workers have to do the first injections of Kaverdzhekt in an office of the doctor; the patient can do self-injections only after detailed instructing and development of the equipment of self-injections, and also assessment by the doctor of skills and abilities of the patient to holding this procedure; intra cavernous introduction should be carried out with observance of rules of an asepsis.

Constant observation of a condition of the patient who is carrying out independent injections is especially necessary in an initiation of treatment when dose adjustment can be required; further 1 time in 3 months for the purpose of assessment of safety and efficiency of therapy and dose adjustment is recommended to visit the attending physician (if it is necessary).

The bottle with ready divorced drug is applied once, and after use is thrown out; the patient should be instructed about rules of destruction of a bottle, needle and syringe.

As a result of intra cavernous administration of vasoactive drugs, including Kaverdzhekta, can develop a priapism – an erection, lasting more than 6 watch; for decrease in risk of its development it is necessary to enter the smallest effective dose, and lasting more than 4 hours it is necessary to report about all cases of an erection to the doctor immediately; therapy of a priapism is carried out according to the developed medical practice.

Intra cavernous introduction of an alprostadil can become the reason of development of fibrosis, including an angulation of a penis, Peyroni's disease and formation of fibrous small knots; frequency of developing of fibrosis can grow with increase in duration of use of drug; for the purpose of identification of symptoms of diseases regular inspection of patients, including attentive survey of a penis is necessary. At development of an angulation of a penis, Peyroni's disease or cavernous fibrosis therapy alprostadily should be stopped.

As intra cavernous introduction can be followed by small bleeding, patients have to be informed on ways of protection against the infections transmitted through blood and sexually such as HIV (human immunodeficiency virus). Tendency to bleedings from an intra cavernous injection at the patients receiving treatment by anticoagulants like heparin or warfarin is increased.

Continuous monitoring is necessary: to the patients receiving MAO inhibitors, and at a prolonged erection – to patients after a course of α-adrenomimetik (the probability of development of hypertensive crisis is high); at coronary heart disease, chronic heart failure or pulmonary diseases as the sexual intercourses or sexual stimulation can lead to an exacerbation of a disease.

Strict observance of compliance of the used dosage form of Kaverdzhekt to specific indications is important for its use.

Medicinal interaction

Каверджект it is impossible to mix or to enter at the same time with other medicines, and also to apply together with other drugs to therapy of erectile dysfunction.

Pharmacokinetic interaction with other substances / drugs is not studied. Combined use of an alprostadil with diuretics, hypotensive, anti-diabetic (including insulin) drugs or non-steroidal anti-inflammatory drugs (NPVS) has no effect on efficiency or safety of injections of Kaverdzhekt.

Efficiency and safety of combined use of Kaverdzhekt with other vasoactive drugs were not investigated.

Thanks to availability of benzyl alcohol in solvent extent of linkng of solution with bottle walls decreases. Therefore when using water for injections with the content of benzyl alcohol solution turns out steadier, fuller administration of drug is provided.

Terms and storage conditions

To store in the dry place unavailable to children, at a temperature not above 25 °C. Not to freeze.

Period of validity:

• Lyophilisate for preparation of solution for intra cavernous introduction – 2 years;
• Solvent – 3 years.

Ready solution needs to be stored in an original bottle in the place, unavailable to children, at a temperature up to 25 °C no more than 24 watch. Not to cool and not to freeze.