Coverject - Instructions For Use, Reviews, Price, Analogues

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Coverject

Coverject: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacodynamics and pharmacokinetics
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Drug interactions
10. 10. Analogs
11. 11. Terms and conditions of storage
12. 12. Terms of dispensing from pharmacies
13. 13. Reviews
14. 14. Price in pharmacies

Latin name: Caverject

ATX code: G04BE01

Active ingredient: Alprostadil (Alprostadil)

Manufacturer: Pfizer Menufecuring Belgium N. V. (Belgium / USA)

Description and photo update: 2019-06-08

Prices in pharmacies: from 1492 rubles.

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Caverject is a drug of a wide spectrum of pharmacological action, used for the treatment of erectile dysfunction.

Release form and composition

Dosage form - lyophilisate for preparing a solution for intracavernous administration: lyophilized porous mass or powder from almost white to white; solvent - colorless transparent (in vials, 1 bottle in a plastic box, complete with solvent (in a disposable syringe of 1 ml), 2 needles for injection and 2 napkins).

The composition of 1 bottle includes:

• Active ingredient: alprostadil - 10 or 20 mcg;
• Auxiliary components: lactose, sodium citrate.

Solvent: benzyl alcohol - 9000 mcg, water for injection - up to 1 ml.

Pharmacodynamics and pharmacokinetics

Alprostadil - the active component of Caverject - is an analogue of the natural form of prostaglandin E1 (PGE ₁) found in nature. It has a wide spectrum of pharmacological action: for example, its use leads to inhibition of platelet aggregation and vasodilation.

With intracavernous administration, Caverject inhibits α1-adrenergic receptors in tissues, improves microcirculation, increases blood flow and promotes relaxation of the muscles of the corpora cavernosa. Alprostadil stimulates erection by dilating the cavernous arteries and relaxing the trabecular smooth muscles of the corpora cavernosa. The consequence of this is the expansion of the lacunar spaces and the creation of obstacles to free blood flow by pressing the venules to the protein membrane (occlusion of the veins of the penis).

Caverject begins to act in 5-10 minutes after injection, the duration of action is 1-3 hours.

In the treatment of erectile dysfunction, alprostadil is injected intracavernously into the cavernous bodies of the penis. Its absolute bioavailability has not been determined. This compound binds to plasma proteins: with albumin - by 81% and with fraction IV-4 of α-globulin - by 55%. Clinically significant binding to leukocytes or erythrocytes is not observed.

Alprostadil forms several metabolites, which are also processed before being evacuated from the body. Approximately 80% of this circulating compound is metabolized on the first pass through the lungs, mainly through beta and omega oxidation.

The primary metabolites of alprostadil include 15-keto-PGE ₁, 13,14-dihydro-15-oxo-PGE ₁, which have practically no biological activity, and 13,14-dihydro-PGE ₁, which inhibits platelet aggregation and lowers blood pressure.

Alprostadil metabolites are excreted mainly through the kidneys: almost 90% of the administered dose is excreted in the urine within one day. The rest is excreted in the feces.

The active substance of Caverject does not have mutagenic activity. When administered in a daily dose of not more than 2 mg / kg, no changes in spermatogenesis or effects on reproductive function have been recorded.

Indications for use

• Treatment of erectile dysfunction of psychogenic, neurogenic, vascular or mixed etiology;
• Diagnostics of erectile dysfunction in combination with other diagnostic tests.

Contraindications

Absolute:

• Multiple myeloma, sickle cell anemia, leukemia and other diseases that predispose to priapism;
• Anatomical defects of the penis (cavernous fibrosis, penile angulation, Peyronie's disease);
• Penile implant;
• Diagnosed hypersensitivity to Caverject's components.

Also, you should not use the drug in men who are not recommended or contraindicated in sexual activity.

It is necessary to use Caverject with caution in persons under 18 years of age, since the efficacy and safety of its use in this age group has not been studied.

Instructions for the use of Caverjekt: method and dosage

The solution prepared from the lyophilisate is intended for direct intracavernous administration into the dorsolateral part of the proximal third of the penis using injection needles 27-30 G in size and 13 mm in length.

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

Depending on the causes of erectile dysfunction, it is necessary to adhere to the following schemes (taking into account the erectile reaction) until a dose that causes an erection is sufficient for a full sexual intercourse duration (but not more than 1 hour). Dose calculation in case of erectile dysfunction of neurogenic etiology (spinal cord injury):

• I (initial) injection - 1.25 μg;
• II injection - 2.5 mcg;
• III injection - 5 mcg.

The value of the step-by-step increase in the dose of the drug until the optimal one is 5 μg

Dose calculation in case of erectile dysfunction of psychogenic, vascular and mixed etiology:

• I (initial) injection - 2.5 mcg;
• II injection - in case of partial response to the first injection - 5 μg; in the absence of a response - 7.5 μg;
• III injection - not done.

The value of a step-by-step increase in the dose of the drug until the optimal one is 5-10 mcg.

If there is no reaction to the next injection, the next, higher dose must be administered after 1 hour. If there is a response, the interval between injections should be at least a day.

The patient should be under the supervision of a doctor until there is a complete cessation of erection - detumescence.

With maintenance therapy, the dose chosen for self-injection should provide an erection sufficient for intercourse of no more than 1 hour. If this time is exceeded, the dose must be reduced.

Self-therapy at home begins with the dose determined in the doctor's office, if it needs to be changed, then you should consult with your doctor and, in accordance with his instructions, choose the dose (the least effective). It is recommended to administer injections no more than 3 times a week and no more than 1 time a day. The standard time required for a stable erection to appear is 5-20 minutes from the start of drug administration.

Six months after the start of treatment, the required average dose of alprostadil is 20.7 mcg. For most patients, the maintenance dose is 5-20 mcg; the maximum allowable is 60 mcg.

When using Caverject as an adjunct to diagnose erectile dysfunction, a single dose should be used to induce a normal erection. In pharmacological tests, the drug is administered as an additional one (for Doppler or duplex ultrasound testing, in the xenon-133 washout test, penile arteriography or radioisotope phallography) to visualize and assess the state of the penile vessels.

To prepare a solution from the lyophilisate, you must use the ready-made composition supplied in the syringe or water for injection with benzyl alcohol 0.9% as a diluent for dilution. The volume of the resulting solution after dilution in 1 ml of solvent is 1.13 ml, with the content of alprostadil - 10.5 μg or 20.5 μg in 1 ml. As a result of the injection, 10 μg or 20 μg of alprostadil, respectively, gets into the body, since 0.5 μg is lost due to adsorption on the walls of the vial and syringe. After the drug is diluted, no substances should be added to the vial.

Before administration, the solution should be visually inspected for discoloration or particles.

To carry out the Caverject self-injection procedure, the patient should:

1. Wash hands thoroughly with soap and water;
2. Remove the protective plastic cap from the bottle;
3. Wipe the rubber stopper of the bottle with one of the supplied alcohol-soaked napkins (discard the used napkin);
4. Unpack the large needle marked "22 G11 / 2"; without removing the plastic protective cap from the needle, connect it to the syringe by putting the base on the neck of the syringe and pressing firmly;
5. Remove the protective cap from the needle;
6. Remove excess water from the syringe: bring the plunger to the "1 ml" mark, holding the syringe vertically, with the needle tip up;
7. Pierce the rubber stopper of the bottle with a needle in the central part, push the piston down, introduce water into the bottle;
8. Holding the bottle and syringe as a whole, gently dissolve the powder with light circular movements; do not use the solution if it is cloudy, has acquired a color, or contains any inclusions;
9. Without removing the syringe, turn the bottle upside down, make sure that the tip of the needle is below the level of the solution, slowly pull the plunger towards you until the level of the solution reaches the required mark on the syringe;
10. Tap the syringe lightly to remove air bubbles, or re-enter the solution into the vial, and then slowly draw it back into the syringe;
11. Remove the needle from the bottle and carefully put the protective cap on it;
12. Open the package with a smaller needle marked "27G 1/2", without taking out the needle, put the package aside;
13. Remove the large needle with the protective cap from the syringe, put it aside for later discard;
14. Take the smaller needle from the opened package (holding the syringe in one hand) and, without removing the protective plastic cap from the needle, connect it to the syringe, as the large needle was previously connected;
15. The self-administration procedure of the drug should be carried out in a reclining position, sitting or standing;
16. Injections should be given only in one of the two areas of the penis, called the corpus cavernosum, avoiding the needles entering the visible veins; subsequent injections must be carried out alternately in one and the other side of the penis, choosing each time a new point for the introduction of the needle on the corresponding side;
17. With your thumb and forefinger, take the penis by the head and pull it back, holding it firmly with your fingers so that it does not slip out during the procedure; For men who have not undergone excision of the foreskin (circumcision), the foreskin should be removed to determine the exact injection site;
18. Thoroughly treat the skin at the injection site with a second napkin from the kit soaked in alcohol, then put it aside;
19. Take the syringe with your thumb and forefinger (without placing your thumb on the plunger) and with a confident movement insert the needle into the injection site indicated by the doctor at an angle of 90 °;
20. Press the plunger with your thumb or forefinger and inject the entire contents of the syringe with a slow, confident movement;
21. Holding the penis on both sides, remove the needle from it; press a napkin soaked in alcohol to the injection site and hold for about 3 minutes; when blood appears, the napkin must be pressed until the bleeding stops;
22. After using the contents of the plastic container, it must be thrown away, observing the appropriate safety rules: put the used needles, the vial and the syringe back into the plastic container, from which first remove the red plastic locking device and set aside; close the container tightly until it clicks, remove the notched central part of the label (with a painted red lock), exposing the groove; push the red locking device fully into the slot to lock the container (when it is in place, the container is securely locked and can therefore be discarded). The container containing the vial, needles and used syringe cannot be included in the recycling process.

Side effects

Local reactions:

• More than 1%: burning sensation and pain in the penis, prolonged erection lasting 4-6 hours (4%), fibrosis of the penis (including angulation, Peyronie's disease, formation of fibrous nodules (3-4%)), hematoma (3%) and ecchymosis (2%) at the injection site (as a rule, these side effects are associated with the injection technique, and not with the action of alprostadil);
• Less than 1%: priapism with an erection lasting more than 6 hours (0.4%) (in most cases, spontaneous relaxation of the penis was observed), hemorrhages, balanitis, itching, inflammation and swelling at the injection site, a feeling of warmth in the penis, bleeding from the urethra canal, fungal infection, numbness, irritation, skin hyperesthesia, erythema, phimosis, "venous discharge" from the corpora cavernosa, ejaculation disorder, painful erection.

Systemic reactions:

• More than 1%: dizziness, headache, increased blood pressure (BP), back pain, flu-like syndrome, upper respiratory tract infections, sinusitis, cough, nasal congestion, prostatitis, pain syndrome;
• Less than 1%: pelvic pain; testicles - thickening, swelling, pain, warmth; scrotum - redness, pain, swelling; urination - violation, frequency, urgency; spermatocele, hematuria, tachycardia, decreased blood pressure, vasodilation, peripheral vascular disorders, supraventricular extrasystole, vasovagal reactions, hypoesthesia, muscle weakness, hyperhidrosis, rash, pruritus, nausea, dry mouth, cramps in the calf muscles dilated pupils.

An increase in heart rate and a decrease in blood pressure were recorded when using Caverject at doses of more than 20 μg and 30 μg, most likely they were dose-dependent, but were not clinically significant; therapy due to symptomatic hypotension was interrupted only by 3 patients.

Symptoms of an overdose of alprostadil may be priapism and / or prolonged erection, irreversible deterioration of erectile function, pain in the penis. If an erection continues for less than 6 hours, monitoring is necessary, since often the termination of an erection, a decrease in the size of the genitals due to outflow of blood (detumescence) occurs spontaneously. If the effect lasts more than 6 hours, an intracavernous injection of α-adrenergic agonists (ephedrine, phenylephrine, epinephrine, ethylephrine) should be done, aspiration of blood from the corpora cavernosa or surgery should be performed. The patient is recommended to be kept under medical supervision until the disappearance of systemic phenomena and / or until the onset of complete detumescence.

Overdose

Overdose symptoms are: irreversible deterioration of erectile function, priapism and / or prolonged erection, pain in the penis.

If the state of erection persists for less than 6 hours, it is recommended to monitor the condition with a specialist, since spontaneous detumescence is often observed (a decrease in the size of the genitals due to outflow of blood, the disappearance of an erection). If an erection lasts more than 6 hours, an intracavernous injection of α-adrenergic agonists (for example, ethylephrine, phenylephrine, epinephrine, ephedrine) is performed or blood is aspirated from the corpora cavernosa. In severe cases, you should resort to surgery. The patient should remain under medical supervision until the disappearance of systemic phenomena and / or until the onset of complete detumescence of the penis.

special instructions

A diagnosis of treatable causes of erectile dysfunction should be carried out before starting therapy with alprostadil.

The first injections of Caverject should be done in the doctor's office by specially trained medical personnel; the patient can do self-injections only after detailed instructions and mastery of the self-injection technique, as well as the doctor's assessment of the patient's skills and abilities to carry out this procedure; intracavernous administration should be carried out in compliance with the rules of asepsis.

Constant monitoring of the condition of the patient conducting self-injections is especially necessary at the beginning of treatment, when dose adjustment may be required; then it is recommended to visit the attending physician once every 3 months in order to assess the safety and effectiveness of therapy and adjust the dose (if necessary).

The bottle with the finished diluted drug is used once, and after use it is thrown away; the patient must be instructed on the rules for the destruction of the vial, needle and syringe.

As a result of intracavernous administration of vasoactive drugs, incl. Caverject, priapism may develop - an erection lasting more than 6 hours; to reduce the risk of its development, it is necessary to enter the lowest effective dose, and all cases of erection lasting more than 4 hours should be immediately reported to the doctor; priapism therapy is carried out in accordance with established medical practice.

Intracavernous administration of alprostadil can cause the development of fibrosis, including angulation of the penis, Peyronie's disease and the formation of fibrous nodules; the incidence of fibrosis may increase with the duration of drug use; in order to detect signs of disease, regular examination of patients is necessary, including a careful examination of the penis. With the development of angulation of the penis, Peyronie's disease or cavernous fibrosis, therapy with alprostadil should be discontinued.

Since intracavernous administration may cause minor bleeding, patients should be educated about how to protect against blood and sexually transmitted infections such as HIV (Human Immunodeficiency Virus). Increased tendency to bleeding from intracavernous injection in patients receiving treatment with anticoagulants such as heparin or warfarin.

Constant monitoring is necessary: for patients receiving MAO inhibitors, and with prolonged erection - for patients after a course of α-adrenergic agonists (there is a high probability of developing a hypertensive crisis); with ischemic heart disease, chronic heart failure, or pulmonary disease, since sexual intercourse or sexual stimulation can exacerbate the disease.

It is important to strictly adhere to the compliance of the Caverject dosage form used with the specific indications for its use.

Drug interactions

According to the instructions, Caverject should not be mixed or simultaneously administered with other drugs, as well as used in conjunction with other drugs for the treatment of erectile dysfunction.

Pharmacokinetic interaction with other substances / drugs has not been studied. The combined use of alprostadil with diuretics, antihypertensive, antidiabetic (including insulin) drugs or non-steroidal anti-inflammatory drugs (NSAIDs) does not have any effect on the effectiveness or safety of Caverject's injections.

The efficacy and safety of the combined use of Caverject with other vasoactive drugs have not been studied.

Due to the presence of benzyl alcohol in the solvent, the degree of binding of the solution to the walls of the vial is reduced. Therefore, when using water for injection containing benzyl alcohol, the solution is more stable, and a more complete administration of the drug is provided.

Analogs

Kaverjekt's analogs are: Alprostan, Prostin BP, Vazaprostan, VAP 20, Muse, Edeks.

Terms and conditions of storage

Store in a dry place out of the reach of children, at a temperature not exceeding 25 ° C. Do not freeze.

Shelf life:

• Lyophilisate for preparing a solution for intracavernous administration - 2 years;
• Solvent - 3 years.

The prepared solution must be stored in the original bottle out of the reach of children at temperatures up to 25 ° C for no more than 24 hours. Do not refrigerate or freeze.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Coverject

There are various reviews about the Coverject. Some patients talk about the effectiveness of Caverject in the treatment of impotence due to psychological causes. Other patients claim that the administration of the drug was useless, since the duration of the erection was insignificant and it was not possible to perform intercourse. Probably, not all patients received the correct dose, or they did not take it at all.

Price for Coverject in pharmacies

The price for a bottle of Caverject with a concentration of 10 mcg alprostadil is 800-900 rubles on average.

Coverject: prices in online pharmacies

Drug name Price Pharmacy

Caverject 10 μg lyophilisate for preparation of solution for intracavernous administration 1 pc. 1492 RUB Buy

Anna Kozlova Medical journalist About the author

Education: Rostov State Medical University, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!