Caverject

Caverject is a representative of a group of drugs that have the ability to affect the genitourinary system and hormones of the reproductive system.

The drug is widely used in urology to restore erectile function. The pharmacological group that includes Caverject consists of drugs that are analogs of prostaglandin E1.

The drug starts to act within 5-10 minutes after administration. The duration of the drug's activity is from 1 to 3 hours, depending on the severity of the pathological process, the presence of concomitant pathology and the patient's age.

The dosage should be selected by the doctor for each patient individually. The first injections of the drug should be carried out in a hospital setting, after which independent injections by the patient are possible, provided that he is well prepared and skilled.

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Indications Caverject

The drug is used in urology for therapeutic and diagnostic purposes. Thus, indications for the use of Caverject include the treatment of erectile dysfunction, the cause of which may be psychogenic and neurogenic disorders. These include pathology of the nervous system, psychoemotional lability, constant stressful situations, worries, heavy workload at work and insufficient time allocated for sleep.

In addition, vascular pathology can be the cause of erectile dysfunction. As a result of spasm of blood vessels, there is an incomplete delivery of oxygen and nutrients to the genitals, which has a direct impact on erection.

It is worth noting that it is not always one factor that affects sexual function, but also a combination of several, which leads to erectile dysfunction of mixed origin.

Indications for the use of Caverject also suggest the use of the drug for the diagnosis of erectile dysfunction as an auxiliary component.

For a full treatment of erectile function, it is necessary not only to correctly diagnose, but also to identify the cause of the pathology. In addition to direct treatment of erectile function, the causative factor should be eliminated, otherwise the therapeutic effect may not be long-lasting.

Release form

The drug is used for intracavernous administration, therefore its release form is represented by a lyophilisate for the preparation of an injection solution.

Important physical and chemical properties of the preparation are lyophilized powder with a white or beige tint. In addition, the kit includes a special solvent, which is a liquid without color, suspensions, with the smell of benzyl alcohol.

The main active component of the drug is alprostadil. It is contained in a quantity of 10 mcg per bottle. In addition, it is necessary to indicate auxiliary components in the form of lactose monohydrate and sodium citrate. The release form of the solvent is represented by water for injection with benzyl alcohol with a concentration of 9 mg / ml.

The drug packaging contains a syringe filled with solvent, 1 ml in volume, an injection needle in a plastic case, and a bottle with powder (lyophilisate).

This form of release allows the preparation of the drug immediately before administration. Any remaining medication after a single use is prohibited, since the drug cannot be stored for a long time in a diluted form.

Pharmacodynamics

The main active ingredient of the drug is contained in animal tissues and fluids. Alprostadil has various therapeutic effects, among which the most pronounced are vasodilatory action, inhibition of platelet aggregation and protection of blood vessels.

The pharmacodynamics of Caverject is due to the action of alprostadil, an analogue of prostaglandin E1. Thanks to it, after intracavernous administration, blocking of alpha1-adrenoreceptors in tissues, relaxation of the muscle fibers of the cavernous bodies, activation of local blood circulation, including microcirculation, is observed.

Due to the removal of spasm and dilation of the arteries of the cavernous bodies and smooth trabecular muscles, a powerful blood flow and expansion of the lacunae of the cavernous bodies is ensured.

Pharmacodynamics Caverject provides increased blood flow, while the corporal veno-occlusive mechanism is activated, resulting in decreased blood flow through the veins located under the protein coat. Thus, the onset of an erection is stimulated.

From the moment of administration of the drug to the development of an erection, it may take from 5 to 10 minutes. The therapeutic effect of the drug is noted for 1-3 hours. The duration of the erection depends on the patient's age, the severity of the pathology that provoked erectile dysfunction, as well as the presence of concomitant diseases.

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Pharmacokinetics

The drug is intended for intracavernous administration and is characterized by rapid metabolism. After intravenous administration, about 80% of alprostadil circulating in the bloodstream is metabolized during passage through the respiratory system (lungs) via omega- and beta-oxidation.

As a result of enzymatic oxidation, several metabolites are obtained, including keto groups. Keto metabolites have lower therapeutic activity compared to the main active substance of the drug.

Pharmacokinetics Caverject ensures the excretion of 90% of alprostadil metabolites by the urinary organs within 24 hours. The remaining 10% are excreted by the intestines. The entire administered dose is metabolized, so the drug is not excreted unchanged. In addition, there is no accumulation of alprostadil in tissues.

After intracavernous administration of 20 mcg alprostadol, no significant increase in the concentration of the active ingredient in the blood was detected after 30 and 60 minutes. However, the amount of metabolites of the drug increased and reached a maximum half an hour after the administration of Caverject. An hour after using the drug, the level of metabolites returned to previous values.

Alprostadil circulates in the bloodstream bound to proteins, in particular albumins and to a lesser extent globulins. The drug's association with erythrocytes and leukocytes has not been proven. After intracavernous administration, the drug is rapidly metabolized and exerts its therapeutic effect.

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Dosing and administration

The drug is intended for intracavernous administration. For this purpose, it is necessary to use a 27-30 gauge needle. The method of administration and dosage must be selected by the doctor individually.

Intracavernous injection should be performed under sterile conditions. The injection site is on the dorsolateral surface of the upper third of the penis (closer to the testicles). To avoid local adverse reactions, the injection site should be changed each time, treated with an alcohol swab, and the needle should not be inserted into visible veins.

To prepare the medicine, remove the plastic cap from the bottle and wipe the rubber cap with an alcohol swab before administration. Then inject 1 ml of the solution into the bottle with a syringe and needle to dilute the powder. To speed up the dissolution process, shake the bottle several times.

Now you should draw the drug into the syringe (a little more than the intended dose), change the needle and remove the air from the syringe (this will cause a little medicine to spill out).

After treating the injection site, you need to make an injection. The remaining volume of the drug should not be used anymore, since the medicine cannot be stored in a dissolved state.

For diagnostic purposes, Caverject is used in a dose of 20 mcg (for men without neurological pathology) and no more than 10 mcg (with neurological pathology), after which it should be spread over the penis with massage movements. The therapeutic effect is assessed by determining the time of the onset of erection and its duration. If the erection lasts more than an hour, it is necessary to take measures to accelerate the elimination of the drug. To avoid the development of priapism, by the time the patient leaves the clinic, he should be relieved of his erection and the penis should be completely relaxed.

The method of administration and dosage are determined based on the severity of the pathology, the patient's age and the presence of concomitant diseases. The initial dose for men with spinal cord damage is 1.25 mcg, the subsequent doses are 2 times larger. The fourth dose should be 10 mcg and then increased by 5 mcg until the effective dose for the desired effect is obtained.

In case of vascular, mixed or psychogenic causes of erectile dysfunction, it is recommended to start with 2.5 mcg, then increase by 5 mcg until the required therapeutic effect is achieved.

Once the result is achieved, the dose should not be used more than once a day and more than 3 times a week. At the beginning of the treatment, intracavernous injections with the drug should be performed by a health worker, after which, having mastered the principles of administration, the patient can independently perform the manipulation at home.

The optimal dose is the amount of the drug used that provides an erection for 1 hour. It is not recommended to exceed the maximum dosage (60 mcg) to prolong the erection for more than an hour. In most cases, 5-20 mcg of alprostadol is sufficient.

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Use Caverject during pregnancy

During pregnancy, special control is required over the medications that the woman takes. In the first three months, the process of organ formation occurs, interference in which can subsequently manifest itself in their incomplete development and insufficient functionality of the systems.

However, this does not mean that the remaining 6 months of pregnancy do not require attention, since during this period of time the growth and development of the fetus occurs, which is also important for its vital functions.

The last trimester of pregnancy is important because the woman's mammary glands are most intensively preparing for feeding the baby. When taking medications in the last stages, the likelihood of their metabolites penetrating into breast milk increases, which threatens the health and life of the baby.

The use of Caverject during pregnancy is absolutely contraindicated due to the fact that the drug is not intended for use by women. In addition, it is prohibited for use during breastfeeding, as well as in childhood.

Contraindications

Before using any medication, you must first familiarize yourself with its contraindications in order to avoid the development of side effects and deterioration of the condition.

Contraindications to the use of Caverject include individual intolerance to alprostadol or excipients that are part of the drug.

In addition, the drug is prohibited for use in diseases that contribute to the development of priapism. These include sickle cell anemia, red blood cell abnormality, myeloma disease or leukemia. It is also necessary to take into account anatomical anomalies of the penis structure, such as Peyronie's disease, angulation and cavernous fibrosis, stricture of the urethra and hypospadias.

Contraindications to the use of Caverject imply a ban on the use of the drug by men with penile implants. In addition, men who are contraindicated in sexual activity for various reasons are also not recommended to use Caverject. The drug is prohibited at the age of under 18 and after 75 years, since there is no data on the therapeutic effects of the drug in this group of patients.

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Side effects Caverject

Clinical studies have identified side effects of Caverject that have been observed with its single or long-term use.

In some cases, there is an infection of the upper respiratory tract, including fungal pathogens. From the nervous system, there is dizziness, headache, loss of consciousness and changes in the sensitivity of the skin.

In addition, mydriasis, hematoma at the injection site, ecchymosis and flu-like syndrome are sometimes observed. The cardiovascular system may react to the introduction of Caverject with rhythm and conduction disturbances in the form of supraventricular extrasystoles, venous damage, decreased pressure and excessive dilation of blood vessels.

Side effects of Caverject also include nausea, dry mouth, rash, hyperhidrosis, flushing, nasal congestion, and cough.

The musculoskeletal system may respond to the use of the drug with muscle spasms, pain in the buttocks, lower limbs and lower back.

From the urinary and reproductive systems, it is worth highlighting dysuric symptoms, the appearance of blood in the urine, frequent urge to urinate, urinary incontinence, as well as swelling of the testicles, pain in the penis, increased erectile function, damage to the penis and dysfunction of the prostate gland.

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Overdose

After intracavernous administration of the drug, a prolonged erection or priapism may develop. A man should notify the doctor if he has an erection lasting more than 4 hours. If priapism (a prolonged erection) persists for more than 6 hours, then therapeutic measures must be taken. This condition is observed with an overdose of Caverject.

Initial therapy is aspiration of the penis. To do this, a butterfly needle must be inserted into the cavernous spaces and 20-50 ml of blood must be aspirated. If necessary, the manipulation must be repeated on the other side of the penis and continued until 100 ml has been collected.

If overdose occurs as a result of using an excessively large dose and aspiration is ineffective, then intracavernous administration of an alpha-adrenergic drug is recommended. Monitoring of the patient's blood pressure and pulse is mandatory when using vasoconstrictors.

Overdose has a particularly negative impact on health in cases of ischemic damage to the vessels supplying the myocardium, cerebral ischemia, hypertension, and also when using monoamine oxidase inhibitors.

In case of prolonged erection, it is necessary to prepare a 200 mcg/ml concentration of phenylephrine solution and administer 0.5-1 ml every 5-10 minutes. If this medicine is not available, it is permissible to use adrenaline with a concentration of 20 mcg/ml.

After the introduction of these drugs and insufficient effect, blood aspiration from the penis should be continued. The maximum dose of phenylephrine is 1 mg, and for adrenaline - 100 mcg (5 ml). In the absence of effect from drugs and aspiration, surgical treatment should be used - shunting.

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Interactions with other drugs

Studies on the simultaneous use of Caverject with other drugs for the treatment of erectile dysfunction, such as sildenafil, have not been conducted to avoid the development of a prolonged erection.

In addition, you should not use Caverject with drugs that can prolong erection, such as papaverine. The interaction of Caverject with other drugs that affect erection is contraindicated, since too long an erection can threaten overall health.

The use of Caverject with sympathomimetic drugs may reduce the activity of alprostadol, which may not provide the desired result in terms of erectile function.

The interaction of Caverject with other drugs with antihypertensive action is manifested by an increase in the effect of the latter, which threatens excessive pressure reduction and collapse. Alprostadol activates the pharmacodynamics of vasodilators, anticoagulants and antiplatelet agents.

The combined use of Caverject and drugs that affect the blood clotting system may result in bleeding.

At the same time, intracavernous administration of alprostadol with the use of diuretics, insulin, NSAIDs and oral hypoglycemic drugs does not cause side effects.

Storage conditions

In order to preserve the medicinal properties of the drug for a certain period of time, it is necessary to take into account the recommendations for its storage.

Thus, it is necessary to maintain an optimal level of temperature, humidity and lighting to avoid premature loss of the medicinal properties of the drug.

Storage conditions for Caverject include control over the temperature of the room where the drug is located. It should not exceed 25 degrees. In addition, it should be taken into account that direct sunlight has a detrimental effect on the structure of the drug, which can change its pharmacokinetics and pharmacodynamics.

A mandatory condition is that children should not have access to the medicine. Children may get hurt by the bottle or needle, and if the powder is taken orally, it may cause side effects and poisoning. To avoid this, Caverject should be stored in places inaccessible to children.

Special instructions

Caverject is an effective medicine for the treatment of erectile dysfunction, but requires special attention when using. Thus, using a large dosage, an erection can last up to 4-6 hours or even more, which threatens the general condition of a man. To avoid surgical treatment of an overdose of the drug, it is necessary to strictly follow the doctor's recommendations and not exceed the dosage in order to prolong an erection for more than an hour.

Shelf life

Provided that the rules for storing the drug are followed, the drug retains its therapeutic properties throughout its entire shelf life.

When manufacturing a medicine, the expiration date must be indicated, which includes the date of manufacture and last use. After the expiration date of Caverject, which is 2 years, it is prohibited to use and the drug should be disposed of.

If during the expiration date the medicine is exposed to sunlight, excessive humidity, or the bottle has lost its seal, then alprostadol may change its structure and, accordingly, the effects it has on the human body.