What are the main uses of alprostadil for erectile dysfunction. How does alprostadil work to treat ED. What are the most common side effects of using alprostadil. What important drug interactions should be considered with alprostadil.

Understanding Alprostadil and Its Role in Treating Erectile Dysfunction

Alprostadil is a medication primarily used to treat erectile dysfunction (ED) in men. It belongs to a class of drugs known as vasodilators, which work by relaxing blood vessels and increasing blood flow to specific areas of the body. In the case of alprostadil, it helps increase blood flow to the penis, enabling men to achieve and maintain an erection suitable for sexual activity.

The medication comes in different forms, including:

• Urethral suppositories
• Intracavernosal injections
• Topical creams

Each form has its own advantages and considerations, which should be discussed with a healthcare provider to determine the most suitable option for individual patients.

How Does Alprostadil Work to Combat Erectile Dysfunction?

Alprostadil’s mechanism of action is straightforward yet effective. When administered, it causes the following physiological changes:

1. Relaxation of smooth muscles in blood vessels
2. Dilation of arteries in the penis
3. Increased blood flow to erectile tissues
4. Compression of veins to prevent blood outflow

These combined effects result in an erection that typically occurs within 5 to 10 minutes of administration and can last for about 30 to 60 minutes. This duration makes alprostadil a viable option for men seeking a reliable, on-demand solution for erectile dysfunction.

Proper Administration and Dosage Guidelines for Alprostadil

The correct administration of alprostadil is crucial for its effectiveness and safety. For urethral suppositories, the most common form, the process involves:

1. Urinating before administration to lubricate the urethra
2. Removing the protective cover from the applicator
3. Inserting the suppository into the penis as directed
4. Gently massaging the penis to aid in medication absorption

Dosage varies based on individual factors and response to treatment. Generally, healthcare providers recommend starting with a lower dose and adjusting as needed. It’s important not to exceed two doses within a 24-hour period to minimize the risk of side effects.

Can alprostadil be used daily?

Alprostadil is typically not recommended for daily use. Most healthcare providers advise using it on an as-needed basis, with a maximum of two doses in a 24-hour period. This approach helps reduce the risk of side effects and maintains the medication’s effectiveness.

Common Side Effects and Safety Considerations of Alprostadil

While alprostadil is generally well-tolerated, it can cause certain side effects. The most common include:

• Pain or discomfort in the penis, testicles, or groin area
• Minor bleeding or spotting from the penis
• Dizziness
• Swelling, particularly in leg veins
• Rapid heartbeat

These side effects are usually mild and transient. However, if they persist or worsen, it’s important to consult a healthcare provider promptly. In rare cases, more serious side effects may occur, such as priapism (a prolonged, painful erection lasting more than 4 hours), which requires immediate medical attention.

Are there any long-term risks associated with alprostadil use?

Long-term studies on alprostadil have not shown significant risks with prolonged use when administered as directed. However, as with any medication, it’s important to have regular check-ups with a healthcare provider to monitor for any potential issues. Some men may experience changes in penile tissue over time, but this is generally rare when the medication is used correctly.

Drug Interactions: What to Watch Out for When Using Alprostadil

Alprostadil can interact with various medications, potentially affecting its efficacy or increasing the risk of side effects. According to the information provided, there are 38 known drug interactions with alprostadil, of which 36 are moderate and 2 are minor. Some of the most frequently checked interactions include:

• Erectile dysfunction medications (e.g., sildenafil, tadalafil, vardenafil)
• Blood thinners (e.g., apixaban, rivaroxaban)
• Antihypertensive medications (e.g., metoprolol)
• Pain relievers (e.g., acetaminophen, celecoxib)
• Hormone therapies (e.g., testosterone)

It’s crucial to inform your healthcare provider about all medications, supplements, and herbal products you’re taking to avoid potential interactions.

How do alprostadil interactions with other ED medications work?

Interactions between alprostadil and other erectile dysfunction medications like sildenafil (Viagra), tadalafil (Cialis), or vardenafil (Levitra) can lead to a dangerously prolonged erection or severe hypotension (low blood pressure). These medications work through similar mechanisms, and combining them can amplify their effects. For this reason, it’s generally advised not to use alprostadil in conjunction with other ED treatments unless specifically directed by a healthcare provider.

Alprostadil and Underlying Health Conditions: Important Considerations

Certain health conditions can affect the safety and efficacy of alprostadil treatment. The drug interaction checker mentions three disease interactions with alprostadil:

1. Respiratory function
2. Bleeding disorders
3. Hypotension (low blood pressure)

Patients with these conditions should be closely monitored when using alprostadil, and in some cases, alternative treatments may be recommended. Additionally, alprostadil may not be suitable for individuals with:

• Penile implants or anatomical deformities
• History of priapism
• Sickle cell anemia
• Leukemia
• Multiple myeloma

A thorough medical evaluation is essential before starting alprostadil treatment to ensure its safety and appropriateness for each individual patient.

Can alprostadil be used in patients with cardiovascular disease?

Alprostadil can be used in patients with cardiovascular disease, but caution is advised. The medication can cause a temporary drop in blood pressure, which may be problematic for individuals with pre-existing heart conditions. A thorough cardiovascular evaluation should be performed before prescribing alprostadil to these patients. In some cases, the benefits may outweigh the risks, but close monitoring is essential, and lower doses may be recommended.

Comparing Alprostadil to Other Erectile Dysfunction Treatments

While alprostadil is an effective treatment for erectile dysfunction, it’s not the only option available. Other common treatments include:

• Oral medications (e.g., sildenafil, tadalafil, vardenafil)
• Vacuum erection devices
• Penile implants
• Lifestyle modifications

Each treatment has its own set of advantages and drawbacks. For example, oral medications are often the first-line treatment due to their ease of use, but they may not be effective for all men. Alprostadil, while more invasive, can be effective for those who don’t respond to oral medications or can’t take them due to other health conditions.

How does the effectiveness of alprostadil compare to oral ED medications?

Alprostadil tends to have a higher success rate compared to oral medications, with some studies reporting effectiveness in up to 80% of patients. This is particularly true for men who don’t respond to oral treatments. However, the more invasive nature of alprostadil administration (urethral suppository or injection) may make it less preferable for some patients. The choice between alprostadil and oral medications often depends on individual factors, including the underlying cause of ED, other health conditions, and personal preferences.

Lifestyle Factors and Alprostadil: Maximizing Treatment Effectiveness

While alprostadil can be highly effective in treating erectile dysfunction, its benefits can be enhanced by adopting certain lifestyle changes. These modifications not only improve the medication’s effectiveness but also contribute to overall sexual and general health:

• Maintaining a healthy weight
• Regular exercise, particularly cardiovascular activities
• Quitting smoking
• Limiting alcohol consumption
• Managing stress through relaxation techniques or therapy
• Following a balanced diet rich in fruits, vegetables, and whole grains

These lifestyle factors can improve blood flow, boost testosterone levels, and enhance overall cardiovascular health, all of which contribute to better erectile function.

How does smoking affect the efficacy of alprostadil?

Smoking can significantly reduce the effectiveness of alprostadil and other erectile dysfunction treatments. Nicotine and other toxins in cigarettes damage blood vessels and impair blood flow throughout the body, including to the penis. This can make it more difficult to achieve and maintain an erection, even with medication. Quitting smoking can lead to noticeable improvements in erectile function and may enhance the effectiveness of alprostadil treatment.

The Future of Erectile Dysfunction Treatment: Emerging Therapies and Research

While alprostadil and other current treatments have proven effective for many men with erectile dysfunction, research continues to explore new therapies and improvements to existing ones. Some promising areas of research include:

1. Gene therapy to promote nerve regeneration and improve erectile function
2. Stem cell treatments to restore damaged erectile tissue
3. Novel drug delivery systems for more targeted and efficient medication administration
4. Combination therapies that leverage multiple mechanisms of action
5. Personalized medicine approaches based on genetic factors and individual health profiles

These emerging therapies aim to provide more tailored, effective, and potentially less invasive options for men with erectile dysfunction. As research progresses, it’s likely that new treatments will complement or potentially replace some current options, offering hope for improved outcomes and quality of life for men struggling with ED.

What role might regenerative medicine play in future ED treatments?

Regenerative medicine, particularly stem cell therapy and platelet-rich plasma (PRP) treatments, shows promise in the field of erectile dysfunction. These approaches aim to repair and regenerate damaged penile tissue, potentially offering a more long-term solution compared to current symptom-focused treatments. Early studies have shown encouraging results, with some patients experiencing improved erectile function and reduced reliance on medications. However, more research is needed to fully understand the long-term efficacy and safety of these treatments before they can become mainstream options.

As research in this field continues, it’s important for patients to stay informed about new developments and discuss emerging treatment options with their healthcare providers. The future of erectile dysfunction treatment looks promising, with the potential for more personalized, effective, and less invasive therapies on the horizon.

Alprostadil Interactions Checker – Drugs.com

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There are 38 drugs known to interact with
alprostadil, along with
3 disease interactions.

Of the total drug interactions,
36 are moderate, and 2 are minor.

Does alprostadil interact with my other drugs?

Enter other medications to view a detailed report.

• View all 38 medications that may interact with alprostadil
• View alprostadil disease interactions (3)

Most frequently checked interactions

View interaction reports for alprostadil and the medicines listed below.

• Major
• Moderate
• Minor
• Unknown

• Activated Charcoal (charcoal)
• Alcohol (contained in alcoholic beverages) (ethanol)
• AndroGel (testosterone)
• Aspirin Low Strength (aspirin)
• Benadryl (diphenhydramine)
• Celebrex (celecoxib)
• Cialis (tadalafil)
• Claritin (loratadine)
• CoQ10 (ubiquinone)
• Crestor (rosuvastatin)
• Cymbalta (duloxetine)
• Eliquis (apixaban)
• Fish Oil (omega-3 polyunsaturated fatty acids)
• Flomax (tamsulosin)
• Flonase (fluticasone nasal)
• Humalog (insulin lispro)
• Lasix (furosemide)
• Levitra (vardenafil)
• Lyrica (pregabalin)
• Metoprolol Succinate ER (metoprolol)
• Metoprolol Tartrate (metoprolol)
• Nexium (esomeprazole)
• Paracetamol (acetaminophen)
• Paxlovid (nirmatrelvir / ritonavir)
• Tylenol (acetaminophen)
• Viagra (sildenafil)
• Vitamin B12 (cyanocobalamin)
• Vitamin C (ascorbic acid)
• Vitamin D3 (cholecalciferol)
• Xarelto (rivaroxaban)

Alprostadil disease interactions

There are 3 disease interactions with alprostadil which include:

• respiratory function
• bleeding
• hypotension

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More about alprostadil

• alprostadil consumer information
• Compare alternatives
• Reviews (177)
• Side effects
• Dosage information
• During pregnancy
• Drug class: impotence agents
• En español

Related treatment guides

• Erectile Dysfunction
• Patent Ductus Arteriosus

Drug Interaction Classification

These classifications are only a guideline. The relevance of a particular drug interaction to a specific individual is difficult to determine. Always consult your healthcare provider before starting or stopping any medication.

Major	Highly clinically significant. Avoid combinations; the risk of the interaction outweighs the benefit.
Moderate	Moderately clinically significant. Usually avoid combinations; use it only under special circumstances.
Minor	Minimally clinically significant. Minimize risk; assess risk and consider an alternative drug, take steps to circumvent the interaction risk and/or institute a monitoring plan.
Unknown	No interaction information available.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

Medical Disclaimer

Alprostadil Intra-Urethral: Uses, Side Effects, Interactions, Pictures, Warnings & Dosing

Uses

This medication is used to treat male sexual function problems (erectile dysfunction). It works by helping the blood flow into the penis to achieve and maintain an erection.This medication is not for use in women or children.

How to use Alprostadil Suppository

Read the Patient Information Leaflet if available from your pharmacist before you start using alprostadil and each time you get a refill. Learn all preparation and usage instructions. If you have any questions, ask your doctor or pharmacist.

This medication is used by inserting the suppository into the penis as directed by your doctor. Remove the protective cover from the applicator before inserting into the penis. The dosage is based on your medical condition and response to treatment. This medication should usually work within 5 to 10 minutes to produce an erection that lasts for about 30 to 60 minutes. Do not use more than 2 doses in a 24-hour period.

Tell your doctor if your condition lasts or gets worse (for example, the drug does not produce an erection or it becomes more difficult to get an erection).

Side Effects

Penis/testicle/groin pain, minor bleeding or spotting from the penis, dizziness, swelling (especially of leg veins), and rapid heartbeat may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.

Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

Tell your doctor right away if you have any serious side effects, including: fainting.

Rarely, males may have a painful or prolonged erection lasting 4 or more hours. If this occurs, stop using this drug and get medical help right away, or permanent problems could occur.

In female partners, vaginal burning/itching may occur. It is not clear if this side effect is caused by the medication or sexual intercourse itself. The use of a water-based lubricant may help prevent vaginal irritation.

A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

In the US – Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.

In Canada – Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

Precautions

Before using alprostadil, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: penis conditions (such as angulation, cavernosal fibrosis, Peyronie’s disease, urethral stricture/obstruction, urethritis, infection), indwelling urethral catheter, bleeding disorders, blood system cancers (such as leukemia, multiple myeloma), heart disease, low blood pressure, sickle cell anemia.

This drug may make you dizzy. Alcohol or marijuana (cannabis) can make you more dizzy. Do not drive, use machinery, or do anything that needs alertness until you can do it safely. Limit alcoholic beverages. Talk to your doctor if you are using marijuana (cannabis).

Use of this drug does not protect against sexually transmitted diseases (such as HIV, hepatitis B, gonorrhea, syphilis). To decrease your risk of infection, always use an effective barrier method such as a latex or polyurethane condom during all sexual activity. Consult your doctor or pharmacist for more details.

This medication is not for use in women. If this drug is used by a male for sexual intercourse with a pregnant woman, an effective barrier method such as a latex or polyurethane condom should be used. Consult your doctor or pharmacist for more details.

Interactions

Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor’s approval.

Does Alprostadil Suppository interact with other drugs you are taking?

Enter your medication into the WebMD interaction checker

Overdose

If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center. Symptoms of overdose may include: fainting, painful/prolonged erection.

Do not share this medication with others.

Not applicable.

Store unopened foil pouches in the refrigerator. If necessary, this product may also be stored at room temperature for up to 14 days. Keep all medications away from children and pets.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

Selected from data included with permission and copyrighted by First Databank, Inc. This copyrighted material has been downloaded from a licensed data provider and is not for distribution, except as may be authorized by the applicable terms of use.

CONDITIONS OF USE: The information in this database is intended to supplement, not substitute for, the expertise and judgment of healthcare professionals. The information is not intended to cover all possible uses, directions, precautions, drug interactions or adverse effects, nor should it be construed to indicate that use of a particular drug is safe, appropriate or effective for you or anyone else. A healthcare professional should be consulted before taking any drug, changing any diet or commencing or discontinuing any course of treatment.

instructions for use, analogues, articles » Directory of drugs

List of trade names

Analogue of natural PgE1, has vasodilating (at the level of arterioles, precapillary sphincters, muscular arteries), antiaggregant and angioprotective action. Improves microcirculation and peripheral circulation, promotes the opening of collateral vessels. Reduces peripheral vascular resistance, blood pressure, reflexively increases heart rate, which leads to an increase in the IOC. Improves the rheological properties of blood, helping to increase the elasticity of red blood cells and reducing adhesion / aggregation of platelets. It has a fibrinolytic effect. It has an effect on metabolism, increases the utilization of glucose and oxygen, inhibits the release of free radicals and lysosomal enzymes from granulocytes and macrophages, stimulates protein synthesis, has a beneficial effect on lipid metabolism (suppressing cholesterol synthesis and lowering LDL concentration), inhibits the proliferation of smooth muscle cells. Stimulates the smooth muscles of the intestines, bladder and uterus; suppresses the secretion of gastric juice.

Pharmacokinetics

Alprostadil is an endogenous natural product with a short half-life (about 10 s). When administered intravenously, it is metabolized in the lungs (with a single passage up to 60-90%). As a result of enzymatic oxidation, 3 biologically active metabolites are formed: 15-keto-PgE1, 15-keto-13,14-dihydro-PgE1 and 13,14-dihydro-PgE1 (PgE0). Keto metabolites have a lower biological effect compared to alprostadil, the PgE0 metabolite has a comparable effect to PgE1. PgE0 acts longer, its T1 / 2 is about 1 min (alpha phase) and 30 min (beta phase). In all likelihood, the pharmacodynamic effect is mainly due to this biologically active stable metabolite. The main metabolites are excreted by the kidneys – up to 88% and with feces – 12%.

Obliterating diseases of arteries III-IV stage. (according to Fontaine’s classification), accompanied by pain at rest or trophic changes.
Obliterating endarteritis with severe “intermittent” claudication (with impossible surgical revascularization of the lower limb),
obliterating atherosclerosis,
diabetic angiopathy,
thromboangiitis obliterans (Buerger’s disease),
Raynaud’s syndrome with trophic disorders,
vasculitis ,
scleroderma,
spasms of the calf muscles,
damaging effects of physical factors, especially extreme vibration.
The need to temporarily maintain the functioning of the ductus arteriosus until the time of corrective surgery for congenital ductus-dependent heart defects in newborns (including mitral atresia, pulmonary atresia, tricuspid valve, tetralogy of Fallot).

Hypersensitivity, pregnancy, lactation. In newborns: respiratory depression, respiratory distress syndrome, a state of spontaneous persistently open arterial duct.
With care. Acute and subacute myocardial infarction, previous myocardial infarction within the last 6 months, severe or unstable angina pectoris, decompensated CHF, arterial hypotension, cardiovascular insufficiency (special attention should be paid to controlling the volume load of the carrier solution), pulmonary edema, severe arrhythmias heart, broncho-obstructive syndrome (severe with signs of respiratory failure), infiltrative changes in the lungs, liver failure (including history), increased risk of bleeding (gastric or duodenal ulcer, severe damage to cerebral vessels, proliferative retinopathy with a tendency to bleeding, extensive trauma, etc. ), hemodialysis (treatment with the drug should be carried out in the post-dialysis period), type 1 diabetes mellitus, especially with extensive vascular lesions (in elderly patients). Concomitant therapy with vasodilating or anticoagulant drugs. In newborns: bradypnea, arterial hypotension, tachycardia or hyperthermia.

In chronic obliterating diseases of the arteries, 10-20 mcg is administered intravenously (using an infusion device) for 1-2 hours 1 time per day. If the drug is administered through an established catheter, an intravenous infusion is carried out for 12 hours at a dose of 0.1-0.6 ng / kg / min (5-10 μg).
In / in – 40 mcg for 2 hours 2 times a day (after dissolving the contents of the ampoule in 50 ml of 0.9% NaCl solution) or 50-200 mcg 1 time per day (in more severe conditions – 50-100 mcg 2 times a day). As a solvent, use 200-500 ml 0.9% NaCl solution, 5-10% dextrose solution, the duration of the infusion should be at least 2 hours. The solution should be prepared immediately before administration. The duration of treatment is on average 14 days, with a positive effect, treatment with the drug can be continued for another 7-14 days. The course of treatment should not exceed 4 weeks. In the absence of a positive effect within 2 weeks from the start of treatment, further use of the drug should be discontinued.
In case of impaired renal function (serum creatinine concentration more than 1.5 mg / l), intravenous administration begins with 20 mcg. If necessary, after 2-3 days, a single dose is increased to 40-60 mcg. For patients with renal insufficiency and heart failure, the maximum volume of fluid administered is 50-100 ml / day. The course of treatment – 4 weeks. In congenital ductus-dependent malformations of newborns, it is administered continuously by infusion through an umbilical arterial catheter (led directly to the orifice of the arterial duct) or one of the large veins at an initial rate of 0.05-0.1 (up to 0.4) mcg / kg / min. After achieving a therapeutic effect, the infusion rate is reduced to the minimum maintenance – 0. 01-0.02 μg / kg / min. If severe side effects occur, the administered dose should be reduced.

From the digestive system: discomfort in the epigastric region, possible diarrhea, nausea, vomiting, increased activity of “liver” transaminases; rarely – hyperbilirubinemia.
From the CCC: lowering blood pressure, tachycardia, cardialgia; rarely – the development or aggravation of heart failure, cardiac arrhythmias, AV blockade, acute pulmonary edema.
From the nervous system: possible headache, dizziness, excessive fatigue, feeling unwell. Allergic reactions: possible skin rash, itching. On the part of the musculoskeletal system: with prolonged continuous administration (from 4 weeks or more) – reversible hyperostosis of tubular bones. Laboratory indicators: leukocytosis, leukopenia, rarely – an increase in the titer of C-reactive protein.
Local reactions: phlebitis (proximal to the site of intravenous injection, up to 40% of patients).
Other: increased sweating, hyperthermia, swelling of the limb, into the vein of which the infusion is carried out.
In newborns: hyperthermia, decreased blood pressure, hyperemia of the skin, diarrhea, bradycardia, tachycardia, skin rashes, convulsions, respiratory depression (up to apnea), rarely – disseminated intravascular coagulopathy. With a long course of treatment (within a few weeks): hyperostosis in the bones of the lower extremities. Extremely rare (up to 1% of cases): shock, acute HF, hyperbilirubinemia, bleeding, drowsiness, bradypnea, decreased respiratory function, tachypnea, anuria, impaired renal function, hypoglycemia, ventricular fibrillation, stage II AV block, supraventricular arrhythmia, tension neck muscles, irritability, hypothermia, hypercapnia, hyperemia of the skin, hematuria, peritoneal symptoms, tachyphylaxis, hyperkalemia, thrombocytopenia, anemia.
Overdose. Symptoms: decrease in blood pressure, hyperemia of the skin, weakness; in newborns, in addition: apnea, bradycardia.
Treatment: slowing down or stopping the infusion, if signs of depression of the respiratory center appear in newborns, mechanical ventilation is indicated.

Pharmaceutically incompatible with other solutions. Enhances the effect of antihypertensive drugs (including vasodilators), as well as anticoagulants and antiplatelet agents.

The prepared solution is recommended to be used immediately after preparation, it is possible to temporarily store the resulting solution for no more than 24 hours at a temperature of 2 to 8 degrees. C. Alprostadil can only be used by doctors with experience in angiology, familiar with modern methods of continuous monitoring of CVS and having the appropriate equipment for this. During the period of treatment, it is necessary to control blood pressure, heart rate, biochemical parameters of the blood, the blood coagulation system (in case of violations of the blood coagulation system or with simultaneous therapy with drugs that affect the coagulation system). Patients with ischemic heart disease, renal insufficiency (serum creatinine more than 1.5 mg / dl) should be monitored in a hospital during treatment with alprostadil and within 1 day after stopping treatment. To avoid the appearance of symptoms of overhydration in such patients, the volume of fluid administered should, if possible, not exceed 50-100 ml per day. It is necessary to dynamically monitor the patient’s condition (control of blood pressure and heart rate), if necessary – control of body weight, fluid balance, measurement of central venous pressure or echocardiography.
In newborns, the drug should be used under constant control of blood pressure, if there are conditions for mechanical ventilation. In patients with chronic obliterating diseases of the arteries of the lower extremities, infusion therapy is a necessary part of complex treatment. The clinical effect is long-term and may appear with a certain delay after the end of the course of treatment.
Phlebitis (proximal to the injection site) is usually not a reason to stop therapy, signs of inflammation disappear after a few hours after stopping the infusion or changing the injection site, specific treatment is not required in such cases. Catheterization of the central vein can reduce the incidence of this side effect of the drug.
Compliance with the dosage form of alprostadil used for specific indications for its use should be strictly observed.

official instructions for use, analogues, price, availability in pharmacies

Currently, the drug is not listed in the State Register of Medicines or the specified registration number has been excluded from the register.

Registration certificate P N012232/01

Trade name of the drug: Alprostan

International non-proprietary name of the drug. Alprostadil

Dosage form:

Concentrate for solution for infusion 0.1 mg/0.2 ml

Composition

Active substance: 1 ampoule contains 0.1 mg of alprostadil.
Excipients: absolute ethanol up to 0.2 ml.

Description

Clear, colorless solution.

Pharmacotherapeutic group

Vasodilator – preparation PGE ₁ .

ATX code: [C01EA01].

Pharmacological properties

The active substance of the drug Alprostan – alprostadil (synthetic analogue of natural prostaglandin E ₁ ) is a vasodilator, angioprotective agent. It acts in a complex manner, improving microcirculation and peripheral circulation, causing vasodilation at the level of arterioles, precapillary sphincters, and muscular arteries. With intracavernous administration, it relaxes the smooth muscles of the cavernous bodies, which helps to increase blood flow and improve microcirculation in them. With intra-arterial administration, it contributes to the temporary preservation of a functioning arterial duct in newborns.
Improves the rheological properties of blood, helping to increase the elasticity of erythrocytes; has an effect on hemocoagulation, reducing adhesion and aggregation of platelets. It has a fibrinolytic effect. It has an anti-atherogenic effect, slowing down the activation of neutrophils, excessive proliferation of vascular wall cells.
Reduces total peripheral vascular resistance, blood pressure, reflexively increases heart rate, which leads to an increase in cardiac output. Stimulates the smooth muscles of the intestines, bladder and uterus; suppresses the secretion of gastric juice.

Pharmacokinetics

The half-life is about 10 seconds. Metabolized in the lungs with a single passage up to 60-90%, as a result of enzymatic oxidation, three biologically active metabolites are formed: 15-keto-PGE1, 15-keto-13,14-dihydro-PGE1 and 13,14-dihydro-PGE1 (PGE0) . Keto metabolites have a lower biological effect compared to alprostadil, the metabolite 13,14-dihydro-PGE1 (PGE0) has a comparable effect to PGE1. Important is the fact that PGE0 acts longer, its half-life is about 1 minute (alpha phase) and 30 minutes (beta phase). In all likelihood, the pharmacodynamic effect is mainly due to this biologically active stable metabolite. The main metabolites are excreted in the urine – up to 88%, and feces – up to 12%.

Indications for use

Chronic obliterating diseases of the arteries of the extremities III-IV stage (according to Fontaine’s classification), accompanied by pain at rest or trophic changes (obliterating endarteritis with severe “intermittent claudication”, when surgery is not indicated; atherosclerosis of the arteries of the extremities; diabetic angiopathy; Buerger’s disease, Raynaud’s syndrome with trophic disorders; vasculitis in systemic scleroderma; peripheral circulatory disorders as a result of exposure to overlimiting vibration).
The need for temporary preservation of a functioning ductus arteriosus before reconstructive cardiac surgery for congenital ductus-dependent heart defects in newborns.

Contraindications

Hypersensitivity to alprostadil; pregnancy and lactation; acute and subacute myocardial infarction, severe or unstable form of angina pectoris; heart failure in the stage of decompensation, cardiac arrhythmias; severe broncho-obstructive syndrome with signs of respiratory failure, edema or infiltrative changes in the lungs; severe liver dysfunction; conditions characterized by a risk of bleeding (gastric or duodenal ulcer, severe damage to cerebral vessels, proliferative retinopathy with a tendency to bleeding, extensive trauma, etc. ). Simultaneous appointment of vasodilators and anticoagulants.
Age under 18 (excluding neonatal period) and over 75 years of age.
In neonatology: hypersensitivity to alprostadil, respiratory depression, respiratory distress syndrome, state of spontaneous persistently open ductus arteriosus.
Caution should be exercised in patients with arterial hypotension, cardiovascular insufficiency (particular attention should be paid to controlling the load “volume” due to the solvent), the increase in infusion volume should be limited in patients with severe heart failure due to the risk of pulmonary edema and possible stop hearts; in elderly patients with insulin-dependent diabetes mellitus, especially with extensive vascular lesions; when prescribing the drug to newborns in case of bradypnea, arterial hypotension, tachycardia or hyperthermia.

Dosage and administration

Use strictly as directed by your doctor to avoid complications.
In the treatment of adult patients with chronic obliterating diseases of the arteries of the extremities, Alprostan is prescribed intravenously at a dose of 50 to 200 mcg 1 time per day or, in more severe conditions, from 50 to 100 mcg 2 times a day. As a solvent, 200-500 ml of saline, 5% or 10% glucose solution are used, the duration of the infusion should be at least 2 hours. The solution should be prepared immediately before administration. The duration of the course of treatment is on average 14 days, with a positive effect, treatment with the drug can be continued for another 7-14 days. The course of treatment should not exceed 4 weeks. In the absence of a positive effect within 2 weeks from the start of therapy, further use of the drug should be discontinued.
In newborns, with congenital ductus-dependent defects, Alprostan is administered by continuous infusion into large veins or into the umbilical artery. The initial infusion rate is 0.01 to 0.05 µg/kg/min. When a therapeutic effect is achieved, the dose is reduced to the minimum maintenance dose (usually 0.01-0.02 μg / kg / min). If necessary, as an exception, the dose can be increased to 0.1 mcg / kg / min. If severe side effects occur, the administered dose should be reduced.
Recommended dilution of Alprostan, concentrate for infusion.

When diluting 1 ampoule (0.2 ml) of Alprostan, a concentrate for infusion in 9.8 ml of a carrier solution (physiological saline, 5% or 10% glucose solution), a concentration of 100 μg of alprostadil in 10 ml of solution is obtained. The resulting solution can be diluted in a larger volume of solvent. The solution is recommended to be used immediately after preparation, temporary storage of the resulting solution is possible for no more than 24 hours at a temperature of 2 – 8 ° C.

Side effect

In the treatment of limb ischemia, intravenous administration of alprostadil may be complicated by the appearance of signs of phlebitis proximal to the injection site, signs of inflammation disappear a few hours after stopping the infusion or changing the injection site, specific treatment in such cases is not required. Catheterization of the central vein can reduce the incidence of this side effect of the drug.
The number of adverse reactions may increase depending on the concentration, volume and rate of infusion. When using the drug, headache, dizziness, increased fatigue, feeling unwell, increased sweating are possible; disorders of the digestive system in the form of a feeling of discomfort in the epigastric region, nausea, vomiting, diarrhea; swelling of the limb, into the vein of which the drug solution is infused; arterial hypotension, tachycardia, angina attack, hyperthermia, allergic reactions; transient increase in the activity of hepatic transaminases in the blood serum, hyperbilirubinemia, hematuria.
A long course of treatment (from 4 or more weeks) may be complicated by reversible hyperostosis of tubular bones. There may be changes in the blood in the form of leukocytosis, leukopenia, as an exception, an increase in the titer of C-reactive protein is possible.
In newborns: hyperthermia, arterial hypotension, hyperemia of the skin, diarrhea, bradycardia, tachycardia, skin rash, convulsions, decreased respiratory function (up to apnea), DIC may develop. With a long course of treatment (within several weeks), hyperostosis of the bones of the lower extremities may appear. Possible: shock, acute heart failure, hyperbilirubinemia, bleeding, drowsiness, decreased respiratory function (bradypnea, tachypnea), decreased renal function, anuria, hypoglycemia, cardiac arrhythmias, AV blockade, neck muscle hypertonicity, irritability, hypothermia, hypercapnia , hyperemia of the skin, hematuria, peritoneal symptoms, tachyphylaxis, increased levels of potassium in the blood, thrombocytopenia, anemia.
If side effects occur, the dose of the drug should be reduced.

Overdose

In case of overdose, the following symptoms may appear: lowering of blood pressure, flushing of the skin, general weakness. If signs of overdose appear, the infusion of the drug should be slowed down or stopped. There is usually no need for specific treatment. If signs of depression of the respiratory center appear in newborns, artificial lung ventilation should be resorted to.

Interaction with other drugs

With the simultaneous appointment of alprostadil, the effect of antihypertensive and vasodilators is enhanced. With the simultaneous appointment of alprostadil with anticoagulant and antiplatelet agents, the risk of bleeding increases.

Special instructions

Alprostadil should only be used by physicians experienced in angiology, familiar with modern methods of continuous monitoring of the state of the cardiovascular system and having the appropriate equipment for this.
During the period of treatment, it is necessary to control the hemodynamic parameters of the acid-base balance, the biochemical parameters of the blood, the blood coagulation system (in case of violations of the blood coagulation system or during simultaneous therapy with drugs that affect the coagulation system).
Patients with ischemic heart disease, renal insufficiency (serum creatinine more than 1.5 mg / l) should be monitored in a hospital during treatment with alprostadil and within 1 day after stopping treatment. In order to avoid the appearance of symptoms of overhydration in such patients, the volume of fluid administered should, if possible, not exceed 50-100 ml per day. It is necessary to dynamically monitor the patient’s condition (control of blood pressure and heart rate), if necessary, control of body weight, fluid balance, measurement of central venous pressure or echocardiography.
In newborns, the drug should be used under constant monitoring of blood pressure, if there are conditions for mechanical ventilation.
In patients on hemodialysis, treatment with the drug should be carried out in the post-dialysis period.
In patients with chronic obliterating diseases of the arteries of the lower extremities, the use of the drug is part of a complex treatment, the clinical effect is long-term and may occur with a certain delay after the end of the course of treatment.

Release form

0.2 ml in colorless glass ampoules. 5 ampoules are placed in a molded PVC container.