Piperazine

Piperazine (in the form of piperazine adipate) is an antihelminthic drug used to treat certain species of roundworms (nematodes), particularly ascarids (Ascaris lumbricoides) and pinworms (Enterobius vermicularis). Piperazine acts by paralyzing the musculature of helminths, which prevents their ability to attach to the intestinal walls of the host. As a result, the parasites are naturally eliminated from the body with fecal matter.

Piperazine acts by specifically blocking neuromuscular transmission in worms, causing their paralysis without stimulating excretion. This distinguishes it from some other antihelminthic drugs, which can cause more active helminth excretion and associated symptoms. Due to its action, piperazine is considered relatively safe, especially for treating infestations in children.

Before starting treatment with piperazine, it is necessary to make sure that there are no contraindications to its use. These may include chronic kidney and liver disease, neurological disorders and individual intolerance to the drug components. It is also important to ensure adequate hydration during treatment and take into account the possibility of the need for a repeated course to prevent recurrence of infection, especially in enterobiasis, where the risk of re-infection is high.

Indications Piperazinef

1. Ascaridosis: A helminthiasis caused by a species of intestinal worm known as Ascaris lumbricoides (ascarids). Ascaridosis can lead to various symptoms such as abdominal pain, nausea, vomiting, diarrhea, and breathing problems if the worms migrate to the lungs.
2. Enterobiasis: An infection caused by Enterobius vermicularis. This infection is common in children and can cause itching in the anus area, especially at night when the female worm emerges from the rectum to lay eggs around the anus.
3. Trichocephalosis: An infection caused by the intestinal worm Trichuris trichiura (trichocephalus). Trichocephalosis can lead to abdominal pain, diarrhea, as well as developmental delays and poor food absorption.
4. Necatoriasis: A helminthiasis caused by hookworms of the genus Necator. These parasites can cause intestinal bleeding and anemia.
5. Strongyloidiasis: An infection caused by nematodes of the genus Strongyloides. Strongyloidosis can lead to symptoms similar to those seen in ascaridosis and other helminthic diseases.

Release form

1. Tablets: Convenient form for adults and older children, allowing precise control of dosage.
2. Powder: Can be dissolved in water to create a suspension, which makes it easier for young children or people who have difficulty swallowing tablets to take the drug.
3. Oral solution: Ready-to-use liquid form, which may also be preferred for children and patients requiring individualized dosage.

Pharmacodynamics

1. Paralyzing helminths: Piperazine acts on the nervous system of helminths by blocking glutamate-gatcine, a neurotransmitter responsible for transmitting signals between nerve cells and muscles. This leads to paralysis of the helminths' muscles and their rejection from the intestine.
2. Specificity of action: Piperazine usually acts on helminths found in the intestines, particularly ascarids (roundworms). It is less effective against other types of parasites, such as tapeworms.
3. No action on the human nervous system: Since piperazine blocks specific neurotransmitters characteristic of the nervous system of helminths, its action does not have a negative effect on the human nervous system.
4. Lack of absorption into the bloodstream: Piperazine is poorly absorbed from the intestine into the bloodstream, meaning that its action is limited primarily in the intestine where the parasites are located.
5. Rapid excretion: After use, piperazine is rapidly excreted from the body through the kidneys, which reduces the risk of toxic effects.
6. Low human toxicity: Piperazine has low human toxicity and is generally well tolerated.

Pharmacokinetics

1. Absorption: Piperazine is generally well absorbed from the gastrointestinal tract after oral administration.
2. Distribution: It may be distributed evenly throughout tissues and body fluids.
3. Metabolism: Piperazine may undergo some metabolization in the liver, but the bulk remains unchanged.
4. Excretion: Excretion of piperazine occurs mainly through the kidneys as unchanged drug.
5. Half-life: The half-life of piperazine is approximately 3-6 hours.

Dosing and administration

The following are general guidelines, but it is important to follow your doctor's instructions and the instructions provided with the medication.

For the treatment of ascaridosis and enterobiasis:

Adults and children over 2 years of age:

• Theusual dosage is 3.5 grams of piperazine adipate per day for two consecutive days.
• The dose may be divided into two doses (morning and evening) or taken once.
• For children, the dosage is selected depending on age and weight. Approximately, the recommended dose is 75 mg per kilogram of body weight per day.

Infants and children under 2 years of age:

• The dosage should be strictly determined by your doctor, but it is usually lower than for older children and adults.

Method of preparing a solution from powder:

If the drug is used in powder form, it must be dissolved in water according to the instructions on the package. As a rule, the powder is mixed with the specified amount of water until a homogeneous suspension is obtained, which can then be drunk.

Important points:

• After the course of treatment, it is recommended to conduct a control stool analysis for the presence of helminth eggs to make sure that the therapy is effective.
• In some cases, it may be necessary to repeat the course a week or two after the initial treatment, especially for enterobiasis, to prevent recurrences.
• During the treatment period, it is important to observe personal hygiene, wash your hands regularly and keep your home clean to minimize the risk of re-infection and infection of others.

Use Piperazinef during pregnancy

Piperazine (piperazine adipate) is a drug that is sometimes used to treat helminth infections. However, its use during pregnancy may be limited due to insufficient data on its safety for the fetus.

In most cases, the use of piperazine is not recommended during pregnancy, especially in the first trimester when the fetal organs are being formed. There are insufficient controlled studies to fully evaluate the potential risks and benefits of its use during this period.

Contraindications

1. Allergic reaction: People with known hypersensitivity to piperazine adipate or other components of the drug should avoid its use.
2. Liver disease: In patients with severe liver disease, it is recommended to consult a physician before starting treatment with piperazine.
3. Pregnancy and lactation: There are limited safety data on the use of piperazine adipate during pregnancy and lactation, therefore it should be used with caution in these cases.
4. Pediatric age: The use of piperazine adipate in children should be carried out under the supervision of a physician and in compliance with dosage recommendations.
5. Seizure Disorders: Piperazine adipate may cause seizures in some patients, so it should be used with caution in people with a predisposition to seizures or with seizure disorders.
6. Kidney disease: Patients with serious kidney disease are also advised to consult a doctor before starting treatment with piperazine.

Side effects Piperazinef

1. Gastrointestinal disorders: Includes nausea, vomiting, diarrhea, abdominal pain, and dyspepsia (digestive disorders).
2. Nervous system: Dizziness, headache, drowsiness and fatigue may occur.
3. Allergic reactions: In rare cases, allergic reactions such as skin rash, itching or angioedema may occur.
4. Genitourinary system: It is possible to develop difficulties with urination, a feeling of discomfort in the area of the urethra.
5. Central nervous system: Convulsions may occur with prolonged use or when the dose is exceeded.
6. Metabolic disorders: In some cases piperazine may cause changes in blood electrolyte levels such as hypernatremia or hypokalemia.
7. Cardiovascular system: Decrease in blood pressure is possible.
8. Others: Asthenia (general weakness), dry mouth and loss of appetite may occur.

Overdose

1. Toxic effects on the nervous system: Central nervous system symptoms such as dizziness, drowsiness, insomnia, headache and seizures may occur.
2. Esophageal irritation and GI dysfunction: Overdose may cause nausea, vomiting, abdominal pain, diarrhea and other GI disorders.
3. Allergic reactions: In some cases, allergic reactions such as skin rash, itching or angioedema may occur.
4. Other symptoms: Other symptoms of overdose are possible, including increased body temperature, abnormal heart rhythm, and even coma.

Interactions with other drugs

1. Centrally acting drugs: Because piperazine may cause sedation and other central side effects, it should be used with caution when used concomitantly with other drugs that may also have a depressant effect on the central nervous system, such as sleeping pills, sedatives, and analgesics.
2. Anticonvulsants: Concomitant administration of piperazine with anticonvulsants may increase sedative effect and risk of undesirable side effects.
3. Drugs that increase the QT interval: Interaction of piperazine with drugs that increase the duration of the QT interval may increase the risk of cardiac arrhythmias.
4. Drugs that reduce intestinal peristalsis: Concomitant use with drugs that reduce intestinal peristalsis, such as anticholinergic drugs or opioids, may result in a risk of paralytic intestinal obstruction.
5. Drugs withhepatotoxicity: In concomitant administration of piperazine with drugs that may have hepatotoxic effect, caution should be exercised and liver function should be monitored regularly.