Piperaz 100%

Indications

• Gastrointestinal disturbances
• Toxin adsorption in cases of poisoning
• Diarrhea
• Gastroenteritis

Dosage

Children: Refer to the specific product guidelines or consult clinical resources for dosing recommendations.

Adults: Refer to the specific product guidelines or consult clinical resources for dosing recommendations.

Mechanism of action

Bentonite works by adsorbing toxins and pathogens in the gastrointestinal tract. The high surface area and negative charge of bentonite particles attract positively charged ions, allowing it to bind to various substances, including bacteria and toxins, thereby facilitating their removal from the body.

Pharmacodynamics

Bentonite's pharmacodynamic properties are largely attributed to its adsorptive capacity. It can effectively bind to various drugs and toxins, reducing their bioavailability. This property makes it useful in treating cases of poisoning or overdose, as it can prevent the absorption of harmful substances in the intestines.

Pharmacokinetics

Bentonite is not absorbed systemically. After oral administration, it remains in the gastrointestinal tract where it exerts its effects. The clay is eventually excreted in the feces. The onset of action can vary depending on the formulation and the presence of other substances in the gastrointestinal tract.

Adverse effects

• Constipation
• Abdominal discomfort
• Nausea

Interactions

• May reduce the absorption of other medications when taken concurrently

Precautions

• Use with caution in patients with gastrointestinal obstructions
• Ensure adequate hydration to prevent constipation

Pregnancy

Bentonite is generally considered safe during pregnancy; however, clinical data is limited.

Breast-feeding

Bentonite is likely safe during breastfeeding, but consult a healthcare professional for personalized advice.

Storage

Store in a cool, dry place away from direct sunlight.

Formulations

• Powder
• Capsules
• Suspension

Indications

• Food preservative
• Treatment of urea cycle disorders
• Metabolic disorders involving benzoyl-CoA

Dosage

Children: Refer to the BNF for Children for specific dosing guidelines based on condition.

Adults: Refer to the BNF for specific dosing guidelines based on condition.

Mechanism of action

Benzoate acts mainly by inhibiting the growth of bacteria and fungi through its ability to lower the pH, creating an environment that is less favorable for microbial growth. It is also involved in metabolic pathways where it helps in the conjugation of toxic substances, facilitating their excretion from the body.

Pharmacodynamics

Benzoate is known for its antimicrobial properties, which are particularly effective against a wide range of fungi and bacteria. Its efficacy as a preservative is due to its ability to penetrate microbial cell membranes and disrupt their metabolic processes. Additionally, it has been observed to modulate various metabolic pathways, particularly those associated with aromatic compound degradation.

Pharmacokinetics

After ingestion, benzoate is rapidly absorbed in the gastrointestinal tract. It is metabolized primarily in the liver, where it undergoes conjugation with glycine to form hippurate, which is then excreted in the urine. The half-life of benzoate varies depending on individual metabolic rates but is generally short due to its efficient conversion and excretion.

Pregnancy

There is limited data on the use of benzoate in pregnancy. Consultation with healthcare professionals is advised before use.

Breast-feeding

Limited data is available on the excretion of benzoate in breast milk. Caution is recommended when administering to nursing mothers.

Storage

Store in a cool, dry place away from direct sunlight. Keep out of reach of children.

Indications

• Ascariasis
• Partial intestinal obstruction due to Ascaris lumbricoides

Dosage

Children: Refer to BNF for Children for specific dosing information.

Adults: Refer to BNF for specific dosing information.

Mechanism of action

Piperazine functions as a GABA receptor agonist, selectively binding to muscle membrane GABA receptors in nematodes. This binding induces hyperpolarization of nerve endings, leading to flaccid paralysis of the worms. By blocking the response of worm muscle to acetylcholine, piperazine alters cell membrane permeability to ions, resulting in hyperpolarization and suppression of spontaneous spike potentials, thereby facilitating the expulsion of the worm through normal intestinal peristalsis.

Pharmacodynamics

Piperazine is effective as an anthelminthic, particularly for treating infections from Ascaris lumbricoides. It induces reversible muscle paralysis in nematode parasites by hyperpolarizing their cell membranes. The primary clinical use is in addressing complications such as partial intestinal obstruction caused by these worms, a condition more frequently encountered in children.

Pharmacokinetics

The pharmacokinetics of piperazine, including absorption, distribution, metabolism, and excretion, have not been well-characterized in the available literature. However, it is generally understood that piperazine is absorbed from the gastrointestinal tract and is metabolized in the liver. Further detailed studies may be required to elucidate its complete pharmacokinetic profile.

Adverse effects

• Nausea
• Vomiting
• Abdominal pain
• Diarrhea
• Headache
• Dizziness

Precautions

• Use with caution in patients with renal impairment
• Consider potential interactions with other central nervous system depressants

Pregnancy

Limited data are available on the safety of piperazine during pregnancy. Use only if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

Piperazine is excreted in breast milk; use with caution and consider the need for monitoring the infant.

Storage

Store in a cool, dry place away from light. Keep out of reach of children.

Formulations

• Piperazine citrate
• Piperazine hydrate

Mechanism of action

Piperazine is a GABA receptor agonist. Piperzine binds directly and selectively to muscle membrane GABA receptors, presumably causing hyperpolarization of nerve endings, resulting in flaccid paralysis of the worm. While the worm is paralyzed, it is dislodged from the intestinal lumen and expelled live from the body by normal intestinal peristalsis. Piperazine blocks the response of the /target species/ worm muscle (best studied in Ascaris), causing flaccid paralysis of the worm. While the worm is paralyzed, it is dislodged from the intestinal lumen and expelled live from the body by normal intestinal peristalsis. The predominant effect of piperazine on /the target species/ Ascaris is to cause a flaccid paralysis that results in expulsion of the worm by peristalsis. ... Piperazine blocks the response of Ascaris muscle to acetylcholine, apparently by altering the permeability of the cell membrane to ions that are responsible for the maintenance of the resting potential. The drug causes hyperpolarization and suppression of spontaneous spike potentials with accompanying paralysis. Piperazine citrate causes reversible muscle paralysis in intestinal nematodes, presumably by causing hyperpolarization of nerve endings /in this target species/. /Piperazine citrate/ Piperazine and its salts, as a gamma-aminobutyric acid (GABA)-like substance, induce a reversible flaccid paralysis in the /target/ nematode parasites. This is provoked by a hyperpolarization of the cell membrane followed by suppression of spontaneous spike potentials. THe paralyzed nematodes are expelled from the gut lumen by normal peristaltic actions. In mammals, motorcortical GABAa inhibition is important for initiation of smooth flexion and/or extension movements of the extremities affecting motor and postural control. When injected into the hand motor cortical area of three infant macaque monkeys, the GABA agonist muscimol disrupted forelimb movement showing a posture of dropped wrist and fingers as if the radial nerve were paralysed. Interestingly, the three investigated animals exhibited large inter-individual differences in sensitivity to the action of the same dose of muscimol, being low in one, moderate in the second and substantial in the third. Injection into the medial segment of globus pallidus elicited choreiform movements and injections into substantia nigra pars reticulata provoked severe axial posture anomalies with rotational behaviour as well as contralateral hypotonia. Although the symptoms induced by piperazine in sensitive species exhibits some of these features, it is possible that its effects in mammals also involve other modes of action as well, in as much as a nicotinic action on rat sympathetic ganglia in vitro was reported in one series of experiments.

Pharmacodynamics

Piperazine is an anthelminthic especially useful in the treatment of partial intestinal obstruction caused by Ascaris worms, which is a condition primarily seen in children. Piperazine hydrate and piperazine citrate are the main anthelminthic piperazines.