Levifarm 20% Water Soluble Powder

Indications

• Helminth infections
• Strongyloides infections
• Brugia malayi infections
• Wuchereria bancrofti infections
• Adjunctive therapy in colon cancer with fluorouracil

Dosage

Children: For children aged 1 month to 9 years: Initially 1 mg/kg daily in divided doses on the first day, then increased to 3

Adults: Initially 1 mg/kg daily on the first day, then increased to 6 mg/kg daily in divided doses, with the maximum dose not exceeding 9 mg/kg per day.

Mechanism of action

Levamisole exerts its antiparasitic action by acting as an agonist at L-subtype nicotinic acetylcholine receptors in the muscles of nematodes. This results in paralysis of the worms, preventing their reproductive capabilities. As an immunomodulator, Levamisole restores depressed immune functions, enhances T-cell activation, stimulates antibody formation, and increases macrophage and neutrophil activities.

Pharmacodynamics

Levamisole's pharmacodynamics are characterized by its dual role as an anthelmintic and an immunomodulator. As an anthelmintic, it specifically targets nematodes by agonizing their nicotinic acetylcholine receptors, leading to muscle paralysis. The immunomodulatory effects include activation of natural killer (NK) cells and T-cells, enhancing the host's immune response, and improving macrophage function.

Pharmacokinetics

Levamisole is rapidly absorbed after oral administration, with peak plasma concentrations occurring within 1 to 2 hours. It is extensively metabolized in the liver, and its metabolites are excreted in urine. The elimination half-life is approximately 4 to 6 hours. Care should be taken in patients with hepatic impairment, as dose adjustments may be necessary.

Contra-indications

• Blood disorders

Adverse effects

• Arthralgia (long term use)
• Diarrhoea
• Dizziness
• Headache
• Influenza-like illness (long term use)
• Insomnia (long term use)
• Myalgia (long term use)
• Nausea
• Rash (long term use)
• Seizure (long term use)
• Taste altered (long term use)
• Vasculitis (long term use)
• Vomiting

Interactions

• Levamisole moderately decreases exposure to albendazole
• Levamisole increases exposure to ivermectin

Precautions

• Epilepsy
• Sjögren’s syndrome

Pregnancy

Embryotoxic in animal studies, avoid if possible.

Breast-feeding

No information available.

Storage

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

Formulations

• 50 mg chewable tablets

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

• Lactose intolerance
• As a filler or excipient in pharmaceutical formulations

Dosage

Children: Refer to the BNF for Children for specific dosing information based on age and clinical context.

Adults: Refer to the BNF for specific dosing information based on clinical context.

Mechanism of action

Lactose is metabolized in the intestine by the enzyme lactase into its constituent monosaccharides, glucose and galactose. In individuals with lactase deficiency, unabsorbed lactose passes into the colon, where it is fermented by bacteria, leading to gas production and osmotic effects that contribute to diarrhea.

Pharmacodynamics

The pharmacodynamics of lactose are primarily related to its effects on gastrointestinal function. In healthy individuals, lactose is effectively broken down into glucose and galactose, which are absorbed and utilized for energy. In individuals with lactose intolerance, the unabsorbed lactose can cause osmotic diarrhea and colonic fermentation, leading to discomfort and symptoms associated with lactose intolerance.

Pharmacokinetics

Lactose is not absorbed in the gastrointestinal tract until it is hydrolyzed into glucose and galactose by lactase. The absorption of glucose and galactose occurs in the small intestine. The half-life is not applicable as lactose is not typically administered as a medication but is rather ingested as a natural component of food. Its metabolism primarily occurs in the intestine.

Adverse effects

• Bloating
• Diarrhea
• Abdominal pain
• Flatulence

Precautions

• Use with caution in patients with lactose intolerance.
• Consider potential for gastrointestinal upset in sensitive individuals.

Pregnancy

Lactose is generally considered safe for use during pregnancy. However, consult a healthcare professional for individual advice.

Breast-feeding

Lactose is safe to use while breastfeeding, as it is a natural sugar present in breast milk.

Storage

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

Formulations

• Powder
• Granules
• Tablets
• Syrup

Indications

• Fluid replacement therapy in dehydration
• Electrolyte replenishment
• As a diluent for intravenous medications
• Wound irrigation
• Intra-amniotic instillation for abortion procedures

Dosage

Children: Paediatric dosing of saline is dependent

Adults: The dosage of saline varies depending on the clinical indication. For fluid resuscitation, isotonic saline (0.9% NaCl) is typically administered at a rate determined by the patient's condition and response to therapy. Refer to specific clinical guidelines for detailed dosing.

Mechanism of action

Sodium and chloride, the major electrolytes in extracellular fluid, control extracellular volume and blood pressure. Changes in sodium concentrations are linked to water balance disorders. Intra-amniotic instillation of hypertonic sodium chloride injection may induce abortion, potentially mediated by prostaglandins released from damaged decidual cells, resulting in uterine contractions that lead to evacuation of the fetus and placenta.

Pharmacodynamics

Sodium, as the principal cation in extracellular fluid, regulates water distribution, fluid balance, and osmotic pressure. It plays a crucial role in maintaining acid-base equilibrium in conjunction with chloride and bicarbonate. Chloride, the major extracellular anion, closely follows sodium metabolism, with fluctuations in acid-base balance reflected in chloride concentrations.

Pharmacokinetics

Saline is administered intravenously or through other routes depending on clinical needs. Once in the body, sodium and chloride are distributed in the extracellular fluid compartment. The elimination of sodium occurs primarily through renal excretion, while chloride follows similar pathways. The pharmacokinetic properties can vary based on the concentration of the saline solution and the physiological state of the patient.

Pregnancy

Saline is generally considered safe for use during pregnancy, but its use should be justified based on the clinical situation.

Breast-feeding

Saline is considered safe to use during breastfeeding, as it is not expected to affect the milk or nursing infant.

Storage

Store at room temperature, away from light and moisture. Do not freeze.

Formulations

• 0.9% Sodium Chloride Injection
• 20% Sodium Chloride Injection

Mechanism of action

The mechanism of action of levamisole as an antiparasitic agent appears to be tied to its agnositic activity towards the L-subtype nicotinic acetylcholine receptors in nematode muscles. This agonistic action reduces the capacity of the males to control their reproductive muscles and limits their ability to copulate. The mechanism of action of Levamisole as an anticancer drug in combination with fluorouracil is unknown. The effects of levamisole on the immune system are complex. The drug appears to restore depressed immune function rather than to stimulate response to above-normal levels. Levamisole can stimulate formation of antibodies to various antigens, enhance T-cell responses by stimulating T-cell activation and proliferation, potentiate monocyte and macrophage functions including phagocytosis and chemotaxis, and increase neutrophil mobility, adherence, and chemotaxis.

Pharmacodynamics

Levamisole is a synthetic imidazothiazole derivative that has been widely used in treatment of worm infestations in both humans and animals. As an anthelmintic, it probably works by targeting the nematode nicotinergic acetylcholine receptor. As an immunomodulator, it appears that Levamisole is an immunostimulant which has been shown to increase NK cells and activated T-cells in patients receiving this adjuvantly along with 5FU for Stage III colon cancer.

Mechanism of action

Sodium and chloride - major electrolytes of the fluid compartment outside of cells (i.e., extracellular) - work together to control extracellular volume and blood pressure. Disturbances in sodium concentrations in the extracellular fluid are associated with disorders of water balance. Intra-amniotic instillation of 20% sodium chloride injection induces abortion and fetal death. Although the mechanism has not been conclusively determined, some studies indicate that the drug's abortifacient activity may be mediated by prostaglandins released from decidual cells damaged by hypertonic solutions of sodium chloride. Hypertonic sodium chloride-induced uterine contractions are usually sufficient to cause evacuation of both the fetus and placenta; however, abortion may be incomplete in 25-40% of patients. /20% injection/

Pharmacodynamics

Sodium, the major cation of the extracellular fluid, functions primarily in the control of water distribution, fluid balance, and osmotic pressure of body fluids. Sodium is also associated with chloride and bicarbonate in the regulation of the acid-base equilibrium of body fluid. Chloride, the major extracellular anion, closely follows the metabolism of sodium, and changes in the acid-base balance of the body are reflected by changes in the chloride concentration.