D-WORM GOLD

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 nematode infections
• Ascariasis
• Strongyloidiasis
• Hookworm infections

Dosage

Children: Refer to appropriate clinical guidelines for dosing information as specific dosages are not provided.

Adults: Refer to appropriate clinical guidelines for dosing information as specific dosages are not provided.

Mechanism of action

Ocyclozonide exerts its anthelmintic effects by interfering with the energy metabolism of helminths. It is believed to inhibit the enzyme fumarate reductase, which is crucial for the conversion of fumarate to succinate in the electron transport chain of the parasite. This disruption leads to reduced ATP production, resulting in impaired energy metabolism and eventual death of the parasite.

Pharmacodynamics

The pharmacodynamic profile of oxyclozonide reveals its capacity to selectively target nematodes while sparing mammalian cells. This selectivity is attributed to its specific action on the metabolic pathways unique to helminths. The drug's effectiveness is influenced by the life stage of the parasite, with juvenile forms typically being more susceptible than adult worms. Resistance development has been noted in some parasitic populations, necessitating careful management of treatment regimens.

Pharmacokinetics

Ocyclozonide exhibits variable absorption when administered orally, with peak plasma concentrations occurring within a few hours post-administration. It undergoes hepatic metabolism and has a potentially long half-life, allowing for less frequent dosing. The drug is primarily excreted via the fecal route, with minimal renal elimination. Its pharmacokinetic properties can be affected by factors such as age, liver function, and concurrent medications.

Adverse effects

• Gastrointestinal disturbances
• Allergic reactions
• Dizziness
• Headaches

Precautions

• Use with caution in patients with a history of hypersensitivity to the drug
• Monitor liver function in prolonged use

Pregnancy

Safety in pregnancy has not been established. Use only if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

It is not known whether oxyclozonide is excreted in human breast milk. Caution should be exercised when administering to breastfeeding women.

Storage

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

Formulations

• Tablets
• Suspensions

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.