Praziquantel (Tablets) Instructions for Use

Marketing Authorization Holder

LIFE SCIENCES OHFK, LLC (Russia)

Manufactured By

OHFK, JSC (Russia)

ATC Code

P02BA01 (Praziquantel)

Active Substance

Praziquantel (Rec.INN registered by WHO)

Dosage Form

Praziquantel

Film-coated tablets, 600 mg: 6 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets white, oblong, biconvex, with 3 dividing lines on both sides of the tablet; the core on the cross-section is from almost white to white with a yellowish tint.

Excipients: sodium carboxymethyl starch, microcrystalline cellulose (type 102), crospovidone, povidone, sodium lauryl sulfate, magnesium stearate, shell (hypromellose, macrogol 6000, titanium dioxide (E171)).

6 pcs. – polymer jars (1) – cardboard packs.
6 pcs. – contour cell blisters (1) – cardboard packs.

Clinical-Pharmacological Group

Anthelmintic drug

Pharmacotherapeutic Group

Anthelmintic agent; agents for the treatment of trematode infections; quinoline derivatives and related compounds

Pharmacological Action

Anthelmintic agent, a pyrazinoisoquinoline derivative. It has a broad spectrum of activity, which includes many trematodes and cestodes. Thus, Praziquantel is highly active against all human pathogenic agents of schistosomiasis, clonorchiasis, paragonimiasis, opisthorchiasis, as well as against Fasciolopsis buski, Heterophyes heterophyes and Metagonimus yokogawai (intestinal flukes). Among trematodes, Fasciola hepatica is resistant to praziquantel; the mechanism of resistance is not clear. Praziquantel is highly effective against the agents of intestinal cestodiasis: hymenolepiasis (Hymenolepis nana), diphyllobothriasis (Diphyllobothrium latum), taeniarhynchosis (Taeniarhynchus saginatus), taeniasis (Taenia solium), and also acts on cysticerci.

Praziquantel is characterized by two main effects on sensitive helminths. In low doses, it causes an increase in muscle activity, followed by contraction of the musculature and spastic paralysis. In slightly higher doses, it causes damage to the tegument (the outer covering of flatworms). The mechanism of action is not fully understood. It is believed that the effect of praziquantel is due to its ability to increase membrane permeability to calcium ions (and some other mono- and divalent cations).

Pharmacokinetics

Rapidly and completely absorbed from the gastrointestinal tract. C_max is reached in 1-3 hours. Plasma protein binding is 80%. Metabolized in the liver to form inactive mono- and polyhydroxylated metabolites. T_1/2 is 0.8-1.5 hours for praziquantel and 4-6 hours for its metabolites. Excreted mainly by the kidneys (80% within 4 days), predominantly as metabolites: 90% is excreted within 24 hours. A small amount is excreted in the feces. Passes into breast milk in small amounts. In case of renal impairment, excretion is slowed down; in case of liver damage, the intensity of metabolism decreases, which is accompanied by a longer presence of unchanged praziquantel in the body with the creation of high concentrations.

Indications

Schistosomiasis, including intestinal schistosomiasis and urogenital schistosomiasis; opisthorchiasis, clonorchiasis, paragonimiasis, metagonimiasis, fasciolopsiasis and other trematodoses caused by sensitive helminths. Intestinal cestodoses: hymenolepiasis, diphyllobothriasis, taeniarhynchosis, taeniasis. Neurocysticercosis.

ICD codes

Dosage Regimen

Determine the dosage based on the specific helminth infection and the patient’s body weight.

Administer a single dose of 10 mg/kg to 50 mg/kg.

For schistosomiasis, administer 40 mg/kg as a single dose or 20 mg/kg twice daily for one day.

For clonorchiasis, opisthorchiasis, and paragonimiasis, administer 25 mg/kg three times daily for one or two days.

For intestinal cestodiasis (taeniasis, diphyllobothriasis), administer 10-25 mg/kg as a single dose.

For hymenolepiasis, administer 25 mg/kg, repeated after 7-10 days.

For neurocysticercosis, administer 50 mg/kg per day in three divided doses for 14 days; concomitant corticosteroid therapy is recommended.

Take tablets unchewed during or immediately after a meal with a small amount of water.

Do not divide the 600 mg tablet; use it for dosing regimens requiring a full 600 mg increment.

Avoid grapefruit juice during treatment as it may increase plasma concentrations.

In patients with hepatic impairment, use with extreme caution due to reduced metabolism and potential for toxicity.

Adverse Reactions

From the central nervous system and peripheral nervous system headache, dizziness, drowsiness, myalgia; in the treatment of neurocysticercosis, manifestations of meningism, thinking disorders, increased intracranial pressure, hyperthermia are possible.

From the digestive system abdominal pain, nausea, vomiting; rarely – transient increase in liver transaminase levels.

Allergic reactions rarely – fever, skin rashes.

Contraindications

Hypersensitivity to praziquantel, cysticercosis of the eye, first trimester of pregnancy, lactation, children under 4 years of age, hepatic insufficiency, cysticercosis of the liver.

Use in Pregnancy and Lactation

Praziquantel is contraindicated for use in the first trimester of pregnancy and during lactation (breastfeeding).

In the second and third trimesters of pregnancy, Praziquantel is used only for strict indications.

If it is necessary to use during lactation, it is recommended to interrupt breastfeeding on the day of praziquantel intake and for the next 72 hours.

Use in Hepatic Impairment

Contraindicated in hepatic insufficiency, cysticercosis of the liver.

Pediatric Use

Contraindicated in children under 4 years of age.

Special Precautions

Praziquantel is not used for cysticercosis of the eye due to the danger of developing damage to the eye tissues during the death of cysticerci.

Effect on ability to drive vehicles and mechanisms

During the intake of praziquantel and for the next 24 hours, it is necessary to refrain from driving vehicles and other potentially hazardous activities.

Drug Interactions

Dexamethasone reduces the plasma concentration of praziquantel.

Storage Conditions

Store at 2°C (36°F) to 30°C (86°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.