Praziquantel CAS 55268-74-1, Praziquantel, CAS 55268-74-1
Muscle spasmodic palsy: Rapidly increase the permeability of the insect cell membrane to Ca²⁺, causing the insect's muscles to become rigid and contract, and detaches from the host tissue (such as the vessel wall).
55268-74-1
C19H24N2O2
312.41
259-559-6
CAS | 55268-74-1 |
Molecular formula | C19H24N2O2 |
Molecular weight | 312.41 |
EIENCS | 259-559-6 |
Form | powder or crystals |
Melting point | 136-138 C |
boling point | 1377℃ |
Density | 1.1209 |
Solubility | ethanol: soluble5mg/mL |
PKA | -0.98±0.20(Predicted) |
Color | Crystals from EtOAc/hexane |
Storage temp | Sealed in dry,Store in freezer, under -20°C |
Dual insecticidal mechanism
Muscle spasmodic palsy: Rapidly increase the permeability of the insect cell membrane to Ca²⁺, causing the insect's muscles to become rigid and contract, and detaches from the host tissue (such as the vessel wall).
Cortical damage and immune exposure: Destroying the syncytic cortex of the insect body exposes antigens, attracting immune cells such as eosinophils to attack the insect body, and inhibiting glucose metabolism/nucleic acid synthesis in the insect body.
Broad-spectrum insecticidal activity
It is highly effective against adult and larval larvae (cercariae and cercariae) of schistosoma japonicum, tapeworms (beef/pork tapeworms), cysticercosis, lung flukes and Clonorchis sinensis, but ineffective against eggs.
Disease type | Treatment plan | Remarks |
---|---|---|
Chronic schistosomiasis | Take 60 mg/kg, divided into 2 to 3 doses, for a course of 1 to 2 days | Weight over 60 kilograms is calculated as 60 kilograms |
Acute schistosomiasis | Take 120 mg/kg in 2 to 3 divided doses for a 4-day course | Dexamethasone should be used in combination to prevent immune responses |
Clonorchis sinensis | Take 210 mg/kg three times a day for three consecutive days | The cure rate is over 90% |
Paragonimiasis | 25 mg/kg, three times a day, for three consecutive days | Brain type requires hospitalization |
Cysticercosis | Take 120-180 mg/kg, divided into 3-5 days | Cerebral cysticercosis requires pretreatment to reduce intracranial pressure |
Tapeworm disease | Take 10-25 mg/kg at one time, and then take magnesium sulfate for laxative treatment one hour later | A higher dose is required for short tapeworms |
Absorption:After oral administration, 80% is rapidly absorbed, and the peak blood drug value reaches approximately 1 hour (1 mg/L @15 mg/kg).
Distribution:It is widely distributed in the liver, kidneys and lungs, and can pass through the blood-brain barrier (cerebrospinal fluid concentration ≈ 20% blood drug concentration).
Metabolism/Excretion:The liver metabolizes it into hydroxyl products, with a half-life of 0.8 to 1.5 hours, and 80% is excreted through the kidneys within 4 days
Common adverse reactions
Dizziness (30%), nausea (20%), abdominal pain (15%), transient elevation of transaminase (5%).
Severe reactions: supraventricular tachycardia, anaphylactic shock (rare).
Contraindications and caution:
Absolute contraindications: Cysticercosis (blindness caused by the death of the parasite), allergy to praziquantel, and combination use of rifampicin (inducing metabolic failure).
Relative contraindications: Pregnancy/lactation period (milk concentration ≈ 25% serum), severe heart, liver or kidney diseases, history of epilepsy.
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