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Penehyclidine Hydrochloride Injection

Function and Efficacy

This product is a new type of selective anticholinergic drug that can enter the brain through the blood-brain barrier. It can block the stimulatory effect of acetylcholine on muscarinic receptors (M receptors) and nicotinic receptors (N receptors) in the brain; therefore, it can better antagonize the central poisoning symptoms caused by organophosphorus poisons (pesticides), such as convulsions, central respiratory and circulatory failure, and irritability. At the same time, it also has a strong blocking effect on the stimulatory effect of acetylcholine on M receptors in the periphery; therefore, it can better antagonize the muscarinic poisoning symptoms caused by organophosphorus poisons (pesticides), such as bronchial smooth muscle spasm and increased secretion, sweating, dilation, miosis, and gastrointestinal smooth muscle spasm or contraction. It can also increase respiratory rate and respiratory flow, but since this product has no obvious effect on M2 receptors, it has no obvious effect on heart rate; it has no obvious antagonistic effect on peripheral N receptors. This product has low toxicity, with mouse LD50 of 261.7 mg/kg (im), 71.2 mg/kg (iv); rat LD50 of 450.7 mg/kg (im), 71.2 mg/kg (iv); in long-term toxicity tests on rats and dogs, except for some common anticholinergic reactions, no other abnormalities were found, and the intramuscular local irritation test met the requirements. The mutagenicity test was negative; there was no obvious general reproductive toxicity at a dose equivalent to 75 times the human dose; no teratogenic effect and embryotoxicity were found at a dose equivalent to 300 times the human dose, and no behavioral teratogenic effect was found.

Ingredients

The main ingredient of this product is penehyclidine hydrochloride

Name Description Content CAS NO. Manufacturer
Penehyclidine HCl (Mixture of IsoMers)Ingredients

This product is a new type of selective anticholinergic drug that can enter the brain through the blood-brain barrier. It can block the stimulatory effect of acetylcholine on muscarinic receptors (M receptors) and nicotinic receptors (N receptors) in the brain; therefore, it can better antagonize the central poisoning symptoms caused by organophosphorus poisons (pesticides), such as convulsions, central respiratory and circulatory failure, and irritability. At the same time, it also has a strong blocking effect on the stimulatory effect of acetylcholine on M receptors in the periphery; therefore, it can better antagonize the muscarinic poisoning symptoms caused by organophosphorus poisons (pesticides), such as bronchial smooth muscle spasm and increased secretion, sweating, dilation, miosis, and gastrointestinal smooth muscle spasm or contraction. It can also increase respiratory rate and respiratory flow, but since this product has no obvious effect on M2 receptors, it has no obvious effect on heart rate; it has no obvious antagonistic effect on peripheral N receptors.

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151937-76-7 9

Appearance

This product is a colorless clear liquid.

Indication

Used for emergency treatment of organophosphorus poisoning (pesticide) and maintenance of atropine in the late stage of poisoning or after cholinesterase (ChE) aging.

Usage and Dosage

Intramuscular injection, the first dose is selected according to the degree of poisoning. Mild poisoning 1-2 mg, if necessary, combined with 500-750 mg of pralidoxime. Moderate poisoning 2-4 mg, combined with 750-1500 mg of pralidoxime. Severe poisoning 4-6 mg, combined with 1500-2500 mg of pralidoxime. 45 minutes after the first medication, if there are only muscarinic symptoms such as nausea, vomiting, sweating, and salivation, only 1-2 mg of penehyclidine hydrochloride should be used; if there are only nicotinic symptoms such as muscle tremors and muscle weakness or ChE activity is less than 50%, only 1000 mg of pralidoxime should be used. If there is no pralidoxime, pralidoxime can be used instead. If the above symptoms are present, sometimes repeat the first half dose of penehyclidine hydrochloride and pralidoxime 1-2 times. In the late stage of poisoning or after ChE aging, 1-2 mg of penehyclidine hydrochloride can be used to maintain atropine, with an interval of 8-12 hours each time.

Adverse Reactions

When the dosage is appropriate, it is often accompanied by dry mouth, flushed face and dry skin. If the dosage is too large, dizziness, urinary retention, delirium and fever may occur. Generally, no special treatment is required and the symptoms will be relieved after stopping the drug.

Precautions

Not suitable for patients with glaucoma

Special Population Medication

Precautions for children: Not yet clear. Precautions for pregnancy and lactation: Not yet clear.

Drug Interactions

When this product is used in combination with other anticholinergic drugs (atropine, scopolamine and anisodamine, etc.), it has a synergistic effect and the dosage should be reduced as appropriate.

Storage

Sealed storage for five years

Packaging Specification

1ml:1mg

Validity Period

60 months

Manufacturer

Avanc Pharmaceutical Co., Ltd.

  • Founded in:

    2002-01-28
  • Address:

    No. 55, Songshan Street, Taihe District, Jinzhou City, Liaoning Province
  • Tax NO.:

    91210700734224812X
  • Registered Funds:

    660 million yuan
  • Website:

  • Email:

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