1、The active ingredients： penehyclidine hydrochloride.
Chemical name: 3-(2-cyclopentyl-2-hydroxy-2 phenylethoxy) quinine naphthenic hydrochloride
Chemical structural ：
Molecular formula: C20H29NO2·HClMolecular weight: 351.922
2、Excipients: water for injection
This product is colorless clear liquid.
【Indications and usage】
This product is a selective anticholine drug.
1.It is administrated before anesthesia to inhibit secretion of salivary gland and airway gland.
2.It is used for he first aid treatment of organophosphorus poisoning (pesticide) and the maintenance of atropinization after the late period of poisoning or cholinesterase (ChE) aging.
【Usage and dosage】
1.For adult indications dosing at 0.5mg ~ 1mg half an hour before anesthesia.
2.Treating organophosphorus (pesticide) poisoning:
Mild poisoning: 1 ~ 2mg (unit), and combined with 500 ~ 750mg pralidoxime chloride if necessary.
Moderate poisoning: 2 ~ 4mg (unit), combined with 750 ~ 1500mg pralidoxime chloride.
Severe poisoning: 4 ~ 6mg (unit), combined with 1, 500mg ~ 2, 500mg pralidoxime chloride.
45 minutes after the first dose, penehyclidine hydrochloride should be administered at doses of 1 ~ 2 mg if patients experience only muscarinic symptoms such as nausea, vomiting, sweating and salivation. If emergence of the nicotinoid symptoms, such as muscle fibrillation and muscle weakness, or the activity of ChE (cholinesterase) in the whole blood less than 50%, 1000mg of pralidoxime chlorideshould be administeredand pralidoxime chloride could be replaced by pralidoxime. If patients experience the above symptoms Penehyclidine Hydrochloride and pralidoxime chloride should be administered at half of first dose 1-2 times. Atropinization can be maintained with 1-2mg penehyclidine hydrochloride after poisoning or ChE aging with intervals of 8-12 hours.
【Adverse Reactions】 The most common side effects of penehyclidine hydrochloride include dry mouth, red face and dry skin, etc. Large dosage can lead to dizziness, urine retention, delirium and increased body temperature. Generally special treatment is not required the symptoms could be relieved after discontinue drug.
Penehyclidine Hydrochloride is contraindicated in patients with Glaucoma patients
1.This product has no obvious effect on the heart (M2 receptor), so it has no obvious effect on the heart rate.
2.When this product is used for the treatment of organophosphorus poisoning (pesticide), it should not be judged as "atropinization" by the rapid heartbeat, but should be judged by the symptoms such as dry mouth and disappearance of sweat or dry skin.
3.Due to the inhibition of respiratory gland secretion, so for patients with serious respiratory tract infection with less or viscous sputum, this product should be used carefully .
4.Atropine should not be used when the heartbeat is not lower than normal.
5.The elimination half-life of this product is long. The interval time of each administration should not be too short, and the dose should not be too large.
【Use in pregnant and lactating women】
Safety and effectiveness in pregnant and lactating women have not been established.
【Use in pediatric patients】
Safety and effectiveness in pediatric patients have not been established.
【Use in geriatric patients】
This product could aggravate dysuria in geriatric patients with prostatic hypertrophy, and should be observed carefully during treatment.
When used in combination with other anticholinergic drugs (atropine, scopolamine, anisodamine, etc.), the dosage should be reduced as appropriate.
When overdosing, dizziness, dry mouth, blurred vision, delirium, urinary retention, elevated body temperature, hallucinations, disorientation and coma may occur; Generally special treatment is not required, the symptoms could be relieved after discontinue drug; When necessary treat based on symptoms and administrate of sedatives.
【 Pharmacology and Toxicology 】
Pharmacological effects: This product is new selective anticholinergic drug and it can f bind with M and N choline receptorsto inhibit the muscarinic actions of acetylcholine on structures innervated by postganglionic cholinergic nerves，and on smooth muscles，which respond to endogenous acetylchololine. This drugs can penetrate the blood-brain barrier, so it has strong and comprehensive central and peripheral anticholine effects.This product has obvious selectivity for M receptors and it mainly acts on M1 and M3 receptors, but has weak or no obvious effect on M2 receptors. It does not block the function of M2 receptors in presynaptic membrane to regulate the release of Ach from nerve endings and stabilize heart rate. At the same time, this product also has certain effects on N1 and N2 receptors.This product can better resist the effect of acetylcholine, relieve the smooth muscle spasm caused by the high excitement of vagus nerve caused by the large release of acetylcholine in the body; Relieve acute microcirculation dysfunction caused by continuous spasm of pulmonary and cerebral microvessels. At the same time, it can antagonize the central poisoning symptoms caused by organophosphorus poisoning (pesticide poisoning), such as convulsion, central respiratory failure and restlessness. It can also strongly antagonize muscarinic poisoning symptoms caused by organophosphate poisoning (pesticide poisoning), such as bronchial smooth muscle spasm and secretion increase, sweating, salivation, pupil contraction and gastrointestinal smooth muscle spasm and contraction. It also increases breathing rate and flow.
The results of animal experiments showed that both mice and rabbits showed stronger resistance to saliva secretion than atropine, and the ED50 of rabbits was only 0.03mg/kg, about 17 times stronger than atropine.This product can significantly inhibit the secretion of saliva and tracheal mucus in mice (p<0.001), and the effect is stronger than that of atropine injection.After the injection, the relaxation of spastic contraction of stomach, small intestine, colon and gallbladder in anesthetized and awake rabbits was stronger than atropine (p<0.05), and the relaxation of spastic contraction of bladder was significantly stronger than atropine (p<0.01).
Toxicology research: long-term toxicity test showed that: 0.68, 3.38, 13.50 mg/kg (equivalent to 40, 199, 794 people of clinical dosage of often times) intramuscular injection in rats, respectively, this article 0.015, 0.9 mg/kg (equivalent to 0.9 of people often use clinical, 53 times) intramuscular injection respectively in dogs, 1 times a day for 12 weeks, besides some common fight choline reaction, no other abnormal; General reproductive toxicity test showed that: 2.5, 12.5, 62.5 PPM (equivalent to 15, 75, 375 of people dosage) oral in male mice respectively for 60 days in a row, females for 14 consecutive days, in addition to the high dose group have certain toxicity in mice, the occurrence of this product in mice gametes, impregnation, delivery and
postnatal F1 seed rat growth did not see the obvious effect; The mutagenesis test was negative. Teratogenic effects and embryo toxicity were not observed within 300 times the human dosage.
After intramuscular injection of 1mg penehyclidine hydrochloride into healthy adults, penehyclidine hydrochloride could be detected in the blood after 2 minutes, and the blood concentration reached the peak at about 0.56 hours, the peak concentration was about 13.20 g/L, and the elimination half-life was about 10.35 hours. Animal experiments showed that the product was distributed to all tissues of the body, including submandibular gland, lung, spleen and intestine.The product is mainly excreted by urine and bile, and the 24-hour total excretion is about 94.17% of the dosage.
【Storage】Sealed storage and it should be used within the expiry date.
【Expiry Date】60 months
【Approval Number】 H20020606