alias missoulin, pulvinone, mysolin, is a kind of odorless white crystalline powder, slightly bitter taste, no acid. Chemical name: 5-ethyl-5-phenyl-dihydro-4,6 (1H, 5H) - pyrimidine Dione, molecular formula: C12H14N2O2, molecular weight: 325.4242, melting point: 281~282 ℃, slightly bitter taste, no acid, slightly soluble in ethanol, almost insoluble in water, acetone or benzene. Promethasone is an antiepileptic drug. Clinically, it is mainly used for the treatment of tonic clonic seizures (Grand seizures), simple partial seizures and complex partial seizures with single drug or combined drugs. It is also used for the treatment of idiopathic tremor and senile tremor.
Primidone is an antiepileptic drug belonging to the isoprene class, with a molecular formula of C12H14N2O2 and a molecular weight of 218.26. It is a white or light yellow crystalline powder, odorless and odorless. Almost insoluble in water, but easily soluble in organic solvents such as chloroform, benzene, ethanol, and acetone. Under alkaline or acidic conditions, it is easily hydrolyzed. Relatively stable and not easily affected in dry air. Under the action of strong acids, bases, oxidants, ozone, ultraviolet radiation, etc., it is prone to decomposition and degradation. It has a certain℃of toxicity and can lead to poisoning and death. Relevant safety and protective measures need to be followed during preparation, storage, and use.
Pumidone, as a classic antiepileptic drug, is primarily used to control various types of epileptic seizures and achieve therapeutic goals by regulating neuronal excitability.
Pumidone is a first-line treatment for generalized tonic clonic seizures. Its mechanism of action involves reducing the excitatory effect of glutamate while enhancing the inhibitory effect of gamma aminobutyric acid (GABA), thereby inhibiting monosynaptic and polysynaptic transmission in the central nervous system. Clinical studies have shown that monotherapy can reduce the frequency of seizures by more than 50% in 60% -70% of patients, and the efficacy can be further improved to 80% when combined with medication.
is necessary to start with a small dose (50mg/day) and gradually titrate to an effective dose (250mg, 3 times a day) to reduce adverse reactions such as ataxia and dizziness.
For simple partial seizures (such as focal motor or sensory seizures) and complex partial seizures (accompanied by consciousness disorders), amiodarone effectively inhibits the spread of epileptic discharges by increasing the motor cortex electrical stimulation threshold. A randomized controlled trial involving 300 patients showed that monotherapy with amiodarone can reduce partial seizure frequency by 55% -65%, with better efficacy when combined with carbamazepine or sodium valproate. Attention should be paid to monitoring blood drug concentration (treatment range 5-12 μ g/mL) to avoid insufficient dosage or poisoning.
Children: The initial dose for patients under 8 years old is 50mg/day, taken before bedtime, gradually increasing to 125-250mg/day, divided into 3 doses; Children over 8 years old should adjust their dosage according to adult dosage.
Elderly individuals: Due to slowed metabolism, the initial dose should be halved (125mg/day), and cognitive function should be closely monitored to avoid exacerbating brain dysfunction.
Patients with liver and kidney dysfunction: The dosage should be adjusted according to the creatinine clearance rate, and it is contraindicated for those with severe liver dysfunction.
The efficacy of Pumidone in tremor control has been clinically validated, especially for idiopathic tremor and senile tremor.
For elderly patients with tremor, amiodarone can significantly improve their daily living abilities. A 12 week open label study showed that treatment with amiodarone (125-250mg/day) can shorten the completion time of actions such as eating and dressing by 20% -30% for patients. Attention should be paid to monitoring the blood pressure and gait stability of elderly patients to avoid the risk of falls.
is a second-line treatment for essential tremor, with a relief rate of 60% -70% for head and hand tremors. Its mechanism of action may be related to regulating the cerebellar thalamic cortical pathway. A double-blind crossover trial showed that amiodarone (250mg/day) can increase patients' writing speed by 30% and reduce tremor amplitude by 50%. Treatment should start with a small dose and gradually increase to an effective dose to avoid acute adverse reactions such as dizziness and nausea.
Although the indications of amiodarone mainly focus on epilepsy and tremors, its potential in the treatment of neuropathic pain and neurological symptoms is gradually being revealed.
Pumidone has a certain analgesic effect on trigeminal neuralgia by stabilizing neuronal membrane potential and reducing abnormal discharges. A small-scale clinical trial showed that the combination of amiodarone (250mg/day) and carbamazepine in the treatment of trigeminal neuralgia can reduce the frequency of pain attacks by 40%, but further verification of its long-term efficacy and safety is needed.
The sedative and anti anxiety effects of amiodarone stem from its regulation of GABA receptors. Clinical observations have found that some epilepsy patients have significantly reduced anxiety scores (such as HAM-A scale) after receiving treatment with amiodarone. However, its antidepressant effect still lacks large-scale clinical trials to support it, and it is currently not recommended for use as a first-line antidepressant drug.
Pumidone is often used in combination with other antiepileptic drugs or adjunctive medications to optimize treatment plans.
Sodium valproate can inhibit the metabolism of amiodarone, increasing its blood concentration by 30% -50%, thereby enhancing its antiepileptic efficacy. During combination therapy, the dose of amiodarone should be reduced by 25% -50%, and blood drug concentration should be closely monitored to avoid poisoning.
Carbamazepine can induce the metabolism of amiodarone and reduce its blood drug concentration. During combination therapy, it is necessary to increase the dose of amiodarone (about 20%) to maintain efficacy. Meanwhile, carbamazepine may exacerbate the neurotoxicity of amiodarone (such as ataxia) and requires regular assessment of neurological function.
Pumidone and phenobarbital both induce liver enzymes to accelerate metabolism, and their combined use may lead to a significant decrease in blood drug concentration and efficacy. In addition, the combination of the two may increase the risk of central nervous system depression, leading to respiratory depression or coma.
The use of Pumidone in special populations requires careful assessment of risks and benefits.
can pass through the placental barrier, increasing the risk of fetal abnormalities such as craniofacial abnormalities and nail dysplasia. Pregnant women should try to avoid using it as much as possible. If medication is necessary, vitamin K (10mg/day) should be supplemented in the last month of pregnancy to prevent neonatal bleeding. When lactating women use medication, their infants may experience central nervous system depression (such as drowsiness and sucking weakness), and it is necessary to weigh the pros and cons before deciding whether to discontinue the medication.
Patients with liver dysfunction may experience poisoning due to slow metabolism, which may lead to the accumulation of amiodarone and its metabolites (such as phenobarbital). Pumidone is contraindicated for individuals with severe liver dysfunction. Patients with renal insufficiency need to adjust their dosage according to creatinine clearance rate to avoid drug accumulation.
Pumidone may induce acute attacks of porphyria, manifested as abdominal pain, neurological and psychiatric symptoms, and photosensitivity. Patients with porphyria are prohibited from using amiodarone.
Brief description of production method: add ethyl acetate to sodium alcohol, reflux for half an hour, cool to room temperature, add diethyl phenylmalonate and thiourea, and add flow for 9h. Cool to 0 ℃, add ethanol, and drop hydrochloric acid at 0-5 ℃ to ph=3-3.5. Add zinc powder, raise the temperature to reflux, slowly add hydrochloric acid, and keep the solution containing 2-3% acid. After adding, keep the temperature for 3h. Filter while it is hot, and recover ethanol from the filtrate. Cool to 20 ℃, add water, filter, and wash the filter cake to get the finished product.
Pharmacology and toxicology: This product is an antiepileptic drug. The main metabolite in the body is phenobarbital, which plays a role together. In vitro electrophysiological experiments showed that it opened the chloride channels of nerve cells and hyperpolarized cells, similar to - Role of aminobutyric acid (GABA). At the therapeutic concentration, it can reduce the excitatory effect of glutamate and strengthen - The inhibitory effect of aminobutyric acid inhibits the single synaptic and multi synaptic transmission of the central nervous system, resulting in the decrease of the excitability of the whole nerve cell and the increase of the electric stimulation threshold of the motor cortex. Raising the seizure threshold can also inhibit the spread of epileptic discharges.
Pharmacokinetics: it is easily absorbed by oral administration. Tmax is 2.7 ~ 5.2h (adults) and 4 ~ 6h (children). The bioavailability is as high as 92%. It is widely distributed and can pass through the fetal chemicalbook disc. It is secreted in the milk. The VD is 0.64 ~ 0.72l/kg, and the plasma protein binding rate is low. T1/2 about 10h. Liver metabolism, kidney excretion.
high is an antiepileptic drug for nervous system disease such as epilepsy and tremor. Its molecular formula is C12H14N2O2, and its molecular weight is 218.25 g/mol. Its chemical name is 5-ethoxy-5-methyl-2,4-diazacyclohexanone.
The molecular structure of Primidone contains a five membered heterocycle (2,4-diazacyclohexanone ring), two methyl groups and one ethoxy group. In its molecular formula, "C" represents carbon, which plays a connecting role in the molecular structure of Primidone, while "H" represents hydrogen atom, thus maintaining molecular integrity. In addition, "N" represents a nitrogen atom, "O" represents an oxygen atom, and "E" represents an ethoxy group.
Primidone's molecular structure can be described by many methods, the most common of which is the use of linear and molecular orbital graphs. In a linear structure, each atom of the molecular formula is connected to form a molecular chain based on the bonding relationship between atoms in the molecule. The molecular orbital diagram shows the orbital interaction between carbon and nitrogen atoms and the distribution of electron cloud, thus revealing the chemical properties and reaction mode inside Primidone molecule.
In the molecular structure of Primidone, a double bond is formed between the nitrogen atom on the five membered heterocyclic ring and the adjacent carbon atom, while a single bond is formed between the other nitrogen atom and the carbon atom in the opposite position on the ring. The two methyl groups on the ring are connected to adjacent carbon atoms and tilt in the same direction. The ethoxy group is connected to a carbon atom on a five membered heterocyclic ring, and its adjacent oxygen atom forms a single bond with the carbon atom.
Because the molecular structure of Primidone contains several five membered heterocycles and carbon atomic groups, its chemical properties are complex and changeable. It can be metabolized through reactions such as hydrolysis, deacetylation, and oxidation, thereby exerting its effects in the body. At the same time, this drug also has certain toxic side effects, so it is necessary to strictly control its dosage and monitor its safety during use.
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1. Acidity and alkalinity
Primidone is a weakly alkaline compound with a pKa value of approximately 7.0-7.5. Under acidic conditions, Primidone is easily hydrolyzed and produces the main metabolites phenobarbital and phenylethylmalonamide (PEMA). Under alkaline conditions, Primidone is prone to extraction with sodium dodecyl sulfate ethanol to obtain its free alkaline state. In addition, Primidone can also undergo acid-base reactions with some drugs or components, affecting their absorption and metabolism.
2. Oxidation-reduction properties
Primidone itself is not prone to redox reactions. However, under the action of some oxidants, such as hydrogen peroxide, hydrogen peroxide, chromic acid, etc., Primidone is prone to oxidation reactions, generating corresponding oxidation products. In addition, under reducing conditions, Primidone is prone to hydrolysis reactions and generates phenobarbital and PEMA.
3. Esterification reaction
Primidone contains two carboxyl functional groups and a C-O-C linked ester group, making it prone to esterification reactions. Primidone can react with some alcohol compounds to generate corresponding Primidone esters, which may have anti epileptic activity.
4. Electrophile addition reaction
Primidone contains an unsaturated bond, so it can undergo electrophilic addition reaction reaction. Under the action of some electrophilic reagents, such as halogen, nitro, carboxyl, etc., Primidone is prone to addition reaction to generate corresponding addition products.
5. Amination reaction
Primidone contains an amino functional group, making it prone to amination reactions. Under the action of some amino reagents, such as ammonia, ethylenediamine, etc., Primidone is prone to undergo amination reactions, generating corresponding amination products.
6. Photochemical reaction
Primidone is vulnerable to ultraviolet radiation. In photochemical reaction, Primidone is prone to pyrolysis or wheel addition reaction to generate corresponding photochemical products.
In a word, Primidone is a compound with many chemical properties, such as acid-base, redox, esterification, electrophilic addition reaction, amination, photochemical reaction, etc. Special attention needs to be paid to safety and protective measures during preparation, storage, and use.
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