地西泮片（安定）（DiazepamTablets（Valium））

地西泮片(安定)（Diazepam Tablets (Valium)）Diazepam Tablets (Valium) Diazepam Tablets
(psychotropic drugs)
[indications]
1., mainly used for anxiety, sedation and hypnosis, but also for antiepileptic and anticonvulsant;
2., relieve inflammatory reflex muscle spasm;
3. for the treatment of panic disorder;
4. muscle tension headache;
5. can be treated for familial, senile, and idiopathic tremors;
6. can be used for anesthesia, money, medication.
[usage and dosage]
Adult dose:
Anti anxiety, once a 2.5-10mg, 2-4 times a day;
Calm down, 2.5-5mg at a time, 3 times a day;
Hypnosis, 5-10mg, bedtime clothes;
Acute alcohol withdrawal, once a day, 10mg, 3-4 times a day,
and then reduced to 5mg once a day, 3-4 times a day.
Pediatric routine dose:
The following 6 months of no more than 6 months, a 1-2.5mg or 40-200ug/kg according to the weight or body surface area 1.17-6mg/m2, 3-4 times a day, according to the amount of increase or decrease proportionally, the maximum dose is less than 10mg.
[adverse effects]
1. common adverse reactions: lethargy, dizziness, weakness, etc., large doses can have ataxia, tremor.
2. rare skin rashes and decreased white blood cells.
3. individual patients were excited, multilingual, sleep disorders, and even hallucinations. These symptoms soon disappear after withdrawal.
4. long-term continuous use of drugs can produce dependence and addiction, withdrawal may occur withdrawal symptoms, showing excitement or depression.
[contraindication] pregnant women, pregnant women and newborns are prohibited.
[matters needing attention]
1. allergic to benzene, two, or nitrogen, may be allergic to
this medicine.
2., liver and kidney function impairment can prolong the half-life of this medicine.
3. sudden withdrawal of epilepsy can cause epileptic status.
4., severe mental depression can aggravate the condition, and even suicidal tendencies, preventive measures should be taken.
5., avoid long-term use of large and addictive, such as long-term use should be gradually reduced, it should not be stopped.
6., the amount of tolerance of this drug is small, the initial dosage should be small.
Be careful with the following:
1. severe acute alcoholism may aggravate the central nervous system inhibition.
2. severe myasthenia gravis, the condition may be aggravated.
3. acute or latent attack of angle closure glaucoma can be aggravated by the anticholinergic effect of this product.
4. low blood protein, can lead to drowsiness and difficult to wake up.
5. ADHD can have abnormal reaction.
6. severe chronic obstructive pulmonary disease may aggravate respiratory failure.
7., surgical or long-term bedridden patients, cough response can be suppressed.
8., drug abuse and addicts.
[pregnant women and lactating women]
1. within three months of pregnancy, this medicine has increased the risk of fetal teratogenic, long-term use of pregnant women can be addictive, so that the newborn showing withdrawal symptoms, irritability, tremor, vomiting, diarrhea;
Late pregnancy medication affects neonatal central nervous activity.
Medication before delivery and at birth may lead to weaker muscle tension in neonates and should be disabled.
2., this product can be secreted into the milk, breast-feeding women should avoid using.
[children medication] central nervous system of children is very sensitive to this medicine, should be carefully administered.
[] the elderly elderly patients are more sensitive to the drug
dosage should be reduced.
[drug interaction]
1. combined with central depressant can increase respiratory depression.
2., addiction increases the risk of addiction when used in combination with other addictive drugs.
3., with wine and general anesthetics, clonidine, analgesics, phenothiazine, monoamine oxidase, A inhibitors and tricyclic antidepressants, can be synergistic with each other, should adjust the dosage.
4., combined with antihypertensive drugs and diuretic antihypertensive drugs, can increase the role of blood pressure.
5., the combination of propranolol and cimetidine drug clearance slowed, plasma half-life.
6., with the use of paracetamol, because the latter slows down the metabolism, the need to adjust the amount of paracetamol.
7., when combined with levodopa, can reduce the efficacy of the latter.
8., combined with rifampin, increase the elimination of this product, lower blood concentration.
9. isoniazid inhibits the elimination of this product, resulting in increased serum concentration.
Ten
The combination of digoxin and digoxin can increase the blood concentration of digoxin and cause poisoning.
[drug overdose] persistent psychosis, severe lethargy, jitter, confusion of language, faltering heartbeat, shortness of breath, shortness of breath, difficulty, and severe fatigue. Excessive or poisoning should be symptomatic treatment, including supportive therapy to promote vomiting and respiratory cycle, benzene two nitrogen Zhuo receptor antagonist flumazenil (flumazenil) can be used for the drug overdose rescue and diagnosis. When intoxication occurs, abnormal use of barbiturates should not be applied.
[pharmacology and toxicology] this product is long acting benzene two nitrogen Zhuo class medicine. Benzene two nitrogen drugs are central nervous system inhibitors, can cause different parts of the central nervous system inhibition, with the increase in dosage, clinical manifestations can be mild sedation, hypnosis, or even coma. The site of action and mechanism of this kind of medicine has not been fully elucidated, that can enhance or facilitatory r- aminobutyric acid (GABA) inhibitory neurotransmitter role of GABA in benzene two nitrogen Zhuo receptor interaction, mainly in the central nervous system in various parts, the inhibition of outburst before and after outburst. The drug is an agonist of the benzene two receptor, and the benzene two nitrogen receptor is a
functional supramolecular (supramolecular) functional unit, also known as the two component of the benzene, the -GABA receptor, and the pro chloride complex. The receptor complex is located in the nerve cell membrane and regulates the discharge of the cell, mainly from the threshold valve (gating) function of the chloride channel. The activation of GABA receptors leads to chloride channel development, the chloride ions flow through the nerve cell membrane, induced hyperpolarization of postsynaptic neurons, inhibiting neuronal discharge, the inhibition of translation in order to reduce neuronal excitability, reduce the next step depolarization in excitatory neurotransmitter. Increasing the frequency of chloride channel development for benzene two nitrogen compounds may be achieved by increasing the binding or facilitation of GABA with its receptor and by linking the GABA receptor with the chloride channel. Benzene, two, also acts on GABA dependent receptors.
(1) anti anxiety, sedative and hypnotic effect.
By stimulating the GABA receptor in the ascending reticular activating system, the inhibition of GABA in the central nervous system was enhanced, and the inhibition and occlusion of the cortical reticular formation after stimulated cortex and limbic arousal were enhanced. Molecular pharmacological studies suggest that reducing or antagonizing the synthesis of GABA, the sedative and hypnotic effects of this drug decrease, such as increasing its concentration, can enhance the hypnotic effect of benzene two nitrogen drugs.
(2) forgetting effect.
Diazepam can interfere with the establishment of memory pathways at therapeutic doses, thereby affecting near memory.
(3) anticonvulsant effect.
It is possible to inhibit the spread of epileptic activity by inhibiting presynaptic foci in the cortex, thalamus, and limbic system, but it can not eliminate the abnormal activity of the lesion.
(4) skeletal muscle relaxation.
It mainly inhibits the efferent efferent pathway and single synaptic efferent pathway of spinal cord. Because of inhibiting neurotransmitters or blocking excitatory synaptic transmission, diazepam inhibits both synaptic and single synaptic reflexes. Benzene, two, or nitrogen, may also directly inhibit motor and neuromuscular function.
[pharmacokinetics]
Oral absorption is rapid and complete, with bioavailability of about 76%. 0.5-2 hours, the peak blood concentration, 4-10 days blood concentration reached steady state, T1/2 for 20-70 hours. Plasma protein binding rate was as high as 99%. Diazepam and its metabolites in high fat solubility, easy to penetrate the blood-brain barrier; through the placenta, can be secreted into the milk, this product is mainly metabolized in the liver, metabolites nordiazepam and medroxyprogesterone diazepam, also have pharmacological activity in different degree, 30-100
hours nordiazepam can reach T1/2. This product has the enterohepatic circulation, long-term accumulation of drug. Metabolites can be trapped in the blood for days or even weeks, and are slowed down after withdrawal. Diazepam is excreted mainly through free or combined forms of metabolites.。