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Chapter XIX sedative hypnoticsRequirements of Outline
Benzodiazepine pharmacological effects of drugs, mechanism, clinical applications and adverse reaction
Diazepam, estazolam, triazolam characteristics of the pharmacological effects of
The pharmacological effects of barbiturates, clinical applications and adverse reaction
Chloral hydrate, methaqualone characteristics of the pharmacological effects of1.4-benzo-derivatives of nitrous
Pharmacological effects
1. Anxiolytic effects of regulation and selective inhibition of limbic system on emotional reactions.
2. Sedative and hypnotic effects:
Features (1) shortening the fourth non-rapid eye movement sleep rapid eye movement sleep relatively little effect
(2) the high therapeutic index, little effect on respiration
(3) No induction of hepatic drug metabolizing enzyme
(4) dependence, withdrawal symptoms less70% of the dreams in this period, active dreams, sometimes nightmares occur
3. Anticonvulsant effect of a strong antiepileptic effect. All kinds of convulsions. Diazepam is the first choice for status epilepticus.
4. Central role of clinical muscle relaxation for the brain or spinal cord injury and muscle strain caused by muscle rigidity such as muscle spasticity, in order to reduce muscle spasm and pain.And drugs acting on different parts of the brain -aminobutyric acid type A (GABA) receptors are closely related.3. Anticonvulsant: a variety of seizure
Epilepsy: iv: the first choice for status epilepticusHigher dose: ataxia, coma, respiratory depression, alcohol inhibited the increase at the same time.
Long-term use: tolerance, dependence (but lesser)
Note:
Caution: The liver, kidney and respiratory dysfunction, elderly patients, glaucoma, myasthenia gravis who, driver, operator of high-altitude operations and machineOral: fast, fully
Intramuscular injection: slow, irregular (fluid pH to precipitate)
Intravenous injection: the role of fast, short (fat-soluble large)
2. Plasma protein binding rate: 99%
3. The transformation of hepatic drug metabolizing enzyme, active metabolites, long-term
Pharmacological effects
1. Anxiolytic effects: selective high and low dose can inhibit the limbic system of the hippocampus and amygdala neurons, the issuance and delivery of electrical activity
2. Hypnosis: to extend light sleep, slow wave sleep was significantly shorter
3. Anticonvulsant, antiepileptic: drug of choice for status epilepticus
4. Muscle relaxation: does not affect the normal activities
Adverse reactions
Common are drowsiness, dizziness, weakness, followed by memory loss, headaches, ataxia and so on.
Rapid intravenous injection can cause apnea or cardiac arrest.
Pregnant and lactating women should not be applied.
Other benzodiazepine drugs (diazepam ~, ~ alprazolam)Triazolam: quick, short-acting, powerfulFlurazepam1.R1, R2, R3 substituents can be divided into:
Long: barbiturates, phenobarbital
In effect: pentobarbital, amobarbital2.C5 substituents to benzene ring replaced by a strong antiepileptic effect.
3.C2 S on O is replaced by increased fat-soluble, quick effect, maintain a short time
Pharmacokinetics
1. Are easily absorbed oral or intramuscular
2. Thiopental highest fat-soluble
3. Phenobarbital less fat-soluble
Pharmacological effects and clinical application
1. Sedation, hypnosis: reduce REM sleep
2. Anticonvulsant: hypnotic doses of barbiturates than to protect the animals tolerated 10 times the lethal dose of strychnine and pentylenetetrazol seizure and from death. For a variety of clinical seizures, grand mal epilepsy.
3. Before the administration of anesthesia and anesthesia for minor surgery or endoscopy anesthesia.
4. Enhance the central role of inhibitors of other drugs can increase central inhibition.
Adverse reactions
Consequential effects, tolerance, dependence, respiratory depression, liver drug metabolizing enzyme induction10 times the hypnotic dose of oral can cause moderate poisoning
2. Rescue:1. Sleepiness, ataxia and other side effects less
2. On the rapid eye movement sleep phase of a small decrease occurred nightmare
3. Discontinuation was mild after the compensatory6. None of liver drug metabolizing enzyme inductionChloral hydrate
Features:
1. Does not reduce the rapid eye movement sleep, no hangover aftermath effect.
2. Can be used in intractable insomnia or other sleep medication effects of poor patients.
3. A variety of inspection and before the operation, from the sedation.
4. Anticonvulsant effect of large dose.
5. Have a stimulating effect on the gastrointestinal tract.
Methaqualone
1. In addition to sedative and hypnotic effects, there are anticonvulsant, local anesthetic, antitussive and anti-histamine effect.
2. Clinical mainly used for neurasthenia, insomnia, before anesthesia administration.
X-type
1. Diazepam and phenobarbital interaction with (ABCE)D. anti-shock2. Diazepam Which of the following characteristics without (E)
A. wider range of oral safety
B. The role is indirectly achieved by increasing GABA function
C. long-term use can produce tolerance
D. Plasma protein binding rate of 99%
E. is a typical enzyme inducer drug
No. 21190102 Q & A
3. On the role of the characteristics of diazepam, Which is wrong (D)
A. less than the amount of time that is anti-anxiety sedative effect
B. Influence of small rapid eye movement sleep
C. inhibitors enhance the role of other central
D. increase the dose of anesthesia can cause
E. has a central role in muscle relaxation4. Diazepam adverse reaction (ABC)
A. drowsiness, dizziness, fatigue
B. Large doses can produce ataxia
C. long-term use can produce tolerance, dependenceB-
A. diazepam, phenobarbital B. C. D. triazolam thiopental E. chloral hydrate
5. Quick, short-acting benzodiazepine drugs (D)
No. 21190105 Q & A
6. Ultrashort barbiturates efficiency (C)
No. 21190106 Q & A
7. Mainly from the renal excretion of drug prototypes (B)
No. 21190107 Q & A
8. Drug of choice for status epilepticus (A)
No. 21190108 Q & A
9. Oral, although easy to absorb, but there is a strong irritant of the stomach (E)10. Which of the following phenobarbital has no effect (C)D. anticonvulsant11. On barbiturates, the correct description are: (ABCD)
A. universal central inhibition
B. toxic dose can cause respiratory paralysis and death central nervous system
C. Phenobarbital has strong anticonvulsant and antiepileptic effects
D. Barbiturates easy to produce tolerance
E. barbiturates inhibited the enzyme activity of liver drug
No. 21190111 Q & A
12. The following description of the right are: (BCE)
A. Barbiturates easily absorbed orally, intramuscular injection of hard to absorb
B. The fat-soluble highest thiopental
C. Phenobarbital mainly excreted by the kidneys prototype
D. The pH value of urine excretion of phenobarbital in small
E. barbiturates extend the opening hours of Cl-channels
No. 21190112 Q & A
13. Barbiturate poisoning can take measures: (ABCDE)
A. artificial respiration
B. Application of central stimulant
C. intravenous infusion of sodium bicarbonateChapter antiepileptic drugs and of Outline
Phenytoin, carbamazepine, sodium valproate pharmacological effects, clinical applications and adverse reaction
Ethosuximide, phenobarbital, flutter meters ketone, diazepam, clonazepam clinical application
The pharmacological effects of magnesium sulfate and clinical applicationFirst, the epilepsy
Epilepsy: brain lesions localized excessive neuronal excitability, resulting in paroxysmal discharge appears to sparound the brain dysfunction syndrome transient.Second, according to the symptoms can be divided into:Third, antiepileptic drugs
There are many antiepileptic mechanism of action, but can be summed up in two ways, namely, excessive discharge of neurons inhibit the lesion, or acting on normal nerve tissue around the lesion, inhibit the proliferation of abnormal discharge.
Biochemical mechanisms of antiepileptic drugs:
1. Stabilize cell membrane.
2. Promote the GABAA receptor-Cl-channel function.
3. Other: block glutamate receptors. Inhibitory neuron function.Absorption: Oral absorption is slow, irregular, and plasma protein binding rate of about 90%
Elimination: The inactivation of liver drug metabolic enzyme, large individual differences1. Anticonvulsant:
Stronger, one large attack first choice, but can increase a small attack, the slow onset (6 to 10 days of the effective concentration)
Mechanisms: inhibition of Na, Ca2
Influx, K outflow, enhanced brain GABA function
2. Treatment of central and peripheral neuropathic pain: The membrane stabilizing effects.1. Local stimulation of oral, intramuscular injection, intravenous infusion, intravenous, gingival hyperplasia, the incidence rate of 20%
2. Nervous system response nystagmus, ataxia, dizziness, diplopia
3. Hematopoietic system - folate deficiency megaloblastic anemia, aplastic
Treatment: folinic CF
4. Allergic skin rash, agranulocytosis, aplastic anemia, liver damage
5. Other hirsutism (women), breast enlargement (men), low blood calcium, swollen lymph nodes1. Reduce the excitability of cells in lesions;
2. Enhance the excitement of normal tissue around the lesion threshold
Pharmacological effects
1. Acting on GABA receptors in the membrane, after highlighting, so that Cl-channels open longer, resulting in nerve cell membrane hyperpolarization, reducing its excitability;
2. Role in highlighting the membrane and reduce the prominence of Ca2 permeability of the membrane to reduce the Ca2-dependent neurotransmitter release.
Clinical
For the prevention and treatment of epilepsy grand mal status epilepticus, with rapid onset, better efficacy, longer half-life, low toxicity, low cost, the big attack, limited attack better effect, but increased a small attack.1. Psychomotor seizures antiepileptic drug of choice, especially for pediatric patients, the effect of small seizures worse.
2. Central pain its more effective than phenytoin.
3. Manic depression, their side effects than lithium salt is small and good effect.
4. Neurogenic diabetes insipidus by promoting the secretion of antidiuretic hormone function.The most common are diplopia and ataxia. Other side effects include dizziness, nausea, and vomiting.
(D) Sodium valproate
1. Broad-spectrum antiepileptic drugs
2. Brain GABA transaminase inhibitor
3. The best effect of small seizures, petit mal seizures preferred major mergerFirst choice of small attack preventionAnd has anticonvulsant and antiepileptic effect, commonly used in clinical treatment of epilepsy drugs diazepam, nitrazepam and clonazepam.Limitations attack*



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