MindMap Gallery Pharmacology Chapter 15, 16, 17 Sedative-hypnosis, anticonvulsants, epilepsy drugs, Parkinson's disease
This is a mind map about Chapters 15, 16, and 17 of Pharmacology, which mainly includes sedative-hypnosis, anticonvulsants, epilepsy drugs, Parkinson's drugs, etc.
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This is a mind map about bacteria, and its main contents include: overview, morphology, types, structure, reproduction, distribution, application, and expansion. The summary is comprehensive and meticulous, suitable as review materials.
This is a mind map about plant asexual reproduction, and its main contents include: concept, spore reproduction, vegetative reproduction, tissue culture, and buds. The summary is comprehensive and meticulous, suitable as review materials.
This is a mind map about the reproductive development of animals, and its main contents include: insects, frogs, birds, sexual reproduction, and asexual reproduction. The summary is comprehensive and meticulous, suitable as review materials.
sedative hypnotics
benzodiazepines
Rapid and complete absorption after oral administration
Diazepam is highly lipid-soluble, easily passes through the blood-brain barrier and placental barrier, and is metabolized in the liver
Pharmacological effects and clinical applications
No anesthetic effect
anti-anxiety
Anti-anxiety in small doses
Achieved through the action of BZ receptors in the limbic system
Calm and sleep
Suitable for patients who wake up easily and early and cannot fall asleep after waking up
Mainly prolongs the second phase of non-rapid eye movement sleep
Anticonvulsant, antiepileptic
central muscle relaxation
mechanism
Enhance GABA effect
GABA is a macromolecular complex that acts as a ligand-gated CI channel on neuronal membranes.
GABA acts on GABA receptors to increase the permeability of the cell membrane to Cl-. A large amount of Cl- enters the cell membrane, causing membrane hyperification and reducing neuronal excitability.
Benzodiazepines bind to the BZ receptor on the GABA receptor complex, which can induce conformational changes in the receptor, promote the binding of GABA to GABA receptors, increase the frequency of C1~ channel opening, increase Cl inflow, and produce central inhibition. effect.
Adverse reactions
The most common adverse reactions are drowsiness, dizziness, fatigue and memory loss.
Too fast intravenous injection, respiratory depression and circulatory depression
Dependence and addiction after long-term use, rebound and withdrawal after discontinuation
Flumazenil can be used for differential diagnosis and rescue in overdose poisoning of benzodiazepines.
Flumazenil is an antagonist of the benzodiazepine binding site and specifically and competitively antagonizes the specific binding sites of benzodiazepine derivatives and GABA receptors.
barbiturates
It is a pharmaceutical enzyme inducer, and long-term use may cause a decrease in efficacy.
Calm and sleep
Change normal sleep patterns, shorten rapid eye movement sleep, and cause non-physiological sleep. After long-term use and discontinuation of the drug, the REMS sleep phase may be prolonged in a rebound manner, accompanied by excessive dreams.
anticonvulsant
anaesthetization
Thiopental sodium can be used for intravenous anesthesia
Adverse reactions
Moderate doses can inhibit the respiratory center, and are contraindicated in patients with severe pulmonary insufficiency or head injury resulting in respiratory depression.
Long-term dependence, leading to addiction
In case of poisoning, sodium bicarbonate can be used to promote urinary excretion.
New non-benzodiazepine sedative-hypnotics
Zolpidem
Selectively stimulates GABA, and the BZ receptor on the receptor regulates chloride channels
For sedation and hypnosis only
It has less interference with normal sleep phases, can shorten sleep latency, reduce the number of awakenings and extend the total sleep time.
Zopiclone
fast and swift
Help patients fall asleep quickly and maintain adequate sleep depth,
Less residual effects and hangovers. There is no obvious resistance or rebound after long-term use.
Suitable for difficulty falling asleep
Zaleplon
It is suitable for short-term treatment of adults who have difficulty falling asleep, and can effectively shorten the time it takes to fall asleep.
other
Chloral hydrate
Strong gastric mucosal irritation
antiepileptic drugs
Epilepsy classification and medication
localized seizures
Simple localized seizure (focal type)
carbamazepine
Complex focal seizures (psychomotor seizures)
carbamazepine
Broad spectrum epilepsy drugs
One of the first-choice drugs for simple localized seizures and grand mal seizures
It can also treat diabetes insipidus and has a strong antidepressant effect, and is effective in mania and depression that are ineffective against lithium salts.
Generalized seizures
Absence seizures (petit mal)
ethosuximide
Adverse reactions
gastrointestinal reactions
granulocytopenia
spasmodic seizure
Clonazepam
Tonic-convulsive seizures (grand mal seizures)
Phenytoin
The drug of choice for grand mal and localized seizures
Adverse reactions
Gingival hyperplasia
status epilepticus
diazepam
Major seizures combined with petit mal seizures
sodium valproate
Broad spectrum epilepsy drugs
Hepatotoxic
anticonvulsants
Magnesium sulfate
Pharmacological effects
Mg participates in the regulation of various enzyme activities and plays an important role in nerve impulse transmission and maintenance of neuromuscular stress.
Mg2 and Ca2 have similar chemical properties and can specifically compete for Ca* binding sites and antagonize the effects of Ca*.
Relax skeletal muscle, cardiac muscle, and vascular smooth muscle, thereby exerting muscle relaxant and antihypertensive effects.
Clinical application
injection
Mainly used to relieve eclampsia, tetanus and other convulsions
Also commonly used in hypertensive crisis
Oral administration has cathartic and choleretic effects
External hot compress can reduce inflammation and reduce swelling
Adverse reactions
Excessive blood magnesium can inhibit the respiratory center and vasomotor center of the medulla oblongata, causing respiratory depression, sudden drop in blood pressure and cardiac arrest.
The safe range for injections is very narrow
Symptoms of poisoning may occur if the concentration exceeds 3.5mmol/L.
Loss of tendon reflexes is a sign of respiratory depression
In case of poisoning, artificial respiration should be performed immediately, and calcium chloride and calcium gluconate should be slowly injected to counteract the poisoning.
antiparkinsonian drugs
antiparkinsonian drugs
parkinson
Degenerative diseases of the central nervous system with progressive extrapyramidal dysfunction
symptom
Rest tremor
Muscle stiffness,
slow movement,
Impaired postural reflexes,
Severe patients are accompanied by memory impairment and dementia
Dopamine-like drugs
Dopamine prodrug: levodopa (L-DOPA)
internal processes
After oral administration, most of it is decarboxylated into dopamine by L-aromatic amino acid deenzyme (AADC) in the intestinal mucosa, liver and other peripheral tissues.
Only dopamine formed in the brain through the blood-brain barrier can produce anti-Parkinsonian effects
Only about 1% of L-DOPA can enter the central nervous system to exert therapeutic effects.
L-DOPA is the precursor of dopamine. After passing through the blood-brain barrier, it supplements the lack of dopamine in the striatum and exerts a therapeutic effect.
Dopamine cannot be used to treat PD because it cannot easily cross the blood-brain barrier.
Clinical application
Good effect on mild disease and young patients
Good effect on muscle stiffness and movement difficulties, but poor effect on muscle tremor
Improve muscle stiffness and movement difficulties first, then improve muscle tremors
works slowly
Adverse reactions
early response
gastrointestinal reactions
L-DOPA is deformed into DA in the peripheral and central centers, respectively, directly stimulating the gastrointestinal tract and stimulating the D2 receptors in the medulla bulbar emetic chemoreceptor area.
Application of AADC inhibitors can significantly reduce
orthostatic hypotension
DA acts on sympathetic nerves to feedbackly inhibit NA release
DA acts on DA receptors in the arterial wall to relax blood vessels
long term reaction
hyperkinesia
Due to overstimulation of dopamine receptors after taking large amounts of LDOPA
"On-off reaction"
Symptoms fluctuate
insanity
Can be treated with clozapine
medicine interactions
Vitamin B6
The prosthetic group of dopa decarboxylase can accelerate the peripheral decarboxylation of levodopa into DA, reducing the efficacy.
antipsychotic drugs
Blocks central DA receptors, reduces efficacy, and causes drug-induced PD
Lishepin
Depleting DA in the nigrostriatal body reduces efficacy
Not suitable for use with L-DOPA
Levodopa synergists: amino acid decarboxylate (AADC) inhibitors
The detachment of L-DOPA in the periphery is inhibited and the amount of L-DOPA entering the central nervous system is increased.
The dosage is reduced, the adverse reactions are reduced, and the symptom fluctuations are reduced.
Cannot pass the blood-brain barrier and can only inhibit peripheral AADC when combined with L-DOPA
It can only reduce the generation of DA in the periphery
The compound preparation composed of L-DOPA is called Xinningmei
Dopamine receptor agonist: bromocriptine
Activates D2 receptors in the substantia nigra-striatal pathway
Clinical application
Parkinson's Disease
Treatment of galactorrhea-amenorrhea syndrome
Inhibit prolactin secretion
acromegaly
Inhibit growth hormone secretion
Dopamine-releasing drugs: amantadine
Promote L-DOPA to enter the cerebral circulation, increase DA synthesis, release and reduce DA reuptake; it may also be related to antagonizing NMDA-R
Better than anticholinergics, not as good as L-DOPA
Clinical application
shaking paralysis
Antiviral
anticholinergics
trihexyphenidyl
Attenuation of ACh effects in the nigrostriatal pathway by antagonizing cholinergic receptors
Better anti-tremor effect
Be applicable:
① Patients with mild symptoms;
② Those who cannot tolerate or are prohibited from taking L-dopa;
③ Effective against extrapyramidal reactions caused by antipsychotic drugs;
④ Use in combination with L-dopa.
Drugs to treat Alzheimer's disease
Alzheimer's disease
A highly age-related degenerative disease of the central nervous system characterized by progressive cognitive impairment and memory impairment.
cholinesterase (AChE) inhibitors
Donepezil
Inhibit cholinesterase (AChE) to increase ACh levels
The dose is small, the toxicity is low, and the price is low. First choice
NMDA receptor non-competitive antagonists
memantine
Excitatory amino acid receptor antagonist
For the treatment of moderate to severe Alzheimer's type dementia