All patients taking tranquilizers must be warned that they may feel:
A- Anxious
B- Nauseated
C- Clumsy
D- Drowsy.
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Tranquilizers:
Heterogeneous group of substances that, according to the dose or the active substance it contains, triggers a calming, anxiolytic, relaxing, soporific or anticonvulsant effect.
Features:
The most significant are its effects against anxiety and its action as a muscle relaxant. Its incorporation into the therapy allowed the control of distress without the simultaneous occurrence of wakefulness. These drugs frequently produce habituation.
Essential pharmacological mechanisms:
Its effects are produced by agonist or reinforcing action of inhibitory neurotransmitters such as glycine, gammaaminobutyric acid (GABA) and especially in the GABA-A receptor, which in addition to its anxiety-reducing effect competes with the dopamine tone.
On the other hand, they are antagonists of serotonin and glutamic acid. They also raise prostaglandin E, with anticonvulsant effect. Specific receptors for benzodiazepines have recently been described, which raises the inference that following the opioid model, natural substances in the CNS of chemical structure similar to these drugs could exist.
Structure on the nervous system:
The fundamental structures of the nervous system in which they exert their action:
The fundamental action originates at the level of the limbic system, modulating center of approach and avoidance behaviors, as well as significant visceral regulator. They also act on the hypothalamus and medullary synaptic connections with remarkable blocking effect, determining its action as a muscle relaxant. The action on reticular formation is less important.
Effects:
Effects on psychopathological manifestations.
These drugs are anxiolytic, antiphobic, anti-obsessive, anticonvulsant; There are currently tranquilizers of specific effects on sleep disorders.
- Effects on the level of wakefulness:
It is very discreet, except for specific drugs that can be used as hypnotics and whose administration is only indicated as a temporary resource at night.
- Vegetative effects:
They cause discrete vagolytic and sympatholytic effects in conventional doses, however, it should be noted that benactizine has a remarkable vagolytic effect and that benzodiazepines, such as diazepam and chlorodiazepóxide, can cause compensatory tachycardia of the decrease in respiratory rate determined by its effect as muscle relaxant.
- Extrapyramidal effects:
As generalization they do not produce them, and they can even be used as a therapeutic for some extrapyramidal conditions determined by neuroleptics. There are exceptional reports of extrapyramidal effects with some benzodiazepines.
- Effects on seizure threshold:
They are significant and are related to their potentiating action of the inhibitory neurotransmitters, as well as their prostaglandin E releasing effect, of remarkable anticonvulsant action. It should be remembered that parenteral diazepam is the first choice in the treatment of epileptic status.
Habitability risk:
It is notable, especially if they are administered in high doses and for a long time. The general practitioner should use the lowest effective doses and suspend the indication as soon as symptoms are controlled. The addictive risk is higher in hypnotic drugs, followed by meprobamate.
Fundamental indications:
Anxiety of neurotic level, phobias, psychophysiopathological manifestations, as sleep inducers and as a complement to antiepileptic treatment.
Contraindications:
In myasthenia gravis, in subjects with addictions and in the first 3 months of pregnancy. The general practitioner should know that in alcoholics there is a cross tolerance with tranquilizers, so that to produce anxiolytic effects high doses would be necessary. In these cases it is recommended to use a neuroleptic such as haloperidol or trifluoperacin, although diacepam or injectable chlorodiazepóxide is indicated in acute cases until the crisis is overcome.
Toxicity and side effects:
Polymorphic dermatomotoxies, ataxia, occasional sleepiness, nystagmus, alcohol potentiation, temporary decrease in libido, constipation, dyspepsia, discrete hypotension, exceptionally cholangiolytic bacteria similar to those reported with chlorpromazine, although its hepatotoxic effect is discrete. These drugs are depressants of the nervous system, their prolonged use can cause hypotimia and in cases of long-lived drugs, such as diazepam and chlorodiazepóxide, an accumulation occurs that increases the risk of daytime sleepiness, concentration and memory difficulties, as well as falls, the latter more frequent in the elderly.
------------------------------
Tranquilizers:
Heterogeneous group of substances that, according to the dose or the active substance it contains, triggers a calming, anxiolytic, relaxing, soporific or anticonvulsant effect.
Features:
The most significant are its effects against anxiety and its action as a muscle relaxant. Its incorporation into the therapy allowed the control of distress without the simultaneous occurrence of wakefulness. These drugs frequently produce habituation.
Essential pharmacological mechanisms:
Its effects are produced by agonist or reinforcing action of inhibitory neurotransmitters such as glycine, gammaaminobutyric acid (GABA) and especially in the GABA-A receptor, which in addition to its anxiety-reducing effect competes with the dopamine tone.
On the other hand, they are antagonists of serotonin and glutamic acid. They also raise prostaglandin E, with anticonvulsant effect. Specific receptors for benzodiazepines have recently been described, which raises the inference that following the opioid model, natural substances in the CNS of chemical structure similar to these drugs could exist.
Structure on the nervous system:
The fundamental structures of the nervous system in which they exert their action:
The fundamental action originates at the level of the limbic system, modulating center of approach and avoidance behaviors, as well as significant visceral regulator. They also act on the hypothalamus and medullary synaptic connections with remarkable blocking effect, determining its action as a muscle relaxant. The action on reticular formation is less important.
Effects:
Effects on psychopathological manifestations.
These drugs are anxiolytic, antiphobic, anti-obsessive, anticonvulsant; There are currently tranquilizers of specific effects on sleep disorders.
- Effects on the level of wakefulness:
It is very discreet, except for specific drugs that can be used as hypnotics and whose administration is only indicated as a temporary resource at night.
- Vegetative effects:
They cause discrete vagolytic and sympatholytic effects in conventional doses, however, it should be noted that benactizine has a remarkable vagolytic effect and that benzodiazepines, such as diazepam and chlorodiazepóxide, can cause compensatory tachycardia of the decrease in respiratory rate determined by its effect as muscle relaxant.
- Extrapyramidal effects:
As generalization they do not produce them, and they can even be used as a therapeutic for some extrapyramidal conditions determined by neuroleptics. There are exceptional reports of extrapyramidal effects with some benzodiazepines.
- Effects on seizure threshold:
They are significant and are related to their potentiating action of the inhibitory neurotransmitters, as well as their prostaglandin E releasing effect, of remarkable anticonvulsant action. It should be remembered that parenteral diazepam is the first choice in the treatment of epileptic status.
Habitability risk:
It is notable, especially if they are administered in high doses and for a long time. The general practitioner should use the lowest effective doses and suspend the indication as soon as symptoms are controlled. The addictive risk is higher in hypnotic drugs, followed by meprobamate.
Fundamental indications:
Anxiety of neurotic level, phobias, psychophysiopathological manifestations, as sleep inducers and as a complement to antiepileptic treatment.
Contraindications:
In myasthenia gravis, in subjects with addictions and in the first 3 months of pregnancy. The general practitioner should know that in alcoholics there is a cross tolerance with tranquilizers, so that to produce anxiolytic effects high doses would be necessary. In these cases it is recommended to use a neuroleptic such as haloperidol or trifluoperacin, although diacepam or injectable chlorodiazepóxide is indicated in acute cases until the crisis is overcome.
Toxicity and side effects:
Polymorphic dermatomotoxies, ataxia, occasional sleepiness, nystagmus, alcohol potentiation, temporary decrease in libido, constipation, dyspepsia, discrete hypotension, exceptionally cholangiolytic bacteria similar to those reported with chlorpromazine, although its hepatotoxic effect is discrete. These drugs are depressants of the nervous system, their prolonged use can cause hypotimia and in cases of long-lived drugs, such as diazepam and chlorodiazepóxide, an accumulation occurs that increases the risk of daytime sleepiness, concentration and memory difficulties, as well as falls, the latter more frequent in the elderly.
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