Analeptics stimulants

As indicated, most of the analeptic stimulants were used as pharmacological treatments for overdosage of CNS depressants. Doxapram (Dopram) is sometimes used to counteract postanesthetic respiratory depression and as an aid in chronic obstructive pulmonary disease. Pentylenetetrazol (Metrazol) was used experimentally on rare occasions to activate the electroencephalogram. Strychnine is used almost exclusively in animal studies as a tool for studying CNS mechanisms because it is a relatively specific glycine antagonist. 

Another suggested mechanism of action involves the chloride channel. As discussed previously, the chloride channel is intimately associated with neuronal inhibition, and its activity appears to be modulated at many different sites. Caffeine can compete for binding at the benzodiazepine site and would therefore be expected to reduce chloride conductance. Thus, caffeine may act functionally like the analeptic stimulants that limit chloride channel activation. 

Which of the following mechanisms of action account for the effects of all analeptic stimulants except strychnine ... 

A. Analeptic stimulants, such as pentylenetetrazol and picrotoxin, act by inhibiting chloride influx at the GABAa receptor-chloride channel complex. This antagonism can occur through interaction with one of several binding sites or allosteric modifiers of receptor-channel function. 

Analeptic Stimulant such as caffeine or amphetamine that... 

Therapeutic Function Analeptic, Stimulant, Antidepressant Chemical Name Pyrrolidine, l-(l-(phenylmethyl)butyl)-, hydrochloride Common Name Prolintane hydrochloride Promotil... 

Analeptics stimulate the release of neurotransmitters, norepinephrine, and dopamine from the brain and from the peripheral nerve terminals of the sympathetic nervous system, resulting in euphoria and increased alertness. Patients can experience sleeplessness, restlessness, tremors, irritability, and cardiovascular problems (increased heart rate, palpitations, dysrhythmias, and hypertension). 

Compounds that have agonistic properties at glutamate or aspartate receptors are also CNS stimulants, readily cause convulsions, and presumably could also be employed as analeptics. Three separate excitatory amino acid receptor subtypes have been characterized pharmacologically, based on the relative potency of synthetic agonists. These three receptors are named for their respective prototypical agonists A/-methyl-D-aspartate [6384-92-5]... 

The term analeptics refers to convulsants and respiratory stimulants (i.e. central nervous system stimulants). They comprise a reverse group of agents (for example amphifrnazole and doxapram (respiratory stimulants) and strychnine, biculline and picrotoxin). Analeptics are mainly experimental drugs. Only amphifrnazole and doxapram are occasionally used for the treatment of acute ventilatory failure. 

The CNS stimulants include the analeptics, drugs tiiat stimulate the respiratory center of the CNS the amphetamines, drugs witii a high abuse potential because of dieir ability to produce euphoria and wakefulness and the anorexiants, drugs used to suppress die appetite... 

Doxapram (Dopram) and caffeine (combination of caffeine and sodium benzoate) are two analeptics used in medicine Doxapram increases the depth of respirations by stimulating special receptors located in the carotid... 

Caffeine is a mild to potent CNS stimulant, with the degree of its stimulating effect dependent on the dose administered. Caffeine stimulates the CNS at all levels, including the cerebral cortex, die medulla, and the spinal cord. Caffeine has mild analeptic (respiratory stimulating) activity. Other actions include cardiac stimulation (which may produce tachycardia), dilatation of coronary and peripheral blood vessels, constriction of cerebral blood vessels, and skeletal muscle stimulation. Caffeine also has mild diuretic activity. 

ANALEPTICS. When a CNS stimulant is prescribed for respiratory depression, initial patient assessments will include the blood pressure, pulse, and respiratory rate. It is important to note the depth of the respirations and any pattern to the respiratory rate, such as shallow respirations or alternating deep and shallow respirations. The nurse reviews recent laboratory tests (if any), such as arterial blood gas studies. Before administering the drug, the nurse ensures that the patient has a patent airway. Oxygen is usually administered before, during, and after drug administration. 

Respiratory depression can be a serious event requiring administration of a respiratory stimulant. When an analeptic is administered, the nurse notes and records the rate, depth, and character of the respirations before the drug is given to provide a database for evaluation of the effectiveness of drug therapy. Oxygen is usually ordered for before and after administration of a respiratory stimulant. After administration, the nurse monitors respirations closely and records the effects of therapy. 

The detection limits for analeptics and stimulants are 2 to 5 pg substance per chromatogram zone [6]. P-Blockers can be detected at 50-100 ng per chromatogram zone [5]. 

Several semisynthetic derivatives of yohimbine alkaloids show interesting pharmacological activity. For example, 17-methylthiomethoxyyohimbane stereoisomers (612 and 613) are valuable central nervous system depressants (349) and several hydrazides of yohimbinecarboxylic acid (614 and 615-type compounds) are useful cardiac stimulants, respiratory analeptics, and antihypertensives (350-353). 

CNS stimulants can be classified as Psychomotor stimulants compounds that display a stimulatory effect primarily on brain functions and which activate mental and physical activity of the organism. They are made up of methylxanthines (caffeine, theophylline, pentoxifyllin), amphetamines (dextroamphetamine, methamphetamine), and also methylphenidate and pemoline. Respiratory stimulants or analeptics compounds, which cause certain activations of mental and physical activity of the organism, and primarily excite the vasomotor and respiratory centers of the medulla (doxapram, almitrine).Drwgi that suppress appetite or anorectics drags that activate mental and physical activity of the organism, but primarily accentuate the excitatory center of satiation in the hypothalamus (phentermine, diethylpropion).In order to increase mental capability, nootropics — drugs that increase the functional state of the brain — are sometimes used, the effect of which is associated with blood flow and metabolism of the brain. 

Analeptics are drugs that have a stimulatory effect on the respiratory and vasomotor centers of the medulla. Analeptics are primarily used as antagonists in depressant drug overdose (hypnotics, narcotics). Having a relatively small range of therapeutic action, they can stimulate other parts of the CNS even in minor overdoses, causing a number of undesirable side effects such as stimulation of the cardiovascular system, hyperreflexia, vomiting, and seizures. 

Two precautions should be kept in mind Neuromuscular blocking drugs inhibit, concentration-dependently, all skeletal muscles including those necessary for respiration. If these muscles are paralyzed by these drugs artificial respiration must be applied since central or peripheral nerve stimulation, for example with analeptics are useless. Furthermore is it important to realize that the individual subjected to a efficient neuro-muscular blockade is fully conscious and aware of any pain although completely unable to express discomfort. 

Although the use of CNS stimulants (also known as analeptics or convulsants) has declined, certain com-... 

Treatment for severe ethanol overdose is generally supportive. Increased intracranial pressure can be relieved by intravenous administration of hypertonic mannitol. Hemodialysis can accelerate the removal of ethanol from the body. Stimulants of ethanol metabolism, such as fructose, are not sufficiently effective, and use of analeptics is not recommended because of the possibility of precipitating convulsions. 

Psychostimulants are medications that can increase drive and performance. Their most frequent use is in attention deficit hyperactivity disorder (ADHD) and in narcolepsy. They are also called stimulants or, less commonl today, analeptics. 

These are the group of drugs which are used to stimulate the central nervous system. Some of them are also known as analeptics, but they are not much useful clinically due to non-selectivity of action. 

Drugs that stimulate respiration (analeptics) have a place in anaesthetic practice but are not a substitute for mechanical ventilation. They have a direct effect on respiratory drive they do not share a common molecular structure. Respiratory stimulation is generally better achieved by antagonising the depressant effects of the depressant drug, e.g. flumazenil for benzodiazepines naloxone for opioids. 

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