Respiratory stimulant

However, there are occasions ia which the use of a respiratory stimulant may be warranted. By far the leading respiratory stimulant marketed ia the United States is doxapram [309-29-5] (13), prepared by a unique rearrangement of the pyrroHdine [3471-97-4] (14) to the pyrroHdinone [3192-64-1] (15), followed by alkylation using morpholine (15). 

Conversion of the carboxylic acid to the diethyl amide interestingly leads to an agent that exhibits the properties of a respiratory stimulant. One synthesis of this agent starts with the preparation of the mixed anhydride of nicotinic and benzene-sulfonic acid (4). An exchange reaction between the anhydride and diethyl benzenesulfonamide affords nikethemide (5). ... 

Respiratory stimulant. An agent that enhances the frequency and/ or depth of respiration. 

Therapeutic Function Central and respiratory stimulant Chemical Name N,N-Diethyl-4-hydroxy-3-methoxybenzamide Common Name Vanillic acid diethylamide Structural Formula coxtc HjIj... 

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. 

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. 

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. 

Ketamine (Ketalar) is a rapid-acting general anesthetic. It produces an anesthetic state characterized by profound analgesia, cardiovascular and respiratory stimulation, normal or enhanced skeletal muscle tone, and occasionally mild respiratory depression. Ketamine is used for diagnostic and surgical procedures that do not require relaxation of skeletal muscles, for induction of anesthesia before the administration of other anesthetic drugp, and as a supplement to other anesthetic drags. 

A more highly substituted pyrrolidone, doxapram, shows activity as a respiratory stimulant. Preparation of this agent involves an interesting rearrangement, which in effect results in a ring exchange reaction. Alkylation of the anion from diphenylacetonitrile with the chloropyrrolidine 14 affords 15. Hydrolysis of the nitrile function leads to the... 

Some quinolizine derivatives are employed as drugs. One of them is flumequine 280, a member of the quinolone family of antibacterial agents. Cytisine 9 is a ligand of the nicotinic acetylcholine receptor that acts primarily as a cholinomimetic at the ganglionar level, being used as a respiratory stimulant in some countries. Cytisine analogues with improved ability to cross the blood-brain barrier have also been developed <1999FA438>. 

Substituted pyrrolidin-2-ones are generally resistant to metabolic hydrolysis as seen in the cases of rolipram and doxapram. Metabolic studies of the antidepressant rolipram (5.64) in several mammalian species, including humans, did not reveal any cleavage of the pyrrolidinone ring [174], Similarly, no metabolite with an opened pyrrolidin-2-one ring was found for doxapram (5.65), a respiratory stimulant [174],... 

Carbon dioxide gas is an asphyxiant, a potent respiratory stimulant, and both a stimulant and depressant of the central nervous system. Fatalities have occurred after people have entered enclosures where air has been largely displaced by CO2. Therefore, fixed, automatic CO2 systems require a time delay pre-evacuation alarm period (often 30 seconds), warning signs, and an alarm signal incorporated into the system design to allow sufficient time for personnel evacuation prior to CO2 release. Verification of the oxygen level must be made prior to reentry. 

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. 

Pharmacology The methyixanthines (theophylline, its soluble salts and derivatives) directly relax the smooth muscle of the bronchi and pulmonary blood vessels, stimulate the CNS, induce diuresis, increase gastric acid secretion, reduce lower esophageal sphincter pressure, and inhibit uterine contractions. Theophylline is also a central respiratory stimulant. Aminophylline has a potent effect on diaphragmatic contractility in healthy people and may then be capable of reducing fatigability and thereby improve contractility in patients with chronic obstructive airways disease. Pharmacokinetics ... 

Pharmacology Amphetamines are sympathomimetic amines with CNS stimulant activity. CNS effects are mediated by release of norepinephrine from central noradrenergic neurons. Peripheral activities include elevation of systolic and diastolic blood pressures and weak bronchodilator and respiratory stimulant action. Pharmacokinetics ... 

Respiratory stimulants are not recommended. Side effects have precluded the use of drugs such as almitrine. 

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