Analeptic

Analeptics counteract narcosis, with a specific stimulant action on the central nervous system. These are primarily employed to combat the drug-induced respiratory depression. An excessive dose of analeptics may result a wide-spread stimulation of the brain that may ultimately cause convulsions. 

A few important drugs imder this eategoiy are namely nikethamide, ethamivan, pemoline, pentetrazol, doxapram, and bemegride. 

N-Diethylnicotinamide N, N-Diethylpyridine-3-carboxamide Diethylamide nicotinic acid  

Coramine (Ciba-Geigy) Corazon (Grossmann, Switz) 

A molecule each of nicotinic and benzenesulphonic acid undergoes dehydration to yield a corresponding anhydride, which on contact with diethyl benzenesulphonamide affords an exchange reaction to give nikethamide. 

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Thymo analeptics and hlood-platelet 1624 aggregation inhibitors... 

Many 1,2,3,5-benzenetetrol derivatives are used mediciaaHy. For example, khellin [82-02-0] (65), which is a naturally occurring benzopyranone, is used as a coronary vasodilator and bronchodilator (233). Derivatives of khellin are effective local anesthetics and antiarrythmics (234). Similarly, amine derivatives (68) that are prepared from khellinone oxime (66) exhibit hypnotic, sedative, anticonvulsant, antiinflammatory, cardiac analeptic, diuretic, and antiulcerous activity (235) (see Analgesics, antipyretics, and antiinflammatory agents). 

Some naturally occurring analeptics have been known for centuries. Two of the best known and most thoroughly studied are strychnine [57-24-9] (1) and picrotoxin [124-87-8] a 1 1 combination of picrotoxinin [17617-45-7] (2) and picrotin [21416-53-5] (3). These continue to be of interest in the study of mammalian neurotransmission. 

BicucuUine [485-49-4] (8) is another analeptic compound known to act by competitively antagonizing GABA at its receptor (9). There is no evidence that bicucuUine has been evaluated in humans. Several other compounds, such as the steroid R5135 (10) or the arylarninopytidazines SR 95103 (11) and SR 95531 (12), appear to antagonize GABA competitively in a manner similar to that of bicucuUine. 

Flurothyl [333-36-8] (bis-(2,2,2-trifluoroeth5i)ether) (9), an analeptic having strong convulsant properties, has been used for chemical shock therapy (13). The compound is unique in that it is a volatile fluorinated ether and its stmcture resembles those of many halogenated general anesthetics. Chemical shock therapy is rarely used. 

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]... 

Benzodiazepiaes have largely replaced barbiturates and barbiturate-like agents for use as anxiolytics and sedative—hypnotics. Because benzodiazepiaes rarely produce levels of CNS depression that require therapeutic iatervention, the need for analeptics has decreased considerably. 

Health and Safety Factors. Clinical side effects and LD q values of most commercially available analeptics have been summarized (2). Overdoses produce symptoms of extreme CNS excitation, including resdessness, hyperexcitabiUty, skeletal muscle hyperactivity, and ia some cases convulsions. 

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. 

ANALEPTICS. After administration of an analeptic, the nurse carefully monitors the patient s respiratory rate and pattern until the respirations return to normal. The nurse monitors the level of consciousness, the blood pressure and pulse rate at 5- to 15-minute intervals or as ordered by the primary health care provider. The nurse may draw blood for arterial blood gas analysis at intervals to determine the effectiveness of the analeptic, as well as the need for additional drug therapy. It is... 

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. 

Nausea and vomiting may occur with the administration of an analeptic therefore, the nurse should keep a suction machine nearby should vomiting occur. Urinary retention may be seen with the administration of doxapram therefore, the nurse measures intake and output and notifies the primary health care provider if the patient is unable to void or the bladder appears distended on palpation. 

Ms. Allison is prescribed an analeptic for respiratory depression. Discuss what preadministration and ongoing assessmentsyou would make when airing for Ms. A llison. 

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