Sedatives, Hypnotics, and Analgesics

Clinical studies showed that elderly patients are more sensitive to drugs such as sedatives, hypnotics, and analgesics. The most extensive studies show a decrease in responsiveness to /3-adrenoreceptors, stimulants, and blockers. Hypothermia is poorly tolerated by the elderly, as their body temperature regulation is impaired. 

Sedative and hypnotic drugs, such as benzodiazepines and barbiturates, increase the half-life from 50% to 150% in patients between 30 and 70 years of age. The most alarming toxicity is ataxia, which must be considered to avoid accidents. Ataxia is an alarming effect hence the patient is advised not to drive if taking these drugs. Elderly patients are found to be more sensitive to opioids and should use them with caution. 

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Heterocannabinoids 46 have shown sedative-hypnotic and analgesic activity in cats and rodents. 106,107 Compound 53 showed sedation and anticonvulsant activity in mice.108 Kessoglycol mono-acetate (54) was reported to have a sedative-hypnotic profile in animals.109... 

Phenobarbital. Is a sedative, hypnotic, and somewhat analgesic. It is addictive. 

Another example comes from the benzodiazepine series where tetrazepam can be compared with diazepam. However, in this case a slight difference in the activity profile exists tetrazepam is less sedative, hypnotic and anticonvulsant than diazepam on the other hand, it has more muscle relaxant and analgesic effects, which indicates its use in visceral and articular pain. From the chemical point of view, the cyclohexenic double bond is introduced in a rather unexpected manner by means of a radicalar rearrangement of an //-chloroamide (Fig. 19.33). 

Class selective a -adrenergic agonist with sedative, hypnotic, anxiolytic, analgesic and sympatholytic effects... 

It is hard to interpret the previous studies on metaxalone due to many study limitations. There were only 200 patients recruited in the two mid-1960s trials that led to FDA approval. However, there was no clear description of the duration and type of back pain and treatment before enrollment. Whether there were concomitant analgesics, sedatives, hypnotics, and/or physical therapy had not been elucidated clearly. Although Dent et al. illuminated the use of associated medications before and during their trial, there were only 228 patients enrolled in the study pubhshed in 1975. 

The CCK system shares one property with the opioid system, ie, the existence of selective nonpeptide antagonists. These include aspedicine, a natural benzodiazepine (136), and Devazepide (L-364,718 MK-329) (137). Selective, potent peptide antagonists for CCK, eg, Cl-988 and PD 134308, have been developed that maybe useful as anxiolytics and as dmgs which increase the analgesic effect of morphine but at the same time prevent morphine tolerance (138) (see Hypnotics, sedatives, anticonvulsants, and anxiolytics). 

See Alkaloids Analgesics, antipyretics, and antiinflammatory agents Hypnotics, sedatives, anticonvulsants, and anxiolytics. 

Nabitan (39) is a cannabis-inspired analgesic whose nitrogen atom was introduced in order to improve water solubility and perhaps to affect the pharmacological profile as well. The phenolic hydroxyl of benzopyran synthon is esterified with 4-(l-piperidino)butyric acid under the influence of dicyclohexyl carbodi mi de. In addition to being hypotensive and sedative-hypnotic, nabitran (39) is a more potent analgesic than codeine. The preparation of synthon begins with aceto-... 

Meperidine (Demerol) [C-ll] [Narcotic Analgesic] Uses Moderate/ severe pain Action Narcotic analgesic Dose Adults. 25-50 mg IV, 50-100 mg IM Peds. 1 mg/kg IV/IM (onset w/in 5 min IV and 10 min IM duration about 2 h) Caution [C, ] Contra Convulsive disorders and acute abdomen Disp Prefilled 1 mL syringes 25, 50, 75, 100 mg/mL various amps and vials oral syrup and tabs SE N/V (may be severe), dizziness, weakness, sedation, miosis, resp d ession, xerostomia (dry mouth) Interactions t CNS depression W/ opiates, sedatives/ hypnotics TCNS stimulation W/amphetamines t risk of tox W7 phenytoin EMS Pt should be receiving O2 prior to administration have resuscitation equipment and naloxone available naloxone can be used as an antidote to reverse resp depression aspirate prior to IM administration inadv tent IV admin of IM doses may cause tach and syncope mix w/ NS to make a 10 mg/mL soln and inj very slowly N/V may be sev e may premedicate w/ an antiemetic... 

Opium has been replaced by safer, more effective analgesics and sedative/hypnot-ics for diagnost ic or operative medication useful as an antidiarrheal... 

Deep sedation is similar to a light state of general (intravenous) anesthesia involving decreased consciousness from which the patient is not easily aroused. Because deep sedation is often accompanied by a loss of protective reflexes, an inability to maintain a patent airway, and lack of verbal responsiveness to surgical stimuli, this state may be indistinguishable from intravenous anesthesia. Intravenous agents used in deep sedation protocols include the sedative-hypnotics thiopental, methohexital, midazolam, or propofol, the potent opioid analgesics, and ketamine. 

Chamomile has been used medicinally since the time of ancient Rome for its purported sedative, antispasmodic, and antirheumatic effects. Today, it is used topically to treat a variety of inflammatory conditions involving the mouth, skin, respiratory tract (via inhalation), and gastrointestinal tract. It is also used internally as a gastrointestinal antispasmodic and an anti-inflammatory agent. Chamomile is believed to have sedative, hypnotic, analgesic, and immunostimulant effects. 

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