Sedatives, Hypnotics, and Antipsychotics

Overdoses of paracetamol can be very dangerous, as the drug has a narrow therapeutic index and may cause hepatic and renal necrosis. Nausea, vomiting, lethargy, and sweating are the early overdose symptoms. Paracetamol must be given with caution in alcoholics and patients with liver and kidney damage. 

Diclofenac is a phenylacetic acid derivative used mainly as sodium salt for the treatment of various pain and inflammation. Intramuscular injection occasionally causes tissue damage at the injection site. Suppositories may cause local irritation transient burning and stinging are reported when used for the eye and large doses can cause aplastic anemia.14 

In the patient with contact lenses, it is advised not to use diclofenac preparations for ophthalamic treatment. Diclofenac also is contraindicated for intravenous administration in patients with renal impairment, hypovolemia, dehydration, asthma, or cerebrovascular bleeding. 

Patients who are receiving diazepam therapy should not operate machinery or drive motor vehicles. 

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Anxiolytic sedatives, hypnotics, and antipsychotics are lumped together in this section because all of them act by some form of intervention with the brain and... 

Information about prescription drag use alcohol or other substance use family medical history and history of trauma, depression, or head injury should be obtained. It is important to rule out medication use as a contributor or cause of symptoms (e.g., anticholinergics, sedatives, hypnotics, opioids, antipsychotics, and anticonvulsants) as contributors to dementia symptoms. Other medications may contribute to delirium, e.g.,... 

Many medicines affect performance, not only psychotropic drugs (amongst which sedative antidepressants, benzodiazepines, hypnotics and antipsychotics are the most obvious examples) but also antihistctrnines, antimuscaiinics, analgesics including some NSAIDs, (e.g. indomethacin), antiepileptics, antidiabetics (hypoglycaemia) and some antihypertensives. Alcohol and caimabis are discussed on pages 178 and 190. 

Antidepressants Antipsychotic Agents Sedatives, Hypnotics, and Tranquilizers Anticonvulsants. 

Drug interactions The most important drug interactions involving opioid analgesics are additive CNS depression with ethanol, sedative-hypnotics, anesthetics, antipsychotic drugs, tricyclic antidepressants, and antihistamines. Concomitant use of certain opioids (eg, meperidine) with MAO inhibitors increases the incidence of hyperpyrexic coma. Meperidine has also been implicated in the serotonin syndrome when used together with selective serotonin rcuptake inhibitors. 

Introduction - Although an effort has been made in this chapter to exclude depressants classified in other chapters as antipsychotic and antianxiety agents, certain benzodiazepines will be considered here because of the number of compounds in this series which have been found clinically to possess sedative-hypnotic and anticonvulsant activity. In most cases, compounds with more than preliminary pharmacological data or representatives of new structural types were selected for inclusion in this chapter. 

Other sedative-hypnotic medications, such as barbiturates, may play a useful role in severe withdrawal from this group of drugs. For example, in a case series of GBL withdrawal, use of intravenous pentobarbital in the range of 1-2 mg/kg/hour lowered the total requirement for intravenous lorazepam (Sivilotti et al. 2001). Antipsychotic medications are often used to reduce psychotic agitation. However, because antipsychotic medications lower the seizure threshold and may contribute to loss of central control of temperature leading to hyperthermia or neuroleptic malignant syndrome (NMS), they are not indicated as first-line medications for GHB withdrawal delirium (Dyer and Roth 2001 McDaniel and Miotto 2001 Sharma et al. 2001). If anti-... 

A number of medications have been associated with an increased risk of falling, including drugs affecting mental status such as antipsychotics, benzodiazepines, tricyclic antidepressants, sedative-hypnotics, anticholinergics, and corticosteroids. Some cardiovascular and antihypertensive drugs also can contribute to falls, especially those causing orthostatic hypotension.9... 

Mechanism of Action A phenothiazine that acts as an antihistamine, antiemetic, and CNS-antipsychotiC typical hypnotic. As an antihistamine, inhibits histamine at histamine receptor sites. As an antiemetic, diminishes vestibular stimulation, depresses labyrinthine function, and acts on the chemoreceptor trigger zone. As a sedative-hypnotic, produces CNS depression by decreasing stimulation to the brainstem reticular formation. Therapeutic Effect Prevents allergic responses mediated by histamine, such as rhinitis, urticaria, and pruritus. Prevents and relieves nausea and vomiting. Pharmacokinetics ... 

Pharmacodynamics, antipsychotics also differ in their pharmacodynamics, i.e. their pharmacological and clinical profiles of action. A rough distinction is made between highly sedative, hypnotic antipsychotics (e.g. clopenthixol, levomepromazine) and other products with weaker initial sedative action (e.g. fluphenazine and haloperidol). Sedative antipsychotics are prescribed for states of major unrest, often combined with insomnia, whereas the less sedative antipsychotics are preferred for patients suffering from delusions and hallucinations but in whom heavy sedation during daytime is undesirable. 

Garza-Trevino ES, Hollister LE, Overall JE, et al. Efficacy of combinations of intramuscular antipsychotics and sedative-hypnotics for control of psychotic agitation. Am J Psychiatry 1989 146 1598-1601. 

Benzodiazepines are used as hypnotics because they have the ability to increase total sleep time. They demonstrate minimal cardiovascular effects, but do have the ability to increase heart rate and decrease cardiac output. Most CNS depressants, including the benzodiazepines, exhibit the ability to relax skeletal muscles. Clozapine, a dibenzodiazepine, is used in the treatment of schizophrenia. It has both sedative and antipsychotic actions, and is the only FDA-approved medication indicated for treatment-resistant schizophrenia, and for reducing the risk of suicidal behavior in patients with schizophrenia. This drug can have potentially life-threatening side effects, but appears to have no abuse potential and will not be considered further. 

Other classes of drugs not included in Figure 22-3 that may exert sedative effects include most antipsychotic and many antidepressant drugs and certain antihistaminic agents (eg, hydroxyzine, promethazine). As discussed in other chapters, these agents differ from conventional sedative-hypnotics in both their effects and their major therapeutic uses. Since they commonly exert marked effects on the peripheral autonomic nervous system, they are sometimes referred to as "sedative-autonomic" drugs. Certain antihistaminics with sedative effects are available in over-the-counter sleep aids. Their autonomic properties and their long durations of action can result in adverse effects. 

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