Diazepam muscle relaxant

Drowsiness is the most common reaction seen with the use of skeletal muscle relaxants. Additional adverse reactions are given in die Summary Drug Table Drugp Used to Treat Musculoskeletal Disorders. Some of the adverse reactions tiiat may be seen with the administration of diazepam include drowsiness, sedation, sleepiness, letiiargy, constipation or diarrhea, bradycardia or tachycardia, and rash. 

The skeletal muscle relaxants are contraindicated in patients with known hypersensitivity. Baclofen is contraindicated in skeletal muscle spasms caused by rheumatic disorders. Carisoprodol is contraindicated in patients with a known hypersensitivity to meprobamate. Cyclobenzaprine is contraindicated in patients with a recent myocardial infarction, cardiac conduction disorders, and hyperthyroidism, hi addition, cyclobenzaprine is contraindicated within 14 days of the administration of a monoamine oxidase inhibitor. Oral dantrolene is contraindicated in patients with active hepatic disease and muscle spasm caused by rheumatic disorders and during lactation. See Chapter 30 for information on diazepam. 

There is an increased central nervous system (CNS) depressant effect when the skeletal muscle relaxants are administered with other CNS depressants, such as alcohol, antihistamines, opiates, and sedatives. There is an additive anticholinergic effect when cyclobenzaprine is administered with other drugs with anticholinergic effects (eg, antihistamines, antidepressants, atropine, haloperidol). See Chapter 30 for information on diazepam. 

Some of these drugp may have additional uses as sedatives, muscle relaxants, anticonvulsants, and in the treatment of alcohol withdrawal. For example, clo-razepate (Tranxene) and diazepam (Valium) are used as anticonvulsants (see Chap. 28). Additional uses of the individual antianxiety drugp are given in the Summary Drug Table Antianxiety Drugp. 

Benzodiazepine The family name for a group of drugs with anticonvulsant, muscle relaxant and sedative-hypnotic properties. Examples include chlorodiazepoxide (Librium), diazepam (Valium), flunitrazepam and temazepam. These drugs have largely superseded the barbiturates. 

Sedative and anxioiytic effects A number of flavonoids have been shown to bind to benzodiazepine receptors and have anxiolytic effects (Medina et al. 1997). The anxiolytic effects of chrysin were examined in mice (Wolfman et al. 1994). Chrysin (1 mg/kg IP) reduces behavioral measures of anxiety (elevated-plus maze) in a manner similar to diazepam (0.3-0.6 mg/kg), which was reversed by pretreatment with a benzodiazepine antagonist, Ro 15-1788. The anxiolytic effect is not likely due to sedation because there is no concurrent reduction in motor activity at the doses used. Unlike diazepam, chrysin does not produce muscle relaxation at higher doses. 

The synthesis of these compounds will be described in Section 3.1, Opioid analgesics. Besides opioids, benzodiazepines (diazepam, lorazepam, and midazolam), which have anxiolytic, sedative, and anticonvulsant effects, that cause amnesia and muscle relaxation, are frequently used to relieve patients anxiety during anesthesia. 

Muscle relaxant As an adjunct for the relief of skeletal muscle spasm because of reflex spasm caused by local pathology, spasticity caused by uppermotor neuron disorders, athetosis, stiff-man syndrome, used parenterally in the treatment of tetanus (diazepam). 

Diazepam (Valium, Diastat) [C-IVj [Anxiolytic, Skeletal Muscle Relaxant, Anticonvulsant, Sedative/Hypnotic/ Benzodiazepine] Uses Anxiety, EtOH withdrawal, muscle spasm, status epilepticus, panic disorders, amnesia, preprocedure sedation Action Benzodiazepine Dose Adults. Status epilepticus 5-10 mg IV/IM Anxiety 2-5 mg IM/IV Preprocedure 5-10 mg IV just prior to procedure Peds. Status epilepticus 0.5-2 mg IV/IM Sedation 0.2-0.5 mg/kg IV (onset w/in 5IV and 30 min IM duration about 1 h IV and IM) Caution [D, / -] Contra Coma, CNS depression, resp d es-sion, NAG, severe uncontrolled pain, PRG Disp Tabs 2, 5, 10 mg soln 1, 5 mg/mL inj 5 mg/mL rectal gel 2.5, 5, 10, 20 mg/mL SE Sedation, amnesia, bradycardia, i BP, rash, X resp rate Interactions T Effects W/ antihistamines, azole antifungals, BBs, CNS depressants, cimetidine, ciprofloxin, disulfiram, INH, OCP, omeprazole, phenytoin, valproic acid, verapamil, EtOH, kava kava, valman T effects OF digoxin, diuretics X effects w/ barbiturates, carbamazepine. 

Benzodiazepines also possess muscle relaxant activity. Their pharmacology is discussed in Chapter 30. Diazepam Valium) has been used for control of flexor and extensor spasms, spinal spasticity, and multiple sclerosis. The muscle relaxant effect of the benzodiazepines may be mediated by an action on the primary afferents in the spinal cord, resulting in an increased level of presynaptic inhibition of muscle tone. Polysynaptic reflexes are inhibited. The most troublesome side effect is drowsiness, which is dose dependent. Tolerance to both the therapeutic effects and the side effects develops. 

Diazepam (Valium) Anxiety, muscle relaxation, status epilepticus... 

Fluoxentine has been detected in water and municipal STP effluents (Kolpin et al., 2002 Metcalfe et al., 2003 Brooks et al., 2003, 2005). The muscle relaxant diazepam (a tranquilizer) detected in low concentrations (i.e., 40 ng L ) in STP effluents in Germany (Temes et al., 2001) and at 0.7-1.2ngL in the Po River in Italy (Zuccato et al., 2000). Also frequently detected among the antiepHeptic dmgs is carbamazepine (Temes, 1998 Andreozzi et al., 2002 Tixier et al., 2003). It has very low removal rates in STPs. For example, Temes (1998) reported removal of only 7% in wastewater treatment plants in Germany. In a recent survey by Metcalfe et al. (2004), all 26 samples collected contained detectable levels of carbamazepine, making it the most frequently detected dmg in Canadian waters. Other epileptic dmgs detected in water include primidone (Drewes et al., 2002,2003). 

Pazinaclone. Pazinaclone is a nonbenzodiazepine partial agonist. Animal work has shown that it has anxiolytic and anticonvulsant activity. Pazinaclone does not, however, produce the sedative, muscle relaxant, or motor coordination effects seen with diazepam (Waka and Fukada 1991). Phase II clinical trials are currently under way in the United States, Europe, and Japan, which have so far demonstrated that it is well tolerated and seems to cause significantly less sedation than do benzodiazepines (Uchiumi et al. 1992). 

Benzodiazepines are highly effective anxiolytics and sedatives. They also have muscle relaxant, amnestic, and anticonvulsant properties. Benzodiazepines effectively treat both acute and chronic generalized anxiety and panic disorder. The high-potency benzodiazepines alprazolam and clonazepam have received more attention as antipanic agents, but double-blind studies also have confirmed the efficacy of diazepam and lorazepam in the treatment of panic disorder. Although only a few benzodiazepines are specifically approved by the... 

Nevertheless, the GABAergic properties of benzodiazepines remain their most important clinical application. Over the past 30 years, the most widely used benzodiazepine drug has been diazepam (1.6). It is an anxiolytic, sedative, and muscle relaxant the anxious, depressed person becomes more outgoing and relaxed. There have been many diazepam analogs. Oxazepam (4.177) and lorazepam (4.178) have similar effects. Temazepam (4.179), flunitrazepam (4.180), and flurazepam (4.181) are useful sedative-hypnotics. Clonazepam (4.182) is a clinically useful anticonvulsant. Brotizolam (4.183), a novel benzodiazepine analog, seems to be an effective sedative-hypnotic. Midazolam (4.184) is an imidazolo-benzodiazepine that is water soluble and thus easily injectable. It is a hypnotic sedative with marked amnestic (i.e., memory loss) properties and is used in dentistry, endoscopic procedures, and induction to anesthetics in the elderly and in... 

The tranquillizers like benzodiazepines (diazepam 5-10 mg oral, or lorazepam 2 to 4 mg IM, IV are now preferred for preanaesthetic medication because they produce tranquillity, have better muscle relaxant property and smoothen induction. Other tranquillizer compounds include phenothiazines which possess sedative, antiemetic and antihistaminic properties. They can be given orally as well as parenterally. 

Meprobamate and the benzodiazepines have frequently been used as central muscle relaxants, though evidence for general efficacy without accompanying sedation is lacking. A possible exception is diazepam, which has useful relaxant effects in skeletal muscle spasticity of central origin (see Chapter 27). 

Diazepam/ Valium/Roche Management of anxiety disorders, skeletal muscle relaxant... 

Most muscle relaxants are absorbed fairly easily from the gastrointestinal tract, and the oral route is the most frequent method of drug administration. In cases of severe spasms, certain drugs such as methocarbamol and orphenadrine can be injected intramuscularly or intravenously to permit a more rapid effect. Likewise, diazepam and dantrolene can be injected to treat spasticity if the situation warrants a faster onset. As discussed earlier, continuous intrathecal baclofen administration may be used in certain patients with severe spasticity, and local injection of botulinum toxin is a possible strategy for treating focal dystonias and spasticity. Metabolism of muscle relaxants is usually accomplished by hepatic microsomal enzymes and the metabolite or intact drug is excreted through the kidneys. 

The pharmacologic effects of Rohypnol include sedation, muscle relaxation, and anxiety reduction. The sedative effects are said to be seven to 10 times that of diazepam (Valium). In high doses, flunitrazepam can cause malignant hyperthermia, or a sharp increase in body temperature that can cause muscle breakdown and failure of the kidneys and cardiovascular system. 

Flunitrazepam (Rohypnol), also known as roofies, is a benzodiazepine with physiological effects similar to diazepam (Valium), although it is about 10 times more potent. The drug produces sedative-hypnotic effects that include muscle relaxation and amnesia it can also produce physical and psychological dependence. It is illegal and not approved for use in the United States. 

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