A mild sleep-inducing drug, C21H23ClFN3O, used especially in the form of its hydrochloride in the treatment of insomnia.
[FLU(O)R(O)- + (DI)AZEPAM.]
flurazepam
Dictionary:
flu·raz·e·pam (flʊ-răz'ə-păm')  |
n.
A mild sleep-inducing drug, C21H23ClFN3O, used especially in the form of its hydrochloride in the treatment of insomnia.
A mild sleep-inducing drug, C21H23ClFN3O, used especially in the form of its hydrochloride in the treatment of insomnia.
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| Drug Info: Flurazepam |
Brand names: Dalmane®
Chemical formula:
- Drug Forms:
- Flurazepam Hydrochloride Oral capsule (below)
- Flurazepam capsules
Flurazepam Hydrochloride Oral capsule
What is this medicine?
FLURAZEPAM (flure AZ e pam) is a benzodiazepine. It is used to treat insomnia. This medicine helps you to fall asleep and sleep through the night.
This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.
What should I tell my health care provider before I take this medicine?
They need to know if you have any of these conditions:
•an alcohol or drug abuse problem
•bipolar disorder, depression, psychosis or other mental health condition
•kidney disease
•liver disease
•lung or breathing disease
•myasthenia gravis
•Parkinson's disease
•porphyria
•seizures or a history of seizures
•suicidal thoughts
•an unusual or allergic reaction to flurazepam, other benzodiazepines, other medicines, foods, dyes, or preservatives
•pregnant or trying to get pregnant
•breast-feeding
How should I use this medicine?
Take this medicine by mouth with a glass of water. It is only for use at bedtime. Follow the directions on the prescription label. Do not take your medicine more often than directed. Do not stop taking except on the advice of your doctor or health care professional.
Talk to your pediatrician regarding the use of this medicine in children. Special care may be needed. While this medicine may be prescribed for children as young as 15 years for selected conditions, precautions do apply.
Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.
What if I miss a dose?
If you miss a dose, take it as soon as you can. If it is almost time for your next dose, take only that dose. Do not take double or extra doses.What may interact with this medicine?
Do not take this medicine with any of the following medications:
•itraconazole
This medicine may also interact with the following medications:
•barbiturate medicines for inducing sleep or treating seizures, like phenobarbital
•herbal or dietary supplements, like kava kava, melatonin, or valerian
•medicines for anxiety or sleeping problems, like alprazolam, diazepam, lorazepam or triazolam
•medicines for depression, mental problems or psychiatric disturbances
•phenytoin
•prescription pain medicines
This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.
What should I watch for while using this medicine?
Visit your doctor or health care professional for regular checks on your progress. This medicine is for short term periods of use. Your body can become dependent on this medicine, ask your doctor or health care professional if you still need to take it. However, if you have been taking this medicine regularly for some time, do not suddenly stop taking it. You must gradually reduce the dose or you may get severe side effects. Ask your doctor or health care professional for advice. Even after you stop taking this medicine it can still affect your body for several days.
Do not take this medicine unless you are able to get a full night's sleep before you must be active again. You may not be able to remember things that you do in the hours after you take this medicine. Some people have reported driving, making phone calls, or preparing and eating food while asleep after taking this medicine. Take this medicine right before going to sleep. Tell your doctor if you are have any problems with your memory.
You may get drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how this medicine affects you. Do not stand or sit up quickly, especially if you are an older patient. This reduces the risk of dizzy or fainting spells. Alcohol may interfere with the effect of this medicine. Avoid alcoholic drinks.
Do not treat yourself for coughs, colds or allergies without asking your doctor or health care professional for advice.
What side effects may I notice from receiving this medicine?
Side effects that you should report to your doctor or health care professional as soon as possible:
•allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
•confusion
•depression
•feeling faint or lightheaded
•mood changes, excitability or aggressive behavior
•muscle cramps
•problems with balance, speaking, walking
•tremors
•unusual activities while asleep like driving, eating, making phone calls
•unusually weak or tired
Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
•dizziness, drowsiness
•headache
•nausea, vomiting
•stomach pain
This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
Where should I keep my medicine?
Keep out of the reach of children. This medicine can be abused. Keep your medicine in a safe place to protect it from theft. Do not share this medicine with anyone. Selling or giving away this medicine is dangerous and against the law.
Store at room temperature between 15 and 30 degrees C (59 and 86 degrees F). Throw away any unused medicine after the expiration date.
Last updated: 7/1/2002
Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.
| Veterinary Dictionary: flurazepam |
A benzodiazepine hypnotic and sedative, usually used as the hydrochloride salt.
| Wikipedia: Flurazepam |
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Flurazepam
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| Systematic (IUPAC) name | |
| 7-chloro-1-[2-(diethylamino)ethyl]-5-(2-fluorophenyl)-1,3-dihydro-2H-1,4-benzodiazepin-2-one | |
| Identifiers | |
| CAS number | 17617-23-1 |
| ATC code | N05CD01 |
| PubChem | 3393 |
| DrugBank | APRD00983 |
| Chemical data | |
| Formula | C21H23ClFN3O |
| Mol. mass | 387.88 g/mol |
| Pharmacokinetic data | |
| Bioavailability | 83% |
| Metabolism | Hepatic |
| Half life | 40–250 hours |
| Excretion | Renal |
| Therapeutic considerations | |
| Pregnancy cat. |
X (Contraindicated in pregnancy) |
| Legal status | |
| Routes | Oral |
 (what is this?) (verify) |
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Flurazepam (marketed under the brand names Dalmane and Dalmadorm) is a drug which is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. It produces a metabolite with a very long half-life (40-250 hours), which may stay in the bloodstream for up to four days.[1] Flurazepam is therefore unsuitable as a sleeping medication for some individuals due to next day sedation. Effects start approximately 1/2 to 1 hour after oral administration.
Contents |
Indications
It is used for short-term treatment of patients with insomnia. Insomnia can be described as a difficulty falling asleep, frequent awakening, early awakenings or a combination of each. Flurazepam is a long acting benzodiazepine and is sometimes used in patients who have difficulty in maintaining sleep. Intermediate half life benzodiazepines are also useful for patients with difficulty in maintaining sleep (eg. loprazolam, lormetazepam, temazepam). Hypnotics should only be used on a short term basis or in those with chronic insomnia on an occasional basis.[1]
Side effects
The most common adverse effects are dizziness, drowsiness, lightheadedness, and ataxia. Flurazepam has abuse potential and should never be used with alcohol or any other substance that can cause drowsiness. Additive and possibly fatal results may occur. Flurazepam users should only take this drug strictly as prescribed, and should only be taken directly before the user plans on sleeping a full night. Next day drowsiness is common.
Tolerance, dependence and withdrawal problems
Main article: Benzodiazepine withdrawal syndrome
A review paper found that long term use of flurazepam is associated with drug tolerance, drug dependence, rebound insomnia and CNS related adverse effects. Flurazepam is best used for a short time period and at the lowest possible dose to avoid complications associated with long term use. Non-pharmacological treatment options however, were found to have sustained improvements in sleep quality.[2] Flurazepam and other benzodiazepines such as fosazepam, and nitrazepam lost some of their effect after seven days administration in psychogeriatric patients.[3] Flurazepam shares cross tolerance with barbiturates and barbiturates can easily be substituted by flurazepam in those who are habituated to barbiturate sedative hypnotics.[4]
After discontinuation of flurazepam a rebound effect or benzodiazepine withdrawal syndrome may occur about four days after discontinuation of medication.[5]
Elderly
An extensive review of the medical literature regarding the management of insomnia and the elderly found that there is considerable evidence of the effectiveness and durability of non-drug treatments for insomnia in adults of all ages and that these interventions are underutilized. Compared with the benzodiazepines including flurazepam, the nonbenzodiazepine sedative-hypnotics appeared to offer few, if any, significant clinical advantages in efficacy in elderly persons. Tolerability in elderly patients, however, is improved marginally in that benzodiazepines have moderately higher risks of falls, memory problems, and disinhibition ("Paradoxical agitation") when compared to non-benzodiazepine sedatives. It was found that newer agents with novel mechanisms of action and improved safety profiles, such as the melatonin agonists, hold promise for the management of chronic insomnia in elderly people. Chronic use of sedative-hypnotic drugs for the management of insomnia does not have an evidence base and has been discouraged due to concerns including potential adverse drug effects as cognitive impairment (anterograde amnesia), daytime sedation, motor incoordination, and increased risk of motor vehicle accidents and falls. In addition, the effectiveness and safety of long-term use of sedative hypnotics has been determined to be no better than placebo after 3 months of therapy and worse than placebo after 6 months of therapy. (NEJM, 1983, 1994, et seq.)[6]
Pharmacology
Flurazepam is a "classical" benzodiazepine, other classical benzodiazepines include; diazepam, clonazepam, oxazepam, lorazepam, nitrazepam, bromazepam and clorazepate.[7] Flurazepam generates an active metabolite with a very long elimination half life of 40-250 hours. Residual 'hangover' effects after nighttime administration of flurazepam, such as sleepiness, impaired psychomotor and cognitive functions, may persist into the next day, which may impair the ability of users to drive safely and increase risks of falls and hip fractures.[8]
Flurazepam is lipophilic, is metabolised hepatically via oxidative pathways. The main pharmacological effect of flurazepam is to increase the effect of GABA at the GABAA receptor via binding to the benzodiazepine site on the GABAA receptor causing an increase influx of chloride ions into the GABAA neuron.[9][10] Flurazepam is a unique benzodiazepine in that it is a partial agonist of benzodiazepine receptors whereas other benzodiazepines are full agonists of benzodiazepine receptors.[11]
Flurazepam is contraindicated in pregnancy. It is recommended to withdraw flurazepam during breast feeding, as flurazepam is excreted in breast milk.[12]
Drug misuse
See also: Benzodiazepine drug misuse
Flurazepam is a drug with the potential for misuse. Two types of drug misuse can occur either recreational misuse is where the drug is taken to achieve a high or when the drug is continued long term against medical advice.[13]
Legal status
Flurazepam is a Schedule IV drug under the Convention on Psychotropic Substances.[2]
See also
References
- ^ Rickels K. (1986). "The clinical use of hypnotics: indications for use and the need for a variety of hypnotics". Acta Psychiatrica Scandinavica Suppl. 332: 132–41. doi:. PMID 2883820.
- ^ Kirkwood CK (1999). "Management of insomnia". J Am Pharm Assoc (Wash) 39 (5): 688–96; quiz 713–4. PMID 10533351.
- ^ Viukari M; Linnoila M, Aalto U. (January 1978). "Efficacy and side effects of flurazepam, fosazepam, and nitrazepam as sleeping aids in psychogeriatric patients". Acta Psychiatrica Scandinavica 57 (1): 27–35. doi:. PMID 24980.
- ^ Rooke KC. (1976). "The use of flurazepam (dalmane) as a substitute for barbiturates and methaqualone/diphenhydramine (mandrax) in general practice". J Int Med Res. 4 (5): 355–9. PMID 18375.
- ^ Hindmarch I. (November 1977). "A repeated dose comparison of three benzodiazepine derivative (nitrazepam, flurazepam and flunitrazepam) on subjective appraisals of sleep and measures of psychomotor performance the morning following night-time medication". Acta Psychiatrica Scandinavica 56 (5): 373–81. doi:. PMID 22990.
- ^ Bain KT (June 2006). "Management of chronic insomnia in elderly persons". Am J Geriatr Pharmacother 4 (2): 168–92. doi:. PMID 16860264.
- ^ Braestrup C; Squires RF. (1 April 1978). "Pharmacological characterization of benzodiazepine receptors in the brain". Eur J Pharmacol 48 (3): 263–70. doi:. PMID 639854.
- ^ Vermeeren A. (2004). "Residual effects of hypnotics: epidemiology and clinical implications". CNS Drugs. 18 (5): 297–328. doi:. PMID 15089115.
- ^ Oelschläger H. (July 4, 1989). "[Chemical and pharmacologic aspects of benzodiazepines]". Schweiz Rundsch Med Prax. 78 (27-28): 766–72. PMID 2570451.
- ^ Lehoullier PF, Ticku MK (March 1987). "Benzodiazepine and beta-carboline modulation of GABA-stimulated 36Cl-influx in cultured spinal cord neurons". Eur. J. Pharmacol. 135 (2): 235–8. doi:. PMID 3034628.
- ^ Chan CY; Farb DH (01 September 1985). "Modulation of neurotransmitter action: control of the gamma-aminobutyric acid response through the benzodiazepine receptor" (PDF). J Neurosci 5 (9): 2365–73. PMID 2863335. http://www.jneurosci.org/cgi/reprint/5/9/2365.
- ^ Olive G; Dreux C. (January 1977). "Pharmacologic bases of use of benzodiazepines in peréinatal medicine". Arch Fr Pediatr. 34(1): 74–89. PMID 851373.
- ^ Griffiths RR, Johnson MW (2005). "Relative abuse liability of hypnotic drugs: a conceptual framework and algorithm for differentiating among compounds". J Clin Psychiatry 66 Suppl 9: 31–41. PMID 16336040.
External links
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| Drug Info. Gold Standard. Copyright © 2008 by Gold Standard. All rights reserved. Read more |
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