Linked Life Data

Temazepam (Capsule)

Source:http://www4.wiwiss.fu-berlin.de/dailymed/resource/drugs/2620

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Temazepam (Capsule)
dailymed-instance:dosage
While the recommended usual adult dose is 15 mg before retiring, 7.5 mg may be sufficient for some patients, and others may need 30 mg. In transient insomnia, a 7.5 mg dose may be sufficient to improve sleep latency. In elderly or debilitated patients, it is recommended that therapy be initiated with 7.5 mg until individual responses are determined.
dailymed-instance:descripti...
Temazepam is a benzodiazepine hypnotic agent. The chemical name is 7-chloro-1,3-dihydro-3-hydroxy-1-methyl-5-phenyl-2H-1,4-benzodiazepin-2-one. Its structural formula may be represented as follows: Temazepam is a white, crystalline substance, very slightly soluble in water and sparingly soluble in alcohol, USP. Temazepam capsules, 15 mg and 30 mg, are for oral administration. Each capsule contains colloidal silicon dioxide, gelatin, magnesium stearate, microcrystalline cellulose, powdered cellulose, sodium lauryl sulfate, titanium dioxide, FD&C yellow #6. Additionally, the 30 mg capsule contains D&C yellow #10.
dailymed-instance:clinicalP...
Pharmacokinetics: In a single and multiple dose absorption, distribution, metabolism, and excretion (ADME) study, usingH labeled drug, temazepam was well absorbed and found to have minimal (8%) first pass metabolism. There were no active metabolites formed and the only significant metabolite present in blood was the O-conjugate. The unchanged drug was 96% bound to plasma proteins. The blood level decline of the parent drug was biphasic with the short half-life ranging from 0.4 to 0.6 hours and the terminal half-life from 3.5 to 18.4 hours (mean 8.8 hours), depending on the study population and method of determination. Metabolites were formed with a half-life of 10 hours and excreted with a half-life of approximately 2 hours. Thus, formation of the major metabolite is the rate limiting step in the biodisposition of temazepam. There is no accumulation of metabolites. A dose-proportional relationship has been established for the area under the plasma concentration/time curve over the 15 to 30 mg dose range. Temazepam was completely metabolized through conjugation prior to excretion; 80% to 90% of the dose appeared in the urine. The major metabolite was the O-conjugate of temazepam (90%); the O-conjugate of N-desmethyl temazepam was a minor metabolite (7%).<br/>Bioavailability, Induction, and Plasma Levels: Following ingestion of a 30 mg temazepam capsule, measurable plasma concentrations were achieved 10 to 20 minutes after dosing with peak plasma levels ranging from 666 to 982 ng/mL (mean 865 ng/mL) occurring approximately 1.2 to 1.6 hours (mean 1.5 hours) after dosing. In a 7 day study, in which subjects were given a 30 mg capsule of a marketed bioequivalent temazepam product 1 hour before retiring, steady state (as measured by the attainment of maximal trough concentrations) was achieved by the third dose. Mean plasma levels of temazepam (for days 2 to 7) were 260��210 ng/mL at 9 hours and 75��80 ng/mL at 24 hours after dosing. A slight trend toward declining 24 hour plasma levels was seen after day 4 in the study, however, the 24 hour plasma levels were quite variable. At a dose of 30 mg once-a-day for 8 weeks, no evidence of enzyme induction was found in man.<br/>Elimination Rate of Benzodiazepine Hypnotics and Profile of Common Untoward Effects: The type and duration of hypnotic effects and the profile of unwanted effects during administration of benzodiazepine hypnotics may be influenced by the biologic half-life of the administered drug and for some hypnotics, the half-life of any active metabolites formed. Benzodiazepine hypnotics have a spectrum of half-lives from short (<4 hours) to long (>20 hours). When half-lives are long, drug (and for some drugs their active metabolites) may accumulate during periods of nightly administration and be associated with impairments of cognitive and/or motor performance during waking hours; the possibility of interaction with other psychoactive drugs or alcohol will be enhanced. In contrast, if half-lives are shorter, drug (and, where appropriate, its active metabolites) will be cleared before the next dose is ingested, and carry-over effects related to excessive sedation or CNS depression should be minimal or absent. However, during nightly use for an extended period, pharmacodynamic tolerance or adaptation to some effects of benzodiazepine hypnotics may develop. If the drug has a short elimination half-life, it is possible that a relative deficiency of the drug, or, if appropriate, its active metabolites (i.e., in relationship to the receptor site) may occur at some point in the interval between each night's use. This sequence of events may account for 2 clinical findings reported to occur after several weeks of nightly use of rapidly eliminated benzodiazepine hypnotics, namely, increased wakefulness during the last third of the night, and the appearance of increased signs of daytime anxiety.<br/>Controlled Trials Supporting Efficacy: Temazepam improved sleep parameters in clinical studies. Residual medication effects ("hangover") were essentially absent. Early morning awakening, a particular problem in the geriatric patient, was significantly reduced. Patients with chronic insomnia were evaluated in 2 week, placebo controlled sleep laboratory studies with temazepam at doses of 7.5 mg, 15 mg and 30 mg, given 30 minutes prior to bedtime. There was a linear dose-response improvement in total sleep time and sleep latency, with significant drug-placebo differences at 2 weeks occurring only for total sleep time at the 2 higher doses, and for sleep latency only at the highest dose. In these sleep laboratory studies, REM sleep was essentially unchanged and slow wave sleep was decreased. No measurable effects on daytime alertness or performance occurred following temazepam treatment or during the withdrawal period, even though a transient sleep disturbance in some sleep parameters was observed following withdrawal of the higher doses. There was no evidence of tolerance development in the sleep laboratory parameters when patients were given temazepam nightly for at least 2 weeks. In addition, normal subjects with transient insomnia associated with first night adaptation to the sleep laboratory were evaluated in 24 hour, placebo controlled sleep laboratory studies with temazepam at doses of 7.5 mg, 15 mg and 30 mg, given 30 minutes prior to bedtime. There was a linear dose-response improvement in total sleep time, sleep latency and number of awakenings, with significant drug-placebo differences occurring for sleep latency at all doses, for total sleep time at the 2 higher doses and for number of awakenings only at the 30 mg dose.
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dailymed-instance:contraind...
Benzodiazepines may cause fetal damage when administered during pregnancy. An increased risk of congenital malformations associated with the use of diazepam and chlordiazepoxide during the first trimester of pregnancy has been suggested in several studies. Transplacental distribution has resulted in neonatal CNS depression following the ingestion of therapeutic doses of a benzodiazepine hypnotic during the last weeks of pregnancy. Reproduction studies in animals with temazepam were performed in rats and rabbits. In a perinatal-postnatal study in rats, oral doses of 60 mg/kg/day resulted in increasing nursling mortality. Teratology studies in rats demonstrated increased fetal resorptions at doses of 30 and 120 mg/kg in one study and increased occurrence of rudimentary ribs, which are considered skeletal variants, in a second study at doses of 240 mg/kg or higher. In rabbits, occasional abnormalities such as exencephaly and fusion or asymmetry of ribs were reported without dose relationship. Although these abnormalities were not found in the concurrent control group, they have been reported to occur randomly in historical controls. At doses of 40 mg/kg or higher, there was an increased incidence of the 13th rib variant when compared to the incidence in concurrent and historical controls. Temazepam is contraindicated in pregnant women. If there is a likelihood of the patient becoming pregnant while receiving temazepam, she should be warned of the potential risk to the fetus. Patients should be instructed to discontinue the drug prior to becoming pregnant. The possibility that a woman of childbearing potential may be pregnant at the time of institution of therapy should be considered.
dailymed-instance:supply
Temazepam Capsules USP, are available containing either 15 mg or 30 mg of temazepam. The 15 mg product is a peach capsule imprinted with MYLAN 4010. They are available as follows: NDC 0378-4010-01bottles of 100 capsules NDC 0378-4010-05bottles of 500 capsules The 30 mg product is a yellow capsule imprinted with MYLAN 5050. They are available as follows: NDC 0378-5050-01bottles of 100 capsules NDC 0378-5050-05bottles of 500 capsules STORE AT CONTROLLED ROOM TEMPERATURE 15��to 30��C (59��to 86��F). PROTECT FROM LIGHT. Dispense in a tight, light-resistant container as defined in the USP using a child-resistant closure.
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dailymed-instance:overdosag...
Manifestations of acute overdosage of temazepam can be expected to reflect the CNS effects of the drug and include somnolence, confusion, and coma, with reduced or absent reflexes, respiratory depression, and hypotension. The oral LDof temazepam was 1963 mg/kg in mice, 1833 mg/kg in rats, and>2400 mg/kg in rabbits.<br/>Treatment: If the patient is conscious, vomiting should be induced mechanically or with emetics. Gastric lavage should be employed utilizing concurrently a cuffed endotracheal tube if the patient is unconscious to prevent aspiration and pulmonary complications. Maintenance of adequate pulmonary ventilation is essential. The use of pressor agents intravenously may be necessary to combat hypotension. Fluids should be administered intravenously to encourage diuresis. The value of dialysis has not been determined. If excitation occurs, barbiturates should not be used. It should be borne in mind that multiple agents may have been ingested. Flumazenil, a specific benzodiazepine receptor antagonist, is indicated for the complete or partial reversal of the sedative effects of benzodiazepines and may be used in situations when an overdose with a benzodiazepine is known or suspected. Prior to the administration of flumazenil, necessary measures should be instituted to secure airway, ventilation, and intravenous access. Flumazenil is intended as an adjunct to, not as a substitute for, proper management of benzodiazepine overdose. Patients treated with flumazenil should be monitored for re-sedation, respiratory depression, and other residual benzodiazepine effects for an appropriate period after treatment. The prescriber should be aware of a risk of seizure in association with flumazenil treatment, particularly in long-term benzodiazepine users and in cyclic antidepressant overdose. The complete flumazenil package insert including CONTRAINDICATIONS, WARNINGS, and PRECAUTIONS should be consulted prior to use. Up-to-date information about the treatment of overdose can often be obtained from a certified Regional Poison Control Center. Telephone numbers of certified Regional Poison Control Centers are listed in the Physicians' Desk Reference.
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Temazepam
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Temazepam (Capsule)
dailymed-instance:adverseRe...
During controlled clinical studies in which 1076 patients received temazepam at bedtime, the drug was well tolerated. Side effects were usually mild and transient. Adverse reactions occurring in 1% or more of patients are presented in the following table: The following adverse events have been reported less frequently (0.5% to 0.9%): Central Nervous System: anorexia, ataxia, equilibrium loss, tremor, increased dreaming Cardiovascular: dyspnea, palpitations Gastrointestinal: vomiting Musculoskeletal: backache Special Senses: hyperhidrosis, burning eyes Amnesia, hallucinations, horizontal nystagmus and paradoxical reactions including restlessness, overstimulation and agitation were rare (less than 0.5%).
dailymed-instance:indicatio...
Temazepam is indicated for the short-term treatment of insomnia (generally 7 to 10 days). For patients in whom the drug is used for more than 2 to 3 weeks, periodic reevaluation is recommended to determine whether there is a continuing need. For patients with short-term insomnia, instructions in the prescription should indicate that temazepam should be used for short periods of time (7 to 10 days). Temazepam should not be prescribed in quantities exceeding a 1-month supply. Insomnia is characterized by complaints of difficulty in falling asleep, frequent nocturnal awakenings, and/or early morning awakenings. Both sleep laboratory and outpatient studies provide support for the effectiveness of temazepam administered 30 minutes before bedtime in decreasing sleep latency and improving sleep maintenance in patients with chronic insomnia. In addition, sleep laboratory studies have confirmed similar effects in normal subjects with transient insomnia .
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Temazepam