Source:http://www4.wiwiss.fu-berlin.de/dailymed/resource/drugs/1318
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Valium (Tablet)
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| dailymed-instance:dosage |
Dosage should be individualized for maximum beneficial
effect. While the usual daily dosages given below will meet the needs
of most patients, there will be some who may require higher doses.
In such cases dosage should be increased cautiously to avoid adverse
effects.
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| dailymed-instance:descripti... |
Valium (diazepam) is a benzodiazepine derivative.
The chemical name of diazepam is 7-chloro-1,3-dihydro-1-methyl-5-phenyl-2H-1,4-benzodiazepin-2-one.
It is a colorless to light yellow crystalline compound, insoluble
in water. The empirical formula is CHClNO and the molecular weight is 284.75. The structural formula
is as follows: Valium is available for oral
administration as tablets containing 2 mg, 5 mg or 10 mg diazepam.
In addition to the active ingredient diazepam, each tablet contains
the following inactive ingredients: anhydrous lactose, corn starch,
pregelatinized starch and calcium stearate with the following dyes:
5-mg tablets contain FD&C Yellow No. 6 and D&C Yellow No.
10; 10-mg tablets contain FD&C Blue No. 1. Valium 2-mg tablets
contain no dye.
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| dailymed-instance:clinicalP... |
Diazepam is a benzodiazepine
that exerts anxiolytic, sedative, muscle-relaxant, anticonvulsant
and amnestic effects. Most of these effects are thought to result
from a facilitation of the action of gamma aminobutyric acid (GABA),
an inhibitory neurotransmitter in the central nervous system.<br/>Pharmacokinetics:<br/>Absorption: After oral administration>90% of diazepam is absorbed
and the average time to achieve peak plasma concentrations is 1���1.5 hours with a range of 0.25 to 2.5 hours. Absorption is delayed
and decreased when administered with a moderate fat meal. In the presence
of food mean lag times are approximately 45 minutes as compared with
15 minutes when fasting. There is also an increase in the average
time to achieve peak concentrations to about 2.5 hours in the presence
of food as compared with 1.25 hours when fasting. This results in
an average decrease in Cof 20% in addition to a 27%
decrease in AUC (range 15% to 50%) when administered with food.<br/>Distribution: Diazepam and its metabolites are highly bound to
plasma proteins (diazepam 98%). Diazepam and its metabolites cross
the blood-brain and placental barriers and are also found in breast
milk in concentrations approximately one tenth of those in maternal
plasma (days 3 to 9 post-partum). In young healthy males, the volume
of distribution at steady-state is 0.8 to 1.0 L/kg. The decline in
the plasma concentration-time profile after oral administration is
biphasic. The initial distribution phase has a half-life of approximately
1 hour, although it may range up to>3 hours.<br/>Metabolism: Diazepam is N-demethylated by CYP3A4 and 2C19 to
the active metabolite N-desmethyldiazepam, and is hydroxylated by
CYP3A4 to the active metabolite temazepam. N-desmethyldiazepam and
temazepam are both further metabolized to oxazepam. Temazepam and
oxazepam are largely eliminated by glucuronidation.<br/>Elimination: The initial distribution phase is followed by a prolonged
terminal elimination phase (half-life up to 48 hours). The terminal
elimination half-life of the active metabolite N-desmethyldiazepam
is up to 100 hours. Diazepam and its metabolites are excreted mainly
in the urine, predominantly as their glucuronideconjugates. The clearance
of diazepam is 20 to 30 mL/min in young adults. Diazepam accumulates
upon multiple dosing and there is some evidence that the terminal
elimination half-life is slightly prolonged.<br/>Pharmacokinetics in Special Populations:<br/>Children: In children 3 - 8 years old the mean half-life of
diazepam has been reported to be 18 hours.<br/>Newborns: In full term infants, elimination half-lives around
30 hours have been reported, with a longer average half-life of 54
hours reported in premature infants of 28 - 34 weeks gestational age
and 8 - 81 days post-partum. In both premature and full term infants
the active metabolite desmethyldiazepam shows evidence of continued
accumulation compared to children. Longer half-lives in infants may
be due to incomplete maturation of metabolic pathways.<br/>Geriatric: Elimination half-life increases by approximately
1 hour for each year of age beginning with a half-life of 20 hours
at 20 years of age. This appears to be due to an increase in volume
of distribution with age and a decrease in clearance. Consequently,
the elderly may have lower peak concentrations, and on multiple dosing
higher trough concentrations. It will also take longer to reach steady-state.
Conflicting information has been published on changes of plasma protein
binding in the elderly. Reported changes in free drug may be due to
significant decreases in plasma proteins due to causes other than
simply aging.<br/>Hepatic Insufficiency: In mild and moderate cirrhosis, average half-life
is increased. The average increase has been variously reported from
2-fold to 5-fold, with individual half-lives over 500 hours reported.
There is also an increase in volume of distribution, and average clearance
decreases by almost half. Mean half-life is also prolonged with hepatic
fibrosis to 90 hours (range 66 - 104 hours), with chronic active hepatitis
to 60 hours (range 26 - 76 hours), and with acute viral hepatitis
to 74 hours (range 49 - 129). In chronic active hepatitis, clearance
is decreased by almost half.
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| dailymed-instance:contraind... |
Valium is contraindicated in patients with a known
hypersensitivity to diazepam and, because of lack of sufficient clinical
experience, in pediatric patients under 6 months of age. Valium is
also contraindicated in patients with myasthenia gravis, severe respiratory
insufficiency, severe hepatic insufficiency, and sleep apnea syndrome.
It may be used in patients with open-angle glaucoma who are receiving
appropriate therapy, but is contraindicated in acute narrow-angle
glaucoma.
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| dailymed-instance:supply |
For oral administration, Valium is supplied as round,
flat-faced scored tablets with V-shaped perforation and beveled edges.
Valium is available as follows: 2 mg, white - bottles of 100 (NDC
0140-0004-01); 5 mg, yellow - bottles of 100 (NDC 0140-0005-01) and
500 (NDC 0140-0005-14); 10 mg, blue - bottles of 100 (NDC 0140-0006-01)
and 500 (NDC0140-0006-14). Engraved on tablets: 2 mg���2 VALIUM (front) ROCHE (twice on scored side) 5 mg���5 VALIUM (front) ROCHE (twice on scored side) 10 mg���10 VALIUM (front) ROCHE (twice on scored side)<br/>STORAGE: Store at room temperature 59��to 86��F (15��to 30��C). Dispense in tight, light-resistant containers as defined
in USP/NF.
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| dailymed-instance:genericDr... | |
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Overdose of benzodiazepines is usually manifested
by central nervous system depression ranging from drowsiness to coma.
In mild cases, symptoms include drowsiness, confusion, and lethargy.
In more serious cases, symptoms may include ataxia, diminished reflexes,
hypotonia, hypotension, respiratory depression, coma (rarely), and
death (veryrarely). Overdose of benzodiazepines in combination with
other CNS depressants (including alcohol) may be fatal and should
be closely monitored.
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| dailymed-instance:genericMe... |
diazepam
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| dailymed-instance:fullName |
Valium (Tablet)
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| dailymed-instance:warning |
Valium is not recommended in the treatment of psychotic
patients and should not be employed instead of appropriate treatment. Since Valium has a central nervous system depressant effect,
patients should be advised against the simultaneous ingestion of alcohol
and other CNS-depressant drugs during Valium therapy. As with other agents that have anticonvulsant activity, when Valium
is used as an adjunct in treating convulsive disorders, the possibility
of an increase in the frequency and/or severity of grand mal seizures
may require an increase in the dosage of standard anticonvulsant medication.
Abrupt withdrawal of Valium in such cases may also be associated with
a temporary increase in the frequency and/or severity of seizures.<br/>Pregnancy: An increased risk of congenital malformations and
other developmental abnormalities associated with the use of benzodiazepine
drugs during pregnancy has been suggested. There may also be non-teratogenic
risks associated with the use of benzodiazepines during pregnancy.
There have been reports of neonatal flaccidity, respiratory and feeding
difficulties, and hypothermia in children born to mothers who have
been receiving benzodiazepines late in pregnancy. In addition, children
born to mothers receiving benzodiazepines on a regular basis late
in pregnancy may be at some risk of experiencing withdrawal symptoms
during the postnatal period. Diazepam has been
shown to be teratogenic in mice and hamsters when given orally at
daily doses of 100 mg/kg or greater (approximately eight times the
maximum recommended human dose [MRHD=1 mg/kg/day] or greater on a
mg/mbasis). Cleft palate and encephalopathy are the most
common and consistently reported malformations produced in these species
by administration of high, maternally toxic doses of diazepam during
organogenesis. Rodent studies have indicated that prenatal exposure
to diazepam doses similar to those used clinically can produce long-term
changes in cellular immune responses, brain neurochemistry, and behavior. In general, the use of diazepam in women of childbearing
potential, and more specifically during known pregnancy, should be
considered only when the clinical situation warrants the risk to the
fetus. The possibility that a woman of childbearing potential may
be pregnant at the time of institution of therapy should be considered.
If this drug is used during pregnancy, or if the patient becomes pregnant
while taking this drug, the patient should be apprised of the potential
hazard to the fetus. Patients should also be advised that if they
become pregnant during therapy or intend to become pregnant they should
communicate with their physician aboutthe desirability of discontinuing
the drug.<br/>Labor and Delivery: Special care must be taken when Valium is used during
labor and delivery, as high single doses may produce irregularities
in the fetal heart rate and hypotonia, poor sucking, hypothermia,
and moderate respiratory depression in the neonates. With newborn
infants it must be remembered that the enzyme system involved in the
breakdown of the drug is not yet fully developed (especially in premature
infants).<br/>Nursing Mothers: Diazepam passes into breast milk. Breastfeeding is
therefore not recommended in patients receiving Valium.
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| dailymed-instance:name |
Valium
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