What Is The Elimination Half-Life Of Diazepam In The Elderly Population?
- The initial dispersion phase is followed by a lengthy terminal elimination phase that lasts for several weeks (half-life up to 48 hours).
- The active metabolite N-desmethyldiazepam has a terminal elimination half-life of up to 100 hours, making it one of the longest active metabolites known.
- Diazepam and its metabolites are eliminated mostly in the urine, where they are found primarily as glucuronide conjugates, which are toxic to the kidneys.
9In elderly individuals, the volume of diazepam dispersion increases by about double, compared to younger patients. When compared to younger individuals, the elimination half-life is extended from 24 hours in young patients to around 90 hours in older patients. Changes that occur with age Compounds that are water soluble:
What is the half life of hellodiazepam?
Verified Hello, Diazepam is a longer-acting drug with a terminal elimination half-life of around 48 hours. However, the terminal elimination half-life of the active metabolite N-desmethyldiazepam is estimated to be up to 100 hours or more in some cases. Terminal elimination half life may be significantly longer if the medication is used on a regular basis.
Why does diazepam have a longer elimination half-time than lorazepam?
- The elimination half-time of diazepam metabolism is extended in the presence of cirrhosis of the liver and in the elderly population, owing to an elevated Vd of high lipid solubility in the presence of these conditions.
- Diazepam has a longer elimination half-life than lorazepam, but it has a shorter duration of effect than lorazepam because it dissociates from the GABAA receptor more quickly than lorazepam.
How long does it take for diazepam to leave your system?
- When eating, oral intake can range from 15 minutes to 2.5 hours (1.25 hours when fasting; 2.5 hours when eating) (Greenblatt 1989b) Pediatric patients should be sedated for 60 to 120 minutes (Krauss 2006) 15 to 30 minutes in the status epilepticus It should be noted that diazepam accumulates with repeated administration, resulting in a modest prolongation of the terminal elimination half-life.
What happens to diazepam metabolism as we age?
The metabolism of diazepam. Cirrhosis of the liver is associated with increases in the elimination half-time of diazepam of up to fivefold, which rises gradually with increasing age, which is consistent with the greater susceptibility of these individuals to the sedative effects of the medication.
What is the half-life of diazepam in the elderly?
2 Following intravenous injection of 14C-labeled diazepam, the half-life and volume of distribution in the elderly were about twice larger than similar estimates in younger participants (mean standard deviation, 71.527.6 h versus 44.516.5 h and 1.390.32 g kg1, respectively).
What is the half-life of a benzodiazepine in an elderly patient?
Alprazolam, which has an intermediate half-life of 6 to 20 hours, may provide therapeutic benefit in some elderly people, but diazepam, which has a longer half-life of 24 hours, is contraindicated in this population.
Can elderly take diazepam?
Adults: 2 to 10 milligrams (mg) taken twice or four times daily. Older adults—At start, 2 to 2.5 mg once or twice a day, one or two times a week. If necessary, your doctor may decide to raise your dose. Children 6 months and older: At start, 1 to 2.5 mg 3 or 4 times per day for the first 6 months.
Is drug half-life longer in older adults?
As we get older, we experience significant changes in our bodily composition. Lipophilic medications may have a greater volume of distribution (Vd) due to their longer half-lives, whereas water-soluble pharmaceuticals have a smaller Vd due to their shorter half-lives.
What is the duration of diazepam?
When taken intravenously, diazepam begins to work within 1 to 3 minutes, but the beginning of effect after oral administration spans between 15 and 60 minutes. Diazepam has a lengthy duration of effect, with a duration of action of more than 12 hours in some cases.
Which benzo has the shortest half-life?
| Drug | Half-life | Latency |
|---|---|---|
| Benzodiazepine hypnotics | ||
| Triazolam | Short | ! |
| Midazolam | Short | ! |
| Brotizolam | Short | ! |
What is flurazepam used to treat?
- Flurazepam is a medication that is used to treat insomnia (trouble with sleeping).
- This medication assists you in falling asleep more quickly and staying asleep throughout the night.
- Flurazepam is classified as a benzodiazepine.
- Benzodiazepines are a class of medications known as central nervous system (CNS) depressants, which are medications that work by slowing the nervous system’s activity.
What is the difference between lorazepam and diazepam?
To be used as a sedative, 10 mg of diazepam is comparable to 22.5 mg of lorazepam. Diazepam is more readily absorbed after oral administration than after intravenous administration, however this is not true for lorazepam. Following the administration of diazepam, the clinical impact and amnesia begin more quickly, but remain for a longer period of time.
Which benzodiazepine is best for elderly?
Appropriate usage refers to the administration of very low dosages of short-acting benzodiazepines, such as lorazepam, oxazepam, or temazepam on a daily or bi-daily basis (0.5 mg or less).
What is the half-life of temazepam?
Peak plasma concentrations are reached within 3 hours following oral administration of a dosage of 30 mg, with a typical half-life of 10 to 15 hours. In this way, temazepam is taken up more slowly and digested more quickly than flurazepam, which is the only other benzodiazepine medication available in the United States that is especially designed for insomnia treatment.
What are the contraindications of diazepam?
- Who should not be prescribed DIAZEPAM? low levels of albumin proteins in the blood
- drunkenness with alcohol
- drug misuse
- depression
- myasthenia gravis, a skeletal muscular illness
- and other conditions
- Wide-angle glaucoma
- closed-angle glaucoma
- deterioration of a devastating chronic lung disease known as COPD
- and other conditions.
What is the most common side effect of diazepam?
It is possible to experience drowsiness, dizziness, fatigue, blurred vision, or unsteadiness. If any of these symptoms persist or worsen, notify your doctor or pharmacist as soon as possible. Please keep in mind that this medicine has been recommended by your doctor because he or she has determined that the benefit to you outweighs the risk of adverse effects.
Who Cannot diazepam?
In babies younger than 6 months of age, diazepam should not be given to the child. if you have or have had open-angle glaucoma (an rise in internal eye pressure that destroys the optic nerve), depression or other mental disorder, seizures, heart problems, or any other medical condition, notify your doctor.
What is the first pass effect of diazepam?
The absorption of diazepam, a nonbasic lipophilic amine, was found to be 30% during the first pass through the human lung, which was much less than the uptake of verapamil, which was shown to be 50%. Only 14 percent of the injected medication collected in the lung during the first pass while using thiopental, an acidic lipophilic barbiturate.
What happens to the half-life of lipophilic drugs in patients who are geriatric compared with younger patients?
Body fat normally grows with age, but total body water generally declines. High-lipophilic medicines such as diazepam and chlordiazepoxide (for example) have a greater volume of distribution in the presence of fat, which may result in a significant increase in their elimination half-lives.
How does ageing related changes affect medication use in older people?
As we get older, physiological changes might have an impact on the way our bodies metabolize medications, perhaps leading to unpleasant responses. Older adults are more likely than younger people to be taking many drugs (known as ″polypharmacy″), which increases the likelihood that pharmaceuticals would be implicated in hospitalization.