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Diazepam was the second benzodiazepine to be invented after chlordiazepoxide (Librium) in 1960 by DR. It was the most popular medication prescribed by psychiatrist, anesthesiologist and family practitioner.
Diazepam has no effect on GABA levels and no effect on glutamate decarboxylase activity, but has a slight effect on gamma-aminobutyric acid transaminase activities. Anxiolytic effect of diazepam is a result of direct inhibitory action on areas of the limbic system, thalamus and hypothalamus. The muscle relaxant properties of diazepam are produced via inhibition of polysynaptic pathways in the ventral horn of spinal cord.
Diazepam undergoes oxidative metabolism by demethylation, hydroxylation and glucoronidation in the liver by cytochrome P 450 enzyme system. Diazepam does not increase or decrease hepatic enzyme activities, and does not alter the metabolism of other compounds.
Agents that have an effect on hepatic cytochrome P450 pathways or conjugation can alter the rate of diazepam metabolism. Most of the drug is metabolized to inactive or active metabolites and very little diazepam is excreted unchanged.
Because of these active metabolites, the serum values of diazepam alone are not useful in predicting the effects of the drug. Diazepam has a biphasic ? life of about one to three days, and two to seven days for the active metabolite desmethyldiazepam.
Inhibition of cyclic 450 enzymes by following medications prolongs the metabolism of benzodiazepines.
Stimulation of liver enzyme by following medications leads to rapid metabolism of diazepam.Increase rate of metabolism causes decreases drug levels and therapeutic effects.
When administered orally, it is rapidly absorbed by intestinal mucosa and has a relatively fast onset of action. Diazepam is highly lipid-soluble, and is widely distributed throughout the body after administration.
Continuous daily therapeutic dosage of diazepam will quickly build up to a high concentration in the body. Food that alkalinize the urine can lead to slower absorption and elimination of diazepam, thus increases benzodiazepine plasma levels and activities. Levodopa- benzodiazepine antagonizes action effects of levodopa on dopamine receptors (antagonist).
Anterograde (extended forward) amnesia (loss of memory)- patient may not remember events or experiences during the brief period following taking medication. Tolerance and dependence- Frequent and prolonged treatment of Benzodiazepine results in increase tolerance and dependence to Benzodiazepine.
Withdrawal- Abrupt (sudden) withdrawl of Benzodiazepine causes severe withdrawl symptoms, which could be life threatening. Prolonged ? life- ? life is 70 days, thus residual drug remains in the body for prolonged period. Recovery from withdrawal symptoms without any active treatment takes approximately 4 to 6 months. Anaphylaxis (Hypersensitivity or Severe Generalized Allergic Reaction)- Anaphylaxis is rarely seen following Benzodiazepine treatment. Psychological or physical dependence can develop within a few weeks or months of prescription.
Pseudoaddiction is developed when therapeutic dosage does not give same clinical benefit as before.
Patient will be considered as drug addict since he is running short of medications frequently. Taking other sedatives or opioids to overcome withdrawal or benzodiazepine craving symptoms. Frequent visits to physician office claiming insomnia and anxiety are not responding in spite to higher dosage. Mild withdrawal symptoms after discontinuation of benzodiazepine is observed in few patients treated for short period. Patient continues with benzodiazepine during pregnancy because of dependence and necessity of continuation of treatment.
Blood examination and urine drug test is mandatory and necessary to monitor patient's prescription behavior to deter abuse and sharing medications with family members and colleagues. In ER or hospital similar studies are performed to find out medico legalcause of death in case patient is receiving benzodiazepines medications. Insomnia is a psychiatric illness seen in-patientsecondary to chronic tobacco smoking, excessive caffeine consumption and taking recreational stimulants.
Diazepam leads to addiction in most of the patients after continuous use for prolonged period as therapeutic medications. Most abuse benzodiazepine in order of highest to lowest are Alprazolam (Xanax), Clonazepam (Klonopin), Lorazepam (Ativan) and Diazepam (Valium). Diazepam is classified as schedule 4-control substance and has low potential for abuse relative to the drugs or other substances in schedule III. Clonazepam works by increasing the effects of GABA, a neurotransmitter that moderates the movement of nerve signals in the brain. The Food and Drug Administration (FDA) approved clonazepam in 1975 under the brand name Klonopin for the Roche drug company.


Clonazepam is a controlled substance because it’s possible for people to abuse the drug or become dependent on it. In 2011 alone, there were 76,557 emergency room visits resulting from the abuse or misuse of clonazepam, an increase of 122 percent from 2004.
About one in 500 people taking medications like clonazepam develop suicidal thoughts, usually within a week of starting treatment. Friends and family members should also be on the alert for any unusual changes in your behavior. Research has not shown whether clonazepam is safe and effective in treating panic attacks in anyone younger than 18. Always tell your doctor if you have allergies to any medications, including other benzodiazepines. Common brand names for benzodiazepines include Valium, Xanax, Librium, Dalmane, and Ativan. You should not take clonazepam if you have untreated open-angle glaucoma, so tell your doctor about any eye symptoms you experience.
Once you have been on clonazepam for a significant length of time, there is some chance you will become dependent on the drug.
Withdrawal symptoms may include hallucinations, shaking, cramps, anxiety, sweating, and difficulty sleeping.
Many drugs may affect the way clonazepam works, and clonazepam may affect other drugs you are taking. It’s very important to let your doctor know about all drugs you take, including illegal drugs, over-the-counter (OTC) drugs, and any herbs or supplements.
Between 2004 and 2007 the FDA MedWatch program received 1,349 Individual Safety Reports naming Klonopin (clonazepam, also marketed as Rivotril) the Primary Suspect Drug for 1,100 distinct adverse reactions including cardiac arrest, completed suicide, impaired driving ability, impaired work ability, memory impairment and morbid thoughts.
This site contains copyrighted material, the use of which has not always been specifically authorized by the copyright owner. Bonkers Home       About       Contact       Funding       Affiliates      Become an M.D. Drowsiness, dizziness, tiredness, loss of coordination, or increased saliva production may occur. Drug interactions may change how your medications work or increase your risk for serious side effects.
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The solution for parenteral injection should be protected from light and prevented from freezing.
Coupling of GABA neurotransmitter with receptor opens up chloride channel, which inhibits forward progress of impulse.
Total accumulated benzodiazepine in body tissue is far in excess of the actual dose for any given day. Urine pH becomes acidic because of excretion of some nutrition, metabolites and medications.
The elimination half-life of diazepam and also the active metabolite desmethyl-diazepam increases significantly in the elderly, which may result in prolonged action, as well as accumulation of the drug during repeated administration. But if Benzodiazepine is discontinued after long term use then side effects can be mild to severe in intensity. Severe withdrawal symptoms are observed in patients treated with benzodiazepine for prolonged period, if abruptly discontinued. Treatment of benzodiazepine is necessary in few patients with history of seizure disorder who are resistance to all other antiepileptic medications. Immunoassay is followed by a confirmatory chromatography studies if results are suggesting possible addiction or illegal behavior. Immunoassay of urine with dipstick study is rapid and not always reliable screening investigation.
In most of the cases immunoassay is usually followed by chromatographic study to conform the values. Insomnia patients are treated by psychiatrist and given prescription of one of the benzodiazepine. Clonazepam can interact with many medications, so make sure your doctor is aware of all medicines you take. There is evidence that clonazepam may increase the risk for birth defects if you take them while pregnant. Talk to your doctor about other options if you're considering breastfeeding while taking clonazepam. The most common ones in people treated for seizures are drowsiness, ataxia (a type of clumsiness), and behavior changes.
If any of these effects persist or worsen, tell your doctor or pharmacist promptly.Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects.
This product may contain inactive ingredients, which can cause allergic reactions or other problems.


This copyrighted material has been downloaded from a licensed data provider and is not for distribution, expect as may be authorized by the applicable terms of use. The information is not intended to cover all possible uses, directions, precautions, drug interactions or adverse effects, nor should it be construed to indicate that use of a particular drug is safe, appropriate or effective for you or anyone else.
Benzodiazepine drugs including diazepam increase the inhibitory processes in the cerebral cortex.
Anticonvulsant properties of diazepam and other benzodiazepines may be in part or entirely due to binding to voltage-dependent sodium channels rather than binding GABA-a receptors. Thus only 1 to 4% of the absorbed diazepam in the blood is available for therapeutic (medicinal) effects. Following complication may occur with infants if medication is continued during third trimester.
Few patients may not get prescription from physician and instead prefer to purchase from other sources.
They are more commonly abused than opiate pharmaceutical, which accounted for 32% of visits to the emergency department. A healthcare professional should be consulted before taking any drug, changing any diet or commencing or discontinuing any course of treatment. Benzodiazepines slows the recovery of sodium channels from inactivation, thus repetitive stimulation of cortex and sub cortical centers do not trigger epileptic activities.
Positive or presence of benzodiazepine suggest patient is taking prescribed medications and negative or absence of benzodiazepine in urine indicate patient may not be taking medication as prescribed.
Favorable effect of diazepam eventually leads to potential abuse and can cause serious side effects. Do not drive, use machinery, or do any activity that requires alertness until you are sure you can perform such activities safely. Patient will run short of medication, if treating physician does not give him adequate amount and dosage of benzodiazepine. Absence of urine benzodiazepine indicates need for chromatographic urine examination of left over sample to confirm the dipstick result. Section 107, the material on this site is distributed without profit to those interested in receiving the included information for research and educational purposes.
It belongs to a class of drugs called benzodiazepines.How to use KlonopinRead the Medication Guide provided by your pharmacist before you start taking clonazepam and each time you get a refill.
Ask your pharmacist about using those products safely.Does Klonopin interact with other medications? If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. Therefore, discuss the risks and benefits of treatment with clonazepam with your doctor.Older adults may be more sensitive to the effects of this drug, especially drowsiness and confusion. Consult your doctor for more details.Missed DoseIf you miss a dose, take it as soon as you remember. These side effects can increase the risk of falling.During pregnancy, this medication should be used only when clearly needed. If it is near the time of the next dose, skip the missed dose and resume your usual dosing schedule.
You may report side effects to Health Canada at 1-866-234-2345.List Klonopin side effects by likelihood and severity.
Do not double the dose to catch up.StorageStore at room temperature away from light and moisture. Do not increase your dose, take it more often, or take it for a longer time than directed.Take this medication regularly to get the most benefit from it. However, since untreated seizures are a serious condition that can harm both a pregnant woman and her unborn baby, do not stop taking this medication unless directed by your doctor.
To help you remember, take it at the same times each day.Do not stop taking this medication without consulting your doctor. If you are planning pregnancy, become pregnant, or think you may be pregnant, immediately talk to your doctor about the benefits and risks of using this medication during pregnancy.This drug passes into breast milk and may have undesirable effects on a nursing infant.
Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so.
Your dose may need to be gradually decreased.This medication may cause withdrawal reactions, especially if it has been used regularly for a long time or in high doses. Consult your doctor before breast-feeding.What should I know regarding pregnancy, nursing and administering Klonopin to children or the elderly?
Consult your doctor or pharmacist for more details, and report any withdrawal reactions right away.When this medication is used for a long time, it may not work as well.
Talk with your doctor if this medication stops working well.Along with its benefits, this medication may rarely cause abnormal drug-seeking behavior (addiction).
Take this medication exactly as prescribed to lessen the risk of addiction.If you have several different types of seizure disorders, you may experience a worsening of seizures when you first start using clonazepam. Your doctor may need to add or adjust the dose of your other medications to control the seizures.Tell your doctor if your condition persists or worsens.What conditions does Klonopin treat?




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