Restoril - General Information
A benzodiazepine that acts as a gamma-aminobutyric acid modulator and anti-anxiety agent. [PubChem]
Pharmacology of Restoril
Restoril is a benzodiazepine used as a hypnotic agent in the management of insomnia. Restoril produces CNS depression at limbic, thalamic, and hypothalamic levels of the CNS. Restoril increases the affinity of the neurotransmitter gamma-aminobutyric acid (GABA) for GABA receptors by binding to benzodiazepine receptors. Results are sedation, hypnosis, skeletal muscle relaxation, anticonvulsant activity, and anxiolytic action.
Restoril for patients
Your doctor has prescribed temazepam to help you sleep. The following information is intended to guide you in the safe use of this medicine. It is not meant to take the place of your doctor's instructions. If you have any questions about temazepam capsules be sure to ask your doctor or pharmacist.
Temazepam is used to treat different types of sleep problems such as
- trouble falling asleep
- waking up too early in the morning
- waking up to often during the night
Some people may have more than one of these problems.
Temazepam belongs to a group of medicines known as "benzodiazepines". There are many different benzodiazepine medicines used to help people sleep better. Sleep problems are usually temporary, requiring treatment for only a short time, usually 7-10 days. However, if your sleep problems continue, consult your doctor. He/She will determine whether other measures are needed to overcome your sleep problems. Some people have chronic sleep problems that may require prolonged use of sleep medicine. However, you should not use these medicines for long periods without taking with your doctor about the risks and benefits of prolonged use.
Common Side Effects: All medicines have side effects. The most common side effects of benzodiazepine sleeping medicines include:
- difficulty with coordination
You may find that these medicines make you sleepy during the day. How drowsy you feel depends upon how your body reacts to the medicine, which benzodiazepine sleeping medicine you are taking, and how large a dose your doctor has prescribed. Day-time drowsiness is best avoided by taking the lowest dose possible that will still help you sleep at night. Your doctor will work with you to find the dose of temazepam that is best for you.
To manage these side effects while you are taking the medicine:
- Use extreme care while doing anything that requires complex alertness, such as driving a car, operating machinery, or piloting an aircraft. As with any medications used to help people sleep better, you should be very careful when you first start taking temazepam until you know how the medicine will affect you.
- NEVER drink alcohol while you are being treated with temazepam or any benzodiazepine medicine. Alcohol can increase the side effects of temazepam or any other benzodiazepine medicine.
- Do not take any other medicines without asking your doctor first. This includes medicines you can buy without a prescription. Some medicines can cause drowsiness and are best avoided while taking temazepam.
- Always take the exact dose of temazepam prescribed by your doctor. Never change your dose without consulting your doctor first.
There are many problems that may occur while taking benzodiazepine sleeping medicines.
Benzodiazepine sleeping medicines may cause a special type of memory loss or "amnesia". When this occurs, a person may not remember what has happened for several hours after taking the medicine. This is usually not a problem since most people fall asleep after taking the medicine
Memory loss can be a problem, however, when sleeping medicines are taken while traveling, such as during an airplane flight and the person wakes up before the effect of the medicine is gone. This has been called "traveler's amnesia".
Memory problems were noticed in fewer than 1 in 100 patients taking temazepam in clinical trials. Memory problems can be avoided if you take temazepam only when you are able to get a full night's sleep (7-8 hours) before you need to be active again. Be sure to talk to your doctor if you think you are having memory problems.
When benzodiazepine sleeping medicines are used every night for more than a few weeks, they may lose their effectiveness to help you sleep. This is known as "tolerance".
If tolerance to the medicine develops, other effects may occur depending upon which benzodiazepine you are taking. Tolerance to benzodiazepine sleeping medicines that are shorter acting may cause you to:
- wake up during the last third of the night.
- become anxious or nervous when you are awake
These effects are less common with temazepam because it is intermediate acting.
All the benzodiazepine sleeping medicines can cause dependence, especially when these medicines are used regularly for longer than a few weeks or at high doses. Some people develop a need to continue taking their medicines. This is known as dependence or "addiction".
When people develop dependence, they may have difficulty stopping the benzodiazepine sleeping medicine. If the medicine is suddenly stopped, the body is not able to function normally and unpleasant symptoms may occur.They may find they have to keep taking the medicine either at the prescribed dose or at increasing doses just to avoid withdrawal symptoms.
All people taking benzodiazepine sleeping medicines have some risk of becoming dependent on the medicine. However, people who have been dependent on alcohol or other drugs in the past may have a higher chance of becoming addicted to benzodiazepine medicines. This possibility must be considered before using these medicines for more than a few weeks.
If you have been addicted to alcohol or drugs in the past, it is important to tell your doctor before starting temazepam or any benzodiazepine sleeping medicine.
Withdrawal symptoms may occur when a benzodiazepine sleeping medicine is stopped suddenly after being used for a long time. But these symptoms can occur even if the medicine has been used for a week or two.
In mild cases, withdrawal symptoms may include unpleasant feelings. In more severe cases, abdominal and muscle cramps, vomiting, sweating, shakiness, and, rarely, seizures may occur. These more severe withdrawal symptoms are very uncommon.
Another problem that may occur when taking benzodiazepine sleeping medicines are stopped is known as "rebound insomnia". This means that a person may have more trouble sleeping the first few nights after the medicine is stopped than before starting the medicine. If you should experience rebound insomnia, do not get discouraged. This problem usually goes away on its own after 1 or 2 nights.
If you have been taking temazepam or any other benzodiazepine sleeping medicine for more than 1 or 2 weeks, do not stop taking it on your own. Your doctor may give you special directions on how to gradually decrease your dose before stopping the medicine. Always follow your doctor's directions.
Changes in Behavior and Thinking
Some people using benzodiazepine sleeping medicines have experienced unusual changes in their thinking and/or behavior, including: more outgoing or aggressive behavior than normal; loss of personal identity; confusion; strange behavior; agitation; hallucinations; worsening of depression; and suicidal thoughts.
How often these effects occur depends on several factors, such as a person's general health or the use of other medicines. Clinical studies with temazepam revealed that unusual behavior changes occurred in less than 1 in 100 patients.
It is also important to realize that it is rarely clear whether these behavioral changes are caused by the medicine, an illness, or occur on their own. In fact, sleep problems that do not improve may be due to illnesses that were present before the medicine was used. If you or your family notice any changes in your behavior, or if you have any unusual or disturbing thoughts, call your doctor immediately.
Certain benzodiazepines have been linked to birth defects when taken by a pregnant woman in the early months of pregnancy. These medicines can also cause sedation of the unborn baby when used during the last weeks of pregnancy.
Temazepam should not be taken at any time during pregnancy. Be sure to tell your doctor if you are pregnant, if you ar planning to become pregnant, or if you become pregnant while taking temazepam.
Safe Use Of Benzodiazepine Sleeping Medicines
To ensure the safe and effective use of temazepam or any other benzodiazepine sleeping medicine, you should observe the following cautions:
1. Temazepam is a prescription medicine and should be used ONLY as directed by your doctor. Follow your doctor's instructions about how to take, when to take, and how long to use temazepam.
2. Never use temazepam or any other benzodiazepine sleeping medicine for longer than 1 or 2 weeks without first asking your doctor.
3. If you notice any unusual or disturbing thoughts or behavior during treatment with temazepam or any other benzodiazepine sleeping medicine, contact your doctor.
4. Tell your doctor about any medicines you may be taking, including medicines you may buy without a prescription. You should also tell your doctor if you drink alcohol. DO NOT use alcohol while taking temazepam or any other benzodiazepine sleeping medicine.
5. Do not take temazepam or any other benzodiazepine sleeping medicine unless you are able to get a full night's sleep before you become active again. For example, temazepam or any other benzodiazepine sleeping medicine should not be taken on an overnight airplane flight of less than 7-8 hours since "traveler's amnesia" may occur.
6. Do not increase the prescribed dose of temazepam or any other benzodiazepine sleeping medicine unless instructed by your doctor.
7. Use extreme care while doing anything that requires complete alertness, such as driving a car, operating machinery, or piloting an aircraft, when you first start taking temazepam or any other benzodiazepine sleeping medicine until you know whether the medicine will have some carryover effect in you the next day.
8. Be aware that you may have more sleeping problems (rebound insomnia) the first night or two after stopping temazepam or any other benzodiazepine sleeping medicine.
9. Be sure to tell your doctor if you are pregnant, if you ar planning to become pregnant, or if you become pregnant while taking temazepam. Temazepam or any other benzodiazepine sleeping medicine should not be taken at any time during pregnancy.
10. As with all prescription medicines, never share temazepam or any other benzodiazepine sleeping medicine with anyone else. Always store temazepam or any other benzodiazepine sleeping medicine in the original container out of reach of children.
The pharmacokinetic profile of temazepam does not appear to be altered by orally administered cimetidine dosed according to labeling.
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.
Additional information about Restoril
Restoril Indication: For the short-term treatment of insomnia (generally 7-10 days).
Mechanism Of Action: Benzodiazepines bind nonspecifically to benzodiazepine receptors, which affects muscle relaxation, anticonvulsant activity, motor coordination, and memory. As benzodiazepine receptors are thought to be coupled to gamma-aminobutyric acid-A (GABAA) receptors, this enhances the effects of GABA by increasing GABA affinity for the GABA receptor. Binding of the inhibitory neurotransmitter GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell.
Drug Interactions: Not Available
Food Interactions: Avoid alcohol.
Avoid excessive quantities of coffee or tea (Caffeine).
Generic Name: Temazepam
Synonyms: Methyloxazepam; N-Methyloxazepam; Hydroxydiazepam; Oxydiazepam
Drug Category: Anti-anxiety Agents; Adjuvants, Anesthesia; Benzodiazepines; GABA Modulators
Drug Type: Small Molecule; Approved
Absorption: Well absorbed, minimal first-pass metabolism.
Toxicity (Overdose): Not Available
Protein Binding: 96%
Biotransformation: Hepatic. Temazepam is completely metabolized through conjugation prior to excretion. The major metabolite is the O-conjugate of temazepam (90%).
Half Life: 10-20 hours
Dosage Forms of Restoril: Capsule Oral
Chemical IUPAC Name: 7-chloro-3-hydroxy-1-methyl-5-phenyl-3H-1,4-benzodiazepin-2-one
Chemical Formula: C16H13ClN2O2
Temazepam on Wikipedia: https://en.wikipedia.org/wiki/Temazepam
Organisms Affected: Humans and other mammals