Barbiturates are drugs that act as central nervous system depressants, and can therefore produce a wide spectrum of effects, from mild sedation to total anesthesia. They are also effective as anxiolytics, hypnotics, and anticonvulsants. Barbiturates also have analgesic effects; however, these effects are somewhat weak, preventing barbiturates from being used in surgery in the absence of other analgesics (opioids or volatile anesthetics such as halothane). They have addiction potential, both physical and psychological. Barbiturates have now largely been replaced by benzodiazepines in routine medical practice – for example, in the treatment of anxiety and insomnia – mainly because benzodiazepines are significantly less dangerous in overdose as there is no specific antidote for barbiturate overdose. However, barbiturates are still used in general anesthesia, for epilepsy, for the treatment of acute migraines and cluster headaches (in the compound drugs fioricet and fiorinol), occasionally for the treatment of recurrent migraines and cluster headaches (under stringent protocols with mandatory physician monitoring for addiction and abuse), and (where legal) assisted suicide and euthanasia. Barbiturates are derivatives of barbituric acid.
When thinking about drug abuse, people often assume that the substance used is illegal. However, that is not always true. The abuse of prescription drugs has increased dramatically in the past years, especially when it comes to barbiturates. Before taking barbiturates (regardless if this is done legally or illegally), it is important to know what effects they have. Personal health and safety should always be a serious matter of concern.
Phenobarbital (INN) or phenobarbitone (BAN) is a long-acting barbiturate and the most widely used anti-seizure medication globally. It has sedative properties, but as with other barbiturates, benzodiazepines are more commonly used for this purpose. Phenobarbital produces sedation by increasing the proportion of bound GABA receptors that are in the long-duration active state.
The World Health Organization recommends phenobarbital as a first-line medication for partial and generalized tonic–clonic seizures in developing countries. In the more developed world, it is no longer recommended as a first- or second-line choice for most seizure types, though it is still commonly used to treat neonatal seizures. The injectable form is mostly used to control status epilepticus, while by mouth it is used to prevent seizures in people with epilepsy. It is occasionally used to treat an inability to sleep, anxiety and to help with drug withdrawal as well as surgery.
Side effects include a decreased level of consciousness along with a decreased effort to breathe. There is concern of both abuse and withdrawal following long term use. It may also increase the risk of suicide. It is pregnancy category B or D in the United States and category D in Australia, meaning that it is may cause harm when taken by pregnant women. A lower dose is recommended in those with poor liver or kidney function, as well as those who are older.
It is a core medicine in the WHO Model List of Essential Medicines, which is a list of minimum medical needs for a basic health care system. It is the oldest still commonly used anti-seizure medication having first been sold in 1912.
Diazepam /daɪˈæzɨpæm/, first marketed as Valium /ˈvæliəm/, is a medication of the benzodiazepine type. It is commonly used to treat a range of conditions including anxiety, alcohol withdrawal syndrome, benzodiazepine withdrawal syndrome, muscle spasms, seizures, trouble sleeping, and restless legs syndrome. It may also be used to cause memory loss during certain medical procedures. It can be taken by mouth, inserted into the rectum, injected into muscle, or injected into a vein. When given into a vein effects begin in one to five minutes and last up to an hour. By mouth effects may take 40 minutes to begin.
Common side effects include sleepiness and trouble with coordination. Serious side effects are rare. They include suicide, decreased breathing, and an increased risk of seizures if used too frequently in those with epilepsy. Occasionally excitement or agitation may occur. Long term use can result in tolerance, dependence, and withdrawal upon dose reduction. Abrupt stopping after long term use can be potentially dangerous. After stopping cognitive problems may persist for six months or longer. They are not recommended during pregnancy or breastfeeding. Its mechanism of action is by increasing the effect of the neurotransmitter gamma-Aminobutyric acid (GABA).
Diazepam was first synthesized by Leo Sternbach, and was first manufactured by Hoffmann-La Roche. It has been one of the most frequently prescribed medications in the world since its launch in 1963. In the United States it was the highest selling medication between 1968 and 1982, selling more than two billion tablets in 1978 alone. In 1985 the patent ended, and there are now more than 500 brands available on the market. Diazepam is on the World Health Organization's List of Essential Medicines, the most important medications needed in a basic health system.
Alprazolam /ælˈpræzəlæm/ or /ælˈpreɪzəlæm/ (trade name Xanax /ˈzænæks/), available under other generic names, is a short-acting anxiolytic of the benzodiazepine class of psychoactive drugs commonly used and FDA approved for the medical treatment of panic disorder, and anxiety disorders, such as generalized anxiety disorder (GAD) or social anxiety disorder (SAD). It was the 12th most prescribed medicine in 2010. Alprazolam, like other benzodiazepines, binds to specific sites on the GABAA receptor. It possesses anxiolytic, sedative, hypnotic, skeletal muscle relaxant, anticonvulsant, and amnestic properties. Alprazolam is available for oral administration in compressed tablet (CT) and extended-release capsule (XR) formulations.
Alprazolam has a fast onset of action and symptomatic relief. Ninety percent of peak effects are achieved within the first hour of using either the CT formulation or the XR formulation in preparation for panic disorder, and full peak effects are achieved in 1.5 and 1.6 hours respectively. Peak benefits achieved for generalized anxiety disorder (GAD) may take up to a week Tolerance to the anxiolytic/antipanic effects is controversial with some authoritative sources reporting the development of tolerance, and others reporting no development of tolerance; tolerance will however, develop to the sedative-hypnotic effects within a couple of days. Withdrawal symptoms or rebound symptoms may occur after ceasing treatment abruptly following a few weeks or longer of steady dosing, and may necessitate a gradual dose reduction.
Alprazolam was first released by Upjohn (now a part of Pfizer). It is covered under U.S. Patent 3,987,052, which was filed on 29 October 1969, granted on 19 October 1976, and expired in September 1993. Alprazolam was released in 1981. The first approved indication was panic disorder and within two years of its original marketing Upjohn's Xanax became a blockbuster drug in the US. Presently, Alprazolam is the most prescribed and the most misused benzodiazepine on the U.S. retail market. The potential for misuse among those taking it for medical reasons is controversial with some expert reviews stating that the risk is low and similar to that of other benzodiazepine drugs and others stating that there is a substantial risk of misuse and dependence in both patients and non-medical users of alprazolam and that the pharmacological properties of alprazolam, high affinity binding, high potency, having a short elimination half-life as well as a rapid onset of action may increase the misuse potential of alprazolam. Compared to the large number of prescriptions, relatively few individuals increase their dose on their own initiative or engage in drug-seeking behavior. Alprazolam is classified as a schedule IV controlled substance by the U.S. Drug Enforcement Administration (DEA).