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| Products: | Generic Ativan |
| Available Doses: | 2.5mg |
| Min. Price: | from $2.48 Per Pill |
| Bestseller Price: | 90 pills x 2.5mg – $346.50 |
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Origins of the drug
Ativan, also known under the name lorazepam, belongs to a group of drugs called benzodiazepines. In 1977, two research groups in Denmark and Switzerland independently discovered benzodiazepine “receptors” in the human brain. It was initially assumed that these “receptors” are in close proximity to ion channels that are controlled by the inhibitory neurotransmitter GABA. Today we know that benzodiazepines do not have their own receptor, but that their binding site lies between two subunits of the so-called GABAA receptor, a ligand-gated chloride channel.
Application of Ativan as a hypnotic
Ideally, a sleeping pill should be able to promote falling asleep, produce no adverse effects such as daytime sleepiness, have no dependence resulting from prolonged use, have a broad therapeutic range, and interfere with the physiology of natural sleep as little as possible. While there are no perfect hypnotics available today, the benefits of benzodiazepines also come with certain drawbacks.
Doctors advise using benzodiazepines only if your sleep disturbance cannot be eliminated by non-pharmacological measures (such as adapted sleep hygiene). The duration of use should not exceed four weeks in order to avoid developing tolerance with dose increases. For patients who have trouble falling asleep, benzodiazepines with a short half-life (2-4 hours), such as triazolam, midazolam, or Z-substances, such as zolpidem and zaleplon are most suitable; for those unable to stay asleep, temazepam, lormetazepam, nitrazepam or zopiclone (with a medium-length half-life of 4-8 hours) are commonly prescribed. Due to a long half-life of Ativan (12 hours), this medication finds use in the management of sleep disorders only when they are part of a major case of anxiety and/or depression.
Biochemistry of Benzodiazepines
In the central nervous system, GABAA receptors consisting of two α-, two β- and one γ-subunit occur most commonly. Today, as many as 19 different GABAA subunits are known in humans, which determine the physiological activity of the chloride channel. This large diversity explains why benzodiazepines are effective only in certain regions of the CNS.
What effect the GABA-regulated chloride channels have on the membrane potential depends on the ion concentration in and around the cell. Typically, the cell becomes hyperpolarized upon opening of these ion channels, which happens as follows: chloride ions flow into the cell, the membrane potential turns more negative and makes more difficult for the electrical signal to pass through.
Comparison of Ativan with other benzodiazepines
When looking at their pharmacodynamic properties, drugs of this group show different affinities for the benzodiazepine binding site. For example, as opposed to chlordiazepoxide, lorazepam and alprazolam show a much higher affinity. Diazepam, bromazepam, and oxazepam come second. Clobazam and dipotassium clorazepate have a relatively low tendency to bind. The potency of a certain benzodiazepine grows with the affinity, and the better this kind of a drug binds, the lower its therapeutic dose.
Low doses are better by any measure, especially when it concerns side effects of the medicine. Doctors usually increase the dosage depending on the effect intended. The following sequence of effects correlates with an increasing degree of receptor occupancy:
anxiolytic -> sedative -> sleep-inducing -> sleep-stimulating -> central muscle-relaxing.
Although the three GABAA receptor agonists — zolpidem, zaleplon, and zopiclone — do not have a benzodiazepine structure, they still contain nitrogen as a bicyclic structural element, similarly to benzodiazepines. Zolpidem and zaleplon have some selectivity for the α1 subunit of the GABAA receptor, but this is not true for zopiclone. As a result, the affinity of these Z-substances is significantly weaker as compared to flunitrazepam. Ativan (lorazepam), in its turn, is even more capable of binding and proves highly effective at lower doses than those of the drugs above.
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