Posted by ed_uk2010 on January 6, 2015, at 10:14:21
In reply to Re: How strong is Clonazepam really?, posted by michaels97320 on January 5, 2015, at 10:44:47
>Diazepam is said to be long acting....
Most information you read will state that diazepam is always long acting because it has a 'long half life' - this is misleading and is based on poor knowledge of the drug. The long half life refers to the slow elimination phase of the drug from the body. In practice, elimination half life is only one factor controlling a drug's real-life duration of action. Long half life drugs accumulate after regular repeated dosing and the duration of action always *becomes* long, regardless or whether or not it was long initially. In contrast, the duration of action after single or isolated doses is not controlled solely by the drugs half life. In the case of diazepam and clonazepam, it is controlled partly by fat solubility. Diazepam is extremely fat soluble (lipid soluble), the result of this is that is rapidly absorbed, and penetrates into the brain very quickly. Its action often wears off sharply around 3 hours after a single dose because it is redistributed out of the brain into fatty tissues elsewhere in the body... this terminates its sedative effect. If it's not at high levels in the brain, it's not going to help. Its action after a single dose is therefore not terminated by it being eliminated from the body - but by it being redistributed out of the brain. It has a short 'distribution half life' in spite of its long elimination half life.
After repeated dosing (usually at least daily), fat stores become saturated and diazepam's long-acting metabolite also reaches high levels (the metabolite is a new substance produced from diazepam in the liver). As a result, the level in the brain remains high and the drug is now truly long-acting.
Clonazepam has a moderately long half life, but not as long as diazepam or its metabolite, and therefore accumulates to a lesser extent. Its low lipid solubility results in a more gradual onset of action after taking a dose. It may not provide the very sudden/abrupt relief that you get with an adequate dose of diazepam after a single dose. It is absorbed over several hours, penetrates the brain more slowly... and leaves the brain more slowly. It lasts many hours right from the start. It has a long 'distribution half life'. After daily dosing for weeks or months, it may need to be given more frequently than diazepam - unlike diazepam, it lacks a long acting metabolite.
>Diazepam... I find it to come on quite quickly, I can definitely "feel" it and after the initial 2-3 hour peak effect, loses its potency. Clonazepam seemed to be less distinct in the time of onset, but there was an overall mood stabilizing effect.
That is typical. Most doctors will just tell you that both drugs are long-acting. This is not correct because the duration of action of diazepam is highly dependent on whether it is used 'when needed' or regularly. Clonazepam is much easier to understand, it is simply long-acting in most situations.
>One of the major advantages of benzos for me is the "relief euphoria" which occurs with diazepam, not really with clonazepam.
This property is very useful for ending a panic attack, for example, but can be problematic for anyone who likes the effect too much. If you ensure that you only take it when you absolutely need it, rather than when you want it, you should be OK. If you don't truly need a dose, don't take it - there is much more risk of developing tolerance and dependence if you do. Alternate day dosing can still produce some physical dependence, however, but taking 5mg of diazepam on alternate days will not produce such intense dependence as taking regular clonazepam 2mg.
>a very strong anxiolytic. It feels more like a mood stabilizer than anything. That's not a bad thing, but I can take an actual mood stabilizer for that and not get a benzo addiction out of it.
I don't personally find it especially helpful, it's too 'flattening'. Many people do benefit from it, however.
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Here is a summary of duration of action....
Diazepam - duration of action after a single dose: usually surprising short, except in the frail or elderly, where it can last much longer. There may be some mild persistent effects for many hours but most of the effects are gone within a few hours. For me, single doses last 2-3 hours at most.
Duration of action after regular dosing for weeks or more: now long. Some people who take it regularly find it lasts all day every day with once daily dose. This property makes diazepam a useful drug for long term users to gradually taper off benzos.Lorazepam - duration of action after a single dose: medium. Duration of action after repeated dosing: still medium.
As a result, those who take it regularly for anxiety normally take it 2-3 times a day, sometimes 4. It often lasts about 6-12 hours, which changes little over time.Clonazepam: duration of action after a single dose: quite long. Duration of action after repeated dosing: still quite long.
It's most commonly given twice a day for severe anxiety, but 1-3 times a day is common. 2mg is a lot to take at once, for someone who doesn't usually take it. The most common dose is between 0.25mg and 1mg twice a day (usually 0.5-1mg twice a day for panic disorder). Very high doses are sometimes used in psych units to calm severe agitation.............................
Speed of onset of action after a single dose (regular dosing at a suitable time intervals should not produce large ups and downs):
Diazepam: Extremely fast on an empty stomach. With food: still fast but not as fast.
Lorazepam: Moderate, clearly slower than diazepam (this applies to both sublingual and oral routes). Often helps after about an hour.
Clonazepam: tends to build up gradually over a few hours. May end up being much stronger than it first appeared, and this can catch you by surprise due to its gradual nature.
poster:ed_uk2010
thread:1074710
URL: http://www.dr-bob.org/babble/20150102/msgs/1074860.html