Afobazole (aka Fabomotizole)

Afobazole



Afobazol is a novel anxiolytic drug with nootropic properties used in Russia to treat anxiety and some cardiac disorders. According to clinical trials, its efficacy in patients with generalized anxiety disorder and adjustment disorder is comparable to benzodiazepines.

The active ingredient is Fabomotizole. Afobazole was discovered in the beginning of 2000s at Zakusov Institute of Pharmacology. This institute is also known for its discoveries of dipeptide nootropic Noopept, adaptogen Ladasten (Bromantane) and anxiolytic peptide Selank.

What makes it special among other anti-anxiety medications is that Afobazol does not have sedative, hypnotic and muscle relaxant action and does not form dependence.  Besides that, studies in models of local and global ischemia have revealed neuroprotective effects of the drug.


Mechanism of action


Afobazol mechanism of action is different from benzodiazepines. It is not a benzodiazepine receptor site agonist. At the same time, it prevents stress-induced changes of GABA-benzodiazepine receptor complex and restores its sensitivity to endogenous inhibitory mediators.

The drug acts on sigma-1 receptors, melatonin MT1, and MT3 receptors and shown to reversibly inhibit MAO-A. It also has some neurotrophic properties, although they are not as pronounced as in another non-sedative anxiolytic, Stresam. In studies performed on rats, Afobazol prevented stress-induced BDNF decrease and increased NGF and BDNF content in hippocampal HT22 cells culture.


Indications and usage


Indications for use are:

  • Generalized anxiety disorder.
  • Neurasthenia.
  • Adjustment disorder.
  • Anxiety related insomnia.
  • Neurocirculatory dystonia.
  • Premenstrual syndrome.
  • Alcohol abstinence syndrome.
  • Nicotine withdrawal.


In Russia and other CIS countries, Afobazole is a non-prescription drug. It is one of the few effective OTC anxiolytics available among with Adaptol (Mebicar) and Phenibut. And because of its effectiveness and the fact that benzodiazepines require a prescription, it rapidly grows in popularity. Sales rose from 100 thousands of packages in 2006 to one million of packages in 2015.


Side effects and contraindications


The treatment is usually well-tolerated by the patients. Possible adverse effects as stated by the official instruction are headaches and allergic reactions. The drug is not habit-forming and do not cause withdrawal after cessation.

Contraindications for use are pregnancy and lactation, age below 18 years old.



References
  1. Seredinin S.B, Voronin M.V "Neuroreceptor mechanisms involved in the action of Afobazole."
  2. Silkina I.V, Aleksandrin V.V, Ganshina T.S, Seredinin S.B, Mirzoyan R.S "Afobazole increases cerebral blood flow in rats with global ischemia."
  3. Ganshina T.S, Kurdymov I.N, Turilova A.I, Mirzoyan R.S, Seredinin S.B "Afobazole effects on cerebral circulation under hemorrhagic stroke model conditions."
  4. Abramova E.V, Voronin M.V, Seredinin S.B "Interaction of afobazole with sigma-1 receptors in mice brain."
  5. Silkina I.V, Zenina T.A, Seredinin S.B, Mirzoyan R.S "Effect of afobazole on the accumulation of free radical oxidation products and the catalase activity in rats with cerebral ischemia."
  6. Seredinin A.B, Melkumyan D.S, Valdman E.A, Yarkova M.A, Seredinina T.S, Voronin M.V, Lapitskaya A.S "Effects of afobazole on the bdnf content in brain structures of inbred mice with different phenotypes of emotional stress reaction."


Here are the reviews from the Russian on-label users. They were translated from otzovik website, sorted by newest. Every kind of reviews included, either positive or negative.

5/5

I am an impressionable person that takes everything to heart. Besides that, I’ve had an unsuccessful marriage, my husband affected my nerves badly, so I felt anxious about everything and started to fear every rustle.

Before that, I’ve tried valerian root, motherwort tincture and mint tea to combat these symptoms. Didn’t wanted to take any serious medications, especially without doctor’s advice, because it may worsen the situation. But the traditional remedies don’t have much effect, cause sleepiness, their effect is short-term and the anxiety comes back again.

So I visited the doctor. He suggested me to take Afobazole. This drug is a mild tranquilizer, it scared me a bit, I feared the possible dependence.

I felt the effect after about a week, the anxiety has gone, I started to react calmer, my mood has improved, I started to sleep better.

After the full course, I felt like a different man – calm and balanced. The drug did not formed dependence. After cessation, the effect is still present.

Can’t say that everything changed drastically. Stressful situations still get on my nerves, but not as much as before. And now I know that in case of stress or anxiety you can take Afobazol.

But of course, there is no need to self-medicate and take it without regulation!

3/5

As a man that tried every psychoactive pill available, including antipsychotics, I can say the following: Afobazol is a strong medication. I’m not simply having weak nerves, as most people that left positive feedback, I have bipolar disorder. In depressive phases, I take tranquilizers+antidepressants… Was prescribed with Afobazole as an experiment, can’t take any other medicines anymore. Tried it three years ago for the first time, only one pill before bed for one month. The effect was surprisingly good: falling asleep very quickly, long quality sleep, lots of energy during the day, felt slightly euphoric and even lost couple kilograms. After Stresam and Phenazepam, I slept all day long and didn’t had the energy to go to the bathroom, and now so much energy and positive. Withdrawal syndrome was pronounced, weakness, apathy, insomnia, anger. But with horse doses of sedative drinks like valerian mint I was able to go through it. Still carried afobazole for a rainy day though. And this day comes.

My second course was half-year long, my dependence grows, the effect became less pronounced, and the overall impression was strange, now it gives me insomnia, aggression, appetite, weight gain (five kilograms after a half year). I decided to quit and in the first day I slept till noon, didn’t wanted to eat, didn’t had the energy to go to the grocery, didn’t enjoyed music nor films, anything. Thought about death and the lack of dreams. After a week I drank a pill and it calmed me down immediately, but still had some anger with sadness.

So here are the “bunk pills, without withdrawal syndrome”. Don’t know how to quit them. I’ll visit a psychiatric clinic, maybe they will suggest anything.

5/5

I worked hard for a half year to afford vacation across Europe. And just before my vacation, I was fired. Just booked some hotels before that, I was in a terrible mood and without funds for my trip. So I moved to my mom and spent couple days just laying down. Mom bought Afobazol and gave it to me, one pill after breakfast, lunch, and dinner. I wouldn’t decide to take it on my own as I was apathetic, didn’t wanted to do anything, including the treatment of my depression. It was hard to remember but after about five days I started to live again. Started to walk outside, talk (before that mom literally needed to pull words out of me). After the 1,5 weeks, I was fully recovered, this terrible lack of self-confidence and the feeling of resentment has gone. I updated my resume and started to look for a new job. And now I’m returning back to Moscow, applying for a new job, and I hope that in the next year I will fulfill my dream. And thanks to Afobazole – this turned out to be a good medication.

5/5

I’ve had a stressful period at job. Reports and inspections. A large amount of work, struggles, also I’ve caught the flu. And my calmness has gone into oblivion. Constant thoughts, worries, increased heartbeat. This all makes the situation worse. My wife asked me to take this pills. Initially, I was against that idea, because I don’t like to take any unnecessary pills, especially for such questionable disease as stress.

But then I thinked, if there is a chance to improve the situation, why not try it.

And I was wrong. After taking it my condition gets significantly better, of course, I still had some problems, but the result was inevitable. Using it I was able to go through the hard situation, and then cease the medication easily, there wasn’t any withdrawal.

4/5

I’ve started to use these pills seven years ago when I was in a very stressful situation where valerian root won’t help.

I visited a pharmacy and said that everything is bad and I need something to calm me down. The pills are indeed very strong and just after two days, I became calm as a clam. Not without side effects of course, felt like a vegetable. But maybe it’s for the better. Because I wanted to stay calm and continue to be active in my job and in my hobbies.

Now I have chosen a different medication, it’s called Adaptol, I’m taking it when I feel nervous.

4/5

Recently I had to come up with tachycardia and its treatment. And I was prescribed with Afobazole in the complex treatment.

I took one pill twice daily after a meal. Regarding the side effects, I’ve noticed only allergic reaction and headache. Alas, the second side effects I mentioned appeared all the time during evenings. Didn’t had any problems with sleep, though.

As a part of a complex therapy, this drug helped me. So I can recommend it definitely. Be sure to consult with the doctor before taking it and be healthy!

5/5

Started to suffer from insomnia recently. I wake up at 3 AM just like with an alarm clock, and can’t sleep. It’s not good to think this way, but I was happy to hear that I’m not the only man that suffered from such problem. I’ve noticed, that many of my friends, office workers just like me, complaining about the same problem on the facebook. I’m just 30 years old, slept very well before. Didn’t wanted to think that this is me getting old. And yet didn’t wanted to take any of the strong medications, to sleep for a hours and be a vegetable, so I decided to start with Afobazol, my friend recommended it to me. Can’t afford to take strong sleeping pills because I still have to wake up in the morning and go to work.

I took three pills daily, the last pill an hour before bedtime. Insomnia has gone after a week. I continued to take this drug and took the whole course. Also I’ve noticed that I became much calmer, started to worry less about job, it became easier to switch between work and free time. Very useful thing for those who work as hard as me.

I can reccomend this for everyone who suffers from similar problem. Didn’t noticed any side effects, so I will repeat the course if necessary.

2/5

Took this as a support after severe stress. Experienced apathy, insomnia, bad mood, and anxiety.

After the three days of application: anxiety is still there, still can’t fall asleep, but now I’m waking up midnight less often. Waking up became harder, though.

When I wake up, I feel like after taking some strong sleeping pill, a very intense brain fog. Besides that, I’ve noticed dry mouth, burning eyes, orange urine color, even thought that I have a healthy diet and drink enough amount of water.

So, I suggest you cope on your own if there is no extreme necessity. Or you can take glycine, or some natural remedies, which is even better. Good health to everyone!

Leave a Reply

Your email address will not be published. Required fields are marked *