Enta- and opicapone experience

[Daisies22]

About a month ago I was prescribed Opicapone 50 mg which I took under medical supervision. Roughly an hour after taking the 50 mg capsule I experienced very strong adverse reaction characterised with high pulse rate and blood pressure, extreme stiffness (rigidity), fragmented breathing, inability to initiate any voluntary movement, whole-body shaking. These are the same end of dose symptoms which I have when I am on Madopar only, but this time they were much worse, which I found inexplicable. The episode lasted about 4 hours and only then I regained control over my movements. We were allowed to leave the hospital minus the medication.The next morning I noticed that my ON period was really long - 15-16 hours and during this time I felt completely normal.

That day I had my second appointment in the hospital. My Neurologist's view, and I agree with him, was that 50 mg was too high a dose for me. We had a brief conversation and it was, rather randomly decided to try Opicapone 25 mg. I took it four consequtive days and had a completely unexpected overdose which put me in A&E with chest pain and difficulties breathing, I lost my voice temporarily, I felt really dizzy and was unable to sit in bed. Thankfully, blood test did not confirm a suspected heart attack and I was allowed to go home at around midnight.

The following four days I felt better as the 25 mg seemed to work and smooth out the rather jumpy concentration of levodopa in plasma vs time curve. I liked how I felt I hoped that the worst was over when I started having the same reactions I had to the 50 mg capsule. I stopped taking the 25 mg and tried to survive the above - described symptoms. It has been nearly a month and I am still not fully recovered. I am not sure how long this medication will stay in my system.

Apologies for the long explanation. I guess my question is - are there any other PwP on opicapone who had similar experience to mine? If you are still on opicapone how do you dose this medication so that you do not have such severe adverse effects?

Has anybody tried both Entacapone and Opicapone, and which one do you prefer and why?

Thank you in advance for the patience to read the above and for any comments you might have.

[park_bear]

I believe your symptoms can all be attributed to opicapone slowing down destruction of levodopa in your bloodstream. Entacapone is less effective and shorter acting, which for you would be an advantage.

[Daisies22 in reply to park_bear]

Thanks PB. I completely agree.When you say "shorter acting", how many hours might that be?

Also, I take Madopar 7 times a day. Will I have to take 7 Entacapone as well?

[park_bear in reply to Daisies22]

Maximum daily dosage of entacapone is 4 per day. So from that we can estimate it lasts approximately one quarter as long as opicapone.

[Daisies22 in reply to park_bear]

Thanks PB. I think your suggestion is a very good starting point. Knowing how sensitive I am to anti-Parkinson's medication I most probably will start with one per day and then will try to adjust the dose of the madopar I take, I'm desperate to reduce it as it affects me so badly.Thank you again.

D.

[park_bear in reply to Daisies22]

Also, they are tablets which can be split into half doses if you wish.

[Daisies22 in reply to park_bear]

Ah yes. Splitting tablets into half doses is less time consuming than weighing the content of a capsule and adjusting the mg I need. Luckily, we've found this: KUBEI USB Rechargeable Digital... amazon.co.uk/dp/B08JYPVL9Z?...

which I thought was working remarkably well!

It is just that I'm worried that if I take a pill every day, and the medication is active for more than 24 h, sooner or later i will experience the equivalent of a stacking effect which will give me another overdose.

D.

[park_bear in reply to Daisies22]

"The mean elimination half-life of opicapone is one to two hours. Despite the short half-life, the observed half-life of opicapone-induced COMT inhibition in human red blood cells was 61.6 hours with a standard deviation of 37.6 hours."

"The elimination of entacapone is biphasic, with an elimination half-life of 0.4 h - 0.7 h based on the β-phase and 2.4 h based on the γ-phase."

ncbi.nlm.nih.gov/pmc/articl...

"The absorption of entacapone, like that of LD, is highly variable between different individuals and exhibits high intraindividual variability as well"

"Entacapone increases the daily ON time by an average of 1 to 2 hours and correspondingly reduces the daily OFF time in patients with PD with motor fluctuations. The daily LD dose has been reduced by 10% to 30%. These positive effects are sustained in long-term use over several years

Food does not appear to affect the absorption and bioavailability of entacapone.

When 200 mg of entacapone is administered together with LD and carbidopa, it increases the AUC of LD by approximately 35%, and the elimination half-life of LD is prolonged from 1.3 hours to 2.4 hours. In general, the average peak LD plasma concentration and the time of its occurrence (Tmax of 1 hour) are unaffected"

[Nitro53 in reply to park_bear]

My Doc has me on Entacapone 5X a day

[LAJ12345]

my husband takes 3x 1/3 entacapone tablets which was seeming to work well with other things for nearly a year but he has recently been becoming over anxious again and worrying about nothing.

That might be unrelated. We have extra people in the house with all the kids back home and new kittens so I think he is struggling with the lively household.

[puretone]

My partner has tried both entacapone and opicapone and in both cases had a great first day but struggled to breathe on day two. I've encouraged her to try again along with a ~30% decrease in her madopar dose as I suspect the problem might be overly high peak levodopa inducing a kind of respiratory dyskinesia (if such an issue exists). I wish she could try 25mg tabs but here in Australia the only opicapone is 50mg caps. It's strange that her neurologist made no mention of the possibility of too much levodopa associated with COMT inhibitors.

[Windermere1 in reply to puretone]

when you take entacapone or Opicopone you need to reduce c/l by at least one tablet per day to avoid od symptoms

[park_bear in reply to puretone]

Levodopa induced respiratory dyskinesia - Yes this is a thing:

movementdisorders.onlinelib...

api.repository.cam.ac.uk/se...

"levodopa-induced diaphragmatic dyskinesias may lead to rapid strenuous and distressful dyspnoea"

Also discussed here: healthunlocked.com/cure-par...

Agree reducing her levodopa dosage is in order

[Jaguarorbust]

For working out what’s going on, the Parkinson’s Measurement website has been brilliant. For me, Entacapone or Sastravi is around 10% ‘stronger’ than Sinemet and lasts 25% longer for the same mg of LD.

Opicapone on the other hand works like a booster and gives me around 70% more benefit from the same LD dosage, so after a few days Opicapone I needed just over half the dose of Sinemet/Sastravi/Madopar that I had been taking.

parkinsonsmeasurement.org/t...

Puts your meds in, then imagine 2 horizontal lines on the graph, the lower one is where you go from on to off and the upper one is where you experience the effects of too much. Tinker with tablet size and timing to keep your blood level in between the two. Well that’s the theory….

[Parkie1]

I am also sensitive to anti Parkinson's meds. I take 8 x 50mg madopar per day, plus rotigatine patch 4mg which I am trying to reduce gradually due to increased dyskinesia. I tried entacapone 1st, and could only take one per day because it made me hyper from the very 1st tablet. I stopped it within 2 weeks. I was then given opicapone which made me even more hyper, like a teenager on ecstasy! I stopped it before the week was out and then was given rotigatine which seems to be milder. I must say that as far as smoothing out the "offs" are concerned, it's very effective,(comt inhibitors, i.e.)but it's far too strong for me. I've been trying B1 for 9 months now and think I've hit the sweet spot which is why I feel that I need less rotigatine, but if it's offered to you you can keep it to a small dose.

[Lorraine33]

unfortunately my hwp did not have physical reactions but hallucinations which began benignly but after 5 days he looked at me and asked who was I. It is sad as, like you they made such a difference to the Parkinson’s symptoms.

His prof. said a lower dosage would lead to same thing . So had to stop.

[Grey_Area]

1 x 50mg Opicapone caused me very similar problems and in addition extreme wakefulness (didn't sleep AT ALL for three nights) and a urinary tract infection. I only managed three doses.

4 x200mg (one every 6 hours) Entacapone did not cause as severe a reaction, though apart from an initial (first day) improvement in off time of thirty minutes or so also did not provide any real benefit.

I'm in the process of transferring to Stalevo, but this effectively means I am switching from a 50:50 mix of normal and slow release L dopa to entirely normal release and I believe this is reducing my on time and possibly worsening my dystonia in my thighs.

I have had to deal with all this while living alone. It is not policy to routinely admit to hospital while assessing medication changes in the UK.

[Windermere1 in reply to Grey_Area]

I started stevalo 3 weeks ago and it’s helped my on time by 2 hours. I have also even able to drop one Madopar dose.

[park_bear in reply to Grey_Area]

I live in splendid isolation and I love it. Among other things, strong motivation to keep the Parkinson's under good control.

[Daisies22 in reply to Grey_Area]

Thank you for your comments, it is helpful to know what to expect from Entacapone (I'm still waiting for the prescription to reach my GP).Also, I completely agree with the comment you've made in the last paragraphof your reply, except that nothing was routine in my case, I wish it was.

Best wishes,

D.

[Grey_Area in reply to Daisies22]

"Waiting for GP to respond"...I seriously think I'm going to have that on my tombstone...

[Daisies22 in reply to Grey_Area]

This made me smile!

[MARC1]

I would say that I'm suffering the same symptoms of Opicapone as many of you are reporting. I take 7 x 100/25 throughout the day plus 50mg dispersible when I wake up, add madopar CR @ 9pm and Opicapone at 10pm. For the last 2 months I've been having a really bad tremor which could take up to 3hrs to subside, accompanied with rigidity either in my shoulders or in my legs leaving me almost unable to walk(like walking through Tar) within 5 minutes of taking my prescribed dose of Madopar. This has really not helped with my anxiety and left me with little confidence to venture out and meet up with friends. All along I've been wondering has something changed in the Madopar or am I not taking enough, or overdosing!! Just to add I've been given the go ahead for the Produodopa pump later this year so hopefully this wll smooth my side effects out.Can i say a big thankyou to everyone for answering Daisies22 question as it has certainly helped me.

[park_bear in reply to MARC1]

Rigidity - dystonia - can be caused by too much Levodopa as well as too little. Can usually be determined by when it occurs in relation to levodopa levels. Starting up 5 minutes after taking a dose seems a bit quick, but what do I know. You could try reducing your medication just a little bit and see if that helps, like taking six doses over the course of the day instead of seven, with the consent of your MD. If you decide to try this, keep notes to track any changes.

[Daisies22 in reply to MARC1]

Dear MARC1,

Thank you for your post! I have read it several times and it moved me to tears. There are a lot of similarities here.

In my case, I am absolutely certain that what I survived was an overdose of Madopar as the presence of Opicapone in my bloodstream makes the Madopar more effective /potent. That is why the total levodopa dose for the day should be reduced. I knew this but didn't know that this should have been done so early into the treatment.

In addition to the above my Neurologist denied, on two different occasions that such a thing exists. He still insists that 50 mg at night is the correct prescription, no need to reduce the amount of Madopar. I disagree.

I will not go into more details, it's suffice to say that what I went through when in A&E was horrendous.

I am so sorry that you are suffering so much. I hope you will be able to reduce the amount of Madopar you take per day, this certainly helps me - 100 mg down and the number of ectopics I was having is now much more bearable.

D.

[Gallowglass]

hi! Lots of good answers! My experience is only with Entacapone which worked for a month or two and gave me 15 minutes of extra ON time each time I took CL (2 pills of 25/100 C L four times a day). Then it stopped working at all so I quit taking it. No bad side effects taking it or stopping cold turkey.

So then I decided to try to reduce CL because it only gave me 1 hour ON time and 3 hours of horrible OFF times . So I started taking just one CL every two hours and gradually increasing the time between CL pills. I gradually went from 10 CL pills per day to 6! ON times are 45 minutes but the off time symptoms are not nearly as bad! My main OFF time symptoms are dizziness and painful dystonia. I’m getting a new Neuro in hopes of finding one who can help me get more ON time.

[Daisies22 in reply to Gallowglass]

Hi," 1 hour ON time and 3 hours of horrible OFF times"!

This sounds very familiar.

Going from 10 CL to 6 CL per day is a great achievement! I'm impressed.

All the best.

D.

[JerryinSATX]

I was put on Entacapone by my old neurologist when my off time was increasing. I was only taking 2x/day as it caused severe postural hypotension and racing heartbeat while on my daily walks.

My new MDS suggested the new version but I decided to decline. I’ve started going to the Y and exercise classes 5x/week and my average tremor time is ~ 30 minutes per day or less.

[Daisies22 in reply to JerryinSATX]

Exercise classes. May I ask what kind of exercise that is?(I'm pretty sure that in a few minutes I will be told to start walking fast but levodopa affects me so badly that I spend at least 8 hours per day unable to make any voluntary movements. During that time my whole body shakes uncontrollably.)

I'm finding the whole experience very distressing and physically and emotionally draining.

[JerryinSATX]

Here is a link to the Silver Sneakers exercise classes information: tools.silversneakers.com/Cl...

The person leading the class makes a lot of difference as to the energy level and fun. Luckily my Medicare insurance pays for my gym membership.

My schedule is

Monday- SS Circuit

Tuesday- SS Boom Muscle

Wednesday- rest day

Thursday- TRX (not SS) suspension straps body weight training

Friday- SS Enerchi & SS Yoga

Saturday- SS Reps FX

Sunday- rest day

[Daisies22 in reply to JerryinSATX]

Thank you. This is too intense for me. At the moment the aim is to walk half a mile a day...

[Fricnfrac1999]

My husband has tried both. He had no bad side effects with either but they absolutely didn't help any either so he would taking them. Last year he was 52 when he tried them. (During this he was on, and still is on, 25/100 CL and also pramipexole)

[Daisies22 in reply to Fricnfrac1999]

Thank you for your reply.Your husband is two years younger than me. Sometimes I wonder if Young Onset of Parkinson's disease is so different that nothing really works.

My Neurologist keeps saying that he has never had or heard of a case like mine. Perhaps this just gives him an excuse to do nothing to improve my quality of life

Best wishes.

D.

[Grey_Area]

I've weaned myself off Entacapone/Stalevo over the last week, and despite some bad days feel overall "better". One thing I've only just noticed is my appetite for food has returned; on the Entacapone I simply never felt properly hungry. 48 hours after stopping it, decent, honest hunger pangs returned. I've just enjoyed my first stir-fry in what seems like ages!

[Daisies22 in reply to Grey_Area]

Glad to hear that you feel better in the absence of Entacapone. Are you taking something else which smooths out the concentration of levodopa versus time curve? What medication are you on at the moment?As for myself I can say that I'm still waiting for my GP to respond. They must have got the electronic version of the prescription from the hospital ages ago! I'm already losing interest!

[Grey_Area in reply to Daisies22]

No, I'm not taking Entacapone or any sort of extender. Just back to two half Sinemet CR every six hours. Yes, off-time can last for a long time, but I don't feel as panicky or debilitated. Weakness is an increasing problem.

I have a specialist (neurologist) appointment on the 1st of August if I can get there so I'm hoping they'll listen to me this time. I've tried all their daft ideas. Maybe I can persuade them to listen to some of mine!

[Buckholt]

Davies, sorry if I’ve missed an update in a later post, but are you now taking Entacapone, and is so, how are you getting on?