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I looked through the existing saphris threads, but they're all pretty general. I'm wondering when people are taking it, and how much they're taking?

I'm the first person my pdoc's prescribed it for, so she doesn't have any of the feedback she usually would about what works best for people.

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I am taking it at the dose recommended for BP dx, 10 m.g. twice a day. It does not sedate me at all and manages my sx well at that dose.

I imagine you could try a lower dose for prophylaxis or whatnot but since I am cross tapering seroquel at the moment and that is tough, I am doing the standard dose.

Anna

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Let me preface my response with the fact that pdoc, tdoc and I have all commonly agreed upon the term "Med Weenie" to describe my tolerance for medication and its side effects. I'm usually relegated to what would be a kiddie-sized dose of medications, cutting things in half, or just being otherwise stuck with the smallest doses possible. That being said, I'm only on 5 mg of Saphris, once a day at bedtime. We had tried going up to 10 mg, but the side effects were more than my Med Weenie self could handle - major drowsiness, incredible joint pain, etc, so we backed it down to the 5 mg dose and the joint pain subsided, but the drowsiness was still pretty bad, so that's why it's a bedtime med for me. It's not a magic bullet for my depression or my paranoia, but it does tend to keep my manias in check fairly well. I guess I'm definitely not a typical case, but everyone is definitely different. Heck, a single Tylenol will knock me out for 12-16 hours, so I'm definitely the low end of the med tolerance spectrum.

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It seems like the onset of action would be fairly rapid, similar to other APs.

From RXList

Pharmacokinetics

Following a single 5-mg dose of SAPHRIS, the mean Cmax was approximately 4 ng/mL and was observed at a mean tmax of 1 hour. Elimination of asenapine is primarily through direct glucuronidation by UGT1A4 and oxidative metabolism by cytochrome P450 isoenzymes (predominantly CYP1A2). Following an initial more rapid distribution phase, the mean terminal half-life is approximately 24 hrs. With multiple-dose twice-daily dosing, steady-state is attained within 3 days. Overall, steady-state asenapine pharmacokinetics are similar to single-dose pharmacokinetics.

Absorption

Following sublingual administration, asenapine is rapidly absorbed with peak plasma concentrations occurring within 0.5 to 1.5 hours. The absolute bioavailability of sublingual asenapine at 5 mg is 35%. Increasing the dose from 5 mg to 10 mg twice daily (a two-fold increase) results in less than linear (1.7 times) increases in both the extent of exposure and maximum concentration. The absolute bioavailability of asenapine when swallowed is low ( < 2% with an oral tablet formulation).

The intake of water several (2 or 5) minutes after asenapine administration resulted in decreased asenapine exposure. Therefore, eating and drinking should be avoided for 10 minutes after administration [see DOSAGE AND ADMINISTRATION].

Distribution

Asenapine is rapidly distributed and has a large volume of distribution (approximately 20 - 25 L/kg), indicating extensive extravascular distribution. Asenapine is highly bound (95%) to plasma proteins, including albumin and α1-acid glycoprotein.

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It was rapid, Ss. I feel more stable than I have in a long time. Not sure if that's because i'm on a full therapeutic dose and was only on about 300 m.g. of quel because that's all I can tolerate, or if it's just a better med for me. i suspect the latter. It took me about 3 days to start feeling quite... different. LITERALLY like it was knitting things toegether in my haed that had been scattered for a long time, if that description makes any sense.

I plan to stay at current dosage unless i get wild and wacky side effects whilst I am reducing the benzos after seroquel is all gone (down to 0 tonight yay!) I see no reason to play around with it and reduce. i have no side effects, so eh?

Anna

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My pdoc was strange. She scoffed at the fact that people are supposed to take in both in the morning and at night, even though that's the right way to do it according to the med sheet. She also started me on only 5 mg. When it wasn't helping, she put me on 10 mg at night but still said don't take it in the morning. It seemed strange anyway. But for me it made me really irritable so I cannot say whether it helped or not...I had to switch to Risperdal because I started getting suicidal on it.

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It was rapid, Ss. I feel more stable than I have in a long time. Not sure if that's because i'm on a full therapeutic dose and was only on about 300 m.g. of quel because that's all I can tolerate, or if it's just a better med for me. i suspect the latter. It took me about 3 days to start feeling quite... different. LITERALLY like it was knitting things toegether in my haed that had been scattered for a long time, if that description makes any sense.

I plan to stay at current dosage unless i get wild and wacky side effects whilst I am reducing the benzos after seroquel is all gone (down to 0 tonight yay!) I see no reason to play around with it and reduce. i have no side effects, so eh?

Anna

I can totally see that. I'm already noticing in a big way that I'm waking up actually feeling AWAKE, for the first time in an awfully long time. So yeah, that parts all kinds of good. It is pretty sedating shortly after I take it, which is making twice daily dosing a challenge. But, once a day seems to be letting a little depression seep in, so... Hopefully it will all kind of even out, because I'm really liking the whole awake thing.

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I'm not sure of why the twice a day dosing, but it works for me quite well. i've never felt sedated for a minute on it, but then I drink a lot of coffee during the morning when i take THAT dose, and have been on seroquel for the most part since 1999. I think I am totally immune to sedating effects of AAPs other than seroquel now.... i mean, even on daytime quel, i COULD stay awake (sorta) if I really had to.

but, it was getting bad, and with everything going on and the cholesterol on top of it, I'm glad I had the brilliant thought of calling pdoc and asking for that change. it was just... time. and it is so much way better.

I think the sedation may wear off if you give it a bit, ss

Anna

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a lot of people do seem to dose it once a day and do alright sylvan, so it might be worth a try anyway. me, I am big on even coverage and even my Er depakote, I take some in the morning, and some at night. i have a little pill BOTTLE I CARRY around with me with stuff in it and stuff, heh. I have to take my klonopin at 7 and 3, the rest of my meds are either a.m. or p.m.

I am on such a ridiculous regimen anyway I just... don't worry about it.

Anna

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I'm not on this, but I'm considering it. Mostly I just want to comment on the schedule. I have meds that need to be taken twice a day. I have two pill boxes - night and day. I take my day dose at 2pm, so I don't have to worry about sleeping too late and missing them. Then I take the night ones before going to bed.. ends up being between 8-10.. I try to stick to that regardless if I'm actually going to bed at that time. It works very well for me. Just something to think about.

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  • 3 weeks later...

I'm a little late here, but I'll try anyway.

Right. But the thing is, I'd still have 50% of it in me.

Looking at the plasma levels, this would seem to be the case. However, Organon specifically said that 5 mg BID was the minimum effective dose before they even started clinical trials. They do not appear to have even used once-daily dosing for anything other than small-scale metabolic studies. While I don't know why Orangon chose BID dosing, it does seem to work, and there doesn't seem to be any efficacy data for once-daily dosing. You could always try taking it once a day and see if it works for you.

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Interestingly, there was some controversy inside the FDA about whether they should even approve the 10 mg BID dose. They did, however, advise Scherling-Plough to investigate a lower dose (2.5 mg BID), because they didn't actually establish the lowest effective dose:

It is not apparent from the studies you have conducted in schizophrenia that the lowest effective dose of asenapine has been identified. We request that you further characterize the utilization of asenapine in the treatment of adults with schizophrenia with a dose lower than 5 mg twice daily (e.g. 2.5 mg twice daily) through an adequate and well controlled trial.ref, page 4
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