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Dr. Bob is Robert Hsiung, MD,
bob@dr-bob.orgShown: posts 1 to 6 of 6. This is the beginning of the thread.
Posted by ed_uk on May 3, 2006, at 13:09:59
Sulpiride (Dolmatil) and amisulpride (Solian) are antipsychotics which are used in the treatment of schizophrenia. Although these drugs cause less EPS than typical APs, hyperprolactinemia is still a common problem, leading to numerous unpleasant side effects eg. sexual dysfunction, lactation etc.
Carmoxirole is a peripherally-acting dopamine agonist, it does not cross the blood brain barrier in significant quantities. In theory, carmoxirole could reverse amisulpride-induced hyperprolactinemia without affecting antipsychotic efficacy.
Eur J Pharmacol. 2002 Jun 28;447(1):109-14.
Carmoxirole is able to reduce amisulpride-induced hyperprolactinemia without affecting its central effect.Marchese G, Ruiu S, Casti P, Bartholini F, Saba P, Gessa GL, Pani L.
Neuroscienze S.c.a.r.l., Cagliari, Italy.
Prolactin blood level and apomorphine-induced yawning were studied in rats treated with the substituted benzamide amisulpride in association with bromocriptine or carmoxirole; two dopamine D(2) receptor agonists with high or low propensity to cross the brain-blood barrier, respectively. Administration of amisulpride produced a maximum increase in rat serum prolactin level (315+/-18%) vs. vehicle-treated animals (ED(50)=0.25+/-0.017 mg/kg, s.c.). The concurrent administration of carmoxirole or bromocriptine completely reversed the hyperprolactinemia induced by amisulpride (0.5 mg/kg, s.c.) (ID(50)=14.9+/-0.8 mg/kg and 0.81+/-0.03 mg/kg, respectively). Carmoxirole (15 mg/kg, i.p.) did not affect yawning induced by apomorphine (0.08 mg/kg, s.c.) nor amisulpride (0.5 mg/kg, s.c.) blockade of apomorphine-induced yawning. Conversely, a significant increase in the number of yawns was observed when bromocriptine (0.8 mg/kg, i.p.) was associated with apomorphine in the absence or presence of amisulpride. These results suggested that a peripheral dopamine D(2) receptor agonists could be a useful tool in alleviating amisulpride-induced hyperprolactinemia without possibly affecting its central effect.
.........................................unfortunately, carmoxirole is not available as a medication.
Ed
Posted by flip_flop on May 4, 2006, at 4:12:22
In reply to Carmoxirole - reducing amisulpride's side effects, posted by ed_uk on May 3, 2006, at 13:09:59
I recently started taking cabergoline (Cabaser) to reverse amisulpride-induced hyperprolactinemia. After 3 weeks on cabergoline, the prolactin levels were lower than before, so it seems to be working. I believe it takes a couple of months for the prolactin levels to become normalized.
Posted by blueberry on May 4, 2006, at 6:48:12
In reply to Carmoxirole - reducing amisulpride's side effects, posted by ed_uk on May 3, 2006, at 13:09:59
I saw a similar study for the dopamine agonist bromocriptine. They used it to lower prolactin in amisulpride patients and it had no effect on the amisulpride efficacy or other symptoms.
Posted by ed_uk on May 4, 2006, at 14:49:32
In reply to Re: Carmoxirole - reducing amisulpride's side effe, posted by flip_flop on May 4, 2006, at 4:12:22
I'm concerned that bromocriptine and cabergoline both cross the blood brain barrier. Antagonism of amisulpride's antipsychotic effect is possible.
Ed
Posted by flip_flop on May 5, 2006, at 3:56:28
In reply to Re: Carmoxirole - reducing amisulpride's side effe, posted by ed_uk on May 4, 2006, at 14:49:32
Doesn't amisulpride only have an antipsychotic effect (dopamine blockade) at high dosages?
Posted by ramsea on December 7, 2006, at 12:11:34
In reply to Re: Carmoxirole - reducing amisulpride's side effe, posted by flip_flop on May 4, 2006, at 4:12:22
I have been taking amisulpride for six months for bipolar depression and it has worked extremely well. I have taken up to 350mg but usually 200.
My prolactin level has shot up to 3400 where tops in this test for normal is 450, so I am sky-high.
I hate to give this drug up, but does anyone know--1)permanent damage that results from high prolactin?
2) is it dose related--like if I found that 50mg still helped me would my prolactin levels go down correspondingly?
This is the end of the thread.
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