Gene/Protein
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Symptom
Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
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Drug
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Target Concepts:
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Query: UMLS:C0027497 (
nausea
)
23,468
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
In a clinical trial the effect of L-deprenil, a selective irreversible inhibitor of monoamine oxidase (M.A.O.) "type B" in potentiating the anti-kinetic properties of levodopa has been investigated in 223 patients. Both drugs were given orally, levodopa as '
Madopar
' (levodopa plus the peripherally acting decarboxylase inhibitor, benserazide) 250 mg three times daily and L-deprenil 5 mg once or twice daily. The addition of L-deprenil to madopar therapy resulted in a statistically significant (P less than 0-01-0-001) reduction in patients' functional disability on average within 60 min after a single oral dose and lasting for 1 to 3 days. Dyskinesia occurred in 16 patients, psychosis in 14, orthostatic hypotension in 5, and
nausea
in 8. Reduction of the L-deprenil dose to 5 mg in these patients eliminated some of the side-effects. Two-thirds of the patients with side-effects had suffered from parkinsonism for between 7 and 15 years. 14% of the patients failed to respond to madopar-deprenil therapy. It is suggested that L-deprenil may act through inhibition of brain M.A.O. as well as by a psychostimulant effect similar to that of amphetamine which occurs through the release of dopamine. Both mechanisms would make more dopamine available at dopamine receptor sites.
...
PMID:Implications of combined treatment with 'Madopar' and L-deprenil in Parkinson's disease. A long-term study. 6 60
The multiple-dose (200 mg levodopa t.i.d.) pharmacokinetic profile of two controlled-release products of levodopa (
Madopar
HBS and Sinemet CR) was compared to conventional
Madopar
capsules in 18 healthy volunteers in a cross-over, randomized design. A pronounced controlled-release profile of the
Madopar
HBS and Sinemet CR product was demonstrated compared to conventional
Madopar
capsules with a significant (p < 0.001) decrease (-40 and -55%) in Cmax and a significant (p < 0.001) increase (+237 and +256%) in morning Cmin for the 200 mg t.i.d. dosage schedule. Almost equivalent bioavailability (85-90%) of levodopa was demonstrated for the controlled-release formulations relative to that of conventional
Madopar
capsules. The
Madopar
HBS formulation was bioequivalent with Sinemet CR with respect to levodopa, but it exhibited a moderately higher fluctuation index compared to Sinemet CR as a result of somewhat higher Cmax and lower Cmin values for the
Madopar
HBS formulation. 3-OMD (a metabolite of levodopa) levels were significantly (p < 0.05) higher for
Madopar
HBS and
Madopar
compared to Sinemet CR. The higher 3-OMD levels for the levodopa/benserazide combinations are consistent with a more potent decarboxylase inhibitory activity of benserazide as compared to carbidopa. The number of adverse events was highest for conventional
Madopar
(n = 18) compared to the controlled-release formulations (n = 12 for Sinemet CR and only 2 for
Madopar
HBS). A more efficient inhibition of dopamine formation from levodopa (resulting in higher 3-OMD levels) by
Madopar
HBS was consistent with the superior tolerability (especially for initial
nausea
) observed for the
Madopar
HBS formulation as compared to Sinemet CR.
...
PMID:Comparative multiple-dose pharmacokinetics of controlled-release levodopa products. 149 May 3
During a long-term double-blind study, which began February 1985, we have treated 16 patients with Morbus Parkinson or Parkinson's syndrome with deprenyl or identically appearing placebo tablets. The aim of the study is to ascertain whether a reduction of other antiparkinsonian medication, especially
Madopar
, can be achieved with deprenyl, in order to minimize the known late undesirable collateral effects ("on-off"-phenomena, dyskinesias). The criteria used in evaluation of the course of disease are the clinical-neurological findings as well as a series of motor performance tests. The results to date indicate that the dose of
Madopar
could be reduced in 7 of the 16 patients. Two of these patients were receiving
Madopar
alone, while 5 had been given anti-cholinergics in addition. In one female patient the dose of
Madopar
had to be reduced due to the development of dyskinesias. It is noteworthy that the psychological condition of the patients remained constant. There was no increase in side-effects, e.g. headaches, dizziness,
nausea
, etc. with administration of the study substance. In 3 patients with longstanding Parkinson's disease treated with
Madopar
or Nacom, who were not included in the study, the doses of the above drugs could be maintained or reduced by addition of deprenyl.
...
PMID:Levodopa and monoamine oxidase inhibitor combination therapy. A controlled clinical trial. 332 20