Drug information of lisuride

lisuride


An ergot derivative that acts as an agonist at dopamine D2 receptors (dopamine agonists). It may also act as an antagonist at dopamine D1 receptors, and as an agonist at some serotonin receptors (serotonin agonists).

Mechanism of effect

Lisuride is an anti-Parkinson drug chemically related to the dopaminergic ergoline Parkinson's drugs. Lisuride binds to the 5-HT(1A) and 5-HT(2A/2C) receptors. It is also thought to bind to the dopamine receptor and to act as a dopamine agonist. Evidence has also emerged that Lisuride also binds to the Histamine H1 receptor.

Pharmacodynamic

There is evidence that lisuride lowers prolactin levels and, in low doses, prevents migraine attacks.

Pharmacokinetics

Mechanism of action:

Lisuride is an anti-Parkinson drug chemically related to the dopaminergic ergoline Parkinson's drugs. Lisuride binds to the 5-HT(1A) and 5-HT(2A/2C) receptors. It is also thought to bind to the dopamine receptor and to act as a dopamine agonist. Evidence has also emerged that Lisuride also binds to the Histamine H1 receptor.
:Protein binding

about 15%


 

Drug indications

parkinson , Acromegaly

Parkinson's disease
Acromegaly
Suppression of lactation

Dosage

Oral
Parkinson's disease
Adult: Initially, 0.1 mg at bedtime, additional doses of 0.1 mg at wkly intervals may be given, 1st in the morning then at midday. Further increases of 0.1 mg wkly may be made until an optimum response is obtained, using the same sequence of increases, starting w/ the bedtime dose. Max: 2 mg daily in 3 or 4 divided doses.
Oral
Suppression of lactation
Adult: 0.2 mg bid to tid for 14 days starting w/in the 1st 24 hr of delivery or abortion.
Oral
Acromegaly, Hyperprolactinaemia-associated disorders
Adult: 0.1 mg in the evening of the 1st day, followed by 0.1 mg at midday and in the evening of the 2nd day, then 0.1 mg in the morning, at midday and in the evening of the 3rd day. Treatment is continued and adjusted according to prolactin levels (hyperprolactinaemia) or growth hormone levels (acromegaly).

Drug contraindications

Serious peripheral arterial disorders and coronary insufficiency. Concomitant use w/ phenylpropanolamine.

Side effects

Anxiety , nausea , dry mouth , vomiting , sweating

Nausea, vomiting, dry mouth, obstipation, peripheral oedema, sweating, hallucination, anxiety, confusion, nightmares, insomnia, decreased appetite, dyskinesia, somnolence, vertigo, headache, dystonia, myoclonus, orthostatic hypotension, cold extremities, erythromelalgia, palpitation, dyspnoea.

Enhanced sedative effect w/ drugs that have CNS depressant effects (e.g. benzodiazepines, antipsychotics). Mutual antagonistic effect w/ antipsychotic neuroleptics (except clozapine). Risk of vasoconstriction and/or hypertensive crisis w/ sympathomimetics (alpha and indirect) and vasoconstrictive ergot alkaloids. Increased risk of neuropsychic disorders w/ anticholinergic antiparkinsonians. Effects may be attenuated by neuroleptics and other dopamine antagonists.

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