Rotigotine

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Genes that may be involved
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Neupro; Belgium: Neupro; Bulgaria: Neupro; Cyprus: Neupro; Czech Republic: Neupro; Denmark: Neupro; Estonia: Neupro; Finland: Neupro; Germany: Neupro; Greece: Neupro; Hungary: Neupro; Ireland: Neupro; Italy: Neupro; Latvia: Neupro; Lithuania: Neupro; Luxembourg: Neupro; Malta: Neupro; Netherlands: Neupro; Poland: Neupro; Portugal: Neupro; Romania: Neupro; Slovakia: Neupro; Slovenia: Neupro; Spain: Neupro; Sweden: Neupro; UK: Neupro.

Drug combinations

Chemistry

Rotigotine: C~19~H~25~NO~S~. Mw: 315.47. (1) 1-Naphthalenol, 5,6,7,8-tetrahydro-6-[propyl [2-(2-thienyl)ethyl]amino-(6S)-; (2)(-)-(S)-5,6,7,8-Tetrahydro-6-[propyl[2-(2-thienyl)ethyl]amino]-1-naphthol; (3)(6S)-6-[Propyl(2-(2-thienyl)ethyl)amino]-5,6,7,8-tetrahydro-1-naphthalenol. CAS-99755-59-6 (2004).

Pharmacologic Category

Antiparkinsonian Agents; Non-Ergot-Derivative Dopamine Receptor Agonists. (ATC-Code: N04BC09).

Mechanism of action

A non-ergot dopamine agonist with specificity for D~3~-, D~2~-, and D~1~-dopamine receptors. Although precise mechanism of action of rotigotine is unknown, it is believed to be due to stimulation of postsynaptic dopamine D~2~-type auto receptors within substantia nigra in brain, leading to improved dopaminergic transmission in motor areas of basal ganglia, notably caudate nucleus/putamen regions.

Therapeutic use

Treatment of signs and symptoms of early-stage idiopathic Parkinson’s disease.

Pregnancy and lactiation implications

Fetal death and adverse effects on embryo-fetal development observed in some, but not all animal studies. There are no adequate, well-controlled studies in pregnant women. Excretion in breast milk unknown (not recommended in nursing women).

Unlabeled use

Contraindications

Hypersensitivity to rotigotine or any component of the formulation.

Warnings and precautions

Rare cases of pleural, retroperitoneal fibrosis and/or cardiac valvulopathy reported in patients treated with ergot-derived dopamine agonists, generally with prolonged use (potential of rotigotine to cause similar fibrotic complications unknown). May cause hallucinations. Dopamine agonists used for Parkinson’s disease or restless legs syndrome associated with compulsive behaviors and/or loss of impulse control. Risk for melanoma development increased in Parkinson’s disease patients. Dopamine agonists may cause orthostatic hypotension and syncope. Use with caution in risk of hypotension (such as patients receiving antihypertensive drugs) or where transient hypotensive episodes would be poorly tolerated (cardiovascular disease or cerebrovascular disease). Use commonly associated with somnolence. Use with caution in patients receiving other CNS depressants or psychoactive agents. Effects with other sedative drugs or ethanol may be potentiated. Use with caution in pre-existing cardiovascular disease (therapy associated with inconsistent increases in blood pressure, increased heart rate, and fluid retention). Use with caution in pre-existing dyskinesia (may be exacerbated). Patch may contain aluminum and sodium metabisulfite. Patch exposure to heat sources should be avoided (may result in severalfold increases in drug absorption). Therapy should not be discontinued abruptly. Other dopaminergic agents associated with syndrome resembling neuroleptic malignant syndrome on withdrawal and/or significant dosage reduction.

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