pramipexole

Pramipexole (INN, trade names Mirapex® and Sifrol®) is a medication indicated for treating Parkinson's disease and restless legs syndrome (RLS). It is also sometimes used off-label as a treatment for cluster headache or to counteract the problems with low libido experienced by some users of SSRI antidepressant drugs. Pramipexole has shown robust effects on pilot studies in bipolar disorder. Pramipexole is classified as a non-ergoline dopamine agonist.

Mechanism of action

The basal ganglia is a region of the human brain involved in the regulation of body movement; hence, when components of the basal ganglia are damaged, disorders of body movement may occur.

Parkinson's disease is a neurodegenerative disease affecting the substantia nigra, a component of the basal ganglia. The substantia nigra has a high quantity of dopaminergic neurons, which are neurons that release the neurotransmitter known as dopamine. When dopamine is released, it may activate dopamine receptors in the striatum, which is another component of the basal ganglia. When neurons of the substantia nigra deteriorate in Parkinson's disease, the striatum no longer receives dopamine signals. As a result, the basal ganglia can no longer regulate body movement effectively and motor function becomes impaired.

By acting as an agonist to the dopamine receptors, pramipexole may directly stimulate dopamine receptors in the striatum, thereby restoring the dopamine signals needed for proper functioning of the basal ganglia. Pramipexole affects the inhibitory D2-family of dopamine receptors, pramipexole is a depressant.

Pramipexole binds to dopamine receptors, with particularly high affinity for the D3 receptor subtype.[1]

Adverse effects

Some of the more common side effects of pramipexole include:[2]
  • Dizziness, lightheadedness, or fainting, especially when standing up (orthostatic hypotension)
  • Drowsiness
  • Hallucinations (seeing, hearing, or feeling things that are not there)
  • Weight loss
  • Nausea
  • Trouble in sleeping
  • Twitching, twisting, or other unusual body movements
  • Unusual tiredness or weakness
Several unusual adverse effects of this medication may include compulsive gambling, hypersexuality, and overeating. These side effects may be linked to the D3 receptor agonist activity of pramipexole. D3 receptors are located in brain regions involved in mood, behavior, and rewards.[3]

References

1. ^ Mierau J, Schneider F, Ensinger H, Chio C, Lajiness M, Huff R (1995). "Pramipexole binding and activation of cloned and expressed dopamine D2, D3 and D4 receptors.". Eur J Pharmacol 290 (1): 29-36. PMID 7664822. 
2. ^ MedlinePlus Drug Information: Pramipexole (Systemic). United States National Library of Medicine. Retrieved on 2006-09-27.
3. ^ Mayo Clinic Staff; M. Leann Dodd (July 15, 2005). Parkinson's drug can cause compulsive gambling. Mayo Clinic. Retrieved on 2006-09-27.

External links

An International Nonproprietary Name (INN; also known as rINN, for recommended International Nonproprietary Name) is the official non-proprietary or generic name given to a pharmaceutical substance, as designated by the World Health Organization (WHO).
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A medication, medicine or drug is any substance or combination of substances administered to human beings or animals to treat or prevent disease; alternatively to assist in medical diagnosis.
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Restless legs syndrome
Classification & external resources

Sleep pattern of a Restless Legs Syndrome patient (red) vs. a healthy sleep pattern (blue).
ICD-10 G 25.8
ICD-9 333.
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Off-label use is the practice of prescribing drugs for a purpose outside the scope of the drug's approved label, most often concerning the drug's indication. In the United States, the Food and Drug Administration (FDA) requires numerous clinical trials to prove a drug's safety and
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Cluster headache
Classification & external resources

The Cluster Headache by JD Fletcher
ICD-10 G 44.0
ICD-9 346.2

DiseasesDB 2850

eMedicine EMERG/229   NEURO/67
MeSH D003027 Cluster headaches
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Psychoanalysis

Constructs
Psychosexual development
Psychosocial development
Conscious • Preconscious • Unconscious
Id, ego, and super-ego
Libido • Drive
Transference • Sublimation • Resistance
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MeSH D001714

Bipolar disorder is a psychiatric condition defined as recurrent episodes of significant disturbance in mood. These disturbances can occur on a spectrum that ranges from debilitating depression to unbridled mania.
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Ergoline is a chemical compound whose structural skeleton is contained in a diverse range of alkaloids and a few psychedelic drugs (ololiuhqui, LSD). Ergoline derivitives are used clinically for the purpose of vasoconstriction (5-HT 1 Agonists - Ergotamine) and in the treatment of
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A dopamine agonist is a compound that activates dopamine receptors, mimicking the effect of the neurotransmitter dopamine.

Uses

Some medical drugs act as dopamine agonists; they are typically used for treating Parkinson's disease, and may be useful for restless legs
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The basal ganglia (or basal nuclei) are a group of nuclei in the brain interconnected with the cerebral cortex, thalamus and brainstem. Mammalian basal ganglia are associated with a variety of functions: motor control, cognition, emotions and learning.
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The human brain controls the central nervous system (CNS), by way of the cranial nerves and spinal cord, the peripheral nervous system (PNS) and regulates virtually all human activity.
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Neurodegenerative disease (Greek νέυρο-, néuro-, "nerval" and Latin dēgenerāre, "to decline" or "to worsen") is a condition in which cells of the brain and spinal cord are lost.
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The substantia nigra (Latin for "black substance", Soemering) or locus niger is a heterogeneous portion of the midbrain, separating the pes (foot) from the tegmentum (covering), and a major element of the basal ganglia system.
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The basal ganglia (or basal nuclei) are a group of nuclei in the brain interconnected with the cerebral cortex, thalamus and brainstem. Mammalian basal ganglia are associated with a variety of functions: motor control, cognition, emotions and learning.
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Neurons (also known as neurones and nerve cells) are electrically excitable cells in the nervous system that process and transmit information. In vertebrate animals, neurons are the core components of the brain, spinal cord and peripheral nerves.
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Neurotransmitters are chemicals that are used to relay, amplify and modulate signals between a neuron and another cell. According to the prevailing beliefs of the 1960s, a chemical can be classified as a neurotransmitter if it meets the following conditions:

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Dopamine is a hormone and neurotransmitter occurring in a wide variety of animals, including both vertebrates and invertebrates. In chemical structure, it is a phenethylamine.
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striatum is a subcortical part of the telencephalon. It is the major input station of the basal ganglia system. Anatomically, the striatum is the caudate and the putamen.

History


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agonist is a substance that binds to a specific receptor and triggers a response in the cell. It mimics the action of an endogenous ligand (such as hormone or neurotransmitter) that binds to the same receptor.
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Dopamine receptors are a class of metabotropic G protein-coupled receptors that are prominent in the vertebrate central nervous system (CNS). The neurotransmitter dopamine is the primary endogenous ligand for dopamine receptors.
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striatum is a subcortical part of the telencephalon. It is the major input station of the basal ganglia system. Anatomically, the striatum is the caudate and the putamen.

History


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Dopamine receptors are a class of metabotropic G protein-coupled receptors that are prominent in the vertebrate central nervous system (CNS). The neurotransmitter dopamine is the primary endogenous ligand for dopamine receptors.
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MeSH D007024 Orthostatic hypotension (also known as postural hypotension, orthostatic intolerance and, colloquially, as head rush or a dizzy spell
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A hallucination is a perception in the absence of a stimulus that is believed to be genuine, ie. the subject experiences an imaginary stimulus as being real. A pseudohallucination is similar to an hallucination in all respects except that of absolute belief in the authenticity of
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Nausea
Classifications and external resources

ICD-10 R 11.
ICD-9 787.0

Nausea (Latin: Nausea, Greek: Ναυτεία
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Sleep is the state of natural rest observed throughout the animal kingdom, in all mammals and birds, and in many reptiles, amphibians, and fish.

In humans, other mammals, and many other animals that have been studied — such as fish, birds, ants, and fruit-flies —
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Problem gambling is an urge to gamble despite harmful negative consequences or a desire to stop. The term is preferred to compulsive gambling among many professionals, as few people described by the term experience true compulsions in the clinical sense of the word.
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Hypersexuality
Classification & external resources

ICD-10 F 52.7
ICD-9 302.89

Hypersexuality is desire to engage in human sexual behavior at a level high enough to be considered clinically significant.
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Overeating is a behavior that, while generally not a medical problem, in some cases is a symptom of binge eating disorder or bulimia. In more general terms it refers to the persistent consumption of excess food in relation to the energy that the person expends, leading to weight
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