About Parkinson Disease

Medications Overview

Physicians can use different combinations of the many available medical strategies based on the needs of each patient and physicians' treatment philosophy. Considerations related to the choice of medications include efficacy for symptomatic control, side effects, safety, practicality and cost.



Blockers and Inhibitors

These types of drugs block or inhibit the breakdown of levodopa or dopamine which in turn helps maintain dopamine levels in the motor neurons

Catecholamine-O-Methyltransferase (COMT) Inhibitor
COMT breaks down levodopa in the bloodstream reducing the amount that is able to cross the blood brain barrier to become available for conversion into dopamine in the brain. This class of drug blocks the action of the COMT enzyme which in turn maintains a higher level of L-dopa resulting in an increased the amount of dopamine (similar to action of carbidopa).

There are two types of COMT Inhibitors used in Parkinson's disease

  • Entacapone cannot cross the blood-brain barrier, and only works peripherally
  • Tolcapone can cross the blood brain barrier and prevents the breakdown of both dopamine and L-dopa by COMT enzymes in both the central and peripheral nervous system

Both must be taken with taken with levodopa in order for it to work

  • Entacapone (Comtan®)

Comtan®200 mg

  • Carbidopa/Levodopa + Entacapone (Stalevo®)

Stalevo®12.5/50/200 mg
Stalevo®25/100/200 mg
Stalevo®25/150/200 mg

  • Tolcapone (Tasmar®)

Tasmar® 100 mg
Tasmar® 200 mg

Monoamine Oxidase B (MOAB) Inhibitors
When released dopamine is not used (bound) in the transmission of the message, it can be taken back up into the releasing neuron. Monoamine Oxidase (MOA)is an enzyme that breaks down dopamine in the neuron (outside of the storage vesicles) to keep dopamine levels in the storage vesicles from over capacity. MAO-B (B is the type of receptor) inhibitors, bind to and inhibit the MAOB enzyme from breaking down dopamine. Prolonged use may enhance release of dopamine. MAOB Inhibitors can be taken alone (mono- therapy) or in combination with medications containing levodopa (adjunctive therapy).

  • Rasagiline (Azilect®) Azilect®1.0 mg, Azilect®.05 mg
  • Selegiline (Eldepryl®) Eldepryl®100 mg
  • Selegiline HCL Orally disintegrating (Zelepar®) Zelepar®1.25 mg

Dopamine Supplementation or Augmentation Therapy

Dopamine Agonists: Dopamine agonists are drugs that stimulate the parts of the human brain that are influenced by dopamine. In effect, the brain is tricked into thinking it is receiving the dopamine it needs. Dopamine Agonist therapy does not replace dopamine; it makes the existing dopamine more effective by binding to the same receptor sites on the neurons normally occupied by dopamine. These agonist stimulated neurons require less dopamine to complete the neural transmission.

Dopamine agonists can be taken alone (mono- therapy) or in combination with medications containing levodopa (adjunctive therapy)

  • Pramipexole (Mirapex®)

Mirapex®.125 mg
Mirapex®.25 mg
Mirapex®.50 mg
Mirapex®1.0 mg

  • Ropinerole (Requip®)

Requip®.25 mg
Requip®.50 mg
Requip®1.0 mg
Requip®2.0 mg
Requip®3.0 mg
Requip®4.0 mg
Requip®5.0 mg

  • Ropinerole (Requip XL®) Extended Release

Requip XL®2.0 mg
Requip XL®4.0 mg
Requip XL®8.0 mg

  • Apomorphine Hydrocloride injection (Apokyn®)

Common treatments for motor symptoms of Parkinson's disease

Dopamine Replacement Therapy
Although the dopamine deficiency causes the motor problems associated with PD, dopamine cannot cross the blood brain barrier (moving from the blood stream into the brain), and therefore it can’t be directly used as a medication to treat the disease. Levodopa is a precursor of the dopamine neurotransmitter and can be converted to dopamine once inside the brain.

Carbidopa/Levodopa: Levodopa is the gold standard medication for PD with the broadest antiparkinsonian effects of any treatment. In the brain, neurons typically convert levodopa to dopamine. Levodopa works by replacing the dopamine lost in PD. It is combined with carbidopa to prevent nausea and ensure levodopa is not metabolized before it enters the brain.

  • Carbidopa/Levodopa (Sinemet®)

Dosage:
Sinemet®10/100
Sinemet®25/100
Sinemet®25/250
Sinemet CR®25/100 (Controlled Release)
Sinemet CR®25/250 (Controlled Release)

Generic Carbidopa/Levodopa in immediate release form is available from a number of manufactures in the same dosages.

Rytary™ is an extended-release formulation of carbidopa/levodopa. It consists of capsules that contain beads of carbidopa and levodopa that dissolve and are absorbed at different rates. Following administration, therapeutic levodopa levels are relatively rapidly achieved (similar to carbidopa/levodopa immediate release [IR]) and are maintained for 4-5 hours. It is critically important to recognize that dosages of Rytary are not interchangeable with other carbidopa/levodopa products.

  • Carbidopa/Levodopa orally disintegrating (Parcopa®)

Parcopa® 10/100 mg
Parcopa® 25/100 mg
Parcopa® 25/250 mg

Now avialable in Generic Form in same dosage

  • Carbidopa/Levodopa+Entacapone (Stalevo®)

Stalevo®12.5/50/200 mg
Stalevo®25/100/200 mg
Stalevo®25/150/200 mg

Duopa™ is an enteral suspension of carbidopa and levodopa. Duopa is delivered continuously by a pump into the intestine for up to 16 hours daily. The maximum recommended daily dose of Duopa is 2000 mg of levodopa (i.e., one cassette per day) administered over 16 hours.

Other Medications

Anticholinergics: Anticholinergics do not act directly on the dopaminergic system. Instead, they decrease the activity of acetylcholine, a neurotransmitter that regulates movement and memory.

Amantadine (Symmetrel™) promotes the release of dopamine from nerve terminals, blocks its re-uptake and inhibits a glutamate receptor in the brain. It may decrease the activity of acetylcholine, which regulates movement and memory.

Droxidopa (Northera™) is a synthetic precursor of norepinephrine, which works to increase blood pressure in a condition that can accompany Parkinson’s disease called neurogenic orthostatic hypotension (NOH). This condition can cause an abnormal drop in blood pressure when changing positions.


 

 





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