Sinemet – the safest form of L-dopa therapy available

Sinemet is at the forefront of treatment for those suffering from Parkinson’s disease. Although Parkinson’s disease cannot be cured, Sinemet helps to alleviate some of its symptoms, bringing relief to sufferers of the disease. However, as we will see below, Sinemet may not just be of interest to Parkinson’s disease sufferers. It is also known to increase levels of growth hormone – a subject that is often of great interest to life extensionists.

Before we look at just how Sinemet can help those with Parkinson’s disease, it is probably helpful to understand a little bit more about the disease itself.

Parkinson’s disease

The symptoms of Parkinson’s disease were first formally described by London physician James Parkinson (whose name was eventually given to the disease) back in 1817. However, historical references suggest that the disease itself has probably existed for thousands of years.

Parkinson’s disease affects 100,000s of people right around the world with both men and women being equally susceptible. In the United States, at least 500,000 people are believed to suffer from Parkinson’s disease, with about 50,000 new cases reported annually. In Australia, where more than 30,000 people live with illness, it is the second most common degenerative neurological condition after Alzheimer's disease. These figures are set to rise with our increasingly elderly populations because age is the biggest risk factor. The average age of onset of the disease is around 60 – with both prevalence and incidence increasing with advancing age. It is rare in people under the age of 40 (about 1 in 10 new diagnosis relate to people in this age group) but rises significantly in people aged over 70.

Parkinson’s disease is a progressive, neurodegenerative disorder of the nervous system with the symptoms manifesting themselves as a result of a lack of a neurotransmitter chemical called dopamine in the brain. Neurotransmitters act like the brain’s messenger service sending chemical messages between brain cells (neurons). When levels of dopamine fall significantly, the symptoms of Parkinson’s disease appear.

The reason that the symptoms affect movement in particular is due to the areas of the brain that are affected by this lack of dopamine. Hidden deep in the brain are specialised areas responsible for coordinating body movements and helping to keep the body’s muscular movements smooth and regular. These areas include the basal ganglia, the substantia nigra and the cerebellum. The series of nerve pathways that connect theses areas with each other relies upon dopamine manufactured in the substantia nigra to send the appropriate messages. In Parkinson’s disease, these pathways become disrupted because of the severe depletion of dopamine in the substantia nigra (the symptoms of Parkinson’s disease usually become apparent when dopamine levels have fallen by around 80%). This results in abnormalities in movement including one or more of the following:

• Tremor - an involuntary rhythmic shaking in an extremity (such as the hand, arm or leg) or in the face. The tremor lessens when the extremity affected is moved


• Bradykinesia - a medical term meaning slowness of movement. Initiating movement and changing positions becomes difficult. Walking becomes more of a shuffle and a sufferer may stoop. A lack of facial expression, with a fixed unblinking stare, is not uncommon. Even the voice is affected - it begins to sound monotonous and very quiet


• Muscular rigidity - especially in the arms, shoulders and neck


• Unfortunately these symptoms worsen over time although the rate of change varies from person to person. Depression is common, and about one in three sufferers experience dementia. Eventually the symptoms become so severe that the sufferer experiences difficulty in performing even the simplest of normal daily activities which means that they can no longer look after themselves.


• As yet the actual cause of these changes in the brain is not known. As we have said age is probably the greatest risk factor and it does appear that there is a tendency to genetic susceptibility (you are more likely to develop Parkinson’s disease if you have a relative with the disease). In some cases environmental toxins are thought to be to blame. Whatever the cause, a present we are limited to treating the symptoms.

How does Sinemet help?

In the early stages of the disease, treatment isn't always needed as the symptoms do not particularly affect daily life. The rate at which symptoms worsen is very individual. As the disease progresses, however, treatment becomes necessary.

Whilst there are several different drugs are available, Sinemet is most helpful in improving slow movement and muscle stiffness. It is also useful in helping to treat shaking, difficulty in swallowing and drooling.

As with many drugs used in the treatment of Parkinson’s disease, Sinemet contains Levodopa also called L-dopa. L-dopa is probably the best known of all Parkinson’s disease treatments. It would seem obvious to suggest that if the symptoms of Parkinson’s disease are caused by a lack of dopamine, then you should simply administer dopamine in order to reverse this depletion and alleviate the symptoms. The problem with this theory is that dopamine does not appear to cross the blood-brain barrier which means that the administered dopamine would not be able to enter the brain where it is required. This is where L-dopa takes centre stage. L-dopa is what is known as a metabolic precursor of dopamine. It can cross the blood-brain barrier, and can then be converted into dopamine in the brain where it is needed.

When it was introduced in the 1960s, L-dopa revolutionised the treatment of Parkinson’s disease and patients found that their symptoms literally disappeared overnight. But, it became apparent that after 3-5 years of L-dopa therapy, the drug’s effects wore off. Dosages needed to be gradually increased in order to try and produce the same level of relief from symptoms. This also meant that any side effects also increased and could even become more problematic to the sufferer than the disease itself.

Given this limitation on L-dopa therapy, doctors now generally resist using L-dopa in the early stages of Parkinson’s disease. But when treatment with L-dopa does become necessary, Sinemet stands out from other treatments because it is the safest form of L-dopa therapy available. This is due to the fact that Sinemet contains L-dopa in combination with Carbidopa, which helps to stop L-dopa crossing into blood before being delivered to the brain.

The slow release version of Sinemet is known as ‘Sinemet CR’ and contains 100mg of L-dopa and 25mg of Carbidopa. The “CR” denotes slow release.

Can Sinemet be used for anything other than treating the symptoms of Parkinson’s disease?

L-dopa is known to be a very potent anti-oxidant. The most common, ‘non-standard’ use of L-dopa is to increase growth hormone levels. One study demonstrated that healthy 60 year old men were able to boost their growth hormone levels to those of 30 year old men by taking a daily dose of 500mg of L-dopa. Increasing the level of human growth hormone in the ageing body back to a younger, more healthy level has been shown to provide a number of benefits including:

• Increasing energy and stamina
• Improving deep, restful sleep
• Sharpening thinking and improving memory
• Improving mood and the sense of well being
• Building muscle and increasing fitness
• Aiding weight loss
• Lowering blood pressure
• Regulating cholesterol levels

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Frequently Asked Questions About Sinemet®

Disclaimer: Please note that only your own physician can determine your precise needs, but in order to give you some information these answers are based upon the ‘average person’ and clinical/ published results.

Is it true that B6 diminshes the effectiveness of Sinemet?

The general consensus is that vitamin B6 helps to breakdown L-dopa (the active constituent of Sinemet) into dopamine - which is the neurotransmitter ‘lost’ in Parkinson's. In the past this was a caution as the result could be a flood of dopamine leading to side effects, however since Sinemet is L-dopa combined with Carbidopa, this actually slows down the release of dopamine and helps to prevent cross over into blood.

Therefore we cannot see there would be a great loss of effectiveness with Sinemet and B6 concurrent consumption. You may like to see our biochemists article for further information: www.antiaging-systems.com/extract/l-dopa.htm

Dosage

The usual starting dose is one 25/100mg tablet taken three times a day. This dose will then be adjusted depending on the severity of the condition, the response to the treatment and whether the patient is taking other medicines. Do not stop taking Sinemet, or lower the dosage, without seeking medical advice first.

If Sinemet is being taken to increase levels of growth hormone, the tablets are best taken prior to bedtime.

Side Effects

As with all medicines, taking Sinemet can result in unwanted side effects in a few people. Some of the side effects can be quite serious, others very mild but whatever the side effect, it should be discussed with a health care professional as soon as possible. Do not be alarmed by the lists below, many people do not experience any side effects at all and if they do they are usually very mild.

Listed below are some side effects that, if experienced, are generally mild in nature:

• Abnormal uncontrolled movements including muscle twitching or spasms, which may or may not resemble Parkinson's symptoms
• Dizziness or lightheadedness, particularly when standing quickly, which may be worsened by alcohol consumption. You should be careful driving or operating machinery until you know how Sinemet affects you.
• Nausea, vomiting, loss of appetite
• Dark saliva
• Dream abnormalities
• Sleepiness or sudden onset of sleep
• Slow movements
• Twitching or spasm of the eyelids
• Increased desire for sex
• Compulsive behaviours such as gambling, shopping, eating, taking medicines and repetitive purposeless activities

Some side effects, whilst generally rare, are more serious and should be reported immediately to your doctor. These include:

• Blood in the urine or difficult/painful urination
• Changes in mood such as depression
• Forgetfulness
• Signs of anaemia, such as tiredness, being short of breath, and looking pale
• Signs of frequent or worrying infections such as fever, severe chills, sore throat or mouth ulcers
• Bruising or bleeding more easily than normal, nose bleeds
• Fainting
• Skin rash, itchiness
• Pinkish, itchy swellings on the skin, also called hives or nettlerash
• Numbness or tingling in the hands or feet
• Signs of melanoma, such as new skin spots or changes to the size, shape, colour or edges of an existing skin spot, freckle or mole.

If you experience any of the following side effects tell your doctor immediately or go to accident and emergency at your nearest hospital. Again such side effects are generally rare:

• Swelling of the face, lips, mouth, throat or tongue which may cause difficulty in swallowing or breathing
• Bleeding from the back passage, black sticky bowel motions or bloody diarrhoea
• Vomiting blood or material that looks like coffee grounds
• Chest pain
• Fast or irregular heartbeats, also called palpitations
• Muscle stiffness accompanied by fever
• Mental changes such as feeling very fearful or paranoid, hallucinations
• Shortness of breath, difficulty breathing

Caution

Do not take Sinemet with other dopamine enhancing substances (such as Deprenyl or Hydergine) unless you are being supervised by your doctor. A British trial revealed an increase in mortality in Parkinson's patients who took both L-dopa and Deprenyl. We do not agree with the findings of this trial as there appear to be a number of flaws in it and many other trials have shown only beneficial results.

Do not take Sinemet if:

• You are allergic to it or any of its ingredients.
• You have any unusual skin lumps or moles which have not been examined by your doctor
• You have ever had skin cancer or melanoma
• You have narrow-angle glaucoma
• You are taking MAO inhibitors

If any of the following apply to you, you should discuss taking Sinemet with your doctor before you start taking it:

• You have or have had any medical conditions, particularly if you are suffering from depression, mental disturbances, heart disease (including arrhythmia), lung disease (including asthma), kidney, liver or hormonal problems, convulsions or fits, glaucoma or peptic ulcer disease
• You have had an increased desire for sex or compulsive behaviours such as gambling, shopping, eating, medicine use or repetitive purposeless activities with other medicines for Parkinson’s disease.
• You have previously been or are currently being treated with L-dopa
• You have any allergies to any other medicines or substances such as foods or dyes.

Before you start taking Sinemet, tell your doctor about any other medications that you are taking whether on prescription or bought over the counter as they could interfere with the actions of Sinemet.

Do not eat a high protein diet. If you do, the amount of levodopa absorbed by your body may be affected. If you are uncertain, your doctor, pharmacist or a dietician will be able to check your diet for you.

Pregnancy and breast feeding

If you are pregnant or planning on becoming pregnant, you should discuss this with your doctor before you start taking Sinemet. You will need to discuss the possible risks and benefits of using Sinemet.

Because one of the active ingredients in Sinemet passes into breast milk, you should not take Sinemet if you are breast feeding as your baby may potentially be harmed by it.

Sinemet is the safest form of L-dopa. This is because of its combination with Carbidopa, which helps prevent L-dopa crossing into blood before being delivered to the brain. Vitamin B6 helps to breakdown L-dopa into Dopamine, and for many years patients were told NOT to ingest B6 with L-dopa. Now the addition of Carbidopa in Sinemet has helped to prevent this process, and make it safer to use L-dopa. It is also believed to be beneficial if Vitamin C is taken with Sinemet as it is used in its pathways. Overall, Sinemet should remain a drug only for the most committed and knowledgeable life extensionist.