Carbidopa/levodopa , also known as levocarb and co-careldopa , is a combination of two carbidopa and levodopa medications. It is mainly used to manage the symptoms of Parkinson's disease but does not change the course of the disease. It was taken by mouth. It takes two to three weeks of treatment before the benefits are seen. Each dose then begins to work in about ten minutes with an effect duration of about five hours.
Common side effects include movement problems and nausea. More serious side effects include depression, low blood pressure with standing, sudden drowsiness, psychosis, and increased risk-taking behavior. Carbidopa prevents splitting of levodopa outside of the brain. In the brain, levodopa is broken down into dopamine which has its effect.
It's in the List of Essential Medicines of the World Health Organization, the most effective and safe drugs needed in the health system. It is available as a generic drug and quite expensive. Wholesale prices in developing countries are around 1.80 to 3.00 USD per month. In the United States, a month's supply is about 50 to 150 USD.
Video Carbidopa/levodopa
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Penyakit Parkinson
It is mainly used to improve the symptoms of Parkinson's disease but does not change the course of the disease. It takes two to three weeks of treatment before the benefits are seen. Each dose then begins to work in about ten minutes with an effect duration of about five hours.
Formulations that can be given in an intra-intestinal pump, known as Duodopa are being developed.
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Other uses include doponia-responsive dystonia (DRD) and restless leg syndrome.
There is tentative evidence that it is useful in amblyopia when used with other treatments.
Maps Carbidopa/levodopa
Side effects
Common side effects include movement problems, and nausea. The most common early adverse event is hallucinations, since the movement problem materializes 5-10 years after starting treatment. More serious side effects include depression, low blood pressure with standing, sudden drowsiness, and drive to gamble, engaging in sexual behavior, or other risk-taking behavior.
Action mechanism
Levodopa is converted to dopamine by the action of a naturally occurring enzyme called DOPA decarboxylase. It occurs both in peripheral circulation and in the central nervous system after levodopa has passed the blood-brain barrier. Activation of central dopamine receptors improves symptoms of Parkinson's disease; However, activation of peripheral dopamine receptors causes nausea and vomiting. For this reason levodopa is usually given in combination with DOPA decarboxylase inhibitors (DDCI), in this case carbidopa, which is highly polar (and imposed on physiological pH) and can not cross the blood-brain barrier, but prevents peripheral conversion of levodopa to dopamine. and thus reduce the undesirable peripheral side effects of levodopa. The use of carbidopa also increases the quantity of levodopa in the bloodstream that is available to enter the brain.
History
In 1960 the Austrian biochemist By Hornykiewicz, while at the University of Vienna, examined the autopsy results of patients who died with Parkinson's disease. He suggested that the disease was associated with, or caused by, a decrease in dopamine levels in the basal ganglia of the brain. Because dopamine itself does not enter the brain, it attempts to treat twenty patients with a mixture of racemic dihydroxypenylalanine (DOPA), which can enter the brain and convert there into dopamine by DOPA decarboxylase action. The results are positive, as do other experiments in Montreal run by AndrÃÆ'Â © Barbeau. Unfortunately, other researchers were unable to replicate these early results, and the use of DOPA remained in question until 1967, when George Cotzias at Brookhaven National Laboratories in Upton, New York, used DOS megadoses, up to 16 grams per day. Not long after these results are known, Curt Porter at Merck shows that L-DOPA is an active stereoisomer, thus reducing the effective dose to half.
With L-DOPA identified as an active form, Alfred Pletscher and his colleagues at Hoffman-LaRoche synthesized benserazide, DOPA decarboxylase inhibitors, which further reduced the required dose. Drugs that combine L-DOPA with benserazide are marketed under the Madopar brand name. Independent work was done by Victor Lotti at Merck in West Point, Pennsylvania. Merck has synthesized and patented carbidopa, another dopa decarboxylase inhibitor in 1962, and in 1971 Lotti showed that the use of L-form of carbidopa, further reduced therapeutic dosage of L-DOPA. The combination of L-carbidopa and L-DOPA is marketed under the Sinemet brand name.
Society and culture
Cost
It is available as a generic drug and quite expensive. Globally, the wholesale price of this drug is about 1.80 to 3.00 USD per month. In the United States, a month's supply is about 50 to 150 USD.
Name
The generic name under the BAN system is Co-careldopa.
It is sold under several brand names, including Sinemet (Merck Sharp & Dohme Limited), Pharmacopa, Atamet, Apo-Levocarb, Duodopa, Kinson, and Pharmacopa, among others.
Extended release formulations are sold as Rytary and Sinemet-CR. The extended-release enteral solution is sold as Duopa.
Disadvantages
In 1991, Merck licensed the right to manufacture and sell Sinemet to a newly created joint venture, DuPont Merck Pharmaceutical Company. In the same year, approvals for sustained release formulations (Sinemet CR) that could be taken less frequently were also obtained. DuPont purchased Merck's shares in a joint venture in 1998 and began operating the company as DuPont Pharmaceuticals (DuPont Pharma), but Merck continued to manufacture drugs for DuPont. Beginning in late 2009 and continuing through 2011, Merck discontinued drug-making pending regulatory approval due to changes in active ingredient suppliers. This resulted in the shortcomings of Sinemet and Sinemet CR brand name products, although alternative generic versions are still available.
Other deficiencies seem to occur; seems to have started in late 2017.
See also
- Stalevo in combination with entacapone
References
External links
- Levodopa and Carbidopa in the U.S. National Library of Medicine, National Institutes of Health
- SinemetÃ,® CR Product Monograph at Merck Canada
- SinemetÃ,® Data Sheet at Ministry of Health, New Zealand
Source of the article : Wikipedia
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