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Madoka if you rearranged letters it says never do now get it dope as in weed david oppa is a drug used to treat parkinson’s disease and it’s motor symptoms it came from the herb that is known as mucuna pruriens and it’s found in the tropics and is well known for producing edge this herb has many different species that are found mostly in the tropical regions

Predominantly in india and africa in ancient times the seeds of amp earrings were used in the variety of interesting remedies especially in the traditional indian medicine practice called lavetta in the vedic times back then the seed was notably used for its anti-venom and anti-inflammatory property as an anti-venom has been claimed that if the seeds were swallow

Intact the individual will be productive for a full year against effects of any snake bites in india the seeds have traditionally been used as an aryan tonic and that’s an aphrodisiac for male virility in case you don’t know i forgot what parkinson’s disease is it is a neurodegenerative disorder characterized by a loss of dopaminergic neurons which lowers the

Level of dopamine in the substantia of the brain leading to parkinson’s patients experiencing symptoms such as resting tremors bradykinesia postural instability and muscle rigidity and this is where levodopa comes in to the rescue levodopa is a precursor of dopamine which is used to make a foot insufficient dopamine in parkinson’s patient example of commercially

Available products include concern as tablets and dual dopa as an intestinal gel for almost 50 years administration of loved oprah to patients with parkinson’s has helped to significantly improve the smooth motor movement in lowering blood pressure and increased the production and regulation of human growth hormone which benefits both men and women it is the most

Potent hormone in the human body and it controls the aging process let’s take a look at the structure of levodopa it is a naturally occurring amino acid as you can see from the name it is an acidic compound from the structure we can see a primary amine sitting right next to the carboxylic acid if in levodopa a little bit of basic property two phenyl groups on the

Left are weak acidic groups that make the molecule more polar and involves in hydrogen bonding carbocylic acid as you might guess is yet another acidic functional group that can act as hydrogen bond donor and acceptor it is also the key functional group that differentiates levodopa from dopamine despite levodopa being a polar acidic compound it is mostly absorbed

In the small intestine via large neutral amino acid transport machinery this is why high-protein diet with levodopa should be avoided as it will increase the competition for the amino acid transporter in the small intestine as well as the blood-brain barrier levodopa again the precursor amino acid of dopamine believe it or not is already in our body naturally and

Are exactly the same as the levodopa that we administer it originates from l-tyrosine through conversion by tyrosine hydrolyze to become levodopa it is nt carboxylase to form dopamine now nobody over by itself doesn’t do anything at all it is only useful once it is converted to dopamine that interacts with dopamine receptors for local synaptic neurotransmission

There are a lot of pathways in the brain associated with dopamine neurotransmission these are called dopaminergic pathways most notably the missal limbic pathway for reward system a positive reinforcement and nigrostriatal pathway for motor control and associative learning in general the therapeutic target of levodopa would be to successfully cross the blood-brain

Barrier and meet dope at the coppers laced in dopaminergic pathway to be converted to dopamine for synaptic neurotransmission moving on to the extraction of levodopa the extraction from empyrean nowadays is not widely used as a source for the dopa because it is less efficient and synthesis regardless here’s our works the most efficient way to extract levodopa from

Ambience is through a process called ml 1299 assuming a hundred grams of dried mill seeds are put into the process it will be divided with acetone by shaking for 48 hours every one temperature the deferred of material are extracted with water a throw in a one to one ratio then add a sorbic acid and shake overnight the residue are then removed by filtration then

Pool and concentrated is then crystallized and recrystallized in order to give pure crystals of levodopa of 1.78 grams which is 1.78 percent of yield after four days of processing and from that we can see why the production of levodopa is mainly from chemical synthesis the most efficient chemical synthesis is called ajinomoto process commercialized a new sputtered

Japanese that can have a dude of 80% levodopa in just twelve hours of process and the scale of production was reported to be a hundred ten tons per year of dopa now all this sounds very intricate but how in the world did we figure out l-dopa was appropriate for parkinson’s disease back in the mid twentieth century there was no high-throughput screening or any

Electronic library of molecules to test ligand receptor activities it was merely an educated guess by a swedish pharmacologist by the name of arvid carlsson in mid 1950s throughout his research for rezar pean a drug for schizophrenia he found that levodopa was able to remove the parkinsonian side-effect induced by rezar pain it was later confirmed by the austrian

Scientist ollie horning facch that the post modern brains of parkinsonian patients had depleted dopamine levels in the striatum of the brain in 1961 along with neurologist walter burke mayer they injected levodopa into 20 severely parkinsonian patients and achieved a temporary miracle witnessing the transition of rigid limbs to controlled movements for a few hours

Which was never achieved before by 1967 an oral dose of levodopa was developed by cordials and the large dose was administered to patients with severe pd and approved to significantly reduce parkinsonian symptoms however due to the high dose given the patient’s experience side effects that included nausea and vomiting so how do we make it better now the side

Effects experienced were due to levodopa being converted to dopamine in the periphery this meant that very little levodopa crossed the blood-brain barrier thus limiting its therapeutic effect and this is where carbidopa comes in carbidopa is a dopa decarboxylase inhibitor which is used in combination with levodopa to prevent the conversion of levodopa to dopamine

In the bravery ultimately this allows more levodopa to cross the blood-brain barrier to produce dopamine in the brain now this allowed to reduce the dosage administered and minimize the side effects experienced thus alleviating the associated clinical symptoms of parkinson’s disease with the knowledge of optimizing a compounds pharmacokinetics and pharmacodynamics

Scientists were eight to create a lover dokas little brother with very similar structures through chemical synthesis the compound is called mille of adobo levodopa is pretty much love adobo but with a methyl ester that certification of the carboxylic group increases the solubility by approximately 250 times it’s made as anna faris in tablet and our physiological

Ph mileva dopa exists in an ionized form whereas levodopa exists in ionized form thus increasing in slip of felicity to enhance its absorption across intestinal walls with a more rapid onset of action with a longer half-life compared to the combinational therapy of levodopa and carbidopa it is shown to have a shorter t max and c max which is an overall improvement

It is currently undergoing fda approval in the usa if you don’t believe what i’m saying so far here’s some proof back in 1969 a major study was completed to measure the effects of oral levodopa and 80 patients with parkinson’s disease 71 of these patients were seemed to have an improvement of more than 50% in their general performance while 90% of patients had

A partial improvement of all parkinsonian symptoms however a number of side effects were observed which include hypotension nausea confusion delusions and involuntary movements as good as levodopa sounds there are some negatives now almost 50 years since levodopa was first used the side effects caused by are still proving to be an issue scientists nowadays are

Working to counteract these adverse effects by targeting pathways that cause dyskinesia and impaired voluntary movements associated with the chronic use of levodopa and pd patients a study in 2016 by miguel’s involves using parkinson’s disease induced meit’s the effects of combination therapy using levodopa and a modified hirable remedy kd 5040 were measured

Using a number of behavioral tests the results indicated that the herb lowered the effective dose of levodopa and alleviated levodopa induced dyskinesia these findings suggest that the herb may be used as a complementary therapy to enhance the efficacy of levodopa and alleviate its adverse effects in patients with parkinson’s disease however this was only tested in

The particular mouse model and therefore further studies need to be done apart from that different dosage forms are also being developed for more convenient application or administration preferably a once a daily regimen researchers have attempted to formulate levodopa into a transdermal patch however it failed to reach the therapeutic efficacy of oral of adobo

Currently researchers are attempting to make an extended-release pro drug out of levodopa and are optimizing an intra intestinal gel application for continuous infusion of levodopa these two methods will hopefully improve the half-life of the drug and there you have it folks love adobo the gold standard treatment for parkinson’s disease since 1970 although it’s

Somewhat flawed improvements are surely on their way

Transcribed from video
Levodopa By Mert Aras