Skip to main content

BENSERAZIDE Uses, Side Effects, and More....

 BENSERAZIDE 

BRAND NAME:- Prolopa 


Benserazide is a peripheral decarboxylase inhibitor that increases the amount of levodopa crossing into the brain and its subsequent conversion to dopamine. 

PHARMACODYNAMIC:- 

When used as a therapy for treating Parkinson's disease, levodopa's specific mechanism of action revolves around its metabolism into dopamine in the body 3,2. Unfortunately, the resultant increase in the levels of circulating dopamine in the blood and to various extracerebral tissues can result in a number of side effects like nausea, vomiting, or even cardiac arrhythmias that may diminish patient adherence 3,2. A decarboxylase inhibitor like benserazide is consequently an effective compound to combine with levodopa as it is incapable of crossing the blood-brain barrier itself and therefore allows levodopa to elicit its primary action in the central nervous system, but will prevent the formation of dopamine from levodopa in extracerebral tissues - thereby acting to minimize the occurrence of extracerebral side effects.


MECHANISM OF ACTION:- 


The combination of levodopa and benserazide is an anti- Parkinsonian agent . Levodopa itself is the metabolic precursor of dopamine. In Parkinson's disease, dopamine is depleted to a large degree in the striatum, Pallidum, and substantia nigra in the central nervous system (CNS) . The administration of levodopa to treat the disease is subsequently proposed to facilitate raises in the levels of available dopamine in these areas . The metabolism of levodopa to dopamine occurs via the enzyme dopa decarboxylase, although unfortunately, this metabolism can also occur in extracerebral tissues . As a result, the full therapeutic effect of an administered dose of levodopa may not be obtained if portions of it are catabolized outside of the CNS and various patient adherence diminishing extracerebral side effects due to the extracerebral presence of dopamine like nausea, vomiting, or even cardiac arrhythmias can also happen .

Subsequently, a peripheral decarboxylase inhibitor like benserazide, which blocks the extracerebral decarboxylation of levodopa, when administered in combination with levodopa has obvious and significant advantages. Such benefits include reduced gastrointestinal side effects, a more rapid and complete response at the initiation of therapy, and a simpler dosing regimen .

It is important to note, however, that benserazide is hydroxylated to trihydroxybenzylhydrazine in the intestinal mucosa and the liver 3,2, and that as a potent inhibitor of the aromatic amino acid decarboxylase , it is this trihydroxybenzylhydrazine metabolite of benserazide that mainly protects levodopa against decarboxylation to dopamine in the gut and also around the rest of the body outside of the blood-brain barrier .

Regardless, because Parkinson's disease progresses even with the therapy of levodopa and benserazide, this kind of combined therapy is only ever indicated if it is capable of improving the quality of life and adverse effect profile of using such drugs for Parkinson's patients and there is little to be gained by switching to or starting this combination therapy if patients are already being managed with stable, effective, and well-tolerated levadopa-only therapy .

Finally, it is also proposed that benserazide hydrochloride may be able to treat beta thalassaemia by maintaining the active expression of the gene for fetal hemoglobin so that constant production of fetal hemoglobin may replace the missing adult hemoglobin variation that is characteristic of patients with the condition, thereby decreasing the need for blood transfusion therapy .


USED:- 

Benserazide is a medication used to treat Parkinson's disease, parkinsonism, and restless leg syndrome.


SIDE EFFECTS:- 

Dizziness, lightheadedness, nausea, vomiting, loss of appetite, trouble sleeping, unusual dreams, or headache may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly. This medication may cause saliva, urine, or sweat to turn a dark color.


DOSE:- DIRECTION BY PHYSICIAN.

Comments

Popular posts from this blog

Carbidopa Uses, Side Effects, and More

 Carbidopa Brand name:- lodosyn.  Carbidopa is always given with levodopa. It works by preventing levodopa from being broken down before it reaches the brain. This allows for a lower dose of levodopa, which causes less nausea and vomiting. Pharmacodynamic:-  When mixed with levodopa, carbidopa inhibits the peripheral conversion of levodopa to dopamine and the decarboxylation of oxitriptan to serotonin by aromatic L-amino acid decarboxylase. This results in an increased amount of levodopa and oxitriptan available for transport to the central nervous system. Carbidopa also inhibits the metabolism of levodopa in the GI tract, thus, increasing the bioavailability of levodopa. The presence of additional units of circulating levodopa can increase the effectiveness of the still functional dopaminergic neurons and it has been shown to alleviate symptoms for a time. The action of carbidopa is very important as levodopa is able to cross the blood-brain barrier while dopamine cannot...

BOTULINUM TOXIN Uses, Side Effects, and More

 BOTULINUM TOXIN ( A or B ) BRAND NAME:- BOTOX ,DYSPORT  BOTULINUM TOXIN  A and B are highly potent exotoxins produced by Clostridium botulinum that are responsible for ' botulism' ( a type of food poisoning). These neurotoxic proteins cause long- lasting loss of cholinergic transmission by interacting with axonal proteins involved in exocytotic release of Ach. Localized injection of minute quantity of botulinum toxin.  PHARMACODYNAMIC :- Botulinum toxin A inhibits the release of acetylcholine, relieving muscle contraction and spasm associated with many conditions, such as incontinence and dystonia. Cosmetically, botulinum toxin A paralyses muscles in the face to temporarily treat wrinkles. The maximum effects of muscle paralysis occur four to seven days after a dose.When injected at therapeutic doses, botulinum toxin A causes partial chemical denervation of muscle tissue, causing local reduction of muscle activity. Muscle atrophy may result, axonal sprouting may beg...

BENDROFLUMETHIAZIDE Uses, Side Effects, and More

 BENDROFLUMETHIAZIDE Brand name:- Bendrofulazide, Aprinox. BENDROFLUMETHIAZIDE is a type of medicine called a diuretic. It's used to treat high blood pressure (hypertension) and the build-up of fluid in your body (oedema). Diuretics are sometimes called "water tablets" because they make you pee more. This helps get rid of extra fluid in your body. Bendroflumethiazide is only available on prescription. It usually comes as tablets. It can also come as a liquid you swallow, but this has to be specially ordered.  PHARMACODYNAMIC:-  Bendroflumethiazide, a thiazide diuretic, removes excess water from the body by increasing how often you urinate (pass water) and also widens the blood vessels which helps to reduce blood pressure. It inhibits Na+/Cl- reabsorption from the distal convoluted tubules in the kidneys. Thiazides also cause loss of potassium and an increase in serum uric acid. Thiazides are often used to treat hypertension, but their hypotensive effects are not necessari...