Arcalion 200

vitamin derivative - sulbutamin

1. Arcalion 200Arcalion 200
Prepared byPrepared by:: Ph/Ahmed ElbaghdadyPh/Ahmed Elbaghdady

2. Composition:Composition:
Sulbutamine 200mgSulbutamine 200mg
•Excipient q.s.f. one coated tabletExcipient q.s.f. one coated tablet
Pharmaceutical Form:
Box containing two blisters of 20 sugar coated tablet
each.

3. Pharmacotherapeutic class: Pharmacotherapeutic class:
Psychostimulant Psychostimulant ““act on nervous systemact on nervous system””

4. Pharmacological actions: Pharmacological actions: ““ therapeutic therapeutic
IndicationIndication””::
(1) Treatment of Asthenia(1) Treatment of Asthenia
““Asthenia is a condition of chronic fatigue that is Asthenia is a condition of chronic fatigue that is
cerebral rather than neuromusclar in origincerebral rather than neuromusclar in origin””
(2) Improves memory through the potentiation of (2) Improves memory through the potentiation of
cholinergic dopaminergic and glutamargic cholinergic dopaminergic and glutamargic
transmissiontransmission..
•
•..

5. ))33((Beriberi or (Wernicke-Korsakoff psychosisBeriberi or (Wernicke-Korsakoff psychosis syndrome )vitamin B1 deficiencysyndrome )vitamin B1 deficiency
Beriberi is a nervous system ailment caused by a thiamine deficiency
(deficiency of vitamin B1) in the diet. Thiamine is involved in the breakdown of
energy molecules such as glucose and is also found on the membranes of neurons.
Symptoms of beriberi include severe lethargy and fatigue, together with
complications affecting the cardiovascular, nervous, muscular, and gastrointestinal
systems
Wernicke’s encephalopathy is the most frequently encountered manifestation of
thiamine deficiency in Western society

8. Sulbutiamine THIAMINE

Sulbutiamine is a synthetic derivative of thiamine )vitamin B
1
(. As a dimer of two
modified thiamine molecules, it is a lipophilic compound that crosses the blood-brain
barrier more readily than thiamine and increases the levels of thiamine and thiamine
phosphate esters in the brain.

9. 1-Thiamine is released by the action of phosphatase and pyrophosphatase in the
upper small intestine. At low concentrations, the process is carrier mediated and at
higher concentrations, absorption occurs via passive diffusion.
2-Active transport is greatest in the jejunum and ileum (it is inhibited by alcohol
consumption and by folic deficiency(.
3-. The cells of the intestinal mucosa have thiamine pyrophosphokinase activity, The
majority of thiamine present in the intestine is in the pyrophosphorylated form ThDP,
4-Discharge of the vitamin by those cells is dependent on Na+-dependent ATPase.
5-It is rapidly absorbed after intramuscular administration.

11. 1-The majority of thiamine in serum is bound to proteins, mainly albumin. Approximately
90% of total thiamine in blood is in erythrocytes.
2-Uptake of thiamine by cells of the blood and other tissues occurs via active transport
and passive diffusion. About 80% of intracellular thiamine is phosphorylated and most is
bound to proteins.
3-Human storage of thiamine is about 25 to 30 mg with the greatest concentrations in
skeletal muscle, heart, brain, liver, and kidneys. ThMP and free (unphosphorylated)
thiamine is present in plasma, milk, cerebrospinal fluid, and likely all extracellular fluids.
4-Unlike the highly phosphorylated forms of thiamine, ThMP and free thiamine are
capable of crossing cell membranes. Thiamine contents in human tissues are less than
those of other species.

12. sulbutamine reaches its maximum plasma concentration after 5 hours.
MSC
MEC
C
max
t
max
AUC
Therapeutic
range
(window)
Absorption
phase
Elimination
phase
P
l
a
s
m
a


C
o
n
c
e
n
t
r
a
t
i
o
n
Time

13. 1. Central Compartment
2. Peripheral Compartment(s)
3. Special Compartments

14. PHASE 1 reactions
PHASE 2 reactions

17. 1-Thiamine is mainly the transport form of the vitamin, while the active forms are
phosphorylated thiamine derivatives.
2-Thiamine functions as a coenzyme in more than 24 enzymes, most importantly
pyruvate dehydrogenase (for energy production in the Krebs cycle), transketolase (for
lipid and glucose metabolism, production of branched chain amino acids also in hexose
monophosphate shunt.
BICHEMICAL FUNCTION OF THIAMINE THIAMINE PRYOPHOSPHATEBICHEMICAL FUNCTION OF THIAMINE THIAMINE PRYOPHOSPHATE

18. 1-Thiamine monophosphate ThMP :
There is no known physiological
2-Thiamine diphosphate ThDP:
is a coenzyme for several enzymes that catalyze the transfer of two-carbon units and in
particular the dehydrogenation (decarboxylation and subsequent conjugation with
coenzyme A) of 2-oxoacids (alpha-keto acids(.

Examples include:
Present in most species
A-pyruvate dehydrogenase
B-(α-ketoglutarate dehydrogenase(
C-transketolase
3-Thiamine triphosphate (ThTP( :
Thiamine triphosphate (ThTP) was long considered a specific neuroactive form of
thiamine. However, recently it was shown that ThTP exists in bacteria, fungi, plants and
animals.
4-Adenosine thiamine triphosphate (AThTP( :
Adenosine thiamine triphosphate (AThTP) or thiaminylated adenosine triphosphate has
recently been discovered in Escherichia coli where it accumulates as a result of carbon
starvation.

19. 5-Adenosine thiamine diphosphate (AThDP( :
Adenosine thiamine diphosphate (AThDP) or thiaminylated adenosine diphosphate
exists in small amounts in vertebrate liver, but its role remains unknown.
All B vitamins are water-soluble, meaning that the body does not store them..

20. Thiamine in the Krebs Thiamine in the Krebs
CycleCycle

21. Thiamine in the Pentose Thiamine in the Pentose
Phosphate PathwayPhosphate Pathway

23. 1-When intakes at low level, little or no thiamine is excreted in the urine.

2-Amount ingested in excess of the minimal requirements are exerted in the
urine as intact thiamine or pyrmidine.
3-As the intake of thiamine is further increased more of the excess is excreted
unchanged.

24. Contraindications:Contraindications:
This drug must not be used in case of past history of allergy to one of This drug must not be used in case of past history of allergy to one of
the ingredient of the tablet.the ingredient of the tablet.
Find doubt, you mast ask you physician or pharmacist for adviceFind doubt, you mast ask you physician or pharmacist for advice..
Special warningsSpecial warnings : :
11--Due to the presence of lactose this drug shouldnDue to the presence of lactose this drug shouldn’’t be used in the t be used in the
case galactosemia, the syndrome of malabsorption of glucose and case galactosemia, the syndrome of malabsorption of glucose and
galactose or a deficit in lactose galactose or a deficit in lactose ““rare metabolic diseasesrare metabolic diseases””..
22--May be some very unhappy interactions in case you are using some May be some very unhappy interactions in case you are using some
other type of antidepressant in parallel as well special those treating other type of antidepressant in parallel as well special those treating
Bipolar diseaseBipolar disease..

25. GalactosemiaGalactosemia::
Lactose in food (such as dairy products) is broken down by the enzyme Lactose in food (such as dairy products) is broken down by the enzyme
lactase into glucose and galactose. In individuals with galactosemia, the lactase into glucose and galactose. In individuals with galactosemia, the
enzymes needed for further metabolism of galactose are severely enzymes needed for further metabolism of galactose are severely
diminished or missing entirely, leading to toxic levels of galactose-1-diminished or missing entirely, leading to toxic levels of galactose-1-
phosphate in various tissues, as in the case of classic galactosemia, phosphate in various tissues, as in the case of classic galactosemia,
resulting in hepatomegaly (an enlarged liver), cirrhosis, renal failure, resulting in hepatomegaly (an enlarged liver), cirrhosis, renal failure,
cataracts, brain damage, and ovarian failure. Without treatment, mortality in cataracts, brain damage, and ovarian failure. Without treatment, mortality in
infants with galactosemia is about 75%infants with galactosemia is about 75%..

26. Bipolar diseaseBipolar disease::
Bipolar disorders are one of several medical conditions called depressive Bipolar disorders are one of several medical conditions called depressive
disorders. Depressive disorders affect the way a person's brain functionsdisorders. Depressive disorders affect the way a person's brain functions. .

27. Drug interaction and other interaction:
To avoid possible interaction between. several drugs, always inform your physician or
your pharmacist if you are taking other medication.

28. Pregnancy and breast feeding:
1-The use of this drag should generally be avoided during pregnant if you discovers
that you are pregnant consult your doctor he alone can judge the necessity of
continuing treatment.
2-The use of this drug should be avoided in breast feeding women.
In both case seek the advice of you physician or pharmacist before taking a medication.

29. For adult use only oral Route.
2 to 3 tablets a day.
Tablets should be swallowed whole with a large glass of water, dividing
the doses between the morning and midday meals.
Duration of treatment is limited to 4 weeks.
This drug has been dispensed to you personally in specific situation:
1- it can’t be adapted to another case.
2- do not recommend it, to another person.
Dosage :

30. Adverse effects :
Like any active substance, in some individuals this drug may induce unpleasant
effects varying severity:
1- possibility of skill allergy, digestive disorders agitation, headache, tremor and
malaise.
Due to the presence of sunset yellow fcf. Risk of allergic reaction.
Tell your physician or yours pharmacist if you experience any undesirable and
unpleasant effect which are not mentioned in this leaf let.

31. Precautions:
If symptoms persist for more thane 4 weeks consults physician.
In doubt, do not hesitate to consult your physician or pharmacist for advice.

32. ReferencesReferences
11--Harper Biochemistry 23 editionHarper Biochemistry 23 edition..
22--Nutritional neuroscience Harris R. Nutritional neuroscience Harris R.
leiberemanleibereman..
33--MARTINDALE INDEX 30 editionMARTINDALE INDEX 30 edition..