The document discusses prostaglandin-endoperoxide synthase (PTGS), also known as cyclooxygenase (COX), which is responsible for the formation of prostanoids like prostaglandins. It has two isoforms, COX-1 and COX-2. COX-1 is constitutively expressed and regulates normal physiological functions, while COX-2 is induced during inflammation. Non-steroidal anti-inflammatory drugs (NSAIDs) inhibit these enzymes to reduce inflammation. Several NSAIDs are described, including their mechanisms of action, medical uses, and potential adverse effects.
synthesis of hetero-cyclic drugs which act as anti-malarial drugs where you get all information about synthesis, preparation, properties, uses of drugs.
synthesis of hetero-cyclic drugs which act as anti-malarial drugs where you get all information about synthesis, preparation, properties, uses of drugs.
Contents includes at least three strategies of synthesis for each of three, four, five and six membered heterocylic ring with one or two heteroatoms. One mechanism described out of the three strategies. Few name reactions are described and the other are simple synthetic methods. This presentation was prepared for the partial fulfillment of Master of Pharmacy. The content was taken from the various books, mentioned in slide with the title of references.
Active constituent of drugs used in diabetic therapyAkshay Kank
In this slide the active constituents which is isolated from herbal sources used for to treat the type 1 and type 2 diabetes is covered. 'Gymnema' and 'swerita chirata' herbal plant is also covered in the slide.This work help in to focus the herbal emphasis on diabetes.
Chemistry of Prostaglandins, leukotrienes and thromboxanes(Advance medicinal ...Rohit kaushiK.
1st discovered in human serum in 1930, were found to be stimulate uterine contraction and reduce pressure.
Presumed to be synthesized by prostate gland hence the name.
Later found that synthesized in all tissue except erythrocytes.
It have a cyclopentane ring (formed from 8 to 12 carbon atoms) and two side chains, with carboxyl group on one side.
They differ In their structure due to substituent group double bond on cyclopentane ring.
Prostaglandins are structurally resemble with prostanoic acid, 20-carbon fatty acid.
Abbreviated as PG, with the class designated by a capital letter A,B,D,E,F,G,H and I, followed by a number.
PGE and PGF; 1st isolated from the biological fluids.
The letters refer to the different ring structure, except in PGG and PGH: same ring structure (cyclo endohydroperoxide).
In the same series, depending upon double bonds on the side chains designated as PGE1, PGE2, PGE3..etc
The number of double bonds varies from 1-3.
PROSTAGLANDINS RECEPTORS
They function close to the site of synthesis and are deactivated to inactive metabolites before moving into the circuation.
Act locally in very low concentration, and acts on GPCR receptors.
INHIBITION OF PROSTAGLANDINS
Corticosteroids (e.g. cortisol) prevent the formation of arachidonic acid by inhibiting the enzyme phospholipase A2.
Anti inflammatory drugs inhibits the synthesis of prostaglandins.
They block the action of cyclooxygenase.
Aspirin irreversibly inhibits cyclooxygenase.
DEGRADATION OF PROSTAGLANDINS
All eicosanoids are metabolized rapidly.
Degradation mainly occurs in liver and lung.
Two enzymes, namely 15-α-hydroxy PG dehydrogenase & 13-PG reductase, convert hydroxyl group at C15 to keto group & then to C13 and C14 dihydroderivative.
BIOCHEMICAL ACTION OF PROSTAGLANDINS
The Prostaglandins (PGE, PGA, & PGI2) are vasodilator in nature. So they decreases blood pressure.
PGE1 & PGE2 induce the symptoms of inflammation (redness, swelling, edema etc.) due to arteriolar vasodilator, and cause rheumatoid arthritis, psoriasis etc. so Corticosteroids are used to treat these conditions.
PGE2 & PGF2 are used for the medical termination of pregnancy and induction of labor.
Pyrogens (fever causing) promote PG synthesis leading to the formation of PGE2.
Migraine is also due to PGE2.
PGE2 along with histamine and bradykinin causes pain.
PGI2 inhibit platelet aggregation.
They are used in the treatment of gastric ulcers, hyoertention, thrombosis, asthma etc.
Prostaglandins are also employed in the medical termination of pregnancy, prevention of conception, induction of labor etc.
Leukotrienes are synthesized by leucocytes, mast cells, lung, heart, spleen etc. by lipoxygenase pathway of arachidonic acid.
Leukotrienes are 20- Carbon polyenoic fatty acids having a number of substituents.
Depending upon the substitutions, they are divided into LTA, LTB, LTD, and LTE.
Each type is divided into sub-groups depending upon the number of double bonds which vary from 3-5.
Leukotrienes possess
Contents includes at least three strategies of synthesis for each of three, four, five and six membered heterocylic ring with one or two heteroatoms. One mechanism described out of the three strategies. Few name reactions are described and the other are simple synthetic methods. This presentation was prepared for the partial fulfillment of Master of Pharmacy. The content was taken from the various books, mentioned in slide with the title of references.
Active constituent of drugs used in diabetic therapyAkshay Kank
In this slide the active constituents which is isolated from herbal sources used for to treat the type 1 and type 2 diabetes is covered. 'Gymnema' and 'swerita chirata' herbal plant is also covered in the slide.This work help in to focus the herbal emphasis on diabetes.
Chemistry of Prostaglandins, leukotrienes and thromboxanes(Advance medicinal ...Rohit kaushiK.
1st discovered in human serum in 1930, were found to be stimulate uterine contraction and reduce pressure.
Presumed to be synthesized by prostate gland hence the name.
Later found that synthesized in all tissue except erythrocytes.
It have a cyclopentane ring (formed from 8 to 12 carbon atoms) and two side chains, with carboxyl group on one side.
They differ In their structure due to substituent group double bond on cyclopentane ring.
Prostaglandins are structurally resemble with prostanoic acid, 20-carbon fatty acid.
Abbreviated as PG, with the class designated by a capital letter A,B,D,E,F,G,H and I, followed by a number.
PGE and PGF; 1st isolated from the biological fluids.
The letters refer to the different ring structure, except in PGG and PGH: same ring structure (cyclo endohydroperoxide).
In the same series, depending upon double bonds on the side chains designated as PGE1, PGE2, PGE3..etc
The number of double bonds varies from 1-3.
PROSTAGLANDINS RECEPTORS
They function close to the site of synthesis and are deactivated to inactive metabolites before moving into the circuation.
Act locally in very low concentration, and acts on GPCR receptors.
INHIBITION OF PROSTAGLANDINS
Corticosteroids (e.g. cortisol) prevent the formation of arachidonic acid by inhibiting the enzyme phospholipase A2.
Anti inflammatory drugs inhibits the synthesis of prostaglandins.
They block the action of cyclooxygenase.
Aspirin irreversibly inhibits cyclooxygenase.
DEGRADATION OF PROSTAGLANDINS
All eicosanoids are metabolized rapidly.
Degradation mainly occurs in liver and lung.
Two enzymes, namely 15-α-hydroxy PG dehydrogenase & 13-PG reductase, convert hydroxyl group at C15 to keto group & then to C13 and C14 dihydroderivative.
BIOCHEMICAL ACTION OF PROSTAGLANDINS
The Prostaglandins (PGE, PGA, & PGI2) are vasodilator in nature. So they decreases blood pressure.
PGE1 & PGE2 induce the symptoms of inflammation (redness, swelling, edema etc.) due to arteriolar vasodilator, and cause rheumatoid arthritis, psoriasis etc. so Corticosteroids are used to treat these conditions.
PGE2 & PGF2 are used for the medical termination of pregnancy and induction of labor.
Pyrogens (fever causing) promote PG synthesis leading to the formation of PGE2.
Migraine is also due to PGE2.
PGE2 along with histamine and bradykinin causes pain.
PGI2 inhibit platelet aggregation.
They are used in the treatment of gastric ulcers, hyoertention, thrombosis, asthma etc.
Prostaglandins are also employed in the medical termination of pregnancy, prevention of conception, induction of labor etc.
Leukotrienes are synthesized by leucocytes, mast cells, lung, heart, spleen etc. by lipoxygenase pathway of arachidonic acid.
Leukotrienes are 20- Carbon polyenoic fatty acids having a number of substituents.
Depending upon the substitutions, they are divided into LTA, LTB, LTD, and LTE.
Each type is divided into sub-groups depending upon the number of double bonds which vary from 3-5.
Leukotrienes possess
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Acenofenac and acetaminophen( paracetamol) role as N.S.I.D in the treatment of pain and Inflammation with pharmacology and indication, adverse effects and contraindications
The Indian Dental Academy is the Leader in continuing dental education , training dentists in all aspects of dentistry and
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Acids and bases buffers ARRHENIUS CONCEPT
THE LEWIS CONCEPT-THE ELECTRON DONOR ACCEPTOR SYSTEM
BRONSTED-LOWRY CONCEPT (PROTON TRANSFER
THEORY
buffer action
ph scale
buffer capacity
acid base balance
isotonicity method
isotonic soltions
buffer solutions in pharmaceutical preparations
WHAT IS PHARMACOPOEIA?
TYPES OF PHARMACOPOEIA
HISTORY OF PHARMACOPOEIA
CONTENT OF PHARMACOPOEIA
WHAT IS MONOGRAPH?
PURPOSE OF MONOGRAPH
TYPES OF MONOGRAPH
IMPORTANCE OF CONTENT OF MONOGRAPH
MONOGRAPH DEVELOPMENT PROCESS
Definition of Impurity
Types of Impurities
Sources of Impurity
foreign unwanted matter present in a compound which are differ from the actual molecular formula.
According to ICH “An impurity in a drug of the new drug substance that is not the substance”.
Chemically a compound is impure if it contains undesirable foreign matter i.e. impurities. Thus chemical purity is freedom from foreign matter
Impurities can have unwanted pharmacological or toxicological effect that seriously impact product quality and patient safety.
The International Conference on Harmonization (ICH) has formulated a workable guideline regarding the control of impurities.
Impurities in pharmaceutical are the unwanted chemicals that remains with the active pharmaceutical ingredient (API’s), or develop during formulation or upon aging of both API and formulated API’s to medicine.
The presence of the unwanted chemicals, even in small amount , may influence the efficacy and safety of pharmaceutical product
Recrystallization is the most convenient method for purifying organic compounds that are solids at room temperature.
Compounds obtained from natural sources, or from reaction mixtures, almost always contain impurities.
The impurities may include some combination of insoluble, soluble, and colored impurities. To obtain a pure compound these impurities must be removed.
Each type of impurity is removed in a separate step in the recrystallization procedure.
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Digital Tools and AI for Teaching Learning and Research
Cox inhibitor
1. Miss. Aarti V. Shingan
M. Pharm in pharmaceutical Chemistry
2. Known as :prostaglandin-endoperoxide
synthase(PTGS)
Responsible for formation of prostanoides
1.prostaglandin,
2.thamboxen,
3.prostacylin.
Involved in the inflammtory Responce.
3. Contains two separate active sites for
prostaglandin synthase
One side contains the cyclooxygenase active
The Opposite active side active side contains
peroxidase active site which is Involved in
activating the heme group neccesory for
cyclooxygenase reaction
It has two forms COX-1 and COX-2.
4. Continiously stimulate by the body
Constitutive (its concentration in the body
remain stable)
creates prostaglandin uses for basic house
keeping throughout the body
Prostaglandin stimulate normal body
function such as stomach mucous
production, regulation of gastric acid and
kidney water
5. Induced ( normally not in present in cells)
Built only in special cells (Ex: lung cells)
Used for singnaling pain and inflamation
Produces prostaglandins for inflammtory
responce
Stimulated only as part of immune
responce
Production is stimulated by inflammtory
cytokines and growth factors
11. Properties :
Colour: pale yellow
appearance: crystalline powder
solubility: soluble in water sparingly soluble in alcohol
M.P : 155-162 0C
chemical formula: C19H21ClNNaO7
Assay: the sample in acetone and pass nitrogen for 15 min
and titrate with 0.1M NAOH using phenolphthalein as
indicator.
12. 1. The centre of acidity is usually located one carbon atom
adjecent to a flat surface represented by an aromatic or hetero
aromatic ring .
2. The distance between these centre is critical because
increasing this distance to two or three carbon generally
decreasing activity.
3. Increasing acidity of of COOH group Increasing activity.
4. Substitution of methyl group on the carbon atom separating
the aromatic ring leads to the enhancement of anti-
inflammatory activity.
14. Mechanism of action :
indomethacin ,a non –steroidal anti-inflmmatory drug
(NSAIDs) ,it is a selective COX-1 inhibitor
the enzyme that participate in prostaglandin synthesis
from archidonic acid
Prostaglandin are hormone like molecule normally found in
the body , where they have a wide variety of effects, some
of which leads to pain ,fever, and inflammation.
By inhibiting the synthesis of prostaglandins , indomethacin
can reduce pain, fever, and inflammation.
15. Medical uses:
indomethacin is an analgesic,antipyretic and anti-
inflammatory . Clinical indication for indomethacin
include :
Joint diseases : rheumatoid arthritis ,oateoarthritis
,gouty arthritis ;Headaches etc
Adverse effect: peptic ulcer ,dypepsia,heartburn,mild
dirrhea ,edema9swelling due to fluid retention ) ,
hyperkalemia(highpotassiumlevel), hypernatremia(high
sodium level ) .
16. IUPAC Name :
2-(4-isobutyl
phenyl) propionic
acid
17. Properties :
Colour: colourless ,
appearance: crystalline powder
solubility: insoluble in water, soluble in most organic
solvents like alcohols, acetone,and dichloromethane.
M.P : 75-780C
chemical formula: C13H18O2
Assay: Dissolve the sample in methanol and titrate
against 0.1M NaOH USING Phenolphthalin indicator as
indicator ,until colour is obtained .
18.
19. Mechanism of action: it is a non –steroidal anti-inflmmatory
drug (NSAIDs) ,it is a selective COX-1 inhibitor
the enzyme that participate in prostaglandin synthesis
from archidonic acid
Prostaglandin are hormone like molecule normally found in
the body , where they have a wide variety of effects, some
of which leads to pain ,fever, and inflammation.
By inhibiting the synthesis of prostaglandins , ibuprofen
can reduce pain, fever, and inflammation
20. Medical uses:
Ibuprofen is used primarily to treat fever (including post-
vaccination fever),
mild to moderate pain (including pain relief after surgery),
painful menstruation, osteoarthritis, dental pain,
headaches, and pain from kidney stones.
About 60% of people respond to any NSAID; those who do
not respond well to a particular one may respond to
another.
It is used for inflammatory diseases such as juvenile
idiopathic arthritis and rheumatoid arthritis.
It is also used for pericarditis and patent ductus arteriosus.
21. Adverse effects :
include nausea, dyspepsia, diarrhea, constipation,
gastrointestinal ulceration/bleeding, headache, dizziness,
rash, salt and fluid retention, and high blood pressure.
Infrequent adverse effects include esophageal ulceration,
heart failure, high blood levels of potassium, kidney
impairment, confusion, and bronchospasm.Ibuprofen
can exacerbate asthma
22. IUPAC name :
2-(6-methoxy
2-naphthyl)
propionic acid
23. Properties :
Colour: white
appearance: crystalline powder
solubility insoluble in water, soluble in most organic
solvents like methanol,ethanol.
M.P : 155-162 0C
chemical formula: C19H21ClNNaO7
Assay: dissolve the sample in a mixture of water and
methanol(1:3)and titrate with 0.1M NAOH using
phenolphthalein as indicator.
24.
25. Mechanism of action: it is a non –steroidal anti-
inflmmatory drug (NSAIDs) ,it is a selective COX-1
inhibitor
the enzyme that participate in prostaglandin synthesis
from archidonic acid
Prostaglandin are hormone like molecule normally found
in the body , where they have a wide variety of effects,
some of which leads to pain ,fever, and inflammation.
By inhibiting the synthesis of prostaglandins , naproxen
can reduce pain, fever, and inflammation.
26. Medical uses :
Inflammatory sources of pain that may respond to
naproxen's anti-inflammatory activity are conditions
such as migraine,
osteoarthritis,
kidney stones,
rheumatoid arthritis,
psoriatic arthritis,
gout,
ankylosing spondylitis,
menstrual cramps, tendinitis, and bursitis.
27. adverse effects:
include
dizziness, drowsiness,
headache,
rash,
bruising,
gastrointestinal upset.
Heavy use is associated with increased risk of end-
stage renal disease and kidney failure.
29. Properties :
Colour: light yellow,
appearance: crystalline powder
solubility soluble in water, slightly soluble
solvents like methanol,ethanol.
M.P : 155-157 0C
chemical formula: C15H15NO3
30.
31. Mechanism of action:
Although the mechanism of action of tolmetin is
unknown, research involving humans and animals has
shown that tolmetin does not achieve anti-inflammatory
response by stimulation of the adrenal or pituitary gland,
but it has shown tolmetin restrains prostaglandin
synthetase in vitro and reduces plasma levels of
prostaglandin E, possibly causing the anti-inflammatory
response.
32. Medical uses: Is used alone or with other treatment to reduce
pain , swelling, and joint stiffness from rheumatoid arthritis and
osteoarthritis . It is used for juvenile rheumatoid arthrites
Adverse effect:
Tolmetin can increase the risk of heart or circulatory conditions
such as heart attacks and strokes. It should not be taken shortly
before or after coronary artery bypass surgery.
Tolmetin can also increase the risk of gastrointestinal conditions
such as perforation or bleeding, which is fatal. Antacids can be
taken with tolmetin to relieve stomachaches that often occur.
Overdose can result in drowsiness, nausea, epigastric pain, and
vomiting
33. Adverse effect:
Tolmetin can increase the risk of heart or circulatory
conditions such as heart attacks and strokes.
It should not be taken shortly before or after coronary
artery bypass surgery.
Tolmetin can also increase the risk of gastrointestinal
conditions such as perforation or bleeding, which is fatal.
Antacids can be taken with tolmetin to relieve
stomachaches that often occur.
Overdose can result in drowsiness, nausea, epigastric pain,
and vomiting.
36. Properties :
Colour: pale yellow
appearance: crystalline powder
solubility: soluble in water sparingly soluble in
alcohol
M.P : 157-159 0C
chemical formula: C17H14FNO2S
37. A para-sulfamoylphenyl at position 1 of the pyrazole was
found to have a higher potency for COX-2 selective inhibition.
At the 3-position of the pyrazole, a trifluoromethyl or
difluoromethyl provides superior selectivity and
potencyCelecoxib is compound 22;
the 4-sulfamoylphenyl on the 1-pyrazol substituent is
required for COX-2 inhibition and the 4-methyl on the 5-
pyrazol system has low steric hindrance to maximize potency,
while the 3-trifluoromethyl group provides superior
selectivity and potency.
To explain the selectivity of celecoxib, it is necessary to
analyze the free energy of binding difference between the
drug molecule and COX-1 compared to COX-2 enzymes
38.
39. Celecoxib is used for osteoarthritis, rheumatoid
arthritis, acute pain, musculoskeletal pain,
painful menstruation, ankylosing spondylitis, and to reduce
the number of colon and rectal polyps in people with familial
adenomatous polyposis.
It may also be used in children with juvenile rheumatoid
arthritis who are older than two years of age and weigh more
than 10 kg (22 lb).
Mental illness
Tentative evidence supports its use in treating a number of
psychiatric disonrders, including major depression, bipolar
disorder, and schizophrenia.
Familial adenomatous polyposis
40. Adverce effect:
Cardiovascular events: NSAIDs are associated with an increased
risk of serious (and potentially fatal) adverse cardiovascular
thrombotic events, including myocardial infarction and stroke
Gastrointestinal events: NSAIDs may increase risk of serious
gastrointestinal (GI) ulceration, bleeding, and perforation (may
be fatal). These events may occur at any time during therapy
and without warning.
Use cautionHematologic effects: Anemia may occur;
monitor hemoglobin or hematocrit in people on long-
term treatment. Celecoxib does not usually
affect prothrombin time, partial thromboplastin
time or platelet counts; it does not inhibit platelet
aggregation at approved doses.
with a history of GI disease (bleeding or ulcers).
42. Properties :
Colour: light yellow
appearance: crystalline powder
solubility: . Soluble in 1- octanol ,soluble in water
sparingly soluble in alcohol , acetone
M.P : 155-162 0C
chemical formula: C17H14O4S
43.
44. ROFICOXIB
Mechanism of action
Cyclooxygenase (COX) has two well-studied isoforms,
called COX-1 and COX-2. COX-1 mediates the
synthesis of prostaglandins responsible for protection
of the stomach lining, while COX-2 mediates the
synthesis of prostaglandins responsible for pain and
inflammation.
By creating "selective" NSAIDs that inhibit COX-2, but
not COX-1, the same pain relief as traditional NSAIDs
is offered, but with greatly reduced risk of fatal or
debilitating peptic ulcers. Rofecoxib is a selective
COX-2 inhibitor, or "coxib"
45. Medical uses :Rofecoxib is a nonsteroidal
anti-inflammatory drug that was used in the
treatment of osteoarthritis, acute pain
conditions, and dysmenorrhoea.
Adverce effect:Aside from the reduced
incidence of gastric ulceration, rofecoxib
exhibits a similar adverse effect profile to
other NSAIDs.