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Therapeutic enzymes
Enzymes
 Enzymes are proteins that serve as biological
catalysts.
 Most enzymatic reactions, under optimal
conditions, proceeds 108 to 1011 times more
rapidly than the corresponding non-enzymatic
reaction.
 Since most chemical reactions in the body
require the action of an enzyme, enzymes
often serve as the focal point for the regulation
of body function. 2
Streptokinase
 Extracellular bacterial protein produced by
Streptococcus haemolyticus group C.
 a widely employed thrombolytic agent.
 It is administered to treat a variety of
thrombo-embolic disorders, including:
 pulmonary embolism (blockage of the pulmonary
artery)
 deep-vein thrombosis ( usually in the legs)
 arterial occlusions
 acute myocardial infarction.
3
Streptokinase
 Induces its thrombolytic effect by binding
specifically and tightly to plasminogen.
 the streptokinase–plasminogen complex
catalyses the proteolytic conversion of
plasminogen to active plasmin.
 Limitations:
 Elicits immunity
 causes mild or severe allergy
 increased risk of haemorrhage
4
Streptokinase
 Streptokinase-activated plasminogen is
capable of lysing not only clot-associated
fibrin, but also free plasma fibrinogen.
Can result in low serum fibrinogen levels
and, hence, compromise haemostatic ability.
 It should not be administered to, for example,
patients suffering from coagulation disorders
or bleeding conditions such as ulcers
5
Urokinase
 Urokinase is an enzyme produced by the
kidney and is found in both the plasma and
urine.
 Capable of proteolytically converting
plasminogen into plasmin.
 Urokinase is used clinically under the same
circumstances as streptokinase.
 Because of its human origin, adverse 6
Asparaginase
 An enzyme that catalyzes hydrolysis of L-
asparagine to L-aspartate and ammonia
 It is usually obtained from E.coli or Erwinia
caratovora
 Used in chemotherapy of different forms of
leukimia in combination with other drugs.
 Lack of intracellular L-asparagine results in
decrease in protein synthesis and causes
apoptosis.
7
Recombinant human DNase
(Pulmozyme®)
 Used in the treatment of cystic fibrosis (CF)
since the end of 1993.
 CF is an inherited, life-threatening disorder
that damages the lungs and digestive tract.
It is caused by a defective gene that
triggers the production of thickened mucus
which clogs airways and blocks the
secretion of digestive enzymes.
8
Recombinant human DNase
(Pulmozyme®)
 There is no cure for CF but there are
treatments that can improve both the length
and quality of one's life.
 These include airway clearance
techniques, inhaled antibiotics, mucus
thinners, pancreatic enzymes, a high-
calorie diet, and newer generation
medications known as CFTR modulators.
9
Recombinant human DNase
(Pulmozyme®)
 Recombinant human DNase selectively
cleaves DNA which present at high
concentrations in the secretions of CF
patients following release from leukocytes
that accumulate in response to infection.
 Its reduces the viscoelasticity of the
secretion.
10
Digestive aids
 Aid digestion, particularly for conditions in
which deficiencies of natural digistive enzyme
exist.
 They contain some or all of the following
catagories of enzymes: amylolytic, proteolytic,
cellulytic, and lipolytic.
 In addition the preparations often include bile
salts.
 The acidic conditions of the stomach may
denature some of these enzymes.
11
Digestive aids
 The ingested enzymes would be exposed
to endogenous proteolytic activities
associated with the stomach and small
intestine.
 The preparations are formulated as tablets
coated with an acid-resistant polymer to
protect the enzyme as it passes through the
stomach.
12
Digestive aids
 Pancreatin
 pancreatic extract usually obtained from the
pancrease of slaughterhouse animals
(bovine and porcine).
 It contains a mixture of enzymes,
principally amylase, protease and lipase.
 formulated as enteric-coated granules or
capsules.
13
Digestive aids
 Individual enzymes papain, pepsin or
bromelains (proteases) or α-amylase are
sometimes used in place of pancreatin.
 Bromelain is a protease enzyme found in
the juice and stem of pineapple. It is similar
to Pepsin.
 Papain is protease enzyme derived from
the latex of papaya.
14
Digestive aids
 Cellulase
 Is not produced in the human digestive
system
 Its ingestion improve digestion of high-fibre
diets.
 enzyme preparations are obtained from
Aspergillus niger or other fungal sources.
15
Digestive aids
 α-galactosidase
absent in human digistive system
is used to reduce gassiness or bloating
following ingestion of grains, cereals,
nuts, seeds or vegetables containing
raffinose, verbascose, and stachyose.
16
Digestive aids
 β-galactosidase (Lactase)
 It is derived from yeast.
 catalyses the hydrolysis of lactose,
releasing the constituent monosaccharides.
 Add to or ingested with milk for patients
suffering from lactose intolerance (lactase
insufficiency).
17

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Therapeutic enzymes 2012.pptx

  • 2. Enzymes  Enzymes are proteins that serve as biological catalysts.  Most enzymatic reactions, under optimal conditions, proceeds 108 to 1011 times more rapidly than the corresponding non-enzymatic reaction.  Since most chemical reactions in the body require the action of an enzyme, enzymes often serve as the focal point for the regulation of body function. 2
  • 3. Streptokinase  Extracellular bacterial protein produced by Streptococcus haemolyticus group C.  a widely employed thrombolytic agent.  It is administered to treat a variety of thrombo-embolic disorders, including:  pulmonary embolism (blockage of the pulmonary artery)  deep-vein thrombosis ( usually in the legs)  arterial occlusions  acute myocardial infarction. 3
  • 4. Streptokinase  Induces its thrombolytic effect by binding specifically and tightly to plasminogen.  the streptokinase–plasminogen complex catalyses the proteolytic conversion of plasminogen to active plasmin.  Limitations:  Elicits immunity  causes mild or severe allergy  increased risk of haemorrhage 4
  • 5. Streptokinase  Streptokinase-activated plasminogen is capable of lysing not only clot-associated fibrin, but also free plasma fibrinogen. Can result in low serum fibrinogen levels and, hence, compromise haemostatic ability.  It should not be administered to, for example, patients suffering from coagulation disorders or bleeding conditions such as ulcers 5
  • 6. Urokinase  Urokinase is an enzyme produced by the kidney and is found in both the plasma and urine.  Capable of proteolytically converting plasminogen into plasmin.  Urokinase is used clinically under the same circumstances as streptokinase.  Because of its human origin, adverse 6
  • 7. Asparaginase  An enzyme that catalyzes hydrolysis of L- asparagine to L-aspartate and ammonia  It is usually obtained from E.coli or Erwinia caratovora  Used in chemotherapy of different forms of leukimia in combination with other drugs.  Lack of intracellular L-asparagine results in decrease in protein synthesis and causes apoptosis. 7
  • 8. Recombinant human DNase (Pulmozyme®)  Used in the treatment of cystic fibrosis (CF) since the end of 1993.  CF is an inherited, life-threatening disorder that damages the lungs and digestive tract. It is caused by a defective gene that triggers the production of thickened mucus which clogs airways and blocks the secretion of digestive enzymes. 8
  • 9. Recombinant human DNase (Pulmozyme®)  There is no cure for CF but there are treatments that can improve both the length and quality of one's life.  These include airway clearance techniques, inhaled antibiotics, mucus thinners, pancreatic enzymes, a high- calorie diet, and newer generation medications known as CFTR modulators. 9
  • 10. Recombinant human DNase (Pulmozyme®)  Recombinant human DNase selectively cleaves DNA which present at high concentrations in the secretions of CF patients following release from leukocytes that accumulate in response to infection.  Its reduces the viscoelasticity of the secretion. 10
  • 11. Digestive aids  Aid digestion, particularly for conditions in which deficiencies of natural digistive enzyme exist.  They contain some or all of the following catagories of enzymes: amylolytic, proteolytic, cellulytic, and lipolytic.  In addition the preparations often include bile salts.  The acidic conditions of the stomach may denature some of these enzymes. 11
  • 12. Digestive aids  The ingested enzymes would be exposed to endogenous proteolytic activities associated with the stomach and small intestine.  The preparations are formulated as tablets coated with an acid-resistant polymer to protect the enzyme as it passes through the stomach. 12
  • 13. Digestive aids  Pancreatin  pancreatic extract usually obtained from the pancrease of slaughterhouse animals (bovine and porcine).  It contains a mixture of enzymes, principally amylase, protease and lipase.  formulated as enteric-coated granules or capsules. 13
  • 14. Digestive aids  Individual enzymes papain, pepsin or bromelains (proteases) or α-amylase are sometimes used in place of pancreatin.  Bromelain is a protease enzyme found in the juice and stem of pineapple. It is similar to Pepsin.  Papain is protease enzyme derived from the latex of papaya. 14
  • 15. Digestive aids  Cellulase  Is not produced in the human digestive system  Its ingestion improve digestion of high-fibre diets.  enzyme preparations are obtained from Aspergillus niger or other fungal sources. 15
  • 16. Digestive aids  α-galactosidase absent in human digistive system is used to reduce gassiness or bloating following ingestion of grains, cereals, nuts, seeds or vegetables containing raffinose, verbascose, and stachyose. 16
  • 17. Digestive aids  β-galactosidase (Lactase)  It is derived from yeast.  catalyses the hydrolysis of lactose, releasing the constituent monosaccharides.  Add to or ingested with milk for patients suffering from lactose intolerance (lactase insufficiency). 17