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PHARMACOLOGY I
LECTURE 2
MUTUA W. MUTHEU
SOURCES OF DRUGS
1)Plant Sources
A number of plants have medicinal qualities and have been used for centuries as
drugs or drug sources.
Plant part Drugs
Leaves
Digoxin, digitoxin (from Digitalis purpurea/foxglove
plant); atropine (from Atropa belladonna)
Flowers Vincristine, vinblastine (from Vinca rosea)
Fruits
Physostigmine (from Physostigma venenosum/calabar
bean)
Seeds
Strychnine (from Nux vomica); physostigmine (from
Physostigma venenosum/calabar bean)
Roots
Emetine (from Cephaelis ipecacuanha); reserpine
(from Rauwolfa serpentina)
Bark
Quinine (from Cinchona); atropine (from Atropa
belladonna)
Stem Tubocurarine (from Chondrodendron tomentosum)
2)Animal Sources
 Many important drugs are derived from animal source.
 In most instances, these medicinal substances are derived from the animal’s body
secretions, fluid or glands.
 Examples; Insulin, heparin, adrenaline, thyroxin, cod liver oil, musk, beeswax,
enzymes, and antitoxins sera are some examples of drugs obtained from animal
sources.
 Like plant products, drugs from animal sources may be crude (unrefined) or refined
material.
3)Microbial sources
 Several life-saving drugs have been historically derived from
microorganisms.
 Examples include;
penicillin produced by Penicillium chrysogenum
streptomycin from Streptomyces griseus
chloramphenicol from Streptomyces venezuelae
neomycin from Streptomyces fradiae
bacitracin from Bacillus subtilis etc.
Xanthan (polysaccharide gum secreted by Xanthomonas campestris)
dextran (polysaccharide of glucose synthesized by lactic acid bacteria
Leuconostoc mesenteroides,Streptococcus mutans, Lactobacillus brevis)
curdian (β-1,3-glucan polymer, product of Agrobacterium biobar and
Alcaligenes faecalis)
Pullulan (a polysaccharide polymer of maltotriose units produced from starch by
the fungus Aureobasidium pullulans) etc.
4)Marine source
 Bioactive compounds from marine flora and fauna have extensive past and present use
in the prevention, treatment or cure of many diseases.
 Coral, sponges, fish, and marine microorganisms produce biologically potent
chemicals with interesting anti-inflammatory, anti-viral, and anticancer activity.
 For example; curacin A from marine cyanobacterium
 Lyngbya majuscule,eleutherobin from coral Eleutherobia sp. discodermolide from
marine sponge Discodermia dissoluta, etc. show potent anti-tumour activity.
5)Mineral sources
 Minerals (both metallic and non-metallic minerals) have been used as drugs
since ancient times.
 Our body requires trace elements of minerals in order to maintain
homeostasis. Patients lacking an adequate level of these materials may take
specific mineral-based drugs to raise the level of minerals
Examples include;
 ferrous sulfate in iron deficiency anemia;
 magnesium sulfate as purgative; magnesium trisilicate, aluminum hydroxide and
sodium bicarbonate as antacids for hyperacidity and peptic ulcer
 zinc oxide ointment as skin protectant, in wounds and eczema
 gold salts (solganal, auranofin) as anti-inflammatory and in rheumatoid arthritis;
selenium as anti-dandruff.
6)Synthetic/chemical derivative
 A synthetic drug is produced using chemical synthesis, which rearranges chemical
derivatives to form a new compound.
 The synthetic sources of drugs evolved with human skills in the laboratory and
advanced knowledge and understanding of phytochemical investigation
 Synthetically manufactured drugs generally have higher yields that are significantly
associated with quality, purity and low cost.
 The of the earliest synthetic drugs was sulphonamide, which began with the
synthesis of prontosil dye.
 Other examples include;
 acetylsalicylic acid (aspirin or ASA)
 oral antidiabetics, antihistamines
thiazide diuretics
 chloroquine
Chlorpromazine
general
local anaesthetics
Paracetamol
phenytoin
7)Semi-synthetic Sources
 Semi-synthetic drugs are neither completely natural nor completely synthetic.
 They are a hybrid and are generally made by chemically modifying substances that are
available from natural source to improve its potency, efficacy and/or reduce side
effects.
 Sometimes, semi-synthetic processes are used to prepare drugs when the natural sources
may yield impure compounds or when the synthesis of drugs (complex molecules) may
be difficult, expensive, and commercially unviable.
 Examples include recombinant Hepatitis B vaccine, recombinant insulin and others.
Examples of semi-synthetic medicine include;
 heroin from morphine
 bromoscopolamine from scopolamine
 homatropine from atropine
 ampicillin from penicillin
8. Biosynthetic sources (genetically engineered drugs)
 This is relatively a new field which is being developed by mixing discoveries from
molecular biology, recombinant DNA technology, DNA alteration, gene splicing,
immunology, and immune pharmacology.
 Drugs developed using living organisms with the help of biotechnology or genetic
engineering are known as biologics, biopharmaceuticals, recombinant DNA expressed
products, bioengineered, or genetically engineered drugs
Summary
The end

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PHARMACOLGY I-Lecturer 2a notes h-1.pptx

  • 2. SOURCES OF DRUGS 1)Plant Sources A number of plants have medicinal qualities and have been used for centuries as drugs or drug sources.
  • 3. Plant part Drugs Leaves Digoxin, digitoxin (from Digitalis purpurea/foxglove plant); atropine (from Atropa belladonna) Flowers Vincristine, vinblastine (from Vinca rosea) Fruits Physostigmine (from Physostigma venenosum/calabar bean) Seeds Strychnine (from Nux vomica); physostigmine (from Physostigma venenosum/calabar bean) Roots Emetine (from Cephaelis ipecacuanha); reserpine (from Rauwolfa serpentina) Bark Quinine (from Cinchona); atropine (from Atropa belladonna) Stem Tubocurarine (from Chondrodendron tomentosum)
  • 4. 2)Animal Sources  Many important drugs are derived from animal source.  In most instances, these medicinal substances are derived from the animal’s body secretions, fluid or glands.  Examples; Insulin, heparin, adrenaline, thyroxin, cod liver oil, musk, beeswax, enzymes, and antitoxins sera are some examples of drugs obtained from animal sources.  Like plant products, drugs from animal sources may be crude (unrefined) or refined material.
  • 5. 3)Microbial sources  Several life-saving drugs have been historically derived from microorganisms.  Examples include; penicillin produced by Penicillium chrysogenum streptomycin from Streptomyces griseus chloramphenicol from Streptomyces venezuelae neomycin from Streptomyces fradiae bacitracin from Bacillus subtilis etc.
  • 6. Xanthan (polysaccharide gum secreted by Xanthomonas campestris) dextran (polysaccharide of glucose synthesized by lactic acid bacteria Leuconostoc mesenteroides,Streptococcus mutans, Lactobacillus brevis) curdian (β-1,3-glucan polymer, product of Agrobacterium biobar and Alcaligenes faecalis) Pullulan (a polysaccharide polymer of maltotriose units produced from starch by the fungus Aureobasidium pullulans) etc.
  • 7. 4)Marine source  Bioactive compounds from marine flora and fauna have extensive past and present use in the prevention, treatment or cure of many diseases.  Coral, sponges, fish, and marine microorganisms produce biologically potent chemicals with interesting anti-inflammatory, anti-viral, and anticancer activity.  For example; curacin A from marine cyanobacterium  Lyngbya majuscule,eleutherobin from coral Eleutherobia sp. discodermolide from marine sponge Discodermia dissoluta, etc. show potent anti-tumour activity.
  • 8. 5)Mineral sources  Minerals (both metallic and non-metallic minerals) have been used as drugs since ancient times.  Our body requires trace elements of minerals in order to maintain homeostasis. Patients lacking an adequate level of these materials may take specific mineral-based drugs to raise the level of minerals
  • 9. Examples include;  ferrous sulfate in iron deficiency anemia;  magnesium sulfate as purgative; magnesium trisilicate, aluminum hydroxide and sodium bicarbonate as antacids for hyperacidity and peptic ulcer  zinc oxide ointment as skin protectant, in wounds and eczema  gold salts (solganal, auranofin) as anti-inflammatory and in rheumatoid arthritis; selenium as anti-dandruff.
  • 10. 6)Synthetic/chemical derivative  A synthetic drug is produced using chemical synthesis, which rearranges chemical derivatives to form a new compound.  The synthetic sources of drugs evolved with human skills in the laboratory and advanced knowledge and understanding of phytochemical investigation  Synthetically manufactured drugs generally have higher yields that are significantly associated with quality, purity and low cost.
  • 11.  The of the earliest synthetic drugs was sulphonamide, which began with the synthesis of prontosil dye.  Other examples include;  acetylsalicylic acid (aspirin or ASA)  oral antidiabetics, antihistamines thiazide diuretics  chloroquine Chlorpromazine general local anaesthetics Paracetamol phenytoin
  • 12. 7)Semi-synthetic Sources  Semi-synthetic drugs are neither completely natural nor completely synthetic.  They are a hybrid and are generally made by chemically modifying substances that are available from natural source to improve its potency, efficacy and/or reduce side effects.  Sometimes, semi-synthetic processes are used to prepare drugs when the natural sources may yield impure compounds or when the synthesis of drugs (complex molecules) may be difficult, expensive, and commercially unviable.  Examples include recombinant Hepatitis B vaccine, recombinant insulin and others.
  • 13. Examples of semi-synthetic medicine include;  heroin from morphine  bromoscopolamine from scopolamine  homatropine from atropine  ampicillin from penicillin
  • 14. 8. Biosynthetic sources (genetically engineered drugs)  This is relatively a new field which is being developed by mixing discoveries from molecular biology, recombinant DNA technology, DNA alteration, gene splicing, immunology, and immune pharmacology.  Drugs developed using living organisms with the help of biotechnology or genetic engineering are known as biologics, biopharmaceuticals, recombinant DNA expressed products, bioengineered, or genetically engineered drugs