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Introduction to
Pharmacology
Dr. Karun Kumar
JR – II
Dept. of Pharmacology
Definition
• Pharmacology  Study of drugs & their effects on
life processes
• Pharmakon
Earlier  Magic charm for treating disease
Later  Remedy or drug
History of pharmacology
• 1st phase  Noxious plant & animal prep. Were
admin. To diseased patient to rid the body of evil
spirits believed to cause illness
• 2nd phase  Experience enabled people to
understand which subst. were beneficial in relieving
particular disease symptoms
• 3rd phase  Rational or scientific phase (Advances
in chemistry & physiology; understanding of
disease mechanisms)
• 1st effective drugs Simple external prep. (cool
mud or soothing leaf)
• 1500 BC  Egyptian presc. (castor oil, opium)
• China  Ancient scrolls (herbal medicines)
• Dioscorides (Greek army surgeon)  > 600
medicinal plants that he collected in his trip
• Susruta (Hindu physician)  Ayurvedic medicine
• Isolation of pure drug compounds from natural
sources
1. Isolation of morphine from opium  1804
2. Magendie & Bernard  Curare eff. On NMJ
• 1st med school Pharma lab  Rudolf Buchheim in
Estonia
• Buchheim & 1 of his students (Oswald
Schmiedeberg) trained many others including John
Jacob Abel
• Sir Colonel Ram Nath Chopra  1st to establish a
center of study and research in pharmacology in
India, at the Calcutta School of Tropical Medicine
• 1st pharmacology dept.  Estd. At University of
Michigan (1891) by John Jacob Abel
20th century developments
• Isolation & use of insulin for DM
• Discovery of antimicrobials
• Discovery of antineoplastic drugs
• Advent of modern psychopharmacology
• Pharmacology & its subdivisions  Pk, pd
• Toxicology  Study of poisons and organ toxicity
• Pharmacotherapeutics  Use of drugs in the
treatment of disease
• Pharmacy  Science and profession concerned
with the preparation, storage, dispensing, and
proper use of drug products
• Pharmacognosy  study of drugs isolated from
natural sources including plants, microbes, animal
tissues, and minerals.
• Medicinal chemistry  Specializes in the design
and chemical synthesis of drugs
• Pharmaceutical chemistry or pharmaceutics 
Formulation and chemical properties of
pharmaceutical products, such as tablets, liquid
solutions and suspensions, and aerosols
Natural sources of drugs
• Alkaloids  Substances that that contain nitrogen
groups and produce an alkaline reaction in aqueous
solution
• Structure-activity relationship  Relationship
among the drug molecule,its target receptor, and
the resulting pharmacologic activity Eg inhibit
angiotensin synthesis, treat hypertension, and anti
(HIV).
Drug preparations
• Crude drug preparations  Obtained from natural
sources
• Pure drug compounds  From natural sources or
synthesized in the laboratory
• Pharmaceutical preparations  Intended for
administration to patients
Crude drug preparations
1. Drying or pulverizing a plant or animal tissue
2. Extracting substances from a natural product with
the aid of hot water or a solvent such as alcohol.
Eg. coffee and tea, made from distillates of the
beans and leaves of Coffea arabica and Camellia
sinensis plants, and opium, which is the dried
juice of the unripe poppy capsule of the plant
Papaver somniferum.
Pure drug compounds
• Frederick Sertürner isolated the fist pure drug from
a natural source when he extracted a potent
analgesic agent from opium in 1804 and named it
morphine, from Morpheus, the Greek god of
dreams
• Frederick Banting and John Macleodi  Isolation of
insulin from the pancreas
Drug sources & preparations
Dosage forms
• Drug products suitable for administration of a
specific dose of a drug to a patient by a particular
route of administration
• Solid dosage forms  Tablets, Capsules, SR/ER
• Liquid dosage forms  Solutions, suspensions,
syrups, elixirs
Tablets & Capsules
• Most common preparations for oral administration
• In the manufacture of tablets, a machine with a punch
and die mechanism compresses a mixture of powdered
drug and inert ingredients into a hard pill
• Inert ingredients include
1. Fillers  Specific components that provide bulk
2. Lubricants  prevent sticking to the punch and die
during manufacture
3. Adhesives  Maintain tablet stability in the bottle
4. Disintegrants  Facilitate solubilization of the tablet
when it reaches gastrointestinal fluids
Enteric coated tablets
• Consist of polymers that will not disintegrate in
gastric acid but will break down in the more basic
pH of the intestines
• Used to protect drugs that would be destroyed by
gastric acid and to slow the release and absorption
of a drug when a large dose is given at one time, for
example, in the formulation of the antidepressant
floxetine, called PROZAC WEEKLY
SR/ER preparations
• Release the drug from the preparation over many hours.
• 2 methods to extend the release of a drug
1. Controlled diffusion  Release of the drug from the
pharmaceutical product is regulated by a rate-controlling
membrane
2. Controlled dissolution  Done by inert polymers that
gradually break down in body fluids
• Some products use osmotic pressure to provide a sustained
release of a drug. These products contain an osmotic agent
that attracts gastrointestinal fluid at a constant rate. The
attracted fluid then forces the drug out of the tablet
through a small laser-drilled hole
Capsules
• Hard capsules  Enclose powdered drugs
• Soft capsules  Enclose a drug in solution
• The gelatin shell quickly dissolves in gastrointestinal
fluids to release the drug for absorption into the
circulation
Solutions and suspensions
• Syrups  Sweetened aqueous solutions
• Elixirs  sweetened aqueous-alcoholic solutions
are known as elixirs. Alcohol is included in elixirs as
a solvent for drugs that are not suffciently soluble
in water alone.
• Sterile solutions and suspensions  Parenteral
administration
• Sterile ophthalmic solutions and suspensions 
Eyedropper into the conjunctival sac
Skin patches
• Drug preparations in which the drug is slowly
released from the patch for absorption through the
skin into the circulation
• Most suitable for potent drugs, which are therefore
effective at relatively low doses, that have sufficient
lipid solubility to enable skin penetration
Aerosols
• Aerosol  Administered by inhalation through the
nose or mouth
• Ointment & creams  semisolid preparations
intended for topical application . They contain an
active drug that is incorporated into a vehicle (e.g.,
polyethylene glycol or petrolatum) which enables
the drug to adhere to the tissue for a sufficient
length of time to exert its effect
• Lotions  Liquid preparations often formulated as
oil-in-water emulsions and are used to treat
dermatologic conditions.
• Suppositories  Products in which the drug is
incorporated into a solid base that melts or
dissolves at body temperature. Used for rectal,
vaginal, or urethral administration
Routes of drug administration
1. Enteral (Drug abs. through GIT)
• Sulblingual  under tongue ; no fpm (lipid soluble);
NG, hyoscyamine
• Buccal  b/w cheek and gum; no fpm (lipid
soluble); lollypop of Fentanyl (breakthrough cancer
pain)
• Oral  PO (per os  by mouth)
• Rectal (N/V; little fpm)  Local - Haemorrhoids
Oral route
2. Parenteral
• I.v.
• I.m. and S.c.  Drug solns. & particle suspensions
• Intrathecal  subarachnoid space (meningitis)
• Epidural  Labor & delivery (above the dura)
• Intraart.  arthritis ; intrad.  all.; insufflation
(intranasal admin.)  sinus medications
• Transdermal  NG ointment for HF & angina;
Fentanyl transdermal for chr. Pain (skin patch/oint)
• Inhalational  Local (Anti-asthma / rhinitis)
systemic (GA  Sevoflurane)
• Topical  Surface of body (Skin, eyes, nose, mouth,
throat, rectum, vagina)
Drug names
1. Chemical  acetylsalicylic acid (chemists)
2. Nonproprietary (generic)  USAN (US adopted
name) class to which drug belongs oxacillin is a
type of Pn; INN (Intl. nonpropr. Name); BAN
(British approved name)
3. Proprietary (brand)  Flomax for Tamsulosin;
Diuril for chlorothiazide; Maxair  Pirbuterol

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Introduction to pharmacology

  • 1. Introduction to Pharmacology Dr. Karun Kumar JR – II Dept. of Pharmacology
  • 2. Definition • Pharmacology  Study of drugs & their effects on life processes • Pharmakon Earlier  Magic charm for treating disease Later  Remedy or drug
  • 3. History of pharmacology • 1st phase  Noxious plant & animal prep. Were admin. To diseased patient to rid the body of evil spirits believed to cause illness • 2nd phase  Experience enabled people to understand which subst. were beneficial in relieving particular disease symptoms • 3rd phase  Rational or scientific phase (Advances in chemistry & physiology; understanding of disease mechanisms)
  • 4. • 1st effective drugs Simple external prep. (cool mud or soothing leaf) • 1500 BC  Egyptian presc. (castor oil, opium) • China  Ancient scrolls (herbal medicines) • Dioscorides (Greek army surgeon)  > 600 medicinal plants that he collected in his trip • Susruta (Hindu physician)  Ayurvedic medicine • Isolation of pure drug compounds from natural sources 1. Isolation of morphine from opium  1804 2. Magendie & Bernard  Curare eff. On NMJ
  • 5. • 1st med school Pharma lab  Rudolf Buchheim in Estonia • Buchheim & 1 of his students (Oswald Schmiedeberg) trained many others including John Jacob Abel • Sir Colonel Ram Nath Chopra  1st to establish a center of study and research in pharmacology in India, at the Calcutta School of Tropical Medicine • 1st pharmacology dept.  Estd. At University of Michigan (1891) by John Jacob Abel
  • 6. 20th century developments • Isolation & use of insulin for DM • Discovery of antimicrobials • Discovery of antineoplastic drugs • Advent of modern psychopharmacology
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  • 8. • Pharmacology & its subdivisions  Pk, pd • Toxicology  Study of poisons and organ toxicity • Pharmacotherapeutics  Use of drugs in the treatment of disease • Pharmacy  Science and profession concerned with the preparation, storage, dispensing, and proper use of drug products
  • 9. • Pharmacognosy  study of drugs isolated from natural sources including plants, microbes, animal tissues, and minerals. • Medicinal chemistry  Specializes in the design and chemical synthesis of drugs • Pharmaceutical chemistry or pharmaceutics  Formulation and chemical properties of pharmaceutical products, such as tablets, liquid solutions and suspensions, and aerosols
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  • 11. Natural sources of drugs • Alkaloids  Substances that that contain nitrogen groups and produce an alkaline reaction in aqueous solution • Structure-activity relationship  Relationship among the drug molecule,its target receptor, and the resulting pharmacologic activity Eg inhibit angiotensin synthesis, treat hypertension, and anti (HIV).
  • 12. Drug preparations • Crude drug preparations  Obtained from natural sources • Pure drug compounds  From natural sources or synthesized in the laboratory • Pharmaceutical preparations  Intended for administration to patients
  • 13. Crude drug preparations 1. Drying or pulverizing a plant or animal tissue 2. Extracting substances from a natural product with the aid of hot water or a solvent such as alcohol. Eg. coffee and tea, made from distillates of the beans and leaves of Coffea arabica and Camellia sinensis plants, and opium, which is the dried juice of the unripe poppy capsule of the plant Papaver somniferum.
  • 14. Pure drug compounds • Frederick Sertürner isolated the fist pure drug from a natural source when he extracted a potent analgesic agent from opium in 1804 and named it morphine, from Morpheus, the Greek god of dreams • Frederick Banting and John Macleodi  Isolation of insulin from the pancreas
  • 15. Drug sources & preparations
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  • 17. Dosage forms • Drug products suitable for administration of a specific dose of a drug to a patient by a particular route of administration • Solid dosage forms  Tablets, Capsules, SR/ER • Liquid dosage forms  Solutions, suspensions, syrups, elixirs
  • 18. Tablets & Capsules • Most common preparations for oral administration • In the manufacture of tablets, a machine with a punch and die mechanism compresses a mixture of powdered drug and inert ingredients into a hard pill • Inert ingredients include 1. Fillers  Specific components that provide bulk 2. Lubricants  prevent sticking to the punch and die during manufacture 3. Adhesives  Maintain tablet stability in the bottle 4. Disintegrants  Facilitate solubilization of the tablet when it reaches gastrointestinal fluids
  • 19. Enteric coated tablets • Consist of polymers that will not disintegrate in gastric acid but will break down in the more basic pH of the intestines • Used to protect drugs that would be destroyed by gastric acid and to slow the release and absorption of a drug when a large dose is given at one time, for example, in the formulation of the antidepressant floxetine, called PROZAC WEEKLY
  • 20. SR/ER preparations • Release the drug from the preparation over many hours. • 2 methods to extend the release of a drug 1. Controlled diffusion  Release of the drug from the pharmaceutical product is regulated by a rate-controlling membrane 2. Controlled dissolution  Done by inert polymers that gradually break down in body fluids • Some products use osmotic pressure to provide a sustained release of a drug. These products contain an osmotic agent that attracts gastrointestinal fluid at a constant rate. The attracted fluid then forces the drug out of the tablet through a small laser-drilled hole
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  • 22. Capsules • Hard capsules  Enclose powdered drugs • Soft capsules  Enclose a drug in solution • The gelatin shell quickly dissolves in gastrointestinal fluids to release the drug for absorption into the circulation
  • 23. Solutions and suspensions • Syrups  Sweetened aqueous solutions • Elixirs  sweetened aqueous-alcoholic solutions are known as elixirs. Alcohol is included in elixirs as a solvent for drugs that are not suffciently soluble in water alone. • Sterile solutions and suspensions  Parenteral administration • Sterile ophthalmic solutions and suspensions  Eyedropper into the conjunctival sac
  • 24. Skin patches • Drug preparations in which the drug is slowly released from the patch for absorption through the skin into the circulation • Most suitable for potent drugs, which are therefore effective at relatively low doses, that have sufficient lipid solubility to enable skin penetration
  • 25. Aerosols • Aerosol  Administered by inhalation through the nose or mouth • Ointment & creams  semisolid preparations intended for topical application . They contain an active drug that is incorporated into a vehicle (e.g., polyethylene glycol or petrolatum) which enables the drug to adhere to the tissue for a sufficient length of time to exert its effect
  • 26. • Lotions  Liquid preparations often formulated as oil-in-water emulsions and are used to treat dermatologic conditions. • Suppositories  Products in which the drug is incorporated into a solid base that melts or dissolves at body temperature. Used for rectal, vaginal, or urethral administration
  • 27. Routes of drug administration 1. Enteral (Drug abs. through GIT) • Sulblingual  under tongue ; no fpm (lipid soluble); NG, hyoscyamine • Buccal  b/w cheek and gum; no fpm (lipid soluble); lollypop of Fentanyl (breakthrough cancer pain) • Oral  PO (per os  by mouth) • Rectal (N/V; little fpm)  Local - Haemorrhoids
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  • 35. 2. Parenteral • I.v. • I.m. and S.c.  Drug solns. & particle suspensions • Intrathecal  subarachnoid space (meningitis) • Epidural  Labor & delivery (above the dura) • Intraart.  arthritis ; intrad.  all.; insufflation (intranasal admin.)  sinus medications • Transdermal  NG ointment for HF & angina; Fentanyl transdermal for chr. Pain (skin patch/oint) • Inhalational  Local (Anti-asthma / rhinitis) systemic (GA  Sevoflurane) • Topical  Surface of body (Skin, eyes, nose, mouth, throat, rectum, vagina)
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  • 41. Drug names 1. Chemical  acetylsalicylic acid (chemists) 2. Nonproprietary (generic)  USAN (US adopted name) class to which drug belongs oxacillin is a type of Pn; INN (Intl. nonpropr. Name); BAN (British approved name) 3. Proprietary (brand)  Flomax for Tamsulosin; Diuril for chlorothiazide; Maxair  Pirbuterol