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By the end of this lecture, the student should be able to
 Discuss the different routes of drug administration
 Identify the advantages and disadvantages of various routes
of drug administration
 Know the various mechanisms of drug absorption
 List different factors affecting drug absorption
 Define bioavailability
Pharmacokinetics
Pharmacokinetics of drugs
(ADME)
Are studies of
 Absorption
 Distribution
 Metabolism
 Excretion of drugs
Administration
Blood
Absorption
Distribution
Metabolism
Excretion
Different organs &
tissues
Drug
Site of action
Sites of
Administration
Absorption & distribution Elimination
 Enteral via gastrointestinal tract (GIT).
 Oral
 Sublingual
 Rectal
 Parenteral administration = injections.
 Topical application
 Inhalation
Disadvantages
Advantages
- Slow effect
-No complete absorption
- Destruction by pH and enzymes
- GIT irritation
- Food - Drug interactions
-Drug-Drug interactions
- First pass effect
- (low bioavailability).
Not suitable for
 vomiting & unconscious patient
 emergency
 bad taste drugs
- Easy
- Self use
- Safe
- Convenient
- cheap
- No need for
sterilization
First pass Metabolism
 Drugs taken orally are first taken to liver (via
portal circulation) where they are metabolized
before reaching to rest of body.
 so the amount reaching system circulation is
less than the amount absorbed
Results ?
Low bioavailability = low serum level of active
drug that can produce action
04 GENERAL PHARMACOLOGY (absorption).ppt
First pass effect
Oral Dosage Forms (oral formulations)
 Tablets (enteric coated tablets)
 Capsules (hard and soft gelatin capsules)
 Syrup
 Suspension
 Emulsion
Tablets
Hard- gelatin
capsule
Spansule
Soft- gelatin
capsule
Suspension
Emulsion
Disadvantages
Advantages
Not for
- irritant drugs
- Frequent use
 Rapid effect
 can be used in emergency
 High bioavailability
 No first pass effect.
 No GIT irritation
 No food drug - interaction
Dosage form: friable tablet
Disadvantages
Advantages
 Irregular
absorption &
bioavailability.
 Irritation of
rectal mucosa.
Suitable for
 children
 Vomiting or unconscious
patients
 Irritant & Bad taste drugs.
 less first pass metabolism
(50%)
Dosage form:
suppository or enema
Intradermal (I.D.) (into skin)
Subcutaneous (S.C.) (under skin)
Intramuscular (I.M.) (into muscles)
Intravenous (I.V.) (into veins)
Intra-arterial (I.A.) (into arteries)
Intrathecal (I.T.) (cerebrospinal fluids )
Intraperitoneal (I.P.) (peritoneal cavity)
Intra - articular (Synovial fluids)
Disadvantages
Advantages
 Only for water
soluble drugs
 Infection
 Sterilization.
 Pain
 Needs skill
 Anaphylaxis
 Expensive
Not suitable for oily
solutions or poorly
soluble substance
 Rapid action (emergency)
 High bioavailability
 No food-drug interaction
 No first pass metabolism
 No gastric irritation
Suitable for
 Vomiting &unconscious
 Irritant & Bad taste drugs.
Dosage form:
Vial or ampoule
Ampoule Vial
Single use Repeated use
Injection Special Utility Limitations
I.D. minute volume (0.1 ml)
suitable for vaccinations
& sensitivity test
not suitable for large volumes
S.C. 0.1 ml  1 ml
suitable for poorly soluble
suspensions and for
instillation of slow-release
implants e.g. insulin zinc
preparation
not suitable for large volumes
I.M. larger volume 3-5 ml Suitable
for moderate volumes, for oily
solutions or poorly soluble
substances
not suitable for irritant drugs
Abscess- necrosis may happen
I.V. suitable for large volumes and
for irritating substances
not suitable for oily solutions
or poorly soluble substances
Must inject solutions slowly as
a rule
 Drugs are applied to skin, ear, eye, nose, vagina,
respiratory tract
 Usually used to provide local action.
 No first pass metabolism.
 Used for lipid soluble drugs
Disadvantages
Advantages
Not suitable for
irritant drugs
Only for some
drugs as
inhalation
anesthetics &
bronchodilators
 mucous membrane of respiratory
system
 rapid absorption (large surface
area)
 provide local action in
 limited systemic effect
 less side effects.
 no first pass effect
Dosage form: aerosol, nebulizer
Nebulizer Atomizer
Is the passage of drug from its site of
administration to its site of action through
cell membranes.
Sites of
Administration
Sites of
action
Cell membrane
04 GENERAL PHARMACOLOGY (absorption).ppt
 Is the fraction of unchanged drug that enters
systemic circulation after administration and
becomes available to produce an action
 I.V. provides 100% bioavailability.
 Oral usually has less than I.V.

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04 GENERAL PHARMACOLOGY (absorption).ppt

  • 1. By the end of this lecture, the student should be able to Discuss the different routes of drug administration Identify the advantages and disadvantages of various routes of drug administration Know the various mechanisms of drug absorption List different factors affecting drug absorption Define bioavailability Pharmacokinetics
  • 2. Pharmacokinetics of drugs (ADME) Are studies of Absorption Distribution Metabolism Excretion of drugs
  • 4. Sites of Administration Absorption & distribution Elimination
  • 5. Enteral via gastrointestinal tract (GIT). Oral Sublingual Rectal Parenteral administration = injections. Topical application Inhalation
  • 6. Disadvantages Advantages - Slow effect -No complete absorption - Destruction by pH and enzymes - GIT irritation - Food - Drug interactions -Drug-Drug interactions - First pass effect - (low bioavailability). Not suitable for vomiting & unconscious patient emergency bad taste drugs - Easy - Self use - Safe - Convenient - cheap - No need for sterilization
  • 7. First pass Metabolism Drugs taken orally are first taken to liver (via portal circulation) where they are metabolized before reaching to rest of body. so the amount reaching system circulation is less than the amount absorbed Results ? Low bioavailability = low serum level of active drug that can produce action
  • 10. Oral Dosage Forms (oral formulations) Tablets (enteric coated tablets) Capsules (hard and soft gelatin capsules) Syrup Suspension Emulsion
  • 12. Disadvantages Advantages Not for - irritant drugs - Frequent use Rapid effect can be used in emergency High bioavailability No first pass effect. No GIT irritation No food drug - interaction Dosage form: friable tablet
  • 13. Disadvantages Advantages Irregular absorption & bioavailability. Irritation of rectal mucosa. Suitable for children Vomiting or unconscious patients Irritant & Bad taste drugs. less first pass metabolism (50%) Dosage form: suppository or enema
  • 14. Intradermal (I.D.) (into skin) Subcutaneous (S.C.) (under skin) Intramuscular (I.M.) (into muscles) Intravenous (I.V.) (into veins) Intra-arterial (I.A.) (into arteries) Intrathecal (I.T.) (cerebrospinal fluids ) Intraperitoneal (I.P.) (peritoneal cavity) Intra - articular (Synovial fluids)
  • 15. Disadvantages Advantages Only for water soluble drugs Infection Sterilization. Pain Needs skill Anaphylaxis Expensive Not suitable for oily solutions or poorly soluble substance Rapid action (emergency) High bioavailability No food-drug interaction No first pass metabolism No gastric irritation Suitable for Vomiting &unconscious Irritant & Bad taste drugs. Dosage form: Vial or ampoule
  • 16. Ampoule Vial Single use Repeated use
  • 17. Injection Special Utility Limitations I.D. minute volume (0.1 ml) suitable for vaccinations & sensitivity test not suitable for large volumes S.C. 0.1 ml 1 ml suitable for poorly soluble suspensions and for instillation of slow-release implants e.g. insulin zinc preparation not suitable for large volumes I.M. larger volume 3-5 ml Suitable for moderate volumes, for oily solutions or poorly soluble substances not suitable for irritant drugs Abscess- necrosis may happen I.V. suitable for large volumes and for irritating substances not suitable for oily solutions or poorly soluble substances Must inject solutions slowly as a rule
  • 18. Drugs are applied to skin, ear, eye, nose, vagina, respiratory tract Usually used to provide local action. No first pass metabolism. Used for lipid soluble drugs
  • 19. Disadvantages Advantages Not suitable for irritant drugs Only for some drugs as inhalation anesthetics & bronchodilators mucous membrane of respiratory system rapid absorption (large surface area) provide local action in limited systemic effect less side effects. no first pass effect Dosage form: aerosol, nebulizer
  • 21. Is the passage of drug from its site of administration to its site of action through cell membranes. Sites of Administration Sites of action Cell membrane
  • 23. Is the fraction of unchanged drug that enters systemic circulation after administration and becomes available to produce an action I.V. provides 100% bioavailability. Oral usually has less than I.V.