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Routes of drug administration
Prof. Shaikh Abusufiyan
Assistant Professor,
AIKTC-School of Pharmacy,
New Panvel-410206
Pharma Learning Forever
At the end of this e-learning session you are able to…
A. Explain different routes of
drug administration and their
advantages and disadvantages
Copyright @shaikhabusufiyan2022
 The choice of appropriate route in a given situation
depends both on:
drugs
patient related factors.
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1. Physical and chemical properties of the drug
- Solid/liquid/ gas
 Solubility and stability
 PH and irritancy
2. Site of desired action - localized and aprochable
3. Rate and extent of absorption of the drug from
different routes.
 Mostly common considerations are:
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4. Effect of digestive juices and first pass metabolism
of the drug.
5. Rapidity with which the response is desired (eg.
routine treatment or emergency).
6. Accuracy of dosage required (i.v. and inhalation).
7. Condition of the patient (unconscious, vomiting)
etc.
Copyright @shaikhabusufiyan2022
 Local routes:
 Topical
 Deeper tissues
 Arterial supply
Routes can be broadly divided into those for
(a) Local action and (b) Systemic action.
 Systemic routes:
 Oral
 Sublingual or buccal
 Rectal
 Cutaneous
 Inhalation
 Nasal
 Parentral
 Subcutaneous
 Intravenous
 Intramuscular and Intradermal
Copyright @shaikhabusufiyan2022
LOCAL ROUTES
 Only be used for localized lesions at accessible sites
and for drugs whose systemic absorption from these
sites is minimal or absent.
Advantages:
 High concentrations are attained at the desired site
without exposing the rest of the body.
Copyright @shaikhabusufiyan2022
 Systemic side effects are absent or minimal.
 For drugs (in suitable dosage forms) that are
absorbed from these routes, the same can serve as
systemic route of administration, e.g. glyceryl
trinitrate (GTN)
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The local routes are:
1. Topical
2. Deeper tissues
3. Arterial supply
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1. Topical
 This refers to external application of the drug to the
surface for localized action.
Advantages:
 More convenient and encouraging to the patient.
 Drugs can be efficiently delivered in the form of
lotion, ointment, cream,
powder
rinse, paints, drops, spray, lozengens, suppositories or
pesseries.
Copyright @shaikhabusufiyan2022
Other forms of Topical applications
 Non-absorbable drugs given orally for action on g.i.
mucosa Eg. sucralfate, vancomycin.
 Inhalation of drugs for action on bronchi
(salbutamol, cromolyn sodium)
 Irrigating solutions/ jellys (povidone iodine,
lidocaine) applied to urethra
Copyright @shaikhabusufiyan2022
2. Deeper tissues:
 Deep areas can be approached by using a syringe and needle
 But the drug should be such that systemic absorption is
slow.
Eg.
- A. intra-articular injection (hydrocortisone acetate)
- B. intrathecal injection (lidocaine),
- C. retrobulbar injection (hydrocortisone acetate).
A
B
C
3. Arterial supply:
 Eg:
Close intra-arterial injection is used for contrast media
in angiography
Anticancer drugs can be infused in femoral or brachial
artery
Copyright @shaikhabusufiyan2022
SYSTEMIC ROUTES
 It is intended to be absorbed
Into the blood stream and distributed all over
Copyright @shaikhabusufiyan2022
1. Oral
 oldest and commonest mode
Advantages:
 It is safer
 more convenient
 does not need assistance
 noninvasive
 often painless
 need not be sterile -- cheaper.
 Both solid dosage forms and liquid dosage forms can be
given orally.
Copyright @shaikhabusufiyan2022
Innovative dosage forms:
Dragées
 Medicated candies or sugar coated pills can be
referred to as dragées (A).
Spansules
 A capsule that when swallowed releases one or more
medicinal drugs over a set period is called as
spansules. A
B
Copyright @shaikhabusufiyan2022
Disadvantages:
 Action of drugs is slower - not for emergencies.
 Unpalatable drugs (chloramphenicol) - difficult to
administer - drug may be filled in capsules to
circumvent this.
 May cause nausea and vomiting (emetine).
Copyright @shaikhabusufiyan2022
 Cannot be used for uncooperative /unconscious
/vomiting patient.
 Absorption of drugs may be variable and certain
drugs are not absorbed (streptomycin)
 Some are destroyed by digestive juices (Penicillin G,
insulin) or in liver (testostrone, lidocaine).
Copyright @shaikhabusufiyan2022
2. Sublingual (s.i.) or buccal
 The drug is placed under the tongue or crushed in
the mouth and spread over the buccal mucosa.
 Only lipid soluble and non-irritating drugs can be
administered.
 Absorption is relatively rapid- action can be
produced in minutes.
Copyright @shaikhabusufiyan2022
Advantages
 Liver is bypassed and drugs with high first pass
metabolism can be absorbed directly into systemic
circulation.
Eg
 buprenorphine,
 desamino-oxytocin.
Copyright @shaikhabusufiyan2022
3. Rectal
 Certain irritant and unpleasant drugs can be put into rectum
(suppositories or retention enema) for systemic effect.
Advantages:
 Used when the patient is having recurrent vomiting or is
unconscious.
Disadvantages:
 Inconvenient and embarrassing;
 absorption is slower, irregular and often unpredictable
 Drug absorbed into external haemorrhoidal veins.
 Rectal inflammation can result from irritant drugs.
 Eg. Diazepam, indomethacin, paraldehyde, ergotamine
3. Cutaneous (Over skin)
 Highly lipid soluble drugs can be applied for slow
and prolonged absorption.
 Advantages:
 The liver is also bypassed.
 The drug can be incorporated in an ointment and
applied over specified area of skin.
 Absorption of the drug can be enhanced by
rubbing the preparation,
by using an oily base
and by an occlusive dressing.
Copyright @shaikhabusufiyan2022
Transdermal therapeutic systems:
 These are devices in the form of adhesive patches of various
shapes and sizes (5-20 cm)
 It deliver the drug at a constant rate into systemic
circulation via the stratum corneum.
 The drug (in solution or bound to a polymer) is held in a
reservoir
Copyright @shaikhabusufiyan2022
 The drug is delivered at the skin surface by diffusion
 The drug is delivered at a constant and predictable rate
 site of application:
usually chest
abdomen/ upper arm
lower back, buttock ect.
Copyright @shaikhabusufiyan2022
 Transdermal patches of GTN, Fentanyl, nicotine and
estradiol are available in India
 These have been designed to last the effect for 1-7
days.
 They are increasingly popular, because they provide
Smooth plasma concentrations of the drug without
fluctuations;
Minimize inter individual variations and SE.
More convenient
Patient compliance is better.
Copyright @shaikhabusufiyan2022
Disadvantage:
 Local irritation and erythema occurs in some, but is
generally mild
 Can be minimized by changing the site of
application each time by rotation.
 Discontinuation has been necessary in 2-7 %.
Copyright @shaikhabusufiyan2022
5. Inhalation
 Volatile liquids & gases are given by inhalation e.g.
general anaesthetics.
Absorption :Take place from the vast surface of
alveoli: action is very rapid.
Elimination: When administration is discontinued
the drug diffuses back and rapidly eliminated in
expired air. Copyright @shaikhabusufiyan2022
Advantages:
 Controlled administration is possible with moment
to moment adjustment.
Disadvantage:
 Irritant vapours (ether) --> cause inflammation of
respiratory tract and increase secretion.
Copyright @shaikhabusufiyan2022
6. Nasal
 The mucous membrane of the nose - readily
absorb many drugs
Advantage:
 Digestive juices and liver are bypassed.
Disadvantage:
 Only certain drugs are used by this route.
 Eg. desmopressin as a spray or nebulized solution.
Copyright @shaikhabusufiyan2022
Parenteral: (Par-beyond, enteral-intestinal)
 Administration by injection which takes the drug
directly into the tissue fluid or blood without
crossing the intestinal mucosa.
 ADVANTAGES:
 The limitations of oral administration are
circumvented.
Copyright @shaikhabusufiyan2022
 Drug action is faster and surer (valuable in
emergencies).
 Gastric irritation & vomiting are not provoked.
 Can be employed even in
unconscious
uncooperative or vomiting patient.
 There are no chances of interference by food or
digestive juices.
Copyright @shaikhabusufiyan2022
Disadvantages:
 The preparation has to be sterilized ---> costlier.
 More risky than oral
 The technique is
invasive and painful,
assistance of another person is mostly needed
 There are chances of local tissue injury
Copyright @shaikhabusufiyan2022
The important parenteral routes are:
(i) Subcutaneous (s.c.): The drug is deposited in the
loose subcutaneous tissue
Disadvantages:
 It is richly supplied by nerves (irritant drugs cannot
be injected)
 It is less vascular (absorption is slower than IM).
 Only small volumes can be injected s.c.
 Self-injection is possible because deep penetration is
not needed.
Copyright @shaikhabusufiyan2022
 Precaution: Should be avoided in shock patients
who are vasoconstricted: absorption will be
delayed.
 Repository (depot) preparations - prolonged action.
 Some special forms of this route are:
 (a) Dermojet
 (b) Pellet implantation
 (c) Sialistic (nonbiodegradable) and biodegradable
implants etc. Copyright @shaikhabusufiyan2022
(a) Dermojet:
 A high velocity jet of drug solution is projected from
a microfine orifice using a gun like implement.
 The solution passes through the superficial layers
and gets deposited in the subcutaneous tissue.
Advantages:
 It is essentially painless & suited for mass
inoculations.
Copyright @shaikhabusufiyan2022
(b) Pellet implantation:
 The drug in the form of a solid pellet is introduced
with a trochar and cannula.
 This provides sustained release of the drug over
weeks and months e.g. DOCA, testosterone.
Copyright @shaikhabusufiyan2022
(c) Sialistic (nonbiodegradable) and
biodegradable implants
 Crystalline drug is packed in tubes or capsules made of
suitable materials and implanted under the skin.
 Slow and uniform leaching of the drug occurs over
months providing constant blood levels.
 The nonbiodegradable implant has to be removed later on
but not the biodegradable one.
 Eg. for hormones and contraceptives (e.g. NoRPLANT).
Copyright @shaikhabusufiyan2022
(ii) Intramuscular (i.m.):
 The drug is injected in one of the large skeletal
muscles-- triceps, rectus femoris etc.
 Muscle is less richly supplied with sensory nerves
(mild irritants can be injected).
 It is more vascular (absorption is faster).
 It is less painful - self injection is often
impracticable.
 Depot preparations (oily solutions/ aqueous
suspensions) can be injected by this route.
Copyright @shaikhabusufiyan2022
 Intramuscular injections should be avoided in
anticoagulant treated patients
because it can produce local haematoma.
Copyright @shaikhabusufiyan2022
 The intima of veins is insensitive and drug gets
diluted with blood
even highly irritant drugs can be injected
But may produces thrombophlebitis of the injected
vein & necrosis of adjoining tissues if extravasation
occurs.
 These complications can be minimized by diluting
the drug or injecting it into a running i.v. line.
Copyright @shaikhabusufiyan2022
 The dose of the drug required is smallest
(bioavailability is 100%)
 And even large volumes can be infused.
 The response is accurately measurable (e.g. BP) &
titration of the dose with the response is possible.
Disadvantages:
 Most risky route
 Vital organs like heart, brain etc get exposed to high
concentrations of the drug.
 Only aqueous solutions (not suspensions) can be
injected and there are no depot preparations.
Copyright @shaikhabusufiyan2022
(iv) Intradermal iniection:
 The drug is injected into the skin raising a bleb (e.g.
BCG vaccine, sensitivity testing) or making
puncture of the epidermis.
Copyright @shaikhabusufiyan2022
Reference:
K D Tripathi. Essentials of Medical Pharmacology. Seventh Edition. Jaypee
Publication. Page no:3-10.
Copyright @shaikhabusufiyan2021
Disclaimer (Images)
The images used in this presentation are found from different sources all over the
Internet, and are assumed to be in public domain and are displayed under the fair
use principle for education purpose.
Copyright @ Presentation
The said presentation is copyright under Copyright @shaikhabusufiyan2022
The presentation is for education purpose only, don’t use the same for any legal
perspective.
Copyright @shaikhabusufiyan2022
Copyright @shaikhabusufiyan2022

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Routs of drug administration.pptx

  • 1. Routes of drug administration Prof. Shaikh Abusufiyan Assistant Professor, AIKTC-School of Pharmacy, New Panvel-410206 Pharma Learning Forever
  • 2. At the end of this e-learning session you are able to… A. Explain different routes of drug administration and their advantages and disadvantages Copyright @shaikhabusufiyan2022
  • 3.  The choice of appropriate route in a given situation depends both on: drugs patient related factors. Copyright @shaikhabusufiyan2022
  • 4. 1. Physical and chemical properties of the drug - Solid/liquid/ gas  Solubility and stability  PH and irritancy 2. Site of desired action - localized and aprochable 3. Rate and extent of absorption of the drug from different routes.  Mostly common considerations are: Copyright @shaikhabusufiyan2022
  • 5. 4. Effect of digestive juices and first pass metabolism of the drug. 5. Rapidity with which the response is desired (eg. routine treatment or emergency). 6. Accuracy of dosage required (i.v. and inhalation). 7. Condition of the patient (unconscious, vomiting) etc. Copyright @shaikhabusufiyan2022
  • 6.  Local routes:  Topical  Deeper tissues  Arterial supply Routes can be broadly divided into those for (a) Local action and (b) Systemic action.  Systemic routes:  Oral  Sublingual or buccal  Rectal  Cutaneous  Inhalation  Nasal  Parentral  Subcutaneous  Intravenous  Intramuscular and Intradermal Copyright @shaikhabusufiyan2022
  • 7. LOCAL ROUTES  Only be used for localized lesions at accessible sites and for drugs whose systemic absorption from these sites is minimal or absent. Advantages:  High concentrations are attained at the desired site without exposing the rest of the body. Copyright @shaikhabusufiyan2022
  • 8.  Systemic side effects are absent or minimal.  For drugs (in suitable dosage forms) that are absorbed from these routes, the same can serve as systemic route of administration, e.g. glyceryl trinitrate (GTN) Copyright @shaikhabusufiyan2022
  • 9. The local routes are: 1. Topical 2. Deeper tissues 3. Arterial supply Copyright @shaikhabusufiyan2022
  • 10. 1. Topical  This refers to external application of the drug to the surface for localized action. Advantages:  More convenient and encouraging to the patient.  Drugs can be efficiently delivered in the form of lotion, ointment, cream, powder rinse, paints, drops, spray, lozengens, suppositories or pesseries. Copyright @shaikhabusufiyan2022
  • 11. Other forms of Topical applications  Non-absorbable drugs given orally for action on g.i. mucosa Eg. sucralfate, vancomycin.  Inhalation of drugs for action on bronchi (salbutamol, cromolyn sodium)  Irrigating solutions/ jellys (povidone iodine, lidocaine) applied to urethra Copyright @shaikhabusufiyan2022
  • 12. 2. Deeper tissues:  Deep areas can be approached by using a syringe and needle  But the drug should be such that systemic absorption is slow. Eg. - A. intra-articular injection (hydrocortisone acetate) - B. intrathecal injection (lidocaine), - C. retrobulbar injection (hydrocortisone acetate). A B C
  • 13. 3. Arterial supply:  Eg: Close intra-arterial injection is used for contrast media in angiography Anticancer drugs can be infused in femoral or brachial artery Copyright @shaikhabusufiyan2022
  • 14. SYSTEMIC ROUTES  It is intended to be absorbed Into the blood stream and distributed all over Copyright @shaikhabusufiyan2022
  • 15. 1. Oral  oldest and commonest mode Advantages:  It is safer  more convenient  does not need assistance  noninvasive  often painless  need not be sterile -- cheaper.  Both solid dosage forms and liquid dosage forms can be given orally. Copyright @shaikhabusufiyan2022
  • 16. Innovative dosage forms: Dragées  Medicated candies or sugar coated pills can be referred to as dragées (A). Spansules  A capsule that when swallowed releases one or more medicinal drugs over a set period is called as spansules. A B Copyright @shaikhabusufiyan2022
  • 17. Disadvantages:  Action of drugs is slower - not for emergencies.  Unpalatable drugs (chloramphenicol) - difficult to administer - drug may be filled in capsules to circumvent this.  May cause nausea and vomiting (emetine). Copyright @shaikhabusufiyan2022
  • 18.  Cannot be used for uncooperative /unconscious /vomiting patient.  Absorption of drugs may be variable and certain drugs are not absorbed (streptomycin)  Some are destroyed by digestive juices (Penicillin G, insulin) or in liver (testostrone, lidocaine). Copyright @shaikhabusufiyan2022
  • 19. 2. Sublingual (s.i.) or buccal  The drug is placed under the tongue or crushed in the mouth and spread over the buccal mucosa.  Only lipid soluble and non-irritating drugs can be administered.  Absorption is relatively rapid- action can be produced in minutes. Copyright @shaikhabusufiyan2022
  • 20. Advantages  Liver is bypassed and drugs with high first pass metabolism can be absorbed directly into systemic circulation. Eg  buprenorphine,  desamino-oxytocin. Copyright @shaikhabusufiyan2022
  • 21. 3. Rectal  Certain irritant and unpleasant drugs can be put into rectum (suppositories or retention enema) for systemic effect. Advantages:  Used when the patient is having recurrent vomiting or is unconscious. Disadvantages:  Inconvenient and embarrassing;  absorption is slower, irregular and often unpredictable  Drug absorbed into external haemorrhoidal veins.  Rectal inflammation can result from irritant drugs.  Eg. Diazepam, indomethacin, paraldehyde, ergotamine
  • 22. 3. Cutaneous (Over skin)  Highly lipid soluble drugs can be applied for slow and prolonged absorption.  Advantages:  The liver is also bypassed.  The drug can be incorporated in an ointment and applied over specified area of skin.  Absorption of the drug can be enhanced by rubbing the preparation, by using an oily base and by an occlusive dressing. Copyright @shaikhabusufiyan2022
  • 23. Transdermal therapeutic systems:  These are devices in the form of adhesive patches of various shapes and sizes (5-20 cm)  It deliver the drug at a constant rate into systemic circulation via the stratum corneum.  The drug (in solution or bound to a polymer) is held in a reservoir Copyright @shaikhabusufiyan2022
  • 24.  The drug is delivered at the skin surface by diffusion  The drug is delivered at a constant and predictable rate  site of application: usually chest abdomen/ upper arm lower back, buttock ect. Copyright @shaikhabusufiyan2022
  • 25.  Transdermal patches of GTN, Fentanyl, nicotine and estradiol are available in India  These have been designed to last the effect for 1-7 days.  They are increasingly popular, because they provide Smooth plasma concentrations of the drug without fluctuations; Minimize inter individual variations and SE. More convenient Patient compliance is better. Copyright @shaikhabusufiyan2022
  • 26. Disadvantage:  Local irritation and erythema occurs in some, but is generally mild  Can be minimized by changing the site of application each time by rotation.  Discontinuation has been necessary in 2-7 %. Copyright @shaikhabusufiyan2022
  • 27. 5. Inhalation  Volatile liquids & gases are given by inhalation e.g. general anaesthetics. Absorption :Take place from the vast surface of alveoli: action is very rapid. Elimination: When administration is discontinued the drug diffuses back and rapidly eliminated in expired air. Copyright @shaikhabusufiyan2022
  • 28. Advantages:  Controlled administration is possible with moment to moment adjustment. Disadvantage:  Irritant vapours (ether) --> cause inflammation of respiratory tract and increase secretion. Copyright @shaikhabusufiyan2022
  • 29. 6. Nasal  The mucous membrane of the nose - readily absorb many drugs Advantage:  Digestive juices and liver are bypassed. Disadvantage:  Only certain drugs are used by this route.  Eg. desmopressin as a spray or nebulized solution. Copyright @shaikhabusufiyan2022
  • 30. Parenteral: (Par-beyond, enteral-intestinal)  Administration by injection which takes the drug directly into the tissue fluid or blood without crossing the intestinal mucosa.  ADVANTAGES:  The limitations of oral administration are circumvented. Copyright @shaikhabusufiyan2022
  • 31.  Drug action is faster and surer (valuable in emergencies).  Gastric irritation & vomiting are not provoked.  Can be employed even in unconscious uncooperative or vomiting patient.  There are no chances of interference by food or digestive juices. Copyright @shaikhabusufiyan2022
  • 32. Disadvantages:  The preparation has to be sterilized ---> costlier.  More risky than oral  The technique is invasive and painful, assistance of another person is mostly needed  There are chances of local tissue injury Copyright @shaikhabusufiyan2022
  • 33. The important parenteral routes are: (i) Subcutaneous (s.c.): The drug is deposited in the loose subcutaneous tissue Disadvantages:  It is richly supplied by nerves (irritant drugs cannot be injected)  It is less vascular (absorption is slower than IM).  Only small volumes can be injected s.c.  Self-injection is possible because deep penetration is not needed. Copyright @shaikhabusufiyan2022
  • 34.  Precaution: Should be avoided in shock patients who are vasoconstricted: absorption will be delayed.  Repository (depot) preparations - prolonged action.  Some special forms of this route are:  (a) Dermojet  (b) Pellet implantation  (c) Sialistic (nonbiodegradable) and biodegradable implants etc. Copyright @shaikhabusufiyan2022
  • 35. (a) Dermojet:  A high velocity jet of drug solution is projected from a microfine orifice using a gun like implement.  The solution passes through the superficial layers and gets deposited in the subcutaneous tissue. Advantages:  It is essentially painless & suited for mass inoculations. Copyright @shaikhabusufiyan2022
  • 36. (b) Pellet implantation:  The drug in the form of a solid pellet is introduced with a trochar and cannula.  This provides sustained release of the drug over weeks and months e.g. DOCA, testosterone. Copyright @shaikhabusufiyan2022
  • 37. (c) Sialistic (nonbiodegradable) and biodegradable implants  Crystalline drug is packed in tubes or capsules made of suitable materials and implanted under the skin.  Slow and uniform leaching of the drug occurs over months providing constant blood levels.  The nonbiodegradable implant has to be removed later on but not the biodegradable one.  Eg. for hormones and contraceptives (e.g. NoRPLANT). Copyright @shaikhabusufiyan2022
  • 38. (ii) Intramuscular (i.m.):  The drug is injected in one of the large skeletal muscles-- triceps, rectus femoris etc.  Muscle is less richly supplied with sensory nerves (mild irritants can be injected).  It is more vascular (absorption is faster).  It is less painful - self injection is often impracticable.  Depot preparations (oily solutions/ aqueous suspensions) can be injected by this route. Copyright @shaikhabusufiyan2022
  • 39.  Intramuscular injections should be avoided in anticoagulant treated patients because it can produce local haematoma. Copyright @shaikhabusufiyan2022
  • 40.  The intima of veins is insensitive and drug gets diluted with blood even highly irritant drugs can be injected But may produces thrombophlebitis of the injected vein & necrosis of adjoining tissues if extravasation occurs.  These complications can be minimized by diluting the drug or injecting it into a running i.v. line. Copyright @shaikhabusufiyan2022
  • 41.  The dose of the drug required is smallest (bioavailability is 100%)  And even large volumes can be infused.  The response is accurately measurable (e.g. BP) & titration of the dose with the response is possible. Disadvantages:  Most risky route  Vital organs like heart, brain etc get exposed to high concentrations of the drug.  Only aqueous solutions (not suspensions) can be injected and there are no depot preparations. Copyright @shaikhabusufiyan2022
  • 42. (iv) Intradermal iniection:  The drug is injected into the skin raising a bleb (e.g. BCG vaccine, sensitivity testing) or making puncture of the epidermis. Copyright @shaikhabusufiyan2022
  • 43. Reference: K D Tripathi. Essentials of Medical Pharmacology. Seventh Edition. Jaypee Publication. Page no:3-10. Copyright @shaikhabusufiyan2021
  • 44. Disclaimer (Images) The images used in this presentation are found from different sources all over the Internet, and are assumed to be in public domain and are displayed under the fair use principle for education purpose. Copyright @ Presentation The said presentation is copyright under Copyright @shaikhabusufiyan2022 The presentation is for education purpose only, don’t use the same for any legal perspective. Copyright @shaikhabusufiyan2022