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Routes of Administration of drugs
By.
Dr.Abdul latif Mahesar
ROUTES OFADMINISTRATION
►Enteral (Alimentary)
► Par - enteral
( Other than Alimentary)
ROUTES OFADMINISTRATION
Enteral (Alimentary canal)
 Oral
 Buccal & Sublingual
 Rectal
 Nasogastric
Par - enteral ( Other than Alimentary)
 Par - enteral injections
Intravenous , intramuscular, intradermal,
Subcutaneous, intrarterial, intrarticular,
intraperitoneal, intrathecal
 Inhalation
 Topical
ORAL
MERITS
 Commonest, Safest
 Convenient ,
 No skill required, self medication
 Painless, & acceptable
 Cost effective
 No maximal/strict sterilization required
ORAL
 MERITS cont’d
 Due to slow rate of absorption adverse effects occurs less and
slowly as compared to
parenteral route
 Large volume (doses) can be given
 Systemic / local effects in G.I.T
For local effect
e.g.,
neomycin (an aminoglycoside),
anthelmintics
antiamoebic.
ORAL con’d
De-merits
 Absorption varies (delay, decrease, or
increase )
affected by ---- food or drugs that affect GI
motility
e.g. antimuscarinic, opioids )
 (Dose may not accurately be delivered)
 Irritation of gastric mucosa
 Patient compliance not ensured
ORAL cont’d
Demerits
 First pass metabolism ( First pass effect,
Presystemic elimination)
 Metabolism of drug (to inactive form)
after administration before it reaches the
systemic circulation Usually with orally
administered drugs
ORAL
De-merits cont’d
 First pass metabolism
- Orally administered drugs
- First pass effect in GIT
- Hepatic first pass metabolism
during its first passage thru liver
 Greater the first pass effect, lesser will be
the bioavailability
BIOAVAILABILITY
is the fraction of administered drug that
gain access to the systemic circulation
(after absorption) in a chemically
unchanged form
ORAL cont’d
Demerits cont’d
- Drugs with high first pass effect needs
to be given in high doses
- Variation in first pass effect
among individuals cause variation in
drug response
ORAL cont’d
Demerits cont’d
 Not suitable for :
Unconscious patients
Vomiting patients
Emergency --- (Slow onset of action)
 GIT diseases or abnormality may
affect the absorption of drug
ORAL cont’d
Demerits
- Following drugs can not be given by oral route:
- Drugs destroyed by Stomach pH
(some Penicillins e.g., benzyl penicillin)
- Drugs destroyed by Intestinal enzymes
(e.g., Insulin, oxytocin)
- Hydrophilic drugs which can not absorbed
(e.g., Aminoglycosides, but can be given for
local effect such as neomycin)
ORAL cont;d
Demerits cont’d
Uneven distribution (for local effect),
in some diseases of gut whole thickness of wall is
affected (e.g. severe bacillary dysentery, typhoid)
& effective blood concentrations ( as well as
luminal concentrations ) may be needed.
Drug interaction:
one drug can affect the absorption of other
drug e.g., antacids decrease the absorption of
tetracyclines.
SUBLINGUAL & BUCCAL
Merits
 Rapid onset of action
 useful in emergency
(glyceryl trinitrate, nifedipine & ergotamine),
especially if tablet is crushed, giving greater
surface area for solution
 Effect can be terminated by spitting out tablet
SUBLINGUAL & BUCCAL
Merits
 No sterilization required
 No skill
 first pass hepatic metabolism is avoided
 Increase in bioavailability
 Not affected by gastric acidity or intestinal enzymes
SUBLINGUAL & BUCCal
Demerits
 Inconvenient for frequent use
 Irritation of oral mucosa & excessive
salivation
 Promotes swallowing, so losing the advantage of
bypassing the first pass effect
 Patient compliance not ensured
 Not suitable for large doses and vomiting patients
 Bitter, irritant can not be given
RECTAL
 Dose requirement same or slightly greater than
oral route
RECTAL
Merits
 Can be used for producing both the systemic effects
and local effects
 Drugs that are irritant to stomach can be given by
suppository (aminophylline, indomethacin)
 Suitable in unconscious, vomiting , motion
sickness, migraine or when a patient can not swallow , &
when cooperation is lacking (sedation in children)
RECTAL
Merits
 No sterilization
 No skill
 Avoid 50% first pass hepatic metabolism (from
lower rectum)
 For local effect e.g. in proctitis or colitis
RECTAL
Demerits
 Psychological, patient may be embarrassed and dislike this
way
 Irritation of mucosa & inflammation may occur
with repeated use
 Emergency (slow onset of action)
 Absorption unreliable, especially if rectum is full of
feces
PAR-ENTERAL INJECTIONS
Dosage forms:
Solution,
Suspension
PAR-ENTERAL INJECTIONS
Intravenous ( I / V ),
Intramuscular ( I / M ),
Subcutaneous ( S / C )
Intra dermal
Intra articular
Intrathecal
Intraperitoneal
I / V INJECTIONS & INFUSIONS
Merits
 Rapid onset of action
 useful in emergency
 No first pass effect, 100% bioavailability,
 Dose more accurately delivered & give smooth
effective, & highly predictable blood
concentration
 Suitable in vomiting , motion sickness, migraine,
unconscious patients, or when a patient can not
swallow , & when cooperation is lacking
- Large volume (doses) of drug can be given
Intra venous and I.V infusions cont’d
Merits
 Suitable in vomiting , motion sickness, migraine,
unconscious patients, or when a patient can not
swallow , & when cooperation is lacking
 Large volume (doses) of drug can be given
Intra venous and I.V infusions cont’d
 Following drugs which can not be given by
oral route, are given intravenously
 Drugs destroyed by stomach pH
(some Penicillins e.g., benzyl penicillin)
 Drugs destroyed by intestinal enzymes
(e.g., Insulin)
 Hydrophilic drugs which can not absorbed
(e.g., Aminoglycosides)
Intra venous and I.V infusions cont’d
Merits
- Drugs that are too irritant (anticancer agents) to be
given by other routes
- In I.V. infusion ----Rapid modification of dose and
immediate cessation of administration if unwanted
effects occur
I / V INJECTIONS & INFUSIONS
De-merits
 Costly
 Inconvenient
 More chances of adverse effects, most
dangerous
 Maximal Sterilization, chances of infection
Skill, no self medication
 Local irritation at site of administration
I / V INJECTIONS & INFUSIONS
Demerits
 Local venous thrombosis with:
prolonged infusion
irritant formulations
microparticulate components of infusion
fluids, especially if small veins are used
Infection of intravenous catheter and small
thrombi on its tip during prolonged infusions
PARENTERAL : I / M INJECTIONS
Merits
 Reliable and suitable for irritant drugs and
depot preparations (penicillins , neuroleptics,
medroxyprogesterone) can be used at monthly
or longer intervals
 Absorption is more rapid than following
subcutaneous injection or oral route
(soluble preparations are absorbed within 10 – 30 mins.)
: I / M INJECTIONS
De-merits
 Inconvenient
 Painful especially for frequent use
 More chances of adverse effects than oral
Sterilization,
 Chances of infection
 Skill required
 Local irritation at site of administration
I / M INJECTIONS
De-merits
Not acceptable for self administration
If any adverse effect occur tha can not be
removed.
S / C INJECTIONS
Merits
 Can be used for local and systemic effects both
 Reliable and acceptable for self administration
(e.g. diabetic patients taking Insulin)
For local effect --- e.g. local anesthetics
S / C INJECTIONS
De-merits
 Poor absorption in peripheral circulatory
failure
 repeated injections at one site can cause
lipodystrophy, resulting in erratic
absorption (insulin)
INHALATION
 Can be used for local & systemic effects both
As a gas, --- e.g. ---- General anaesthetics
As an aerosol,--- e.g. ---- β2 –adrenoceptor agonist
bronchodilators
As a powder, e.g. sodium chromoglycate
INHALATION
Merits
 Drugs as gases can be rapidly taken up or eliminated,
giving the close control that has marked the use of
this route in general anesthesia
 Self administration is practicable
 Aerosols & powders provide high local concentration
for action on bronchi, minimizing systemic effects
 Aerosols can also be used for systemic effect, e.g
ergotamine for migraine
INHALATION
De-merits
 Special apparatus is needed
 Drug must be nonirritant.
 If the patient is unconscious
Obstructed bronchi (mucus plugs in asthma)
may
cause therapy to fail
TOPICAL application
For local effect
 Skin
 Mucous membrane (eye, nose , ear , lungs,
anal canal, rectum, urethra, vagina, etc. )
For systemic effect ----- Transdermal
TOPICALAPPLICATION: FOR LOCAL EFFECT
Dosage forms
Ointment, lotion, cream, etc
Merits
usually high local concentration can be used
without systemic effect
TOPICAL APPLICATION: FOR LOCAL EFFECT
Demerits
systemic effects can occur especially when there is
tissue destruction e.g.,
adrenal steroids & neomycin --- to ---- skin,
atropine & β-adrenoceptor blocker --- to --- eye
TOPICALAPPLICATION: FOR SYSTEMIC EFFECT:
TRANSDERMAL DELIVERY SYSTEM (TDS)
Dosage form:
 Patches, ointment
as a sticking plaster (Patch) attached to skin or
as an ointment
glyceryl trinitrate
postmenopausal hormone replacement
TOPICALAPPLICATION: FOR SYSTEMIC EFFECT
Merits:
 Used for slow continuous administration for long
duration
 Fluctuations in plasma concentration are largely
avoided
 Usually No first pass effect
 Drug can be removed if required
TOPICALAPPLICATION: FOR SYSTEMIC EFFECT:
Demerits:
 Only small number of drugs can be used by
this route
 Slow onset of action
 Local reactions

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03.(LEC 3) ROUTES OF DRUG ADMINSTRATION.ppt

  • 1. Routes of Administration of drugs By. Dr.Abdul latif Mahesar
  • 2. ROUTES OFADMINISTRATION ►Enteral (Alimentary) ► Par - enteral ( Other than Alimentary)
  • 3. ROUTES OFADMINISTRATION Enteral (Alimentary canal)  Oral  Buccal & Sublingual  Rectal  Nasogastric
  • 4. Par - enteral ( Other than Alimentary)  Par - enteral injections Intravenous , intramuscular, intradermal, Subcutaneous, intrarterial, intrarticular, intraperitoneal, intrathecal  Inhalation  Topical
  • 5. ORAL MERITS  Commonest, Safest  Convenient ,  No skill required, self medication  Painless, & acceptable  Cost effective  No maximal/strict sterilization required
  • 6. ORAL  MERITS cont’d  Due to slow rate of absorption adverse effects occurs less and slowly as compared to parenteral route  Large volume (doses) can be given  Systemic / local effects in G.I.T For local effect e.g., neomycin (an aminoglycoside), anthelmintics antiamoebic.
  • 7. ORAL con’d De-merits  Absorption varies (delay, decrease, or increase ) affected by ---- food or drugs that affect GI motility e.g. antimuscarinic, opioids )  (Dose may not accurately be delivered)  Irritation of gastric mucosa  Patient compliance not ensured
  • 8. ORAL cont’d Demerits  First pass metabolism ( First pass effect, Presystemic elimination)  Metabolism of drug (to inactive form) after administration before it reaches the systemic circulation Usually with orally administered drugs
  • 9. ORAL De-merits cont’d  First pass metabolism - Orally administered drugs - First pass effect in GIT - Hepatic first pass metabolism during its first passage thru liver  Greater the first pass effect, lesser will be the bioavailability
  • 10. BIOAVAILABILITY is the fraction of administered drug that gain access to the systemic circulation (after absorption) in a chemically unchanged form
  • 11. ORAL cont’d Demerits cont’d - Drugs with high first pass effect needs to be given in high doses - Variation in first pass effect among individuals cause variation in drug response
  • 12. ORAL cont’d Demerits cont’d  Not suitable for : Unconscious patients Vomiting patients Emergency --- (Slow onset of action)  GIT diseases or abnormality may affect the absorption of drug
  • 13. ORAL cont’d Demerits - Following drugs can not be given by oral route: - Drugs destroyed by Stomach pH (some Penicillins e.g., benzyl penicillin) - Drugs destroyed by Intestinal enzymes (e.g., Insulin, oxytocin) - Hydrophilic drugs which can not absorbed (e.g., Aminoglycosides, but can be given for local effect such as neomycin)
  • 14. ORAL cont;d Demerits cont’d Uneven distribution (for local effect), in some diseases of gut whole thickness of wall is affected (e.g. severe bacillary dysentery, typhoid) & effective blood concentrations ( as well as luminal concentrations ) may be needed. Drug interaction: one drug can affect the absorption of other drug e.g., antacids decrease the absorption of tetracyclines.
  • 15. SUBLINGUAL & BUCCAL Merits  Rapid onset of action  useful in emergency (glyceryl trinitrate, nifedipine & ergotamine), especially if tablet is crushed, giving greater surface area for solution  Effect can be terminated by spitting out tablet
  • 16. SUBLINGUAL & BUCCAL Merits  No sterilization required  No skill  first pass hepatic metabolism is avoided  Increase in bioavailability  Not affected by gastric acidity or intestinal enzymes
  • 17. SUBLINGUAL & BUCCal Demerits  Inconvenient for frequent use  Irritation of oral mucosa & excessive salivation  Promotes swallowing, so losing the advantage of bypassing the first pass effect  Patient compliance not ensured  Not suitable for large doses and vomiting patients  Bitter, irritant can not be given
  • 18. RECTAL  Dose requirement same or slightly greater than oral route
  • 19. RECTAL Merits  Can be used for producing both the systemic effects and local effects  Drugs that are irritant to stomach can be given by suppository (aminophylline, indomethacin)  Suitable in unconscious, vomiting , motion sickness, migraine or when a patient can not swallow , & when cooperation is lacking (sedation in children)
  • 20. RECTAL Merits  No sterilization  No skill  Avoid 50% first pass hepatic metabolism (from lower rectum)  For local effect e.g. in proctitis or colitis
  • 21. RECTAL Demerits  Psychological, patient may be embarrassed and dislike this way  Irritation of mucosa & inflammation may occur with repeated use  Emergency (slow onset of action)  Absorption unreliable, especially if rectum is full of feces
  • 23. PAR-ENTERAL INJECTIONS Intravenous ( I / V ), Intramuscular ( I / M ), Subcutaneous ( S / C ) Intra dermal Intra articular Intrathecal Intraperitoneal
  • 24. I / V INJECTIONS & INFUSIONS Merits  Rapid onset of action  useful in emergency  No first pass effect, 100% bioavailability,  Dose more accurately delivered & give smooth effective, & highly predictable blood concentration  Suitable in vomiting , motion sickness, migraine, unconscious patients, or when a patient can not swallow , & when cooperation is lacking - Large volume (doses) of drug can be given
  • 25. Intra venous and I.V infusions cont’d Merits  Suitable in vomiting , motion sickness, migraine, unconscious patients, or when a patient can not swallow , & when cooperation is lacking  Large volume (doses) of drug can be given
  • 26. Intra venous and I.V infusions cont’d  Following drugs which can not be given by oral route, are given intravenously  Drugs destroyed by stomach pH (some Penicillins e.g., benzyl penicillin)  Drugs destroyed by intestinal enzymes (e.g., Insulin)  Hydrophilic drugs which can not absorbed (e.g., Aminoglycosides)
  • 27. Intra venous and I.V infusions cont’d Merits - Drugs that are too irritant (anticancer agents) to be given by other routes - In I.V. infusion ----Rapid modification of dose and immediate cessation of administration if unwanted effects occur
  • 28. I / V INJECTIONS & INFUSIONS De-merits  Costly  Inconvenient  More chances of adverse effects, most dangerous  Maximal Sterilization, chances of infection Skill, no self medication  Local irritation at site of administration
  • 29. I / V INJECTIONS & INFUSIONS Demerits  Local venous thrombosis with: prolonged infusion irritant formulations microparticulate components of infusion fluids, especially if small veins are used Infection of intravenous catheter and small thrombi on its tip during prolonged infusions
  • 30. PARENTERAL : I / M INJECTIONS Merits  Reliable and suitable for irritant drugs and depot preparations (penicillins , neuroleptics, medroxyprogesterone) can be used at monthly or longer intervals  Absorption is more rapid than following subcutaneous injection or oral route (soluble preparations are absorbed within 10 – 30 mins.)
  • 31. : I / M INJECTIONS De-merits  Inconvenient  Painful especially for frequent use  More chances of adverse effects than oral Sterilization,  Chances of infection  Skill required  Local irritation at site of administration
  • 32. I / M INJECTIONS De-merits Not acceptable for self administration If any adverse effect occur tha can not be removed.
  • 33. S / C INJECTIONS Merits  Can be used for local and systemic effects both  Reliable and acceptable for self administration (e.g. diabetic patients taking Insulin) For local effect --- e.g. local anesthetics
  • 34. S / C INJECTIONS De-merits  Poor absorption in peripheral circulatory failure  repeated injections at one site can cause lipodystrophy, resulting in erratic absorption (insulin)
  • 35. INHALATION  Can be used for local & systemic effects both As a gas, --- e.g. ---- General anaesthetics As an aerosol,--- e.g. ---- β2 –adrenoceptor agonist bronchodilators As a powder, e.g. sodium chromoglycate
  • 36. INHALATION Merits  Drugs as gases can be rapidly taken up or eliminated, giving the close control that has marked the use of this route in general anesthesia  Self administration is practicable  Aerosols & powders provide high local concentration for action on bronchi, minimizing systemic effects  Aerosols can also be used for systemic effect, e.g ergotamine for migraine
  • 37. INHALATION De-merits  Special apparatus is needed  Drug must be nonirritant.  If the patient is unconscious Obstructed bronchi (mucus plugs in asthma) may cause therapy to fail
  • 38. TOPICAL application For local effect  Skin  Mucous membrane (eye, nose , ear , lungs, anal canal, rectum, urethra, vagina, etc. ) For systemic effect ----- Transdermal
  • 39. TOPICALAPPLICATION: FOR LOCAL EFFECT Dosage forms Ointment, lotion, cream, etc Merits usually high local concentration can be used without systemic effect
  • 40. TOPICAL APPLICATION: FOR LOCAL EFFECT Demerits systemic effects can occur especially when there is tissue destruction e.g., adrenal steroids & neomycin --- to ---- skin, atropine & β-adrenoceptor blocker --- to --- eye
  • 41. TOPICALAPPLICATION: FOR SYSTEMIC EFFECT: TRANSDERMAL DELIVERY SYSTEM (TDS) Dosage form:  Patches, ointment as a sticking plaster (Patch) attached to skin or as an ointment glyceryl trinitrate postmenopausal hormone replacement
  • 42. TOPICALAPPLICATION: FOR SYSTEMIC EFFECT Merits:  Used for slow continuous administration for long duration  Fluctuations in plasma concentration are largely avoided  Usually No first pass effect  Drug can be removed if required
  • 43. TOPICALAPPLICATION: FOR SYSTEMIC EFFECT: Demerits:  Only small number of drugs can be used by this route  Slow onset of action  Local reactions