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Routes of Administration of Drugs

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Routes of Administration of drugs

By.
Dr.Abdul latif Mahesar
ROUTES OF ADMINISTRATION

►Enteral (Alimentary)

► Par - enteral
( Other than Alimentary)
ROUTES OF ADMINISTRATION

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


TOPICAL APPLICATION: 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
TOPICAL APPLICATION: 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
TOPICAL APPLICATION: 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


TOPICAL APPLICATION: 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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