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Routes of Drug Administration
Sreenu Thalla
Clinical Pharmacologist
Systemic Routes
 Drugs administered by this route enter blood and produce systemic
effects.
 Medication, nutrition or other substances into the circulatory system so
that the entire body is affected.
 It classify 2 broad categories like Enteral (oral, sublingual, and rectal)
and Parenteral (inhalation, injection, transdermal) routes.
1. Oral Route
 It is the most common and acceptable route for drug administration. Dosage forms are
tablet, capsule, syrup, mixture, etc., e.g., paracetamol tablet for fever, omeprazole
capsule for peptic ulcer are given orally.
Advantages
Safer Cheaper Painless
Disadvantages
• Not suitable for emergency as onset of action of orally administered drugs
is slow
• It is not suitable for/in:
• Unpalatable and highly irritant drugs
• Unabsorbable drugs (e.g. aminoglycosides)
• Drugs that are destroyed by digestive juices (e.g. insulin)
• Drugs with extensive first-pass metabolism (e.g. lignocaine)
• Unconscious patients
• Uncooperative and unreliable patients
• Patients with severe vomiting and diarrhoea
Convenient for
repeated and
prolonged use
Can be self-
administered
2. Sublingual/Buccal Route
 The preparation is kept under the tongue.
 The drug is absorbed through the buccal mucous membrane and enters the
systemic circulation directly
 Eg. nitroglycerin for acute anginal attack and buprenorphine for myocardial
infarction.
Advantages
Quick onset of action.
Action can be terminated by spitting
out the tablet.
Bypasses first-pass metabolism
Self-administration is possible.
Disadvantages
It is not suitable for:
Irritant and lipid-insoluble drugs.
Drugs with bad smell and taste.
3. Rectal Route
 Drugs can be given in the form of solid or liquid.
a. Suppository: It can be used for local (topical) effect as well as systemic effect, e.g.
indomethacin for rheumatoid arthritis.
b. Enema: Retention enema can be used for local effect as well as systemic effect. The
drug is absorbed through rectal mucous membrane and produces systemic effect, e.g.
diazepam for status epilepticus in children.
• Useful in the patient is having recurrent
vomiting or unconscious stage.
• Potential of long term drug absorption
with various intrauterine devices (IUDs).
• Some irritant and unpleasant drugs can be
introduced into rectum as suppositories.
Advantages
• This is rather inconvenient and embarrassing.
• Absorption is slower, irregular and unpredictable.
• Bleeding problems such as discomfort to real pathologies.
Disadvantages
Parenteral Routes
 Routes of administration other than enteral route are called parenteral routes.
• Onset of action of drugs is faster; hence it is
suitable for emergency.
• Useful in: Unconscious, Uncooperative and
unreliable patients.
• It is suitable for: Irritant drugs, Drugs with high
first-pass metabolism, Drugs not absorbed orally,
Drugs destroyed by digestive juices.
Advantages
• Preparations should be sterile and is expensive.
• Requires invasive techniques that are painful.
• Cannot be usually self-administered.
• Can cause local tissue injury to nerves, vessels etc.
• Require aseptic conditions.
Disadvantages
1. Inhalation
• Quick onset of action.
• Dose required is very
less, so systemic
toxicity is minimized.
• Amount of drug
administered can be
regulated.
Drugs which are gaseous (e.g., nitrous oxide) or readily vaporized (e.g., isoflurane) may
be inhaled.
 Solid drugs may also be given by inhalation route in the form of aerosols or suspended
powder (e.g., salbutamol and beclomethasone). The inhalation route may be used for
producing both local (e.g., bronchodilatation in asthma) as well as systemic effects
(anesthesia).
Advantages Disadvantages
• Local irritation may
cause increased
respiratory secretions
and bronchospasm.
Advancements
Nebulizer
Metered Dose
Inhaler (MDI)
Powder
Inhaler
(DPI)
2. Injections
Injectable Routes of DrugAdministration
 The drug is injected into the layers of the skin, e.g. Bacillus Calmette–Guerin (BCG)
vaccination and drug sensitivity tests. It is painful and only a small amount of the drug
can be administered.
 Intradermal injectionalso known as the mantoux method.
Purpose : Injects medication below the epidermis drugs are absorbed slowly.
Typically used for diagnosis of tuberculosis and allergens.
a. Intradermal Route
Methods of
Intradermal
Injections
Normal Size
Needle
Shorter
Needle
Without
Needle
b. Subcutaneous Route (s.c.)
 The drug is injected into the subcutaneous tissues of the thigh, abdomen and arm,
e.g. adrenaline, insulin, etc.
 Only small amount can be injected S.C self injection is possible because deep
penetration in not needed
Advantages
• Self-administration is possible
(e.g. insulin).
• Depot preparations can be
inserted into the subcutaneous
tissue, e.g. norplant for
contraception.
Disadvantages
• It is suitable only for nonirritant
drugs.
• Drug absorption is slow; hence it
is not suitable for emergency.
Advancement in Subcutaneous Route
Dermojet
• A high velocity jet of drug solution is projected from a microfineorifice
using a gun like implement.
• The solution passes through the superficial layers and gets deposited in the
subcutaneous tissue.
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.
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.
• Examples - for hormones and contraceptives (e.g. NoRPLANT).
c. Intramuscular Route (I.M.)
 Drugs are injected into large muscles such as deltoid,
gluteus maximus, e.g. paracetamol, diclofenac, etc.
 A volume of 5–10 mL can be given at a time.
Advantages
Disadvantages
• Absorption is more rapid as compared to
oral route.
• Mild irritants, depot injections, soluble
substances and suspensions can be given
by this route.
• Aseptic conditions are needed.
• Intramuscular injections are painful and
may cause abscess.
• Self-administration is not possible.
• There may be injury to the nerves.
d. Intravenous Route (i.v.)
 Injection into a peripheral vein over 1 to 2 minutes (bolus) or longer as an infusion.
 Drugs are injected directly into the blood stream through a vein. Drugs are
administered as:
1. Bolus: Single, relatively large dose of a drug injected rapidly or slowly as a single unit
into a vein. For example, i.v. ranitidine in bleeding peptic ulcer.
2. Intravenous infusion: For example, dopamine infusion in cardiogenic shock;
mannitol infusion in cerebral oedema; fluids infused intravenously in dehydration.
3. Slow intravenous injection: For example, i.v. morphine in myocardial infarction.
Advantages
• Bioavailability is 100%.
• Quick onset of action; therefore, it is
the route of choice in emergency.
• Large volume of fluid can be
administered, e.g. intravenous
fluids in patients with severe
dehydration.
• Highly irritant drugs, e.g.
anticancer drugs can be given
because they get diluted in blood.
• Hypertonic solution can be infused
by intravenous route, e.g. 20%
mannitol in cerebral oedema.
Disadvantages
• Local irritation may cause phlebitis.
• Self-medication is not possible.
• Once the drug is injected, its
action cannot be halted.
• Strict aseptic conditions are needed.
• Extravasation of some drugs can
cause injury, necrosis and
sloughing of tissues.
• Depot preparations cannot be given
by i.v. route.
Precautions - Drug injected slowly and before injecting, make sure that the tip of the
needle is in the vein.
3. Transdermal Route
 The drug is administered in the form of a patch or ointment that delivers the drug into
the circulation for systemic effect .
 For example, scopolamine patch for sialorrhoea and motion sickness, nitroglycerin
patch/ointment for angina, oestrogen patch for hormone replacement therapy (HRT).
Advantages
• Self-administration is possible
• Prolonged duration of action
• Minimize systemic side effects
• Provide a constant plasma
concentration of the drug
• Patient compliance is better
Disadvantages
• Expensive
• Local irritation may cause
itching and dermatitis
• Patch may fall-off unnoticed
• Drug must be lipophilic in
nature
Absorption Pattern, Advantages and Disadvantages of the Most
Common Routes of Administration
Route of
Administration
Absorption Pattern Advantages Disadvantages
Oral Variable; affected by
many factors
• Safest, economic and most
common route
• Food may affect
absorption
•Drug may be
metabolized before
systemic absorption
Intravenous Absorption not required •Suitable for irritating
substances and complex
mixtures
•Dosage titration
permissible
•Ideal for high molecular
weight proteins and peptide
drugs
•Unsuitable for oily
substances
• Bolus injection may
result in adverse effects
•Strict aseptic
techniques needed
Subcutaneous • Depends on drug
diluents:
Aqueous solution:
prompt
Depot preparations:
slow and sustained
• Suitable for slow-release
drugs
•Ideal for some poorly
soluble suspensions
• Pain or necrosis if
drug is irritating
•Unsuitable for drugs
administered in large
volumes
Route of
Administration
Absorption Pattern Advantages Disadvantages
Intramuscular •Depends on drug
diluents:
Aqueous solution:
prompt
Depot preparations:
slow and sustained
•Suitable for oily vehicles
and certain irritating
substances
• Preferable to intravenous
if patient must self administer
•Affects certain lab
tests (creatine kinase)
•Can cause
intramuscular
hemorrhage
(precluded during
anticoagulation
therapy)
Transdermal
(Patch)
Slow and sustained •Ideal for drugs that are
lipophilic and have poor oral
bioavailability
•Ideal for drugs that are
quickly eliminated from the
body
• May cause delayed
delivery of drug
to pharmacological site
of action
•Limited to drugs
that can be taken in
small daily doses
Rectal Erratic and variable • Bypasses destruction by
stomach acid
•Ideal if drug causes
vomiting
•Ideal in patients who are
vomiting, or comatose
• Drugs may irritate the
rectal mucosa
•Not a well-accepted
route
Route of
Administration
Absorption Pattern Advantages Disadvantages
Inhalation Systemic absorption
may occur; this is not
always desirable
• Ideal for gases
• Effective for patients with
respiratory problems
•Localized effect to target
lungs: lower doses used
compared to that with oral
or parenteral administration
•Most addictive
route (drug can enter
the brain quickly)
•Patient may have
difficulty regulating
dose
Sublingual Depends on the drug:
Few drugs (example,
nitroglycerin) have
rapid, direct
systemic absorption
Most drugs erratically
or incompletely
absorbed
•Bypasses destruction by
stomach acid
•Drug stability
maintained because the pH
of saliva relatively neutral
•May cause immediate
pharmacological
effects
•Limited to drugs that
can be taken in small
doses
•May lose part of the
drug dose if
swallowed
Route of
Administration
Dosage Form
Oral Solution, Syrups. Suspensions, Emulsions, Gels, Powders,
Granules, Capsules, Tablets
Parenteral Injections (solutions, suspensions, Emusions forms)
implants, irrigation & dialysis solutions
Topical Ointment, Creams, Pastes, Lotions, Gels, Topical Aerosols,
Transdermal patches
Rectal Suppositories, Ointments, Creams, Powders, Solutions
Respiratory Aerosol (solustions suspensions, emulsions, powders
forms) inhalations, sprays, gases
Nasal Solutions, inhalations
Ear Solutions, Suspensions, ointments, creams
Eye Solutions, ointments, creams
ROA

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ROA

  • 1. Routes of Drug Administration Sreenu Thalla Clinical Pharmacologist
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  • 9. Systemic Routes  Drugs administered by this route enter blood and produce systemic effects.  Medication, nutrition or other substances into the circulatory system so that the entire body is affected.  It classify 2 broad categories like Enteral (oral, sublingual, and rectal) and Parenteral (inhalation, injection, transdermal) routes.
  • 10. 1. Oral Route  It is the most common and acceptable route for drug administration. Dosage forms are tablet, capsule, syrup, mixture, etc., e.g., paracetamol tablet for fever, omeprazole capsule for peptic ulcer are given orally. Advantages Safer Cheaper Painless Disadvantages • Not suitable for emergency as onset of action of orally administered drugs is slow • It is not suitable for/in: • Unpalatable and highly irritant drugs • Unabsorbable drugs (e.g. aminoglycosides) • Drugs that are destroyed by digestive juices (e.g. insulin) • Drugs with extensive first-pass metabolism (e.g. lignocaine) • Unconscious patients • Uncooperative and unreliable patients • Patients with severe vomiting and diarrhoea Convenient for repeated and prolonged use Can be self- administered
  • 11. 2. Sublingual/Buccal Route  The preparation is kept under the tongue.  The drug is absorbed through the buccal mucous membrane and enters the systemic circulation directly  Eg. nitroglycerin for acute anginal attack and buprenorphine for myocardial infarction. Advantages Quick onset of action. Action can be terminated by spitting out the tablet. Bypasses first-pass metabolism Self-administration is possible. Disadvantages It is not suitable for: Irritant and lipid-insoluble drugs. Drugs with bad smell and taste.
  • 12. 3. Rectal Route  Drugs can be given in the form of solid or liquid. a. Suppository: It can be used for local (topical) effect as well as systemic effect, e.g. indomethacin for rheumatoid arthritis. b. Enema: Retention enema can be used for local effect as well as systemic effect. The drug is absorbed through rectal mucous membrane and produces systemic effect, e.g. diazepam for status epilepticus in children. • Useful in the patient is having recurrent vomiting or unconscious stage. • Potential of long term drug absorption with various intrauterine devices (IUDs). • Some irritant and unpleasant drugs can be introduced into rectum as suppositories. Advantages • This is rather inconvenient and embarrassing. • Absorption is slower, irregular and unpredictable. • Bleeding problems such as discomfort to real pathologies. Disadvantages
  • 13. Parenteral Routes  Routes of administration other than enteral route are called parenteral routes. • Onset of action of drugs is faster; hence it is suitable for emergency. • Useful in: Unconscious, Uncooperative and unreliable patients. • It is suitable for: Irritant drugs, Drugs with high first-pass metabolism, Drugs not absorbed orally, Drugs destroyed by digestive juices. Advantages • Preparations should be sterile and is expensive. • Requires invasive techniques that are painful. • Cannot be usually self-administered. • Can cause local tissue injury to nerves, vessels etc. • Require aseptic conditions. Disadvantages
  • 14. 1. Inhalation • Quick onset of action. • Dose required is very less, so systemic toxicity is minimized. • Amount of drug administered can be regulated. Drugs which are gaseous (e.g., nitrous oxide) or readily vaporized (e.g., isoflurane) may be inhaled.  Solid drugs may also be given by inhalation route in the form of aerosols or suspended powder (e.g., salbutamol and beclomethasone). The inhalation route may be used for producing both local (e.g., bronchodilatation in asthma) as well as systemic effects (anesthesia). Advantages Disadvantages • Local irritation may cause increased respiratory secretions and bronchospasm. Advancements Nebulizer Metered Dose Inhaler (MDI) Powder Inhaler (DPI)
  • 15. 2. Injections Injectable Routes of DrugAdministration
  • 16.  The drug is injected into the layers of the skin, e.g. Bacillus Calmette–Guerin (BCG) vaccination and drug sensitivity tests. It is painful and only a small amount of the drug can be administered.  Intradermal injectionalso known as the mantoux method. Purpose : Injects medication below the epidermis drugs are absorbed slowly. Typically used for diagnosis of tuberculosis and allergens. a. Intradermal Route Methods of Intradermal Injections Normal Size Needle Shorter Needle Without Needle
  • 17. b. Subcutaneous Route (s.c.)  The drug is injected into the subcutaneous tissues of the thigh, abdomen and arm, e.g. adrenaline, insulin, etc.  Only small amount can be injected S.C self injection is possible because deep penetration in not needed Advantages • Self-administration is possible (e.g. insulin). • Depot preparations can be inserted into the subcutaneous tissue, e.g. norplant for contraception. Disadvantages • It is suitable only for nonirritant drugs. • Drug absorption is slow; hence it is not suitable for emergency.
  • 18. Advancement in Subcutaneous Route Dermojet • A high velocity jet of drug solution is projected from a microfineorifice using a gun like implement. • The solution passes through the superficial layers and gets deposited in the subcutaneous tissue. 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. 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. • Examples - for hormones and contraceptives (e.g. NoRPLANT).
  • 19. c. Intramuscular Route (I.M.)  Drugs are injected into large muscles such as deltoid, gluteus maximus, e.g. paracetamol, diclofenac, etc.  A volume of 5–10 mL can be given at a time. Advantages Disadvantages • Absorption is more rapid as compared to oral route. • Mild irritants, depot injections, soluble substances and suspensions can be given by this route. • Aseptic conditions are needed. • Intramuscular injections are painful and may cause abscess. • Self-administration is not possible. • There may be injury to the nerves.
  • 20. d. Intravenous Route (i.v.)  Injection into a peripheral vein over 1 to 2 minutes (bolus) or longer as an infusion.  Drugs are injected directly into the blood stream through a vein. Drugs are administered as: 1. Bolus: Single, relatively large dose of a drug injected rapidly or slowly as a single unit into a vein. For example, i.v. ranitidine in bleeding peptic ulcer. 2. Intravenous infusion: For example, dopamine infusion in cardiogenic shock; mannitol infusion in cerebral oedema; fluids infused intravenously in dehydration. 3. Slow intravenous injection: For example, i.v. morphine in myocardial infarction.
  • 21. Advantages • Bioavailability is 100%. • Quick onset of action; therefore, it is the route of choice in emergency. • Large volume of fluid can be administered, e.g. intravenous fluids in patients with severe dehydration. • Highly irritant drugs, e.g. anticancer drugs can be given because they get diluted in blood. • Hypertonic solution can be infused by intravenous route, e.g. 20% mannitol in cerebral oedema. Disadvantages • Local irritation may cause phlebitis. • Self-medication is not possible. • Once the drug is injected, its action cannot be halted. • Strict aseptic conditions are needed. • Extravasation of some drugs can cause injury, necrosis and sloughing of tissues. • Depot preparations cannot be given by i.v. route. Precautions - Drug injected slowly and before injecting, make sure that the tip of the needle is in the vein.
  • 22. 3. Transdermal Route  The drug is administered in the form of a patch or ointment that delivers the drug into the circulation for systemic effect .  For example, scopolamine patch for sialorrhoea and motion sickness, nitroglycerin patch/ointment for angina, oestrogen patch for hormone replacement therapy (HRT).
  • 23. Advantages • Self-administration is possible • Prolonged duration of action • Minimize systemic side effects • Provide a constant plasma concentration of the drug • Patient compliance is better Disadvantages • Expensive • Local irritation may cause itching and dermatitis • Patch may fall-off unnoticed • Drug must be lipophilic in nature
  • 24. Absorption Pattern, Advantages and Disadvantages of the Most Common Routes of Administration Route of Administration Absorption Pattern Advantages Disadvantages Oral Variable; affected by many factors • Safest, economic and most common route • Food may affect absorption •Drug may be metabolized before systemic absorption Intravenous Absorption not required •Suitable for irritating substances and complex mixtures •Dosage titration permissible •Ideal for high molecular weight proteins and peptide drugs •Unsuitable for oily substances • Bolus injection may result in adverse effects •Strict aseptic techniques needed Subcutaneous • Depends on drug diluents: Aqueous solution: prompt Depot preparations: slow and sustained • Suitable for slow-release drugs •Ideal for some poorly soluble suspensions • Pain or necrosis if drug is irritating •Unsuitable for drugs administered in large volumes
  • 25. Route of Administration Absorption Pattern Advantages Disadvantages Intramuscular •Depends on drug diluents: Aqueous solution: prompt Depot preparations: slow and sustained •Suitable for oily vehicles and certain irritating substances • Preferable to intravenous if patient must self administer •Affects certain lab tests (creatine kinase) •Can cause intramuscular hemorrhage (precluded during anticoagulation therapy) Transdermal (Patch) Slow and sustained •Ideal for drugs that are lipophilic and have poor oral bioavailability •Ideal for drugs that are quickly eliminated from the body • May cause delayed delivery of drug to pharmacological site of action •Limited to drugs that can be taken in small daily doses Rectal Erratic and variable • Bypasses destruction by stomach acid •Ideal if drug causes vomiting •Ideal in patients who are vomiting, or comatose • Drugs may irritate the rectal mucosa •Not a well-accepted route
  • 26. Route of Administration Absorption Pattern Advantages Disadvantages Inhalation Systemic absorption may occur; this is not always desirable • Ideal for gases • Effective for patients with respiratory problems •Localized effect to target lungs: lower doses used compared to that with oral or parenteral administration •Most addictive route (drug can enter the brain quickly) •Patient may have difficulty regulating dose Sublingual Depends on the drug: Few drugs (example, nitroglycerin) have rapid, direct systemic absorption Most drugs erratically or incompletely absorbed •Bypasses destruction by stomach acid •Drug stability maintained because the pH of saliva relatively neutral •May cause immediate pharmacological effects •Limited to drugs that can be taken in small doses •May lose part of the drug dose if swallowed
  • 27. Route of Administration Dosage Form Oral Solution, Syrups. Suspensions, Emulsions, Gels, Powders, Granules, Capsules, Tablets Parenteral Injections (solutions, suspensions, Emusions forms) implants, irrigation & dialysis solutions Topical Ointment, Creams, Pastes, Lotions, Gels, Topical Aerosols, Transdermal patches Rectal Suppositories, Ointments, Creams, Powders, Solutions Respiratory Aerosol (solustions suspensions, emulsions, powders forms) inhalations, sprays, gases Nasal Solutions, inhalations Ear Solutions, Suspensions, ointments, creams Eye Solutions, ointments, creams