ROUTES OF DRUG ADMINISTRATION

Pharmacology Study Notes

1. OVERVIEW & CLASSIFICATION

Route of administration determines:
• Onset of action
• Duration of effect
• Bioavailability
• First-pass metabolism
• Patient compliance

CLASSIFICATION:
A. Enteral Routes: Oral, Sublingual, Buccal, Rectal
B. Parenteral Routes: IV, IM, SC, ID, Inhalation
C. Topical Routes: Skin, Eye, Nasal, Vaginal

2. ENTERAL ROUTES
A. ORAL (PO) - Per Os
ADVANTAGES DISADVANTAGES

• Most convenient & acceptable • Slow onset (30-60 min)

• Safe (can reverse with emesis/lavage) • Variable absorption

• Economic • First-pass metabolism

• No sterility required • Cannot use in vomiting/unconscious

• Self-administration possible • Drug-food interactions

• No trained personnel needed • Cannot use for irritant drugs

Clinical Examples:
• Tablets/Capsules: Paracetamol, Aspirin, Antibiotics
• Liquids: Cough syrups, Antacids
• Modified release: Sustained/Controlled release forms

B. SUBLINGUAL (SL)
ADVANTAGES DISADVANTAGES

• Rapid onset (1-3 min) • Limited drug volume

• Avoids first-pass metabolism • Requires patient cooperation

 • Good vascularity • Bitter taste of some drugs

• Can be spat out if toxic • Cannot eat/drink/smoke

• Convenient for emergencies • Limited to lipophilic drugs

Examples: Nitroglycerin, Nifedipine, Buprenorphine

C. BUCCAL
• Similar to sublingual but drug placed between cheek and gum
• Longer contact time than sublingual
• Examples: Miconazole oral gel, Testosterone

D. RECTAL (PR)
ADVANTAGES DISADVANTAGES

• Useful when oral route unavailable • Unpredictable absorption

• Partial avoidance of first-pass • Patient discomfort

• Local + systemic effects • Cultural/social objections

• Useful in unconscious patients • Defecation expels drug

• Good for pediatric use • Cannot use in diarrhea/rectal disease

Examples: Diclofenac suppositories, Paracetamol, Metronidazole

3. PARENTERAL ROUTES
A. INTRAVENOUS (IV)
ADVANTAGES DISADVANTAGES

• Immediate onset • Risk of embolism/thrombosis

• 100% bioavailability • Infection risk

• Precise control of blood levels • Cannot be reversed

• Can give large volumes • Extravasation injury

• Useful in emergencies • Requires trained personnel

• Can give irritant drugs • More expensive

Types:
• IV bolus: Single rapid injection
• IV infusion: Continuous administration
Examples: Antibiotics, Cardiac drugs, Emergency medications

B. INTRAMUSCULAR (IM)
ADVANTAGES DISADVANTAGES
 • Faster than oral (10-30 min) • Pain at injection site

• Can give depot preparations • Risk of nerve damage

• Good absorption • Cannot be reversed

• Can give oily vehicles • Risk of hematoma

• Relatively safe • Requires training

• Good for uncooperative patients • Contraindicated in bleeding disorders

Sites: Deltoid, Gluteus, Vastus lateralis

Examples: Vaccines, Antibiotics, Haloperidol decanoate

C. SUBCUTANEOUS (SC)
ADVANTAGES DISADVANTAGES

• Self-administration possible • Slower absorption than IM

• Sustained absorption • Limited volume (max 2 mL)

• Less painful than IM • Local irritation possible

• Good for protein drugs • Cannot use in shock/dehydration

• Depot preparations possible • Contraindicated in bleeding disorders

Examples: Insulin, Heparin, Growth hormone, Vaccines

D. INTRADERMAL (ID)
• Very small volume (0.1-0.2 mL)
• Mainly for diagnostic tests and vaccines
• Examples: TB skin test, Allergy testing, BCG vaccine
4. INHALATION ROUTE
ADVANTAGES DISADVANTAGES

• Rapid onset for systemic effects • Requires patient coordination

• Large surface area for absorption • Unpredictable dose delivery

• Non-invasive • Device dependency

• Direct access to respiratory tract • Risk of respiratory irritation

• Avoids first-pass metabolism • Cannot use in severe airway obstruction

Types:
• MDI (Metered Dose Inhaler): Salbutamol, Beclomethasone
• DPI (Dry Powder Inhaler): Formoterol
• Nebulizers: For severe asthma/COPD
• General anesthesia: Halothane, Sevoflurane

5. TOPICAL ROUTES
A. DERMAL/TRANSDERMAL
ADVANTAGES DISADVANTAGES

• Non-invasive • Slow absorption

• Sustained release possible • Limited to potent drugs

• Avoids first-pass metabolism • Skin irritation/sensitization

• Patient convenience • Individual variation in absorption

• Can be removed if needed • Cannot use on broken skin

Examples:
• Topical: Antifungals, Corticosteroids, Antibiotics
• Transdermal patches: Nitroglycerin, Nicotine, Fentanyl

B. OTHER TOPICAL ROUTES

Ocular (Eye):
• Local effect: Antiglaucoma drugs, Anti-infectives
• Advantages: Direct access, lower systemic exposure
• Disadvantages: Rapid washout by tears, poor penetration
Intranasal:
• Rapid absorption due to rich blood supply
• Examples: Sumatriptan, Desmopressin, Decongestants
• Advantage: Direct CNS access for some drugs
Intravaginal:
• Local effects: Antifungals, Hormones
• Examples: Clotrimazole, Metronidazole
6. SPECIALIZED ROUTES
Route Indication Examples
Intrathecal CNS infections, Spinal anesthesia Antibiotics, Bupivacaine

Intraosseous Emergency vascular access Fluids, Emergency drugs

Intraperitoneal Peritoneal dialysis, Cancer therapy Dialysis fluid, Chemotherapy

Intra-articular Joint diseases Corticosteroids, Hyaluronic acid

Intracardiac Cardiac arrest (rarely used) Epinephrine

Epidural Labor analgesia, Surgery Local anesthetics, Opioids

7. FACTORS AFFECTING ROUTE SELECTION

Patient Factors Drug Factors Clinical Factors

• Age (pediatric/geriatric) • Physical/Chemical properties • Urgency of treatment

• Consciousness level • Stability in different pH • Duration of therapy

• Compliance • First-pass metabolism • Local vs systemic effect

• Disease state • Bioavailability • Monitoring requirements

• Ability to swallow • Formulation availability • Cost considerations

• Vascular access • Dose frequency needed • Healthcare setting

8. QUICK COMPARISON - ONSET & BIOAVAILABILITY

Route Onset Bioavailability First-Pass Duration

IV Immediate 100% No Short-medium

Inhalation Rapid (1-2 min) Variable No Short-medium

Sublingual Rapid (1-3 min) 75-90% Minimal Short

IM Fast (10-30 min) 75-100% No Medium-long

SC Moderate (20-60 min) 75-90% No Long

Oral Slow (30-120 min) 5-100% Yes Medium-long

Rectal Variable (30-90 min) Variable Partial Medium-long

Transdermal Very slow (hours) 80-90% No Very long

9. HIGH-YIELD EXAM POINTS

• Sublingual nitroglycerin: Rapid onset, avoids first-pass metabolism
 • IV route: 100% bioavailability, immediate onset, cannot be reversed
• First-pass metabolism: Avoided by IV, IM, SC, sublingual, rectal (partial), inhalation
• Rectal route: Good for pediatrics, unconscious patients, when oral route unavailable
• Transdermal patches: Sustained release, non-invasive, good compliance
• IM injections: Never give in gluteal region in children <2 years (sciatic nerve risk)
• Sublingual: Cannot eat/drink/smoke during administration
• IV extravasation: Can cause tissue necrosis with vesicant drugs
• Protein drugs: Usually given SC/IM/IV (destroyed orally by enzymes)
• Emergency drugs: IV preferred for immediate effect
• Insulin: SC route standard, IV in emergencies (DKA)
• Vaccines: IM (most), ID (BCG), oral (polio, rotavirus)
• Bioequivalence: Different routes of same drug are NOT bioequivalent
• Volume limits: ID (0.1-0.2 mL), SC (max 2 mL), IM (max 5 mL)

10. ABSOLUTE CONTRAINDICATIONS

• Oral: Unconscious, severe vomiting, bowel obstruction
• IV: Thrombophlebitis at injection site, extravasation risk for vesicants
• IM/SC: Bleeding disorders, anticoagulation, shock/poor perfusion
• Rectal: Severe diarrhea, rectal trauma/surgery, neutropenia
• Inhalation: Severe airway obstruction, inability to coordinate breathing
• Topical: Hypersensitivity to drug/vehicle, broken skin (for some drugs)