Basic

Pharmacology
Dr. Amir El-gendy
Lecturer of Pharmacology & Toxicology
Faculty of Pharmacy
Delta University

Lecture 2
 Routes of Drug Administration
The route of administration is
determined by:
1. The properties of the drug
(water or lipid solubility,
ionization, etc.).
2. The therapeutic objectives
(for example, the desirability
of a rapid onset of action or
the need for long-term
administration or restriction
to a local site).

Basic Pharmacology 1
 1) Enteral route
A- Oral route (swallowed)
Advantages
✓ It is the simplest and most common means of administering
drugs.
✓ Convenient (Easily self-administered).
✓ Cheap.
✓ Limit the number of systemic infections that could complicate
treatment.
✓ Toxicities or overdose by the oral route may be overcome with
activated charcoal or gastric lavage or by emesis (easy recall)
Basic Pharmacology 2
 A- Oral route (swallowed)
Disadvantages
X The drug is exposed to harsh G.I. environments (as acidity of
stomach, alkalinity of intestine, presence of food, motility or
enzymes) that may decrease its absorption.
X Most drugs absorbed from GIT enter portal circulation to
liver before they are distributed into the general circulation
(fist pass metabolism) ➔ drugs extensively metabolized
before entering systemic circulation ➔  efficacy of many
oral drugs ( bioavailability) so, they should be given in high
dose or change the route of administration.
➢ Examples: 90% of nitroglycerin is cleared by 1st pass
metabolism ➔ so, taken sublingual and testosterone is 80%.
Basic Pharmacology 3
Basic Pharmacology 4
 A- Oral route (swallowed)
Disadvantages

X Ingestion of drugs with food or with other drugs, can

interfere with absorption.
X Presence of food in the stomach delays gastric emptying ➔
so drugs that are destroyed by acid become unavailable for
absorption.
X Oral route is not suitable for certain conditions as
unconscious patients (comatosed), vomiting or emergency.

Basic Pharmacology 5
B- Sublingual route (under tongue)
Advantages Disadvantages

✓ Rapid absorption (the drug enters

X Limited to certain types
systemic circulation directly due
of drugs (unsuitable for
to high vascularity under the
irritant & bitter taste
tongue) ➔ rapid onset.
✓ Convenience. drugs).
✓ Low incidence of infection. X Limited to drugs that can
✓ Avoidance of the harsh GI be taken in small doses.
environment. X May lose part of the
✓ Avoidance of first-pass drug dose if swallowed
metabolism (suitable for
nitroglycerine).

Basic Pharmacology 6
C- Buccal route
The same as sublingual route but the drug is absorbed
through the buccal mucosa.

Basic Pharmacology 7
D- Rectal route
Advantages Disadvantages

✓ 50% - 70% of drainage of rectal

X Rectal absorption is often
region bypass portal circulation
irregular and incomplete.
(bypass 1st pass).
X Many drugs irritate the
✓ Like sublingual, no destruction by
intestinal enzymes or acidity
rectal mucosa.
(escape GI harsh). X If the drug is
✓ Commonly used to administer ulcerogenic→ taken
antiemetic agents. rectally → it will cause
✓ Suitable in patients with vomiting ulcer.
or unconscious. X Not useful in diarrhea.

Basic Pharmacology 8
Basic Pharmacology 9
 2) Parenteral routes (injection)
Advantages Disadvantages

✓ Used for drugs that are poorly absorbed

from GIT (e.g. heparin) and For agents X Irreversible.
unstable in GIT (e.g. insulin).
(difficult recall).
✓ Treatment of unconscious patients that
X Pain and fear.
require a rapid onset of action.
X High incidence of
✓ The highest bioavailability.
infection.
✓ The drug is not subjected to first-pass
metabolism or harsh GI environments.
✓ Provide the most control over the actual
dose of drug delivered to the body.

Basic Pharmacology 10
A- Intravenous (I.V)
Advantages

✓ Rapid effect and a maximal degree of control over the circulating

levels of the drug.
✓ Used for drugs that are not absorbed orally and there is no other
choice (e.g. rocuronium which is neuromuscular blocker).
✓ The drug avoids GIT & first-pass metabolism by the liver.
✓ Injection of large volume.
✓ Valuable in emergency.
✓ Suitable for irritant and painful drugs (the substance is rapidly
diluted by the blood).

Basic Pharmacology 11
A- Intravenous (I.V)
Disadvantages
X No recall by emesis or activated charcoal (only hemodialysis can be
done for the free drug and not suitable with drugs that strongly
bind with plasma proteins or have high volume of distribution).
X May introduce bacteria (infection) through contamination at the
site of injection → requires aseptic conditions.
X May induce hemolysis or shock by the too-rapid delivery of high
conc. of drug to the plasma → so, the rate of infusion must be
controlled.
X Restricted to aqueous drugs, not for suspension or emulsions
(may cause embolism).
X Needs skills and assistance.

Basic Pharmacology 12
Basic Pharmacology 13
B- Intra-arterial

The same as I.V. but used to deliver the drug directly to

the organ of concern to decrease side effects.
Examples: Antitumor drugs

Basic Pharmacology 14
C-Intramuscular (I.M)
Advantages Disadvantages

✓ Drugs can be aqueous solutions

or specialized depot preparations
(suspension or emulsion).
X Maximum volume for
✓ E.g. sustained-release haloperidol
decanoate which slowly diffuses injection is 10 ml.
from muscle and produces an X Not rapid as I.V.
extended neuroleptic effect X Painful.
(antipsychotic) and depot
medroxyprogesterone
(contraceptive injection every 3
months)

Basic Pharmacology 15
D-Subcutaneous (S.C)
Advantages Disadvantages
X Limited volume
X should not be used with
✓ Self administration.
drugs that cause tissue
✓ Examples: for drugs injected
irritation, because severe
S.C: (insulin & heparin)
pain and necrosis may occur
X Not rapid as I.V or I.M

➢ Minute amounts of epinephrine (vasoconstrictor) are combined with the

local anesthetic Lidocaine or procaine → limitation of the local anesthesia
to site of administration (↑ action), ↑duration and ↓systemic side effects
of the local anesthetic.
➢ S.C. Implantation of Solids: such as contraceptive rod (etonogestrel) and
also insulin pumps that can be implanted in diabetic patients.
Basic Pharmacology 16
Basic Pharmacology 17
 3) Other routes of administration

Basic Pharmacology 18
A) Inhalation
Advantages

✓ Rapid delivery of a drug across large surface area of mucous

membranes of respiratory tract (almost rapid effect as I.V)
✓ Escapes 1st-pass metabolism.
✓ Used for drugs that are gases (some anesthetics) or those that
can be dispersed in an aerosol.
✓ Effective and convenient for patients with respiratory complaints
(asthma, or chronic obstructive pulmonary disease) because the
drug is delivered directly to the site of action and systemic side
effects are minimized (e.g. albuterol, and corticosteroids such as
fluticasone).
✓ Considered a route of administration as well as a route of
excretion.
Basic Pharmacology 19
A) Inhalation
Disadvantages
X Most addictive route, (drug can enter the brain quickly).
X Patient may have difficulty regulating dose.
X Some patients may have difficulty using inhalers.

Basic Pharmacology 20
B) Intranasal
✓ Nasal decongestants → e.g. xylometazoline
✓ Desmopressin (synthetic vasopressin (ADH) ) → treatment of
diabetes insipidus.
✓ Salmon calcitonin (hormone) as nasal spray → treatment of
osteoporosis.
✓ The abused drug (cocaine) → taken by intranasal sniffing.

Basic Pharmacology 21
C) Intrathecal

➢ Injection between vertebrae

into spinal cord (in
subarachnoid space) to
introduce drugs directly into
CSF in case of the inability
of the drug to cross BBB.
✓ Example: intrathecal injection
of the antifungal
“amphotericin B” (doesn’t
cross BBB) in treating
cryptococcal meningitis

Basic Pharmacology 22
D) Topical examples

✓ Clotrimazole is applied as a cream directly to skin in ttt of

dermatophytosis.
✓ Tropicamide or cyclopentolate are instilled (drop by drop) into eye to
dilate the pupil.

Basic Pharmacology 23
E) Transdermal

➢ Systemic effects by application of drugs to the skin, usually via a

transdermal patch.
➢ Rate of absorption can vary, depending on the physical characteristics
of the skin at the site of application as well as the lipid solubility of the
drug.
➢ This route is most often used for the sustained delivery of drugs
✓ Antianginal drug: nitroglycerin patch.
✓ Antiemetic drug: scopolamine (hyoscine) patch
✓ Once-a-week contraceptive patch.
✓ Nicotine transdermal patches: used to facilitate smoking cessation.

Basic Pharmacology 24
 “Everything is theoretically impossible,
until it is DONE.”

Physiology – Lecture 2 25