PHARMACOLOGY

SECTION 5
2nd year Medical Students

2026 Practical
YAS 208 & 210
 Routes of Administration&Dosage forms
Routes of drug Administration:

Enteral Others(Not enteral)

-Buccal -Oral -Rectal -Parenteral -Inhalation -Topical

Enteral route (Oral administration) (Solid and liquid):

Solid Dosage Forms:

Tablet Capsules Powders Effervescent

- Simple -Hard gelatin - Packets - Packets
- Sugar coated - Soft gelatin - Bulk - Bulk
- Enteric coated -Enteric coated
- Sustained release -Sustained release

Tablets
Solid dosage form of varying shape, size & weight in which the drug is
compressed with inert substance (excipients).
Tablets:
Simple

Sugar Coated
-Mask bad taste.
-Improve appearance
-Protest against air & light
Enteric Coated

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- -1 - -Remain intact in the stomach
- But dissolved in the intestine
- Protect the stomach
Sustained Release Tablets
Controlled-release (CR) – Sustained –release (SR) = Slow –release = Extended –
release = Retard= Timed – release
Capsules

Powders

 Effervescent granules
 By adding NaHCO3 & Citric or tartaric acid.
 When added to water release CO2 & improve palatability.

Liquid Dosage Forms:

Aqueous Alcoholic
 Solution & Mixture.  Elixir
 Syrup.
 Suspension.
 Tincture
 Emulsion.
 Decoction.
 Infusion.

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 Sublingual Dosage Forms:
 Sublingual pellets (Linguets): small tablets to be placed under tongue to
reach directly to systemic circulation (e.g., nitroglycerine).
 Sublingual tablets should be:
o Small in size.
o Have good taste.
o Easily dissolved.

Oro-Disperesible Tablets/Films:

 ODTs/ODFs release drug in mouth for absorption through local oro-mucosal

tissues & through pregastric (e.g., oral cavity, pharynx, and esophagus), gastric
(i.e., stomach) & postagastric (e.g., small and large intestines) segments of GIT.
 They are particularly useful for pediatric and geriatric patient populations with
special needs such as dysphagia, Parkinson's disease, and oral cancer.

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 Rectal Dosage Forms

Drugs are absorbed through rectal mucosa to reach systemic circulation.

One of two forms:
Suppository:
 Solid at room temperature melt at body temperature.
 The base usually employed for it is either cocoa butter or gelatin.
Enema:
Fluid administered into the rectum & colon.

Evacuant (cleaning Retention enema

enema)
Aim Evacuate the colon from A mean of giving the drug (the
faeces. drug retained in the rectum).
Examples Treatment of constipation Prednisolone in treatment of
Pre-Operative preparation Ulcerative colitis.
of bowel
Before colonoscopy
Method Large volume (1 liter). Small volume (1/4 liter)
Rapid flow at high head Slow flow at low head position.
position. - Non irritant.
- Mild irritant

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 Advantages & disadvantages of Enteral Routes

Oral Sublingual Rectal

Convenient -Rapid action. 1-Mostly Bypass 1st metabolism by
-Safe, -Easy administration. GIT& Liver enzymes
-Easy, -Bypass 1st pass 2-Suitable for: a-Patients:
Advantages

-Economic metabolism -Unconscious

-Can control the dose -Uncooperative (children)
by spitting out the -Vomiting
tablets. b-Drugs:
-Moderately irritant.
-Large volume.
-Unpalatable.

Oral Sublingual Rectal

Not suitable for: -Inconvenient -Rectal inflammation up to

a-Patients: if frequent. anal polypi.
-Unconscious -Excessive - Unreliable absorption
Disadvantages

-Uncooperative salivation especially if the rectum is

-Excessive vomiting or diarrhea Which induce full of feces.
b-Emergencies swallowing.
c-Drugs:
-Drugs could be destroyed by digestive
enzymes or by gastric acidity
-Drugs could be affected by
-Drugs could be destroyed through first-
pass metabolism (e.g., lidocaine)
-Some drugs are not absorbed from GIT
if systemic action in intended (e.g.,
streptomycin).

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 Non-Enteral Dosage Forms
Inhalation route
Target:
1-Local effect:
a. Upper air ways: e.g. steam inhalation with Eucalyptus oil (soothing effect) in
laryngitis.
b. Lower air ways: as bronchodilators in bronchial asthma.
2-Systemic effect:
- The lung is a good site for absorption.
Examples:
a. Oxygen therapy.
b. Inhalation anesthesia.

Dosage forms:
1-Gas: as oxygen, nitrous oxide (inhalation anesthetic).
2- Vapor of a volatile liquid as halothane (inhalation anesthetic).
3- Aerosol:
- Fine liquid particles suspended in air.
- Aerosol is delivered by:
1- Nebulizer or
2- Atomizer (Metered dose Inhaler, MDI)
3- Powder: A finely divided drug powder inhaled A finely divided drug powder
inhaled by deep inspiration with the aid of a dry powder inhaler.
4- Hot steam inhalation.
Dosage forms:
1-Gas: as oxygen, nitrous oxide (inhalation anesthetic).
2- Vapor of a volatile liquid as halothane (inhalation anesthetic).

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3-Aerosol:
- Fine liquid particles suspended in Air. – Aerosol is delivered by :
a- Nebulizer.

b. Atomizer (Metered Dose Inhaler, MDI) ‫بخاخة‬

4-Powder: -A finely divided drug powder inhaled by deep inspiration with the aid of a
dry powder inhaler.
Capsules:

Ready filled

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5-Hot steam inhalation

Advantages of Inhalation :
Excellent & Rapid absorptions, due to:
- Large surface area.
- Rich blood supply of the alveoli.
- Thin porous membrane.
Disadvantages of Inhalation:
- Inaccurate dosing.
- Drug may irritate pulmonary epithelium.

Topical Routes
Desired Effect
Systemic : * Transdermal delivery system
Local: * On different sites.
Topical Administration
Systemic Effect
Advantages:
 Prolonged duration.
 Minimal fluctuation.
 Avoidance of hepatic first pass elimination
Examples:
1- Nitroglycerin: ointment or patch.
2- Fentanyl skin patch

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 Topical administration (Local Effect)
1-Ointment:
 An ointment is an opaque or translucent, viscous, greasy (often)
semisolid preparation applied to the skin or mucous membranes.
 Ointments are anhydrous (containing no water).
 Occlusive bases are best for dry skin lesions and favor drug absorption.

2-Cream:
 A cream is an opaque, viscous, somewhat greasy, semisolid
preparation applied to the skin or mucous membranes.
 Creams are emulsions of oil and water (contain water).
 Non-occlusive bases are best for acute exudative lesions and can be used in nearly any area,
even for intertriginous areas (groin, axilla, infra-mammary fold).

3-Lotion:
 An aqueous liquid preparation applied to skin or mucous membranes
by pouring (without rubbing) or with the aid of cotton pad.
 For example: calamine lotion (anti-pruritic).
 Most suitable for application in hairy regions such as the scalp because of its low viscosity.
 It can economically cover a wide area of skin.

4-Dusting powder:
 Powders absorb moisture and decrease friction.
 More useful than creams in moist or macerated intertriginous areas.
 Examples: talc powder (lubricant), boric acid powder (antiseptic).
Topical dosage forms according to organs
Eye:
1- Eye drops. 2-Eye ointment 3-Eye lotion
Ear
1- Ear drops
2- Ear ointmen

Topical administration local effect

Nose:
1- Nasal drops.
2- Nasal spray.
3- Nasal inhaler (e.g., Vicks nasal inhaler as decongestant)

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Mouth
1- Mouth wash.
2- Mouth gargle.
3- Lozenge.
4- Paint.
5- Paste.
Vagina:
1- Vaginal tablet.
2- Vaginal suppositories, also referred as ovules or pessaires.
3- Vaginal cream.
4- Vaginal douche.
Parenteral Routes

Dosage Forms

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 Inhalation Route

Topical Route

QUIZ 1
 The advantage of this route  Mention this route of
is (enumerate 2). administration & the
 One of the disadvantages dosage form.
of this route..  An advantage of this
 This route is preferred in route is…
…patients.  Enumerate two drugs
 Mention 4 Dosage forms of administered by this
drugs that can be given by route.
inhalation.

 Regarding this route ? Could it result in systemic side effects?

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mechanism and example - 11 -
 Dosage form  Ampoule
Route  IM
Site  Gluteal, (upper lateral quadrant)
 Vastus,
 Deltoid.
 Rectus femoris.
Advantages  OILY Prep
 Rapid onset
Disadvantages  Pain
 Hematoma-Abcess
Precautions  Aspitrate before injection

A A-Syringe
B-Cannula
Route  IV
Site Adult
 Veins hand, Foream.
 Ex jugular
Infant:
 Scalp, umbilicus
Advantages  Bypass 1st pass
 100% bioavailability.
 ER (best route in emergencies)
 Immediate onset of action
 Irritant (can be used for irritant drugs)
 Large vol
B Disadvantages Local
I.V. Pyrogens  Thrombophelibitis
Anaphylaxis  Pain, inflame
Systemic
 Allergic reaction
 Velocity reactions as aminophylline
arrhythmias, hypotension

 Pyrogenic Disease
 No retreat once the drug is injected.
Types of IV  IV Bolus
 Slow IV Injection
 IV. Infusion

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 Pharmacokinetic Calculations
In what ways does the diagram below resemble a patient?

How can we….

1. Calculate the loading dose, knowing the Vd and the target plasma concentration?
 The loading dose
It is the dose which can raise the conc. of drug in plasma to a desired, target
concentration.

Loading dose = Vd x C C = desired conc.

Loading dose is used if we need to reach a desired concentration very rapidly as in an

emergency situation.
Q1- We need to give digoxin to a patient with heart failure and atrial fibrillation. The desired target
concentration is 1.5g/L, and Vd of digoxin =500L. What is the required IV loading dose?
….………………………………………………………………………….
.What is the required IV loading dose?
a) 0.5 mg
b) 0.75mg
c) 1.0 mg
d) 1.5mg

Q2- How can we calculate the volume of distribution, by knowing the drug concentration and
the administered dose?
….………………………………………………………………………….
The plasma concentration of theophylline after a simple IV dose of 300mg was 9mg/liter.
Calculate the volume of distribution (Vd):
a) 15 liters.
b) 45 liters
c) 33 liters
d) 90 liters
Remember the digoxin example…How can you explain a digoxin VD of 500L??

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Apparent volume of distribution:
Hypothetical volume at which the drug should be distributed to attain the estimated plasma
concentration of the drugs.

Plasma conc. = dose(mg)/Vd

i.e.
Vd = dose(mg)/plasma conc.:
Dose(mg) = plasma conc X Vd.
A drug given as 200mg single dose, results in a peak plasma concentration of 0.04 mg/ml.
The apparent volume of distribution (Vd) is:
a. 3liters.
b. 4 liters.
c. 5 liters
d. 7 liters.
Exercice Vd applications:
 The expected initial plasma concentration of gentamicin after injecting it IV in a dose of 80mg to a
60kg female, knowing that the Vd of gentamicin is 0.25 L/kg.
….………………………………………………………………………….
 Now, how to…………..
Calculate maintenance dose, from the clearance and the desired plasma concentration.
Maintenance dose
It is the dose needed to replace the drug eliminated since the preceding dose so maintain steady
state.

Maintenance dose = Cl X Css. X dose interval (Tm)

Infusion rate = clearance X Css

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Exercise on Clearance and maintenance:
 Consider that you need to infuse a drug to maintain a concentration of 2 mg/L.
 The drug is exclusively cleared by the kidney as the patient's estimated Clcr is 100mL/min.
We know that the drug is neither secreted nor reabsorbed by the renal tubules.
….………………………………………………………………………….
It is desired to maintain a plasma concentration of 0.15 g/L of carbenicillin in a patient. Plasma
clearance equals 8.82 L/hour. Calculate the infusion rate:
N.S. a 36-year-old, 60kg woman, is to be given an anticonvulsant agent. Calculate a daily dose that
will produce an average Steady State plasma concentration of around 6 mg/L.
 Bioavailability is 100%.
 Maintenance dose = [(Cl)(CSS ave) (Tau)]/
o Cl: 0.065 L/kg/hr.
Clearance
Volume of body fluid from which drug is removed in unit time (L/h)

Clearance = Kel x Vd
Kel = elimination rate constant/hr
So, what does Kel stand for?
 Remember when we said regarding "First Order Kinetics" that
A fixed Percentage of drug is eliminated per unit time
That fixed percentage is in fact called: Kel "The Elimination Rate Constant"
 A drug has a volume of distribution (Vd) of 49 liters, Kel = 0.23l/hour calculate the clearance:
a. 1.32 L/hour.
b. 3.32 L/hour.
c. 11.32 L/hour.
d. 1.0 L/hour
 How to Determine the elimination rate constant?
By knowing the Vd and the clearance.
 The clearance and volume of distribution of tobramycin are 4.8 L/h and 40 L, respectively.

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 What is the Elimination Rate Constant?
Clearance = K x Vd K
or  el= elimination rate constant/hr
So………  (K el)= constant/t1/2
Kel = Clearance (in L/hr)/Vd (in L)  (K el) = 0.693/t1/2

The clearance and volume of distribution of tobramycin are 4.8 L/h and 40 L, respectively.
What is the Elimination Rate Constant?
a. 0.32 / hr
b. 0.52 / hr
c. 0.12 /hr
d. 0.74 /hr
How to ……….
Calculate the t1/2 based on the elimination rate constant
Elimination rate constant (K el)

The rate constant of elimination per hour.

Elimination rate  1/t1/2
What is the t1/2 of a drug where the elimination rate constant (Kel) is 0.11 hr-1?
a) 6 hours.
b) 2 hours
c) One hour
d) 10 hours

Plasma half life of a drug (t1/2): Drug concentration in plasma

Def: Time needed for the drug concentration in the plasma to be reduced by one half.
Plasma half life (t1/2)
Time needed for the drug concentration in
The plasma to be reduced by one half (50%)


Half – life (t1/2) is important to indicate the time required to attain steady state.

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 A patient on digoxin therapy has developed digitalis toxicity. The plasma digoxin level
was 4ng/ml. How long should you stop digoxin in order to reach a therapeutic level of 1
ng/ml. t1/2 for digoxin in this patient is 1.6 days.
a. 2.4 days
b. 3.2 days
c. 4.8 days
d. 6.4 days

 The half-life of a drug is about 36 hours. How long will it take for blood levels of the drug
to reach a steady concentration (plateau)? A normal volunteer will receive a new drug in a
phase 1 clinical trial. The clearance and volume of distribution are 1.386 L/h and 80 L
respectively. Calculate the t1/2 of the drug in this person.
a.83 h b. 77h c.58 h d. 40 h

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