PHARMACOLOGICAL

PROPERTIES OF
DRUG
Dra. Yanti Mariana
Pharmacological Properties of Drug

Block System

Clini
c
 PHARMACOLOGICAL
PROPERTIES
1. Mechanism of action
2. Effect
3. Adverse Drug Reaction = side
effects
4. Indication
5. Contraindication
6. Pharmacokinetics
7. Dosage Regimen
 Drug
Pharmacokineti
cs
Mechanism of
Dosage Action
regimen

Main Side effect

effect

Indication Contraindicati
on
Learning Objective
1. Describe the pharmacological
properties - Acetaminophen
- Bronchodilator drug

2. Describe the pharmacological

properties
- Amoxicillin
3. Describe the role of PP in rational
use of drug
ACETAMINOPHEN

Class Nonopioid analgesic and antipyretic

- Its analgesic & antipyretic effects do not differ
significantly from those of aspirin
- has no significant antiinflammatory or anti-
uricosuric activity
MECHANISM OF ACTION
- a weak inhibitor of cycloxygenase in the presence
of peroxide found in inflammatory lesions
- antipyretic effect :
inhibit cyclooxygenase (COX) enzyme in the brain
- does not inhibit neutrophil activation (as other
NSAIDS)
 Mechanism of action of Acetosal ( Aspirin )
stimulus

Disturbance of cell membrane (phospholipid)

Arachidonic acid

5 HETE cyclooxygenase

PG-G2

PGI2 PG-F2 TX-A2 PGE2

Vasodilation Bronchocontriction Platelet Vasodilation

Pain senzitation Uterine contraction Agregation Pain senzitation

Gastric cytoprotection Broncho- Fever

Inhib. of platelet constriction Gastric secretion

aggregation Uterine
contraction
 Fever/hyperpyrexia
stimulus Vasodilation
inflammation
Pain
 EFFECT OF ACETAMINOPHEN
1. Antipyretic
2. Analgesic
3. Antiinflammatory (high
dose)
INDICATION
1. Hyperpyrexia
2. Mild to moderate pain
3. Substitute for aspirin in
peptic ulcer, hemophillia
patient or patient using
anticoagulant, uricosuric
drug or at risk for Reyes
syndrome
SIDE EFFECT, ADR
- In recommended therapeutic dosage
usually well-tolerated
- Skin rash (erytheme, urticaria)
- Drug fever
- Mucosal lesion
- Neutropenia, thrombocytopenia,
pancytopenia (in very few cases)

TOXIC EFFECTS
Hepatotoxicity
Adult : after single dose of 10-15 g
(150 t0 250 mg/kg BW)
CONTRAINDICATION
- Hepatic insufficiency
- Renal insufficiency
- Pregnancy
- Hypersensitive patient
PHARMACOKINETICS

A : Rapidly & almost completely

Route onset peak duration

Oral 15-30 min 30 - 60 2-6 h

D : - throughout most body fluid

- protein binding 20 50 %

M : t : + 2 hours

E : 90 100% recovered in the urine

 DOSAGE REGIMEN
Preparation : tablet / syrup / drops
Adult : 500 mg 3-4 times daily
Children : 250-500 mg 3-4 times daily
Infant : 0.6 1.2 ml 3-4 times daily
Frequency of its administration
Timing of its administration
Duration of treatment
 Which is the appropriate
preparation for these
following condition ?

Fever
Arthralgia
 PHATOGENESIS OF BRONCHIAL
ASTHMA

Precipitating factors
Bronchodilator
drugs

Contraction of bronchial
muscle

Mediators Inflammation
Mucus secretion
 BRONCHODILATOR DRUG
I. ADRENERGIC AGONIST
ADRENALIN (EPHINEPRIN), EPHEDRIN
ISOPROTERENOL
ALBUTEROL (SALBUTAMOL)

II. XANTIN
THEOPHYLIN

III. MUSCARINIC ANTAGONIST

IPRATROPIUM BROMIDA
 ADRENALIN
Class : symphatomimetic
adrenergic agonist
MECHANISM OF ACTION
Adrenalin will interact with all adrenergic
receptor (adrenoceptor)
adrenalin

1 2 1 2

Contraction relaxation
contraction
Distribution of adrenoceptor
adrenoceptor

1 2 1 2

Bronchus
Vascular
heart
Uterine
Gland
glucose
V. urinaria
level
eye
EFFECT OF ADRENOCEPTOR AGONIST
1 : vasoconstriction peripheral
resistance BP

1 : heart contraction CO BP
heart rate tachycardia

2 : bronchocontriction Bronchodilation
uterine relaxation
glucose level
 EFFECT OF ADRENOCEPTOR AGONIST
 EFFECT OF ADRENALIN

What is the therapeutic effect ?

What are the side effects ?
What is the indication ?

What are the

contraindication ?
 Anaphylactic Shock
Drug

Histamine vasodilation

BP
INDICATION
acute bronchial asthma
others : Anaphylactic shock
CONTRAINDICATION :
1. Hypertension
2. Tachyarrhythmia
3. Ischemic heart disease
4. Hyperthyroidism
5. Prostatic Hypertrophy
 ISOPROTERENOL

Isoproterenol bind to 1 and 2

adrenoceptor

What are the side effects of

isoproterenol ?
What are the contraindication ?
 SALBUTAMO
L

Salbutamol bind to 2 adrenoceptor

What are the side effects of salbutamol ?

What are the contraindication ?

 Which is the appropriate drug for
:

B A with hypertension
B A with DM
B A with prostatic hypertrophy
B A with CAD
 Drug
Pharmacokineti
cs
Mechanism of
Dosage Action
regimen

Spectrum Side effect

activity

Indication Contraindicati
on
 AMOXICILLIN

Class : Amoxicillin is classified as Penicillin

group
Penicillin

Penicillin G Nafcillin Ampicillin

Carbenicilin
Penicillin V Cloxacillin Amoxicillin Ticarcillin
 MECHANISM OF ACTION
All the penicillin inhibit bacterial growth by interfering
with a specific step in bacterial cell wall synthesis
Amoxicillin

PBP

BLOCK OF SYNTHESIS PEPTIDOGLICAN

Autolicyn

Lysis of bacteria

Penicillin group is bactericidal only if cells are actively

growing and synthesizing cell wall
SELECTION OF TOXICITY OF
AMOXICILIN : HIGH
 SPECTRUM ACTIVITY
Amoxicilin is broad (extended) spectrum AM
Gram (+) coccus : streptococcus pneumonia
Gram (+) coccus : L. Monocytogenes
Gram (-) enteric : E. Coli
Proteus mirabilis
Salmonella typhi
Gram (-) bacillin : H. Influenza
INDICATION : Infection of sensitive
microbial
 ADVERSE DRUG
REACTION
1. Hypersensitivity
reaction :
- skin rashes
- angioedema
- anaphylaxis
shock

skin rashes
 angioedem
a

2. Nausea, vomiting, GI upset, diarrhea

3. Super infection
oral and rectal candidiasis
 DOSAGE REGIMEN

Dosage of the drug:

The frequency of its administration
The timing of its administration
The duration of treatment