25/05/2015

INTRODUCTION
TO
PHARMACOLOGY
Department of Pharmacology
Medical School Unsoed

LEARNING OBJECTIVE
Students should be able to:

Name the major pharmacology sub- sub-discipline

Identify, with examples, the major sources of
drugs

Give examples of drugs discovered

Discuss issues relating to the naming of drugs
and the complications that can arise from
naming inconsistencies

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What is Pharmacology?

discipline It is the study
Pharmacology is a scientific discipline
of the effects of chemical agents of therapeutic value
(drugs) or potential toxicity on biological systems, i.e.
what do drugs do and how do they do it.

It relates to other major bioscience disciplines such as
physiology, biochemistry, cellular and molecular
biology, microbiology, immunology, genetics, and
pathology.

Why Do We Study Pharmacology?

A competent doctor must understand why his/her patient is

getting a medication, and HOW IT WORKS

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Pharmacology sub-
sub-disciplines

Pharmacodynamics: study of the molecular, biochemical, and
physiological effects of drugs on cellular / body systems and
their mechanisms of action

Pharmacokinetics: study of the (fate) absorption, distribution,
and excretion of drugs

Pharmacogenomics: The study of genetic influences on the
effectiveness and fate of drugs

Toxicology: the study of the adverse or toxic effects of drugs and
other chemical agents Therapeutics

Pharmacoeconomics

Pharmacoepidemiology

What are the goals of Pharmacology?

To understand all
aspects of drug action
and efficacy to BENEFIT
Benefits
develop
drugs/treatment
regimes that have
selective (beneficial)
actions without
adverse effects (i.e. RISK
Risk
they don’t make
things worse).

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What is a drug?

A drug is a chemical/substance that is usually
used to treat a disease/condition

When administered appropriately causes a range
of physiological and biochemical /molecular
changes in a complex biological system that
relate to its composition, structure and target

When is a drug not a drug?

Drugs sold/marketed for the treatment of disease must
have regulatory approval (e.g. FDA) and have gone
through extensive evaluation procedures

Food supplements may contain substances that alleviate
various conditions (potential drugs) but have not been
properly validated and approved for clinical use

Food supplements must not make claims about
therapeutic properties - only drugs can be sold on that
basis

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Where do drugs come from?

Plants

Human--derived proteins/steroids
Human

Fungi/bacteria

Synthetic chemicals

Recombinant proteins

Drugs From the Natural World

121 prescription drugs in use today for cancer
treatment - 90 are derived from plant species. ~74% of
these were discovered by investigating a folklore claim.

Recent example - taxol

1981--2002: 48 of 65 approved cancer drugs were
1981
natural products, based on natural products or
mimicked natural products in some way

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Where do drugs come from?

1. Extracts from plants and herbs

Opium poppy:

Dried juice from seeds yields morphine, a natural opiate

Physicians only effective drug of choice early 1900s

Powerful painkiller and inducer of euphoria (and constipation)

Foxglove leaves contain digitalis (digoxin):

Reversible inhibitor of Na/K ATPase

Widely used to treat congestive heart failure

At high doses it can be letha

Where do drugs come from?

2. From the body itself

Hormones

Insulin, used to treat diabetes

Thyroxine, for treatment of thyroid insufficiency

Growth hormone, for treatment of short stature

NB: Most hormonal drugs are now produced by

recombinant DNA technology (if they are proteins)

or by chemical synthesis (e.g. steroids, peptides)

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Where do drugs come from?

3. From micro-
micro-organisms
(fungi, bacteria)

Antibiotics

Penicillin - prototypic b-
b-lactam
antibiotic, discovered by
Alexander Fleming in 1928 as a
product of penicillium notatum (a
mold growing in his lab)

Interferes with bacterial cell wall
synthesis

Where do drugs come from?

4. Chemical modification of the body's own

hormones/chemical regulators Hormonal drugs

Ethinyl estradiol - readily adsorbed form of oestrogen

Prednisolone - synthetic steroid with glucocorticoid-
glucocorticoid-like actions

Anti--cancer drugs
Anti

6-mercaptopurine and 6-
6-thioguanine – modified base components of
DNA/RNA - interfere with RNA synthes

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Where do drugs come from?

5. Chemical synthesis of novel compounds
with desirable properties

Indomethacin, celecoxib - COX inhibitors
(NSAIDS)

Cimetidine - Histamine receptor modulator

Simvastatin - HMG-
HMG-CoA reductase inhibitor

Sulfonylureas - ATP-
ATP-sensitive K+ channel
modulators

And many, many more……………………….

Not Always an Exact Science…

Many drugs were discovered by chance:

Antidepressants

Some monoamine oxidase inhibitors and tricyclic
antidepressants

Discovered during failed attempts to develop treatments for
tuberculosis and pre-
pre-anaesthetic agents, respectively.

Cisplatin

Platinum-containing drug used to treat a number of
Platinum-
cancers

Discovered while investigating the effects of electrical
fields on bacterial cell growth.

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Drug Exploration, Identification &

Validation

Pharmaceutical companies now invest heavily in
identifying new drugs and getting them
approved for sale.

Very active drug discovery programmes,testing
hundreds of thousands of compounds

Average cost of finding and marketing a new
drug = ~$US800 m

Drug Names

The generic name is related to the structure/

composition/source of the drug. This is the
preferred name for general use.

The brand name is the drug company's
marketing name for the drug, e.g.

paracetamol vs. Pamol/Panadol

aspirin vs. Dispirin

sildenafil vs. Viagra

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Generic Names

Generic names often have similar sounding

endings that give some insight into the
class/type of drug.

Selective COX-
COX-2 inhibitors:

celecoxib, rofecoxib, etoricoxib, valdecoxib

Naming Complications

Brand names can change over time as patents expire or

Pharmaceutical Companies merge etc

Most drugs are marketed by numerous names in
different countries

e.g. Panadol [UK] = Tylenol [USA])

Even generic names can differ in different countries

e.g. paracetamol [UK] = acetaminophen [US]

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Brand names for PREDNISONE:

Apo-Prednisone; Adasone; Cartancyl; Colisone; Cordrol;
Apo-
Cortan; Cortancyl; Dacortin; Dacorten; Decortin;
Decortisyl; Delcortin; Dellacort; Dellacort A; Delta-
Delta-Dome;
Deltacortene; Deltacortone; Deltasone; Deltison; Deltisona;
Di-
Di-Adreson; DiAdreson; Econosone; Encorton; Fernisone;
Hostacortin; Liquid Pred; Me-
Me-Korti; Meticorten; Nisona;
Novoprednisone; Orasone; Origen Prednisone; Panafcort;
Panasol; Paracort; Parmenison; Pehacort; Predeltin;
Prednicen--M; Prednicorm; Prednicort; Prednicot; Prednidib;
Prednicen
Predniment; Prednitone; Rectodelt; Sone; Sterapred;
Ultracorten; Winpred.

DRUGS NAME

Obat jadi  Obat murni atau campuran dalam sediaan
baku dengan nama teknis sesuai farmakope indonesia
atau buku-
buku-buku lain yang ditetapkan

Obat baru  obat dengan zat aktif atau adtitif yang
belum dikenal,
dikenal, belum masuk dalam farmakope dan atau
belum digunakan secara resmi

Obat paten  obat jadi dengan nama dagang dan
kemasan pabrik yang memproduksi

Obat standar  obat dengan formula yang tercantum
standar
dalam literatur standar/
standar/resmi

Obat asli  obat yang langsung didapat dari bahan
alam,, diolah secara sederhana berdasarkan pengalaman
alam
untuk pengobatan tradisional

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DRUGS CLASIFICATION

Obat Narkotika

Obat Keras

Obat Bebas Terbatas

Obat Bebas

NARKOTIKA
(UU 22 TH 1997)

Golongan I

Hanya untuk kepentingan Ilmu Pengetahuan

Pengawasan ketat oleh Menkes

Co : Kokain, Heroin, Canabis sativa (marihuana).

Golongan II

Untuk kepentingan ilmu pengetahuan dan pelayanan kesehatan

Distribusi diatur pemerintah

Co : Morfin dan garamnya, petidin

Golongan III

Untuk kepentingan ilmu pengetahuan dan pelayanan kesehatan

Distribusi diatur pemerintah

Co : Kodein

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OBAT KERAS

Obat Keras (OK)

Obat Keras Tertentu (OKT)

Obat Wajib Apotek (OWA)

OBAT KERAS

Semua obat yang diperoleh harus dengan resep
dokter

Tanda bulatan : garis lingkaran dan huruf K warna
hitam dengan dasar warna merah

K

Semua obat dengan parenteral

Antibiotik, hormon

Semua obat baru

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OBAT KERAS TERTENTU

Psikotropika  semua obat yang berkhasat
SSP
psikoaktif melalui pengaruhnya terhadap SSP
menyebabkan perubahan mental dan perilaku

Psikotropika

Potensi adiksi

Potensi toleransi

OKT Lanj.
PSIKOTROP KETERANGAN
Gol 1  Hanya untuk ilmu pengetahuan, not used for therapy
 Potensi adiksi sangat kuat
 Co : Brolamfetamin, LSD

Gol 2  berkhasiat terapi dapat untuk ilmu pengetahuan dan terapi

 Potensi adiksi kuat
 Co : Amfetamin, sekobarbital

Gol 3  berkhasiat terapi cukup banyak untuk ilmu pengetahuan dan

terapi
 Potensi adiksi sedang

 Co : Amobarbital, fentobarbital

Gol 4  Berkhasiat terapi  banyak dan luas digunakan untuk ilmu

pengetahuan dan terapi
 Potensi adiksi ringan

 Co : Diazepam, klordiazepoksid, nitrazepam, meprobamat

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OBAT WAJIB APOTEK

Obat keras yang dapat diserahkan tanpa resep dokter

Tujuan

Meningkatkan kemampuan masy menolong sendiri

Meningkatkan kekmampuan self therapy secara tepat, aman dan rasional

Contoh

Obat saluran cerna

Obat Kulit

Obat anti TBC

Obat sitim muskuloskeletal

Obat saluran nafas

Obat mata dan telinga

OBAT BEBAS TERBATAS

Obat keras yang diberi batas takaran dan kemasan

Digunakan untuk pengobatan ringan yang dikenali oleh penderita

Tanpa resep dokter

Tanda lingkaran 

Tanda Peringatan  dasar hitam dan tulisan putih

P1 awas obat keras, baca aturan pemakaiannya
P1

P2 awas obat keras, hy untuk kumur, jangan ditelan
P2

P3 awas obat keras, Hanya untuk bagian luar badan
P3

P4 awas obat keras, hanya untuk dibakar
P4

P5 awas obat keras, tidak boleh ditelan
P5

P6 awas obat keras, obat wasir, jangan ditelan
P6

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OBAT BEBAS

Dapat dibeli tanpa resep dokter

Tanda lingkaran 

Aman

Cara pemakaian mudah

How Do We Study
Pharmacology?

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General Concepts
Drug Dose
Administration

Disintegration
Pharmaceutical of Drug

Pharmacokinetics Absorption/distribution
metabolism/excretion

Pharmacodynamics Drug/Receptor
Interaction

Pharmacotherapeutics Drug Effect

or Response

How are Drugs

Administered?

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Routes of Drug Delivery

Parenteral Inhaled
(IV)
Oral

Transdermal
Parenteral
Topical (SC, IM)

Rectal

We Will Discus More Within PK-

PK-PD
of The Drugs ...

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