1. Pharmacokinetics is the study of how the body affects a drug after administration through absorption, distribution, metabolism, and excretion. Pharmacodynamics is the study of how drugs act on the body through their receptors. 2. Drugs are absorbed, distributed to tissues, metabolized mainly in the liver, and excreted from the body primarily through urine or bile. Many factors influence these processes. 3. The goal of drug therapy is to achieve effects at the site of action while avoiding toxicity. Understanding pharmacokinetics and pharmacodynamics principles allows for safer and more effective use of medications.

1. DRUG METABOLISM:
PHARMACOLOGY, PHARMACOKINETICS, ANDPHARMACODYNAMICS
DRUGANDFOODINTERACTION
Poltekkes Kemenkes Pangkalpinang
Emmy Kardinasari, S.Si., M.Sc.

3. What is a drug?
•A chemical substance, especially one prescribed by
a medical provider, that is used in the diagnosis,
treatment, or prevention of a condition or disease.
•All of the active chemical substances that can
be produced from biological source of synthetic
• Drug is produced to cure diseases.
•Drug must e used under medical professionals.
•Many drugs are being illegally used

4. Pharmachology (Farmakologi)
• Pharmachology is a branch of medicine that deals with the
interaction of drugs with the systems and processes of living
animals, in particular, the mechanisms of drug action as well
as the therapeutic and other uses of the drug.
• Pharmacon (drug) and logos (Science or knowledge).
• Farmakologi berasal dari kata pharmacon (obat) dan logos (ilmu
pengetahuan). Farmakologi didefinisikan sebagai ilmu yang mempelajari
obat dan cara kerjanya pada sistem biologis. Farmakognosi adalah ilmu
yang mempelajari tentang interaksi obat, sistemnya, dan proses yang
terjadi di dalam tubuh organisme. Dalam farmakologi juga dipelajari
tentang mekanisme dan efek pengobatan.

5. Farmakologi

6. •Medication
•To achieve systemic
counter to disease
•To cure disease
•To control
biochemical
parameter in the
body
The purpose of consuming drugs or medicine?

7. The Methods of Drugs Consumption

8. The Methods of Drugs Consumption (1)

9. The Methods of Drugs Consumption (2)

10. The Working System of Drugs
This is an overview of how drugs work at the molecular level and how this complex system is
influenced by genetic factors, developmental changes, disease processes, and the
environment.

11. Pharmaceuticals: Dissolving the Drug in
The Body

12. •PHARMACOKINETICS: pharmacokinetics studying the
effect the organism has on the drug.
•PHARMACODYNAMICS: pharmacodynamics studying
the action of the drug on the organism
THE PROCESS OF DRUG METABOLISM

13. PHARMACOKINETICS
Pharmacokinetics → pharmacokinetics studying the effect
the organism has on the drug. Think of pharmacokinetics as a
drug’s journey through the body, during which it passes
through four different phases: absorption, distribution,
metabolism, and excretion (ADME).
The four steps are:
• Absorption: Describes how the drug moves from the site of
administration to the site of action.
• Distribution: Describes the journey of the drug through the
bloodstream to various tissues of the body.
• Metabolism: Describes the process that breaks down the
drug.
• Excretion: Describes the removal of the drug from the body.

15. 1. ABSORBSI
→ Describes how the drug moves from the site of
administration to the site of action.
• Pergerakan partikel-partikel obat dari saluran gastrointestinal ke dalam
cairan tubuh melalui absorpsi pasif, absorpsi aktif, atau pinositosis.
• Kebanyakan obat oral diabsorpsi di usus halus melalui kerja permukaan
vili mukosa yang luas. Jika sebagian dari vili ini berkurang, karena
pengangkatan sebagian dari usus halus, maka absorpsi juga berkurang.

17. • Absorption is the movement of a drug from its site of administration to
the bloodstream. The rate and extent of drug absorption depend on
multiple factors, such as:
• Route of administration
• The formulation and chemical properties of a drug
• Drug-food interactions
• The administration (e.g., oral, intravenous, inhalation) of a drug
influences bioavailability, the fraction of the active form of a drug that
enters the bloodstream and successfully reaches its target site.
• Intravenous drug doesn’t require absorption and bioavailability is 100%
because the active form of the medicine is delivered immediately to the
systemic circulation. However, orally administered medications have
incomplete absorption and result in less drug delivery to the site of
action.

18. → Penyerapan obat dapat melalui beberapa jalan sesuai
dengan pemakaiannya antara lain melalui saluran cerna,
selaput lendir, rektum, dan jaringan bwh kulit.
→ Setelah obat mencapai pembuluh darah, obat akan
didistribusikan (diedarkan) ke seluruh tubuh melalui sirkulasi
darah.

19. 2. DISTRIBUTION
• Describes the journey of the drug through the bloodstream to
various tissues of the body.
• The process of drug distribution is important because it can affect how
much drug ends up in the active sites, and thus drug efficacy and
toxicity.
• A drug will move from the absorption site to tissues around the body,
such as brain tissue, fat, and muscle.
• Many factors could influence this, such as blood flow, lipophilicity,
molecular size, and how the drug interacts with the components of
blood, like plasma proteins.
• Example:
• a drug like warfarin is highly protein-bound, which means only a small
percentage of the drug is free in the bloodstream to exert its therapeutic effects

21. 3. METABOLISM
• Drug metabolism is a crucial aspect of medical practice and
pharmacology.
• Most drugs undergo chemical alteration by various bodily systems to
create compounds that are more easily excreted from the body.
• These chemical alterations occur primarily in the liver and are known as
biotransformations.
• Biotransformations occur by mechanisms categorized as either:
• Phase I (modification)
• Phase II (conjugation)
• Phase III (additional modification and excretion.)
• Biotransformasi (metabolisme), yaitu proses perubahan struktur kimia obat dalam
tubuh terutama di organ hati (dalam jumlah yang sangat rendah terjadi di usus, ginjal,
paru-paru, limpa atau dalam darah) yang dikatalisis oleh enzim.

22. Phase of Drug Metabolism
The metabolism of xenobiotics is often divided into three phases:
modification, conjugation, and excretion. These reactions act in concert to detoxify
xenobiotics and remove them from cells.

23. The Phases of Drug Metabolism
Phase 1:
Phase I modifications alter the chemical structure of the drug, usually
by oxidation, reduction, hydrolysis, cyclization/decyclization, and the
removal of hydrogen or the addition of oxygen. In some instances, this
process will change an inactive prodrug into a metabolically active
drug.
Phase 2:
Phase II modifications involve reactions that couple the drug molecule
with another molecule in a process called conjugation. Conjugation
usually renders the compound pharmacologically inert and water-
soluble, so that the compound can easily be excreted. Mechanisms of
conjugation include methylation, acetylation, sulphation,
glucuronidation, and glycine or glutathione conjugation. These
processes can occur in the liver, kidney, lungs, intestines, and other
organ systems.

24. Cytochrome P450 (CYP450) enzymes are responsible for the biotransformation
or metabolism of about 70-80% of all drugs in clinical use.

25. What are some factors that affect drug metabolism?
• Genetics can impact whether someone metabolizes drugs more
quickly or slowly.
• Age can impact liver function; the elderly have reduced liver function
and may metabolize drugs more slowly, increasing risk of
intolerability, and newborns or infants have immature liver function
and may require special dosing considerations.
• Drug interactions can lead to decreased drug metabolism by enzyme
inhibition or increased drug metabolism by enzyme induction.
• Food drug interaction can affect the rate of pharmacokinetics of
drugs.

26. The Biotransformation

27. 4. Excretion
• Elimination involves both the metabolism and the excretion of the drug
through the kidneys, and to a much smaller degree, into the bile.
• Excretion into the urine through the kidneys is one of the most important
mechanisms of drug removal.
Many factors affect excretion, such as:
• Direct renal dysfunction, which could prolong the half-life of certain drugs
and necessitate dose adjustments.
• Age, which can contribute to differing rates of excretion and impact dosing of
medications.
• Pathologies that impact renal blood flow, such as congestive heart failure
and liver disease can make drug excretion less efficient
• Whether it’s a patient who just had gastric bypass surgery, a CYP2D6 poor
metabolizer, or a patient with renal dysfunction, an individual’s
characteristics affect these four processes, which can ultimately influence
medication selection.

28. 4. Excretion
→ Rute utama dari eliminasi obat adalah melalui ginjal, rute-rute
lain meliputi empedu, feses, paru-paru, saliva, keringat, dan air
susu ibu. Obat bebas, yang tidak berikatan, yang larut dalam air,
dan obat-obat yang tidak diubah, difiltrasi oleh ginjal. Obat-obat
yang berikatan dengan protein tidak dapat difiltrasi oleh ginjal.
Sekali obat dilepaskan ikatannya dengan protein, maka obat
menjadi bebas dan akhirnya akan diekskresikan melalui cairan lain.
→ Obat dan metabolitnya diekresikan (dikeluarkan) dari tubuh
melalui berbagai organ eksresi, obat atau metabolit yang
larut dalam air diekskresikan lebih cepat dari pada obat
kurang larut dalam air. Kecuali pada obat atau metabolit
yang diekresikan melalui paru-paru.
→ Ginjal merupakan organ ekskres yang penting. Ekskresi
juga dpt melalui feses, air mata, air susu, dan rambut ttp dlm
jumah yg relatif sedikit

30. Farmakodinamika

31. Farmakodinamika → the study of an effect and action of
drug’s at molecular, biochemical, and physiologic levels.
Process:
→ Drugs bind the cell’s receptors to allow access at the
targeted action site in the cells.
→ The binding at the receptor will cause the change in
biochemical and physiology system in the cells.

32. • Farmakodinamik mempelajari efek
obat terhadap fisiologi dan biokimia
selular dan mekanisme kerja obat.
Respons obat dapat menyebabkan
efek fisiologis primer atau sekunder
atau kedua-duanya.
• Efek primer adalah efek yang
diinginkan, dan efek sekunder
mungkin diinginkan atau tidak
diinginkan.
• Contoh: Difenhidramin (Benadryl),
suatu antihistamin.
• Efek primer dari difenhidramin adalah
untuk mengatasi gejala-gejala alergi,
dan efek sekundernya adalah
penekanan susunan saraf pusat yang
menyebabkan rasa kantuk.
• Efek sekunder ini tidak diinginkan jika
sedang mengendarai mobil, tetapi
pada saat tidur, dapat menjadi
diinginkan karena menimbulkan sedasi
ringan.
Farmakodinamika

33. This shows the types of drugs effect of receptor proteins and its actions in
the targeted cells.

34. Target of Drug
Action

35. Target of Drug
Action

36. Why Pharmacodynamics is important?
These studies help determine the dose or dose range of a drug that is
needed to achieve a meaningful response without causing severe adverse
effects.
Wrong dosage can subsequently lead to many negative effects including:
• Acute CNS Abnormalities (e.g., confusion, coma, seizures)
• Acute CV Conditions (e.g., prolonged QT, vital sign changes)
• Cell Mutations & Cancer
• Chronic Conditions (e.g., neuropathy, pulmonary fibrosis, metabolic
syndrome)
• Death
• End-Organ Damage (e.g., kidney, liver)

37. What affects pharmacodynamics?
• Age
• Sex
• Body weight or body surface area
• Pregnancy
• Kidney and liver function
• Drug interactions
• Smoking

38. TERIMA KASIH 