DRUGS

Question 1

Are low molecular weight chemical substances that interact with macromolecular targets in the body to produce effect.

Answer 1

DRUGS

Question 2

what the drug does to the body

Answer 2

pharmacodynamics

Question 3

• Body’s own natural chemicals
• within
  ➢ Ex. Neurotransmitters, hormones, autacoids

Answer 3

endogenous compounds

Question 4

• Foreign substances such as drugs (Xenobiotics)
• outside

Answer 4

exogenous compounds

Question 5

drug is powerful and selective ; select this part when designing a drug

Answer 5

therapeutic

Question 6

drug is less powerful.

Answer 6

subtherapeutic

Question 7

drugs is less selective

Answer 7

toxic

Question 8

what the body does to the drug

Answer 8

pharmacokinetics

k - katawan

Question 9

GOAL: Design a drug that will interact as powerfully and selectively as possible for the target

Answer 9

pharmacodynamics

Question 10

GOAL: Design a drug so that it is capable of reaching that target

Answer 10

pharmacokinetics

Question 11

Dictates the fate or destiny of the drug (ADME)
Absorption
Distribution
Metabolism
Excretion

Answer 11

pharmacokinetics

Question 12

• also called Liberation
• extract and get the API away from excipient and dissolve (drug in aqueous solution) – pre-requisite for drug absorption.

Answer 12

Drug Release

Question 13

process of drug entry into the systemic circulation ; wherein the drug in the GI tract will now proceed to the bloodstream

Answer 13

Absorption

Question 14

main site for absorption

Answer 14

small intestine

Question 15

main site of metabolism

Answer 15

liver

Question 16

drug will be distributed to different organs and tissues (possess proteins and nucleic acids)

Answer 16

Distribution

Question 17

composed of processes metabolism (chemical reaction that makes the drug inactive) and excretion (functional loss of the drug from the body)

Answer 17

Elimination

Question 18

organ responsible for excretion

Answer 18

kidney

Question 19

the most common mechanism controlling drug release.

Answer 19

Diffusion

Question 20

• Extract API from dosage form and done via dissolution process— aqueous solution.
• When the conventional dosage forms are administered orally or topically, the active drug in the dosage form is immediately released and absorbed into the systemic circulation.

Answer 20

Liberation

Question 21

➢ Most complicated route due to numerous barriers
➢ GIT
➢ The most common and popular route

Answer 21

Oral administration

Question 22

tasks of organs that could transmit the drug to enter the blood.

Answer 22

absorption environment

Question 23

ABSORPTION ENVIRONMENT

❖ both have acidic and basic environment.
❖ pH 1.5-2 fed state (more production and release of hydrochloric acids)
❖ pH 2-6 fasting state

Answer 23

STOMACH

Question 24

ph level of fed state in stomach

Answer 24

1.5 - 2

Question 25

ph level of **fasting state** in stomach

Answer 25

2 - 6

Question 26

# **ABSORPTION ENVIRONMENT** ❖ **main site** of absorption ❖ **basic** environment ❖ anatomical feature is **high surface area** because of the **presence** of **villi** and **microvilli**. ❖ **greater perfusion**

Answer 26

small intestine

Question 27

Drug is **absorbed** if it is

Answer 27

LUNA **Lipophilic** (**cell membrane** is **lipophilic**; like dissolves like) **Unionized** **Non**-polar

Question 28

Drug is **excreted** if it is

Answer 28

HIPE **Hydrophilic** **Ionized** **Polar**

Question 29

Drugs are weak ____

Answer 29

electrolytes weak acids weak bases

Question 30

acid + acid basic + basic

Answer 30

unionized, absorbed

Question 31

acid + basic basic + acid

Answer 31

ionized, excreted

Question 32

# **TRUE OR FALSE** A weakly **basic** drug is **absorbed** in the small intestine because it **exists** in its **lipophilic**, **unionized**, and **polar** formed

Answer 32

FALSE - non polar

Question 33

➢ **Less complication** ➢ **Direct** to Systemic Circulation ➢ **Rapidly** distributed ➢ **IV**, **IM**, **SC**, **Intraspinal**, **Intracerebral**

Answer 33

Parenteral administration

Question 34

➢ **Protects the brain** from exposure to chemicals and metabolites, due to the presence of **tightly joined epithelial cells** lining the cerebral capillaries **➢ Lipophilic**

Answer 34

Blood Brain Barrier

Question 35

Higher perfusion, ____ distribution

Answer 35

higher

Question 36

* **Delivery of drug** to the tissue is **controlled by** the **specific blood flow** to a given tissue. * Drug delivery to the **target site**

Answer 36

Perfusion

Question 37

**Chemical conversion** of drugs to make them **inactive** → HIPE

Answer 37

Biotransformation

Question 38

# **DRUG METABOLISM** **All substances** in the **circulatory system**, including **drugs**, **metabolites**, and **nutrients**, will pass through the

Answer 38

liver

Question 39

are agents that are **initially inactive** and **become active via metabolism**

Answer 39

prodrug

Question 40

* **Pre-systemic** metabolism * **Reduction of bioavailability** = subtherapeutic * a **significant proportion** of a drug is **metabolized** by **hepatic enzymes** during the initial trip through the liver * **Drug removal by the liver** after absorption

Answer 40

First-pass effect

Question 41

➢ stimulate → **enhance** ➢ **↑ IA** ➢ **increased metabolism**, **↓** Concentration in plasma

Answer 41

Enzyme **induc**tion | induce

Question 42

➢ **decreased metabolism**, **↑** Concentration in plasma

Answer 42

Enzyme **inhibit**ion

Question 42

drug **reenters** the intestinal tract from the liver **through bile duct**

Answer 42

Enterohepatic recirculation

Question 43

➢ **Bile acid** ➢ **Reabsorption** of bile acid ➢ Drugs such as **Oral contraceptive pills**

Answer 43

Biliary recycling

Question 44

# **EXCRETION** ➢ Most **abundant** ➢ Majority of drugs are ____ excretion

Answer 44

urine / urinary

Question 45

# **EXCRETION | RENAL CLEARANCE** **unbound** (free) drug is **passively filtered** by the **glomerulus**

Answer 45

Glomerular Filtration

Question 46

# **EXCRETION | RENAL CLEARANCE** drug is **actively secreted** → urine

Answer 46

tubular secretion

Question 47

# **EXCRETION | RENAL CLEARANCE** drug is passively **reabsorbed** back into the blood

Answer 47

Tubular reabsorption