M5

Question 1

• the process by which the drug is CHEMICALLY converted in the body to a metabolite

Answer 1

METABOLISM

Question 2

METABOLISM is also known as

Answer 2

BIOTRANSFORMATION

Question 3

METABOLISM is usually an ____ process

Answer 3

enzymatic

Question 4

MAIN SITE of metabolism

Answer 4

LIVER

Question 5

what is the primary goal of METABOLISM

Answer 5

to convert durgs into an INACTIVE form

to facilitate HIPE

Question 6

EXCEPTIONS (METABOLISM)

• drugs that are INACTIVE and must be bio-transformed in the body to have pharmacologic activity
• they are intentionally designed to:
  
  • improve drug stability
  • increase systematic drug absorption
  • prolong the duration of activity

Answer 6

PRODRUGS

Question 7

PRODRUGS

ACEIs that are NOT prodrugs

Answer 7

Captopril
Lisinopril

Question 8

PRODRUGS

CLOPIDOGREL to ____

Answer 8

Perindopril Cysteinyl Derivative

Question 9

PRODRUGS

DIPIVEFRIN to ____

Answer 9

EPINEPHRINE

Question 10

PRODRUGS

what type of drug is Clopidogrel

Answer 10

antiplatelet

Question 11

PRODRUGS

what does Clopidogrel INHIBITS

Answer 11

Adenosine Diphosphate

Question 12

PRODRUGS

a derivative of Epinephrine that is used for glaucoma

Answer 12

Dipivefrin

Question 13

PRODRUGS

Hetacillin to ____

Answer 13

Ampicillin

Question 14

PRODRUGS

Sulfasalazine to ____

Answer 14

5-ASA

Question 15

PRODRUGS

L-dopa to ____

Answer 15

Dopamine

Question 16

PRODRUGS

Phenacetin to ____

Answer 16

Paracetamol

Question 17

PRODRUGS

Primidone to ____

Answer 17

Phenobarbital

Question 18

PRODRUGS

Prednisone to ____

Answer 18

Prednisolone

Question 19

TOXIC METABOLITES

Acetaminophen to ____ that causes LIVER NECROSIS

Answer 19

NAPQI
N-acetyl-p-benzoquinone-imine

Question 20

TOXIC METABOLITES

NAPQI causes ____

Answer 20

LIVER NECROSIS

Question 21

TOXIC METABOLITES

Benzo(a)pyrene to ____ that are CARCINOGENIC

Answer 21

Benzo(a)pyrene epoxides

Question 22

ACTIVE METABOLITE

Codeine to ____ (demethylation)

Answer 22

MORPHINE

Question 23

ACTIVE METABOLITE

Diazepam to ____

Answer 23

OXAZEPAM

Question 24

ACTIVE METABOLITE

Procainamide to ____

Answer 24

N-acetoprocainamide

Question 25

# **ACTIVE METABOLITE** **Phenylbutazone** to ____

Answer 25

oxyphenbutazone

Question 26

# **SITE OF METABOLISM** * BOTH a **synthesizing** and an **excreting** organ

Answer 26

LIVER

Question 27

# **SITE OF METABOLISM** LIVER: * **HMW** drugs

Answer 27

BILIARY excretion STOOL

Question 28

# **SITE OF METABOLISM** LIVER: * **LMW** drugs

Answer 28

RENAL excretion URINE

Question 29

# **SITE OF METABOLISM** LIVER: * **basic anatomical unit**

Answer 29

LIVER LOBULE

Question 30

# **SITE OF METABOLISM** LIVER: * **liver lobule** contains ____ in a network of interconnected lymph and blood vessels

Answer 30

PARENCHYMAL CELLS

Question 31

# **SITE OF METABOLISM** BLOOD SUPPLY OF LIVER: * brings **OXYGEN-RICH** blood to the liver

Answer 31

HEPATIC ARTERY

Question 32

# **SITE OF METABOLISM** BLOOD SUPPLY OF LIVER: * brings **NUTRIENT-rich** blood from the **digestive organs (GI Tract)** to the liver

Answer 32

HEPATIC PORTAL VEIN

Question 33

# **SITE OF METABOLISM** BLOOD SUPPLY OF LIVER: * inside the liver, the blood from both sources **mixes** in **tiny spaces** called

Answer 33

SINUSOIDS

Question 34

# **SITE OF METABOLISM** BLOOD SUPPLY OF LIVER: * blood then **LEAVES** the liver through the ____ | liver to heart

Answer 34

HEPATIC VEIN

Question 35

# **SITE OF METABOLISM** BLOOD SUPPLY OF LIVER: * ____ **drains bile** and biliary excretion products from both lobes **into the gallbladder** to the intestine for excretion

Answer 35

COMMON BILE DUCT

Question 36

# **SITE OF METABOLISM** LIVER: * the **chemical** used in the **determination of SECRETORY FUNCTION** of the liver

Answer 36

BROMOSULPHTHALEIN

Question 37

# **SITE OF METABOLISM** OTHER SITES

Answer 37

kidney GIT Placenta Plasma

Question 38

# **FACTORS INFLUENCING *DRUG METABOLISM*** DRUG METABOLISM in the liver depends on **BOTH** ____ and ____

Answer 38

blood flow & enzyme location

Question 39

# **FACTORS INFLUENCING *DRUG METABOLISM*** BLOOD FLOW & ENZYME LOCATION: * **enzyme concentration** is ____, and some are only accessible from **specific ____**

Answer 39

NOT UNIFORM BLOOD FLOW DIRECTIONS

Question 40

# **FACTORS INFLUENCING *DRUG METABOLISM*** BLODD FLOW & ENZYME LOC: * ____ **alter** liver structure and blood flow, causing changes in drug bioavailability

Answer 40

HEPATIC DISEASES

Question 41

# **FACTORS INFLUENCING *DRUG METABOLISM*** AGE-RELATED VARIATIONS: * ____ are at risk for **drug toxicity** due to **inefficient conjugation** | cannot metabolize in **full capacity**

Answer 41

NEONATES

Question 42

effect of **CHLORAMPHENICOL** in babies

Answer 42

gray baby syndrome

Question 43

# **FACTORS INFLUENCING *DRUG METABOLISM*** SOCIAL HABITS that can **increase hepatic clearance** of some drugs by inducing emtabolic enzymes

Answer 43

Alcohol & Smoking

Question 44

# **FACTORS INFLUENCING *DRUG METABOLISM*** DISEASE CONDITIONS: * conditions such as ____ or ____ can **reduce** liver blood flow, significantly **impairing drug metabolism**

Answer 44

CIRRHOSIS or HEART FAILURE

Question 45

# **FACTORS INFLUENCING *DRUG METABOLISM*** DRUG INTERACTIONS: * enzyme **INDUCERS** can **increase** metabolism = ____ **drug levels**

Answer 45

DECREASED

Question 46

# **FACTORS INFLUENCING *DRUG METABOLISM*** DRUG INTERACTIONS: * enzyme **INHIBITORS** can **decrease** metabolism = ____ **drug levels**

Answer 46

INCREASED

Question 47

effect of enzyme **INHIBITORS** to **PRODRUGS**

Answer 47

DECREASED effects/levels

Question 48

# **FACTORS INFLUENCING *DRUG METABOLISM*** GENETIC FACTORS: * **ELIMINATE** drugs (***Isoniazid, Hydralazine***)

Answer 48

RAPID acetylators (ASIANS)

Question 49

# **FACTORS INFLUENCING *DRUG METABOLISM*** GENETIC FACTORS: * risk **higher plasma levels** and **INCREASED TOXICITY**

Answer 49

SLOW acetylators (CAUCASIANS)