IC11

Question 1

What is an alkaloid

Answer 1

Nitrogen-containing compound

Question 2

Classification of cocaine

Answer 2

Tropane Alkaloid

Question 3

Fg in cocaine

Answer 3

Two esters, tertiary amine

Question 4

Where is cocaine extracted from

Answer 4

coca leaf

Question 5

Apart from cocaine, coca also contains ______ and ____, with_____ as a minor constituent

Answer 5

cinnamoylcocaine; tropacocaine; methylecgonine

Question 6

Strong bases have higher/lower pKa value?

Answer 6

Higher

Question 7

What modifications in benzocaine retain the local anesthetic property and improve water solubility?

Answer 7

Replacement of tropine with amine to give procaine

Question 8

Amide incr/ decr polarity?

Answer 8

Incr

Question 9

Ester or amide group is more susceptible to hydrolysis?

Answer 9

Ester

Question 10

Aminoester local anaesthetic formation: SN1 or SN2?

Answer 10

SN2 (1-step)

Question 11

Aminoamide local anaesthetic formation: SN1 or SN2?

Answer 11

SN1 (2-step)

Question 12

Generally, LA with ____and ____ exhibit faster onset and lower toxicity.

Answer 12

higher lipid solubility; lower pKa values

Question 13

Most LA have pKa values of ____

Answer 13

7.5 – 9

Question 14

Lidocaine is an amino___

Answer 14

amide

Question 15

Lower conc of LA used may indicate lower/higher potency

Answer 15

Higher

Question 16

_____is used clinically for treatment of heroin addiction

Answer 16

Methadone

Question 17

Morphine is metabolized in the body to _____

Answer 17

morphine 3- O-glucuronide

Question 18

Advantages of morphine 3- O-glucuronide over morphine

Answer 18

• more effective and longer lasting analgesic
• fewer side-effects

Question 19

Codeine is the ____ of morphine which is a widely used analgesic and it has about ___ the potency of morphine.

Answer 19

3-O-methyl ether; 1/10

Question 20

Long-term use of codeine can cause ___

Answer 20

constipation

Question 21

How does codeine exert anti-tussive effect

Answer 21

depresses the cough centre & raise the threshold for sensory cough impulses.

Question 22

3 examples of drugs that belong to morphinan class

Answer 22

Morphine, codeine and thebaine

Question 23

How is Pholcodine derived from morphine

Answer 23

alkylation of morphine with N-(chloroethyl)morpholine

Question 24

Dihydrocodeine is a____ form of codeine

Answer 24

reduced

Question 25

Diamorphine or heroin is the____ of morphine

Answer 25

diacetate

Question 26

PPty of heroin

Answer 26

- highly addictive analgesic - hypnotic - increased lipophilic character -> better transport & absorption

Question 27

Advantages/ disadvantages of pentazocine

Answer 27

- good analgesic - non- addictive - can induce withdrawal symptoms

Question 28

Pethidine is more/ less potent than morphine

Answer 28

Less

Question 29

Advantages/ disadvantages of pethidine

Answer 29

- prompt, short-acting analgesia - less constipating than morphine - can be addictive

Question 30

Structure of pethidine

Answer 30

Only the aromatic ring and the piperidine systems are retained.

Question 31

Why is fentanyl more active than morphine?

Answer 31

Fentanyl has higher lipophilicity and excellent transport properties.

Question 32

Fentanyl has ___ structure

Answer 32

4-anilino (contains N)

Question 33

Fentanyl and derivatives are ___acting and used during ___

Answer 33

rapid; operative procedures

Question 34

Nalbuphine, produced _____ from____

Answer 34

semi-synthetically; thebaine

Question 35

Ppty of nalbuphine

Answer 35

mixed agonist– antagonist properties

Question 36

____ is used to treat opiate poisoning, including that in children born to heroin addicts.

Answer 36

Naloxone

Question 37

MOA for naloxone

Answer 37

potent antagonist at all opioid receptors; no agonist activity

Question 38

MOA for Naltrexone

Answer 38

antagonist at opioid receptors