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PR3154 > IC11 > Flashcards

IC11 Flashcards

1
Q

What is an alkaloid

A

Nitrogen-containing compound

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2
Q

Classification of cocaine

A

Tropane Alkaloid

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3
Q

Fg in cocaine

A

Two esters, tertiary amine

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4
Q

Where is cocaine extracted from

A

coca leaf

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5
Q

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

A

cinnamoylcocaine; tropacocaine; methylecgonine

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6
Q

Strong bases have higher/lower pKa value?

A

Higher

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7
Q

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

A

Replacement of tropine with amine to give procaine

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8
Q

Amide incr/ decr polarity?

A

Incr

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9
Q

Ester or amide group is more susceptible to hydrolysis?

A

Ester

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10
Q

Aminoester local anaesthetic formation: SN1 or SN2?

A

SN2 (1-step)

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11
Q

Aminoamide local anaesthetic formation: SN1 or SN2?

A

SN1 (2-step)

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12
Q

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

A

higher lipid solubility; lower pKa values

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13
Q

Most LA have pKa values of ____

A

7.5 – 9

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14
Q

Lidocaine is an amino___

A

amide

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15
Q

Lower conc of LA used may indicate lower/higher potency

A

Higher

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16
Q

_____is used clinically for treatment of heroin addiction

A

Methadone

17
Q

Morphine is metabolized in the body to _____

A

morphine 3- O-glucuronide

18
Q

Advantages of morphine 3- O-glucuronide over morphine

A
  • more effective and longer lasting analgesic
  • fewer side-effects
19
Q

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

A

3-O-methyl ether; 1/10

20
Q

Long-term use of codeine can cause ___

A

constipation

21
Q

How does codeine exert anti-tussive effect

A

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

22
Q

3 examples of drugs that belong to morphinan class

A

Morphine, codeine and thebaine

23
Q

How is Pholcodine derived from morphine

A

alkylation of morphine with N-(chloroethyl)morpholine

24
Q

Dihydrocodeine is a____ form of codeine

A

reduced

25
Q

Diamorphine or heroin is the____ of morphine

A

diacetate

26
Q

PPty of heroin

A
  • highly addictive analgesic
  • hypnotic
  • increased lipophilic character -> better transport & absorption
27
Q

Advantages/ disadvantages of pentazocine

A
  • good analgesic
  • non- addictive
  • can induce withdrawal symptoms
28
Q

Pethidine is more/ less potent than morphine

A

Less

29
Q

Advantages/ disadvantages of pethidine

A
  • prompt, short-acting analgesia
  • less constipating than morphine
  • can be addictive
30
Q

Structure of pethidine

A

Only the aromatic ring and the piperidine systems are retained.

31
Q

Why is fentanyl more active than morphine?

A

Fentanyl has higher lipophilicity and excellent transport properties.

32
Q

Fentanyl has ___ structure

A

4-anilino (contains N)

33
Q

Fentanyl and derivatives are ___acting and used during ___

A

rapid; operative procedures

34
Q

Nalbuphine, produced _____ from____

A

semi-synthetically; thebaine

35
Q

Ppty of nalbuphine

A

mixed agonist– antagonist properties

36
Q

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

A

Naloxone

37
Q

MOA for naloxone

A

potent antagonist at all opioid receptors; no agonist activity

38
Q

MOA for Naltrexone

A

antagonist at opioid receptors

PR3154 (19 decks)

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