Lesson B4 - Pharmacology Flashcards

1
Q

Opium contains at least 20 different

chemical compounds, two of which are

A

morphine and codeine, are analgesic (pain-relieving) drugs.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

In the early 1800’s, morphine was isolated as the major analgesic agent from

A

opium

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

The purification of morphine revolutionized the use of opiates. Since then, morphine has been used worldwide for the treatment of

A

pain and diarrhea.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

The term “opioid” refers to

A

any natural or synthetic substance which exerts actions on the body
that are similar to those induced by morphine and that are antagonized (blocked) by the drug
naloxone.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Opioids include:

A
  1. Opiate narcotics (analgesic agents obtained from the opium poppy).
  2. Substances structurally related to morphine.
  3. Synthetic drugs with structures different from that of morphine.
  4. Endogenous brain peptides that exert analgesic actions (opioid peptides: enkephalins and
    endorphins) .
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

There are now at least three known families of

endorphins; these are:

A

enkephalins, dynorphins and β-endorphins.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

There are several types of opioid receptors; three will be discussed…

A
  1. Mu (µ) receptors are present in all structures in the brain and spinal cord
  2. Kappa (k) receptors are involved in analgesia, dysphoria and miosis (pin-point pupils)
  3. Delta (δ) receptors have as their endogenous ligand, the enkephalins
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Opioid receptors are located in the

A

peripheral as well as the central nervous system-These are located in the gastrointestinal tract and are responsible for the constipation caused by opiates.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Agonists:

A

Illicit a full response.
Natural – morphine and codeine
Semi-synthetic – heroin
Synthetic – meperidine and methadone

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Mixed Agonists/Antagonists:

A

Pentazocine is the best example of this group. This group can illicit a response when given alone, but can block part of the
response to morphine, when given together with morphine.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Antagonists:

A

These agents block the response to morphine, heroin and other
opiates at the respective receptor. Administration of an antagonist to an addict will precipitate “withdrawal”.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

The prototype antagonist is naloxone. It has no analgesic activity
and is used in:

A

(a) Reversal of opioids overdose.
(b) Treatment of opioid dependence.
(c) Diagnosis of opioid physical dependence.
(d) Naltrexone – an opioid antagonist is used to treat alcohol dependence.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

The therapeutic uses listed below apply to morphine and most of the other opiates:

A

 Relief of severe pain (e.g. post-surgical pain and pain experienced by some terminally
ill patients). Analgesia is the major use for the opiates.

 Treatment of diarrhea.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Pharmacological Effects of Opioid Agonists

A
  1. Analgesia.
  2. Euphoria
  3. Sedation.
  4. Hypnosis/sleep (narcotic effect).
  5. Relief or prevention of cough.
  6. Respiratory depression (basis of toxicity) → respiratory arrest.
  7. Decreased gastrointestinal motility (constipation).
  8. Constriction of the pupils of the eyes (miosis).
  9. Nausea, vomiting.
  10. Drug dependence. Develops to all opiate analgesics.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Morphine and related opioids act on specific receptors on neurons – the

A

opioid receptors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Morphine and related opioids act on specific receptors on neurons – the opioid receptors.
Responses are elicited when these receptors are activated. Naloxone does

A

not activate these

receptors. However, it occupies and blocks the opioid receptors (an antagonist).

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Narcotic (Opioid) Drug Dependence -Tolerance:

A

Loss of effectiveness with repeated administration. Tolerance to most, but not
all, pharmacological effects occurs; the exceptions are constriction of the pupils and the
constipating effect

18
Q

Physical dependence: Develops after repeated administration. A pronounced withdrawal
syndrome can occur and is an indicator of

A

physical dependence. It is not life threatening.

19
Q

Narcotic (Opioid) Drug Dependence-Physical dependence: A withdrawal syndrome can occur after discontinuing the drug or after administration of Naloxone. The withdrawal syndrome is manifested as:

A

(a) Restlessness, anxiety, insomnia.
(b) Sweating, fever, chills
(c) Increased respiratory rate
(d) Retching and vomiting
(e) Cramping
(f) Explosive diarrhea

20
Q

The kinds of symptoms, as well as their severity and duration, are determined by

A

the particular drug, the chronicity and pattern of use, the typical daily dose, concurrent use of
other drugs, the route of administration, and the health of the user.

21
Q

Psychological dependence: (addiction) Pronounced craving and compulsion for narcotic
(opioid) analgesics

A

can develop

22
Q

The basis for the psychic dependence is the

A

euphoric action of the

opioids which serves as a very powerful reinforcing factor in the drug-seeking behaviour.

23
Q

Opioid overdose is a medical emergency. Overdose of all opioid drugs can produce profound

A

respiratory depression which is the cause of death.

24
Q

The euphoria produced by opioid analgesics is the primary reason for their abuse. Factors which
determine abuse of opioids are:

A

Inherent properties of the compound. How much euphoria and reinforcement does it
produce?
 The size of the dose.
 The route of administration.
 The use of opioids in combination with other drugs.

25
Q

Effects of opioid abuse:

A

A large number of intravenous drug users suffer deleterious effects of chronic needle
use.
 Abscesses and infections at the site of administration. The major concern is the spread
of disease through contaminated needles (hepatitis and AIDS).
 Lifestyle of the user is often aberrant. They may need to resort to crime or prostitution
to obtain money for drugs. They spend all their money on drugs and leave very little
for nutrition, etc. They do not seek medical help when ill as their use of drugs will be
detected and thus they are often in poor health. They may abandon friends and
family.

26
Q

Treatment of Opioid Dependence

A
  1. Cessation of drug use. Oral methadone replaces the drug of dependence and the dose of
    methadone is slowly reduced over time.
  2. Methadone maintenance. This is a method where methadone replaces the drug of
    dependence but the dose is not reduced. The individual substitutes methadone dependence
    for street heroin or other drug dependence.
27
Q

Morphine may be taken

orally in tablet form, smoked, sniffed and

A

injected

28
Q

Effects of Short-Term Use – Low Doses

CNS: Effects or morphine use include suppression of the sensation of pain and emotional
response to it, euphoria, drowsiness, lethargy, relaxation, difficulty in concentrating, decreased
physical activity in some users, and

A

increased physical activity in others, mild anxiety or fear, pupillary constriction, blurred vision, impaired night vision, and suppression of cough reflex.

29
Q

Effects of Short-Term Use – Higher Doses

Intensification of morphine’s low-dose effects may occur with administration of higher doses.
Duration of effects also increases with increased dosage. As the dose increases, sensitivity and
emotional response to painful stimuli decrease, probability of sleep increases, ability to
concentrate is increasingly impaired, breathing becomes progressively slower and more shallow,
heart rate gradually slows and

A

blood pressure decreases.

30
Q

Effects of Long-Term Use morphine-

There does not appear to be marked physiological deterioration or psychological impairment on
long-term use. Adverse effects of long-term use include mood instability, pupillary constriction
(impairs night vision), constipation, reduced libido, menstrual irregularity, and

A

respiratory impairment.

31
Q

Heroin is

A

diacetylmorphine. It is produced synthetically from morphine.

32
Q

Heroin was used in the

early 1900’s for medical purposes as an

A

analgesic.

33
Q

The legitimate medical uses are extremely low. Heroin is more potent than morphine,
but between the two drugs, it is not more

A

efficacious.

34
Q

It should be noted that heroin is rapidly converted to morphine

A

in the body.

35
Q

CNS: Effects of heroin use include suppression of the sensation of pain, euphoria, mental
clouding, heightened feelings of well-being, relaxation and drowsiness in some, and in others
talkativeness and

A

activity

36
Q

Effects of Short-Term Use – heroin Higher doses

As the dose is increased, the magnitude and duration of the response also increase. The response
to painful stimuli is blunted further. The individual becomes less able to concentrate, and wishes
to

A

sleep

37
Q

Effects of Long-Term Use

As with morphine, heroin, when administered under medical supervision, does not result in
marked physiological or psychological

A

impairment

38
Q

Tolerance and Dependence

Tolerance develops to heroin with chronic use as it does to all other opiates. Powerful physical
and psychological dependence develops rapidly upon regular

A

high dose use

39
Q

Potential for Abuse

The dependence liability of heroin is the greatest of the opioids in common use, including

A

morphine

40
Q

heroin enters the brain quickly after intravenous administration and there is immediate and

A

intense gratification.

41
Q

The inherent harmfulness in low to moderate doses is

A

low