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Psychiatric Pharmacology > Narcotic Opioid Analgesics > Flashcards

Narcotic Opioid Analgesics Flashcards

1
Q

Morphine is a _____ opioid agonist while Codeine is a ______ opioid agonist. Thebaine is a _______ for other opioid drugs.

A
  1. strong
  2. weak
  3. Precursor
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2
Q

Endogenous opioid peptides or otherwise known as endorphins have 3 major families. They are the _______ , ________ (pentapeptides) and _________.

A
  1. Beta-endorphins
  2. Enkephalins
  3. Dynorphins
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3
Q

The brain has modulatory circuits to regulate the perception of pain. Attitude, mood, and physical exercise can ___________ pain. It is better to control pain before it ________.

A
  1. influence the perception of

2. becomes severe

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4
Q

The pain pathway starts from primary afferent neurons (in periphery) to the thalamus via the __________. The amplitude of the pain signal can be modulated via an efferent pathway (-) that reduces depolarization of __________ signal.

A

Spinothalamic tract (+)

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5
Q

Opioids work by inhibiting of the ______ of pain signals, altering the _______ of pain and possibly elevating the _______(?).

A
  1. propagation
  2. emotional perception
  3. pain threshold
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6
Q

Opioid receptors are located at ________ nociceptive terminals (peripheral analgesia), The spine (spinal analgesia) and The _____ (supraspinal analgesia).

A
  1. Peripheral

2. brain

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7
Q

The 3 major subtypes μ (Mu), δ (Delta) and κ (Kappa) are all _________ receptors. Majority of functional effects are due to action of _____ and ______.

A
  1. G Protein Coupled
  2. μ (Mu)
  3. κ (Kappa)
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8
Q

______ seems to be major receptor in both analgesic and psychoactive effects except dysphoria (feeling of unease, discomfort) while ______ is the major receptor sub type for dysphoria.

A
  1. μ (Mu)

2. κ (Kappa)

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9
Q

At _____ doses, opioids have beneficial sedation and analgesic effects by acting on nociceptive terminals, spine and brainstem.

A

Lower

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10
Q

At higher doses, opioids have side effects such as Reduced ______, Euphoria, Pupil constriction, Dysphoria, Severe sedation and _______ (potentially fatal) due to effects on GI tract, “emotional brain”, ________, respiratory nuclei.

A
  1. gut motility
  2. Respiratory depression
  3. Occulomotor
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11
Q

Elderly patients usually require a ______ dose of opioids to achieve effective pain relief than younger patients.

A

lower

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12
Q

Neuropathic pain usually requires ______ opioid doses than nociceptive pain.

A

higher

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13
Q

______ doses are usually required for continuous maintenance of pain relief than administration in response to recurrence of pain.

A

Lower

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14
Q

Opioid analgesics should be started at _______ and carefully titrated until _______ is obtained (based on patient response), or until persistent and unacceptable _____ warrant a re-evaluation of therapy.

A
  1. a low dose
  2. an adequate level of analgesia
  3. side effects
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15
Q

Failure of at least _______ with incremental dosing in the ______ patient may indicate that the pain syndrome is unresponsive to opioid therapy.

A
  1. partial analgesia

2. opioid-naive

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16
Q

For some patients with chronic pain, opioids do not exert an appreciable analgesic effect until _________ has been achieved.

A

a threshold dose

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17
Q 
Opioids have many clinical uses. 
Analgesia: Codeine, morphine, pethidine
Anaesthetic adjuvant: \_\_\_\_\_\_
Cough suppressant / antitussive: \_\_\_\_\_\_\_
Anti-diarrhoeal: \_\_\_\_\_\_\_\_
A
  1. Fentanyl
  2. Codeine
  3. Diphenoxylate
18
Q

Morphine is a ______ μ agonist ( _____δ and κ agonist). It has _____ maximum analgesic efficacy and liability for addiction/abuse.

A
  1. Strong
  2. weaker
  3. high
19
Q

Methadone and Fentanyl are _____ μ agonists ( _______ δ and κ affinity). They have ____ maximum analgesic efficacy and liability for addiction/abuse.

A
  1. Strong
  2. no significant
  3. high
20
Q

Methadone and Fentanyl are _____ μ agonists ( _______ δ and κ affinity). They have ____ maximum analgesic efficacy and liability for addiction/abuse. Methadone is ____ -acting (plasma half-life > 24 hrs) while Fentanyl is ____ -acting (anaesthetic adjuvant).

A
  1. Strong
  2. no significant
  3. high
  4. long
  5. short
21
Q

Pethidine(Meperidine) is a _____ μ agonist (probably _____ δ and κ agonist). It has a _____ duration of action than morphine (especially in neonate therefore used in labour).

A
  1. Strong
  2. weaker
  3. Shorter*
  • good as it is less likely to remain in neonate, more useful in labour
22
Q

Pethidine(Meperidine) is N-demethylated in the liver to _______ , leading to ___________ effects at high doses.

A
  1. norpethidine

2. hallucinogenic and convulsant

23
Q

Pethidine(Meperidine) causes ______ rather than sedation and has Antimuscarinic effects (i.e. parasympatholytic) therefore dry mouth, blurring of vision but no _____ and less _____ of smooth muscle.

A
  1. Restlessness
  2. miosis
  3. spasm
24
Q

Codeine/ Dihydrocodeine is a ____ μ and δ agonist (probably ____ κ agonist) with _____ maximum analgesic efficacy. It carries ______ liability for addiction/abuse.

A
  1. Weak
  2. not a
  3. Low
  4. Moderate
25
Q

~10 % of codeine/ Dihydrocodeine is converted to morphine / dihydromorphine which leads to ~10 % of population showing _______ effect due to lack of demethylating enzyme.

A

reduced analgesic

26
Q

Tramadol is a _____ μ agonist and also a _____ inhibitor of 5-HT and noradrenaline re-uptake. It is noted that ondansetron (serotonin 5-HT3 receptor antagonists) reduces analgesic effect of tramadol, meaning tramadol may mediate analgesic effect via ______ MOA (theory).

A
  1. Weak
  2. Weak
  3. 5-HT
27
Q

Opioids can cause respiratory depression via Actions in the nucleus tractus solitarius and nucleus ambiguus. This reduces ______ to CO2 (and H+) and suppresses ________. Opioids should be avoided in ______.

A
  1. responses
  2. voluntary breathing
  3. Infants
28
Q

Respiratory depression should not occur at normal therapeutic doses but can be lethal in:

  • overdose
  • ______ disease
  • _____ dysfunction
  • combination with other ________ drugs
  • __________ patient group
A
  1. respiratory
  2. hepatic
  3. CNS depressant
  4. Young children
29
Q

Opioid induced Nausea / vomiting most probably due to actions on the _____________ in the area postrema of the medulla (usually reduces with ________ use).

A
  1. chemoreceptor trigger zone

2. repeated or chronic

30
Q

Constipation is caused by opioids due to reduced gastrointestinal motility (esp. with _____ use). Opioids can also cause ________, which may require caution against operating machinery or driving.

A
  1. chronic

2. Drowsiness

31
Q

Opioids cause ______ (pinpoint pupils) due to actions in the oculomotor nucleus. ______ is a diagnostic feature of opioid overdose. But we should note that mydriasis can also follow if hypoxia occurs.

A

Miosis

32
Q

Opioids cause _______ due to increased bladder sphincter tone (esp. in patients with ____________.)

A
  1. Urinary retention

2. prostatic hypertrophy

33
Q

Opioids cause ___________ and ________ due to actions in cardio regulatory nuclei in the medulla.

A
  1. Postural hypotension

2. bradycardia

34
Q

Opioids carry an _______________ effect with long-term use, most likely through CNS effects on the immune system.

A

Immunosuppressant

35
Q

Morphine can also trigger _________, leading to urticaria and itching, bronchoconstriction and hypotension due to vasodilatation. As such, Morphine should be used with caution in _________.

A
  1. histamine release from mast cells

2. asthmatics

36
Q

Opioids have Tolerance issues meaning they are ____ effective after prolonged use and dose ______ required. Together with addiction tendencies, opioids can lead to risk of overdose.

A
  1. less

2. escalation

37
Q

Physical Dependence on opioids can manifest as physical withdrawal symptoms. They include: _____ , ______ , chills, hot flushes, _____ pain, lacrimation (tears), rhinorrhea (runny nose), nausea, vomiting, abdominal cramps, ______.

A
  1. anxiety
  2. irritability
  3. joint
  4. diarrhea
38
Q

Opioid antagonists should be used with extreme caution in patients with opiate dependency as they can precipitate potentially fatal ________.

A

withdrawal syndrome

39
Q

Opioid antagonists such as Naloxone/ Naltrexone/ Nalmefene show _____ μ antagonism; also δ and κ antagonism. They are used to counteract ________.

A
  1. Strong

2. opioid overdose

40
Q

Naloxone is _____-acting (usually intravenous for immediate overdose crisis)
Naltrexone is long-acting (____ administration post crisis and also used for ___________________________)
Nalmefene is long-acting ( _______ administration) and can replace Naloxone + Naltrexone.

A
  1. short
  2. oral
  3. long term treatment of addiction
  4. intravenous

Psychiatric Pharmacology (8 decks)

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