Pharm_Narcotic Analgesics Flashcards

1
Q

Elderly patients usually require a ____ dose to achieve effective pain relief than younger patients.

A

Elderly patients usually require a lower dose to achieve effective pain relief than younger patients.

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2
Q

Neuropathic pain (spine to brain) usually requires ____ opioid doses than nociceptive pain.

A

Neuropathic pain (spine to brain) usually requires higher opioid doses than nociceptive pain.

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3
Q

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

A

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

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4
Q

What are the three major opioid receptor types?

A

µ (Mu)
δ (Delta)
κ (Kappa)

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5
Q

Dosing considerations for Opioid Analgesics
- Patients on Chronic Pain

A

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

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6
Q

Dosing considerations for Opioid Analgesics
- Opioid Naive patients

A

Opioid analgesics should be started at a low dose and carefully titrated until an adequate level of analgesia is obtained, or until persistent and unacceptable side effects warrant a re-evaluation of therapy.

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7
Q

What does it imply if partial analgesia with incremental dosing in opioid-naive patient fails to achieve its therapeutic effect?

A

Failure of at least partial analgesia with incremental dosing in the opioid-naive patient may indicate that the pain syndrome is unresponsive to opioid therapy

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8
Q

What are the clinical uses of opioid agonists?
- List drug class & examples

A

Analgesia:
Codeine, morphine, pethidine

Anaesthetic adjuvant:
Fentanyl

Cough suppressant / antitussive: Codeine

Anti-diarrhoeal:
Diphenoxylate

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9
Q

What is the most important reason why Opioids should be avoided in infants?

A

Respiratory Depression (RD)

It Should not occur at normal therapeutic doses but can be lethal in:

1) Overdose (OD)
2) Respiratory disease (RD)
3) hepatic dysfunction
4) Combination with other CNS depressants
5) Young children

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10
Q

What are the common adverse effects of Narcotic Analgesics (Opioids)?

A
  • N&V
  • Drowsiness
  • Constipation (reduced GI motility)

Nausea / vomiting most probably due to actions on the chemoreceptor trigger zone in the area postrema of the medulla (usually reduces with repeated or chronic use).

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11
Q

What are the common adverse effects of Narcotic Analgesics (Opioids)
Overdose?

M.U.M.

A

1) Miosis (pinpoint pupils) will be present for a patient that just collapse due to drug OD.
However, Miosis may no longer be present due to a drug OD, for e.g. patient collapsed due to drug OD 30mins to 1 hr ago.

2) **Mydriasis **(pupils remains dilated regardless of light in the environment)

3) Urinary Retention due to increased bladder sphincter tone (esp. patients with prostatic hypertrophy)

4) Postural hypotension & Bradycardia

5) Immunosuppressant effect with long-term use

6) Trigger Histamine release from mast cells:
- urticaria and itching
- bronchoconstriction
- hypotension due to vasodilatation

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12
Q

List some of the commonly used Opioid Antagonists

Opioids themself are agonist, we need antagonist to reverse the OD.

A

Naloxone (IV) / Naltrexone (PO) / Nalmefene (IV)

Strong µ (Mu) antagonism;
also δ (Delta) & κ (Kappa) antagonism.

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13
Q

When do we require the use of Opioid Antagonists?

A

For drug overdose (OD), to reverse drug OVERDOSE.

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14
Q

What is the main difference between drug toxicity vs drug overdose?

A

**Drug overdose: **
Over-consumption over a short period of time.

**Drug toxicity: **
Chronic usage

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15
Q

Route of administration and duration of action for Opioid Antagonists.

Naloxone / Naltrexone / Nalmefene

A

Naloxone (IV) / Naltrexone (PO) / Nalmefene (IV)

Naloxone is short-acting (usually IV)
Naltrexone is long-acting (PO)

Nalmefene is long-acting (IV)(new)

Used to counteract opioid overdose & toxicity

  • Nalmefene replaced the use of Naloxone and Naltrexone

Recall why are these drugs used again?

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16
Q

What is the commonly mis-used opioid in Singapore? What is the active ingredient responsible for misuse?

A

Cough mixture
- Consist of Codeine

17
Q

What is the commonly mis-used opioid in US?

A

Heroin
(Diamorphine, a derivative of morphine)

Previously produced by Bayer (the same company that produced Aspirin)

18
Q

What is the difference between Tolerance, Physical Dependence,
Addiction?

Which of the above will cause Opioid withdrawal symptoms?

A

If patient develops Tolerance, the same drug will be less effective after prolonged use. Dose escalation will be required.

Physical dependence vs Addiction.
- Phy. dependence leads to withdrawal symptoms
- Addiction leads to psychological craving, and compulsive use and there’s no self-control.

Addiction & tolerance lead to risk of OD (overdose)

19
Q

List some of the opioid withdrawal symptoms

A

Opioid withdrawal can manifest as:
- Anxiety, irritability,
- Chills, hot flushes,
- Joint pain,
- lacrimation (tears), rhinorrhea (runny nose),
- N&V
- Abdominal cramps,
- Diarrohea.

20
Q

Contraindications of Narcotic Analgesia (Opioids)

A

1) Children
2) Patients with postural hypotension
3) Immunocompromized patients
4) Asthmatic patients (trigger histamine release)
5) COPD patients (histamine release causes bronchoconstriction)

21
Q

List some of the Strong Opioid Agonist
& considerations for its use.

A

Morphine:
Strong µ agonist (weaker δ and κ agonist).
High maximum analgesic efficacy.
High liability for addiction/abuse.

Methadone and Fentanyl:
Strong µ agonists (no significant δ and κ affinity).
High maximum analgesic efficacy.
High liability for addiction/abuse.

**Methadone is long-acting ** (plasma half-life > 24 hrs).

**Fentanyl is short-acting ** (anaesthetic adjuvant).

Pethidine (Meperidine):
- Strong µ agonist (probably weaker δ and K agonist).
- Shorter duration of action than morphine (especially in neonate therefore used in labour).
- N-demethylated in the liver to norpethidine (hallucinogenic and convulsant effects at high dose)
- Restlessness rather than sedation
- Antimuscarinic (i.e. parasympatholytic) therefore dry mouth, blurring of vision but no miosis and less spasm of smooth muscle.

22
Q

List some of the Moderate Opioid Agonist
& considerations for its use.

A

Codeine / Dihydrocodeine:
- Weak µ and δ agonist (probably not a K agonist).
- Low maximum analgesic efficacy.
- Moderate liability for addiction/abuse.
~10 % converted to morphine / dihydromorphine.
~10 % of population show reduced analgesic effect due to lack of demethylating enzyme.

Tramadol:
- Weak µ agonist.
- Weak inhibitor of 5-HT and noradrenaline re-uptake.
(OK: Tramadol + Metoclopramide)

(Not OK: Tramadol + Ondansetron)
as it blocks analgesic effect.