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Analgesics
April final
23
Pharmacology
Undergraduate 2
04/18/2012

Additional Pharmacology Flashcards

 


 

Cards

Term
What are the classifications of analgesics: 
Definition

1. narcotic analgesics (opioids)

2. non-narcotic analgesics (antipyretics)

Term
Name 4 types of opioids with examples: 
Definition

1. Endogenous: eg: endorphins, enkephalins, dynorphins.

2. Plant alkaloids: Morphine, codeine, thebaine. 

3. Semisynthetic: Diamorphine (heroine), hydromorphine 

4. Synthetic: pethidine (meperidine), methadone, fentanyl. 

Term
Where do opioids bind?
Definition
Specific receptors in the CNS and other tissues. 
Term
Opioid receptors: 
Definition

G protein-coupled receptors

Types: 1. Delta (1&2)

Kappa (1 2 and 3)

Mu (1 2 and 3)

Term

Name an opioid antagonist:

(b) Name a mixed opioid agonist/antagonist: 

Definition

(a) Naloxone

(b) Pentazocine

Term
3 characteristics of naloxone: 
Definition

1. Competitive opioid receptor antagonist. 

2. Has no analgesic effect. 

3. Causes withdrawal symptoms. 

Term
3 therapeutic uses of Naloxone: 
Definition

1. Treatment of opioid overdose (antidote)

2. Diagnosis and treatment of opioid dependence. 

3. Should always be available when opioid agonists are given through IV route. 

Term
2 characteristics of pentazocine: 
Definition

1. Has agonist action (analgesia)

2. Weak antagonist action. 

Term
When is pentazocine contraindicated?
Definition
With opioid agonists like morphine, can induce withdrawal symptoms. 
Term
3 desirable pharmacological actions of opioids: 
Definition

Analgesia

Sedation

Antitussive

Term
Sometimes desirable pharmacological actions of opioids: 
Definition

1. Constipation

2. Hypotension

Term
Undesirable pharmacological actions of opioids: 
Definition

1. Nausea/vomiting

2. Mental clouding. confusion, coma. 

3. Tolerance. 

4. Respiratory depression. 

5. Physical dependence. 

6. Addiction. 

Term
Therapeutic indications of opioids: 
Definition

1. Cough (codeine only)

2. Pain (analgesic effect)

3. Anxiety. 

4. Diarrhea (opium only)

5. Opioids dependence. (Methadone only)

Term
Which are the strongest known analgesics?
Definition
Opioids as analgesics. 
Term
Dose of opioids as analgesics: 
Definition
Variable dose with no upper limit. 
Term
What types of pain are treated by opioids? 
Definition

Acute pain: post-operative. 

Chronic severe: 

Terminal illnesses like cancer (palliative care)

Dependence is not the issue

most annoying adverse effect?

Term
Why do opioids have to be stopped gradually?
Definition
To avoid withdrawal manifestations. 
Term
Steps of inhibition of pain impulse with opioids: 
Definition

Decreased presynaptic release of chemical

transmitters that are mobilized by pain

impulse.

   ii. Blockade of postsynaptic effect of these

transmitters.

  iii. Activation of descending inhibitory

pathways to block pain input.

  iv. Decreased emotional reaction to pain by 

acting on limbic system of the brain

Term
Cross tolerance
Definition
Term
Treatment of opioid dependence: 
Definition

Methadone: 

Same opioid effect, prevent withdrawal manifestations, much less dependence. 

Buprenorphine: 

Alternatitive to methadone

Naloxone: 

Opioid antagonistic effect

Blocks drug seeking behaviour

Term
Acute opioid toxicity: Mild/early
Definition

• Pinpoint pupils (PPP)

• Hypoventilation:  slow, shallow respiration

• Hypotension and bradycardia

• Flaccid muscles

Term
Acute opioid toxicity: Severe/late
Definition

Severe respiratory depression → respiratory arrest

• Severe cardiovascular depression

• Seizures (with pethidine overdose)

• Coma

Term
Treatment of acute opioid toxicity: 
Definition

Naloxone (antidote):

• Reverses toxic manifestations

• Shorter half-life → repeat dose

– General supportive measures

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