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Pharamcology > Opioid Analgesics > Flashcards

Opioid Analgesics Flashcards

1
Q

Morphine is obtained from which plant

A

Papaver sominiferum

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2
Q

Classify opioids

A
  1. Opioid agonists:
    i)Natural Opium alkaloids
    ii)Semi synthetic opiates
    iii)Synthetic opioids
  2. Opioid agonist-antagonists
  3. Partial Mu-receptor agonist and Kappa-receptor antagonist
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3
Q

Name natural opium alkaloids

A
  1. Morphine
  2. codeine
  3. Thebaine
  4. papaverine
  5. Noscapine 
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4
Q

Name semi synthetic opiates

A
  1. Heroin
    2. hydromorphone
  2. Oxymorphone
  3. Pholcodine
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5
Q

Name synthetic opioids

A
  1. Pethidine
  2. Tramadol
  3. Methadone
  4. Dextropropoxyphene
  5. Fentanyl
  6. Alfentanil
  7. Sufentanil
  8. Remifentanil
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6
Q

Name opioid agonist-antagonist

A
  1. Pentazocine
  2. Butorphanol
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7
Q

Name partial mu-receptor agonist and Kappa-receptor antagonist

A

Buprenorphine

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8
Q

What are the effects of activating mu opioid receptors

A
  1. analgesia
  2. respiratory depression
  3. dependency
  4. sedation
  5. euphoria
  6. meiosis
  7. decrease in G.I. motility
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9
Q

What are the effects of activating kappa receptors

A
  1. Analgesia
  2. Respiratory depression
  3. dependence
  4. dysphoria
  5. Psychotomimetic effect
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10
Q

what are the effects of activating delta receptors

A
  1. Analgesia
  2. respiratory depression
  3. proconvulsant action
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11
Q

Where are opioid receptors located

A

Spinal, superaspinal and peripheral nerves

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12
Q

What is the most common cause of death in a cute opioid poisoning

A

Respiratory depression

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13
Q

How does morphine cause respiratory depression, both rate and depth

A

It reduces sensitivity of the respiratory centre to CO2

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14
Q

What are the functions/actions of morphine

A
  1. Miosis 
  2. Analgesia
  3. Respiratory depression
  4. Physical and psychological dependence
  5. histamine release, hypotension, hypothermia
  6. itching
  7. nausea and vomiting
  8. euphoria
  9. cough suppression, Constipation
  10. Vagal stimulation (bradycardia) (vasodilation)
  11. Sedation and hypnosis
  12. Urinary retention
  13. Increases intrabilary pressure
  14. Physical and psychological dependence
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15
Q

How does morphine produce miosis, constriction of the pupil?

A

Stimulation of III cranial nerve Nucleus

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16
Q

How does morphine cause nausea vomiting

A

Direct stimulation of CTZ in the medulla

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17
Q

Which drugs can be used to control Opioid induced nausea and vomiting

A
  1. 5-HT3 antagonists
  2. H1 blockers 
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18
Q

What does morphine relieve

A
  1. Pain
  2. fear
  3. anxiety
  4. apprehension
  5. feeling of sickness
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19
Q

How does morphine cause vasodilation full of BP

A
  1. Depression of VMC
  2. Histamine release
  3. direct action on blood vessels
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20
Q

What is the metabolite of morphine that is more potent and excreted in the urine

A

Morphine-6-glucuronide

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21
Q

What are the signs and symptoms of dependence of morphine

A
  1. Irritability
  2. body shakes
  3. yawning
  4. lacrimation, sweating
  5. fever
  6. diarrhoea
  7. palpitation
  8. insomnia
  9. high blood pressure
  10. weight loss
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22
Q

Dependence of morphine is mediated through which receptor

A

Mu receptors

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23
Q

Which drug can be used to substitute Morphine during with drawl

A

Methadone or buprenorphine

24
Q

How do you treat morphine dependence

A
  1. Hospitalization
  2. Gradual withdrawal of morphine
  3. Substitution therapy using opioid agonist
  4. 1 mg Methadone will substitute 4mg Morphine. Dose is reduced slowly and completely stopped within 10 days.
  5. Pure opioid antagonist like naltrexone is used for detoxification to produce opioid blockade to prevent relapse.
  6. Psychotherapy, occupational therapy, community treatment, rehabilitation
25
Q

Why are opioid agonist, like methadone, are preferred when treating morphine dependence

A
  1. Are they effective
  2. longer duration of action
  3. Withdrawal symptoms are mild: 1 mg of methadone or substitute 4 mg of morphine
26
Q

What are the signs of acute morphine poisoning

A

Cyanosis, coma, Convulsions, shock, hypertension, pinpoint pupils, respiratory depression

27
Q

What is the treatment for acute morphine poisoning

A
  1. Hospitalization
  2. Maintain airway, breathing and circulation
  3. Ventilation support
  4. gastric lavage with potassium permanganate
  5. Specific antidote: naltrexone 0. 420. 8 mg IV. Dose is repeated till respiration becomes normal
28
Q

What are the adverse effects of morphine

A
  1. Nausea, vomiting, constipation, respiratory depression, hypotension, mental clouding, confusion, itching
  2. Difficulty in micturition
  3. Respiratory depression in newborn due to administration of morphine to mother during labour
  4. Drug tolerance
  5. Drug dependence
  6. Acute morphine poisoning
  7. Seizure threshold is lowered
29
Q

Why is morphine contraindicated in cases with head injuries

A
  1. Vomiting, miosis and mental clouding can interfere with assessment of progress in head injury patients
  2. Cerebral vasodilation increases intracranial tension
30
Q

What are the contraindications of morphine

A
  1. Head injury
  2. asthma
  3. chronic obstructive pulmonary disease (COPD)
  4. hypotensive states
  5. hypothyroidism and hypopituitarism
  6. infants and elderly
  7. undiagnosed acute abdominal pain
31
Q

Which opioid drugs are used to suppress dry cough

A

Codeine
Dextromethorphan

32
Q

Codeine potentiates analgesic affect of which drugs

A

Aspirin
paracetamol

33
Q

What are the main side effects of codeine

A

Constipation and sedation

34
Q

Codeine should be avoided in which patients

A

Children and asthmatics

35
Q

What is the difference between codeine and pholcodeine 

A

Codeine has analgesic affect while pholcodeine doesn’t

36
Q

What is the metabolite of Pheyidine?  what are its adverse effects

A

Norphethidine 
Same as morphine as well as tremors, hallucinations, muscle twitches, and rarely convulsions


37
Q

Why is diphenoxylate not used for the treatment of Diarrhoea anymore

A

It causes paralytic ileus

38
Q

What are the therapeutic uses of opioids

A
  1. Analgesic
  2. pre-anesthetic medication
  3. acute pulmonary oedema
  4. post anaesthetic medication
  5. cough
  6. diarrhoea
39
Q

Which opiates are used in the treatment of diarrhoea

A

Loperamide
Diphenoxylate

40
Q

What are the adverse effects of Pethidine?

A
  1. Similar Morphine effects
  2. Anticholinergic
  3. Seizures, tremors
  4. with SSRI serotonin syndrome
41
Q

Which drugs cause serotonin syndrome with SSRI

A

Tramadol
pethidine 

42
Q

Actions of which drug cannot be completely reversed by naltrexone

A

Buprenorphine

43
Q

Which drug is also able Inhibit the uptake of norepinephrine and serotonin

A

Tramadol

44
Q

What are the actions of tramadol

A
  1. Analgesia
  2. respiratory depression
  3. physical and psychological dependence
  4. nausea and vomiting
  5. euphoria
  6. constipation
  7. sedation
45
Q

Which drug is 100 times more potent than morphine as an analgesic 

A

Fentanyl

46
Q

What are the effects of methadone

A
  1. Miosis
  2. analgesia
  3. respiratory depression
  4. physical and psychological dependence
  5. nausea and vomiting
    6! euphoria
  6. cough suppression, constipation
  7. sedation 
47
Q

Which drug because cardiotoxicity and Pulmonary oedema as adverse affect

A

Dextropropxyphene

48
Q

Which drug may cost hallucination and nightmares as an adverse effect

A

Pentazocine

49
Q

What are the effects of Pentazocine

A
  1. Analgesia
  2. respiratory depression
  3. physical and psychological dependence
  4. Nausea and vomiting
  5. constipation
  6. biliary spasm 
50
Q

What are the effects of buprenorphine 

A

Same as morphine but is more potent than morphine in causing analgesia

51
Q

Name opioid antagonist

A
  1. Naltrexone
  2. Naloxone
  3. Nalmefene
52
Q

What are the uses of naloxone 

A
  1. Treatment of morphine and other opioid poisoning
  2. Opioid overdose
  3. Neonatal asphyxia
53
Q

What are the uses of naltrexone

A
  1. Opioid blocking therapy to prevent relax
  2.  treatment of alcoholism
54
Q

What is the function of methynaltrexone

A

Treatment of constipation due to opioids 

55
Q

Name Endogenious opioid peptides that are involved in placebo and acupuncture induced analgesia

A

Endorphins, enkephalins, dynorphins. 

Pharamcology (15 decks)

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