Opioid Drugs

OPIOID DRUGS

Q. 1 Which  one  of  the  opioid  has  maximum plasma protein binding capacity:
 A Morphine
 B Sufentanil
 C Fentanyl  
 D Pethidine
Q. 1 Which  one  of  the  opioid  has  maximum plasma protein binding capacity:
 A Morphine
 B Sufentanil
 C Fentanyl  
 D Pethidine
Ans. B

Explanation:

Protein binding capacity of opioids: Morphine: 30-40%., Pethidine: 70%, Fentanyl: 84%. Alfentanil: 92%., Sufentanil: 93%.


Q. 2 Buprenorphine is:
 A Pure agonist
 B Pure antagonist
 C Partial agonist
 D None
Q. 2 Buprenorphine is:
 A Pure agonist
 B Pure antagonist
 C Partial agonist
 D None
Ans. C

Explanation:

Partial agonist


Q. 3

Which of the following drug is used for long term maintenance in opioid addiction?

 A

Naloxone

 B

Naloxone

 C

Butylphenol

 D

Methadone

Q. 3

Which of the following drug is used for long term maintenance in opioid addiction?

 A

Naloxone

 B

Naloxone

 C

Butylphenol

 D

Methadone

Ans. D

Explanation:

 Methadone has a long half life of 15-40 hours.
Because of the extended duration of action it suppresses the withdrawal symptoms in dependent patients and is therefore used for long term maintenance in opioid addiction.
 
Methadone is a slow-acting agonist of -opioid receptor.
It is absorbed well from the GI tract and can be detected in plasma within 30 minutes of oral ingestion.
 Peak concentrations occur in brain within 1-2 hours of subcutaneous or intramuscular administration. 
 
It is primarily used  for the relief of chronic pain, in the treatment of opioid abstinence syndromes, and for treating heroin users. Methadone causes prolongation of QT interval. It causes serious cardiac arrhythmias including torsade de pointes. 
 
Ref: Yaksh T.L., Wallace M.S. (2011). Chapter 18. Opioids, Analgesia, and Pain Management.

Quiz In Between


Q. 4

Buprenorphine on opioid receptors is:

 A

Pure agonist

 B

Pure antagonist

 C

Partial agonist

 D

None

Q. 4

Buprenorphine on opioid receptors is:

 A

Pure agonist

 B

Pure antagonist

 C

Partial agonist

 D

None

Ans. C

Explanation:

Pure morphine like opioids in general acts on Mu and K receptors.

Mixed agonists-antagonists:
  • Nalorphine
  • Butorphanol
  • Pentazocine
Partial agonists:
  • Buprenorphine
Pure competitive opioid antagonists
  • Naloxone
  • Naltrexone
  • Nalmefene
Ref: K.D.T 6th Ed Page 464.

Q. 5

Symptoms of opioid withdrawal are all, EXCEPT:

 A

Polyuria

 B

Yawning

 C

Fever

 D

Insomnia

Q. 5

Symptoms of opioid withdrawal are all, EXCEPT:

 A

Polyuria

 B

Yawning

 C

Fever

 D

Insomnia

Ans. A

Explanation:

Opioid withdrawal syndrome may resemble a severe flu-like illness.

The syndrome is characterized by rhinorrhea, sneezing, yawning, lacrimation, abdominal cramping, leg cramping, piloerection (gooseflesh), nausea, vomiting, diarrhea, dilated pupils, fever, and insomnia.

Heroin and methadone withdrawal symptoms peak in 36-72 hours and 72-96 hours, respectively, and may last for 7-10 days and at least 14 days, respectively.


Q. 6

Which of the following physiological effect is not produced by stimulation of Kappa opioid receptor?

 A

Sedation

 B

Diuresis

 C

Meiosis

 D

Constipation

Q. 6

Which of the following physiological effect is not produced by stimulation of Kappa opioid receptor?

 A

Sedation

 B

Diuresis

 C

Meiosis

 D

Constipation

Ans. D

Explanation:

Constipation is due to stimulation of µ receptor. The effect of stimulation of Kappa opioid receptor includes analgesia, dieresis, sedation, meiosis and dysphoria.

Ref:  Review of Medical Physiology by Ganong, 20th Edition, Page 107.

 

Quiz In Between


Q. 7

Which of the following is not an opioid peptide?

 A

Epinephrin

 B

Leu5-enkephalins

 C

Met – enkephalins

 D

All

Q. 7

Which of the following is not an opioid peptide?

 A

Epinephrin

 B

Leu5-enkephalins

 C

Met – enkephalins

 D

All

Ans. A

Explanation:

A i.e. Epinephrin

Epinephrine is adrenaline (not an opoid). /3-endorphins, Met & Leu-encephalins and Dynorphins are endogenous opioidsQ.

Endogenous opioids

Some peptides having morphine like action are isolated from mammalian brain, pituitary, spinal cord and GIT hence, they are called endogenous opioids. They are active in small amounts; bind with high affinity to the opioid receptors and modulate pain, mood, hedonic (pleasure) related, motor behavior, pituitary hormone release & GIT motility.

There are 3 distinct families of opioid peptides. Each family is derived from a distinct precursor and has a characteristic anatomical distribution.



Q. 8

The follwing are opioid withdrawl symptoms except:

 A

Insomnia

 B

Piloerection

 C

Rhinorrhea

 D

Constipation

Q. 8

The follwing are opioid withdrawl symptoms except:

 A

Insomnia

 B

Piloerection

 C

Rhinorrhea

 D

Constipation

Ans. D

Explanation:

D i.e. Constipation


Q. 9

Acute opioid withdrawl is characterizedby

 A

Rhinorrhoea

 B

Piloerection

 C

Insomnia

 D

All

Q. 9

Acute opioid withdrawl is characterizedby

 A

Rhinorrhoea

 B

Piloerection

 C

Insomnia

 D

All

Ans. D

Explanation:

A, B, C i.e. Rhinorrhoea, Piloerection, Insomnia

Quiz In Between


Q. 10

The drug which is used for long term maintenance in opioid addiction:

 A

Naloxone

 B

Nalorphine

 C

Butarphamol

 D

Methadione

Q. 10

The drug which is used for long term maintenance in opioid addiction:

 A

Naloxone

 B

Nalorphine

 C

Butarphamol

 D

Methadione

Ans. D

Explanation:

D i.e. Methadone 

Naloxone is used in opioid overdoseQ and ultrarapid detoxification of opioid dependent (addicts)Q. Due to short duration of action (t1/2 = 1-2 hour), frequent dosing is required, which makes it unsuitable for maintenance treatmentQ. Naltrexone & Nalmefene are used in rapid detoxification and maintenance of ultrarapid detoxification in opioid addicts (dependent). And methadone is used in short term detoxification, long term detoxification & long term maintenance in opioid dependant (addicts)Q. 


Q. 11

Which of the following is an alternative to methadone for maintenance treatment of opiate dependence?

 A

Diazepam

 B

Chlordiazepoxide

 C

Buprenorphine

 D

Dextropropoxyphene

Q. 11

Which of the following is an alternative to methadone for maintenance treatment of opiate dependence?

 A

Diazepam

 B

Chlordiazepoxide

 C

Buprenorphine

 D

Dextropropoxyphene

Ans. C

Explanation:

C i.e. Buprenorphine


Q. 12

Which drug is most commonly used world wide in maintenance treatment for opioid dependence:

 A

Naltrexone

 B

Methadone

 C

Imipramine

 D

Disulfiram

Q. 12

Which drug is most commonly used world wide in maintenance treatment for opioid dependence:

 A

Naltrexone

 B

Methadone

 C

Imipramine

 D

Disulfiram

Ans. B

Explanation:

B i.e. Methadone

Quiz In Between


Q. 13

Which of the following drugs is used in Ml?

 A

Cocaine

 B

Pethidine

 C

Morphine

 D

Butorphanol

Q. 13

Which of the following drugs is used in Ml?

 A

Cocaine

 B

Pethidine

 C

Morphine

 D

Butorphanol

Ans. C

Explanation:

Ans. is ‘c’ i.e., Morphine


Q. 14

Which one of the following drug is not a non-opioid analgesic drug?

 A

Meloxicam

 B

Methadone

 C

Nimesulide

 D

Nabumetone

Q. 14

Which one of the following drug is not a non-opioid analgesic drug?

 A

Meloxicam

 B

Methadone

 C

Nimesulide

 D

Nabumetone

Ans. B

Explanation:

Ans. is ‘b’ i.e., Methadone

Meloxicam, Nimesulide and Nabumetone are NSAIDs.

o NSAIDs are also called nonnarcotic, nonopioid or aspirin like analgesics.

o Methadone is an opioid.


Q. 15

The drug for OPD analgesia is –

 A

Morphine

 B

Pethidine

 C

Fentanyl

 D

Alfentanil

Q. 15

The drug for OPD analgesia is –

 A

Morphine

 B

Pethidine

 C

Fentanyl

 D

Alfentanil

Ans. D

Explanation:

Ans. is ‘d’ i.e., Alfentanil

Drugs useful for day care surgery

o Propofol              o Sevoflurane, desflurane & isoflurane

o Midazolam          o Mivacurium

o Alfantanil

 

Quiz In Between


Q. 16

Opioid agonist are A/E –

 A

Morphine

 B

Codeine

 C

Ketamine

 D

Methadone

Q. 16

Opioid agonist are A/E –

 A

Morphine

 B

Codeine

 C

Ketamine

 D

Methadone

Ans. C

Explanation:

Ans. is ‘c’ i.e., Ketamine

Opioid nonists

  1. Natural: – Morphine, codeine.
  2. Semisynthetic: – diacetylmorphine (Heroin), Pholcodeine, hydromorphone, Oxymorphone, Hydrocodone, oxycodone.
  3. Synthetic: – Pethidine (mepridine), Fentanyl, methadone, Dextropropoxyphene, Tramadol, Sulfentanil, Alfentanil, Remifentanil, Levorphenol, Dextromoramide, Dipipanone.

Q. 17

Morphine causes vomiting by acting on-

 A

C.T.Z

 B

Gastric mucosa

 C

Both of the above

 D

None of the above

Q. 17

Morphine causes vomiting by acting on-

 A

C.T.Z

 B

Gastric mucosa

 C

Both of the above

 D

None of the above

Ans. A

Explanation:

Ans. is ‘a’ i.e., C.T.Z


Q. 18

Opioid tolerance develops to all of the following actions, except:

 A

Miosis

 B

Analgesia

 C

Euphoria

 D

Nausea and vomiting

Q. 18

Opioid tolerance develops to all of the following actions, except:

 A

Miosis

 B

Analgesia

 C

Euphoria

 D

Nausea and vomiting

Ans. A

Explanation:

Ans. is ‘a’ i.e., Wasis

Tolerance is exhibited to most actions of morphine except for miosis and constipation.

Quiz In Between


Q. 19

The effect of morphine which has least tolerance is?

 A

Analgesia

 B

Respiratory depression

 C

Constipation

 D

Bradycardia

Q. 19

The effect of morphine which has least tolerance is?

 A

Analgesia

 B

Respiratory depression

 C

Constipation

 D

Bradycardia

Ans. C

Explanation:

Ans. is ‘c’ i.e., Constipation


Q. 20

Morphine withdrawal is characterized by all except-

 A

Miosis

 B

Muscle aches and body pain

 C

Yawning

 D

Rhinorrhoea

Q. 20

Morphine withdrawal is characterized by all except-

 A

Miosis

 B

Muscle aches and body pain

 C

Yawning

 D

Rhinorrhoea

Ans. A

Explanation:

Ans. is ‘a’ i.e., Miosis

Morphine withdrawal

o Manifestations of morphine withdrawl.

  • Lacrimation             
  • Anxiety & fear               
  • Mydriasis       
  • Diarrhea          
  • Palpitation
  • Sweating                   
  • Restlessness                    
  • Insomnia         
  • Dehydration
  • Rapid weight loss
  • Yawning                    
  • Gooseflash (Piloerection)
  • Abdominal colic                        
  • Rise in BP

Q. 21

Which of the following drug is most commonly used world wide in maintenance doses for opioid dependence?

 A

naltrexone

 B

Methadone

 C

Imipramine

 D

Disulfiram

Q. 21

Which of the following drug is most commonly used world wide in maintenance doses for opioid dependence?

 A

naltrexone

 B

Methadone

 C

Imipramine

 D

Disulfiram

Ans. B

Explanation:

Ans. is ‘b’ i.e., Methadone

Methodone maintenance is the most common form of pharmacoligical treatment for opioid dependence.

Quiz In Between


Q. 22

Morphine can be used in all the following conditions except-

 A

Head injury

 B

Asthma

 C

Hypothyroidism

 D

Diabetes

Q. 22

Morphine can be used in all the following conditions except-

 A

Head injury

 B

Asthma

 C

Hypothyroidism

 D

Diabetes

Ans. A

Explanation:

Ans. is ‘a’ i.e., Head injury

o Head injury is a contraindication for morphine – KDT 6th/e p. 457.

o In Bronchial asthma morphine should be avoided, but it is not given as contraindication to morphine.


Q. 23

As compared to morphine, methadone is –

 A

Superior analgesic and inferior hypnotic

 B

Superior hypnotic and inferior analgesic

 C

Superior analgesic and superior hypnotic

 D

Inferior analgenic and inferior hypnotic

Q. 23

As compared to morphine, methadone is –

 A

Superior analgesic and inferior hypnotic

 B

Superior hypnotic and inferior analgesic

 C

Superior analgesic and superior hypnotic

 D

Inferior analgenic and inferior hypnotic

Ans. A

Explanation:

Ans. is ‘a’ i.e., Superior analgesic and inferior hypnotic

  • I mg of methadone can be substituted for 4 mg of morphine.
  • Methadone is less hypnotic than morphine (sedative action is less intense).

Q. 24

Methadone is used in the management of opioid addiction because-

 A

Its analgesic activity is less than that of morphine

 B

It is an opioid receptor antagonist

 C

It is not addictive

 D

It is longer acting and causes milder withdrawal symptoms

Q. 24

Methadone is used in the management of opioid addiction because-

 A

Its analgesic activity is less than that of morphine

 B

It is an opioid receptor antagonist

 C

It is not addictive

 D

It is longer acting and causes milder withdrawal symptoms

Ans. D

Explanation:

Ans. is ‘d’ i.e., It is longer acting and causes milder withdrawal symptoms

Quiz In Between


Q. 25

Opioid with monoamine action is?

 A

Tramadol

 B

Pentazocine

 C

Pethidine

 D

Meperidine

Q. 25

Opioid with monoamine action is?

 A

Tramadol

 B

Pentazocine

 C

Pethidine

 D

Meperidine

Ans. A

Explanation:

Ans. is ‘a’ i.e., Tramadol

  • Unlike other opioids, tramadol inhibits reuptake of NA and 5-HT and thus activates monoaminergic spinal inhibition of pain —> action can be abolished by 5-HT3 antagonist (ondansetron).

Q. 26

Most potent opioid is-

 A

Fentanyl

 B

Sulfentanil

 C

Pethidine

 D

Morphine

Q. 26

Most potent opioid is-

 A

Fentanyl

 B

Sulfentanil

 C

Pethidine

 D

Morphine

Ans. B

Explanation:

Ans. is ‘b i.e., Sufentanil

The order of potency

Sufentanil > Fentanyl >Buprenotphine> Hydromorphone, Oxymorphone> Butorphanol > Levorphenol > Oxycodone > Hydrocodone >Nalbuphine, morphine, Methadone> Pentazocine> codeine > Mepridine (Pethidine) > Propoxyphane.

Remember

o Sufentanil is most potent opioid analgesic – Katzung 101Ve p. 491

o Mepridine (Pethidine) and propoxvphene are least potent opioid analgesics. – Katzung 10dle p. 491.


Q. 27

Which opioid does not require kidney & liver for metabolism

 A

Remifentanyl

 B

Sufentanil

 C

Al fentanyl

 D

Fentanyl

Q. 27

Which opioid does not require kidney & liver for metabolism

 A

Remifentanyl

 B

Sufentanil

 C

Al fentanyl

 D

Fentanyl

Ans. A

Explanation:

Ans. is ‘a’ i.e., Remifentanyl

  • Remifentanyl

         Faster acting than other fentanyl congeners.

         Unique in that it is metabolized by plasma estreases, so dose reduction is not required in renal and hepatic failure.

Quiz In Between


Q. 28

Which of the following actions is ascribed to delta type of opioid receptors –

 A

Supraspinal analgesia

 B

Respiratory depression

 C

Euphoria

 D

Reduced intestinal motility

Q. 28

Which of the following actions is ascribed to delta type of opioid receptors –

 A

Supraspinal analgesia

 B

Respiratory depression

 C

Euphoria

 D

Reduced intestinal motility

Ans. A

Explanation:

Ans. is ‘a i.e., Supraspinal analgesia

(Mu)

o Analgesia (spinal + supraspinal) o Respiratory depression

o Euphoria

  • Reduced G1 motility
  • Sedation
  • Miosis
  • Physical dependence
  • Increased feeding

1c (Kappa)

  • Analgesia (spinal + Supraspinal)
  • Respiratory depression (lower ceiling)
  • Dysphoria

o Reduced GI motility

  • Sedation
  • Diuresis
  • Increased feeding
  • Psychomimetic effects

S (Delta)

  • Analgesia (spinal + Supraspinal)
  • Modulation of GH & DA release
  • Increased feeding

a (sigma) receptor (nonpioid receptor) mediates naloxone insensitive effects of pentazocine, e.g., dysphoria, psychomimetic action, tachycardia and mydriasis.

Remember

o Psychomimetic effects (hallucinations, anixety and night mares) of agonist-antagonists (nalbuphine, dezocine) are due to K receptors.

o Certain endogenous peptides (endrophins, enkephalins and dynorphins) act on these opioid receptors and produce analgesia.

o A new endogenous peptide nociception has been isolated which acts on orphanin like receptors (ORLs) or nociception/orphanin fQ (N/oFQ) receptors.

o Endorphins have major action on receptors.

o Enkephalins have major action on 6 receptors.

o Dynorphins have major action on x receptors.


Q. 29

Buprenorphine is partial agonist of-

 A

Mu ( ) receptor

 B

Delta (d) receptor

 C

Kappa (K) receptor

 D

Sigma (σ) receptor

Q. 29

Buprenorphine is partial agonist of-

 A

Mu ( ) receptor

 B

Delta (d) receptor

 C

Kappa (K) receptor

 D

Sigma (σ) receptor

Ans. A

Explanation:

Ans. is ‘a’ i.e., Mu ( ) receptor

Nature of interaction of opioid ligands with the three major types of opioid receptors, along with equivalent analgesic doses

Ligand

(mu)

lc (kappa)

S (delta)

Analgesic dose (mg)

1. Morphine

Ago. (St)

Ago. (W)

Ago. (W)

10

2. Nalorphine

Anta. (St)

Ago. (M)

 

 

3. Pentazocine

P. Ago., Anta. (W)

Ago. (M)

 

30-60

4. Butorphanol

P. Ago. (W)

Ago. (St)

 

1-3

5. Buprenorphine

P. Ago.

Anta. (M)

 

0.3-0.4

6. Naloxone

Anta. (St)

Anta. (M)

Anta. (W)

 

7. Naltrexone

Anta. (St)

Anta. (M)

Anta. (W)

 

8. Met/Leu enkephalin

Ago. (M)

 

Ago. (St)

 

9. (3-Endorphin

Ago. (St)

 

Ago. (St)

 

10. Dynorphin A, B

Ago. (W)

Ago. (St)

Ago. (W)

 


Q. 30

Buprenorphine is calssified as –

 A

Partial agonist at μ receptor

 B

Partial agonist at K receptor

 C

Full agonist at μ receptor

 D

Full agonist at K receptor

Q. 30

Buprenorphine is calssified as –

 A

Partial agonist at μ receptor

 B

Partial agonist at K receptor

 C

Full agonist at μ receptor

 D

Full agonist at K receptor

Ans. A

Explanation:

Ans. is ‘a’ i.e., Partial agonist at receptor

o Buprenorphine is partial agonist on mu receptor and antagonist at Kappa receptor.

Quiz In Between


Q. 31

Opioid agonist-antagonist is

 A

Pethidine

 B

Pantazocine

 C

Buprenorphine

 D

Methadone

Q. 31

Opioid agonist-antagonist is

 A

Pethidine

 B

Pantazocine

 C

Buprenorphine

 D

Methadone

Ans. B

Explanation:

Ans. is ‘b’ i.e., Pantazocine

  1. Agonist-antagonists (k analgesics) – Nalorphine, Pentazocine, Butorphenol.
  2. Partial/weak agonist + x antagonist – Buprenorphine.
  3. Pure antagonists – Naloxone, Naltrexone, Nalmefene.

o Clinically agonist – Antagonists and partial/weak agonists are analgesics of comparable efficacy to low doses of morphine and they cause low ceiling respiratory depression, and have lower abuse potential.

  • Important points about specific agents.

Butorphanol (partial agonist & weak antagonsit, x agonist)

o Analgesia and respiratory depression have a lower ceiling.

o It causes equivalent analgesia but more sedation than morphine.

  • The most outstanding feature is that butorphanol can neither substiture for nor antagonize morphine —› weak interaction with receptors.

Q. 32

Which drug has ceiling effect –

 A

Morphine

 B

Pethidine

 C

Fentanyl

 D

Buprenorphine

Q. 32

Which drug has ceiling effect –

 A

Morphine

 B

Pethidine

 C

Fentanyl

 D

Buprenorphine

Ans. D

Explanation:

Ans. is ‘d’ i.e., Buprenorphine

Ceiling effects

o A particular effect of drug increases with increasing the dose of drug. However, with some opioids (particularly agonist-antagonist) when the ceiling (roof) is reached further increment in dose not result in increase in effect. Ceiling effect is particularly seen on respiratory depression, i.e., higher doses do not produce further respiratory depression.


Q. 33

One of the followig opioid derivatives is a partial agonist as well as antagonist-

 A

Buprenorphine

 B

Naloxone

 C

Nalorphine

 D

Naltrexone

Q. 33

One of the followig opioid derivatives is a partial agonist as well as antagonist-

 A

Buprenorphine

 B

Naloxone

 C

Nalorphine

 D

Naltrexone

Ans. C

Explanation:

Ans. is ‘c’ i.e., Nalorphine

Quiz In Between


Q. 34

Which analgesic is not used in Acute myocardial infarction –

 A

Morphine

 B

Pentazocine

 C

Pethidine

 D

Buprenorphine

Q. 34

Which analgesic is not used in Acute myocardial infarction –

 A

Morphine

 B

Pentazocine

 C

Pethidine

 D

Buprenorphine

Ans. B

Explanation:

Ans. is ‘b’ i.e., Pentazocine

Its use is associated with tachycardia & rise in BP is due to sympathetic stimulation. This increases cardiac work and hence is better avoided in coronary ischemia and myocardial infarction.

Note – Petnidine also causes tachycardia (anticholinergic action) —> contraindicated in MI.


Q. 35

True about Dezocine –

 A

Slower acting than morphine

 B

Less potent than morphine

 C

Acts via GABA

 D

Doesn’t increase histamine release

Q. 35

True about Dezocine –

 A

Slower acting than morphine

 B

Less potent than morphine

 C

Acts via GABA

 D

Doesn’t increase histamine release

Ans. D

Explanation:

Ans. is ‘d’ i.e., Doesn’t increase histamine release

Dezocine

Dezocine is an opioid agonist-antagonist.

o Its analgesic potency, onset and duration of action in the relief of postoperative pain are comparable to morphine. o It has no effect on histamine and catecholamines secretion.

o Like other agonist-antagonist it exhibits ceiling effect for respiratory depression.

  • It has a high affinity for receptors and moderate affinity for 8 receptors.

Q. 36

Drug that should not be given with Apomorphine is?

 A

Dopamine agonist

 B

Spironolactone

 C

Ondansetron

 D

Aspirin

Q. 36

Drug that should not be given with Apomorphine is?

 A

Dopamine agonist

 B

Spironolactone

 C

Ondansetron

 D

Aspirin

Ans. C

Explanation:

Ans. is ‘c’ i.e., Ondansetron

Apomorphine

o Apomorphine is a dopamine agonist. It is a semisynthetic derviative of morphine and acts as a dopaminergic agonist on CTZ.

o It is indicated for the actue, dintermittent treatment of hypomotility and off episodes in advanced Parkinson’s disease.

o The precise mechanism of action of apomrphine is not known; it is believed to be due to the stimulation of postsynaptic dopamine D, type receptors within the caudate-pautamen in the brain.

o Apomorphine is contraindicated in patients with a hypersensitivity to apomorphine or its ingredients (metabisulfite).

o The concomittant use of apomorphine with 5-HT? antagonist drugs (ondansetron)grainsetron, dolastron, palonasetron and alosetron) is contraindicated because of profound hypotension and loss of consciousness.

o Potential side-effect of apomorphine include dopaminergic effects such as nausea, orthostatic hypotension or somnolence. Other effects are bruising, itching, pain, swelling, or redness at injection site; dizziness; drowsiness; flushing; headache; nausea; pale skin; runny nose; vomiting; and yawing.

Quiz In Between


Q. 37

Drug contraindicated in renal failure is

 A

Morphine

 B

Pethidine

 C

Fentanyl

 D

Alfentanil

Q. 37

Drug contraindicated in renal failure is

 A

Morphine

 B

Pethidine

 C

Fentanyl

 D

Alfentanil

Ans. B

Explanation:

B i.e. Pethidine

Meperidine (pethidine, demerol), a phenylpiperidine is metabolized chiefly in liver to nonmeperidine, which is eliminated by the kidney and liver. In patients or addicts who are tolerant to the depressant effects of meperidine, large doses repeated at short interval may produce an excitatory syndrome including hallncination, tremors, muscle twitches, dilated pupils, hyperactive reflexes and convulsions. These excitatory symptoms are d/t accumulation of normeperidine, which has a half life of 15-20 hours, compared to 3 hours for meperidine. In patients with cirrhosis, the bioavailability of meperidine is –80% increased and t1/2 of both meperidine and normeperidine are prolonged.

Since normeperidine is eleminated by kidney and liver, decreased renal or hepatic function predispose to neurotoxic effects of nor-meperidineQ. Meperidine is also not recommended for the treatment of chronic pain b/o concerns of metabolite toxicity. It should not be used for longer than 48 hours or in doses > 600 mg/day.

Major pathway for morphine metabolism is conjugation with glucuronic acid forming morphine -6- glucuronide and morphine -3- glucuronide. Morphine-6-glucuronide is twice as potent as morphine with somewhat longer t1/2. (t1/2 of morphine is 2 hours) and pharmacological actions indistinguishable from those of morphine. With chronic morphine administration, the 6-glucuronide accounts for most of analgesia and its blood levels exceed those of morphine. Morphine-6-glucuronide is excreted by kidney, so its levels increase in renal failure, perhaps explaining morphine’s potency and long action in compromised renal function. So in patients with renal failure decreased protein binding of morphine (resulting in higher plasma free drug level) and accumulation of morphine -6- glucuronide predispose them to respiratory depression. So morphine is given cautiously in low doses in renal failure.

Respiratory depression is also reported in patients with CRF receiving sufentanyl. Except for slightly decreased protein binding, the free drug volume of distribution and clearance of alfentanil appears to be unaffected by renal failure. Fentanyl, has short half life and its metabolites are inactive. Therefore, it is a good choice in patients with renal diseaseQ.

In renal disease (renal failure) remifentanil > fentanyl > alfentanil > sufentanil are safe. Whereas morphine (d/t morphine 6 glucoronide) 1/t respiratory depression is used very cautiously in low dose and meperidine (pethidine) is contraindicated d/t very long acting metabolite nor-meperidine causing neurotoxic excitatory syndrome.


Q. 38

Which of the following agents is used for the treatment of postoperative shivering?

 A

Thiopentone

 B

Suxamethonium

 C

Atropine

 D

Pethidine

Q. 38

Which of the following agents is used for the treatment of postoperative shivering?

 A

Thiopentone

 B

Suxamethonium

 C

Atropine

 D

Pethidine

Ans. D

Explanation:

D i.e. Pethidine 

• In anaesthesia, shivering occurs as a protective mechanism as inhalational agents, spinal/epidural block causes vasodilatation leading to heat loss. Shivering can be abolished by inhibition of hypothalamus.

  • Halothane most commonly leads to shivering.
  • Treatment of shivering

1. Pethidine or pentazocineQ

2. Oxygen inhalation. Oxygen consumption may increase upto 4 times (400%) during shivering. So oxygen inhalation during shivering is mandatory.


Q. 39

Narcotic of choice for out patient anesthesia: 

 A

Morphine

 B

Alfentanyl

 C

Fentanyl

 D

Pethidine

Q. 39

Narcotic of choice for out patient anesthesia: 

 A

Morphine

 B

Alfentanyl

 C

Fentanyl

 D

Pethidine

Ans. B

Explanation:

B i.e. Alfentanyl

All of these are short acting narcotic analgesics the shortest acting among them is Remifentanil.

 

Drug

Onset

Duration of action

Remifentanil

30 – 60 second

3 – 5 minute

Alfentanil

0.5 minute

5 – 10 minute

Fentanyl &

Sufentanil

1 – 4 minute

30 minute .

–  Remifentanyl, Alfentanyl & Sufentanil have short duration of action so can be used as outpatient anesthetic agents.

Desflurane & Sevoflurane provide the fastest wake up time among volatile anesthetic outpatient agents.

Quiz In Between


Q. 40

All are opioid agonist – antagonist compounds except

 A

Buprenorphine

 B

Nalbuphine

 C

Pentazocine

 D

Nalmefene

Q. 40

All are opioid agonist – antagonist compounds except

 A

Buprenorphine

 B

Nalbuphine

 C

Pentazocine

 D

Nalmefene

Ans. D

Explanation:

D i.e. Nalmefene


Q. 41

Which of these is not an opioid agonist:

AIIMS 10

 A

Heroin

 B

Ketamine

 C

Methadone

 D

Fentanyl

Q. 41

Which of these is not an opioid agonist:

AIIMS 10

 A

Heroin

 B

Ketamine

 C

Methadone

 D

Fentanyl

Ans. B

Explanation:

Ans. Ketamine


Q. 42

A 28-year-old male patient is brought to casualty in comatose state with pin-point pupils, reduced respira- tory rate and bradycardia. Most likely diagnosis:

UPSC 09; CMC (Vellore) 14

 A

Tricyclic antidepressant poisoning

 B

Opioid poisoning

 C

Benzodiazepine poisoning

 D

Organophosphorus poisoning

Q. 42

A 28-year-old male patient is brought to casualty in comatose state with pin-point pupils, reduced respira- tory rate and bradycardia. Most likely diagnosis:

UPSC 09; CMC (Vellore) 14

 A

Tricyclic antidepressant poisoning

 B

Opioid poisoning

 C

Benzodiazepine poisoning

 D

Organophosphorus poisoning

Ans. B

Explanation:

Ans. Opioid poisoning

Quiz In Between


Q. 43

All are true of opioid withdrawal, except:

NIMHANS 10; PGI 14

 A

Yawning

 B

Hallucinations

 C

Lacrimation

 D

Piloerection

Q. 43

All are true of opioid withdrawal, except:

NIMHANS 10; PGI 14

 A

Yawning

 B

Hallucinations

 C

Lacrimation

 D

Piloerection

Ans. B

Explanation:

Ans. Hallucinations


Q. 44

Usual sign of opioid withdrawal:   

PGI 13

 A

Stupor

 B

Constipation

 C

Constricted pupil

 D

Yawning

Q. 44

Usual sign of opioid withdrawal:   

PGI 13

 A

Stupor

 B

Constipation

 C

Constricted pupil

 D

Yawning

Ans. D

Explanation:

Ans. Yawning


Q. 45

The drug which is used for long-term maintenance in opioid addiction:           

AIIMS 06; Punjab 09; AI 11

 A

Nalorphine

 B

Naloxone

 C

Butarphanol

 D

Methadone

Q. 45

The drug which is used for long-term maintenance in opioid addiction:           

AIIMS 06; Punjab 09; AI 11

 A

Nalorphine

 B

Naloxone

 C

Butarphanol

 D

Methadone

Ans. D

Explanation:

Ans. Methadone

Quiz In Between


Q. 46

Methadone is used to treat withdrawal symptoms of:

PGI 12; NEET 13

 A

Cocaine

 B

Heroin

 C

Amphetamine

 D

Barbiturate

Q. 46

Methadone is used to treat withdrawal symptoms of:

PGI 12; NEET 13

 A

Cocaine

 B

Heroin

 C

Amphetamine

 D

Barbiturate

Ans. B

Explanation:

Ans. Heroin


Q. 47

Buprenorphine partial agonist at which opioid receptor?

 A

Mu

 B

Kappa

 C

Delta

 D

Lambda

Q. 47

Buprenorphine partial agonist at which opioid receptor?

 A

Mu

 B

Kappa

 C

Delta

 D

Lambda

Ans. A

Explanation:

Ans. is ‘a’ i.e., Mu

Buprenorphine is partial agonist on mu receptor and antagonist at Kappa receptor.


Q. 48

Sufentanil is a/an –

 A

Analgesic

 B

Antibiotic

 C

Anticholinergc

 D

Newer antihistaminic

Q. 48

Sufentanil is a/an –

 A

Analgesic

 B

Antibiotic

 C

Anticholinergc

 D

Newer antihistaminic

Ans. A

Explanation:

Ans. is ‘a’ i.e., Analgesic

Quiz In Between


Q. 49

Treatment in post operative shivering‑

 A

Pethidine

 B

Piritramide

 C

Methadone

 D

Pentazocine

Q. 49

Treatment in post operative shivering‑

 A

Pethidine

 B

Piritramide

 C

Methadone

 D

Pentazocine

Ans. A

Explanation:

Ans. is ‘a’ i.e., Pethidine

Post-anaesthesia shivering (PAS)

  • Post anaesthesia (post operative) shivering occurs in 40% of patients recovering from general anaesthesia.
  • Some time it is preceded by central hypothermia and peripheral vasoconstriction, indicating that it is a thermoregulatory mechanism
  • Pethidine is most effective drug for treatment of PAS.
  • Other drugs used are –clonidine, doxapram, ketanserin, alfentonil, butorphanol, chlorpromazine.

Q. 50

All are used for treatment of morphine dependence except ‑

 A

Methadone

 B

Clonidine

 C

Naltreoxone

 D

Disulfiram

Q. 50

All are used for treatment of morphine dependence except ‑

 A

Methadone

 B

Clonidine

 C

Naltreoxone

 D

Disulfiram

Ans. D

Explanation:

Ans. is ‘d’ i.e., Disulfiram

Treatment of morphine or heroin poisoning

  • Treatment can be divided into :‑

A.Treatment of toxicity (overdose)

  • Overdose is a medical emergency, and is treated with opioid antagonist to reverse the complications (respiratory depression) by antagonizing the action on opioid receptors. Intravenous naloxone is the antagonist of choince for morphine (heroin) poisoning. Oral naltrexone is used for maintenance therapy, once acute poisoning has been treated by iv naloxone. Intravenous nalmefene is another specific antagonist.

A.Treatment of dependence

  • Treatment of dependence include medically supervised withdrawal and detoxification, followed by maintenance therapy :

a. Detoxification

  • Detoxification process include abrupt withdrawal of opioid followed by management of the emergent withdrawal symptoms, i.e., treatment of withdrawal syndrome. Detoxification can be done by any of the following :
  1. Substitution of long-acting opioid agonism :- Methadone is the treatment of choice. Because of its agonistic activity on opioid receptors it suppresses withdrawal symptoms. L-alpha-acetyl­methadol/Levomethyl (LAAM) is the other opioid agonist which was used for this purpose. However it is no longer in use because some patients developed prolonged QT intervals (torsades de points).
  2. Substitution of partial agonist Buprenorphine can be used in place of methadone because of its partial agonistic activity on opioid receptor.
  3. Substitution by a2 agonists Clonidine acts as a sympatholytic agent due to its agonistic action on central presynaptic a2 receptors which reduce nor-adrenergic activity. Therefore, clonidine reduces the adrenergic withdrawal symptoms. Lofexidine another a2 agonist, is an alternative to clonidine.
  4.  Clonidine plus naltrexone :- A more rapid detoxification can occur when clonidine is used along with naltrexone. Naltrexone, when given in opioid dependent patient, causes withdrawal symptoms because of its antagonistic action. These can be treated with clonidine. The addition of short acting Benzodiazepine (lorazepam or oxazepam) and NSAIDs, will help relieve withdrawl
  5. symptoms not covered by clonidine. It should be kept in mind that naltrexone should not be used alone for detoxification (to treat withdrawl syptoms) as it precipitates or worsens the withdrawl syndrome.
  6. 5.0ther drugs :- Dextropropoxyphene, diphenoxylate

b. Maintenance therapy

  • Once detoxification phase is over (i.e., withdrawal symptoms have been managed), the patient is maintained on any of the following drugs to prevent relapse by reducing craving and preventing `kick’ or ‘euphoria’ produced by opioids (morphine or heroin). Drugs used are :-
  1. 1.Methadone :- Reduces craving and `kick/euphoria’ from morphine or heroin because their opioid receptors are already occupied.
  2. 2.LAAM and buprenorphine :- Similarly reduce craving.
  3. 3.Opioid antagonists (naltrexone) Naltrexone can be used orally to assist in the rehabilitation of ex-opioid abusers who are fully withdrawn (otherwise it induces an acute withdrawl syndrome). Naltrexone prevents relapse by discouraging substance seeking behavior —) If a patient, who is on naltrexone maintenance therapy, takes an opioid, there is no ‘kick’ or ‘euphoria’ as opioid receptors are already blocked. Naltrexone can be used with clonidine as in detoxification.

Q. 51

Drug of choice for substitution therapy in morphine dependence-

 A

Methadone

 B

Clonidine

 C

Naloxone

 D

Nalmefene

Q. 51

Drug of choice for substitution therapy in morphine dependence-

 A

Methadone

 B

Clonidine

 C

Naloxone

 D

Nalmefene

Ans. A

Explanation:

Ans. is ‘a’ i.e., Methadone

Quiz In Between


Q. 52

Drug used for post-operative shivering ‑

 A

Atropine

 B

Pethidine

 C

Thiopenone

 D

Suxamethonium

Q. 52

Drug used for post-operative shivering ‑

 A

Atropine

 B

Pethidine

 C

Thiopenone

 D

Suxamethonium

Ans. B

Explanation:

Ans. is ‘b’ i.e., Pethidine

Post-anaesthesia shivering (PAS)

  • Post anaesthesia (post operative) shivering occurs in 40% of patients recovering from general anaesthesia.
  • Some time it is preceded by central hypothermia and peripheral vasoconstriction, indicating that it is a thermoregulatory mechanism.
  • Pethidine is most effective drug for treatment of PAS.
  • Other drugs used are -clonidine, doxapram, ketanserin, alfentonil, butorphanol, chlorpromazine.

Q. 53

High dose of morphine is used without much danger in ‑

 A

Gall bladder surgery 

 B

Labour

 C

Myocardial infarction 

 D

Head injury

Q. 53

High dose of morphine is used without much danger in ‑

 A

Gall bladder surgery 

 B

Labour

 C

Myocardial infarction 

 D

Head injury

Ans. C

Explanation:

 Ans. is ‘c’ i.e., Myocardial infarction 

  • Morphine should be given promptly in myocardial infarction to allay apprehension and reflex sympathetic stimulation.

About other options

  • Morphine should be used cautiously in gall bladder and biliary tract dysfunction as it causes spasm of sphincter of oddi and can cause acute rise of intrabiliary pressure.
  • Used during labour, morphine can cause neonatal respiratory distress.
  • Head injury is a contraindication for morphine use.

Precautions and contraindications of Morphine:

1. Head injury : morphine is contraindicated in patients with head injury (KDT). Reasons are ‑

  • By retaining CO2 it increases intracranial tension which will add to that caused by head injury itself.
  • Even therapeutic doses can cause marked respiratory depression in these patients.
  • Vomiting, miosis, and altered mentation produce by morphine interfere with assessment of progress in head injury cases.
  1. Branchial asthma: Morphine can precipitate an attack by its histamine releasing action.
  2. Hypothyroidism, liver and kidney disease patients are more sensitive to morphine
  3. Infants and elderly are more susceptible to the respiratory depressant action of morphine.
  4. It is dangerous in patients with respiratory insufficiency (Emphysema, pulmonary fibrosis, corpulmonale), sudden deaths have occurred.
  5. Hypotensive states and hypovolemia exagerate fall in BP due to morphine.
  6. Undiagnosed acute abdominal pain —> morphine can aggravate certain conditions e.g., diverticulitis, biliary colic, pancreatitis.
  7. Elderly male —> chances of urinary retention are high.
  8. Unstable personalities –> are liable to continue its use and become addicted.

Q. 54

Antitussive opioid is ‑

 A

Ethylmorphin

 B

Pethidine

 C

Methadone

 D

Buprenorphine

Q. 54

Antitussive opioid is ‑

 A

Ethylmorphin

 B

Pethidine

 C

Methadone

 D

Buprenorphine

Ans. A

Explanation:

Ans. is ‘a’ i.e., Ethylmorphine

Antitussives (cough center suppressants)

  • Opioids : Codeine, ethylmorphine, pholcodeine.
  • Non-opioids : Noscapine, dextro methorphan, chlophedianol.
  • Antihistaminics : Chlorpheniramine, diphenhydromine, promethazine.
  • Peripherally active : Prenoxdiazine.

Q. 55

Morphine ‑

 A

Stimulates CTZ zone of medulla

 B

Stimulates respiratory centre of medulla

 C

Depresses CTZ zone of medulla

 D

None of the above

Q. 55

Morphine ‑

 A

Stimulates CTZ zone of medulla

 B

Stimulates respiratory centre of medulla

 C

Depresses CTZ zone of medulla

 D

None of the above

Ans. A

Explanation:

Ans. is ‘a’ i.e., Stimulates CTZ zone of medulla

Quiz In Between



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