Opioid analgesics 5

Question 1

Physicald depence meaning?

Answer 1

Physiologic state in which a person’s continued use of drug is required for his or her well-being.

Question 2

Depedence represents the establishment of what?

Answer 2

Represent the establishment of a new equilibrium between the neuron and its environment (neuroadaptation), wherein the neuron becomes less responsive to the drug while requiring continued drug effect to maintain cellular homeostasis

Question 3

what happen to depedence if the is abruptly withdrawal of opioids

Answer 3

If abruptly withdrawn, the equilibrium is disturbed and a rebound hyperexcitability occurs owing to the loss of the inhibitory influence of the drug.

Question 4

what is withdrawal syndrome

Answer 4

the manifestations of which depend on drug

Question 5

what happen due to cross-tolerance

Answer 5

Due to cross-tolerance, one opioid drug can substitute for another opioid drug and prevent symptoms of withdrawal in a physically dependent person.

Question 6

The basis for outpatient treatment of opioid dependence by the use of what?

Answer 6

Methadone or buprenorphine

Question 7

List the 2 competitive opioid receptor antagonists

Answer 7

Naloxone
Naltrexone

Question 8

List the indications for Competitive opioid receptor antagonists

Answer 8

Indications:
* Opioid overdose
* Opioid and alcohol dependence
* Decreasing opioid-associated constipation

Question 9

RoA of Naloxone

Answer 9

Administered intravenously to rapidly terminate respiratory depression (after surgery) and other toxic effects of opioid agonists in adults and children, neonate
after delivery and mother had opioids.

Question 10

explain the half-life of Naloxone

Answer 10

Short half-life, repeated doses (every 45 minutes) needed to counteract the effects of the longer-lasting opioid agonists.

Question 11

explain the bioavailability for Naloxone

Answer 11

Low bioavailability and is not effective when given orally, it does not block the effects of the oral opioid but would block opioid effects or even precipitate withdrawal if used by the intravenous route.

Question 12

List the adverse effects of Naloxone

Answer 12

Adverse effects: May precipitate active withdrawal syndrome in opioid dependentmpatient, rarely – sympathetic effects: hypertension, tachycardia, acute pulmonary oedema

Question 13

list the combination products for Naloxone

Answer 13

Combination products:
Oxycodone/naloxone combination: TarginAct®
Used in combination with buprenorphine to treat opioid dependence: Suboxone®

Question 14

explain RoA, half-life and Bioavailabity of Naltrexone

Answer 14

Naltrexone (Naltima®)
Oral formulation and extended-release injectable suspension
High oral bioavailability and longer half-life: used on a long-term basis by opioid addicts who have undergone detoxification and are no longer using opioids

Question 15

Naltrexone is used to treat what?

Answer 15

Used to treat alcohol and opioid dependence (who have been opioid free for 7-10 days).

Question 16

explain the contraindications for Naltrexone

Answer 16

Contraindications: current opioid dependence, acute opioid withdrawal, acute hepatitis, liver failure, pregnancy

Question 17

RoA and indication for Buprenorphine

Answer 17

• Route of administration: sublingual
• Used as monotherapy and in combination with naloxone for both detoxification and maintenance therapy for opioid dependence
• Used for moderate to severe pain

Question 18

Buprenorphine is partial agonist and may precipitate withdrawal symptoms if used with what?

Answer 18

full agonist

Question 19

explain the duration of action for buprenorphine

Answer 19

Long duration of action and analgesic potency 25-40 times that of morphine

Question 20

Buprenorphine is potent to ?

Answer 20

Potent Mu-receptor partial agonist, weak kappa agonist, and deltaopioid antagonist.

Question 21

Lng acting opioid agonist

Answer 21

Methadone

Question 22

when to use Methadone

Answer 22

Used as substitution therapy for opioid addicts (do not produce euphoria)

Question 23

Explain the dosage of methadone

Answer 23

Administered as single or divided doses and tapered according to clinical response and supervised consumption is important.