Opiod Analgesics Flashcards
Opium is derived from plants called
Opium poppy ( papaver seminiferous)
What is an opium
A dried powder mixture of 20 alkaloids that is obtained from the unripe seeds of opium poppy
The opium is classified into two groups which are
Phenanthrene
Benzoisoquinoline
The phenathrene alkaloids include
Morphine (10%)
Thebaine(0.2%)
Codeine( 0.5%)
The phenathrene alkaloids include
Morphine (10%)
Thebaine(0.2%)
Codeine( 0.5%)
The benzoisoquinoline include
Papaverine(1%)
Noscapine(6%)
The opiods can produce ……… effects in the body
Analgesia
Relief from diarrhoea
Euphoria
Sedation
Cough suppression
Classes of synthetic opiods are
Morphinan
Benzomorphan
Phenylpiperidine
Diphenylheptane
Opiods that are morphinans include
Levophanol
Butorphanol
The benzomorphans are
Pentazocine
Phenazocine
The phenylp8peridines are
Fentanyl
Afentanil
Remifentanil
Miperidine
Sufentanil
Diphenoxylate
The phenylheptylamines are
Propoxpynes
Methadone
The mixed opiods are
Morphinan
Butorphanol
Benzomorphan
Pentazocine
Miscellaneous
Tramadol
Tapentadol
Phenanthrene
Nalbuphine
Buprenorphine
Which of the opioid receptor is regarded as the one responsible for majority of the side effects associated with opioids
Sigma receptor
The sigma receptor is regarded more as a ……….. receptor rather than an opioid
Phenylcyclidine
The first tissue where the opioid receptor was first isolated is……..
Vas deferense
The first ligand to act on the opioid receptor is ………..
Ketocyclazocine
What is Nociceptin
NOP OP4
Non opioid branch of opiod receptor
Site spinal cord and brain
Adverse effect
Depression
Anxiety
Appetite
Development of tolerance to u agonist.
All endogenous ligands are similar because
- They are formed from a large polypeptide precursor
- They act in small quantity
- Their activity is antagonised by naloxone
- They bind with high affinity to the opioid receptor
List the endogenous ligand their precursors and receptor they work on
Enkephalin ( leu and met) ; pro-enkephalin DOP
Dynorphin(A and B); pro-dynorphin
KOP
Endomorphin 1 and 2: unknown
B endorphin ; pro-opiomelacortin
MOP
The overall effect of opioids include
Reduction in cAMP
Hyperpolarisation of the cell.
Decrease in neurotransmitter release by neural cells
What percentage of morphine is excreted unchanged in the liver
10%
Patients with Hepatic and renal insufficiency are administered……… doses
Lower doses 1/2 -1/4
Morphine reduces peristalsis through stimulation of what receptors
M and and D
The route of administration for morphine include
Oral
IM
IV
Intrathecal
Rectal
Nebulized
Transdermal patch
Fentanyl has a …… duration of action and ……… potency compared to morphine
Shorter action
Higher potency
Fentanyl is better administered through which routes in emergency cases
Trandermal
Subcutaneous