Pain Management Medications Flashcards
Paracetamol is a pain reliever medication that can be analgesic (pain reliever) and antipyretic (reduces fever). Why are paracetamols not considered as NSAIDs?
- works almost entirely in the CNS
- as it works on the CNS is does not have anti-inflammatory effects
Paracetamol is a pain reliever medication that can be analgesic (pain reliever) and antipyretic (reduces fever). Paracetamols are not considered as NSAIDs because they have no anti-inflammatory properties. What is the mechanism of action of paracetamol?
- reversible inhibition of COX 1 and 2
- COX 1 and 2 create prostaglandins
Paracetamol is a pain reliever medication that can be analgesic (pain reliever) and antipyretic (reduces fever). Paracetamols are not considered as NSAIDs because they have no anti-inflammatory properties. Paracetamol inhibits COX 1 and 2 which create prostaglandins. How do prostaglandins then cause pain and fever?
- cause hypersensitivity of nociceptors to pain
- stimulate the hypothalamus and an increase in temperature
Ibuprofen is non-steroidal anti-inflammatory drug (NSAID). When we talk about pain medication, ibuprofen has anti-inflammatory, analgesic (pain relief) and antipyretic (reduce fever) properties. What is the mechanism of action of ibuprofen?
- non-selective, meaning it will bind and inhibit any COX
- competitively binds and inhibits COX-1 and COX-2 which is reversible
COX- 1 and COX-2 create prostaglandin E2 (PGE2) and prostacyclin (PGI2). These are lipids that are able to induce effects when we cause damage to tissue in the body. How do these lipids cause pain, inflammation and fever?
- cause hypersensitivity of nociceptors to pain by increasing Na+/Ca2+ influx
- stimulate the hypothalamus and an increase in temperature
- cause vasodilation and thus inflammation
What class of drug is ibuprofen?
- non-steroidal anti-inflammatory drug (NSAID)
Ibuprofen is non-steroidal anti-inflammatory drug (NSAID). When we talk about pain medication, what 3 things is Ibuprofen able to treat?
- anti-inflammatory
- analgesic (pain relief)
- antipyretic (reduce fever)
Ibuprofen is non-steroidal anti-inflammatory drug (NSAID). When we talk about pain medication, ibuprofen has anti-inflammatory, analgesic (pain relief) and antipyretic (reduce fever) properties. Ibuprofen reversibly competitively binds and is non-selective, meaning it will bind and inhibit any COX, hence the reason it inhibits both COX-1 and COX-2. COX-1 activity is constitutive, meaning that it is always active and has important physiological properties. Why is the inhibition of COX-1 long term not a good thing in the stomach?
- COX-1 produces prostaglandin E2 (PGE2) which is important for mucus production in stomach
- long term used of Ibuprofen reduces mucus production and increases risk of ulcers
Ibuprofen is non-steroidal anti-inflammatory drug (NSAID). When we talk about pain medication, ibuprofen has anti-inflammatory, analgesic (pain relief) and antipyretic (reduce fever) properties. Ibuprofen reversibly competitively binds and is non-selective, meaning it will bind and inhibit any COX, hence the reason it inhibits both COX-1 and COX-2. COX-1 activity is constitutive, meaning that it is always active and has important physiological properties. Why is the inhibition of COX-1 long term not a good thing in the kidneys?
- COX-1 produces prostaglandin E2 (PGE2) and prostocyclin (PGI2)
- PGE2 and PGI2 are vasodilators
- without vasodilation kidney blood flow will be reduced and lead to CKD
Ibuprofen is non-steroidal anti-inflammatory drug (NSAID). When we talk about pain medication, ibuprofen has anti-inflammatory, analgesic (pain relief) and antipyretic (reduce fever) properties. Ibuprofen reversibly competitively binds and is non-selective, meaning it will bind and inhibit any COX, hence the reason it inhibits both COX-1 and COX-2. COX-1 activity is constitutive, meaning that it is always active and has important physiological properties. Why is the inhibition of COX-1 and 2 a good thing?
- reduces prostaglandin E2 (PGE2) and prostacyclin (PGI2) that can in-turn:
1 - reduces hypersensitivity of nociceptors to pain
2 - reduces the stimulate to the hypothalamus that increases temperature
3 - reduces cause vasodilation and thus inflammation
Ibuprofen is non-steroidal anti-inflammatory drug (NSAID). When we talk about pain medication, ibuprofen has anti-inflammatory, analgesic (pain relief) and antipyretic (reduce fever) properties. Ibuprofen reversibly competitively binds and is non-selective, meaning it will bind and inhibit any COX, hence the reason it inhibits both COX-1 and COX-2. COX-1 activity is constitutive, meaning that it is always active and has important physiological properties (stomach and kidney). COX-2 has inducible activity, meaning it needs to be turned on. When tissue is damaged how is COX-2 turned on?
- COX-2 can be turned on by macrophages, TNF and EGF
Ibuprofen is non-steroidal anti-inflammatory drug (NSAID). When we talk about pain medication, ibuprofen has anti-inflammatory, analgesic (pain relief) and antipyretic (reduce fever) properties. Ibuprofen reversibly competitively binds and is non-selective, meaning it will bind and inhibit any COX, hence the reason it inhibits both COX-1 and COX-2. Does ibuprofen work predominantly peripherally or centrally in the body?
- can be both
- mainly peripherally
What is the main mechanism of action of opioids?
- act as agonist on opioid receptors
- able to bind with K+ receptors on post synapse causing hyperpolarisation
- able to bind with Ca2+ receptors inhibiting release of neurotransmitters from pre-synapse
All opioid receptors are the same. Are they ionotropic or metabotropic?
- metabotropic
- GPCR and all are Gai
All opioid receptors are metabotropic GPCRs. Opioids act as agonist on opioid receptors and the following can occur:
- able to bind with K+ receptors on post synapse causing hyperpolarisation
- able to bind with Ca2+ receptors inhibiting release of neurotransmitters from pre-synapse
Which GPCR do opioids bind to and what is the response of the cell?
- Gai
- inhibit adenylyl cyclase reducing cAMP and PkA
- essentially causes hyperpolarisation and no action potential
Codeine is a weak opioid (weak as it is compared with morphine) and has a ceiling effect, what does this mean?
- increasing the drug concentration no longer provides any analgesic (pain relief) effects
Opioids can lead to tolerance, dependance and addiction and can be toxic. How can patients be treated if opioids become toxic?
- naloxone
- opioid receptor antagonist
- essentially blocks Gai receptors
