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48 Cards in this Set

  • Front
  • Back
NSAIDs inhibit the enzyme ________, they are known as COX-inhibitors.
Cyclooxygenase
Salicylates include ______.
Aspirin
Acetaminophen, Ibuprofen, and Naproxen are referred to as ______ NSAIDs.
Traditional
Traditional NSAIDs were developed after it was discovered that earlier NSAIDs irritated the ________ system and caused ______.
Gastrointestinal
Stomach Bleeding.
What enzyme is required for gastrointestinal function?
Cyclooxygenase-1 (COX-1)
Earlier NSAIDs were nonselective and blocked the _______ enzyme cause significant GI problems.
COX-1
Selectively blocking COX-2 enzymes alleviate pain by reducing the production of _______.
Prostaglandins
COX-2 inhibitors
Celecoxib, Rofecoxib, Valdecoxib
Rofecoxib and Valdecoxib were discontinued after it was discovered to be linked to _______ in patients taking these drugs on daily basis.
Heart attacks
Corticoid steroid are able to inhibit _____ which is why they are widely used as anti-inflammatories.
PLA
Opiates receptors are ______.
They contain _____ transmembrane segments.
Metabotropic
Seven
Nociceptin
(Mu receptors/Delta receptors/Kappa receptors/Nociceptin receptors)
Nociceptin receptor
Naloxone
(Mu receptors/Delta receptors/Kappa receptors/Nociceptin receptors)
Mu receptors
Delta receptors
Kappa receptors
Quinolone
(Mu receptors/Delta receptors/Kappa receptors/Nociceptin receptors)
Nociceptin receptors
Cyprodime
(Mu receptors/Delta receptors/Kappa receptors/Nociceptin receptors)
Mu receptors
Deltorphins
(Mu receptors/Delta receptors/Kappa receptors/Nociceptin receptors)
Delta receptors
Endorphins
(Mu receptors/Delta receptors/Kappa receptors/Nociceptin receptors)
Mu receptors
Naltrexone
(Mu receptors/Delta receptors/Kappa receptors/Nociceptin receptors)
Mu receptors
Delta receptors
Kappa receptors
Enkephalins
(Mu receptors/Delta receptors/Kappa receptors/Nociceptin receptors)
Delta receptors
Dynorphins
(Mu receptors/Delta receptors/Kappa receptors/Nociceptin receptors)
Kappa receptors
Diprenorphine
(Mu receptors/Delta receptors/Kappa receptors/Nociceptin receptors)
Mu receptors
Delta receptors
Kappa receptors
Naltriben
(Mu receptors/Delta receptors/Kappa receptors/Nociceptin receptors)
Delta receptors
Quadazocine
(Mu receptors/Delta receptors/Kappa receptors/Nociceptin receptors)
Kappa receptors
Analgesic effects are mediated by what types of receptors?
Mu receptors
Respiratory suppressant effects are mediated by what types of receptors?
Delta receptors
Sedation effects are mediated by what type of receptors?
Kappa receptors
Sensation of pain are mediated by what types of receptors?
Nociceptin receptors
Appetite suppressant effects are mediated by what types of receptors?
Kappa receptors
Cough suppressant effects are mediated by what types of receptors?
Mu receptors
Antidepressant effects are mediated by what types of receptors?
Delta receptors
COX-2 inhibitors have no effect in the ___ system.
They're active in inflammatory events, and ______ functions.
GI
Cardiovascular
Analgesia and Anti-inflammatory synthesis
PIP2 -----> PLA/corticosteroid inhibition > arachadonic acid ----> COX-1 or COX-2 > prostaglandins: vanilloid receptors, ASICs, etc > free radicals
Opioids antagonist ligands
Naloxone, Naltrexone, Diprenorphine
Opioids endogenous ligands
Endorphins, deltorphins, enkephalins, dynorphins, nociceptin
Endorphins
Endogenous Ligand for Mu receptors
Deltophins and Enkephalins
Endogenous ligands for Delta receptors
Dynorphins
Endogenous ligand for Kappa receptors
Nociceptin
Endogenous ligand for Nociceptin receptors
Exogenous opium alkaloids
Morphine (most potent)
Codeine
Thebaine
Narcotine (weakest)
Papaverine
Modified Opiates
Diacetylmorphine
Hydromorphone
Oxycodone
Hydrocodone
Synthetic Opiates
Buprenophrine
Methadone
Meperidine
Propoxyphene
Fentanyl
Sufentanil
Buprenophrine
Partial Agonist
Long Acting (days)
Methadone
Long Acting (days)
Meperidine
Medium action (hours)
Propoxyophene
Weak
Medium action (hours)
Fentanyl
Short acting (minutes)
Sufentanil
Short acting (minutes)
Opiate antagonist for OD Tx
Naloxone
Naltrexone
Diprenorphine