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