MOA - Pain/GU Flashcards
Baclofen
Inhibits both monosynaptic and polysynaptic reflexes at the spinal level, possibly by hyperpolarization of afferent terminals, although actions at supraspinal sites may also occur and contribute to its clinical effect. Is an analogue of γ-aminobutyric acid (GABA), but there is no conclusive evidence that actions on GABA systems are involved in the production of its clinical effects
Buprenorphine/Naloxone
One component is a μ-opioid receptor partial agonist and a -opioid receptor antagonist. The other component is a μ-opioid receptor antagonist that causes opioid withdrawal when injected parenterally and is included in the formulation to reduce the risk of abuse.
Carisoprodol
blocks interneuronal activity in descending reticular formation and spinal cord, resulting in muscle relaxation
Celecoxib
Inhibition of the COX-2 enzyme isoform is thought to be responsible for the anti-inflammatory effects of NSAIDs.
Codeine/Acetaminophen
3-methylmorphine, a phenanthrene opioid with very low affinity for opioid receptors. Its analgesic activity appears to result from conversion to morphine.
Cyclobenzaprine
reduction in tonic motor activity, influencing both gamma (γ) and alpha (α) motor systems.
Diclofenac
Nonselective inhibitor of cyclo-oxygenase-1 (COX-1) and cyclo-oxygenase-2 (COX-2).
Etodolac
Nonselective inhibitor of cyclo-oxygenase-1 (COX-1) and cyclo-oxygenase-2 (COX-2) and reversibly alters platelet function and prolongs bleeding time
Fentanyl Transdermal
Phenylpiperidine opioid agonist with predominant effects on mu-opioid receptors, about 50-100 times more potent than morphine
Hydrocodone (w/o acetaminophen)
Binds to opiate receptors, resulting in altered perception of pain
Ibuprofen
Nonselective inhibitor of COx-1 and Cox-2 and reversibly alters platelet function and prolongs bleeding time
Indomethacin
Nonselective inhibitor of COX-1 and COX-2, and reversibly alters platelet function and prolongs bleeding time.
Lidocaine
amide-type local anesthetic agent and is suggested to stabilize neuronal membranes by inhibiting the ionic fluxes required for the initiation and conduction of impulses. The penetration of lidocaine in patch form into intact skin is sufficient to produce an analgesic effect but less than the amount necessary to produce a complete sensory block.
Meloxicam
Nonselective inhibitor of COX-1 and COX-2 which results in decreased formation of prostaglandin precursors; has antipyretic, analgesic, and anti-inflammatory properties; reversibly alters platelet function and prolongs bleeding time.
Methadone
Binds to opiate receptors in CNS, causing inhibition of ascending pain pathways, alterings perception to pain, and producing generalized CNS depression.
Methocarbamol
not been established but may be due to general CNS depression. It has no direct action on the contractile mechanism of striated muscle, the motor end plate, or the nerve fiber
Morphine
pure mu agonist, decreases brain stem respiratory centers’ response to carbon dioxide tension and electrical stimulation, decreases gastric, biliary, and pancreatic secretions, induces peripheral vasodilation, promotes opioid-induced hypotension due to histamine release
Nabumetone
Prodrug, converted into 6-methoxy-2-naphthylacetic acid (6MNA), a nonselective inhibitor of cyclo-oxygenase-1 (COX-1) and cyclo-oxygenase-2 (COX-2) that reversibly alters platelet function and prolongs bleeding time
Naproxen
Nonselective inhibitor of COX-1 and COX-2
Oxycodone
A pure mu agonist. Mu receptors are responsible for analgesia, respiratory depression, miosis, decreased GI motility, and euphoria. In the CNS, it promotes analgesia and respiratory depression by decreasing the brainstem respiratory centers’ response to carbon dioxide tension and electrical stimulation. It also decreases gastric, biliary, and pancreatic secretion, induces peripheral vasodilation, and promotes opioid-induced hypotension due to histamine release.
Pentosan
low-molecular-weight heparin-like compound. The mechanism of action of pentosan in relieving pain associated with interstitial cystitis is not known, but it has been found to adhere to the mucosal membrane of the bladder wall and may act as a buffer to control cell permeability, which prevents irritating solutes in urine from reaching the cells.
Tramadol
A mu agonist and a weak inhibitor of serotonin and norepinephrine reuptake. Mu receptors are responsible for analgesia, respiratory depression, miosis, decreased GI motility, and euphoria. In the CNS, it promotes analgesia and respiratory depression by decreasing brainstem respiratory centers’ response to carbon dioxide tension and electrical stimulation.
Tizanidine
A centrally acting muscle relaxant. The drug is an imidazole derivative, structurally unrelated to other muscle relaxants. Tizanidine is an agonist of α2-adrenergic receptors, which decreases spasticity by increasing presynaptic inhibition; however, it does not have antihypertensive properties.
Darifenacin
competitive muscarinic receptor antagonist
Dutasteride
Inhibits conversion of testosterone to 5 alpha-dihydrotestosterone (DHT) by 5 alpha-reductase isoform 1 and 2
Finasteride
Inhibits the conversion of testosterone to 5 alpha-dihydrotestosterone (DHT) by 5 alpha-reductase, isoform 2
Mirabegron
Activates B-3 adrenergic receptor causing relaxation of detrusor muscle and icnreasing bladder capacity
Oxybutynin
A competitive muscarinic receptor antagonist. Muscarinic receptors play an important role in several major cholinergically mediated functions, including contractions of the urinary bladder smooth muscle and stimulation of salivary secretion.
Sildenafil
Inhibition of phosphodiesterase type 5 (PDE5) by sildenafil increases the amount of cyclic guanosine monophosphate (GMP) enhancing erectile function and pulmonary vasculature relaxation. Penile erection during sexual stimulation is mediated by the release of nitric oxide (NO) from nerve terminals and endothelial cells, which stimulates the synthesis of cyclic GMP in smooth muscle cells. Cyclic GMP causes smooth muscle relaxation and increased blood flow into the corpus cavernosum and vasodilation in the pulmonary bed.
Solifenacin
A competitive muscarinic receptor antagonist. Muscarinic receptors play an important role in several major cholinergically mediated functions, including contractions of the urinary bladder smooth muscle and stimulation of salivary secretion.
Tadalafil
Inhibition of phosphodiesterase type 5 (PDE5) by tadalafil enhances erectile function by increasing the amount of cyclic GMP enhancing erectile function and pulmonary vasculature relaxation. Penile erection during sexual stimulation is mediated by the release of nitric oxide (NO) from nerve terminals and endothelial cells, which stimulates the synthesis of cyclic GMP in smooth muscle cells. Cyclic GMP causes smooth muscle relaxation and increased blood flow into the corpus cavernosum and vasodilation in the pulmonary bed.
Tamsulosin
selectively block postsynaptic α1-adrenergic receptors.
Tolterodine
Competitive muscarinic receptor antagonist, high binding affinity for cholinergic muscarinic receptors that mediate contraction of urinary bladder and salivation, exerts significant effects on lower urinary tract by increasing residual urine and decreasing detrusor pressure
Vardenafil
Inhibits phosphodiesterase type 5 (PDE5) to enhance erectile function by increasing the amount of cyclic GMP. Penile erection during sexual stimulation is mediated by the release of nitric oxide (NO) from nerve terminals and endothelial cells, which stimulates the synthesis of cyclic GMP in smooth muscle cells. Cyclic GMP causes smooth muscle relaxation, increasing blood flow into the corpus cavernosum
Phenazopyridine
Excreted in urine where it exerts a topical analgesic effect on mucosa of urinary tract. Relieves pain, burning, urgency and frequency. Precise MOA is unknown
