Buprenorphine behaves like a partial agonist/antagonist at µOR. Pentazocine is an antagonist at µOR and an agonist at кOR. Both are classified as “low-ceiling” opioids (B), because neither is capable of eliciting the maximal analgesic effect obtained with morphine or meperidine. The antagonist action of partial agonists may result in an initial decrease in effect of a full agonist during changeover to the latter. Intoxication with buprenorphine cannot be reversed because it binds…
All semisynthetic derivatives (hydromorphone) and fully synthetic derivatives (pentazocine, pethidine = meperidine, l-methadone, and fentanyl) are collectively referred to as opioids. The high analgesic effectiveness of xenobiotic opioids derives from their affinity for receptors normally acted upon by endogenous opioids (enkephalins, в-endorphin, dynorphins;
Baclofen (p- chlorophenyl-GABA) was designed to be an orally active GABA-mimetic agent and is an agonist at GABAB receptors. Activation of these receptors by baclofen results in hyperpolarization, probably by increased K+ conductance
Drugs that modify this reflex arc may modulate excitatory or inhibitory synapses. Thus, to reduce the hyperactive stretch reflex, it is desirable to reduce the activity of the Ia fibers that excite the primary motoneuron or to enhance the activity of the inhibitory internuncial neurons
Type of antidepressant. It is given if the depressed client has not responded to Tricyclic antidepressants and SSRI’s. This type of med interacts with a bunch of other meds, that’s why it’s usually not drug of choice for depression.
Methylxanthines - Caffeine belongs to a class of compounds called methylxanthines. Other methylxanthines include theobromine (found in chocolate) and theophylline (found in tea, and sometimes used in the treatment of asthma).