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The mechanism of action of narcotic analgesics: NA - norepinephrine; ENK - enkephalin; 5-HT - serotonin; • - opioid receptor When opioid receptors are stimulated in the gray periaqueductal substance and some other parts of the brain stem, the descending antinociceptive system is activated, which has an inhibitory effect on the transmission of pain impulses along the afferent pathways of the spinal cord (supraspinal action). Descending inhibitory influences are carried out with the participation of serotonin and norepinephrine.
As a result of the action of narcotic analgesics on the higher parts of the central nervous system, the emotional assessment of pain changes, its perception decreases (even if the feeling of pain persists, it worries the patient less).
Among Buy Proscar (Finasteride) 5mg online - Men's Health substances that stimulate opioid receptors, there are full opioid receptor agonists (substances that can cause the maximum
online (Finasteride) Men's Buy - 5mg effect Proscar Healthfor a given system), partial opioid receptor agonists (substances that always cause an effect less than the maximum), and opioid receptor agonists-antagonists (stimulate the receptors of one subtype and block receptors of another Buy Proscar (Finasteride) 5mg online - Men's Health subtype). • Full opioid receptor agonists: - natural narcotic analgesics (opiates) - morphine, omnopon ?
- synthetic narcotic analgesics - trimeperidine, fentanyl. • Partial agonists and agonists-antagonists of opioid receptors - buprenorphine, butorphanol, nalbuphine, pentazocine ?
• Antagonists of narcotic analgesics - naloxone, nal-trexone. Natural narcotic analgesics (opiates) The source of morphine and other natural narcotic analgesics is opium, an air-dried milky juice that is obtained from cuts on immature poppy pods ( Papaver somniferum ).
Opium has been used as a pain reliever for over 6,000 years (in ancient Egypt, Greece and Rome), and its ability to cause physical and mental addiction has been a concern since the 18th century. Alkaloids of the phenanthrene series (morphine, codeine) have analgesic and antitussive activity; alkaloids of the isoquinoline series are not analgesics, they have an antispasmodic effect (papaverine).
Morphine is a derivative of phenanthrene, the main alkaloid of opium (10% concentration). Morphine was isolated from opium in 1806 by the German scientist Serturner, who named it after the sleep god Morpheus . The chemical structure of morphine was established in 1925, and in 1952 its synthesis was carried out, but on an industrial scale it turned out to be more appropriate to obtain it from plant materials. ) on the body is associated with the excitation of opioid receptors located both in the central nervous system and in peripheral tissues. Stimulation of central opioid receptors determined the pharmacological effects of morphine (Fig.
13.2) analgesia; euphoria (the occurrence of pleasant sensations and an unmotivated state of freedom from worries and problems).
There is a feeling of comfort and feelings of hunger, thirst, etc.
As a result, drug dependence develops - an irresistible desire to re-take morphine (morphinism). Some sick and healthy people who do not experience pain may develop a feeling of anxiety and weakness, feeling unwell (dysphoria). Pharmacological effects of morphine: a - reactions of the physiological systems of the body to the action of morphine: 1 - blockade of the transmission of pain impulses; b - muscle spasm of the sphincter of the anus in white mice after the administration of morphine: 1 - the position of the tail of mice before the administration of morphine, 2 - after the administration Sedation - a state of rest, drowsiness, impaired reasoning ability (without loss of memory) and superficial sleep. Antitussive effect due to inhibition of the cough center (addiction quickly develops to the effect).