Synthesized in 1904 by the German chemist A.Einhorn (1857-1917). In 1904, when Heinrich Braun (1903) German specialist renowned in local anesthesia devised a procaine-adrenaline mixture marketed by Hoechst under the Novocaïne® brand that was to dominate the market for 50 years. The Brand Name of Procaine is - NOVOCAIN® - comes from the Latin word "Novus," meaning "new," plus "cocaine widely used until the 1960s. Procaine has greater effectiveness in getting the effects of cocaine as a local anesthetic and did not provoke the addictive potential or the other negative side effects. But despite this fact its popularity diminished afterward because Procaine has been dethroned by compounds less toxic local anesthetic agents and longer duration of action
In plasma and tissue, ACE catalyses the conversion of angiotensin I to the angiotensin II (active vasoconstrictor), as well as the breakdown of the bradykinin (vasodilator). Therefore ramiprilat reduces angiotensin II formations and inhibits bradykinin breakdown. This results in vasodilation. Since angiotensin II also stimulates the release of aldosterone, ramiprilat causes a reduction in aldosterone secretion. The reduction in aldosterone secretion causes an increase in urinary output.
What is the specific mechanism responsible for producing this effect (Be specific)? (6 marks) The antidiuretic hormone (ADH) is synthesized by neurons located in the hypothalamus and are stored in and secreted by the posterior pituitary gland (Silverthorn et al., 2013). The high osmolarity of a dehydrated person is the primary stimulus for the secretion of ADH (Saladin, 2004). This hormone acts on the collecting duct of the nephron (Silverthorn et al., 2013). ADH increases and water reabsorption and decreases osmolarity of renal filtrate (reduces urine output) by two mechanisms.
Leukotrienes (LT) are fatty acid-derived mediators containing a conjugated triene structure. They are formed when arachidonic acid (Chapter 26) is liberated from the cell membrane of cells, as a result of cell activation by allergic or other noxious stimuli. 5-Lipoxygenase is the enzyme required for the synthesis of LTA4, which is an unstable epoxide precursor of the two subgroups of biologically important leukotrienes. LTB4 is a dihydroxy 20-carbon-atom fatty acid which is a potent pro-inflammatory chemo-attractant. The other group is the cysteinyl leukotrienes (LTC4, LTD4 and LTE4).
M3 Cholinergic receptors are the one that responsible for parasympathetic detrusor contraction. Thus oxybutynin compete with acetylcholine (ACh), binding Oxybutynin lead inactivation of Phospholipase C and result in inhibition of Calcium ion releasing and lead to relaxation of detrusor muscle. Oxybutynin studies determine that Oxybutynin can increase maximum urinary bladder holding capacity and increases the volume to detrusor contraction. Oxybutynin is appropriate for the patients that having conditions of involuntary detrusor contractions such as Mrs.
Loperamide is a potent Mu-opioid receptor agonist [13, 15] that acts on the myenteric plexus of the gut wall. It inhibits acetylcholine release from the myenteric plexus and inhibits the peristalsis. It also increases the tone of anal sphincter. Loperamide also inhibits the secretions directly by interacting with calmodulin, this may be responsible for the anti diarrheal action.  Activating the Mu receptor prolongs the orocecal and colonic transit times by disrupting the gut’s electrical activity, increasing gut capacity, and delaying the passage of fluids through the small intestine, it has no direct effect on absorption  and when used to manage patients with ileostomy diarrhea investigators have obtained significant reduction in faecal loss, improvement in electrolytes and fluid balance have with loperamide therapy.
All You Need To Know About Chelation Therapy Content: You may have read about it and wondered that what’s chelation therapy? Chelation therapy is usually a chemical course of action in which an artificial solution-EDTA (ethylenediaminetetraacetic acid)-is injected into the bloodstream of a patient to eliminate heavy metals and minerals from the human body. Chelation implies to grab something.” When EDTA is injected in a patient’s veins, it catches heavy metals and minerals for example iron, calcium, aluminium, arsenic, copper, mercury and lead, and then eliminate them from the body. Other than as a cure for lead poisoning, Chelation therapy is a bit controversial topic among experts. You should also keep in mind that chelation therapy is always done on an outpatient basis.
The kind of drug tolerance models that has passed from one generation to another, be it emphasises on receptor changes or on altered metabolism, it describes or explains the mechanisms that are underlying tolerance as orgasmic change which results automatically due to the exposure of drugs. Nevertheless, there has been many recent demonstrations of tolerance phenomena which postulates that there is much more to drug tolerance than just drug exposure by itself. At a more specific level, learning and increased knowledge resulting from drug administration may be more inclined to play a significant role in expression, maintenance and expression of drug tolerance (Siegel, 1983). It was noted by Siegel (1975) that any instances when a certain drug is tested or taken can be perceived as a Pavlovian conditioning trial where environmental cues are joined with the effects that is brought about by the drug. Through the process of conditioning, the learning of associating drug effects with surroundings or environments by animals may occur, predictably associated with the administration of drugs.
Social anxiety disorder can be treated with medication, psychotherapy, or both. A number of medications originally prescribed for the treatment of depression are now being used to treat anxiety disorders. They are selective serotonin reuptake inhibitors and monoamine oxidase inhibitors. Selective serotonin reuptake inhibitors act on the brain on a chemical messenger called serotonin; they tend to have fewer side effects than older antidepressants. Monoamine oxidase inhibitors are the oldest of the antidepressant medications; phenelzine, the most commonly prescribed MAOI, is helpful for people with panic disorder and social anxiety disorder.
Prostaglandins E2 and I2 are the predominant prostaglandins synthesized by the gastric mucosa and are known to inhibit the secretion of gastric acid and stimulate the secretion of mucus and bicarbonate5. Peptic ulcer diseases comprise heterogeneous disorder which manifests as a break in the
Labetalol and Carvedilol block beta and alpha-1 receptors. By blocking alpha receptors, this adds to the blood vessel dilating effects. Some of the beta blockers have intrinsic sympathomimetic activity (ISA), which means they mimic the effects of norepinephrine and epinephrine and cause an increase in blood pressure and heart rate. (Ogbru & Marks,
The inventor of LSD, Dr. Albert Hofmann, was known to microdose in his old age. He said in an interview (https://www.erowid.org/culture/characters/hofmann_albert/hofmann_albert_interview1.shtml), however, that his first “trip” with the psychedelic was crushing and that “the unpredictability of effects is the major danger of LSD”. “My first planned self-experiment with LSD was a "bum trip" as one would say nowadays,” he said, adding that if the use of the drug were at present legal, which is not the case, then is would be “handled best by a ripe, stabilized person with a meaningful reason for taking LSD”. Microdosing and doping James Oroc, the author of the book Tryptamine Palace: 5-MeO-DMT and the Sonoran Desert Toad, extensively wrote about the correlation between psychedelics and extreme sports, arguing that microdosing reportedly improves both stamina and abilities in athletes. A report by the Cycling Independent Reform Commission (CIRC) looked at the problem of doping in professional cycling, focusing in particular on how some riders are now microdoping to stay within the limits of the Biological Passport.