Class (72) Narcotics Analgesic Antagonist | Medicinal Chemistry 01 | B.Pharmacy 04th Semester
3 هزار بار بازدید -
پارسال
-
Download the "Solution Pharmacy" Mobile
Download the "Solution Pharmacy" Mobile App to Get All Uploaded Notes, Model Question Papers, Answer Papers, Online Tests and other GPAT Materials - https://play.google.com/store/apps/de...
Solution Pharmacy will cover this syllabus of medicinal chemistry 01 for B.Pharmacy 4th semester
Unit 05 -
(01) Drugs acting on the central nervous system – general anaesthetics
(02) Inhalational anaesthetics – Halothane, methoxyflurane, enflurane, sevoflurane, isoflurane, desflurane
(03) Ultra-short acting barbiturate – methohexital sodium, Thiopental sodium
(04) Dissociative anaesthetics – Ketamine hydrochloride
(05) Narcotic and non-narcotic analgesic
(06) Morphine and related drugs – SAR of morphine analogous, morphine sulphate, codeine, meperidine hydrochloride, loperamide hydrochloride, pentazocine,
(07) Narcotic analgesic- nalorphine,
(08) Anti-inflammatory agents – Sodium salicylate, aspirin, mefenamic acid, meclofenamate, indomethacin, tolmetin, diclofenac, ketorolac, ibuprofen, naproxen, piroxicam, phenacetin, acetaminophen, antipyrine, phenylbutazone
The two most commonly used centrally-acting opioid receptor antagonists are naloxone and naltrexone. Naloxone comes in intravenous, intramuscular, and intranasal formulations and is FDA-approved for the use in an opioid overdose and the reversal of respiratory depression associated with opioid use.
Naltrexone is available in both oral and long-acting injectable formulations and is FDA-approved to treat opioid and alcohol use disorders as a maintenance treatment. The most commonly used peripheral opioid receptor antagonist is methylnaltrexone, which is a potent competitive antagonist acting at the digestive tract and is also FDA-approved for the treatment of opioid-induced constipation.Methylnaltrexone comes in oral tablets and as a subcutaneous injection.
Mechanism of Action
Centrally acting opioid receptor antagonists are potent competitive inhibitors with the highest affinity for the mu receptor. Naloxone is the most common choice in opioid overdose emergencies, and naltrexone is utilized primarily in opioid and alcohol use disorders to help maintain abstinence primarily by decreasing cravings. The competitive antagonism of the central mu receptors stimulates the respiratory drive, increases alertness, terminates analgesia and euphoria, and causes mydriasis.
Peripherally acting opioid receptor antagonists do not readily cross the blood-brain barrier but are potent competitive inhibitors at the mu receptor, which are found in high concentration at peripheral nerve terminals in bronchial smooth muscle and the digestive tract. Antagonism of these peripheral mu receptors can lead to intestinal hypermotility. Some studies suggest that up to 60% of opioid analgesia originates from the peripheral opioid receptors and that antagonizing through pharmacologic means may lead to an acute pain crisis
E-Mail for official and other work - [email protected]
#solutionpharmacy #Pharmacologyclass #Pharmacognosyvideos #GPAT
Solution Pharmacy will cover this syllabus of medicinal chemistry 01 for B.Pharmacy 4th semester
Unit 05 -
(01) Drugs acting on the central nervous system – general anaesthetics
(02) Inhalational anaesthetics – Halothane, methoxyflurane, enflurane, sevoflurane, isoflurane, desflurane
(03) Ultra-short acting barbiturate – methohexital sodium, Thiopental sodium
(04) Dissociative anaesthetics – Ketamine hydrochloride
(05) Narcotic and non-narcotic analgesic
(06) Morphine and related drugs – SAR of morphine analogous, morphine sulphate, codeine, meperidine hydrochloride, loperamide hydrochloride, pentazocine,
(07) Narcotic analgesic- nalorphine,
(08) Anti-inflammatory agents – Sodium salicylate, aspirin, mefenamic acid, meclofenamate, indomethacin, tolmetin, diclofenac, ketorolac, ibuprofen, naproxen, piroxicam, phenacetin, acetaminophen, antipyrine, phenylbutazone
The two most commonly used centrally-acting opioid receptor antagonists are naloxone and naltrexone. Naloxone comes in intravenous, intramuscular, and intranasal formulations and is FDA-approved for the use in an opioid overdose and the reversal of respiratory depression associated with opioid use.
Naltrexone is available in both oral and long-acting injectable formulations and is FDA-approved to treat opioid and alcohol use disorders as a maintenance treatment. The most commonly used peripheral opioid receptor antagonist is methylnaltrexone, which is a potent competitive antagonist acting at the digestive tract and is also FDA-approved for the treatment of opioid-induced constipation.Methylnaltrexone comes in oral tablets and as a subcutaneous injection.
Mechanism of Action
Centrally acting opioid receptor antagonists are potent competitive inhibitors with the highest affinity for the mu receptor. Naloxone is the most common choice in opioid overdose emergencies, and naltrexone is utilized primarily in opioid and alcohol use disorders to help maintain abstinence primarily by decreasing cravings. The competitive antagonism of the central mu receptors stimulates the respiratory drive, increases alertness, terminates analgesia and euphoria, and causes mydriasis.
Peripherally acting opioid receptor antagonists do not readily cross the blood-brain barrier but are potent competitive inhibitors at the mu receptor, which are found in high concentration at peripheral nerve terminals in bronchial smooth muscle and the digestive tract. Antagonism of these peripheral mu receptors can lead to intestinal hypermotility. Some studies suggest that up to 60% of opioid analgesia originates from the peripheral opioid receptors and that antagonizing through pharmacologic means may lead to an acute pain crisis
E-Mail for official and other work - [email protected]
#solutionpharmacy #Pharmacologyclass #Pharmacognosyvideos #GPAT
پارسال
در تاریخ 1402/03/24 منتشر شده
است.
3,013
بـار بازدید شده