Class (71) Opioid Analgesic Mechanism of Action | Medicinal Chemistry 01 | B.Phamacy 04th semester
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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
Opioid Analgesic
Opioids are a group of analgesic agents commonly used in clinical practice. There are three classical opioid receptors (DOP, KOP and MOP), while the novel NOP receptor is considered to be a non-opioid branch of the opioid receptor family. Opioids can act at these receptors as agonists, antagonists or partial agonists.
Analgesia elicited by clinically applied opioids act predominantly via the MOP receptor.
1. Mu (µ) (agonist morphine)
Mu receptors are found primarily in the brainstem and medial thalamus. Mu receptors are responsible for supraspinal analgesia, respiratory depression, euphoria, sedation,
decreased gastrointestinal motility, and physical dependence. These are also called OP3 or MOR (morphine opioid receptors).
2. Kappa (κ) (agonist ketocyclazocine)
Kappa receptors are found in the limbic and other diencephalic areas, brain stem, and spinal cord, and are responsible for spinal analgesia, sedation, dyspnea, dependence, dysphoria, and respiratory depression. These are also known as OP2 or KOR (kappa opioid receptors).
3. Delta (δ) (agonist delta-alanine-delta-leucine-enkephalin) Delta receptors are located largely in the brain and their effects are not well studied. They may be responsible for psychomimetic and dysphoric effects. They are also called OP1 and DOR (delta opioid receptors).
4. Sigma (σ) (agonist N-allylnormetazocine)
Sigma receptors are responsible for psychomimetic effects, dysphoria, and stress-induced depression. They are no longer considered opioid receptors, but rather the target sites for phencyclidine (PCP) and its analogs.
Mechanism of opioid
Opioids and non-steroidal anti-inflammatory drugs (NSAIDs) are the commonest drugs used to treat pain. Opioids mimic the actions of endogenous opioid peptides by interacting with mu, delta or kappa opioid receptors. The opioid receptors are coupled to G1 proteins and the actions of the opioids are mainly inhibitory. They close N-type voltage-operated calcium channels and open calcium-dependent inwardly-rectifying potassium channels. This results in hyperpolarization and a reduction in neuronal excitability. They also decrease intracellular cAMP which modulates the release of nociceptive neurotransmitters (e.g. substance P). Inhibition of prostaglandin synthesis by cyclooxygenase is the principal mode of the analgesic and anti-inflammatory actions of NSAIDs. Cyclo-oxygenase is inhibited irreversibly by aspirin and reversibly by other NSAIDs. The widespread inhibition of cyclo-oxygenase is responsible for many of the adverse effects of these drugs. NSAIDs also reduce prostaglandin production within the CNS. This is the main action of paracetamol.
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
Opioid Analgesic
Opioids are a group of analgesic agents commonly used in clinical practice. There are three classical opioid receptors (DOP, KOP and MOP), while the novel NOP receptor is considered to be a non-opioid branch of the opioid receptor family. Opioids can act at these receptors as agonists, antagonists or partial agonists.
Analgesia elicited by clinically applied opioids act predominantly via the MOP receptor.
1. Mu (µ) (agonist morphine)
Mu receptors are found primarily in the brainstem and medial thalamus. Mu receptors are responsible for supraspinal analgesia, respiratory depression, euphoria, sedation,
decreased gastrointestinal motility, and physical dependence. These are also called OP3 or MOR (morphine opioid receptors).
2. Kappa (κ) (agonist ketocyclazocine)
Kappa receptors are found in the limbic and other diencephalic areas, brain stem, and spinal cord, and are responsible for spinal analgesia, sedation, dyspnea, dependence, dysphoria, and respiratory depression. These are also known as OP2 or KOR (kappa opioid receptors).
3. Delta (δ) (agonist delta-alanine-delta-leucine-enkephalin) Delta receptors are located largely in the brain and their effects are not well studied. They may be responsible for psychomimetic and dysphoric effects. They are also called OP1 and DOR (delta opioid receptors).
4. Sigma (σ) (agonist N-allylnormetazocine)
Sigma receptors are responsible for psychomimetic effects, dysphoria, and stress-induced depression. They are no longer considered opioid receptors, but rather the target sites for phencyclidine (PCP) and its analogs.
Mechanism of opioid
Opioids and non-steroidal anti-inflammatory drugs (NSAIDs) are the commonest drugs used to treat pain. Opioids mimic the actions of endogenous opioid peptides by interacting with mu, delta or kappa opioid receptors. The opioid receptors are coupled to G1 proteins and the actions of the opioids are mainly inhibitory. They close N-type voltage-operated calcium channels and open calcium-dependent inwardly-rectifying potassium channels. This results in hyperpolarization and a reduction in neuronal excitability. They also decrease intracellular cAMP which modulates the release of nociceptive neurotransmitters (e.g. substance P). Inhibition of prostaglandin synthesis by cyclooxygenase is the principal mode of the analgesic and anti-inflammatory actions of NSAIDs. Cyclo-oxygenase is inhibited irreversibly by aspirin and reversibly by other NSAIDs. The widespread inhibition of cyclo-oxygenase is responsible for many of the adverse effects of these drugs. NSAIDs also reduce prostaglandin production within the CNS. This is the main action of paracetamol.
E-Mail for official and other work - [email protected]
#solutionpharmacy #Pharmacologyclass #Pharmacognosyvideos #GPAT
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