Notes in Pharm 212 Opioids and Steroids

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Published	04/01/2024	WHAT ARE OPIOIDScompound with {{c1::morphine like}} activityextract of {{c1::unripe seed capsule of papaver somniferum}}contains {{c1::2 types of alka…
Published	04/01/2024	OPIOID RECEPTORS ❑ {{c1::Stereospecific}}, {{c1::saturable}} binding ❑ Bind to the {{c1::endogenous ligand}} and {{c1::opioid peptides}} ❑ {{c2::Four}…
Published	04/01/2024	MORE ON OPIOID RECEPTORS ❑ Most of available opioid analgesics act at {{c1::µ opioid receptor}} ❑ Activation of μ opioid receptor causes {{c2::an…
Published	04/01/2024	OPIOID RECEPTOR TRANSDUCTION MECHANISM 1) {{c1::Agonist binding}} 2) {{c1::Conformational changes in the GPCR}} 3) Effectsμ,δ -- {{c2::Inhibition of a…
Published	04/01/2024	Kappa agonists {{c1::Butorphanol}} {{c1::Pentazocine}}* {{c1::Nalorphine}}* {{c1::Salvia}} *μ-antagonist as well
Published	04/01/2024	Delta agonist/μ partial agonist  {{c1::Dezocine}}
Published	04/01/2024	Antagonists (μ, κ, δ) {{c1::Naloxone}} {{c1::Naltrexone}}{{c1::Nalmefene}}
Published	04/01/2024	Mu agonists{{c1::morphine}} ({{c5::also κ− & δ− receptor activation}}){{c1::heroine}}{{c1::meperidine}}{{c2::methadone}}{{c2::fentanyl}} ({{c6::mo…
Published	04/01/2024	CLASSIFICATION OF OPIOIDS {{c1::Natural opium alkaloids}} -- i.e. {{c2::Morphine}}, {{c2::Codeine}} {{c1::Semisynthetic opiates}} -- i.e. {{c2::heroin…
Published	04/01/2024	ENDOGENOUS OPIOID PEPTIDES Opioids act like {{c1::opioid peptides}}; they are {{c1::agonists}}A number of endogenous opioid peptides having morphine l…
Published	04/01/2024	PAIN PATHOPHYSIOLOGY Pain is {{c1::an ill-defined, unpleasant sensation, evoked by an external or internal noxious stimulus.}}{{c1::Analgesic}} reliev…
Published	04/01/2024	CLINICAL USE OF OPIOID ANALGESICS ❑ {{c1::Analgesia}} (main use) ❑ {{c1::Cough}} ❑ {{c1::Diarrhea}} ❑ {{c1::Acute Pulmonary Edema}} -- {{c2::excess fl…
Published	04/01/2024	TOXICITY & UNDESIRED EFFECTS ❑ {{c1::Respiratory depression}} (the main one) ❑ {{c1::Nausea and vomiting}} ❑ {{c1::GIT discomfort}} ❑ {{c2::Dyspho…
Published	04/01/2024	ACUTE MORPHINE POISONING > {{c1::50 mg}} of morphine Lethal dose is {{c1::250 mg }}symptoms -- {{c2::Stupor}}, {{c2::coma}}, {{c2::shallo…
Published	04/01/2024	TOLERANCE AND DEPENDENCE frequent repeated therapeutic doses of morphine --> {{c1::gradual loss in effectiveness.}} To reproduce the original respo…
Published	04/01/2024	TOLERANCE AND DEPENDENCE ❑ Maintenance of normal sensitivity of receptors requires {{c1::reactivation by endocytosis and recycling.}} ❑ Activation of …
Published	04/01/2024	WITHDRAWAL ❑ Withdrawal is manifested by significant effects on {{c1::muscle movement}} and {{c1::control}} ({{c2::shivering}})❑ These phenomena are h…
Published	04/01/2024	CONTRAINDICATIONS AND CAUTIONS IN THERAPY ❑ Use in patients with {{c1::head injuries}} ❑ Use during {{c1::pregnancy}} ❑ Use in patients with impaired …
Published	04/01/2024	PERIPHERALLY ACTING OPIOID ❑ Opioid receptor – {{c1::outside central nerve system}} Peripherally acting opioid agonist → {{c1::analgesia}} without {{…
Published	04/01/2024	OPIOID WITH OTHER ANALGESICS Goal of using analgesics in combination Achieve {{c1::superior analgesia}} Reduce {{c1::dose}} of each drug Minimize {{c1…
Published	04/01/2024	STEROID HORMONES one of the most widely used classes of therapeutic agents. These drugs are used in: {{c1::Birth control}} {{c1::Hormone-replacement t…
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Published	04/01/2024	SEX HORMONES {{c1::Estrogens}} originate in the {{c1::adrenal cortex}} and mainly {{c1::gonads}} affect {{c1::maturation and function of secondar…
Published	04/01/2024	CORTICOSTEROID HORMONES {{c4::Glucocorticoids}} (very diverse function)functionaffect mainly {{c1::carbohydrate, protein, and fat metabolism}}dec…
Published	04/01/2024	STEROID HORMONE RECEPTORS Steroid hormones are {{c1::lipid soluble molecules (hydrophobic)}}{{c1::enter the cell}} and bind to {{c1::hormone receptors…
Published	04/01/2024	A GENERAL SCHEME FOR STEROID HORMONE RECEPTOR INTERACTIONS 1. {{c1::Steroid crosses cell membrane into cytoplasm}} 2. {{c2::Steroid binds cytosolic re…
Published	04/01/2024	ESTROGEN RECEPTOR (ER) There are two distinct estrogen receptors (ERs). {{c1::estrogen receptor α (ERα)}} {{c1::estrogen receptor β (ERβ)}}ERα found i…
Published	04/01/2024	OTHER RECEPTORS ❑ Progesterone receptor (PR) can be found in two forms, but these are derived from a {{c1::single gene}}. {{c2::Progesterone rece…
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