27413556
Description
Flashcards by Majd Fawaz, updated more than 1 year ago
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Created by Majd Fawaz
about 5 years ago
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| Question | Answer |
| Define - Analgesics - Narcotics - Opium - Opioid - Opiate | - Analgesics: Agents that reduce pain + No loss of consciousness - Narcotics: Agents that reduce pain + Loss of consciousness - Opium: Crude extract of 20 alkaliods from Papavera Somniferum - Opioid: Substances with morphine like effects - Opiate: Natural Opioids |
| Name the first 4 amino acids in endogeneous opioid peptide | - TYR-GLY-GLY-PHE - They bind to the receptor |
| - (-) Morphine - Good analgesic agonist - pH=7 ==> Acid form (N+) - Must be protected or phenol will oxidize into inactive quinone | |
| - Benzoquinone - Inactive metabolite of Morphine | |
| - 3-Deoxymorphine - 10% potency of morphine - Better lipophilicity - Better bioavailability | |
| - Codeine - Weak u agonist (15% morphine) - Potent antitussive activity (for cough) - Undergoes partial (10%) O-demethylation --> morphine (still addictive) - Higher lipophilicity - Higher bioavailability | |
| - Ethylmorphine - 10% morphine | |
| - 3-Monoacetylmorphine (3-MAM) - Metabolite of Heroin | |
| - Diacetylmorphine (Heroin) - Weak u agonist - More lipophilic --> Better CNS Distribution --> More potent than Morphine --> More popular for abuse - Hydrolizes to give 6-MAM, 3-MAM, Morphine | |
| - 6-Deoxymorphine - More lipophilic --> More potent - x10 Morphine | |
| - 6-Methoxymorphine - x5 Morphine | |
| - 6-Ethoxymorphine - x2.5 Morphine | |
| - 6-MAM - Potent u agonist - Active metabolite of Heroin (>potent) - x4.2 Morphine | |
| - Morphone - 66% Morphine | |
| - Dihydromorphine - x1.2 Morphine | |
| - Hydromorphone - x5-6 Morphine | |
| - Oxymorphone - x10 Morphine - More analgesic activity - Less antitussive activity | |
| - Dihydrocodeine - x1.15 Codeine - 30% of Morphine | |
| - Hydrocodone - x5 Codeine - 70% of Morphine | |
| - Oxycodone - Equipotent to Morphine - x7 Codeine - Better bioavailability than Morphine - Less antitussive activity than Codeine | |
| - Normorphine - Less BBB penetration (Less active) - Metabolite of Morphine and Codeine | |
| - N-phenethylnormorphine - Very potent agonist activity (exception) | |
| - Nalbuphine - Mixed agonist/antagonist | |
| - Naloxone - Pure nonselective antagonist - Not orally active (First Pass Gluco) - Short Half life | |
| - Naltrexone - Pure nonselective antagonist - Given orally - Gives active metabolite (B-Naltrexol) | |
| - 6B-Naltrexol - Active metabolite of Naltrexone | |
| - Norcodeine - Inactive metabolite of Codeine | |
| - Morphine-6-glucuronide - Active metabolite of Morphine | |
| - Morphine-3-glucuronide - Inactive metabolite of Morephine | |
| - Name the 2 opioids - Name the CYP + Process - Elaborate on the CYP | - CYP 2D6 polymorphisim (Fast or Slow) |
| - (-) Levorphanol - Strong u agonist - x10 Morphine - Chemical Class: Morphinane | |
| - Butorphanol - Mixed Agonist/Antagonist - Chemical Class: Morphinane | |
| - (+) Dextromethorphan (3-Methoxydextrophan) - Chemical Class: Morphinane - Lacks analgesia - Has antitussive activity | |
| - Metazocine - Potent u agonist (>Morphine) - Chemical Class: Benzomorphane | |
| - Cyclazocine - Mixed Agonist/Antagonist - Chemical Class: Benzomorphane | |
| - Phenazocine - Pure potent u agonist (> x10 Morphine) - Chemical Class: Benzomorphane | |
| - Pentazocine - Mixed Agonist/Antagonist - Chemical Class: Benzomorphane | |
| - Pentazocine + Naloxone - Potent analgesic (oral) - If given IV (abuse), Naloxone will antagonize Pentazocine --> Withdrawl Symptoms --> Discourage abuse Note: Naloxone has no effect orally at 0.5 mg | |
| - Meperidine (Demerol) - 25% Morphine (analgesic) - Chemical Class: Phenylpiperidine - Short DOA (ester hydrolysis) - Achiral (No isomers) | |
| - Meperidinic acid - Inactive metabolite of Meperidine | |
| - Normeperidine - Less active metabolite of Meperidine - Longer half life - Neurotoxicity (Seizures) | |
| - MPPP ( N-Methyl Phenyl-4-Propionoxy Piperidine) - Reverse Ester: * Long DOA * Good leaving group - Decomposes into MPTP --> MPP+ | |
| - MPTP (1-Methyl-4-Phenyl-1,2,3,6-TetrahydroPyridine) - Metabolite of MPPP | |
| - MPP+ (1-methyl-4-phenylpyridinium) - Metabolite of MPTP by MAO-B - DA neuron damage --> Parkinsonism | |
| - Fentanyl - Potent u agonist (x80) - Chemical Class: Anilidopiperidines - Very Lipophilic --> Fast penetration of BBB + High affinity u (Noncovalent bonds) | |
| - Sufentanyl - Potent u agonist (x800) - Chemical Class: Anilidopiperidines - Very lipophilic --> Fast penetration of BBB + High affinity u (Noncovalent bonds) - So potent --> Used as anesthetic | |
| - Alfentanyl - Potent narcotic analgesic (x20) - Tetrazolinone makes it less lipophilic --> less potent than the rest | |
| - Methadone - u agonist (=morphine) - Chemical Class: Diphenylheptane - Same pharmacology and toxicology of Morphine except: * Given orally * Longer DOA - Used on recovering addicts: * Cross tolerance (Heroin) * No needles (No HIV risk) * Long DOA * Not addictive - Used on terminally ill patients | |
| - Methadol - Active metabolite of Methadone | |
| - Normethadol - Active metabolite of Methadone/Methadol | |
| - Normethadone - Active metabolite of Methadone | |
| - Dinormethadone - Active metabolite of Methadone/Normethadone | |
| - Dinormethadol - Active metabolite of Methadone/Methadol/Normethadol/Normethadone/Dinormethadone | |
| - (+) Propoxyphene - 10% Morphine - Chemical Class: Diphenyl propionate - Less abuse potential than Codeine - Withdrawn from the market * Used for suicide * Causes arrhythmias | |
| - Diphenoxylate - Opioid agonist (min. analgesia) - Chemical Class: Meperidine/Methadone hybrid - Used for diarrhea (Slowing Intestinal Contractions) - Rapid metabolism into Difenoxin (zwitterion) --> Limit CNS Penetration --> Limit abuse - Addiction in high doses --> Lomotil (Diphenoxylate+Atropine) | |
| - Difenoxin - x5 more active | |
| - Loperamide - Opioid agonist + No analgesia (No BBB) - Chemical Class: Meperidine/Methadone hybrid - Orally active - High lipophilicity - Nonhydrolyzable amide analogue of Meperidine - No central activity: * Efflux protein P-gp * First Pass Metabolism * Low dissolution - Low abuse potential | |
| - Etorphine - Extremey potent analgesic - Chemical Class: Oripavine - Sever resperatory depression - Used on large animals (elephants) | |
| - Buprenorphine - Partial u agonist - Chemical Class: Oripavine - x25-50 morphine - Sligh longer DOA - Moderate abuse potential (maintenance therapy) | |
| - Tramadol (Tramal) - Weak u agonist (100-fold less) - Orally active - Opioid + Nonopioid analgesia --> Naloxone can't fully reverse effect - O-demthylated metabolite is responsible for opioid activity - Less resperatory depression than Morphine | |
| - Dezocine - Mixed agonist/antagonist (Unknown Receptor) - Equipotent to Morphine - Only primary amine opioid | |
| Define: -Tolerance -Dependence | - Tolerance: Decreased response to a drug with repeated use. Develops with most but not eye and GI opioids (Drug Present) - Dependence: Withdrawl signs that develope cocurrently with Tolerance. (Drug Absent) |
| Withdrawl Symptoms | Flu Like Symptoms (Severity inc. 2-3 days) - Sneezing - Lacrimation - Weakness - Depression - Muscle cramps, Nausea, Vomting, Diarrhea - Agitation, Poor sleep - dysphoria - Increased HR, BP |
| Side Effects | - Euphoria - CNS Depression - Nausea+Vomiting - Resperatory Depression - Urinary Retention - Diaphorisis+Flushing - Miosis - Constipation - Itching |
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