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Pain Medications : Strong Opioids Last Updated: Jul 1, 2011 - 8:08:19 PM


OPIOIDS GLOSSARY
By steve Steele
Jan 15, 2000 - 3:36:17 PM

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  • Abstinence syndrome = withdrawal symptoms

     

  • Affinity = in crude terms, the "strength" of the interaction between a ligand and a receptor. When two ligands exist at equimolar concentration, the ligand whose affinity is higher will tend to displace the other from a receptor, assuming the low-affinity ligand is bound reversibly to the receptor.

     

  • Agonist = a compound that will bind to a receptor to form a complex which elicits a full pharmacological response, peculiar to the nature of the receptor involved.

     

  • Antagonist = a compound that will bind to a receptor to form a complex which does not give rise to any response, as if the receptor were unoccupied.

     

  • Delta receptors = a term used collectively to refer to two characterised subtypes of opioid receptors (delta-1, delta-2) that possess numerous features in common which are not present in the mu receptors or kappa receptors.

     

  • Dynorphin = an endogenous peptide which functions as a selective agonist for the kappa opioid receptors.

     

  • Endorphin(s), beta-endorphin = an endogenous peptide which functions as a selective agonist for the mu-opioid receptors.

     

  • Endomorphin = a term which refers to two small (5 amino-acids) endogenous peptides, known as endomorphin-1 and endomorphin-2, which function as mu-agonists with greater selectivity than beta-endorphin.

     

  • Enkephalin = one of a number of endogenous peptides which function as selective agonists for the delta-opioid receptors.

     

  • Full agonist = see "agonist"

     

  • Inverse agonist = in the context of receptors which exert some basic signalling activity even the absence of an agonist (characteristic known as "constitutive activity"), an agent which binds to a receptor, suppressing this activity to some degree.

     

  • Intrinsic activity = a measure of the maximum response to an agonist.

     

  • Kappa receptors = a term used collectively to refer to three characterised subtypes of opioid receptors (kappa-1, kappa-2, kappa-3) that possess numerous features in common which are not present in the mu receptors or delta receptors.

     

  • Ligand = molecule which binds to a receptor to form a complex.

     

  • MMT (methadone maintenence therapy) = medical treatment of addiction with the (less euphorigenic) opioid methadone

     

  • Mixed agonist-antagonist = see "partial agonist"

     

    Morphinan: The chemical base of many psychoactive drugs including opioid analgesics and cough suppressants. 

  • Narcotic = literally "sleep/stupor-inducing agent". Term usually applied indiscriminately to describe any exogenous compound with a "sedating" profile. Use of the term with reference to the opioids is not recommended, due to its ambiguity, and arguably negative connotation. Class of substances that can blunt the senses. Narcotics can be used to treat pain, induce sleep or as a sedative. In large quantities, narcotics can cause euphoria, stupor and coma. Regular, prolonged use can lead to dependence and addiction.

     

  • Neurotransmitter = any endogenous compound that plays a role in synaptic nervous transmission.

     

  • Opiate = compound containing the fundamental morphine or thebaine structure possessing some affinity to any, or all, of the opioid receptor subtypes. Examples are heroin, buprenorphine and naltrexone.

     

  • Opioid = Refers to any synthetic narcotic that has opiate-like properties but is not an opium derivative. Also refers to any of a group of naturally occurring peptides that bind or produce other action at opiate receptor sites.Partial agonist: A compound which binds and activates a given receptor, but unlike a full agonist, illicits only a partial pharmacological response.
  • Opioid peptides Group of chemicals that have opiate-like effects and that may be produced by the body itself or absorbed from certain food products.Opioid peptides have effects on mood, emotion, control of pain and appetite.  
  • Partial agonist = a compound which possesses affinity for a receptor, but unlike a full agonist, will elicit only a small degree of the pharmacological response peculiar to the nature of the receptor involved, even if a high proportion of receptors are occupied by the compound.

  • Pharmacophore: A group of atoms in the molecule of a drug that causes the drug’s action.  Structure activity relationship (SAR): The relationship that exists between the chemical structure of a drug and its activity. the minimum functionality, or 3-D configuration of specific atoms or groups, that a molecule must have in order to exhibit biological activity.

     

  • SAR (structure activity relationship) = the relationship between the chemical structure of a psychoactive compound to its strength and/or effects

     

  • Selectivity = the relationship between the affinity of a compound for a particular receptor and its affinity for other types of opioid receptor. For instance, a compound that will bind with high affinity to the mu-receptors, but with very low affinity to kappa and delta receptors, is said to possess high selectivity for mu.

     

  • Semi-synthetic opiate/opioid = a compound with some opioid receptor affinity, synthesised by functional modification of a product extracted from opium.

     

  • Synthetic opiate/opioid = a compound with some opioid receptor affinity, synthesised using no products extracted from opium.
  • Glossary for Opioid poisoning

    • Bradycardia: Excessively slow heart beat.
    • Coma: Prolonged unconsciousness
    • Drug-related conditions: Medical conditions related to drug usage, including adverse reactions, intoxication, and overdose.
    • Hypothermia: Low body temperature
    • Low blood pressure: Blood pressure that is too low
    • Miosis: A condition which is characterized by the contraction of the pupil of the eyes
    • Poisoning, overdose or adverse reactions: Medical conditions related to poisons, drug overdosage, or drug adverse reactions.
    • Respiratory depression: Also known as bradyapnea is the decreased rate of breathing.

    Glossary for Opioid withdrawal

    • Anorexia: Any type of appetite loss; often refers to anorexia nervosa
    • Dilated pupils: A condition characterized by the dilatation of the pupils of the eye
    • Drug-related conditions: Medical conditions related to drug usage, including adverse reactions, intoxication, and overdose.
    • Increased sweating: A condition which is characterized by an abnormal excess of sweating
    • Insomnia: Insomnia is defined as repeated difficulty with the initiation, duration, maintenance, or quality of sleep that occurs despite adequate time and opportunity for sleep that results in some form of daytime impairment.
    • Mental health conditions: Medical conditions related to mental health, emotions, behavior, personality, psychology, psychiatry, and so on.
    • Restlessness: state of overactive restlessness
    • Runny nose: Rhinitis is the medical term describing irritation and inflammation of some internal areas of the nose
    • Yawning: When one opens their mouth for a deep inhalation usually involuntary

    Glossary for Opioid addiction

    • Addiction conditions: Medical conditions related to addiction of any kind, including substances or behavioral addictions.
    • Depression: Various syndromes with excessive anxiety, phobias, or fear.
    • Drug-related conditions: Medical conditions related to drug usage, including adverse reactions, intoxication, and overdose.
    • HIV/AIDS: HIV is a sexually transmitted virus and AIDS is the progressive immune failure that HIV causes.
    • Hepatitis: Any type of liver inflammation or infection.
    • Kwashiorkor: A malnutrition state that is produced by severe protein deficiency
    • Mental health conditions: Medical conditions related to mental health, emotions, behavior, personality, psychology, psychiatry, and so on.
    • Poor appetite: Loss or reduction in appetite for food
    • Respiratory failure: Failure of the respiratory system
    • Social problems: Difficulty relating to other people
    • Society problems: Difficulty interacting in society.
    • Sudden death: The sudden death of an individual
    • Weight loss: Loss of body weight.
    • Withdrawal symptoms: The occurrence of a group a symptoms that occur due to a withdrawal reaction that occurs when discontinuing use of a substance
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