Opiates Flashcards
Narcotic
Older term initially used to describe a drug that caused “narcosis” or sleep, but then became a loosely applied universal term for many illegal drugs, primarily for legislative purposes. Not a pharmacologically accurate term
Opiate
Any drug that is derived from the opium poppy, including natural and synesthetics
Opioid
General term for any drug(or endogenous peptide) that acts on the opiate receptor
Opium
Coagulated juice of the poppy pod that contains various opiates
Endorphine
Endogenous opiate like peptide that modifies the actions of other transmitters
Opiate Receptor Subtypes
mu
kappa
delta
nociception
Mu
Analgesia, physical dependence, respiratory depression, miosis, euphoria, reduced GI motility
Kappa
Analgesia, sedation, physical dependence
Delta
analgesia, anti depressant, physical dependence
Nociception
Anxiety, depression, appetite, develop tolerance to mu agonists
Endogenous Opiates
Enkephalins were first discovered, very potent (delta)
Beta endorphin (mu) and dynorphin (kappa)
Rapidly inactivated
Located in hypothalmus, forebrain, limbic medial thalamus, locus coeruleus to mediate pain perception and mood and released from pituitary during stress
Medical Use for Opiates
Pain
Cough
Diarrhea
Pain
Most common human experiences in which people seek medical treatment
Chronic pain is defined as that which lasts at least 3 months
It is difficult to measure because subjective
Types of Pain
Nociceptive- Physiological process of transmitting pain producing stimuli that emerge from tissue damage
Neuropathic- caused by lesion of the nervous system as a result of trauma, injury, or infection
Opiate Induced Analgesia
Blocks both perception and emotional components of pain
Does not impair conciousness
Reduces dull chronic pain
Patient Controlled Analgesia
- Patients control their pain by activating a pump on demand
Receives immediate dose, does not need to wait for nursing staff and physicians to administer the dose
Typically patient lets staff know, it takes 30-60 minutes
Faster alleviation of pain = less medication used
Euphoria
Intense sense of well-being and contentment, with a complete lack of concern for anything
Ecstatic- with sexual connotations
Primary reason for abuse
Physiological Effects
Histamine release- itching, red eye, sweating, fall in BP
Reduces gastric motility- constipation
Respiratory Depression- cause of death in overdose
Pupillary Constriction
Side Effects/Toxicity
Respiratory Depression
Opiates inhibit brainstem ability to detect buildup in CO2
Most important cause of death during overdose
Physiological Tolerance
Develops to everything, except for pupils and GI tract
Accounts for the increase in dose
Rate of development not the same- slow for respiratory rate
Lethal effects require 4-8 times the dose
Cross tolerance to all opiates
Physical Dependence
Withdrawal or abstinence signs
craving, anxiety
yawn, sweating, pupil dilation
tremors, flashes, insomnia
Heroin
Conversion of morphine to heroin is preferred by drug traffickers because
- 10 times more potent
Less space to hide
more lipid soluble
enters the brain more quickly
rapidly converted to morphine in bloodstream
Oxycodone
Developed in 1996 as timed release formulation
Abusers avoid the delay by crushing the tablets and snort or mix with water and inject in IV
Immediately delivers entire dose, sometimes combined with ecstasy
FDA released black box warning, prescription instructions
Reformulation- pills cannot be crushed, turned into a gel when mixed with water
- Decreased abuse by a little, more people turned to heroin
Public Heath
53 million Americans used prescription drugs for non-medical reasons
70% obtain from relatives and friends
DISPOSE OF ALL PRESCRIPTION DRUGS WHEN FINISHED