Drugs of Abuse Flashcards
What is recreational drug use?
Use of a pharmacologically active agent for purposes other than it’s intended medicinal or other purpose.
Psychoactive substances
What are the recreational drug classes?
Cannabinoids, Cocaine, Amphetamine-like, Opioids and sedative hypnotics
What is tolerance?
A state at which there is no longer the desired response to a drug. More drug will be required to achieve the same response.
Not necessarily addiction.
How high can tolerance potentially be?
200 fold
Diazepam, methamphetamine
How long until tolerance is typically lost?
10-14 days
What is reverse tolerance?
Sensitization. A tolerant person takes a break, and then when they start again they won’t be able to take as much as they were before.
When are the impairing effects of a drug greater?
During rise to maximal concentration in comparison to downward slope
What is functional tolerance (pharmacodynamic tolerance)?
Change in the post synapses of the CNS due to exposure to psychoactive drugs (or hormones)
What are the short and long term effects of functional tolerance?
Short (few days): desensitization of receptors (from something like phosphorylation)
Long (few weeks): down or up regulation of receptors/signalling pathways
What is functional cross tolerance?
When 2 drugs work on the same receptor, if tolerance occurs to one, it will most likely occur to the other.
What is metabolic tolerance (pharmacokinetic tolerance)?
The adaptation of metabolic “machinery” to repeated exposure to a drug (similar to drug resistance)
Enzyme induction, drug metabolism (CYP P450, Glucuronidation)
Different from inherent susceptibility (polymorphisms)
What is metabolic cross tolerance?
When 2 drugs are metabolized similarly tolerance to one can cause tolerance in the other
What is withdrawal?
An unpleasant maladaptive behavioural change that occurs when blood tissue concentrations of a substance decline in an individual who had maintained prolonged heavy use of the substance (symptoms vary between classes of drugs)
Which drugs have physiological withdrawal symptoms?
Alcohol, hypnotics, anxiolytics, opioids and sedatives
What is dependence?
The state at which the user functions normally only when taking the drug
Reinforced by withdrawal symptoms
What is an example of physiological dependence?
An alcoholic’s withdrawal from alcohol (CNS depression) can be life-threatening
What is an example of psychological dependence?
Repeated cocaine use, they will continue drug seeking habits in spite of risks and repeated dosing needed to keep the “high”
What pathway can play a role in drug cravings?
Dopaminergic pathway
Separate neruochemical pathways for physiological vs psychological dependence
What is addiction characterized by?
Inability to consistently Abstain, impairment in Behavioural control, Craving, Diminished recognition of significant problems with one’s behaviours and interpersonal relationships and a dysfunctional Emotional response
What are opiates?
Plant extracts and semi-synthetics derived from the poppy
Morphine, heroine
What are opioids?
The umbrella term for opiates and synthetics like fentanyl.
Be aware of the source of the drug.
What are some examples of endogenous opioids?
Enkephalins, endorphins, dynorphins
What are some desirable effects of opioids?
Analgesia, euphoria, sedation, anxiety relief, depression of cough reflex
Which receptors do opioids bind to?
Mu, kappa, delta
Most are selective for mu
Pentazocine works on kappa
What are some undesirable effects of opioids?
Dysphoria (dizziness, nausea), vomiting, constipation, urinary retention, withdrawal, respiratory depression
What are some symptoms associated with overdose?
Pulmonary congestion, frothing of the mouth, snoring heavily prior to death, blockade of respiratory centres (pneumonia patients at risk)
What the routes of administration for opioids?
Oral, IV, IM, Smoked (more immediate high than oral), Intranasal, Transdermal (more lipophilicity)
What is the prolonged affect of opioids due to?
Accumulation of drug/formation of active metabolites
Which polymorphism can affect opioid metabolism?
Morphine 6-glucuronide is active, morphine 3-glucuronide is not
What are some symptoms of opioid toxicity?
Convulsions, meperidine metabolism to normeperidine, decreased respiration, orthostatic hypotension, stroke, ECG abnormalities, intestinal obstruction
How long will opioid abstinence syndrome last?
7-10 days
What occurs in 8-12 hours of opioid abstinence?
Lacrimation, respiration, yawning, rhinorrhea
What occurs in 12-14 hours of opioid abstinence?
Irritability, restlessness, mydriasis, anorexia, piloerection, weaknesses
What occurs in 48-72 hours of opioid abstinence?
Sneezing, hyperthermia, aching muscles, insomnia, hypertension, abdominal cramps