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Drugs of Abuse Flashcards

(51 cards)

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1
Q

What is Drug Abuse?

A

• Abuse is the excessive self-administration of
any substance for nonmedical purposes.
• Some drugs of abuse do not lead to addiction.
• This is the case of substances that alter
perception without causing sensations of reward
and euphoria, such as the hallucinogens.

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2
Q

What behaviors indicate addiction?

A 
Behaviors that include one or more of the following:
• impaired control over drug use
• compulsive use
• continued use despite harm
• craving
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3
Q

What is physical dependence and how can withdrawal syndrome be reproduced?

A

• State of adaptation manifested by drug class
specific withdrawal syndrome.
• The withdrawal syndrome can be produced by:
• abrupt cessation
• rapid dose reduction
• administration of an antagonist.

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4
Q

What is withdrawal syndrome?

A

• Physiological and behavioral changes directly

related to sudden cessation or reduction in use of a drug to which the body has become adapted.

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5
Q

What is considered tolerance?

A

• A state of adaptation in which exposure to a
drug induces changes that result in a diminution
of one or more of the drug’s effects over time.
• Tolerance may occur to both the desired and
undesired effects of drugs, and may develop at
different rates for different effects.
Physical dependence and Tolerance
• Normal responses that often occur with the
persistent use of certain medications.

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6
Q

Mechanisms of Addiction?

A

• The mesolimbic dopamine system is the prime
target of addictive drugs.
• As a general rule, all addictive drugs activate
the mesolimbic dopamine system.

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7
Q

Types of drugs of abuse?

A
  • CNS DEPRESSANTS
  • PSYCHOSTIMULANTS
  • NICOTINE
  • OPIOIDS
  • MARIJUANA
  • PSYCHEDELIC AGENTS
  • INHALANTS
  • ANABOLIC STEROIDS
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8
Q

list 3 cns depressants?

A
  • Ethanol
  • Benzodiazepines
  • Barbiturates
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9
Q

Ethanol classification and moa?

A

• Ethanol is classed as a depressant because it
produces sedation and sleep.
• The initial effects of ethanol are often perceived
as stimulation due to suppression of inhibitory
systems.
• Ethanol influences several cellular functions:
• GABAA receptors
• Kir3/GIRK channels
• Adenosine reuptake
• Glycine receptors
• NMDA receptors
• 5-HT3 receptors.

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10
Q

Describe ethanol withdrawal syndrome?

A

• Heavy consumption of ethanol leads to acquired
tolerance and physical dependence.
• Withdrawal syndrome may include tremor, nausea, vomiting, sweating, agitation and anxiety.
• This may be followed by hallucinations.
• Generalized seizures may appear after 24-48 h.
• After 48-72 h delirium tremens may appear.
• Delirium tremens is associated with 5-15%
mortality.

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11
Q

TREATMENT OF ALCOHOL WITHDRAWAL?

A

• Long half-life benzodiazepines are the preferred agents: Diazepam and chlordiazepoxide.
• Because of their long half-life, withdrawal is smoother, and rebound withdrawal symptoms are less likely.
• Lorazepam and oxazepam are intermediateacting drugs.
• They may be preferable in the elderly and
those with liver failure.

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12
Q

Treatment of alcohol addiction?

A 
• Three drugs are FDA-approved for treatment of
alcoholism:
• Disulfiram: Aldehyde dehydrogenase
inhibitor. Used to create aversion to drinking.
• Naltrexone: Orally available opioid
antagonist. Reduces craving for alcohol.
• Acamprosate: NMDA receptor antagonist.
Prevents relapse.
Topiramate
• Facilitates GABA function, antagonizes
glutamate receptors.
• May reduce cravings.
• Not FDA-approved.
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13
Q

Benzodiazepine overview, withdrawal syndrome, and management of withdrawal?

A

• Can cause physical dependence and addiction.
• Addiction is rare.
• Signs and symptoms include: tremors, anxiety,
perceptual disturbances, dysphoria, psychosis,
and seizures.
• The syndrome can be life-threatening.
• If the patient is on a short-acting drug, they are
switched to a long-acting drug.
• Diazepam is the most used agent.
• Then the dose is gradually reduced.

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14
Q

What does barbiturate abuse resemble?

A

• Abuse problems with barbiturates resemble those seen with benzodiazepines.

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15
Q

List three psychostimulants?

A
  • Methylxanthines
  • Cocaine
  • Amphetamines
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16
Q

List 3 methylxanthines and moa?

A

• Caffeine, theophylline & theobromine.
• Caffeine is the most widely consumed stimulant.
• Methylxanthines block presynaptic adenosine
receptors.
• Activation of adenosine receptors inhibits
norepinephrine release.
• Therefore blockade of adenosine receptors
increases norepinephrine release.

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17
Q

Actions of caffeine dose on CNS?

A

CNS
• 100–200 mg caffeine (1 - 2 cups of coffee) cause decrease in fatigue and increased mental
alertness.
• 1.5 g caffeine (12 to 15 cups of coffee) produces
anxiety and tremors.
• The spinal cord is stimulated only by very high
doses (2–5 g) of caffeine.

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18
Q

METHYLXANTHINES:

TOLERANCE AND WITHDRAWAL

A

• Tolerance can rapidly develop to the stimulating
properties of caffeine.
• Withdrawal consists of feelings of fatigue and
sedation.
• Addiction is rare.
• Caffeine is not listed in the category of addicting
stimulants.

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19
Q

Cocaine overview and moa?

A

• Due to its abuse potential, cocaine is classified
as a Schedule II drug by the DEA.
• Cocaine inhibits dopamine, norepinephrine and
serotonin reuptake.
• The prolongation of dopaminergic effects in the
brain’s limbic system produces the intense
euphoria that cocaine initially causes.

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20
Q

Cocaine’s action on the cns?

A

CNS
• Stimulation of cortex and brainstem.
• Increases mental awareness and produces a
feeling of well-being and euphoria.
• Paranoia may occur after repeated doses.
• At high doses: tremors and convulsions, followed by respiratory and vasomotor
depression

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21
Q

Cocaine action on the SNS?

Study These Flashcards
A

SYMPATHETIC NERVOUS SYSTEM
• Peripherally, cocaine potentiates the action of
norepinephrine resulting in adrenergic
stimulation.
• Adrenergic stimulation produces tachycardia,
hypertension, mydriasis, and diaphoresis

22
Q

Describe cocaine withdrawal syndrome?

Study These Flashcards
A

• Dysphoria, depression, sleepiness, fatigue, cocaine craving and bradycardia.
• Cocaine withdrawal is generally mild.
• Treatment of withdrawal symptoms is usually not
required.
• Many agents, mainly antidepressants and
dopamine agonists have been tested as treatments for cocaine abuse.
• None have demonstrated clear efficacy

23
Q

Amphetamines overview and moa?

Study These Flashcards
A

• Amphetamines are classified as Schedule II
drugs by the DEA.
• Amphetamines increase release of catecholamines.
• They are also weak inhibitors of MAO.
• They are also possible direct catecholaminergic
agonists in the brain.

24
Q

AMPHETAMINES: ACTIONS on CNS and SNS?

Study These Flashcards
A

CNS
• Behavioral effects similar to those of cocaine.
• Due to release of dopamine.
• Increased alertness, decreased fatigue,
depressed appetite and insomnia.
• At high doses, psychosis and convulsions.
SYMPATHETIC NERVOUS SYSTEM
• Activate receptors through norepinephrine
release.

25
Amphetamine uses?
• Attention deficit syndrome: Amphetamine and methylphenidate. • Narcolepsy: Amphetamine and methylphenidate.
26
Describe amphetamine tolerance and withdrawal?
``` • Tolerance can be marked. • An abstinence syndrome can occur upon withdrawal. • Symptoms include increased appetite, sleepiness, exhaustion, and mental depression. • Antidepressants may be indicated. ```
27
Nicotine overview and moa?
• Second only to caffeine as the most widely used CNS stimulant. • Second only to alcohol as the most abused drug. • Full agonist of the nicotine receptor. • The rewarding effect of nicotine requires involvement of the ventral tegmental area , where nicotinic receptors are expressed on dopamine neurons. • When nicotine excites these neurons, dopamine is released.
28
Nicotine actions?
• In low doses: ganglionic stimulation by depolarization. • At high doses: ganglionic blockade. CNS • Cigarette smoking or administration of low doses of nicotine produces some degree of euphoria and relaxation. • Improves attention, learning, problem solving, and reaction time. • High doses of nicotine result in central respiratory paralysis and severe hypotension caused by medullary paralysis. • Nicotine is an appetite suppressant.
29
Describe nicotine withdrawal symptoms?
• Nicotine withdrawal is mild. • Involves irritability and sleeplessness. • However, nicotine is among the most addictive drugs. • Relapse is very common.
30
Treatment for nicotine addiction?
NICOTINE REPLACEMENT THERAPY • Nicotine can be administered by transdermal patch, gum, nasal spray, vapor inhaler or by lozenge for buccal absorption. SUSTAINED-RELEASE BUPROPION • MOA unclear. VARENICLINE • Partial agonist at nicotinic receptors in the CNS. • Reduces the reward of smoking.
31
4 most common opioids and describe opioid tolerance, dependence, and addiction?
• All opioids induce strong tolerance and dependence. • Addiction to heroin or other short-acting opioids produces behavioural disruptions and usually is incompatible with a productive life. • The withdrawal syndrome is unpleasant but not life-threatening. • It includes dysphoria, lacrimation, rhinorrhea and yawning.
32
OPIOIDS: TREATMENT OF OPIOID WITHDRAWAL?
DETOXIFICATION USING OPIOID AGONISTS • The illicit agent is replaced by a long-acting opioid. • The dose is slowly reduced. • Drugs used: Methadone or buprenorphine. • Methadone is a useful drug for detoxification and maintenance of the chronic relapsing heroin addict.
33
Describe DETOXIFICATION USING OPIOID ANTAGONISTS?
• Naltrexone is an antagonist with a high affinity for the μ opioid receptor. • Naltrexone will not satisfy craving or relieve withdrawal symptoms. • Naltrexone can be used after detoxification for patients with high motivation to remain opioidfree.
34
Overview of Marijuana?
• The smoke from burning cannabis contains 61 different cannabinoids. • D9-tetrahydrocannabinol (D9-THC, THC, dronabinol) produces most of the effects.
35
MARIJUANA: MECHANISM OF ACTION?
• Two cannabinoid receptor subtypes:CB1 & CB2. • Both are G protein-linked receptors. • Both couple to Gi. • CB1 receptors are found primarily in the brain and mediate the psychological effects of THC. • CB2 receptors are present mainly on immune cells.
36
MARIJUANA: ACTIONS? Tolerance and dependence?
• THC can produce euphoria, followed by drowsiness and relaxation. • Affects short-term memory and mental activity. • Impairs highly skilled motor activity. • Other effects: appetite stimulation, xerostomia, visual hallucinations, delusions, enhancement of sensory activity. • At high doses: toxic psychosis. • Tolerance and mild physical dependence occur with continued, frequent use of the drug.
37
MARIJUANA: USES?
• Therapeutic THC is called dronabinol. • Dronabinol is FDA-approved for: • Anorexia associated with weight loss in patients with AIDS. • Nausea and vomiting associated with cancer chemotherapy (second line).
38
List 5 PSYCHEDELIC AGENTS
``` • LSD • MESCALINE • PSILOCYBIN • PHENCICLIDINE • MDMA • Psychedelic drugs affect thought, perception and mood. • They don’t cause marked psychomotor stimulation or depression. ```
39
3 lsd like group of drugs?
The LSD-like group of drugs include: • LSD • Mescaline • Psilocybin
40
LSD moa?
• The hallucinogenic actions of LSD appear to be mediated by agonist effects at 5-HT2 receptors in the CNS.
41
LSD: CLINICAL PRESENTATION?
• Patients who have taken LSD generally present with a combination of somatic and psychomimetic symptoms. • Somatic symptoms are usually due to sympathomimetic effects. • Somatic symptoms include: mydriasis, hypertension, tachycardia, increased body temperature, flushing, sweating, tremors and piloerection.
42
LSD: PHYSICAL DEPENDENCE AND | WITHDRAWAL and AE?
• LSD does not cause addiction. • There is no withdrawal syndrome. • Users may require medical attention because of “bad trips”. • Severe agitation may require medication: diazepam is effective.
43
Overview and actions of Phencyclidine?
• Dissociative anesthetic. • Blocks reuptake of norepinephrine and dopamine. • Causes cholinergic and anticholinergic effects. • Has actions at nicotinic and opioid receptors. • The dissociative properties of PCP are believed to be due to non-competitive antagonism at NMDA receptors.
44
PHENCYCLIDINE: CLINICAL PRESENTATION?
• Clinical manifestations include violent or bizarre behavior, psychosis, nystagmus, tachycardia, hypertension, diaphoresis, miosis, anesthesia, and analgesia. • An important diagnostic clue is nystagmus.
45
PHENCYCLIDINE: TREATMENT?
* There is no specific antidote for PCP. * Extreme violent psychotic behavior requires sedation with parenteral benzodiazepines. * Seizures should be treated with benzodiazepines.
46
Overview of MDMA(ecstasy)?
• MDMA fosters feelings of empathy and intimacy without impairing intellectual capacities. • MDMA causes release of biogenic amines. • It most strongly increases the concentration of serotonin in the synaptic cleft. • Withdrawal is characterized by depression, lasting up to several weeks. • MDMA produces degeneration of serotonergic neurons in rats.
47
Name 3 inhalants?
* NITROUS OXIDE * VOLATILE ORGANIC SOLVENTS * ORGANIC NITRITES
48
Effects of Nitrous oxide?
NITROUS OXIDE • Produces euphoria and analgesia and then loss of consciousness. • Usually taken as 35% N2O mixed with O2. • Administration of 100% N2O may cause asphyxia and death
49
What are categorized under volatile organic solvents, effects, and toxicities?
VOLATILE ORGANIC SOLVENTS • Include gasoline, paint thinner, lighter fluid, glue and degreasers. • Produce sense of exhilaration and lightheadedness. • Toxicity depends on the properties of individual solvents. • Implicated in cancer, cardiotoxicity, neuropathies and hepatotoxicity.
50
Describe organic nitrites?
ORGANIC NITRITES • Amyl nitrite and butyl nitrite are used to enhance erection. • They are not addictive.
51
What are anabolic steroids used for?
• Used to increase muscle size by body-building | competitors.

Pharmacology (49 decks)

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