8.1: Drug of Abuse Flashcards by Margaux Amaro

No medical indication
Abuse vs Misuse
Euphoria
Altered perception
“Compulsive” 🡪 Addiction

Drug of Abuse

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Identify if Dependence or Addiction:

Physical
Tolerance
Withdrawal Syndrome

Dependence

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Identify if Dependence or Addiction:

Psychological
Compulsion
Relapsing
Craving

Addiction

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Identify what Regulation Schedule:

High potential for abuse, no known medical use and lacks accepted safety for use.

Schedule I

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What are the examples of Schedule I?

Heroin
Lysergic acid diethylamide

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Identify what Regulation Schedule:

Potential for abuse with proven and accepted medical use but WITH SEVERE RESTRICTIONS, because abuse may cause severe psycho/physio dependence.

Schedule II

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What are the examples of Schedule II?

Morphine
Cocaine
Methadone
Methampetamine
Phencyclidine

MoCoMeMeP

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Identify what Regulation Schedule:

Less potential for abuse than schedule I or II; with accepted medical use
Abuse may cause moderate or low physical dependence or high psychological dependence

Schedule III

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Regulation Schedule:

What are the examples of Schedule III?

Anabolic steroids
Codeine with hydrocodone
Aspirin or Tylenol

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Identify what Regulation Schedule:

The drug or other substance has a low potential for abuse relative to the drugs or other substances in Schedule III
Abuse of the drug or other substance may lead to limited physical dependence or psychological dependence relative to the drugs or other substances in Schedule III

Schedule IV

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What are the examples of Schedule IV?

Valium
Xanax

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Identify what Regulation Schedule:

The drug or other substance has a low potential for abuse relative to the drugs or other substances in Schedule IV

Schedule V

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Regulation Schedule:

What are the examples of Schedule V?

Cough syrups
Codeine

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What are the pharmacokinetic tolerance?

Reduction of concentration
Shorter duration of action

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What are the pharmacodynamic tolerance?

Recruitment of Adaptor protein (β-arrestin)
Desensitization
Receptor internalization

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Enumerate the withdrawal symptoms:

Restlessness
Eating more than usual
Excessive hunger
Anxiety/tension
Impatience
Depression
Disorientation
Loss of energy/fatigue
Tremors
Craving for cigarettes

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This is a high motivation to obtain and use and has a negative consequences.

Addiction

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They revert back because of the environment and drug availability. It has re-exposure, stress, and context recall.

Relapse

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This alter perception and has no reward/euphoria. It targets cortical and thalamic system.

Nonaddictive Drug of Abuse

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Examples of nonaddictive drug of abuse:

Hallucinogens
Dissociative anesthetics
LSD
PCP/Ketamine
Dextromethorphan

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What are the Class I drugs that Activate G-protein coupled receptors?

GHB
LSD, Mescaline & Psilocybin
Opioids
Cannabinoids

GLOC :3

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What are the Class II drugs that Bind to Ionotropic receptors?

Nicotine
Benzodiazepines
Alcohol
Ketamine & PCP
Inhalants

NiBAKIn

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What are the Class III Drugs that Bind to Transporters of Biogenic Amines?

Cocaine
Amphetamines
Ecstasy (MDMA)

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Identify this nonaddictive drug abuse:

Strong analgesics
Opiates – morphine, codeine, thebaine, papaverine
Narcotic – “sleep inducing”
Leads to respiratory arrest

Opioids

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# Identify the opioid receptor subtypes: - Supraspinal and spinal analgesia - **Sedation** - **Inhibition of respiration** - Slowed gastrointestinal transit - Modulation of hormone and neurotransmitter release

µ (mu)

Identify the opioid receptor subtypes: - Supraspinal and spinal analgesia - Modulation of hormone and neurotransmitter release

δ (delta)

Identify the opioid receptor: - Supraspinal and spinal analgesia - **Psychotomimetic effects** - Slowed gastrointestinal transit

κ (kappa)

What are the common opioid analgesics that are strong agonist (+++,++, ++)?

- Morphine - Oxycodone - Hydromorphone - Oxymorphone - Methadone - Meperidine - Fentanyl - Sufentanil - Alfentanil - Remifentanil - Levorphanol MOHOMMFeSARL :D

What are the common opioid analgesics that are **partial or weak agonist** (±)?

- Buprenorphine - Butorphanol - Codeine - Hydrocodone - Pentazocine BuBuCoHyP :P

What are the common opioid analgesics that are antagonist (-)?

Nalbuphine

Plant source of opioids:

*Papaver somniferum*

# True or False: Opioids is a **powerful narcotic painkiller** where the principal active ingredient is **morphine.**

True

Mode of administration of opioids:

Subcutaneous, Intravenous

Effects of opioids:

Insomnia, hallucination, nightmares

# True or False: Opioids is a histamine release and have more pronounced effects than heroin.

True

It is a **diamorphine addictive drug** as a **white or brown powder** that tends to be used with other drugs.

Heroin

Mode of administration of Heroin:

Fast-acting; Intravenous

What is the half-life of heroin?

3-5 hours, several doses per day

Hours of withdrawal of heroin:

5-10 hours after

It is **derived from codeine** and synthesized from **thebaine**. This type of drug is in **tablet** or **oral** form.

Oxycodone

This type of drug has a **serious interaction with MAO’s**, and has resulted in **MPTP** which can cause **parkinsonism**.

Meperidine (pethidine; Demerol)

# Degrees of tolerance: What are the effects of **high degree** of **opioid efficacy**?

- Analgesia - Euphoria, dysphoria - Mental clouding - Sedation - Respiratory depression - Antidiuresis - Nausea and vomiting - Cough suppression

# Degree of tolerance: What are the effects of **moderate degree** of opioid efficacy?

Bradycardia

# Degrees of tolerance: What are the effects of **minimal or none degree** of **opioid efficacy**?

- Miosis - Constipation - Convulsions

What are the **adverse effects** of opioid analgesics in **acute** use?

- Respiratory depression - Nausea/vomiting - Pruritus - Urticaria - Constipation - Urinary retention - Delirium - Sedation - Myoclonus - Seizures

What are the **adverse effects** of opioid analgesics in **chronic** use?

- Hypogonadism - Immunosuppression - Increased feeding - Increased growth hormone secretion - Withdrawal effects - Tolerance, dependence - Hyperalgesia - Impairment while driving

# Identify what drug group based on the interaction with opioids Increased CNS depression, particularly respiratory depression.

Sedative-hypnotics

# Identify what drug group based on the interaction with opioids: Increased **sedation**, variable effects on **respiratory depression.** Accentuation of **cardiovascular effects** (antimuscarinic and α-blocking actions).

Antipsychotic agents

# Identify what drug group based on the interaction with opioids: **Relative contraindication** to all opioid analgesics because of the **high incidence of hyperpyrexic coma**; **hypertension** is also reported.

Monoamine oxidase inhibitors

# Identify the opioid drug interaction - alcohol, barbiturates, benzodiazepines, gamma-hydroxybutyric acid (GHB) - can be short- to long-acting - the longer the duration the less the withdrawal - **anxiety**, tremors, twitches, vomiting

Sedative-hypnotics

Clinical uses of sedative-hypnotics:

- Relief of anxiety - Insomnia - Sedation and amnesia before and during medical and surgical procedures - Treatment of epilepsy and seizure states - Component of balanced anesthesia (IV administration) - Control of ethanol or other sedative-hypnotic withdrawal states - Muscle relaxation in specific neuromuscular disorders - Diagnostic aids or for treatment in psychiatry

# Identifythis nonaddictive drug use: - **rare occurrence** of physiologic dependence - ***“Therapeutic Dose Dependence”*** - weight loss, change in perception, paresthesia, headache

Benzodiazepines

What type of **benzodiazepine drug** is used for date rape and has a **Schedule IV** and **anterograde amnesia?**

Flunitrazepam (Rohypnol)

- GABAa receptors - usually short-acting drugs - not used as much as other drugs

Barbiturates

Example of drugs of barbiturates:

Secobarbital, pentobarbital Na

# Identify this non-addictive drug of abuse: - euphoria - Alcoholism - Affect **GABAa and NMDA** - withdrawal (motor agitation, anxiety, insomnia, hallucination, abnormal vital signs, seizures)

Alcohol

# Identify this nonaddictive drug abuse: - **GABAb** - naturally found in body - can be found in **fermented drinks like guava** (Psidium guajava) - euphoric, sedative, anabolic - widely sold until **1992** - liquid ecstasy, soap, easy lay, vita-G - **Georgia homeboy** - use with alcohol can produce **breathing problems**

Gamma Hydroxybutyric Acid

What are the withdrawal effects of Gamma Hydroxybutyric Acid?

Insomnia, anxiety, tremors, sweating

What is the treatment for short and long acting drugs?

Chlordiazepoxide or Phenobarbital

What is the treatment for alcohol?

Disulfiram, naltrexone

Plant source of Cannabinoids:

Cannabis sativa

# Identify this nonaddictive of abuse: - **CB1 receptors** - Can be smoked or joined with ingredients in making **brownies** or **fermented products** (beer) - Effects in **2-3 inhalations** (“high,” euphoria, laughter, relaxation) - **Schedule I**

Cannabinoids

# Identify this drug: - **Antiemetic** - tolerance - uncertain effect on fetus - **Amotivational syndrome** - **diseases related to smoking**

Marijuana

Examples of Cannabinoids:

- Dronabinol - Nabilone (chemotherapy) - Nabiximol (MS)

What are the four hallucinogens that cause hallucinations?

- LSP - PCP - Ketamine - Scopolamine

Plant source of LSD:

Claviceps purpurea

Identify what hallucinogens: - synthetic agent related to **ergot alkaloids** - NE, dopamine, serotonin - **5-HT1a & 5-HT1c agonists** - one of the most potent drugs **1ug/kg** - absence of known fatalities - duration based on dose - waxing and waning effects

LSD (Lysergic acid diethylamide)

# Identify what Hallucinogen based on its effects: * rise in body temp * Hallucinations * **uterine contractions** * **elevated sugar levels** * goosebumps * Euphoria * **pupil dilation**

Lysergic acid diethylamide (LSD)

Plant source of Mescaline:

Lophophora williamsii

# Identify what hallucinogens: * restricted but allowed occasionally to **North American Indians** * **5-6mg/kg**

Mescaline

# Identify what hallucinogen: - **250ug/kg** - **mydriasis**, muscle relaxation, dizziness

Psilocybin

Plant source of Psilocybin:

Psilocybe mushroom

# Identify what hallucinogen: - anesthetic - **“special K” “vitamin K”** - dream-like states, hallucination, delirium, amnesia, high BP, depression, - **fatal respiratory problems**

Ketamine

# Identify what hallucinogen: - **veterinary anesthetic** - smoked with tobacco, snorted - MOA: **Oral**, **IV** - **antagonize NMDA** - animals will self administer it - **Olney’s lesions** - long t1/2 - users tend to be **violent and suicidal** - **“bad-trips”**

Phencyclidine (angel dust, PCP)

Plant source of Scopolamine:

Hyoscyamus niger

# Identify what hallucinogen: - **block central muscarinic receptors** - unpleasant to users - same effects as other hallucinogen - **"Devil's breath"**

Scopolamine

Plant source of Cocaine:

Erythroxylon coca

# Identify what hallucinogen: - **dopaminergic reuptake transmitter** - inhibit reuptake of dopamine and NE - free base is absorbed as fast as **IV** - t1/2= **1hr**, repeated **30min**

Cocaine

# Identify what hallucinogen based on its effects: - symptoms include a **feeling of bugs under skin** - paranoia and schizophrenia like state - exhaustion by lack of sleep and food appetite, exhaustion, depression

Cocaine

# Identify what hallucinogen: - increase **catecholinergic neurotransmitters** - **dopamine** not be metabolized thus **released** - treat **narcolepsy** and **ADHD** - **paranoid psychosis** - **necrotizing arteritis** - OD is rarely fatal - managed by benzodiazepines

Amphetamines | alpha-methyl-phenethylamine

# Identify what hallucinogen: - **Schedule II** - decreased appetite, increase stamina, energy sexual drive - **loss of REM sleep**, tremor, restlessness, anxiety, - related drugs (shabu, ecstasy)

Amphetamines

What are the drugs that targets the **NMDA receptor antagonist**?

Phencyclidine, ketamine

What is the drug that targets **acetylcholine receptor agonist** (nAChr)?

Nicotine

What are the drugs that **reverses transport** of serotonin receptor (SERT) **>** dopamine receptor (DAT) and norepinephrine receptor (NET)?

Ecstasy

What is the drug that **inhibits** dopamine receptor (**DAT**), serotonin receptor (**SERT**), and norepinephrine receptor (**NET**)?

Cocaine

What is the drugs that **reverses transport** of dopamine receptor (**DAT**), norepinephrine receptor (**NET**), serotonin receptor (**SERT**), and vesicular monoamine transporter (**VMAT**)?

Amphetamine

What is the drug that targets the **GABAa receptor positive modulator**?

Benzodiazepines

What is the drug that targets the **GABAa receptor positive modulator, 5-HT3 receptor, nAChR, NMDAR, Kir3 channels**?

Alcohol

What is the drug that targets **5-HT(2A)R partial agonist**?

LSD, mescaline, psilocybin

What is the drug that targets **μ (Mu) receptor agonist**?

Opioids

What is the drug that targets **CB1 receptor agonist**?

Cannabinoids

What is the drug that targets **GABAb receptor weak agonist**?

γ-Hydroxybutyric acid (GHB)

# Identify this substance of abuse: - **“uppers”** - **reverse the effects of fatigue** on both mental and physical tasks. - **Nicotine** - tobacco products - **Caffeine** - coffee, tea, some soft drinks, and many non-prescription medicines

Stimulants

Plant source of Nicotine:

Nicotiana tobacum

Identify this substance of abuse: - **nicotinic cholinergic receptor agonist** - **1 drop is fatal** - strong psychological and physiological dependence (more addictive than heroin and cocaine) - dopamine - SIDS, carcinogenic

Nicotine

Identify this substance of abuse: - adenosine receptors - low chance of abuse and addiction - 5 cups/ day

Caffeine (1, 3, 7-trimethylxanthine)

# Identify this substance of abuse: - anesthetic gases - industrial solvents - aerosol propellants - organic nitrites

Inhalants

Identify this substance of abuse: - psychoactive effects - alcohol-like intoxications, hallucinations, - hypoxia, pneumonia, cardiac failure - headache, nausea, vomiting, slurred speech, loss of motor coordination, wheezing

Inhalants

# Identify this substance of abuse: - difficulty in concentrating, **dreaminess**, euphoria, **numbness**, tingling - **N2O = 35% used; 100% death** - **ether** & **chloroform**

Anesthetics

# Identify this substance of abuse: - gasoline, toluene, benzene, trichloro-ethylene - 5-15min - euphoria, “drunk” feeling, disorientation (slow passage of time) - Eg. Glue, correction fluid, gas

Industrial solvents

# Identify this substance of abuse: - **amyl nitrite, isobutyl nitrite** - dizziness, rapid heart rate, lowered BP, “speeding,” **flushing of skin** - enhance, **prolong erection**

Organic nitrites

# Identify this substance of abuse: * Liver, kidney, peripheral nerve, and brain damage * bone marrow suppression * pulmonary disease * death

Toxicities

# Identify this substance of abuse: - cyclopentanoperhydrophenanthrene ring - bone growth, appetite, puberty, muscle growth - **Schedule III** - change in libido, irritability, violence, mood swings, forgetfulness, confusion - fatigue, depressed mood, craving for steroids

Anabolic Steroids

# Identify this substance of abuse: - hypertrophied muscles, acne, oily skin, **hirsutism in females**, **gynecomastia in males**, needle punctures - high LDL; low HDL - **elevated liver function**

Anabolic Steroids

A **nonselective antagonist** drug that is used for **opioid overdose.**

Naloxone

An **antagonist drug** that is used for **treatment for alcoholism, opioid addiction.**

Naltrexone

A **slow-acting agonist** of **μ-opioid receptor** that is used for **substitution therapy for opioid addicts.**

Methadone

An **"enantiopure" methadone** containing only the **left-enantiomer** of the molecule that is used for **substitution therapy**.

Levomethadone

A salt containing **morphine sulfate pentahydrate** that is used for **substitution therapy**.

Morphine sulphate

A **partial agonist** at **μ-opioid receptors** that is used for **oral substitution therapy** for opioid addicts.

Buprenorphine

A **partial agonist** of **nicotinic acetylcholine receptor** that is used for **smoking cessation.**

Varenicline

A **positive modulator** of the **GABAa receptors** that **increases frequency of channel opening** and is used for **delirium tremens.**

Oxazepam

An **antagonist** of **NMDA glutamate receptors** that is used for **treatment of alcoholism**.

Acamprosate

A **CB1 receptor inverse antagonist** drug that is used to treat obesity but withdrawn, smoking cessation but not approved, but remains an **off-label indication**.

Rimonabant

An **agonist melatonin receptor** hypnotic drugs that is used for patients who have difficulty in falling asleep, and is located in the **suprachiasmatic nuclei** of the brain.

Ramelteon

A **5-HT receptor partial agonist** drug that has a **slow-onset of anxiolytic effects** and has a **minimal psychomotor impairment**.

Buspirone

An **orexin antagonist** that **blocks the binding** of orexins, neuropeptides that promote **wakefulness.**

Suvorexant

**Newer hypnotics** that **bind selectively** to GABAa subgroup receotors, **acting like Benzodiazepines** to enhance membrane hyperpolarization.

* Eszopiclone * Zaleplon * Zolpidem

**Barbiturate drugs** that is a dose-dependent depressant effects on the CNS and has a **steeper dose-response relationship** than Benzodiazepines.

- Amorbital - Butabarbital - Mephobarbital - Pentobarbital - Phenobarbital - Secobarbital

An **antagonist drug** at **benzodiazepine-binding** sites on the GABAa receptor.

Flumazenil

**Benzodiazepine drugs** that is a **dose-dependent depressant** effects on the CNS.

- Alprazolam - Chlordiazepoxide - Clonazepam - Clorazepate - Diazepam - Estazolam - Fluazepam - Lorazepam - Midazolam - Oxazepam - Quazepam - Temazepam - Triazolam bwct basta puro am last

A **barbiturate drug** that is lipid-soluble, intravenous administration, and use for the **induction of anesthesia.**

Thiopental and methohexital

8.1: Drug of Abuse Flashcards

(122 cards)