MT6314 DRUGS OF ABUSE Flashcards by JASMINE GRACE DE GUZMAN

T OR F: Drugs of abuse have medical indication

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“Compulsive” use leads to?

Addiction

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Drugs of abuse mainly cause?

Euphoria and altered perception

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Dependence or Addiction: Physical

Dependence

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Dependence or Addiction: Psychological

Addiction

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Dependence or Addiction: Tolerance

Dependence

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Dependence or Addiction: Compulsion

Addiction

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Dependence or Addiction: Withdrawal syndrome

Dependence

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Dependence or Addiction: Relapsing and Craving

Addiction

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Dependence or Addiction: No psychoactive drugs

Dependence

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What Class: GPCRs

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What Class: Opioids, THC, GHB

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What Class: Benzodiazepines, nicotine

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What Class: ethanol, channels

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What Class: cocaine, ecstasy, amphetamine

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What Class: transporters

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Class 1 and 2 are found in?

Ventral Tegmental Area

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Class 3 is found in?

Ventral Tegmental Area and Nucleus Accumbens

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Pharmacokinetic or Pharmacodynamic Tolerance: reduction of concentration

KINTETIC

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Pharmacokinetic or Pharmacodynamic Tolerance: Shorter duration of action

KINETIC

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Pharmacokinetic or Pharmacodynamic Tolerance: Recruitment of Adaptor protein (beta-arrestin)

DYNAMIC

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Pharmacokinetic or Pharmacodynamic Tolerance: Desensitization and receptor internalization

DYNAMIC

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Example of an adaptor protein?

Beta-arrestin

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Common signs of withdrawal?

Elevated BP, body temp
Tachycardia
Sweating
Tremulousness
Dilated pupils
Disorientation
Hyper arousal
Grand mal seizure

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Symptoms of withdrawal?

Anxiety Insomnia Illusions Hallucinations Paranoid ideas Nausea Irritability

High motivation to obtain and use

Addiction

Has negative consequences

Addiction

Re-exposure Stress Context Call

Relapse

Alter perception, no reward or euphoria

Nonaddictive drugs of abuse

Nonaddictive drugs of abuse target?

Cortical and thalamic systems

Examples of nonaddictive drugs of abuse?

Hallucinogens Dissociative anesthetics LSD PCP/ Ketamine Dextromethorphan

What kind of drug classifications are in the pharmacology of drug abuse?

Drugs that activate G-protein coupled receptors Drugs that bind to ionotropic receptors Drugs that bind to transporters of biogenic amines

WHAT TYPE OF DRUG ACCRDG. TO PHARMACOLOGY: Opioids Cannabinoids

Drugs that activate G-protein coupled receptors

WHAT TYPE OF DRUG ACCRDG. TO PHARMACOLOGY: GHB LSD, Mescaline and Psilocybin

Drugs that activate G-protein coupled receptors

WHAT TYPE OF DRUG ACCRDG. TO PHARMACOLOGY: Nicotine Benzodiazepines Alcohol

Drugs that bind to ionotropic receptors

WHAT TYPE OF DRUG ACCRDG. TO PHARMACOLOGY: Ketamine, PCP Inhalants

Drugs that bind to ionotropic receptors

WHAT TYPE OF DRUG ACCRDG. TO PHARMACOLOGY: Cocaine Amphetamines Ecstacy

Drugs that bind to transporters of biogenic amines

Strong analgesics

Opioids

Examples of opiates?

Morphine Codeine Thebaine Papaverine

"Sleep inducing" opioid

Narcotic

WHAT OPIOID RECEPTOR SUBTYPE: Supraspinal and spinal analgesia; inhibition of respiration, slow GI transit, modulation of hormone and neurotransmitter release

WHAT OPIOID RECEPTOR SUBTYPE: Supraspinal and spinal analgesia, modulation of hormone and neurotransmitter release

delta

WHAT OPIOID RECEPTOR SUBTYPE: Supraspinal and spinal analgesia; psychotomimetic effects, slow GI transit

kappa

Endogenous opioid peptide affinity of mu receptors?

Endorphins > Enkephalins > Dynorphins

Endogenous opioid peptide affinity of delta receptors?

Enkephalins > endorphins and dynorphins

Endogenous opioid peptide affinity of kappa receptors?

Dynorphins >> Endorphins and enkephalins

Scientific name of Opium?

Papaver somniferum

What is an powerful narcotic, painkiller?

Opioids

Principal active ingredient in opioids?

MORPHINE

Effects of opioids?

insomnia, hallucination, nightmares histamine release

Routs of administration of opioids?

SC, IV

Opioids have more pronounced effects than what drug?

heroin

Other names of heroin?

Smack, H, ska, junk

What kind of chemical is heroin?

diamorphine

What form is heroin usually in?

addictive drug as a white or brown powder

T or F: Heroin is usually used alone

F, tends to be used with other drugs

Route and speed of administration of heroin?

fast-acting; IV

Half life of heroin and how many doses?

3-5 hrs, therefore several doses/ day

How long is withdrawal of heroin?

Withdrawal 5-10 hrs after

Oxycodone is synthesized from?

thebaine

Oxycodone is derived from?

codeine

What form is oxycodone usually in?

tablet or oral form

Other names for Meperidine?

pethidine; Demerol

Meperidine has serious interactions with?

MAOIs

Attempts to illicitly produce meperidine has resulted in?

MPTP which can cause parkinsonism

What is MPTP?

MPTP: methyl-phenyl-tetrahydropyridine

What carries the pain signals to the dorsal horn of the spinal cord?

Primary afferent neurons

How do pain signals synapse with the secondary neuron?

via glutamate and neuropeptide transmitters

Pain stimuli can be attenuated in the periphery by what?

opioids acting at opioids receptors

Pain stimuli can be blocked in the afferent axon by?

local anesthetics

APs reaching the dorsal horn can be attenuated at the presynaptic ending by?

opioids calcium blockers (ziconotide) a2 agonists drugs that increase synaptic concentrations of norepinephrine (tapentadol)

T or F: Opioids inhibit the post synaptic neuron

Inhibition of opioid analgesics happen in what part of the nervous system?

spinal cord

Possible site of action of opioid analgesics can be in the?

amygdala anterior cingulate gyrus Dorsal root ganglion ventral posterolateral nucleus in thalamus

Sites of action of opioid in pain modulating neurons in?

medulla with midbrain periaqueductal gray area rotral ventral medulla locus coerculus

What degree of tolerance in opioids: analgesia

high

What degree of tolerance in opioids: bradycardia

moderate

What degree of tolerance in opioids: miosis

minimal or none

What degree of tolerance in opioids: mental clouding and sedation

high

What degree of tolerance in opioids: antidiuresis

high

What degree of tolerance in opioids: respiratory depression and cough suppression

high

What degree of tolerance in opioids: constipation and convulsions

minimal or none

What degree of tolerance in opioids: nausea and vomiting; euphoria, dysphoria

high

What degree of tolerance in opioids: mental clouding, sedation

high

Chronic or Acute use of opioids: urticaria

Acute

Chronic or Acute use of opioids: constipation and urinary retention

Acute

Chronic or Acute use of opioids: respiratory depression; nausea/vomiting

Acute

Chronic or Acute use of opioids: pruritis and delirium

Acute

Chronic or Acute use of opioids: sedation, myoclonus, seizures

acute

Chronic or Acute use of opioids: hypogonadism, immunosuppression

Chronic

Chronic or Acute use of opioids: Increased feeding, increase GH secretion

Chronic

Chronic or Acute use of opioids: Withdrawal effects, tolerance, dependence

Chronic

Chronic or Acute use of opioids: abuse, addiction, hyperalgesia

Chronic

Chronic or Acute use of opioids: Impairment while driving

Chronic

What drug group: Increased CNS depression, particularly respiratory depression

Sedative-hypnotics

What drug group: Increased sedation

Antipsychotic agents

What drug group: Variable effects on respiratory depression

Antipsychotic

What drug group: Accentuation of cardiovascular effects (antimuscarinic and a-blocking actions)

Antipsychotic

What drug group: relative contraindication to all opioid analgesics

Monoamine oxidase inhibitors

MAOIs have a relative contraindication to all opioid analgesics because?

of high incidence of hypercpyrexis coma

What drug group: hypertension has also been reported

Monoamine Oxidase Inhibitors

Examples of sedative hypnotics?

alcohol, barbiturates, benzodiazepines, gamma-hydroxybutyric acid (GHB)

Length of action of sedative-hypnotics?

can be short- to long- acting

T or F: In sedative hypnotics, the longer the duration, the more chances of withdrawal

F, the longer the duration the less the withdrawal

Effects of sedative hypnotics?

anxiety, tremors, twitches, vomiting

Clinical uses of sedative hypnotics?

relief of anxiety insomnia sedation and amnesia epilepsy and seizures component of balances anesthesia (IV) control of ethanol or other sedative-withdrawal states muscle relaxation diagnostic aids

What drug: minor active metabolites

Eszopiclone

What drug: rapid oral absorption

Alprazolam

What drug: active metabolites with long t1/2

Flurazepam

What drug: no active metabolites

Lorazepam and Oxazepam; Zolpidem

What drug: slow oral absorption

Temazepam

What drug: rapid onset, short duration of action

Triazolam

What drug: metabolized via aldehyde dehydrogenase

Zaleplon

What drug: Produg; hydrolyzed to active form in stomach

Clorazepate

What drug: active metabolites; erratic bioavailability from IM injection

Chlordiazepoxide

Has rare occurrence of physiologic dependence

Benzodiazepines

Benzodiazepines are also known as?

“Therapeutic Dose Dependence”

Effects of Benzodiazepines?

weight loss, change in perception, paresthesia, headache

What is used for date rape?

Flunitrazepam Rohypnol: roofies (1mg tab)

What schedule is Flunitrazepam?

Schedule IV

What does Flunitrazepam cause?

anterograde amnesia

What kind of receptors are barbiturates?

GABAa receptors

Length of action of barbiturates?

usually Short- acting drugs

Examples of barbiturates?

Secobarbital, pentobarbital Na

T or F: Barbiturates are more commonly used than the other drugs

F, not used as much as other drugs

What drug leads to euphoria and Alcoholism?

Alcohol

Alcohol affects?

Affect GABAa and NMDA

Alcohol withdrawal leads to what effects?

motor agitation, anxiety, insomnia, hallucination, abnormal vital signs, seizures

Affects GABAb receptors

Gamma Hydroxybutyric Acid

What drug is naturally found in body?

Gamma Hydroxybutyric Acid

Where else can Gamma Hydroxybutyric Acid be found?

can be found in fermented drinks like guava (Psidium guajava)

Gamma Hydroxybutyric Acid is what kind of drug?

euphoric, sedative, anabolic

What form can Gamma Hydroxybutyric Acid take?

liquid ecstasy, soap, easy lay, vita-G

What drug: Georgia homeboy

Gamma Hydroxybutyric Acid

Gamma Hydroxybutyric Acid use with alcohol can cause?

breathing problems

Gamma Hydroxybutyric Acid withdrawal effects include?

insomnia, anxiety, tremors, sweating

Treatment for Gamma Hydroxybutyric Acid for short acting and long acting drugs?

chlordiazepoxide or phenobarbital

Treatment for alcohol?

disulfiram, naltrexone

Main treatment for Gamma Hydroxybutyric Acid?

support groups

Kinds of cannabinoids?

Marijuana

Scientific name of marijuana?

Cannabis sativa

Other names of marijuana?

cannabinol, tetrahydrocannabinol, cannabidiol

Marijuana affects what receptors?

cannabinoid receptors (CB1)

Marijuana is usually taken into the body through?

smoking

How does marijuana take effect?

effects in 2-3 inhalations

What are the effects of marijuana?

“high,” euphoria, laughter, relaxation

What schedule is marijuana?

Schedule I

Marijuana effects on the body?

- antiemetic - tolerance - uncertain effect on fetus - Amotivational syndrome - diseases related to smoking

Examples of medical cannabinoids?

* Dronabinol * Nabilone - Chemotheraphy Px * Nabiximol - Multiple sclerosis

Examples of hallucinogens?

- LSD - PCP - Ketamine - Scopolamine

LSD is known as?

Lysergic acid diethylamide Claviceps purpurea

LSD is a synthetic agent related to?

ergot alkaloids

Neurotransmitters affected by LSD?

norepinephrine (NE), dopamine, serotonin

Agonists affected by LSD?

5-HT1a & 5-HT1c agonists

What is known as one of the most potent drugs 1ug/kg?

LSD

Does LSD have any fatalities?

LSD duration is based on?

dose

What kind of effects does LSD have?

waxing and waning effects * rise in body temp * Hallucinations * uterine contractions * elevated sugar levels * goosebumps * Euphoria * pupil dilation

What drug: Lophophora williamsii

Mescaline

What drug: restricted but allowed occasionally to North American Indians

Mescaline

Usually dosage of Mescaline?

5-6mg/kg

What drug: Psilocybe mushroom

Psilocybin

Usual Dosage of Psilocybin?

250ug/kg

Effects of Psilocybin on the body?

mydriasis, muscle relaxation, dizziness

Ketamine is also known as?

“special K” “vitamin K”

What drug: anesthetic

Ketamine

Effects of ketamine?

dream-like states, hallucination, delirium, amnesia, high BP, depression, fatal respiratory problems

Other names of Phencyclidine?

angel dust, PCP

Phencyclidine is a derivative of?

phenylcyclohexamine

What drug: veterinary anesthetic; animals will self administer it

Phencyclidine

Route of intake of Phencyclidine?

smoked with tobacco, snorted, Oral, IV

Phencyclidine antagonizes?

NMDA

What drug: Olney's lesions

Phencyclidine

Length of t1/2 of Phencyclidine?

long

What drug: users tend to be violent and suicidal; “bad-trips”

Phencyclidine

What drug: Hyoscyamus niger

Scopolamine

Scopolamine blocks what?

central muscarinic receptors

What drug is unpleasant to users?

Scopolamine

Scopolamine is also known as?

Devils breath

What drug: Erythroxylon coca

Coccaine

What transmitter is concerned with cocaine?

dopaminergic reuptake transmitter

Cocaine inhibits the reuptake of?

dopamine and NE

T OR F: Free based cocaine is absorbed slower than IV

F, just as fast

Half life of cocaine?

1hr, repeated 30mins

Symptoms of cocaine include?

- symptoms include a feeling of bugs under skin - paranoia and schizophrenia like state - exhaustion by lack of sleep and food - appetite, exhaustion, depression

What drug: alpha-methyl-phenethylamine

Amphetamines

Amphetamines increase?

catecholinergic neurotransmitters

What is more metabolized and is just released in the use of amphetamines?

dopamine

Amphetamines are used to treat?

narcolepsy and ADHD

Amphetamines causes?

- paranoid psychosis - necrotizing arteritis

T or F: OD in amphetamine use is rarely fatal

Amphetamines are managed by?

benzodiazepines

Schedule of amphetamines?

Schedule II

Effects of amphetamines?

-decreased appetite, inc. stamina, energy sexual drive -loss of REM sleep, tremor, restlessness, anxiety

Related drugs to amphetamines?

shabu, ecstasy

Ecstasy is also known as?

Methylene-dioxymethamphetamine (MDMA)

Ecstasy causes?

intimacy and empathy

What drug: * “raves” designer drug * SERT

Ecstacy

What drug: Agonist

Opioids Cannabinoids

What drug: Activate G-protein coupled receptors

Opioids Cannabinoids GHB LSD, mescaline, psilocybin

What drug: Mol target - m-OR

Opioids

What drug: Mol target - CB1R

Cannabinoids

What drug: Mol target - GABABR

GHB

What drug: Mol target - 5-HT2AR

LSD, mescaline, psilocybin

What drug: Weak agonist

GHB

What drug: Partial agonist

LSD, mescaline, psilocybin

What drug: drugs that bind to ionotropic receptors and ion channels

nicotine alcohol benzodiazepines phencyclidine ketamine

What drug: drugs that bind to transporters of biogenic amines

cocaine amphetamine ecstacy

What drug: Mol target - nAChR

nicotine

What drug: Effect on dopamine receptors - disnhibition

opioids canabinoids GHB benzodiazepines

What drug: Effect on dopamine receptors - blocks DA uptake

cocaine amphetamine ecstacy

Effect on dopamine receptors - excitation

nicotine alcohol

Stimulants are also known as?

uppers

What do stimulants do?

reverse the effects of fatigue on both mental and physical tasks.

Other names of nicotine?

Nicotiana tobacum

Nicotine is an agonist against?

nicotinic cholinergic receptor

How fatal is nicotine?

1 drop is fatal

Effects of nicotine?

strong psychological and physiological dependence (more addictive than heroin and cocaine)

T or F: Nicotine is carcinogenic and causes sudden infant death syndrome

Other names of caffeine?

1,3,7-trimethylxanthine

Caffeine is from?

xanthine alkaloid from Coffea arabica

What kind of receptors is caffeine?

adenosine receptors

T or F: Low chances of abuse and addiction are seen in caffeine

Types of inhalants?

- anesthetic gases - industrial solvents - aerosol propellants - organic nitrites

Effects of inhalants on the body?

- psychoactive effects - alcohol-like intoxications, hallucinations, - hypoxia, pneumonia, cardiac fauilure - headache, nausea, vomiting, slurred speech, loss of motor coordination, wheezing

What has difficulty in concentrating, dreaminess, euphoria, numbness, tingling?

Anesthetics

When are Anesthetics fatal?

N2O= 35% used; 100% death

Examples of anesthetics?

ether & chloroform

Examples of industrial solvents?

gasoline, toluene, benzene, trichloro-ethylene Glue, correction fluid, gas

How many minutes do industrial solvents last?

5-15min

Effects of industrial solvents?

euphoria, “drunk” feeling, disorientation

What substance: amyl nitrite, isobutyl nitrite

Organic nitrites

Effects of Organic nitrites?

- dizziness, rapid heart rate, lowered BP, “speeding,” flushing of skin - enhance, prolong erection

Toxicities of Organic nitrites?

* Liver, kidney, peripheral nerve, and brain damage * bone marrow suppression, * pulmonary disease * death

cyclopentanoperhydrophenanthrene ring

Anabolic Steroids

bone growth, appetite, puberty, muscle growth

Anabolic Steroids

Schedule of Anabolic Steroids?

Effects of Anabolic Steroids?

- change in libido, irritability, violence, mood swings, forgetfulness, confusion - fatigue, depressed mood, craving for steroids - hypertrophied muscles, acne, oily skin, hirsutism in females, gynecomastia in males, needle punctures - high LDL; low HDL - elevated liver function

The most commonly abused drug in the world

Alcohol

Continue consumption of alcohol despite suffering consequences

Alcohol abuse

Inability to control drinking, devoting much time to getting and using alcohol, or recovering from its effects

Alcohol dependence

use disorders are complex; has genetic and environmental factors

Alcohol

Main molecular target of opioids?

mu-OR

Main molecular target of cannabinoids?

CB1 receptors

Main molecular target of GHB?

GABAb

Main molecular target of LSD, mescaline, psilocybin?

5-HT1 receptors

Main molecular target of nicotine?

nACh receptors

Main molecular target of alcohol?

NMDAs and GABAa

Main molecular target of ketamine and PCP?

NMDAR

Main molecular target of benzodiazepines?

GABAa

Main molecular target of Cocaine, Amphetamine and Ecstasy?

Cocaine - DAT, SERT, NET Amphetamine - DAT, SERT, NET, VMAT Ecstasy - SERT > DAT, NET

Pharmacology of benzodiazepines?

Positive modulator

Pharmacology of PCP and ketamine?

Antagonist

"uppers"

Stimulants

What do stimulants do?

Reverse fatigue

Examples of stimulants?

Nicotine and Caffeine

Nicotine is an antagonist of?

nicotinic cholinergic receptors

Nicotine causes increase in what hormone?

Dopamine

Nicotine causes?

SIDS, and cancer (carcinogen)

Caffeine is involved with what receptors?

Adenosine receptors

How much percent of N2O is used to ensure 100% death?

35%

Anabolic steroids are what schedule?

Mu opioid receptor partial / weka agonists

Petazocine Buprenorphine Butorphanol Codeine Hydrocodone

Mu opioid receptor antagonist

Nalbuphine

Delta opioid receptor antagonist

Buprenorphine

Delta opioid receptor agonist (+)

Sufentanil

Kappa opioid receptor agonist (+)

Morphine Sufentanil Pentazocine

Kappa opioid receptor agonist (++,+++)

Nalbuphine (++) Butorphanol (+++)

Kappa opioid antagonist

Buprenorphine

MT6314 DRUGS OF ABUSE Flashcards

(269 cards)