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BPS > Kruse DSA: Drugs of Abuse > Flashcards

Kruse DSA: Drugs of Abuse Flashcards

1
Q

Opioid receptor antagonists

A
  • Naloxone

- Naltrexone

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2
Q

Synthetic Opioid

A

methadone

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3
Q

Partial Mu opioid receptor agonist

A

-buprenorphine

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4
Q

Nicotinic receptor partial agonist

A

-Varenicline

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5
Q

Benzodiazepines

A
  • oxazepam

- lorazepam

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6
Q

NMDA receptor antagonist

A

acamprosate

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7
Q

What is abstinence syndrome

A

-the signs and sx that ocur on withdrawal of a drug in a dependent person

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8
Q

addiction

A

-compulsive drug-using behavior in which the person uses the drug for personal satisfaction, often in the face of known risks to health; formerly termed psychological dependence

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9
Q

Controlled substance

A

-drug that has abuse liability that is listed on governmental schedules of controlled substances

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10
Q

Schedule 1

A

-no medical use; high addiction potential

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11
Q

Schedule 2

A

-medical use; high addiction potential

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12
Q

Schedule 3

A
  • medical use

- moderate abuse potential

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13
Q

Schedule 4

A

-Medical use; low abuse potential

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14
Q

Dependence

A

-a sate characterized by signs and sx, frequently the oppostite of those caused by a drug, when it is withderawn from chronic use or when the dose is abruptly lowered

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15
Q

Designer drug

A
  • a synthetic derivative of a drug, with slightly modified structure but no major change in pharmacodynamic action
  • circumvention of the schedule of controlled drugs is a motivation for the illicit synthesis of designer drugs
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16
Q

=Tolerance

A
  • a decreased response to a drug, necessitating larger doses toachieve the same effect
  • this can result from increased disposition of the drug, an ability to compensate for the effects of a drug, or changes in receptor or effector systems involved in drug actions
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17
Q

Sensitization

A

-an increase in response with repetition of the same dose of the drug

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18
Q

Withdrawal

A
  • adaptive changes that become fully apparent once drug exposure is terminated; generally due to readaptation of the CNS to the absence of the drug of dependence
  • withdrawal is the evidence of physical dependence
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19
Q

If we knock out the D2 receptors, what did we eliminate?

A

-the reward properties of morphine

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20
Q

Is the dopaminergic pathway responsible for the positive reward AND the negative withdrawal effects?

A
  • no!

- just the positive reward

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21
Q

What are the 3 classes of molecular targets that have been identified in the mesolimbic system?

A
  • Gio coupled receptors
  • ionotropic receptors
  • Monoamine transporters
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22
Q

Which drugs get the Gio receptors?

A
  • Opioids
  • Cannabinoids
  • Gamma hydroxybutyric acid
  • LSD
23
Q

Drugs thatbing to ionotrpic receptors and ion channels

A

-Nicotine
-Alcohol
-Benzos
=-Phencyclidine, ketamine

24
Q

Drugs that bind to transporters of biogenic amines

A
  • Cocaine
  • Amphetamine
  • Ecstasy
25
Q

What are the nonaddictive drugs of abuse?

A
  • LSD, mescaline, psilcybin

- Phencyclidine (PCP, angel dust) and ketamine (Special K)

26
Q

What do drugs that activate Dio coupled receptors do?

A

-cause disinhibition of DA neurons

27
Q

What do mu opioids do in the VTA?

A

-inhibit the GABA ergic inhibitory interneurons, which leads toa disinhibition of DA neurons

28
Q

How do you treat the withdrawal sx of opioids?

A

-With naloxone!

29
Q

MOA of naloxone

A
  • pure opioid antagonist that reverses effects of a dose of opiates within minutes
  • provokes an acute withdrawal syndrome in situations where a dependent person has opiates in their system (so probs make sure they’re out of there)
30
Q

Methadone, buprenorphine

A
  • long acting opioids used for substituion therapy
  • tolerance and physical dependence develop more slowly in comparison to other opioids
  • given with supervised intake
  • abrupt discontinuation precipitates a withdrawal syndrome
31
Q

What do endocannabinoids do?

A

-bind to presynaptic CB1 receptors and inhibit the release of either glutamate or GABA

32
Q

What does THV do?

A

-cuases disinhibition of DA neurons by presynaptic inhibition of GABA neurons in the ventral tegmental area (VTA)

33
Q

What is dronabinol?

A

-FDA approved THV analog used for anorexia and weight loss in AIDS pts and cancer-chemotherapy induced nausea and vomiting

34
Q

What is Nabilone?

A

-THV analog used for the tx of refractory nausea and vomiting associated with cancer chemotherapy and as an adjunct in chronic pain management

35
Q

What is Gamma hydroxybutyric acid (GHB)?

A

-produced during the metabolism of GABA, but the endogenous function is unknown
-GABAb receptor
-date rape drug
-hyperpolarizes DA neurons and inhibits DA release at high conc….
only inhibits GABA neurons for recreational use

36
Q

What does GHB target?

A

-GABAb receptors on both GABA and DA neurons, but those on GABA neurons are more sensitive to GHB and lead to disinhibition of DA neurons when activated

37
Q

How does THC act?

A

-presynaptic inhibition

38
Q

MOA for nicotine

A
  • selective agonist of the nAChR

- Neuronal nAChRs are expressed on DA neurons in the VTA; activatin fulfills the DA requirement of addictive drugs

39
Q

Tx for Nicotine addiction

A
  • gum, lozenge, inhalers, transdermal applications
  • Bupropion
  • Varenicline
40
Q

What does Bupropion do?

A
  • antidepressant with unknown MOA

- Used alone or in combo with nicotine-replacement therapy and/or behavioral therapy

41
Q

What does Varenicline do?

A
  • partial neuronal nAChR agonist approved for treating smoking cessation
  • prevents nicotine stimulation of mesolimbic dopamine system associated with nicotine addiction
42
Q

What are some examples of biogenic amine transporters?

A

-DAT, NET, VMAT, and SERT

43
Q

Cocaine

A
  • local anesthetic in peripheral nervous system
  • Blocks the DAT and increases the DA concentration in the nucleus accumbens (rewarding)
  • Blocks NET and activates the symp nervous system, high pressure, tachy, vetnricular arrhythmias, pupil dilation!
44
Q

Is there an antidote for cocaine overdose?

A

no

45
Q

MOA of ampthetamines

A
  • cause the release of endogenus biogenic aminesby reversing the action of biogenic amine transporters at the plasma membrane
  • taken up into cell by DAT
  • block intracellular VMAT, depletes vesicles of NT content
  • DA and other amines increase inthe cytoplasm, flow out through the DAT the other way into the synapse!!!
46
Q

Ecstasy MOA

A
  • similar to amphetamines (reverse action of biogenic amine transporters
  • Preferential affinity for the SERT and increases EC concentration of serotonin
47
Q

What are the acute toxic effects of MDMA (ecstasy)?

A

-hyperhtermia, dehydration, serotonin syndrome, and seizures

48
Q

overdose effects of amphetamines and cocaine

A

-agitation, htn, tachycardia, delusions, hallucinations, hyperthemia, seizures, death

49
Q

withdrawal sx for amphetamines and cocaine

A

-apathy, iritability, increased sleep time, disorientation, depression

50
Q

Overdose effects for barbiturates, benzodiazepines, ethanol

A

-slurred speech, drunken behavior, dilated pupils, weak and rapid pulse, clammy skin, shallow respiration, coma, death

51
Q

Withdrawal sx for barbiturates, benzos, and ethanol

A

-anxiety, insomnia, delirium, tremors, seizures, death

52
Q

Overdose effects of heroin, other strong opioids?

A

-constricted pupils, clammy skin, nausea, drowsiness, respiratory depression, coma, death

53
Q

Withdrawal sx for heroin and other strong opioids

A

-nausea, chills, cramps, lacrimation, rhinorrhea, yawning, hyperpnea, tremor

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