Pharm/Tox Exam 2

pure food and drug act

prohibit the manufacture, sale, or transportation of adulterated, misbranded, poisonous, or deleterious foods, drugs, medicines, and liquors in interstate and foreign commerce

harrison narcotics act

regulated and taxed the production, importation, and distribution of opiates and coca products

marijuana tax act

placed a severe excise tax and complex registration system on the sale, possession, and cultivation of cannabis, effectively criminalizing the drug at the federal level

acidic

marijuana is one of the few ___ drugs

the 5-member Carbon chain

what part of Marijuana’s structure makes it stay in the fat?

roughly 30 days

how long does marijuana stay in the urine

increase amount of DA in the NAc

marijuana binding to the CB1 and CB2 receptors in linked to ___

link to opioid system

some of marijuana’s effects are reversed by narcan, which implies ___

decreased glutamate and GABA release

activation of CB1 receptor by marijuana leads to ___

excitatory

glutamate is the primary ___ neurotransmitter

inhibitory

GABA is the primary ___ neurotransmitter

10-35%

inhaled bioavailability of marijuana ranges from ___

7 days

half life of marijuana

30+ days

total elimination of marijuana could take ___

4-5 days

marijuana peaks in the fat in about ___

liver, CYP450

marijuana is metabolized in the ___, mainly by ___

glucuronidated

marijuana must be ___ before being excreted in the urine

30-40 minutes, 4-6 hours

after inhalation of marijuana, effects hit after ___ and can last ___

it is lipophilic and blood is hydrophilic

the bioavailability of marijuana is low because ___

highly lipophilic

marijuana binds to plasma proteins because it is ___

hydroxylated and oxidized

marijuana is easier to get out of the body when it has been ___

DA

many people will say marijuana isn’t addictive because they think it doesn’t have effects on ___

antiemesis

what is the depressive effect of marijuana

time seems to move faster, colors look brighter, emotions are more meaningful, hallucinations

what are the perception changes from marijuana

enhancing the CNS depression to dangerous levels

marijuana interacts with muscle relaxers and benzos by ___

analgesia without hallucination

John W. Huffman began creating synthetic cannabinoids in search of

full agonists

synthetic cannabinoids are ___

make drugs more potent because they get through the BBB faster

how do halogens affect drugs

Ring system-provides steric requirements for receptor interaction

Oxygen off the ring system-allows for hydrogen bonding with the receptor

Alkyl side chain-allows for hydrophobic interactions with the receptor

what are the three requirements for the pharmacophore of synthetic cannabinoids

smaller

does a smaller or larger binding affinity mean a more potent drug

CB1 and CB2

like marijuana, synthetic cannabinoids bind to the ___ receptors

full

are synthetic cannabinoids full or partial agonists at the CB receptors

Hypothermia, analgesia, catalepsy, and hypolocomotion

synthetic cannabinoid tetrad effects

vegetation bought at garden stores

dilute drug in acetone

spray on plant that was ground up

acetone evaporates and the powder is left on the plant

describe how synthetic cannabinoids are made

CYP450

many synthetic cannabinoids are metabolized by ___

active metabolites

marijuana and synthetic cannabinoids both create

hydroxylation and glucuronidation

what must occur in order to make an inactive metabolite of synthetic cannabinoids

hallucinogen

a psychoactive agent that can cause hallucinations, perceptual anomalies, or other substantial changes in though, emotion and consciousness

harmaline

DMT is very fast acting unless mixed with ___

ergot & ergotism

what fungus is LSD found in and what is it known to cause

5HT2A

LSD binds and activates ___

personally perceive stimuli

current belief is that LSD affects how people ___

1A, 1B, 2A, 2C

what serotonin receptors affect addiction

71%

oral bioavailability of LSD

3 hours

half-life of LSD

6-10 hours depending on dose

psychological effects of LSD generally last between ___

CYP450

main metabolism enzyme for LSD

hydroxylation, glucuronidation

metabolism of LSD includes ___ followed by ___

DMT and harmaline

what is ayahuasca made of

MAOI

adding a ___ to DMT is what lengthens effects because it stops metabolism

sympathomimetic

mimicking sympathetic nervous system

2 methyls on the Nitrogen

what part of DMT’s structure makes it so lipophilic

5HT

DMT has the highest affinity to the ___ receptor

5-15 minutes

if inhaled, DMT only lasts ___

100 minutes

taken orally as ayahuasca, DMT peaked around ___

nausea and vomiting

most common side effect of DMT

magic mushrooms

psilocybin is also known as ___

2 methyls

what structure on psilocybin makes it so lipophilic

5HT

psilocybin binds to the ___ receptors

psilocybin → psilocin → phase 1 metabolism-oxidation rxns → phase 2 glucuronidation

aqueous → less aqueous → very aqueous

what are the steps of metabolism of psilocybin

3 hours

half life of psilocin

10-40 minutes, 2-6 hours

effects of psilocybin begin ___ after ingestion and typically last ___

seratonin

PCP mimics ___ even though they don’t look similar

dissociative anesthetics (not true hallucinogens)

PCP and ketamine are classified as ___

dissociative anesthetics

a feeling of disconnection or detachment from the environment and the body

angel dust and rocket fuel

PCP is also known as ___

NMDA receptor antagonist

PCP acts as an ___

IV

when used medically, how is PCP administered

orally, IV, nasal, smoking

when used illicitly, how is PCP taken

30 seconds - 5 minutes

if taken via IV or inhalation, effects of PCP hit after ___

15-60 minutes

if taken orally, effects of PCP hit after ___

typically 4-6 hours, but can last up to 2 days

how long do the effects of PCP last

yes

can PCP cross the BBB easily

hydroxylation by CYP450, glucuronidated

metabolism of PCP includes ___, then the metabolites are then ___ before excretion

fast

are ionotropic receptors fast or slow

you removed a methyl group

what does “nor” mean

wanted a less hallucinogenic compound than PCP

why was ketamine synthesized

vet med

what is ketamine primarily used for today

glutamate, ionotropic

NMDA receptors are activated by ___ and are ___

antagonists prevent the receptor from activating and sending pain signals

how do PCP and ketamine prevent pain

IV or IM

ketamine is usually administered via ___

93%

ketamine IM bioavailability

near 100%

ketamine IV bioavailability

CYP3A4, CYP2B6, norketamine

Ketamine undergoes extensive metabolism by ___ and ___ to turn it into ___

2-4 hours

half life of ketamine

euphoria

what is the NAc for

decision making

what is the PFC for

emotional response

what is the amygdala for

memory

what is the hippocampus for

learning and cognition

what is the VTA for

a natural or synthetic substance that has psychological or physiological effects on the body

definition of a drug