Pharmacology & Toxicology Exam 1

pharmacology and toxicology

the effect of drug on body / adverse effects of drugs on body

euphoria

state in which one feels pleasure / excitement and intense feelings of joy and happiness

dysphoria

state in which the person feels intense dissatisfaction or unease, possibly resulting in anxiety, agitation, or outward physical distress

addiction

most severe, chronic-stage of substance use disorder in which there is a substantial loss of self control

craving

strong desire or urge

substance use disorder

clinical diagnostic term used in the fifth edition of DSM-5

2 or more within 12 months

how many symptoms do you need to present with and how often to be diagnosed with substance abuse disorder

positive

craving is linked to ___ reinforcement

negative

lack of control is linked to ___ reinforcement

binding to receptors, effects on signaling, downstream consequences of that signaling

pharmacology is ___ (3)

adverse effects on signaling, usually concerned with things like ED₅₀ and LD₅₀

toxicology is ___ (2)

effective dose for 50% of population to respond

what is ED₅₀

lethal dose to kill 50% of population

what is LD₅₀

they have larger litters and are adults within ~3 months

why are rats typically used as test subjects

dogs

which animals are the closest bone models to humans

85%

what percentage of the time, if it happens to animals, it’ll happen to humans

cell lines to animals to healthy humans to disease-state humans

order of testing / test subjects

decision making and impulse control

what is the prefrontal cortex for

processed pleasure

what is the nucleus accumbens for

processes emotions and triggers survival responses

what is the amygdala for

memory and learning

what is the hippocampus for

releases dopamine

what is the ventral tegmental area for

physiology

study of a living system

receptors

proteins that receive a signal and causes a response

inotropic, G-protein, kinase linked, and nuclear

4 types of receptors

inotropic and G-protein receptors

which two types of receptors work together to give better control over the system

inotropic

which receptor is fast acting

G-protein

which receptor is slow acting

cationic and anionic

two types of inotropic receptors

drug

natural or synthetic and must have physiological or psychological effects

absorption, distribution, metabolism, and excretion

what does ADME stand for

ADME

acronym for pharmacokinetics

oral, inhalation, insufflation, injections, topical, buccal, and anal

common routes of administration of drugs

Cytochrome P450

responsible for the breakdown of most things in the body

VTA increases in size while the NAc decreases in size

how do the VTA and the NAc change in size with addiction

morphine and codeine

what are the two natural drugs

sympatheic nervous system

fight or flight is accomplished through the ___

methamphetamine only differs by the addition of a methyl group

how does methamphetamine differ from amphetamine

increased

amphetamine causes a(n) ___ amount of dopamine in synapse

being a full agonist to the trace amine-associated receptor 1 (TAAR1) and by inhibiting function at the vesicular monoamine transporter 2 (VMAT2)

what are the two ways amphetamine increases the amount of dopamine, norepi, and serotonin in the synapse

far less pronounced

the effects of amphetamine on serotonin are the same as dopamine and norepi, except

75%

taking amphetamine orally will have an availability of ___

15-40%

what percentage of left over amphetamine is bound to plasma proteins in the blood

diet

the absorption of amphetamine is dictated by one’s ___

CYP2D6 and Dopamine β-hydroxylase

main enzymes involved in metabolism of amphetamines

persistent depletion of dopamine leads to terminal degradation meaning some terminals are removed and you can’t activate something that’s not there

how do you build a tolerance

dopamine dysregulation syndrome: randomly dropping dopamine into the system

what is punding

tolerance (nerve terminal degeneration), punding, agitation, and paranoia

what are the four effects amphetamine will have on the CNS

tachycardia and edema

what are the two effects of amphetamine on the cardiac system

tachycardia

increased heart rate

edema

swelling

they have a compound effect because they both result in increased amounts of dopamine and norepi in the synapse

how do monoamine oxidase inhibitors (MAOIs) and antidepressants interact with amphetamines

3: a₁, a₂, and b₃

how many receptors does ephedrine bind to and what are they

adrenergic

what type of receptors does ephedrine bind to

in smooth muscle

where are a₁ receptors located

in coronary smooth muscle

where are a₂ receptors located

in bronchiole smooth muscle

where are b₂ receptors located

vasoconstriction

activation of the a₁ receptor from ephedrine leads to ___

anorexia

centrally, activation of the a₁ receptor by ephedrine causes ___

sedation and analgesia

centrally, activation of the a₂ and ß₂ receptors by ephedrine causes ___

inhibits the release of norepi

activation of the a₂ receptor from ephedrine ___

vasodilation of bronchi

activation of the ß₂ receptor from ephedrine leads to ___

releasing NE from nerve terminals

implication is that ephedrine acts by ___

tachycardia, arythmias, angina, and hypertension

effects of ephedrine on the cardiac system

flushing and sweating

effects of ephedrine on the dermatological system

restlessness/insomnia, confusion, paranoia, and agitation

effects of ephedrine on the CNS

dyspnea and edema

effects of ephedrine on the respiratory system

dyspnea

shortness of breath

edema

swelling caused by excess fluid trapped in your body's tissues

agonist

nicotine is a(n) ___ at nicotinic acetylcholine receptors (nAchRs)

a4ß2, VTA, DA

nicotine activates ___ receptors within the ___, which releases ___

endogenous opioids

nicotine binds to opioid receptors causing the release of ___

sympathetic

nicotine activates the ___ nervous system

release of epinephrine, increased heart rate, blood pressure, respiration, and glucose release

activation of the SNS by nicotine causes ___

increases the amount of various neurotransmitters including DA, 5-HT, NE, Epi, and Endorphins

nicotine is a “volume inducer”, which means it ___

antagonist

nicotine is a(n) ___ at nAchRa₉ and nAchRa₁₀

10-20 seconds

inhaled nicotine reaches the brain in about ___

2 hours

half-life of nicotine

CYP2D6 and Flavin-containing monooxygenase 3 (FMO3)

main enzymes involved in metabolism of nicotine are ___

cotinine

main metabolite of nicotine is ___

menthol

metabolism of nicotine is inhibited by ___

lightheadedness, headache, and irritability

nicotine effects on CNS

atherosclerosis, increased blood pressure, and tachycardia

nicotine effects on cardiac system

DA transporter and serotonin transporter

cocaine binds and blocks the function of ___ (2)

higher amount of DA in the synaptic cleft

cocaine blocking the function of DA transporters leads to ___

higher amount of serotonin in synaptic cleft

cocaine blocking the function of serotonin transporters leads to ___

ion, Sodium, decreases

cocaine has effects on ___ channels, notably ___ channels, which ___ post-synaptic firing

seconds to minutes

cocaine is effective within ___

route of administration

time it takes for the effects of cocaine to hit depends on ___

33%

cocaine bioavailability when taken orally

60-80%

cocaine bioavailability when taken via insufflation

1% unchanged

cocaine excreted only ____ in urine

45-90 minutes

half-life of cocaine

liver

cocaine is extensively metabolized in the ___

P450 and 3A4

main enzymes used in the metabolism of cocaine

esterases

what do the majority of cocaine metabolism

hyperactivity, headache, and potentially seizures

what effects does cocaine have on the CNS

vasoconstriction, arrhythmia, coronary artery spasms (which can lead to MIs)

what effects does cocaine have on the cardiac system

edema

what effect does cocaine have on the respiratory system

hyperthermia and rhabdomyolysis

what other effects does cocaine have on the body