Drugs and Behavior - TAMU - Unit 6 Cocaine & Amphetamines

What drug class are cocaine and amphetamines a part of?

psychostimulants

3 multiple choice options

What are the major properties of psychomotor stimulants?

stimulate alertness and arousal, stimulate motor activity

What are some different types of stimulants?

cocaine, amphetamines, nicotine, caffeine

What is cocaine's natural source?

coca leaves

What kind of base/acid is cocaine?

weak base

3 multiple choice options

When did cocaine become widely used and praised for its properties?

1800s-1900s

3 multiple choice options

What is the concentration of cocaine in coca leaves?

< 2%

3 multiple choice options

How are coca leaves usually absorbed?

absorbed by mouth

What does chewing lime powder/ash with coca leaves do to absorption?

decreases ionization of cocaine by increasing saliva pH

3 multiple choice options

What is coca paste?

a crude extraction from coca leaves

What is coca paste's cocaine concentration?

~80% cocaine sulfate

3 multiple choice options

What is coca paste's route of administration?

smoking

What are other names for cocaine?

"paco", "basuco"

What is cocaine HCl (hydrochloride)?

a crystalline powder extracted and purified from coca paste

What is the cocaine concentration of cocaine HCl?

very high

1 multiple choice option

What are the common routes of administration for cocaine HCl?

orally, intranasally, injected IV

What is one route of administration for cocaine HCl that cannot be done?

smoking

3 multiple choice options

What is cocaine free base made from?

cocaine HCl, water, base, extracted w/ ether

What is cocaine free base's primary route of administration?

vaporized and smoked

What is crack cocaine made from?

cocaine HCl, baking soda

What is crack's cocaine concentration?

75-90%

3 multiple choice options

What is crack's primary route of administration?

smoked

Crack led to a new epidemic of cocaine use in _________.

1980s-90s

3 multiple choice options

What kind of medical effects does cocaine have?

anesthetic

What DEA schedule is cocaine?

schedule 2

What is the primary mechanism of cocaine?

blocks monoamine transporters, like DAT

What mechanisms of cocaine occur in high doses?

inhibits voltage-gated Na+ channels

3 multiple choice options

What is the peak subjective effect for crack cocaine?

~1-2 min

3 multiple choice options

What is the half-life of cocaine?

0.5-1.5 hrs

3 multiple choice options

What major metabolite is detectable in the urine for several days after cocaine usage?

benzoylecgonine

1 multiple choice option

Is benzoylecgonine an inactive or active metabolite?

inactive

1 multiple choice option

What metabolite is formed when cocaine and ethanol are ingested simultaneously and has a longer half-life than cocaine?

cocaethylene

1 multiple choice option

Is cocaethylene an inactive or active metabolite?

active

1 multiple choice option

Are amphetamines synthetic or natural?

they are both synthetic and natural

3 multiple choice options

Is ephedrine synthetic or natural?

natural

3 multiple choice options

What are the active components in decongestants?

ephedrine, pseudoephedrine

Is cathinone synthetic or natural?

natural

3 multiple choice options

Where does cathinone come from?

"khat" or "qat" shrub leaves; commonly chewed

What are the synthetic variants of cathinone?

methcathinone, mephedrone

What are the synthetic variants of cathinone commonly known as?

"bath salts"

What DEA schedule are the synthetic variants of cathinone on?

schedule 1

When was amphetamine synthesized?

1887

When was methamphetamine synthesized?

~1919

When was amphetamine medical use developed?

1920-30s

What are examples of past medical amphetamine usage?

benzedrine inhaler, narcolepsy

When were amphetamines widely adopted?

1940s

When was the peak usage of "speed"?

early 1970s

Forms of synthetic amphetamines include:

d-amphetamine, L-amphetamine, adderall

What are the most common amphetamine routes of administration?

orally, IV, SC

What are the most common methamphetamine routes of administration?

orally, snorted, IV, smoked

What are some amphetamine-related synthetics?

methylphenidate, modafinil

What are some historical medical uses of amphetamines that are no longer used?

mild depression, as a diet pill

What group widely used amphetamines during WWII?

the military

In 1970, ____ of the population were regular amphetamine users.

> 10%

3 multiple choice options

What are the current medical uses of amphetamines?

narcolepsy, ADHD

What DEA schedule are amphetamines on?

schedule 2

Amphetamines have a ___________ metabolism and elimination as compared to cocaine.

slower

2 multiple choice options

What is the half-life of amphetamines?

7-30 hrs

Is mood amplification a mild/moderate or severe effect of cocaine/amphetamine usage?

mild/moderate

1 multiple choice option

Is extreme energy or exhaustion a mild/moderate or severe effect of cocaine/amphetamine usage?

severe

1 multiple choice option

Is total insomnia a mild/moderate or severe effect of cocaine/amphetamine usage?

severe

1 multiple choice option

Is motor excitement/restlessness a mild/moderate or severe effect of cocaine/amphetamine usage?

mild/moderate

1 multiple choice option

Is rambling/incoherent speech a mild/moderate or severe effect of cocaine/amphetamine usage?

severe

1 multiple choice option

Is hyperactive ideation a mild/moderate or severe effect of cocaine/amphetamine usage?

mild/moderate

Is increased sexual interest a mild/moderate or severe effect of cocaine/amphetamine usage?

mild/moderate

1 multiple choice option

Is decreased sexual interest a mild/moderate or severe effect of cocaine/amphetamine usage?

severe

1 multiple choice option

Is anger/verbal aggression a mild/moderate or severe effect of cocaine/amphetamine usage?

mild/moderate

1 multiple choice option

Is total anorexia a mild/moderate or severe effect of cocaine/amphetamine usage?

severe

1 multiple choice option

Are delusions of grandiosity a mild/moderate or severe effect of cocaine/amphetamine usage?

severe

1 multiple choice option

What are the autonomic effects of cocaine/amphetamine usage?

increased blood pressure, hyperthermia, bronchodilation

(T/F) Cocaine has a shorter duration of action compared to amphetamines.

True

1 multiple choice option

(T/F) Cocaine produces worse cardiovascular effects compared to amphetamines.

True

1 multiple choice option

(T/F) Cocaine has lower convulsive/seizure properties than amphetamines.

False

1 multiple choice option

Locomotor activity can appear to go down with _____ AMPH doses because rats perform stereotypy behavior instead.

high

1 multiple choice option

In chronic, high-dose users of stimulants, withdrawal symptoms are mostly _____________.

psychological

1 multiple choice option

____________ to some effects of psychostimulants: autonomic effects, anorexic effects.

tolerance

1 multiple choice option

____________ to some effects of psychostimulants: rewarding effects, psychotomimetic effects (psychosis), locomotor stimulant effects.

sensitization

1 multiple choice option

(T/F) MDMA is used clinically.

False

1 multiple choice option

MDMA was used as a club drug in:

1980s-90s

What DEA schedule is MDMA on?

schedule 1

What is MDMA's common route of administration?

orally

What is MDMA's half-life?

8 hrs

Increased energy and sociability/empathy; mild euphoria; Increased heart rate and temperature.

MDMA effects at low doses

Mild hallucinogenic; Hyperthermia & dehydration; increased H.R. and B.P. → stroke.

MDMA effects at high doses

Cocaine blocks the reuptake of which specific monoamines?

DA, NE, 5-HT

What two actions of amphetamines lead to very high DA in synaptic cleft?

vesicles release transmitter, monoamines transported out of neuron via reversal of transporter

Serotonin is a type of:

indolamine

Dopamine, norepinephrine, and epinephrine are all types of:

catecholamines

What amino acid is the precursor for catecholamines?

tyrosine

What enzyme is the rate-limiting step in catecholamine synthesis?

tyrosine hydroxylase

Catecholamines are inactivated by:

reuptake via transporters and/or enzymatic degradation

What is the primary mechanism for catecholamine inactivation?

catecholamine reuptake

Which transporter packages all monoamines into vesicles?

vesicular monoamine transporter (VMAT2)

What is dopamine's unique synaptic transporter?

DAT

What is serotonin's unique synaptic transporter?

SERT

What is norepinephrine's unique synaptic transporter?

NET

What enzymes are involved in catecholamine metabolism?

MAO, COMT

What are the five dopamine receptors (all GPCRs)?

D1, D2, D3, D4, D5

What dopamine receptors are coupled to Gs?

D1, D5

What dopamine receptors are coupled to Gi?

D2, D3, D4