Nicotine - Mechanism - Effect - likelihood of dependence

- Binds to Nicotinic Acetylcholine receptors - Excitatory/Stimulant effect - Dependence has a genetic component

IDT - Drugs of Abuse, Ishmael Flashcards by Josh Miller

The Continued, compulsive obsession with obtaining, consuming and experiencing the effects of self-administered drugs

Substance Dependence (addiction)

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Drugs that have psychoactive properties have a ____________ which makes it __________ to be abused.

Positive reinforcing action

More Likely

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The return to a drug use after abstinence

Relapse

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What changes must be made in order to achieve continued recovery?

behavioral, social, psychological and physiologic changes

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What area of the brain is responsible for the pathway in addiction?

Nucleus accumbens, projections from the Ventral Tegmental area.

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Why are drugs that block dopamine receptors less likely to be self-administered?

They may have dysphoric effects that people would rather avoid.

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What are the natural rewards that may be devalued and overriden in addictive pathways?

Food
Water
Sex
Nurturing

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What is tolerance?

The decrease in pharmacologic response on repeated administration of the drug

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What is sensitization?

Responses/side effects become stronger than previously anticipated.

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Classification when administration of the drug is required to maintain normal function and avoid withdrawal syndrome.

Physiologic dependence

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When a drug dependence is removed from a physically dependent person, this unwanted side effects might occur

Withdrawal syndrome

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The process of by which an individual that is physically dependent on a drug is withdrawn from it

Detoxification

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The 7 classes of drugs that have been recognized as obsessively self-administered by humans

Methylxanthines
Nicotine
Alcohol
Marijuana
Stimulants
Opiates
Hallucinogenic/Dissociative drugs

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Nicotine

Mechanism
Effect
likelihood of dependence

Binds to Nicotinic Acetylcholine receptors
Excitatory/Stimulant effect
Dependence has a genetic component

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Pharmacologic treatment strategies for smoking cessation

NRT 
- patches, gum, e-cig etc 
- Reduces withdrawal by changing behavior 
Anti Depressants (no SSRIs)
- Bupropion
- Nortriptyline
Varenicline
 - Chantix, selective partial agonist

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Varenicline (Chantix)

Target
Efficacy

Selective alpha4beta2 nicotinic receptor partial agonist

Causes sufficient dopamine release to reduce cravings/withdrawal but prevents full activation of receptor.

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Why can Nicotine be so addicting?

Nicotinic receptors within the VTA and impact dopamine release in the nucleus accumbens

(mixes behavioral, cognitive and psychological signals)

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How do Buproprion and Nortrtiptyline differ in their mechanism of action for smoking cessation

Buproprion targets NET and DAT

Nortriptyline (NET < SERT ««< DAT)

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The observed phenomenon where the pharmacologic effect of alcohol having greater effect while rising than falling, even though blood ethanol concentration is the same.

The Acute Tolerance
or
Mellanby Effect

Effects of Alcohol on CNS

slurred speech
motor incoordination
impaired judgement
uninhibited behavior
increased self-confidence
sedation
relief of anxiety
increased pain threshold

What is the first thing you lose during consumption of alcohol?

Cognitive functions, as the neuronal populations are more sensitive

Describe the Asian Glow

Asian populations lack aldehyde dehydrogenase or have a mutation which allows the alcohol’s aldehyde intermediate to build up and cause dysphoric effects.

Disulfiram

An inhibitor of aldehyde dehdryogenase, supposed to make people sick when they drink in order to ween bad drinking behaviors

Alcohol withdrawal symptoms

Tremors (Shakes)
Increased BP
Rapid Breathing
Sweating/Nausea
Alcohol Hallucinations
Seizures
Delirium Tremens

What class of medications can be used to lessen alcohol withdrawal symptoms

Benzodiazepenes OTC - vitamins (thiamine, magnesium)

What is the main psychoactive ingredient in marijuana?

delta9-tetrahydrocanabinol

Why is marijuana not associated with severe withdrawal?

Not high enough dose to overload reward pathway and cause dependency

When did the Oregon Medical Marijuana Act get passed

Dec 1998; Approved for recreational use in Oregon in 2015

What debilitating medical conditions may be prescribed marijuana?

``` Agitation related to Alzheimer Cachexia Cancer Glaucoma HIV/Aids Nausea PTSD Severe Pain Seizures Persistent muscle spasms ```

How do endogenous cannabinoids modulate NT release

They decrease calcium ions by binding at CB receptors on the presynpatic neuron

Medicinal marijuana use vs | Recreational marijuana use

Medicinal - Symptom relief | Recreational - Pleasure

What routes of administration are often used for consumption of marijuana

Smoking Oral (edibles) Vaporizing

What route of marijuana consumption allows allows rapid and predictable bioavailabiity and allows for self-titration?

Smoking the Ganj

What is CUD?

Cannabis Use disorder - pattern of substance abuse that leads to clinically significant impairment - Social, occupational and recreational activities reduced in favor of drug - tolerance, withdrawal may develop, causing behavioral and physical effects, persistence in spite of negative consequences just like other drugs

What medication was used to treat morphine addiction in 1884?

Cocaine

What legitimate medical use can cocaine be used for?

Local anesthetic and vasoconstriction (use dependent Na+ channel blocker) - Upper respiratory tract - ear - nose - throat

Cocaine's mechanism of action

Binds to and blocks the Dopamine, SR and NE transporters, enhancing DA levels especially in the nucleus accumbens

What conditions can amphetamines be used to treat?

ADHD Narcolepsy Obesity

What is the primary effects of CNS stimulants?

Increased Alertness Increased locomotor activity Stereotype behavior, Euphoria, excitement, overconfidence and anorexia

What are the chances of developing dependence with amphetamine meds?

High, rapid, as it creates euphoria and is needed to avoid the unpleasant ftigue and depression that follows

What is the affect on dopamine transport by amphetamines?

Creates a "Reverse Transport", because amphetamines act as substrates of NET, SERT, DAt and VMAT, they may deplete the pH gradient in vesicles and cause efflux of endogenous neurotransmitters.

What do Cocaine and SSRI's/SNRI's have in common?

They are both non-transported inhibitors, binding to the receptor but not being actively transported themselves.

What are the 3 types of ADHD?

Inattentive Hyperactive-impulsive Combined

In individuals that have been diagnosed with ADHD, what is the likelihood of dependence or abuse?

Much lower, and is considered safe, with no convincing evidence it may lead to this.

What is the effect of stimulants in treatment of ADHD?

Tends to reduce the hyperactivity, impulsiveness and works to improve the ability to focus.

How is Atomoxetine unique from other CNS stimulants?

It targets the NE transporter and inhibits its function rather than acting as a stimulant, so it has low abuse liability