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PHAR 100 - Module 2 > Stimulants - 2.3 > Flashcards

Stimulants - 2.3 Flashcards

1
Q

Stimulants are …

A

drugs that increase brain activity

ex. amphetamines, cocaine, nicotine, caffeine

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2
Q

Amphetamines

A

include amphetamines, dextroamphetamines, methamphetamines.

amphetamine related compounds are methylphenidate (Ritalin); treats ADHD, and MDMA (Ecstasy); fosters feeling of intimacy and empathy and improves intellectual capacities but is neurotoxic

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3
Q

Chemistry of amphetamines

A
  • synthetic organic compounds
  • structurally similar to norepinephrine and dopamine
  • synthesized readily (resulted in illegal manufacturing of these substances). Purity is questionable due to unreacted chemicals and cutting agents
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4
Q

CNS effects of amphetamines

A
  1. decreased threshold for transmitting sensory input to cerebral cortex, lead to excitation.
  2. euphoria and reward
  3. temperature regulation and feeding center modifications, lead to appetite suppression
  4. aggressive behaviour and mood swings increase
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5
Q

CNS excitation causes…

A
  • overstimulation
  • restlessness
  • dizziness
  • mild confusion
  • tremor
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6
Q

Effects of Short-Term use of amphetamines

A
  • heart attack, heart pain, blood p changes, fainting
  • cardiovascular collapse
  • increase respiratory rate
  • seizure, high fever, or stroke if overdose
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7
Q

Effects of Long-Term use of amphetamines

A
  • chronic sleep problems
  • poor appetite
  • anxiety, repetitive behaviour, psychoses, aggressive behaviour
  • elevated blood p and abnormal cardiac rhythm
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8
Q

Therapeutic Uses of amphetamines and treatment

A
  1. Narcolepsy (chronic sleep disorder)
  2. ADHD (disruptive behaviour, decreased attention/concentration spans)

Treatment: Ritalin

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9
Q

Amphetamine Abuse Potential

A

Extremely high due to powerful euphoria

  • water soluble forms of drug allow for large doses to be injected resulting in rapid and intense responses.
  • inherent harmfulness due to long-term toxicities.
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10
Q

Amphetamine Tolerance, Dependence, and Addiction

A

Tolerance - develops to euphoria and mood elevating effects, anorectic effects, cardiovascular/respiratory stimulatory effects, and lethal effects.

Dependence - Cessation result in mood depression, prolonged sleep, appetite increase, lack of energy, fatigue.

Addiction - feeling or euphoria and rush from self-admin acts as rewards and users crave these feelings.

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11
Q

Cocaine

A
  • classified as a local anesthetic and as CNS stimulant.
  • In terms of law, cocaine is classified as a narcotic
  • Cocaine one of the most popular recreational drugs.
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12
Q

Pharmacology

A
  • causes generalized CNS stimulation in dose dependent (more coke more CNS stim)
  • inhibits active uptake into presynaptic nerve terminal, primarily dopamine and serotonin
  • increase concentration of these transmitters in synaptic cleft
  • increase activation of postsynaptic receptors.
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13
Q

Cocaine effects in CNS

A
  • almost indistinguishable from amphetamine in acute effects and pattern of toxicity.
  • coke has shorter duration of action
  • lower incidence of complications associated with intravenous use (usually sniffed or smoked)
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14
Q

Therapeutic uses of Cocaine

A
  • legitimate use of coke is for local anesthetic for mouth and throat but rarely used.
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15
Q

Origins of Cocaine

A

naturally occurring alkaloid in leaves of coca bush

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16
Q

Cocaine Abuse Potential and Dependence

A
  • widely abused and used with other psychoactive drugs

- sniffed or smoked but can be injected

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17
Q

Long term effects of cocaine

A
  • Toxic psychosis, including paranoia
  • Hallucinations or sensations of insects crawling under the skin.
  • Impaired sexual function.
  • Permanent brain damage and impairment of neuronal function may occur.
  • High blood pressure and an irregular heart rhythm.
  • Changes to the nasal mucosa, as the drug is sniffed.
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18
Q

Nicotine

A

naturally occurring substance in tobacco responsible for dependence in smokers

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19
Q

Absorption of Nicotine

A
  • exists in cig smoke in very small particles. when inhaled, droplets are rapidly absorbed.
  • absorbed from gastrointestinal tract, oral mucosa, and skin
  • depth of inhalation and frequency of smoking determines dose of nicotine absorbed.
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20
Q

Distribution of Nicotine

A

distributed throughout body, rapidly gains access to brain

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21
Q

How is Nicotine metabolized?

A

rapidly metabolized in liver

22
Q

How is Nicotine Excreted?

A

excreted in urine

23
Q

Mechanism of Action for Nicotine

A
  • stimulated nicotinic receptors at synapses
  • activation of receptors increases psychomotor activity, cognitive function, attention, and memory.
  • large doses cause agitation, tremors, and seizures
  • effects in CNS mediated by nicotinic receptor-mediated release of CNS neurotransmitters dopamine and serotonin
24
Q

Therapeutic Uses of Nicotine

A
  • only used in smoking cessation programs (admin through chewing gum, transdermal patches, buccal spray)
25
Q

Effects of Short-Term use of Nicotine

A
  • dizziness, headache, nausea, vomiting, abdominal cramps, coughing and gagging
  • produces mild euphoria , enhanced arousal, increase ability to concentrate, sense of relaxation, small increase in: heart rate, blood p.
  • suppress appetite
26
Q

Effects of Long-Term use of Nicotine

A
  • Cardiovascular disease caused by nicotine and CO; CO reduces capacity of red blood cells to carry oxygen.
  • increase incidence of atherosclerosis (plaque in vessel) and thrombi formation (blood clot)
  • Lung Disease increase: smoker’s syndrome (difficulty breathing, wheezing, chest pain, congested lung, infection increase) and emphysema (chronic obstructive lung disease)
  • Increase risk of cancer in lung, oral cavity, throat, bladder, and uterus.
27
Q

Effects of Second-Hand Smoke

A
  • increased risk of cardiovascular disease and cancer

- increase risk of bronchitis, pneumonia, asthma, and sudden infant death syndrome in children.

28
Q

Effects of Smoking in Pregnancy

A
  • Risk of fetus being small for gestational age or preterm birth
  • Effects reverse is mother stops smoking early on
  • increase chance of low birth weight neonate due to decreased oxygen delivery to fetus
29
Q

Nicotine Abuse Potential

A
  • high degree of abuse liability

- cessation attempts of smoking often fail as craving is great

30
Q

Nicotine Tolerance

A
  • does not appear

- will smoke to keep nicotine blood levels at a range

31
Q

Nicotine Dependence

A
  • withdrawal causes irritability, restlessness, anxiety, insomnia, fatigue, inability to concentrate.
  • smokers get state of withdrawal in morning after waking up
32
Q

Nicotine Addiction

A

Manifests as extreme urge to smoke

33
Q

Where does Caffeine affect?

A

predominantly CNS and cardiovascular system

34
Q

Where is Caffeine found

A

tea, coffee, chocolate, cola drinks, over-the-counter stimulants, analgesics, diuretics

35
Q

Pharmacology of Caffeine

A
  • rapidly and completely absorbed when taken orally
  • distributes to all parts of body and freely crosses into brain and placenta
  • genetics determines rate of metabolism and excretion.
  • blood level significant at 30 mins and peak 2 hours after ingestion
36
Q

What does 100-250mg of caffeine do?

A

increases mental performance, motor activity, decreases drowsiness and fatigue

37
Q

Activation of adenosine receptors does what?

A

stimulates GABAergic neurons which inhibit dopamine release

38
Q

Caffeine actions are exerted how?

A

by competitively blocking adenosine receptors in brain which causes neurons to be released which causes an increase in dopamine release.

39
Q

Short-Term Effects of Caffeine in CNS

A
  • produce mild mood elevation and reduces fatigue, small increase in performance may exist.
  • flow of though is clearer and rapid
  • abstainers experience nervousness and it can interfere with sleep.
  • high doses will produce irritability, nervousness, rambling flow of thoughts and speech, and psychomotor agitation.
40
Q

Cardiovascular Short-Term Effects due to Caffeine

A
  • produces constriction of cerebral blood vessels (useful during headache)
  • peripheral blood flow increase
  • cardiac muscle stimulated
  • high does cause rapid and irregular heartbeat.
41
Q

Respiratory Short-Term Effects due to Caffeine

A

mild stimulation of respiratory rate and relaxation of bronchial smooth muscle

42
Q

How is Caffeine used clinically?

A

stimulate breathing in preterm newborns to help immature their brains and lungs to remember to breathe

43
Q

What is a lethal dose of Caffeine?

A

equal to about 10g, about 57 medium cups of coffee

44
Q

Long-Term effects of Caffeine

A

excess use over long period of time leads to restlessness, nervousness, insomnia, increased urinary output, gastric upset, rambling speech, and thought

45
Q

What affect does nicotine have on caffeine in a person who has taken both?

A

increases metabolism of caffeine, duration of action is shortened.

46
Q

Sally just quit smoking but she usually drinks 3 large cups of black coffee every day. What will happen to her? What should she do?

A

her metabolism of caffeine will return to normal so the caffeine will be active in her body longer than she’s used to.

She should decrease the amount of caffeine she has daily to compensate this.

47
Q

Sophie just found out she is 3 months pregnant. She doesn’t usually drink coffee but now she’s more tired during the day. Is it okay if she drinks coffee?

A

Consumption of caffeine is not associated with fetal abnormalities. Sophie can have modest doses of caffeine (3 cups of coffee per day) without measurable effects on her baby.

She should remember that her caffeine metabolism is slower since she is pregnant.

48
Q

Caffeine Abuse Potential

A
  • Abuse liability is slow but caffeine does act as a mild reinforcer.
  • inherent harmfulness is very low
49
Q

Is there such thing as a tolerance to caffeine?

A

tolerance does develop at least in some people

50
Q

Molly used to drink 5 shots of espresso every single day. She finally decided to stop out of nowhere and now she is experiencing the following symptoms:

  • headache, fatigue, and drowsiness

Why is she feeling this way?

A

Molly was DEPENDENT on her daily caffeine intake and now she is experiencing withdrawal symptoms.

51
Q

Can caffeine be addictive?

A

It can be mildly addictive

PHAR 100 - Module 2 (4 decks)

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