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Pharmacology > Convulsants / Stimulants > Flashcards

Convulsants / Stimulants Flashcards

1
Q

What are convulsants used for?

A
  • Provacative diagnosis of epilepsy
  • Keeps people awake as well
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2
Q

What drugs can we use as convulsants?

A
  • pentylenetetrazole (Metrazole)
  • strychnine - rat poison
  • picrotoxin
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3
Q

What rat poison convulsant is added to heroin and causes overdose?

A

strychnine

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4
Q

What are stimulants used for?

A

As an antidote for depression = “analeptics”

no one drug is very effective

Primarily used to reverse respiratory, cardiac and CNS depression

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5
Q

What are the primary classes of stimulants?

A
  • Xanthenes
  • Sympathomimetics (centrally acting)
  • Convulsants
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6
Q

What stimulants are used for asthma, chronic bronchitis and COPD?

A

Xanthenes

  • Theophylline
  • Aminophylline
  • Caffeine
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7
Q

What are the pharmacologic effects of xanthenes?

A
  • 50-200 mg of caffeine or theophylline is needed to increase cortical activity
  • OTC stimulants have 100-200 mg
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8
Q

What is the order of potency of xanthenes in their locations?

A
  • Cerebral cortex - 50-200 mg
  • Brain stem - >250 mg
  • Spinal cord = 1000 mg can lead to convulsions, shakiness
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9
Q

What are some of the effects of xanthenes?

A
  • Blood vessel dilation (Beta 2 effect)
  • Dilation - coronary and peripheral blood vessels
  • Constriction - cerebral blood vessels (treatment for headache)
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10
Q

What is more potent theophylline or caffeine?

A

Theophylline

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11
Q

What do xanthenes do to cardiac muscle?

A

Increase the output, stimulation (Beta 1)

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12
Q

Does caffeine cause hypertension or hypotension?

A

Hypotension - normal heart rate, will cause arrhythmias in someone who is at risk, not in normal heart

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13
Q

What do xanthenes do to smooth muscles?

A

Relaxation (beta2), bronchial dilation

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14
Q

What xanthene is a popular asthma medication?

A

Theophylline

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15
Q

What can caffeine do to skeletal muscles?

A

Cause contractions - pain stiffness, pyschic tension in neck –> headaches

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16
Q

What is more potent in the following, Theophylline or Caffeine?

  • CNS
  • Blood Volume
  • Heart
  • Smooth muscles
  • Skeletal muscles
  • Diuresis
A
  • CNS - caffeine = theophylline
  • BloodVolume - theophylline
  • Heart - theophylline
  • Smooth muscles - theophylline
  • Skeletal muscles - caffeine
  • Diuresis - theophylline
17
Q

What are the 3 ways xanthenes act as diuretics?

A
  1. Increased GFR
  2. Inhibits ADH
  3. Increased perfusion to kidney
18
Q

What are the adverse reactions of xanthenes?

A
  • CNS - dizziness, convulsions
  • GI - nausea & vomiting
  • CVS - hypotention, palpitations
  • Habit forming
19
Q

What dose of caffeine is required to produce toxicity?

A

300 mg (6 cups of tea)

20
Q

How much caffeine a day produces physical dependence?

A

600 mg/day > 6 cups of coffee

21
Q

When does withdrawal syndrome begin with caffeine?

A

within 24 hours of discontinuance

headahce, lethargy, irritability, anxiety

Tolerance develops

22
Q

What are the therapeutic uses of xanthenes?

A
  • Asthma
  • Chronic bronchitis
  • COPD
  • Status asthmaticus - life threatening asthma attach
  • Maintains wakefulness
  • Migraines
  • Some CNS depressent poisonings - opioids
  • Acute pulmonary edema and apnea in preterm infants
  • Diuretic
23
Q

What’s the mechanism of action for amphetamines?

A
  • Direct alpha-1 or dopamine receptor agonists
  • MAO inhibitors
  • Re-uptake inhibitors
  • Presynaptic releasers of endogenous catecholamines
24
Q

What type of drug are amphetamines?

A

CNS sympathomimetics

25
Q

What effects do CNS sympathomimetics have?

A
  • Decrease fatigue
  • Wakefulness
  • Physical performance
  • Reduced REM sleep
26
Q

What are the indications/therapeutic use of CNS sympathomimetics?

A
  • Narcolepsy - only good therapeutic indication
  • Hyperkinetic syndromes - ADD/ADHD
    • Abnormal electrical activity, helps reduce behavior problems/concentration
27
Q

What are the adverse effects of CNS sympathomimetics?

A
  • Acute toxicity - irritability, insomnia, xerostomia, nausea, palpitations, sweating
  • Chronic toxicity - psychosis resembling paranoid schizophrenia
  • Dependency/addiction
28
Q

What’s the mechanism of action for cocaine?

A
  • Blocks sodium/potassium ATP-ase reuptake mechanism
  • Dopamine and NE remains in synapse
  • Crosses blood brain barrier, increases sympathetic effects
  • Causes euphoria once reaches CNS
29
Q

What does cocaine do?

A

Increases peripheral resistance, increases cardiac output, energy expenditure

30
Q

What types of drugs are there for ADHD?

A
  • Adrenergic agonists = CNS stimulation
    • methylphenidate (Ritalin)
  • Stimulants
    • dextroamphetamine (Dexadrine)
  • Selective Norepinephrine Reuptake Inhibitor
    • atomoxetine (Straterra)
31
Q

How does Ritalin work?

A

Blocks reuptake of dopaminergive neurons, avoid vasoconstrictors

32
Q

How does Dexadrine work?

A

Blocks the reuptake of dopamine and norepinephrine - inhibits monamine oxidase, avoid vasoconstrictor

33
Q

How does atomoxetine (Straterra) work?

A

Selectively inhibits reuptake of norepinephrine with little to no activity at other reuptake or receptor sites

use vasoconstrictor with caution

34
Q

What is ephedrine (Pretz-D) used for?

A

It’s an amphetamine for cough and cold medications to relieve bronchial and nasal congestion

35
Q

Which amphetamines have been pulled from the market?

A
  • phenylpropanolamine (PPA) - appetite suppressants (OTC diet pills), deaths from heart attack and stroke
  • ephedra - used to be OTC diet pills, deaths from heart attach and stroke, stimulants for performance enhancement
36
Q

What do you have to be aware/cautious about with patients using amphetamines?

A

Administering local anesthetics with vasoconstrictors

37
Q

What stimulant is sold as parenteral drug to reverse general anesthesia or drug-induced respiratory depression?

A

doxapram (Dopram)

38
Q

What is one of the most addicting substances known?

A

Nicotine

39
Q

What do low/high doses of nictone do?

A
  • Low: from smoke stimulates nicotinic receptors in brain stem and cortex
  • High: causes convulsions, which can be fatal

Pharmacology (25 decks)

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