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Pharm > psychomotor stimulants > Flashcards

psychomotor stimulants Flashcards

1
Q

psychomotor stimulants

A

Amphetamines, Cocaine, Methylxanthines & Convulsive Stimulants

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2
Q

amphetamine (BENZEDRINE, BIPHETAMINE, ADDERAL)

A

stimulant

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3
Q

d-amphetamine (DEXEDRINE, BIPHETAMINE, ADDERAL)

A

-greater effect in CNS than amphetamine

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4
Q

Lisdexamfetamine (Vyvanse)

A

prodrug, amphetamine is linked to lysine

  • Moderate rate of conversion to amphetamine limits abuse
  • Used for ADHD but might not work as well as traditional amphetamines in some patients
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5
Q

methamphetamine (DESOXYN) - “speed” “crank” - “ice”

A
  • methyl group: resistant to metabolism by MAO and increases its lipid solubility
  • intense effects in the CNS, widely abused
  • “ice”: crystalline smokable form, like crack
  • meth is much longer acting than crack cocaine: 12 hours or more vs 15-30 min. for crack!
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6
Q

methylphenidate (RITALIN)

and (permoline (Cylert) FYI)

A

similar to amphetamines - used to tx ADD in kids - paradoxical effect of amphetamine and related agents is to stimulate areas of the brain such as the locus ceruleus that enable the child to focus attention

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7
Q

Cathinone (Khat, “Kat”, or “Cat”)

A
  • plant from Eastern Africa and Mid East
  • analogs easy to synthesize chemically (DOAs in US, Europe)
  • “bath salts” from the internet and in “head shops”.
  • usually taken by “snorting”
  • Some products include: “Ivory Wave”, “Vanilla Sky”, “Raving Dragon” and “Purple Wave”.
  • recently banned by the DEA
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8
Q

Ephedrine

A
  • sympathomimetic agent
  • used in various OTC pep pills
  • banned by FDA but can get over internet
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9
Q

Modafanil (Provigil) and Armodafanil (Nuvigil)

A

newer drugs, used to tx narcolepsy and shift work disorders

-unclear MOA, have many amphetamine-like effects

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10
Q

Pharmacological Effects (amphetamine, methamphetamine): CNS

A
  • stimulation: ^arousal and wakefulness via stimulating the reticular activating system
  • euphoria: most pleasant, some dysphoric and anxious
  • delay of “fatigue induced” decline in intellectual/motor performance
  • rebound effects (crash) may lead to cycle of drug use
  • tolerance and dependence: both psychological and physical (w/drawal: fatigue, lethargy, depression)
  • amphet. psychosis: like paranoid shizo, but reversible
  • appetite suppression: action on hypothalamus, tolerance develops
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11
Q

Pharmacological Effects (amphetamine, methamphetamine): Peripheral effects

A

primarily sympathomimetic

  • autonomic - HTN, tachy, arrhythmias, mydriasis (dilated)
  • metabolic - decreased food intake; malnutrition
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12
Q

Pharmacological Effects (amphetamine, methamphetamine): toxicity

A

sympathomimetic effects -

  • CV: HTN, tachy, arrhythmias, and sudden death
  • CNS: excessive stimulation, hostility, aggression, psychotic reactions (amphetamine psychosis), tactile hallucinations (formication)
  • dental problems (meth mouth) and lung damage from smokable forms
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13
Q

MOA

A
  • acute effect: enhanced release and inhibition of the uptake of NE and DA (acute effect)
  • possible direct stimulation of alpha receptors in reward centers of brain
  • chronic effect: decreased levels of DA in reward centers of brain
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14
Q

pharmacokinetics

A
  • absorption from GI tract
  • IV use by abusers
  • metabolism by liver but large amounts are excreted unchanged
  • enhanced excretion in acidic urine
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15
Q

use of amphetamines

A
  • ADD: “hyperkinetic syndrome” in children - paradoxical effect in that it may stimulate catecholamine pathways in the brain that enable the child to focus attention properly
  • narcolepsy
  • obesity and weight reduction (but tolerance develops and drugs aren’t effective long term)
  • stimulants
  • abuse
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16
Q

Cocaine

A

from Erythroxylon coca plant of Peru and Columbia
hydrochloride vs. free base vs. “crack”:

cocaine “base/paste” (crude coca extract)–>COCAINE-HCL (50-75mg/line)–>cocaine-free base
either heat to remove water–>CRACK (15-25 mg/dose)
or ether extraction/evaporation–>FREE BASE (15-25 mg/dose)

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17
Q

cocaine entry pharmacokinetics

A
  • HCl salt - water soluble; absorption through mucous membranes - commonly “snorted”
  • HCl salt - IV use by abusers
  • inhalation of the lipid soluble free base forms provides very rapid delivery of a concentrated bolus to the brain
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18
Q

cocaine metabolism

A

metabolism by plasma esterase and by liver

  • half-life of HCl form is about 1 hour
  • major metabolite is benzoylecognine
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19
Q

when cocaine used in combo with etOH..??

A

an active metabolite

(cocaethylene) is formed. Since it has a much longer half-life than cocaine, the drug effects may be prolonged

20
Q

cocaine pharmo effects

A

local anesthetic with vasoconstriction
CNS effects (like amphetamines):
-stimulation, ^ arousal
-euphoria, dysphoria
-increased confidence and social activity
-powerful reinforcer on reward center
-tolerance and dependence: psychological and physical (w. drawl: lethargy, fatigue, depression)
-psychotic symptoms like amphetamines at high doses

21
Q

cocaine peripheral effects

A

autonomic - HTN; tachy; arrhythmias; sudden death, mydriasis

  • teratogenic effects - low birth weight, mental retardation, neuro/dev deficit
  • deterioration and perforation of nasal septum with chronic snorting
  • lung damage and pulmonary edema from smoking crack
  • AIDS, hepatitis and other infections from IV use
22
Q

state of cocaine dependence results from ??

A

drug induced adaptive changes in specific dopaminergic pathways in limbic areas of the brain

23
Q

a primary effect of acutely admin. cocaine is to ??

A

block the synaptic reuptake dopamine that is available to act on the target cell
-the extra dopamine that is present in the synapse is thought to act on the target cells to produce the euphoria and reinforcing effects of acutely administered cocaine

24
Q

what is thought to be responsible for the craving for cocaine and the development of tolerance and dependence?

A

With repetitive usage, the presynaptic neuron is unable to replenish lost dopamine

25
Q

how do antipsychotics affect acutely admin. cocaine??

amphetamines produce what sort of effects??

A

inhibit many of the behavioral effects (via blocking dopamine receptors)

produce effects that closely resemble those of cocaine (stimulate the synaptic release of dopamine)

26
Q

novel tx for cocaine dependence/addiction

A
  • nutritional supplements to replenish dopamine stores
  • l-DOPA to increase brain levels of dopamine
  • certain opioids (buprenorphine): used to decrease cravings, tx for addiction
27
Q

novel cocaine dependence tx: ?? block the reuptake of dopamine but do not deplete levels of dopamine (may suppress cravings)

A

Antidepressant drugs: i.e. bupropion (Wellbutrin)

28
Q

novel cocaine dependence tx: ?? is being tried in hopes that it may provide some stimulation of the post synaptic receptors until dopamine stores can be replenished (substitute)

A

Bromocriptine (Parlodel): dopamine agonist

29
Q

caffeine

A

methylated xanthine

30
Q

Theophylline

A

methylated xanthine, used in the treatment of asthma

31
Q

Aminophylline

A

methylated xanthine,

Ethylenediamine salt of theophylline - used in the treatment of sever asthma

32
Q

caffeine and related methylxanthine CNS effects

A

-cortical stimulation
-increased mental alertness and improvement in some types of mental
function
-respiratory stimulation – caffeine and theophylline are sometimes used to
treat apnea in preterm infants

33
Q

caffeine tolerance and dependence -

A

caffeine is both psychologically and physically addicting. The withdrawal syndrome consists of headache, fatigue, and depression, but is usually relatively mild. Some degree of dependence can result from drinking 3-4 cups of coffee/day for 2-4 weeks.

34
Q

caffeine cardiac effects

A

-cardiac stimulation: increased rate and contractility; usually not severe but may cause problems in OD or in pts with cardiac conditions
Some people are far more sensitive to caffeine than others

35
Q

caffeine vascular effects

A

-peripheral (dilation of most vascular beds)
-renal: dilation; diuretic effect
-cerebral: constriction; caffeine is sometimes included in headache
preparations

36
Q

other caffeine peripheral effects

A
  • relaxation of bronchioles - use of theophylline and aminophylline in asthma
  • stimulation of gastric secretion - avoid use in patients with peptic ulcer disease
  • controversies regarding carcinogenesis and teratogenesis
37
Q

Methylxanthine Overdose is characterized by ??

A

excessive CNS stimulation which can result in life threatening seizures. In addition, there may be excessive cardiac stimulation and eventual cardiovascular collapse.
Tx is mainly symptomatic (anticonvulsants and antiarrhythmics)

38
Q

MOA of caffeine, etc.

A
  • inhibition of phosphodiesterase
  • blockade of adenosine receptors
  • release of Ca2+
39
Q

caffeine uses

A
  • CNS stimulants (Vivarin, No Doz, etc..)
  • asthma - theophylline and aminophylline
  • in combination with other drugs (e.g. headache remedies)
  • as diuretics (e.g. caffeine in OTC preps)
  • as respiratory stimulants in preterm infants
  • in beverages
40
Q

Health Effects Associated with Chronic Uses of Caffeine??

A

up for debate

  • possibly associated with a variety of disorders (e.g. HTN, arrhythmias, cancer, PUD, etc..)
  • should be avoided by individuals with various health problems (e.g. CV disease, peptic ulcers, seizure disorders, etc..)
41
Q

Strychnine

A

Spinal cord stimulant (mostly toxicologic); potent convulsant used as a rat poison

42
Q

Strychine MOA

tx??

A
  • antagonist at glycine receptors in the spinal cord and other areas of the CNS. This removes post synaptic inhibitory influences and leads to the development of severe toxic seizures
    tx: symptomatic support plus the use of diazepam to control seizures.
43
Q

Tetanus Toxin

A

spinal cord stimulant; released by C. tetani
Produces generalized tetanus and tonic convulsions similar to those produced by strychnine.
-inhibits release of glycine from Renshaw cells in the spinal cord and other areas.
Tx: symptomatic support, diazepam for the control of seizures, and appropriate antimicrobial therapy.

44
Q

Doxapram (DOPRAM) FYI

questionable efficacy

A

Respiratory Stimulant (Analeptic)

  • Acts on carotid chemoreceptors and medullary respiratory centers to stimulate respiration.
  • tx of drug induced respiratory depression particularly after surgery.
45
Q

Doxapram (DOPRAM) SEs FYI

A

excessive CNS stimulation: headache, hyperreflexia, spasticity, and convulsions
CV effects: flushing, HTN, tachycardia, and arrhythmias

46
Q

Nikethamide (CORAMINE) FYI

A 
Respiratory Stimulant (Analeptic)
Old drug that used to be used to stimulate respiration in barbiturate poisoning - not very effective - now obsolet

Pharm (45 decks)

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