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Neuro 2 Midterm > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

What are the 3 key neurons involved in parkinsonism?

A

dopaminergic, GABAergic, cholinergic

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2
Q

How does the distribution of levodopa in both the presence and absence of a dopamine decarboxylase inhibitor change?

A

increased distribution with a dopamine decarboxylase inhibitor

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3
Q

What are the 5 dopamine receptor agonists used for movement disorders?

A 
Levodopa
Apomorphine
Bromocriptine
Pramipexole
Ropinirole
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4
Q

What are the 2 MAO inhibitors used for movement disorders?

A

Selegiline

Rasagiline

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5
Q

What are the 2 COM-T inhibitors used for movement disorders? (catechol-0-methyltransferase)

A

Tolcapone

Entacapone

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6
Q

What are the 5 anticholinergic drugs used for movement disorders?

A 
Benztropine
Trihexyphenidyl
Biperiden
Orphenadrine
Procyclidine
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7
Q

Which drug is used to treat ALS?

A

Riluzole

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8
Q

Which drugs are used to treat huntington dz?

A

Reserpine, tetrabenazine

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9
Q

Examples of neurodegenerative disorders that manifest as abnormalities in the control of movement including _________ dz and ___________dz. Other a neurodegenerative disorders result in impaired memory or cognitive ability (__________dz) and muscular weakness (____).

A

Parkinson Dz; Huntington Dz

Alzheimer Dz, ALS

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10
Q

A tremor of a part during maintenance of sustained posture (e.g., the outstretched upper limb when holding a cup)

A

postural tremor

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11
Q

A tremor of a part during movement (e.g., the outstretched upper limb when lifting a cup)

A

essential/intention tremor

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12
Q

A tremor consisting of slow, regular movements of the hands and sometimes the lower limbs, neck, face, or jaw; it typically stops upon voluntary movement of the part and is intensified by stimuli such as cold, fatigue, and strong emotions; may be at rest

A

parkinsonian tremor

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13
Q

The occurrence of a variety of continual, rapid, highly complex, jerky, dyskinetic movements that look well coordinated but are actually involuntary

A

chorea

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14
Q

-An involuntary, compulsive, rapid, repetitive, stereotyped movement or vocalization, experienced as irresistible although it can be suppressed for some length of time
-exacerbated by stress and diminished during sleep or engrossing activities
-may be psychogenic or neurogenic in origin and are classified as either simple
(e.g., eye blinking, shoulder shrugging, coughing, grunting, snorting, or barking) or
complex (e.g., facial gestures, grooming motions, coprolalia, echolalia, or echokinesis)

A

Tics

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15
Q

Pt presents with…Dx?

  • Bradykinesia (slowness and poverty of movement)
  • Muscular Rigidity
  • Resting tremor (abates during voluntary movement)
  • Impairment of postural balance leading to disturbances of gait and failling
A

Parkinson disease

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16
Q

What is the pathological hallmark of PD?

A

loss of the pigmented, dopaminergic neurons of the substantia nigra, with the appearance of intracellular inclusions known as Lewy bodies

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17
Q

Under normal conditions, dopaminergic neurons originating in the substantia nigra _____ the GABAergic output from the striatum while cholinergic neurons exert an __________ effect on GABAergic neurons

A

inhibit

excitatory

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18
Q

In PD, loss of dopaminergic neurons results in __________ of GABAergic neurons and disturbed movement

A

disinhibition

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19
Q

Based on the pathophysiology of PD, pts may be treated with which two classes of drugs?

A

dopamine agonists

anticholinergic agents

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20
Q

Levodopa is used to treat PD and is an immediate metabolic precursor to ________.

A

dopamine

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21
Q

What is the MOA of levodopa?

A

agonist of dopamine R (D2)

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22
Q

Levodopa by itself is rapidly absorbed from the small intestine with a peak plasma conc b/t 1-2 hours after oral dose; only 1-3% of the drug enters the bran unaltered. What can we do to combat this?

A

Add carbidopa

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23
Q

Why do we coadminister carbidopa with levodopa? What are the effects?

A

carbidopa=dopamine decarboxylase inhibitor that doesn’t cross the BBB

results in reduced peripheral metabolism of levodopa, increased plasma levels, increased half-life, and increased levodopa available for entry into the brain

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24
Q

Coadministration of levodopa and carbidopa may _______ (increase/reduce) the daily requirements of levodopa by 75%.

A

reduce

less drug and more to brain

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25
Q

T/F: Even though levodopa is effective, long-term tx may experience declining efficacy and response fluctuations. Therefore, the best results occur during first few years of treatment (use once necessary or in severe cases).

A

True!

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26
Q

Levodopa given without a peripheral decarboxylate inhibitor cause ______, _______, and ______ in 80% of pts.

A

anorexia, nausea, vomiting

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27
Q

Vomiting in levodopa can be attributed to dopamine activation of ____________ _____ ____

A

chemoreceptor trigger zone

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28
Q

What are the cardiovascular risks associated with levodopa?

A

cardiac arrhythmias (incr. catecholamines)

postural hypotension at first

HTN with nonselective MOA inhib

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29
Q

T/F: 80% of levodopa pts experience dyskinesias of the face and distal extremities

A

True!

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30
Q

Are there behavioral effects of levodopa?

A

Yes! changes in mood and personality such as depression, anxiety, agitation, insomnia, etc

(tx with atypical antipsychotic agents)

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31
Q

TQ: whats the difference between levodopa wearing off vs. on-off phenomena?

A

wearing off=depends on timing of the dose

on-off=NOT related to dose timing, off period=marked akinesia with on-periods of improved mobility w/ dyskinesia

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32
Q

TQ: What may provide temporary benefit to pts with severe levodopa off-periods?

A

subcutaneous injection of apomorphine!

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33
Q

Which 2 patient groups are contraindicated for levodopa?

A
  • MAO inhibitors

- psychotic pts

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34
Q

The other dopamine agonists act on two different dopamine receptors (D2 and D3). Match the drug to its receptor:
Bromocriptine
Pramipexole
Ropinirole

A

Bromocriptine: D2 agonist
Pramipexole: D3 agonist
Ropinirole: D2 agonist

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35
Q

Pramiprexole is used for both PD and _____ _____ _______.

A

restless leg syndrome

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36
Q

What are the adverse effects of the dopamine receptor agonists Bromocriptine, Pramipexole, Ropinirole?

A
  • GI: anorexia, N/V, constipation, dyspepsia, reflux
  • Cardiovascular: postural hypotension , digital vasospasm (bromocriptine), peripheral edema and arrhythmias
  • Dyskinesias
  • mental disturbances: confusion, hallucinations, delusions
  • headache, nasal congestion
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37
Q

What are the contraindications to using dopamine receptor antagonists? (3)

What additional contraindication is specific for bromocriptine?

A
  • psychotic illness
  • MI
  • peptic ulcers

-bromocryptine contraindicated in pts with peripheral vascular dz due to vasoconstricting effects

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38
Q

What are the two monoamine oxidase (MAO) inhibitors?

A

Selegiline

Rasagiline

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39
Q

There are two forms of MAO. What are they and which is involved with inhibiting levodopa metabolism via Selegiline and Rasagiline?

A

MAO-A: norepi and serotonin
MAO-B: phenylethylamine and benzylamine
(Dopamine and tryptamine metab via both MAO-A and B)

The two MAO inhibitors target MAO-B (and MAO-A (selegiline) at high doses)

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40
Q

Why must we avoid the combined administration of levodopa and a nonselective MAO inhibitor?

A

may lead to a hypertensive crisis due to peripheral accumulation of norepi

(MAO B and A breakdown catecholamines but A is selective for Norepi/serotonin which can lead to an accumulation of norepi…also bad if pt is on an SSRI b/c can cause serotonin syndrome)

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41
Q

What are the two catechol-o-methyltransferse (COMT) inhibitors? What are their MOA?

A

Tolcapone and entacapone prolong the activity of levodopa by inhibiting its peripheral metabolism, which decreases clearance and increases bioavailability

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42
Q

Which COMT inhibitor would you avoid in pts with liver dz? why?

A

Tolcapone! may cause and increase in liver enzymes and death by acute hepatic failure

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43
Q

Which dopamine agonist stimulates the postsynaptic dopamine D2 receptors and is injected for quick, temporary relief of off-periods of akinesia in pts on dopaminergic therapy?

A

Apomorphine

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44
Q

What antiviral agent can help treat parkinsons via unknown causes?

A

Amantadine

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45
Q

What is the main adverse effect of Amantadine? What some other adverse effects?

A

livedo reticularis (purplish mottled discoloration of the skin, usually on the legs)

restlessness, depression, irritability, insomnia, headache, hypotension, heart failure etc

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46
Q

Which patients should you be cautious of when giving Amantadine?

A

pts with a history of seizures or heart failure

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47
Q

Which central acting anticholinergic drugs are available to treat PD? (5)

A 
Benzotropine
trihexyphenidyl
biperiden
orphenadrine
procyclidine
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48
Q

What is the MOA of anticholinergic drugs?

A

centrally acting mAchR antagonists help correct the balance between dopamine and Ach

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49
Q

What are some adverse effects of anticholinergic drugs such as benzotropine?

A

peripheral anticholinergic effects (sedation, mental confusion, constipation, urinary retention, dry mouth, dry eyes)

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50
Q

Huntington dz is characterized by progressive chorea and dementia beginning in adulthood due to the overactivity of ___________ pathways

A

dopaminergic

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51
Q

Drugs that impair dopaminergic neurotransmission alleviate chorea, such as _______ and ________.

A

reserpine and tetrabenzine

52
Q

What is the MOA of reserpine and tetrabenzine in the treatment of huntingtons?

A

Reserpine (irreversible) and Tetrabenzine (reversible) are agents that block the vesicular monoamine transporter and deplete cerebral dopamine stores

53
Q

What is the only drug that has any impact on survival in ALS?

A

Riluzole

54
Q

What is the MOA of riluzole in treating ALS? (3)

A
  • inhibits glutamate release

- blocks post-synaptic glutamate R -inhibits VG-Na channels

55
Q

What are the major AE of riluzole?

A

nausea and weakness

56
Q

What are the first line treatments for restless leg syndrome? (2)

A

Pramipexole and Ropinirole

57
Q

Which drug would you gibe a patient with wilson disease (increased copper in the blood)? What is it MOA?

A

Penicillamine

chelating agent that forms a complex with copper

58
Q

What do all drugs of abuse begin with?

A

Elective use

59
Q

What are the three stages of elective abuse?

A

1) Experimental
2) Social (cigarette break, bars)
3) Sporadic Abuse

60
Q

What can elective drug abuse turn into it?

A 
nonelective abuse
(compulsive abuse)
61
Q

Which 2 drugs quickly turn from elective to nonelective

A

cocaine and meth

62
Q
  • Intensity of the response decreases
  • Duration of response decreases
  • usually both occur
A

Tolerance

user ups dose and frequency

63
Q

Metabolic tolerance (dispositional, pharmacologic)

A

metabolize drug faster and to greater extent

64
Q

Cellular tolerance (adaptive, pharmacodynamic)

A

level to cause euphoria increases
-affected cells adapt to presence of drug (down regulation)

(increase dose, frequency, or both)

65
Q

T/F: If you are tolerant to one drug you are tolerant to many like it

A

TRUE

66
Q

T/F: Tolerance disappears with stoppage

A

TRUE

risk of overdose

67
Q

Heroin tolerance includes? (3)

A

Analgesia, Euphoria, Respiratory depression

little tolerance to constipation and miosis

68
Q

Repeated use causes a state such that sudden withdrawal produces effects (often opposite of drug) is called…

what are some features?

A 
Physical dependence
Features
• Repeated/frequent use 
• Withdrawal time
• Intensity
• Negative reinforcer
• Not with all drugs
69
Q

which intense drugs have a short duration and rapid onset?

A

alcohol heroin

70
Q

what are 2 less intense, slower onset, and longer duration drugs?

A

chlordiazepoxid (helps with alcohol withdrawal)

methadone (long acting heroin)

71
Q

Compulsion requiring continuous or periodic use for pleasure or to avoid discomfort is called…

what are some features?

A

Psychological depedence

 Features
• May be most powerful reinforcing factor in drug
seeking/taking behavior
• Most universal characteristic
• Influenced by setting
• Biological basis
• More harmful than physical dependence
72
Q

What is the drug abuse addiction triad?

A

Tolerance
Physical dependence
Psychological dependence

73
Q

_______ is a chronic Brain Disorder ‐ chronic

disease

A

Addiction

74
Q

What is the most powerful reinforcing factor in drug

seeking/taking behavior?

A

Psychological dependence

75
Q

What are the 2 main causes of AIDS?

A

needle sharing and sex

76
Q

What are in the upper category of drug abuse?(2)

A

nicotine, stimulants

77
Q

What are in the downers category of drug abuse? (2)

A

depressants, narcotics

78
Q

Which category of drug abuse is all arounders?

A

hallucinogens

79
Q

What do we see in sedative-hypnotics, such as alcohol

A
  • CNS
  • Tolerance, Psychological, Physical Dependence
  • Eye signs: Glazed look, nystagmus, corneal reflex, droopy lids
80
Q
  • Acute use – do not function well
  • Overdose – BDZ antidote, others none. Support
  • Withdrawal – life threatening
A

Sedative-hypnotics

81
Q

What are some examples of sedative/hypnotics?

A
  • alcohol
  • barbiturates (reds, yellows, blues…)
  • benzodiazepines
  • gasoline, glue, freon, spray paint, shoe polish, dust remover (Huffing)
82
Q

T/F: Alcohol withdrawal is life threatening

A

TRUTH

83
Q

secobarbital, pentobarbital, amobarbital are barbiturates (sedative hypnotics) and are______-acting and ______ abused.

A

short acting, highly abused

84
Q

Phenobarbital (sedative hypnotic) is a _____-acting and _____-abused

A

long-acting, less-abused (not at all)

85
Q

Which benzodiazepine is a “very dry martini”?

A

diazepam

86
Q

Which benzodiazepine is the date rate drug?

A

rohypnol (C1 drug)

87
Q

alprazolam vs. clonazepam

A

clonazepam is slower acting and slower onset (less likely to be abused)

high abuse of alprazolam

88
Q

colorless, odorless, few drops in drink–>unconscious

A

Date rape drug (GHB)

89
Q

What drug class do the following fall into?

  • Morphine (heroin): “pure” white, “Mexican” brown, smack, horse
  • Codeine ‐ cough syrup abuse
  • OxyContin (Hillbilly Heroin): international internet sales
  • Hydrocodone: increased abuse, now a CII (Vicodin)
  • Dilaudid: drug store heroin, Mr. Brownstone
  • Fentanyl: China white (Acetylfentanyl), 3x as potent as heroin
A

Narcotics

90
Q

How can we abuse-proof oxycontin?

What are the risks assoc?

A

hard coating, harder to crush to snort or inject

causes shift to heroin

(Black box warning implemented as well)

91
Q

Which narcotic is widely abused on the streets?

A

heroin

92
Q

How are we fighting back against abuse? (2)

A

states and cities sue big pharmaceuticals similar to old tobacco suits

monitoring programs

93
Q

What are some reasons medical personnel abuse narcotics? (4)

A
  • access
  • “immune because I am in control”
  • cope with long hours, hard work
  • “just this one time”
94
Q

What are the common narcotics abused by medical personnel? (3)

A

Anesthesiologists-fentanyl
morphine
merperidine

95
Q

What are highly effected by tolerance to narcotics?

What is minimally effected (2)?

A
  • analgesia
  • euphoria
  • mental clouding
  • respiratory depression
  • N/V

minimal: miosis constipation

96
Q

What are the events that lead up to coma and death of narcotic/heroin use?

A
  • Euphoria
  • Psychological dependence
  • Physical dependence
  • Tolerance
  • Miosis
  • Respiratory depression
  • Coma
  • Death
97
Q

Narcotics vs. sedative-hypnotics in regards to….
acute use?
overdose treatment?
withdrawal?

A

-Acute use: narcotics function well, sedative users dont

-Overdose:
naloxone (antidote to heroin), Benzos – flumazenil
Alcohol, barbs ‐ no antidote

-Withdrawal from narcotics: not life‐threatening

98
Q

_______ ____ still require a prescription but now are provided by clinics. Now first responders are sometimes allowed to carry it with them (prefilled syringe). Overdose tx for narcotics

A

Naloxone kits

99
Q

What are some long term drugs used to manage narcotic abuse?

A

-Methadone
-Naltrexone (u blocker)
-Buprenorphine (Several dosage forms)
-Buprenorphine + naloxone
Once daily sublingual

100
Q

All of the following fall under what category of drugs?

  • Cocaine (freebase,crack,rock)
  • Methamphetamine (ice,crank,crystal)
  • Ephedrine,pseudoephedrine
  • Amphetamine (Adderall…)
  • Methylphenidate (Ritalin)
  • Caffeine
  • Nicotine
A

Stimulants (uppers)

101
Q

What is a popular stimulant that is abused that has a DEA restriction and is more addictive than meth?

A

Bath salts

102
Q

What are the effects of stimulants?

A
  • talkativeness
  • paranoia
  • restlessness and insomnia
  • muscle tremors
  • memory lapses and mental confusion
  • hallucination
103
Q

High plasma level=feeling of euphoria happens quickly but then rapidly falls. Leads to pattern of continued use….

A

Stimulants

104
Q

What is a good sign of stimulant use?

A

Mydriasis

105
Q 
For stimulants...what do we see in regards to...
acute use?
chronic use?
overdose?
withdrawal?
A

Acute use: Function well, hyperactive

Chronic use: Paranoia, psychoses

Overdose: Convulsions, arrhythmias, incr body temperature

Withdrawl: Bromocriptine, TCAs

106
Q

CNS fires–>seizures–>increased neuronal firing–>reuptake blockade–> ______ ______ _____

A

exaggerated sympathetic response (cardiovascular complications)

107
Q

What are the symptoms of stimulant OD?

A
  • psychomotor agitation (hypoxia, hypoglycemia, paranoia)
  • seizures: benzos
  • HTN: phentolamine,nitroprusside
  • Cardiac: CCBS NOT BBs
108
Q

What are the treatment of stimulant users?

A
  • Get drug out of system (1 wk-drug/metabolites, 3 wks-4 mo restore NT)
  • Build support system
  • Restructure lives
109
Q

What category do the following drugs fall under?

  • Lysergic Acid Diethylamide ‐ LSD
  • Methylenedioxyamphetamine ‐ XTC, MDA (Molly)
  • Psilocybin
  • Mushrooms ‐ shrooms
  • Peyote ‐ Mescaline
  • PCP, Angel Dust, Hog, Naked But
A

Hallucinogens

110
Q

What are some risks of hallucinogens?

A
  • Altered sense of consciousness -Psychological dependence
  • Physical dependence: not a severe withdrawal
  • Tolerance?
  • Acute overdose
111
Q

Ecstasy (MDA, MMDA) is a ____ hallucinogen and stimulant

A

mild

112
Q
  • Social drug
  • Rave parties
  • Dry mouth, grind teeth, elevated temperatures, obstructive sleep apnea)
  • Cause of death‐ constriction of vessels in heart and brain, dehydration, hyperthermia, may cause hypercarbia
A

Ecstasy

113
Q
  • “Special K”
  • Veterinary Medicine
  • “Trail Mix” ‐ Ketamine + Ecstasy
  • Used as date rape drug
A

Ketamine

114
Q
  • PCP
  • Angel Dust
  • Naked Butt
  • Hog
A

Phencyclidine

115
Q

Pt has bug eyed, walleye…suspect?

A

Phencylidine (PCP)

116
Q 
For phenclyclidine...what do we see in regards to...
acute use?
chronic use?
overdose?
withdrawal?
A

acute use: Hyperactivity, paranoia, analgesia, combativeness, hallucinations

chronic use: Psychosis

overdose: Haloperidol, other
lavage, acidifying agents
(no longer recommended)

Withdrawal: Close observation

117
Q

Marijuana, hashish effects depends on the user and amount they use but can lead to 3 types of effects….

A

stimulant, depressant, hallucinogen

118
Q
  • Temporary alterations in brain function and behavior
  • Some tolerance develops
  • May intensify pre‐existing mental disorders
  • No evidence to suggest it is a “stepping‐stone” to harder drugs
A

Marijuana

119
Q

T/F: Prolonged use of marijuana does NOT produce permanent changes

A

TRUE

120
Q

Marijuana use
-Does NOT lead to “amotivational syndrome”
-Temporary _______ in heart rate and blood
pressure
-Respiratory impairment including lung cancer (aggravates asthma)
-Suppression of sperm count, ovulation
-no birth defects / genetic damage

A

increase

121
Q

What are some uses of marijuana?

A
  • Nausea and vomiting (cancer chemotherapy)

- Wasting disease (AIDS,CA)…

122
Q

Is medical marijuana legalized in some states? (medical clinics, licensed centers, recreational use)

A

YES

123
Q

What effects do we see in marijuana users?

A
  • Mental changes
  • Psychological dependence
  • Physical dependence
  • Tolerance? (reverse?): saturated
  • Acute overdose nonexistent
124
Q

What is the differentiating eye sign for marijuana use?

A

red sclera

125
Q

What is the final common pathway?

A

dopamine (pleasure center)

Neuro 2 Midterm (5 decks)

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