Spring 2013 Pharm review for Reddy Flashcards

1
Q

Name the Excitatory NT in the CNS

A

Glutamate, Substance P

  • dopamine, serotonin, NE, Ach depending on the receptor involved
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2
Q

Name the Inhibitory NT in the CNS

A

GABA, Enkephalins, Glycine (SC)

  • dopamine, serotonin, NE, Ach depending on the receptor involved
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3
Q

What are the four dopaminergic pathways in the brain

A
  1. Nigrostriatal System
  2. Mesolimbic System
  3. Mesocortical System
  4. Tuberinfidibulum System
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4
Q

The Nigrostriatal system regulates

A

movement

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5
Q

The Mesolimbic system regulates

A

emotion, love

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6
Q

The Mesocortical system regulates

A

cognition, motivation

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7
Q

The Tuberinfindibulum system regulates

A

pituitary

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8
Q

Dopamine, NE are both released at nerve terminals, How is the action of these NT terminated

A
  1. Reuptake (about 90%)
  2. MAO-metabolism
  3. COMT-metabolism
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9
Q

Name three drug strategies to increase the amount of NT

A
  1. Inhibit reuptake
  2. Inhibit MAO
  3. Inhibit COMT
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10
Q

Name two examples of drugs used to inhibit NT reuptake

A

cocaine

TCA- Imipramine

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11
Q

Name a drug used to inhibit MAO

A

Selegiline

*used in alzheimer’s dx to inhibit MAO B

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12
Q

Alzheimer’s is characterized by loss of many neurons, especially

A

cholinergic

*Too little Ach

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13
Q

Alzheimer’s results in impairment of

A

memory and cognitive functions

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14
Q

Name a drug used to increase AcH in the brain

A

Donepezil

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15
Q

What NT is implicated in destruction of cholinergic nerve death

A

Glutamate

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16
Q

What drug is used to address glutamates effect on patient’s with alzheimers

A

Memantine

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17
Q

Attention-deficit/Hyperactivity disorder is characterized by

A

Persistent pattern of frequent, severe inattention and/or hyperactivity

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18
Q

What drugs are most frequently used to tx ADHD

A

stimulants

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19
Q

What secondary drug is used to tx ADHD

A

nonstimulant

  • Atomoxetine- given to patient’s refractory to stimulant therapy
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20
Q

Atomoxetine is a

A

selective NE reuptake inhibitor

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21
Q

Name two stimulants used to tx ADHD

A

methylphenidate (ritalin)
amphetamine (adderrall)

  • both work in RAS
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22
Q

methylphenidate’s MOA includes

A

blocking reuptake of dopamine in CNS

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23
Q

amphetamine’s MOA includes

A

increases release of dopamine & NE

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24
Q

Name the three main drug categories used to tx anxiety

A
  1. Benzodiazepine
  2. Non-Benzo Benzos
  3. Buspirone
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25
Q

Benzos agonize what receptor

A

GABA

  • opens chloride channels
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26
Q

Non-Benzo benzos agonize what receptor

A

GABA

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27
Q

Name some benzos

A

“zepam” or “zolam”

Diazepam, Lorazepam, Midazolam

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28
Q

Buspirone partially agonizes what serotonin subtype

A

5-HT 1A

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29
Q

What is the difference b/t Buspirone and Benzos

A

Benzos onset immediate
Buspirone onset takes weeks

Buspirone increases risk for seizures, increased HR (stimulant)

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30
Q

Non-Benzo benzo’s major difference from Benzos is that

A

it is less addictive

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31
Q

Name three major non-benzo benzos

A

Zolpidem
Zaleplon
Eszopiclone

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32
Q

What is the GABA antagonist used to treat overdose of benzos and non-benzo benzos

A

Flumazemil

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33
Q

Name a drug used to inhibit COMT

A

**capone

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34
Q

What two drugs help with insomnia

A

Melatonin (released by pineal gland)

RaMELTeon

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35
Q

Parkinson’s is characterized by

A

too little dopamine in the nigrostriatial pathway

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36
Q

What 1st line drug combination is used to tx parkinsons

A

levadopa and carbidopa

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37
Q

Why is carbidopa added to L-dopa therapy

A

to inhibit L-aa carboxylase from converting L-dopa to Dopamine in the periphery

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38
Q

What is the on-off phenomenon seen with parkinson treatment with L-dopa/carbidopa

A

normal movement followed by resting tremors, rigidity, bradykinesia, etc

  • caused by continued loss of dopamine neurons
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39
Q

Name three other strategies besides replacing dopamine used to tx parkinsons

A

block metabolism of dopamine
dopamine agonism
anti-Ach drugs

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40
Q

name two drugs used to block dopamine metabolism via inhibition of COMT

A

talCAPONE

entaCAPONE

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41
Q

name a drug used to block dopamine metabolism via inhibition of MAO

A

selegiline (MAO B)

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42
Q

Name a dopamine agonist used to tx parkinsons

A

Bromocriptine

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43
Q

Name an anti-cholinergic drug used to tx parkinsons

A

benztropine

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44
Q

Huntington’s disease is characterized by loss of

A

GABA neurons- loss of inhibition

*Too much movement (chorea)

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45
Q

What is the tx strategy for Huntington’s disease

A

control symptoms, support therapy

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46
Q

List the four primary drugs used to tx epilepsy

A

Valproic acid
Ethosuximide
Phenytoin
Carbamazepine

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47
Q

Name the generalized seizures

A

Generalized tonic-clonic (grandMal)
Absence (PetitMal)-originating in occipital area
Myoclonic (muscle involvement)

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48
Q

Name two drugs used to treat generalized tonic-clonic seizures

A

carbamazepine

valproic acid

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49
Q

Name two drugs used to tx absence seizures

A

Ethosuximide-blocks ca2+ current in thalmus

valproic acid

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50
Q

Name the three partial seizures

A

simple partial - No LOC
complex partial - LOC
partial seizures with secondary generalization

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51
Q

Name a drug used to tx all three partial seizures

A

carbamazepine

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52
Q

What is the MOA of most antiepileptic drugs

A

blocking or hyperpolarizing ion channels

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53
Q

What two antiepileptics work by blocking sodium channels

A

Carbamazepine

Phenytoin

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54
Q

What two antiepileptics work by blocking calcium channels

A

Ethosuximide

Valproic acid

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55
Q

What four antiepileptics work by hyperpolorizing neurons

A

Carbamazepine
Benozs
Phenobarbital
Valproic Acid

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56
Q

Name two other strategies used to tx epilepsy

A

enhancement of GABA

reduction of excitatory NT

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57
Q

Name four SSRI used to tx depression

A

Fluoxetine
Sertaline
Citalopram
Escitalopram

58
Q

Name four TCAs used to tx depression

A

Amytryptiline, Nortryptiline

Imipramine, Clomipramine

59
Q

TCAs MOA is

A

nonspecific blockers of serotonin and NE

60
Q

Why is SNRI considered better than TCAs even though they both target the same transporters

A

SNRIs have no SE common to TCAs

61
Q

What are the SE of TCA administration

A

Anticholinergic- urinary retention, dry eyes, constipation, dry mouth
Antihistamine- sedation
alpha 1 blockade-dizziness, orthostatic hypotension

62
Q

What are cholinergic AE

A

DUMB BELSS

D-Diarrhea
U-Urination
M-Miosis
B-Bradycardia
E-Excitation (CNS & Skeletal muscles)
L-Lacrimation
S-Salivation
S-Sweating
63
Q

Schizophrenia is characterized by

A

too much dopamine in the mesolimbic system

64
Q

List the Positive symptoms of schizophrenia

A

Hallucination
Delusions
Bizzare behavior

65
Q

List the Negative symptoms of schizophrenia

A

Affective flattening - dec. in emotional expression

Alogia- decr. in fluency in speech

Avolition- decr. in goal-oriented behavior

66
Q

What are the strategies used to tx schizophrenia

A

Block dopamine receptors
Block Acetylcholine receptors
Block alpha receptors
Block Histamine receptors

67
Q

What are the AE associatesd with tx of schizophrenia

A

face/neck muscle spasms (tx with antichol)»Akathisia (motor restlessness)»>parkinsonism»»tardive dyskinesia

68
Q

Name two “typical” antipsychotics

A

Chlorpromazine
Haloperidol

  • Possess more extrapyramidal SE than atypical
  • Strictly blocks D2 receptors
69
Q

Name two “atypical” antipsychotics

A

Clozapine

Risperidone

70
Q

What is the advantange of using atypical antipsychotics

A

D2 and 5 HT blockers

Atypicals block the inhibitory 5-HT 2A (presynaptically) in the nigrostriatal pathway and mesocortical pathways yielding less extrapyramidal SE and improvement of negative symptoms

71
Q

How does adding 5-HT antagonism improve the antipsychotics

A

By reducing the SE- mostly motor and endocrine

72
Q

What is Neuroleptic Malignant Syndrome

A

is a life-threatening neurological disorder most often caused by an adverse reaction to neuroleptic or antipsychotic drugs

  • dopaminergic system in hypothalamus is disturbed. Loss of ability to control temperature
73
Q

What are symptoms associated with NMS

A
F – Fever 
A – Autonomic instability 
L – Leukocytosis 
T – Tremor 
E – Elevated enzymes (elevated CPK) 
R – Rigidity of muscles
74
Q

How is NMS treated

A

Supportive care
Dantrolene- Skeletal muscle relaxant
Bromocriptine-DA receptor agonist

75
Q

What is Atomoxetine

A

Non-stimulant drug used to tx ADHD that blocks NE reuptake and is given to patients who cannot tolerate stimulants

76
Q

What is Benztropine

A

Benzatropine is a centrally acting anticholinergic/antihistamine agent used in the tx of Parkinsons

77
Q

What is Entacapone

A

COMT inhibitor used sometimes in patient’s tx for Parkinsons to prevent degradation of L-Dopa or Dopamine

78
Q

What is Eszopicclone

A

Eszopiclone is a short acting nonbenzodiazepine sedative hypnotic used to tx anxiety or insomnia

79
Q

What is Duloxetine

A

SNRI used to tx depression

80
Q

What is Enfuviritide

A

HIV fusion inhibitor

81
Q

What is Fluoxetine

A

SSRI used to tx depression

82
Q

What is Flumazenil

A

Benzodiazepine antagonist used to reverse overdose of benzos/nonbenzos.

83
Q

What is Lamotrigine

A

Antiepileptic

84
Q

What is Memantine

A

used in the tx of Alzheimers to act on the glutamatergic system by blocking NMDA-type glutamate receptors.

*Glutamate neurons thought to play a role in cholinergic neuron destruction

85
Q

What is Oseltamivir

A

is an antiviral drug, which may slow the spread of influenza (flu) virus

86
Q

What is Ramelteon

A

Drug used to tx insomnia (Melatonin-like)

87
Q

What is Rifampin

A

A bacteriocidal drug that inhibits bacterial DNA-dependent RNA synthesis by inhibiting bacterial DNA-dependent RNA polymerase

88
Q

What is Amphoteracin B

A

A polyene macrolide antifungal drug that binds with ergosterol, a component of fungal cell membranes, forming a transmembrane channel that leads to monovalent ion (K+, Na+, H+ and Cl−) leakage, which is the primary effect leading to fungal cell death

*Broadest antifungal spectrum so often used as first choice for mycotic infections

89
Q

What is Metronidazole

A

Mixed amebicide (luminal and systemic tx) for treating protozoal or bacterial infections

  • Prodrug that must be acitvated once inside pathogen cells
  • Activating enzyme= Nitroreductase found ONLY in anaerobic organisms
  • Once induced, it inhibits DNA replicaton and kill cells

*Tx: Trichomoniasis, Ambiasis Giardiasis M-(TAG)

90
Q

What is Mebendazole

A

Used to treat Nematodes (round, whip, pin,hook, ascaris worms) found in GI tract by interfering with microtubules and blocking glucose uptake- Worm can’t move and has no energy»>defecated out in feces

91
Q

What is Terbinafine

A

Antifungal drug used to tx dermatophytes by inhbiting squalene epoxidase and decreasing ergosterol syntheis

92
Q

What is Donepezil

A

a centrally acting acetylcholinesterase inhibitor. Its main therapeutic use is in the palliative treatment of Alzheimer’s disease

93
Q

What is Echothiophate

A

Irreversibly binds to plasma cholinesterase. Once bound, the enzyme is permanently inactive and the cell has to make new enzymes

94
Q

What is Artimisinin

A

Antiprotozoa drug used to tx the most severe and resistant form of malaria caused by Plasmodium Falciparum

*Targets Blood schizonides

95
Q

What is Chloroquine

A

Drug of choice for prophylaxis and tx of uncomplicated attacks of malaria. It binds to heme, preventing its growth in RBC resulting in membrane damage and cell lysis

96
Q

What is Pyrimethamine

A

Antiprotozoa drug used to tx malaria by inhibiting folate needed for DNA/RNA synthesis

97
Q

What is Quinine

A

Antiprotozoal drug used to tx malaria by interfering with polymerization (growth) within heme

98
Q

What is Sulfadoxine

A

is an ultra-long-lasting sulfonamide often used in combination with pyrimethamine to treat or prevent malaria by interfering with folate synthesis

99
Q

What class is Azithromycin

A

protein synthesis inhibitor

100
Q

What class is Cefuroxime

A

second generation cephalosporin

101
Q

What class is Ciprofloxacin

A

Inhibits bacterial DNA synthesis

102
Q

What class is Sulfamethoxazole

A

inhibits folate synthesis

103
Q

What class is Tobramycin

A

Aminoglycoside that inhibits protein synthesis

104
Q

What class is Vancomycin

A

Glycopeptide that inhibits cell wall synthesis

105
Q

What class is Linezolid

A

Protein synthesis inhibitor

106
Q

What class is Rifampin

A

RNA syntheis inhibitor

107
Q

What is the function of adding Clavulonic acid to amoxicillin (Augmentin)

A

Clauvulonic acid B-lactamase while amoxicillin (PCN) inhibit cell wall biosynthesis

108
Q

T/F- Most first generation cephalosporins begin with “ceph”

A

True

109
Q

What is post-antibiotic effect

A

Long after antibiotic is administered, effects linger

110
Q

Name a drug or class that exhibits post-antibiotic effects

A

Aminoglycosides

*Oto, nephro, neuro toxic

111
Q

Name the four mechanism of drug resistance

A
  1. Alter their metabolic pathway
  2. Alter target protein (enzyme)
  3. Alter target site
  4. Decreased membrane permeability
112
Q

Drugs used to tx herpes infections are classifed as

A

Nuceloside analogs VS. Non-nucleoside analogs

113
Q

What drug class is most effective for tx herpes

A

Nucleoside analogs

114
Q

Name two nucleoside analogs

A

Acyclovir

Ganciclovir

115
Q

Name a non nucleoside analog

A

Foscarnet

116
Q

What anti-viral is most effective at treating respiratory infections

A

Ribivarin

*PalvizuMAB: monoclonal antibiody used tx

117
Q

What is the reason for combination tx for HIV

A

Therapy with RT inhibitors and Protease inhibitors can reduce the emergence of resistance and produce additive effects

118
Q

What are the classes of drugs used to tx HIV

A

Reverse Transcritase inhibitors
Protease Inhibitors
Fusion Inhibitors
Integrase Inhibitors

119
Q

Reverse Transcriptase Inhibitors are further classified as

A

Nucleoside inhibitors

Nonnucleoside inhibitors

120
Q

Name three nucleoside RT inhibitors

A

Didanosine
Abacavir
Zidovudine

121
Q

Name one nonnucleoside RT inhibitor

A

Efavirenz

122
Q

Name two protease inhibitors used to tx HIV

A

Indinavir
Ritonavir

“NAVIR”

123
Q

Name two fusion inhibitor used to tx HIV

A

Maraviroc

EnFuviritde

124
Q

Name one integrase inhibitor used to tx HIV

A

RalTEGravir

125
Q

What is the drug of choice to tx Giardia (common cause of diarrhea)

A

Metronidazole

126
Q

What is the drug of choice to tx big round worms found in stool

A

Mebendazole

Albendazole

127
Q

Name two drugs used to tx Influenza A

A

Amantadine
Rimantidine

*must be started within 48 hours to be effective

128
Q

Name two drugs used to tx Influenza A & B

A

Zanamivir
Oseltamivir (Tamiflu)

  • If given within 30 hours of onset of flu, both drugs can shorten the duration of illness
  • Neuramindase inhibitors that are prophylactic for flu
129
Q

Zanamivir is given via what route

A

Inhalation ONLY

130
Q

Oseltamivir is given via what route

A

Orally

131
Q

What drug is used to treat Parkinsons as well as Influenza

A

Amantadine

  • blocks NMDA receptor>Incr. glutamate
  • Txs Influenza A
132
Q

What Cancer drug is unique for targeting cancer-specific tyrosine kinase

A

Imatinib (Gleevec)

133
Q

How does Imatinib work

A

works by preventing a central tyrosine kinase enzyme, in this case BCR-Abl, from phosphorylating subsequent proteins and initiating the signaling cascade necessary for cancer development, thus preventing the growth of cancer cells and leading to their death by apoptosis

134
Q

What is the major AE of Cyclophosphamide

A

Myelosuppression-rate limiting

*alkylating agent (N. Mustard)

135
Q

What is the major AE for Methotrexate

A

Myelosuppression-rate limiting

  • Antimetabolite-Inhibits folate
136
Q

What is the major AE for Taxol

A

Myelosuppression-rate limiting

*binds to tubulin PREVENTING microtubule disassembly

137
Q

What is the major AE for Doxorubicin/Daunorubicin

A

Cardiotoxicity

*Anthracycline: intercalating agent that inserts b/t DNA base pairs

138
Q

What is the major AE for Cisplatin

A

Renal toxicity

*Platinum Coordination Complexes with DNA (guanine)

139
Q

What is the major AE of Vincristine

A

neurotoxicity

  • binds to microtubule and blocks assembly
140
Q

Give an example of combination chemotherapy

A

CHOP
C-cyclophoshamide (crosslinks DNA)
H-Hydroxydaunorubicin (Intercalates with DNA)
O-Oncovin(Vincristine)(mitotic spindle poison)
P-Prednisone (anti-inflammatory steroid, binds tubulin)

141
Q

Name receptors involved in N/V with anti-cancer drugs and the drugs used to antagonize them

A
5 HT 3 (ondansetron)
D 2 (Promethazine) & Phenothiazine

*Phenothiazine should be avoided in patient’s with Parkinson’s disease