Drugs Flashcards

1
Q

Tacrine

A

Cholinesterase Inhibitor
Used for AD
Not used much because of side effects

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2
Q

Donepezil

A

Cholinesterase inhibitor

Used for AD

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3
Q

Rivastigmine

A

Cholinesterase inhibitor

Used for AD

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4
Q

Glantamine

A

Cholinesterase Inhibitor

Used for AD

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5
Q

Cholinesterase inhibitors for AD

Side Effects

A

GI
Mucle Cramping
Abnormal Dreams

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6
Q

Memantine

A

NMDA channel blocker
Used to slow AD
Side Effects: headache and dizziness

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7
Q

L-DOPA

A

Restores DA in basal ganglia
Mech: uses AA transporter to enter brain
Decarbozylated to DA in DA cells (L-AAAD)

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8
Q

L-DOPA kinetics

A

2% get in brain (metabolized by peripheral L-AAAD or COMT
Short half-life (1-3 hrs
Absorption dependent on GI content

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9
Q

Carbidopa

A

inhibitor of peripheral L-AAAD

Increases CNS concentration of L-DOPA

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10
Q

Entacapone

A

COMT inhibitor

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11
Q

L-DOPA Use

A

Very effective for PD against all symptoms
benifits outlast half-life
best results for first few years, so not used until symptoms are present

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12
Q

L-DOPA Side Effects

A

Dyskinesia
Dementia, Confusino (treat with antipsychotic [clozapine]
GI
CV (postural hypotension, arrhythmias, HTN

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13
Q

L-DOPA interactions

A

Pyridoxine
MAO inhibitors
Halothane
Antipsychotics that are DA antagonist

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14
Q

L-DOPA contraindication

A

Glaucoma
psychosis
Cardiac disease that ivolves arrhytmias
Malignant melanoma

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15
Q

DA receptor agonist

A

Miic DA without need for intact nerve teminals
Mech: Agonsit of DA receptors in striatum
Advantages: No enzymatic conversion
selectivity for receptor subtypes
longer half life
less DA dependent oxidative stress

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16
Q

Pramipexol

A

D2 agonist

most commonly used currently for PD

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17
Q

Ropinerole

A

D2 agonist

most commonly used currently for PD

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18
Q

Apomorphine

A

High D4 affinity, moderate affinity for D2, D3, and D5

subq injections for immediate thrapy of an off episode

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19
Q

Pramipexol/Ropinerole Kinectics

A

can be titrated to therapeutic doses over a week or less

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20
Q

DA agonists Side effects

A

nausea
fatique
sudden attacks of daytime sleep
CNS toxicity (confusion [dont use in elderly pts], dyskinesia)
Apomorphine can cause increased QT prolongation and injection site RXNs

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21
Q

Selegiline/Rasagiline

A

MAO-B inhibitors
prolong the action of DA amd may reduce oxidative stress on neurons
Mech- selective, irreersible inhibiton of MAO-B

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22
Q

Seleginlin/Rasaglinie Use

A

Prescribed as soon as the diesae is diagnosed
used together with L-DOPA in advanced diseases
anti depreseant
modest effects on progression

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23
Q

Sele/Rasa Side Effects

A

Well tolerated in early disease
late- worsens side effects of L-DOPA
metabolized to amphetamines (nxiety and insomina)

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24
Q

Sele/Rasa interactions

A

when given with meperidine, tricyclic antidepressants and SSRI causes serotionin syndrome

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25
Tolcapone
COMT inhibotr | Prolong DA action
26
Tocapone effective
long half life, both peripheral and central
27
Tolcapone Side Effects
Nausea, orthostatic hypotension, vivid dreams, confusion, hallucinations liver toxicity
28
Trihexyphenidyl/benztropine
Antimuscarnics | antagonist of striatal muscarrinic receptors
29
Antimuscarcnics side effects
sedation, mental confusion | atropine like side effects in the peripheyr
30
Amantadine
increases DA release, mildly anticholinergic, blocks NMDA receptors
31
Amantadine Side effects
Dizziness, lethargy, sleep disturbances peripheral edema contra with CHF
32
Floxetine
Huntington - Depression
33
Tetrabenzine
Huntington - VMAT for movement control
34
Riluzole
NMDA channel inhibitor - inhbits glutamate release; increases uptake Modes but genuine effects on ALS Increases life span 2-3 months
35
LSD
Serotoinin Agonsit Nonspecific - 5-ht2 receptor hallucinogen
36
Buspiron
5-HT1a receptor partical agonist | Antiaxiety
37
Sumatriptan
5-HT 1b/d receptors on cerebral blood vessels | Migranin headashes. abortive
38
triptans
``` Major class of drugs used to stop existing headaches Almotriptan eletriptan Frovatriptan - Long half life Naratriptan - Long half-life riztriptan Sumatripitan (oral nasal sprac, SC Zolmatriptatn (oral nasal spray) ```
39
Triptans
``` Serotonin HT1b/d agonist Inhibit release of vasoactive peptides - CGRP promote vasoconstriction block brainstem pain pathways inhibit trigeminal nucleus caudalis ```
40
Triptans side effects
``` peripheal vasoconstriction nausea vomiting angina dizziness flushing contra (stoke, MI, HTN and ischemic heart disease) ```
41
Other abortive treatments
Ergots - DHE - Many routes, ergotamine - oral NSAIDs with caffeine steroids butalbital/caffeine/ acetaminophen - BAD Choice
42
TCA (amitryptyline, nortriptyline)
sedating anticholinergic effective for many pain source (prophylaxis)
43
Antiseizure Agents
Divalporoex sodium, valporic acid topiramate gabapentin, pregabalin, lamotrigine
44
Vasoactive agents
Propranolol, atenolol | Verapamil, diltiazem
45
Phenytoin
Mech: Alter ion conductance. Use dependent effect on Na channels
46
Phenytoin Kinetics
Dependent upon drug formulation highly protein bound Pharmacokinetics are dose dependent Usual therapeutic level - 10-20 ug.ml
47
Phenytoin Use
Generalized TC seizures | partial seizures
48
Phenytoin Side effects
Interact with drugs that are metabolized by CYP and protein bound Tox CNS (dose dependent, nausea, anorexia, apathy, sedationg, ataxia, nystagmus and diplopia) Gingival hyperplasia hirsuitism teratogenicity - cardiac defects, cleft palate hypersensitiveity reactions - rash
49
Posphenytoin
Like phenytoin water soluble phenytoin analog used IV in satus epilepticus
50
Carbamazepine
Mech: blocks NA channels at therapuetic concetnraiton, does not appear to interact with GABA systems
51
Carbmazepine kinetics
Unpredictable absorptions | hepatic enzyme induction
52
Carbmazepine Uses
``` Partial seizures (drug of choice) Contra in absence seizures ```
53
Carbmazepine Tox
``` Dose related: diplopia and ataxia GI drowsiness blood dyscasia (not Dose related, elderly) teratogen (spinal bifida) ```
54
Oxcarbazepine
newer analog, less CNS effects than carb
55
Ethosuximide
Mech: reduces low-threshold (t-type) Ca currents in thalamic neurons
56
Ethosuximid Use
Drug of choice for absence seizures
57
Ethosuximide kinetics
well absorbed no protein bound Vd = total body water liver metabolism - inhibited by valproic acid long half life
58
Ethosuximide Tox
GI (dose twice daily | lethargy and fatigue
59
Valproic acid
Mech: block reptitive neuronal firing may reduce t-type ca currents increases GABA Concentration
60
Valproic Acid Kinetics
Protein bound, competes with phenytoin distributes in extracellualr fluid inhibits metabolism of phenobarbital, phenytoin, carbamazepine
61
Valproic Acid Use
Absence seizures Absence seizures with concomitant - generalized TC seizures Generalized TC seizures and partial seizures myocolonic seizures
62
Valproic Acid Tox
GI upset wt gain, hair loss idiosyncratic hepatotoxiticty teratogenicity - spinal bifida
63
Felbamate
GGlycine modulatory site on N-methyl-d-aspartate receptor (antagonist) Potentiates GABA
64
Felbamate Use
Partial seizures (refractory)
65
Felbamate Tox
aplastic anemia, hepatic failure
66
Gabapentin
Structural analog of GABA. Gaba in its action not clear (Not a GABA agonsit)
67
Gabapentin (use
Partial seizures w/ or w/o secondarily generalized TC seizures neuropathic pain and ALS
68
Gabapentin tox
not metabolized/ no proteins bindings making it devoid of the usual drug interactions
69
Pregabalin
More potent than GAbapentin | Alpha 2 - Delta subunit of Voltage-gated Ca channels reducing neurotransmitter relaease
70
Pregabalin Use
Adjunctive therapy for partial seizures | management of neuropathic pain associaed with diabetic neuropathy and postherpetic neuralgia and fibromyalgia
71
Pregabalin tox
very limited abuse potential
72
Lamotrigine
blocks repetitive action potential and may block Na channels
73
Lamotrigine use
partial, generalized TC and absence | bipolar disorder
74
Lamotrigine Kinetics
does not interfere with other drugs
75
Lamotrigine effects
serious rash (stevens-johnson syndrome)
76
Topiramate
anatagonizing excitartory amino acids to activate the kainate/ampa of glutamate receptor may also block Na channels similar to phenytoin blocks the spread of sezure rather than raise the seizure threshold
77
Topirmate use
add on therapy of adults with partial seizure | prevention of migraine
78
Topirmate effects
fatigue, nausea, and confusion, wt loss
79
Tiagabine
Inhibits the GABA trasporter, GAT1 and thus reuptake of GABA | increase GABA in synapse
80
Tiagabine Use
Effective add on treatment for both complex and simple partial seizures
81
Tiagabine effects
dizziness, tremor and somnolence
82
levetiracetam
Unknow mech
83
levetiracetam use
partial seizures myoclonic seizures and generalized TC
84
leveteracetam effects
somnolence, asthenia, dizziness
85
zonisamide
Na and Ca channels, reduces the voltage dependent transient inward currents
86
Zonisamide use
stops spread of seizures and suppresses their focus | partial seizures adjunctive treatment
87
Zonisamide effects
ataxia, anorexia, nervousness, fatgue and speech impairment are common
88
Vigabatrin
irreversibly inhibiting GABA metabolisme | GABA transaminase inhibitor
89
Vigabatrin use
complex partial seizures and infantile spasms
90
Vigabatrin effects
permanent effects on vision
91
Clobazam
blocks votage dependent Na and Ca channels, suppresses neuronal hypersynchoronization and inhibits carbonic anhydrase
92
Clobazame Use
seizures with lennox-gastaut syndrom
93
Lacosamide
slow inactivation of volatage gated Na channels
94
Lacosamide use
partial seizures
95
Perampanel
AMPA atagonis
96
Perampanel use
partial seziures
97
Parampanel effects
potent CyP3A inducer
98
Ezogabine
K channel facilator
99
Ezogabine Use
partial onset seizures in adults
100
Ezogabine effects
retinal abnormalities, vision loss and bluish skin discoloration
101
Rufinamide
protective in the maximal electroshock and pentylenetertaol test in rats and mice decrease high frequency firing neurons prolon inactive state of the na channel
102
Rufinamide use
seizures with lennox gastaut syndrome 4 y/o or older | effects in all seizures espesially tonic atonic seizures