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Pharmacology (Dale Turley) > Exam 5: MOA and Clinical Uses > Flashcards

Exam 5: MOA and Clinical Uses Flashcards

1
Q

Serotonin Receptor Agonists (Triptons) MOA ?

A

Serotonin receptor agonist act selectively on serotonin receptors in cranial arteries

Block release of vasoactive substances associated with migraines

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2
Q

Serotonin Receptor Agonists (Triptons) CU ?

A

Migraine relief

Prophylactic use

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3
Q

Ergotamines MOA ?

A

Direct acting vasoconstrictors that stimulate vascular smooth muscle

Decrease in amplitude of extra cranial artery pulses ( threshold of the cranial nerves)

Decrease in the hyperperfusion of the basilar artery

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4
Q

Ergotamines CU ?

A

Abort or prevent vascular-based headaches / migraines

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5
Q

Dopamine pre-cursors MOA ?

A

Carbidopa/Levodopa (Sinemet)

Amantadine (Symmetrel)

General MOA:

In Parkinson disease potentiates CNS dopaminergic responses

Blocks viral particle un-coating and nucleic acid release into host cell, inhibiting viral replication (amantadine)

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6
Q

Carbidopa/Levodopa (Sinemet)

MOA ?

A

Inhibits peripheral dopamine decarboxylation

Crosses blood-brain barrier and serves as dopamine precursor

Once in the brain converted to dopamine which improves nerve conduction

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7
Q

Carbidopa/Levodopa (Sinemet)

MOA cont.. ?

A

Carbidopa does not cross the blood brain barrier

Added to prevent the breakdown of levodopa before it crosses BBB

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8
Q

Carbidopa/Levodopa (Sinemet)

CU ?

A

Parkinson’s disease

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9
Q

Amantadine (Symmetrel)

MOA ?

A

In Parkinson disease potentiates CNS dopaminergic responses

Blocks viral particle un-coating and nucleic acid release into host cell, inhibiting viral replication

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10
Q

Amantadine (Symmetrel)

CU ?

A

Parkinsonism

Extrapyramidal symptoms

Influenza A Tx/prophylaxis

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11
Q

Ropinirole (Requip)

MOA ?

A

Stimulates dopamine receptors (dopamine agonist)

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12
Q

Ropinirole (Requip)

Clinical uses ?

A

Parkinson’s disease (alone or as adjunct to levodopa)

Restless legs syndrome

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13
Q

Benztropine (Cogentin)

MOA ?

A

Cross blood-brain barrier

Direct inhibitory effect on ACH

Block excitability of central neuron pathways of parasympathetic nervous system

Return dopamine/acetylcholine balance

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14
Q

Benztropine (Cogentin) CU ?

A

Parkinson’s disease

Dystonic / Extrapyramidal symptoms (Phenothiazine’s -
Reglan, Phenergan)

Control salivation and drooling

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15
Q

Donepezil (Aricept) and

Memantine (Namenda) MOA ?

A

Glutamate pathways trigger NMDA receptors

If overstimulated from excessive amounts of glutamate ( precursor to GABA)

Metantine attaches to NMDA receptors and protects from overstimulation

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16
Q

Donepezil (Aricept) and

Memantine (Namenda) CU ?

A

Moderate to severe dementia of Alzheimers type

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17
Q

Bupropion (Wellbutrin, Wellbutrin SR, Zyban) MOA ?

A

No effect on blocking Serotonin

Inhibits neuronal uptake of norepinephrine and dopamine (aminoketone)

Results in increasing availability of dopamine and norepinephrine at the post synaptic receptor sites

Also reduces the firing rate of the non-adrenergic neurons (mechanism unknown)

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18
Q

Bupropion (Wellbutrin, Wellbutrin SR, Zyban) CU ?

A

Depression, especially seasonal affective disorder (SAD)

Smoking cessation (Zyban only) when combined with behavior modification therapy

Off label use ADHD in adults (sustained (SR) use only)

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19
Q

Mirtazapine (Remeron)
 MOA ?

A 
Antagonizes alpha-2 adrenergic and serotonin 5-
HT2 receptors (tetracyclic)

Not to be confused with “Tri-cyclic antidepressant” (TCA)

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20
Q

Mirtazapine (Remeron)
 CU ?

A

Major depressive disorder

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21
Q

Amitriptyline (Elavil) MOA ?

A

Increases levels of norepinephrine and serotonin in the synaptic cleft

Have anticholinergic properties

Blocks H-1 and alpha-adrenergic receptors

Properties are reason for numerous side-effects

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22
Q

Amitriptyline (Elavil) CU ?

A

Reactive depression

Depression related to alcohol and cocaine withdrawal (Clomipramine)

Neuropathic Pain (amitriptyline)

Enuresis
OCD
Panic Attack

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23
Q

Phenelzine (Nardil) MOA ?

A

non-selectively inhibits monoamine oxidase, exhibiting antidepressant effects

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24
Q

Phenelzine (Nardil)

CU ?

A

Refractory unipolar depression

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25
Trazodone (Oleptro) | MOA ?
antagonizes serotonin 5-HT2A/C and alpha-1 adrenergic receptors inhibits serotonin reuptake Similar chemical structure to alprazolam (Xanax)
26
Trazodone (Oleptro) CU ?
Off-label panic disorders, agoraphobia, cocaine withdrawal, aggressive behavior Major depression with anxiety, insomnia or chronic pain syndromes Off-label use sedatibe-hypnotic
27
Haloperidol (Haldol) and | Chlorpromazine (Thorazine) MOA ?
selectively antagonizes dopamine D2 receptors (phenothiazine)
28
Haloperidol (Haldol) and | Chlorpromazine (Thorazine) CU ?
Acute, idiopathic psychotic illness Manic phase of Bipolar disorder Schizophrenia
29
Antipsychotics (Second Generation) MOA ?
antagonizes dopamine D2 receptors serotonin 5-HT2 receptors, alpha adrenergic receptors cholinergic muscarinic receptors
30
Antipsychotics (Second Generation) CU ?
Psychosis in patients with schizophrenia Depression with mamia Bipolar disorder Agitation and delusions in patients with dementia
31
Methylphenidate (Ritalin) MOA ?
stimulates CNS activity blocks reuptake and increases release of norepinephrine and dopamine in extra neuronal space (sympathomimetic)
32
Methylphenidate (Ritalin) | CU ?
ADD / ADHD Narcolepsy
33
Methylphenidate (Concerta) and Atomoxetine (Strattera) MOA ?
stimulates CNS activity blocks reuptake and increases release of norepinephrine and dopamine in extra neuronal space (sympathomimetic)
34
Benzodiazepines
 MOA ?
Depress all levels of the CNS by enhancing the action of gamma-butyric acid (GABA) Anxiolytic effect comes from increased action of GABA, thereby decreases the effect of any neuronal excitation
35
Benzodiazepines
 CU ?
Treatment of alcohol addiction and drug withdrawal Anticonvulsant Anxiety disorders Muscle relaxant for spasticity disorders Adjuvant for anesthesia
36
SSRIs MOA ?
Increase the extracellular level of the neurotransmitter serotonin limiting its reabsorption into the presynaptic cell increasing the level of serotonin Increased availability of Serotonin at the receptors results in mood elevation and reduced anxiety
37
SSRIs CU ?
Used in the treatment of stroke patients, including those with and without symptoms of depression Major depression Depression in patients with concurrent illnesses, such as coronary artery disease, glaucoma, hypertension Panic disorder
38

Venlafaxine (Effexor, Effexor SR) MOA ?
inhibits norepinephrine, serotonin, and dopamine reuptake (SNRI)
39

Venlafaxine (Effexor, Effexor SR) CU ?
Major depressive disorder Generalized anxiety disorder Panic disorder Migraine headache prophylaxis
40
Trazodone (DESYRYL) MOA ?
Exact mechanism of action unknown antagonizes serotonin 5-HT2A/C and alpha-1 adrenergic receptors inhibits serotonin reuptake
41
Trazodone (DESYRYL) CU ?
Major depressive disorder Insomnia (CCF case)
42
Bupropion (Wellbutrin SR, Zyban) 
 MOA ?
Exact mechanism of action in smoking cessation or depression unknown Inhibits neuronal uptake of norepinephrine and dopamine (aminoketone - compounds containing both a ketone group and an amine)
43
Bupropion (Wellbutrin SR, Zyban) 
CU ?
Major depressive disorder ADHD (attention deficit hyperactivity disorder) Smoking cessation
44

Mirtazapine (Remeron) 

 MOA ?
Exact mechanism of action unknown antagonizes alpha-2 adrenergic and serotonin 5-HT2 receptors (tetracyclic)
45

Mirtazapine (Remeron) 

 CU ?
Major depressive disorder
46
Duloxetine (Cymbalta)


 MOA ?
Exact mechanism of action unknown antagonizes alpha-2 adrenergic and serotonin 5-HT2 receptors (tetracyclic)
47
Duloxetine (Cymbalta)


 CU ?
Major depressive disorder
48
Lithium MOA ?
Alters neuronal sodium transport
49
Lithium CU ?
Bipolar disorder (acute and maintenance) Adjuvant with other antidepressants to treat major depression Adjuvant with antipsychotics to treat schizophrenia
50
Anorexiants MOA ? Phentermine (Adipex) and Benzphetamine (Didrex) ?
Act like amphetamines Stimulate centers in the hypothalamus and limbic regions Tell the brain is satiated (satisfied) and needs no further calorie intake
51
Phenytoin (Dilantin) MOA ?
Inhibit and stabilize electric discharges from the neurons in the cortex of the brain via sodium calcium and potassium ion exchanges Also affect the brainstem’s role in contributing to the tonic phase of tonic-clonic seizures
52
Anticonvulsants MOA ?
Mechanism of these agents is very complex and stabilize neuron cell membrane by altering sodium potassium and calcium transport causing suppression of excitability of the neurons
53
Iminostilbenes – Mechanism of action ?
Targets the area of the thalamus associated with the spread of seizure neuronal discharge Both medications target the thalamus where they inhibited voltage gated sodium channels resulting in: - Stabilizing hyper-excitatory states - Inhibits repetitive neuronal firing - Decreases propagation of significant impulses
54
Succinimides MOA ?
Decreasing nerve impulses and transmission in the motor cortex Increase in seizure threshold specifically by blocking T type voltage gated calcium channels in the thalamic neurons
55
Succinimides CU ?
Control of absence (petit mal) seizures in children and adults that are refractory to other drugs
56
Iminostilbenes CU ?
Carbamazepine can be used and all types of seizures with the exception of absence seizures Carbamazepine considered to be an equivalent to phenytoin and efficacy and side effects Oxcarbazepine (Trileptal) Can be used alone or in combination with other agents to treat partial seizures in both children and adults Because of their relationship to try-cyclic anti-depressants, these medications can be used to treat bipolar affective disorder (BAD)
57
Lamotrigine (Lamictal) | MOA ?
Mechanism of action unknown Believed to stabilize neuronal membranes and suppress excitatory activity at the sodium and calcium channels
58
Clonazepam (Klonopin) | MOA ?
Also a miscellaneous anticonvulsant similar action to barbiturates as a category more of a benzo , whole they other two are more excitability
59
Gabapentin (Neurontin) | CU ?
Restless leg syndrome Postherpetic neuralgia Most effective as adjunct against partial and generalized seizures
60
Valproate (Depakote) | CU ?
Both agents used in the treatment of refractory complex partial seizures in adults Partial seizures start on one side of the brain as opposed to both sides Liquid at room temperature but when mixed with sodium hydroxide becomes sodium valproate (Depakote, Depacon, Depakene) more mainstream adjuncts - great medicine for HA as well and management they are consider siezure medications but they are also great for cocktails with HA, phenregran as well
61
Pregabalin (Lyrica) MOA ?
Mechanism of action unknown Binds alpha-2-delta subunit of calcium channels reducing neurotransmitter release Provides anti-nociceptive and anti-seizure affects
62
Pregabalin (Lyrica) | CU ?
``` Neuropathic pain Postherpetic neuralgia Partial seizures as adjunct Fibromyalgia (similar to gabapentin) ```
63
Levetiracetam (Keppra) | MOA ?
Mechanism of action unknown selectively prevents hyper-synchronization of epileptiform burst firing
64
Levetiracetam (Keppra) | CU ?
Partial seizures as adjunct : rarely as a primary Juvenile myoclonic epilepsy as adjunct Primary generalized tonic clinic seizures as adjunct monitor serum levels with this one
65
Topiramate (Topamax) | MOA ?
Mechanism of action unknown blocks voltage-dependent sodium channels augments GABA activity antagonizes glutamate receptors glutamate is the precursor inhibits carbonic anhydrase acetazolamide ( diuretic)
66
Topiramate (Topamax) | CU ?
Partial seizures Primary generalized tonic clinic seizures Migraine headache prophylaxis
67
Lacosamide (Vimpat) | MOA ?
Mechanism of action unknown enhances slow inactivation of voltage-sensitive Na channels stabilizing neuronal membranes inhibiting repetitive firing
68
Lacosamide (Vimpat) | CU ?
Partial seizures
69
Anticonvulsants | used for Bipolar ?
Lamotrigine (Lamictal) Carbamazepine (Tegretol) Oxcarbazepine (Trileptol) Valproate (Depakote)
70
Phenobarbital (Luminol) | MOA ?
alters sensory cortex, cerebellar, and motor activities produces sedation, hypnosis, and anesthesia (barbiturate)
71
Phenobarbital (Luminol) | CU ?
Seizure disorder | status epilepticus
72
Zaleplon (Sonata) Zolpidem ( Ambien) Eszopiclone (Lunesta) classified as ?
classified as “non-benzodiazepine hypnotics” act on benzodiazepine receptors in the brain
73
Zaleplon (Sonata) Zolpidem ( Ambien) Eszopiclone (Lunesta) MOA ?
Act on GABA-benzodiazepine receptors by binding to them and producing CNS depression
74
Zaleplon (Sonata) Zolpidem ( Ambien) Eszopiclone (Lunesta) CU ?
Induction of sleep (no analgesic properties)
75
Ramelteon (Rozerem) | MOA ?
Binds to melatonin MT-1 amd MT-2 receptors inducing sleep
76
Ramelteon (Rozerem) | CU ?
Insomnia
77
Over-the-Counter (OTC) Sleep Aids, Active ingredients: ________________ and doxylamine (older antihistamines)
diphenhydramine this will exacerbate older peoples dementia Some are combined with aspirin or acetaminophen and contain either of the two antihistamines

Pharmacology (Dale Turley) (31 decks)

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