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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
Q

Trazodone (Oleptro)

MOA ?

A

antagonizes serotonin 5-HT2A/C and alpha-1 adrenergic receptors

inhibits serotonin reuptake

Similar chemical structure to alprazolam (Xanax)

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26
Q

Trazodone (Oleptro) CU ?

A

Off-label panic disorders, agoraphobia, cocaine withdrawal, aggressive behavior

Major depression with anxiety, insomnia or chronic pain syndromes

Off-label use sedatibe-hypnotic

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27
Q

Haloperidol (Haldol) and

Chlorpromazine (Thorazine) MOA ?

A

selectively antagonizes dopamine D2 receptors (phenothiazine)

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28
Q

Haloperidol (Haldol) and

Chlorpromazine (Thorazine) CU ?

A

Acute, idiopathic psychotic illness

Manic phase of Bipolar disorder

Schizophrenia

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29
Q

Antipsychotics (Second Generation) MOA ?

A

antagonizes dopamine D2 receptors

serotonin 5-HT2 receptors, alpha adrenergic receptors

cholinergic muscarinic receptors

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30
Q

Antipsychotics (Second Generation) CU ?

A

Psychosis in patients with schizophrenia

Depression with mamia

Bipolar disorder

Agitation and delusions in patients with dementia

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31
Q

Methylphenidate (Ritalin) MOA ?

A

stimulates CNS activity

blocks reuptake and increases release of norepinephrine and dopamine in extra neuronal space (sympathomimetic)

32
Q

Methylphenidate (Ritalin)

CU ?

A

ADD / ADHD

Narcolepsy

33
Q

Methylphenidate (Concerta) and Atomoxetine (Strattera) MOA ?

A

stimulates CNS activity

blocks reuptake and increases release of norepinephrine and dopamine in extra neuronal space (sympathomimetic)

34
Q

Benzodiazepines
 MOA ?

A

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
Q

Benzodiazepines
 CU ?

A

Treatment of alcohol addiction and drug withdrawal

Anticonvulsant

Anxiety disorders
Muscle relaxant for spasticity disorders
Adjuvant for anesthesia

36
Q

SSRIs MOA ?

A

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
Q

SSRIs CU ?

A

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
Q


Venlafaxine (Effexor, Effexor SR) MOA ?

A

inhibits norepinephrine, serotonin, and dopamine reuptake (SNRI)

39
Q


Venlafaxine (Effexor, Effexor SR) CU ?

A

Major depressive disorder

Generalized anxiety disorder

Panic disorder

Migraine headache prophylaxis

40
Q

Trazodone (DESYRYL) MOA ?

A

Exact mechanism of action unknown

antagonizes serotonin 5-HT2A/C and alpha-1
adrenergic receptors

inhibits serotonin reuptake

41
Q

Trazodone (DESYRYL) CU ?

A

Major depressive disorder

Insomnia (CCF case)

42
Q

Bupropion (Wellbutrin SR, Zyban) 
 MOA ?

A

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
Q

Bupropion (Wellbutrin SR, Zyban) 
CU ?

A

Major depressive disorder

ADHD (attention deficit hyperactivity disorder)

Smoking cessation

44
Q


Mirtazapine (Remeron) 

 MOA ?

A

Exact mechanism of action unknown

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

45
Q


Mirtazapine (Remeron) 

 CU ?

A

Major depressive disorder

46
Q

Duloxetine (Cymbalta)


 MOA ?

A

Exact mechanism of action unknown

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

47
Q

Duloxetine (Cymbalta)


 CU ?

A

Major depressive disorder

48
Q

Lithium MOA ?

A

Alters neuronal sodium transport

49
Q

Lithium CU ?

A

Bipolar disorder (acute and maintenance)

Adjuvant with other antidepressants to treat major depression

Adjuvant with antipsychotics to treat schizophrenia

50
Q

Anorexiants MOA ? Phentermine (Adipex)
and Benzphetamine (Didrex)
?

A

Act like amphetamines

Stimulate centers in the hypothalamus and limbic regions

Tell the brain is satiated (satisfied) and needs no further calorie intake

51
Q

Phenytoin (Dilantin) MOA ?

A

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
Q

Anticonvulsants MOA ?

A

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
Q

Iminostilbenes – Mechanism of action ?

A

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
Q

Succinimides MOA ?

A

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
Q

Succinimides CU ?

A

Control of absence (petit mal) seizures in children and adults that are refractory to other drugs

56
Q

Iminostilbenes CU ?

A

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
Q

Lamotrigine (Lamictal)

MOA ?

A

Mechanism of action unknown

Believed to stabilize neuronal membranes and suppress excitatory activity at the sodium and calcium channels

58
Q

Clonazepam (Klonopin)

MOA ?

A

Also a miscellaneous anticonvulsant similar action to barbiturates as a category

more of a benzo , whole they other two are more excitability

59
Q

Gabapentin (Neurontin)

CU ?

A

Restless leg syndrome

Postherpetic neuralgia

Most effective as adjunct against partial and generalized seizures

60
Q

Valproate (Depakote)

CU ?

A

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
Q

Pregabalin (Lyrica) MOA ?

A

Mechanism of action unknown

Binds alpha-2-delta subunit of calcium channels reducing neurotransmitter release

Provides anti-nociceptive and anti-seizure affects

62
Q

Pregabalin (Lyrica)

CU ?

A 
Neuropathic pain 
Postherpetic neuralgia 
Partial seizures as adjunct 
Fibromyalgia
(similar to gabapentin)
63
Q

Levetiracetam (Keppra)

MOA ?

A

Mechanism of action unknown

selectively prevents hyper-synchronization of epileptiform burst firing

64
Q

Levetiracetam (Keppra)

CU ?

A

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
Q

Topiramate (Topamax)

MOA ?

A

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
Q

Topiramate (Topamax)

CU ?

A

Partial seizures
Primary generalized tonic clinic seizures
Migraine headache prophylaxis

67
Q

Lacosamide (Vimpat)

MOA ?

A

Mechanism of action unknown

enhances slow inactivation of voltage-sensitive Na channels

stabilizing neuronal membranes

inhibiting repetitive firing

68
Q

Lacosamide (Vimpat)

CU ?

A

Partial seizures

69
Q

Anticonvulsants

used for Bipolar ?

A

Lamotrigine (Lamictal)
Carbamazepine (Tegretol)
Oxcarbazepine (Trileptol)
Valproate (Depakote)

70
Q

Phenobarbital (Luminol)

MOA ?

A

alters sensory cortex, cerebellar, and motor activities

produces sedation, hypnosis, and anesthesia (barbiturate)

71
Q

Phenobarbital (Luminol)

CU ?

A

Seizure disorder

status epilepticus

72
Q

Zaleplon (Sonata)
Zolpidem ( Ambien)
Eszopiclone (Lunesta)
classified as ?

A

classified as “non-benzodiazepine hypnotics”

act on benzodiazepine receptors in the brain

73
Q

Zaleplon (Sonata)
Zolpidem ( Ambien)
Eszopiclone (Lunesta)
MOA ?

A

Act on GABA-benzodiazepine receptors by binding to them and producing CNS depression

74
Q

Zaleplon (Sonata)
Zolpidem ( Ambien)
Eszopiclone (Lunesta)
CU ?

A

Induction of sleep (no analgesic properties)

75
Q

Ramelteon (Rozerem)

MOA ?

A

Binds to melatonin MT-1 amd MT-2 receptors inducing sleep

76
Q

Ramelteon (Rozerem)

CU ?

A

Insomnia

77
Q

Over-the-Counter (OTC) Sleep Aids, Active ingredients: ________________ and doxylamine (older antihistamines)

A

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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