Exam 5: MOA and Clinical Uses Flashcards
Serotonin Receptor Agonists (Triptons) MOA ?
Serotonin receptor agonist act selectively on serotonin receptors in cranial arteries
Block release of vasoactive substances associated with migraines
Serotonin Receptor Agonists (Triptons) CU ?
Migraine relief
Prophylactic use
Ergotamines MOA ?
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
Ergotamines CU ?
Abort or prevent vascular-based headaches / migraines
Dopamine pre-cursors MOA ?
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)
Carbidopa/Levodopa (Sinemet)
MOA ?
Inhibits peripheral dopamine decarboxylation
Crosses blood-brain barrier and serves as dopamine precursor
Once in the brain converted to dopamine which improves nerve conduction
Carbidopa/Levodopa (Sinemet)
MOA cont.. ?
Carbidopa does not cross the blood brain barrier
Added to prevent the breakdown of levodopa before it crosses BBB
Carbidopa/Levodopa (Sinemet)
CU ?
Parkinson’s disease
Amantadine (Symmetrel)
MOA ?
In Parkinson disease potentiates CNS dopaminergic responses
Blocks viral particle un-coating and nucleic acid release into host cell, inhibiting viral replication
Amantadine (Symmetrel)
CU ?
Parkinsonism
Extrapyramidal symptoms
Influenza A Tx/prophylaxis
Ropinirole (Requip)
MOA ?
Stimulates dopamine receptors (dopamine agonist)
Ropinirole (Requip)
Clinical uses ?
Parkinson’s disease (alone or as adjunct to levodopa)
Restless legs syndrome
Benztropine (Cogentin)
MOA ?
Cross blood-brain barrier
Direct inhibitory effect on ACH
Block excitability of central neuron pathways of parasympathetic nervous system
Return dopamine/acetylcholine balance
Benztropine (Cogentin) CU ?
Parkinson’s disease
Dystonic / Extrapyramidal symptoms (Phenothiazine’s -
Reglan, Phenergan)
Control salivation and drooling
Donepezil (Aricept) and
Memantine (Namenda) MOA ?
Glutamate pathways trigger NMDA receptors
If overstimulated from excessive amounts of glutamate ( precursor to GABA)
Metantine attaches to NMDA receptors and protects from overstimulation
Donepezil (Aricept) and
Memantine (Namenda) CU ?
Moderate to severe dementia of Alzheimers type
Bupropion (Wellbutrin, Wellbutrin SR, Zyban) MOA ?
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)
Bupropion (Wellbutrin, Wellbutrin SR, Zyban) CU ?
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)
Mirtazapine (Remeron) MOA ?
Antagonizes alpha-2 adrenergic and serotonin 5- HT2 receptors (tetracyclic)
Not to be confused with “Tri-cyclic antidepressant” (TCA)
Mirtazapine (Remeron) CU ?
Major depressive disorder
Amitriptyline (Elavil) MOA ?
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
Amitriptyline (Elavil) CU ?
Reactive depression
Depression related to alcohol and cocaine withdrawal (Clomipramine)
Neuropathic Pain (amitriptyline)
Enuresis
OCD
Panic Attack
Phenelzine (Nardil) MOA ?
non-selectively inhibits monoamine oxidase, exhibiting antidepressant effects
Phenelzine (Nardil)
CU ?
Refractory unipolar depression
Trazodone (Oleptro)
MOA ?
antagonizes serotonin 5-HT2A/C and alpha-1 adrenergic receptors
inhibits serotonin reuptake
Similar chemical structure to alprazolam (Xanax)
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
Haloperidol (Haldol) and
Chlorpromazine (Thorazine) MOA ?
selectively antagonizes dopamine D2 receptors (phenothiazine)
Haloperidol (Haldol) and
Chlorpromazine (Thorazine) CU ?
Acute, idiopathic psychotic illness
Manic phase of Bipolar disorder
Schizophrenia
Antipsychotics (Second Generation) MOA ?
antagonizes dopamine D2 receptors
serotonin 5-HT2 receptors, alpha adrenergic receptors
cholinergic muscarinic receptors
Antipsychotics (Second Generation) CU ?
Psychosis in patients with schizophrenia
Depression with mamia
Bipolar disorder
Agitation and delusions in patients with dementia