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
Methylphenidate (Ritalin) MOA ?
stimulates CNS activity
blocks reuptake and increases release of norepinephrine and dopamine in extra neuronal space (sympathomimetic)
Methylphenidate (Ritalin)
CU ?
ADD / ADHD
Narcolepsy
Methylphenidate (Concerta) and Atomoxetine (Strattera) MOA ?
stimulates CNS activity
blocks reuptake and increases release of norepinephrine and dopamine in extra neuronal space (sympathomimetic)
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
Benzodiazepines CU ?
Treatment of alcohol addiction and drug withdrawal
Anticonvulsant
Anxiety disorders
Muscle relaxant for spasticity disorders
Adjuvant for anesthesia
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
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
Venlafaxine (Effexor, Effexor SR) MOA ?
inhibits norepinephrine, serotonin, and dopamine reuptake (SNRI)
Venlafaxine (Effexor, Effexor SR) CU ?
Major depressive disorder
Generalized anxiety disorder
Panic disorder
Migraine headache prophylaxis
Trazodone (DESYRYL) MOA ?
Exact mechanism of action unknown
antagonizes serotonin 5-HT2A/C and alpha-1
adrenergic receptors
inhibits serotonin reuptake
Trazodone (DESYRYL) CU ?
Major depressive disorder
Insomnia (CCF case)
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)
Bupropion (Wellbutrin SR, Zyban) CU ?
Major depressive disorder
ADHD (attention deficit hyperactivity disorder)
Smoking cessation
Mirtazapine (Remeron) MOA ?
Exact mechanism of action unknown
antagonizes alpha-2 adrenergic and serotonin 5-HT2 receptors (tetracyclic)
Mirtazapine (Remeron) CU ?
Major depressive disorder
Duloxetine (Cymbalta) MOA ?
Exact mechanism of action unknown
antagonizes alpha-2 adrenergic and serotonin 5-HT2 receptors (tetracyclic)
Duloxetine (Cymbalta) CU ?
Major depressive disorder
Lithium MOA ?
Alters neuronal sodium transport
Lithium CU ?
Bipolar disorder (acute and maintenance)
Adjuvant with other antidepressants to treat major depression
Adjuvant with antipsychotics to treat schizophrenia
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
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
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
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
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
Succinimides CU ?
Control of absence (petit mal) seizures in children and adults that are refractory to other drugs
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)
Lamotrigine (Lamictal)
MOA ?
Mechanism of action unknown
Believed to stabilize neuronal membranes and suppress excitatory activity at the sodium and calcium channels
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
Gabapentin (Neurontin)
CU ?
Restless leg syndrome
Postherpetic neuralgia
Most effective as adjunct against partial and generalized seizures
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
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
Pregabalin (Lyrica)
CU ?
Neuropathic pain Postherpetic neuralgia Partial seizures as adjunct Fibromyalgia (similar to gabapentin)
Levetiracetam (Keppra)
MOA ?
Mechanism of action unknown
selectively prevents hyper-synchronization of epileptiform burst firing
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
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)
Topiramate (Topamax)
CU ?
Partial seizures
Primary generalized tonic clinic seizures
Migraine headache prophylaxis
Lacosamide (Vimpat)
MOA ?
Mechanism of action unknown
enhances slow inactivation of voltage-sensitive Na channels
stabilizing neuronal membranes
inhibiting repetitive firing
Lacosamide (Vimpat)
CU ?
Partial seizures
Anticonvulsants
used for Bipolar ?
Lamotrigine (Lamictal)
Carbamazepine (Tegretol)
Oxcarbazepine (Trileptol)
Valproate (Depakote)
Phenobarbital (Luminol)
MOA ?
alters sensory cortex, cerebellar, and motor activities
produces sedation, hypnosis, and anesthesia (barbiturate)
Phenobarbital (Luminol)
CU ?
Seizure disorder
status epilepticus
Zaleplon (Sonata)
Zolpidem ( Ambien)
Eszopiclone (Lunesta)
classified as ?
classified as “non-benzodiazepine hypnotics”
act on benzodiazepine receptors in the brain
Zaleplon (Sonata)
Zolpidem ( Ambien)
Eszopiclone (Lunesta)
MOA ?
Act on GABA-benzodiazepine receptors by binding to them and producing CNS depression
Zaleplon (Sonata)
Zolpidem ( Ambien)
Eszopiclone (Lunesta)
CU ?
Induction of sleep (no analgesic properties)
Ramelteon (Rozerem)
MOA ?
Binds to melatonin MT-1 amd MT-2 receptors inducing sleep
Ramelteon (Rozerem)
CU ?
Insomnia
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
