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Pharmacology Unit 3 and 4 > Dopaminergic agents > Flashcards

Dopaminergic agents Flashcards

1
Q

Levodopa

A

Class: Dopamine precursor

Mech: Crosses the BBB and converted to dopamine

Thera: Parkinson’s Disease (used late in the course of treatment because get densensitization over time called on-off phenomenon which ends up giving side effects)

Tox: Dyskinesia, psychosis, mania, hypervigilant, nausea, dizziness, anxiety, hypotension, syncope, fatigue

Misc: Given with Carbidopa

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2
Q

Carbidopa

A

Class: N/A

Mech: Inactivates dopamine activity in periphery (does not cross the BBB)

Thera: Parkinson’s Disease (given with levodopa in order to lower peripheral dopamine activity)- helps reduce fatigue, dizziness, nausea

Tox: N/A

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3
Q

L-Methylfolate/S-adenosyl methionine (SAM)

A

Class: 1 Carbon metabolism intermediates

Mech: Increases 1-carbon cycle which ultimately increases the amount of tyrosine converted to dopamine

Thera: Depression (less aggressive than L-DOPA)

Tox: Rare maybe GI upset

Misc: Considered complimentary alternative medicine

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4
Q

Bupropion

A

Class: N/A

Mech: Blocks both dopamine and NE transporters blocking their reuptake into the presynaptic neuron and causing their accumulation within the synapse

Thera: Depression

Tox: DA: Hypervigilence, seizures, nausea, agitation
Insomnia, NE poisoning (dry mouth, sweating, palpitations, hypertension)

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5
Q

Dextroamphetamine
Mixed Amphetamine Salts
Lisdexamfetamine

A

Class: Amphetamines (Lisdexamfetamine is a prodrug to amphetamine)

Mech: 1: Blocks DAT

2: Reverses DAT
3: Increases VMAT2 activity causing even more DA to be dumped into synapse via vesicles

Thera: ADHD

Tox: Strong propensity for addiction (mesolimbic pathway)
High doses may see psychosis
Appetite and subsequent weightloss
Typical DA and NE overdose SEs
DA: Hypervigilence, seizures, nausea, agitation
Insomnia, NE poisoning (dry mouth, sweating, palpitations, hypertension)

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6
Q

Methylphenidate

A

Class: N/A

Mech: Blocks DAT

Thera: ADHD

Tox: See amphetamines although less severe addiction
DA: Hypervigilence, seizures, nausea, agitation
Insomnia, NE poisoning (dry mouth, sweating, palpitations, hypertension)

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7
Q

Modafinil/Armodafinil

A

Class: Stimulant (pseudostimulant actually)

Mech: 1: Increases histamine activity in the tuberomammilary nucleus causing alertness in frontal cortex

2: Increases orexin activity
3: Blocks DAT
4: Manipulate NE receptors postsynaptically

Thera: Fatigue due to narcolepsy, apnea, shiftwork
NOT used for ADHD

Tox: Less addictive than amphetamines or Methylphenidate
DA: Hypervigilence, seizures, nausea, agitation
Insomnia, NE poisoning (dry mouth, sweating, palpitations, hypertension)

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8
Q

Selegiline (low dose)

Rasagiline

A

Class: MAO-B inhibitor

Mech: MAO-B is responsible for breaking down DA primarily. These inhibitors are irreversible

Thera: Parkinson’s Disease

Tox: Hypotension, dizziness, insomnia, weight gain

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9
Q

Isocarboxazid
Phenelzine
Tranylcypromine
Selegine (high doses)

A

Class: MAO-A and B inhibitor

Mech: Responsible for breaking down monoamines DA, NE, 5-HT. Irreversible inhibitor

Thera: Depression

Tox: Hypotension, dizziness, insomnia, weight gain
Hypertensive Crisis
Serotonin Syndrome (antidepressants, narcotics, antihistamines)-tremor, muscle spasm, increased/decreased vitals, hyperthermia, delirium, coma, death

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10
Q

Entacapone

Tolcapone

A

Class: COMTi

Mech: Will cause elevations in DA or NE or other monoamines

Thera: Parkinson’s

Tox: Nausea, fatigue, liver failure (tolcapone)

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11
Q

Bromocriptine
Pramipexole
Ropinerole
Apomorphine injections

A

Class: DA2 receptor agonist

Mech: DA2 receptor is a phasic receptor

Thera: PD, RLS

Tox: Nausea, fatigue, dizziness, mania

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12
Q

Aripiprazole

A

Class: DA3 receptor agonist, also DA2 agonist

Mech: DA3 receptor is a static receptor

Thera: Antipsychotic or depression

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13
Q

Amantadine

A

Class: Antiviral

Mech: 1: Release DA

2: Block DAT
3: Stimulate D2 receptors

Thera: PD, influenza

Tox: Nausea, dizziness, psychosis, insomnia, seizures

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14
Q

Reserpine

A

Class: VMATi

Mech: Vesicles cannot be loaded and released decreasing DA and NE in the synaptic space

Thera: HTN, psychosis

Tox: Less DA increases depression while less NE decreases depression

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15
Q

Tetrabenzamine

A

Class: VMATi

Mech: Vesicles cannot be loaded and released decreasing DA and NE in the synaptic space

Thera: HD

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16
Q

Haloperidol
Fluphenazine
Thiothixine

A

Class: High potency FGA

Mech: High affinity for D2 receptor antagonism however nonselective in that it can occur in any DA pathway

Thera: Psychosis in Schiz

Tox:  Extrapyramidal side effects (EPS)-akathisia (restlessness), dystonia(muscle spasm), parkinsonism, Neuroleptic Malignant Syndrome (hyperthermia, muscle rigidity, vital sign instability, rhabdo)
Tarditive Dyskinesia (permanent choreic or athetotic movements (slow, writhing) due to new D2 receptors being created
17
Q

Chloropromazine

Thioridazine

A

Class: Low potency FGA

Mech: D2 receptor, H1 receptor, Muscarinic, Alpha 1 receptor antagonists

Thera: Psychosis associated with schizo

Tox: D2-EPS
H1-fatigue, increased weight and appetite
Anticholinergic
Anti-alpha1-orthostasis

18
Q

Benztropine
Trihexyphenadyl
Diphenhydramine

A

Class: Anticholinergics

Mech: Inhibiting cholinergic tone in the basal ganglia improves dopaminergic flow in the nigrostriatal pathway

Thera: EPS associated with FGA

Tox: Dry mouth, blurred vision, tachycardia, constipation, confusion, delirium, hallucinations

19
Q 
Risperidone
Paliperidone
Ziprasidone
Iloperidone
Lurasidone
A

Class: “Dones” SGA

Mech: D2 receptor antagonism, 5-HT2a antagonism which allows for greater blocking of DA in the mesolimbic system while allowing better transmission in all other DA pathways

Thera: D2: Antipsychosis, aggression in autism, mania
5-HT: Lessens EPS, anxiety, depression

Tox: Possibly more EPS (distinguish from pines)
Anti-serotonin-headache, GI problems, insomnia, anxiety, suicide risk, Metabolic syndrome (diabetes, hyperlipidemia, HTN, obesity), Stroke in dementia patients

20
Q

Olanzapine
Quetiapine
Asenapine
Clozapine

A

Class: “Pines” SGA

Mech: D2 receptor antagonism, 5-HT2a antagonism which allows for greater blocking of DA in the mesolimbic system while allowing better transmission in all other DA pathways

Thera: D2: Antipsychosis, aggression in autism, mania
5-HT: Lessens EPS, anxiety, depression

Tox: More sedating (H1 antag) and more metabolic syndrome distinguishing from pines
Anti-serotonin-headache, GI problems, insomnia, anxiety, suicide risk, Metabolic syndrome (diabetes, hyperlipidemia, HTN, obesity), Stroke in dementia patients

21
Q

Aripiprazole

A

Class: “Rips” SGA

Mech: Partial agonist of D2 and D3

22
Q

Clozapine

A

Class: Pines SGA

Mech: Antagonizes D2 and 5HT-2a as well as D1, D4

Thera: Most effective anti-psychotic

Tox: Little to no chance of EPS but huge metabolic syndromes
Also may see agranulocytosis

Pharmacology Unit 3 and 4 (14 decks)

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