Week 5: Pharma Flashcards by Adrienne Gorge

What is the mechanism of L-dopa/carbidopa?

It is converted to dopamine in the CNS; L-dopa crosses the BBB and then converts to dopamine when paired with carbidopa. If not paired with Carbidopa, then some if gets converted to dopamine in the peripheral.

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What is the mechanism of Entacapone/Tolcapone?

COMT inhibitors; prevent L-dopa breakdown

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What is the mechanism of Selegiline?

Prevents dopamine breakdown; MAO-b, so prevents both dopamine and 5HT breakdown; increase dopamine levels

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What is the mechanism of Pramipexole, Ropinirole?

Dopamine agonists

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What is the mechanism of Trihexphenidyl?

antimuscarinic

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Side effects of L-dopa/carbidopa

anxiety, agitation, insomnia

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Side effects of L-dopa

Tachycardia, nausea, vomiting

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Side effects of Tolcapone

peripheral hepatotoxicity

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Side effects of Selegiline

nausea, vomiting, hypotension, excessive daytime sleepiness; Serotonin Syndrome; “Cheese effect”: hypertensive crisis due to lack of tyramine breakdown

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Side effects of Trihexyphenidyl

sedation, dry mouth

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Indication for Trihexyphenidyl

tremor predominant symptoms in patient’s with Parkinson’s

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Indication for Ropinirole, Pramipexole

dopamine agonists for bradykinesia, rigidity

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What is the indication for Levodopa (L-Dopa)

Dopamine precursor for Parkinson’s disease

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MOA of Levodopa

Precursor to dopamine; crosses the BBB and gets processed into dopamine

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Side effects of Levodopa

Dyskinesias; dose may wear off early

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On-off syndrome with Levodopa

quick fluctuation b/w drug functioning and not working

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Indication for Carbidopa/Levodopa

Parkinson’s

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MOA of Carbidopa/Levodopa

L-dopa acts as a dopamine precursor, carbidopa block adverse effects in the periphery & allows more L-Dopa to be available to the brain

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Side effects of Carbidopa/Levodopa

Hallucinations, confusion, psychosis, nightmares, mood changes, increased aggressiveness, involuntary movements. orthostatic hypotension, N/V, dyskinesias

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Class of Entacapone

COMT inhibitors

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MOA of Entacapone

inhibit COMT, decreasing L-dopa degradation

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Side effects of Entacapone

dyskinesias/dystonia, hallucinations, confusion, psychosis, diarrhea

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Class of Rasagiline

MAO-b inhibitor

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MOA of Rasagiline

Inhibits monoamine oxidase-B which breaks down dopamine

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Side effects of Rasagiline

Dyskinesias, hallucinations, headache, arthralgia, dyspepsia, depression, falls; HTN crisis

Class of Selegiline

MAO-b inhibitor

MOA of Selegiline

Inhibits monoamine oxidase-B which breaks down dopamine

Side effects of Selegiline

dyskinesias, hallucinations, headache, nausea, diarrhea, insomnia, nervousness, orthostasis, confusion; HTN crisis

Class of Pramipexole

Dopamine receptor agonists

MOA of Pramipexole and Ropinirole

dopamine agonist; stimulates dopamine receptors directly in place of dopamine

Indication of Pramipexole and Ropinirole

Parkinson's; Restless Leg Syndrome

Side effects of Pramipexole and Ropinirole and Rotigotine

Impulse Control disorders, nausea, lower extremity edema, orthostasis, hallucinations, sedation, vivid dreaming, sedation

Class of Trihexyphenidyl

Anticholinergics

MOA of Trihexyphenidyl

Muscarinic antagonist

Side effects of Trihexyphenidyl

Anticholinergic effects (mad as a hatter, dry as a bone, red as a beet, blind as a bat)

Indication of Amantadine

Parkinson's

Side effects of Amantadine

insomnia, toxic psychosis, livedo reticularis, DO NOT USE WITH seizures.

Indication for Primidone

Tremors

MOA of primidone

Barbiturate

What drug is used to treat seratonin syndrome?

cyproheptadine

Indication for donepezil

dementia

MOA of Donepezil

cholinesterase inhibitors

Indication for Memantine

Dementia

MOA of Memantine

NMDA antagonist

Name First Generation antipsychotics/neuroleptics

Chlorpromazine, Perphenazine, Haloperidol, Fluphenazine

MOA of 1st gen. antipsychotics

DA receptor antagonism; dopamine blockade

Side effects of 1st gen. antipsychotics

EPS; anticholinergic SE: dry mouth, constipation, blurred vision, urinary retention

Black box warning of Chlorpromazine

cardiovascular disease or seizures

describe potency of chlorpromazine

low potency = ACh>EPS

Indications for Perphenazine

1st gen. antipsychotic, intractable hiccups, nausea, vomiting

Which 1st gen antipsychotics have high potency EPS>AcH

Perphenazine, Haloperidol, Fluphenazine

Name the 2nd gen. antipsychotics

Risperidone, Olanzapine, Aripiprazole, Quetiapine, Ziprasidone, Paliperidone, Iloperidone, Lurasidone, Asenapine, Brexpiprazole, Cariprazine, Clozapine

MOA of 2nd gen. antipsychotics

DA receptor and 5-HT antagonism/partial agonism

Side effects of 2nd gen. antipsychotics

weight gain, metabolic syndrome, DM Type II

What is a side effect of a dopamine blockage drug

hyperprolactinemia, EPS

2nd gen antipsychotic with highest risk of hyperprolactinemia

Risperidone

2nd gen antipsychotic with highest risk of weight gain

Olanzapine

Black box warning for Olanzapine

do not administer within 1 hour of parenteral benzodiazepines

2nd gen antipsychotic with highest risk of akathisia

Aripiprazole

2nd gen antipsychotic with lowest risk of weight gain and metabolic syndrome

Aripiprazole

Black box warning for Aripiprazole

increased risk of suicidal thoughts in pts. <25

name antipsychotic 2nd gen that is approved for irritability, antidepressant, bipolar disorder

Aripiprazole

2nd gen antipsychotic with highest risk of prolonged QTc

Ziprasidone, iloperidone

Which 2nd gen antipsychotic must be consumed with 300kcal

Ziprasidone, Lurasidone

Which 2nd gen antipsychotic requires an EKG

Ziprasidone

Which 2nd gen antipsychotic are also approved for bipolar disorder

Quetiapine, Aripiprazole, Lurasidone, Asenapine

2nd gen antipsychotic with low risk of weight gain

Brexpiprazole, Lurasidone, Ziprasidone, Cariprazine

Side effects of Clozapine

Agranulocytosis, seizures

MOA of 1st gen. antipsychotics

dopamine blockage (D2) causing increase in cAMP inside neurons

General side effects of antipsychotics

Parkinsonian, hyperprolactinemia, amenorrhea, galactorrhea, gynecomastia,

define pyramidal symptoms

corticospinal tract runs in pyramids in medulla --> damage = weakness (no extremity movement)

Define extrapyramidal symptoms

basal ganglia nuclei and associated tracts which do modulation of movement; damage = movement disorders similar to Parkinson's

EPS symptoms

movement side effects 1. dystonia 2. akathisia 3. bradykinesia 4. tardive dyskenia

Define dystonia

involuntary contractions of muscles, spams, stiffness

Define akathisia

restlessness; urge to move around

Define bradykinesia

"drug-induced Parkinsonism"; slow movements

Define tardive dyskensia

Choreoathetosis: mouth, tongue, face, limbs, smacking of lips, grimacing

Define chorea

irregular migrating contractions

Define athetosis

twisting, writhing

Define Neuroleptic Malignant Syndrome

fever, rigid muscles after 1 week on treatment

Treatment for Neuroleptic Malignant Syndrome

Dantrolene, Bromocriptine

Which is a partial 2nd gen antipsychotic agonist

Aripiprazole

Week 5: Pharma Flashcards

(82 cards)