Unit 3-CNS 1 and II Flashcards
Levodopa
Drug Class
Dopamine precursor
Levodopa
Mechanism
Crosses BBB and is converted to dopamine->improves nigrostriatal functioning
Levodopa
Uses
Given with carbidopa (as Sinemet); first-line treatment for Parkinson’s unless patient is young (want to delay as long as possible)
Levodopa
Side Effects
- Dyskinesias; hypotension, nausea, anxiety, fatigue
- Psychoses if dosed too high
- MAO-A inhibitors are contraindicated (except MAO-B, which only hits DA)
Carbidopa
Drug class
Aromatic amino acid decarboxylase inhibitor
Carbidopa
Mechanism
Inhibits peripheral conversion of L-DOPA to dopamine; does not cross BBB
Carbidopa
Uses
Parkinson’s (given with Levadopa to lower side effects)
Carbidopa
Side effects
Dyskinesias, on-off phenomenon,
MAO-A inhibitors are contraindicated (except MAO-B, which only hits DA)
Bupropion
Drug class
Norepinephrine-dopamine reuptake inhibitor (NDRI)
Bupropion
Mechanism
Blocks dopamine transporter (DAT) -> increased dopamine in synapse
Bupropion
Uses
Parkinson’s
Bupropion
Side effects
Insomnia, anxiety, agitation, nausea, dry mouth, sweating, palpitations
Mild increase in BP
Side effects due to increase in NE (drug acts to block reuptake of both NE and DA)
dextroamphetamine; lisdexamfetamine
Drug class
Stimulants
dextroamphetamine; lisdexamfetamine
Mechanism
- Blocks dopamine transporter (DAT) to block reuptake
- also increases VMAT2 to cause more DA to be ejected from nerve terminal
dextroamphetamine; lisdexamfetamine
Uses
ADHD
dextroamphetamine; lisdexamfetamine
Side effects
Norepi (sympathetic) and dopamine side effects; weight loss; addictive
Psychosis at high doses
Modafinil; Armodafinil
Drug Class
Stimulant
Modafinil; Armodafinil
Mechanism
- Increases histamine activity in the tuberomammilary nucleus–> activates alertness in frontal cortex
- may increase orexin activity
- may block DAT
Modafinil; Armodafinil
Uses
Fatigue due to narcolepsy, apnea, shiftwork (but not ADHD)
Modafinil; Armodafinil
Side effects
- Similar to, but less severe, than amphetamines (ie NE and DA effects)
- Addiction (b/c inncreases DA in mesolimbic pathway ie reward center)
- appetite and weight loss
- psychosis at very high doses
- Can lower birth control effectiveness (use same P450-3A4 enzymes)
Selegiline
Drug class
MAO-B inhibitor
Selegiline
Mechanism
Prevents breakdown of DA
Selegiline
Uses
- Early Parkinson’s (low dose: inhibits MAO-B
- depression (high dose: inhibits MAO-A and B)
- For depression it comes in a patch called EMSAM
Selegiline
Side effects
Hypotension, dizziness, insomnia, weight gain
Nausea, vomiting
Rasagiline
Drug Class
MAO-B inhibitor
Rasagiline
Mechanism
Prevents breakdown of DA
Rasagiline
Uses
Early Parkinson’s
Rasagiline
Side effects
Hypotension, dizziness, insomnia, weight gain
Nausea, vomiting
Tranylcypromine (Parnate); Isocarboxazid (Marplan); Phenelzine (Nardil)
Drug class
MAOI
Tranylcypromine (Parnate); Isocarboxazid (Marplan); Phenelzine (Nardil)
Mechanism
Irreversibly inhibit both MAO-A and MAO-B
Tranylcypromine (Parnate); Isocarboxazid (Marplan); Phenelzine (Nardil)
Uses
Depression
Tranylcypromine (Parnate); Isocarboxazid (Marplan); Phenelzine (Nardil)
Side effects
Hypotension, dizziness, insomnia, weight gain
Hypertensive crisis (with tyramine-rich foods–> increased NE);
serotonin syndrome (MAOI + SSRI)
Interactions with drugs that increase NE and serotonin b/c of its action on MAO-A
Entacapone
Drug class
COMT inhibitor
Entacapone
Mechanism
Prevents breakdown of DA
Short-acting (2 hours)
Entacapone
Uses
Parkinson’s
Entacapone
Side effects
Nausea, fatigue
DA side effects
Tolcapone
Drug class
COMT inhibitor
Tolcapone
Mechanism
Prevents breakdown of DA
Tolcapone
Uses
Parkinson’s
Use only if Entacapone fails
Tolcapone
Side effects
Nausea, fatigue; liver failure
Bromocriptine
Drug class
Ergot D2 receptor agonist
Bromocriptine
Mechanism
Increases DA activity via D2 receptor agonism
Bromocriptine
Uses
Mild Parkinson’s; Restless Legs Syndrome; hyperprolactinemia
Bromocriptine
Side effects
Mania, nausea, dizziness, fatigue
Peripheral DA-like effects
Must be titrated slowly due to hypotension
Pramipexole
Drug class
Selective D2 receptor agonist
Pramipexole
Mechanism
Increases DA activity via D2 receptor agonism
Pramipexole
Uses
Mild Parkinson’s; Restless Legs Syndrome
Less effective with motor symptoms of PD
Pramipexole
Side effects
Mania, nausea, dizziness, fatigue
Peripheral DA-like effects