exam 2 Flashcards by Sarah Kuepers

Levodopa

Parkinson’s Disease
Neurological (improvement in bradykinesia, rigidity)

Psychiatric (improvement in mood)

Is metabolized in DA in the brain by AADC

Side Effects: (pretty true for all DA receptor agonists)

Nausea vomiting, orthostatic hypotension

Dyskinesia, fluctuation in motor performance

Hallucinations, paranoia confusion

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Carbidopa

Parkinson’s Disease
Prevents l-dopa from being being metabolized in DA in the periphery

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Entacapone

Parkinson’s Disease
Reduced wearing off and on/off phenomena

Adverse Effects:

Nausea, dyskinesia, orthostatic hypotension, hallucinations

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Selegiline

Parkinson’s Disease
MAO-B inhibitor (keeps from being metabolized into DOPAC)

Used in combination with l-dopa

At low doses does not cause lethal potentiation of catecholamine

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Pramipexole

Parkinson’s Disease
D2 receptor agonist

Used to treat PD

Can cause sudden sleepiness

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Amantadine

Parkinson’s Disease
Antiviral for influenza

Increase DA release and reduce DA uptake, weak glutamate antagonist

Extended release form approved for PD dyskinesia or l-dopa dyskinesia

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Benztropine

Parkinson’s Disease
Antimuscarinic compound (restores balance of DA and ACh)

Modest effect, earliest treatment of PD

CNS effects

sedation , confusion

Peripheral effects

Dry mouth, constipation, tachycardia, and blurred vision

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Haloperidol

Psychosis
Blocks D2 receptors

First generation or “typical” dopamine receptor antagonist

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Risperidone

Psychosis
Second generation or “atypical” serotonin-dopamine antagonist

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Aripiprazole

Psychosis
Second generation or “atypical” serotonin-dopamine antagonist

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Amitriptyline

Depression and Bipolar Disorder
Tricyclic antidepressant

Mechanism of action:

Inhibit reuptake of both serotonin and NE, but ALSO block M1, H1, and alpha-adrenergic receptors

Adverse effects:

Orthostatic hypotension, anticholinergic effects, antihistamine effects, sexual dysfunction, sedation, cardiac toxicity, seizures, dangerous in overdose

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Venlafaxine

Depression and Bipolar Disorder
serotonin/norepinephrine reuptake inhibitor

Mechanism of action:

Block reuptake of serotonin and NE into the presynaptic terminal

Adverse effects:

Serotonin effects

Nausea and vomiting

Sexual dysfunction

Noradrenergic effects

Dry mouth, increase blood pressure and HR, urinary hesitancy, agitation, excessive sweating

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Fluoxetine

Depression and Bipolar Disorder
Selective serotonin reuptake inhibitor

Mechanism of action:

Block reuptake of 5-HT into presynaptic nerve terminal prolonging serotonin neurotransmission

Adverse effects:

Nausea and GI symptoms

Sexual effects, decreased libido, sexual dysfunction

Mild restlessness, headaches, and insomnia

Noted for:

Ease of use, safety in overdose, relative tolerability, cost, broad spectrum of uses

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Sertraline

Depression and Bipolar Disorder
Selective serotonin reuptake inhibitors

Mechanism of action

Block reuptake of 5-HT into presynaptic nerve terminal prolonging serotonin neurotransmission

Adverse effects:

Nausea and GI symptoms

Sexual effects, decreased libido, sexual dysfunction

Mild restlessness, headaches, and insomnia

Noted for:

Ease of use, safety in overdose, relative tolerability, cost, broad spectrum of uses

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Ketamine

Depression and Bipolar Disorder
NMDA antagonists

Dissociative anesthetic that blocks NMDA receptors

Acts rapidly to cause antidepressant action in majority of patients

IM, SC, oral, sublingual, IV

2 weeks after one dose

Side effects:

Transient perceptual disturbances and’or disturbances, increase in MP and pulse , blurred vision, headache, nausea/vomiting and anxiety

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Bupropion

Depression and Bipolar Disorder
Atypical antidepressant

Mechanism of action:

Weakly blocks DA and NE transporters

Has active metabolites

Also used for smoking (wellbutrin/zyban)

Adverse effects:

Dizziness, agitation, tremor, anorexia, potential for seizures at high doses

Lithium

Depression and Bipolar Disorder
Mood stabilizer for bipolar disorder

Mechanism of action:

Enhance serotonin action (increase release and elevate 5-HT)

Reduces catecholamine activity by enhancing reuptake and reducing release

Flattens extremes of emotion in both directions

Therapeutic doses have no psychotropic effects in normal individuals

Not sedative, euphoric, or depressant

Adverse effects:

Metallic taste to food

Therapeutic levels

GI effects, tremors, polyuria, hypothyroidism, teratogenesis

Excessive lithium levels

> 1.5 mEq/L

Low therapeutic index (coma/death)

Zuranolone

Depression and Bipolar Disorder
GABAA positive allosteric modulator

For postpartum depression

Pill taken orally once a day for 14 days and then lasts up to 45

Usually well tolerated

Adverse effects

Drowsiness, sedation, dry mouth, loss of consciousness, hot flushes

Dizziness, vertigo, skin rash, abdominal pain, UTI, anxiety, numbness, muscle twitching or muscle pain

Box warning: impaired ability to drive

Phenobarbital

Sedatives and Anxiolytics
Anticonvulsant

Mechanism of action:

Barbiturate: binds to GABA receptor (PAM)

Increase duration of Cl- channel openings

At high doses can Cl- channel directly

Problems with barbiturates:

P450 can increase metabolism of other drugs

Rapid tolerance to behavioral effects and not respiratory depression

Physical dependence with severe withdrawal

Low margin of safety

Adverse effects

Sedation, drowsiness, impaired concentration, headache

physical and psychological dependence

Respiratory depression

Cardiovascular depression at high doses

activate action of other CNS depressants

Diazepam

Sedatives and Anxiolytics
*longer acting because it has active metabolites
Benzodiazepine

Anticonvulsant, alcohol withdrawal, muscle spasms, preanesthetic

Mechanisms of action:

PAM, bind to site on GABAA

Increase frequency of channel opening with GABA is bound (increase neuronal inhibition)

Adverse effects:

Motor uncoordination

Ataxia

Anterograde amnesia

Paradoxical excitement

Best given at night

Tolerance develops to sedative effects, more rarely to anxiolytic effects

Some risk for dependence

Lorazepam

Sedatives and Anxiolytics
Benzodiazepine

Anxiety, sleep disorders, seizures, alcohol withdrawal, preanesthetic

Mechanisms of action:

PAM, bind to site on GABAA

Increase frequency of channel opening with GABA is bound (increase neuronal inhibition)

Adverse effects:

Motor uncoordination

Ataxia

Anterograde amnesia

Paradoxical excitement

Best given at night

Tolerance develops to sedative effects, more rarely to anxiolytic effects

Some risk for dependence

Midazolam

Sedatives and Anxiolytics
Benzodiazepine

preanesthetic

Mechanisms of action:

PAM, bind to site on GABAA

Increase frequency of channel opening with GABA is bound (increase neuronal inhibition)

Adverse effects:

Motor uncoordination

Ataxia

Anterograde amnesia

Paradoxical excitement

Best given at night

Tolerance develops to sedative effects, more rarely to anxiolytic effects

Some risk for dependence

Zolpidem

Sedatives and Anxiolytics
Z-drug, no anxiolytic effects

(ambien)

Mechanism of action:

GABAA receptors with alpha 1 subunit (important or sedation)

Act at same site as benzodiazepines

Controlled release best for sleep duration

Low-dose used for getting back to sleep

Adverse effects:

Ambien zombies

Risk of abuse and tolerance low when used as directed

Schedule IV drug

Few withdrawal reactions

Ramelteon

Sedatives and Anxiolytics
Melatonin involved in maintaining circadian rhythm underlying sleep-wake cycle

Mechanism of action:

MT1 and MT2 (GCPRs)

Reduces latency of persistent sleep with no effect on sleep stages

No rebound insomnia or withdrawal symptoms

Not a scheduled drug

Buspirone

Sedatives and Anxiolytics Anti-anxiety with limited severity Partial agonist at 5-HT receptors Lacks CNS depressant properties (not sedative hypnotic) Slow onset of action

Nicotine

Drugs of Abuse and Treatments Mechanism of action: Nicotine is an agonist of the nACh receptor nACh receptors, ligand gated ion channels In CNS (allow Na+ and Ca2+) and PNS (allow Na+) PNS Sym: increase HR, BP, NE and E secretions Para: increase stomach acid, intestinal motility Both stimulant and depressant action (alert but relaxed) Tolerance develops to subjective effects Adverse effects: Nausea, dizziness, sweating, heart racing, stomachache, clammy hands Withdrawal Irritability, anxiety, depressed mood, difficulty concentrating, increased appetite or weight gain

Varenicline

Drugs of Abuse and Treatments Chantix Treatment for nicotine addiction Partial agonist at alpha4beta2 nAChR May increase intoxicating effects of alcohol in some patients, may cause seizures

Bupropion

Drugs of Abuse and Treatments Smoking cessation treatment NET and DAT blocker

Alcohol

Drugs of Abuse and Treatments Mechanism of action: Ats on several receptors Focus on GABA A PAM Very low margin of safety Adverse effects of chronic consumption Liver and GI tract Cardiomyopathy, arrhythmias, hypertension Tolerance, physical and psychological dependence Neurological deficits over time, gate disturbances, ataxia Induces increased levels of drug metabolizing enzymes Increase conversion of acetaminophen to toxic metabolite Additive CNS depression Treatment AA, naltrexone, acamprosate, disulfiram

Morphine

Drugs of Abuse and Treatments Mechanism of action: Mu-opioid receptor agonist Acute and chronic pain, preanesthetic medication, acute chest pain associated with MI Adverse effects Respiratory depression, constipation, cough suppression, tolerance, dependence, itching Drug-drug interactions, barb, benzos, alcohol, anesthetics, antidepressants Antidote IV, IM, intranasal naloxone (narcan) or naltrexone

Heroin

Drugs of Abuse and Treatments Mechanism of action: GPCRs coupled to Gi/Go So many opioid receptors and their subtypes determine action Inhibits Ca channels Hyperpolarization Decrease NT release Pain relief Blocks pain signaling in the spinal cord Abused Metabolize to morphine

Codeine

Methadone

Drugs of Abuse and Treatments Agonist Replacement therapy for opioid addiction Long acting, less withdrawal syndrome

Loperamide

Drugs of Abuse and Treatments Anti-diarrheal opioid (imodium) Does not cross BBB at therapeutic doses Inhibits intestinal peristalsis

Buprenorphine

Drugs of Abuse and Treatments Partial agonist, long half-life Replacement therapy for opioid addiction Formulations with naloxone: antagonist

Naltrexone

Drugs of Abuse and Treatments (ReVia) Treatment for alcoholism MOR antagonist, reducing craving Dose-dependent hepatotoxicity Treatment for morphine

Disulfiram

Drugs of Abuse and Treatments Blocks breakdown of alcohol by inhibiting aldehyde dehydrogenase Unpleasant hangover like symptoms