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pharm 310 > exam 2 > Flashcards

exam 2 Flashcards

1
Q

Levodopa

A

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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2
Q

Carbidopa

A

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

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3
Q

Entacapone

A

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

Adverse Effects:

Nausea, dyskinesia, orthostatic hypotension, hallucinations

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4
Q

Selegiline

A

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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5
Q

Pramipexole

A

Parkinson’s Disease
D2 receptor agonist

Used to treat PD

Can cause sudden sleepiness

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6
Q

Amantadine

A

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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7
Q

Benztropine

A

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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8
Q

Haloperidol

A

Psychosis
Blocks D2 receptors

First generation or “typical” dopamine receptor antagonist

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9
Q

Risperidone

A

Psychosis
Second generation or “atypical” serotonin-dopamine antagonist

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10
Q

Aripiprazole

A

Psychosis
Second generation or “atypical” serotonin-dopamine antagonist

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11
Q

Amitriptyline

A

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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12
Q

Venlafaxine

A

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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13
Q

Fluoxetine

A

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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14
Q

Sertraline

A

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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15
Q

Ketamine

A

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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16
Q

Bupropion

A

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

17
Q

Lithium

A

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)

18
Q

Zuranolone

A

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

19
Q

Phenobarbital

A

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

20
Q

Diazepam

A

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

21
Q

Lorazepam

A

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

22
Q

Midazolam

A

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

23
Q

Zolpidem

A

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

24
Q

Ramelteon

A

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

25
Q

Buspirone

A

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

26
Q

Nicotine

A

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

27
Q

Varenicline

A

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

28
Q

Bupropion

A

Drugs of Abuse and Treatments
Smoking cessation treatment

NET and DAT blocker

29
Q

Alcohol

A

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

30
Q

Morphine

A

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

31
Q

Heroin

A

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

32
Q

Codeine

A

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

Cough suppressant with robitussin

Inhibits cough reflex in the medulla

Metabolize to morphine

33
Q

Methadone

A

Drugs of Abuse and Treatments
Agonist

Replacement therapy for opioid addiction

Long acting, less withdrawal syndrome

34
Q

Loperamide

A

Drugs of Abuse and Treatments
Anti-diarrheal opioid

(imodium)

Does not cross BBB at therapeutic doses

Inhibits intestinal peristalsis

35
Q

Buprenorphine

A

Drugs of Abuse and Treatments
Partial agonist, long half-life

Replacement therapy for opioid addiction

Formulations with naloxone: antagonist

36
Q

Naltrexone

A

Drugs of Abuse and Treatments
(ReVia)

Treatment for alcoholism

MOR antagonist, reducing craving

Dose-dependent hepatotoxicity

Treatment for morphine

37
Q

Disulfiram

A

Drugs of Abuse and Treatments
Blocks breakdown of alcohol by inhibiting aldehyde dehydrogenase

Unpleasant hangover like symptoms

pharm 310 (3 decks)

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