MNI Antidepressants Antipsychotics Anxiolytics Hypnotics Antiepileptics Parkinsons Flashcards

1
Q

Isocarboxazid

A

MAOI; Antidepressant

Hydrazine derivative

AE: Drowsiness, Insomnia, Nausea, Ortho hypotension, weight gain, muscle pain, sex dysfunction. Serotonin Syndrome in combination with 5-HT agent. Cheese reaction in presence of tyramine containing food.

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2
Q

Phenelzine

A

MAOI; Antidepressant

Hydrazine derivative

AE: Drowsiness, Insomnia, Nausea, Ortho hypotension, weight gain, muscle pain, sex dysfunction. Serotonin Syndrome in combination with 5-HT agent. Cheese reaction in presence of tyramine containing food.

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3
Q

Tranylcypromine

A

MAOI; Antidepressant

Non-hydrazine

AE: Drowsiness, Insomnia, Nausea, Ortho hypotension, weight gain, muscle pain, sex dysfunction. Serotonin Syndrome in combination with 5-HT agent. Cheese reaction in presence of tyramine containing food.

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4
Q

Selegiline

A

MAOI; Antidepressant; Parkinson’s Medication

Non-hydrazine.

Parkinson’s Disease: Selective & irreversible MAO-B inhibition= selectively reduces dopamine breakdown in the brain. Used as adjunct to Levodopa.

AE: Drowsiness, Insomnia (is metabolized to amphetamine & methamphetamine), Nausea, Ortho hypotension, weight gain, muscle pain, sex dysfunction. Serotonin Syndrome in combination with 5-HT agent.

Transdermal formulation- Unlikely to cause Cheese Reaction

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5
Q

Cyproheptadine

A

5-HT Antagonist

Used to manage Serotonin Syndrome

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6
Q

Pseudoephedrine

A

alpha agonist

Contraindicated in patients taking MAOI

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7
Q

Phenylpropanolamine

A

alpha agonist

Contraindicated in patients taking MAOI

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8
Q

Amitriptyline

A

Tricyclic Antidepressant

Blocks SERT, NET, a-adrenergics, Muscarinics, Histamine, Cardiac Fast Na Channels

AE: Ortho hypotension, reflex tachy (a-blockade). Blurred vision, xerostomia, urinary retention, constipation, aggravation of glaucoma (M-blockade). Sedation, Weight-Gain (H-blockade). Fatal arrhythmias (Cardiac Na blockade)

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9
Q

Clomipramine

A

Tricyclic Antidepressant

Blocks SERT (more selective!), NET, a-adrenergics, Muscarinics, Histamine, Cardiac Fast Na Channels

AE: Ortho hypotension, reflex tachy (a-blockade). Blurred vision, xerostomia, urinary retention, constipation, aggravation of glaucoma (M-blockade). Sedation, Weight-Gain (H-blockade). Fatal arrhythmias (Cardiac Na blockade)

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10
Q

Desipramine

A

Tricyclic Antidepressant

Blocks SERT, NET (more selective!), a-adrenergics, Muscarinics, Histamine, Cardiac Fast Na Channels

AE: Ortho hypotension, reflex tachy (a-blockade). Blurred vision, xerostomia, urinary retention, constipation, aggravation of glaucoma (M-blockade). Sedation, Weight-Gain (H-blockade). Fatal arrhythmias (Cardiac Na blockade)

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11
Q

Imipramine

A

Tricyclic Antidepressant

Blocks SERT, NET, a-adrenergics, Muscarinics, Histamine, Cardiac Fast Na Channels

AE: Ortho hypotension, reflex tachy (a-blockade). Blurred vision, xerostomia, urinary retention, constipation, aggravation of glaucoma (M-blockade). Sedation, Weight-Gain (H-blockade). Fatal arrhythmias (Cardiac Na blockade)

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12
Q

Nortriptyline

A

Tricyclic Antidepressant

Blocks SERT, NET (more selective!), a-adrenergics, Muscarinics, Histamine, Cardiac Fast Na Channels

AE: Ortho hypotension, reflex tachy (a-blockade). Blurred vision, xerostomia, urinary retention, constipation, aggravation of glaucoma (M-blockade). Sedation, Weight-Gain (H-blockade). Fatal arrhythmias (Cardiac Na blockade)

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13
Q

Sodium Bicarbonate

A

Reverse conduction block in TCA induced arrhythmia

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14
Q

Citalopram

A

SSRI Antidepressant

Block SERT (5-HT reuptake).

AE: Nausea, GI Upset, Diarrhea, sex dysfunction, weight gain. Serotonin Syndrome possible.

Low potential for interactions.

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15
Q

Escitalopram

A

SSRI Antidepressant

Block SERT (5-HT reuptake).

AE: Nausea, GI Upset, Diarrhea, sex dysfunction, weight gain. Serotonin Syndrome possible.

Low potential for interactions.

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16
Q

Sertaline

A

SSRI Antidepressant

Block SERT (5-HT reuptake).

AE: Nausea, GI Upset, Diarrhea, sex dysfunction, weight gain. Serotonin Syndrome possible.

Low potential for interactions.

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17
Q

Fluoxetine

A

SSRI Antidepressant

Block SERT (5-HT reuptake).

AE: Nausea, GI Upset, Diarrhea, sex dysfunction, weight gain. Serotonin Syndrome possible.

Blocks CYP2D6, high interaction potential.

Longer half-life, less likely to have discontinuation syndrome.

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18
Q

Paroxetine

A

SSRI Antidepressant

Block SERT (5-HT reuptake).

AE: Nausea, GI Upset, Diarrhea, sex dysfunction, weight gain. Serotonin Syndrome possible.

Blocks CYP2D6, high interaction potential.

Short half-life, more likely to have discontinuation syndrome.

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19
Q

Fluvoxamine

A

SSRI Antidepressant

Block SERT (5-HT reuptake).

AE: Nausea, GI Upset, Diarrhea, sex dysfunction, weight gain. Serotonin Syndrome possible.

Blocks CYP1A2 CYP2C19 CYP3A4; high interaction potential.

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20
Q

Nefazodone

A

SARI Antidepressant

Block SERT (5HT reuptake) (weakly). Also 5HT2 antagonists (potent).

Hepatotoxic, no longer commonly prescribed.

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21
Q

Trazodone

A

SARI Antidepressant

Block SERT (5HT reuptake) (weakly). Also 5HT2 antagonists (potent).

Also H1 and a1 blockage. Extremely sedating (main use is hypnotic), and causes priapism.

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22
Q

Venlafaxine

A

SNRI Antidepressant

Blocks SERT and NET (5-HT and NEpi reuptake)

Potent SERT blocker, needs higher doses to block NET, also inhibits dopamine reuptake weakly.

Fewer CYP450 interactions than SSRI.

Short half-life, discontinuation syndrome more likely.

Used for patients where SSRIs were not effective. Also, Chronic Pain.

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23
Q

Duloxetine

A

SNRI Antidepressant

Blocks SERT and NET (5-HT and NEpi reuptake) at all doses.

Fewer CYP450 interactions than SSRI.

Used for patients where SSRIs were not effective. Also, Chronic Pain.

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24
Q

Bupropion

A

NDRI Antidepressant

Inhibits NEpi & Dopamine reuptake. Increases release of both.

AE: Seizures. No sexual dysfunction.

Less effective for anxiety than other Antidepressants. Approved for smoking cessation.

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25
Q

Mirtazapine

A

NASSA Antidepressants

Antagonist at central presynaptic A2 receptors. Increases NEpi & 5-HT release.

Antagonist at 5-HT2 and 5-HT3 receptors.

Antagonist at H1: Sedation & Weight gain.

Useful if pt has prominent insomnia or agitation.

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26
Q

Lithium

A

Mood stabilizer

Depletes inositol, causing uncompetitive inhibition of active Gq receptors.

AE: Tremor, sedation, ataxia, aphasia, seizures, weight gain, hypothyroidism, nephrogenic diabetes insipidus, edema, dermatitis, alopecia, leukocytosis.

Category D in pregnancy.

Must monitor serum lithium, thyroid funct, renal funct.

Clearance of Li reduced by Thiazides, NSAIDs, ACEis, ARBs.

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27
Q

Valproate

A

Antiepileptic

Blocks Nav channels and T-type Ca channels and other unknown molecular receptors.

DOC in absence seizures, atypical absence seizures, myoclonic seizures & atonic seizures. Used focal & generalized tonic-clonic seizures. Alternative to Lithium in bipolar. Manage Migraine.

CYP 450 inhibitor (inhibits its own metabolism)

AE: Hepatotoxic, most teratogenic anti-epileptic (folic acid can reduce risk).

Monitor Liver function & CBC

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28
Q

Chlorpromazine

A

Classical Antipsychotic

Low-potency anti-D2. Strong anticholinergic activity. Less likely to produce EPR. More likely to produce sedation & postural hypotension.

AE: Can cause corneal & lens deposits!. Medium Risk for weight gain.

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29
Q

Thioridazine

A

Classical Antipsychotic

Low-potency anti-D2 Strong anticholinergic activity. Less likely to produce EPR. More likely to produce sedation & postural hypotension.

No anti-emetic effects.

AE: Cardiotoxic, can cause retinal deposits!

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30
Q

Haloperidol

A

Classical Antipsychotic

High potency anti-D2. High risk of EPR.

Low risk of metabolic effects.

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31
Q

Fluphenazine

A

Classical Antipsychotic.

High potency anti-D2. High risk of EPR.

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32
Q

Clozapine

A

Atypical Antipsychotic (prototype)

High affinity for D1, D4, 5HT2, Muscarinic and alpha adrenergic blocking. Also D2 blocker.

Least likely to produce EPR. Recommended antipsychotic for pt with tardive dyskinesia.

AE: Agranulocytosis! Largest risk of metabolic dysregulation. Cat B pregnancy!

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33
Q

Risperidone

A

Atypical Antipsychotic

Higher blocking of 5HT2 than D2.

Risk of EPR. Medium risk of metabolic effects.

Approved to treat acute mania or mixed episodes.

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34
Q

Olanzapine

A

Atypical Antipsychotic

Largest risk of metabolic dysregulation.

Approved for maintenance of bipolar disorder. Approved for treating bipolar depression in combination with fluoxetine.

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35
Q

Quetiapine

A

Atypical Antipsychotic

Lowest risk of EPR. Medium risk of metabolic dysregulation.

Approved to treat acute mania or mixed episodes.

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36
Q

Aripiprazole

A

Atypical Antipsychotic

Partial agonist at D2 and 5HT1A receptors. Antagonist at 5HT2A receptors.

No Anti-emetic effects. Lowest risk of metabolic dysregulation. Most prescribed antipsychotic in the states. Approved for maintenance treatment of bipolar.

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37
Q

Pimavanserin

A

Atypical Antipsychotic

Purely a 5HT2A inverse agonist

Approved for the treatment of Parkinson’s Disease psychosis!

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38
Q

Prochlorperazine

A

Antipsychotic

Also used to treat N/V

39
Q

Droperidol

A

Antipsychotic

Also used to treat N/V and to induce neurolept-anesthesia (in combination with fentanyl)

40
Q

Chlordiazepoxide

A

Benzodiazepine; Long-Acting

Metabolized to Desmethylchlordiazepoxide, Demoxepam, Desmethyldiazepam, Oxazepam

Used for management of EtOH withdrawal (no cirrhosis)

AE: Drowsiness & Confusion, Ataxia, Cognitive Impairment, Paradoxical Anxiety Anger & Depression, Dependence, Withdrawal.

41
Q

Clonazepam

A

Benzodiazepine; Long-Acting

Used to treat anxiety, some types of epileptic seizures

AE: Drowsiness & Confusion, Ataxia, Cognitive Impairment, Paradoxical Anxiety Anger & Depression, Dependence, Withdrawal.

42
Q

Diazepam

A

Benzodiazepine; Long-Acting

Metabolized to Desmethyldiazepam & Oxazepam

Used to treat anxiety, muscle spasms, status epilepticus, EtOH withdrawal (no cirrhosis)

43
Q

Flurazepam

A

Benzodiazepine; Long-Acting

Metabolized to hydroxyethyl-flurazepam & desalkyl-flurazepam, which have super long half-lives.

AE: Drowsiness & Confusion, Ataxia, Cognitive Impairment, Paradoxical Anxiety Anger & Depression, Dependence, Withdrawal.

44
Q

Alprazolam

A

Benzodiazepine; Intermediate-Acting

Used to treat anxiety

AE: Drowsiness & Confusion, Ataxia, Cognitive Impairment, Paradoxical Anxiety Anger & Depression, Dependence, Withdrawal.

45
Q

Lorazepam

A

Benzodiazepine; Intermediate-Acting

Conjugated directly, not by P450 system.

Used to treat anxiety, status epilepticus, EtOH withdrawal with cirrhosis or alcoholic hepatitis.

AE: Drowsiness & Confusion, Ataxia, Cognitive Impairment, Paradoxical Anxiety Anger & Depression, Dependence, Withdrawal.

46
Q

Oxazepam

A

Benzodiazepine; Intermediate-Acting

Medication but also metabolite of some long-acting benzos.

Conjugated directly, not by P450 system.

Used to treat EtOH withdrawal with cirrhosis or alcoholic hepatitis.

AE: Drowsiness & Confusion, Ataxia, Cognitive Impairment, Paradoxical Anxiety Anger & Depression, Dependence, Withdrawal.

47
Q

Temazepam

A

Benzodiazepine; Intermediate-Acting

Conjugated directly, not by P450 system.

Used to treat sleep disorders.

AE: Drowsiness & Confusion, Ataxia, Cognitive Impairment, Paradoxical Anxiety Anger & Depression, Dependence, Withdrawal.

48
Q

Midazolam

A

Benzodiazepine; Short-Acting

Used to treat status epilepticus.

AE: Drowsiness & Confusion, Ataxia, Cognitive Impairment, Paradoxical Anxiety Anger & Depression, Dependence, Withdrawal.

49
Q

Triazolam

A

Benzodiazepine; Short-Acting

Used to treat sleep disorders.

AE: Drowsiness & Confusion, Ataxia, Cognitive Impairment, Paradoxical Anxiety Anger & Depression, Dependence, Withdrawal.

50
Q

Flumazenil

A

Benzodiazepine receptor antagonist

Blocks benzos and Z-Drugs

Used to reverse CNS depressant effects of benzo OD. Used to hasten recovery following the use of benzos in anesthetic or diagnostic procedures.

Rapid onset, short half-life. May require frequent administration.

AE: Precipitate benzo withdrawal in benzo-dependent patients. Cause seizures in patients using benzos to control seizures.

51
Q

Thiopental

A

Barbiturate; Ultra short-acting

Used to induce IV anesthesia & manage status epilepticus.

GABAa receptor positive allosteric modulator, increases duration* of channel opening. At high concentrations directly activates Cl channels, blocks Glu receptors, inhibits Nav and Cav channels.

CYP450 inducers. Produce sedation, hypnosis, anesthesia, coma, respiratory depression, death with increasing dose.

52
Q

Phenobarbital

A

Barbiturate

Used in management of tonic-clonic seizures & status epilepticus. Also manage drug induced seizures in non-epileptic patients.

GABAa receptor positive allosteric modulator, increases duration* of channel opening. At high concentrations directly activates Cl channels, blocks Glut receptors, inhibits Nav and Cav channels.

CYP450 inducer.

AE: Produce sedation, hypnosis, anesthesia, coma, respiratory depression, death with increasing dose. Rash, SJ syndrome.

53
Q

Pentobarbital

A

Barbiturate

Used in management of status epilepticus.

GABAa receptor positive allosteric modulator, increases duration* of channel opening. At high concentrations directly activates Cl channels, blocks Glu receptors, inhibits Nav and Cav channels.

CYP450 inducers. Produce sedation, hypnosis, anesthesia, coma, respiratory depression, death with increasing dose.

54
Q

Zolpidem

A

Z-Drug

Short duration of action.

Used for short-term insomnia treatment due to difficulty initiating sleep.

Extended-release: Intermediate duration of action

Used for treatment of insomnia due to difficulty with sleep onset or maintenance.

55
Q

Zalepon

A

Z-Drug

Ultrashort duration of action.

Short-term treatment of insomnia

56
Q

Eszopiclone

A

Z-Drug

Intermediate duration of action.

Treatment of insomnia.

57
Q

Buspirone

A

5-HT1A partial agonist. Pure anxiolytic.

No impairment, drug interactions, withdrawal, dependence, rebound anxiety. 2-3 week onset.

2nd-line for GAD due to inconsistent efficacy data.

58
Q

Ramelteon

A

Melatonin Receptor Agonist

Agonist at MT1 and MT2 receptors.

Treatment of insomnia characterized by difficulty with sleep onset. Minimal abuse potential, can be used long-term.

AE: Dizziness, somnolence, fatigue, endocrine changes, decreased testosterone, inc in prolactin.

59
Q

Suvorexant

A

Dual antagonist at orexin 1 and 2 receptor.

Indicated for treatment of insomnia due to poor sleep onset or maintenance.

AE: Daytime somnolence, worsening depression or suicidal ideation.

CI: Narcolepsy.

60
Q

Lemborexant

A

Dual antagonist at orexin 1 and 2 receptor.

Indicated for treatment of insomnia due to poor sleep onset or maintenance.

AE: Daytime somnolence, worsening depression or suicidal ideation.

CI: Narcolepsy.

61
Q

Propranolol

A

b-blocker

Reduces autonomic symptoms due to phobias. Used to control performance anxiety.

62
Q

Doxepin

A

TCA antidepressant used as a hypnotic.

Highly antagonistic at H1 receptors and no anti-cholinergic effects at therapeutic doses as a hypnotic.

Used to treat insomnia due to difficulty with sleep maintenance.

63
Q

Hydroxyzine

A

Antihistamine with antiemetic activity

Approved for symptomatic relief of anxiety

64
Q

Diphenydramine

A

OTC antihistamine

Useful for treating mild types of insomnia

65
Q

Doxylamine

A

OTC antihistamine

Useful for treating mild types of insomnia

66
Q

Phenytoin

A

Anti-epileptic

Principally blocks Nav channels.

Used principally for Tonic Clonic seizures

CYP450 inducer. Zero-order elimination kinetics.

AE: Diplopia, ataxia, gingival hyperplasia, hirsutism, Rash & SJ syndrome!!!

67
Q

Carbamazepine

A

Anti-epileptic

Principally blocks Nav channels

Used principally for Tonic Clonic seizures. Also used for bipolar disorder as Lithium alternative

CYP450 inducer

AE: Aplastic anemia, agranulocytosis (monitor CBC), Rash & SJ syndrome!!!

68
Q

Lamotrigine

A

Anti-epileptic

Principally blocks Nav channels.

Used for Tonic Clonic seizures. Can be used for absence seizures but not FDA approved for this. Used for atonic seizures. Can also be used for Bipolar.

AE: Rash & SJ syndrome!!!

69
Q

Zonisamide

A

Anti-epileptic

Principally blocks Nav channels & other unknown targets.

Used for focal & generalized seizures.

70
Q

Topiramate

A

Anti-epileptic

Blocks Nav channels, enhances or activates GABAa receptor, blocks Glut receptors.

Used in focal & general tonic-clonic seizures, and migraines.

71
Q

Ethosuximide

A

Anti-epileptic

Blocks T-type Ca channels.

DOC in absence seizures.

72
Q

Tiagabine

A

Anti-epileptic

GABA reuptake inhibitor

73
Q

Vigabatrin

A

Anti-epileptic

GABA aminotransferase inhibitor (inhibits GABA breakdown)

AE: Visual field loss

74
Q

Gabapentin

A

Anti-epileptic

Blocks presynaptic Cav channels, and decreases glutamate release.

Used in neuropathic pain.

75
Q

Pregabalin

A

Anti-epileptic

Blocks presynaptic Cav channels, and decreases glutamate release.

Used in neuropathic pain.

76
Q

Levetiracetam

A

Anti-epileptic

Binds synaptic vesicle glycoprotein 2A (SV2A). Affects release of Glut & GABA.

Used in focal & generalized tonic-clonic seizures. Adjunct therapy in Myoclonic Seizures. 2nd phase therapy in Status Epilepticus.

77
Q

Cannabidiol (CBD)

A

Used in treatment of seizures associated with Dravet syndrome, Lennox-Gastaut syndrome, tuberous sclerosis.

78
Q

Felbamate

A

Anti-epileptic

Unknown mechanism

Used for refractory epilepsy

AE: Aplastic anemia, Hepatotoxicity.

79
Q

Primidone

A

Barbiturate

Precursor of phenobarbital (Primidone metabolized to phenobarbital)

Similar uses & adverse effects to phenobarbital.

First-line for essential tremor.

80
Q

Levodopa

A

Dopamine Precursor

Provides symptomatic relief for Parkinson’s patients. Crosses BBB and is converted by DOPA decarboxylase to Dopamine.

Taken without protein-rich meal, amino acids compete for absorption from SI.

AE: Anorexia, N/V, Tachycardia, Arrhythmias, Hypotension due to peripheral decarboxylation.

CNS AE: Visual & Auditory hallucinations, Dysknesias, Mood changes, depression, anxiety, agitation, insomnia.

CI: Patients with psychosis or on anti-psychotic drugs, angle closure-glaucoma, peptic ulcer disease, cardiac problems, coadministration of non-specific MAO inhibitors, antihypertensive medications.

81
Q

Carbidopa

A

DOPA Decarboxylase Inhibitor

Prevents conversion of Levodopa to Dopamine. Doesn’t cross BBB, acts only peripherally. Reduces peripheral AE of Levodopa and reduces dose necessary for effects since more LDOPA gets to the brain.

82
Q

Sinemet

A

Preparation of Carbidopa & Levodopa in fixed proportion.

83
Q

Bromocriptine

A

Dopamine Agonist (Ergot)

D2 Agonist

Widely used to treat Parkinson’s in the past. Superseded by newer Dopamine Agonists.

AE: AE: Anorexia, N/V, constipation, dyspepsia, peptic ulcer bleeding, postural hypotension, arrhythmias, peripheral edema, dyskinesias. Mental: Confusion, hallucinations, delusions, compulsive behaviors (impulse control disorder).

Ergot-specific AE: Painless digital vasospasm, pulmonary infiltrates, pleural & retroperitoneal fibrosis, erythromelalgia.

CI: Hx of psychotic illness, use of antipsychotic drugs (reduce efficacy of dopamine agonists), coadministration of CNS depressants (inc risk of somnolence & confusion), Hx of recent MI, Hx of active Peptic Ulcer.

84
Q

Pramipexole

A

Dopamine Agonist (NonErgot)

Less effective than Levodopa at treating motor symptoms of PD. Less likely to cause motor fluctuations or dyskinesia.

AE: Anorexia, N/V, constipation, dyspepsia, peptic ulcer bleeding, postural hypotension, arrhythmias, peripheral edema, dyskinesias. Mental: Confusion, hallucinations, delusions, compulsive behaviors (impulse control disorder). Uncontrollable somnolence!

CI: Hx of psychotic illness, use of antipsychotic drugs (reduce efficacy of dopamine agonists), coadministration of CNS depressants (inc risk of somnolence & confusion), Hx of recent MI, Hx of active Peptic Ulcer.

85
Q

Ropinirole

A

Dopamine Agonist (NonErgot)

Less effective than Levodopa at treating motor symptoms of PD. Less likely to cause motor fluctuations or dyskinesia.

AE: Anorexia, N/V, constipation, dyspepsia, peptic ulcer bleeding, postural hypotension, arrhythmias, peripheral edema, dyskinesias. Mental: Confusion, hallucinations, delusions, compulsive behaviors (impulse control disorder). Uncontrollable somnolence!

CI: Hx of psychotic illness, use of antipsychotic drugs (reduce efficacy of dopamine agonists), coadministration of CNS depressants (inc risk of somnolence & confusion), Hx of recent MI, Hx of active Peptic Ulcer.

86
Q

Rotigotine

A

Dopamine Agonist (NonErgot)

Available in a transdermal formulation, once-daily use.

Less effective than Levodopa at treating motor symptoms of PD. Less likely to cause motor fluctuations or dyskinesia.

AE: Anorexia, N/V, constipation, dyspepsia, peptic ulcer bleeding, postural hypotension, arrhythmias, peripheral edema, dyskinesias. Mental: Confusion, hallucinations, delusions, compulsive behaviors (impulse control disorder). Uncontrollable somnolence!

CI: Hx of psychotic illness, use of antipsychotic drugs (reduce efficacy of dopamine agonists), coadministration of CNS depressants (inc risk of somnolence & confusion), Hx of recent MI, Hx of active Peptic Ulcer.

87
Q

Apomorphine

A

Dopamine Agonist (NonErgot)

Used as a rescue therapy for “off” episodes of “On-Off” fluctuations seen in Levodopa.

Pretreatment with antiemetic (trimethobenzamide) recommended.

AE: QT prolongation, dyskinesia, drowsiness, sweating, hypotension.

88
Q

Rasagiline

A

MAO inhibitor.

Selectively irreversibly inhibits MAO-B. Used as Parkinson’s therapy, adjunct to Levodopa.

89
Q

Tolcapone

A

COMT inhibitor. Parkinson’s disease therapy.

Reduces breakdown of Levodopa to 3-O-methyldopa in both CNS and peripheral tissue.

Increases bioavailability of Levodopa and counters compensatory COMT upregulation in Carbidopa usage.

AE: Fulminating Hepatic Necrosis

90
Q

Entacapone

A

COMT inhibitor. Parkinson’s disease therapy.

Reduces breakdown of Levodopa to 3-O-methyldopa in peripheral tissue.

Increases bioavailability of Levodopa and counters compensatory COMT upregulation in Carbidopa usage.

Preferred to tolcapone due to not being hepatotoxic.

91
Q

Amantadine

A

Antiviral Drug used as Parkinson’s therapy

MOA for PD is unknown. Effects modest.

May increase Dopamine release & inhibit reuptake. Also an NMDA receptor antagonist, potential antidyskinetic effect.

AE: Restlessness, agitation, confusion, hallucinations, acute toxic psychosis (at high doses), peripheral edema, headache, heart failure, orthostatic hypotension, dry mouth, urinary retention, GI disturbances, Livedo Reticularis (self resolving within a month)

CI: Use with caution in pt with Hx of seizures of heart failure.

92
Q

Benztropine

A

Antimuscarinic

Adjuvant Parkinson’s Therapy

May improve tremor, drooling & rigidity. Little effect on bradykinesia.

AE: Mood changes, xerostomia, pupillary dilation, confusion, hallucinations, urinary retention.

CI: Glaucoma, prostatic hypertrophy, pyloric stenosis.

93
Q

Trihexyphenidyl

A

Antimuscarinic

Adjuvant Parkinson’s Therapy

May improve tremor, drooling & rigidity. Little effect on bradykinesia.

AE: Mood changes, xerostomia, pupillary dilation, confusion, hallucinations, urinary retention.

CI: Glaucoma, prostatic hypertrophy, pyloric stenosis.