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PAPOM > Neuropharm- Comp 2 > Flashcards

Neuropharm- Comp 2 Flashcards

1
Q

Tricyclic Antidepressants

Mechanism of Action (general) and Names of drugs

A

NE, 5-HT reuptake inhibitor

Also muscarinic receptors block, a1 block, H1 block

Imipramine
Amitriptyline
Desipramine
Nortriptyline
Doxepin
Clomiphene
Amoxapine
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2
Q

Tricyclic Antidepressants

Uses (including specific drugs)

A

General: Major depression chronic pain, obsessive- compulsive disorder

  • Imipramine: bed-wetting
  • Desipramine: least anticholinergic
  • Clomipramine: OCD
  • Amitriptyline: Neuropathic pain, migraine
  • Amoxapine: some D2 blockade
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3
Q

Tricyclic Antidepressants

Toxicities

A

Antimuscarinic: mydriasis, cycloplegia, urinary retention, sedation.
Alpha1 block: hypotension, orthostasis.
Histamine1 block: sedation, weight gain

Overdose: coma, convulsion, cardiotoxicity (Respiratory depression, fever, prolonged QT interval)

Treating TCA tox: Sodium bicarbonate attaches to sodium channel to decrease cardiovascular effects

CYP drug interactions; polymorphism a/w slow metabolism of TCAs

Serotonin Syndrome

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4
Q

Bupropion

Mechanism of Action

A
  • Reuptake inhibition of dopamine and norepinephrine.
  • Noncompetitive antagonist at nicotinic receptor (smoking cessation potential)
  • SEPARATE-> Varenicline: partial nicotinic receptor agonist (erratic behavior, suicide). Not related to bupropion mechanism
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5
Q

Bupropion

Use

A
  • Major depression

- Smoking cessation

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6
Q

Bupropion

Toxicities

A

Lowers seizure threshold, caution in bulimic patients.

No sexual dysfunction
Little M, H1 effects

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7
Q

Mirtazapine

Mechanism of Action

A

Alpha2 block to
increase NE and 5-HT release.

Opposite clonidine mechanism

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8
Q

Mirtazapine

Use

A

Major depression

sedation

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9
Q

Mirtazapine

Toxicity

A

Weight gain, sedation

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10
Q

Serotonin-Norepinephrine
Reuptake Inhibitors
(SNRI)

MOA, examples of drugs

A

Inhibits reuptake of 5HT and NE

Duloxetine, Venlafaxine, Desvenlafaxine, Milnacipran

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11
Q

Serotonin-Norepinephrine
Reuptake Inhibitors
(SNRI)

Use

A

Major Depression, chronic pain, fibromyalgia, neuropathic pain

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12
Q

Serotonin-Norepinephrine
Reuptake Inhibitors
(SNRI)

Toxicities

A

Mechanism like tricyclics. No blockade of H1, alpha1, Muscarinic

Overdose: coma, convulsion, cardiotoxicity.

Serotonin Syndrome

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13
Q 
Selective Serotonin
Reuptake Inhibitor (SSRI)

MOA and Examples

A

Inhibits 5HT reuptake
At least 4 weeks for full effect

Fluoxetine
Fluvoxamine
Citalopram
Paroxetine
Sertraline
Escitalopram
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14
Q

SSRIs

Use

A
  • Major depression
  • anxiety
  • panic disorder
  • OCD
  • post- traumatic stress disorder
  • premenstrual dysphoric disorder
  • bulimia
  • social phobias
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15
Q

SSRIs

Toxicities

A

Insomnia, headache
Nausea, vomiting
Bleeding abnormalities (platelets)
Impotence (use phosphodiesterase 5 inhibitor)

Serotonin syndrome

Drug interactions (most w/ fluoxetine CYP450 2D6) –>least with sertraline, citalopram, and escitalopram

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16
Q

Serotonin Syndrome

Symptoms

A

3 As: Increased activity (neuromuscular), Autonomic stimulation, Agitation

Specific symptoms:

  • MYDRIASIS
  • hyperthermia
  • hypertension
  • tachycardia
  • myoclonus
  • tremor
  • delirium
  • confusion
  • within 24 hrs, unlike NMS
  • GI symptoms
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17
Q
  • Trazodone
  • Nefazodone

MOA

A

Serotonin reuptake inhibitor and blocker (SARI); Alpha1 and H1 block

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18
Q
  • Trazodone
  • Nefazodone

Uses

A
  • Major depression
  • Sedation
  • Sleep aid
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19
Q
  • Trazodone
  • Nefazodone

Toxicities

A
  • Alpha1 block (priapism, possible sedation)
  • H1 block (sedation)

Increased levels of trazodone w/ CYP 3A4 inhibitors
- Nefazodone is hepatotoxic

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20
Q

Phenelzine
Tranylcypromine
Isocarboxazid

Mechanisms of Action

A

Monoamine oxidase A inhibitors (prevents breakdown of (NE, Epi, 5-HT, DA, tyramine)

Exception:
Selegiline (MAOIb, prevents dopamine breakdown) –> Tx for Parkinson’s disease

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21
Q

Phenelzine
Tranylcypromine
Isocarboxazid

(MAOIs toxicity)

A
  • Hypertension with tyramine-containing foods or sympathomimetics (cold medicine)
  • Must avoid tyramine foods: Aged cheese and meats, red wine, chocolate, avocado.

Serotonin syndrome (W/ SSRIs, TCAs, meperidine, dextromethorphan, triptans, linezolid, St. John’s Wort)

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22
Q

Lithium

MOA

A

Blocks inosine 5’monophosphatase (Gq), PKC and decreases DAG, IP3 and therefore Ca2+

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23
Q

Lithium

Use

A

Bipolar disorder

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24
Q

Lithium

Toxicity

A
  • Na+ loss promotes Li+ reabsorption (toxicity with diuretics)
  • NSAIDs, ACEI facilitate Li+ reabsorption in PCT
    Amiloride (enhances Li+ excretion)
  • Narrow therapeutic index (1.5 mEq vs. 2mEq)
  • Tremors (use a beta blocker)
  • Leukocytosis
  • Polyuria, polydipsia (Loss of ADH response). Amiloride benefit here.
  • Hypothyroidism
  • Ebstein anomaly, a congenital heart condition (use lamotrigine in pregnancy)
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25
Q

Valproate

MOA

A

Broad-spectrum:

  1. Blocks Na+ channels and T-type calcium channel
  2. Decrease glutamate at NMDA receptors
  3. Increases GABA receptor action
  4. Increases GABA synthesis
  5. Blocks degradation of GABA
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26
Q

Valproate

Use

A

Alternative to lithium in bipolar mania

Tonic-clonic, absence, and partial seizures, migraine prophylaxis

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27
Q

Valproate

Toxicity

A

“Valproate Syndrome” includes spina bifida, neural tube defects, autism.

  • Weight gain
  • Hepatitis
  • Inhibitor of CYP2D6 and 3A4
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28
Q

Carbamazepine

MOA

A

Blocks sodium channels, blocks NE reuptake

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29
Q

Carbamazepine

Use

A

Bipolar disease

Tonic-clonic and partial seizures, trigeminal neuralgia

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30
Q

Carbamazepine

Toxicity

A
  • Drowsiness
  • Ataxia
  • Diplopia
  • SIADH (water “intox”)
  • Aplastic anemia
  • Teratogen (neural tube defects)
  • Stevens-Johnson syndrome (HLA allele in ethnic population).
  • Inducer of CYP 3A4
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31
Q

Lamotrigine

MOA

A

Potentiates GABA, blocks voltage-gated Na+ channels, glutamate blockade

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32
Q

Lamotrigine

Use

A

Manic phase of bipolar syndrome

Partial, tonic-clonic, and absence seizures, Lennox-Gastaut syndrome

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33
Q

Lamotrigine

Toxicity

A

Black Box Warning for Stevens-Johnson syndrome= rash

CNS effects

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34
Q

Atypical Antipsychotics

General Mechanism

A

5-HT2A&raquo_space;>D2; D3 and D4 block

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35
Q

Atypical Antipsychotics

General MOA and ADEs

A
  • Increase DA release to relieve negative symptoms of psychosis (and positive too)
  • Few EPS effects
  • Hyperprolactinemia
  • All prolong QT interval, contraindicated with certain cardiovascular issues
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36
Q

Risperidone

MOA and Use

A

5-HT2A&raquo_space;>D2; D3 and D4 block

  • Atypical antipsychotic, approved for mania
37
Q

Risperidone

Toxicity

A
  • Hypotension from alpha1 blockade.
  • Increase prolactin, hyperlipidemia, hyperglycemia

Palperidone is active metabolite

38
Q

Olanzapine

MOA and Use

A

Blockade of
5-HT2A > H1 > D4 > D2 > α1 > D1

Approved in combination with fluoxetine for mania
Atypical antipsychotic

39
Q

Olanzapine

Toxicity

A
  • Less ANS effects.
  • Fewer extrapyramidal effects (EPS)
  • Weight gain
  • Sedation
    Metabolic changes like risperidone - hyperglycemia, hyperlipidemia
40
Q

Quetiapine

MOA and Use

A

Blockade of
H1 > α1 > M1,3 > D2 > 5-HT2A

D2 blockade, BUT binds for a short time.

  • Atypical antipsychotic, approved for mania
41
Q

Quetiapine

Toxicity

A
  • Minimal muscarinic block
  • H1 (sedation)
  • alpha1 (orthostasis)
42
Q

Aripiprazole

MOA and Use

A
  • Partial D2 agonist
  • 5-HT2A antagonist

Approved for mania, atypical antipsychotic

43
Q

Aripiprazole

Toxicity

A
  • Weight gain

- Akathisia

44
Q

Ziprasidone

MOA and Use

A

Blocks 5-HT and NE reuptake

Atypical antipsychotic, approved for mania

45
Q

Ziprasidone

Toxicity

A

Skin reactions, eosinophilia

46
Q

Chlorpromazine

MOA and use

A

D2» 5HT2 antagonist

  • Typical antipsychotic; treats positive symptoms of psychosis
  • low potency, inexpensive, used most often; phenothiazine
47
Q

Chlorpromazine

Toxicity

A
  • H1 block (sedation), a1 block (orthostasis)
  • M1 block
  • Parkinsonian effects - EPS, dystonias, tardive dyskinesias
  • Deposits in cornea and lens
  • Neuroleptic malignant syndrome
  • Increased prolactin
48
Q

Fluphenazine

MOA and use

A

D2» 5HT2 antagonist, High clinical potency

Typical antipsychotic; A phenothiazine/piperazine

49
Q

Fluphenazine

Toxicity

A

High incidence of tardive dyskinesias, parkinsonian effects

less autonomic toxicities

50
Q

Thiothixene

MOA and use

A

D2» 5HT2 antagonist, clinically most potent antipsychotic

Typical antipsychotic; a thioxanthene

51
Q

Thiothixine

Toxicity

A
  • Mid level tox. of extrapyramidal symptoms
  • Injectable form— less tardive dyskinesias, less upreg of D2 receptors
  • Sedation and hypotension
52
Q

Haloperidol

MOA and use

A

D2» 5HT2 antagonist; very potent antipsychotic

Typical antipsychotic; Also for Tourette’s

A butyrophenone

53
Q

Haloperidol

Toxicities

A

Most severe EPS: parkinsonism, akastheisa, akinesia, dystonias

54
Q

Thioridazine

MOA and use

A 
More 5HT2 antagonist, less D2
low potency (M block)

Typical psychotic

55
Q

Thioridazine

Toxicity

A

-Low eps effects
- ocular toxicity- brown vision from deposits in retina
- cardiotoxic effects: t wave, AV block, arrhythmias
HIGHEST risk of prolonged QT interval
- Na+ channel block

56
Q

Tardive dyskinesias

Characteristics

A
  • Drugs that decrease dopamine release will cause upreg of receptors
  • occurs months to years later
  • tongue protrusion, lip smacking, abnormal mvmts, “ rabbit nose”
  • typically not reversible
  • manage by starting with lowest dose, assess Pt periodically
57
Q

Neuroleptic Malignant Syndrome

Characteristics and Tx

A

Life threatening effect of typical antipsychotics, inhaled anesthetics, and succinylcholine
- occurs weeks to months later, unlike serotonin syndrome

S and S: muscle rigidity, hyperthermia, tachycardia, altered consciousness, rhabdomyolysis.
- CK is elevated syndrome
DECREASED reflexes

Treatment: d/c drug, supportive care, and dantrolene or bromocriptine

  • manage EPS and dystonias with anticholinergics or amantidine
  • manage akasthesia (restlessness) with propranolol
58
Q

Dantrolene

MOA and use

A
  • interferes with release of Ca2+ from sarcoplasmic reticulum via ryanodine receptor bind
  • used IV for NMS, skeletal m. Relaxant, malignant hyperthermia
59
Q

Dantrolene

Toxicity

A

Hepatotoxicity
GI effects
CNS effects

60
Q

Clozapine

MOA and use

A

D4 = a1 > 5HT2a > D2 = D1

Atypical antipsychotic, not approved for mania

61
Q

Clozapine

Toxicity

A
  • Nighttime drooling (paradox, ? M block)
  • Weight gain
  • Agranulocytosis- weekly blood counts for first 6 mo of Tx, every 3 wks after that
  • Hypotension
62
Q

Barbituates
General MOA and Use
- Short acting v. long acting?

A
  • Bind to the Cl- channel and facilitate GABA action (prolong duration of channel opening)
  • open channel in absence of GABA (independent)

Use: anxiety and insomnia (fallen out of use), seizures (phenobarbital), induction of anesthesia (thiopental)

Pentobarbital, Secobarbital- Short acting
Phenobarbital- long acting
Amobarbital, Thiopental - middle

63
Q

Barbituates

Toxicities

A
  • Can induce FULL respiratory effect (b/c GABA independent)- “No ceiling effect”
  • Highly sedative with a hangover effect
  • Tolerance, physical dependence, and withdrawal. Taper slowly!
  • Highly abused (pentobarbital esp., b/c short acting)
  • CYP450 inducers
  • Lipid-soluble (thiopental): redistributed from brain.
  • Elderly/ liver disease may see an increase in t1/2.
64
Q

Benzodiazepines

MOA and General use

A
  • Potentiates GABA by increasing frequency of
    Cl- channel opening
  • Needs GABA to open channel (“Ceiling effect”, safer than barbs)

Use: anxiety, sedative-hypnotic, insomnia, anterograde amnesia, muscle relaxant, anticonvulsant.

65
Q

Benzodiazepines

Use of Specific drugs

A
  • Chlordiazepoxide and Diazepam (long acting drugs): EtOH detoxification.
  • Alprazolam: Panic disorder. Most abused b/c short acting.
  • Lorazepam, Clonazepam, Diazepam: Seizure disorder.
  • Midazolam: anesthesia
  • Estazolam and Flurazepam: insomnia
  • Oxazepam, temezepam, and lorazepam are the safest for the elderly –bypass phase I metabolism (Only undergo glucuronide conjugation, which is ).
  • Flunitrazepam (Rohypnol)- “date rape” drug bc antergograde amnesia
66
Q

Benzodiazepines

Short acting v. Long acting

A
  • Alprazolam (aka Xanax), Oxazepam- short acting
  • Chlordiazepoxide, diazepam (aka valium), flurazepam: metabolites make drug long acting
  • Lorazepam (aka Ativan), Temazepam- intermediate acting
67
Q

Benzodiazepines

Toxicities

A
  • Respiratory depression ONLY when combined with other CNS depressants
  • Drowsiness, hangover
  • Mild euphoria (abuse potential)
  • Anterograde amnesia
  • Physical dependence, can built tolerance
  • Withdrawal: rebound anxiety, insomnia, seizures (esp. with alprazolam)
  • Fetal malformations (hypotonia)
68
Q

Ethanol

MOA and Toxicity

A
  • Potentiates GABA. Euphoria (small doses)
  • Reward center (release of dopamine)
  • Increased norepinephrine release (cardiovascular effects)
  • Zero-order elimination; CYP 2E1 induction- toxic with acetominophen
  • Fetal Alcohol Syndrome (teratogen)
  • Wernicke’s (thiamine deficiency)
  • Loss of liver function; lose glutathione so unable to get rid of Reactive Oxidative Species
  • ? Increased inflammation resulting in malignancy
  • treat abuse with long-acting benzo, naltrexone (opioid blocker), or acamprostate (Glu blocker that increases GABA)
  • Benzo for delirium tremens
69
Q

Flumazenil

MOA and Use

A
  • Antagonist at BDZ binding site at the GABA receptor
  • Blocks actions of benzos and “zz” drugs but not for other sedative-hypnotic drugs.
  • IV increases recovery following BDZ administration in anesthetic procedures.
70
Q

Flumazenil

Toxicities

A

Agitation, confusion, and withdrawal symptoms (in chronic BDZ users)

71
Q

Zolpidem, Eszopiclone, Zaleplon

MOA and Use

A
  • “Zzz” drugs; Ambien aka Zolpidem
  • Benzo-like action on Cl- channels (Binds specific GABAa subunit)
  • Sleep aid; Minor effect on REM sleep
  • Shorter duration of action
  • Less hangover effect and daytime sedation
  • Potentiated by EtOH
72
Q

Zolpidem, Eszopiclone, Zaleplon

Toxicities

A
  • Anterograde amnesia
  • Hallucinations
  • Delusions
  • Impaired judgement
  • Sleepwalking
73
Q

Ramelteon

MOA and Use

A
  • MT-1, MT-2 melatonin receptor agonist
  • Sleep aid; Not addictive (not a controlled substance); No GABA transmission
  • No significant toxicity; Substrate for CYP 1A2
74
Q

Suvorexant

MOA and Use

A
  • Orexin antagonist (blocks orexin normal action, which indicates arousal/wakefullness)
  • Sleep aid/sedative
  • No significant toxicity
75
Q

Amphetamine and Dextroamphetamine

MOA and Use

A
  • CNS stimulation, inhibits reuptake of NE and DA
  • increases release of these catecholamines from nerve terminals

Use: Narcolepsy

76
Q

Amphetamine and Dextroamphetamine

Toxicity

A

Sympathomimetic effects (cardiostimulation/CV, insomnia, weight loss)

77
Q

Methylphenidate, Modafanil

MOA and Use

A
  • Inhibit DA reuptake

- Use: Narcolepsy

78
Q

Methylphenidate, Modafanil

Toxicity

A
  • Less anxiety and anorexia than amphetamines

- Cardiovascular effects

79
Q

Propranolol

MOA and Use

A
  • Beta-1, Beta-2 antagonist
  • Blocks SANS contribution to anxiety
  • “situational anxiety”
80
Q

Propranolol

Toxicity

A
  • CNS depression
  • Fatigue
  • Bradycardia
  • Asthma
  • Hypoglycemia because of B2 blockade
81
Q

Buspirone (Buspar®)

MOA and Use

A
  • 5-HT1 Agonist

- Generalized anxiety; No sedation or addiction

82
Q

Buspirone (Buspar®)

Toxicity

A
  • Headache, dizzy, nervous

- Several weeks (3-4) for full effect

83
Q

Sominex®, Unisom® Tylenol-PM®

MOA and Use

A
  • All have Diphenydramine as an active ingredient

- OTC Sleep aid/sedative

84
Q

Sominex®, Unisom® Tylenol-PM®

Toxicity

A
  • H1 block: orthostasis
  • Lipophilic, cross the blood brain barrier
  • Muscarinic dryness: Dryness, constipation, mydriasis, urinary retention, increase AV and SA node conduction
  • Muscarinic blockade is not indicated in BPH and glaucoma.
85
Q

Disulfiram

Use

A
  • Inhibits aldehyde dehydrogenase
  • Anti-EtOH abuse
  • CANNOT use with alcohol
86
Q

Clonidine

MOA and Use

A
  • Alpha 2 agonist

- Reduce sympathetic NS effects following EtOH, opioid, and nicotine withdrawal

87
Q

Treatment of stimulant overdose

A
  • Acidify urine

- Supportive therapy (lorazepam and haloperidol)

88
Q

Typical Antipsychotic Toxicities

A
  • M, H1, alpha1 blockade
  • EPS (dystonia, pseudoparkinsonism)
  • Akathisia
  • Menstrual irregularities (prolactin
    release)
  • Tardive dyskinesia
  • Neuroleptic malignant syndrome
89
Q

Hypertensive crisis symptoms

A 
Occipital headache
Stiff neck
Nausea/vomiting
Photophobia 
Palpitations

Due to drug interaction with tyramine and MAOI-A

PAPOM (3 decks)

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