specific drugs Flashcards

1
Q

alprazolam

A

Xanax, Xanax XR, Alprazolam Intensol, Niravam (discontinued)

Benzodiazepine.
panic disorder + GAD.

Increase GABA affinity at GABAA receptor

1: not common to overdose on alprazolam alone. However, use with other CNS depressants (alcohol) can be fatal.

2: Abrupt discontinuation of this medication can be fatal; the risk of seizures is greatest 24-72 hours following discontinuance

3: Several conditions and populations may be negatively impacted, including: obesity, alcoholic liver disease, smokers, kidney disease, history of seizures, history of addiction or psychosis

Pregnancy: Category D - Evidence of risk to fetus (abnormalities during first trimester, floppy baby, withdrawal syndrome)

Elderly: longer clearance, reduce dosage

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2
Q

buspirone

A

BuSpar, Vanspar

Serotonin 5-HT1A receptor agonist (not related to other anxiolytics)

does not exhibit sedative effects

GAD; most commonly used to enhance the effect of an SSRI or SNRI antidepressant.

-lower risk of addiction = often prescribed for pxts with history of SUDs who need to be treated for an anxiety disorder.

limited clinical effectiveness on panic disorders, severe anxiety, phobias, and OCD

GERIATRIC: ✔️ tx option for irritability in pxts with dementia as well as pediatric patients
PREGNANT: not known; should only be used if needed
CHILDREN: not FDA approved, but used under close medical supervision

Contraindications
-taken benzos in the past
-with other CNS depressants (benzos)
impaired hepatic or renal function
-MAIOs and grapefruit

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3
Q

venlafaxine

A

Effexor
SSNRI / anxiolytic
Reduces: MDD, GAD, social anxiety, PD
-Selective reuptake of 5-HT, NE, DA

especially good for GAD, Social, Panic but can increase BP; not recommended in elderly
Higher toxicity risk than other SSNRIs

may have amphetamine-like effects; off-label use for cocaine dependence
Not recommended for bipolar patients
may be more likely than other antidepressants to trigger a manic state
Primarily used for anxiety

Increased liability for suicide

CONTRAINDICATIONS
-blood pressure conditions
-history of bipolar disorder (family history)
-MAOI or other 5HT drugs
-seizures

Pregnancy C; animal risk but no known human risk
Geriatric Use: ✔️ No concerns (but take caution for those w/ blood pressure or liver/kidney concerns)
Adolescents: increased risk of increased SI

The extended release version of Effexor XR requires less doses and doesn’t necessarily have the uncomfortable symptoms as Effexor (e.g. nausea)

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4
Q

propranolol

A

Hemangeol, Inderal, Innopran XL
Beta Blocker / anxiolytic

HEART ISSUES: slows heart rates, so don’t use w/ issues; don’t ween off too quickly; side effect is Aggravated Congestive Heart Failure

does not treat mental symptoms of GAD but is helpful in physical symptom treatment

binds to Beta-1 and Beta-2 adrenergic receptors –> prevents sympathetic effects
Adrenaline + noradrenaline blocked → prevent faster heart rate and physical anxiety symptoms

Notable side effects: Psychosis

Contraindications
asthma or other breathing issues (Smokers, COPD)

Special Populations
children + older ppl: no data, could last longer in elderly
pregnancy: could stunt growth
will show up in breast milk

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5
Q

lamotrigine

A

Lamictal
Antiepileptic / anticonvulsant
off-label for BIPOLAR DISORDER (increases time between mood eps and delays onset of depressive eps)
Not useful for acute mania

**must be monitored for signs of fatal rash and Stevens-Johnson disease
–> Adolescents more prone to this reaction - ptxs younger than 16 shouldn’t take it **

good for txt-resistant pxts

blockade of sodium channel → reduces glutamate release

In contrast to other antiepileptics, can improve cognitive functioning

safest antiepileptic to use in pregnancy (category C)

Contraindications
Valproic acid - reduces half-life of lamotrigine
CNS depressants (increased potency)
Reduces oral contraceptives efficacy

Children
Adjunctive treatment for seizures in patients above 2 years old
-not established for under 18

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6
Q

ziprasidone

A

Geodon
second-gen antipsychotic but PRIMARILY used for acute bipolar 1 episodes (especially effective when I.M.)

ANXIOLYTIC, ANTIDEPRESSANT ACTIONS
LOW WEIGHT GAIN

-Predecessor of risperidone
-used w/ lithium or valproate
-Also used for schizophrenia

binding affinity for DA, 5-HT, adrenergic, and histaminergic receptors

Contraindications:
-higher risk for QT prolongation than most other antipsychotics and should be considered last in those with heart problems.

Hypoglycemia, can be deadly

should not be combined with other antipsychotics and has harmful interactions with dolasetron, metoclopramide, saquinavir.

Pregnancy category C
Elderly: can cause an increased risk for stroke, cognitive decline, and death in patients with dementia.

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7
Q

lurasidone

A

​​Latuda
Second-gen antipsychotic / bipolar disorder presentations (approved in 2013 for bipolar disorder)

Affects DA + 5HT receptors
Has highest affinity for the 5-HT7 receptor, in comparison to other second-generation antipsychotics

Low activity on muscarinic M1, histamine H1, alpha-1, and 2A adrenergic receptors

Minimizes the risk of orthostatic hypotension, sedation, weight gain, and cognitive blunting associated with other antipsychotic agents

Contraindications
Hypersensitivity, Severe Renal Impairment, Severe Hepatic Impairment, QT Prolongation

Pregnant: may cause EPS or withdrawal symptoms in fetus

Geriatric: Black box warning for increased risk of death in elderly patients with dementia

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8
Q

​​quetiapine

A

Seroquel, Seroquel XR
second-gen antipsychotic / bipolar disorder

Abused more frequently than other antipsychotics, primarily due to sedative and anxiolytic effects

used often to treat adolescent mania

Seroquel XR:
-not approved for patients with dementia-related psychosis or patients younger than 18 years

Antagonism of DA D2 + 5HT2A
higher affinity for serotonin
high affinity to histaminergic and alpha-1 adrenergic receptors
Histamine H1 → drowsiness
adrenergic α1 receptors → orthostatic hypotension (low blood pressure from sitting or standing)
muscarinic M1 → anticholinergic effects

Lower occurrence of abnormal motor movements

2 Black Box Warnings:
Increased risk of death in elderly individuals with dementia-related psychosis
Increased risk of SI in adolescents
Don’t give to <10 yr olds → suicidality
Elderly: decrease in plasma clearance by 30-50% → decrease dosage

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9
Q

valproate / valproic acid

A

Depakote, Depakene, Stavzor

anticonvulsant / Bipolar disorder

Better for mixed episodes than lithium
Teratogenic

-GABA agonist/glutamate antagonist –> increased GABA

Interactions: aspirin, rifampin

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10
Q

carbamazepine

A

Tegretol

anticonvulsant / Bipolar disorder

***side effects can include a rare, life-threatening dermatological reaction caused by a metabolite, carbamazepine-epoxide.
risk is 10x higher for those of Asian ancestry

Leucopenia / agranulocytosis:
More serious reactions involve
leucopenia: relatively benign reduction in white blood cell count
Agranulocytosis: severe reduction in white blood cell count
received a “black box” warning and a recommendation for periodic blood tests.
leaves pxts open to infections.***

Block Na+ channels; decreases neuronal activity (anti-epileptic)

-May be better than lithium for rapid cyclers, mixed mania

-Pregnancy category: D - Better than valproate but still not recommended

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11
Q

Lithium

A

Lithium - Bipolar disorder
Because lithium closely resembles table salt, when a patient lowers his or her normal salt intake or loses excessive amounts of salt, such as through sweating, lithium blood levels
may rise, quickly producing toxicity

Drug Interactions: diuretics, ACE inhibitors, NSAIDs
high toxicity; very low TI - 2.5x therapeutic dose can kill.

Effective in 75% pxts
Symptoms - renal failure, tremor, seizures, cognitive deficits, coma, death (kidney failure)

requires routine blood tests;
no antidote to lithium.

Does not bind to receptors. commonalities with antidepressants: nueroprotective, increases BDNF and NAA)
Inhibits PI signaling pathway, GSK-3 + increases glutathione (increases neuronal health)

Patient Noncompliance - 50% due to cognitive effects, weight gain, lethargy, missing manic episodes

When going off of li, increased risk of manic episodes, suicide (14-fold)

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12
Q

oxcarbazepine

A

Trileptal
anticonvulsant / Bipolar disorder

better safety index; no GI issues, no alterations in liver enzymes (fewer drug interactions), no leucopenia (no monitoring required)

Addition of O molecule to carbamazapine; as efficacious as carbamazepine

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13
Q

gabapentin / pregabalin

A

Neurontin / Lyrica
Anticonvulsant / Bipolar disorder

Excellent safety profile; not metabolized by liver, excreted intact - therefore can safely be used for tx of alcoholism

GABA analogues (very similar structure to GABA but act in a different way)
has little or no action on the GABA receptors; decreases Ca2+ entry into presynaptic terminals - results in less neurotransmitter release, resulting in antiepileptic, analgesic, and anxiolytic effects.

Not a stand-alone txt, but may be beneficial in combination with Lithium

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14
Q

topiramate

A

Topamax
Not super useful as a txt for BD, per se, however induces weight loss, which can counteract weight gain seen with other BD drugs

Originally developed as an anti-diabetic Rx
Used to txt migraines

May increase lithium concentration in blood, so must monitor closely

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15
Q

loxapine

A

Loxitane / Adasuve

1st gen antipsychotic

inhaled version (Adasuve) approved by FDA in 2012

Very similar to clozapine

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16
Q

molindone

A

Moban

first gen antipsychotic

Induces weight loss, which is an important advantage over traditional antipsychotics

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17
Q

pimozide

A

Orap

first gen antipsychotic

In USA, used more for Tourette’s syndrome

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18
Q

clozapine

A

Clozaril

The first atypical antipsychotic (1970s) and still the gold standard / model
Effective in clients previously treatment resistant
Very little motor side effects, if any (can be used in PD patients)
Agranulocytosis in 1 - 2% of pxts (death) → makes it too expensive
Contraindicated if pxt is taking other drugs that reduce WBC cell counts (i.e.antibiotics)

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19
Q

olanzapine

A

Zyprexa

2nd gen antipsychotic

reduces positive symptoms & improves negative symptoms

similar binding profile to clozapine but it does not work as well

Contraindications
Heart or liver problems
Pregnant (Category C)
Diabetes, insulin resistance
Stroke
Dementia

20
Q

sertindole

A

Serlect
2nd gen antipsychotic
5-HT2 antagonist (highest affinity), D2 antagonist
Does not bind to H receptors, so no sedative effects
Not FDA approved bc of high incidence of QT prolongation and CSD. can adversely affect the heart, an action that can lead to severe cardiac arrhythmias.
removed from the market

21
Q

amisulpiride

A

Solian
Low diabetogenic effects
Highly selective D2/D3 antagonist, but only in limbic
system (not basal ganglia)

22
Q

xanomeline-trospium

A

KarXT
3rd gen / atypical antipsychotic very new

Xanomeline: treats positive and negative symptoms of schizophrenia + Alzheimer-related symptoms.
Trospium - used to help prevent side effects that Xanomeline can cause.
Improves cognition AND reduces psychosis
doesn’t rely on the dopaminergic or serotonergic pathway; instead interacts with muscarinic receptor and indirectly affect dopamine

Used in elderly people ✔️
Pregnancy: prematurity, very high and very low birth weight

23
Q

lumateperone

A

Caplyta
2nd generation antipsychotic with FDA approval for treatment of schizophrenia and
depression in Bipolar I & II.

Serotonin: More affinity for 5-HT2A than D2 receptors, creating antidepressant effects
more effective at negative symptoms than other antipsychotics while also targeting positive symptoms

Potentially lethal for elderly people with dementia
Should not be used with children and adolescents
Pregnant women: EPS and/or withdrawal symptoms for child / fetus

24
Q

paliperidone

A

Invega - 2006 tablets / 2015
Atypical antipsychotic
Long-acting-injectable 1x per month or 6 months

  1. it’s safety has been underscored by decades of study on its predecessor, risperidone.
    –> slightly better risk profile for serious side-effects.

only FDA-approved drug as a monotherapy for schizoaffective

Contraindications:
Elderly patients with dementia-related psychosis trials show increased risk of death
QT Prolongation

Cleared for use in geriatric population with schizophrenia

25
cariprazine
Vraylar, Regalia, Symvenu atypical antipsychotic negative symptoms (schizophrenia) and depressive symptoms (bipolar I disorder) should not be used by elderly with dementia-related psychosis lower blockade of DA receptors compared to other antipsychotics children and adolescents: safe ✔️ discontinue in pxts w/ severe depression to prevent suicidal thoughts and behavior Pregnancy ❌ extrapyramidal and withdrawal symptoms
26
ashwagandha
Withania somnifera Comes in topical form as lotion and oil GABA mimetic effect In rare instances, liver failure considered an adaptogen - can become ineffective if taken for a long period of time Drug interactions: Antidiabetes drugs Antihypertensive drugs Immunosuppressants Benzodiazepines CNS depressants Thyroid hormone pills Special Populations Be aware of precautions if you: Are pregnant Are breast-feeding Have an auto-immune disease Will be undergoing surgery Have a thyroid disorder
27
St John’s Wort
Hypericum Perforatum --can interact dangerously with SSRIs → can lead to “serotonin syndrome” --Negative effect on contraceptives -action v similar to TCAs: inhibits reuptake of 5-HT, DA, NE Used to treat menopausal symptoms, moderate depression, and somatization disorder CONTRAINDICATIONS Paired with other drugs can lead to a decrease in efficacy or increased side effects May increase risk of psychosis + mania Pregnant and breastfeeding ❌
28
valerian
Valeriana Officinalis sedative; "Nature's valium” Hasn’t been found to affect contraceptives Contraindications Children Under 3 Years or when pregnant ❌ Liver Disease Anesthesia CNS depressants Anticonvulsants Tricyclic antidepressants Other sleep aids / antihistamines Antifungal medications Primarily targets GABA reuptake but also targets 5HT, adenosine (possible), and NE (possible) Linked to rare instances of liver injury
29
Kava
piper methysticum Comprised of 6 known kavalactones Sedative & depressant; anxiety, insomnia, withdrawal symptoms Roots are consumed as a tea GABA receptors, reversible inhibition of MAO-B, and reduced uptake of NE and DA Risk of hepatotoxicity / liver failure when long-term use; banned in some countries Contraindications Hepatitis: acute, chronic, or any history Might increase the effects of anesthesia patients with renal or liver disease, blood disorders, or Parkinson Special Populations: pregnancy: ❌ under 18 years: ❌ may experience greater effects elderly: ❌ side effects that can affect reaction time, digestive problems, and dizziness
30
Ma-Huang
Ephedra sinica Ephedrine (drug) is a natural product of the ephedra plant -banned since 2004 ***Stroke/cardiac arrest, especially if used w/ caffeine.*** Increases release of adrenaline, NE, DA Side Effects Increased blood pressure Increased cardiac load increased body temp treats: asthma, flu, increase alertness/focus, performance enhancement, weight loss
31
maprotiline
Ludiomil atypical antidepressant -modified TCA ***Epileptogenic (can induce seizures - took it out of running)*** NET antagonist
32
amoxapine
Ascendin atypical antidepressant ***Blocks actual dopamine receptors (can induce Parkinsonian-like EPS)*** ***Better than most tricyclics for relieving anxiety and behavioral agitation*** NET antagonist
33
clomipramine
Anafranil atypical antidepressant ****Used to treat anxiety and pain as well as depression, particularly OCD and Panic Disorder**** Classified as a mixed serotonin-norepinephrine reuptake inhibitor.
34
trazodone
Desyrel atypical antidepressant ***Heavy sedative effects; primarily used as a hypnotic (sleeping pill)*** Weak NET, SERT antagonist Blocks (essentially all) 5-HT2A receptors
35
bupropion
Wellbutrin, Zyban atypical antidepressant Quiz: pharmacodynamic mechanism of bupropion: blocks DA and NE reuptake
36
fluoxetine
Prozac ***1st SSRI released*** Efficacy is comparable to TCAs, without AChM or H side-effects long half-life; once-weekly oral pill is available under trade name Prozac Weekly
37
sertraline
Zoloft SSRI ***Higher risk of serotonin syndrome and withdrawal syndrome due to it's higher potency and increased 5HT selectivity*** As efficacious as TCAs
38
fluvoxamine
Luvox Efficacious as TCAs ***Shortest half-life of all SSRIs*** ***Inhibits CYP1A2, which is increased by elements of tobacco smoke; smokers may require a higher dose to experience therapeutic effects*** High affinity for NE α1, which produces anxiolytic effects
39
citalopram
Celexa SSRI high doses associated with ECG irregularities and rare fatalities. better for patients who are taking multiple medications. The elderly have a reduced ability to metabolize citalopram has been reported to moderately reduce alcohol consumption in problem alcoholics.
40
duloxetine
Cymbalta SSNRI ***Not recommended for bipolar pxts; may induce mania*** Additional approvals for GAD, diabetic neuropathy and fibromyalgia
41
milnacipran
Savella SSNRI ***Approved for treatment of fibromyalgia. blocks NMDA-type glutamate receptors in the spinal cord --> analgesic action*** Comparable to TCAs, but better tolerated; comparable to SSRIs, no difference in tolerability Not yet approved by FDA for depression
42
nefazodone
Serzone ***Increased risk for severe liver damage*** antidepressant distinct from other ones chemically. strongest action is 5-HT2 receptor blockade --> distinguishes from SSRIs Low risk for sexual dysfunction
43
escitalopram
(Lexapro, Cipralex) twice as potent as citalopram Elderly: Studies have demonstrated clinically significant low blood sodium
44
paroxetine
Paxil - SSRI Three Main Things: Stronger inhibitor of serotonin reuptake than other members of SSRIs Doctors believe that those with social anxiety are the group that may be dependent Contraindications MAOIs, thioridazine, and pimozide (serotonin syndrome) thioridazine and paroxetine can induce cardiac arrhythmias
45
esketamine
Spravato treatment-resistant depression; constant monitoring Nasal spray; only meant for short-term Can not do anything that requires being alert until good night’s sleep Contains esketamine, a derivative of ketamine NMDA receptor antagonist → affects glutamate receptors in the brain → neurotrophic factors Schedule 3, highly addictive drug with potential for abuse. Can cause neonatal fatality No difference noticed in older adults
46
gepirone
Exxua Antidepressant First and only oral selective 5HT1A receptor agonist for MDD act as an antidepressant and anxiolytic Less of typically unwanted side effects, such as weight gain and sexual dysfunction Contraindicated in people that have experienced: History of congenital long QT syndrome Used a MAOI medication within 14 days Pregnancy → ❌ Decrease in suicidal thoughts in older adults > 65 years compared to placebo
47
selegiline
MAOI / Emsam Transdermal (skin patch) application developed; eliminates many drug interactions + wine and cheese effect.