specific drugs Flashcards
alprazolam
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
buspirone
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
venlafaxine
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)
propranolol
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
lamotrigine
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
ziprasidone
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.
lurasidone
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
quetiapine
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
valproate / valproic acid
Depakote, Depakene, Stavzor
anticonvulsant / Bipolar disorder
Better for mixed episodes than lithium
Teratogenic
-GABA agonist/glutamate antagonist –> increased GABA
Interactions: aspirin, rifampin
carbamazepine
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
Lithium
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)
oxcarbazepine
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
gabapentin / pregabalin
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
topiramate
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
loxapine
Loxitane / Adasuve
1st gen antipsychotic
inhaled version (Adasuve) approved by FDA in 2012
Very similar to clozapine
molindone
Moban
first gen antipsychotic
Induces weight loss, which is an important advantage over traditional antipsychotics
pimozide
Orap
first gen antipsychotic
In USA, used more for Tourette’s syndrome
clozapine
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)
olanzapine
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
sertindole
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
amisulpiride
Solian
Low diabetogenic effects
Highly selective D2/D3 antagonist, but only in limbic
system (not basal ganglia)
xanomeline-trospium
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
lumateperone
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
paliperidone
Invega - 2006 tablets / 2015
Atypical antipsychotic
Long-acting-injectable 1x per month or 6 months
- 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
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
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
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 ❌
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
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
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
maprotiline
Ludiomil
atypical antidepressant -modified TCA
Epileptogenic (can induce seizures - took it out of running)
NET antagonist
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
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.
trazodone
Desyrel
atypical antidepressant
Heavy sedative effects; primarily used as a hypnotic (sleeping pill)
Weak NET, SERT antagonist
Blocks (essentially all) 5-HT2A receptors
bupropion
Wellbutrin, Zyban
atypical antidepressant
Quiz: pharmacodynamic mechanism of bupropion: blocks DA and NE reuptake
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
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
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
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.
duloxetine
Cymbalta
SSNRI
Not recommended for bipolar pxts; may induce mania
Additional approvals for GAD, diabetic neuropathy and fibromyalgia
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
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
escitalopram
(Lexapro, Cipralex)
twice as potent as citalopram
Elderly:
Studies have demonstrated clinically significant low blood sodium
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
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
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
selegiline
MAOI / Emsam
Transdermal (skin patch) application developed; eliminates many drug interactions + wine and cheese effect.
