pharm Flashcards
SSRIs
escitalopram (Lexapro) citalopram (Celexa) fluoxetine (Prozac/Sarafem) paroxetine (Paxil, Pexeva, Brisdelle) sertraline (Zoloft)
SSRI SEs
decreased libido, sexual dysfunction, prolonged ejaculation
SNRIs
desvenlafaxine (Pristiq)
venlafaxine (Effexor)
duloxetine (Cymbalta)
SNRI SEs
cleaner than SSRIs but more expensive
antidepressant used for smoking cessation, lowers seizure threshold in bulimic pts
buproprion
what is mirtazipine used for primarily
appetite stimulant
antidepressant used as sleep aid
trazodone
TCAs
-triptylines
imipramine (enuresis)
doxepin
main use of TCAs
neuropathic pain
SEs TCAs
3 Cs: convulsions, cardiac toxicity, coma
also anticholinergic SEs
MAO-i
Selegeline
Phenylzine
*cause HTN emergency when eating wine/cheesd (high tyramine)
mood stabilizers for acute mania
1st line: lithium or valproic acid (Depakote)
2nd line: quetiapine (Seroquel) alone or with the above agents; lamotrigine (Lamictal)
3rd line: carbamazepine
lithium SEs
teratogen
nephrotoxic, nephr. DI
narrow therapeutic index
valproic acid SEs
spina bifida
pancreatitis
thrombocytopenia
agranulycytosis
quetiapine SEs
weight gain
QTc prolongation (get EKG)
somnolence
other uses for carbamazepine
trigeminal neuralgia, absence seizures in kids
life-threatening SE of valproic acid
pancreatitis
carbamezipine good for ?
risks?
bipolar and trigeminal neurolagia
SEs: SJS (also lamotrigine), agranulocytosis
anticonvulsants decrease efficacy of ?
OCPs and warfarin
EPS
Parkinsonism
Akathisia: restlessness
Dystonia: sustained, painful contraction of muscles of neck, tongue, eyes, diaphragm
-occur early: hrs-days of starting meds, reversible
-occurs with high-potency, typical anti psychs (1st gen)
FL for EPS
benztropine (Cogentin)
or Benadryl
Tardive dyskinesia
choreoathetoid muscle movements (mouth, tongue typ)
- occurs YEARS after antipsychotic use (high-potency 1st gen)
- typically irreversible
Important CYP 450 inducers – decrease drug levels
Tobacco, carbamazepine, barbiturates, Saint johns wort
Important CYP 450 inhibitors – increase drug levels
Fluvoxamine, fluoxetine, Paroxetine, duloxetine, sertraline
I.e. Lots of SSRIs
Most antidepressants take how long to see effect
3 to 4 weeks, maybe a short as 1 to 2 or as long as 6 to 8
SSRI withdrawl phenomenon
Dizziness, headache, nausea, insomnia, malaise; taper to avoid
What is one hypothesis why SSRIs often have delayed effect
They may cause downstream effects increasing brain plasticity
meds that may increase risk serotonin syndrome
Dextromethorphan – cold remedy
Triptan’s used for migraines
MAOIs: Don’t use SSRIs within two weeks
Distinct advantages of sSRIs
Low incidence of side effects, most of which resolve with time, no food restrictions, safer in overdose
How to deal with the sexual side effects of SSRIs
Reduce the dose, changed to non SSRI, augment with bupropion, and Viagra
Fluoxetine -brand name?
safe for? SEs?
Prozac
longest half life, safe in pregnancy and for kids
common SEs: insomnia, anxiety, sexual dysfunction
can ^ levels of antipsychs, ^SEs
Sertraline -brand name?
SEs?
Zoloft
higher risk of GI disturbances
very few drug interactions
same SEs as Prozac: insomnia, anxiety, sexual dysfunction
Paroxetine -brand name?
problem with 1/2 life?
Paxil
protein bound, so drug interactions
SEs: anticholinergic (sedation, constipation, weight gain), sexual dysfunction
*withdrawal phenomenon due to short half-life
Fluvoxamine -brand name?
Currently approved only for?
Luvox
Only for use in OCD
side effects: nausea and vomiting
multiple drug interactions due to CYP inhibition
Citalopram -brand name?
What unique problem?
Celexa
Fewest drug interactions
dose dependent QTC prolongation
Escitalopram -brand name?
Similar to?
Lexapro
Levo-enantiomer of citalopram
Similar efficacy, possibly fewer side effects
also dose depending QTC prolongation
SSRI black box warning
Potentially increasing suicidal thinking and behavior – applies to kids and young adults to age 25, but maybe accurate for adults as well
Why do SSRIs have significantly fewer side effects and TCAs and MAOIs
Serotonin selectivity – do not act on histamine, adrenergic, muscarinic receptors
Other SSRI side effects
G.I.: nausea, diarrhea - eat with food
Insomnia, vivid dreams, headache, anorexia, weight loss
Sexual dysfunction 30 to 40%: decreased libido, anorgasmia, delayed ejaculation
Restlessness: akathisia like
Serotonin syndrome
Hyponatremia: rare
Seizures: 0.2% rate, lower than TCAs
Serotonin syndrome
Fever, diaphoresis, tachycardia, hypertension, delirium, neuromuscular excitability: especially hyperreflexia and electric jolt limb movements
Rhabdomyolysis, renal failure, may lead to death
Venlafaxine – brand-name?
Effexor, used for depression, Anxiety, neuropathic pain
Low drug interaction
XR form available for once a day dosing
side effects like SSRIs but increase BP as well
New form of “venlafaxine”
DesVenlafaxine – Pristiq
Expensive, no known benefit over venlafaxine
Duloxetine – Brandname?
Cymbalta
depression, neuropathic pain, fibromyalgia
side effects like SSRIs, more dry mouth and constipation – NE effects, hepatotoxicity in those at risk, expensive
Bupropion- Brandname?
Advantages over SSRIs?
Wellbutrin (NE-Dopamine RI)
Relative lack of sexual side effects compared to sSRIs, some efficacy in treating adult ADHD, smoking cessation
side effects include increasing anxiety, increased risk of seizures and psychosis at high doses, countraindicated in patients with seizure or eating disorders or on MAOI
Trazadone- brand name? class?
other similar drug?
Desyrel, other: Nefazodone (Serzone)
Serotonin Receptor Antagonist/Agonist
MDD, MDD + anxiety, insomnia (typically initiated with SSRI for insomnia)
Trazadone and Nefazodone SEs
nausea, dizziness, othostatic hypotension, arrhythmias, sedation, priapism
DO NOT have sexual SEs of SSRIs and do not affect REM
Nefazodone: black box for liver failure, not commonly used!
Mirtazapine- brand name? class?
Remeron, Adrenergic receptor antagonist
MDD, esp. if weight loss or insomnia good for elderly
SE: sedation, weight gain, dizziness, tremor, dry mouth, constipation, agranulocytosis (rare)
fewer drug interactions and sexual SEs compared to SSRIs
TCA action
inhibit reuptake of NE and serotonin
long 1/2 lives, most dosed daily
Amitriptyline- brand name? type and use?
Elavil, tertiary TCA
chronic pain, migraines, insomnia
Imipramine- brand name? type and use?
Tofranil, tertiary TCA
IM form, enuresis, panic disorder
Clomipramine- brand name? type and use?
Anafranil, tertiary TCA
OCD, more serotonin specific
Doxepin- brand name? type and use?
Sinequan, tertiary TCA
chronic pain, sleep aid in low doses
Nortriptyline
Pamelor, Aventyl, secondary TCA
lease likely to cause orthostatic hypotension
chronic pain
Desipramine
Norpramin, secondary TCA
more activating, less sedating, least anticholinergic
tertiary vs secondary amines
tertiary are highly anticholinergic/histaminergic/adrenergic (more sedating with greater lethality in OD)
secondary are metabolites of tertiary (less anti-HAM)
Amoxapine
Asendin, tetracyclic antidepressant
may cause EPS, metabolite of loxapine (antipsychotic)
how much TCA can be lethal in OD?
1-2 g (a 1-week supply)
antidepressants for atypical depression
MAOIs considered more effective than TCAs
atypical features: ^sleep, ^appetite, leaden paralysis, ^sensitivity to interpersonal rejection
TCA SEs
highly protein bound and lipid soluble: can interact with other meds
SEs due to lack of specificity
antihistaminic: sedation, weight gain
serotonergic: erectile/ejaculatory dysfunction in males, anorgasmia in females
TCA antiadrenergic SEs
CV: orthostatic hypotension, dizziness, reflex tachycardia, arrhythmias (block Na2+ channels), EKG changes: wide QRS, QT, PR intervals)
do not use in pts with conduction abnormalities or recent MI
TCA antimuscarinic effects
dry mouth, constipation, urinary retention, blurred vision, tachycardia, exacerbation of narrow angle glaucoma
TCA OD symptoms
agitation, tremores, ataxia, arrhythmias, delirium, hypoventilation from CNS depression, myoclonus, hyperreflexia, seizures, coma
seizure rate with TCAs
0.4%, more common at higher plasma levels and with tetracyclics and clomipramine
Naltrexone- brand names? how it works?
Revia, 50 mg/d up to 100 mg/d
IM- Vivitrol, 380 mg every four weeks
Opioid receptor blocker, works by decreasing desire/craving and “high” associated with alcohol
Maybe greater benefit seen in men with family history of alcoholism
In patients with opioid dependence, will precipitate withdrawal
Contraindicated in acute hepatitis or liver failure
Modifies HPA axis to suppress ethanol consumption
Acamprosate- brand name? how it works?
Campral, 666 mg TID, 333 mg if renal impairment
GABA agonist/glutamate antagonist
Should be started post – detox for relapse prevention and patients who have stopped drinking
major advantage – can be used in patients with liver disease but countraindicated in to be a renal disease
COMBINE Trial shows limited effectiveness Campral compared to placebo (while Naltrexone was effective)
Disulfiram- brand name? how it works?
Antabuse
Blocks aldehyde dehydrogenase in the liver and causes adverse reaction to alcohol: Flushing, headache, nausea/vomiting, palpitations, shortness of breath
Contraindicated in severe cardiac disease, pregnancy, psychosis
Monitor LFTs
best used in highly motivated patients need med adherence
Topiramate- brand name? how it works?
Topamax, Second line
Anticonvulsant – potentiates GABA and inhibits glutamate receptors
reduces cravings for alcohol and decreases alcohol use
Score used to screen for alcohol use disorder
AUDIT-C
scored 0 to 12 with positive for men 4+ and women 3+
Timing of initiating alcohol abstinence pharmacotherapy
Naltrexone can be initiated while the individual is still drinking – permits treatment in a community setting at point of maximum crisis without need for enforced abstinence or detox
Disulfiram should only be used by abstinent patients
Acamprosate should only be used once abstinence is achieved
Naltrexone- genetics
Maybe effective in individuals with Asp-40 allele variant of OPRM1 gene
First generation versus second generation antipsychotics
First generation: block dopamine D2 receptors
Second generation: block dopamine D2 and serotonin 2A receptors, More effective for treating negative symptoms
low potency typical antipsychotics
Chlorpromazine -Thorazine
Side effects: orthostatic hypotension, blue gray skin discoloration, photosensitivity,
also used to treat nausea, vomiting, intractable hiccups
Thioridazine- Mellaril
Associated with retinitis pigmentosa
General side effects of low potency typical antipsychotics
Higher HAM effects: antihistamininc, anti-adrenergic, Anti-muscarinic. Compared to high potency
Lower incidence of EPS and possibly NMS, more lethal an OD due to QTC prolongation and potential for heart block and Vtach
Rare risk for agranulocytosis and slightly higher seizure risk that high potency
Mid potency typical antipsychotics
Loxapine: Loxitane Higher risk of seizures, metabolite is an anti-depressant Thiothixene: Navane Can cause ocular pigment changes Molindone: Moban Perphenazine: Trilafon
Hi potency Typical antipsychotics
Les sedation, Orthostatic hypotension, and anti-cholinergic effects
Greater risk for EPS and TD
Haloperidol: Haldol – can be given PO/IM/IV, decanoate – long-acting – form available
Fluphenazine: Prolixin – decanoate form available
Pimozide: Orap- associated with QTC prolongation and VTach
