Anx-depp-Bipolar Flashcards
What are uses of BZD?
Anx disorder
Insomnia
Seizure disorder
Status Epilepticus: IV ONLY
Premedication for anesthesia (IV/IM)
Off-lable use:
- Alcohol withdrawal - Chemotherapy-assoc N/V - Essential tremor
Which BZD’s are my LONG-ACTING BDZ’s?
- Chlordiazepoxide (LIBRIUM)
- anx: 5-25mg PO tid-qid
- alcohol withdrawal
- Clonazepam (klonopin)
- panic disorder
- seizure disorder
- Diazepam (Valium)
- Flurazepam (Dalmane)
Which Benzo’s are INTERMEDIATE (10-20 hrs)?
Lorazepam (Ativan)
TEMAZEPAM (Restoril)
Estazolam (Prosom)
Short-Acting- BZD’s (<12 HOURS)
Alprazolam (Xanax, Xanax-XR)
- 3A4 SUBSTRATE (use with caution w/ INHIBTORS & INDUCERS)
Oxazepam
Triazolam (Halcion)
Midazolam
-SHORT ACTING BENZO’s have the HIGHEST risk of abuse because of RAPID RISE AND FALL of levels!!
Which BZD’s are recommended for OLDER patients?
Lorazepam
Oxazepam
Temazepam
LOT!!
For patients taking MULTIPLE MEDS, on METHADONE, or COMPROMISED LIVER FX, which BZD’s do you recommend?
LOT
LORAZEPAM
OXAZEPAM
TEMAZEPAM
LOT drugs are mostly cleared by KIDNEYS and thus have DECREASE P450 drug INTERACTIONS. (Most BZD’s except for LOT are metabolized by CYP3A4)
Benzodiazepine SE and PRECAUTIONS
Drowsiness/ impair driving
Memory impairment: ANTEROGRADE AMNESIA
Tolerance**
Rebound or Withdrawal s/s FOLLOWING discontinuation
Drug abuse: CAUTION in pts w/ HISTORY of ALCOHOL or DRUG ABUSE
BBW: Can be lethal if combined with OPIODS, ALCOHOL, Or other meds that depress the CNS: result in RESPIRATORY DEPP & DEATH!!
-PREGNANCY CAT D**
BZD Withdrawal SYMPTOMS?
-DISTURBED SLEEP
-TREMORS
-MUSCLE ACHES
POOR COORDINATION
MILD PARANOIA
CONFUSION
PSYCHOSIS
SEIZURES**
OVERDOSE: results in RESPIRATORY DEPRESSION, HYPOTENSION, COMA, DEATH
-ANTIDOTE: Flumazenil!!
Buspar
BUSPIRONE
MOA: unknown
- NO EFFECT ON GABA
- AFFINITY for serotonin 5-HT1A
- AFFINITY for dopamine D2- receptors
Treats: ANXIETY
Dose: MAX —> 30mg BID
MAJOR CYP3A4 SUBSTRATE
DONT GIVE W/ MAOI
Counseling point: TAKES UP TO 4 weeks to work!!
SE: dizziness, drowsiness, HA, Nervousness
Anxiolytic SUPPLEMENTS
Kava-kava - caution: HEPATOTOXIC
Valerian ROOT - Insomnia; not for ANX
PASSION flower - A calming herb
St. John’s Wort - INCREASES 5HT-3
Hops - Relaxing and sedative effect
Chamomile - sedative, ANX, relieves GI distress, MAY INCREASE INR(has warfarin derivatives)
B-Complex: essential for SYNTHESIS of serotonin; Vitamin B deficiency has been associated with ANX & DEPRESSION.
L-Tryptophan and 5-HTP: Precursors used by body for synthesis of serotonin
SSRI
GENERAL INFO
RECEPTOR SPECIFICITY**
MOA: inhibit reuptake of serotonin (5-HT) at ALL receptors, acting as a SEROTONIN AGONIST
5-HT1: involves DEPRESSION
5-HT2: involves SEXUAL DISFX
5-HT3: involves GI side EFFECTS
AD’s increase the risk of SUICIDAL THINKING & behavior in short term studies in pts < 24YO w MDD AND A DECREASED RISK IN those > 65 yrs old.
SSRI SIDE EFFECTS:
- SSRI’s reduce platelet aggregation (INCREASE BLEEDING)
- Link to Increase GI BLEEDING
CAUTION W/: NSAIDS, aspirin, WARFARIN
Luvox & Celexa: Known to have LESS Bleeding
- Activating or Sedating
(Fluoxetine: Activating)
(Fluvoxamine: Sedating) - GI effects: Nausea/ Diarrhea
- Weight Gain!!
- Sexual dysfx!!
- HeadAche
- Hyponatremia
- Orthostatic Hypotension
- Bone Fractures
- Ocular effects
- Suicidal thinking
PREGNANCY CAT C (pulmonary HTN)
-Paxil: Heart Defects
-Anticholinergic: Dry mouth
SSRI DRUG INTERACTIONS
Fluvoxamine- STRONG CYP1A2 INH
Fluoxetine/Paroxetine- STRONG CYP2D6 INHIBITORS
- Avoid combining w/ TAMOXIFEN!! - Avoid w/ Codeine (CYP2D6 substrate)
Vortioxetine: substrate of CYP2D6 & CYP3A4
Vilazodone: substrate of CYP3A4
Celexa
Citalopram
Treats: MAJOR DEPP DISORDER
form: tabs; solution (10mg/5mL)
Max: 40mg/d; 20mg/d > 60YO DUE TO QT prolongation**
CAUTION: Cardiac disease, low k/mg, liver impairment
Drug Interactions: 2C19 SUBSTRATE
- avoid going over 20mg w/ CYP2C19 inhibitors: OMEPRAZOLE & Cimetidine
Lexapro
EsCitalopram
Treats: MDD; GAD
DOSE: 10qd AM/PM
MAX: 20mg/d after one week QD
FORMS: tabs; soln
DI: Major substrate of CYP2C19/ CYP3A4
Prozac/ Sarafem
Treats: MDD, OCD, Bulimia nervosa, PreMENSTRUal dysphoric disorder, PANIC disorder
- approved in CHILDREN W/ MDD > 8 yo
- approved in children w/ OCD >7 YO
Forms: caps; solution
MAX: 80mg/d
CAUTION: **MAOI’s should be D/C at least 14 days before initiating fluoxetine. If on fluoxetine, d/c fluoxetine at least 5 weeks before going on MAOI due to its LONG half life
DI: PROZAC is a STRONG inhibitor of CYP2D6
LuVOX
Fluvoxamine
Treats: OCD
FORMS: tabs; ER caps
Administer: BEDTIME(VERY SEDATING)
CYP2c19 substrate
CYP450 Inhibitor: PRIMARILY 1A2
PAXIL, PAXIL CR, PEXEVA, Brisdelle
ParoxeTiNE
Indication: MDD, GAD, OCD, panic disorder, PMDD, SAD, PTSD, Vasomotor symptoms of menapause (BRISDELLE) ONLY
CYP450 STRONG Inhibitor of : 2D6
- DO NOT D/C abruptly
Pregnancy CATEGORY D due to CARDIAC TOX!!
Zoloft
Sertraline
Treats: MDD, OCD, Panic disorder, PMDD
DOSE: MAX:200mg/d
-Moderate/Weak inhibitor of CYP450
:CYP2D6 ( like paxil/prozac)
FOOD ^ BIOAVAILABILITY
But can take W/WO food.
Trintellix
Vortioxetine
Treats: MDD
MOA: SRI/ 5HT1a agonist/ 5HT1b partial agonist/ 5HT3a; 5HT7 ANTAGONIST
DOSE: MAX: 20mg/d
CONTRAINDICATION: Dont use MAOI’s within 21 days of STOPPING TrinTELLIX
SE: NAUSEA, no effect on WEIGHT GAIN
DI: SUBSTRATE of CYP2D6 & CYP3A4. Decrease dose by 1/2 w INHIBITORS
BUPROPION ^ TRINTELLIX BY 2X’s
SNRI
GENERAL INFO
Serotonin-Norepi-Reuptake- INHIBITOR
Venlafaxine(EFFEXOR)
DesVenlafaxine(Pristiq)
DesVenlafaxine(Khedezla)
DULOXETINE (CYMBALTA)
Milnacipran (SAVELL)
LevoMilnacipran(Fetzima)
ALL SNRI need DOSE ADJUSTMENT IN RENAL/HEPATIC
SE: NAUSEA(most common), CONSTIPATION, DRY MOUTH, DIZZINESS, SWEATING, ^^BP^^, sexual dysfx.
SNRI SIDE EFFECTS:
HEADACHE/HYPONATREMIA
OCULAR
BONE FRACTURES
SUICIDAL THINKING
GI: Nausea; GI Bleeding, ^ risk of BLEED
^^^ BLOOD PRESSURE^^^
NE “psuedoanticholinergic” EFFECT ( Constipation, dry mouth, Urinary RETENTION)
- NAUSEA, dizziness, Dry Mouth, Sweating, BP
Effexor
Venlafaxine
Treats: MDD, GAD, panic disorder (XR- ONLY)
Dose: Administer w/ FOOD
Forms: tabs(BID/TID), XR CAPS, ER TABS
CRCL<30 reduce dose by 1/2
SE: Activating/ Sedating, agitation, GI, HTN, HA
PRISTIQ
DESVENLAFAXINE SUCCINATE
SNRI**
Treats: DEPRESSION
CRCL< 30 50mg QOD
^^ BP^^
Khedezla
Desvenlafaxine BASE
SNRI
TREATS: MDD
MAX:400mg/d
Cymbalta/ Irenka
Moa: SNRI
INDICATION: Depression, GAD, fibromyalgia, chronic musculoskeletal pain, chronic osteoarthritis pain, and chronic low back PAIN.
Max: 120mg
DI: Substrate CYP1A2, CYP2D6/ Inhibits CYP2D6
- AVOID in CrCL < 30mL/min & Hepatic impairment
Monitor: BP
Savella
Milnacipran
SNRI
Treats: Fibromyalgia
(3 drugs approved for fibromyalgia are: Lyrica, Cymbalta, Savella)
Max:200mg
ESRD: NOT RECOMMENDED
Fetzima
LEVOmilnacipran
SNRI
TREATS: MDD(NOT fibromyalgia)
CYP3A4 SUBSTRATE
- ESRD: NOT RECOMMENDED
Dose: ONCE DAILY
DO NOT TAKE W/ ALCOHOL
NE & DOPAMINE (NDRI)
REUPTAKE INHIBITORS
BUPROPION
- Wellbutrin SR
- Wellbutrin XL
- Aplenzin (ER)
- Zyban
Wellbutrin; Aplenzin; Zyban
BuPROPION
MOA: D2/NE agonist
- preferred if worried about sexual dysfx
Indication: MDD/Smoking cessation/ SAD- seasonal affective DISORDER
- MAX dose/d:
- IR: 450mg/d
- SR: 400mg/d
- XL: 450mg
Aplenzin: 522mg
SE: SEIZURES
Bupropion
SE & DRUG INTERACTIONS
SE: 1) ACTIVATION
2) SEIZURES
CAUTION: bulimia**, Alcoholics, Seizures, psychosis
WEIGHT-LOSS
GI Effects
DI: Moderate CYP2D6 Inhibitor
Avoid ethanol, Valerian root, St. Johns WORT, SAMe, kava kava( may increase CNS depression)
Serotonin MODULATORS
Trazodone
Nefazodone
Vilazodone
Trazodone
MOA: blocks serotonin reuptake (LESS POTENT than SSRI’s) & alpha-Adrenergic Blocker!!)
- Serotonin Modulators
Treats: MDD, Sleep disorder
SE: GI, sexual dysfx, Orthostasis, PRIAPISM!!
Nefazodone
MOA: serotonin reuptake blocker & alpha1 blocker
Treats: MDD
BBW: HEPATOTOXICITY monitor LFT’s
viiBRYD
Vilazodone
CLASS: Serotonin MODULATOR
MOA: blocks 5HT reuptake & partial 5HT1a receptor AGONIST
treats: MDD
DOSE: Start 10mg WD w FOOD x 7 days
Maint/ max: 40mg QD w FOOD
-: NO WEIGHT GAIN
DI: SUBSTRATE OF CYP3A4
Contraindications: 14 days D/C with MAOI’s
Se: Same as SSRI’s
Remeron
Mirtazapine
Treats: MDD
MOA: alpha2 antagonist —> ^ NOR; 5HT3
- Antagonist @ 5HT2a, 5HT2C, 5HT3
Form: tabs; ODT**
SE: 1) Sedation
2) appetite(^ weight gain) 3) ^ lipids 4) anticholinergic (dry mouth, constipation) 5) QT Prolongation
TCA MOA
MOA: Blocks NOR & 5HT3 reuptake
Tertiary - Higher 5HT3 Affinity
Secondary - Higher NOR affinity
Also stimulate:
- alpha adrenergic: Orthostasis
- Histaminergix : Weight gain; Sedation
- anticholinergic: dry mouth, urinary ret, constip
TCA SIDE EFFECTS
1) sedation
2) anticholinergic
3) weight gain
4) tachycardia/arrhythmias
- risk of QTc prolongation
- Lower seizure threshold
DO NOT D/C abruptly
Elavil
Amitriptyline (Tertiary)
TCA
TREATS: 1) Depression
- OFF-LABLE: 1) chronic pain
2) Diabetic Neuropathy
3) migraine ppx
4) PTSD
Anafranil
Clomipramine (Tertiary)
Class: TCA
TREATS: OCD
Silenor
Doxepin (Tertiary)
Class: TCA
Treats: Depression/anxiety/INSOMNIA
OFF-LABLE: 1) CHRONIC UTICARIA (Hives)
Tofranil
Imipramine (Tertiary)
Class: TCA
- Indicated: Depression
* * ENURESIS** BED WETTING!!!
OFF-LABLE: Bulimia, Neuropathic PAIN
Surmontil
TRIMIPRAMINE (Tertiary)
Class: TCA
Amoxapine
TCA(secondary)
MOA: Blocks NE & DOPAMINE (ONLY ONE)
Norpramin
Desipramine
TCA : 2nd
Treats: Depression
OFF-LABLE: Neuropathic pain
Maprotiline
TCA: SecondAry
PaMEloR
Nortriptyline
CLASS: TCA: 2nd
Treats: DEPRESSION
OFF-LABLE: 1) Chronic pain
2) IBS
3) Post-Herpetic Neuralgia
4) Smoking cessation
Protriptyline
Class: TCA; 2nd
What meds can also be used for BED-WETTING?
1) Imipramine
2) anticholinergics
- fesoterodine
- oxybutynin
- Tolterodine
3) DDAVP (Desmopressin)
MONOAMINE OXIDASE INHIBITORS
Inhibit MAOa & MAOb
- 1) Isocarboxazid (Marplan) - 2)phenelzine (Nardil) - 3) Tranylcypromine (Parnate)
Selegilime (EmSAM)
QD PATCH (SELECTIVE FOR MAOb at low doses and NONSELECTIVE AT HIGHER)
MAOI
SE; MOA; Indications
MOA: MAOI’s inhibit the BREAKDOWN OF DOPAMINE; 5HT3, and NOR-EPi
Indications: MDD
- Can be effective in treatment resistant depression
E: Insomnia, anticholinergic, Orthostasis, Weight Gain, Edema, Sexual dysfx.
MAOI DRUG INTERACTIONS:
VERY IMPORTANT
1) Dextromethorphan - Hyperpyrexia
2) Meperidine; Fentanyl; Methadone; Tramadol (^ Effect of MAOI)
3) Morphine/Hydromorphone/Hydrocodone
- (^^ CNS Depression & hypotension)
4) TCA; SSRI:
5) Oral INHALATION; Anticholinergics; Umeclidinium: Tiotropium
- May enhance Anticholinergic effects
6) Sympathomimetics( amphetamines, Ephedrine, psuedophedrine, Beta-Agonist) - Hypertensive CRISIS
Emsam
Selegiline
Indication: MDD
FORM: PATCHES (DAILY)
What are other MAOI’s that arent in the depression chapter?
1) Linezolid (ABX)
2) Tidezolid (ABX)
3) Rasagiline
4) Procarbazine (Chemo)
Which AP’s are approved for MDD?
1) Abilify
2) Symbyax (Olanzapine/Fluoxetine)
3) Quetiapine (XR)
4) Brexipiprazole (Rexulti)
OTC meds for DEPRESSiON
1) SAM-e
2) ST. John’s WORT
- Photosensitivity - P450 Inducer - Watch for Serotonin Syndrome
Celexa
Citalopram
Treats: MAJOR DEPP DISORDER
form: tabs; solution (10mg/5mL)
Max: 40mg/d; 20mg/d > 60YO DUE TO QT prolongation**
CAUTION: Cardiac disease, low k/mg, liver impairment
Drug Interactions: 2C19 SUBSTRATE
- avoid going over 20mg w/ CYP2C19 inhibitors: OMEPRAZOLE & Cimetidine
Lexapro
EsCitalopram
Treats: MDD; GAD
DOSE: 10qd AM/PM
MAX: 20mg/d after one week QD
FORMS: tabs; soln
DI: Major substrate of CYP2C19/ CYP3A4
Prozac/ Sarafem
Treats: MDD, OCD, Bulimia nervosa, PreMENSTRUal dysphoric disorder, PANIC disorder
- approved in CHILDREN W/ MDD > 8 yo
- approved in children w/ OCD >7 YO
Forms: caps; solution
MAX: 80mg/d
CAUTION: **MAOI’s should be D/C at least 14 days before initiating fluoxetine. If on fluoxetine, d/c fluoxetine at least 5 weeks before going on MAOI due to its LONG half life
DI: PROZAC is a STRONG inhibitor of CYP2D6
Which meds can be used for BiPolar DISORDER?
1) Lithium
2) Anticonvulsants
- Divalproex sodium (Depakote)
- Lamotrigine (Lamictal)
- Carbamazapine (Equetro)
3) Antipsychotic
- Quetiapine XR
- Olanzapine (Zyprexa); Symbyax
- Ziprasidone
- Aripiprazole
- Lurasidone
- Asenapine (Saphris)
In General: Lithium or Depakote combined w/ an antipsychotic is more EFFECTIVE than monotherapy
DOC for Bipolar
Lithium, IF TOLERABLE
Which drugs have been shown to be effective in treating BiPolaR DePressIoN?
1) Lithium
2) quetiapine
3) Lurasidone
4) symbyax (Olanzapine + Fluoxetine)
Which Anticonvulsant is effective for prevention of RECURRENT depressive episodes?
Lamictil (Lamotrigine)
Which two Anticonvulsant can be for maint Tx but are usually less effective than Lithium?
Valproate (Depakote)
Carbamazepine
Lithobid
Lithium
Indication: 1) Bipolar Depression
2) Off-label; Depression
MOA: Unknown; Believe to influence reuptake of 5HT and/or NOR
- (+) charge element similar to Na/K
- EFFECT ON electrolytes (Na, K, Ca, Magnesium)
OPPOSITE effect on SODIUM
Lithium DOSAGE Forms
Lithium Carbonate
- (IR) forms: 150,300, 600 CAPS
300mg tabs (Eskalith)
- (CR): 300mg Lithobid
- XR: 300mg & 450mg
Lithium citrate SYRUP
- 8mEq/5mL soln (5mL = 8meq= 300mg)
Lithium DOSAGE!!
Starting dose: 300-600mg BID-TID
Effective range: 900-1800mg/day(15-20 mg/kg)
- Elderly and Renal: Decrease dose
- 300mg/ day w/ LEVELS of 0.4-0.6 mEq are
Usually effective in elderly patients
- Pregnancy cat D
* *100% RENALLY CLEARED**
Therapeutic Monitoring: Draw serum levels JUST BEFORE next dose, after 5(FiVE) days of TREATMENT
- Acute Levels: 0.8-1.2 mEq/L - Maintenance: 0.6-1.0 mEq/L
Lithium effect usually begin in 1 WEEK and full effect w/I 2-3 WEEKS
Lithium SIDE EFFECTS
1) GI(N/VD) take w/ FOOD**!!!
2) Fine intentional HAND TREMOR
3) Nephrogenic diabetic insipid-us:
- Chronic lithium ingestion can cause ADH not to
work causing POLYURIA/POLYDIPSIA which may
cause Lithium TOXICITY!!
- If possible D/C lithium
- For patients whom lithium therapy is necessary
Add POTASSIUM (K)- sparring Diuretic,
AMiLoRiDe
4) Leukocytosis (^WBC)
5) Thyroid**
6) Parathyroid - Hypercalcemia: Hyperparathyroidsm
7) Weight gain **
8) Bradycardia
9) Acne: Alopecia
10) CNS adverse RXN: Ataxia, Blackout spells,
Cogwheel rigidity
Lithium toxicity
1) > 1.5: TREMOR, Vomiting, CONFUsion, Ataxia, slurred speech
HOLD DOSE
2) > 2: arrhythmias, SEIZURES, COMA
- NS IV infusion, Hemodialysis
3) > 3.5: Lethal Toxicity!!
LITHIUM DRUG INTERACTIONS
- Thiazides; ACEI’s, NSAIDS
- Sodium RESTRICTION, dehydration, RENAL IMPAIRMENT
- ** ^^ Na will DECREASE LITHIUM!!
- SODIUM BICARB MAY ALSO DECREASE LITHIUM!!
Lithium w/ SSRI’s: Serotonin Syndrome
S/s: confusion, agitation, Diarrhea, Tremor, diaphoresis
Which NSAID can be recommended w/ Lithium?
Sulindac
Aspirin
