CNS

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Acetylcholine Esterase Inhibitors (AChEI)

Aka cholinesterase inhibitors. EVD: May stabilize dementia & behavior and decrease visual hallucinations in Lewy Body dementia.
AE: N, V, D, muscle cramps, insomnia, syncope, nightmares. DI: Can inhibit anticholinergic drugs. DOS: Restart at low dose if off drug for >3d. Taper for 1w if D/C. OTH: 3-6 months of Tx for modest benefit.


donepezil=Aricept: AVL: PO. IND: Mod-severe Alzheimer’s, PD dementia. AE: N11%, D10%, V5%, insomnia9%, fatigue5%, muscle cramps6%, anorexia4%, dizziness8%, depression3%. Known QT prologation. PK: t1/2=70h. F~100%. DOS: Start=5mg/d. Max=10mg/d (consider after 4-6w).
galantamine=Reminyl: AVL: PO. IND: Mild-mod Alzheimer’s. ADM: T w/ food in am. AE: N24%, V13%, D9%, HA8%, fatigue5%, dizziness9%, indigestion5%, anorexia9%, depression7%. HC Warning: Potential to cause SJS. PK: t1/2=6h.
DOS: Start=8mg/d x4w. Maint=16mg/d. Max=24mg/d (if std dose tolerated for 4w).


rivastigmine=Exelon: AVL: PO, topical (patch). IND: Mild-moderately severe Alzheimer’s, Lewy Body Dementia, PD dementia. AE: PO: N23%, V17%, D5%, weakness6%, anorexia5%, dizziness7%, HA6%, depression4%. Patch: N21%, V19%, D10%, abdominal pain4%, anorexia4%, dizziness7%, insomnia4%. PK: t1/2=2h.

 

Anticholinergics

IND: Restore DA/acetylcholine balance in Parkinson's. EVD: Useful for tremor, foot dystonia, and drooling. AE: Dry mouth, C, urinary retention, hyperthermia, confusion, sedation, worsening glaucoma. Warning: Avoid in elderly. DI: amantadine (also has anticholinergic effect).


benztropine=Cogentin: AVL: PO, injection. DOS: PD: 1-2mg BID.


ethopropazine=Parsitan: AVL: PO. DOS: PD: Initial=25mg BID. Max=50mg TID.
procyclidine=Kemadrin: AVL: PO (tab, elixir). DOS: Adj for renal fxn. PD=5mg TID
trihexyphenidyl=Artane: AVL: PO. DOS: Adj for renal fxn. PD: Initial=1mg BID. Std=2mg TID.

 

Anticonvulsants aka Antiepileptics

brivaracetam=Brivlera: AVL: PO. IND: Epilepsy.


carbamazepine=Tegretol: AVL: PO (tab200mg, CR tab200, 400mg, liq20mg/mL, chewtab100, 200mg). IND: Bipolar, epilepsy. AE: Rash5-10%. PK: t1/2=35-40h then 12-17h after 2w of use. F=85%. PB=70%. Vd=1L/kg. Cleared hepatically. Metabolized by 3A4. Induces 3A4, 2D6. MON: Serum level=17-50uM. DOS: Bipolar: Initial=100mg BID. Std=800-1200mg/d divided BID-QID. Max=1600mg/d. Epilepsy: Initial=100mg BID. Increase by 200mg/d q3–4d. Usual maintenance: 400–1200mg/d in 2–4 divided doses, with meals when possible.


divalproex=Epival: AVL: PO. IND: Bipolar, epilepsy. MON: Serum level=350-800uM. DOS: Bipolar: 750-2000mg/d adj to serum levels. Epilepsy: Initial=250mg BID. Increase by 250mg/d q3–4d. Std=750–1000mg/d in 2 divided doses.
eslicarbamazepine=Aptiom: AVL: PO. IND: monotherapy for partial-onset seizures. DOS: Adj for renal fxn. Epilepsy: Initial=400 mg once/d × 1w. Std=800-1200mg once/d. Max=1600mg once/d (monotherapy).
ethosuximide=Zarontin: AVL: PO (cap, syrup50mg/mL). IND: Absence seizures. AE: GI upset. DOS: Initial=500mg/d in 1 or 2 divided doses. Increase by 250 mg/d q4–7d. Std=750–1000mg/d.
gabapentin=Neurontin: AVL: PO. IND: Bipolar (not 1st line), neurological pain. AE: Tremor, vision changes. DOS: Adj for renal fxn. Max=4g/d. Epilepsy: Initial=300mg once/d. Increase by 300mg/d q5–7d up to 300 mg TID, then titrate TID dose. Std=900–3600mg/d divided Q6–8H. OTH: GABA derivative.


lacosamide=Vimpat: IND: Epilepsy.


lamotrigine=Lamictal: AVL: PO (tab25, 100, 150, 200mg, chewtab2, 5, 25mg). IND:Bipolar (maintenance & depression), epilepsy. AE: Cog impairment, dizziness, ataxia (loss of control of movements), sedation, HA, diplopia, N, V, rash10% (can be serious). DI: Valproic acid significantly inhibits lamotrigine’s clearance (often used together). PK: t1/2=25h. MON: No blood level monitoring. DOS: Adj for renal and hepatic fxn. Bipolar: Initial=12.5-25mg qhs. Std=50-250mg divided BID. Max=250mg/d. Epilepsy: Initial=25mg q2d to 50 mg/d x 2w. Then same dose BID × 2w. Then increase by 100mg/d at 1-2-w intervals. Std=200–400mg/d in 2 divided doses. OTH: No antidote for overdose.


oxcarbazepine=Trileptal: AVL: PO. IND: Epilepsy.
perampanel=Fycompa: AVL: PO. IND: Epilepsy.
phenytoin=Dilantin: AVL: PO, IV. IND: Partial and tonic-clinic seizures. MOA: Blocks Na channels. AE: Gingival hyperplasia, rash5-10%, PK: t1/2=7-42h (non-linear kinetics). F~1. PB=90%. Vd=0.7L/kg. Salt Factor (S)=0.92 for caps and injection. S=1 for infatabs. 95% eliminated by the liver. Cleared mainly by 2C9 but also 2C19. Follows Michalis Menten kinetics. DOS: Loading dose=20mg/kg (used adjusted wt if obese).
pregabalin=Lyrica: AVL: PO. DOS: Adj for renal fxn. Anxiety: Initial=150 mg/d divided BID or TID. Can increase to 150mg BID after 1w.


rufinamide=Banzel: AVL: PO. IND: Epilepsy.
stiripentol=Diacomit: AVL: PO. IND: Epilepsy.
topiramate=Topamax: AVL: PO. IND: Epilepsy.


valproic acid=Depakene: AVL: PO (cap250, 500mg, liq50mg/mL). IND: Bipolar, epilepsy. AE: N, D, sedation, thrombocytopenia, leukopenia, hair loss, wt gain, menstrual disturbances, polycystic ovaries, encephalopathy. PK: t1/2=6-16h. F=90%. Cleared hepatically. Inhibits 2C9. MON: Plasma level=350-700uM. DOS: Bipolar: Initial=250mg BID. Std=1000-3000mg divided BID or TID. Max=60mg/kg. Epilepsy: Initial=250mg BID. Increase by 250mg/d Q3–4d as necessary. Std=750–1000mg/d in 2–4 divided doses.
vigabatrin=Sabril: AVL: PO. IND: Epilepsy. DOS: Initial=1000 mg/d in 1–2 divided doses. Std=2000–4000mg/d in 1–2 divided doses.

 

Antipsychotics

IND: Schizophrenia, bipolar, delirium, Tourette’s, PTSD, ADHD w/ aggression. EVD: All FGAs and SGAs (except clozapine), have similar efficacy for positive/psychotic symptoms. SGAs may be better for negative symptoms, mood and cognitive deficits. AE: Sedation, weight gain, neuroleptic Malignant Syndrome (NMS) (keep hydrated to avoid), insomnia, extrapyramydal symptoms (EPS), tardive dyskinesia, hyperprolactinemia, hypotension, anticholinergic AEs. OTH: Low potency antipsychotics tend to cause sedation while high potency causes EPS. Switching antipsychotic res: Psychiatry.net and SwitchRx (free but need to register).
First-Generation Antipsychotis (FGAs) aka Typical, Traditional, Conventional

chlorpromazine=Largactil: AVL: PO,IM. PK: t1/2=30h. DOS: Equivalence (vs olanzapine 20mg)=600mg. Start=100mg/d. Maint=300-600mg/d. Max=800mg/d. Divided HS-TID.


flupentixol=Fluanxol: AVL: PO. PK: t1/2=35h. DOS: Equivalence (vs olanzapine 20mg)=30mg. Start=3mg/d. Maint=6-12mg/d. Max=18mg/d. Divided HS-BID.


fluphenazine=Moditen: AVL: PO. PK: t1/2=13-33h. DOS: Equivalence (vs olanzapine 20mg)=30mg. Start=2.5mg/d. Maint=5-15mg/d. Max=20mg/d. Divided HS-BID.


haloperidol=Haldol: AVL: PO, IM (haloperidol decanoate). PK: PO: t1/2=20h. IM: t1/2=3w. DOS: PO: equivalence (vs olanzapine 20mg)=30mg. Start=0.5-1mg/d. Maint=1-5mg/d. Max=10mg/d. Divided HS-BID. IM: equivalence (vs olanzapine 20mg)=5.4mg. Start=50mg. Maint=50-150mg. Max=200mg. Given q4w.


loxapine=Loxapac=Xylac: AVL: PO, IM. PK: t1/2 (of active metabolite)=5-19h. DOS: Equivalence (vs olanzapine 20mg)=30mg. Start=10-20mg/d. Maint=20-100mg/d. Max=200mg/d. Divided HS-TID.


methotrimeprazine=Nozinan: AVL: PO, IM. PK: t1/2=30h. DOS: Equivalence (vs olanzapine 20mg)=30mg. Start=50mg/d. Maint=100-300mg/d. Max=500mg/d. Divided HS-TID.


perphenazine=Trilafon: AVL: PO (tab, liquid). PK: t1/2=9-21h. DOS: Equivalence (vs olanzapine 20mg)=30mg. Start=8mg/d. Maint=12-24mg/d. Max=40mg/d. Divided HS-BID.


pimozide=Orap: AVL: PO. PK: t1/2=29-55h. DOS: equivalence (vs olanzapine 20mg)=30mg. Start=2mg/d. Maint=4-6mg/d. Max=10mg/d. Divided BID.


thiothixene=Navane: AVL: PO. PK: t1/2=34h. DOS: Equivalence (vs olanzapine 20mg)=30mg. Start=5mg/d. Maint=15-30mg/d. Max=40mg/d. Divided HS-BID.


trifluoperizine=Stelazine: AVL: PO (tab,liquid). PK: t1/2=7-18h DOS: Equivalence (vs olanzapine 20mg)=30mg. Start=5mg/d. Maint=10-20mg/d. Max=40mg/d. Divided HS-BID.


zuclopenthixol=Clopixol: AVL: PO. ADM: T HS. PK: t1/2=20h. DOS: Equivalence (vs olanzapine 20mg)=30mg. Start=20mg/d. Maint=20-60mg/d. Max=80mg/d. Not divided.


★★ Second-Generation Antipsychotis (SGAs) aka Atypical or Novel ★★

AE: Can affect BG levels. OTH: Have greater 5-HT affinity relative to D2.


aripiprazole=Abilify: AVL: PO (SL), IM (long acting). IND: Bipolar. MOA: Has slightly different binding affinities vs other SGAs. Partial agonist at D2 and 5-HT1A and potent antagonist at 5-HT2A. EVD: Potentially effective for negative and depressive symptoms. ADM: T w/ or without food in am (stimulating). Don’t eat/drink for 10min after taking SL. PK: t1/2 (of active metabolite)=75-94h. DOS: Equivalence (vs olanzapine 20mg)=30mg. Start=10mg/d. Maint=15-30mg/d. Max=30mg/d. Not divided.


asenapine=Saphris: AVL: PO (SL). IND: Bipolar. MOA: Has slightly different binding affinities vs other SGAs. Potent antagonist for many 5-HT and DA receptors. ADM: SL: Don’t eat or drink for 10min. PK: t1/2 =24h. DOS: Start=10mg/d. Maint=10-20mg/d. Max=20mg/d. Divided BID.
clozapine=Clozaril: AVL: PO. MOA: Weak D2 antagonist. EVD: Only antipsychotic w/ efficacy for Tx resistant schizophrenia. Used after 2 failed antipsychotics due to risk of agranulocytosis and need for blood monitoring. AE: agranulocytosis1.3% PK: t1/2=14h. MON: Clozapine level: clozapine+desmethylclozapine=total clozapine. Lower limit=1050nM. Upper limit=N/A. DOS: Equivalence (vs olanzapine 20mg)=4000mg. Start=25mg/d. Maint=200-500mg/d. Max=800mg/d. Divided HS-TID.


lurasidone=Latuda: AVL: PO. IND: Bipolar (depressive episode). ADM: T w/ meal >500Cal (to increase F). PK: t1/2=18h. DOS: Start=40mg/d. Maint=40-80mg/d. Max=160mg/d. Once/d (not divided). OTH: Minimal effect on weight, glucose, cholesterol, TG.


olanzapine=Zypexa: AVL: PO, IM. IND: Bipolar. PK: t1/2=21-54h. DOS: Start=5mg/d. Maint=10-20mg/d. Max=30mg/d. T HS.


paliperidone=Invega: AVL: PO, IM. IND: Bipolar. ADM: T w/ or without food HS. PK: PO: t1/2=23h. IM: t1/2=25-49d. DOS: PO: equivalence (vs olanzapine 20mg)=9mg. Start=3mg/d. Maint=6-9mg/d. Max=12mg/d. Not divided. IM: Start=150mg (then 100mg on day 8). Maint=25-150mg. Max=150mg. OTH: Paliperidone is an active metabolite of risperidone.


quetiapine=Seroquel: AVL: PO (IR and ER). IND: GAD, bipolar. PK: t1/2 (of active met)=6-12h. DOS: Equivalence (vs olanzapine 20mg)=750mg. Bipolar: Std=300mg/d. Max=600 mg/d. GAD: Start=50mg/d. Maint=150mg/d. Max=400mg/d. Other: Start=100mg/d. Maint=400-800mg/d. Max=1000mg/d. Divided HS-BID.


risperidone=Risperdal: AVL: PO, IM (Risperidal Consta). IND: ADHD. PK: PO: t1/2 (of active met)=20-24h. IM: t1/2=3-6d. DOS: PO: Equivalence (vs olanzapine 20mg)=6mg. Schizophrenia: Start=1mg/d. Maint=4-6mg/d. Max=8mg/d. Divided HS or BID. ADHD: Initial=0.25–0.5 mg HS. Increase weekly by 0.5 mg/day prn. Std=0.75–1.5 mg/d. IM: Equivalence (vs olanzapine 20mg)=3.6mg. Start=25mg. Maint=25-50mg. Max=50mg. Given q2w.


ziprasidone=Zeldox: AVL: Avail PO. IND: Bipolar. MOA: Unlinke other SGAs, has antagonist activity at 5-HT1D. EVD: First SGA to not be associated w/ significant wt gain. ADM: T w/ meal >500Cal (doubles F). PK: t1/2=6-10h. DOS: Equivalence (vs olanzapine 20mg)=160mg. Start=40mg/d. Maint=120-160mg/d. Max=200mg/d. T once/ in am or divide BID.

 

Azapirone

buspirone=BuSpar: AVL: PO (tab10mg). White splitable tab. Brand not availableNS. IND: GAD, anxiety w/ Hx of aggression or if benzos cause disinhibition. MOA: 5-HT1A receptor agonist on presynaptic neurons in the dorsal raphe and on postsynaptic neurons in the hippocampus. This slows the firing rate of the neurons in the dorsal raphe. Buspirone also binds and blocks at DA2 presynaptic receptors. It also causes increased firing in the locus ceruleus. Net result is 5HT activity is suppressed while NE and DA cell firing is enhanced. EVD: Similar efficacy vs benzos without risk of dependence. Less sedation vs benzos. Anxiolytic effect can be after days but max Tx effect after >3w. Pts 6–17yo w/ GAD taking 7.5–30mg BID x 6w found no more effective vs placebo. ADM: T w/ or without food consistently (not prn). AE: Dizziness12% , drowsiness10%, common AE (1-10%): Numbness, HA, tremor, fainting, seizures, tachycardia/chest pain, rash, sweating, N, dry mouth, upset stomach, D, C, V, muscle ache, tinnitus, sore throat, insomnia, nervousness, excitement, anger/hostility, confusion, depression, sleep disturbances. PRG: FDA cat B. LAC: Distributed into milk in rats. Avoid if possible. DI: MAOIs, 3A4 inhibitors. PK: t1/2=2-4h. Tmax=40-90min. F=4%. PB=86–95% Metabolized by 3A4. Excreted mainly as metabolites in the urine (mostly) adn feces. COS: Expensive vs other antidepressants. DOS: Adj for hepatic and renal fxn. Start=5 mg BID or TID. Increase by 5mg/d q2–4d prn. Max=60mg/d divided Bid or TID. OTH: Not well studied <18yo. Has been used in pts 6–17yo w/ GAD without unusual AEs.

 

Barbiturates

phenobarbital=Phenobarb: AVL: PO. IND: Epilepsy. AE: Sedation, rash5%, depression, decreased libido. PK: Potent CYP inducer. DOS: Epilepsy: 90-120mg once/d at HS.


primidone: AVL: PO. IND: Epilepsy. AE: Sedation, rash5%, depression, decreased libido. PK: Gets metabolized to phenobarbital. Potent cyp inducer. DOS: Epilepsy: Initial=125mg HS × 3d then 125mg BID × 3d then 125mg TID × 3d. Std=500–1000mg/d in 3–4 divided doses.

 

Benzodiazepines aka Benzos

MOA: Binds to GABAA receptors.


alprazolam=Xanax: DI: fluvoxamine, grapefruit juice, ketoconazole, nefazodone, theophylline.


bromazepam:


clobazam=Frisium: AVL: PO. IND: Epilepsy. AE: Irritability, depression. DOS: Epilepsy: Initial=5–15mg/d at HS. Std=20–40mg/d once/d or divided BID.
clonazepam=Rivotril=KlonopinUSA: AVL: PO. IND: GAD, panic, agoraphobia. AE: Sedation/fatigue, hallucinations, lightheadedness, Fatigue often lessens w/ time as body gets used to medication. CI: Myasthenia Gravis, closed angle glaucoma. PK: t1/2=20-80hrs. time to peak=1-2hrs. DOS: ANXIETY=0.25–0.5mg BID. SEIZURE:0.5mg TID. Max=20mg/d.


diazepam:


flurazepam:


lorazepam=Ativan: AVL: PO (tab0.5, 1, 2mg),SL, IV. IND: Anxiety (airplane, panic attack), akathesia, agitation, social phobias. AE: sedation, decreased cognition, memory impairment, repiratory depression, confusion, muscle weakness, HA, anticholinergic, sexual dysfunction, gynecomatia, D/C syndrome. CI: Sleep apnea. PK: Short acting vs other benzos. DOS: Anxiety: 1-10mg/d divided BID or TID. Insomnia: 1-4mg HS.


midazolam:


nitrazepam=Mogadon: AVL: PO. IND: Epilepsy.


oxazepam:


temazepam:


triazolam:


 

Catechol-O-Methyl Transferase (COMT) Inhibitors

IND: Parkinson's pts w/ wearing off. MOA: Inhibits the COMT enzyme which breaks down levodopa in periphery. Only beneficial if given w/ levodopa. DOS: Reduce levodopa dose 10-30% when starting COMT inhibitor (risk of dyskinesia).


entacapone=Comtan: AVL: Avail PO (tab200mg). ADM: T w/ each Levodopa dose. AE: Orange urine and skin discoloration, N, V, D. AUX: Don't crush. DOS: 100 or 200mg w/ each dose of levodopa. Max=1.6g/d.


tolcapone=Tasmar: AVL: PO (tab200m) SAP only. Pts must already been taking (hepatotoxic).

 

Cholinesterase Inhibitors

IND: Mild-moderate dementia. EVD: All 3 appear to be equally effective. AE: N, D, HA, V, syncope, insomnia/nightmares, agitation, leg cramps, urinary incontinence.


donepezil=Aricept: IND: May be used in mod-severe dementia. Black Box Warning: Neuroleptic malignant syndrome and rhabdomyolosis. DOS: Initial=5mg/d x 4-6w. Target=10mg/d.


galantamine=Reminyl: Black Box Warning: SJS. DOS: Initial=8mg/d x 1-2w. Target=16mg/d. Max=32mg/d.
rivastigmine=Exelon: AVL: PO, Patch. IND: Lewy Body Dementia. DOS: PO: Initial=1.5mg BID x 2w & increase 1.5mg per dose x 2w. Target=3mg BID. Max=6mg BID. Patch: Placed and removed q24h. If naïve: Patch 5 x 4w. Target=Patch 10. Conversion from oral to patch: If oral dose <6mg/d use patch 5. If oral dose=6-12mg/d use patch 10. Apply 1st patch the day after the last oral dose.

 

CNS Stimulant (Miscellaneous)

modafinil=AlertecCAN=ProvigilUS: AVL: Avail PO (tab100mg). IND: Insomnia, ADHD (not approved). DOS: Initial=100mg/d. Std=200-400mg/d. Max=400mg/d. OTH: Not classified as controlled substance like other stimulantsCAN (reg schedule I)


 

DOPA Decarboxylase Inhibitors

IND: Parkinson's. ADM: Given w/ levodopa to increase distribution to brain and decrease N, V. OTH: Doesn’t cross BBB.


carbidopa:


benserazide:


pergolide: AVL: Only through SAP. Withdrawn due to cardiac valvulopathy.

 

Dopamine Agonists

IND: Single thereapy in early Parkinson's and w/ levodopa for later stages. Often preferred for younger patients (<50-70yo) MOA: Activates DA receptor. Doesn’t slow disease progression. EVD: Less motor complications than L-dopa but more hallucinations. AE: Reward seeking behavior, N, dizziness, sleep attacks, confusion, hallucinations, C, Edema, orthostatic hypotension. Can give w/ domperidone to decrease N. DI: SSRIs and MOIs increase risk of serotonin syndrome but less than levodopa. DOS: Increase dose q4-6w.


bromocriptine: DOS: Parkinson's: Initial=1.25mg BID. Std=5–10mg TID. OTH: Ergot/fungal derivative.
pergolide: AVL: Withdrawn in Canada2007 due to association w/ cardiac valvulopathy.
pramipexole=Mirapex: AVL: PO. IND: Parkinson's RLS. DOS: Adj for renal fxn. Initial=0.125mg TID. Usual=0.5–1.5mg TID. Max=1.5mg TID.


ropinirole=ReQuip: IND: Parkinson's RLS. PK: Metabolized by CYPs.


rotigotine=Neupro: AVL: Patch. ADM: Can be applied to belly, thigh, hip, flank, shoulder, upper arm. Avoid same site twice within 2w. CI: skin disease. DOS: Initial=2mg/24h. Maint=6-8mg/24h. Max=16mg/24h. Can increase dose weekly.


 

Dopamine Precursor

levodopa=L-DOPA: IND: Parkinson’s. MOA: Gets converted to DA in the CNS by dopa decarboxylase. EVD: Delaying use can preserve its effectiveness (especially in young pts). Improves: tremor, rigidity, bradykinesia. ADM: Needs to be given w/ DOPA decarboxylase inhibitors to enhance distribution to brain and decrease N, V. Don’t T w/ protein (decreased F).
AE: N, V, anorexia, hallucination, night mares, increased libido, dyskinesia50% at 5y, decreased BP, psychosis. DI: MAOI (hypertensive crisis), serotonergic drugs (serotonin syndrome), Fe (decreased F). Amino acids from protein compete for F in gut and through BBB (F decreases 30% w/ meal). PK: IR: Onset=30min. Duration=4h. CR: Onset=1-3h. Duration=5h. DOS: Start=100mg/d. Maint=300-2000mg/d. Can be divided 6x/d. Increase dose 20-30% if going from IR to CR (Less F w/ CR). Avoid abrupt withdrawal. Increase frequency if wearing off effect. OTH: Levodopa crosses BBB.

 

Lithium Salts

lithium carbonate=Carbolith=Litane=Duralith(ER)=Lithmax(CR): AVL: PO (cap150, 300, 600mg, ER tab300mg). MOA: Increases the release of 5HT and possibly increases the reuptake of NE. EVD: Starts to work in 1-2w. Reduces risk of suicide in people with bipolar disorder. AE: Memory loss, problems creating new memories, blunting emotions (ex. not feeling happy at party or not feeling sad at funeral), tremor, N, V, D, polyuria/polydipsia, increased K, kidney & thyroid toxicity, acne, psoriasis, wt gain. Possible QT prologation. DI: Increased [Li] with NSAIDs, Ca channel blockers, ACEi, ARBs, low Na. PK: t1/2=20-26h. PB=0. Cleared renally. MON: Serum levels=0.8-1.1mM (geriatric=0.4-0.6mM). Measure 9-13h after first dose. DOS: Initial=300mg BID. Then adj based on levels. IR divided once/d-TID. ER divided once/d or BID. OTH: Maintain consistent salt diet.


lithium citrate: AVL: PO (liq60mg/mL). IND: Bipolar. PK: t1/2=20-26h. PB=0. Cleared renally. DOS: Initial=5mL BID. Then adj based on levels. Divided once/d-TID.

 

Monoamine Oxidase Inhibitors (MAOIs)

MOA: Irreversibly inhibits MAO which is an enzyme that metabolizes 5HT, noradrenaline, DA. AE: Common: Dizziness/lightheadedness, weight gain/fluid retention, sexual dysfunction, insomnia. DI: Serotonergic drugs like SSRIs (serious risk of serotonin syndrome). DA agents like levodopa can cause hypertensive crisis. Foods w/ tyramine can cause hypertensive crisis ex: Aged cheese, cured meats, tap beer, marmite, fava beans, soy products, beer/wine in moderation. OTH: Switching antidepressants res: Psychiatry.net and SwitchRx (free but need to register).


phenelzine=Nardil: IND: Panic, agoraphobia. DOS: Anxiety=45–90mg/d.


tranylcypromine=Pamate:

 

Monoamine Oxidase-B (MAO-B) Inhibitors

IND: Parkinson's. Often used early in Parkinson's to decrease need/dose of L-dopa. MOA: Irreversibly inhibits monoamine oxidase B (enzyme that metabolizes DA in the brain). DI: SSRIs, SNRIs, TCAs, MAOIs (serotonin effect), meperidine, DM, alpha-agonists. PK: Can be metabolized to amphetamine metabolite.


rasagiline=Azilect: AVL: PO (tab0.5, 1mg). EVD: 5-10x more potent vs selegiline. AE: HA, arthralgia’s, dyspepsia, depression, orthostatic hypotension. DOS: Adj for hepatic fxn. PD: Monotherapy: 1mg/d. Multitherapy=0.5-1mg once/d. OTH: 2nd Generation MAO-B.


selegiline=Emsam: aka L-deprenyl. AVL: PO (tab5mg). AE: Insomnia, agitation, N, dizziness, orthostatic hypotension, rash. PK: Has amphetamine metabolite causing stimulant like AEs. DOS: 2.5-5mg once/d. OTH: 1st generation MAO-B.

 

N-Methyl-D-Aspartate (NMDA) Antagonist

amantadine=Symmetrel: AVL: PO (tab100mg or syrup10mg/mL). IND: Parkinson's (early for tremor and late for dyskinesia). AE: Confusion, nightmares, insomnia, anticholinergic effects. DOS: Adj for renal fxn. PD: Initial=100mg/d. Maint=100mg BID or TID. Max=200mg BID. Give 2w trial to evaluate efficacy.


memantine=Ebixa: AVL: PO. IND: Mod-severe Alzheimer’s. EVD: May help with agitation/aggression. AE: Dizzy, drowsy, confusion. Caution if: Hx of seizures or heart disease. DOS: Dementia: Initial=5mg/d. Increase by 5mg/d at weekly intervals. Target=10mg BID at week 4. OTH: Can be used w/ cholinesterase inhibitors.

 

Noradrenaline-Dopamine Reuptake Inhibitor (NDRI)

OTH: Switching antidepressants resource: Psychiatry.net and SwitchRx (free but need to register).

bupropion=Wellbutrin=Zyban: AVL: PO (XR tab150,300mg). IND: ADHD, depression, seasonal affective disorder, smoking cessation. Zyban only used for smoking cessation. MOA: Inhibits the reuptake of NE and DA. No effect on 5HT. EVD: Not very effective for anxiety. No sexual AEs. Can delay weight gain. May be more effective with an NRT patch. Smoking cessation efficacy=19%. ADM: T w/ or without food. Typically in the am (stimulating). D/C syndrome less frequent w/ bupropion vs other antidepressants but still need to taper. AE: HA30% rapid HR11% N, V insomnia25%, agitation17% dizziness15% , sweating22%, weight loss22% C15% irritability, restlessness, dry mouth, dry skin, rash, blurred vision, tremor, seizures0.5-1%. CI: Seizure disorder, heavy drinking, bulimia/anorexia, past stroke or head trauma. DI: EtOH decreases seizure threshold. PK: t12/=21h. Metabolized by and inhibits 2B6. XL tabs given q24h while XR q8h. AUX: Don't crush/chew. DOS: Smoking Cessation: Start 1-2w before quit date. 150mg OD x 3d then BID x 7-12w. ADHD: Initial=2–3mg/kg/d. Std=200–300 mg/d divided in 2 doses. Single dose max=150mg. Decrease dose for kidney or liver impairment.

 

Reversible Inhibitor of Monoamine Oxidase A (RIMA)

OTH: Switching antidepressants resource: Psychiatry.net and SwitchRx (free but need to register).
moclobemide=Manerix: AVL: PO (tab100, 150, 300mg). IND: Social anxiety. MOA: Selectively and reversibly inhibits MAO-A which is an enzyme that metabolizes 5HT and noradrenergic neurotransmitters. AE: N, insomnia. DI: meperidine, SSRIs, TCA. PK: t1/2=1-3h. DOS: Anxiety=300-600mg/d. Other: Initial=150mg BID. Maint=300-600mg TID. Max >600mg TID.

 

Selective Presynaptic Norepinephrine Reuptake Inhibitor

atomoxetine=Strattera: AVL: PO (cap10, 18, 25, 40, 60, 80,100mg). MOA: Potent inhibitor of NE without affecting DA, 5HT.
EVD: Takes 3-4w to see effect. 6–12w of Tx reduced ADHD symptoms by at least 25–30% in 60–70% of pts. ADM: T w/ food to minimize GI upset. AE: Abdominal pain18%, decreased appetite16%, V11%, tierdness10%, N9%, sexual dysfunction6%, indigestion5%, dizziness5%, rash3%, insomnia, liver toxicityrare, MI/strokerare, anaphalaxisrare, suicidal ideationrare. DI: MAOI, SSRIs, DM (serotonin syndrome), 2D6 inhibitors (paroxetine, fluoxetine, quinidine). PK: t1/2: Extensive metabolizers=5.2h. Poor metabolizers=21.6h. F=63-94%. PB=98%. Met by 2D6 (main). Doesn’t inhibit CYPs. DOS: Adj for hepatic fxn. Can T once/d in am or divide BID (am & afternoon) ADHD: Children <70kg: 0.5mg/kg/d x 7-14d. Then: 0.8mg/kg/d x7-14d. Then 1-1.2mg/kg/d ongoing. >70kg: 40 mg/d x 7-14d. Then 60mg/d x 7-14d. Then 80 mg/d if necessary. Max=100mg/d. Safety <6yo not established. OTH: Not classified as a stimulant.

 

Selective Serotonin Reuptake Inhibitors (SSRIs)

AE: Agitation (on initiation), N, anorgasmia, insomnia, D, GI bleed, dose-dependent QT prolongation. Discontinuation syndrome: anxiety, N, insomnia, chills, confusion. DI: Serotonin syndrome w/ MAOIs. DOS: Taper should be over 1-4w. OTH: Switching antidepressants resource: Psychiatry.net and SwitchRx (free but need to register).


citalopram=Celexa: AVL: PO. IND: Panic, agoraphobia, social anxiety. EVD: SSRI w/ fewest DIs. AE: Prolonged QT (8.5msec at 20mg/d. 18.5msec at 60mg/d). DOS: Anxiety: Std=20–40mg/d. Max=60mg/d.


escitalopram=Cipralex: AVL: PO. IND: agoraphobia, panic, GAD. AE: QT prologation. DOS: Anxiety=10-20mg/d.


fluoxetine=Prozac: IND: Panic, agoraphobia, social anxiety. EVD: Typically no D/C syndrome because of long t1/2. Most anorexic and most stimulating SSRI. PK: t1/2=10-14d. DOS: Anxiety=20-80mg/d.


fluvoxamine=Luvox: AVL: PO. IND: agoraphobia, panic, social anxiety. EVD: SSRI w/ most C, N, and sedation. ADM: T HS (sedating). DOS: Anxiety= 150–300mg/d.


paroxetine=Paxil: AVL: PO (IR and CR). IND: Agoraphobia, panic, social anxiety.
AE: SSRI w/ most anticholinergic AEs. PK: t1/2=3-65h. DOS: Anxiety: IR=20-60mg/d. CR=12.5–37.5mg/d.


sertraline=Zoloft: AVL: PO. IND: Agoraphobia, panic, social anxiety. AE: SSRI w/ most male sexual dysfunction and D.

 

Serotonin Antagonist/Reuptake Inhibitor (SARI)

OTH: Switching antidepressants resource: Psychiatry.net and SwitchRx (free but need to register).
trazodone=Desyrel: AVL: PO. IND:Insomnia, dementia. AE: Hypotension, priapism0.02%, QT prolongation. DI: Serotonergic drugs (serotonin syndrome).

 

Stimulants

EVD: 70% of pts will have clinically significant decrease in ADHD symptoms. If no effect after 4w, switch to a different stimulant. Kids treated with stimulants have a lower risk of substance-use disorders (drug and alcohol) later in life than untreated ADHD kids. AE: Decreased appetite, wt loss, insomnia HA, N, V, D, rebound hyperactivity, anger/irritability, depression, anxiety, psychosis, suicidal thoughts, priapismrare. MTA study found after 3y, children where 2cm shorter and weighed 2.7kg less than children not medicated.
amphetamine (mixed salts)=Adderall XR: AVL: PO (Cap5, 10, 15, 20, 25, 30mg). ADM: T in AM to avoid insomnia. DOS: ADHD: Initial=5mg once/d. Std=10-30mg once/d in am. Max=30mg/d.


dextroamphetamine(DEX)=Dexedrine: AVL: PO (IR tab5mg and SR spansule10, 15mg). PK: t1/2=1-2h. F=75%. Hepatic metabolism by 2D6. DOS: ADHD: IR: 2.5-40mg/d or 0.15mg/kg/d divided in 1-3 doses. SR: 10–40mg or 0.15mg/kg once/d in am.


lisdexamfetamine=Vyvance: AVL: PO (cap20, 30, 40, 50, 60mg). ADM: T in am to avoid insomnia. PK: t1/2=13h (metabolite). DOS: ADHD: >6yo: Initial=30mg once/d in am. Increase to 50mg after 1w if necessary.


methylphenidate(MPH)=Biphentin=Concerta=Ritalin: EVD: ~90% of stimulants used. PK: t1/2=2-3h. Onset=20-30min. F=20-25%. Delivery: Ritalin=IR&SR. Concerta=Bi-layer Controlled Release Tabs. Biphentin=Controlled Relase. DOS: ADHD=5-60mg/d (0.3mg/kg/d).

 

Tricyclic Antidepressants (TCAs)

MOA: Inhibit reuptake of NE and 5HT. EVD: Secondary amines have less dry mouth, weight gain, and dizziness. AE: : Increased BP, weight gain, sexual dysfunction. DI: MAOI (serotonin syndrome), cimetidine (increased TCA). OTH: Psychiatry.net and SwitchRx (free but need to register).
2o(Secondary) Amine
Have greater effect on NE than 5HT. Less AE vs tertiary TCAs.
desipramine=Norpramin: AVL: PO. IND: ADHD, agoraphobia, GAD, panic. AE: Possible QT prolongation. DOS: Anxiety=75-300mg/d. ADHD: 6–12yo=10–20mg/d in 3 or 4 divided doses. Adolescents=30–50mg/d in 3–4 divided doses. Max=150mg/d.


nortriptyline=Aventyl: AVL: PO. IND: Depression (best TCA), smoking cessation. MOA: Noradrenergic (not sedating). ADM: AE: C, weight gain, trouble urinarting, drowsiness, dizziness, dry mouth, sun sensitivity, suicidal thoughts (especially <25yo). Possible QT PK: t1/2=37h. DOS: ADHD: 6–12yo=10–20 mg/d po in 3 or 4 divided doses. Adolescents=30–50mg/d in 3–4 divided doses. Max=150 mg/d. OTH:
3o Teriary Amines
Works on 5HT and NE. May have > effect on men than women. amitriptyline=Elavil: AVL: PO. IND: Sedation, neuropathic pain, depression, anxiety.


clomipramine=Anafranil: IND: Agoraphobia, OCD, panic, depression, and chronic pain. MOA: Similar to SSRI. DOS: Anxiety=75–225mg/d.


imipramine=Tofranil AVL: PO. IND: ADHD, agoraphobia, GAD, panic. AE: Possible QT prolongation. DOS: Anxiety: 75-300mg/d. ADHD: 6–12yo=10–20 mg/d po in 3 or 4 divided doses. Adolescents=30–50mg/d in 3–4 divided doses. Max=150 mg/d.

 

Z-Drugs (Nonbenzo Sedative/Hypnotic)

zolpidem=Sublinox=AmbienUSA: AVL: SL10mg tabs IND: Insomnia. PK: t1/2=2.5h. tpeak=1.5h DOS: 10mg HS


zopiclone=Imovane AVL: PO5,7.5mg tabs IND: Insomnia MOA: Binds to the GABAa receptor (same as benzos). AE: Metallic taste in the mouth, dry mouth, upset stomach, D, dizziness (increased risk of falls), confusion, amnesia. CI: liver failure, severe sleep apnea. DI: EtOH (both CNS depressants). PK: t1/2=4-7h. tpeak=1.5h DOS: Pts >65 should start w/ half of a 7.5mg tab. Should not exceed 7-10d of use but often used daily. OTH: There is a risk of dependence which is dose dependent.

 

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