ANTIPSYCHOTICS (AP): Comparison Chart B Jensen BSP © www.RxFiles.ca Nov 2018 Name: Generic/TRADE GROUP Clinical ADVERSE EVENTS -AE (%) ANTI- DOSE: INITIAL/d; USUAL DOSE $ (& receptor activity) g =generic Equivalency-mg Anticholinergic Sedation Hypotension EPS EMETIC MAX/d; Elderly Dosing RANGE /Month ChlorproMAZINE LARGACTIL, g Pregnancy 25-75mg; 1000mg po 100mg po BID 12 (25 ,50 ,100 mg tab)(liquid made by some pharmacies) 100 >30 >30 >30 >10 category Aliphatic 50mg/2ml amp: D/C 2016) D2, 1, 5-HT2A Intractable: may help P L 1200mg Retinal pigmentosa 200mg po BID 14 Cholestatic jaundice <1%, Weight gain ~3-5kg, Seizures <1%, Photosensitivity <3%. Hiccups ; schizo ≥6mos ++++ Methotrimeprazine NOZINAN, g Phenothiazine 70 >30 >30 >30 >10 Mild: 5-25mg; 25mg po BID 28 (2, 5, 25, 50mg tab) + P L 1000mg po 50mg po BID 37 ⌂ (5mg/ml soln, 25mg/ml amp) H1,5HT2A Periciazine(Pericyazine) NEULEPTIL 15 >30 >30 >10 >2 ++++ 5-20mg AM + 5mg po AM + 42 (5,10,20mg cap; 10mg/ml liquid) D2 Phenothiazine 10-40mg PM po 10mg po PM FluPHENAzine MODECATE,MODITEN, g 5 >2 >2 >2 >30 + 2.5-10mg; 20mg po 1-5mg po daily 17-23 (DEPOT with preservative 125mg/5ml Vial & 15mg IM P L 2.5-12.5mg; 100mg 12.5-50mg IM/SC 35 /5ml vial 100mg/1ml amp; 1, 2 , 5mg tab) D2, 5-HT2A, 5-HT7 q4week IM/SC q2-3w q2-4w ~20mg/dCATIE Perphenazine TRILAFON, g Piperazine 4-16mg; 64mg po 8mg po BID 17 8 >10 >10 >10 >10 ++++ (2,4,8,16mg tab); (5mg/ml amp ) D2, 5-HT2A, H1 P L Trifluoperazine STELAZINE, g 6 >2 >2 >10 >30 ++++ 4-10mg; 40mg po 5mg po TID 34 P L (1,2,5,10, 20 mg tab; 10mg/ml soln) D2, 5-HT2A 10mg BID 29 Flupentixol FLUANXOL 10 >10 >2 >2 >30 ++ 3mg; 12mg po 3mg po BID 47 (DEPOT 20mg/1ml amp, 100mg/1ml amp; P L 0.5,3mg tab) D2, 5-HT2A 24mg IM q4week 5-20mg;100mg IM q2-3w 20-40mg IM q2-3w 27-42 Zuclopenthixol CLOPIXOL Thioxanthene 50 >10 >30 >2 >30 ++ 10-50mg; 100mg po 10mg po BID 36 (10,25mg tabs), D1-2, 5HT2A, 1 120mg IM q4week (LESS with 100-200mg IM q2w; 150-300mg IM 28-44 P L Acuphase (50mg/1 ml amp)DEPOT200mg/1 ml amp) DEPOT) 400mg q2-3w Not Interchangable Dibenzodiazepine P L CloZAPine CLOZARIL, g 50 6.25-25mg (25-50mg/d) 100mg po TID 268 {patients must register with specific monitoring program!} >30 >30 >30 >2 + Tx: Atropine eye drop/Atrovent nasal spray nocturnal 1% Max: 200mg po BID (25 , 50 , 100 , 200 mg tab) AE:Dizzy,constipation, N/V,HA, fever, nightmares,sweat,HR,BP,salivation , enuresis , seizure(5%-dose related),agranulocytosis CBC qweek(q24week if stable), weight ,ECG 's, 347 D1-5,5HT1&2,7 1-2,H1,M1-5 37% >10% hypomotility 1A2,3A4,2D6,2C19 level level cardiomyopathy; ALT , diabetes, lipids, akathisia , GI . DI: clozapine : CBZ (& neutropenia) & smoking; Cipro, fluvoxamine, caffeine & eryc clozapine ; benzodiazepines -rare resp. arrest. prolactin effect. Level: 1050 - 1650 nmol / L 900mg FDA: suicide risk in schizophrenics Haloperidol HALDOL, g 2 - 6 1.5-3mg; 100mg po 2mg po BID 28 >2 >2 >2 >30 +++ (0.5 ,1 ,2 ,5 ,10 mg tab; 2mg/ml soln ; 40mg IM q4week or Butyrophenone (LESS with with preservative 10-15x po daily dose. P L 50mg; 450mg IM q4w 5mg po BID 42 DEPOT 250mg/5ml, 500mg/5ml Vial, DEPOT) 100mg/1ml Amp ; 5mg/ml amp) D2>D1 QT interval esp. with IV dosing, May mortality, ALT 16%, Weight gain 1 kg; schizo/Tourette’s >3yrs approved 0.25-2mg/d 50-200mg IMq2-4w 57-87 Loxapine LOXAPAC IM, XYLAC Dibenzoxapine 10-20mg; 250mg po 10mg po BID 31 (5,10,25,50 mg tab); (2.5mg tab) 15 >10 >30 >10 10-30 + D/C Weight gain minimal P L (25mg/ml soln ; 50mg/ml amp ) D2, 5HT2A -inhaled powder ADASUVE 25mg po BID 42 USA OLANZapine ZYPREXA, g Reg + Zydis, g Thienobenzodiazepine 5-10mg; 20mg po 10mg daily 33 2.5 - 5 >10 >30 >2 >2 + $ CATIE (2.5,5,7.5,10,15mg tab) (ZYDIS 5,10,15mg tab )(20mg ) P L AE:somnolence, dry mouth, dizzy, headache, asthenia, constipation, nightmares, blurred vision, urinary incontinence, dyspepsia, ALT 6%, diabetes, weight , BP, 2.5-5mg/d 15-20mg po daily 54-75 ; , , , , & ( ) >10% postural 0.9% DRESS 1A2,2D6,P-gp smoking by fluvoxamine FDA FDA 10mg IM D1-4 5HT2A,C 1 H1 M1-3 5 approved 1996 akathisia , hypotension , Sz’s , ?stroke/death, triglycerides/cholesterol; skin . DI: olanzapine by: ; ; prolactin BPAD 1: acute tx of manic & mixed episodes13yr ; Schizophrenia Age 13yr AE: esp weight,TG,diabetes Pimozide ORAP, g Diphenylbutyl 2-4mg; 20mg po 6mg po daily 45 2 >2 >10 >2 >30 + 2D6 P L (2,4mg tab) D2, 5-HT7 piperidine QTc with >8mg/d or DI: azole antifungals, diltiazem, fluvoxamine, macrolides, sertraline, paroxetine, PI’sHIV& verapamil. FDA: for kids >12yr QUEtiapine SEROQUEL, g DI: 3A4 Dibenzothiazepine + 50mg; 800mg po 200mg po TID 35 (25, 50, 100, 200, 300mg tab),(150mg ); 60 - 75 10-30 >10-30 >10 >2 P L ~540mg/d CATIE 600mg hs 35 12.5-200mg/d (XR g: 50,150,200,300,400mg) AE : somnolence , dizzy, drowsy, nightmares, constipation, dry mouth, lens changes beagles-annual slit lamp exam, BP, wt, seizures 0.8%, dyspepsia, headache, abuse, urinary, DRESS, BPAD: acute tx of manic, depressive & mixed 10yr FDA 300mg po BID 35 D1-2, 5HT1A&2A,1,H1 (avail. 1997) failure n=3 17% 11% 0.4% effect incontinence, diabetes,ALT 9% ,akathisia >2%,?stroke/death,triglyceride ,cholesterol ,hypothyroidism ,?pancreatitis/platelet, low EPS , prolactin effect Schizo: 13yr FDA ; 600-800mg XR od $75 g - $98 g ODT=$44 RisperiDONE RISPERDAL, g Benzisoxazole + P L 1-2mg; 8mg po 1mg po BID 25 2 >2 >2-10 >10-30 >10 CATIE ODT=$77 0.25-2mg/d 2mg po BID 41 (0.25,0.5 ,1,2 ,3 ,4 mg tab;DEPOT 12.5,25,37.5,50mg vial ; CONSTA M-TAB , g melts 0.5,1,2,3,4 mg tab; 1mg/ml soln) 25mg; 50mg IM q2w 25-50mg IM q2w 368-708 FDA D1-4, 5HT1A&2A,1,2,H1 -little M1(approved 1993) AE: sedation, headache, dry mouth, constipation, blurred vision, urinary incontinence, insomnia, agitation, asthenia, BP, akathisia >10%, appetite, TTP, IFIS, BPSD; BPAD: acute manic & mixed tx 10yr ; FDA FDA FDA Jul’18 3A4,2D6,P-gp Autism:irritability Age 5-16yr ; Schizophrenia Age 13yr (Perseris: 90-120mg SC monthly) seizures 0.3%, photosensitive, ?stroke/death, weight . Oral liquid not mix with cola/tea. DI: ?furosemide. EPS dose >2-4mg/day & prolactin/TG. ARIPiprazole ABILIFY, g Phenylpiperazine 10-15mg; 30mg po 10-15mg po AM 45-52 7.5 <2 >10 >2 >2 + P L (2,5,10,15,20,30mg tab) DEPOT 300, 400mg IM vial 400mg IM q4w ≤400mg IM q4w MAINTENA behavior FDA minimal 3A4/2D6 483 AE: suicidal ;wt , sexual AE,anxiety, tremor;gamble; compulsive behavior, stimulate, akathisia, EPS, SJS,QT, BP; DI: : CBZ, eryc, fluox & parox-etine. VAST-D autistic /Tourette 6-17yr D2-D4, 5HT1A,2A/C, 5HT7 Schizo ≥15yr; BPAD ≥13yr;MDD ; & for adult BPAD I of these may need ↓dose than ♂ disorders withdrawal General: Onset 7day; good trial is ≤4-6wk. 25% of pts respond poorly to Tx, yet 30% respond to clozapine. ♀ Positive S&Sx: hallucinations, delusions, thought ; Negative S&Sx: social , isolation & apathy. = dose-renal dysfx =scored Neuroleptic Malignant Syndrome-upto 1%, often within 30day;esp. younger males,high potency depot; mortality of 10%,S/SX: >39oC, muscle rigidity, delirium, autonomic instability (i.e. BP),CPK,HR, arrhythmias, tremors, seizures & coma.Tx: D/C neuroleptic, cooling blanket, hydrate, dantrolene, bromocriptine & benzodiazepines. Tardive dyskinesia-after months to yrs of neuroleptics, in elderly.S&Sx: fly catching/protruding motions of tongue, tics of the face, chewing motions or excessive blinking.Tx: D/C/change/ neuroleptic,anticholinergics, tetrabenazine, donepezil, Vit E 400-1600iu/d. Depot Meds-after 3-6 months many accumulate; thereby, requiring dose, onset of action for most are 2-3 days (Peak 4-7day), except Clopixol ACUPHASE with onset: 2-4hr,duration: 2-3days and max. sedation at 8hr. (see pg 155) Pregnancy: Consider risk vs benefit! Use lowest possible dose, if possible try to D/C before delivery; neonate EPS risk & withdrawl sx. Avoid if possible esp. during 1st trimester. Phenothiazines are not thought to be teratogenic most data with chlorpromazine. Atypicals: not routinely recommended (assoc. with ‘large for gestational age’ babies), but benefits may outweigh risk. No known congential malformations? risperidone. Recommend folic acid ≤5mg/day & monitor blood sugars developmental toxicity. Level by: antacid, cholestyramine, carbamazepine, phenobarbital, phenytoin, rifampin & smoking. Level by: amitripyline, amiodarone, cimetidine, ciprofloxacin, diltiazem, erythromycin, fluoxetine, fluvoxamine, grapefruit juice, isoniazid, ketoconazole, nefazodone, paroxetine, propranolol, quinidine, ranolazine & ritonavir. EPS Acute dystonia-spasm of face,neck&back-like seizure(Onset 1-5day esp. young male,Tx:benztropine) Akathisia-motor restless-not verbal,pacing,fidgety(Onset 5-60day,esp. old female;Tx:dose/ low potency,lorazepam,propranolol,diphenhydramine) Parkinsonism-rigid,bradykinesia,shuffling gait,tremor (Onset 5-30day esp. old female;Tx:benztropine, amantadine) Rabbit Syndrome-rapid chewing movements (Onset after months esp. old females; Tx: benztropine). =EDS = Non-formulary Sask $105 BPAD (FDA BPAD1 age 10-17yr) interval 1A2 Asenapine SAPHRIS: 5,10mg SL tab BID Wait 10min after SL tab, before eat/drink. D2 & 5HT2A. MayQT ,EPS, akathisia, somnolence, allergic rx, minimal wt; mouth numbness,poor taste.